In Vitro Antioxidant-Activity Evaluation of Gallic-Acid-Grafted Chitosan Conjugate Synthesized by Free-Radical-Induced Grafting Method.

PubMed

Hu, Qiaobin; Wang, Taoran; Zhou, Mingyong; Xue, Jingyi; Luo, Yangchao

2016-07-27

The major objective of this work was to develop a green and facile process to prepare gallic acid-chitosan conjugate and comprehensively evaluate the physicochemical properties and biological activities of an as-prepared water-soluble chitosan derivative. A free-radical-induced grafting approach using an ascorbic acid-hydrogen peroxide redox pair was adopted. The obtained conjugate was characterized by Fourier transform infrared spectroscopy, UV-vis, X-ray diffraction, and pKa analysis. The antioxidant activities were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6)-sulphonic acid (ABTS), reducing power, and oxygen-radical antioxidant-capacity assays. The results showed that the mass ratio of gallic acid to chitosan played a vital role in determining the grafting degree and ζ potential of the conjugates, with the ratio of 0.5:1 being the optimal ratio that resulted in the highest grafting degree. The antioxidant assays demonstrated that conjugation significantly improved the antioxidant activities, being dramatically higher than that of free chitosan. It was notable that the DPPH- and ABTS-scavenging activities of conjugate at 0.4 mg/mL reached the same level as the free gallic acid at the equivalent concentration. Our study demonstrated a green and facile synthesis approach to preparing a novel water-soluble chitosan derivative that may have promising potentials in the food industry.

Identification of the flavonoids in mungbean (Phaseolus radiatus L.) soup and their antioxidant activities.

PubMed

Li, He; Cao, Dongdong; Yi, Jianyong; Cao, Jiankang; Jiang, Weibo

2012-12-15

Mung bean soup (MBS) has been traditionally taken as a kind of health food in China. To learn the mechanisms underlying its health benefits, antioxidant capacities of the soup prepared with three cultivars of mung bean were measured. The highest DPPH radical scavenging or ferric reducing activity was observed in soup of mung bean cv. Huang. The MBS of cv. Huang and Mao exhibited higher ABTS(+) reducing activities than MBS of cv. Ming. The two major flavonoids in the MBS were purified and identified as vitexin and isovitexin, respectively. Modeling samples containing vitexin and isovitexin at the same levels as them in the MBS were prepared to assess their antioxidant contributions in the MBS. Our results showed that antioxidant capacities of the MBS mainly derived from vitexin and isovitexin, these flavonoids accounted for the most of total DPPH radicals scavenging, ferric reducing and ABTS(+) reducing scavenging activities in MBS of all the three cultivars. Copyright © 2012 Elsevier Ltd. All rights reserved.

Antioxidant and radical-scavenging activities of Slovak honeys - An electron paramagnetic resonance study.

PubMed

Zalibera, Michal; Staško, Andrej; Šlebodová, Anna; Jančovičová, Viera; Čermáková, Tatiana; Brezová, Vlasta

2008-09-15

The antioxidant properties of 15 honey samples from different floral sources and various Slovak regions were investigated by means of electron paramagnetic resonance spectroscopy. Cation radical of ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) diammonium salt), DPPH (1,1-diphenyl-2-picrylhydrazyl) and hydroxyl radicals generated by the photochemical decomposition of hydrogen peroxide were used as oxidants. The antioxidant activities found with ABTS(+), expressed as trolox equivalent antioxidant capacity (TEAC), ranged from 0.15 to 1.14mmolkg(-1), and those determined with DPPH, from 0.04 to 0.32mmolkg(-1). TEAC values correlated well with results found by elimination of DPPH, and both values revealed a linear relationship with the concentration of phenolics obtained with the Folin-Ciocalteu phenol test (expressed as gallic acid equivalents, GAE). The colour coordinates (CIE L(∗)a(∗)b(∗)), as well as reflectance spectra determined for original honeys using a white background, demonstrated that the colour difference (ΔE(∗)) and coordinate b(∗) interrelate with TEAC values. The radical-scavenging capacities (RSC) of the honey samples determined in the experiments with photochemically decomposed hydrogen peroxide, generating reactive OH radicals in the presence of spin trapping agent, differ from those found with ABTS(+) and DPPH. Here, probably, the reactive OH radicals, having higher redox potential, are scavenged by a variety of compounds not effective with ABTS(+) and DPPH (e.g., saccharides, proteins). Copyright © 2008 Elsevier Ltd. All rights reserved.

Effect of ultrafine grinding on physicochemical and antioxidant properties of dietary fiber from wine grape pomace.

PubMed

Zhu, Feng-Mei; Du, Bin; Li, Jun

2014-01-01

Wine grape pomace dietary fiber powders were prepared by superfine grinding, whose effects were investigated on the composition, functional and antioxidant properties of the wine grape pomace dietary fiber products. The results showed that superfine grinding could effectively pulverize the fiber particles to submicron scale. As particle size decrease, the functional properties (water-holding capacity, water-retention capacity, swelling capacity, oil-binding capacity, and nitrite ion absorption capacity) of wine grape pomace dietary fiber were significantly (p < 0.05) decreased and a redistribution of fiber components from insoluble to soluble fractions was observed. The antioxidant activities of wine grape pomace and dietary fiber before and after grinding were in terms of DPPH radical scavenging activity, ABTS diammonium salt radical scavenging activity, ferric reducing antioxidant power, and total phenolic content. Compared with dietary fiber before and after grinding, micronized insoluble dietary fiber showed increased ABTS radical scavenging activity, ferric reducing antioxidant power, and total phenolic content yet decreased DPPH radical scavenging activity. Positive correlations were detected between ABTS radical scavenging activity, ferric reducing antioxidant power, and total phenolic content.

9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.

PubMed

Makhaeva, Galina F; Lushchekina, Sofya V; Boltneva, Natalia P; Serebryakova, Olga G; Rudakova, Elena V; Ustyugov, Alexey A; Bachurin, Sergey O; Shchepochkin, Alexander V; Chupakhin, Oleg N; Charushin, Valery N; Richardson, Rudy J

2017-11-01

We investigated the inhibitory activity of 4 groups of novel acridine derivatives against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE) using the methods of enzyme kinetics and molecular docking. Antioxidant activity of the compounds was determined using the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS + ) radical decolorization assay as their ability to scavenge free radicals. Analysis of the esterase profiles and antiradical activities of the acridine derivatives showed that 9-aryl(heteroaryl)-N-methyl-9,10-dihydroacridines have a high radical-scavenging activity but low potency as AChE and BChE inhibitors, whereas 9-aryl(heteroaryl)-N-methyl-acridinium tetrafluoroborates effectively inhibit cholinesterases but do not exhibit antiradical activity. In contrast, a group of derivatives of 9-heterocyclic amino-N-methyl-9,10-dihydroacridine has been found that combine effective inhibition of AChE and BChE with rather high radical-scavenging activity. The results of molecular docking well explain the observed features in the efficacy, selectivity, and mechanism of cholinesterase inhibition by the acridine derivatives. Thus, in a series of acridine derivatives we have found compounds possessing dual properties of effective and selective cholinesterase inhibition together with free radical scavenging, which makes promising the use of the acridine scaffold to create multifunctional drugs for the therapy of neurodegenerative diseases. Copyright © 2017 Elsevier Ltd. All rights reserved.

Anti-inflammatory, cyclooxygenase (COX)-2, COX-1 inhibitory, and free radical scavenging effects of Rumex nepalensis.

PubMed

Gautam, Raju; Karkhile, Kailas V; Bhutani, Kamlesh K; Jachak, Sanjay M

2010-10-01

Evaluation of the topical anti-inflammatory activity of chloroform and ethyl acetate extracts of RUMEX NEPALENSIS roots in a TPA-induced acute inflammation mouse model demonstrated a significant reduction in ear edema. The extracts were further tested on purified enzymes for COX-1 and COX-2 inhibition to elucidate their mechanism of action, and a strong inhibition was observed. Six anthraquinones and two naphthalene derivatives were isolated from the ethyl acetate extract. Among the isolated compounds, emodin was found to be a potent inhibitor with slight selectivity towards COX-2, and nepodin exhibited selectivity towards COX-1. Emodin, endocrocin, and nepodin also exhibited significant topical anti-inflammatory activity in mice. Interestingly, nepodin showed better radical scavenging activity than trolox and ascorbic acid against DPPH and ABTS radicals. The strong radical scavenging activity of chloroform and ethyl acetate extracts could be explained by the presence of nepodin as well as by the high phenolic content of the ethyl acetate extract. Thus, the anti-inflammatory effect of R. NEPALENSIS roots was assumed to be mediated through COX inhibition by anthraquinones and naphthalene derivatives and through the radical scavenging activities of naphthalene derivatives. © Georg Thieme Verlag KG Stuttgart · New York.

Spectroscopic studies on the antioxidant activity of p-coumaric acid.

PubMed

Kiliç, Ismail; Yeşiloğlu, Yeşim

2013-11-01

p-coumaric acid (4-hydroxycinnamic acid), a phenolic acid, is a hydroxyl derivative of cinnamic acid. It decreases low density lipoprotein (LDL) peroxidation and reduces the risk of stomach cancer. In vitro radical scavenging and antioxidant capacity of p-coumaric acid were clarified using different analytical methodologies such as total antioxidant activity determination by ferric thiocyanate, hydrogen peroxide scavenging, 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH) scavenging, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging activity and superoxide anion radical scavenging, ferrous ions (Fe(2+)) chelating activity and ferric ions (Fe(3+)) reducing ability. p-Coumaric acid inhibited 71.2% lipid peroxidation of a linoleic acid emulsion at 45μg/mL concentration. On the other hand, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), α-tocopherol and ascorbic acid displayed 66.8%, 69.8%, 64.5% and 59.7% inhibition on the peroxidation of linoleic acid emulsion at the same concentration, respectively. In addition, p-coumaric acid had an effective DPPH scavenging, ABTS(+) scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, ferric ions (Fe(3+)) reducing power and ferrous ions (Fe(2+)) chelating activities. Also, those various antioxidant activities were compared to BHA, BHT, α-tocopherol and ascorbic acid as references antioxidant compounds. These results suggested that p-coumaric acid can be used in the pharmacological and food industry because of these properties. Copyright © 2013 Elsevier B.V. All rights reserved.

Antioxidant Activities of Functional Beverage Concentrates Containing Herbal Medicine Extracts.

PubMed

Park, Seon-Joo; Kim, Mi-Ok; Kim, Jung Hoan; Jeong, Sehyun; Kim, Min Hee; Yang, Su-Jin; Lee, Jongsung; Lee, Hae-Jeung

2017-03-01

This study investigated the antioxidant activity of functional beverage concentrates containing herbal medicine extracts (FBCH) using various antioxidant assays, such as 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, and reducing power assay. The total polyphenolic content of FBCH (81.45 mg/100 g) was higher than Ssanghwa tea (SHT, 37.56 mg/100 g). The antioxidant activities of FBCH showed 52.92% DPPH and 55.18% ABTS radical scavenging activities at 100 mg/mL, respectively. FBCH showed significantly higher antioxidant activities compared to the SHT (DPPH, 23.43%; ABTS, 22.21%; reducing power optical density; 0.23, P <0.05). In addition, intracellular reactive oxygen species generation significantly decreased in a concentration-dependent manner following FBCH treatment. These results suggest that the addition of herbal medicine extract contributes to the improved functionality of beverage concentrates.

Catalytic effects of silver plasmonic nanoparticles on the redox reaction leading to ABTS˙+ formation studied using UV-visible and Raman spectroscopy.

PubMed

Garcia-Leis, A; Jancura, D; Antalik, M; Garcia-Ramos, J V; Sanchez-Cortes, S; Jurasekova, Z

2016-09-29

ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) is a compound extensively employed to evaluate the free radical trapping capacity of antioxidant agents and complex mixtures such as biological fluids or foods. This evaluation is usually performed by using a colourimetric experiment, where preformed ABTS radical cation (ABTS˙ + ) molecules are reduced in the presence of an antioxidant causing an intensity decrease of the specific ABTS˙ + UV-visible absorption bands. In this work we report a strong effect of silver plasmonic nanoparticles (Ag NPs) on ABTS leading to the formation of ABTS˙ + . The reaction of ABTS with Ag NPs has been found to be dependent on the interfacial and plasmonic properties of NPs. Specifically, this reaction is pronounced in the presence of spherical nanoparticles prepared by the reduction of silver nitrate with hydroxylamine (AgH) and in the case of star-shaped silver nanoparticles (AgNS). On the other hand, spherical nanoparticles prepared by the reduction of silver nitrate with citrate apparently do not react with ABTS. Additionally, the formation of ABTS˙ + is investigated by surface-enhanced Raman scattering (SERS) and the assignment of the most intense vibrational bands of this compound is performed. The SERS technique enables us to detect this radical cation at very low concentrations of ABTS (∼2 μM). Altogether, these findings allow us to suggest the use of ABTS/Ag NPs-systems as reliable and easy going substrates to test the antioxidant capacity of various compounds, even at concentrations much lower than those usually used in the spectrophotometric assays. Moreover, we have suggested that ABTS could be employed as a suitable agent to investigate the interfacial and plasmonic properties of the metal nanoparticles and, thus, to characterize the nanoparticle metal systems employed for various purposes.

Antioxidant Contents and Antioxidant Activities of White and Colored Potatoes (Solanum tuberosum L.).

PubMed

Lee, Sang Hoon; Oh, Seung Hee; Hwang, In Guk; Kim, Hyun Young; Woo, Koan Sik; Woo, Shun Hee; Kim, Hong Sig; Lee, Junsoo; Jeong, Heon Sang

2016-06-01

This study was performed to evaluate and compare the antioxidant substance content and antioxidant activities of white (Superior) and colored (Hongyoung, Jayoung, Jasim, Seohong, and Jaseo) potatoes. The potatoes were extracted with 80% ethanol and were evaluated for the total polyphenol, flavonoid, and anthocyanin contents and for 1,1-diphenyl- 2-picrylhydrazyl (DPPH)/2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity, reducing power, and ferrous metal ion chelating effect. The total polyphenol, flavonoid, and anthocyanin contents of Hongyoung and Jayoung were higher than white and other colored potatoes. All colored potato extracts, except for Jaseo and Seohong, showed higher ABTS radical scavenging activities than the general white potato extract. Hongyoung and Jayoung had the highest ABTS and DPPH radical scavenging activities. Optical density values for the reducing power of Jayoung and Jaseo at concentration of 2 mg/mL were 0.148 and 0.090, respectively. All colored potato extracts had lower ferrous metal ion chelating effect than the white potato. A significant (P<0.05) positive correlation was observed between total polyphenol content and total flavonoid content (r=0.919), anthocyanin content (r=0.992), and ABTS radical scavenging activity (r=0.897). Based on these results, this research may be useful in developing the Hongyoung and Jayoung cultivars with high antioxidant activities.

Antioxidant Activity of the Essential Oil and its Major Terpenes of Satureja macrostema (Moc. and Sessé ex Benth.) Briq.

PubMed

Torres-Martínez, Rafael; García-Rodríguez, Yolanda Magdalena; Ríos-Chávez, Patricia; Saavedra-Molina, Alfredo; López-Meza, Joel Edmundo; Ochoa-Zarzosa, Alejandra; Garciglia, Rafael Salgado

2018-01-01

The aim of this study was to investigate the in vitro antioxidant activity of Satureja macrostema (Moc. and Sessé ex Benth.) Briq. (Lamiaceae) essential oil, a Mexican medicinal plant known as nurite. Fresh aerial parts of S. macrostema plants cultivated in greenhouse for 3 months were subjected to hydrodistillation in a Clevenger apparatus to obtain essential oil. Volatile compounds were identified by gas chromatography (GC) and GC/mass spectrometry. Antioxidant effectiveness of essential oil and its major terpenes of S. macrostema was examined by three different radical scavenging methods: 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and total antioxidant capacity (TAC). The concentrations tested were 0.001, 0.01, 0.1, and 1 mg/mL. The major volatile compounds were caryophyllene, limonene, linalool, pulegone, menthone, and thymol. S. macrostema essential oil showed the highest free radical scavenging activity with DPPH and ABTS methods (53.10% and 92.12%, respectively) at 1 mg/mL and 98% with TAC method at 0.1 mg/mL. Thymol exerted the highest antioxidant capacity with 0.1 mg/mL, reaching 83.38%, 96.96%, and 98.57% by DPPH, ABTS, and TAC methods. Caryophyllene, limonene, linalool, pulegone, and menthone exhibited an antioxidant capacity <25% with the DPPH and ABTS methods; however, limonene showed a TAC of 85.41% with 0.01 mg/mL. The essential oil of S. macrostema and thymol showed a free radical scavenging activity close to that of the synthetic butylated hydroxytoluene. The major volatile compounds of essential oil of Satureja macrostema were caryophyllene, limonene, linalool, pulegone, menthone and thymolThe essential oil of S. macrostema showed a high free radical scavengingThymol exerted the highest antioxidant capacity by DPPH, ABTS and TAC methods. Abbreviations used: GC: Gas Chromatography; DPPH: 2,2-diphenyl-1-picrylhydrazyl; ABTS: 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid; TAC: Total antioxidant capacity.

Assessment of antioxidant activity of cane brown sugars by ABTS and DPPH radical scavenging assays: determination of their polyphenolic and volatile constituents.

PubMed

Payet, Bertrand; Shum Cheong Sing, Alain; Smadja, Jacqueline

2005-12-28

Seven cane brown sugars (four from La Réunion, two from Mauritius, and one from France) were investigated for their polyphenol content and volatile composition in relation to their free radical scavenging capacity determined by ABTS and DPPH assays. The thin layer coated on the sugar crystal was extracted by Soxhlet extractor with dichloromethane. The volatile compounds of brown sugars were studied by GC-MS, and 43 compounds were identified. The total phenolic content of brown sugars was determined according to the Folin-Ciocalteu method. Phenolic compounds were quantified in the brown sugar extracts by LC-UV-ESI-MS. Brown sugar aqueous solutions exhibited weak free radical scavenging activity in the DPPH assay and higher antioxidant activity in the ABTS assay at relatively high concentration. The brown sugar extracts showed interesting free radical scavenging properties despite the low concentration of phenolic and volatile compounds. Sugar is a common foodstuff traditionally used for its sweetening properties, which might be accompanied by antioxidant properties arising from molecules (polyphenols, Maillard products) other than sucrose of the cane brown sugars.

Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.

PubMed

Gautam, Raju; Jachak, Sanjay M; Kumar, Vivek; Mohan, C Gopi

2011-03-15

Stellatin (4), isolated from Dysophylla stellata is a cyclooxygenase (COX) inhibitor. The present study reports the synthesis and biological evaluation of new stellatin derivatives for COX-1, COX-2 inhibitory and anti-inflammatory activities. Eight derivatives showed more pronounced COX-2 inhibition than stellatin and, 17 and 21 exhibited the highest COX-2 inhibition. They also exhibited the significant anti-inflammatory activity in TPA-induced mouse ear edema assay and their anti-inflammatory effects were more than that of stellatin and indomethacin at 0.5mg/ear. The derivatives were further evaluated for antioxidant activity wherein 16 and 17 showed potent free radical scavenging activity against DPPH and ABTS radicals. Molecular docking study revealed the binding orientations of stellatin and its derivatives into the active sites of COX-1 and COX-2 and thereby helps to design the potent inhibitors. Copyright © 2011 Elsevier Ltd. All rights reserved.

Drying effects on the antioxidant properties of polysaccharides obtained from Agaricus blazei Murrill.

PubMed

Wu, Songhai; Li, Feng; Jia, Shaoyi; Ren, Haitao; Gong, Guili; Wang, Yanyan; Lv, Zesheng; Liu, Yong

2014-03-15

Three polysaccharides (ABMP-F, ABMP-V, ABMP-A) were obtained from Agaricus blazei Murrill via methods such as freeze drying, vacuum drying and air drying, respectively. Their chemical compositions were examined, and antioxidant activities were investigated on the basis of assay for hydroxyl radical, DPPH radical, ABTS free radical scavenging ability and assay for Fe(2+)-chelating ability. Results showed that the three ABMPs have different physicochemical and antioxidant properties. Compared with air drying and vacuum drying methods, freeze drying method resulted to ABMP with higher neutral sugar, polysaccharide yield, uronic acid content, and stronger antioxidant abilities of hydroxyl radical, DPPH radical, ABTS radical scavenging and Fe(2+)-chelating. As a result, Agaricus blazei Murrill polysaccharides are natural antioxidant and freeze drying method serves as a good choice for the preparation of such polysaccharides and should be used to produce antioxidants for food industry. Copyright © 2014. Published by Elsevier Ltd.

Isolation, identification and antioxidant activity of bound phenolic compounds present in rice bran.

PubMed

Wang, Wei; Guo, Jia; Zhang, Junnan; Peng, Jie; Liu, Tianxing; Xin, Zhihong

2015-03-15

The bound phenolic compounds in rice bran were released and extracted with ethyl acetate based on alkaline digestion. An investigation of the chemical constituents of EtOAc extract has led to the isolation of a new compound, para-hydroxy methyl benzoate glucoside (8), together with nine known compounds, cycloeucalenol cis-ferulate (1), cycloeucalenol trans-ferulate (2), trans-ferulic acid (3), trans-ferulic acid methyl ester (4), cis-ferulic acid (5), cis-ferulic acid methyl ester (6), methyl caffeate (7), vanillic aldehyde (9) and para-hydroxy benzaldehyde (10). The structures of these compounds were determined using a combination of spectroscopic methods and chemical analysis. Among the compounds isolated, compound 3, 5 and 7 exhibited strong DPPH and ABTS(+) radical scavenging activities, followed by compounds 4 and 6. Compound 1 and 2 showed potent DPPH and ABTS(+) radical scavenging activities, compound 8 displayed moderate antioxidant activity against ABTS(+) radical, whereas compound 9 and 10 showed weak antioxidant activity. Copyright © 2014 Elsevier Ltd. All rights reserved.

Absolute rate constants of alkoxyl radical reactions in aqueous solution. [Tert-butyl hydroperoxide

DOE Office of Scientific and Technical Information (OSTI.GOV)

Erben-Russ, M.; Michel, C.; Bors, W.

1987-04-23

The pulse radiolysis technique was used to generate the alkoxyl radical derived from tert-butyl hydroperoxide (/sup t/BuOOH) in aqueous solution. The reactions of this radical with 2,2'-azinobis(3-ethyl-6-benzothiazolinesulfonate) (ABTS) and promethazine were monitored by kinetic spectroscopy. The unimolecular decay rate constant of the tert-butoxyl radical (/sup t/BuO) was determined to be 1.4 x 10/sup 6/ s/sup -1/. On the basis of this value, the rate constants for /sup t/BuO attack on quercetin, crocin, crocetin, ascorbate, isoascorbate, trolox c, glutathione, thymidine, adenosine, guanosine, and unsaturated fatty acids were determined. In addition, the reaction of /sup t/BuO with the polyunsaturated fatty acids (PUFA)more » was observed by directly monitoring the formation of the fatty acid pentadienyl radicals. Interestingly, the attack of /sup t/BuO on PUFA was found to be faster by about one order of magnitude as compared to the same reaction in a nonpolar solvent.« less

Antioxidant Activity of the Essential Oil and its Major Terpenes of Satureja macrostema (Moc. and Sessé ex Benth.) Briq.

PubMed Central

Torres-Martínez, Rafael; García-Rodríguez, Yolanda Magdalena; Ríos-Chávez, Patricia; Saavedra-Molina, Alfredo; López-Meza, Joel Edmundo; Ochoa-Zarzosa, Alejandra; Garciglia, Rafael Salgado

2017-01-01

Background: The aim of this study was to investigate the in vitro antioxidant activity of Satureja macrostema (Moc. and Sessé ex Benth.) Briq. (Lamiaceae) essential oil, a Mexican medicinal plant known as nurite. Materials and Methods: Fresh aerial parts of S. macrostema plants cultivated in greenhouse for 3 months were subjected to hydrodistillation in a Clevenger apparatus to obtain essential oil. Volatile compounds were identified by gas chromatography (GC) and GC/mass spectrometry. Antioxidant effectiveness of essential oil and its major terpenes of S. macrostema was examined by three different radical scavenging methods: 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2’-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and total antioxidant capacity (TAC). The concentrations tested were 0.001, 0.01, 0.1, and 1 mg/mL. Results: The major volatile compounds were caryophyllene, limonene, linalool, pulegone, menthone, and thymol. S. macrostema essential oil showed the highest free radical scavenging activity with DPPH and ABTS methods (53.10% and 92.12%, respectively) at 1 mg/mL and 98% with TAC method at 0.1 mg/mL. Thymol exerted the highest antioxidant capacity with 0.1 mg/mL, reaching 83.38%, 96.96%, and 98.57% by DPPH, ABTS, and TAC methods. Caryophyllene, limonene, linalool, pulegone, and menthone exhibited an antioxidant capacity <25% with the DPPH and ABTS methods; however, limonene showed a TAC of 85.41% with 0.01 mg/mL. Conclusion: The essential oil of S. macrostema and thymol showed a free radical scavenging activity close to that of the synthetic butylated hydroxytoluene. SUMMARY The major volatile compounds of essential oil of Satureja macrostema were caryophyllene, limonene, linalool, pulegone, menthone and thymolThe essential oil of S. macrostema showed a high free radical scavengingThymol exerted the highest antioxidant capacity by DPPH, ABTS and TAC methods. Abbreviations used: GC: Gas Chromatography; DPPH: 2,2-diphenyl-1-picrylhydrazyl; ABTS: 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid; TAC: Total antioxidant capacity. PMID:29491647

Captopril and 6-mercaptopurine: whose SH possesses higher antioxidant ability?

PubMed

Li, Guo-Xiang; Liu, Zai-Qun

2009-12-01

Antioxidant capacities of captopril (CAP), 6-mercaptopurine (6-MP) and 9-(beta-D-ribofuranosyl)-6-mercaptopurine (6-MPR) were investigated by interacting them with 2,2'-diphenyl-1-picrylhydrazyl (DPPH), galvinoxyl radical, and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) cation radical (ABTS(+)(*)), and by protecting DNA and erythrocyte against 2,2'-azobis(2-amidinopropane hydrochloride) (AAPH) induced oxidation. It was found that CAP possessed the highest ability to donate the hydrogen atom in -SH to DPPH and galvinoxyl, while 6-MPR had the strongest ability to reduce ABTS(+)(*). In the process of protecting DNA and erythrocytes against AAPH-induced oxidation, CAP can trap 0.5 and 1.3 radicals, 6-MP can trap 0.6 and 2.2, and 6-MPR can trap 1.0 and 3.0 radicals, respectively. CAP can also protect erythrocytes against hemin-induced hemolysis.

Radiation and quantum chemical studies of chalcone derivatives.

PubMed

Gaikwad, P; Priyadarsini, K I; Naumov, S; Rao, B S M

2010-08-05

The reactions of oxidizing radicals ((*)OH, Br(2)(*-), and SO(4)(*-)) with -OH-, -CH(3)-, or -NH(2)-substituted indole chalcones and hydroxy benzenoid chalcones were studied by radiation and quantum chemical methods. The (*)OH radical was found to react by addition at diffusion-controlled rates (k = 1.1-1.7 x 10(10) dm(3) mol(-1) s(-1)), but Br(2)(*-) radical reacted by 2 orders of magnitude lower. Quantum chemical calculations at the B3LYP/6-31+G(d,p) level of theory have shown that the (C2-OH)(*), (C11-OH)(*), and (C10-OH)(*) adducts of the indole chalcones and the (C7-OH)(*) and (C8-OH)(*) adducts of the hydroxy benzenoid chalcones are more stable with DeltaH = -39 to -28 kcal mol(-1) and DeltaG = -32 to -19 kcal mol(-1). This suggests that (*)OH addition to the alpha,beta-unsaturated bond is a major reaction channel in both types of chalcones and is barrierless. The stability and lack of dehydration of the (*)OH adducts arise from two factors: strong frontier orbital interaction due to the low energy gap between interacting orbitals and the negligible Coulombic repulsion due to small absolute values of Mulliken charges. The transient absorption spectrum measured in the (*)OH radical reaction with all the indole chalcone derivatives exhibited a maximum at 390 nm, which is in excellent agreement with the computed value (394 nm). The formation of three phenolic products under steady-state radiolysis is in line with the three stable (*)OH adducts predicted by theory. Independent of the substituent, identical spectra (lambda(max) = 330-360 and approximately 580 nm) were obtained on one-electron oxidation of the three indole chalcones. MO calculations predict the deprotonation from the -NH group is more efficient than from the substituent due to the larger electron density on the N1 atom forming the chalcone indolyl radical. Its reduction potential was determined to be 0.56 V from the ABTS(*-)/ABTS(2-) couple. In benzenoid chalcones, the (*)OH adduct spectrum is characterized by a peak at 270 nm and a broad maximum centered in the range 430-450 nm with an intense bleaching at 340 nm. The spectrum formed by electron transfer in these derivatives with lambda(max) = 280 and 380 nm (epsilon(280) = 5000 dm(3) mol(-1) cm(-1) and epsilon(380) = 700 dm(3) mol(-1) cm(-1)) was assigned to its phenoxyl radical. Our pulse radiolysis experiments in combination with quantum chemical calculations demonstrate that chalcones are efficient scavengers of damaging oxyl radicals.

Antioxidant and antigenotoxic activities in Acacia salicina extracts and its protective role against DNA strand scission induced by hydroxyl radical.

PubMed

Chatti, Ines Bouhlel; Boubaker, Jihed; Skandrani, Ines; Bhouri, Wissem; Ghedira, Kamel; Chekir Ghedira, Leila

2011-08-01

The antioxidant potency of Acacia salicina extracts was investigated. Total antioxidant capacity was determined using an ABTS(+) assay. Superoxide radical scavenging was measured using riboflavin-light-nitro blue tetrazolium (NBT) assay. In addition, the content of phenols, total flavonoids and sterols were measured in the tested extracts. The petroleum ether exhibited a potent scavenging activity toward ABTS radical cations. Whereas, chloroform extract showed the highest activity against superoxides radicals and was also able to protect pKS plasmid DNA against hydroxyl radicals induced DNA damages. The antimutagenicity of these extracts was assayed using the Ames assay against Salmonella typhimurium TA98 and S. typhimurium TA 1535 tester strains at different concentrations. These extracts decreased significantly the mutagenecity induced by sodium azide (SA) and 4-nitro-o-phenylenediamine (NOP). The antioxidant and antimutagenecity activities exhibited by A. salicina depended on the chemical composition of the tested extracts. Copyright © 2011 Elsevier Ltd. All rights reserved.

Antioxidant Properties of Water-Soluble Gum from Flaxseed Hulls

PubMed Central

Bouaziz, Fatma; Koubaa, Mohamed; Barba, Francisco J.; Roohinejad, Shahin; Chaabouni, Semia Ellouz

2016-01-01

Soluble flaxseed gum (SFG) was extracted from flax (Linum usitatissimum) hulls using hot water, and its functional groups and antioxidant properties were investigated using infrared spectroscopy and different antioxidant assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), reducing power capacity, and β-carotene bleaching inhibition assay), respectively. The antioxidant capacity of SFG showed interesting DPPH radical-scavenging capacity (IC50 SFG = 2.5 mg·mL−1), strong ABTS radical scavenging activity (% inhibition ABTS = 75.6% ± 2.6% at 40 mg·mL−1), high reducing power capacity (RPSFG = 5 mg·mL−1), and potent β-carotene bleaching inhibition activity (IC50 SFG = 10 mg·mL−1). All of the obtained results demonstrate the promising potential use of SFG in numerous industrial applications, and a way to valorize flaxseed hulls. PMID:27490574

Evaluation of Both Free Radical Scavenging Capacity and Antioxidative Damage Effect of Polydatin.

PubMed

Jin, Ju; Li, Yan; Zhang, Xiuli; Chen, Tongsheng; Wang, Yifei; Wang, Zhiping

Cellular damage such as oxidation and lipid peroxidation, and DNA damage induced by free-radicals like reactive oxygen species, has been implicated in several diseases. Radicals generated by 2,2-azobis (2-amidino-propane) dihydrochloride (AAPH) are similar to physiologically active ones. In this study we found that polydatin, a resveratrol natural precursor derived from many sources, has the capacity of free radical scavenging and antioxidative damage. Using free radical scavenging assays, the IC50 values of polydatin were 19.25 and 5.29 μg/ml with the DPPH and the ABTS assay, respectively, and 0.125 mg ferrous sulfate/1 mg polydatin with the FRAP assay. With the AAPH-induced oxidative injury cell model assay, polydatin showed a strong protective effect against the human liver tumor HepG2 cell oxidative stress damage. These results indicate that the antioxidant properties of polydatin have great potential for use as an alternative to more toxic synthetic antioxidants as an additive in food, cosmetics and pharmaceutical preparations for the treatment of oxidative diseases.

[Correlation Between Functional Groups and Radical Scavenging Activities of Acidic Polysaccharides from Dendrobium].

PubMed

Liao, Ying; Yuan, Wen-yu; Zheng, Wen-ke; Luo, Ao-xue; Fan, Yi-jun

2015-11-01

To compare the radical scavenging activity of five different acidic polysaccharides, and to find the correlation with the functional groups. Alkali extraction method and Stepwise ethanol precipitation method were used to extract and concentrate the five Dendrobium polysaccharides, and to determine the contents of sulfuric acid and uronic acid of each kind of acidic polysaccharides, and the scavenging activity to ABTS+ radical and hydroxyl radical. Functional group structures were examined by FTIR Spectrometer. Five kinds of Dendrobium polysaccharides had different ability of scavenging ABTS+ free radical and hydroxyl free radical. Moreover, the study had shown that five kinds of antioxidant activity of acidic polysaccharides had obvious correlation withuronic acid and sulfuric acid. The antioxidant activity of each sample was positively correlated with the content of uronic acid, and negatively correlated with the content of sulfuric acid. Sulfuric acid can inhibit the antioxidant activity of acidic polysaccharide but uronic acid can enhance the free radical scavenging activity. By analyzing the structure characteristics of five acidic polysaccharides, all samples have similar structures, however, Dendrobium denneanum, Dendrobium devonianum and Dendrobium officinale which had β configuration have higher antioxidant activity than Dendrobium nobile and Dendrobium fimbriatum which had a configuration.

In vitro antioxidant potential of dicliptera roxburghiana

PubMed Central

2013-01-01

Background Stress caused by free radicals accumulation result into many hazardous diseases. A number of investigations are focusing to find out the plant oriented natural antioxidant moieties. The basic aim of this research was to investigate the antioxidant potential, total Phenolic and flavonoids contents and photochemical screening of the crude methanol extract and its derived various fractions Dicliptera roxburghiana of Acanthaceae family. Methods Crude methanol extract of aerial parts of Dicliptera roxburghiana (DRME) was partitioned in to n-hexane (DRHF), chloroform (DRCF), ethyl acetate (DREF), n-butanol (DRBF) and the remaining soluble portion as residual aqueous fraction (DRAF). We evaluated the antioxidant activities of the extract and various fractions through different analytical methods such as DPPH, superoxide anion, ABTS, H2O2, hydroxyl radical and phosphomolybdate radical inhibition. In vitro lipid peroxidation and reducing power of the plant was also analyzed. Total flavonoid and phenolic contents of the extract and all fractions were also quantified. Plant was also subjected for preliminary phytochemical screening to confirm the presence or absence of various constituents in the plant. Results Phytochemical screening confirmed the presence of flavonoids, phenolics, tannins, alkaloids, saponins, terpenoids and coumarines. Quantitative analysis revealed the maximum amount of total phenolic and flavonoid contents in DRME while lowest in DRHF. Methanol extract, DREF, DRCF and DRBF exhibited promising antioxidant potential for DPPH, ABTS, H2O2, phosphomolybdate, superoxide anion and hydroxyl radical scavenging capabilities, while these were not appreciable for DRHF and DRAF. All fractions except DRHF and DRAF possess strong reducing power ability and showed appreciable lipid peroxidation inhibition. Conclusion These research investigations revealed that Dicliptera roxburghiana is a potent source of natural antioxidants. Hence the plant can be used for management of different stress and anxiety related ailments. PMID:23777321

Evaluation of Physiological Activities of the Citron (Citrus junos Sieb. ex TANAKA) Seed Extracts

PubMed Central

Kim, Seong Yeong; Shin, Kwang-Soon

2013-01-01

Citron seed extracts (CSEs) were made using distilled water (CSEW), ethanol (CSEE), and n-hexane (CSEH), to measure the total polyphenol contents, DPPH and ABTS radical scavenging activities, and anti-complementary activity. The total polyphenol content was observed the highest in CSEE (188.71 μg/mL), and occurred in the following order: CSEE>CSEW (141.11 μg/mL)>CSEH (26.19 μg/mL) at 10 mg/mL. CSEE (63.56%) and CSEW (56.61%) showed significantly higher DPPH radical scavenging activities when compared with CSEH (28.57%). ABTS radical scavenging activities of CSEE (45.53%) and CSEW (40.02%) were also observed to be higher, whereas CSEH did not show ABTS radical scavenging activity. Anti-complementary activity of CSEE (26.85%) showed a greater activity than that of CSEW (7.84%) at 1,000 μg/mL. Limonin and nomilin contents had the highest values (1.882% and 2.089%) in CSEE, and with 0.327% and 0.139% in CSEW; however, CSEH showed relatively very low values at 0.061% and 0.026%, respectively. Among the CSEs tested, CSEE as a by-product from citron may provide an important source of dietary antioxidant compounds with rich polyphenol and limonoid contents, and immunopotentiating activity, including the complement activation factor. PMID:24471132

Isolation, purification and characterization of antioxidative peptide of pearl millet (Pennisetum glaucum) protein hydrolysate.

PubMed

Agrawal, Himani; Joshi, Robin; Gupta, Mahesh

2016-08-01

Pearl millet (Pennisetum glaucum) is a rich source of protein, used for present study to hydrolyze protein, peptide separation and its functional activity. Antioxidative bioactive peptide was successfully identified from pearl millet using trypsin enzyme. Different antioxidative potential of isolated peptide were assessed based on activity of DPPH radical, ABTS radical, hydroxyl radical, Fe(2+) chelating ability and reducing power. Bioactive peptide separated by gel-filtration chromatography, showed the higher antioxidant activity as tested by different free radicals. The activity of pearl millet protein hydrolysate fraction was found for DPPH assay (67.66%), ABTS assay (78.81%), Fe(2+) chelating ability (51.20%), hydroxyl assay (60.95%) and reducing power (0.375nm) was further purified using reversed-phase UFLC and subjected to matrix assisted laser desorption/ionization time-of-flight/time-of-flight mass spectrometry (MALDI-TOF/TOF-MS) for sequential identification of the peptide. The sequence SDRDLLGPNNQYLPK was identified as antioxidant peptide. Copyright © 2016 Elsevier Ltd. All rights reserved.

Effects of extraction methods on the antioxidant activities of polysaccharides from Agaricus blazei Murrill.

PubMed

Jia, Shaoyi; Li, Feng; Liu, Yong; Ren, Haitao; Gong, Guili; Wang, Yanyan; Wu, Songhai

2013-11-01

Five polysaccharides were obtained from Agaricus blazei Murrill (ABM) through different extraction methods including hot water extraction, single enzyme extraction (pectinase, cellulase or papain) and compound enzymes extraction (cellulase:pectinase:papain). Their characteristics such as the polysaccharide yield, polysaccharide content, protein content, infrared spectra were determined, and antioxidant activities were investigated on the basis of hydroxyl radical, DPPH free radical, ABTS free radical and reducing power. The results showed that five extracts exhibited antioxidant activities in a concentration-dependent manner. Compared with other methods, the compound enzymes extraction method was found to present the highest polysaccharides yield (17.44%). Moreover, compound enzymes extracts exhibited the strongest reducing power and highest scavenging rates on hydroxyl radicals, DPPH radicals and ABTS radicals. On the contrary, hot water extraction method had the lowest polysaccharides yield of 11.95%, whose extracts also exhibited the lowest antioxidant activities. Overall, the available data obtained in vitro models suggested that ABM extracts were natural antioxidants and compound enzymes extraction was an appropriate, mild and effective extracting method for obtaining the polysaccharide extracts from Agaricus blazei Murrill (ABM). Copyright © 2013 Elsevier B.V. All rights reserved.

Combination of Antioxidants from Different Sources Could Offer Synergistic Benefits: A Case Study of Tea and Ginger Blend.

PubMed

Makanjuola, Solomon A; Enujiugha, Victor N; Omoba, Olufunmilayo S; Sanni, David M

2015-11-01

Tea and ginger are plants with high antioxidant potential. Combinations of antioxidants from different sources could also produce synergistic antioxidant effects. This study investigated the influence of solvent on antioxidant content of tea, ginger, and tea + ginger blends. Under the investigated extraction conditions, water was the most effective extraction solvent to maximise peroxide scavenging and iron chelating activity of tea, ginger, and their blends. Aqueous ethanol was the most effective solvent to maximise ABTS radical scavenging activity and ethanol was the best solvent to maximise DPPH radical scavenging activity. A good multivariate regression model that explains the relationship between the total flavonoid content of the extracts and their antioxidant activities was obtained (R2 and Q2 of 0.93 and 0.83, respectively). Extracts of tea-ginger blends exhibited synergistic effects in their ABTS and DPPH radical scavenging activity.

The comparison of anti-oxidative kinetics in vitro of the fluid extract from maidenhair tree, motherwort and hawthorn.

PubMed

Bernatoniene, Jurga; Kucinskaite, Agne; Masteikova, Ruta; Kalveniene, Zenona; Kasparaviciene, Giedre; Savickas, Arunas

2009-01-01

The aim of the study was to perform a quantitative analysis of fluid extracts of maidenhair tree (Ginkgo biloba L.), motherwort (Leonurus cardiaca L.) and hawthorn (Crataegus monogyna Jacq.), to evaluate their antioxidant activity and to compare their ability to inactivate free radicals. The antioxidant activity was measured using the DPPH*and the ABTS*+ radical scavenging reaction systems. The study showed that the manifestation of the radical scavenging capacity in the DPPH* reaction system was in the following order: the fluid extract of hawthorn (70.37 +/- 0.80%) > the fluid extract of maidenhair tree (82.63 +/- 0.23%) > the fluid extract of motherwort (84.89 +/- 0.18%), while in the ABTS*+ reaction system, the manifestation of the radical scavenging capacity was in the following order: the fluid extract of hawthorn (87.09 +/- 0.55%) > the fluid extract of motherwort (88.28 +/- 1.06%) > the fluid extract of maidenhair tree (88.39 +/- 0.72%). The results showed that in the DPPH* reaction system, fluid extract of motherwort manifested higher antioxidant activity, compared to the fluid extracts of maidenhair tree and hawthorn. By contrast, in the ABTS*+ reaction system, higher antioxidant activity was found in the fluid extract of maidenhair tree, compared to the fluid extracts of motherwort and hawthorn. This would suggest that preparations manufactured from these herbal raw materials could be used as effective preventive means and valuable additional remedies in the treatment of diseases caused by oxidative stress.

Extraction, Structural Characterization, and Potential Antioxidant Activity of the Polysaccharides from Four Seaweeds

PubMed Central

He, Jinzhe; Xu, Yaoyang; Chen, Hongbo; Sun, Peilong

2016-01-01

Four seaweed polysaccharides were extracted from Sarcodia ceylonensis, Ulva lactuca L., Gracilaria lemaneiformis, and Durvillaea antarctica, respectively, by microwave-assisted extraction. The effect of three significant variables (extraction time, extraction temperature, and the ratio of water to raw material) on the process for extracting polysaccharides was investigated, along with the optimization of the extraction using the response surface method (RSM) with a Box–Behnken design. The polysaccharide structure, monosaccharide composition, degree of sulfation, and molecular weight (MW) distribution were analyzed by infrared (IR) spectrometry, gas chromatography (GC), and high-performance gel permeation chromatography (HPGPC). IR spectrometry showed that Sarcodia ceylonensis polysaccharide (SCP), Ulva lactuca L. polysaccharide (ULLP), and Durvillaea antarctica polysaccharide (DAP) were all sulfated polysaccharides and, except Gracilaria lemaneiformis polysaccharide (GLP), all belong to β-pyranosidic polysaccharides. The average molecular weight (MW) of SCP, ULLP, GLP, and DAP was 466, 404, 591, and 482 kDa, respectively. The quantitative and comparative results with external standards indicated that the main monosaccharide in SCP and ULLP was mannose; and GLP and DAP were mainly composed of galactose and glucose, respectively. Then the in vitro antioxidant activity of all of the polysaccharides was evaluated using different assays—2,2–azino –bis (3-ethylbenzthiazoline-6- sulfonate) (ABTS), hydroxyl radical, nitrite scavenging capacity, and reducing power—and the relationship between their antioxidant activity and chemical characteristics were also examined. ULLP presented the highest ABTS radical scavenging activity; ULLP, SCP and DAP also showed a strong effect on the ABTS radical scavenging activity. SCP and ULLP exhibited excellent hydroxyl radical scavenging activities, about 83.33% ± 2.31% and 80.07% ± 2.17%, respectively, at 4 mg/mL. The reducing power of DAP was relatively more pronounced than that of the three other polysaccharides. However, the nitrite scavenging activities of the four seaweed polysaccharides were weaker than other antioxidant activity (ABTS), hydroxyl radical scavenging capacity, and reducing power. In addition, GLP exhibited lower activities than the other three samples in all of the tests for the antioxidant activity. PMID:27916796

Extraction, Structural Characterization, and Potential Antioxidant Activity of the Polysaccharides from Four Seaweeds.

PubMed

He, Jinzhe; Xu, Yaoyang; Chen, Hongbo; Sun, Peilong

2016-11-28

Four seaweed polysaccharides were extracted from Sarcodia ceylonensis , Ulva lactuca L., Gracilaria lemaneiformis , and Durvillaea antarctica , respectively, by microwave-assisted extraction. The effect of three significant variables (extraction time, extraction temperature, and the ratio of water to raw material) on the process for extracting polysaccharides was investigated, along with the optimization of the extraction using the response surface method (RSM) with a Box-Behnken design. The polysaccharide structure, monosaccharide composition, degree of sulfation, and molecular weight ( M W ) distribution were analyzed by infrared (IR) spectrometry, gas chromatography (GC), and high-performance gel permeation chromatography (HPGPC). IR spectrometry showed that Sarcodia ceylonensis polysaccharide (SCP), Ulva lactuca L. polysaccharide (ULLP), and Durvillaea antarctica polysaccharide (DAP) were all sulfated polysaccharides and, except Gracilaria lemaneiformis polysaccharide (GLP), all belong to β-pyranosidic polysaccharides. The average molecular weight ( M W ) of SCP, ULLP, GLP, and DAP was 466, 404, 591, and 482 kDa, respectively. The quantitative and comparative results with external standards indicated that the main monosaccharide in SCP and ULLP was mannose; and GLP and DAP were mainly composed of galactose and glucose, respectively. Then the in vitro antioxidant activity of all of the polysaccharides was evaluated using different assays-2,2-azino -bis (3-ethylbenzthiazoline-6- sulfonate) (ABTS), hydroxyl radical, nitrite scavenging capacity, and reducing power-and the relationship between their antioxidant activity and chemical characteristics were also examined. ULLP presented the highest ABTS radical scavenging activity; ULLP, SCP and DAP also showed a strong effect on the ABTS radical scavenging activity. SCP and ULLP exhibited excellent hydroxyl radical scavenging activities, about 83.33% ± 2.31% and 80.07% ± 2.17%, respectively, at 4 mg/mL. The reducing power of DAP was relatively more pronounced than that of the three other polysaccharides. However, the nitrite scavenging activities of the four seaweed polysaccharides were weaker than other antioxidant activity (ABTS), hydroxyl radical scavenging capacity, and reducing power. In addition, GLP exhibited lower activities than the other three samples in all of the tests for the antioxidant activity.

In vitro antioxidant activity of polysaccharide from Gardenia jasminoides ellis

USGS Publications Warehouse

Fan, Y.; Ge, Z.; Luo, A.

2011-01-01

A water-soluble polysaccharide, GP, was isolated from Gardenia jasminoides Ellis through hot water extraction followed by ethanol precipitation. The in vitro free radicals scavenging tests exhibited that GP has significant scavenging abilities especially for ABTS, DPPH, and hydroxyl radicals, which suggests that the polysaccharide GP is a novel antioxidant. ?? 2011 Academic Journals.

LPS-induced NO inhibition and antioxidant activities of ethanol extracts and their solvent partitioned fractions from four brown seaweeds

NASA Astrophysics Data System (ADS)

Cho, Myoung Lae; Lee, Dong-Jin; Lee, Hyi-Seung; Lee, Yeon-Ju; You, Sang Guan

2013-12-01

The nitric oxide inhibitory (NOI) and antioxidant (ABTS and DPPH radical scavenging effects with reducing power) activities of the ethanol (EtOH) extracts and solvent partitioned fractions from Scytosiphon lomentaria, Chorda filum, Agarum cribrosum, and Desmarestia viridis were investigated, and the correlation between biological activity and total phenolic (TP) and phlorotannin (TPT) content was determined by PCA analysis. The yield of EtOH extracts from four brown seaweeds ranged from 2.6 to 6.6% with the highest yield from D. viridis, and the predominant compounds in their solvent partitioned fractions had medium and/or less polarity. The TP and TPT content of the EtOH extracts were in the ranges of 25.0-44.1 mg GAE/g sample and 0.2-4.6 mg PG/g sample, respectively, which were mostly included in the organic solvent partitioned fractions. Strong NOI activity was observed in the EtOH extracts and their solvent partitioned fractions from D. viridis and C. filum. In addition, the EtOH extract and its solvent partitioned fractions of D. viridis exhibited little cytotoxicity to Raw 264.7 cells. The most potent ABTS and DPPH radical scavenging capacity was shown in the EtOH extracts and their solvent partitioned fractions from S. lomentaria and C. filum, and both also exhibited strong reducing ability. In the PCA analysis the content of TPT had a good correlation with DPPH ( r = 0.62), ABTS ( r = 0.69) and reducing power ( r = 0.65), however, an unfair correlation was observed between the contents of TP and TPT and NOI, suggesting that the phlorotannins might be responsible for the DPPH and ABTS radical scavenging activities.

Free radical-scavenging delta-lactones from Boletus calopus.

PubMed

Kim, Jin-Woo; Yoo, Ick-Dong; Kim, Won-Gon

2006-12-01

The methanol extracts from the fruiting body of the mushroom Boletus calopus showed free radical-scavenging activity. Bioactivity-guided fractionation of the methanol extracts led to a new hydroxylated calopin named calopin B, along with the known delta-lactones calopin and cyclocalopin A. The structure of the new calopin analogue was elucidated by spectroscopic methods. All compounds showed potent free radical-scavenging activity against superoxide, DPPH, and ABTS radicals with IC (50) values of 1.2 - 5.4 microg/mL.

Antiglycation activity of lipophilized epigallocatechin gallate (EGCG) derivatives.

PubMed

Wang, Mingfu; Zhang, Xinchen; Zhong, Ying Joy; Perera, Nishani; Shahidi, Fereidoon

2016-01-01

Lipophilized EGCG derivatives were synthesized by esterification of EGCG with aliphatic fatty acids and demonstrated to possess many advantages, such as higher lipophilicity and apparent health benefits over the parent EGCG. This study used a total of seven lipophilized EGCG derivatives with fatty acids of different chain lengths attached and examined the impact of lipophilization on EGCG's antiglycation activity in vitro. The length of fatty acid chain was found to be an important factor, which positively correlated with ABTS radical scavenging capacity but long chain bulky substitutes prevented methylglyoxal (MGO) trapping. Except docosahexaenoic acid (DHA), lipophilization generally showed no interference with EGCG's in vitro inhibitory activity of advanced glycation endproducts (AGEs) formation. Therefore, the lipophilized EGCG derivatives are promising candidates worthy of further exploration for preventing AGEs accumulation in vivo and hence treating AGEs-associated diseases. Copyright © 2015 Elsevier Ltd. All rights reserved.

Comparative study on the antioxidant activities of extracts of Coreopsis tinctoria flowering tops from Kunlun Mountains, Xinjiang, north-western China.

PubMed

Yao, Xincheng; Gu, Chengzhi; Tian, Liping; Wang, Xinbing; Tang, Hui

2016-01-01

Coreopsis tinctoria flowering tops (CTFs) from the Kunlun Mountains in Xinjing (north-western China) have been used for tea production for about a century. This study aims to assess the antioxidant activities and total phenolic, flavonoid and proanthocyanidin contents of various solvent extracts of CTF. CTF was extracted using n-hexane, chloroform, ethyl acetate, n-butanol, 75% aqueous ethanol (AEE) and water. The antioxidant activities of the CTF extracts were investigated through DPPH, ABTS, *OH, *O2(-), total antioxidant capacity and reducing power assays. The results showed that n-butanol extract showed the highest contents of total phenols and flavonoids, with DPPH, ABTS and *OH radical-scavenging activities with IC50 values of 134, 90.72 and 13.8 μg mL(-1), respectively. The AEE demonstrated the strongest DPPH and ABTS radical-scavenging activities, with IC50 values of 103 and 75.16 μg mL(-1), respectively. Given its high antioxidant effect, CTF is a good source of natural antioxidants or functional food materials.

Effect of olive cultivar on bioaccessibility and antioxidant activity of phenolic fraction of virgin olive oil.

PubMed

Quintero-Flórez, Angélica; Pereira-Caro, Gema; Sánchez-Quezada, Cristina; Moreno-Rojas, José Manuel; Gaforio, José J; Jimenez, Antonio; Beltrán, Gabriel

2017-06-05

This study aims to characterize the phenolic profile and antioxidant capacity of seven monovarietal virgin olive oils (VOOs) and evaluate their in vitro gastrointestinal stability. 'Picual', 'Blanqueta', 'Sevillana', 'Habichuelero', and 'Chetoui' olive cultivars were selected for VOO extraction. The oils were subjected to in vitro digestion. The recovery index (RI) of phenolic compounds after each digestion step and the bioaccessibility index (BI) were evaluated. In addition, the antioxidant activity of the bioaccessible fraction (BF) of VOOs was determined by DPPH, ABTS, and ORAC assays, as well as by studying the intracellular reactive oxygen species in Caco-2 cells. Differences were found in the composition of phenolic compounds in VOOs depending on cultivars. During the digestive process, important losses of phenolic compounds were observed between the buccal and duodenal steps, unlike HTy and Ty, which presented increased recovery due to the hydrolysis of secoiridoid derivatives. Differences in the bioaccessibility of phenolic compounds were found between varieties of VOOs. 'Sevillana' VOO had the highest total bioaccessibility (36%), followed by the 'Picual' (19%), 'Chetoui' (17%), 'Habichuelero' (10%), and 'Blanqueta' (8%) varieties. The BF of all the varieties of VOO showed similar radical ABTS scavenging capacity, 'Chetoui', and 'Blanqueta'-BF having the highest radical DPPH scavenging capacity, and 'Habichuelero' and 'Picual'-BF showing protective effects against the peroxyl radical measured by ORAC FL assay. All VOO-BFs presented decreases in ROS levels in Caco-2 cells. Our results suggest differences in the bioaccessibility of phenolics from diverse VOO varieties, which could lead to different biological properties. Therefore, this study represents a first step toward the development of novel dietary strategies focusing on the phenolic supplementation of different VOOs to preserve human health.

ABTS as an Electron Shuttle to Enhance the Oxidation Kinetics of Substituted Phenols by Aqueous Permanganate.

PubMed

Song, Yang; Jiang, Jin; Ma, Jun; Pang, Su-Yan; Liu, Yong-Ze; Yang, Yi; Luo, Cong-Wei; Zhang, Jian-Qiao; Gu, Jia; Qin, Wen

2015-10-06

In this study, it was, interestingly, found that 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonate (ABTS), a widely used electron shuttle, could greatly accelerate the oxidation of substituted phenols by potassium permanganate (Mn(VII)) in aqueous solutions at pH 5-9. This was attributed to the fact that these substituted phenols could be readily oxidized by the stable radical cation (ABTS(•+)), which was quickly produced from the oxidation of ABTS by Mn(VII). The reaction of Mn(VII) with ABTS exhibited second-order kinetics, with stoichiometries of ∼5:1 at pH 5-6 and ∼3:1 at pH 7-9, and the rate constants varied negligibly from pH 5 to 9 (k = (9.44 ± 0.21) × 10(4) M(-1) s(-1)). Comparatively, the reaction of ABTS(•+) with phenol showed biphasic kinetics. The second-order rate constants for the reactions of ABTS(•+) with substituted phenols obtained in the initial phase were strongly affected by pH, and they were several orders of magnitude higher than those for the reactions of Mn(VII) with substituted phenols at each pH. Good Hammett-type correlations were found for the reactions of ABTS(•+) with undissociated (log(k) = 2.82-4.31σ) and dissociated phenols (log(k) = 7.29-5.90σ). The stoichiometries of (2.2 ± 0.06):1 (ABTS(•+) in excess) and (1.38 ± 0.18):1 (phenol in excess) were achieved in the reaction of ABTS(•+) with phenol, but they exhibited no pH dependency.

Preparative isolation and purification of antioxidative diarylheptanoid derivatives from Alnus japonica by high-speed counter-current chromatography.

PubMed

Lim, Soon Sung; Lee, Min Young; Ahn, Hong Ryul; Choi, Soon Jung; Lee, Jae-Yong; Jung, Sang Hoon

2011-12-01

This study employed the online HPLC-2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS)(+) bioassay to rapidly determine the antioxidant compounds occurring in the crude extract of Alnus japonica. The negative peaks of the ABTS(+) radical scavenging detection system, which indicated the presence of antioxidant activity, were monitored by measuring the decrease in absorbance at 734 nm. The ABTS(+)-based antioxidant activity profile showed that three negative peaks exhibited antioxidant activity. High-speed counter-current chromatography (HSCCC) was used for preparative scale separation of the three active peaks from the extract. The purity of the isolated compounds was analyzed by HPLC and their structures were identified by (1)H- and (13)C-nuclear magnetic resonance spectrometry (NMR), heteronuclear multiple bond correlation (HMBC), and heteronuclear single quantum correlation (HSQC). Two solvent systems composed of n-hexane/ethylacetate/methanol/water (4:6:4:6, v/v) and of ethyl acetate/methanol/water (1:0.1:1, v/v) were performed in high-speed counter-current chromatography. Consequently, a total of 527 mg of hirsutanonol 5-O-β-D-glucopyranoside, 80.04 mg of 3-deoxohirsutenonol 5-O-β-D-glucopyranoside, and 91.0 mg of hirsutenone were obtained with purity of 94.7, 90.5, and 98.6%, respectively. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Laccase/Mediator Systems: Their Reactivity toward Phenolic Lignin Structures.

PubMed

Hilgers, Roelant; Vincken, Jean-Paul; Gruppen, Harry; Kabel, Mirjam A

2018-02-05

Laccase-mediator systems (LMS) have been widely studied for their capacity to oxidize the nonphenolic subunits of lignin (70-90% of the polymer). The phenolic subunits (10-30% of the polymer), which can also be oxidized without mediators, have received considerably less attention. Consequently, it remains unclear to what extent the presence of a mediator influences the reactions of the phenolic subunits of lignin. To get more insight in this, UHPLC-MS was used to study the reactions of a phenolic lignin dimer (GBG), initiated by a laccase from Trametes versicolor , alone or in combination with the mediators HBT and ABTS. The role of HBT was negligible, as its oxidation by laccase occurred slowly in comparison to that of GBG. Laccase and laccase/HBT oxidized GBG at a comparable rate, resulting in extensive polymerization of GBG. In contrast, laccase/ABTS converted GBG at a higher rate, as GBG was oxidized both directly by laccase but also by ABTS radical cations, which were rapidly formed by laccase. The laccase/ABTS system resulted in Cα oxidation of GBG and coupling of ABTS to GBG, rather than polymerization of GBG. Based on these results, we propose reaction pathways of phenolic lignin model compounds with laccase/HBT and laccase/ABTS.

Protective effect of aqueous extract from Spirulina platensis against cell death induced by free radicals.

PubMed

Chu, Wan-Loy; Lim, Yen-Wei; Radhakrishnan, Ammu Kutty; Lim, Phaik-Eem

2010-09-21

Spirulina is a commercial alga well known to contain various antioxidants, especially phycocyanin. Apart from being sold as a nutraceutical, Spirulina is incorporated as a functional ingredient in food products and beverages. Most of the previous reports on antioxidant activity of Spirulina were based on chemical rather than cell-based assays. The primary objective of this study was to assess the antioxidant activity of aqueous extract from Spirulina based on its protective effect against cell death induced by free radicals. The antioxidant activity of the cold water extract from food-grade Spirulina platensis was assessed using both chemical and cell-based assays. In the cell-based assay, mouse fibroblast cells (3T3) cells were incubated for 1 h in medium containing aqueous extract of Spirulina or vitamin C (positive control) at 25, 125 and 250 μg/mL before the addition of 50 μM 1,1-diphenyl-2-picrylhydrazyl (DPPH) or 3-ethylbenzothiazoline-6-sulfonic acid (ABTS). The cells were incubated for another 24 h before being assessed for cell death due to apoptosis using the Cell Death Detection ELISA Kit. Spectrophotometric assays based on DPPH and ABTS were also used to assess the antioxidant activity of the extract compared to vitamin C and vitamin E (positive controls). Spirulina extract did not cause cytotoxic effect on 3T3 cells within the range of concentrations tested (0 - 250 μg/mL). The extract reduced significantly (p < 0.05) apoptotic cell death due to DPPH and ABTS by 4 to 5-fold although the activity was less than vitamin C. Based on the DPPH assay, the radical scavenging activity of the extract was higher than phycocyanin and was at least 50% of vitamin C and vitamin E. Based on the ABTS assay, the antioxidant activity of the extract at 50 μmug/mL was as good as vitamin C and vitamin E. The results showed that aqueous extract of Spirulina has a protective effect against apoptotic cell death due to free radicals. The potential application of incorporating Spirulina into food products and beverages to enhance their antioxidant capacity is worth exploring.

Antioxidant activity of a new aromatic geranyl derivative of the resinous exudates from Heliotropium glutinosum Phil.

PubMed

Modak, Brenda; Rojas, Macarena; Torres, René; Rodilla, Jesús; Luebert, Federico

2007-05-21

Heliotropium glutinosum Phil. (Heliotropiceae) is a resinous bush that grows at a height of 2000 m in Chañaral, Chile. From the resinous exudates of Heliotropium glutinosum Phil. a new aromatic geranyl derivative: 4-methoxy-3-[(2)-7'-methyl-3'-hydroxymethyl-2',6'-octadienyl] phenol (1) and three flavonoids: 5,3'-dihydroxy-7,4'-dimethoxyflavanone (2), 5,4'-dihydroxy-7-methoxyflavanone (3) and 4'-acetyl-5-hydroxy-7-methoxyflavanone (4) were isolated and their structures were determined. Their antioxidant activity were evaluated using the bleaching of ABTS and DPPH derived cation radical methods and expressed in terms of FRE (fast reacting equivalents) and TRE (total reacting equivalents), where FRE is a good measure of the quick protection of a given compound against oxidants and TRE measures the degree of long-term protection of the antioxidant, or how effective it is against a strong oxidative stress.

Mechanism of free radical generation in platelets and primary hepatocytes: A novel electron spin resonance study.

PubMed

Wang, Chiun-Lang; Yang, Po-Sheng; Tsao, Jeng-Ting; Jayakumar, Thanasekaran; Wang, Meng-Jiy; Sheu, Joen-Rong; Chou, Duen-Suey

2018-01-01

Oxygen free radicals have been implicated in the pathogenesis of toxic liver injury and are thought to be involved in cardiac dysfunction in the cirrhotic heart. Therefore, direct evidence for the electron spin resonance (ESR) detection of how D‑galactosamine (GalN), an established experimental hepatotoxic substance, induced free radicals formation in platelets and primary hepatocytes is presented in the present study. ESR results demonstrated that GalN induced hydroxyl radicals (OH•) in a resting human platelet suspension; however, radicals were not produced in a cell free Fenton reaction system. The GalN‑induced OH• formation was significantly inhibited by the cyclooxygenase (COX) inhibitor indomethasin, though it was not affected by the lipoxygenase (LOX) or cytochrome P450 inhibitors, AA861 and 1‑aminobenzotriazole (ABT), in platelets. In addition, the present study demonstrated that baicalein induced semiquinone free radicals in platelets, which were significantly reduced by the COX inhibitor without affecting the formed OH•. In the mouse primary hepatocytes, the formation of arachidonic acid (AA) induced carbon‑centered radicals that were concentration dependently enhanced by GalN. These radicals were inhibited by AA861, though not affected by indomethasin or ABT. In addition, GalN did not induce platelet aggregation prior to or following collagen pretreatment in human platelets. The results of the present study indicated that GalN and baicalein may induce OH• by COX and LOX in human platelets. GalN also potentiated AA induced carbon‑centered radicals in hepatocytes via cytochrome P450. The present study presented the role of free radicals in the pathophysiological association between platelets and hepatocytes.

Optimization of Supercritical Fluid Extraction of Total Alkaloids, Peimisine, Peimine and Peiminine from the Bulb of Fritillaria thunbergii Miq, and Evaluation of Antioxidant Activities of the Extracts

PubMed Central

Ruan, Xiao; Yang, Li; Cui, Wen-Xia; Zhang, Men-Xing; Li, Zhao-Hui; Liu, Ben; Wang, Qiang

2016-01-01

Supercritical fluid extraction (SFE) was used to extract total alkaloids, peimisine, peimine and peiminine from the bulb of Fritillaria thunbergii Miq. The antioxidant capacity of the extracts was evaluated by DPPH radical scavenging activity (DPPH-RSA), ABTS radical scavenging activity (ABTS-RSA) and ferric reducing capacity (FRAP) assay. A central composite design (CCD) with four variables and five levels was employed for optimization of process parameters, and response surface plots were constructed in accordance with a second order polynomial model. Under optimal conditions of 3.0 h, 60.4 °C, 26.5 MPa and 89.3% ethanol, the highest yields were predicted to be 3.8 mg/g for total alkaloids, 0.5 mg/g for peimisine, 1.3 mg/g for peimine and 1.3 mg/g for peiminine, and the antioxidant capacity of extracts displayed EC50, DPPH value of 5.5 mg/mL, EC50, ABTS value of 0.3 mg/mL and FRAP value of 118.2 mg ascorbic acid equivalent (AAE)/100 g. PMID:28773648

Isolation and characterisation of in vitro and cellular free radical scavenging peptides from corn peptide fractions.

PubMed

Wang, Liying; Ding, Long; Wang, Ying; Zhang, Yan; Liu, Jingbo

2015-02-16

Corn gluten meal, a corn processing industry by-product, is a good source for the preparation of bioactive peptides due to its special amino acid composition. In the present study, the in vitro and cellular free radical scavenging activities of corn peptide fractions (CPFs) were investigated. Results indicated that CPF1 (molecular weight less than 1 kDa) and CPF2 (molecular weight between 1 and 3 kDa) exhibited good hydroxyl radical, superoxide anion radical and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonicacid) diammonium salt (ABTS) radical scavenging activity and oxygen radical absorbance capacity (ORAC). Meanwhile, the in vitro radical scavenging activity of CPF1 was slightly higher than that of CPF2. Both CPF1 and CPF2 also exhibited significant cytoprotective effects and intracellular reactive oxygen species scavenging activity in Caco-2 cells exposed to hydrogen peroxide (H2O2). The amino acid composition analysis revealed that the CPF were rich in hydrophobic amino acids, which comprised of more than 45% of total amino acids. An antioxidant peptide sequence of Tyr-Phe-Cys-Leu-Thr (YFCLT) was identified from CPF1 using matrix-assisted laser desorption/ionization time-of-flight/time-of-flight mass spectrometry (MALDI TOF/TOF MS). The YFCLT exhibited excellent ABTS radical scavenging activity with a 50% effective concentration (EC50) value of 37.63 µM, which was much lower than that of Trolox. In conclusion, corn gluten meal might be a good source to prepare antioxidant peptides.

An exploratory study on the peroxyl-radical-scavenging activity of 2,6-dimethyl-5-hepten-2-ol and its heterocyclic analogues

NASA Astrophysics Data System (ADS)

Stobiecka, Agnieszka; Sikora, Magdalena; Bonikowski, Radosław; Kula, Józef

2016-03-01

The structural properties and radical scavenging activity of 2,6-dimethyl-5-hepten-2-ol (1) and its new heterocyclic analogues, i.e. 2-methyl-4-(5-methylfuran-2-yl)-butan-2-ol (2) and 2-methyl-4-(5-methylthiophen-2-yl)-butan-2-ol (3) and have been studied by using the experimental and theoretical methods for the first time. Activity of title compounds against the peroxyl radical was determined by using standard fluorimetric test, i.e. the Oxygen Radical Absorbance Capacity assay (ORACFL). Furthermore, the electron-donating ability of odorants has been evaluated by using colorimetric ABTS assay. According to the experimental results obtained from the ORACFL test 2,6-dimethyl-5-hepten-2-ol was characterized by the highest activity in comparison with the novel counterparts. Nevertheless, all investigated compounds exhibited pronounced anti-peroxyl radical activity comparable to that exerted by the one of the most prominent antioxidant among the monoterpene alcohols, i.e. by linalool. On the other hand, the title compounds exerted relatively low capacity to quench the radical cation of ABTS. Theoretical calculations based on the Density Functional Theory (DFT) method with the hybrid functional B3LYP were carried out in order to investigate selected structural and electronic properties including the geometrical parameters as well as the energy of frontier molecular orbitals of parent molecules and the resulting radicals. Furthermore, the possible mechanism of peroxyl-radical-scavenging has been determined by using the thermodynamic descriptors such as the bond dissociation enthalpies (BDEs) and ionization potentials (IPs). These theoretical data pointed out the relevance of HAT mechanism in the peroxyl-radical-scavenging exhibited by 2,6-dimethyl-5-hepten-2-ol and its new heterocyclic analogues in polar and non-polar medium.

Sequestering ability of butylated hydroxytoluene, propyl gallate, resveratrol, and vitamins C and E against ABTS, DPPH, and hydroxyl free radicals in chemical and biological systems.

PubMed

Soares, Daniele G; Andreazza, Ana C; Salvador, Mirian

2003-02-12

The antioxidant capacity of butylated hydroxytoluene (BHT; 2,6-di-tert-butyl-p-cresol), propyl gallate (3,4,5-trihydroxybenzoic acid n-propyl ester), resveratrol (trans-3,4',5-trihydroxystilbene), and vitamins C (l-ascorbic acid) and E [(+)-alpha-tocopherol] was studied in chemical and biological systems. The chemical assays evaluated the capacity of these antioxidants to sequester 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS.) and 1,1 diphenyl-2-picrylhydrazyl (DPPH.). A new colorimetric method to determine hydroxyl radical scavenging is also described. The biological tests use the eucaryotic cells of Saccharomyces cerevisiae treated with the antioxidants in the presence of the stressing agents apomorphine, hydrogen peroxide, and paraquat dichloride (methylviologen; 1,1'-dimethyl-4,4'-bipyridinium dichloride). The results in chemical systems showed that all of the antioxidants were able to significantly inhibit the oxidation of beta-carotene by hydroxyl free radicals. The assays in yeast showed that the antioxidant activity of the tested compounds depended on the stressing agent used and the mechanism of action of the antioxidant.

Antimicrobial and antioxidant activities of Flammulina velutipes polysaccharides and polysaccharide-iron(III) complex [corrected].

PubMed

Dong, Ya-Ru; Cheng, Shu-Jie; Qi, Guo-Hong; Yang, Zhi-Ping; Yin, Shi-Yu; Chen, Gui-Tang

2017-04-01

FVP is polysacchrides obtained from Flammulina velutipes. A polysacchride named FVP2 was isolated from FVP by DEAE cellulose-52 chromatography and Sephadex G-100 size-exclusion chromatography. FVP-Fe and FVP2-Fe were synthesized by neutralization of FeCl 3 carbohydrate solution. The antibacterial and antifungal activities of FVP, FVP2, FVP-Fe, FVP2-Fe were investigated and their antioxidant effects on hydroxyl, 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion, 2,2'-azobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, reducing power, inhibition of malondialdehyde (MDA) were assessed in vitro. The results suggested that FVP-Fe and FVP2-Fe significantly suppressed the growth of bacteria Staphylococcus aureus, Escherichia coli, and Bacillus subtilis, and have relatively strong antioxidant activity to scavenge superoxide anion radical. In addition, FVP exhibited strong antioxidant activity to eliminate hydroxyl, DPPH, ABTS radicals, had high reducing power and inhibited the MDA production of health mice liver homogenate induced by auto-oxidation and Fe 2+ -H 2 O 2 system. Copyright © 2016 Elsevier Ltd. All rights reserved.

Biological activity of clovers - free radical scavenging ability and antioxidant action of six Trifolium species.

PubMed

Kolodziejczyk-Czepas, Joanna; Nowak, Pawel; Kowalska, Iwona; Stochmal, Anna

2014-10-01

Clovers were chosen on the basis of traditional medicine recommendations, agricultural value, or available information on their promising chemical profiles. This study evaluates and compares free radical scavenging and antioxidant properties of six clover species: Trifolium alexandrinum L. (Leguminosae), Trifolium fragiferum L., Trifolium hybridum L., Trifolium incarnatum L., Trifolium resupinatum var. majus Boiss., and Trifolium resupinatum var. resupinatum L. Free radical scavenging activity of the extracts (1.5-50 µg/ml) was estimated by reduction of 1,1-diphenyl-2-picrylhydrazyl (DPPH(•)) and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic) acid (ABTS(•)) radicals. The Trifolium extract effects on total antioxidant capacity of blood plasma were determined by the reduction of ABTS(•+) and DPPH(•) radicals, as well as with the use of the ferric reducing ability of plasma (FRAP) assay. The UPLC analysis of chemical profiles of the examined extracts showed the presence of three or four groups of phenolic substances, including phenolic acids, clovamides, isoflavones, and other flavonoids. The measurements of free radical scavenging and ferric reducing ability of the examined clover extracts revealed the strongest effect for T. alexandrinum. Furthermore, antioxidant activity assays in human plasma have shown protective effects of all extracts against peroxynitrite-induced reduction of total antioxidant capacity. Trifolium plants may be a rich source of bioactive substances with antioxidant properties. The examined extracts displayed free radical scavenging action and partly protected blood plasma against peroxynitrite-induced oxidative stress; however, the beneficial effects of T. alexandrinum and T. incarnatum seem to be slightly higher.

Antioxidant capacity and radical scavenging effect of polyphenol rich Mallotus philippenensis fruit extract on human erythrocytes: an in vitro study.

PubMed

Gangwar, Mayank; Gautam, Manish Kumar; Sharma, Amit Kumar; Tripathi, Yamini B; Goel, R K; Nath, Gopal

2014-01-01

Mallotus philippinensis is an important source of molecules with strong antioxidant activity widely used medicinal plant. Previous studies have highlighted their anticestodal, antibacterial, wound healing activities, and so forth. So, present investigation was designed to evaluate the total antioxidant activity and radical scavenging effect of 50% ethanol fruit glandular hair extract (MPE) and its role on Human Erythrocytes. MPE was tested for phytochemical test followed by its HPLC analysis. Standard antioxidant assays like DPPH, ABTS, hydroxyl, superoxide radical, nitric oxide, and lipid peroxidation assay were determined along with total phenolic and flavonoids content. Results showed that MPE contains the presence of various phytochemicals, with high total phenolic and flavonoid content. HPLC analysis showed the presence of rottlerin, a polyphenolic compound in a very rich quantity. MPE exhibits significant strong scavenging activity on DPPH and ABTS assay. Reducing power showed dose dependent increase in concentration absorption compared to standard, Quercetin. Superoxide, hydroxyl radical, lipid peroxidation, nitric oxide assay showed a comparable scavenging activity compared to its standard. Our finding further provides evidence that Mallotus fruit extract is a potential natural source of antioxidants which have a protective role on human Erythrocytes exhibiting minimum hemolytic activity and this justified its uses in folklore medicines.

Antioxidant Capacity and Radical Scavenging Effect of Polyphenol Rich Mallotus philippenensis Fruit Extract on Human Erythrocytes: An In Vitro Study

PubMed Central

Gautam, Manish Kumar; Sharma, Amit Kumar; Tripathi, Yamini B.; Goel, R. K.; Nath, Gopal

2014-01-01

Mallotus philippinensis is an important source of molecules with strong antioxidant activity widely used medicinal plant. Previous studies have highlighted their anticestodal, antibacterial, wound healing activities, and so forth. So, present investigation was designed to evaluate the total antioxidant activity and radical scavenging effect of 50% ethanol fruit glandular hair extract (MPE) and its role on Human Erythrocytes. MPE was tested for phytochemical test followed by its HPLC analysis. Standard antioxidant assays like DPPH, ABTS, hydroxyl, superoxide radical, nitric oxide, and lipid peroxidation assay were determined along with total phenolic and flavonoids content. Results showed that MPE contains the presence of various phytochemicals, with high total phenolic and flavonoid content. HPLC analysis showed the presence of rottlerin, a polyphenolic compound in a very rich quantity. MPE exhibits significant strong scavenging activity on DPPH and ABTS assay. Reducing power showed dose dependent increase in concentration absorption compared to standard, Quercetin. Superoxide, hydroxyl radical, lipid peroxidation, nitric oxide assay showed a comparable scavenging activity compared to its standard. Our finding further provides evidence that Mallotus fruit extract is a potential natural source of antioxidants which have a protective role on human Erythrocytes exhibiting minimum hemolytic activity and this justified its uses in folklore medicines. PMID:25525615

DNA and BSA damage inhibitory activities, and anti-acetylcholinesterase, anti-porcine α-amylase and antioxidant properties of Dolichos lablab beans.

PubMed

Habib, Hosam M; Theuri, Serah W; Kheadr, Ehab; Mohamed, Fedah E

2017-02-22

The underutilized Kenyan variety of Dolichos lablab bean seeds serve as a good source of natural antioxidants, which can probably be effective in reducing the risk of occurrence of several diseases. This study was undertaken for the first time to address the limited knowledge regarding the antioxidant activities of lablab beans. Moreover, their DNA damage inhibitory activity, bovine serum albumin (BSA) damage inhibitory activity, and the inhibition of acetylcholinesterase and porcine α-amylase were also investigated. The antioxidant capacity of Dolichos lablab bean seeds extracted with methanol, water or methanol/water combination was evaluated by the ferric-reducing antioxidant power (FRAP) assay, free radical-scavenging activity, 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide (NO) radical-scavenging assay, and 2,20-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Results reported in the present study indicate that water, methanol and water/methanol extracts of lablab bean flour exhibited good antioxidant activity by effectively scavenging various free radicals, such as DPPH, NO, and ABTS radicals. The extracts also exhibited protective effects against DNA and BSA damage and inhibitory effects on porcine α-amylase. Findings of this study suggest that extracts from the lablab bean flour would have potential application in food supplements, and pharmaceutical and cosmetic industries.

Characterisation of Pomegranate-Husk Polyphenols and Semi-Preparative Fractionation of Punicalagin.

PubMed

Aguilar-Zárate, Pedro; Wong-Paz, Jorge E; Michel, Mariela; Buenrostro-Figueroa, Juan; Díaz, Hugo R; Ascacio, Juan A; Contreras-Esquivel, Juan C; Gutiérrez-Sánchez, Gerardo; Aguilar, Cristóbal N

2017-09-01

Pomegranate-husk is the main by-product generated from the pomegranate industry. It is a potential source of compounds highly appreciated by different costumers. Punicalagin is the main compound present in pomegranate-husk. To characterise the pomegranate-husk total polyphenols by HPLC-ESI-MS and to establish a method for the recovery of punicalagin using a medium pressure liquid chromatography (MPLC) system. The characterisation of total pomegranate-husk polyphenols was carried out using liquid chromatography coupled to mass spectrometry. Thus, 200 mg of pomegranate-husk polyphenols were fractionated by MPLC. The isolated punicalagin was characterised by HPLC-MS and was tested as standard reagent for the measurement of its scavenging capacity reducing DPPH and ABTS radicals. Twenty peaks were identified by analytical HPLC-MS analysis from the pomegranate-husk polyphenols. The main compounds were the punicalagin anomers, punicalin and ellagic acid. The MPLC method allowed three fractions to be obtained. In fraction three 39.40 ± 8.06 mg of punicalagin anomers (purity > 97.9%) were recovered. The scavenging capacity of punicalagin showed an IC 50 of 109.53 and 151.50 μg/mL for DPPH and ABTS radicals, respectively. The MPLC system was an excellent tool for the separation of the main ellagitannins from pomegranate husk and for the isolation of punicalagin anomers. Fraction three was rich in high purity punicalagin anomers. The IC 50 was obtained for DPPH and ABTS radicals. Copyright © 2017 John Wiley & Sons, Ltd. Copyright © 2017 John Wiley & Sons, Ltd.

Spectroscopic studies on the antioxidant activity of p-coumaric acid

NASA Astrophysics Data System (ADS)

Kiliç, Ismail; Yeşiloğlu, Yeşim

2013-11-01

p-coumaric acid (4-hydroxycinnamic acid), a phenolic acid, is a hydroxyl derivative of cinnamic acid. It decreases low density lipoprotein (LDL) peroxidation and reduces the risk of stomach cancer. In vitro radical scavenging and antioxidant capacity of p-coumaric acid were clarified using different analytical methodologies such as total antioxidant activity determination by ferric thiocyanate, hydrogen peroxide scavenging, 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH) scavenging, 2,2‧-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging activity and superoxide anion radical scavenging, ferrous ions (Fe2+) chelating activity and ferric ions (Fe3+) reducing ability. p-Coumaric acid inhibited 71.2% lipid peroxidation of a linoleic acid emulsion at 45 μg/mL concentration. On the other hand, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), α-tocopherol and ascorbic acid displayed 66.8%, 69.8%, 64.5% and 59.7% inhibition on the peroxidation of linoleic acid emulsion at the same concentration, respectively. In addition, p-coumaric acid had an effective DPPHrad scavenging, ABTSrad + scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, ferric ions (Fe3+) reducing power and ferrous ions (Fe2+) chelating activities. Also, those various antioxidant activities were compared to BHA, BHT, α-tocopherol and ascorbic acid as references antioxidant compounds. These results suggested that p-coumaric acid can be used in the pharmacological and food industry because of these properties.

Silibinin phosphodiester glyco-conjugates: Synthesis, redox behaviour and biological investigations.

PubMed

Romanucci, Valeria; Agarwal, Chapla; Agarwal, Rajesh; Pannecouque, Christophe; Iuliano, Mauro; De Tommaso, Gaetano; Caruso, Tonino; Di Fabio, Giovanni; Zarrelli, Armando

2018-04-01

New silibinin phosphodiester glyco-conjugates were synthesized by efficient phosphoramidite chemistry and were fully characterized by 2D-NMR. A wide-ranging study focused on the determination of their pKa and E° values as well as on their radical scavenging activities by different assays (DPPH, ABTS + and HRSA) was conducted. The new glyco-conjugates are more water-soluble than silibinin, and their radical scavenging activities are higher than those of silibinin. The conjugation therefore improves both the water solubilities and antioxidant activities of the flavonolignan moieties. The serum stability was evaluated under physiological conditions, and the glyco-conjugates degraded with half-lives of 40-70 h, making them useful in pro-drug approaches. We started by treating androgen-dependent prostate cancer (PCa) LNCaP cells and then expanded our studies to androgen-independent PCa PC3 and DU145 cells. In most cases, the new derivatives significantly reduced both total and live cell numbers, albeit at different levels. Anti-HIV activities were evaluated and the glucosamine-phosphate silibinin derivative showed higher activity (IC 50  = 73 μM) than silibinin. Copyright © 2018 Elsevier Inc. All rights reserved.

Protective effect of aqueous extract from Spirulina platensis against cell death induced by free radicals

PubMed Central

2010-01-01

Background Spirulina is a commercial alga well known to contain various antioxidants, especially phycocyanin. Apart from being sold as a nutraceutical, Spirulina is incorporated as a functional ingredient in food products and beverages. Most of the previous reports on antioxidant activity of Spirulina were based on chemical rather than cell-based assays. The primary objective of this study was to assess the antioxidant activity of aqueous extract from Spirulina based on its protective effect against cell death induced by free radicals. Methods The antioxidant activity of the cold water extract from food-grade Spirulina platensis was assessed using both chemical and cell-based assays. In the cell-based assay, mouse fibroblast cells (3T3) cells were incubated for 1 h in medium containing aqueous extract of Spirulina or vitamin C (positive control) at 25, 125 and 250 μg/mL before the addition of 50 μM 1,1-diphenyl-2-picrylhydrazyl (DPPH) or 3-ethylbenzothiazoline-6-sulfonic acid (ABTS). The cells were incubated for another 24 h before being assessed for cell death due to apoptosis using the Cell Death Detection ELISA Kit. Spectrophotometric assays based on DPPH and ABTS were also used to assess the antioxidant activity of the extract compared to vitamin C and vitamin E (positive controls). Results Spirulina extract did not cause cytotoxic effect on 3T3 cells within the range of concentrations tested (0 - 250 μg/mL). The extract reduced significantly (p < 0.05) apoptotic cell death due to DPPH and ABTS by 4 to 5-fold although the activity was less than vitamin C. Based on the DPPH assay, the radical scavenging activity of the extract was higher than phycocyanin and was at least 50% of vitamin C and vitamin E. Based on the ABTS assay, the antioxidant activity of the extract at 50 μmug/mL was as good as vitamin C and vitamin E. Conclusions The results showed that aqueous extract of Spirulina has a protective effect against apoptotic cell death due to free radicals. The potential application of incorporating Spirulina into food products and beverages to enhance their antioxidant capacity is worth exploring. PMID:20858231

A novel automated direct measurement method for total antioxidant capacity using a new generation, more stable ABTS radical cation.

PubMed

Erel, Ozcan

2004-04-01

To develop a novel colorimetric and automated direct measurement method for total antioxidant capacity (TAC). A new generation, more stable, colored 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid radical cation (ABTS(*+)) was employed. The ABTS(*+) is decolorized by antioxidants according to their concentrations and antioxidant capacities. This change in color is measured as a change in absorbance at 660 nm. This process is applied to an automated analyzer and the assay is calibrated with Trolox. The novel assay is linear up to 6 mmol Trolox equivalent/l, its precision values are lower than 3%, and there is no interference from hemoglobin, bilirubin, EDTA, or citrate. The method developed is significantly correlated with the Randox- total antioxidant status (TAS) assay (r = 0.897, P < 0.0001; n = 91) and with the ferric reducing ability of plasma (FRAP) assay (r = 0.863, P < 0.0001; n = 110). Serum TAC level was lower in patients with major depression (1.69 +/- 0.11 mmol Trolox equivalent/l) than in healthy subjects (1.75 +/- 0.08 mmol Trolox equivalent/l, P = 0.041). This easy, stable, reliable, sensitive, inexpensive, and fully automated method described can be used to measure total antioxidant capacity.

Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.

PubMed

Kurt, Belma Zengin; Gazioglu, Isil; Basile, Livia; Sonmez, Fatih; Ginex, Tiziana; Kucukislamoglu, Mustafa; Guccione, Salvatore

2015-09-18

New benzofuranylthiazole derivatives containing the aryl-urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. The result showed that all the synthesized compounds exhibited inhibitory activity on both AChE and BuChE with 1-(4-(5-bromobenzofuran-2-yl)thiazol-2-yl)-3-(2-fluorophenyl)urea (e25, IC50 value of 3.85 μM) and 1-(4-iodophenyl)-3-(4-(5-nitrobenzofuran-2-yl)thiazol-2-yl)urea (e38, IC50 value of 2.03 μM) as the strongest inhibitors against AChE and BuChE, respectively. Compound e38 was 8.5-fold more potent than galanthamine. The selectivity index of e25 and e38 was 2.40 and 0.37 against AChE and BuChE, respectively. Compound e2, e4 and e11 (IC50 = 0.2, 0.5 and 1.13 μM, respectively) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 = 1.18 μM). Best poses of compounds e38 on BuChE and e25 on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and phenyl ring are anchored to the side chains of both enzymes by π-π(pi-pi) interactions. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Antioxidant activities of Lampaya medicinalis extracts and their main chemical constituents

PubMed Central

2014-01-01

Background Lampaya medicinalis Phil. (Verbenaceae) is a plant used by Aymara and Quechua ethnic groups from Northern Chile as folk medicine in the treatment and cure of various diseases. The aim of this study was to investigate the in vitro antioxidant activity, total phenols content, total flavonoids content, total antioxidant activity, reducing power, brine shrimp cytotoxicity and identify the principal chemical constituents. Methods The crude hydroethanolic extract (HEE) and its partitioned fraction: hexane (HF), dichloromethane (DF), ethyl acetate (EAF), n-butanol (BF) and soluble residual aqueous fraction (RWF) were evaluated for their antioxidant activity using different assays namely, DPPH, ABTS, FRAP, β-carotene bleaching assay. The content of total phenolics and total flavonoids were measured by Folin-Ciocalteau and by the AlCl3 colorimetric method, respectively. Reducing power was determined by phosphomolybdate and hexacyanoferrate (III) methods. Biotoxicity assays were performed on shrimps of Artemia salina. The EAF was fractionated using chromatographic methods. Results Considerable amount of phenolic and flavonoid contents were recorded in the hydroethanolic extract (HEE) and its derived fractions. Although HEE and all its derived fractions exhibited good antioxidant activities, the most distinguished radical scavenging potential was observed for ethyl acetate fraction (EAF). EAF showed the higher radical scavenging activity by DPPH (95%) and by ABTS (98%), antioxidant activity by FRAP (158.18 ± 5.79 mg equivalent Trolox/g fraction), β-carotene bleaching assay (86.8%), the highest total phenols content (101.26 ± 1.07 mg GAE/g fraction), the highest total flavonoids content (66.26 ± 3.31 μg quercetin/g fraction). The EAF extract showed an reducing power of 78% and 65% using the phosphomolybdate and hexacyanoferrate (III) assays, respectively. Four flavonoids, two p-hydroxyacetophenone derivatives and one iridoid were isolated from Lampaya medicinalis for the first time. Conclusion EtOAc soluble fraction (EAF) shows the strongest antioxidant activity, and it can be attributed to its high content in phenolic and flavonoid compounds. It can be concluded that L.medicinalis can be used as an effective natural source of antioxidant, as ethnomedicine and as a commercial basis for the development of nutraceuticals. PMID:25047047

Syzyguim guineense Extracts Show Antioxidant Activities and Beneficial Activities on Oxidative Stress Induced by Ferric Chloride in the Liver Homogenate

PubMed Central

Pieme, Constant Anatole; Ngoupayo, Joseph; Khou-Kouz Nkoulou, Claude Herve; Moukette Moukette, Bruno; Njinkio Nono, Borgia Legrand; Ama Moor, Vicky Jocelyne; Ze Minkande, Jacqueline; Yonkeu Ngogang, Jeanne

2014-01-01

The aim of this study was to determine the in vitro antioxidant activity, free radical scavenging property and the beneficial effects of extracts of various parts of Syzygium guineense in reducing oxidative stress damage in the liver. The effects of extracts on free radicals were determined on radicals DPPH, ABTS, NO and OH followed by the antioxidant properties using Ferric Reducing Antioxidant Power assay (FRAP) and hosphomolybdenum (PPMB). The phytochemical screening of these extracts was performed by determination of the phenolic content. The oxidative damage inhibition in the liver was determined by measuring malondialdehyde (MDA) as well as the activity of the antioxidant enzymes superoxide dismutase (SOD), catalase (CAT) and peroxidase. Overall, the bark extract of the ethanol/water or methanol showed the highest radical scavenging activities against DPPH, ABTS and OH radicals compared to the other extracts. This extract also contained the highest phenolic content implying the potential contribution of phenolic compounds towards the antioxidant activities. However, the methanol extract of the root demonstrated the highest protective effects of SOD and CAT against ferric chloride while the hydro-ethanol extract of the leaves exhibited the highest inhibitory effects on lipid peroxidation. These findings suggest that antioxidant properties of S. guineense extracts could be attributed to phenolic compounds revealed by phytochemical studies. Thus, the present results indicate clearly that the extracts of S. guineense possess antioxidant properties and could serve as free radical inhibitors or scavengers, acting possibly as primary antioxidants. The antioxidant properties of the bark extract may thus sustain its various biological activities. PMID:26785075

Influence of freezing down to 77.15 K on structure and antioxidant power of some proteins

NASA Astrophysics Data System (ADS)

Rozanova, S. L.; Narozhnyi, S. V.; Nardid, O. A.

2017-06-01

The purpose of the present work was to investigate influence of different freeze-thawing protocols on structure and antioxidant properties of isolated proteins. In our experiments we have studied human serum albumin, human hemoglobin and cytochrome C derived from equine heart frozen down to 77.15 K with 1-2 deg/min and 300 deg/min rate with following thawing on a water bath at 293.15 K. Native proteins were assumed as a control. Influence of freeze-thawing protocols on protein structure was investigated using spectrophotometric and fluorescent assays. Antioxidant activities of isolated proteins were estimated by their ability to reduce ABTS+ radical. It has been established that unfolding derived from freeze-thawing exposure leads to protein antioxidant activity increasing while decreasing of such an activity may be connected with macromolecule aggregation. Character of freeze-thawing influence on antioxidant activity of proteins depends on molecule structure peculiarities and freezing protocols.

Differential effects of ABT-510 and a CD36-binding peptide derived from the type 1 repeats of thrombospondin-1 on fatty acid uptake, nitric oxide signaling, and caspase activation in vascular cells.

PubMed

Isenberg, Jeff S; Yu, Christine; Roberts, David D

2008-02-15

ABT-510 is a potent mimetic of an anti-angiogenic sequence from the second type 1 repeat of thrombospondin-1. ABT-510 and the original d-Ile mimetic from which it was derived, GDGV(dI)TRIR, are similarly active for inhibiting vascular outgrowth in a B16 melanoma explant assay. Because GDGV(dI)TRIR and thrombospondin-1 modulate nitric oxide signaling by inhibiting the fatty translocase activity of CD36, we examined the ability ABT-510 to modulate fatty acid uptake into vascular cells and downstream nitric oxide/cGMP signaling. Remarkably, ABT-510 is less active than GDGV(dI)TRIR for inhibiting myristic acid uptake into both endothelial and vascular smooth muscle cells. Correspondingly, ABT-510 is less potent than GDGV(dI)TRIR for blocking a myristate-stimulated increase in cell adhesion to collagen and nitric oxide-driven accumulation of cGMP. ABT-510 at concentrations sufficient to inhibit CD36 fatty acid translocase activity synergizes with thrombin in aggregating platelets and blunts the activity of NO to delay aggregation, but again less than GDGV(dI)TRIR. In contrast, ABT-510 is more potent than GDGV(dI)TRIR for inducing caspase activation in vascular cells. Thus, we propose that ABT-510 is a drug with at least two mechanisms of action, and its potent anti-tumor activity may be in part independent of CD36 fatty acid translocase inhibition.

Differential Effects of ABT-510 and a CD36-binding Peptide Derived from the Type 1 Repeats of Thrombospondin-1 on Fatty Acid Uptake, Nitric Oxide Signaling, and Caspase Activation in Vascular Cells

PubMed Central

Isenberg, Jeff S.; Yu, Christine; Roberts, David D.

2008-01-01

ABT-510 is a potent mimetic of an anti-angiogenic sequence from the second type 1 repeat of thrombospondin-1. ABT-510 and the original d-Ile mimetic from which it was derived, GDGV(dI)TRIR, are similarly active for inhibiting vascular outgrowth in a B16 melanoma explant assay. Because GDGV(dI)TRIR and thrombospondin-1 modulate nitric oxide signaling by inhibiting the fatty translocase activity of CD36, we examined the ability ABT-510 to modulate fatty acid uptake into vascular cells and downstream nitric oxide/cGMP signaling. Remarkably, ABT-510 is less active than GDGV(dI)TRIR for inhibiting myristic acid uptake into both endothelial and vascular smooth muscle cells. Correspondingly, ABT-510 is less potent than GDGV(dI)TRIR for blocking a myristate-stimulated increase in cell adhesion to collagen and nitric oxide-driven accumulation of cGMP. ABT-510 at concentrations sufficient to inhibit CD36 fatty acid translocase activity synergizes with thrombin in aggregating platelets and blunts the activity of NO to delay aggregation, but again less than GDGV(dI)TRIR. In contrast, ABT-510 is more potent than GDGV(dI)TRIR for inducing caspase activation in vascular cells. Thus, we propose that ABT-510 is a drug with at least two mechanisms of action, and its potent anti-tumor activity may be in part independent of CD36 fatty acid translocase inhibition. PMID:18068687

Determination of the antioxidant activity and polyphenol contents of wild Lingzhi or Reishi medicinal mushroom, Ganoderma lucidum (W.Curt. Fr.) P. Karst. (higher Basidiomycetes) from central Himalayan hills of India.

PubMed

Mohsin, Mohammed; Negi, P; Ahmed, Z

2011-01-01

The antioxidant potential of wild strain of Lingzhi or Reishi medicinal mushroom Ganoderma lucidum from Central Himalayan Hills (2000 m MSL) was evaluated, and compared with its in vitro cultured mycelia grown on malt extract broth in the laboratory. Antioxidant activities of both wild and cultivated G. lucidum in terms of IC₅₀ (mg/ mL) were determined against different in vitro radical systems such as DPPH (1, 1-diphenyl-2-picrylhydrazyl), ABTS [2,2'-azinobis (3-ethylenebenzothiazoline-6-sulphonic acid)] and hydroxyl radicals, in addition to ferric reducing antioxidant power assay. Polyphenol contents were also determined, in order to assess their effects on the antioxidant activity of extracts. All the extracts showed significant antioxidant activity, and maximum scavenging was observed in the case of methanolic extracts of wild G. lucidum with minimum IC50 values 0.953 ± 0.040, 0.690 ± 0.014 and 3.295 ± 0.027 mg/mL, respectively, for DPPH, ABTS, and hydroxyl radicals. The efficacy of wild G. lucidum as a rich source of natural antioxidant was established for nutraceutical development.

Antioxidant and enzyme inhibitory activities of Plebeian herba (Salvia plebeia R. Br.) under different cultivation conditions.

PubMed

Chen, Lei; Kang, Young-Hwa

2014-03-12

An adaptation of cultural management to the specific cultural system, as well as crop demand, can further result in the improvement of the quality of horticultural products. Therefore, this study focused on the antioxidant and enzyme inhibitory activities of Plebeian herba (Salvia plebeia R. Br.) grown in hydroponics in comparison with those of the plant grown in soil. The antioxidant activities of Plebeian herba extract were measured as 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging abilities as well as the reducing power by decreasing nitric oxide (NO) and superoxide dismutase activity (SOD) in vitro. Interestingly, by comparison with hydroponics and traditional cultivation, Plebeian herba cultivated in nutrition-based soil improved inhibitory effect on free radicals of DPPH, ABTS, and NO and increased the contents of phenolics such as caffeic acid (1), luteolin-7-glucoside (2), homoplantaginin (3), hispidulin (4), and eupatorin. Free radical scavenging and SOD activity, as well as α-glucosidase inhibitory effect, were higher in Plebeian herba grown in nutrition-based soil than in plants grown in hydroponics and traditional condition.

Antibacterial and antioxidant activities of Vaccinium corymbosum L. leaf extract

PubMed Central

Pervin, Mehnaz; Hasnat, Md Abul; Lim, Beong Ou

2013-01-01

Objective To investigate antibacterial and antioxidant activity of the leaf extract of tropical medicinal herb and food plant Vaccinium corymbosum L. (V. corymbosum). Methods Free radical scavenging activity on DPPH, ABTS, and nitrites were used to analyse phenoic and flavonoid contents of leaf extract. Other focuses included the determination of antioxidant enzymatic activity (SOD, CAT and GPx), metal chelating activity, reduction power, lipid peroxidation inhibition and the prevention of oxidative DNA damage. Antibacterial activity was determined by using disc diffusion for seven strains of bacteria. Results Results found that V. corymbosum leaf extract had significant antibacterial activity. The tested extract displayed the highest activity (about 23.18 mm inhibition zone) against Salmonella typhymurium and the lowest antibacterial activity was observed against Enterococcus faecalis (about 14.08 mm inhibition zone) at 10 mg/ disc. The IC50 values for DPPH, ABTS and radical scavenging activity were 0.120, 0.049 and 1.160 mg/mL, respectively. V. corymbosum leaf extract also showed dose dependent reduction power, lipid peroxidation, DNA damage prevention and significant antioxidant enzymatic activity. Conclusions These findings demonstrate that leaf extract of V. corymbosum could be used as an alternative therapy for antibiotic-resistant bacteria and help prevent various free radical related diseases.

In vitro free radical scavenging activity of ethanolic extract of the whole plant of Evolvulus alsinoides (L.) L.

PubMed

Gomathi, Duraisamy; Ravikumar, Ganesan; Kalaiselvi, Manokaran; Vidya, Balasubramaniam; Uma, Chandrasekar

2015-06-01

To identify the free radical scavenging activity of ethanolic extract of Evolvulus alsinoides. The free radical scavenging activity was evaluated by in vitro methods like reducing power assay, total antioxidant activity, 2,2-diphenyl-1-picrylhydrazyl (DPPH) reduction, superoxide radical scavenging activity, 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS(+)) scavenging activity, hydroxyl radical scavenging assay, and nitric oxide radical scavenging assay, which were studied by using ascorbic acid as standard. The extract showed significant activities in all antioxidant assays compared with the reference antioxidant ascorbic acid. The total antioxidant activity as well as the reducing power was also found to increase in a dose-dependent manner. Evolvulus alsinoides may act as a chemopreventive agent, providing antioxidant properties and offering effective protection from free radicals.

In-vitro free radical scavenging activity of biosynthesized gold and silver nanoparticles using Prunus armeniaca (apricot) fruit extract

NASA Astrophysics Data System (ADS)

Dauthal, Preeti; Mukhopadhyay, Mausumi

2013-01-01

In-vitro free radical scavenging activity of biosynthesized gold (Au-NPs) and silver (Ag-NPs) nanoparticles was investigated in the present study. Natural precursor Prunus armeniaca (apricot) fruit extract was used as a reducing agent for the nanoparticle synthesis. The free radical scavenging activity of the nanoparticles were observed by modified 1,1'-diphynyl-2-picrylhydrazyl, DPPH and 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid), ABTS assay. The synthesized nanoparticles were characterized by UV-Visible spectroscopy, dynamic light scattering, transmission electron microscopy (TEM), X-ray diffraction (XRD), energy dispersive spectroscopy, and fourier transform infrared spectroscopy (FTIR). Appearance of optical absorption peak at 537 nm (2.20 keV) and 435 nm (3 keV) within 0.08 and 0.5 h of reaction time was confirmed the presence of metallic Au and Ag nanoclusters, respectively. Nearly spherical nanoparticles with majority of particle below 20 nm (TEM) for both Au-NPs and Ag-NPs were synthesized. XRD pattern confirmed the existence of pure nanocrystalline Au-NPs while few additional peaks in the vicinity of fcc silver-speculated crystallization of metalloproteins of fruit extract on the surface of the Ag-NPs and vice versa. FTIR spectra was supported the role of amino acids of protein/enzymes of fruit extract for synthesis and stabilization of nanoparticles. Dose-dependent scavenging activity was observed for Au-NPs and Ag-NPs in both DPPH and ABTS in-vitro assay. 50 % scavenging activity for DPPH were 11.27 and 16.18 mg and for ABTS 3.40 and 7.12 mg with Au-NPs and Ag-NPs, respectively.

Fluctuations in Phenolic Content and Antioxidant Capacity of Green Vegetable Juices during Refrigerated Storage.

PubMed

Kim, Seong Yeong

2015-09-01

Shinseoncho and kale were made into green vegetable juices by building block [shinsenocho branch (SB), shinsenocho leaf (SL), kale branch (KB), and kale leaf (KL)]. Fluctuations in their phenolic contents and antioxidant capacities were analyzed during refrigerated storage at 4°C for 28 days. Total polyphenolic contents of leaf parts showed a decreasing tendency after 4 days (SL) or 7 days (KL), whereas branch parts showed fluctuating values during the entire storage period. The 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging capacity was rapidly decreased in SB and in SL at 28 days (P<0.001), whereas KL showed a slightly increasing tendency after 14 days. For the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity, SL showed a sharp fall at 28 days (P<0.001), and KL showed a decreasing tendency after 14 days (P<0.001). SB showed a steady decrease during the entire storage period and KB indicated a nearly zero (0.97%) at 28 days. Pearson's coefficients for the correlation between antioxidant capacities measured by the ABTS and DPPH assays, and the total polyphenolic contents were determined. The results showed that the ABTS assay (r=0.934, P<0.001) was more strongly positively correlated with the total phenolic contents than the DPPH assay (r=0.630, P<0.001). In conclusion, when considering all building blocks, green vegetable juices, including kale and shinseoncho may have kept antioxidant capacities for up to 14 days under refrigeration, and the ABTS assay better reflects a positive correlation with the total phenolic contents when compared to the DPPH assay.

Comparative study of the antioxidant capacity and polyphenol content of Douro wines by chemical and electrochemical methods.

PubMed

Rebelo, M J; Rego, R; Ferreira, M; Oliveira, M C

2013-11-01

A comparative study of the antioxidant capacity and polyphenols content of Douro wines by chemical (ABTS and Folin-Ciocalteau) and electrochemical methods (cyclic voltammetry and differential pulse voltammetry) was performed. A non-linear correlation between cyclic voltammetric results and ABTS or Folin-Ciocalteau data was obtained if all types of wines (white, muscatel, ruby, tawny and red wines) are grouped together in the same correlation plot. In contrast, a very good linear correlation was observed between the electrochemical antioxidant capacity determined by differential pulse voltammetry and the radical scavenging activity of ABTS. It was also found that the antioxidant capacity of wines evaluated by the electrochemical methods (expressed as gallic acid equivalents) depend on background electrolyte of the gallic acid standards, type of electrochemical signal (current or charge) and electrochemical technique. Copyright © 2013 Elsevier Ltd. All rights reserved.

Antigenotoxic and free radical scavenging activities of extracts from Moricandia arvensis.

PubMed

Skandrani, I; Sghaier, M Ben; Neffati, A; Boubaker, J; Bouhlel, I; Kilani, S; Mahmoud, A; Ghedira, K; Chekir-Ghedira, L

2007-01-01

This study evaluates genotoxic and antigenotoxic effects of extracts from leaves of Moricandia arvensis, which are used in traditional cooking and medicines. Extracts showed no genotoxicity when tested with the SOS Chromotest using E. coli PQ37 and PQ35 strains, except for the total oligomers flavonoids enriched extract. Petroleum ether and methanol extracts are the most active in reducing nitrofurantoin genotoxicity, whereas methanol and total oligomers flavonoids enriched extracts showed the most important inhibitory effect of H2O2 genotoxicity. In addition, these two extracts showed important free radical scavenging activity toward the DPPH. radical, whereas the chloroform extract exhibited the highest value of TEAC against ABTS+. radical.

Comparison of antioxidant capacity of cow and ewe milk kefirs.

PubMed

Yilmaz-Ersan, Lutfiye; Ozcan, Tulay; Akpinar-Bayizit, Arzu; Sahin, Saliha

2018-05-01

This research aimed to evaluate the effects of using either grain or commercial starter culture on the antioxidative capacity of cow and ewe milk kefirs. The antioxidant capacity of kefir samples during fermentation and 21 d of storage was assessed by using 3 assays: 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical cation decolorization; 2,2-diphenyl-1-picrylhydrazyl (DPPH • ) radical scavenging activity assay; and Fe +3 -reducing power (ferric reducing antioxidant power assay, FRAP). Vitamin E and β-carotene contents were also quantified. All kefir samples exhibited varying values for DPPH, ABTS, and FRAP assays depending on the starter culture and milk type. Vitamin E and β-carotene contents were similar in all kefir samples during storage. The results of this study suggest that milk type (cow or ewe) and culture type (kefir grains or commercial starter) were the significant parameters for the antioxidative activity of kefir. Copyright © 2018 American Dairy Science Association. Published by Elsevier Inc. All rights reserved.

Comparative study of antioxidant properties and total phenolic content of 30 plant extracts of industrial interest using DPPH, ABTS, FRAP, SOD, and ORAC assays.

PubMed

Dudonné, Stéphanie; Vitrac, Xavier; Coutière, Philippe; Woillez, Marion; Mérillon, Jean-Michel

2009-03-11

Aqueous extracts of 30 plants were investigated for their antioxidant properties using DPPH and ABTS radical scavenging capacity assay, oxygen radical absorbance capacity (ORAC) assay, superoxide dismutase (SOD) assay, and ferric reducing antioxidant potential (FRAP) assay. Total phenolic content was also determined by the Folin-Ciocalteu method. Antioxidant properties and total phenolic content differed significantly among selected plants. It was found that oak (Quercus robur), pine (Pinus maritima), and cinnamon (Cinnamomum zeylanicum) aqueous extracts possessed the highest antioxidant capacities in most of the methods used, and thus could be potential rich sources of natural antioxidants. These extracts presented the highest phenolic content (300-400 mg GAE/g). Mate (Ilex paraguariensis) and clove (Eugenia caryophyllus clovis) aqueous extracts also showed strong antioxidant properties and a high phenolic content (about 200 mg GAE/g). A significant relationship between antioxidant capacity and total phenolic content was found, indicating that phenolic compounds are the major contributors to the antioxidant properties of these plants.

Construction of a Cordyceps sinensis exopolysaccharide-conjugated selenium nanoparticles and enhancement of their antioxidant activities.

PubMed

Xiao, Yidong; Huang, Qilin; Zheng, Zhaomin; Guan, Han; Liu, Shiyu

2017-06-01

A Cordyceps sinensis exopolysaccharide (EPS)-conjugated selenium nanoparticles (SeNPs) were successfully constructed through the reduction of SeO 3 2- . The EPS-SeNPs were characterized in terms of formation, morphology, size, Se distribution and phase by UV-vis, FT-IR, transmission electron microscopy (TEM), dynamic light scattering (DLS), energy dispersive X-ray (EDX) and wide angle X-ray diffraction (WAXD) measurements. Results revealed that the SeNPs conjugated to EPS were amorphous and could be well dispersed at a size range of 80-125nm. The interactions between the OH groups of EPS and SeNPs substituted for intermolecular interaction in native EPS to form new CO⋯Se bonds, resulting in good dispersion of SeNPs in the EPS matrix. Besides, the EPS-SeNPs at different Se/P ratios exhibited significant scavenging ability on superoxide anion radical (O 2 - ) and ABTS radical cation (ABTS + ) when compared to pure EPS, indicating that the conjugated SeNPs reinforced antioxidant effect of EPS. This work not only provides a simple and efficient way to construct well-dispersed SeNPs in aqueous system, and demonstrates the vital role of the EPS as a biopolymer template for dispersion, stabilization and size control of SeNPs, but also finds the EPS-SeNPs can potentially serve as a good antioxidant towards O 2 - and ABTS + . Copyright © 2017 Elsevier B.V. All rights reserved.

Optimization of Penicillium aurantiogriseum protease immobilization on magnetic nanoparticles for antioxidant peptides' obtainment.

PubMed

Duarte Neto, José Manoel Wanderley; Maciel, Jackeline da Costa; Campos, Júlia Furtado; Carvalho Junior, Luiz Bezerra de; Marques, Daniela Araújo Viana; Lima, Carolina de Albuquerque; Porto, Ana Lúcia Figueiredo

2017-08-09

This work reports an optimization of protease from Penicillium aurantiogriseum immobilization on polyaniline-coated magnetic nanoparticles for antioxidant peptides' obtainment derived from bovine casein. Immobilization process was optimized using a full two-level factorial design (2 4 ) followed by a response surface methodology. Using the derivative, casein was hydrolyzed uncovering its peptides that were sequenced and had antioxidant properties tested through (2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) (ABTS) radical scavenging and hydrogen peroxide scavenging assays. Optimal conditions for immobilization were 2 hr of immobilization, offered protein amount of 200 µg/mL, immobilization pH of 6.3 and 7.3 hr of activation. Derivative keeps over 74% of its original activity after reused five times. Free and immobilized enzyme casein hydrolysates presented similar peptide mass fingerprints, and prevalent peptides could be sequenced. Hydrolysates presented more than 2.5× higher ROS scavenging activity than nonhydrolyzed casein, which validates the immobilized protease capacity to develop casein-derived natural ingredients with potential for functional foods.

Free radical-scavenging activities of Crataegus monogyna extracts.

PubMed

Bernatoniene, Jurga; Masteikova, Rūta; Majiene, Daiva; Savickas, Arūnas; Kevelaitis, Egidijus; Bernatoniene, Rūta; Dvorácková, Katerina; Civinskiene, Genuvaite; Lekas, Raimundas; Vitkevicius, Konradas; Peciūra, Rimantas

2008-01-01

The aim of this study was to investigate antiradical activity of aqueous and ethanolic hawthorn fruit extracts, their flavonoids, and flavonoid combinations. Total amount of phenolic compounds and the constituents of flavonoids were determined using a high-performance liquid chromatography. The antioxidant activity of Crataegus monogyna extracts and flavonoids (chlorogenic acid, hyperoside, rutin, quercetin, vitexin-2O-rhamnoside, epicatechin, catechin, and procyanidin B(2)) quantitatively was determined using the method of spectrophotometry (diphenyl-1-picrylhydrazyl (DPPH.) radical scavenging assay and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid)(ABTS.+) radical cation decolorization assay). The level of tyrosine nitration inhibition was determined using a high-performance liquid chromatography. Ethanolic hawthorn fruit extract contained 182+/-4 mg/100 mL phenolic compounds, i.e. threefold more, as compared to aqueous extract. The antioxidant activity according to DPPH. reduction in the ethanolic extracts was higher 2.3 times (P<0.05). The ABTS.+ technique showed that the effect of ethanolic extracts was by 2.5 times stronger than that of aqueous extracts. Tyrosine nitration inhibition test showed that the effect of ethanolic extracts was by 1.4 times stronger than that of aqueous extracts. The investigation of the antiradical activity of the active constituents in aqueous and ethanolic extracts revealed that epicatechin and catechin contribute to radical-scavenging properties more than other components. Procyanidin B(2) only insignificantly influenced the antiradical activity of the extracts. Both aqueous and ethanolic hawthorn extracts had antiradical activity, but ethanolic extract had stronger free radical-scavenging properties, compared to the aqueous extract. The antioxidant activity of the studied preparations was mostly conditioned by epicatechin and catechin. The individual constituents of both extracts had weaker free radical-scavenging properties than the combination of these substances did.

Antioxidant properties of Aller-7, a novel polyherbal formulation for allergic rhinitis.

PubMed

D'Souza, P; Amit, A; Saxena, V S; Bagchi, D; Bagchi, M; Stohs, S J

2004-01-01

Allergic rhinitis, a frequently occurring immunological disorder affecting men, women and children worldwide, is a state of hypersensitivity that occurs when the body overreacts to a substance such as pollen, mold, mites or dust. Allergic rhinitis exerts inflammatory response and irritation of the nasal mucosal membranes leading to sneezing; stuffy/runny nose; nasal congestion; and itchy, watery and swollen eyes. A novel, safe polyherbal formulation (Aller-7/NR-A2) has been developed for the treatment of allergic rhinitis using a unique combination of extracts from seven medicinal plants including Phyllanthus emblica, Terminalia chebula, Terminalia bellerica, Albizia lebbeck, Piper nigrum, Zingiber officinale and Piper longum. In this study, the antioxidant efficacy of Aller-7 was investigated by various assays including hydroxyl radical scavenging assay, superoxide anion scavenging assay, 1,1-diphenyl-2-picryl hydrazyl (DPPH) and 2,2-azinobis-ethyl-benzothiozoline-sulphonic acid diammonium salt (ABTS) radical scavenging assays. The protective effect of Aller-7 on free radical-induced lysis of red blood cells and inhibition of nitric oxide release by Aller-7 in lipopolysaccharide-stimulated murine macrophages were determined. Aller-7 exhibited concentration-dependent scavenging activities toward biochemically generated hydroxyl radicals (IC50 741.73 microg/ml); superoxide anion (IC50 24.65 microg/ml by phenazine methosulfate-nicotinamide adenine dinucleotide [PMS-NADH] assay and IC50 4.27 microg/ml by riboflavin/nitroblue tetrazolium [NBT] light assay), nitric oxide (IC50 16.34 microg/ml); 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical (IC50 5.62 microg/ml); and 2,2-azinobis-ethyl-benzothiozoline-sulphonic acid diammonium salt (ABTS) radical (IC50 7.35 microg/ml). Aller-7 inhibited free radical-induced hemolysis in the concentration range of 20-80 microg/ml. Aller-7 also significantly inhibited nitric oxide release from lipopolysaccharide-stimulated murine macrophages. These results demonstrate that Aller-7 is a potent scavenger of free radicals and that it may serve.

Free radical scavenging actions of three Trifolium species in the protection of blood plasma antioxidant capacity in vitro.

PubMed

Kolodziejczyk-Czepas, Joanna; Nowak, Pawel; Moniuszko-Szajwaj, Barbara; Kowalska, Iwona; Stochmal, Anna

2015-01-01

Three clover [Trifolium L. (Leguminosae)] species were selected on the basis of data from traditional medicine, phytochemical profiles, and agricultural significance. The in vitro evaluations of free radical scavenging properties, ferric reducing abilities, and antioxidant effects of extracts from T. pratense L. (crude extract and phenolic fraction), T. pallidum L., and T. scabrum L. (phenolic fractions) were performed. Activities of the Trifolium extracts were determined at their final concentrations of 1.5-50 µg/ml. Free radical scavenging properties of methanol extract solutions were estimated by the reduction of DPPH(•) and ABTS(•) radicals. Measurements of the total antioxidant capacity (TAC) were carried out to assess the antioxidant activities of the extracts in human blood plasma under conditions of oxidative stress, induced by 200 μM peroxynitrite. The phenolic fraction of T. pratense displayed the strongest ABTS(•) and DPPH(•) radical scavenging effects (EC50 value of 21.69 and 12.27 µg/ml, respectively). The EC50 value for T. pallidum extract attained 29.77 and 30.06 µg/ml. The two remaining extracts were less potent scavengers (EC50 value higher than 50 µg/ml). Similar differences were obtained during evaluation of the ferric reducing abilities. Analysis of antioxidant properties of the extracts in blood plasma did not provide such evident differences in their actions, however, it indicated that the T. pratense phenolic fraction displayed the strongest effect. The examined Trifolium extracts partly protected blood plasma and enhanced its non-enzymatic antioxidant defense against harmful action of peroxynitrite in vitro.

Chemical constituents and their acetyl cholinesterase inhibitory and antioxidant activities from leaves of Acanthopanax henryi: potential complementary source against Alzheimer's disease.

PubMed

Zhang, Xiao Dan; Liu, Xiang Qian; Kim, Yang Hee; Whang, Wan Kyunn

2014-05-01

The aim of this study was to investigate chemical constituents of the leaves of Acanthopanax henryi, and their antioxidant, acetyl cholinesterase inhibitory activities. Caffeoyl quinic acid derivates and flavonoids were obtained from A. henry, through column chromatography technologies, and the content of major constituents was determined by the HPLC-UV method. Anti-oxidant activity of the isolated metabolites was evaluated by free radical scavenging (DPPH, ABTS radicals) and superoxide anion scavenging. The results showed that di-caffeoyl quinic acid derivates had stronger antioxidant activity than positive controls (ascorbic acid, trolox and allopurinol). Acetyl cholinesterase inhibitory activity was estimated on the constituents, among which, quercetin, 4-caffeoyl-quinic acid and 4,5-caffeoyl quinic acid were found to have strong acetyl cholinesterase inhibitory activity with IC50 values ranging from 62.6 to 121.9 μM. The present study showed that some of the tested constituents from the leaves of A. henryi exhibit strong antioxidant and acetyl cholinesterase inhibitory effects. This suggest that the leaves of A. henryi can be used as a new natural complementary source of acetyl cholinesterase inhibitors and anti-oxidant agents, thus being a promising potential complementary source against Alzheimer's disease.

Reactivities of various mediators and laccases with kraft pulp and lignin model compounds.

PubMed

Bourbonnais, R; Paice, M G; Freiermuth, B; Bodie, E; Borneman, S

1997-12-01

Laccase-catalyzed oxygen delignification of kraft pulp offers some potential as a replacement for conventional chemical bleaching and has the advantage of requiring much lower pressure and temperature. However, chemical mediators are required for effective delignification by laccase, and their price is currently too high at the dosages required. To date, most studies have employed laccase from Trametes versicolor. We have found significant differences in reactivity between laccases from different fungi when they are tested for pulp delignification in the presence of the mediators 2,2(prm1)-azinobis(3-ethylbenzthiazoline-6-sulfonate) (ABTS) and 1-hydroxybenzotriazole (HBT). A more detailed study of T. versicolor laccase with ABTS and HBT showed that HBT gave the most extensive delignification over 2 h but deactivated the enzyme, and therefore a higher enzyme dosage was required. Other mediators, including 1-nitroso-2-naphthol-3,6-disulfonic acid, 4-hydroxy-3-nitroso-1-naphthalenesulfonic acid, promazine, chlorpromazine, and Remazol brilliant blue, were also tested for their ability to delignify kraft pulp. Studies with dimeric model compounds indicated that the mechanisms of oxidation by ABTS and HBT are different. In addition, oxygen uptake by laccase is much slower with HBT than with ABTS. It is proposed that the dication of ABTS and the 1-oxide radical of HBT, with redox potentials in the 0.8- to 0.9-V range, are required for pulp delignification.

Reactivities of Various Mediators and Laccases with Kraft Pulp and Lignin Model Compounds

PubMed Central

Bourbonnais, R.; Paice, M. G.; Freiermuth, B.; Bodie, E.; Borneman, S.

1997-01-01

Laccase-catalyzed oxygen delignification of kraft pulp offers some potential as a replacement for conventional chemical bleaching and has the advantage of requiring much lower pressure and temperature. However, chemical mediators are required for effective delignification by laccase, and their price is currently too high at the dosages required. To date, most studies have employed laccase from Trametes versicolor. We have found significant differences in reactivity between laccases from different fungi when they are tested for pulp delignification in the presence of the mediators 2,2(prm1)-azinobis(3-ethylbenzthiazoline-6-sulfonate) (ABTS) and 1-hydroxybenzotriazole (HBT). A more detailed study of T. versicolor laccase with ABTS and HBT showed that HBT gave the most extensive delignification over 2 h but deactivated the enzyme, and therefore a higher enzyme dosage was required. Other mediators, including 1-nitroso-2-naphthol-3,6-disulfonic acid, 4-hydroxy-3-nitroso-1-naphthalenesulfonic acid, promazine, chlorpromazine, and Remazol brilliant blue, were also tested for their ability to delignify kraft pulp. Studies with dimeric model compounds indicated that the mechanisms of oxidation by ABTS and HBT are different. In addition, oxygen uptake by laccase is much slower with HBT than with ABTS. It is proposed that the dication of ABTS and the 1-oxide radical of HBT, with redox potentials in the 0.8- to 0.9-V range, are required for pulp delignification. PMID:16535747

Antioxidant capacity of flavonoids and a new arylphenol of the resinous exudate from Heliotropium sinuatum.

PubMed

Modak, Brenda; Torres, René; Lissi, Eduardo; delle Monache, Franco

2003-12-01

From the resinous exudate of Heliotropium sinuatum (family Boraginaceae), a new compound: 4-(3',5'-dihydroxynonadecyl)phenol 1, together with eight previously described flavonoids, were isolated and their antioxidant activities were assessed by quenching measurements with ABTS and DPPH cation radicals.

Flavonoids as Putative Inducers of the Transcription Factors Nrf2, FoxO, and PPARγ

PubMed Central

Duckstein, Nils; Hasler, Mario; Rimbach, Gerald

2017-01-01

Dietary flavonoids have been shown to extend the lifespan of some model organisms and may delay the onset of chronic ageing-related diseases. Mechanistically, the effects could be explained by the compounds scavenging free radicals or modulating signalling pathways. Transcription factors Nrf2, FoxO, and PPARγ possibly affect ageing by regulating stress response, adipogenesis, and insulin sensitivity. Using Hek-293 cells transfected with luciferase reporter constructs, we tested the potency of flavonoids from different subclasses (flavonols, flavones, flavanols, and isoflavones) to activate these transcription factors. Under cell-free conditions (ABTS and FRAP assays), we tested their free radical scavenging activities and used α-tocopherol and ascorbic acid as positive controls. Most of the tested flavonoids, but not the antioxidant vitamins, stimulated Nrf2-, FoxO-, and PPARγ-dependent promoter activities. Flavonoids activating Nrf2 also tended to induce a FoxO and PPARγ response. Interestingly, activation patterns of cellular stress response by flavonoids were not mirrored by their activities in ABTS and FRAP assays, which depended mostly on hydroxylation in the flavonoid B ring and, in some cases, extended that of the vitamins. In conclusion, the free radical scavenging properties of flavonoids do not predict whether these molecules can stimulate a cellular response linked to activation of longevity-associated transcription factors. PMID:28761622

In vitro antioxidant activity of rice protein affected by alkaline degree and gastrointestinal protease digestion.

PubMed

Liu, Ye; Wang, Zhengxuan; Li, Hui; Liang, Mingcai; Yang, Lin

2016-12-01

To elucidate whether and how alkali treatment, which is a common process for rice protein (RP) extraction, affects antioxidant activity of RP, the different degree of alkali (from 0.1% to 0.4% of NaOH) was used to extract RP (RP-1, RP-2, RP-3, RP-4). The antioxidant capacities of scavenging free radicals [2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid] diammonium salt, ABTS; 1,1-diphenyl-2-picrylhydrazyl, DPPH), chelating metals (iron, copper) and reducing power investigated in the hydrolysates of RPs (RP-1, RP-2, RP-3, RP-4) during in vitro pepsin-pancreatin digestion were effectively affected by alkali treatment. The present study demonstrated that the weakest antioxidant responses to ABTS radical-scavenging activity, DPPH radical-scavenging activity, iron chelating activity, copper chelating activity and reducing power were produced by RP-4 extracted by the highest alkali proportion (0.4% NaOH). The present study indicates that antioxidant capacity of RP could be more readily depressed by strict alkali degree and affected by gastrointestinal proteases. Results suggest that alkali extraction is a vital process to regulate the antioxidant activity of RP through modifying the compositions of amino acids, which are dependent on alkali magnitude. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

Isolation and identification of phenolic antioxidants in black rice bran.

PubMed

Jun, Hyun-Il; Shin, Jae-Wook; Song, Geun-Seoup; Kim, Young-Soo

2015-02-01

Black rice bran contains phenolic compounds of a high antioxidant activity. In this study, the 40% acetone extract of black rice bran was sequentially fractionated to obtain 5 fractions. Out of the 5 fractions, ethyl acetate fraction was subfractionated using the Sephadex LH-20 chromatography. The antioxidant activity of phenolic compounds in the extracts was investigated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical assay, 2,2-azino-bis-(3-ethylenebenzothiozoline-6-sulfonic acid) (ABTS) radical cation assay, reducing power. The subfraction 2 from ethyl acetate fraction had the highest total phenolic contents (TPC) (816.0 μg/mg) and the lowest EC50 values (47.8 μg/mL for DPPH radical assay, 112.8 μg/mL for ABTS radical cation assay, and 49.2 μg/mL for reducing power). These results were 3.1, 1.3, and 2.6 times lower than those of butylated hydroxytoluene (BHT), respectively. At a concentration of 100 μg/mL, the antioxidant activity and TPC of various extracts was closely correlated, with correlation coefficients (R(2) ) higher than 0.86. The major phenolic acid in subfraction 2 was identified as ferulic acid (178.3 μg/mg) by HPLC and LC-ESI/MS/MS analyses. Our finding identified ferulic acid as a major phenolic compound in black rice bran, and supports the potential use of black rice bran as a natural source of antioxidant. © 2015 Institute of Food Technologists®

Antioxidant capacity of chewing stick miswak Salvadora persica.

PubMed

Mohamed, Saleh A; Khan, Jalaluddin A

2013-02-21

Chewing stick (miswak Salvadora persica L.) is an effective tool for oral hygiene. It possessed various biological properties including significant antibacterial and anti-fungal effects. In the present study, we evaluated the antioxidant compounds in miswak. Miswak root was extracted with 80% methanol. Methanol extract as antioxidant was evaluated by using DPPH, ABTS and phosphomolybdenum complex assays and analysis by GC-MS. Peroxidase, catalase and polyphenoloxidase assays were performed for crude extract of miswak root. The methanol extract of miswak contained the highest amount of crude extract among the various solvent extracts. The methanol extract showed a concentration dependent scavenging of DPPH and ABTS radicals with IC50 values 4.8 and 1.6 μg crude extract, respectively. The total antioxidant activities, based on the reduction of molybdenum (VI) to molybdenum (V), increased with increasing crude extract content. The correlation coefficients (R2) between total crude extract and DPPH, ABTS scavenging activities and the formation of phosphomolybdenum complex were 0.97, 0.99 and 0.95, respectively. The GC-MS analysis showed that the methanol extract doesn't contain phenolic and flavonoid compounds or under detected limit. After silylation of methanol extract, three compounds namely 2-furancarboxaldehyde-5-(hydroxymethyl), furan-2-carboxylic acid-3-methyl- trimethylsilyl ester and D-erythro-pentofuranose-2-deoxy-1,3,5-tris-O-(trimethylsilyl) were identified by GC-MS analysis. These furan derivatives as they contain hydroxyl groups could be possessed antioxidant activities. The antioxidant enzymes were also detected in the miswak extract with high level of peroxidase and low level of catalase and polyphenoloxidase. The synergistic actions of antioxidant compounds and antioxidant enzymes make miswak is a good chewing stick for oral hygiene and food purposes.

Phytochemical analysis and free radical scavenging activity of medicinal plants Gnidia glauca and Dioscorea bulbifera.

PubMed

Ghosh, Sougata; Derle, Abhishek; Ahire, Mehul; More, Piyush; Jagtap, Soham; Phadatare, Suvarna D; Patil, Ajay B; Jabgunde, Amit M; Sharma, Geeta K; Shinde, Vaishali S; Pardesi, Karishma; Dhavale, Dilip D; Chopade, Balu A

2013-01-01

Gnidia glauca and Dioscorea bulbifera are traditional medicinal plants that can be considered as sources of natural antioxidants. Herein we report the phytochemical analysis and free radical scavenging activity of their sequential extracts. Phenolic and flavonoid content were determined. Scavenging activity was checked against pulse radiolysis generated ABTS(•+) and OH radical, in addition to DPPH, superoxide and hydroxyl radicals by biochemical methods followed by principal component analysis. G. glauca leaf extracts were rich in phenolic and flavonoid content. Ethyl acetate extract of D. bulbifera bulbs and methanol extract of G. glauca stem exhibited excellent scavenging of pulse radiolysis generated ABTS(•+) radical with a second order rate constant of 2.33 × 10(6) and 1.72 × 10(6), respectively. Similarly, methanol extract of G. glauca flower and ethyl acetate extract of D. bulbifera bulb with second order rate constants of 4.48 × 10(6) and 4.46 × 10(6) were found to be potent scavengers of pulse radiolysis generated OH radical. G. glauca leaf and stem showed excellent reducing activity and free radical scavenging activity. HPTLC fingerprinting, carried out in mobile phase, chloroform: toluene: ethanol (4: 4: 1, v/v) showed presence of florescent compound at 366 nm as well as UV active compound at 254 nm. GC-TOF-MS analysis revealed the predominance of diphenyl sulfone as major compound in G. glauca. Significant levels of n-hexadecanoic acid and octadecanoic acid were also present. Diosgenin (C₂₇H₄₂O₃) and diosgenin (3á,25R) acetate were present as major phytoconstituents in the extracts of D. bulbifera. G. glauca and D. bulbifera contain significant amounts of phytochemicals with antioxidative properties that can be exploited as a potential source for herbal remedy for oxidative stress induced diseases. These results rationalize further investigation in the potential discovery of new natural bioactive principles from these two important medicinal plants.

Antioxidant activity, total phenolic and total flavonoid contents of whole plant extracts Torilis leptophylla L

PubMed Central

2012-01-01

Background The aim of this study was to screen various solvent extracts of whole plant of Torilis leptophylla to display potent antioxidant activity in vitro and in vivo, total phenolic and flavonoid contents in order to find possible sources for future novel antioxidants in food and pharmaceutical formulations. Material and methods A detailed study was performed on the antioxidant activity of the methanol extract of whole plant of Torilis leptophylla (TLM) and its derived fractions {n-hexane (TLH), chloroform (TLC) ethyl acetate (TLE) n-butanol (TLB) and residual aqueous fraction (TLA)} by in vitro chemical analyses and carbon tetrachloride (CCl4) induced hepatic injuries (lipid peroxidation and glutathione contents) in male Sprague-Dawley rat. The total yield, total phenolic (TPC) and total flavonoid contents (TFC) of all the fractions were also determined. TLM was also subjected to preliminary phytochemical screening test for various constituents. Results The total phenolic contents (TPC) (121.9±3.1 mg GAE/g extract) of TLM while total flavonoid contents (TFC) of TLE (60.9 ±2.2 mg RTE/g extract) were found significantly higher as compared to other solvent fractions. Phytochemical screening of TLM revealed the presence of alkaloids, anthraquinones, cardiac glycosides, coumarins, flavonoids, saponins, phlobatannins, tannins and terpenoids. The EC50 values based on the DPPH (41.0±1 μg/ml), ABTS (10.0±0.9 μg/ml) and phosphomolybdate (10.7±2 μg/ml) for TLB, hydroxyl radicals (8.0±1 μg/ml) for TLC, superoxide radicals (57.0±0.3 μg/ml) for TLM and hydrogen peroxide radicals (68.0±2 μg/ml) for TLE were generally lower showing potential antioxidant properties. A significant but marginal positive correlation was found between TPC and EC50 values for DPPH, hydroxyl, phosphomolybdate and ABTS, whereas another weak and positive correlation was determined between TFC and EC50 values for superoxide anion and hydroxyl radicals. Results of in vivo experiment revealed that administration of CCl4 caused a significant increase in lipid peroxidation (TBARS) while decrease in GSH contents of liver. In contrast, TLM (200 mg/kg bw) and silymarin (50 mg/kg bw) co-treatment effectively prevented these alterations and maintained the antioxidant status. Conclusion Data from present results revealed that Torilis leptophylla act as an antioxidant agent due to its free radical scavenging and cytoprotective activity. PMID:23153304

Apigenin sensitizes colon cancer cells to anti-tumor activity of ABT-263

PubMed Central

Shao, Huanjie; Jing, Kai; Mahmoud, Esraa; Huang, Haihong; Fang, Xianjun; Yu, Chunrong

2013-01-01

Apigenin is an edible plant-derived flavonoid that shows modest anti-tumor activities in vitro and in vivo. Apigenin treatment resulted in cell growth arrest and apoptosis in various types of tumors by modulating several signaling pathways. In the present study, we evaluated interactions between apigenin and ABT-263 in colon cancer cells. We observed a synergistic effect between apigenin and ABT-263 on apoptosis of colon cancer cells. ABT-263 alone induced limited cell death while upregulating expression of Mcl-1, a potential mechanism for the acquired resistance to ABT-263. The presence of apigenin antagonized ABT-263-induced Mcl-1 upregulation and dramatically enhanced ABT-263-induced cell death. Meanwhile, apigenin suppressed AKT and ERK activation. Inactivation of either AKT or ERK by lentivirus-transduced shRNA or treatment with specific small molecule inhibitors of these pathways enhanced ABT-263-induced cell death, mirroring the effect of apigenin. Moreover, the combination response was associated with upregulation of Bim and activation of Bax. Downregulation of Bax eliminated the synergistic effect of apigenin and ABT-263 on cell death. Xenograft studies in SCID mice showed that the combined treatment with apigenin and ABT-263 inhibited tumor growth by up to 70% without obvious adverse effects, while either agent only inhibited around 30%. Our results demonstrate a novel strategy to enhance ABT-263 induced anti-tumor activity in human colon cancer cells by apigenin via inhibition of the Mcl-1, AKT and ERK pro-survival regulators. PMID:24126433

Synthesis and antioxidant evaluation of isochroman-derivatives of hydroxytyrosol: structure-activity relationship.

PubMed

Mateos, Raquel; Madrona, Andrés; Pereira-Caro, Gema; Domínguez, Vanessa; Cert, Rosa M A; Parrado, Juan; Sarriá, Beatriz; Bravo, Laura; Espartero, José Luis

2015-04-15

Isochroman-derivatives of the natural olive oil phenol hydroxytyrosol (HT) have been synthesised via Oxa-Pictet-Spengler reaction in high yields. Lipophilicity and antioxidant activity were determined to establish the structure-activity relationship of isochromans compared to HT, BHT and α-tocopherol. Antioxidant capacity was tested in two different media: bulk oils, using the Rancimat test, and brain homogenates, by measuring malondialdehyde (MDA) levels as a lipoperoxidation biomarker. In addition, other antioxidant assays (FRAP, ABTS and ORAC) were carried out. Rancimat and MDA results show that antioxidant activity was related with lipophilicity, directly in brain homogenates and inversely in the oils, in agreement with the polar paradox. Free o-diphenolic groups positively determined the activity in the oils, whereas reducing and radical-scavenging activities were related to the number of free hydroxyl moieties. BHT and α-tocopherol showed lower antioxidant activity than isochromans and HT. We conclude that HT-isochromans present significant potential as bioactive compounds. Copyright © 2014 Elsevier Ltd. All rights reserved.

Antioxidant activity and peroxidase inhibition of Amazonian plants extracts traditionally used as anti-inflammatory.

PubMed

de Vargas, Fabiano S; Almeida, Patricia D O; de Boleti, Ana Paula A; Pereira, Maria M; de Souza, Tatiane P; de Vasconcellos, Marne C; Nunez, Cecilia Veronica; Pohlit, Adrian M; Lima, Emerson S

2016-02-27

The Amazon is the largest rainforest in the world and is home to a rich biodiversity of medicinal plants. Several of these plants are used by the local population for the treatment of diseases, many of those with probable anti-inflammatory effect. The aim of the present investigation was to evaluate the in vitro antioxidant and anti-peroxidases potential of the ethanol extracts of five plants from the Brazilian Amazon (Byrsonima japurensis, Calycophyllum spruceanum, Maytenus guyanensis, Passiflora nitida and Ptychopetalum olacoides). DPPH, ABTS, superoxide anion radical, singlet oxygen and the β-carotene bleaching methods were employed for characterization of free radical scavenging activity. Also, total polyphenols were determined. Antioxidant activities were evaluated using murine fibroblast NIH3T3 cell. Inhibition of HRP and MPO were evaluated using amplex red® as susbtract. The stem bark extracts of C. spruceanum and M. guyanensis provided the highest free radical scavenging activities. C. spruceanum exhibited IC50 = 7.5 ± 0.9, 5.0 ± 0.1, 18.2 ± 3.0 and 92.4 ± 24.8 μg/mL for DPPH(•), ABTS(+•), O2 (-•) and (1)O2 assays, respectively. P. olacoides and C. spruceanum extracts also inhibited free radicals formation in the cell-based assay. At a concentration of 100 μg/mL, the extracts of C. spruceanum, B. japurensis inhibited horseradish peroxidase by 62 and 50 %, respectively. C. spruceanum, M. guyanensis, B. japurensis also inhibited myeloperoxidase in 72, 67 and 56 %, respectively. This work supports the folk use these species that inhibited peroxidases and exhibited significant free radical scavenging and antioxidant activities what can be related to treatment of inflammation.

Chemical composition and inhibitory effects of water extract of Henna leaves on reactive oxygen species, DNA scission and proliferation of cancer cells

PubMed Central

Kumar, Manish; Chandel, Madhu; Kaur, Paramjeet; Pandit, Kritika; Kaur, Varinder; Kaur, Sandeep; Kaur, Satwinderjeet

2016-01-01

From the centuries, Lawsonia inermis L. (Henna) is utilized in traditional health care system as a medicinal and cosmetic agent. The present study was intended to assess antiradical, DNA protective and antiproliferative activity of water extract of Lawsonia inermis L. leaves (W-LI). Antioxidant activity was estimated using various in vitro assays such as DPPH, ABTS, superoxide anion radical scavenging, FRAP, deoxyribose degradation and DNA protection assay. Growth inhibitory effects of W-LI were assessed using MTT assay against different cancer cell lines viz. HeLa, MCF-7, A549, C6 and COLO-205. From the results of antioxidant assays, it was found that W-LI quenched DPPH and ABTS cation radicals with IC50 value of 352.77 µg/ml and 380.87 µg/ml respectively. It demonstrated hydroxyl radical scavenging potential of 59.75 % at highest test dose of 1000 µg/ml in deoxyribose degradation assay. The results of FRAP assay showed that W-LI also possesses significant reducing activity. Extract inhibited hydroxyl radical induced pBR322 plasmid DNA strand scission, thus conferring DNA protection. Growth inhibition of various cancer cell lines was achieved to the varying extent on treatment with W-LI. Further, it was observed that activity was quite promising against colon cancer COLO-205 cells (GI50 121.03 µg/ml). HPLC profiling of W-LI revealed the presence of different polyphenolic compounds such as ellagic acid, catechin, quercetin, kaempferol etc. which might be contributing towards antioxidant and cytotoxic activity. The present study demonstrated that polyphenols rich W-LI extract from leaves of L. inermis possesses ability to inhibit oxidative radicals and cancer cells proliferation. PMID:28337113

Indole Alkaloids from Chaetomium globosum.

PubMed

Xu, Guo-Bo; He, Gu; Bai, Huan-Huan; Yang, Tao; Zhang, Guo-Lin; Wu, Lin-Wei; Li, Guo-You

2015-07-24

Two new indole alkaloids chaetocochin J (1) and chaetoglobinol A (8), along with chetomin (2), chetoseminudin A (3), cochliodinol (9), and semicochliodinol (10), were isolated from the rice culture of the fungus Chaetomium globosum. Their structures were elucidated by spectral analysis. Three new epipolythiodioxopiperazines, chaetocochins G-I (5-7), were identified by the combination of UPLC and mass spectrometric analysis. Chaetocochin I contained two sulfur bridges, one formed by three sulfur atoms between C-3 and C-11a, and the other formed by four sulfur atoms between C-3' and C-6'. Chaetocochin I was readily transformed into chetomin (2), chetoseminudin A (3), chaetocochin D (4), chaetocochin G (5), and chaetocochin H (6) by losing sulfur atoms. Compounds 1-3, and 8 exhibited antibacterial activities against Bacillus subtilis with MICs of 25, 0.78, 0.78, and 50 μg/mL, respectively, but not against Gram-negative bacterium (Escherichia coli). Compounds 2 and 8 were inactive against Candida albicans, Fusarium graminearum, Fusarium vasinfectum, Saccharomyces cerevisiae, and Aspergillus niger even at the high concentrations of 200 and 100 μg/mL, respectively. Compound 8 showed free radical scavenging capacity against the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical (ABTS(+•)), with IC50 values of 143.6 and 45.2 μM, respectively. The free radical scavenging capacity rates of compounds 1-3 on the DPPH and ABTS(+•) were less than 20% at the test concentrations (89.9-108.3 μM). The superoxide anion radical scavenging assay indicated that compounds 1-3, and 8 showed 14.8% (90.9 μM), 18.1% (90.9 μM), 51.5% (88.3 μM), and 30.4% (61.3 μM) superoxide anion radical scavenging capacity, respectively.

In vitro antioxidant and in vivo antidepressant activity of green synthesized azomethine derivatives of cinnamaldehyde

PubMed Central

Chigurupati, Sridevi; Shaikh, Sohrab Akhtar; Mohammad, Jahidul Islam; Selvarajan, Kesavanarayanan Krishnan; Nemala, Appala Raju; Khaw, Chu How; Teoh, Chun Foo; Kee, Ting Hei

2017-01-01

OBJECTIVES: In this study, three (CS-1 to CS-3) azomethine derivatives of cinnamaldehyde were green synthesized, characterized, and their antioxidant and antidepressant activities were explored. MATERIALS AND METHODS: The antioxidant effect of these compounds was initially performed in vitro using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay methods before subjecting them to in vivo experiments. Compounds showing potent antioxidant activity (CS-1 and CS-2) were investigated further for their antidepressant activity using the forced swim test (FST) and tail suspension test (TST). Ascorbic acid (AA) and fluoxetine (20 mg/kg, p.o) were used as reference drugs for comparison in the antioxidant and antidepressant experiments, respectively. RESULTS: It was observed that CS-2 and CS-3 exhibited highest DPPH (half maximal inhibitory concentration [IC50]: 16.22 and 25.18 μg/mL) and ABTS (IC50: 17.2 and 28.86 μg/mL) radical scavenging activity, respectively, compared to AA (IC50: 15.73 and 16.79 μg/mL) and therefore, both CS-2 and CS-3 were tested for their antidepressant effect using FST and TST as experimental models. Pretreatment of CS-2 and CS-3 (20 mg/kg) for 10 days considerably decreased the immobility time in both the FST and TST models. CONCLUSION: The antioxidant and antidepressant effect of CS-2 and CS-3 may be attributed to the presence of azomethine linkage in the molecule. PMID:29033482

Free radicals quenching potential, protective properties against oxidative mediated ion toxicity and HPLC phenolic profile of a Cameroonian spice: Piper guineensis.

PubMed

Moukette Moukette, Bruno; Constant Anatole, Pieme; Nya Biapa, Cabral Prosper; Njimou, Jacques Romain; Ngogang, Jeanne Yonkeu

2015-01-01

Considerations on antioxidants derived from plants have continuously increased during this decade because of their beneficial effects on human health. In the present study we investigated the free radical scavenging properties of extracts from Piper guineense ( P. guineense ) and their inhibitory potentials against oxidative mediated ion toxicity. The free radical quenching properties of the extracts against [1,1-diphenyl-2-picrylhydrazyl (DPPH•), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS•), hydroxyl radical (HO•), nitric oxide (NO•)] radical and their antioxidant potentials by FRAP and phosphomolybdenum were determined as well as their protective properties on liver enzymes. The phenolic profile was also investigated by HPLC. The results obtained, revealed that the extracts significantly inhibited the DPPH, NO, HO and ABTS radicals in a concentration depending manner. They also showed a significant ferrous ion chelating ability through FRAP and phosphomolybdenum antioxidant potential. Their polyphenol contents varied depending on the type of extracts and the solvent used. The hydroethanolic extracts (FFH) and the ethanolic extracts (FFE) of P. guineense leaves showed the higher level of phenolic compounds respectively of 21.62 ± 0.06 mg caffeic acid/g dried extract (CAE/g DE) and 19.01 ± 0.03 CAE/g DE. The HPLC phenolic compounds profile revealed a higher quantity of Eugenol, quercetin, rutin and catechin in the stem than in the leaves. The presence of these molecules could be responsible of the protective potentials of P. guineense extracts against lipid peroxidation and SOD, catalase and peroxidase. In conclusion, P. guineense extracts demonstrated significant antioxidant property and may be used as a prospective protector against metal related toxicity.

Antioxidant activity of nine Fabaceae species growing in Serbia and Montenegro.

PubMed

Godevac, Dejan; Zdunić, Gordana; Savikin, Katarina; Vajs, Vlatka; Menković, Nebojsa

2008-04-01

The aim of this study was to investigate antioxidant capacity of nine Fabaceae species collected on the mountains of Serbia and Montenegro. Antioxidant assays with various reaction mechanisms were used, including total phenolic content by Folin-Ciocalteu, DPPH radical scavenging capacity, Trolox equivalent antioxidant capacity (TEAC) values by ABTS radical cation and inhibition of liposome peroxidation. The investigated plants exhibited strong antioxidant capacity in all the tested methods, and among them, Lathyrus binatus, Trifolium pannonicum, and Anthyllis aurea were found to be the most active.

Antioxidant activities, metal contents, total phenolics and flavonoids of seven Morchella species.

PubMed

Gursoy, Nevcihan; Sarikurkcu, Cengiz; Cengiz, Mustafa; Solak, M Halil

2009-09-01

Seven Morchella species were analyzed for their antioxidant activities in different test systems namely beta-carotene/linoleic acid, DPPH, reducing power, chelating effect and scavenging effect (%) on the stable ABTS*(+), in addition to their heavy metals, total phenolic and flavonoid contents. In beta-carotene/linoleic acid system, the most active mushrooms were M. esculenta var. umbrina and M.angusticeps. In the case of DPPH, methanol extract of M. conica showed high antioxidant activity. The reducing power of the methanol extracts of mushrooms increased with concentration. Chelating capacity of the extracts was also increased with the concentration. On the other hand, in 40 microg ml(-1) concentration, methanol extract of M. conica, exhibited the highest radical scavenging activity (78.66+/-2.07%) when reacted with the ABTS*(+) radical. Amounts of seven elements (Cu, Mn, Co, Zn, Fe, Ca, and Mg) and five heavy metals (Ni, Pb, Cd, Cr, and Al) were also determined in all species. M. conica was found to have the highest phenolic content among the samples. Flavonoid content of M. rotunda was also found superior (0.59+/-0.01 microg QEs/mg extract).

Measurement of total phenolic content and antioxidant activity of aerial parts of medicinal plant Coronopus didymus.

PubMed

Noreen, Hafiza; Semmar, Nabil; Farman, Muhammad; McCullagh, James S O

2017-08-01

To evaluate the total phenolic content and compare the antioxidant activity of various solvent extracts and fractions from the aerial parts of Coronopus didymus through various assays. Total phenolic content was determined using the Folin-Ciocalteu assay and the in vitro antioxidant activity of a number of different extracts was investigated in a dose-dependent manner with three different methods: the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and ferric reducing antioxidant power (FRAP) assays. A flavone was isolated from the most active ethanolic extract with high antioxidant activity using size exclusion chromatography. IC 50 values were calculated for the DPPH and ABTS methods. The FRAP activity was assessed in terms of μM Fe (II) equivalent. The phenolic content was found to be highest in the ethanol extract (CDA Et; 47.8 mM GAE) and the lowest in the dichloromethane extract (CDA DCM; 3.13 mM GAE). The ethanol extract showed high radical scavenging activity towards DPPH and ABTS radicals with IC 50 values of (7.80 × 10 2 ) and (4.32 × 10 2 ) μg/mL, respectively. The most active ethanol extract had a FRAP value of 1921.7 μM Fe (II) equivalent. The isolated flavone F10C (5,7,4'-trihydroxy-3'-methoxy flavone) was far more effective for scavenging free radicals in the DPPH and ABTS assays with IC 50 of 43.8 and 0.08 μg/mL, than the standard trolox, with IC 50 values of 97.5 and 21.1 μg/mL, respectively. In addition, the flavone F10C and the standard ascorbic acid had FRAP values of 1621.7 and 16 038.0 μM Fe (II) equivalents, respectively. The total phenolic content of extracts in decreasing order is ethanol extract (CDA Et) > acetone extract (CDA ACE) > phenolic extract (CDA MW) > n-hexane extract (CDA nHX)> chloroform extract (CDA CHL) > dichloromethane extract (CDA DCM). The ordering of extracts in terms of antioxidant activity from highest to lowest is CDA Et > CDA MW > CDA DCM > CDA CHL > CDA ACE > CDA nHX in DPPH, ABTS and FRAP assays. A significant relationship is found between antioxidant potential and total phenolic content, suggesting that phenolic compounds are the major contributors to the antioxidant activity of C. didymus. Copyright © 2017 Hainan Medical University. Production and hosting by Elsevier B.V. All rights reserved.

Synthesis and Free Radical Scavenging Activity of New Hydroxybenzylidene Hydrazines.

PubMed

Sersen, Frantisek; Gregan, Fridrich; Kotora, Peter; Kmetova, Jarmila; Filo, Juraj; Loos, Dusan; Gregan, Juraj

2017-05-29

Hydroxybenzylidene hydrazines exhibit a wide spectrum of biological activities. Here, we report synthesis and free radical scavenging activity of nine new N-(hydroxybenzylidene)-N'-[2,6-dinitro-4-(trifluoromethyl)]phenylhydrazines. The chemical structures of these compounds were confirmed by 1H-NMR, 13C-NMR, 19F-NMR, IR spectroscopy, LC-MS, and elemental analysis. The prepared compounds were tested for their activity to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH), galvinoxyl radical (GOR), and 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulphonic acid (ABTS) radicals. The free radical scavenging activity expressed as SC50 values of these compounds varied in a wide range, from a strong to no radical scavenging effect. The most effective radical scavengers were hydroxybenzylidene hydrazines containing three hydroxyl groups in the benzylidene part of their molecules. The prepared compounds were also tested for their activity to inhibit photosynthetic electron transport in spinach chloroplasts. IC50 values of these compounds varied in wide range, from an intermediate to no inhibitory effect.

Oxidation of phenolic endocrine disrupting chemicals by potassium permanganate in synthetic and real waters.

PubMed

Jiang, Jin; Pang, Su-Yan; Ma, Jun; Liu, Huiling

2012-02-07

In this study, five selected environmentally relevant phenolic endocrine disrupting chemicals (EDCs), estrone, 17β-estradiol, estriol, 17α-ethinylestradiol, and 4-n-nonylphenol, were shown to exhibit similarly appreciable reactivity toward potassium permanganate [Mn(VII)] with a second-order rate constant at near neutral pH comparable to those of ferrate(VI) and chlorine but much lower than that of ozone. In comparison with these oxidants, however, Mn(VII) was much more effective for the oxidative removal of these EDCs in real waters, mainly due to the relatively high stability of Mn(VII) therein. Mn(VII) concentrations at low micromolar range were determined by an ABTS [2,2-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid diammonium] spectrophotometric method based on the stoichiometric reaction of Mn(VII) with ABTS [Mn(VII) + 5ABTS → Mn(II) + 5ABTS(•+)] forming a stable green radical cation (ABTS(•+)). Identification of oxidation products suggested the initial attack of Mn(VII) at the hydroxyl group in the aromatic ring of EDCs, leading to a series of quinone-like and ring-opening products. The background matrices of real waters as well as selected model ligands including phosphate, pyrophosphate, NTA, and humic acid were found to accelerate the oxidation dynamics of these EDCs by Mn(VII). This was explained by the effect of in situ formed dissolved Mn(III), which could readily oxidize these EDCs but would disproportionate spontaneously without stabilizing agents.

Antioxidant and Anti-Adipogenic Activities of Trapa japonica Shell Extract Cultivated in Korea

PubMed Central

Lee, DooJin; Lee, Ok-Hwan; Choi, Geunpyo; Kim, Jong Dai

2017-01-01

Trapa japonica shell contains phenolic compounds such as tannins. Studies regarding the antioxidant and anti-adipogenic effects of Trapa japonica shell cultivated in Korea are still unclear. Antioxidant and anti-adipogenic activities were measured by in vitro assays such as 2,2-diphenyl-1-picrylhydrazy (DPPH) radical scavenging activity, 2,2′-azinobis( 3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging activity, ferric reducing ability of plasma assay, reducing power, superoxide dismutase-like activity, and iron chelating ability in 3T3-L1 cells. We also measured the total phenol and flavonoids contents (TPC and TFC, respectively) in Trapa japonica shell extract. Our results show that TPC and TFC of Trapa japonica shell extract were 157.7±0.70 mg gallic acid equivalents/g and 25.0±1.95 mg quercetin equivalents/g, respectively. Trapa japonica shell extract showed strong antioxidant activities in a dose-dependent manner in DPPH and ABTS radical scavenging activities and other methods. Especially, the whole antioxidant activity test of Trapa japonica shell extract exhibited higher levels than that of butylated hydroxytoluene as a positive control. Furthermore, Trapa japonica shell extract inhibited lipid accumulation and reactive oxygen species production during the differentiation of 3T3-L1 preadipocytes. Trapa japonica shell extract possessed a significant antioxidant and anti-adipogenic property, which suggests its potential as a natural functional food ingredient. PMID:29333386

Correlation of polyphenolic content with radical-scavenging capacity and anthelmintic effects of Rubus ulmifolius (Rosaceae) against Haemonchus contortus.

PubMed

Akkari, Hafidh; Hajaji, Soumaya; B'chir, Fatma; Rekik, Mourad; Gharbi, Mohamed

2016-05-15

Phenolic content, antioxidant and anthelmintic activities of herbal extracts are of particular interest to drug industry; plant extracts with significant anthelmintic activity have the potential to be used as alternatives to conventional chemical drugs. In the present study, Rubus ulmifolius fruit extracts obtained using solvents of increasing polarity (water, methanol, chloroform and hexane) were examined for their antioxidant and anthelmintic activities in correlation with their polyphenolic content. In vitro antioxidant activity of all extracts was carried out using free radical-scavenging activity by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethilenebenzotiazolin)-6-sulfonic acid (ABTS) radical cation. In vitro anthelmintic activities were investigated on the egg and adult worms of Haemonchus contortus from sheep in comparison to albendazole. Total polyphenol content of R. ulmifolius was higher in more polar extract, ranging from 64.5 in aqueous extract to 1.57 mg gallic acid equivalents per gram of dry weight (GAE/g DW) in hexanic extract. Likewise, highest amounts of flavonoids and condensed tannins were found in aqueous extract (28.06 mg QE/g and 7.42 mg CE/g DW, respectively) compared to hexanic extract (0.71 mg QE/g and 0.29 mg CE/g DW, respectively) (p<0.05). Both DPPH and ABTS antioxidant assays showed that all tested extracts possess free radical scavenging activity, while the inhibitory concentration 50% (IC50) range values were similar for both assays (2.13-45.54 μg/mL and 1.2-43.82 μg/mL, respectively). All plant extracts showed ovicidal activity at all tested concentrations. Fruit methanolic (IC50=2.76mg/mL) and aqueous (IC50=2.08 mg/mL) extracts showed higher inhibitory effects than chloroformic (IC50=7.62 mg/mL) and hexanic (IC50=12.93 mg/mL) extracts on egg hatching (p<0.05). There was a significant correlation of total polyphenol, flavonoids and tannins content with scavenging of either DPPH (r=0.722, 0.764 and 0.752, p<0.01, respectively) or ABTS radicals (r=0.893, 0.765 and 0.722, p<0.01, respectively) and with inhibition of egg hatching (r=0.874, 0.883 and 0.862, p<0.01, respectively). Highest inhibition of motility (100%) of worms was observed 8h post-exposure in aqueous and methanolic extract at 8 mg/mL. To our knowledge, these results depict for the first time that R. ulmifolius possesses in vitro anthelmintic properties. Published by Elsevier B.V.

Mushrooms Collected from Deogyu Mountain, Muju, Korea and Their Antioxidant Activity

PubMed Central

Kim, Seong-Eun; Lee, In-Kyoung; Jung, Yun-A; Yeom, Ji-Hee; Ki, Dae-Won; Lee, Myeong-Seok; Song, Ja-Gyeong; Jin, Yong-Ju; Seok, Soon-Ja

2012-01-01

Mushrooms collected from Deogyu mountain, Korea, in 2011, were identified as four classes, four orders, 13 families, 22 genera, and 33 species. In particular, agaricales was most abundant and comprised more than 70%. Their antioxidant activities were estimated using three different bioassay methods, the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS) radical scavenging assay, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, and reducing power assay. As a result, the methanol extracts of Stereum ostrea, Laetiporus sulphureus var. miniatus, and Tyromyces sambuceus exhibited potent antioxidant activity in all bioassays tested. PMID:22870057

A microtubule inhibitor, ABT-751, induces autophagy and delays apoptosis in Huh-7 cells

DOE Office of Scientific and Technical Information (OSTI.GOV)

Wei, Ren-Jie

The objective was to investigate the upstream mechanisms of apoptosis which were triggered by a novel anti-microtubule drug, ABT-751, in hepatocellular carcinoma-derived Huh-7 cells. Effects of ABT-751 were evaluated by immunocytochemistry, flow cytometric, alkaline comet, soft agar, immunoblotting, CytoID, green fluorescent protein-microtubule associated protein 1 light chain 3 beta detection, plasmid transfection, nuclear/cytosol fractionation, coimmunoprecipitation, quantitative reverse transcription-polymerase chain reaction, small-hairpin RNA interference and mitochondria/cytosol fractionation assays. Results showed that ABT-751 caused dysregulation of microtubule, collapse of mitochondrial membrane potential, generation of reactive oxygen species (ROS), DNA damage, G{sub 2}/M cell cycle arrest, inhibition of anchorage-independent cell growth and apoptosismore » in Huh-7 cells. ABT-751 also induced early autophagy via upregulation of nuclear TP53 and downregulation of the AKT serine/threonine kinase (AKT)/mechanistic target of rapamycin (MTOR) pathway. Through modulation of the expression levels of DNA damage checkpoint proteins and G{sub 2}/M cell cycle regulators, ABT-751 induced G{sub 2}/M cell cycle arrest. Subsequently, ABT-751 triggered apoptosis with marked downregulation of B-cell CLL/lymphoma 2, upregulation of mitochondrial BCL2 antagonist/killer 1 and BCL2 like 11 protein levels, and cleavages of caspase 8 (CASP8), CASP9, CASP3 and DNA fragmentation factor subunit alpha proteins. Suppression of ROS significantly decreased ABT-751-induced autophagic and apoptotic cells. Pharmacological inhibition of autophagy significantly increased the percentages of ABT-751-induced apoptotic cells. The autophagy induced by ABT-751 plays a protective role to postpone apoptosis by exerting adaptive responses following microtubule damage, ROS and/or impaired mitochondria. - Highlights: • An anti-microtubule agent, ABT-751, induces autophagy and apoptosis in Huh-7 cells. • ABT-751 induces early autophagy and delays apoptosis. • ABT-751 induces autophagy via modulations of nuclear TP53 and AKT/MTOR pathways. • ABT-751-induced apoptosis is ROS-, mitochondria- and caspase-dependent. • Inhibition of autophagy enhances ABT-751-induced apoptosis.« less

Silicon containing ibuprofen derivatives with antioxidant and anti-inflammatory activities: An in vivo and in silico study.

PubMed

Pérez, David J; Díaz-Reval, M Irene; Obledo-Benicio, Fernando; Zakai, Uzma I; Gómez-Sandoval, Zeferino; Razo-Hernández, Rodrigo Said; West, Robert; Sumaya-Martínez, María Teresa; Pineda-Urbina, Kayim; Ramos-Organillo, Ángel

2017-11-05

There are many chronic diseases related with inflammation. The chronic inflammation can produce other problems as cancer. Therefore, it is necessary to design drugs with better anti-inflammatory activity than those in the clinic. Likewise, these could be used in chronic treatments with minimum adverse effects. The amide or ester functionality in combination with the insertion of a silyl alkyl moiety is able to improve some drug properties. In this context, the evaluation of a group of silicon containing ibuprofen derivatives (SCIDs) as antioxidants and anti-inflammatory agents is reported. Antioxidant activity was evaluated by the 2,2-Diphenyl-1-picrylhydrazyl (DPPH⨪), 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS • + ) and the Fe(II) chelating ability methods. The anti-inflammatory activity was determined by using the carrageenan induced rat paw edema. The gastrotoxic profile of the SCIDs that displayed significant anti-inflammatory activity was determined by the indomethacin induced ulceration method. The SCIDs performed better than ibuprofen as chelating agents for Fe(II) and as scavengers for the free radicals DPPH• and ABTS • + . On the anti-inflammatory test, compound 4a inhibited the edema up to 87%, while 4d &10b achieved significant inflammation inhibition at a lower effective dose 50 (ED 50 ) than ibuprofen´s. None of the SCIDs endowed with anti-inflammatory activity, showed significant gastrotoxic effects with respect to those displayed by ibuprofen. Based on the experimental results and aided by the theoretical docking approach, it was possible to rationalize how the SCIDs may bind to cyclooxygenase isoforms and helped to explain their reduced gastrotoxicity. The evaluated effects were improved in SCIDs with respect to ibuprofen. Copyright © 2017 Elsevier B.V. All rights reserved.

One-electron redox processes in a cyclic selenide and a selenoxide: a pulse radiolysis study.

PubMed

Singh, Beena G; Thomas, Elizabeth; Kumakura, Fumio; Dedachi, Kenichi; Iwaoka, Michio; Priyadarsini, K Indira

2010-08-19

One-electron redox reactions of cyclic selenium compounds, DL-trans-3,4-dihydroxy-1-selenolane (DHS(red)), and DL-trans-3,4-dihydroxy-1-selenolane oxide (DHS(ox)) were carried out in aqueous solutions using nanosecond pulse radiolysis, and the resultant transients were detected by absorption spectroscopy. Both *OH radical and specific one-electron oxidant, Br(2)(*-) radical reacted with DHS(red) to form similar transients absorbing at 480 nm, which has been identified as a dimer radical cation (DHS(red))(2)(*+). Secondary electron transfer reactions of the (DHS(red))(2)(*+) were studied with 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS(2-)) and superoxide (O(2)(*-)) radicals. The bimolecular rate constants for the electron transfer reaction between (DHS(red))(2)(*+) with ABTS(2-) was determined as 2.4 +/- 0.4 x 10(9) M(-1) s(-1). From this reaction, the yield of (DHS(red))(2)(*+) formed on reaction with *OH radical was estimated in the presence of varying phosphate concentrations. (DHS(red))(2)(*+) reacted with O(2)(*-) radical with a bimolecular rate constant of 2.7 +/- 0.1 x 10(9) M(-1) s(-1) at pH 7. From the same reaction, the positive charge on (DHS(red))(2)(*+) was confirmed by the kinetic salt effect. HPLC analysis of the products formed in the reaction of (DHS(red))(2)(*+) with O(2)(*-) radicals showed formation of the selenoxide, DHS(ox). In order to know if a similar mechanism operated during the reduction of DHS(ox), its reactions with e(aq)(-) were studied at pH 7. The rate constant for this reaction was determined as 5.6 +/- 0.9 x 10(9) M(-1) s(-1), and no transient absorption could be observed in the wavelength region from 280 to 700 nm. It is proposed that the radical anion (DHS(ox))(*-) formed by a one-electron reduction would get protonated to form a hydroxyl radical adduct, which in presence of proton donors, would undergo dehydration to form DHS(*+). Evidence for this mechanism was obtained by converting DHS(*+) to (DHS(red))(2)(*+) with the addition of DHS(red) to the same system. Quantum chemical calculations provided supporting evidence for some of the redox reactions.

Binary solvent extraction system and extraction time effects on phenolic antioxidants from kenaf seeds (Hibiscus cannabinus L.) extracted by a pulsed ultrasonic-assisted extraction.

PubMed

Wong, Yu Hua; Lau, Hwee Wen; Tan, Chin Ping; Long, Kamariah; Nyam, Kar Lin

2014-01-01

The aim of this study was to determine the best parameter for extracting phenolic-enriched kenaf (Hibiscus cannabinus L.) seeds by a pulsed ultrasonic-assisted extraction. The antioxidant activities of ultrasonic-assisted kenaf seed extracts (KSE) were determined by a 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assay, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging assay, β -carotene bleaching inhibition assay, and ferric reducing antioxidant power (FRAP) assay. Total phenolic content (TPC) and total flavonoid content (TFC) evaluations were carried out to determine the phenolic and flavonoid contents in KSE. The KSE from the best extraction parameter was then subjected to high performance liquid chromatography (HPLC) to quantify the phenolic compounds. The optimised extraction condition employed 80% ethanol for 15 min, with the highest values determined for the DPPH, ABTS, and FRAP assay. KSE contained mainly tannic acid (2302.20 mg/100 g extract) and sinapic acid (1198.22 mg/100 g extract), which can be used as alternative antioxidants in the food industry.

Binary Solvent Extraction System and Extraction Time Effects on Phenolic Antioxidants from Kenaf Seeds (Hibiscus cannabinus L.) Extracted by a Pulsed Ultrasonic-Assisted Extraction

PubMed Central

Lau, Hwee Wen; Nyam, Kar Lin

2014-01-01

The aim of this study was to determine the best parameter for extracting phenolic-enriched kenaf (Hibiscus cannabinus L.) seeds by a pulsed ultrasonic-assisted extraction. The antioxidant activities of ultrasonic-assisted kenaf seed extracts (KSE) were determined by a 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assay, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging assay, β-carotene bleaching inhibition assay, and ferric reducing antioxidant power (FRAP) assay. Total phenolic content (TPC) and total flavonoid content (TFC) evaluations were carried out to determine the phenolic and flavonoid contents in KSE. The KSE from the best extraction parameter was then subjected to high performance liquid chromatography (HPLC) to quantify the phenolic compounds. The optimised extraction condition employed 80% ethanol for 15 min, with the highest values determined for the DPPH, ABTS, and FRAP assay. KSE contained mainly tannic acid (2302.20 mg/100 g extract) and sinapic acid (1198.22 mg/100 g extract), which can be used as alternative antioxidants in the food industry. PMID:24592184

Phenolic, flavonoid contents, anticholinesterase and antioxidant evaluation of Iris germanica var; florentina.

PubMed

Ullah, Farhat; Ayaz, Muhammad; Sadiq, Abdul; Hussain, Abid; Ahmad, Sajjad; Imran, Muhammad; Zeb, Anwar

2016-06-01

This study was designed to investigate antioxidant and anticholinesterase potential of Iris germanica var; florentina. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential of plant samples were investigated by Ellman's assay. Antioxidant activity was performed using DPPH, H2O2 and ABTS free radical scavenging assays. Total phenolics and flavonoids contents were expressed in mg GAE/g dry weight and mg RTE/g, respectively. In AChE inhibition assay, Ig.Fl, Ig.Sp and Ig.Cf fractions exhibited highest activity with IC50 values of < 0.1, 5.64 and 19 μg/mL, respectively. In BChE inhibitory assay, Ig.Fl, Ig.Sp, Ig.Cf and Ig.Cr were most active with IC50 of < 0.1, < 0.1, 31 and 78 μg/mL, respectively. In DPPH assay, Ig.Fl and Ig.Cf exhibited highest inhibition of free radicals, 80.52% (IC50 = 9 μg/mL) and 78.30% (IC50 = 8 μg/mL), respectively. In ABTS assay Ig.Cr, Ig.Cf, Ig.Fl and Ig.Sp exhibited IC50 values of < 0.1, 2, 2 and 3 μg/mL, respectively.

Antimicrobial and antioxidant properties of the flavonoid extract from Raphanus sativus L.

NASA Astrophysics Data System (ADS)

Ngoc, Pham Thi Kim; Nguyet, Nguyen Thi Minh; Dao, Dong Thi Anh

2017-09-01

This study was conducted to evaluate the in vitro antimicrobial and antioxidant activities of flavonoid extract from white radish roots (Raphanus sativus L.). Antimicrobial activity was determined by agar diffusion method against 4 strains: Bacillus cereus, Staphylococus aureus, Pseudomonas aeruginosa and Salmonella typhi. Antioxidant activity was determined by ABTS* radical scavenging activity and total antioxidant capacity (TAC). The constituent elements of flavonoid extract were identified by LC-MS. Results showed that the flavonoid extract from Raphanus sativus L. had antibacterial activity against to all four tested bacteria strains with antibacterial ring diameters in the range 8 - 20 mm in the test concentrations from 100 to 1600 mg/ml. Minimum concentration to inhibit (MIC) in the range 20 - 40 mg/ml. In addition, the extract also has the ability to eliminate ABTS* free radical with IC50 = 7.074 µg/ml. The total antioxidant capacity of extract at concentration of 100 µg/ml was 3.424 ± 0.043 mg ascorbic acid/mg. In the extract, there are three flavonoids were found: rutin, quercetin and narigenin. This is the first time narigenin was found in Raphanus sativus L. extract.

Analgesic, antioedematous and antioxidant activity of γ-butyrolactone derivatives in rodents.

PubMed

Salat, Kinga; Librowski, Tadeusz; Moniczewski, Andrzej; Stanisz-Wallis, Krystyna; Wieckowski, Krzysztof; Malawska, Barbara

2012-08-01

In this paper, the analgesic, antioedematous, motor-impairing and antioxidant properties of four γ-butyrolactone derivatives (BM113, BM113A, BM138 and BM138A) are described. Pain was induced by thermal (hot-plate test), chemical (writhing test) or mechanical (Randall-Selitto model) stimulation. All in-vivo assays were carried out in mice pretreated intraperitoneally with the test compounds, except for the evaluation of anti-inflammatory and analgesic activities in the carrageenan-induced paw oedema model, in which rats were pretreated orally with these compounds. In the hot-plate assay, BM113A and BM138A dose dependently prolonged the latency of the nociceptive reaction. Their analgesic activity, measured as a median effective dose (ED(50)=4.7 mg/kg), was similar to that of morphine (2.4 mg/kg). In the writhing test, all four compounds, in particular BM113A and BM138A, showed higher potency than the reference drug acetylsalicylic acid (the ED(50) values were 3.7, 2.3 and 46.1 mg/kg, respectively). BM138 caused a dose-dependent diminution of paw oedema (up to 49%) in the carrageenan model and BM138A at 200 mg/kg reduced mechanical hyperalgesia in the Randall-Selitto test (∼30% when compared with the control). None of the γ-butyrolactone derivatives tested at the ED(50) obtained in the hot-plate test influenced the locomotor activity of mice, although in the rotarod test at 24 rpm, BM113A and BM138 at 100 mg/kg showed some motor-impairing properties. In vitro, a concentration-dependent ABTS radical cation-scavenging activity of BM138 and BM138A (up to 80% inhibition of the radical absorbance) was observed. The results of the present study suggest that BM138 and BM138A could be of interest for future investigations as antinociceptive and antioedematous agents with potential free radical-scavenging properties.

Functional Teas from the Leaves of Arbutus unedo: Phenolic Content, Antioxidant Activity, and Detection of Efficient Radical Scavengers.

PubMed

Erkekoglou, Ioannis; Nenadis, Nikolaos; Samara, Efrosini; Mantzouridou, Fani Th

2017-06-01

The phenolic content/composition and antioxidant activity of hot/cold infusion and decoction from the leaves of Arbutus unedo were studied for the first time. 1,1-diphenyl-2-picrylhydrazyl (DPPH ● ), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical cation (ABTS ●+ ), crocin-bleaching, copper-reducing, and liposome accelerated oxidation assays were used for the evaluation of the activity in vitro. In vivo, the extracts were examined for their ability to protect S. cerevisiae cells from H 2 O 2 induced oxidative stress. An on-line high-performance liquid chromatography-DPPH ● assay was applied to identify potent radical scavengers and comment on their contribution to the total activity. The addition of leaves to boiling water (decoction) was the most appropriate practice to apply since the highest phenol intake (220.2 mg gallic acid/cup served) was obtained. Additionally, its antioxidant activity was equal or superior to that of the other extracts. Flavonols (~51-61 mg/g dry extract) were the main phenols in all the extracts, with quercitrin accounting for ~20% of the total phenol amount. The on-line DPPH ● method verified the high potency of the decoction and indicated as the most active radical scavengers, two galloylquinic acid derivatives and myricitrin, accounting for ~28-45% and ~11-13% of the total scavenging, respectively. Present data may contribute to the future exploitation of A. unedo leaves by the food industry for health-promoting herbal tea preparations and dietary supplements.

Antimutagenic and antioxidant activity of a protein fraction from aerial parts of Urtica dioica.

PubMed

Di Sotto, Antonella; Mazzanti, Gabriela; Savickiene, Nijole; Staršelskytė, Rasa; Baksenskaite, Vaida; Di Giacomo, Silvia; Vitalone, Annabella

2015-06-01

Urtica dioica L. (Urticaceae), stinging nettle, has been employed as a folklore remedy for a wide spectrum of ailments, including urinary disorders, prostatic hyperplasia, and liver diseases. It has been also used traditionally for cancer treatment. To evaluate the potential chemopreventive properties of a protein fraction from the aerial part of Urtica dioica (namely UDHL30). UDHL30 has been tested for the antimutagenic activity in bacteria (50-800 μg/plate; Ames test by the preincubation method) and for the cytotoxicity on human hepatoma HepG2 cells (0.06-2 mg/mL; 24 and 48 h incubation). Moreover, the antioxidant activity of UDHL30 (0.1-1200 μg/mL; ABTS and superoxide-radical scavenger assays) was evaluated as potential protective mechanisms. UDHL30 was not cytotoxic on HepG2 cells up to 2 mg/mL; conversely, it exhibited a strong antimutagenic activity against the mutagen 2-aminoanthracene (2AA) in all strains tested (maximum inhibition of 56, 78, and 61% in TA98, TA100, and WP2uvrA strains, respectively, at 800 μg/plate). In addition, a remarkable scavenging activity against ABTS radical and superoxide anion (IC50 values of 19.9 ± 1.0 μg/mL and 75.3 ± 0.9 μg/mL, respectively) was produced. UDHL30 possesses antimutagenic and radical scavenging properties. Being 2AA a pro-carcinogenic agent, we hypothesize that the antimutagenicity of UDHL30 can be due to the inhibition of CYP450-isoenzymes, involved in the mutagen bioactivation. The radical scavenger ability could contribute to 2AA-antimutagenicity. These data encourage further studies in order to better define the potential usefulness of UDHL30 in chemoprevention.

Anti-Oxidative and Anti-Inflammation Activities of Pork Extracts.

PubMed

Gil, Juae; Kim, Dongwook; Yoon, Seok-Ki; Ham, Jun-Sang; Jang, Aera

2016-01-01

This study was conducted to evaluate the antioxidative and anti-inflammatory effects of boiled pork powder (BPP) and hot water extract powder (HWEP) from 4 cuts of meat from Landrace × Yorkshire × Duroc (LYD). The highest DPPH radical scavenging activities determined were from BPP of Boston butt (13.65 M TE) and HWEP of loin (19.40 M TE) and ham (21.45 M TE). The 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging activities of BPP from shoulder ham (39.28 M TE) and ham (39.43 M TE) were higher than those of other meat cuts, while HWEP of ham exhibited the highest ABTS radical scavenging activity. A higher oxygen radical absorbance capacity was determined for BPP from ham (198.35 M TE) and in HWEP from loin (204.07 M TE), Boston butt (192.85 M TE), and ham (201.36 M TE). Carnosine content of BPP and HWEP from loin and were determined to be 106.68 and 117.77 mg/g on a dry basis, respectively. The anserine content of BPP (5.26 mg/g, dry basis) and HWEP (6.79 mg/g, dry basis) of shoulder ham exhibited the highest value as compared to the extracts from the other meat cuts. The viability of RAW 264.7 cells was increased with increasing HWEP from loin and ham treatment. In addition, the expression of IL-6 and TNF-α was significantly reduced by HWEP from loin and ham, in a dose dependent manner. These results suggested that boiled pork and hot water extract of pork have antioxidative and cytokine inhibitory effects.

Antioxidant and prooxidant nature of hydroxycinnamic acid derivatives ferulic and caffeic acids.

PubMed

Maurya, Dharmendra Kumar; Devasagayam, Thomas Paul Asir

2010-12-01

Dietary polyphenols are beneficial to human health by exerting various biological effects. Ferulic and caffeic acids are hydroxycinnamic acid derivatives widely distributed in plant-derived food products. Studies indicate that some dietary compounds may have concentration-dependent antioxidant or prooxidant activities. The present study concerns such activities of ferulic and caffeic acids. They have concentration-dependent antioxidant effects in terms of inhibition of lipid peroxidation and reactive oxygen species-scavenging after 2,2'-azobis-amidinopropane dihydrochloride-induced damage in mouse liver microsomes and splenic lymphocytes respectively. They also show differential scavenging of nitric oxide, superoxide and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid radical (ABTS*(+)). In DPPH (1,1-diphenyl picrylhydrazyl) assay above 20 μM the absorbance start increasing due to the formation of an unknown adduct which has a shoulder at 517 nm. However, in Fenton reaction, above 5 μM, they behave as prooxidants and the possible mechanisms responsible for their prooxidant property may be related to their ferric reducing ability. These findings may have significant health implications where these natural compounds are being used/consumed. Copyright © 2010 Elsevier Ltd. All rights reserved.

Improvement of antioxidant and moisture-preserving activities of Sargassum horneri polysaccharide enzymatic hydrolyzates.

PubMed

Shao, Ping; Chen, Xiaoxiao; Sun, Peilong

2015-03-01

In the previous study, we have found that polysaccharides isolated from Sargassum horneri exhibited bioactivities. The aim of this study was to investigate the antioxidant and moisture-preserving activities of molecular weight alteration of Sargassum horneri polysaccharide in vitro. For this purpose, the homogeneous active polysaccharide SHP was isolated from Sargassum horneri, and response surface methodology was employed to optimize the enzymatic degradation conditions to get SHP-derived fragments with different molecular weight. Results proved that the polysaccharide is capable of scavenging both ABTS and DPPH radicals in vitro. The study revealed that the polysaccharides had strong moisture-absorption and -retention capacities as compared to propanediol and glycerin. Furthermore, these data demonstrated that molecular weight had a certain effect on antioxidant activities and strong moisture-retention capacities of the polysaccharide from Sargassum horneri. Copyright © 2014 Elsevier B.V. All rights reserved.

A microtubule inhibitor, ABT-751, induces autophagy and delays apoptosis in Huh-7 cells.

PubMed

Wei, Ren-Jie; Lin, Su-Shuan; Wu, Wen-Ren; Chen, Lih-Ren; Li, Chien-Feng; Chen, Han-De; Chou, Chien-Ting; Chen, Ya-Chun; Liang, Shih-Shin; Chien, Shang-Tao; Shiue, Yow-Ling

2016-11-15

The objective was to investigate the upstream mechanisms of apoptosis which were triggered by a novel anti-microtubule drug, ABT-751, in hepatocellular carcinoma-derived Huh-7 cells. Effects of ABT-751 were evaluated by immunocytochemistry, flow cytometric, alkaline comet, soft agar, immunoblotting, CytoID, green fluorescent protein-microtubule associated protein 1 light chain 3 beta detection, plasmid transfection, nuclear/cytosol fractionation, coimmunoprecipitation, quantitative reverse transcription-polymerase chain reaction, small-hairpin RNA interference and mitochondria/cytosol fractionation assays. Results showed that ABT-751 caused dysregulation of microtubule, collapse of mitochondrial membrane potential, generation of reactive oxygen species (ROS), DNA damage, G 2 /M cell cycle arrest, inhibition of anchorage-independent cell growth and apoptosis in Huh-7 cells. ABT-751 also induced early autophagy via upregulation of nuclear TP53 and downregulation of the AKT serine/threonine kinase (AKT)/mechanistic target of rapamycin (MTOR) pathway. Through modulation of the expression levels of DNA damage checkpoint proteins and G 2 /M cell cycle regulators, ABT-751 induced G 2 /M cell cycle arrest. Subsequently, ABT-751 triggered apoptosis with marked downregulation of B-cell CLL/lymphoma 2, upregulation of mitochondrial BCL2 antagonist/killer 1 and BCL2 like 11 protein levels, and cleavages of caspase 8 (CASP8), CASP9, CASP3 and DNA fragmentation factor subunit alpha proteins. Suppression of ROS significantly decreased ABT-751-induced autophagic and apoptotic cells. Pharmacological inhibition of autophagy significantly increased the percentages of ABT-751-induced apoptotic cells. The autophagy induced by ABT-751 plays a protective role to postpone apoptosis by exerting adaptive responses following microtubule damage, ROS and/or impaired mitochondria. Copyright © 2016 Elsevier Inc. All rights reserved.

Antioxidant potential and radical-scavenging effects of flavonoids from the leaves of Psidium cattleianum grown in French Polynesia.

PubMed

Ho, R; Violette, A; Cressend, D; Raharivelomanana, P; Carrupt, P A; Hostettmann, K

2012-01-01

Psidium cattleianum J. Sabine (Myrtaceae) is a traditional medicinal plant in French Polynesia. The leaves and roots possess many medicinal properties. These effects may be correlated with the presence of antioxidant compounds. Seven flavonoids along with a benzoic acid were isolated from the leaves of P. cattleianum. The compounds indicated strong antioxidant and radical-scavenging activities in ALP, DPPH(·), ABTS(·-) and ORAC assays. This study demonstrates that the leaves of P. cattleianum possess main compounds with interesting antioxidant and radical-scavenging activities, as clarified by four biological assays. Our findings may justify the use of these leaves in the traditional medicine of French Polynesia. Among the total eight known compounds, reynoutrin and luteolin were isolated for the first time from the genus Psidium.

[Comparison of the antioxidant properties of selected parts of raspberry (Rubus idaeus) and blackberry (Rubus fruticosus)

PubMed

Zielonka-Brzezicka, Joanna; Nowak, Anna; Zielińska, Magdalena; Klimowicz, Adam

Antioxidants contained in plant raw materials prevent oxidative stress, and reduce the degenerative effects of free radical reactions and damage caused by UV radiation. Antioxidant activity is exhibited, for example, in raspberry (Rubus idaeus), and blackberry (Rubus fruticosus), which have a high content of tannins, flavonoids, phenolic acids, vitamins and minerals. The raw plant material consisted of fresh and dried leaves and fruits of raspberries and blackberries harvested in 2014. This material was extracted using a Soxhlet apparatus and by an ultrasound-assisted technique. To evaluate antioxidant activity DPPH and FRAP methods were used in the first year and DPPH and ABTS methods in the second year of the study. The highest antioxidant activity, evaluated by the DPPH method in 2015, was demonstrated by both raspberry and blackberry fresh leaf extracts, whereas the highest reductive ability, assessed by FRAP, was demonstrated in fresh and dried blackberry leaves. In the next year of the study (2016), the activity of samples evaluated using the DPPH method did not differ significantly, with the exception of fresh raspberry leaf. In this year, the highest antioxidant properties, assessed using the ABTS method, were shown by extracts made of fresh blackberry leaves and fruits, and dried blackberry leaves. All the studied material, both ethanolic leaves and fruit extracts of raspberry and blackberry, reduced free radicals, which was examined using three methods of evaluation of the antioxidative properties (DPPH, FRAP and ABTS). The storage of ethanolic extracts at ambient temperature had no significant impact on the activity reduction of the evaluated plant material. The antioxidant activity of most examined extracts remained consistently high, which may be reflected in the use of the studied materials as sources of antioxidants in the cosmetics and pharmaceuticals industries.

Assessment of Antioxidant and Antibacterial Properties on Meat Homogenates of Essential Oils Obtained from Four Thymus Species Achieved from Organic Growth.

PubMed

Ballester-Costa, Carmen; Sendra, Esther; Fernández-López, Juana; Pérez-Álvarez, Jose A; Viuda-Martos, Manuel

2017-07-28

In the organic food industry, no chemical additives can be used to prevent microbial spoilage. As a consequence, the essential oils (EOs) obtained from organic aromatic herbs and spices are gaining interest for their potential as preservatives. The organic Thymus zygis , Thymus mastichina , Thymus capitatus and Thymus vulgaris EOs, which are common in Spain and widely used in the meat industry, could be used as antibacterial agents in food preservation. The aims of this study were to determine (i) the antibacterial activity using, as culture medium, extracts from meat homogenates (minced beef, cooked ham or dry-cured sausage); and (ii) the antioxidant properties of organic EOs obtained from T. zygis , T. mastichina , T. capitatus and T. vulgaris . The antioxidant activity was determined using different methodologies, such as Ferrous ion-chelating ability assay, Ferric reducing antioxidant power, ABTS radical cation (ABTS • +) scavenging activity assay and 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method; while the antibacterial activity was determined against 10 bacteria using the agar diffusion method in different meat model media. All EOs analyzed, at all concentrations, showed antioxidant activity. T. capitatus and T. zygis EOs were the most active. The IC 50 values, for DPPH, ABTS and FIC assays were 0.60, 1.41 and 4.44 mg/mL, respectively, for T. capitatus whilst for T. zygis were 0.90, 2.07 and 4.95 mg/mL, respectively. Regarding antibacterial activity, T. zygis and T. capitatus EOs, in all culture media, had the highest inhibition halos against all tested bacteria. In general terms, the antibacterial activity of all EOs assayed was higher in the medium made with minced beef than with the medium elaborated with cooked ham or dry-cured sausage.

Antioxidant activity and inhibitory effects of 2-hydroxy-3-methylcyclopent-2-enone isolated from ribose-histidine Maillard reaction products on aldose reductase and tyrosinase.

PubMed

Hwang, Seung Hwan; Wang, Zhiqiang; Suh, Hong-Won; Lim, Soon Sung

2018-03-01

This study aimed to better understand the functional properties of ribose and 20 amino acid Maillard reaction products (MRPs). The ABTS + radical scavenging ability of the ribose-20 amino acid MRPs was evaluated. Among the MRPs, ribose-histidine MRPs (RH-MRPs) showed the highest inhibitory activities on the ABTS + radical scavenging ability, aldose reductase (AR), and tyrosinase compared to other MRPs. Functional compounds with antioxidant and AR inhibitory activities have been recognized as an important strategy in the prevention and treatment of diabetic complications, and the search for tyrosinase inhibitors is important for the treatment of hyperpigmentation, development of skin-whitening agents, and use as preservatives in the food industry. On this basis, we sought to isolate and identify compounds with inhibitory activities against AR and tyrosinase. RH-MRPs were heated at 120 °C for 2 h and fractionated using four solvents: methylene chloride (MC), ethyl acetate, n-butanol, and water. The highest inhibitions were found in the MC fraction. The two compounds from this fraction were purified by silica gel column and preparative thin layer chromatography, and identified as 2-hydroxy-3-methylcyclopent-2-enone and furan-3-carboxylic acid. AR inhibition, tyrosinase inhibition, and ABTS + scavenging (IC 50 ) of 2-hydroxy-3-methylcyclopent-2-enone were 4.47, 721.91 and 9.81 μg mL -1 , respectively. In this study, inhibitory effects of 2-hydroxy-3-methylcyclopent-2-enone isolated from RH-MRP were demonstrated on AR, tyrosinase, and its antioxidant activity for the first time. RH-MRP and its constituents can be developed as beneficial functional food sources and cosmetic materials and should be investigated further as potential functional food sources.

Metronomic low-dose chemotherapy boosts CD95-dependent antiangiogenic effect of the thrombospondin peptide ABT-510: a complementation antiangiogenic strategy.

PubMed

Yap, Ronald; Veliceasa, Dorina; Emmenegger, Urban; Kerbel, Robert S; McKay, Laura M; Henkin, Jack; Volpert, Olga V

2005-09-15

Blocking angiogenesis is a promising approach in cancer therapy. Natural inhibitors of angiogenesis and derivatives induce receptor-mediated signals, which often result in the endothelial cell death. Low-dose chemotherapy, given at short regular intervals with no prolonged breaks (metronomic chemotherapy), also targets angiogenesis by obliterating proliferating endothelial cells and circulating endothelial cell precursors. ABT-510, a peptide derivative of thrombospondin, kills endothelial cell by increasing CD95L, a ligand for the CD95 death receptor. However, CD95 expression itself is unaffected by ABT-510 and limits its efficacy. We found that multiple chemotherapy agents, cyclophosphamide (cytoxan), cisplatin, and docetaxel, induced endothelial CD95 in vitro and in vivo at low doses that failed to kill endothelial cells (cytoxan > cisplatin > docetaxel). Thus, we concluded that some of these agents might complement each other and together block angiogenesis with maximal efficacy. As a proof of principle, we designed an antiangiogenic cocktail combining ABT-510 with cytoxan or cisplatin. Cyclophosphamide and cisplatin synergistically increased in vivo endothelial cell apoptosis and angiosuppression by ABT-510. This synergy required CD95, as it was reversible with the CD95 decoy receptor. In a mouse model, ABT-510 and cytoxan, applied together at low doses, acted in synergy to delay tumor take, to stabilize the growth of established tumors, and to cause a long-term progression delay of PC-3 prostate carcinoma. These antitumor effects were accompanied by major decreases in microvascular density and concomitant increases of the vascular CD95, CD95L, and apoptosis. Thus, our study shows a "complementation" design of an optimal cancer treatment with the antiangiogenic peptide and a metronomic chemotherapy.

Anti-ulcer mechanisms of polyphenols extract of Euphorbia umbellata (Pax) Bruyns (Euphorbiaceae).

PubMed

Minozzo, Bruno Rodrigo; Lemes, Bruna Mikulis; Justo, Aline da Silva; Lara, Jheniffer Ellen; Petry, Victor Emanuel Kubaski; Fernandes, Daniel; Belló, Caroline; Vellosa, José Carlos Rebuglio; Campagnoli, Eduardo Bauml; Nunes, Otalíbio Castiglione; Kitagawa, Rodrigo Rezende; Avula, Bharathi; Khan, Ikhlas Ahmad; Beltrame, Flávio Luis

2016-09-15

Euphorbia umbellata (leitosinha) is used in southern Brazilian folk medicine to treat gastric problems, as well as for its analgesic and anti-inflammatory properties. To evaluate the anti-ulcer effects of methanolic bark fraction (MF) against in vivo and in vitro assays, as well as an antioxidant, antibacterial and chromatographic study of this fraction. In vivo anti-ulcer activity was performed using ethanol and indomethacin models with different MF concentrations (50, 100 or 200mg/Kg). The stomachs of the animals were applied to histological evaluation, and the serum to evaluate the ABTS(•+) radical capture. The 200mg/Kg dose was used to analyze the mechanisms involved in antiulcerogenic properties of methanolic fraction. The in vitro activity was performed using several different antioxidant assays, in addition to anti-Helicobacter pylori and anti-urease experiments. The chromatographic study was carried out by LC-MS analysis. Pharmacological investigation of the MF showed an anti-ulcer potential in ethanol and indomethacin in vivo assays. The material presented a high antioxidant activity for several oxidant in vitro systems (DPPH(•), ABTS(•+), O2(•-), HOCl, TauCl and HRP), as well as an ABTS(•+) capture increasing (7.5%) by the treated animals serum (when compared to the negative control). Prostaglandins, nitric oxide/ cyclic guanosine monophosphate pathway and involvement of the protein components of the glutathione complex are some of the mechanisms related with this potential anti-ulcer action. The histological examination of the stomachs of the animals showed that the MF also prevents local action of offensive agents. Chemical analysis using LC-QTOF-MS revealed the presence of ellagic and gallic acid derivatives and flavonols. The findings provide scientific basis to the ethnopharmacological purpose of the studied plant and the biological activities of MF of E. umbellata stem bark may be due to the presence of phenolic compounds. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

Glucosidase inhibitory activity and antioxidant activity of flavonoid compound and triterpenoid compound from Agrimonia Pilosa Ledeb.

PubMed

Liu, Xi; Zhu, Liancai; Tan, Jun; Zhou, Xuemei; Xiao, Ling; Yang, Xian; Wang, Bochu

2014-01-10

In Chinese traditional medicine, Agrimonia pilosa Ledeb (APL) exhibits great effect on treatment of type 2 diabetes mellitus (T2DM), however its mechanism is still unknown. Considering that T2DM are correlated with postprandial hyperglycemia and oxidative stress, we investigated the α-glucosidase inhibitory activity and the antioxidant activity of flavonoid compound (FC) and triterpenoid compound (TC) from APL. Entire plants of APL were extracted using 95% ethanol and 50% ethanol successively. The resulting extracts were partitioned and isolated by applying liquid chromatography using silica gel column and Sephadex LH 20 column to give FC and TC. The content of total flavonoids in FC and the content of total triterpenoids in TC were determined by using UV spectrophotometry. HPLC analysis was used to identify and quantify the monomeric compound in FC and TC. The α-glucosidase inhibitory activities were determined using the chromogenic method with p-nitrophenyl-α-D-glucopyranoside as substrate. Antioxidant activities were assessed through three kinds of radical scavenging assays (DPPH radical, ABTS radical and hydroxyl radical) & β-carotene-linoleic acid assay. The results indicate FC is abundant of quercitrin, and hyperoside, and TC is abundant of 1β, 2β, 3β, 19α-tetrahydroxy-12-en-28-oic acid (265.2 mg/g) and corosolic acid (100.9 mg/g). The FC & the TC have strong α-glucosidase inhibitory activities with IC50 of 8.72 μg/mL and 3.67 μg/mL, respectively. We find that FC show competitive inhibition against α-glucosidase, while the TC exhibits noncompetitive inhibition. Furthermore, The FC exhibits significant radical scavenging activity with the EC50 values of 7.73 μg/mL, 3.64 μg/mL and 5.90 μg/mL on DPPH radical, hydroxyl radical and ABTS radical, respectively. The FC also shows moderate anti-lipid peroxidation activity with the IC50 values of 41.77 μg/mL on inhibiting β-carotene bleaching. These results imply that the FC and the TC could be responsible for the good clinical effects of APL on T2MD through targeting oxidative stress and postprandial hyperglycaemia. So APL may be good sources of natural antioxidants and α-glucosidase inhibitors exhibiting remarkable potential value for the therapy of T2DM.

Bioassay Directed Isolation and Biological Evaluation of Compounds Isolated from Rubus fairholmianus Gard.

PubMed Central

Plackal George, Blassan; Thangaraj, Parimelazhagan; Sulaiman, Cheruthazhakkatt; Piramanayagam, Shanmughavel; Ramaswamy, Sathish Kumar

2014-01-01

The in vitro and in silico analysis of Rubus fairholmianus acetone extract for antioxidant, antiproliferative, and anti-inflammatory activity led to the isolation of six compounds. Amongst all the six isolated compounds tested, 1-(2-hydroxyphenyl)-4-methylpentan-1-one (compound 1) and 2-[(3-methylbutoxy) carbonyl] benzoic acid (compound 2) were found to be more active in inhibiting BRCA and COX target proteins, which also showed the better results for DPPH and ABTS radical scavenging assays. The promising results of this investigation emphasize the importance of using R. fairholmianus in the treatment of radical generated disorders mainly cancer and other inflammatory diseases. PMID:25254204

Analytical profiling of selected antioxidants and total antioxidant capacity of goji (Lycium spp.) berries.

PubMed

Protti, Michele; Gualandi, Isacco; Mandrioli, Roberto; Zappoli, Sergio; Tonelli, Domenica; Mercolini, Laura

2017-09-05

Goji berries and derived products represent a relevant source of micronutrients, most of which are natural antioxidants and contribute to the high nutritional quality of these fruits. Three brands of dried goji berries have been analysed by a multidisciplinary approach to get an insight into both their content of selected antioxidants and their antioxidant capacity (AC). The former goal has been achieved by developing a liquid chromatographic method coupled to mass spectrometry and combined to a fast solid phase extraction. Several significant representative antioxidant compounds belonging to the following classes: flavonoids, flavan-3-ols, phenolic acids, amino acids and derivatives, and carotenoids have been taken into account. Quercetin and rutin were found to be the predominant flavonoids, chlorogenic acid was the most abundant phenolic acid and zeaxanthin was the major carotenoid. The AC of the goji berries has been evaluated by four analytical methods in order to estimate the contributions of different reactions involved in radicals scavenging. In particular, AC has been determined using 3 standardised methods (DPPH, ABTS, ORAC) and a recently proposed electrochemical method, which measures the scavenging activity of antioxidants towards OH radicals generated both by hydrogen peroxide photolysis and the Fenton reaction. The results obtained from chemical composition and antioxidant capacity assays confirm the high nutritional and commercial value of goji berries and highlight that the three brands do not exhibit significant differences. Copyright © 2017 Elsevier B.V. All rights reserved.

Phenolic Profiles and Contribution of Individual Compounds to Antioxidant Activity of Apple Powders.

PubMed

Raudone, Lina; Raudonis, Raimondas; Liaudanskas, Mindaugas; Viskelis, Jonas; Pukalskas, Audrius; Janulis, Valdimaras

2016-05-01

Apples (Malus domestica L.) are the most common source of phenolic compounds in northern European diet. Besides pectins, dietary fibers, vitamins, and oligosaccharides they contain phenolic compounds of different classes. Apple powders are convenient functional forms retaining significant amounts of phenolic antioxidants. In this study reducing and radical scavenging profiles of freeze-dried powders of "Aldas,ˮ "Auksis,ˮ "Connel Red,ˮ "Ligol,ˮ "Lodel,ˮ and "Rajkaˮ were determined and phenolic constituents were identified using ultra high-performance liquid chromatography coupled to quadrupole and time-of-flight mass spectrometers. A negative ionization mode was applied and seventeen compounds: phenolic acids (coumaroylquinic, chlorogenic), flavonoids (quercetin derivatives), and procyanidin derivatives (B1, B2, and C1) were identified in all tested apple samples. Total values of Trolox equivalents varied from 7.72 ± 0.32 up to 20.02 ± 0.52 and from 11.10 ± 0.57 up to 21.42 ± 0.75 μmol/g of dry weight of apple powder in FRAP (ferric reducing antioxidant power) and ABTS (2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) postcolumn assays, respectively. The greatest Trolox equivalent values were determined for apples of "Aldasˮ cultivar. Chlorogenic acid and procyanidin C1 were the most significant contributors to total reducing and radical scavenging activity in all apple cultivars tested, therefore they could be considered as markers of antioxidant activity. © 2016 Institute of Food Technologists®

Antioxidant activity of food constituents: an overview.

PubMed

Gülçin, İlhami

2012-03-01

Recently, there has been growing interest in research into the role of plant-derived antioxidants in food and human health. The beneficial influence of many foodstuffs and beverages including fruits, vegetables, tea, coffee, and cacao on human health has been recently recognized to originate from their antioxidant activity. For this purpose, the most commonly methods used in vitro determination of antioxidant capacity of food constituents are reviewed and presented. Also, the general chemistry underlying the assays in the present paper was clarified. Hence, this overview provides a basis and rationale for developing standardized antioxidant capacity methods for the food, nutraceutical, and dietary supplement industries. In addition, the most important advantages and shortcomings of each method were detected and highlighted. The chemical principles of these methods are outlined and critically discussed. The chemical principles of methods of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS(·+)) scavenging, 1,1-diphenyl-2-picrylhydrazyl (DPPH(·)) radical scavenging, Fe(3+)-Fe(2+) transformation assay, ferric reducing antioxidant power (FRAP) assay, cupric ions (Cu(2+)) reducing power assay (Cuprac), Folin-Ciocalteu reducing capacity (FCR assay), peroxyl radical scavenging, superoxide anion radical (O (2) (·-)) scavenging, hydrogen peroxide (H(2)O(2)) scavenging, hydroxyl radical (OH(·)) scavenging, singlet oxygen ((1)O(2)) quenching assay and nitric oxide radical (NO(·)) scavenging assay are outlined and critically discussed. Also, the general antioxidant aspects of main food components were discussed by a number of methods which are currently used for detection of antioxidant properties food components. This review consists of two main sections. The first section is devoted to main components in the foodstuffs and beverages. The second general section is some definitions of the main antioxidant methods commonly used for determination of antioxidant activity of components in the foodstuffs and beverages. In addition, there are given some chemical and kinetic basis and technical details of the used methods.

Aldosterone breakthrough in dogs with naturally occurring myxomatous mitral valve disease.

PubMed

Ames, M K; Atkins, C E; Eriksson, A; Hess, A M

2017-06-01

Aldosterone breakthrough (ABT) is the condition in which angiotensin converting enzyme inhibitors (ACEIs) and/or angiotensin receptor blockers fail to effectively suppress the activity of the renin angiotensin aldosterone system. The objective of this study was to determine if ABT occurs in dogs with naturally occurring myxomatous mitral valve disease receiving an ACEI, using the urine aldosterone to creatinine ratio (UAldo:C) as a measure of renin angiotensin aldosterone system activation. This study includes 39 dogs with myxomatous mitral valve disease. A UAldo:C cut-off definition (derived from a normal population of healthy, adult, and client-owned dogs) was used to determine the prevalence of ABT in this population. Spearman analysis and univariate logistic regression were used to evaluate the relationship between UAldo:C and ABT (yes/no) and eight variables (age, serum K + concentration, serum creatinine concentration, ACEI therapy duration and ACEI dosage, furosemide therapy duration and furosemide dosage, and urine sample storage time). Finally, the UAldo:C in dogs receiving spironolactone, as part congestive heart failure (CHF) therapy, was compared to dogs with CHF that were not receiving spironolactone. The prevalence of ABT was 32% in dogs with CHF and 30% in dogs without CHF. There was no relationship between either the UAldo:C or the likelihood of ABT and the eight variables. Therapy with spironolactone lead to a significant elevation of the UAldo:C. Using the UAldo:C and a relatively stringent definition of ABT, it appears that incomplete RAAS blockade is common in dogs with MMVD receiving an ACEI. The prevalence of ABT in this canine population mirrors that reported in humans. While the mechanism of ABT is likely multifactorial and still poorly understood, the proven existence of ABT in dogs offers the potential to improve the prognosis for MMVD with the addition of a mineralocorticoid receptor blocker to current therapeutic regimens. Approximately 30% of dogs being treated for heart disease and CHF satisfied the definition of ABT. Identifying patient subpopulations experiencing ABT may help guide future study design and clinical decision-making. Copyright © 2017 Elsevier B.V. All rights reserved.

Antioxidant activity of Vitex agnus-castus L. extracts.

PubMed

Sağlam, Hüsniye; Pabuçcuoğlu, Aysun; Kivçak, Bijen

2007-11-01

The ethanol, n-hexane and water extracts of Vitex agnus-castus L. leaves and fruits were screened for antioxidant activity. The antioxidant activity of plant extracts was determined by an improved assay based on the decolorization of the radical monocation of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS.+). The water and ethanol extracts showed stronger antioxidant activity than the n-hexane extracts. Copyright (c) 2007 John Wiley & Sons, Ltd.

Synthesis, crystal structure and bioactivity of manganese complexes with asymmetric chiral Schiff base

NASA Astrophysics Data System (ADS)

Zhang, Enfeng; Wei, Yi; Huang, Fuping; Yu, Qing; Bian, Hedong; Liang, Hong; Lei, Fuhou

2018-03-01

A couple of chiral unsymmtrical Schiff base ligands, (1R,2R) (-)chxn (salH) (naftalH) and (1S,2S) (-)chxn (salH) (naftalH) had been synthesized by the condensation of salicylaldehyde and 2-hydroxy-1-naphthaldehyde with two isomers of (1R,2R)-trans-1,2-cyclohexanediamin and (1S,2S)-trans-1,2-cyclohexanediamin, respectively. At the same time, two manganese complexes have been synthesized and fully characterized by FT-IR spectrum, elemental analyses, single crystal X-ray diffraction. The interaction of the two Mn (III) complexes with bovine serum albumin (BSA) was investigated by spectroscopic techniques. The result reveals that the complexes can strongly quench the intrinsic fluorescence of BSA through a static quenching mechanism. The binding constant and binding mode has been determined. The secondary structure and the amino acid residues microenvironment of BSA change in the presence of these complexes. SOD-like activity and ABTS free radical scavenging ability were also studied. The antioxidant capacity of the compounds showed that the complexes and their corresponding BSA adducts showed some SOD activity. The results of ABTS free radical scavenging showed that the activity of the BSA adduct was more obvious than that of the complex.

Antioxidative and anticholinesterase activity of Cyphomandra betacea fruit.

PubMed

Ali Hassan, Siti Hawa; Abu Bakar, Mohd Fadzelly

2013-01-01

Cyphomandra betacea is one of the underutilized fruits which can be found in tropical and subtropical countries. This study was conducted to determine the antioxidant activity and phytochemical contents in different parts (i.e., flesh and peel) of the fruits. Antioxidants were analyzed using DPPH and ABTS free radical scavenging assays as well as FRAP assay. Anticholinesterase activity was determined using enzymatic assay using acetyl cholinesterase enzyme. For 80% methanol extract, the peel of the fruit displayed higher antioxidant activity in both FRAP and ABTS free radical scavenging assays while the flesh displayed higher antioxidant activity in the DPPH assay. Total phenolic and total flavonoid content were higher in the peel with the values of 4.89 ± 0.04 mg gallic acid equivalent (GAE)/g and 3.36 ± 0.01 mg rutin equivalent (RU)/g, respectively. Total anthocyanin and carotenoid content were higher in the flesh of the fruit with the values of 4.15 ± 0.04 mg/100 g and 25.13 ± 0.35 mg/100 g. The anticholinesterase was also higher in the peel of C. betacea. The same trends of phytochemicals, antioxidant, and anticholinesterase were also observed in the distilled water extracts. These findings suggested that C. betacea has a potential as natural antioxidant-rich nutraceutical products.

Antioxidative and Anticholinesterase Activity of Cyphomandra betacea Fruit

PubMed Central

Ali Hassan, Siti Hawa; Abu Bakar, Mohd Fadzelly

2013-01-01

Cyphomandra betacea is one of the underutilized fruits which can be found in tropical and subtropical countries. This study was conducted to determine the antioxidant activity and phytochemical contents in different parts (i.e., flesh and peel) of the fruits. Antioxidants were analyzed using DPPH and ABTS free radical scavenging assays as well as FRAP assay. Anticholinesterase activity was determined using enzymatic assay using acetyl cholinesterase enzyme. For 80% methanol extract, the peel of the fruit displayed higher antioxidant activity in both FRAP and ABTS free radical scavenging assays while the flesh displayed higher antioxidant activity in the DPPH assay. Total phenolic and total flavonoid content were higher in the peel with the values of 4.89 ± 0.04 mg gallic acid equivalent (GAE)/g and 3.36 ± 0.01 mg rutin equivalent (RU)/g, respectively. Total anthocyanin and carotenoid content were higher in the flesh of the fruit with the values of 4.15 ± 0.04 mg/100 g and 25.13 ± 0.35 mg/100 g. The anticholinesterase was also higher in the peel of C. betacea. The same trends of phytochemicals, antioxidant, and anticholinesterase were also observed in the distilled water extracts. These findings suggested that C. betacea has a potential as natural antioxidant-rich nutraceutical products. PMID:24298210

Effects of Cooking and In Vitro Digestion on Antioxidant Properties and Cytotoxicity of the Culinary-Medicinal Mushroom Pleurotus ostreatoroseus (Agaricomycetes).

PubMed

Brugnari, Tatiane; da Silva, Pedro Henrique Alves; Contato, Alex Graça; Inácio, Fabíola Dorneles; Nolli, Mariene Marques; Kato, Camila Gabriel; Peralta, Rosane Marina; de Souza, Cristina Giatti Marques

2018-01-01

In this study we evaluated the antioxidant capacity, antimicrobial activity, and cytotoxicity of an aqueous extract of the Pleurotus ostreatoroseus mushroom, which was cooked. Fresh basidiocarps were heated and steamed at 100°C and the resulting aqueous extract was assessed before and after in vitro digestion. Cooking reduced the amounts of phenolic compounds in the extract. The antioxidant activity of the extract was evaluated through the use of 4 methods. The lowest half-maximal effective concentration (EC50) against ABTS radicals was 0.057 ± 0.002 mg/mL for the uncooked basidiocarp extract. Cooking and the digestive process led to decreased activity (P > 0.05) against ABTS and DPPH radicals. A significant increase in chelating activity (P > 0.05) occurred after the basidiocarps were cooked (EC50 = 0.279 ± 0.007 mg/mL). The reducing power did not significantly change among the different extracts. The uncooked basidiocarp extract was cytotoxic to Vero cells. After cooking and subsequent in vitro digestion, the cytotoxicity of the extracts decreased (P < 0.05). Bacillus subtilis, Staphylococcus aureus, and Candida albicans were sensitive to the fresh mushroom extract. The data showed that after being cooked and digested, the P. ostreatoroseus mushroom maintains antioxidant activity and has a low cytotoxic effect.

Effect of drying procedures on the physicochemical properties and antioxidant activities of polysaccharides from Crassostrea gigas

PubMed Central

Zheng, Yaxu; Qu, Min; Jin, Qiao; Tong, Changqing

2017-01-01

Crassostrea gigas polysaccharides (CGP) were obtained by different drying methods: freeze-drying (FD), spray-drying (SD) or rotary evaporation-drying (RED). The physicochemical properties of CGP were evaluated on the basis of polysaccharide content, protein content, color characteristics, FT-IR spectroscopy, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Antioxidant activities were researched three different free radicals, including DPPH free radicals, ABTS free radicals and reducing power. The results demonstrated that FDCGP, SDCGP and REDCGP have different physicochemical properties and antioxidant activities. Contrasted with FDCGP and REDCGP, SDCGP exhibited stronger antioxidant abilities. Therefore, considering the polysaccharides appearances and antioxidant activities, the spray drying method is a decent selection for the preparation of such polysaccharides, and it should be selected for application in the food industry. PMID:29176846

Comprehensive analysis of commercial willow bark extracts by new technology platform: combined use of metabolomics, high-performance liquid chromatography-solid-phase extraction-nuclear magnetic resonance spectroscopy and high-resolution radical scavenging assay.

PubMed

Agnolet, Sara; Wiese, Stefanie; Verpoorte, Robert; Staerk, Dan

2012-11-02

Here, proof-of-concept of a new analytical platform used for the comprehensive analysis of a small set of commercial willow bark products is presented, and compared with a traditional standardization solely based on analysis of salicin and salicin derivatives. The platform combines principal component analysis (PCA) of two chemical fingerprints, i.e., HPLC and (1)H NMR data, and a pharmacological fingerprint, i.e., high-resolution 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) radical cation (ABTS(+)) reduction profile, with targeted identification of constituents of interest by hyphenated HPLC-solid-phase extraction-tube transfer NMR, i.e., HPLC-SPE-ttNMR. Score plots from PCA of HPLC and (1)H NMR fingerprints showed the same distinct grouping of preparations formulated as capsules of Salix alba bark and separation of S. alba cortex. Loading plots revealed this to be due to high amount of salicin in capsules and ampelopsin, taxifolin, 7-O-methyltaxifolin-3'-O-glucoside, and 7-O-methyltaxifolin in S. alba cortex, respectively. PCA of high-resolution radical scavenging profiles revealed clear separation of preparations along principal component 1 due to the major radical scavengers (+)-catechin and ampelopsin. The new analytical platform allowed identification of 16 compounds in commercial willow bark extracts, and identification of ampelopsin, taxifolin, 7-O-methyltaxifolin-3'-O-glucoside, and 7-O-methyltaxifolin in S. alba bark extract is reported for the first time. The detection of the novel compound, ethyl 1-hydroxy-6-oxocyclohex-2-enecarboxylate, is also described. Copyright © 2012 Elsevier B.V. All rights reserved.

Antioxidant capacity and polyphenolic content of blueberry (Vaccinium corymbosum L.) leaf infusions.

PubMed

Piljac-Zegarac, J; Belscak, A; Piljac, A

2009-06-01

Antioxidant capacity and polyphenolic content of leaf infusions prepared from six highbush blueberry cultivars (Vaccinium corymbosum L.), one wild lowbush blueberry cultivar (Vaccinium myrtillus L.), and one commercially available mix of genotypes were determined. In order to simulate household tea preparation conditions, infusions were prepared in water heated to 95 degrees C. The dynamics of extraction of polyphenolic antioxidants were monitored over the course of 30 minutes. Extraction efficiency, quantified in terms of the total phenol (TP) content, and antioxidant capacity of infusions, evaluated by the ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging assays, were compared with cultivar type and extraction time. The 30-minute infusions exhibited the highest TP content and antioxidant capacity according to all three assays. Wild blueberry infusion had the highest TP content (1,879 mg/L gallic acid equivalents [GAE]) and FRAP values (20,050 microM). The range of TP values for 30-minute infusions was 394-1,879 mg/L GAE with a mean of 986 mg/L GAE across cultivars; FRAP values fell between 3,015 and 20,050 microM with a mean of 11,234 microM across cultivars. All 30-minute infusions exhibited significant scavenging capacity for DPPH(*) and ABTS(*+) radicals, comparable to different concentrations of catechin, gallic acid, and 6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid. Overall, tested infusions showed significant reducing capacity as well as radical scavenging potential, which places blueberry leaf tea high on the list of dietary sources of antioxidants.

Antioxidant and Anticholinesterase Activities of Some Dialkylamino Substituted 3-Hydroxyflavone Derivatives.

PubMed

Culhaoglu, Burcu; Capan, Asli; Boga, Mehmet; Ozturk, Mehmet; Ozturk, Turan; Topcu, Gulacti

2017-01-01

Flavones, are a class of naturally occuring polyphenolic compounds which have 2-phenylchromen-4-one structure. Various studies showed that flavones have several pharmacological activities such as antioxidant, anti-inflammatory, antimicrobial, cytotoxic, antitumour and antiallergic. In the present study, 3-hydroxyflavones also called flavonols, posessing 4'-dialkylamino moiety were synthesized, and their antioxidant and anticholinesterase activities were investigated by comparison with unmodified 3-hydroxflavone. For investigation of antioxidant potential, radical scavenging assays (DPPH•, ABTS+_, O2.-) were used along with CUPRAC and lipid peroxidation inhibitory assays, as well as anticholinesterase activity by Ellman method. The best results were obtained for 4'-N,N-dimethyl flavonol (1) in both antioxidant and anticholinesterase activity tests, possibly due to its least steric hinderance effect. It exhibited remarkable DPPH free radical scavenging activity (2.43±0,09 μg/mL) competing with a standard compound quercetin (2.10±0,10 μg/mL). Moreover, the other tested flavonols also showed high antioxidant activities. Compounds 5 and 6 exhibited close IC50 values to those of compound 1. Antioxidant activity test results were found to be well correlated with anticholinesterase activity test results indicating possible role of antioxidant compounds in the treatment of Alzheimer's disease. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Free Radical Scavenging Properties of Annona squamosa

PubMed

Vikas, Biba; Akhil B, S; P, Remani; Sujathan, K

2017-10-26

Annona squamosa has extensively been used in the traditional and folkloric medicine and found to possess many biological activities. Different solvents, petroleum ether, chloroform, ethyl acetate and methanol extracts of Annona squamosa seeds (ASPE, ASCH, ASEA, ASME) have been used to prepare plant extracts. The present investigations dealt with the free radical scavenging activity of four extracts using various techniques such as total reducing power estimation, total phenolic count, 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging effect, evaluation of ABTS cation decolorisation capacity, FRAP assay, hdroxyl radical scavenging assay, super oxide assay and Nitric oxide radical scavenging assay of the extracts. The results showed that the four extracts of Annona squamosa showed significant reducing power in four extracts. The total phenolic contents in petroleum ether, chloroform, ethyl acetate, methanol extracts and positive control were 0.64±0.17, 0.54±0.27, 0.49±0.24, 0.57±0.22 and 0.66±0.33. The antioxidant capacity by ABTS assay of ASPE, ASCH, ASEA, ASME and positive control, trolox showed 77.75±0.5,73.25±1.7,78.5± 1.2 , 80 ± 0.8 μg/ml and 94.2 ± 0.9 respectively. The (50 % scavenging activity) SA50 of ASPE and ASCH, ASEA and ASME was found to be 34.4 μg/ml, 43.8 μg/ml 34.7 μg/m and 28.8 μg/ml respectively by DPPH assay. The percentage of hydroxyl radical scavenging increased with the increasing concentration of the extracts. ASPE, ASCH, ASEA and ASME showed superoxide radical scavenging activity, as indicated by their values 66 ± 0.5, 68 ± 1 ,63 ± 1 and 70 ± 0.5 μg/ml respectively compared to gallic acid which was 97 ± 0.5 μg/ml. The values for scavenging of nitric oxide for ASPE, ASCH, ASEA and ASME were 91.0 ± 1.0, 66.75 ± 0.5, 71.75 ± 1.1 and 75.75 ± 1.15 μg/ml while value for standard ascorbic acid was 91.0 ± 1.0 μg/ml. The results revealed strong antioxidants in four extracts may lead to the development of potent antioxidant agents from Annona squamosa seeds. Creative Commons Attribution License

A modified method for studying behavioral paradox of antioxidants and their disproportionate competitive kinetic effect to scavenge the peroxyl radical formation.

PubMed

Masood, Nusrat; Fatima, Kaneez; Luqman, Suaib

2014-01-01

We have described a modified method for evaluating inhibitor of peroxyl radicals, a well-recognized and -documented radical involved in cancer initiation and promotion as well as diseases related to oxidative stress and ageing. We are reporting hydrophilic and lipophilic as well as natural and synthetic forms of antioxidants revealing a diversified behaviour to peroxyl radical in a dose-dependent manner (1 nM-10 μM). A simple kinetic model for the competitive oxidation of an indicator molecule (ABTS) and a various antioxidant by a radical (ROO(•)) is described. The influences of both the concentration of antioxidant and duration of reaction (70 min) on the inhibition of the radical cation absorption are taken into account while determining the activity. The induction time of the reaction was also proposed as a parameter enabling determination of antioxidant content by optimizing and introducing other kinetic parameters in 96-well plate assays. The test evidently improves the original PRTC (peroxyl radical trapping capacity) assay in terms of the amount of chemical used, simultaneous tracking, that is, the generation of the radical taking place continually and the kinetic reduction technique (area under curve, peak value, slope, and Vmax).

Radical scavenging activity and LC-MS metabolic profiling of petals, stamens, and flowers of Crocus sativus L.

PubMed

Montoro, Paola; Maldini, Mariateresa; Luciani, Leonilda; Tuberoso, Carlo I G; Congiu, Francesca; Pizza, Cosimo

2012-08-01

Radical scavenging activities of Crocus sativus petals, stamens and entire flowers, which are waste products in the production of the spice saffron, by employing ABTS radical scavenging method, were determined. At the same time, the metabolic profiles of different extract (obtained by petals, stamens and flowers) were obtained by LC-ESI-IT MS (liquid chromatography coupled with electrospray mass spectrometry equipped with Ion Trap analyser). LC-ESI-MS is a techniques largely used nowadays for qualitative fingerprint of herbal extracts and particularly for phenolic compounds. To compare the different extracts under an analytical point of view a specific method for qualitative LC-MS analysis was developed. The high variety of glycosylated flavonoids found in the metabolic profiles could give value to C. sativus petals, stamens and entire flowers. Waste products obtained during saffron production, could represent an interesting source of phenolic compounds, with respect to the high variety of compounds and their free radical scavenging activity. © 2012 Institute of Food Technologists®

Evaluation of Radical Scavenging Activity of Sempervivum tectorum and Corylus avellana Extracts with Different Phenolic Composition.

PubMed

Alberti, Ágnes; Riethmüller, Eszter; Béni, Szabolcs; Kéry, Ágnes

2016-04-01

Semnpervivum tectorum L. and Corylus avellana L. are traditional herbal remedies exhibiting antioxidant activity and representing diverse phenolic composition. The aim of this study was to reveal the contribution of certain compounds to total radical scavenging activity by studying S. tectorum and C. avellana extracts prepared with solvents of different selectivity for diverse classes of phenolics. Antioxidant activity of S. tectorum and C. avellana samples was determined in the ABTS and DPPH radical scavenging assays, and phenolic composition was evaluated by high-performance liquid chromatography/electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS). Correlations between antioxidant activity and phenolic content of houseleek extracts have been revealed. Significant differences regarding antioxidant activity have been shown between S. tectorum 80% (v/v) methanol extract and its fractions. Additionally, synergism among the constituents present together in the whole extract was assumed. Significantly higher radical scavenging activity of hazel extracts has been attributed to the differences in phenolic composition compared with houseleek extracts.

Total phenolic contents and free-radical scavenging activities of grape (Vitis vinifera L.) and grape products.

PubMed

Keser, Serhat; Celik, Sait; Turkoglu, Semra

2013-03-01

Grape is one of the world's largest fruit crops, with an approximate annual production of 58 million metric tons, and it is well known that the grape skins, seeds and stems, waste products generated during wine and grape juice processing, are rich sources of polyphenols. It contains flavonoids, phenolic acids and stilbenes. In this study, we tried to determine antioxidant properties and phenolic contents of grape and grape products (fresh fruit, seed, dried fruit, molasses, pestil, vinegar) of ethanol and water extracts. Antioxidant properties of extracts were investigated by DPPH(√), ABTS(√+), superoxide, H(2)O(2) scavenging, reducing power, metal chelating activity and determination of total phenolic contents. The seed extracts revealed highest ABTS(√+), DPPH(√), H(2)O(2) scavenging and reducing power activities. Furthermore, these extracts showed higher total phenolic contents than other grape product extracts.

Antimicrobial and antioxidant activity of the essential oil from the Carpathian Thymus alternans Klokov.

PubMed

Vitali, Luca A; Dall'Acqua, Stefano; Maggi, Filippo; Martonfi, Pavol; Papa, Fabrizio; Petrelli, Dezemona; Sut, Stefania; Lupidi, Giulio

2017-05-01

The genus Thymus includes several species that are used as flavouring, food preservative as well as in cosmetics. Their secondary metabolites have been extensively studied for pharmacological effects. Nonetheless, some species are neglected and deserve to be explored for chemical composition and biological activities. This is the case with Thymus alternans, a Carpathian bush used as a food additive and for the preparation of a traditional herbal medicine. In this work, we have analysed the chemical composition of T. alternans essential oil by GC and GC-MS and evaluated its antimicrobial and antioxidant activity by disc diffusion, DPPH, ABTS and FRAP methods, respectively. Results showed that T. alternans belongs to the nerolidol chemotype, being rich of this sesquiterpene alcohol (15.8%) which might contribute to the antimicrobial (particularly effective on C. albicans growth) and antioxidant (weak inhibition on ABTS radical and reducing power) activities observed.

Antioxidant activity of methanol extract of Helichrysum foetidum Moench.

PubMed

Tirillini, Bruno; Menghini, Luigi; Leporini, Lidia; Scanu, Nadia; Marino, Stefania; Pintore, Giorgio

2013-01-01

Methanol extract of Helichrysum foetidum Moench (Asteraceae) was investigated for antioxidative properties. The antioxidant activities were investigated by 2,2'-azinobis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) assay, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging, ß-carotene/linoleic acid assay, scavenging of hydrogen peroxide (HRPO test), superoxide anion scavenging (S.A.S. test) and hypochlorous acid scavenging (taurine test). The antioxidant activity was reported as IC50 and reveals Trolox-like antioxidative effects.

A C-di-GMP-proflavine-hemin supramolecular complex has peroxidase activity--implication for a simple colorimetric detection.

PubMed

Nakayama, Shizuka; Roelofs, Kevin; Lee, Vincent T; Sintim, Herman O

2012-03-01

Herein, we demonstrate that the bacterial signaling molecule, c-di-GMP, can enhance the peroxidation of hemin when proflavine is present. The c-di-GMP-proflavine-hemin nucleotidezyme can oxidize the colorless compound 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), ABTS, to the colored radical cation ABTS˙(+) and hence provides simple colorimetric detection of c-di-GMP at low micromolar concentrations.

Glucosidase inhibitory activity and antioxidant activity of flavonoid compound and triterpenoid compound from Agrimonia Pilosa Ledeb

PubMed Central

2014-01-01

Background In Chinese traditional medicine, Agrimonia pilosa Ledeb (APL) exhibits great effect on treatment of type 2 diabetes mellitus (T2DM), however its mechanism is still unknown. Considering that T2DM are correlated with postprandial hyperglycemia and oxidative stress, we investigated the α-glucosidase inhibitory activity and the antioxidant activity of flavonoid compound (FC) and triterpenoid compound (TC) from APL. Methods Entire plants of APL were extracted using 95% ethanol and 50% ethanol successively. The resulting extracts were partitioned and isolated by applying liquid chromatography using silica gel column and Sephadex LH 20 column to give FC and TC. The content of total flavonoids in FC and the content of total triterpenoids in TC were determined by using UV spectrophotometry. HPLC analysis was used to identify and quantify the monomeric compound in FC and TC. The α-glucosidase inhibitory activities were determined using the chromogenic method with p-nitrophenyl-α-D-glucopyranoside as substrate. Antioxidant activities were assessed through three kinds of radical scavenging assays (DPPH radical, ABTS radical and hydroxyl radical) & β-carotene-linoleic acid assay. Results The results indicate FC is abundant of quercitrin, and hyperoside, and TC is abundant of 1β, 2β, 3β, 19α-tetrahydroxy-12-en-28-oic acid (265.2 mg/g) and corosolic acid (100.9 mg/g). The FC & the TC have strong α-glucosidase inhibitory activities with IC50 of 8.72 μg/mL and 3.67 μg/mL, respectively. We find that FC show competitive inhibition against α-glucosidase, while the TC exhibits noncompetitive inhibition. Furthermore, The FC exhibits significant radical scavenging activity with the EC50 values of 7.73 μg/mL, 3.64 μg/mL and 5.90 μg/mL on DPPH radical, hydroxyl radical and ABTS radical, respectively. The FC also shows moderate anti-lipid peroxidation activity with the IC50 values of 41.77 μg/mL on inhibiting β-carotene bleaching. Conclusion These results imply that the FC and the TC could be responsible for the good clinical effects of APL on T2MD through targeting oxidative stress and postprandial hyperglycaemia. So APL may be good sources of natural antioxidants and α-glucosidase inhibitors exhibiting remarkable potential value for the therapy of T2DM. PMID:24410924

Chemical composition and physicochemical properties of Phaeodactylum tricornutum microalgal residual biomass.

PubMed

German-Báez, L J; Valdez-Flores, M A; Félix-Medina, J V; Norzagaray-Valenzuela, C D; Santos-Ballardo, D U; Reyes-Moreno, C; Shelton, L M; Valdez-Ortiz, A

2017-12-01

The production of photosynthetic biofuels using microalgae is a promising strategy to combat the use of non-renewable energy sources. The microalgae residual biomass is a waste by-product of biofuel production; however, it could prove to have utility in the development of sustainable nutraceuticals and functional foods. In this study, a comprehensive characterisation of the under-utilised Phaeodactylum tricornutum microalgae residual biomass is presented. Proximal composition, antioxidant capacity (using three different antioxidant assays; oxygen radical absorbance capacity; radical cation activity, ABTS; and radical scavenging activity, DPPH), and total phenolic content of free and bound polyphenols were determined. Additionally, the physicochemical properties of water activity, pH, water absorption index, water solubility index, and dispersibility were evaluated. Results revealed that P. tricornutum microalgae residual biomass exhibits a relatively high protein and carbohydrate content, with values of 36.67% and 46.78%, respectively; and most carbohydrates were found as total dietary fibre (45.57%), of which insoluble dietary fibre was the most predominant (43.54%). Antioxidant capacity values for total phytochemicals of 106.22, 67.93, 9.54 µM TE g -1 dw were determined by oxygen radical absorbance capacity, ABTS, and DPPH assays, respectively. Total phenolic content was found to be 2.90 mg GAE g -1 dw. Interestingly, antioxidant capacity and total phenolic content were higher in bound than in free phytochemical extracts. The physicochemical analysis showed P. tricornutum microalgae residual biomass to have suitable properties for the generation of a beverage with Aw, pH, water absorption index, water solubility index, and dispersibility values of 0.45, 7.12, 3.40 g gel g -1  dw, 2.5 g solids 100 g -1  dw, and 90%, respectively. Hence, P. tricornutum microalgae residual biomass could be considered a potential source of bioactive compounds suitable for the production of functional food exhibiting antioxidant capacity and high dietary fibre content.

Preliminary study of the antioxidant properties of flowers and roots of Pyrostegia venusta (Ker Gawl) Miers.

PubMed

Roy, Purabi; Amdekar, Sarika; Kumar, Avnish; Singh, Vinod

2011-08-23

Free radical stress leads to tissue injury and can eventually to arthritis, atherosclerosis, diabetes mellitus, neurodegenerative diseases and carcinogenesis. Several studies are ongoing worldwide to find natural antioxidants of plant origin. We assessed the in-vitro antioxidant activities and screened the phytochemical constituents of methanolic extracts of Pyrostegia venusta (Ker Gawl) Miers. We evaluated the antioxidant potential and phytochemical constituents of P. venusta using 1,1-Diphenyl-2-picrylhydrazyl (DPPH), 2, 2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant power (FRAP) assays. Gas chromatography-mass spectroscopy (GC-MS) studies were also undertaken to assess the phytochemical composition of the flower extracts. Phytochemical analyses revealed the presence of terpenoids, alkaloids, tannins, steroids, and saponins. The reducing ability of both extracts was in the range (in μm Fe(II)/g) of 112.49-3046.98 compared with butylated hydroxytoluene (BHT; 63.56 ± 2.62), catechin (972.02 ± 0.72 μm) and quercetin 3208.27 ± 31.29. A significant inhibitory effect of extracts of flowers (IC50 = 0.018 ± 0.69 mg/ml) and roots (IC50 = 0.026 ± 0.94 mg/ml) on ABTS free radicals was detected. The antioxidant activity of the extracts of flowers (95%) and roots (94%) on DPPH radicals was comparable with that of ascorbic acid (98.9%) and BHT (97.6%). GC-MS study revealed the presence of myoinositol, hexadecanoic acid, linoleic acid, palmitic acid and oleic acid in the flower extracts. These data suggest that P. venusta is a natural source of antioxidants. The extracts of flowers and roots of P. venusta contain significant amounts of phytochemicals with antioxidative properties and could serve as inhibitors or scavengers of free radicals. P. venusta could be exploited as a potential source for plant-based pharmaceutical products. These results could form a sound basis for further investigation in the potential discovery of new natural bioactive compounds.

Derivatization of single-walled carbon nanotubes with redox mediator for biocatalytic oxygen electrodes.

PubMed

Sadowska, K; Stolarczyk, K; Biernat, J F; Roberts, K P; Rogalski, J; Bilewicz, R

2010-11-01

Single-walled carbon nanotubes (SWCNTs) were covalently modified with a redox mediator derived from 2,2'-azino-bis-(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and implemented in the construction of electrodes for biocatalytic oxygen reduction. The procedure is based on: covalent bonding of mediator to nanotubes, placing the nanotubes directly on the carbon electrode surface and covering the nanostructured electrode with a Nafion film containing laccase as the biocatalyst. The modified electrode is stable and the problem of mediator (ABTS) leaking from the film is eliminated by binding it covalently to the nanotubes. Three different synthetic approaches were used to obtain ABTS-modified carbon nanotubes. Nanotubes were modified at ends/defect sites or on the nanotube sidewalls and characterized by Raman spectroscopy, TGA and electrochemistry. The accessibility of differently located ABTS units by the laccase active center and mediation of electron transfer were studied by cyclic voltammetry. The surface concentrations of ABTS groups electrically connected with the electrode were compared for each of the electrodes based on the charges of the voltammetric peaks recorded in the deaerated solution. The nanotube modification procedure giving the best parameters of the catalytic process was selected. Copyright © 2010 Elsevier B.V. All rights reserved.

Antioxidative Potential of a Streptomyces sp. MUM292 Isolated from Mangrove Soil

PubMed Central

Chan, Chim Kei

2018-01-01

Mangrove derived microorganisms constitute a rich bioresource for bioprospecting of bioactive natural products. This study explored the antioxidant potentials of Streptomyces bacteria derived from mangrove soil. Based on 16S rRNA phylogenetic analysis, strain MUM292 was identified as the genus Streptomyces. Strain MUM292 showed the highest 16S rRNA gene sequence similarity of 99.54% with S. griseoruber NBRC12873T. Furthermore, strain MUM292 was also characterized and showed phenotypic characteristics consistent with Streptomyces bacteria. Fermentation and extraction were performed to obtain the MUM292 extract containing the secondary metabolites of strain MUM292. The extract displayed promising antioxidant activities, including DPPH, ABTS, and superoxide radical scavenging and also metal-chelating activities. The process of lipid peroxidation in lipid-rich product was also retarded by MUM292 extract and resulted in reduced MDA production. The potential bioactive constituents of MUM292 extract were investigated using GC-MS and preliminary detection showed the presence of pyrazine, pyrrole, cyclic dipeptides, and phenolic compound in MUM292 extract. This work demonstrates that Streptomyces MUM292 can be a potential antioxidant resource for food and pharmaceutical industries. PMID:29805975

Cytoprotective dibenzoylmethane derivatives protect cells from oxidative stress-induced necrotic cell death.

PubMed

Hegedűs, Csaba; Lakatos, Petra; Kiss-Szikszai, Attila; Patonay, Tamás; Gergely, Szabolcs; Gregus, Andrea; Bai, Péter; Haskó, György; Szabó, Éva; Virág, László

2013-06-01

Screening of a small in-house library of 1863 compounds identified 29 compounds that protected Jurkat cells from hydrogen peroxide-induced cytotoxicity. From the cytoprotective compounds eleven proved to possess antioxidant activity (ABTS radical scavenger effect) and two were found to inhibit poly(ADP-ribosyl)ation (PARylation), a cytotoxic pathway operating in severely injured cells. Four cytoprotective dibenzoylmethane (DBM) derivatives were investigated in more detail as they did not scavenge hydrogen peroxide nor did they inhibit PARylation. These compounds protected cells from necrotic cell death while caspase activation, a parameter of apoptotic cell death was not affected. Hydrogen peroxide activated extracellular signal regulated kinase (ERK1/2) and p38 MAP kinases but not c-Jun N-terminal kinase (JNK). The cytoprotective DBMs suppressed the activation of Erk1/2 but not that of p38. Cytoprotection was confirmed in another cell type (A549 lung epithelial cells), indicating that the cytoprotective effect is not cell type specific. In conclusion we identified DBM analogs as a novel class of cytoprotective compounds inhibiting ERK1/2 kinase and protecting from necrotic cell death by a mechanism independent of poly(ADP-ribose) polymerase inhibition. Copyright © 2013 Elsevier Ltd. All rights reserved.

Tolerance to hypometabolism and arousal induced by hibernation in the apple snail Pomacea canaliculata (Caenogastropoda, Ampullariidae).

PubMed

Giraud-Billoud, Maximiliano; Castro-Vazquez, Alfredo; Campoy-Diaz, Alejandra D; Giuffrida, Pablo M; Vega, Israel A

2017-12-19

Pomacea canaliculata may serve as a model organism for comparative studies of oxidative damage and antioxidant defenses in active, hibernating and arousing snails. Oxidative damage (as TBARS), free radical scavenging capacity (as ABTS + oxidation), uric acid (UA) and glutathione (GSH) concentrations, activities of superoxide dismutase (SOD) and catalase (CAT), and the protein expression levels of heat shock proteins (Hsp70, Hsc70, Hsp90) were studied in digestive gland, kidney and foot. Tissue TBARS of hibernating snails (45days) was higher than active snails. Hibernation produced an increase of ABTS + in digestive gland, probably because of the sustained antioxidant defenses (UA and/or GSH and SOD levels). Kidney protection during the activity-hibernation cycle seemed provided by increased UA concentrations. TBARS in the foot remained high 30min after arousal with no changes in ABTS + , but this tissue increased ABTS + oxidation at 24h to expenses increased UA and decreased GSH levels, and with no changes in SOD and CAT activities. The level of Hsp70 in kidney showed no changes throughout the activity-hibernation cycle but it increased in the foot after hibernation. The tissue levels of Hsp90 in snails hibernating were higher than active snails and returned to baseline 24h after arousal. Results showed that chronic cooling produces a significant oxidative damage in three studied tissues and that these tissue damages are overcome quickly (between 30min to 24h) with fluctuations in different antioxidant defenses (UA, GSH, CAT) and heat shock proteins (Hsp70 and Hsp90). Copyright © 2017 Elsevier Inc. All rights reserved.

Investigation on flavonoid composition and anti free radical potential of Sida cordata.

PubMed

Shah, Naseer Ali; Khan, Muhammad Rashid; Ahmad, Bushra; Noureen, Farah; Rashid, Umbreen; Khan, Rahmat Ali

2013-10-22

Sida cordata, a member of Family Malvaceae is used in folk medicine for various ailments including liver diseases. In this study we investigated, its flavonoid constituents, in vitro antioxidant potential against different free radicals and hepatoprotection against carbon tetrachloride (CCl4)-induced liver damage in rat. Dried powder of S. cordata whole plant was extracted with methanol and the resultant (SCME) obtained was fractionated with escalating polarity to obtain n-hexane fraction (SCHE), ethyl acetate fraction (SCEE), n-butanol fraction (SCBE) and the remaining soluble portion as aqueous fraction (SCAE). Diverse in vitro antioxidants assays such as DPPH, H2O2, •OH, ABTS, β-carotene bleaching assay, superoxide radical, lipid peroxidation, reducing power, and total antioxidant capacity were studied to assess scavenging potential of methanol extract and its derived fractions. On account of marked scavenging activity SCEE was selected to investigate the hepatoprotective potential against CCl4 induced toxicity in Sprague-Dawley male rats by assessing the level of serum markers (alkaline phosphatase, alanine transaminase, aspartate transaminase, lactate dehydrogenase, bilirubin, and γ-glutamyltransferase) and of liver antioxidant enzymes such as catalase (CAT), superoxide dismutase (SOD), peroxidase (POD), glutathione-S-transfers (GST), glutathione reductase (GSR), glutathione peroxidase (GSH-Px), and reduced glutathione (GSH) and lipid peroxidation (TBARS). Histology of the liver was performed to study alteration in histoarchitecture. Existence of active flavonoids was established by thin layer chromatographic studies. Considerable amount of flavonoid and phenolic contents were recorded in the methanol extract and its derived fractions. Although the extract and all its derived fractions exhibited good antioxidant activities however, the most distinguished scavenging potential was observed for SCEE. Treatment of SCEE decreased the elevated level of serum marker enzymes induced with CCl4 administration whereas increased the activity of hepatic antioxidant enzymes (CAT, SOD, POD, GST, GSR and GSH-Px). Hepatic concentration of GSH was increased while lipid peroxidation was decreased with SCEE administration in CCl4 intoxicated rats. Presence of apigenin with some unknown compounds was observed in SCEE by using thin layer chromatography. These results revealed the presence of some bioactive compound in the ethyl acetate fraction, confirming the utility of S. cordata against liver diseases in folk medicine.

Heliotropium bacciferum Forssk. (Boraginaceae) extracts: chemical constituents, antioxidant activity and cytotoxic effect in human cancer cell lines.

PubMed

Aïssaoui, Hanane; Mencherini, Teresa; Esposito, Tiziana; De Tommasi, Nunziatina; Gazzerro, Patrizia; Benayache, Samir; Benayache, Fadila; Mekkiou, Ratiba

2018-02-12

Heliotropium bacciferum (Boraginaceae) is a perennial herb, growing in the Bechar region of Algeria, where it is traditionally used for skin diseases and tonsillitis. Herein, we report the isolation and characterization of sixteen secondary metabolites from the aerial part extracts. They include a sterol (1), megastigman type nor-isoprenoids (2, 3, 4, 6, 8, 10), C-11 terpene lactones (5 and 9), and a monoterpene (7) from the chloroform extract (HB-C); monoterpene glucoside (14), and phenolic compounds (11-13, 15, 16) from the methanol one (HB-M). Their structures were elucidated by spectroscopic methods including 1D and 2D NMR experiments, and ESIMS analysis. HB-M showed a significant and concentration dependent scavenging activity in vitro against the radicals DPPH and ABTS, related to the phenol derivatives (11-13, and 15-16), and HB-C inhibited the growth of colon cancer cell lines, mainly for the presence of the antiproliferative C-11 terpene lactones (5 and 9).

Antioxidant and α-glucosidase inhibitory ingredients identified from Jerusalem artichoke flowers.

PubMed

Wang, Yan-Ming; Zhao, Jian-Qiang; Yang, Jun-Li; Idong, Pema Tsering; Mei, Li-Juan; Tao, Yan-Duo; Shi, Yan-Ping

2017-11-09

Jerusalem artichoke (JA, Helianthus tuberosus L.) has been researched extensively due to its wide range of uses, but there are limited studies on its flowers. In this study, we report the first detailed phytochemical study on JA flowers, which yielded 21 compounds. Compound 4 was identified as a major water-soluble yellow pigment of JA flowers. In addition, the methanol extract of JA flowers and the isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Among the tested compounds, compound 13 showed the strongest ABTS + free radical scavenging activity with SC 50 value of 2.30 ± 0.13 μg/mL, and compound 6 showed most potent α-glucosidase inhibitory activity with inhibition rate of 60.0% ± 10.3% at a concentration of 250 μg/mL. Results showed that methanol extract of JA flowers exhibited antioxidant and α-glucosidase inhibitory activities which could be attributed to its phenolic ingredients including chlorogenic acid derivatives, flavonoids and phenols.

Degradation of anthracene by laccase of Trametes versicolor in the presence of different mediator compounds.

PubMed

Johannes, C; Majcherczyk, A; Hüttermann, A

1996-10-01

Laccase of Trametes versicolor was generally able to oxidize anthracene in vitro. After 72 h incubation about 35% of the anthracene was transformed stoichiometrically to 9,10-anthraquinone. Transformation of anthracene increased rapidly in the presence of different mediators that readily generate stable radicals: 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and 1-hydroxybenzotriazole. For the reaction, the presence of both the laccase and the mediator was necessary. In the presence of 0.005 mM 1-hydroxybenzotriazole this conversion had removed 47% of the anthracene after 72 h; 75% of the substrate was oxidized during this period when ABTS (1 mM) was used as mediator. In contrast to reactions without or with only low concentrations of a mediator, there was a discrepancy between the disappearance of anthracene and the formation of 9,10-anthraquinone in mediator-forced reactions. Coupling-products of mediators with anthracene degradation products were found. Anthracene disappeared nearly completely after incubation for 72 h with laccase in a 0.1 mM solution of 1-hydroxybenzotriazole and was transformed to 9,10-anthraquinone in about 80% yield; 90% of the substrate was transformed in the presence of ABTS (2.0 mM) resulting again in 80% quinone. Phenothiazine was not effective in this system.

Phenolic content and antioxidant activity of raspberry and blackberry cultivars.

PubMed

Sariburun, Esra; Sahin, Saliha; Demir, Cevdet; Türkben, Cihat; Uylaşer, Vildan

2010-05-01

Raspberry (Aksu Kirmizisi, Rubin, Newburgh, Hollanda Boduru, Heritage) and blackberry (Bursa 1, Bursa 2, Jumbo, Chester) cultivars were assayed for antioxidant activity (determined as 2,2-azino-di-[3-ethylbenzothialozine-sulphonic acid][ABTS], 2,2-diphenyl-1-picrylhydrazyl radical [DPPH], and cupric ion reducing antioxidant capacity [CUPRAC]), total phenol, total flavonoid, and total anthocyanin contents. In addition, 10 anthocyanins and anthocyanidins were determined in raspberry and blackberry by liquid chromatography-mass spectrometry (LC-MS/MS). Raspberry and blackberry had the highest ABTS, DPPH, CUPRAC, total phenol, and total flavonoid contents in methanol extracts, whereas total anthocyanin contents were the highest in water extracts. The antioxidant activity of the raspberry and blackberry was directly related to the total amount of phenolic compounds detected in the raspberry and blackberry. All antioxidant activity values were highly correlated with anthocyanin content in blackberry (0.93 < or = r < or = 0.99, P = 0.05). On the other hand, high correlation between total flavonoid content and antioxidant activity was recorded in water extract of blackberry (0.91 < or = r < or = 0.93, P = 0.05). ABTS value was highly correlated with total flavonoid content in methanol extract (r = 0.90), whereas total flavonoid content was relatively less correlated with DPPH (r = 0.85) and CUPRAC (r = 0.89).

Antioxidant activity of protein hydrolysates from raw and heat-treated yellow string beans (Phaseolus vulgaris L.).

PubMed

Karaś, Monika; Jakubczyk, Anna; Szymanowska, Urszula; Materska, Małgorzata; Zielińska, Ewelina

2014-01-01

Nowadays, legume plants have been considered not only a source of valuable proteins necessary for the proper functioning and growth of the body but also a source of bioactive compounds such as bioactive peptides, that may be beneficial to human health and protect against negative change in food. The aim of this study was to investigate the effect of heat treatment on the release of antioxidant peptides obtained by hydrolysis of the yellow string beans protein. The antioxidant properties of the hydrolysates were evaluated through free radical scavenging activities (DPPH and ABTS) and inhibition of iron activities (chelation of Fe2+). The results show that the heat treatment had influence on both increased peptides content and antioxidant activity after pepsin hydrolysis of string bean protein. The peptides content after protein hydrolysis derived from raw and heat treated beans were noted 2.10 and 2.50 mg·ml-1, respectively. The hydrolysates obtained from raw (PHR) and heat treated (PHT) beans showed better antioxidant properties than protein isolates (PIR and PIT). Moreover, the hydrolysates obtained from heat treated beans showed the higher ability to scavenge DPPH• (46.12%) and ABTS+• (92.32%) than obtained from raw beans (38.02% and 88.24%, correspondingly). The IC50 value for Fe2+ chelating ability for pepsin hydrolysates obtained from raw and heat treatment beans were noted 0.81 and 0.19 mg·ml-1, respectively. In conclusion, the results of this study showed that the heat treatment string beans caused increase in the antioxidant activities of peptide-rich hydrolysates.

Guava leaves polyphenolics-rich extract inhibits vital enzymes implicated in gout and hypertension in vitro.

PubMed

Irondi, Emmanuel Anyachukwu; Agboola, Samson Olalekan; Oboh, Ganiyu; Boligon, Aline Augusti; Athayde, Margareth Linde; Shode, Francis O

2016-01-01

Elevated uric acid level, an index of gout resulting from the over-activity of xanthine oxidase (XO), increases the risk of developing hypertension. However, research has shown that plant-derived inhibitors of XO and angiotensin 1-converting enzyme (ACE), two enzymes implicated in gout and hypertension, respectively, can prevent or ameliorate both diseases, without noticeable side effects. Hence, this study characterized the polyphenolics composition of guava leaves extract and evaluated its inhibitory effect on XO and ACE in vitro. The polyphenolics (flavonoids and phenolic acids) were characterized using high-performance liquid chromatography (HPLC) coupled with diode array detection (DAD). The XO, ACE, and Fe(2+)-induced lipid peroxidation inhibitory activities, and free radicals (2,2-diphenylpicrylhydrazyl [DPPH]* and 2,2´-azino-bis-3-ethylbenzthiazoline-6-sulphonic [ABTS]*(+)) scavenging activities of the extract were determined using spectrophotometric methods. Flavonoids were present in the extract in the order of quercetin > kaempferol > catechin > quercitrin > rutin > luteolin > epicatechin; while phenolic acids were in the order of caffeic acid > chlorogenic acid > gallic acids. The extract effectively inhibited XO, ACE and Fe(2+)-induced lipid peroxidation in a dose-dependent manner; having half-maximal inhibitory concentrations (IC50) of 38.24 ± 2.32 μg/mL, 21.06 ± 2.04 μg/mL and 27.52 ± 1.72 μg/mL against XO, ACE and Fe(2+)-induced lipid peroxidation, respectively. The extract also strongly scavenged DPPH* and ABTS*(+). Guava leaves extract could serve as functional food for managing gout and hypertension and attenuating the oxidative stress associated with both diseases.

Effect of hydrothermal processing on total polyphenolics and antioxidant potential of underutilized leafy vegetables, Boerhaavia diffusa and Portulaca oleracea

PubMed Central

Nagarani, Gunasekaran; Abirami, Arumugam; Nikitha, Prasad; Siddhuraju, Perumal

2014-01-01

Objective To investigate the effect of different processing methods on antioxidant properties of acetone extract of aerial parts from Boerhaavia diffusa and Portulaca oleracea. Methods The total phenolic and flavonoid contents were determined by Folin-Ciocalteau and aluminum chloride method, respectively. FRAP, metal chelating activity, DPPH, ABTS, nitric oxide, hydroxyl and superoxide radical scavenging activities, carotene/linoleic acid bleaching activity were used for the determination of antioxidant capacity. Results The total phenolics in Boerhaavia diffusa (82.79-162.80 mg GAE/g extract) were found to be higher when compared to that of Portulaca oleracea (22.94-10.02 mg GAE/g extract). Hydrothermal processing enhanced the level of inhibition on synthetic radicals such as DPPH (3 439-309 549 mmol TE/g extract) and ABTS (17 808-53 818 mmol TE/g extract) as well as biologically relevant radicals such as superoxide anion (70%-90%) and nitric oxide (49%-57%). In addition, boiling of the vegetables were found to be maximum capacity of FRAP (6 404.95 mmol Fe (II)/g extract) and metal chelating activity (1.53 mg EDTA/g extract) than the respective raw samples. Conclusions The present investigation suggests that the processing enhance the functionality and improves the availability of bioactive substances of these vegetables. In addition, they also exhibited more potent antioxidant activity. Therefore these natural weeds from the crop land ecosystem could be suggested as cost effective indigenous green vegetables for human diet and potential feed resources for animals. Further extensive studies on role and importance of those weeds in sustaining the agro biodiversity are also needed. PMID:25183131

Phytochemical analysis and antioxidants activities of aqueous stem bark extract of Schotia latifolia Jacq

PubMed Central

Mbaebie, BO; Edeoga, HO; Afolayan, AJ

2012-01-01

Objective To evaluate the phytochemical constituents and antioxidant activities of aqueous extract of Schotia latifolia (S. latifolia) bark locally used for the treatment of oxidative stress-induced ailments in South Africa. Methods The antioxidant and free radical scavenging activity of aqueous extract of the plant was assessed against 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide (NO), 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and the ferric reducing agent. Total phenolics, flavonoids, flavonols and proanthocyanidins were also determined to assess their corresponding effect on the antioxidant activity of this plant. Results The activities of plant extract against DPPH, ABTS and NO radicals were concentration dependent with IC50 value of 0.06, 0.05 and 0.05 mg/mL, respectively. The reducing power of the extract was greater than that of butylated hydroxyl toluene (BHT) and ascorbic acid which were used as standard drugs in a concentration dependent manner. The total phenolics content of the aqueous bark extract was (193.33±0.03 TE/g), followed by flavonoids (72.70±0.01 QE/g), proanthocyanidins (48.76±0.00 CE/g) and flavonols (47.76±0.21 QE/g). Phytochemical analysis revealed the presence of percentage tannin (11.40±0.02), alkaloid (9.80±0.01), steroids (18.20±0.01), glycosides (29.80±0.01) and saponins (6.80±0.00). The results exhibited a positive linear correlation between these polyphenols and the free radical scavenging activities. Conclusions Our findings provide evidence that the crude aqueous extract of S. latifolia is a potential source of natural antioxidants and this justifies its uses in folkloric medicines. PMID:23569880

Phenolic compounds from Citrus leaves: antioxidant activity and enzymatic browning inhibition.

PubMed

Khettal, Bachra; Kadri, Nabil; Tighilet, Karim; Adjebli, Ahmed; Dahmoune, Farid; Maiza-Benabdeslam, Fadila

2017-03-01

Background Phenolic compounds from Citrus are known to be a topic of many studies due to their biological properties including antioxidant activity. Methods Methanolic and aqueous extracts were isolated from Citrus leaves of different species (C. clementina, C. limon, C. hamlin, C. navel, C. aurantifolia, C. aurantium and C. grandis) harvested in Algeria. Results The results showed that aqueous extracts of all species are rich in total phenolic compounds and flavonoids (from 68.23 to 125.28 mg GAE/g DM) and (from 11.99 to 46.25 mg QE/g DM) respectively. The methanolic and aqueous extracts were examined for in vitro antioxidant properties using various antioxidant assays. For aqueous extracts, C. limon showed an important DPPH radical scavenging activity (IC50 35.35 µg/mL), and C. clementina exerted the highest ABTS radical scavenging activity (1,174.43 µM ET/g DM) and a significant ferric reducing potential (30.60 mg BHAE/g DM). For methanolic extracts, C. clementina showed the highest antioxidant activity for all the realized assays (IC50 41.85 µg/mL, 378.63 µM ET/g DM and 13.85 mg BHAE/g DM) for DPPH, ABTS radicals scavenging activities and ferric reducing potential respectively. Antiperoxidase and antipolyphenol oxidase activities of these samples were also evaluated. Conclusions In this investigation, the assessment of antiperoxidase activity proved that the leaves extracts of different species were able to inhibit peroxidase activity. However, this inhibition varied with the species and the source of these enzymes. On the other hand, the aqueous extracts of different species showed moderate inhibition of polyphenol oxidase, while no effect on these enzymes was obtained with methanolic extracts.

Chemical composition and antioxidant capacities of phytococktail extracts from trans-Himalayan cold desert

PubMed Central

2013-01-01

Background Himalayan plants are widely used in traditional system of medicine both as prophylactics and therapeutics for high altitude maladies. Our aim was to evaluate the antioxidant capacities and bioactive compounds of methanol and n-hexane extracts of the phytococktail comprising of sea buckthorn (Hippophae rhamnoides), apricot (Prunus armeniaca) and roseroot (Rhodiola imbricata) from trans-Himalaya. Methods The 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and nitric oxide (NO) radical scavenging capacities and lipid peroxidation inhibition (LPI) property of the extracts were determined. Total antioxidant power was determined by ferric reducing/antioxidant power (FRAP) assay. Total polyphenol, flavonoid, flavonol, proanthocyanidin and carotenoid were also estimated for both extracts. We have identified and quantified the phyto-chemotypes present in the methanol and n-hexane extracts by hyphenated gas chromatography/mass spectrometry (GC/MS) technique. Results Antioxidant capacity assays using DPPH, ABTS, NO, LPI and FRAP exhibited analogous results where the phytococktail showed high antioxidant action. The phytococktail was also found to possess high quantity of total polyphenol, flavonoid, flavonol and carotenoid. A significant and linear correlation was found between the antioxidant capacities and bioactive principles. A total of 32 phyto-chemotypes were identified from these extracts by GC/MS chemometric fingerprinting. Major phyto-chemotypes identified by GC/MS were glycosides, phenylpropanoids and derivatives, terpenoids, alkaloids, phytosterols, fatty acids and esters, alkaloids and derivatives, organic acid esters and aromatic ethers with positive biological and pharmacological actions. Conclusion The phytococktail extracts were found to contain considerable amount of diverse bioactive compounds with high antioxidant capacities. The presence of hydrophilic and lipophilic antioxidants in the phytococktail could have contributed to the higher antioxidant values. Hence, the phytococktail could be used as natural source of antioxidants to ameliorate disorders associated with oxidative stress. PMID:24098968

Optimal binary solvent extraction system for phenolic antioxidants from mengkudu (Morinda citrifolia) fruit.

PubMed

Thoo, Yin Yin; Ho, Swee Kheng; Abas, Faridah; Lai, Oi Ming; Ho, Chun Wai; Tan, Chin Ping

2013-06-14

Antioxidants have been widely used in the food industry to enhance product quality by preventing oxidation of susceptible substances. This work was carried out to maximise the recovery of total phenolic content (TPC), total flavonoid content (TFC), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical-scavenging capacity and 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging capacity from Morinda citrifolia fruit via modification of the ethanol concentration, extraction time and extraction temperature at minimal processing cost. The optimised conditions yielded values of 881.57 ± 17.74 mg GAE/100 g DW for TPC, 552.53 ± 34.16 mg CE/100 g DW for TFC, 799.20 ± 2.97 µmol TEAC/100 g DW for ABTS and 2,317.01 ± 18.13 µmol TEAC/100 g DW for DPPH were 75% ethanol, 40 min of time and 57 °C. The four responses did not differ significantly (p > 0.05) from predicted values, indicating that models obtained are suitable to the optimisation of extraction conditions for phenolics from M. citrifolia. The relative amounts of flavonoids were 0.784 ± 0.01 mg quercetin/g of extract and 1.021 ± 0.04 mg rutin/g of extract. On the basis of the results obtained, M. citrifolia extract can be used as a valuable bioactive source of natural antioxidants.

Cooking Characteristics and Antioxidant Activity of Rice-Barley Mix at Different Cooking Method and Mixing Ratio.

PubMed

Woo, Koan Sik; Kim, Hyun-Joo; Lee, Ji Hae; Ko, Jee Yeon; Lee, Byong Won; Lee, Byoung Kyu

2018-03-01

This study aimed to compare the phenolic compounds and antioxidant activity of barley at different proportion (0, 5, 10, 15, and 20%), and using different cooking methods. The grains used in this experiment are barley ( Hordeum vulgare L. cv. Huinchalssal) and Samkwang rice. The rice-barley mixture was cooked using general and high pressure cooking methods with and without fermented alcohol. The quality characteristics such as water binding capacity, pasting characteristic, water solubility, and swelling power of different proportions of barley were evaluated. The antioxidant characteristics evaluated are total polyphenol, flavonoid contents, 2,2-diphenyl-1-picrylhydrazyl (DPPH), and 2,2-azinobis(3-ethylbenothiazoline-6-sulphonic acid) (ABTS) diammonium salt radical scavenging activities. Results showed that peak [195.0~184.0 rapid visco units (RVU)], trough (130.0~116.2 RVU), final (252.0~221.8 RVU), and setback viscosity (57.0~37.5 RVU) decreased correspondingly with the increase in the amount of barley. Water binding capacity (187.31~136.01%) and swelling power (162.37~127.58%) decreased as amounts of barley increases, however the water solubility (5.35~6.89%) increased. Moreover, the total polyphenol and flavonoid, and the DPPH and ABTS radical scavenging activities contents increased as the amounts of barley in the mixture increases. This study generally aims to provide useful information for the manufacturing of processed products.

Molecular structure, quantum mechanical calculation and radical scavenging activities of (E)-4,6-dibromo-2-[(3,5-dimethylphenylimino)methyl]-3-methoxyphenol and (E)-4,6-dibromo-2-[(2,6-dimethylphenylimino)methyl]-3-methoxyphenol compounds.

PubMed

Alaşalvar, Can; Soylu, Mustafa Serkan; Güder, Aytaç; Albayrak, Çiğdem; Apaydın, Gökhan; Dilek, Nefise

2014-09-15

In this study, (E)-4,6-dibromo-2-[(3,5-dimethylphenylimino)methyl]-3-methoxyphenol and (E)-4,6-dibromo-2-[(2,6-dimethylphenylimino)methyl]-3-methoxyphenol compounds have been synthesized and characterized by using X-ray crystallographic method, FT-IR and Density functional method. The molecular geometry, vibrational frequencies of the title compounds in the ground state have been calculated by using B3LYP with the 6-31G(d,p) basis set. The tautomeric form of the compounds has been demonstrated by using single crystal X-ray method, FT-IR spectrometer and DFT method. In addition, HOMO-LUMO energy gap, molecular electrostatic potential map and NBO analysis of the compounds are performed at B3LYP/6-31G(d,p) level. It may be remarked that the free radical scavenging activities of the title compounds were assessed using DPPH, DMPD+, and ABTS+ assays. The obtained results show that especially compound 2 has effective DPPH (SC50 1.52±0.14 μg/mL), DMPD+ (SC50 1.22±0.21 μg/mL), and ABTS+ (SC50 3.32±0.17 μg/mL) scavenging activities compared with standards (BHA, rutin, and trolox). Copyright © 2014 Elsevier B.V. All rights reserved.

In vitro antioxidant and antiproliferative activities of selenium-containing phycocyanin from selenium-enriched Spirulina platensis.

PubMed

Chen, Tianfeng; Wong, Yum-Shing

2008-06-25

Both selenium and phycocyanin have been reported to show potent cancer chemopreventive activities. In this study, we investigated the in vitro antioxidant and antiproliferative activities of selenium-containing phycocyanin (Se-PC) purified from selenium-enriched Spirulina platensis. The antioxidant activity of Se-PC was evaluated by using four different free radical scavenging assays, namely, the 2,2'-azinobis-3-ethylbenzothiazolin-6-sulfonic acid (ABTS) assay, 1,1-diphenyl-2-picryhydrazyl (DPPH) assay, superoxide anion scavenging assay, and erythrocyte hemolysis assay. The results indicated that Se-PC exhibited stronger antioxidant activity than phycocyanin by scavenging ABTS, DPPH, superoxide anion, and 2,2'-azobis-(2-amidinopropane)dihydrochloride free radicals. Se-PC also showed dose-dependent protective effects on erythrocytes against H 2O 2-induced oxidative DNA damage as evaluated by the Comet assay. Moreover, Se-PC was identified as a potent antiproliferative agent against human melanoma A375 cells and human breast adenocarcinoma MCF-7 cells. Induction of apoptosis in both A375 and MCF-7 cells by Se-PC was evidenced by accumulation of sub-G1 cell populations, DNA fragmentation, and nuclear condensation. Further investigation on intracellular mechanisms indicated that depletion of mitochondrial membrane potential (DeltaPsi m) was involved in Se-PC-induced cell apoptosis. Our findings suggest that Se-PC is a promising organic Se species with potential applications in cancer chemoprevention.

Biguanides sensitize leukemia cells to ABT-737-induced apoptosis by inhibiting mitochondrial electron transport

PubMed Central

Velez, Juliana; Pan, Rongqing; Lee, Jason T.C.; Enciso, Leonardo; Suarez, Marta; Duque, Jorge Eduardo; Jaramillo, Daniel; Lopez, Catalina; Morales, Ludis; Bornmann, William; Konopleva, Marina; Krystal, Gerald; Andreeff, Michael; Samudio, Ismael

2016-01-01

Metformin displays antileukemic effects partly due to activation of AMPK and subsequent inhibition of mTOR signaling. Nevertheless, Metformin also inhibits mitochondrial electron transport at complex I in an AMPK-independent manner, Here we report that Metformin and rotenone inhibit mitochondrial electron transport and increase triglyceride levels in leukemia cell lines, suggesting impairment of fatty acid oxidation (FAO). We also report that, like other FAO inhibitors, both agents and the related biguanide, Phenformin, increase sensitivity to apoptosis induction by the bcl-2 inhibitor ABT-737 supporting the notion that electron transport antagonizes activation of the intrinsic apoptosis pathway in leukemia cells. Both biguanides and rotenone induce superoxide generation in leukemia cells, indicating that oxidative damage may sensitize toABT-737 induced apoptosis. In addition, we demonstrate that Metformin sensitizes leukemia cells to the oligomerization of Bak, suggesting that the observed synergy with ABT-737 is mediated, at least in part, by enhanced outer mitochondrial membrane permeabilization. Notably, Phenformin was at least 10-fold more potent than Metformin in abrogating electron transport and increasing sensitivity to ABT-737, suggesting that this agent may be better suited for targeting hematological malignancies. Taken together, our results suggest that inhibition of mitochondrial metabolism by Metformin or Phenformin is associated with increased leukemia cell susceptibility to induction of intrinsic apoptosis, and provide a rationale for clinical studies exploring the efficacy of combining biguanides with the orally bioavailable derivative of ABT-737, Venetoclax. PMID:27283492

Biguanides sensitize leukemia cells to ABT-737-induced apoptosis by inhibiting mitochondrial electron transport.

PubMed

Velez, Juliana; Pan, Rongqing; Lee, Jason T C; Enciso, Leonardo; Suarez, Marta; Duque, Jorge Eduardo; Jaramillo, Daniel; Lopez, Catalina; Morales, Ludis; Bornmann, William; Konopleva, Marina; Krystal, Gerald; Andreeff, Michael; Samudio, Ismael

2016-08-09

Metformin displays antileukemic effects partly due to activation of AMPK and subsequent inhibition of mTOR signaling. Nevertheless, Metformin also inhibits mitochondrial electron transport at complex I in an AMPK-independent manner, Here we report that Metformin and rotenone inhibit mitochondrial electron transport and increase triglyceride levels in leukemia cell lines, suggesting impairment of fatty acid oxidation (FAO). We also report that, like other FAO inhibitors, both agents and the related biguanide, Phenformin, increase sensitivity to apoptosis induction by the bcl-2 inhibitor ABT-737 supporting the notion that electron transport antagonizes activation of the intrinsic apoptosis pathway in leukemia cells. Both biguanides and rotenone induce superoxide generation in leukemia cells, indicating that oxidative damage may sensitize toABT-737 induced apoptosis. In addition, we demonstrate that Metformin sensitizes leukemia cells to the oligomerization of Bak, suggesting that the observed synergy with ABT-737 is mediated, at least in part, by enhanced outer mitochondrial membrane permeabilization. Notably, Phenformin was at least 10-fold more potent than Metformin in abrogating electron transport and increasing sensitivity to ABT-737, suggesting that this agent may be better suited for targeting hematological malignancies. Taken together, our results suggest that inhibition of mitochondrial metabolism by Metformin or Phenformin is associated with increased leukemia cell susceptibility to induction of intrinsic apoptosis, and provide a rationale for clinical studies exploring the efficacy of combining biguanides with the orally bioavailable derivative of ABT-737, Venetoclax.

Developing energy efficient lignin biomass processing - towards understanding mediator behaviour in ionic liquids.

PubMed

Eshtaya, Majd; Ejigu, Andinet; Stephens, Gill; Walsh, Darren A; Chen, George Z; Croft, Anna K

2016-08-15

Environmental concerns have brought attention to the requirement for more efficient and renewable processes for chemicals production. Lignin is the second most abundant natural polymer, and might serve as a sustainable resource for manufacturing fuels and aromatic derivatives for the chemicals industry after being depolymerised. In this work, the mediator 2,2'-azino-bis(3-ethylbenthiazoline-6-sulfonic acid) diammonium salt (ABTS), commonly used with enzyme degradation systems, has been evaluated by means of cyclic voltammetry (CV) for enhancing the oxidation of the non-phenolic lignin model compound veratryl alcohol and three types of lignin (organosolv, Kraft and lignosulfonate) in the ionic liquid 1-ethyl-3-methylimidazolium ethyl sulfate, ([C2mim][C2SO4]). The presence of either veratryl alcohol or organosolv lignin increased the second oxidation peak of ABTS under select conditions, indicating the ABTS-mediated oxidation of these molecules at high potentials in [C2mim][C2SO4]. Furthermore, CV was applied as a quick and efficient way to explore the impact of water in the ABTS-mediated oxidation of both organosolv and lignosulfonate lignin. Higher catalytic efficiencies of ABTS were observed for lignosulfonate solutions either in sodium acetate buffer or when [C2mim][C2SO4] (15 v/v%) was present in the buffer solution, whilst there was no change found in the catalytic efficiency of ABTS in [C2mim][C2SO4]-lignosulfonate mixtures relative to ABTS alone. In contrast, organosolv showed an initial increase in oxidation, followed by a significant decrease on increasing the water content of a [C2mim][C2SO4] solution.

Phase I safety, pharmacokinetic, and pharmacodynamic study of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 in patients with advanced cancer.

PubMed

Hoekstra, Ronald; de Vos, Filip Y F L; Eskens, Ferry A L M; Gietema, Jourik A; van der Gaast, Ate; Groen, Harry J M; Knight, Raymond A; Carr, Robert A; Humerickhouse, Rod A; Verweij, Jaap; de Vries, Elisabeth G E

2005-08-01

ABT-510 is an angiogenesis inhibitor derived from thrombospondin-1, a naturally occurring inhibitor of angiogenesis. We investigated ABT-510, which was administered subcutaneously in patients with advanced solid malignancies, to assess safety, pharmacokinetics, and serum markers of angiogenesis. ABT-510 was administered subcutaneously as a continuous infusion (100 mg/24 h) and bolus injections (100, 200, and 260 mg once daily; 50 and 100 mg twice daily) in 28-day cycles. Thirty-nine patients received a total of 144 treatment cycles. Administration by continuous infusion was hampered by the onset of painful skin infiltrates at the injection site. In the bolus injection regimens, the most common toxicities observed were mild injection-site reactions and fatigue. Maximum-tolerated dose was not defined, but 260 mg was defined as the maximum clinically practical dose. ABT-510 pharmacokinetics were linear across the dosage ranges tested, and the potential therapeutic threshold (plasma concentrations > 100 ng/mL > 3 h/d) was achieved with all dose regimens. Median serum basic fibroblast growth factor (bFGF) levels decreased from 14.1 pg/mL (range, 0.5 to 77.7 pg/mL) at baseline to 3.2 pg/mL (range, 0.2 to 29.4 pg/mL) after 56 days of treatment (P = .003). No correlations with time on study or ABT-510 dose or exposure were observed for individual changes in bFGF. Stable disease lasting for six cycles or more was seen in six patients. ABT-510 demonstrated a favorable toxicity profile and linear and time-independent pharmacokinetics with biologically relevant plasma concentrations. The significant number of patients with prolonged stable disease and the convenient method of dosing merit further studies with this angiogenesis inhibitor.

ABT-510, a modified type 1 repeat peptide of thrombospondin, inhibits malignant glioma growth in vivo by inhibiting angiogenesis.

PubMed

Anderson, Joshua C; Grammer, J Robert; Wang, Wenquan; Nabors, L Burton; Henkin, Jack; Stewart, Jerry E; Gladson, Candece L

2007-03-01

Anti-angiogenic therapies would be particularly beneficial in the treatment of malignant gliomas. Peptides derived from the second type 1 repeat (TSR) of thrombospondin-1 (TSP-1) have been shown to inhibit angiogenesis in non-glioma tumor models and a modified TSR peptide, ABT-510, has now entered into Phase II clinical trials of its efficacy in non-glioma tumors. As microvascular endothelial cells (MvEC) exhibit heterogeneity, we evaluated the ability of the modified TSR peptide (NAcSarGlyValDallolleThrNvalleArgProNHE, ABT-510) to inhibit malignant glioma growth in vivo and to induce apoptosis of brain microvessel endothelial cells (MvEC) propagated in vitro. We found that daily administration of ABT-510 until euthanasia (days 7 to 19), significantly inhibited the growth of human malignant astrocytoma tumors established in the brain of athymic nude mice. The microvessel density was significantly lower and the number of apoptotic MvEC was significantly higher (3-fold) in the tumors of the ABT-510-treated animals. Similar results were found using a model in which the established tumor is an intracerebral malignant glioma propagated in a syngeneic mouse model. ABT-510 treatment of primary human brain MvEC propagated as a monolayer resulted in induction of apoptosis in a dose- and time-dependent manner through a caspase-8-dependent mechanism. It also inhibited tubular morphogenesis of MvEC propagated in collagen gels in a dose- and caspase-8 dependent manner through a mechanism that requires the TSP-1 receptor (CD36) on the MvEC. These findings indicate that ABT-510 should be evaluated as a therapeutic option for patients with malignant glioma.

Advances in the analytical methods for determining the antioxidant properties of honey: a review.

PubMed

Moniruzzaman, M; Khalil, M I; Sulaiman, S A; Gan, S H

2012-01-01

Free radicals and reactive oxygen species (ROS) have been implicated in contributing to the processes of aging and disease. In an effort to combat free radical activity, scientists are studying the effects of increasing individuals' antioxidant levels through diet and dietary supplements. Honey appears to act as an antioxidant in more ways than one. In the body, honey can mop up free radicals and contribute to better health. Various antioxidant activity methods have been used to measure and compare the antioxidant activity of honey. In recent years, DPPH (Diphenyl-1-picrylhydrazyl), FRAP (Ferric Reducing Antioxidant Power), ORAC (The Oxygen Radical Absorbance Capacity), ABTS [2, 2-azinobis (3ehtylbenzothiazoline-6-sulfonic acid) diamonium salt], TEAC [6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-carboxylic acid (Trolox)-equivalent antioxidant capacity] assays have been used to evaluate antioxidant activity of honey. The antioxidant activity of honey is also measured by ascorbic acid content and different enzyme assays like Catalase (CAT), Glutathione Peroxidase (GPO), Superoxide Dismutase (SOD). Among the different methods available, methods that have been validated, standardized and widely reported are recommended.

New antioxidants from the culture broth of Hericium coralloides.

PubMed

Kim, Ji-Yul; Woo, E-Eum; Lee, In-Kyoung; Yun, Bong-Sik

2018-05-17

In our effort to find antioxidants from the higher fungi, we isolated three new compounds (1-3) with a known compound, spirobenzofuran (4), from the culture broth of Hericium coralloides. Bioassay-guided fractionation led to the isolation of these compounds, and we determined the chemical structures through spectroscopic methods. These compounds exhibited antioxidant activity in the range of IC 50 values of 29-66 μM in the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging assay.

Protective effect of Pterostilbene against free radical mediated oxidative damage

PubMed Central

2013-01-01

Background Pterostilbene, a methoxylated analog of Resveratrol, is gradually gaining more importance as a therapeutic drug owing to its higher lipophilicity, bioavailability and biological activity than Resveratrol. This study was undertaken to characterize its ability to scavenge free radicals such as superoxide, hydroxyl and hydrogen peroxide and to protect bio-molecules within a cell against oxidative insult. Methods Anti-oxidant activity of Pterostilbene was evaluated extensively by employing several in vitro radical scavenging/inhibiting assays and pulse radiolysis study. In addition, its ability to protect rat liver mitochondria against tertiary-butyl hydroperoxide (TBHP) and hydroxyl radical generated oxidative damage was determined by measuring the damage markers such as protein carbonyls, protein sulphydryls, lipid hydroperoxides, lipid peroxides and 8-hydroxy-2'-deoxyguanosine. Pterostilbene was also evaluated for its ability to inhibit •OH radical induced single strand breaks in pBR322 DNA. Result Pterostilbene exhibited strong anti-oxidant activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide in a concentration dependent manner. Pterostilbene conferred protection to proteins, lipids and DNA in isolated mitochondrial fractions against TBHP and hydroxyl radical induced oxidative damage. It also protected pBR322 DNA against oxidative assault. Conclusions Thus, present study provides an evidence for the strong anti-oxidant property of Pterostilbene, methoxylated analog of Resveratrol, thereby potentiating its role as an anti-oxidant. PMID:24070177

Evaluation of free radical scavenging and anti-oxidative capacity of polydatin-nanostructured lipid carriers

NASA Astrophysics Data System (ADS)

Meng, Xiang-Ping; Shi, Fan; Li, Hai-Jie; Yin, Li-De; Wang, Yi-Fei; Wang, Zhi-ping; Chen, Tong-sheng

2016-10-01

Cellular damage induced by free-radicals like reactive oxygen species has been implicated in several diseases. 2, 2-azobis(2-amidino-propane) dihydrochloride(AAPH) generates two potent ROS capable of inducing lipid peroxidation: alkoxy radical(RO-) and peroxy radical (ROO-). These radicals are similar to those that are physiologically active and thus might initiate a cascade of intracellular toxic events leading to oxidation, lipid peroxidation, DNA damage and subsequent cell death. Hence naturally anti-oxidant play a vital role in combating these conditions. In this study, polydatin loaded nanostructured lipid carriers (Pol-NLC) was prepared by hot melting and then high pressure homogenization technique. The effects of Pol-NLC on free radical scavenging and anti-oxidative capacity is investigated. The particle size and zeta potential of Pol-NLC were 113.9 +/- 1.1 nm and -16.3 1 +/- 0.27 mV, respectively. By free radical scavenging assays, the IC50 value of Pol-NLC were 28.71, 9.83 μg/mL with DPPH, ABTS assay respectively, and 0.143 mg ferrous sulfate/1 mg Pol-NLC with FRAP assay. These results indicated that the antioxidant properties of Pol-NLC hold great potential used as an alternative to more toxic synthetic anti-oxidants as an additive in food, cosmetic and pharmaceutical preparations for the oxidative diseases treatment.

Antioxidant Capacity, Cytotoxicity and Antimycobacterial Activity of Madeira Archipelago Endemic Helichrysum Dietary and Medicinal Plants.

PubMed

Gouveia-Figueira, Sandra C; Gouveia, Carla A; Carvalho, Maria J; Rodrigues, Ana I; Nording, Malin L; Castilho, Paula C

2014-10-31

The potential bioactivity of dietary and medicinal endemic Helichrysum plants from Madeira Archipelago was explored, for the first time, in order to supply new information for the general consumer. In vitro antioxidant properties were investigated using DPPH, ABTS(•+), FRAP and β-Carotene assays, and the total phenolic content (TPC) and total flavonoid content (TFC) were also determined. Although the results generally showed a large variation among the three analyzed plants, the methanolic extracts showed the highest antioxidant capacity. Exception is made for H. devium n-hexane extract that showed good radical scavenger capacity associated to compounds with good reducing properties. In the Artemia salina toxicity assay and antimycobaterial activity, H. devium was the most potent plant with the lowest LD50 at 216.7 ± 10.4 and MIC ≤ 50 μg·mL(-1). Chemometric evaluation (Principal Component Analysis-PCA) showed close interdependence between the ABTS, TPC and TFC methods and allowed to group H. devium samples.

A phase I study of ABT-510 plus bevacizumab in advanced solid tumors.

PubMed

Uronis, Hope E; Cushman, Stephanie M; Bendell, Johanna C; Blobe, Gerard C; Morse, Michael A; Nixon, Andrew B; Dellinger, Andrew; Starr, Mark D; Li, Haiyan; Meadows, Kellen; Gockerman, Jon; Pang, Herbert; Hurwitz, Herbert I

2013-06-01

Targeting multiple regulators of tumor angiogenesis have the potential to improve treatment efficacy. Bevacizumab is a monoclonal antibody directed against vascular endothelial growth factor and ABT-510 is a synthetic analog of thrombospondin, an endogenous angiogenesis inhibitor. Dual inhibition may result in additional benefit. We evaluated the safety, tolerability, and efficacy of the combination of bevacizumab plus ABT-510 in patients with refractory solid tumors. We also explored the effects of these agents on plasma-based biomarkers and wound angiogenesis. Thirty-four evaluable subjects were enrolled and received study drug. Therapy was well tolerated; minimal treatment-related grade 3/4 toxicity was observed. One patient treated at dose level 1 had a partial response and five other patients treated at the recommended phase II dose had prolonged stable disease for more than 1 year. Biomarker evaluation revealed increased levels of D-dimer, von Willebrand factor, placental growth factor, and stromal-derived factor 1 in response to treatment with the combination of bevacizumab and ABT-510. Data suggest that continued evaluation of combination antiangiogenesis therapies may be clinically useful.

Optimizing Extraction Conditions of Free and Bound Phenolic Compounds from Rice By-Products and Their Antioxidant Effects.

PubMed

Irakli, Maria; Kleisiaris, Fotis; Kadoglidou, Kalliopi; Katsantonis, Dimitrios

2018-06-13

Rice by-products are extensively abundant agricultural wastes from the rice industry. This study was designed to optimize experimental conditions for maximum recovery of free and bound phenolic compounds from rice by-products. Optimized conditions were determined using response surface methodology based on total phenolic content (TPC), ABTS radical scavenging activity and ferric reducing power (FRAP). A Box-Behnken design was used to investigate the effects of ethanol concentration, extraction time and temperature, and NaOH concentration, hydrolysis time and temperature for free and bound fractions, respectively. The optimal conditions for the free phenolics were 41⁻56%, 40 °C, 10 min, whereas for bound phenolics were 2.5⁻3.6 M, 80 °C, 120 min. Under these conditions free TPC, ABTS and FRAP values in the bran were approximately 2-times higher than in the husk. However, bound TPC and FRAP values in the husk were 1.9- and 1.2-times higher than those in the bran, respectively, while bran fraction observed the highest ABTS value. Ferulic acid was most evident in the bran, whereas p -coumaric acid was mostly found in the husk. Findings from this study demonstrates that rice by-products could be exploited as valuable sources of bioactive components that could be used as ingredients of functional food and nutraceuticals.

Antioxidant availability of turmeric in relation to its medicinal and culinary uses.

PubMed

Tilak, Jai C; Banerjee, Meenal; Mohan, Hari; Devasagayam, T P A

2004-10-01

Turmeric (Curcuma longa) has been used in Indian cooking, and in herbal remedies. Its possible mechanism of action was examined in terms of antioxidant availability during actual cooking conditions and in therapeutic applications using standardized extracts. The assays involve different levels of antioxidant action such as oxygen radical absorbance capacity (ORAC), radical scavenging abilities using 1,1-diphenyl-2-picryl hydrazyl (DPPH), 2,2'-azobis-3-ethylbenzthiazoline-6-sulfonic acid (ABTS), ferric reducing antioxidant power (FRAP) and protection of membranes examined by inhibition of lipid peroxidation besides the content of phenols and total flavonoids. The aqueous and ethanol extracts of two major preparations of turmeric, corresponding to its use in cooking and medicine, showed significant antioxidant abilities. In conclusion, the studies reveal that the ability of turmeric to scavenge radicals, reduce iron complex and inhibit peroxidation may explain the possible mechanisms by which turmeric exhibits its beneficial effects in relation to its use in cooking and medicine. Copyright 2004 John Wiley & Sons, Ltd.

Comparative antioxidant activity of edible Japanese brown seaweeds.

PubMed

Airanthi, M K Widjaja-Adhi; Hosokawa, Masashi; Miyashita, Kazuo

2011-01-01

Japanese edible brown seaweeds, Eisenia bicyclis (Arame), Kjellmaniella crassifolia (Gagome), Alaria crassifolia (Chigaiso), Sargassum horneri (Akamoku), and Cystoseira hakodatensis (Uganomoku) were assayed for total phenolic content (TPC), fucoxanthin content, radical scavenging activities (DPPH, peroxyl radical, ABTS, and nitric oxide), and antioxidant activity in a liposome system. Among the solvents used for extraction, methanol was the most effective to extract total phenolics (TPC) from brown seaweeds. Among 5 kinds of brown seaweeds analyzed, methanol extract from C. hakodatensis was the best source for antioxidants. The high antioxidant activity of the extract was based not only on the high content of phenolics, but on the presence of fucoxanthin. No significant correlation (P > 0.05) was observed between TPC per gram extract with DPPH radical scavenging activity of the methanol extracts. These observed discrepancy would be due to structural variations in the phenolic compounds, and different levels of fucoxanthin in the extracts. The present study also demonstrated the synergy in the antioxidant activity of the combination of brown seaweed phenolics and fucoxanthin.

Characterisation of the antioxidant effects of Aesculus hippocastanum L. bark extract on the basis of radical scavenging activity, the chemiluminescence of human neutrophil bursts and lipoperoxidation assay.

PubMed

Braga, P C; Marabini, L; Wang, Y Y; Lattuada, N; Calò, R; Bertelli, A; Falchi, M; Dal Sasso, M; Bianchi, T

2012-07-01

Oxidative stress is increasingly recognised as a pivotal factor that plays a number of roles in the inflammatory response to environmental signals. It has been claimed that Aesculus hippocastanum extracts have antioxidant and anti-inflammatory activity, but these claims are mainly based on the results of chemical reactions and folk-medicine. The aim of this study was to examine whether a bark extract of Aesculus hippocastanum interferes with reactive oxygen/nitrogen species (ROS/RNS) during the course of human neutrophil respiratory bursts, and to establish the lowest concentration at which it still has antioxidant activity by means of luminol amplified chemiluminescence (LACL). We also studied its ability to counteract lipid peroxidation (LPO) in human cells. Before investigating its antioxidant effects on human cells, we analysed its scavenging activity against ABTS*+, hydroxyl radical, superoxide anion, and Fremy's salt (those last three by means of electron paramagnetic resonance (EPR) spectrometry). The extract of Aesculus hippocastanum exerted its anti-ROS/RNS activity in a concentration-dependent manner with significant effects being observed for even very low concentrations: 10 microg/ml without L-Arg, and 5 microg/ml when L-Arg was added to the fMLP test. The LPO assay confirmed these results, which were paralleled by the EPR study. These findings are interesting for improving the antioxidant network and restoring redox balance in human cells, and extend the possibility of using plant-derived molecules to antagonise the oxidative stress generated in living organisms when the balance is in favour of free radicals as a result of the depletion of cell antioxidants.

Extractability of polyphenols from black currant, red currant and gooseberry and their antioxidant activity.

PubMed

Laczkó-Zöld, Eszter; Komlósi, Andrea; Ülkei, Timea; Fogarasi, Erzsébet; Croitoru, Mircea; Fülöp, Ibolya; Domokos, Erzsébet; Ştefănescu, Ruxandra; Varga, Erzsébet

2018-06-01

In this study, we analyzed extracts of Ribes (black currant, red currant and gooseberry) fruits obtained with methanol, methanol 50% and water. For each extract total polyphenol content, total flavonoid content and total anthocyanin content was assessed. The antioxidant activity of extracts was evaluated by 1,1-Diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging capacity and by the photo-chemiluminescence (PCL) method. Identification and quantification of individual phenolic compounds was performed by means of high performance liquid chromatograph coupled with diode array detector (HPLC-DAD) analyses. From each fruit, best extraction of polyphenols was obtained with methanol 50%. In case of red currants and gooseberry there was no significant difference in flavonoids and anthocyanins extraction rate by the different extraction solvents. For black currants the methanol and methanol 50% extract presented the highest antioxidant activity. For red currants extracts with methanol 50% showed stronger antioxidant activity (IC 50 = 5.71 mg/ml for DPPH, IC 50 = 1.17 mg/ml for ABTS) than those with methanol or water. In case of gooseberry by the DPPH test the water extract proved to be the most active (IC 50 = 5.9 mg/ml). In the PCL test black currants methanol 50% extract was over 6 times more powerful as the ones from red currants. In case of gooseberries, water extract presented the highest antioxidant activity (41.84 μmol AAE/g). In black currant cyanidin-3-glucoside was the major compound. Quercetin 3-O-glucoside was identified in each sample. From cinnamic acid derivatives neochlorogenic acid was present in black currants in the highest amount (356.33 μg/g).

Guava leaves polyphenolics-rich extract inhibits vital enzymes implicated in gout and hypertension in vitro

PubMed Central

Irondi, Emmanuel Anyachukwu; Agboola, Samson Olalekan; Oboh, Ganiyu; Boligon, Aline Augusti; Athayde, Margareth Linde; Shode, Francis O.

2016-01-01

Background/Aim: Elevated uric acid level, an index of gout resulting from the over-activity of xanthine oxidase (XO), increases the risk of developing hypertension. However, research has shown that plant-derived inhibitors of XO and angiotensin 1-converting enzyme (ACE), two enzymes implicated in gout and hypertension, respectively, can prevent or ameliorate both diseases, without noticeable side effects. Hence, this study characterized the polyphenolics composition of guava leaves extract and evaluated its inhibitory effect on XO and ACE in vitro. Materials and Methods: The polyphenolics (flavonoids and phenolic acids) were characterized using high-performance liquid chromatography (HPLC) coupled with diode array detection (DAD). The XO, ACE, and Fe2+-induced lipid peroxidation inhibitory activities, and free radicals (2,2-diphenylpicrylhydrazyl [DPPH]* and 2,2´-azino-bis-3-ethylbenzthiazoline-6-sulphonic [ABTS]*+) scavenging activities of the extract were determined using spectrophotometric methods. Results: Flavonoids were present in the extract in the order of quercetin > kaempferol > catechin > quercitrin > rutin > luteolin > epicatechin; while phenolic acids were in the order of caffeic acid > chlorogenic acid > gallic acids. The extract effectively inhibited XO, ACE and Fe2+-induced lipid peroxidation in a dose-dependent manner; having half-maximal inhibitory concentrations (IC50) of 38.24 ± 2.32 μg/mL, 21.06 ± 2.04 μg/mL and 27.52 ± 1.72 μg/mL against XO, ACE and Fe2+-induced lipid peroxidation, respectively. The extract also strongly scavenged DPPH* and ABTS*+. Conclusion: Guava leaves extract could serve as functional food for managing gout and hypertension and attenuating the oxidative stress associated with both diseases. PMID:27104032

Synthesis of Bioactive Chlorogenic Acid-Silica Hybrid Materials via the Sol–Gel Route and Evaluation of Their Biocompatibility

PubMed Central

Pacifico, Severina

2017-01-01

Natural phenol compounds are gaining a great deal of attention because of their potential use as prophylactic and therapeutic agents in many diseases, as well as in applied science for their preventing role in oxidation deterioration. With the aim to synthetize new phenol-based materials, the sol–gel method was used to embed different content of the phenolic antioxidant chlorogenic acid (CGA) within silica matrices to obtain organic-inorganic hybrid materials. Fourier transform infrared (FTIR) measurements were used to characterize the prepared materials. The new materials were screened for their bioactivity and antioxidant potential. To this latter purpose, direct DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2′-azinobis-(3-ethylbenzothiazolin-6-sulfonic acid) methods were applied: radical scavenging capability appeared strongly dependent on the phenol amount in investigated hybrids, and became pronounced, mainly toward the ABTS radical cation, when materials with CGA content equal to 15 wt% and 20 wt% were analyzed. The in vitro biocompatibility of the synthetized materials was estimated by using the MTT assay towards fibroblast NIH 3T3 cells, human keratinocyte HaCaT cells, and the neuroblastoma SH-SY5Y cell line. As cell viability and morphology of tested cell lines seemed to be unaffected by new materials, the attenuated total reflectance (ATR)-FTIR method was applied to deeply measure the effects of the hybrids in the three different cell lines. PMID:28773198

Synthesis of Bioactive Chlorogenic Acid-Silica Hybrid Materials via the Sol-Gel Route and Evaluation of Their Biocompatibility.

PubMed

Catauro, Michelina; Pacifico, Severina

2017-07-21

Natural phenol compounds are gaining a great deal of attention because of their potential use as prophylactic and therapeutic agents in many diseases, as well as in applied science for their preventing role in oxidation deterioration. With the aim to synthetize new phenol-based materials, the sol-gel method was used to embed different content of the phenolic antioxidant chlorogenic acid (CGA) within silica matrices to obtain organic-inorganic hybrid materials. Fourier transform infrared (FTIR) measurements were used to characterize the prepared materials. The new materials were screened for their bioactivity and antioxidant potential. To this latter purpose, direct DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2'-azinobis-(3-ethylbenzothiazolin-6-sulfonic acid) methods were applied: radical scavenging capability appeared strongly dependent on the phenol amount in investigated hybrids, and became pronounced, mainly toward the ABTS radical cation, when materials with CGA content equal to 15 wt% and 20 wt% were analyzed. The in vitro biocompatibility of the synthetized materials was estimated by using the MTT assay towards fibroblast NIH 3T3 cells, human keratinocyte HaCaT cells, and the neuroblastoma SH-SY5Y cell line. As cell viability and morphology of tested cell lines seemed to be unaffected by new materials, the attenuated total reflectance (ATR)-FTIR method was applied to deeply measure the effects of the hybrids in the three different cell lines.

Influence of extraction conditions on antioxidant properties of passion fruit (Passiflora edulis) peel.

PubMed

Wong, Yuh Shan; Sia, Chiaw Mei; Khoo, Hock Eng; Ang, Yee Kwang; Chang, Sui Kiat; Chang, Sui Kiat; Yim, Hip Seng

2014-01-01

As a by-product of tropical fruit juice industry, passion fruit peel is a valuable functional food. It is rich in antioxidants. To determine its potential antioxidant properties of passion fruit peel, this study aimed to evaluate the effect of extraction conditions on total phenolic content and antioxidant activity. The extraction conditions were selected from different percentages of ethanol (0-100%, v/v), extraction times (60-300 min), and extraction temperatures (25-60°C) that based on the optimal percentage of DPPH radical scavenging activity. The selected extraction condition was applied for further determination of total phenolic content (TPC) of the passion fruit peel extract using Folin-Ciocalteu reagent assay, while the antioxidant activities were evaluated using DPPH and ABTS radicals scavenging assays, ferric reducing antioxidant power (FRAP), and β-carotene bleaching (BCB) assay. The best extraction conditions were 40% ethanol, 60 min extraction time, and extraction temperature of 30°C. The chosen extraction conditions have contributed to the high TPC and antioxidant activity of passion fruit peel. The levels of antioxidant activity obtained from the passion fruit peel were also lower compared to BHA and α-tocopherol. Positive correlations were observed between TPC and antioxidant activities as assessed by DPPH, ABTS, FRAP, and BCB assays. As a waste of passion fruit consumption or by-product of fruit juice industry, its peel could be considered as a potential source of natural antioxidant for possible functional food and industrial applications.

Bioactive Constituents of Juniperus turbinata Gussone from La Maddalena Archipelago.

PubMed

Venditti, A; Maggi, F; Quassinti, L; Bramucci, M; Lupidi, G; Ornano, L; Ballero, M; Sanna, C; Bruno, M; Rosselli, S; Bianco, A

2018-05-22

In this paper is reported a comprehensive phytochemical study of Juniperus turbinata (Cupressaceae) collected from La Maddalena Archipelago (Sardinia, Italy). Both the essential oil and the ethanolic extract were analyzed. The essential oil appears to belong to a new chemotype compared to other Mediterranean juniper accessions, as it was favored by geographic isolation of the isles. It showed a low content of monoterpene hydrocarbons and α-terpineol, ent-manoyl oxide 1,10-di-epi-cubenol as the major constituents. The ethanolic fraction resulted mainly composed by diterpenoids. Among these 15-formyloxyimbricatolic acid (11) is a new natural product since it has hitherto been obtained only by synthetic route. The phenolic fraction was constituted by biflavonoids: cupressuflavone (3), followed by minor amounts of amentoflavone (4) and hinokiflavone (5). The essential oil and six purified compounds (1, 2, 3, 6, 7 and 9) were assessed for biological activities, namely antioxidant (assessed by DPPH · , ABTS ·+ and FRAP methods) and cytotoxic effects towards selected human tumor cell lines (MDA-MB 231, A375 and HCT116 cells). Compound 3 exhibited radical scavenging activity against ABTS ·+ radical which was higher than that of the reference Trolox. Noteworthy, compound 9 showed powerful effects on tumor cell lines, with IC 50 values in the range of 0.060-0.201 μM, which make it a promising anticancer drug candidate. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

Antioxidant activity of phenolic acids and their metabolites: synthesis and antioxidant properties of the sulfate derivatives of ferulic and caffeic acids and of the acyl glucuronide of ferulic acid.

PubMed

Piazzon, A; Vrhovsek, U; Masuero, D; Mattivi, F; Mandoj, F; Nardini, M

2012-12-19

The main metabolites of caffeic and ferulic acids (ferulic acid-4'-O-sulfate, caffeic acid-4'-O-sulfate, and caffeic acid-3'-O-sulfate), the most representative phenolic acids in fruits and vegetables, and the acyl glucuronide of ferulic acid were synthesized, purified, and tested for their antioxidant activity in comparison with those of their parent compounds and other related phenolics. Both the ferric reducing antioxidant power (FRAP) assay and the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging method were used. Ferulic acid-4'-O-sulfate and ferulic acid-4'-O-glucuronide exhibited very low antioxidant activity, while the monosulfate derivatives of caffeic acid were 4-fold less efficient as the antioxidant than caffeic acid. The acyl glucuronide of ferulic acid showed strong antioxidant action. The antioxidant activity of caffeic acid-3'-O-glucuronide and caffeic acid-4'-O-glucuronide was also studied. Our results demonstrate that some of the products of phenolic acid metabolism still retain strong antioxidant properties. Moreover, we first demonstrate the ex vivo synthesis of the acyl glucuronide of ferulic acid by mouse liver microsomes, in addition to the phenyl glucuronide.

Radical-scavenging-linked antioxidant activities of extracts from black chokeberry and blueberry cultivated in Korea.

PubMed

Hwang, Seok Joon; Yoon, Won Byong; Lee, Ok-Hwan; Cha, Seung Ju; Kim, Jong Dai

2014-03-01

The objective of this study was to investigate the radical-scavenging-linked antioxidant properties of the extracts from black chokeberry and blueberry cultivated in Korea. The 70% ethanol extracts were prepared from black chokeberry and blueberry, and evaluated for total phenolic content, total flavonoid content, total proanthocyanidin content, and antioxidative activities, using various in vitro assays, such as DPPH(2,2-diphenyl-1-picrylhydrazyl), ABTS(2,2-azino-bis-(3-ethylenebenzothiozoline-6-sulphonic acid)) radical-scavenging activity, FRAP(ferric-reducing antioxidant power) and reducing power. The major phenolic compounds, including cyanidin-3-galactoside, cyanidin-3-arabinoside, neochlorogenic acid, procyanidin B1, were analysed by HPLC with a photodiode array detector. Results showed that total phenol, flavonoid and proanthocyanidin contents of black chokeberry extract were higher than those of blueberry extract. In addition, black chokeberry extract exhibited higher free radical-scavenging activity and reducing power than did blueberry extract. Cyanidin-3-galactoside was identified as a major phenolic compound, with considerable content in black chokeberry, that correlated with its higher antioxidant and radical-scavenging effects. These results suggest that black chokeberry extracts could be considered as a good source of natural antioxidants and functional food ingredients. Copyright © 2013 Elsevier Ltd. All rights reserved.

Antioxidant activity of Caesalpinia digyna root.

PubMed

Srinivasan, R; Chandrasekar, M J N; Nanjan, M J; Suresh, B

2007-09-05

The antioxidant properties of three successive extracts of Caesalpinia digyna Rottler root and the isolated compound, bergenin, were tested using standard in vitro and in vivo models. The amount of the total phenolic compounds present was also determined. The successive methanol extract of Caesalpinia digyna root (CDM) exhibited strong scavenging effect on 2,2-diphenyl-2-picryl hydrazyl (DPPH) free radical, 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulphonic acid) diammonium salt (ABTS) radical cation, hydrogen peroxide, nitric oxide, hydroxyl radical and inhibition of lipid peroxidation. The free radical scavenging effect of CDM was comparable with that of reference antioxidants. The CDM having the highest content of phenolic compounds and strong free radical scavenging effect when administered orally to male albino rats at 100, 200 and 400mg/kg body weight for 7 days, prior to carbontetrachloride (CCl(4)) treatment, caused a significant increase in the levels of catalase (CAT) and superoxide dismutase (SOD) and significant decrease in the levels of lipidperoxidation (LPO) in serum, liver and kidney in a dose dependent manner, when compared to CCl(4) treated control. These results clearly indicate the strong antioxidant property of Caesalpinia digyna root. The study provides a proof for the ethnomedical claims and reported biological activities. The plant has, therefore, very good therapeutic potential.

In vitro and in vivo antioxidant potentials of an ethanolic extract of Ganoderma lucidum in rat mammary carcinogenesis.

PubMed

Deepalakshmi, K; Mirunalini, S; Krishnaveni, M; Arulmozhi, V

2013-11-01

Considering the importance of diet in the prevention of cellular damage caused by reactive oxygen species which has been implicated for several diseases, this present study was undertaken to evaluate the in vitro and in vivo antioxidant potential of the ethanolic extract of the fruiting bodies of Ganoderma lucidum on 7, 12-dimethylbenz(a)anthracene (DMBA)-induced mammary carcinogenesis in Sprague Dawley rats. Ganoderma lucidum extract was tested for in vitro antioxidant and radical scavenging assays, such as (ABTS(+)) radical cation decolorization assay, DPPH radical scavenging, hydroxyl radical, and superoxide radical scavenging assays. The in vivo antioxidant potentials were analyzed by SOD, CAT, and GPx in plasma, mammary, and liver tissues. In all the in vitro antioxidant and radical scavenging assays the extract exhibited good scavenging activity. In vivo enzymatic antioxidant levels, such as SOD, CAT, and GPx were decreased in DMBA-induced animals. Moreover, pretreatment with G. lucidum (500 mg · kg(-1) bw) to DMBA-induced animals significantly (P < 0.05) increased the levels of SOD, CAT, and GPx in plasma, mammary, and liver tissues compared to DMBA induced animals. From these findings, it is suggested that G. lucidum extract could be considered as a potential source of natural antioxidants and can be used as an effective chemopreventive agent against mammary cancer. Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

Quantification of Phenolic Compounds and In Vitro Radical Scavenging Abilities with Leaf Extracts from Two Varieties of Psidium guajava L.

PubMed Central

Martínez-Flores, Héctor Eduardo; Garnica-Romo, Ma. Guadalupe; Padilla-Ramírez, José Saúl; Saavedra-Molina, Alfredo; Alvarez-Cortes, Osvaldo; Bartolomé-Camacho, María Carmen; Rodiles-López, José Octavio

2018-01-01

Guava leaf (Psidium guajava L.) extracts are used in both traditional medicine and the pharmaceutical industry. The antioxidant compounds in P. guajava leaves can have positive effects including anti-inflammatory, anti-hyperglycemic, hepatoprotective, analgesic, anti-cancer effects, as well as protecting against cardiovascular diseases. In the present study, phenolic compounds and in vitro antioxidant capacity were measured in extracts obtained with polar and non-polar solvents from leaves of two varieties of guava, Calvillo Siglo XXI and Hidrozac. The quantity of total phenolics and total flavonoids were expressed as equivalents of gallic acid and quercetin, respectively. Hydroxyl radical, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and Oxygen Radical Absorbance Capacity using fluorescein (ORAC-FL) in vitro tests were used to assess the radical scavenging abilities of the extracts. The total phenolics were higher in the aqueous fraction of the variety Calvillo Siglo XXI, while in the Hidrozac variety total phenolics were higher in the acetone and chloroform fractions. Total flavonoids were higher in all fractions in the variety Calvillo Siglo XXI. Total phenolics showed a highly positive correlation for ORAC-FL, and a moderately positive correlation with hydroxyl radicals. Finally, total flavonoids showed a slightly positive correlation for ORAC-FL and hydroxyl radicals. Both varieties of guava leaf extract showed excellent antioxidant properties. PMID:29495514

Quantification of Phenolic Compounds and In Vitro Radical Scavenging Abilities with Leaf Extracts from Two Varieties of Psidium guajava L.

PubMed

Camarena-Tello, Julio César; Martínez-Flores, Héctor Eduardo; Garnica-Romo, Ma Guadalupe; Padilla-Ramírez, José Saúl; Saavedra-Molina, Alfredo; Alvarez-Cortes, Osvaldo; Bartolomé-Camacho, María Carmen; Rodiles-López, José Octavio

2018-02-27

Guava leaf ( Psidium guajava L.) extracts are used in both traditional medicine and the pharmaceutical industry. The antioxidant compounds in P. guajava leaves can have positive effects including anti-inflammatory, anti-hyperglycemic, hepatoprotective, analgesic, anti-cancer effects, as well as protecting against cardiovascular diseases. In the present study, phenolic compounds and in vitro antioxidant capacity were measured in extracts obtained with polar and non-polar solvents from leaves of two varieties of guava, Calvillo Siglo XXI and Hidrozac. The quantity of total phenolics and total flavonoids were expressed as equivalents of gallic acid and quercetin, respectively. Hydroxyl radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and Oxygen Radical Absorbance Capacity using fluorescein (ORAC-FL) in vitro tests were used to assess the radical scavenging abilities of the extracts. The total phenolics were higher in the aqueous fraction of the variety Calvillo Siglo XXI, while in the Hidrozac variety total phenolics were higher in the acetone and chloroform fractions. Total flavonoids were higher in all fractions in the variety Calvillo Siglo XXI. Total phenolics showed a highly positive correlation for ORAC-FL, and a moderately positive correlation with hydroxyl radicals. Finally, total flavonoids showed a slightly positive correlation for ORAC-FL and hydroxyl radicals. Both varieties of guava leaf extract showed excellent antioxidant properties.

Exploitation of the Apoptosis-Primed State of MYCN-Amplified Neuroblastoma to Develop a Potent and Specific Targeted Therapy Combination

PubMed Central

Ham, Jungoh; Costa, Carlotta; Sano, Renata; Lochmann, Timothy L.; Sennott, Erin M.; Patel, Neha U.; Dastur, Anahita; Gomez-Caraballo, Maria; Krytska, Kateryna; Hata, Aaron N.; Floros, Konstantinos V.; Hughes, Mark T.; Jakubik, Charles T.; Heisey, Daniel A.R.; Ferrell, Justin T.; Bristol, Molly L.; March, Ryan J.; Yates, Craig; Hicks, Mark A.; Nakajima, Wataru; Gowda, Madhu; Windle, Brad E.; Dozmorov, Mikhail G.; Garnett, Mathew J.; McDermott, Ultan; Harada, Hisashi; Taylor, Shirley M.; Morgan, Iain M.; Benes, Cyril H.; Engelman, Jeffrey A.; Mossé, Yael P.; Faber, Anthony C.

2016-01-01

Summary Fewer than half of children with high-risk neuroblastoma survive. Many of these tumors harbor high-level amplification of MYCN, which correlates with poor disease outcome. Using data from our large drug screen we predicted, and subsequently demonstrated, that MYCN-amplified neuroblastomas are sensitive to the BCL-2 inhibitor ABT-199. This sensitivity occurs in part through low anti-apoptotic BCL-xL expression, high pro-apoptotic NOXA expression, and paradoxical, MYCN-driven upregulation of NOXA. Screening for enhancers of ABT-199 sensitivity in MYCN-amplified neuroblastomas, we demonstrate that the Aurora Kinase A inhibitor MLN8237 combines with ABT-199 to induce widespread apoptosis. In diverse models of MYCN-amplified neuroblastoma, including a patient-derived xenograft model, this combination uniformly induced tumor shrinkage, and in multiple instances led to complete tumor regression. PMID:26859456

Evaluation of free radical scavenging capacity and antioxidative damage effect of resveratrol-nanostructured lipid carriers

NASA Astrophysics Data System (ADS)

Jin, Ju; Shi, Fan; Li, Qiu-wen; Li, Pei-shan; Chen, Tong-sheng; Wang, Yi-fei; Wang, Zhi-ping

2016-03-01

Cellular damage induced by free-radicals like reactive oxygen species has been implicated in several diseases. 2, 2-azobis(2-amidino-propane) dihydrochloride(AAPH) generates two potent ROS capable of inducing lipid peroxidation: alkoxy radical(RO-) and peroxy radical(ROO-). These radicals are similar to those that are physiologically active and thus might initiate a cascade of intracellular toxic events leading to oxidation, lipid peroxidation, DNA damage and subsequent cell death. Hence naturally anti-oxidant play a vital role in combating these conditions. In this study, resveratrol loaded nanostructured lipid carriers (Res-NLC) was prepared by hot melting and then high pressure homogenization technique. The effects of Res-NLC on free radical scavenging capacity and antioxidative damage is investigated. The particle size and zeta potential of Res-NLC were 139.3 ± 1.7 nm and -11.21 ± 0.41 mV, respectively. By free radical scavenging assays, the IC50 value of Res-NLC were 19.25, 5.29 μg/mL with DPPH, ABTS assay respectively, and 0.161 mg ferrous sulfate/1 mg Res-NLC with FRAP assay; and by AAPH-induced oxidative injury cell model assay, Res-NLC showed the strong protective effect against the human liver tumor HepG2 cell oxidative stress damage. These results indicated that the antioxidant properties of Res-NLC hold great potential used as an alternative to more toxic synthetic antioxidants as an additive in food, cosmetic and pharmaceutical preparations for the oxidative diseases treatment.

Antioxidant Capacities, Phenolic Profile and Cytotoxic Effects of Saxicolous Lichens from Trans-Himalayan Cold Desert of Ladakh

PubMed Central

Kumar, Jatinder; Dhar, Priyanka; Tayade, Amol B.; Gupta, Damodar; Chaurasia, Om P.; Upreti, Dalip K.; Arora, Rajesh; Srivastava, Ravi B.

2014-01-01

Fourteen saxicolous lichens from trans-Himalayan Ladakh region were identified by morpho-anatomical and chemical characteristics. The n-hexane, methanol and water extracts of the lichens were evaluated for their antioxidant capacities. The lichen extracts showing high antioxidant capacities and rich phenolic content were further investigated to determine their cytotoxic activity on human HepG2 and RKO carcinoma cell lines. The ferric reducing antioxidant power (FRAP), 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging capacities and β-carotene-linoleic acid bleaching property exhibited analogous results where the lichen extracts showed high antioxidant action. The lichen extracts were also found to possess good amount of total proanthocyanidin, flavonoid and polyphenol. The methanolic extract of Lobothallia alphoplaca exhibited highest FRAP value. Methanolic extract of Xanthoparmelia stenophylla showed the highest ABTS radical scavenging capacity. The n-hexane extract of Rhizoplaca chrysoleuca exhibited highest DPPH radical scavenging capacity. Highest antioxidant capacity in terms of β-carotene linoleic acid bleaching property was observed in the water extract of Xanthoria elegans. Similarly, Melanelia disjuncta water extract showed highest NO scavenging capacity. Among n-hexane, methanol and water extracts of all lichens, the methanolic extract of Xanthoparmelia mexicana showed highest total proanthocyanidin, flavonoid and polyphenol content. From cytotoxic assay, it was observed that the methanolic extracts of L. alphoplaca and M. disjuncta were exhibiting high cytotoxic effects against cancer cell growth. Similarly, the water extract of Dermatocarpon vellereum, Umbilicaria vellea, X. elegans and M. disjuncta and the methanolic extract of M. disjuncta and X. stenophylla were found to possess high antioxidant capacities and were non-toxic and may be used as natural antioxidants for stress related problems. Our studies go on to prove that the unique trans-Himalayan lichens are a hitherto untapped bioresource with immense potential for discovery of new chemical entities, and this biodiversity needs to be tapped sustainably. PMID:24937759

Proximate composition, phenolic content and in vitro antioxidant activity of aqueous extracts of the seaweeds Ascophyllum nodosum, Bifurcaria bifurcata and Fucus vesiculosus. Effect of addition of the extracts on the oxidative stability of canola oil under accelerated storage conditions.

PubMed

Agregán, Rubén; Munekata, Paulo E; Domínguez, Ruben; Carballo, Javier; Franco, Daniel; Lorenzo, José M

2017-09-01

Extracts from three macroalgae species (Ascophyllum nodosum (ANE), Bifurcaria bifurcata (BBE) and Fucus vesiculosus (FVE)) were tested for proximate composition (total solid, protein and total carbohydrate contents), total phenols content (TPC), and for their antioxidant activities in vitro in comparison to that of BHT compound by using four different assays (ABTS radical cation decolouration, DPPH free radical scavenging activity, ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC)). The inclusion of the extracts as oil stabilizers in canola oil in substitution of the synthetic antioxidant (BHT) was also evaluated by assessing lipid oxidation parameters (peroxide value (PV), p-anisidine value (AV), TBARS value, conjugated dienes (CD) and TOTOX index) under accelerated storage conditions (16days, 60°C). There was an inverse relationship between total solid content and total polyphenols content in the seaweed extracts. FVE showed an intermediate TPC (1.15g PGE/100g extract), but it presented the highest in vitro antioxidant activity when measured using the ABTS, DPPH and FRAP tests. BBE, that displayed the highest TPC (1.99g PGE/100g extract), only showed the highest in vitro antioxidant activity when measured using the ORAC test. ANE showed the lowest TPC and the lowest antioxidant activity in all the tests performed. The seaweed extracts added in a 500ppm concentration significantly reduced the oxidation during canola oil storage at 60°C, being this antioxidant effect significantly higher than that of BHT added at 50ppm. Results indicate that seaweed extracts can effectively inhibit the oxidation of canola oil and they can be a healthier alternative to the synthetic antioxidants in the oil industry. Copyright © 2016 Elsevier Ltd. All rights reserved.

The cysteine 34 residue of A1M/α1-microglobulin is essential for protection of irradiated cell cultures and reduction of carbonyl groups.

PubMed

Rutardottir, S; Nilsson, E J C; Pallon, J; Gram, M; Åkerström, B

2013-07-01

α1-microglobulin (A1M) is a 26 kDa plasma and a tissue protein belonging to the lipocalin family. The reductase and free radical scavenger A1M has been shown to protect cells and extracellular matrix against oxidative and irradiation-induced damage. The reductase activity was previously shown to depend upon an unpaired cysteinyl side-chain, C34, and three lysyl side-chains, K92, 118, and 130, located around the open end of the lipocalin pocket. The aim of this work was to investigate whether the cell and matrix protection by A1M is a result of its reductase activity by using A1M-variants with site-directed mutations of the C34, K92, K118, and K130 positions. The results show that the C34 side-chain is an absolute requirement for protection of HepG2 cell cultures against alpha-particle irradiation-induced cell death, upregulation of stress response and cell cycle regulation genes. Mutation of C34 also resulted in loss of the reduction capacity toward heme- and hydrogen peroxide-oxidized collagen, and the radical species 2,2´-azino-bis (3-ethyl-benzo-thiazoline-6-sulphonic acid) (ABTS). Furthermore, mutation of C34 significantly suppressed the cell-uptake of A1M. The K92, K118, and K130 side-chains were of minor importance in cell protection and reduction of oxidized collagen but strongly influenced the reduction of the ABTS-radical. It is concluded that antioxidative protection of cells and collagen by A1M is totally dependent on its C34 amino acid residue. A model of the cell protection mechanism of A1M should be based on the redox activity of the free thiolyl group of the C34 side-chain and a regulatory role of the K92, K118, and K130 residues.

General unknown screening, antioxidant and anti-inflammatory potential of Dendrobium macrostachyum Lindl.

PubMed

Sukumaran, Nimisha Pulikkal; Yadav, R Hiranmai

2016-01-01

D. macrostachyum is an epiphytic orchid abundant in Southern India and is reported for pain relief in folklore. The objective of the present study was to determine in vitro free radical scavenging and anti-inflammatory activity of D. macrostachyum and to perform LCMS based metabolic profiling of the plant. Sequential stem and leaf extracts were assessed for its antioxidant and anti-inflammatory activity by in vitro methods. The antioxidant activity determined by assays based on the decolourization of the radical monocation of DPPH, ABTS and reducing power. Total amount of phenolics for quantitative analysis of antioxidative components was estimated. In vitro anti-inflammatory activity was evaluated using protein denaturation assay, membrane stabilization assay and proteinase inhibitory activity. Methanolic extract of plant was subjected to LCMS. The stem ethanolic extracts exhibited significant IC50 value of 10.21, 31.54 and 142.97 μg/ml respectively for DPPH, ABTS radical scavenging and reducing power activity. The ethanol and water extract was highly effective as albumin denaturation inhibitors (IC50 = 114.13 and 135.818 μg/ml respectively) and proteinase inhibitors (IC50 = 72.49 and 129.681 μg/ml respectively). Membrane stabilization was also noticeably inhibited by the stem ethanolic extract among other extracts (IC50 = 89.33 μg/ml) but comparatively lower to aspirin standard (IC50 = 83.926 μg/ml). The highest total phenol content was exhibited by ethanolic stem and leaf extracts respectively at 20 and 16 mg of gallic acid equivalents of dry extract. On LCMS analysis 20 constituents were identified and it included chemotaxonomic marker for Dendrobium species. The results showed a relatively high concentration of phenolics, high scavenger activity and high anti-inflammatory activity of the stem extract compared to the leaf extract. The results indicate that the plant can be a potential source of bioactive compounds.

General unknown screening, antioxidant and anti-inflammatory potential of Dendrobium macrostachyum Lindl.

PubMed Central

Sukumaran, Nimisha Pulikkal; Yadav, R. Hiranmai

2016-01-01

Context: D. macrostachyum is an epiphytic orchid abundant in Southern India and is reported for pain relief in folklore. Aims: The objective of the present study was to determine in vitro free radical scavenging and anti-inflammatory activity of D. macrostachyum and to perform LCMS based metabolic profiling of the plant. Settings and Design: Sequential stem and leaf extracts were assessed for its antioxidant and anti-inflammatory activity by in vitro methods. Materials and Methods: The antioxidant activity determined by assays based on the decolourization of the radical monocation of DPPH, ABTS and reducing power. Total amount of phenolics for quantitative analysis of antioxidative components was estimated. In vitro anti-inflammatory activity was evaluated using protein denaturation assay, membrane stabilization assay and proteinase inhibitory activity. Methanolic extract of plant was subjected to LCMS. Results: The stem ethanolic extracts exhibited significant IC50 value of 10.21, 31.54 and 142.97 μg/ml respectively for DPPH, ABTS radical scavenging and reducing power activity. The ethanol and water extract was highly effective as albumin denaturation inhibitors (IC50 = 114.13 and 135.818 μg/ml respectively) and proteinase inhibitors (IC50 = 72.49 and 129.681 μg/ml respectively). Membrane stabilization was also noticeably inhibited by the stem ethanolic extract among other extracts (IC50 = 89.33 μg/ml) but comparatively lower to aspirin standard (IC50 = 83.926 μg/ml). The highest total phenol content was exhibited by ethanolic stem and leaf extracts respectively at 20 and 16 mg of gallic acid equivalents of dry extract. On LCMS analysis 20 constituents were identified and it included chemotaxonomic marker for Dendrobium species. Conclusions: The results showed a relatively high concentration of phenolics, high scavenger activity and high anti-inflammatory activity of the stem extract compared to the leaf extract. The results indicate that the plant can be a potential source of bioactive compounds. PMID:27621524

An identified antioxidant peptide obtained from ostrich (Struthio camelus) egg white protein hydrolysate shows wound healing properties.

PubMed

Homayouni-Tabrizi, Masoud; Asoodeh, Ahmad; Abbaszadegan, Mohammad-Reza; Shahrokhabadi, Khadijeh; Nakhaie Moghaddam, Mahboobeh

2015-08-01

Ostrich (Struthio camelus) egg possesses a high amount of food proteins and thus plays an important role in nutrition. Ostrich egg white proteins were hydrolyzed with pepsin and pancreatin to examine its antioxidant properties and further characterized the most active peptide. Ostrich egg white protein hydrolysate (OEWPH) was fractionized using reversed phase high-pressure liquid chromatography (HPLC). The antioxidant activity of OEWPH and its HPLC fraction were investigated based on their scavenging capacity1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS), superoxide ([Formula: see text]), hydroxyl (OH(•-)) radicals, and Cu(+2) chelating. In a wound healing assay, paravertebral excision (1 cm diameter) was made on the skin and the percentage of wound closure was measured at defined intervals (0, 3, 7, and 14 d). A potent antioxidant peptide named DG-10 with the sequence DAESLSRLLG (MW: 1060.18 ± 0.5 Da) was identified from OEWPH. The peptide DG-10 showed DPPH (IC50 = 0.0085 mg/ml), ABTS(•+) (IC50 = 0.56 mg/ml), superoxide (IC50 = 0.36 mg/ml), and hydroxyl (IC50 = 0.4 mg/ml) radical scavenger and copper chelating activity (IC50 = 0.28 mg/ml). In vitro cultured HFLF-pI 5, the cell model, also revealed that DG-10 could protect HFLF-pI 5 cells against H2O2-treated necrosis. Ointment composed of DG-10 peptide exhibited wound-healing properties on adult rats (Wistar strain). The percentage of wound closure in peptide-treated group was 98% by day 14. Our results suggested that DG-10 is a natural agent obtained from ostrich egg possessing considerable antioxidant and wound-healing properties.

Antioxidant components of Viburnum opulus L. determined by on-line HPLC-UV-ABTS radical scavenging and LC-UV-ESI-MS methods.

PubMed

Karaçelik, Ayça Aktaş; Küçük, Murat; İskefiyeli, Zeynep; Aydemir, Sezgin; De Smet, Seppe; Miserez, Bram; Sandra, Patrick

2015-05-15

Antioxidant activity of the juice and seed and skin extracts prepared with methanol, acetonitrile, and water of Viburnum opulus L. grown in Eastern Black Sea Region were studied with an on-line HPLC-ABTS method and off-line antioxidant methods, among which a linear positive correlation was observed. The fruit extracts were analysed with the HPLC-UV method optimised with 14 standard phenolics. Identification of the phenolic components in the juice was made using an HPLC-UV-ESI-MS method. Nineteen phenolic compounds in juice were identified by comparing the retention times and mass spectra with those of the standards and the phenolics reported in the literature. The major peaks in the juice belonged to coumaroyl-quinic acid, chlorogenic acid, procyanidin B2, and procyanidin trimer. Quite different antioxidant composition profiles were obtained from the extracts with the solvents of different polarities. The antioxidant activities of the seed extracts were higher than those of the skin extracts in general. Copyright © 2014 Elsevier Ltd. All rights reserved.

Anti-rancidity effect of essential oils, application in the lipid stability of cooked turkey meat patties and potential implications for health.

PubMed

Loizzo, Monica R; Tundis, Rosa; Menichini, Francesco; Duthie, Garry

2015-02-01

Twenty-three commercial essential oils were tested for their anti-rancidity effect and potential implications to prolong the induction time of corn oil and extend the shelf life of cooked turkey patties. Moreover, the potential health benefit was investigated through DPPH, ABTS, β-carotene bleaching, FRAP, and α-amylase inhibitory assays. Essential oils' composition was investigated by GC-MS. Cumin, thyme, clove, and cinnamon oils improved oxidative stability and increased the induction time of the corn oil 1.5-3 fold. Clove and cinnamon oils were particularly effective in delaying lipid oxidation of cooked turkey patties (time of induction 11.04 and 9.43 h) compared with the plain burger (5.04 h). Both oils are also characterized by a potent radical scavenging activity in ABTS test (IC(50) values of 1.43 and 2.05 μg/ml for cinnamon and clove, respectively). In the α-amylase inhibitory assay, cumin and grape fruits were the most potent with IC(50) values of 21.88 and 23.95 μg/ml, respectively.

The antioxidant and anti-cadmium toxicity properties of garlic extracts

PubMed Central

Boonpeng, Suwannaporn; Siripongvutikorn, Sunisa; Sae-wong, Chutha; Sutthirak, Pornpong

2014-01-01

Cadmium (Cd) contamination is a highly dangerous international problem because it can transfer into the food chain and become bioaccumulated, endangering human health. Cd detoxication is very interesting particularly the method providing no undesirable side effects. Cd also causes lipid oxidation that leads to undesired food quality. Garlic (Allium sativum L.) has been used as conventional food and in herbal therapy and folklore medicine as an antibacterial, antitumorogenic, and antioxidant agent for over 5000 years. In the present work, fresh garlic and pickled garlic extracted with distilled water was brought to determine antioxidant activities in terms of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) radical scavenging assay, ferric reducing ability power (FRAP) assay, chelating activities, superoxide, and hydroxyl scavenging assay. The data showed that pickled garlic extracts significantly possessed more DPPH, ABTS, FRAP, superoxide, and hydroxyl scavenging assays as 11.86, 13.74, 4.9, 46.67, and 15.33 g trolox equivalent/g sample, respectively, compared with fresh one as 7.44, 7.62, 0.01, 4.07, and 8.09 g trolox equivalent/g sample, respectively. However, iron chelating activity of fresh garlic extract was higher than that of pickled garlic while there was no significant difference in the copper chelating activity of both extracts. For anti-Cd properties, pickled garlic was more effective than fresh garlic and contained less toxicity than standard diallyl disulfide (DADS). Therefore, therapeutic properties of pickled garlic favored its consumption compared with fresh and standard DADS for its antioxidant and anti-Cd properties. PMID:25493198

Comparison of the Inhibition of Monoamine Oxidase and Butyrylcholinesterase Activities by Infusions from Green Tea and Some Citrus Peels

PubMed Central

Ademosun, Ayokunle O.

2014-01-01

This study sought to investigate the effect of infusions from green tea (Camellia sinensis) and some citrus peels [shaddock (Citrus maxima), grapefruit (Citrus paradisi), and orange (Citrus sinensis)] on key enzymes relevant to the management of neurodegenerative conditions [monoamine oxidase (MAO) and butyrylcholinesterase (BChE)]. The total phenol contents and antioxidant activities as typified by their 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radicals scavenging abilities, ferric reducing antioxidant properties, and Fe2+ chelating abilities were also investigated. Green tea had the highest total phenol (43.3 mg/g) and total flavonoid (16.4 mg/g) contents, when compared to orange [total phenol (19.6 mg/g), total flavonoid (6.5 mg/g)], shaddock [total phenol (16.3 mg/g), total flavonoid (5.2 mg/g)], and grapefruit [total phenol (17.7 mg/g), total flavonoid (5.9 mg/g)]. Orange (EC50 = 1.78 mg/mL) had the highest MAO inhibitory ability, while green tea had the least MAO inhibitory ability (EC50 = 2.56 mg/mL). Similarly, green tea had the least BChE inhibitory ability (EC50 = 5.43 mg/mL) when compared to the citrus peels' infusions. However, green tea infusions had the strongest highest ABTS radical scavenging ability, reducing power, and Fe2+ chelating ability. The inhibition of MAO and BChE activities by the green tea and citrus peels infusions could make them good dietary means for the prevention/management of neurodegenerative conditions. PMID:25243093

Effect of Pelargonium reniforme roots on alcohol-induced liver damage and oxidative stress.

PubMed

Adewusi, Emmanuel Adekanmi; Afolayan, Anthony Jide

2010-09-01

Ethnobotanical surveys conducted on Pelargonium reniforme Curtis (Geraniaceae) have shown that the aqueous root extracts are used to treat alcohol-induced liver damage. We evaluated the antioxidant properties of the extract and its effects on alcohol-induced hepatotoxicity using Wistar rats. Alcohol-induced hepatotoxicity studies were carried out by observing the effect of the aqueous root extract on some liver marker enzymes, bilirubin, and total protein after liver damage. The levels of some phenolic compounds were determined by standard methods. Also, the reducing power of the plant extract and its ability to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH*) and 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS*+) radicals were determined to evaluate its antioxidant activity. The results obtained show that the plant extract possessed significant antioxidant activity. It had a significant level of phenolic compounds, scavenged DPPH* and ABTS*+ radicals effectively, and demonstrated good reducing power. This may indicate that the plant contained compounds which can remove toxic metabolites following alcohol abuse. Serum analysis of animals treated with only ethanol showed a significant increase in the levels of liver marker enzymes and total and unconjugated bilirubin, while a significant decrease was observed in the levels of conjugated bilirubin and total proteins. Administration of the plant extract restored the levels of these markers to normal levels, and this indicates the ability of the plant extract to restore normal functioning of a damaged liver. The study shows that P. reniforme is a potential source of antioxidants and compounds which are useful in treating alcoholic liver damage.

Molecular modeling and simulation studies of recombinant laccase from Yersinia enterocolitica suggests significant role in the biotransformation of non-steroidal anti-inflammatory drugs

DOE Office of Scientific and Technical Information (OSTI.GOV)

Singh, Deepti; Rawat, Surender; Waseem, Mohd

The YacK gene from Yersinia enterocolitica strain 7, cloned in pET28a vector and expressed in Escherichia coli BL21 (DE3), showed laccase activity when oxidized with 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and guaiacol. The recombinant laccase protein was purified and characterized biochemically with a molecular mass of ≈58 KDa on SDS-PAGE and showed positive zymogram with ABTS. The protein was highly robust with optimum pH 9.0 and stable at 70 °C upto 12 h with residual activity of 70%. Kinetic constants, K{sub m} values, for ABTS and guaiacol were 675 μM and 2070 μM, respectively, with corresponding Vmax values of 0.125 μmol/ml/min and 6500 μmol/ml/min. It also possess antioxidative propertymore » against BSA and Cu{sup 2+}/H{sub 2}O{sub 2} model system. Constant pH MD simulation studies at different protonation states of the system showed ABTS to be most stable at acidic pH, whereas, diclofenac at neutral pH. Interestingly, aspirin drifted out of the binding pocket at acidic and neutral pH, but showed stable binding at alkaline pH. The biotransformation of diclofenac and aspirin by laccase also corroborated the in silico results. This is the first report on biotransformation of non-steroidal anti-inflammatory drugs (NSAIDs) using recombinant laccase from gut bacteria, supported by in silico simulation studies. - Highlights: • Laccase from Yersinia enterocolitica strain 7 was expressed in Escherichia coli BL21 (DE3). • Recombinant laccase was found to be thermostable and alkali tolerant. • The in silico and experimental studied proves the biotransformation of NSAIDs. • Laccase binds to ligands differentially under different protonation state. • Laccase also possesses free radical scavenging property.« less

Stability of total phenolic concentration and antioxidant capacity of extracts from pomegranate co-products subjected to in vitro digestion.

PubMed

Fawole, Olaniyi Amos; Opara, Umezuruike Linus

2016-09-13

Co-products obtained from pomegranate juice processing contain high levels of polyphenols with potential high added values. From value-addition viewpoint, the aim of this study was to evaluate the stability of polyphenolic concentrations in pomegranate fruit co-products in different solvent extracts and assess the effect on the total antioxidant capacity using the FRAP, DPPH˙ and ABTS(+) assays during simulated in vitro digestion. Pomegranate juice, marc and peel were extracted in water, 50 % ethanol (50%EtOH) and absolute ethanol (100%EtOH) and analysed for total phenolic concentration (TPC), total flavonoids concentration (TFC) and total antioxidant capacity in DPPH˙, ABTS(+) and FRAP assays before and after in vitro digestion. Total phenolic concentration (TPC) and total flavonoid concentration (TFC) were in the order of peel > marc > juice throughout the in vitro digestion irrespective of the extraction solvents used. However, 50 % ethanol extracted 1.1 to 12-fold more polyphenols than water and ethanol solvents depending on co-products. TPC and TFC increased significantly in gastric digests. In contrast, after the duodenal phase of in vitro digestion, polyphenolic concentrations decreased significantly (p < 0.05) compared to those obtained in gastric digests. Undigested samples and gastric digests showed strong and positive relationships between polyphenols and the antioxidant activities measured in DPPH, ABTS(+) and FRAP assays, with correlation coefficients (r (2)) ranging between 0.930-0.990. In addition, the relationships between polyphenols (TPC and TFC) and radical cation scavenging activity in ABTS(+) were moderately positive in duodenal digests. Findings from this study showed that concentration of pomegranate polyphenols and the antioxidant capacity during in vitro gastro-intestinal digestion may not reflect the pre-digested phenolic concentration. Thus, this study highlights the need to provide biologically relevant information on antioxidants by providing data reflecting their stability and activity after in vitro digestion.

Use of Banana (Musa acuminata Colla AAA) Peel Extract as an Antioxidant Source in Orange Juices.

PubMed

Ortiz, Lucía; Dorta, Eva; Gloria Lobo, M; González-Mendoza, L Antonio; Díaz, Carlos; González, Mónica

2017-03-01

Using banana peel extract as an antioxidant in freshly squeezed orange juices and juices from concentrate was evaluated. Free radical scavenging capacity increased by adding banana peel extracts to both types of orange juice. In addition, remarkable increases in antioxidant capacity using 2,2'-azino-bis-(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS) radical were observed when equal or greater than 5 mg of banana peel extract per ml of freshly squeezed juice was added. No clear effects were observed in the capacity to inhibit lipid peroxidation. Adding 5 mg banana peel extract per ml of orange juice did not substantially modify the physicochemical and sensory characteristics of either type of juice. However, undesirable changes in the sensory characteristics (in-mouth sensations and colour) were detected when equal or greater than 10 mg banana peel extract per ml of orange juice was added. These results confirm that banana peel is a promising natural additive that increases the capacity to scavenge free radicals of orange juice with acceptable sensory and physicochemical characteristics for the consumer.

The Methodology Applied in DPPH, ABTS and Folin-Ciocalteau Assays Has a Large Influence on the Determined Antioxidant Potential.

PubMed

Abramovič, Helena; Grobin, Blaž; Poklar, Nataša; Cigić, Blaž

2017-06-01

Antioxidant potential (AOP) is not only the property of the matrix analyzed but also depends greatly on the methodology used. The chromogenic radicals 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+), 2,2-diphenyl-1-picrylhydrazyl (DPPH•) and Folin-Ciocalteu (FC) assay were applied to estimate how the method and the composition of the assay solvent influence the AOP determined for coffee, tea, beer, apple juice and dietary supplements. Large differences between the AOP values depending on the reaction medium were observed, with the highest AOP determined mostly in the FC assay. In reactions with chromogenic radicals several fold higher values of AOP were obtained in buffer pH 7.4 than in water or methanol. The type of assay and solvent composition have similar influences on the reactivity of a particular antioxidant, either pure or as part of a complex matrix. The reaction kinetics of radicals with antioxidants in samples reveals that AOP depends strongly on incubation time, yet differently for each sample analyzed and the assay applied.

The Effect of Convolvulus arvensis Dried Extract as a Potential Antioxidant in Food Models

PubMed Central

Mohd Azman, Nurul Aini; Gallego, Maria Gabriela; Juliá, Luis; Fajari, Lluis; Almajano, MaríaPilar

2015-01-01

In this study, the antioxidant activity of the Convolvulus arvensis Linn (CA) ethanol extract has been evaluated by different ways. The antioxidant activity of the extract assessed by 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical cation, the oxygen radical absorbance capacity (ORAC) and the ferric reducing antioxidant power (FRAP) was 1.62 mmol Trolox equivalents (TE)/g DW, 1.71 mmol TE/g DW and 2.11 mmol TE/g DW, respectively. CA ethanol extract exhibited scavenging activity against the methoxy radical initiated by the Fenton reaction and measured by Electron Paramagnetic Resonance (EPR). The antioxidant effects of lyophilised CA measured in beef patties containing 0.1% and 0.3% (w/w) CA stored in modified atmosphere packaging (MAP) (80% O2 and 20% CO2) was determined. A preliminary study of gelatine based film containing CA showed a strong antioxidant effect in preventing the degradation of lipid in muscle food. Thus, the present results indicate that CA extract can be used as a natural food antioxidant. PMID:26785344

Extraction, characterization, and biological activity of polysaccharides from Sophora flavescens Ait.

PubMed

Zhang, Qihong; Yu, Jingbo; Zhang, Leifang; Hu, Meiqun; Xu, Yan; Su, Weike

2016-12-01

Four water-soluble polysaccharides, designated as SF1, SF2, SF3 and SF4, were efficiently extracted from the roots of Sophora flavescens by mechanochemistry under the conditions of rotational speed of 400rpm, grinding time of 10min, powder to ball weight ratio of 1:20, and Na 2 CO 3 loading of 7wt%. The results obtained indicated that all of these four acid heteropolysaccharides are composed of rhamnose, arabinose, xylose, mannose, glucose and galactose, with the average molecular weights of 400.9, 98.6, 99.3, 42.7kDa, respectively. In vitro, SF4 showed the most significant scavenging activity on superoxide radical, ABTS, and DPPH radical, while SF3 had the most significant scavenging activity on hydroxyl radical. Immunological tests demonstrated that SF1, SF2, SF3 and SF4 significantly stimulated nitric oxide production without cytotoxicity in macrophages and promoted splenocyte proliferation. These data suggest that the four polysaccharides fractions have the potential as novel natural sources of antioxidative and immunopotentiating agents. Copyright © 2016 Elsevier B.V. All rights reserved.

Protein hydrolysate from turkey meat and optimization of its antioxidant potential by response surface methodology.

PubMed

Wang, Daoying; Shahidi, Fereidoon

2018-05-01

The objective of this research was to optimize antioxidant potential of hydrolyzed protein using Flavourzyme assisted hydrolysis of turkey meat and compare the antioxidant activity of hydrolysates from turkey meat, chicken, and beef. Response surface methodology (RSM) was used to determine the optimal Flavourzyme hydrolysis conditions for preparation of hydrolysate from turkey meat, which were at a temperature of 50.09°C, pH of 5.42, and processing time of 1.08 hours. For comparison, antioxidant activities of the hydrolysate from turkey meat, chicken, and beef under the optimum conditions were determined using reducing power, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical cation, hydroxyl radical, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. The antioxidant activity of turkey meat and chicken meat was significantly higher than that of beef (P < 0.05). Therefore Flavourzyme could be regarded as an effective hydrolytic enzyme for preparation of antioxidant hydrolysate from turkey meat, indicating the potential use of it as a functional food ingredient with shelf-life extension purposes.

Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages.

PubMed

Thi, Nhuan Do; Hwang, Eun-Sun

2014-09-01

The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols.

Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages

PubMed Central

Thi, Nhuan Do; Hwang, Eun-Sun

2014-01-01

The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols. PMID:25320718

In vitro antioxidant, lipoxygenase and xanthine oxidase inhibitory activities of fractions from Cienfuegosia digitata Cav., Sida alba L. and Sida acuta Burn f. (Malvaceae).

PubMed

Konaté, K; Souza, A; Coulibaly, A Y; Meda, N T R; Kiendrebeogo, M; Lamien-Meda, A; Millogo-Rasolodimby, J; Lamidi, M; Nacoulma, O G

2010-11-15

In this study polyphenol content, antioxidant activity, lipoxygenase (LOX) and Xanthine Oxidase (XO) inhibitory effects of n-hexane, dichloromethane, ethyl acetate and n-butanol fractions of aqueous acetone extracts from S. alba L., S. acuta Burn f and Cienfuegosia digitata Cav. were investigated. The total phenolics, flavonoids, flavonols and total tannins were determined by spectrophotometric methods using Folin-ciocalteu, AlCl3 reagents and tannic acid, respectively. The antioxidant potential was evaluated using three methods: inhibition of free radical 2,2-diphenyl-1-picrylhydramzyl (DPPH), ABTS radical cation decolorization assay and Iron (III) to iron (II) reduction activity (FRAP). For enzymatic activity, lipoxygenase and xanthine oxidase inhibitory activities were used. This study shows a relationship between polyphenol contents, antioxidant and enzymatic activities. Present results showed that ethyl acetate and dichloromethane fractions elicit the highest polyphenol content, antioxidant and enzymatic activities.

Comparative studies of bioactive organosulphur compounds and antioxidant activities in garlic (Allium sativum L.), elephant garlic (Allium ampeloprasum L.) and onion (Allium cepa L.).

PubMed

Kim, Sunyoung; Kim, Dan-Bi; Jin, Wenjie; Park, Junghyuck; Yoon, Wonjin; Lee, Yunyeol; Kim, Soyoung; Lee, Sanghee; Kim, Sungsoo; Lee, Ok-Hwan; Shin, Dongbin; Yoo, Miyoung

2018-05-01

We evaluated organosulphur compounds in Allium vegetables, including garlic, elephant garlic and onion, using high-performance liquid chromatography. Among organosulphur compounds, elephant garlic had considerable γ-glutamyl peptides, and garlic had the highest alliin content. Onion had low level of organosulphur compounds than did elephant garlic and garlic. In addition, antioxidant capacities were evaluated by oxygen radical absorbance capacity (ORAC) values and 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging assay. The results showed that garlic had the highest antioxidant capacity, followed by elephant garlic and onion. Furthermore, a positive correlation was observed between antioxidant activities and organosulphur compounds (R > 0.77). Therefore, our results indicate that there was a close relationship between antioxidant capacity and organosulphur compounds in Allium vegetables.

In vitro antioxidant profiles of some flavonoids

NASA Astrophysics Data System (ADS)

Aksoy, Mine; Gülçin, Ilhami; Küfrevioǧlu, Ö. Irfan

2016-04-01

Baicalin ((2S,3S,4S,5R,6S)-6-(5,6-dihydroxy-4-oxo-2-phenyl-chromen-7-yl)oxy-3,4,5-trihydroxy-tetrahydropyran-2-carboxylic acid) and baicalein (5,6,7-trihydroxyflavone) are a flavone, a type of flavonoid. Baicalin is the glucuronide of baicalein. Phlorizin, or phloridzin is a naturally occurring flavonoid produced in some plants. It belongs to the group of dihydrochalcones. In this study, we investigated the in vitro antioxidant properties of baicalin, baicalein and phloridzin using different methods including ferric ion (Fe3+) reducing power, cupric ion (Cu2+) reducing power (CUPRAC method), reduction of Fe3+-TPTZ complex, 1,1-diphenyl-2-picrylhydrazyl free radicals (DPPH.) scavenging, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid radicals (ABTS.+) scavenging activities. Also, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT) and α-Tocopherol were used as standard antioxidants.

Identification of phenolic antioxidants and bioactives of pomegranate seeds following juice extraction using HPLC-DAD-ESI-MSn.

PubMed

Ambigaipalan, Priyatharini; de Camargo, Adriano Costa; Shahidi, Fereidoon

2017-04-15

Phenolics from free and hydrolyzed fractions of pomegranate juice (PJ) and seeds (PS) were evaluated. In general, total phenolic contents and scavenging of ABTS + , DPPH and hydroxyl radicals, as well as metal chelation of the soluble fraction from PS, were higher than those for PJ. Insoluble-bound phenolics from PS accounted for up to 27% of total scavenging capacity (free+esterified+insoluble-bound). Phenolic acids (13), monomeric flavonoids (8), hydrolysable tannins (12), proanthocyanidin (1) and anthocyanins (12) were tentatively characterized using HPLC-DAD-ESI-MS n . Several compounds were identified for the first time in PJ or PS. The inhibition of DNA damage (induced by hydroxyl and peroxyl radicals), copper-induced LDL-cholesterol peroxidation, as well as alpha-glucosidase and lipase activities were demonstrated, therefore supporting the potential exploitation of PJ and PS as sources of bioactive compounds. Copyright © 2016 Elsevier Ltd. All rights reserved.

Singlet oxygen quenching and radical scavenging capacities of structurally-related flavonoids present in Zuccagnia punctata Cav.

PubMed

Vieyra, Faustino E Morán; Boggetti, Héctor J; Zampini, Iris C; Ordoñez, Roxana M; Isla, María I; Alvarez, Rosa M S; De Rosso, Veridiana; Mercadante, Adriana Z; Borsarelli, Claudio D

2009-06-01

The singlet oxygen (1O2) quenching and free radical (DPPH(*), ABTS(* +) and O2(* -)) scavenging ability of three structurally-related flavonoids (7-hydroxyflavanone HF, 2',4'-dihydroxychalcone DHC and 3,7-dihydroxyflavone DHF) present in the Argentinean native shrub Zuccagnia punctata Cav. were studied in solution by combining electrochemical and kinetic measurements, mass spectroscopy, end-point antioxidant assays and computational calculations. The results showed that the antioxidant properties of these flavonoids depend on several factors, such as their electron- and hydrogen atom donor capacity, the ionization degree of the more acidic group, solvatation effects and electrostatic interactions with the oxidant species. The theoretical calculations for both the gas and solution phases at the B3LYP level of theory for the Osanger reaction field model agreed with the experimental findings, thus supporting the characterization of the antioxidant mechanism of the Z. punctata flavonoids.

Bioactive properties of honey with propolis.

PubMed

Osés, S M; Pascual-Maté, A; Fernández-Muiño, M A; López-Díaz, T M; Sancho, M T

2016-04-01

Nowadays, propolis is used as an innovative preservative and as a bioactive food supplement. Due to its bitter and astringent flavour, propolis is hardly accepted by consumers. The aim of this study was to obtain a likeable food product made with honey and propolis, whose antimicrobial, antioxidant and anti-inflammatory properties were enhanced in comparison with those of the base honeys used. 0.1%, 0.3% and 0.5% soft propolis extracts were added to honeys and the products that most appealed to the users were subjected to further research. Total phenolics, flavonoids, ABTS free radical and hydroxyl radicals scavenging and anti-inflammatory activities increased in all mixtures. Antimicrobial activity of the combined products showed synergic effects, resulting in higher results than those of the base honeys and propolis extracts. Therefore, honeys enriched with small amounts of propolis extracts are promising functional foods. Copyright © 2015 Elsevier Ltd. All rights reserved.

Spectroscopic studies on the antioxidant activity of ellagic acid

NASA Astrophysics Data System (ADS)

Kilic, Ismail; Yeşiloğlu, Yeşim; Bayrak, Yüksel

2014-09-01

Ellagic acid (EA, C14H6O8) is a natural dietary polyphenol whose benefits in a variety of diseases shown in epidemiological and experimental studies involve anti-inflammation, anti-proliferation, anti-angiogenesis, anticarcinogenesis and anti-oxidation properties. In vitro radical scavenging and antioxidant capacity of EA were clarified using different analytical methodologies such as total antioxidant activity determination by ferric thiocyanate, hydrogen peroxide scavenging, 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH) scavenging, 2,2‧-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging activity and superoxide anion radical scavenging, ferrous ions (Fe2+) chelating activity and ferric ions (Fe3+) reducing ability. EA inhibited 71.2% lipid peroxidation of a linoleic acid emulsion at 45 μg/mL concentration. On the other hand, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), α-tocopherol and ascorbic acid displayed 69.8%, 66.8%, 64.5% and 59.7% inhibition on the peroxidation of linoleic acid emulsion at the same concentration, respectively. In addition, EA had an effective DPPH• scavenging, ABTSrad + scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, ferric ions (Fe3+) reducing power and ferrous ions (Fe2+) chelating activities. Also, those various antioxidant activities were compared to BHA, BHT, α-tocopherol and ascorbic acid as references antioxidant compounds. These results suggested that EA can be used in the pharmacological, food industry and medicine because of these properties.

Antioxidant activity profiling by spectrophotometric methods of aqueous methanolic extracts of Helichrysum stoechas subsp. rupestre and Phagnalon saxatile subsp. saxatile.

PubMed

Haddouchi, Farah; Chaouche, Tarik Mohammed; Ksouri, Riadh; Medini, Faten; Sekkal, Fatima Zohra; Benmansour, Abdelhafid

2014-06-01

The aqueous methanolic extracts of two plants from Algeria, Helichrysum stoechas subsp. rupestre and Phagnalon saxatile subsp. saxatile, were investigated for their antioxidant activity. Total phenolics, flavonoids, and tannins were determined by spectrophotometric techniques. In vitro antioxidant and radical scavenging profiling was determined by spectrophotometric methods, through: Total antioxidant capacity, and radical scavenging effects by the DPPH and ABTS methods, reducing and chelating power, and blanching inhibition of the β-carotene. All of the extracts showed interesting antioxidant and radical scavenging activity. The highest contents in phenolics, tannins, and the highest total antioxidant capacity as gallic acid equivalents of 97.5 ± 0.33 mg GAE/g DW was obtained for the flowers of H. stoechas subsp. rupestre extract in the phosphomolybdenum assay. An extract of the leafy stems of P. saxatile subsp. saxatile revealed the highest content of flavonoids, and the highest antioxidant activity by the radical scavenging and β-carotene assays when compared with standards. The best activity was by the scavenging radical DPPH with an IC50 value of 5.65 ± 0.10 μg·mL(-1). The studied medicinal plants could provide scientific evidence for some traditional uses in the treatment of diseases related to the production of reactive oxygen species (ROS) and oxidative stress. Copyright © 2014 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

Comparative chemical profiling, cholinesterase inhibitions and anti-radicals properties of essential oils from Polygonum hydropiper L: a preliminary anti- Alzheimer's study.

PubMed

Ayaz, Muhammad; Junaid, Muhammad; Ullah, Farhat; Sadiq, Abdul; Khan, Mir Azam; Ahmad, Waqar; Shah, Muhammad Raza; Imran, Muhammad; Ahmad, Sajjad

2015-11-04

Cholinesterase inhibition is a vital target for the development of novel and mechanism based inhibitors, owing to their role in the breakdown of acetylcholine (ACh) neurotransmitter to treat various neurological disorders including Alzheimer's disease (AD). Similarly, free radicals are implicated in the progression of various diseases like neurodegenerative disorders. Due to lipid solubility and potential to easily cross blood brain barrier, this study was designed to investigate the anticholinesterase and antioxidant potentials of the standardized essential oils from the leaves and flowers of Polygonum hydropiper. Essential oils from the leaves (Ph.LO) and flowers (Ph.FO) of P. hdropiper were isolated using Clevenger apparatus. Oil samples were analyzed by GC-MS to identify major components and to attribute the antioxidant and anticholinesterase activity to specific components. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials of the samples were determined following Ellman's assay. Antioxidant assays were performed using 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H2O2) free radical scavenging assays. In the GC-MS analysis 141 and 122 compounds were indentified in Ph.LO and Ph.FO respectively. Caryophylene oxide (41.42 %) was the major component in Ph.FO while decahydronaphthalene (38.29 %) was prominent in Ph.LO. In AChE inhibition, Ph.LO and Ph.FO exhibited 87.00** and 79.66***% inhibitions at 1000 μg/ml with IC50 of 120 and 220 μg/ml respectively. The IC50 value for galanthamine was 15 μg/ml. In BChE inhibitory assay, Ph.LO and Ph.FO caused 82.66*** (IC50 130 μg/ml) and 77.50***% (IC50 225 μg/ml) inhibitions respectively at 1000 μg/ml concentration. In DPPH free radical scavenging assay, Ph.LO and Ph.FO exhibited IC50 of 20 and 200 μg/ml respectively. The calculated IC50s were 180 & 60 μg/ml for Ph.LO, and 45 & 50 μg/ml for Ph.FO in scavenging of ABTS and H2O2 free radicals respectively. In the current study, essential oils from leaves and flowers of P. hydropiper exhibited dose dependent anticholinesterase and antioxidant activities. Leaves essential oil were more effective and can be subjected to further in-vitro and in-vivo anti-Alzheimer's studies.

Phytochemical screening and polyphenolic antioxidant activity of aqueous crude leaf extract of Helichrysum pedunculatum.

PubMed

Aiyegoro, Olayinka A; Okoh, Anthony I

2009-11-13

We evaluated the in vitro antioxidant property and phytochemical constituents of the aqueous crude leaf extract of Helichrysum pedunculatum. The scavenging activity on superoxide anions, DPPH, H₂O₂, NO and ABTS; and the reducing power were determined, as well as the flavonoid, proanthocyanidin and phenolic contents of the extract. The extract exhibited scavenging activity towards all radicals tested due to the presence of relatively high total phenol and flavonoids contents. Our findings suggest that H. pedunculatum is endowed with antioxidant phytochemicals and could serve as a base for future drugs.

Phytochemical Screening and Polyphenolic Antioxidant Activity of Aqueous Crude Leaf Extract of Helichrysum pedunculatum

PubMed Central

Aiyegoro, Olayinka A.; Okoh, Anthony I.

2009-01-01

We evaluated the in vitro antioxidant property and phytochemical constituents of the aqueous crude leaf extract of Helichrysum pedunculatum. The scavenging activity on superoxide anions, DPPH, H2O2, NO and ABTS; and the reducing power were determined, as well as the flavonoid, proanthocyanidin and phenolic contents of the extract. The extract exhibited scavenging activity towards all radicals tested due to the presence of relatively high total phenol and flavonoids contents. Our findings suggest that H. pedunculatum is endowed with antioxidant phytochemicals and could serve as a base for future drugs. PMID:20087473

Effect of kilning on the antioxidant and pro-oxidant activities of pale malts.

PubMed

Woffenden, Helen M; Ames, Jennifer M; Chandra, Sachin; Anese, Monica; Nicoli, M Cristina

2002-08-14

Pale malts were prepared using standard and rapid kilning regimes that differed in the temperature and moisture profiles in the kiln. Samples were taken over the last 9 h of kilning, that is, at 18, 20, 22, 25, and 27 h. Antioxidant activity, assessed by redox potential, scavenging of the 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS*+), and ferric reducing/antioxidant power (FRAP), increased at moisture levels below 6.7% for both regimes. The 27 h malt exposed to the rapid regime (moisture content of 4.8%) had a higher activity than the 27 h standard regime sample (moisture content of 4.8%). None of the malts scavenged oxygen. Pro-oxidant activity profiles were different for the malts obtained using each regime and, at 27 h, the rapid procedure gave malt with higher activity. Levels of (+)-catechin and ferulic acid (the most abundant phenolic compounds identified) generally increased as the moisture content of malt fell below 6.7%. Differences in antioxidant and pro-oxidant activities of the 27 h malts are partly attributed to the Maillard reaction, as evidenced by lower L* and higher b* values and higher levels of Maillard-derived flavor compounds, in the sample obtained by the rapid procedure. Levels of lipid-derived flavor compounds were significantly higher after 27 h of kilning using the rapid procedure.

First characterisation of flavonoid- and diarylheptanoid-type antioxidant phenolics in Corylus maxima by HPLC-DAD-ESI-MS.

PubMed

Riethmüller, Eszter; Tóth, Gergő; Alberti, Ágnes; Végh, Krisztina; Burlini, Ilaria; Könczöl, Árpád; Balogh, György Tibor; Kéry, Ágnes

2015-03-25

Corylus maxima Mill. (Betulaceae) leaves have been used in traditional medicine both internally and externally, nevertheless phytochemical exploration of the plant remains incomplete. In this study, the in vitro antioxidant activity and polyphenolic composition of the ethyl acetate and methanolic extracts of C. maxima leaves and bark are reported for the first time. The radical scavenging activities of the extracts were investigated by the ABTS and DPPH assays. All the extracts of C. maxima possessed notable antioxidant activity. By mean of a HPLC-DAD-ESI-TOF and a HPLC-DAD-ESI-MS/MS method, altogether twenty-two phenolics were tentatively characterised: one flavan derivative (1), seven flavonol derivatives (4, 6, 12, 13, 16, 20 and 21) and fourteen diarylheptanoids (2, 3, 5, 7-11, 14, 15, 17-19 and 22). The amount of the two main flavonoids - myricetin-3-O-rhamnoside (6) and quercetin-3-O-rhamnoside (13) - and two diarylheptanoids - oregonin (3) and hirsutenone (15) - in the extracts were determined by a validated HPLC-ESI-MS/MS method in multiple reaction monitoring (MRM) mode. Our results showed that C. maxima could be considered as a valuable source of pharmacologically important natural products that might contribute to the revaluation of the phytotherapeutical potential of the plant. Copyright © 2014 Elsevier B.V. All rights reserved.

The antimicrobial, antioxidative, anti-inflammatory activity and cytotoxicity of different fractions of four South African Bauhinia species used traditionally to treat diarrhoea.

PubMed

Ahmed, Aroke S; Elgorashi, Esameldin E; Moodley, Nivan; McGaw, Lyndy J; Naidoo, Vinasan; Eloff, Jacobus N

2012-10-11

Many Bauhinia species, including those indigenous to South Africa, are used in traditional medicine across the world for treating ailments such as gastrointestinal tract (GIT) disorders, diabetes, infectious diseases and inflammation. Several relevant aspects of different fractions of leaf extracts of Bauhinia bowkeri (BAB), Bauhinia galpinii (BAG), Bauhinia petersiana (BAP), and Bauhinia variegata (BAV) used in South African traditional medicine to alleviate diarrhoea related symptoms were evaluated. The antioxidative activities of the extracts were determined using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH), 2, 2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS(+)) radical scavenging and ferric reducing antioxidant power (FRAP) methods. In vitro antimicrobial activities of the extracts were determined against bacterial strains (Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Enterococcus faecalis) and clinical isolates of the opportunistic fungal strains (Aspergillus fumigatus, Candida albicans, and Cryptococcus neoformans) using a serial dilution microplate method. The polyphenolic contents were quantified using standard methods, and anti-inflammatory activities of the crude extracts were determined using the cyclooxygenase and soybean 15-lipoxygenase enzyme inhibitory assays. The safety of the extracts was evaluated by determining the cytotoxicity against Vero cell lines. The acidified 70% acetone crude extract and their fractions had good antiradical potency against the DPPH and ABTS radicals. The methanol soluble portions of the butanol fractions were more potent (EC(50) ranges from 0.64 ± 0.05 to 1.51 ± 0.07 and 0.88 ± 0.18 to 1.49 ± 0.09 μg/ml against DPPH and ABTS radical respectively) compared to the standard, trolox and ascorbic acid (EC(50) ranges from 1.47 ± 0.24 to 1.70 ± 0.27 μg/ml) for both DPPH and ABTS. The crude extracts contained variable quantities of phenolic content. The crude extracts and their fractions had weak to good antimicrobial activities, inhibiting the growth of the organisms at concentrations ranging from 39 to 2500 μg/ml. The BAG crude extract and its fractions were the most active against the fungi (MICs ranging from 39 to 625 μg/ml) while the BAB extract and its fractions were the least active with the MICs ranging between 39 and 2500 μg/ml. Aspergillus fumigatus was the least susceptible fungus while Cryptococcus neoformans was the most susceptible. The phenolic-rich crude extracts of BAB, BAG, and BAP had moderate to good dose-dependent cyclooxygenase-1 enzyme inhibitory activity with inhibitions between 22.8% and 71.4%. The extracts were however, inactive against cyclooxygenase-2. The extracts had some level of cytotoxicity towards Vero cell lines, reducing cell viability to less than 10% at concentrations more than 50 μg/ml. The biological activities observed in Bauhinia species provide a scientific basis for the use of the plants in traditional medicines to treat diseases with multi-factorial pathogenesis such as diarrhoea, with each aspect of activity contributing to the ultimate therapeutic benefit of the plants. However, the use of the phenolic-rich extracts of these plants to treat diarrhoea or any other ailments in traditional medicine needs to be monitored closely because of potential toxic effects and selective inhibition of COX-1 with the associated GIT injury. Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

Administration of the nicotinic acetylcholine receptor agonists ABT-089 and ABT-107 attenuates the reinstatement of nicotine-seeking behavior in rats

PubMed Central

Lee, Alycia M.; Arreola, Adrian C.; Kimmey, Blake A.; Schmidt, Heath D.

2014-01-01

Current smoking cessation pharmacotherapies have modest efficacy, and most smokers relapse within the first few days after a quit attempt. Nicotine withdrawal-induced craving and cognitive impairments predict smoking relapse during abstinence and suggest that cognitive-enhancing drugs may prevent relapse. ABT-089 and ABT-107 are subtype-selective nAChR agonists that improve cognitive performance in laboratory animals. However, there are no studies examining the effects of ABT-089 and ABT-107 on nicotine self-administration and the reinstatement of nicotine-seeking behavior, an animal model of relapse in human smokers. The goal of the present study was to determine the effects of the α4β2*/α6β2* nAChR agonist ABT-089 and the α7 nAChR agonist ABT-107 on nicotine taking and seeking in rats. The effects of acute ABT-089 and ABT-107 pretreatment on nicotine self-administration and reinstatement were tested in male Sprague Dawley rats. Parallel studies of ABT-089 and ABT-107 on sucrose self-administration and reinstatement were tested in separate groups of rats to determine if the effects of these drug treatments generalized to other reinforced behaviors. Nicotine and sucrose self-administration behaviors were not altered following acute administration of ABT-089 (0, 0.12, 1.2 and 12.0 mg/kg) or ABT-107 (0, 0.03 and 0.3 mg/kg). In contrast, both ABT-089 and ABT-107 pretreatment dose-dependently attenuated nicotine reinstatement. These effects were reinforcer-specific as no effects of ABT-089 or ABT-107 pretreatment on sucrose seeking were noted. Taken together, these findings suggest that ABT-089 and ABT-107 do not affect nicotine consumption, but may reduce the likelihood that a smoking lapse will lead to relapse. PMID:25128791

Thrombospondin-1 peptide ABT-510 combined with valproic acid is an effective antiangiogenesis strategy in neuroblastoma.

PubMed

Yang, Qiwei; Tian, Yufeng; Liu, Shuqing; Zeine, Rana; Chlenski, Alexandre; Salwen, Helen R; Henkin, Jack; Cohn, Susan L

2007-02-15

In the pediatric cancer neuroblastoma, clinically aggressive disease is associated with increased levels of angiogenesis stimulators and high vascular index. We and others have hypothesized that blocking angiogenesis may be effective treatment for this pediatric malignancy. However, little is known about the efficacy of antiangiogenic agents in pediatric malignancies. Recently, promising results have been reported in an adult phase I study of ABT-510, a peptide derivative of the natural angiogenic inhibitor thrombospondin-1. Histone deacetylase inhibitors, such as valproic acid (VPA), have also been shown to have antiangiogenic activity in several cancer models. In this study, we evaluated the effects of ABT-510 and VPA on neuroblastoma tumor growth and angiogenesis. Although only VPA was capable of blocking the proliferation of neuroblastoma cells and inducing neuroblastoma cell apoptosis in vitro, treatment with VPA or ABT-510 alone significantly suppressed the growth of neuroblastoma xenografts established from two different MYCN-amplified cell lines. Combination therapy more effectively inhibited the growth of small neuroblastoma xenografts than single-agent treatment, and in animals with large xenografts, total cessation of tumor growth was achieved with this treatment approach. The microvascular density was significantly reduced in the xenografts treated with combination therapy compared with controls or tumors treated with single agents. In addition, the number of structurally abnormal vessels was reduced, suggesting that these agents may "normalize" the tumor vasculature. Our results indicate that ABT-510 combined with VPA may be an effective antiangiogenic treatment strategy for children with high-risk neuroblastoma.

Free-Radical-Scavenging, Antityrosinase, and Cellular Melanogenesis Inhibitory Activities of Synthetic Isoflavones.

PubMed

Lu, Tzy-Ming; Ko, Horng-Huey; Ng, Lean-Teik; Hsieh, Yen-Pin

2015-06-01

In this study, we examined the potential of synthetic isoflavones for application in cosmeceuticals. Twenty-five isoflavones were synthesized and their capacities of free-radical-scavenging and mushroom tyrosinase inhibition, as well as their impact on cell viability of B16F10 murine melanoma cells and HaCaT human keratinocytes were evaluated. Isoflavones that showed significant mushroom tyrosinase inhibitory activities were further studied on reduction of cellular melanin formation and antityrosinase activities in B16F10 melanocytes in vitro. Among the isoflavones tested, 6-hydroxydaidzein (2) was the strongest scavenger of both ABTS(.+) and DPPH(.) radicals with SC50 values of 11.3 ± 0.3 and 9.4 ± 0.1 μM, respectively. Texasin (20) exhibited the most potent inhibition of mushroom tyrosinase (IC50 14.9 ± 4.5 μM), whereas retusin (17) showed the most efficient inhibition both of cellular melanin formation and antityrosinase activity in B16F10 melanocytes, respectively. In summary, both retusin (17) and texasin (20) exhibited potent free-radical-scavenging capacities as well as efficient inhibition of cellular melanogenesis, suggesting that they are valuable hit compounds with potential for advanced cosmeceutical development. Copyright © 2015 Verlag Helvetica Chimica Acta AG, Zürich.

Fermentation of Smilax china root by Aspergillus usami and Saccharomyces cerevisiae promoted concentration of resveratrol and oxyresveratrol and the free-radical scavenging activity.

PubMed

Yoon, So-Ra; Yang, Seung-Hwan; Suh, Joo-Won; Shim, Soon-Mi

2014-07-01

Smilax china root, which is rich in resveratrol and oxyresveratrol, has been used as emergency foods as well as folk medicine. This study investigated changes in concentration of bioactive components and the free-radical scavenging capacity of Smilax china root during fermentation by Aspergillus usami and Saccharomyces cerevisiae. Resveratrol, oxyresveratrol and piceid were quantified as major constituents in Smilax china root by using UPLC-ESI-MS. The concentration of oxyresveratrol and resveratrol remarkably increased through fermentation and the transformation of piceid to resveratrol. Its concentration in 4% Smilax china root was 1.16-2.95 times higher than that of a 2% preparation throughout fermentation. The vitamin C equivalent antioxidant capacity of 2% Smilax china root was 1.51-1.91 times higher than that of 4% Smilax china root during fermentation. Meanwhile, ABTS free-radical scavenging capacity was enhanced up to 95.07 and 99.35% for 2% and 4% Smilax china root, respectively. Results from our study propose that bioactive components in Smilax China root were highly extracted by fermentation followed by saccharification and ethanol production, resulting in enhanced free-radical scavenging capacity. © 2013 Society of Chemical Industry. © 2013 Society of Chemical Industry.

Preparation of Egg White Liquid Hydrolysate (ELH) and Its Radical-Scavenging Activity

PubMed Central

Noh, Dong Ouk; Suh, Hyung Joo

2015-01-01

In the present study, an optimum protease was selected to hydrolyze the egg white liquid protein for the antioxidant peptides. Alcalase treatment yielded the highest amount of α-amino groups (15.27 mg/mL), while the control (no enzymatic hydrolysis) showed the lowest amount of α-amino groups (1.53 mg/mL). Alcalase also gave the highest degree of hydrolysis (DH) value (43.2%) and was more efficient for egg white liquid hydrolysis than the other enzymes. The Alcalase hydrolysate had the highest radical-scavenging activity (82.5%) at a concentration of 5.0 mg/mL. The conditions for enzymatic hydrolysis of egg white liquid with Alcalase were selected as substrate : water ratio of 2:1. Five percent Alacalse treatment did not show significant (P>0.05) increases of DH and α-amino nitrogen content after 24 h-hydrolysis. Thirty two hour-hydrolysis with 5% Alcalase is sufficient to make antioxidative egg white liquid hydrolysate from egg white liquid. DPPH and ABTS radical-scavenging activities were significantly (P<0.05) higher after enzymatic digestion. These results suggest that active peptides released from egg-white protein are effective radical-scavengers. Thus, this approach may be useful for the preparation of potent antioxidant products. PMID:26451355

The melanin synthesis inhibition and radical scavenging activities of compounds isolated from the aerial part of Lespedeza cyrtobotrya.

PubMed

Lee, Mi Yeon; Kim, Jin Hee; Choi, Jung Nam; Kim, Jiyoung; Hwang, Geum Sook; Lee, Choonghwan

2010-06-01

The EtOAc fraction of Lespedeza cyrtobotrya showed mushroom tyrosinase inhibitory and radical scavenging activity. Four active compounds were isolated based on LH-20 chromatography and HPLC, and the structures were elucidated on the basis of their LC-MS and NMR spectral data, as 2-(2,4-Dihydroxyphenyl)-6-hydroxybenzofuran (1), eriodictyol-7-O-glucopyranoside (2), haginin A (3), and dalbergioidin (4), respectively. 2-(2,4-Dihydroxyphenyl)-6-hydroxybenzofuran (1) showed mushroom tyrosinase inhibitory activity with an IC50 value of 5.2 micronM and acted as a competitive inhibitor. Furthermore, 37.3 micronM of compound 1 reduced 50 % of the melanin content on a human melanoma (MNT-1) cells. The radical scavenging activity of 2-(2,4-dihydroxyphenyl)-6-hydroxybenzofuran (1), eriodictyol-7-O-glucopyranoside (2), haginin A (3), and dalbergioidin (4) was shown with IC50 values of 11.0, 24.5, 9.0 and 36.5 micronM in an ABTS system and with IC50 values of 42.7, 36.0, 37.7 and 61.7 micronM in a DPPH system, respectively. The mushroom tyrosinase inhibitory activity of EtOAc fraction of Lespedeza cyrtobotrya was contributed by compound 1, 3 and 4, and radical scavenging activity of it was contributed by compound 1-4.

Prevention of acetic acid-induced colitis by desferrithiocin analogs in a rat model.

PubMed

Bergeron, Raymond J; Wiegand, Jan; Weimar, William R; Nguyen, John Nhut; Sninsky, Charles A

2003-02-01

Iron contributes significantly to the formation of reactive oxygen species via the Fenton reaction. Therefore, we assessed whether a series of desferrithiocin analogs, both carboxylic acids and hydroxamates, could (1) either promote or diminish the iron-mediated oxidation of ascorbate, (2) quench a model radical species, 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+), and (3) when applied topically, prevent acetic acid-induced colitis in rats. Surprisingly, most of the desferrithiocin analogs inhibited the Fenton reaction to an approximately equivalent degree; however, substantial differences were observed in the capacity of the analogs to scavenge the model radical cation. Four carboxylic acid desferrithiocin analogs and their respective N-methylhydroxamates were tested along with desferrioxamine and Rowasa, a currently accepted topical therapeutic agent for inflammatory bowel disease (IBD), in a rodent model of acetic acid-induced colitis. The colonic damage was quantitated by two independent measurements. Although neither radical scavenging nor prevention of Fenton chemistry was a definitive predictor of in vivo efficacy, the overall trend is that desferrithiocin analogs substituted with an N-methylhydroxamate in the place of the carboxylic acid are both better free radical scavengers and more active against acetic acid-induced colitis. These results represent an intriguing alternative avenue to the development of improved IBD therapeutic agents.

Antimutagenic and free radical scavenger effects of leaf extracts from Accacia salicina

PubMed Central

2011-01-01

Background Three extracts were prepared from the leaves of Accacia salicina; ethyl acetate (EA), chloroform (Chl) and petroleum ether (PE) extracts and was designed to examine antimutagenic, antioxidant potenty and oxidative DNA damage protecting activity. Methods Antioxidant activity of A. salicina extracts was determined by the ability of each extract to protect against plasmid DNA strand scission induced by hydroxyl radicals. An assay for the ability of these extracts to prevent mutations induced by various oxidants in Salmonella typhimurium TA102 and TA 104 strains was conducted. In addition, nonenzymatic methods were employed to evaluate anti-oxidative effects of tested extracts. Results These extracts from leaf parts of A. salicina showed no mutagenicity either with or without the metabolic enzyme preparation (S9). The highest protections against methylmethanesulfonate induced mutagenicity were observed with all extracts and especially chloroform extract. This extract exhibited the highest inhibitiory level of the Ames response induced by the indirect mutagen 2- aminoanthracene. All extracts exhibited the highest ability to protect plasmid DNA against hydroxyl radicals induced DNA damages. The ethyl acetate (EA) and chloroform (Chl) extracts showed with high TEAC values radical of 0.95 and 0.81 mM respectively, against the ABTS.+. Conclusion The present study revealed the antimutagenic and antioxidant potenty of plant extract from Accacia salicina leaves. PMID:22132863

Antioxidant properties of sour cherries (Prunus cerasus L.): role of colorless phytochemicals from the methanolic extract of ripe fruits.

PubMed

Piccolella, Simona; Fiorentino, Antonio; Pacifico, Severina; D'Abrosca, Brigida; Uzzo, Piera; Monaco, Pietro

2008-03-26

Many edible plant metabolites are known to be useful as cellular antioxidants. In the search for antioxidative chemicals from native fruits of the Campania region of Italy, Prunus cerasus L., an acidic cherry widely used for culinary purposes, has been studied. Fruit crude extracts (MeOH, EtOAc, and hexane) were submitted to an antioxidative screening using specific assay media characterized from the presence of highly reactive radical species (DPPH*, ABTS*+, O2*-, NO) or lipoperoxidation markers. The reducing power of the samples was also determined. It was observed that the most polar extracts in MeOH and EtOAc were able to exercise a massive and dose-increasing antioxidative capacity. The peculiar efficacy of the same extracts was revealed by investigating their protein and deoxyribose oxidation capacity. A preliminary analysis of total phenol, flavonoid, and anthocyanin contents together with biological screening data put the basis on P. cerasus fruit phytochemical investigation of methanolic extract. Twenty secondary metabolites were isolated and characterized by spectroscopic (especially 1D and 2D NMR) and spectrometric techniques. 1-(4-Hydroxyphenyl)-1,2-ethanediol-1,2-bis-1-O-beta-D-glucopyranoside (3), (4-hydroxy-3-methoxyphenyl)methanol-1-O-beta-D-gentiobioside (4), epicatechin-3-malate (14), and epicatechin-3-(1''-methyl)malate (15) were isolated for the first time. All of the compounds were evaluated for their radical scavenging activity on DPPH*, O2*-, and NO. Flavonoids and quinic acid derivatives were found to be the more antioxidative substances.

Antioxidant Properties of Fractions for Unripe Fruits of Capsicum annuum L. var. Conoides.

PubMed

Chen, Chung-Yi; Yen, Ching-Yu; Shen, Gao-Mai; Yu, Tzu-Jung; Liao, Yi-Shin; Jian, Ru-In; Wang, Sheng-Chieh; Tang, Jen-Yang; Chang, Hsueh-Wei

2018-02-07

Capsicum plant, especially for C. annuum, is an abundant resource for bioactive antioxidants, but few studies have examined the unripe fruit part of the Capsicum plant. MeOH extract of unripe fruits of C. annuum L. var. conoides (UFCA) was chromatographed over a silica gel column using a gradient of CH2Cl2/MeOH as eluent to produce 9 fractions. Antioxidant activities are evaluated along with cell viabilities of 9 fractions of UFCA. The antioxidant properties were analyzed in terms of total phenol content (TPC), total flavonoid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azinobis (3-ethyl-benzothiazoline-6- sulfonic acid) (ABTS) radical scavenging, ferric reducing, and ferrous ion-chelating ability. The cell viability of human oral cancer cells (Ca9-22) was measured by 3-(4,5-dimethylthiazol-2-yl)-(3-carboxymethoxyphenyl)-2- (4-sulphophenyl)-2H-tetrazolium (MTS) assay. Except for TFC, fractions (Frs.) 1 and 2 showed the lowest level of these antioxidant properties. Frs. 3 to 9 showed dose-responsive induction for antioxidant effects. Fr. 8 and Fr. 5 respectively showed the highest levels of TPC and TFC for 1162 ± 11 gallic acid equivalents (GAE) (mg)/UFCA (g) and 1295 ± 32 quercetin equivalents (QCE) (mg)/UFCA (g). The cell viability of Fr. 3 was moderately decreased (78.2%) while those of Frs. 4, 5, and 9 were dramatically decreased (55.6, 57.8, and 46.8%, respectively) in oral cancer Ca9-22 cells. UFCA-derived 14 compounds/mixtures derived from Frs. 1, 2, 3, 4, and 8 displayed differential antioxidant performance for these analyses. Taken together, fractions of UFCA displayed diverse antioxidant and anticancer effects for oral cancer cells. Some fractions of UFCA may be potent natural antioxidant supplements for antioral cancer cell treatment. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Reaction of hydroxyl radicals with azacytosines: a pulse radiolysis and theoretical study.

PubMed

Pramod, G; Prasanthkumar, K P; Mohan, Hari; Manoj, V M; Manoj, P; Suresh, C H; Aravindakumar, C T

2006-10-12

Pulse radiolysis and density functional theory (DFT) calculations at B3LYP/6-31+G(d,p) level have been carried out to probe the reaction of the water-derived hydroxyl radicals (*OH) with 5-azacytosine (5Ac) and 5-azacytidine (5Acyd) at near neutral and basic pH. A low percentage of nitrogen-centered oxidizing radicals, and a high percentage of non-oxidizing carbon-centered radicals were identified based on the reaction of transient intermediates with 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate), ABTS2-. Theoretical calculations suggests that the N3 atom in 5Ac is the most reactive center as it is the main contributor of HOMO, whereas C5 atom is the prime donor for the HOMO of cytosine (Cyt) where the major addition site is C5. The order of stability of the adduct species were found to be C6-OH_5Ac*>C4-OH_5Ac*>N3-OH_5Ac*>N5-OH_5Ac* both in the gaseous and solution phase (using the PCM model) respectively due to the additions of *OH at C6, C4, N3, and N5 atoms. These additions occur in direct manner, without the intervention of any precursor complex formation. The possibility of a 1,2-hydrogen shift from the C6 to N5 in the nitrogen-centered C6-OH_5Ac* radical is considered in order to account for the experimental observation of the high yield of non-oxidizing radicals, and found that such a conversion requires activation energy of about 32 kcal/mol, and hence this possibility is ruled out. The hydrogen abstraction reactions were assumed to occur from precursor complexes (hydrogen bonded complexes represented as S1, S2, S3, and S4) resulted from the electrostatic interactions of the lone pairs on the N3, N5, and O8 atoms with the incoming *OH radical. It was found that the conversion of these precursor complexes to their respective transition states has ample barrier heights, and it persists even when the effect of solvent is considered. It was also found that the formation of precursor complexes itself is highly endergonic in solution phase. Hence, the abstraction reactions will not occur in the present case. Finally, the time dependent density functional theory (TDDFT) calculations predicted an absorption maximum of 292 nm for the N3-OH_5Ac* adduct, which is close to the experimentally observed spectral maxima at 290 nm. Hence, it is assumed that the addition to the most reactive center N3, which results the N3-OH_5Ac* radical, occurs via a kinetically driven process.

Antioxidant and drug detoxification potential of aqueous extract of Annona senegalensis leaves in carbon tetrachloride-induced hepatocellular damage.

PubMed

Ajboye, Taofeek O; Yakubu, Musa T; Salau, Amadu K; Oladiji, Adenike T; Akanji, Musbau A; Okogun, Joseph I

2010-12-01

 Despite the myriad uses of Annona senegalensis Pers. (Annonaceae) leaves in folklore medicine of Nigeria, the basis is yet to be substantiated by scientific investigations.  To investigate the antioxidant (in vitro and in vivo) and drug detoxification potential of aqueous extract of A. senegalensis leaves in CCl₄-induced hepatocellular damage.  In vitro antioxidant activity of the aqueous extract of A. senegalensis leaves was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH), H₂O₂, superoxide ion, 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulfonate) (ABTS) and ferric ion models while in vivo antioxidant and drug detoxification activities of the extract at 100, 200, and 400 mg/kg body weight were done by assaying the levels of enzymic and non-enzymic indices in CCl₄-induced hepatocellular damage.  The extract at 1 mg/mL scavenged DPPH, H₂O₂, superoxide ion, and ABTS radicals, whereas ferric ion was significantly (P <0.05) reduced. The levels of alkaline and acid phosphatases, alanine and aspartate aminotransferases, superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glucose-6-phosphate dehydrogenase, reduced glutathione, vitamins C and E, glutathione S-transferase, nicotinamide adenine dinucleotide (reduced):Quinone oxidoreductase, uridyl diphosphoglucuronyl transferase, malondialdehyde, and lipid hydroperoxide that decreased in CCl₄ treated animals were significantly attenuated by the extract in a manner similar to the animals treated with the reference drug.  The ability of the aqueous extract of A. senegalensis leaves to scavenge free radicals in vitro and reversal of CCl₄-induced hepatocellular damage in rats suggest antioxidant and drug detoxification activities. Overall, this study has justified the rationale behind some of the medicinal uses of the plant in folklore medicine of Nigeria.

Assessment of Antioxidant and Antibacterial Properties on Meat Homogenates of Essential Oils Obtained from Four Thymus Species Achieved from Organic Growth

PubMed Central

Ballester-Costa, Carmen; Viuda-Martos, Manuel

2017-01-01

In the organic food industry, no chemical additives can be used to prevent microbial spoilage. As a consequence, the essential oils (EOs) obtained from organic aromatic herbs and spices are gaining interest for their potential as preservatives. The organic Thymus zygis, Thymus mastichina, Thymus capitatus and Thymus vulgaris EOs, which are common in Spain and widely used in the meat industry, could be used as antibacterial agents in food preservation. The aims of this study were to determine (i) the antibacterial activity using, as culture medium, extracts from meat homogenates (minced beef, cooked ham or dry-cured sausage); and (ii) the antioxidant properties of organic EOs obtained from T. zygis, T. mastichina, T. capitatus and T. vulgaris. The antioxidant activity was determined using different methodologies, such as Ferrous ion-chelating ability assay, Ferric reducing antioxidant power, ABTS radical cation (ABTS•+) scavenging activity assay and 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method; while the antibacterial activity was determined against 10 bacteria using the agar diffusion method in different meat model media. All EOs analyzed, at all concentrations, showed antioxidant activity. T. capitatus and T. zygis EOs were the most active. The IC50 values, for DPPH, ABTS and FIC assays were 0.60, 1.41 and 4.44 mg/mL, respectively, for T. capitatus whilst for T. zygis were 0.90, 2.07 and 4.95 mg/mL, respectively. Regarding antibacterial activity, T. zygis and T. capitatus EOs, in all culture media, had the highest inhibition halos against all tested bacteria. In general terms, the antibacterial activity of all EOs assayed was higher in the medium made with minced beef than with the medium elaborated with cooked ham or dry-cured sausage. PMID:28788051

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao) Bean

PubMed Central

Ademosun, Ayokunle O.; Ademiluyi, Adedayo O.; Omojokun, Olasunkanmi S.; Nwanna, Esther E.; Longe, Kuburat O.

2014-01-01

Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao) bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl (OH), and nitric oxide (NO)] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL), α-glucosidase (1.84 ± 0.17 mg/mL), and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart]) activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL), NO (6.98 ± 0.886 mg/mL), OH (3.72 ± 0.26 mg/mL), and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension. PMID:25295218

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao) Bean.

PubMed

Oboh, Ganiyu; Ademosun, Ayokunle O; Ademiluyi, Adedayo O; Omojokun, Olasunkanmi S; Nwanna, Esther E; Longe, Kuburat O

2014-01-01

Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao) bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl (OH), and nitric oxide (NO)] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL), α-glucosidase (1.84 ± 0.17 mg/mL), and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart]) activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL), NO (6.98 ± 0.886 mg/mL), OH (3.72 ± 0.26 mg/mL), and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension.

Aqueous extracts of microalgae exhibit antioxidant and anticancer activities

PubMed Central

Shanab, Sanaa MM; Mostafa, Soha SM; Shalaby, Emad A; Mahmoud, Ghada I

2012-01-01

Objective To investigate the antioxidant and anticancer activities of aqueous extracts of nine microalgal species. Methods Variable percentages of major secondary metabolites (total phenolic content, terpenoids and alkaloids) as well as phycobiliprotein pigments (phycocyanin, allophycocyanin and phycoerythrin) in the aqueous algal extracts were recorded. Antioxidant activity of the algal extracts was performed using 2, 2 diphenyl-1-picrylhydrazyl (DPPH) test and 2,2′- azino-bis (ethylbenzthiazoline-6-sulfonic acid (ABTS.+) radical cation assay. Anticancer efficiency of the algal water extracts was investigated against Ehrlich Ascites Carcinoma cell (EACC) and Human hepatocellular cancer cell line (HepG2). Results Antioxidant activity of the algal extracts was performed using DPPH test and ABTS.+ radical cation assays which revealed 30.1-72.4% and 32.0-75.9% respectively. Anticancer efficiency of the algal water extracts was investigated against Ehrlich Ascites Carcinoma Cell (EACC) and Human Hepatocellular cancer cell line (HepG2) with an activity ranged 87.25% and 89.4% respectively. Culturing the promising cyanobacteria species; Nostoc muscorum and Oscillatoria sp. under nitrogen stress conditions (increasing and decreasing nitrate content of the normal BG11 medium, 1.5 g/L), increased nitrate concentration (3, 6 and 9 g/L) led to a remarkable increase in phycobilin pigments followed by an increase in both antioxidant and anticancer activities in both cyanobacterial species. While the decreased nitrate concentration (0.75, 0.37 and 0.0 g/L) induced an obvious decrease in phycobilin pigments with complete absence of allophycocyanin in case of Oscillatoria sp. Conclusions Nitrogen starvation (0.00 g/L nitrate) induced an increase and comparable antioxidant and anticancer activities to those cultured in the highest nitrate content. PMID:23569980

Antioxidant activity and chemical composition of essential oils of three aromatic plants from La Rioja province.

PubMed

Barbieri, Natalia; Costamagna, Milena; Gilabert, Miguel; Perotti, Marina; Schuff, Carola; Isla, María Inés; Benavente, Alba

2016-01-01

The use of many traditional medicinal plants is often hampered by the absence of a proper biochemical characterization, which is essential to identify the bioactive compounds present in it. The essential oils (EOs) of three native species from the La Rioja province were analyzed: Lippia turbinata Griseb and Lippia integrifolia (Griseb.) Hieron (Verbenaceae), and Clinopodium gilliesii (Benth.) Kuntze (Lamiaceae). The aim of this study was to evaluate their EOs antioxidant activity (AA) and their chemical composition. EOs were analyzed by gas chromatography-mass spectrometry (GC-MS). To enhance the aqueous solubilization of the EOs, EO-water emulsions were prepared (concentration range of 0.1-6 mg mL(-1)). AA was determined using ABTS, DPPH, and peroxyl radical scavenging assays, as well as by the β-carotene bleaching test. Piperitenone oxide was a major constituent in L. turbinata, pulegone and piperitenone oxide in C. gilliesii, and β-caryophyllene in L. integrifolia. Lippia turbinata EO was the most active ABTS and DPPH radical scavenger (SC50 values of 0.40 ± 0.14 and 0.74 ± 0.08 mg mL(-1), respectively). Clinopodium gilliesii EO exhibited the highest hydrogen peroxide scavenging activity (SC25 value = 1.52 ± 0.27 mg mL(-1)). In the β-carotene assay, L. turbinata EO was more effective at inhibiting lipid peroxidation than the other two oils (IC25 value = 0.15 ± 0.04 mg mL(-1)). Our results suggest that the AA observed can be justified by the presence of oxygenated monoterpenes, mainly piperitenone oxide. Finally, L. turbinata EO might be used as a safe natural antioxidant and food preservative in the food and cosmetic industries.

Structural elucidation and antioxidant activity of lignin isolated from rice straw and alkali‑oxygen black liquor.

PubMed

Jiang, Bo; Zhang, Yu; Gu, Lihui; Wu, Wenjuan; Zhao, Huifang; Jin, Yongcan

2018-05-17

Alkali‑oxygen cooking of lignocellulose offers lignin many structural properties and bioactivities for biorefinery. In this work, milled wood lignin (MWL) and alkali‑oxygen lignin (AOL) were isolated from rice straw and alkali‑oxygen black liquor, respectively. The lignin structure was characterized by spectroscopy and wet chemistry. Antioxidant activity of lignins was assessed by DPPH·and ABTS scavenging ability assay. Results showed the oxidization and condensation of lignin occurred during alkali‑oxygen cooking. The p-hydroxyphenyl was more easily removed from rice straw than guaiacyl and syringyl units. The ester or ether linkages derived from hydroxycynnamic acids, and the main interunit linkages, i.e. β-O-4' bonds, were mostly cleaved. Lignin-xylan complex had high reactivity under alkali‑oxygen condition. Tricin, incorporated into lignin, was detected in MWL but was absent in AOL. Nitrobenzene oxidation showed MWL can well represent the protolignin of rice straw, and the products yield decreased dramatically after alkali‑oxygen cooking. AOL had higher radical scavenging ability than MWL indicating alkali‑oxygen cooking was an effective pathway for the enhancement of antioxidant activity of lignin. Copyright © 2018 Elsevier B.V. All rights reserved.

Upgrading the antioxidant potential of cereals by their fungal fermentation under solid-state cultivation conditions.

PubMed

Bhanja Dey, T; Kuhad, R C

2014-11-01

Solid-state fermentation (SSF) at 30°C for 72 h with four generally recognized as safe (GRAS) filamentous fungi (Aspergillus oryzae NCIM 1212, Aspergillus awamori MTCC No. 548, Rhizopus oligosporus NCIM 1215 and Rhizopus oryzae RCK2012) showed high efficiency for the improvement of water-soluble total phenolic content (TPC) and antioxidant properties including ABTS(●+) [2,2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid)] and DPPH(●) (2,2'-diphenyl-1-picrylhydrazyl) scavenging capacities of four whole grain cereals, namely wheat, brown rice, maize and oat. A maximum 14-fold improvement in TPC (11·61 mg gallic acid equivalent g(-1) grain) was observed in A. oryzae fermented wheat, while extract of R. oryzae fermented wheat (ROFW) showed maximum of 6·6-fold and fivefold enhancement of DPPH(●) scavenging property (8·54 μmol Trolox equivalent g(-1) grain) and ABTS(●+) scavenging activity (19·5 μmol Trolox equivalent g(-1) grain), respectively. The study demonstrates that SSF is an efficient method for the improvement of antioxidant potentials of cereals and R. oryzae RCK2012 fermented wheat can be a powerful source of natural antioxidants. Antioxidant-rich food products are getting popularity day by day. In this study, potential of solid-state fermentation (SSF) has been studied for the improvement of antioxidant potential of different cereals by GRAS micro-organisms. The comparative evaluation of the antioxidant potential of various fungal fermented products derived from whole grain cereals, such as wheat, brown rice, oat and maize, has been carried out. Among these, Rhizopus oryzae RCK2012-fermented wheat was observed as a potent source of natural antioxidants. A diet containing fermented cereals would be useful for the prevention of free radical-mediated diseases. © 2014 The Society for Applied Microbiology.

In vitro assessment of antioxidant, phytochemical and nutritional properties of extracts from the leaves of Ocimum gratissimum (Linn).

PubMed

Igbinosa, Etinosa O; Uzunuigbe, Edwina O; Igbinosa, Isoken H; Odjadjare, Emmanuel E; Igiehon, Nicholas O; Emuedo, Oke A

2013-01-01

The antioxidant, phytochemical and nutritional properties of acetone, methanol and aqueous extracts of the leaves of Ocimum gratissimum (Linn) were investigated to evaluate the therapeutic and nutritional potential of the leaves of this plant. The antioxidant of the plant extracts were assessed against 1,1-Diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and ferric reducing agent. Total phenolics, flavonoids, flavonols and proanthocyanidins were determined to assess their corresponding effect on the antioxidant activity of this plant. The extracts exhibited DPPH and ABTS(·+) radical scavenging activities, which was comparable to butylated hydroxytoluene (BHT). The phytochemical screening revealed the presence of alkaloids, tannins, saponin, steroids, cardiacglycoside, flavonoid, terpenoids and phenol. The proximate analysis confirms that the leaves contain appreciable amount of ash, crude protein, lipids, fibre and carbohydrates. The macro and micro elements and constituents revealed that the leaves contain significant amount of sodium, potassium, calcium, magnesium, iron, zinc, phosphorus, copper, nitrogen, and manganese. This study shows that the leaf can be used as a therapeutic agent and justifies its application in folkloric medicine.

Antioxidant activity of apples--an impact of maturity stage and fruit part.

PubMed

Duda-Chodak, Aleksandra; Tarko, Tomasz; Tuszyński, Tadeusz

2011-01-01

Recently, many studies have been oriented towards improving methods and efficiency of antioxidants recovery from different fruit and their wastes.The aim of the study was to evaluate antioxidant potential of apple seeds and peel, which constitute the fruit industry wastes, and compare it to apple flesh. Antioxidant activity of apples at different maturity and storage stage were analysed too. The Idared and the Šampion cultivars of apples were used in the study. Antioxidant activity was estimated using ABTS and DPPH assays, and polyphenols profile was determined by HPLC method. Seeds of analysed apple cultivars were characterised by a significantly higher antioxidant capacity and by higher concentrations of polyphenols analysed when compared to their peel and flesh. There were present two predominant compounds: phloridzin in seeds (84% and 72%) and quercetin glycosides in peels (54% and 38%, Idared and Šampion cultivars, respectively). No quercetin glycosides in seeds were found. The capacity to scavenge an ABTS radical, but not DPPH, decreased during ripening of apples, while cold storage resulted in enhanced antioxidant potential. It can be concluded that unripe apples together with apple seeds and peel (fruit industry wastes) constitute a valuable source of polyphenols.

A polyphenol-enriched cocoa extract reduces free radicals produced by mycotoxins.

PubMed

Corcuera, L A; Amézqueta, S; Arbillaga, L; Vettorazzi, A; Touriño, S; Torres, J L; López de Cerain, A

2012-03-01

Polyphenols are characterized by the presence of phenol units in the molecules. These compounds may show antioxidant ability by scavenging reactive oxygen species (ROS) of the free radical type. A polyphenol enriched cocoa extract (PECE) was obtained from cocoa seeds with 28% of procyanidins which were mainly epicatechin oligomers. PECE was very active as free radical scavenger against 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and tris(2,4,6-trichloro-3,5-dinitrophenyl)methyl (HNTTM) radicals; and the tris(2,3,5,6-tetrachloro-4-nitrophenyl)methyl (TNPTM) assay showed that the PECE might not be pro-oxidant. Thus it was considered a good candidate to be tested in in vitro models. It showed mild cytotoxic power on Hep G2 cells and induced ROS in a dose-dependent manner being weak oxidant only at high concentrations near the limit of solubility. The antioxidant properties were assayed in Hep G2 treated with the mycotoxins ochratoxin A (OTA) and/or aflatoxin B1 (AFB1). The PECE was not effective against AFB1 but it increased the cell viability and reduced significantly the amounts of ROS in cells treated with OTA or mixtures of AFB1+OTA. These results are coherent with the role of oxidative pathways in the mechanism of OTA and indicate that polyphenols extracted from cocoa may be good candidates as antioxidant agents. Copyright © 2011 Elsevier Ltd. All rights reserved.

Preventive efficacy of hydroalcoholic extract of Cymbopogon citratus against radiation-induced DNA damage on V79 cells and free radical scavenging ability against radicals generated in vitro.

PubMed

Rao, B S S; Shanbhoge, R; Rao, B N; Adiga, S K; Upadhya, D; Aithal, B K; Kumar, M R S

2009-04-01

This study presents the findings of free radical scavenging and antigenotoxic effect of hydroalcoholic extract of Cymbopogon citratus (CCE). The CCE at a concentration of 60 microg/mL resulted in a significant scavenging ability of 2,2-diphenyl-2-picryl hydrazyl (DPPH; (85%), 2,2-azinobis (3-ethyl benzothiazoline-6-sulphonic acid) (ABTS; 77%), hydroxyl (70%), superoxide (76%), nitric oxide (78%) free radicals generated using in vitro and also a moderate anti-lipid peroxidative effect (57%). Further, the radiation-induced antigenotoxic potential of CCE was assessed in Chinese hamster lung fibroblast cells (V79) using micronucleus assay. The CCE resulted in a dose-dependent decrease in the yield of radiation-induced micronuclei, with a maximum effect at 125 microg/mL CCE for 1 h before 2 Gy of radiation. Similarly, there was a significant (P < 0.05-0.0001) decrease in percentage of micronuclei when V79 cells were treated with optimal dose of CCE (125 microg/mL) before exposure to different doses of gamma radiation, that is, 0.5-4 Gy, compared with radiation alone groups. The results of the micronucleus study indicated antigenotoxic effect demonstrating the radioprotective potential of CCE and, which may partly due to its and antioxidant capacity as it presented its ability to scavenge various free radicals in vitro and anti-lipid peroxidative potential.

Increasing the applications of Crocus sativus flowers as natural antioxidants.

PubMed

Serrano-Díaz, Jéssica; Sánchez, Ana M; Maggi, Luana; Martínez-Tomé, Magdalena; García-Diz, Luis; Murcia, M Antonia; Alonso, Gonzalo L

2012-11-01

Large amounts of floral bio-residues (92.6 g per 100 g of flowers) are generated and wasted in the production of saffron (Crocus sativus) spice. Progress in mechanization of saffron crop offer the opportunity to expand the uses of C. sativus flowers, beyond the spice (dried stigmas). The antioxidant potential of flowers of saffron, their separate parts (tepals, stamens, styles, and stigmas) and floral bio-residues were evaluated by 4 in vitro assays: lipid peroxidation, deoxyribose assay, Rancimat test, and Trolox equivalent antioxidant capacity. Phenolic content and crocetin ester composition were also determined. All the samples studied showed to be potential antioxidants. The highest phenolic, flavonoid, and anthocyanin contents were observed in tepals. Stamens showed lower phenolic, flavonoid, and anthocyanin contents than those of whole flowers, tepals, and floral bio-residues. Crocetin esters were not found in tepals or stamens. Stamens exhibited the most potent LOO(•) and OH(•) radicals scavenging activity, being higher than those of food antioxidant propyl gallate. Flowers of saffron, tepals, stamens, styles, and floral bio-residues showed LOO(•), OH(•), and ABTS(•-) radicals scavenging activity, while stigmas showed LOO(•) and ABTS(•-) radicals scavenging activity. All samples studied improved the oxidative stability of sunflower oil in Rancimat test. These antioxidant properties could suggest the application of this floral material as functional ingredients with the subsequent added value. Saffron spice, the most valuable spice worldwide, is the dried stigma that only represents 7.4% of Crocus sativus flowers. Other parts of the flowers different to stigmas are discarded. Flower harvest and all the postharvest steps to produce saffron spice are performed manually. Mechanization of flower collection, stigma separation, and dehydration process is a revolution in saffron spice production, which increases the productive capacity making it possible to extend the uses of C. sativus flowers, beyond the production of saffron spice. Flowers possessed high-phenolic content and excellent antioxidant properties that could contribute to their application as functional ingredients. © 2012 Institute of Food Technologists®

Evaluation of chemical property, cytotoxicity and antioxidant activity in vitro and in vivo of polysaccharides from Fuzhuan brick teas.

PubMed

Chen, Guijie; Wang, Mingjia; Xie, Minhao; Wan, Peng; Chen, Dan; Hu, Bing; Ye, Hong; Zeng, Xiaoxiong; Liu, Zhonghua

2018-05-03

Fuzhuan brick tea (FBT) possesses various health-promoting functions. However, the available information regarding biological activity of polysaccharides from FBT (FBTPS) is still limited. In this work, the chemical property, cytotoxicity and antioxidant activity in vitro and in vivo of FBTPS were evaluated. It was found that FBTPSs were typical acidic heteropolysaccharides mainly composed of Man, Rha, GalA, Glc, Gal and Ara with little molar content of Rib and GlcA. FBTPS showed little toxicity to human hepatic epithelial (L-02) cell. FBTPS exhibited antioxidant activities, including limited scavenging activity on DPPH free radicals (ranged from 54.3 ± 1.9 to 67.8 ± 2.5%), noticeable scavenging activity on superoxide radicals (over 85%), superior scavenging activity on ABTS radicals (near 100%), and protective effect on H 2 O 2 -induced oxidative injury in rat pheochromocytoma line 12 (PC12) cell. Moreover, FBTPS showed significant amelioration of high-fat diet-induced oxidative injury in mice. The results suggest that FBTPS, as natural safe antioxidants, may have potential application in functional foods. Copyright © 2018 Elsevier B.V. All rights reserved.

Enzyme inhibitory and radical scavenging effects of some antidiabetic plants of Turkey.

PubMed

Orhan, Nilüfer; Hoçbaç, Sanem; Orhan, Didem Deliorman; Asian, Mustafa; Ergun, Fatma

2014-06-01

Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum), are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2) on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml). Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes.

Radical Scavenging Activities of Tannin Extracted from Amaranth (Amaranthus caudatus L.).

PubMed

Jo, Hyeon-Ju; Chung, Kang-Hyun; Yoon, Jin A; Lee, Kwon-Jai; Song, Byeong Chun; An, Jeung Hee

2015-06-01

This study investigates the bioactivity of tannin from amaranth (Amaranthus caudatus L.) extracts. The antioxidant activities of the extracts from amaranth leaves, flowers, and seeds were evaluated. Tannin from leaves of amaranth has been evaluated for superoxide scavenging activity by using DPPH and ABTS(+) analysis, reducing power, protective effect against H2O2-induced oxidative damage in L-132 and BNL-CL2 cells, and inhibition of superoxide radical effects on HL-60 cells. At a concentration of 100 μg/ml, tannin showed protective effects and restored cell survival to 69.2% and 41.8% for L-132 and BNL-CL2 cells, respectively. Furthermore, at the same concentration, tannin inhibited 41% of the activity of the superoxide radical on HL-60 cells and 43.4% of the increase in nitric oxide levels in RAW 264.7 cells. The expression levels of the antioxidant-associated protein SOD-1 were significantly increased in a concentration-dependent manner in RAW 264.7 cells treated with tannin from amaranth leaves. These results suggest that tannin from the leaves of Amaranthus caudatus L. is a promising source of antioxidant component that can be used as a food preservative or nutraceutical.

Synthesis, characterization, Hirshfeld surface analysis and antioxidant activity of a novel organic-inorganic hybrid material 1-methylpiperazine-1,4-diium bis(nitrate)

NASA Astrophysics Data System (ADS)

Gatfaoui, Sofian; Mezni, Ali; Roisnel, Thierry; Marouani, Houda

2017-07-01

The new inorganic-organic hybrid material 1-methylpiperazine-1,4-diium bis(nitrate) (MPN) have been synthesized and crystallized to the orthorhombic system with space group Pnma and the lattice parameters obtained are a = 10.9385(9) Å, b = 6.5698 Å (4), c = 13.7021(10) Å, V = 984.68(12) Å3 and Z = 4. The trigonal (NO3-) anions are connected to the 1-methylpiperazine-1,4-diium cations via a large number of bifurcated and non-bifurcated Nsbnd H⋯O and Csbnd H⋯O hydrogen bonds. The diprotonated piperazine ring adopts a chair conformation, with the methyl group occupying an equatorial position. Intermolecular interactions in the crystal structure were quantified by Hirshfeld surface analysis. Infrared spectrum confirms the existence of the functional groups in the elaborated material. Optical absorption reveals an important band gap energy indicating stability of the title compound. The DTA/TGA and DSC curves indicate that the crystal is thermally stable up to 180 °C. The antioxidant properties were determined via the DPPH radical scavenging, the ABTS radical scavenging, hydroxyl radical scavenging and ferric reducing power (FRP).

Winery by-products: extraction optimization, phenolic composition and cytotoxic evaluation to act as a new source of scavenging of reactive oxygen species.

PubMed

Melo, Priscilla Siqueira; Massarioli, Adna Prado; Denny, Carina; dos Santos, Luciana Ferracini; Franchin, Marcelo; Pereira, Giuliano Elias; Vieira, Thais Maria Ferreira de Souza; Rosalen, Pedro Luiz; de Alencar, Severino Matias

2015-08-15

Nearly 20 million tons of winery by-products, with many biological activities, are discarded each year in the world. The extraction of bioactive compounds from Chenin Blanc, Petit Verdot, and Syrah grape by-products, produced in the semi-arid region in Brazil, was optimized by a Central Composite Rotatable Design. The phenolic compounds profile, antioxidant capacity against synthetic free radicals (DPPH and ABTS), reactive oxygen species (ROS; peroxyl radical, superoxide radical, hypochlorous acid), cytotoxicity assay (MTT) and quantification of TNF-α production in RAW 264.7 cells were conducted. Gallic acid, syringic acid, procyanidins B1 and B2, catechin, epicatechin, epicatechin gallate, quercetin 3-β-d-glucoside, delfinidin 3-glucoside, peonidin 3-O-glucoside, and malvidin 3-glucoside were the main phenolic compounds identified. In general, rachis showed higher antioxidant capacity than pomace extract, especially for Chenin Blanc. All extracts showed low cytotoxicity against RAW 264.7 cells and Petit Verdot pomace suppressed TNF-α liberation in vitro. Therefore, these winery by-products can be considered good sources of bioactive compounds, with great potential for application in the food and pharmaceutical industries. Copyright © 2015 Elsevier Ltd. All rights reserved.

Effects of baking conditions, dough fermentation, and bran particle size on antioxidant properties of whole-wheat pizza crusts.

PubMed

Moore, Jeffrey; Luther, Marla; Cheng, Zhihong; Yu, Liangli Lucy

2009-02-11

This study investigated the effects of processing conditions including bran particle size, dough fermentation time, and baking time and temperature on the extractable antioxidant properties of whole-wheat pizza crust. Experiments were carried out using two different varieties of hard white winter wheat, Trego and Lakin. Antioxidant properties examined included oxygen radical absorbing capacity (ORAC), hydroxyl radical scavenging capacity (HOSC), relative 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity (RDSC), cation 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging capacity, total phenolic contents (TPC), and ferulic acid contents. Results indicated that bran particle size had no effect on the antioxidant properties evaluated. Increasing dough fermentation time from 0 to 48 h had no significant influence on antioxidant properties except HOSC, which increased as much as 28%, possibly as a result of increase in soluble free ferulic acid, which increased as much as 130%. Increasing baking temperature from 204 to 288 degrees C with a 7 min bake time increased all evaluated antioxidant properties by as much as 82%. Increasing baking time from 7 to 14 min with 204 degrees C baking temperature might increase some antioxidant properties as much as 60%. The results from this study suggest that longer dough fermentation times and increased baking time or temperature may be potential approaches to increase the antioxidant availability in whole-wheat pizza crust.

Antimutagenic and free radical scavenger effects of leaf extracts from Accacia salicina.

PubMed

Boubaker, Jihed; Mansour, Hedi Ben; Ghedira, Kamel; Chekir-Ghedira, Leila

2011-12-01

Three extracts were prepared from the leaves of Accacia salicina; ethyl acetate (EA), chloroform (Chl) and petroleum ether (PE) extracts and was designed to examine antimutagenic, antioxidant potenty and oxidative DNA damage protecting activity. Antioxidant activity of A. salicina extracts was determined by the ability of each extract to protect against plasmid DNA strand scission induced by hydroxyl radicals. An assay for the ability of these extracts to prevent mutations induced by various oxidants in Salmonella typhimurium TA102 and TA 104 strains was conducted. In addition, nonenzymatic methods were employed to evaluate anti-oxidative effects of tested extracts. These extracts from leaf parts of A. salicina showed no mutagenicity either with or without the metabolic enzyme preparation (S9). The highest protections against methylmethanesulfonate induced mutagenicity were observed with all extracts and especially chloroform extract. This extract exhibited the highest inhibitiory level of the Ames response induced by the indirect mutagen 2- aminoanthracene. All extracts exhibited the highest ability to protect plasmid DNA against hydroxyl radicals induced DNA damages. The ethyl acetate (EA) and chloroform (Chl) extracts showed with high TEAC values radical of 0.95 and 0.81 mM respectively, against the ABTS(.+). The present study revealed the antimutagenic and antioxidant potenty of plant extract from Accacia salicina leaves. © 2011 Boubaker et al; licensee BioMed Central Ltd.

Preclinical discovery of candidate genes to guide pharmacogenetics during phase I development: the example of the novel anticancer agent ABT-751

PubMed Central

Innocenti, Federico; Ramírez, Jacqueline; Obel, Jennifer; Xiong, Julia; Mirkov, Snezana; Chiu, Yi-Lin; Katz, David A.; Carr, Robert A.; Zhang, Wei; Das, Soma; Adjei, Araba; Moyer, Ann M.; Chen, Pei Xian; Krivoshik, Andrew; Medina, Diane; Gordon, Gary B.; Ratain, Mark J.; Sahelijo, Leonardo; Weinshilboum, Richard M.; Fleming, Gini F.; Bhathena, Anahita

2013-01-01

Objective ABT-751, a novel orally available antitubulin agent, is mainly eliminated as inactive glucuronide (ABT-751G) and sulfate (ABT-751S) conjugates. We performed a pharmacogenetic investigation of ABT-751 pharmacokinetics using in-vitro data to guide the selection of genes for genotyping in a phase I trial of ABT-751. Methods UDP-glucuronosyltransferase (UGT) and sulfotransferase (SULT) enzymes were screened for ABT-751 metabolite formation in vitro. Forty-seven cancer patients treated with ABT-751 were genotyped for 21 variants in these genes. Results UGT1A1, UGT1A4, UGT1A8, UGT2B7, and SULT1A1 were found to be involved in the formation of inactive ABT-751 glucuronide (ABT-751G) and sulfate (ABT-751S). SULT1A1 copy number (> 2) was associated with an average 34% increase in ABT-751 clearance (P= 0.044), an 18% reduction in ABT-751 AUC (P = 0.045), and a 50% increase in sulfation metabolic ratios (P=0.025). UGT1A8 rs6431558 was associated with a 28% increase in glucuronidation metabolic ratios (P =0.022), and UGT1A4*2 was associated with a 65% decrease in ABT-751 Ctrough (P = 0.009). Conclusion These results might represent the first example of a clinical pharmacokinetic effect of the SULT1A1 copy number variant on the clearance of a SULT1A1 substrate. A-priori selection of candidate genes guided by in-vitro metabolic screening enhanced our ability to identify genetic determinants of interpatient pharmacokinetic variability. PMID:23670235

Understanding the Effects of Roasting on Antioxidant Components of Coffee Brews by Coupling On‐line ABTS Assay to High Performance Size Exclusion Chromatography

PubMed Central

Opitz, Sebastian E.W.; Goodman, Bernard A.; Keller, Marco; Smrke, Samo; Wellinger, Marco; Schenker, Stefan

2016-01-01

Abstract Introduction Coffee is a widely consumed beverage containing antioxidant active compounds. During roasting the phytochemical composition of the coffee bean changes dramatically and highly polymeric substances are produced. Besides chlorogenic acids that are already present in green coffee beans, melanoidins show antioxidant capacity as well. Objective To employ post‐column derivatisation by coupling high performance size exclusion chromatography (HPSEC) to an antioxidant assay to investigate the effect of roasting on the properties of antioxidant active compounds in coffee brews. Methodology We have investigated the antioxidant capacity of Coffea arabica (Arabica) and C. canephora (Robusta) beans that were roasted over the full spectrum of roast conditions (four roasting speeds to three roast degrees) by comparing the results from HPSEC coupled on‐line to the ABTS assay with those from two batch assays, Folin Ciocalteu (FC) and oxygen radical absorbance capacity (ORAC) assay. Results The antioxidant capacity showed a general decrease towards slower and darker roasted coffee for all three assays, indicative of heat degradation of active compounds. Hence, low molecular weight (LMW) compounds such as chlorogenic acids (CGAs) decreased progressively already from relatively mild roasting conditions. In contrast, high molecular weight (HMW) compounds (e.g. melanoidins) increased from light to dark roast degrees with lowering magnitude towards slower roasting profiles. Conclusion By coupling HPSEC on‐line to the ABTS assay we were able to separately quantify the contribution of HMW and LMW compounds to the total antioxidant capacity, increasing our understanding of the roast process. © 2016 The Authors. Phytochemical Analysis Published by John Wiley & Sons Ltd. PMID:28008674

Phenolics extraction from sweet potato peels: modelling and optimization by response surface modelling and artificial neural network.

PubMed

Anastácio, Ana; Silva, Rúben; Carvalho, Isabel S

2016-12-01

Sweet potato peels (SPP) are a major waste generated during root processing and currently have little commercial value. Phenolics with free radical scavenging activity from SPP may represent a possible added-value product for the food industry. The aqueous extraction of phenolics from SPP was studied using a Central Composite Design with solvent to solid ratio (30-60 mL g -1 ), time (30-90 min) and temperature (25-75 °C) as independent variables. The comparison of response surface methodology (RSM) and artificial neural network (ANN) analysis on extraction modelling and optimising was performed. Temperature and solvent to solid ratio, alone and in interaction, presented a positive effect in TPC, ABTS and DPPH assays. Time was only significant for ABTS assay with a negative influence both as main effect and in interaction with other independent variables. RSM and ANN models predicted the same optimal extraction conditions as 60 mL g -1 for solvent to solid ratio, 30 min for time and 75 °C for temperature. The obtained responses in the optimized conditions were as follow: 11.87 ± 0.69 mg GAE g -1 DM for TPC, 12.91 ± 0.42 mg TE g -1 DM for ABTS assay and 46.35 ± 3.08 mg TE g -1 DM for DPPH assay. SPP presented similar optimum extraction conditions and phenolic content than peels of potato, tea fruit and bambangan. Predictive models and the optimized extraction conditions offers an opportunity for food processors to generate products with high potential health benefits.

Understanding the Effects of Roasting on Antioxidant Components of Coffee Brews by Coupling On-line ABTS Assay to High Performance Size Exclusion Chromatography.

PubMed

Opitz, Sebastian E W; Goodman, Bernard A; Keller, Marco; Smrke, Samo; Wellinger, Marco; Schenker, Stefan; Yeretzian, Chahan

2017-03-01

Coffee is a widely consumed beverage containing antioxidant active compounds. During roasting the phytochemical composition of the coffee bean changes dramatically and highly polymeric substances are produced. Besides chlorogenic acids that are already present in green coffee beans, melanoidins show antioxidant capacity as well. To employ post-column derivatisation by coupling high performance size exclusion chromatography (HPSEC) to an antioxidant assay to investigate the effect of roasting on the properties of antioxidant active compounds in coffee brews. We have investigated the antioxidant capacity of Coffea arabica (Arabica) and C. canephora (Robusta) beans that were roasted over the full spectrum of roast conditions (four roasting speeds to three roast degrees) by comparing the results from HPSEC coupled on-line to the ABTS assay with those from two batch assays, Folin Ciocalteu (FC) and oxygen radical absorbance capacity (ORAC) assay. The antioxidant capacity showed a general decrease towards slower and darker roasted coffee for all three assays, indicative of heat degradation of active compounds. Hence, low molecular weight (LMW) compounds such as chlorogenic acids (CGAs) decreased progressively already from relatively mild roasting conditions. In contrast, high molecular weight (HMW) compounds (e.g. melanoidins) increased from light to dark roast degrees with lowering magnitude towards slower roasting profiles. By coupling HPSEC on-line to the ABTS assay we were able to separately quantify the contribution of HMW and LMW compounds to the total antioxidant capacity, increasing our understanding of the roast process. © 2016 The Authors. Phytochemical Analysis Published by John Wiley & Sons Ltd. © 2016 The Authors. Phytochemical Analysis Published by John Wiley & Sons Ltd.

Anti-inflammatory, cyclooxygenase inhibitory and antioxidant activities of standardized extracts of Tridax procumbens L.

PubMed

Jachak, Sanjay M; Gautam, Raju; Selvam, C; Madhan, Himanshu; Srivastava, Amit; Khan, Taj

2011-03-01

The standardized EtOAc, MeOH and 70% EtOH extracts of Tridax procumbens aerial parts showed significant inhibition of rat paw edema at a medium dose of 200mg/kg and the EtOAC extract was the most active. These extracts were standardized by HPLC with the help of chemical markers. Further, the extracts were evaluated for COX-1 and COX-2 inhibitory activity and EtOAc extract exhibited the highest inhibition of COX-1 and COX-2 at 50 μg/mL. Cent aurein, centaureidin and bergenin were isolated as COX-1 and COX-2 inhibitory principles from the EtOAc extract. The extracts also exhibited antioxidant activity against DPPH and ABTS free radicals. The anti-inflammatory activity of T. procumbens aerial parts could be at least in part due to COX-1, COX-2 enzyme inhibition and free radical-scavenging activities which may be attributed to the presence of flavonoids and other polyphenols in the extracts. Copyright © 2010 Elsevier B.V. All rights reserved.

Phytochemical composition, in vitro antioxidant activity and antibacterial mechanisms of Neolamarckia cadamba fruits extracts.

PubMed

Pandey, Arti; Negi, Pradeep Singh

2018-05-01

Aqueous extracts of Neolamarckia cadamba fruits prepared at different maturity stages were used for the analysis of various phytochemicals, and their antioxidant and antibacterial activities were determined. Ripe fruit extract had highest phenolics (3.14 mM GAE/ g fruit extract) with caffeic acid, tannic acid, syringic acid and quercetin as major phenolic compounds. The ripe fruit extract showed lowest IC 50 values in DPPH radical scavenging assay (231.33 μg fruit extract/ mL), and highest ABTS radical scavenging activity (111.18 μM TEAC/g). Immature fruit extract showed lowest minimum inhibitory concentration against tested bacteria, and the antibacterial activity was probably due to membrane permeation, as was evident by leakage of genetic material and reduction in propidium iodide uptake by bacterium; and by inhibition of sugar and amino acid uptake. The appreciable amount of phenolic compounds and biological activities in the aqueous extracts of N. cadamba fruits suggests it's potential application as natural preservative.

Cooking quality properties and free and bound phenolics content of brown, black, and red rice grains stored at different temperatures for six months.

PubMed

Ziegler, Valmor; Ferreira, Cristiano Dietrich; Hoffmann, Jessica Fernanda; Chaves, Fábio Clasen; Vanier, Nathan Levien; de Oliveira, Maurício; Elias, Moacir Cardoso

2018-03-01

The changes in cooking quality and phenolic composition of whole black and red rice grains stored during six months at different temperatures were evaluated. Brown rice with known cooking quality properties and low phenolic levels was used for purposes comparison. All rice genotypes were stored at 13% moisture content at temperatures of 16, 24, 32, and 40°C. Cooking time, hardness, free and bound phenolics, anthocyanins, proanthocyanidins, and free radical scavenging capacity were analysed. The traditional rice with brown pericarp exhibited an increase in cooking time and free phenolics content, while rice with black pericarp exhibited a reduction in cooking time after six months of storage at the highest studied temperature of 40°C. There as increases in ferulic acid levels occurred as a function of storage temperature. Red pericarp rice grains showed decreased antioxidant capacity against ABTS radical for the soluble phenolic fraction with increased time and storage temperature. Copyright © 2017 Elsevier Ltd. All rights reserved.

Antiparkinson drug--Mucuna pruriens shows antioxidant and metal chelating activity.

PubMed

Dhanasekaran, Muralikrishnan; Tharakan, Binu; Manyam, Bala V

2008-01-01

Parkinson's disease is a neurodegenerative disorder for which no neurorestorative therapeutic treatment is currently available. Oxidative stress plays an important role in the pathophysiology of Parkinson's disease. The ancient Indian medical system, Ayurveda, traditionally uses Mucuna pruriens to treat Parkinson's disease. In our earlier studies, Mucuna pruriens has been shown to possess antiparkinson and neuroprotective effects in animal models of Parkinson's disease. The antioxidant activity of Mucuna pruriens was demonstrated by its ability to scavenge DPPH radicals, ABTS radicals and reactive oxygen species. Mucuna pruriens significantly inhibited the oxidation of lipids and deoxyribose sugar. Mucuna pruriens exhibited divalent iron chelating activity and did not show any genotoxic/mutagenic effect on the plasmid DNA. These results suggest that the neuroprotective and neurorestorative effect of Mucuna pruriens may be related to its antioxidant activity independent of the symptomatic effect. In addition, the drug appears to be therapeutically safe in the treatment of patients with Parkinson's disease. Copyright (c) 2007 John Wiley & Sons, Ltd.

Release properties of tannic acid from hydrogen bond driven antioxidative cellulose nanofibrous films.

PubMed

Zhou, Bin; Hu, Xiaoqian; Zhu, Jinjin; Wang, Zhenzhen; Wang, Xichang; Wang, Mingfu

2016-10-01

Layer-by-layer (LBL) assembled films have been exploited for surface-mediated bioactive compound delivery. Here, an antioxidative hydrogen-bonded multilayer electrospun nanofibrous film was fabricated from tannic acid (TA), acting as a polyphenolic antioxidant, and poly(ethylene glycol) (PEG) via layer-by-layer assembly. It overcame the burst release behavior of nanofibrous carrier, due to the reversible/dynamic nature of hydrogen bond, which was responded to external stimuli. The PEG/TA nanofibrous films disassembled gradually and released TA to the media, when soaked in aqueous solutions. The release rate of TA increased with increasing bilayer number, pH and temperature, but decreased with enhancing ionic strength. The surface morphology of the nanofibrous mats was observed by scanning electron microscopy (SEM). The following antioxidant activity assay revealed that it could scavenge DPPH free radicals and ABTS(+) cation radicals, a major biological activity of polyphenols. This technology can be used to fabricate other phenolic-containing slowly releasing antioxidative nanofibrous films. Copyright © 2016 Elsevier B.V. All rights reserved.

Antioxidant properties of Australian canola meal protein hydrolysates.

PubMed

Alashi, Adeola M; Blanchard, Christopher L; Mailer, Rodney J; Agboola, Samson O; Mawson, A John; He, Rong; Girgih, Abraham; Aluko, Rotimi E

2014-03-01

Antioxidant activities of canola protein hydrolysates (CPHs) and peptide fractions prepared using five proteases and ultrafiltration membranes (1, 3, 5, and 10kDa) were investigated. CPHs had similar and adequate quantities of essential amino acids. The effective concentration that scavenged 50% (EC50) of the ABTS(+) was greatest for the <1kDa pancreatin fraction at 10.1μg/ml. CPHs and peptide fractions scavenged DPPH(+) with most of the EC50 values being <1.0mg/ml. Scavenging of superoxide radical was generally weak, except for the <1kDa pepsin peptide fraction that had a value of 51%. All CPHs inhibited linoleic acid oxidation with greater efficiency observed for pepsin hydrolysates. The oxygen radical absorbance capacity of Alcalase, chymotrypsin and pepsin hydrolysates was found to be better than that of glutathione (GSH) (p<0.05). These results show that CPHs have the potential to be used as bioactive ingredients in the formulation of functional foods against oxidative stress. Copyright © 2013 Elsevier Ltd. All rights reserved.

Application of Attenuated Total Reflectance-Fourier Transformed Infrared (ATR-FTIR) Spectroscopy To Determine the Chlorogenic Acid Isomer Profile and Antioxidant Capacity of Coffee Beans.

PubMed

Liang, Ningjian; Lu, Xiaonan; Hu, Yaxi; Kitts, David D

2016-01-27

The chlorogenic acid isomer profile and antioxidant activity of both green and roasted coffee beans are reported herein using ATR-FTIR spectroscopy combined with chemometric analyses. High-performance liquid chromatography (HPLC) quantified different chlorogenic acid isomer contents for reference, whereas ORAC, ABTS, and DPPH were used to determine the antioxidant activity of the same coffee bean extracts. FTIR spectral data and reference data of 42 coffee bean samples were processed to build optimized PLSR models, and 18 samples were used for external validation of constructed PLSR models. In total, six PLSR models were constructed for six chlorogenic acid isomers to predict content, with three PLSR models constructed to forecast the free radical scavenging activities, obtained using different chemical assays. In conclusion, FTIR spectroscopy, coupled with PLSR, serves as a reliable, nondestructive, and rapid analytical method to quantify chlorogenic acids and to assess different free radical-scavenging capacities in coffee beans.

ANTIOXIDANT ACTIVITY AND A-AMYLASE INHIBITORY POTENTIAL OF ROSA CANINA L.

PubMed

Jemaa, Houda Ben; Jemia, Amani Ben; Khlifi, Sarra; Ahmed, Halima Ben; Slama, Fethi Ben; Benzarti, Anis; Elati, Jalila; Aouidet, Abdallah

2017-01-01

Diabetes mellitus is one of the most common endocrinal disorders and medicinal plants continue to play an important role in the management of this disease. In this study, Rosa canina was investigated for the antioxidant and α-amylase inhibition activities. Methanolic extract of Rosa canina was investigated for its potential antioxidant activity. The extracts' total phenolic and flavonoid contents and scavenging capacity for free radicals were evaluated. The α-amylase inhibition assay was also carried. Rosa canina extract exhibits a total Phenolic and flavonoid levels respectively (21.918 mg GAE/g and 2.647mg ER/g). The free radical scavenging activity was found to be prominent against DPPH with an IC50 of 0.668 mg/ml and against ABTS with an IC50 of 0.467 mg/ml. Extract showed a significant ferric ion reducing activities with an IC50 of4.962 mg/ml. Rosa canina exerted a higher inhibitory activity against α-amylase. The obtained results support the antidiabetic use of rosa canina .

Optimisation of pressurised liquid extraction of antioxidants from black bamboo leaves.

PubMed

Shang, Ya Fang; Kim, Sang Min; Um, Byung-Hun

2014-07-01

To develop an efficient green extraction approach for recovering bioactive compounds from natural plants, the potential of using pressurised liquid extraction (PLE) was examined on black bamboo (Phyllostachys nigra) leaves, with ethanol/water as solvents. The superheated PLE process showed a higher recovery of most constituents and antioxidative activity, compared to reflux extraction, with a significantly improved recovery of the total phenolic (TP) and flavonoid (TF) content and DPPH radical scavenging ability. For a broad range of ethanol aqueous solutions and temperatures, 50% EtOH and 200°C (static time: 25min) gave the best performance, in terms of the TP and TF (75% EtOH) content yield and DPPH scavenging ability (25% EtOH). Under the optimised extraction conditions, eight main antioxidative compounds were isolated and identified with HPLC-ABTS(+) assay guidance and assessed for radical scavenging activity. The superheated extraction process for black bamboo leaves enhanced the antioxidant properties by increasing the extraction of the phenolic components. Copyright © 2013 Elsevier Ltd. All rights reserved.

Isolation, identification and synthesis of four novel antioxidant peptides from rice residue protein hydrolyzed by multiple proteases.

PubMed

Yan, Qiao-Juan; Huang, Lin-Hua; Sun, Qian; Jiang, Zheng-Qiang; Wu, Xia

2015-07-15

Multiple proteases were optimized to hydrolyze the rice residue protein (RRP) to produce novel antioxidant peptides. An antioxidant peptide fraction (RRPB3) with IC50 of 0.25 mg/ml was purified from the RRP hydrolysate using membrane ultrafiltration followed by size exclusion chromatography and reversed-phase FPLC. RRPB3 was found to include four peptides (RRPB3 I-IV) and their amino acid sequences were RPNYTDA (835.9 Da), TSQLLSDQ (891.0 Da), TRTGDPFF (940.0 Da) and NFHPQ (641.7 Da), respectively. Furthermore, four peptides were chemically synthesized and their antioxidant activities were assessed by DPPH radical scavenging, ABTS radical scavenging assay and FRAP-Fe(3+) reducing assay, respectively. Both RRPB3 I and III showed synergistic antioxidant activity compared to each of them used alone. All four synthetic peptides showed excellent stability against simulated gastrointestinal proteases. Therefore, the peptides isolated from RRP may be used as potential antioxidants in the food and drug industries. Copyright © 2015 Elsevier Ltd. All rights reserved.

Effect of ultrasonic extraction conditions on antioxidative and immunomodulatory activities of a Ganoderma lucidum polysaccharide originated from fermented soybean curd residue.

PubMed

Shi, Min; Yang, Yingnan; Hu, Xuansheng; Zhang, Zhenya

2014-07-15

A crude Ganoderma lucidum polysaccharide (GLPL) was extracted from fermented soybean curd residue by ultrasonic assisted extraction. The optimal extraction conditions were 30 min at 80 °C with 80 W and water to solid ratio of 10, and with this method 115.47 ± 2.95 mg/g of GLPL yield was obtained. Additionally, the antioxidant and immunomodulatory activities of GLPL were investigated. The results showed that GLPL exhibited strong antioxidant effects, which included scavenging activities against DPPH radicals, hydrogen oxide and ABTS radicals with IC50 values of 0.23, 0.48 and 0.69 mg/mL, respectively. For immunomodulatory activities, GLPL was shown to strongly stimulate the proliferation of macrophages (158.02 ± 13.12%), the production of nitric oxide and phagocytosis (21.16 ± 1.65 μM), and, at 40.00 μg/mL, protected macrophage from Doxorubicin (DOX) (0.16 ± 0.003). Copyright © 2014 Elsevier Ltd. All rights reserved.

Phenolic Compounds of Pomegranate Byproducts (Outer Skin, Mesocarp, Divider Membrane) and Their Antioxidant Activities.

PubMed

Ambigaipalan, Priyatharini; de Camargo, Adriano Costa; Shahidi, Fereidoon

2016-08-31

Pomegranate peel was separated into outer leathery skin (PS), mesocarp (PM), and divider membrane (PD), and its phenolic compounds were extracted as free (F), esterified (E), and insoluble-bound (B) forms for the first time. The total phenolic content followed the order PD > PM > PS. ABTS(•+), DPPH, and hydroxyl radical scavenging activities and metal chelation were evaluated. In addition, pomegranate peel extracts showed inhibitory effects against α-glucosidase activity, lipase activity, and cupric ion-induced LDL-cholesterol oxidation as well as peroxyl and hydroxyl radical-induced DNA scission. Seventy-nine phenolic compounds were identified using HPLC-DAD-ESI-MS(n) mainly in the form of insoluble-bound. Thirty compounds were identified for the first time. Gallic acid was the major phenolic compound in pomegranate peel, whereas kaempferol 3-O-glucoside was the major flavonoid. Moreover, ellagic acid and monogalloyl-hexoside were the major hydrolyzable tannins, whereas the dominant proanthocyanidin was procyanidin dimers. Proanthocyanidins were detected for the first time.

Ellagic acid derivatives, ellagitannins, proanthocyanidins and other phenolics, vitamin C and antioxidant capacity of two powder products from camu-camu fruit (Myrciaria dubia).

PubMed

Fracassetti, Daniela; Costa, Carlos; Moulay, Leila; Tomás-Barberán, Francisco A

2013-08-15

The aims of this study were the evaluation of polyphenols and vitamin C content, and antioxidant capacity of dehydrated pulp powder and the dried flour obtained from the skin and seeds residue remaining after pulp preparation from camu-camu (Myrciaria dudia). Fifty-three different phenolics were characterised by HPLC-DAD-ESI-MS-MS and UPLC-HR-QTOF-MS-MS. The phenolic content of camu-camu flour was higher than that of the pulp powder (4007.95 mg/100 g vs. 48.54 mg/100 g). In both products the flavonol myricetin and conjugates, ellagic acid and conjugates and ellagitannins were detected. Cyanidin 3-glucoside, and quercetin and its glycosides were only found in the pulp powder, while proanthocyanidins were only present in the flour (3.5 g/100 g, mean degree of polymerisation 3). The vitamin C content was lower in pulp powder (3.5%) than in the flour (9.1%). The radical-scavenging capacity of both powders was determined by the DPPH, ABTS and ORAC assays, and was higher for camu-camu flour as could be expected for its higher phenolics and vitamin C content. Comparative analyses with fresh camu-camu berries indicate that some transformations occur during processing. Analysis of fresh berries showed that ellagic acid derivatives and ellagitannins were mainly present in the seeds, while proanthocyanidins were present both in the seeds and skin. Copyright © 2013 Elsevier Ltd. All rights reserved.

Antioxidant vitamins and enzymatic and synthetic oxygen-derived free radical scavengers in the prevention and treatment of cardiovascular disease.

PubMed

Nayak, D U; Karmen, C; Frishman, W H; Vakili, B A

2001-01-01

Oxygen-derived free radical formation can lead to cellular injury and death. Under normal situations, the human body has a free radical scavenger system (catalase, superoxide dismutase) that can detoxify free radicals. Antioxidant vitamins and enzymatic and synthetic oxygen-derived free radical scavengers have been used clinically to prevent the formation of oxidized LDL and to prevent reperfusion injury, which is often caused by free radicals. In this article, the pathogenesis of free radical production and cell injury are discussed, and therapeutic approaches for disease prevention are presented.

Metabolism and disposition of ABT-894, a novel α4β2 neuronal acetylcholine receptor agonist, in mice and monkeys.

PubMed

Liu, Hong; Fu, Wentao; Wetter, Jill; Xu, Hongyu; Guan, Zhiwen; Stuart, Patricia

2014-06-01

1.  Metabolism and disposition of ABT-894 was investigated in hepatocytes, in mice and monkeys receiving [(14)C]ABT-894. 2.  In hepatocytes, turnover rate of ABT-894 was slow in all species with more than 90% of parent remaining. M3 (carbamoyl glucuronide) and M6 (mono-oxidation) were detected across species. 3.  ABT-894 showed species-specific disposition profiles. ABT-894 was primarily eliminated by renal secretion in mice. Whereas, monkey mainly cleared ABT-894 metabolically. 4.  ABT-894 underwent two primary routes of metabolism in monkeys: N-carbamoyl glucuronidation to form M3 and oxidation product M1. M3 was the major metabolite in monkey excreta. M3 was observed in mice urine. Circulating levels of M3 in terms of M3/ABT-894 ratios were essentially absent in mice, but were high in monkeys. 5.  Understanding the species difference in the clearance mechanism is the key to the accurate projection of the human clearance and preclinical safety assessment. Lack of species difference in the metabolism of ABT-894 in hepatocytes certainly creates a challenge in predicting its metabolism and pharmacokinetics in human. Based on available metabolism and pharmacokinetic data of ABT-894 in human, monkey is the preferred species in predicting human clearance since it presents a similar clearance mechanism from that observed in human.

In vitro study on the antioxidant activity of a polyphenol-rich extract from Pinus brutia bark and its fractions.

PubMed

Cretu, Elena; Karonen, Maarit; Salminen, Juha-Pekka; Mircea, Cornelia; Trifan, Adriana; Charalambous, Christiana; Constantinou, Andreas I; Miron, Anca

2013-11-01

A crude hydromethanolic extract from Pinus brutia bark and its fractions (diethyl ether, ethyl acetate, n-butanol, and aqueous fractions) were studied with regard to their phenolic content and antioxidant activities. The total phenolics and proanthocyanidins in each extract were quantified by spectrophotometric methods; the polyphenolic profile was analyzed by RP-HPLC-DAD-ESI-MS. All extracts were tested with regard to their ability to scavenge free radicals (ABTS radical cation, superoxide and hydroxyl radicals), reduce ferric ions, and inhibit 15-lipoxygenase. P. brutia bark extracts had high phenolic contents (303.79±7.34-448.90±1.39 mg/g). Except diethyl ether extract, all other extracts contained proanthocyanidins ranging from 225.79±3.94 to 250.40±1.44 mg/g. Several polyphenols were identified by RP-HPLC-DAD-ESI-MS: taxifolin in diethyl ether extract, a taxifolin-O-hexoside, catechin, procyanidin dimers, and trimers in ethyl acetate extract. Except diethyl ether extract, all other extracts were effective scavengers of superoxide and hydroxyl radicals (EC₅₀=33.5±1.1-54.93±2.85 μg/mL and 0.47±0.06-0.6±0.0 mg/mL, respectively). All extracts had noticeable 15-lipoxygenase inhibitory effects (EC₅₀=22.47±0.75-34.43±2.25 μg/mL). We conclude that P. brutia bark is very promising for the dietary supplements industry due to its high free radical scavenging and 15-lipoxygenase inhibitory effects.

Suitability of DPPH spiking for antioxidant screening in natural products: the example of galloyl derivatives from red maple bark extract.

PubMed

Geoffroy, Thibaud R; Meda, Naamwin R; Stevanovic, Tatjana

2017-09-01

To investigate the antioxidant potential in natural products, radical scavenging tests (ABTS, DPPH, ORAC, etc.) are usually considered as the first approach. In addition to the standard colorimetric assays, methods using separation techniques (on-line and pre-column assays) have been developed in the past decades. Based on the peak area (PA) reductions of compounds monitored by HPLC, the pre-column spiking method allows rapid characterisation of natural matrices avoiding laborious isolation steps. However, available information about the significance of the results produced remains scarce. Here, we report, for the first time, a discussion of the potential of the pre-column DPPH spiking method to pinpoint antioxidant compounds using red maple bark extract (RMBE). First, DPPH spiking was conventionally applied to the galloyl compounds in the extract showing the inadequacy of assessing results by PA reductions. The method was then applied to pure galloyl derivatives, evaluating their molar amount reacted (MAR) for more significance. The comparison with the standard DPPH-HPLC/AE method directly monitoring DPPH • inhibition highlighted the inability to retrieve the respective antioxidant efficiencies (AE) of each compound by using DPPH spiking. Despite its limitations, the DPPH spiking method brought to light an autoxidation phenomenon and a matrix/mixture effect investigated through tertiary mixtures of galloyl compounds. Although restricted to the compounds from one natural matrix, this study questions the validity of the spiking method as usually performed and could serve as a basis for further investigations (explorations of other natural products, kinetics considerations). Graphical abstract Investigation of the pre-column DPPH spiking method through the case of galloyl derivatives.

Cafestol overcomes ABT-737 resistance in Mcl-1-overexpressed renal carcinoma Caki cells through downregulation of Mcl-1 expression and upregulation of Bim expression.

PubMed

Woo, S M; Min, K-J; Seo, B R; Nam, J-O; Choi, K S; Yoo, Y H; Kwon, T K

2014-11-06

Although ABT-737, a small-molecule Bcl-2/Bcl-xL inhibitor, has recently emerged as a novel cancer therapeutic agent, ABT-737-induced apoptosis is often blocked in several types of cancer cells with elevated expression of Mcl-1. Cafestol, one of the major compounds in coffee beans, has been reported to have anti-carcinogenic activity and tumor cell growth-inhibitory activity, and we examined whether cafestol could overcome resistance against ABT-737 in Mcl-1-overexpressed human renal carcinoma Caki cells. ABT-737 alone had no effect on apoptosis, but cafestol markedly enhanced ABT-737-mediated apoptosis in Mcl-1-overexpressed Caki cells, human glioma U251MG cells, and human breast carcinoma MDA-MB231 cells. By contrast, co-treatment with ABT-737 and cafestol did not induce apoptosis in normal human skin fibroblast. Furthermore, combined treatment with cafestol and ABT-737 markedly reduced tumor growth compared with either drug alone in xenograft models. We found that cafestol inhibited Mcl-1 protein expression, which is important for ABT-737 resistance, through promotion of protein degradation. Moreover, cafestol increased Bim expression, and siRNA-mediated suppression of Bim expression reduced the apoptosis induced by cafestol plus ABT-737. Taken together, cafestol may be effectively used to enhance ABT-737 sensitivity in cancer therapy via downregulation of Mcl-1 expression and upregulation of Bim expression.

Anticancer agent ABT-737 possesses anti-atopic dermatitis activity via blockade of caspase-1 in atopic dermatitis in vitro and in vivo models.

PubMed

Jeong, Hyun-Ja; Ryu, Ka-Jung; Kim, Hyung-Min

2018-06-29

Previous studies reported that depletion of Bcl-2 has a protective effect against allergic diseases. Furthermore, recently our study showed that anticancer drug has antiallergic inflammatory effect. An anticancer agent ABT-737 is an inhibitor of Bcl-2 and has an anti-inflammatory effect. However, the antiallergic inflammatory activity of ABT-737 is still unknown. Here, we aimed to explore the anti-atopic dermatitis (AD) activity and the mechanism of ABT-737 in AD models. HaCaT cells were used for in vitro experiments. To evaluate the effect of ABT-737 in vivo model, BalB/c mice were orally administered ABT-737 for 6 weeks in 2,4-dinitrofluorobenzene (DNFB)-induced AD-like murine model. Major assays were enzyme-linked immunosorbent assay, reverse transcription-PCR, caspase-1 assay, histamine assay, and H&E staining. ABT-737 significantly decreased thymic stromal lymphopoietin (TSLP) secretion and caspase-1 activity in activated HaCaT cells. In DNFB-induced AD mice, oral administration of ABT-737 alleviated clinical severity and scratching behavior. ABT-737 decreased levels of AD-related biomarkers including IgE, histamine, TSLP, and inflammatory cytokines. In addition, ABT significantly reduced caspase-1 activity in skin lesions of AD mice. ABT-737 elicited an anti-AD activity via suppression of caspase-1 activation in AD in vitro and in vivo models. Therefore, this study provides important information regarding the use of anticancer drugs for controlling allergic inflammatory diseases.

Stable ABTS Immobilized in the MIL-100(Fe) Metal-Organic Framework as an Efficient Mediator for Laccase-Catalyzed Decolorization.

PubMed

Liu, Youxun; Geng, Yuanyuan; Yan, Mingyang; Huang, Juan

2017-06-02

The successful encapsulation of 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), a well-known laccase mediator, within a mesoporous metal-organic framework sample (i.e., MIL-100(Fe)) was achieved using a one-pot hydrothermal synthetic method. The as-prepared ABTS@MIL-100(Fe) was characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, nitrogen sorption, and cyclic voltammetry (CV). Our ABTS@MIL-100(Fe)-based electrode exhibited an excellent electrochemical response, indicating that MIL-100(Fe) provides an appropriate microenvironment for the immobilization and electroactivity of ABTS molecules. ABTS@MIL-100(Fe) was then evaluated as an immobilized laccase mediator for dye removal using indigo carmine (IC) as a model dye. Through the application of laccase in combination with a free (ABTS) or immobilized (ABTS@MIL-100(Fe)) mediator, decolorization yields of 95% and 94%, respectively, were obtained for IC after 50 min. In addition, following seven reuse cycles of ABTS@MIL-100(Fe) for dye treatment, a decolorization yield of 74% was obtained. Dye decolorization occurred through the breakdown of the chromophoric group by the Laccase/ABTS@MIL-100(Fe) system, and a catalytic mechanism was proposed. We therefore expect that the stability, reusability, and validity of ABTS@MIL-100(Fe) as a laccase mediator potentially render it a promising tool for dye removal, in addition to reducing the high running costs and potential toxicity associated with synthetic mediators.

Chemical composition and antioxidant activities of the essential oil from Nandina domestica fruits.

PubMed

Bi, Shu-Feng; Zhu, Guang-Qi; Wu, Jie; Li, Zhong-Kang; Lv, Yong-Zhan; Fang, Ling

2016-01-01

The chemical composition and antioxidant activities of the essential oil from Nandina domestica fruits were studied for the first time. Twenty-two compounds, representing 82.79% of the oil, were identified from the oil. The major compounds were 3-hexen-1-ol (12.9%), linalool (12.3%), 2-methoxy-4-vinylphenol (9.9%), oleic acid (8.0%), furfural (5.8%) and 2,6-di-tert-butyl-4-methylphenol (5.7%). The antioxidant activities of the oil were evaluated using reducing power, metal chelating ability and scavenging capacity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethylbenzthiazoline-6-sulfonate (ABTS) and superoxide anion free radical. The oil exhibited significant antioxidant activities.

Inhibitory properties of bambara groundnut protein hydrolysate and peptide fractions against angiotensin-converting enzymes, renin and free radicals.

PubMed

Arise, Abimbola K; Alashi, Adeola M; Nwachukwu, Ifeanyi D; Malomo, Sunday A; Aluko, Rotimi E; Amonsou, Eric O

2017-07-01

An increased rate of high blood pressure has led to critical human hypertensive conditions in most nations. In the present study, bambara protein hydrolysates (BPHs) obtained using three different proteases (alcalase, trypsin and pepsin) and their peptide fractions (molecular weight: 10, 5, 3 and 1 kDa) were investigated for antihypertensive and antioxidant activities. Alcalase hydrolysate contained the highest amount of low molecular weight (LMW) peptides compared to pepsin and trypsin hydrolysates. LMW peptides fractions (<1 kDa) exhibited the highest inhibitory activity against angiotensin-converting enzyme (ACE) for all the enzymes hydrolysates. For renin inhibition, alcalase hydrolysate showed the highest inhibition at 59% compared to other hydrolysates and their corresponding membrane fractions. The antioxidant power of bambara protein hydrolysates and peptide fractions was evaluated through the inhibition of linoleic acid peroxidation and ABTS scavenging activity. Among the hydrolysates, alcalase exhibited the highest inhibition of linoleic acid oxidation. Furthermore, all BPHs were able to scavenge ABTS •+ to a three-fold greater extent compared to the isolate. BPH and LMW peptide fractions could potentially serve as useful ingredients in the formulation of functional foods and nutraceuticals against high blood pressure and oxidative stress. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

The H3 antagonist ABT-288 is tolerated at significantly higher exposures in subjects with schizophrenia than in healthy volunteers.

PubMed

Othman, Ahmed A; Haig, George; Florian, Hana; Locke, Charles; Gertsik, Lev; Dutta, Sandeep

2014-06-01

ABT-288 is a potent and selective H3 receptor antagonist with procognitive effects in several preclinical models. In previous studies, 3 mg once daily was the maximal tolerated dose in healthy volunteers. This study characterized the safety, tolerability and pharmacokinetics of ABT-288 in stable subjects with schizophrenia. This was a randomized, double-blind, placebo-controlled, dose-escalating study of ABT-288 (10 dose levels, from 1 to 60 mg once daily for 14 days) in stable subjects with schizophrenia treated with an atypical antipsychotic. In each dose group, five to seven and two to three participants were assigned to ABT-288 and placebo, respectively. Of the 67 participants enrolled, nine participants (on ABT-288) were prematurely discontinued, in seven of these due to adverse events. ABT-288 was generally safe and tolerated at doses up to 45 mg once daily. The most common adverse events, in decreasing frequency (from 31 to 5%), were abnormal dreams, headache, insomnia, dizziness, somnolence, dysgeusia, dry mouth, psychotic disorder, parosmia and tachycardia. Adverse events causing early termination were psychotic events (four) and increased creatine phosphokinase, pyrexia and insomnia (one each). The half-life of ABT-288 ranged from 28 to 51 h, and steady state was achieved by day 12 of dosing. At comparable multiple doses, ABT-288 exposure in subjects with schizophrenia was 45% lower than that previously observed in healthy subjects. At trough, ABT-288 cerebrospinal fluid concentrations were 40% of the total plasma concentrations. ABT-288 was tolerated at a 15-fold higher dose and 12-fold higher exposures in subjects with schizophrenia than previously observed in healthy volunteers. The greater ABT-288 tolerability was not due to limited brain uptake. © 2013 The British Pharmacological Society.

Oxidative Stress and Depression among Male Shift Workers in Shahid Tondgouyan Refinery.

PubMed

Khajehnasiri, Farahnaz; Akhondzadeh, Shahin; Mortazavi, Seyed Bagher; Allameh, Abdolamir; Khavanin, Ali; Zamanian, Zahra

2014-04-01

The aim of this study was to determine the oxidative stress; serum level of Total Antioxidant Capacity (TAC)and Malondialdehyde (MDA) level and the depression score among the depressed rotational shift workers in Shahid Tondgouyan Refinery in Tehran (Iran). A cross-sectional study was conducted among all the 189 shift workers in Shahid Tondgouyan oil refinery who were eligible to participate in the study. They did not take any antidepressants for two months or any supplements for two weeks prior to the study entry. Written consent was obtained from the participants. 21- Item Beck Depression Inventory was used to measure the depression level. Furthermore, body weight, height and systolic and diastolic blood pressure were collected from all the participants. The levels of Total Antioxidant Capacity (TAC) and Malondialdehyde (MDA) were measured by 8 ml fasting blood sample. MDA was determined by thiobarbituric acid reaction. Serum total antioxidants were measured using the spectrophotometric ABTS. In the ABTS test, 2,2'-azinobis (3-ethylbenzthiazoline-6-acid) (ABTS) is converted into its radical cation (ABTS•+) by addition of sodium persulphate. This blue-green radical cation absorbs light at 734 nm. ABTS•+ is reactive towards most antioxidants. Descriptive statistics, ANOVA, ANCOVA and regression tests and correlation were used to analyze the data using SPSS software version 16. The age of the participants ranged from 21 to 52 years. The mean age of the participants was 30.58 year (±6.97yr). Of all the participants, 28% (n= 53) had no depression symptoms (depression score between 0 and 9), 65.1% (n=123) were categorized as having mild depression (depression score between 10 and 18) and 6.9% (n=13) were categorized as having moderate depression (depression score between 19 and 29). The participants' BMI ranged from 15.9 to 34.3; the mean BMI of the participants was 24.82 kg/m(2) (+ 3.81 kg/m(2)). The mean of the serum TAC level was 2.51 (± 0.56) mg/dl, and the mean serum MDA level was 3.67(± 1.08) μmol/l. There was a significant difference in the mean TAC concentration between the non-depressed group and the group with mild depression (p=0.029). Depression was associated with reduced mean TAC concentration and an increase in MDA level. There was a linear relationship between the depression score and shift work experience among the rotational shift workers, which showed a high level of stress and depression among the shift-workers.

Chemical Composition and Antioxidant Activities of Three Polysaccharide Fractions from Pine Cones

PubMed Central

Xu, Ren-Bo; Yang, Xin; Wang, Jing; Zhao, Hai-Tian; Lu, Wei-Hong; Cui, Jie; Cheng, Cui-Lin; Zou, Pan; Huang, Wei-Wei; Wang, Pu; Li, Wen-Jing; Hu, Xing-Long

2012-01-01

The traditional method of gas chromatography-mass spectrometry for monosaccharide component analysis with pretreatment of acetylation is described with slight modifications and verified in detail in this paper. It was then successfully applied to the quantitative analysis of component monosaccharides in polysaccharides extracted from the pine cones. The results demonstrated that the three pine cone polysaccharides all consisted of ribose, rhamnose, arabinose, xylose, mannose, glucose and galactose in different molar ratios. According to the recovery experiment, the described method was proved accurate and practical for the analysis of pine cone polysaccharides, meeting the need in the field of chemical analysis of Pinus plants. Furthermore; the chemical characteristics, such as neutral sugar, uronic acids, amino acids, molecular weights, and antioxidant activities of the polysaccharides were investigated by chemical and instrumental methods. The results showed that the chemical compositions of the polysaccharides differed from each other, especially in the content of neutral sugar and uronic acid. In the antioxidant assays, the polysaccharide fractions exhibited effective scavenging activities on ABTS radical and hydroxyl radical, with their antioxidant capabilities decreasing in the order of PKP > PAP > PSP. Therefore, although the polysaccharide fractions had little effect on superoxide radical scavenging, they still have potential to be developed as natural antioxidant agents in functional foods or medicine. PMID:23203063

Antioxidant and Anti-Inflammatory Activities of Hydrolysates and Peptide Fractions Obtained by Enzymatic Hydrolysis of Selected Heat-Treated Edible Insects.

PubMed

Zielińska, Ewelina; Baraniak, Barbara; Karaś, Monika

2017-09-02

This study investigated the effect of heat treatment of edible insects on antioxidant and anti-inflammatory activities of peptides obtained by in vitro gastrointestinal digestion and absorption process thereof. The antioxidant potential of edible insect hydrolysates was determined as free radical-scavenging activity, ion chelating activity, and reducing power, whereas the anti-inflammatory activity was expressed as lipoxygenase and cyclooxygenase-2 inhibitory activity. The highest antiradical activity against DPPH • (2,2-diphenyl-1-picrylhydrazyl radical) was noted for a peptide fraction from baked cricket Gryllodes sigillatus hydrolysate (IC 50 value 10.9 µg/mL) and that against ABTS •+ (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical) was the highest for raw mealworm Tenebrio molitor hydrolysate (inhibitory concentration (IC 50 value) 5.3 µg/mL). The peptides obtained from boiled locust Schistocerca gregaria hydrolysate showed the highest Fe 2+ chelation ability (IC 50 value 2.57 µg/mL); furthermore, the highest reducing power was observed for raw G. sigillatus hydrolysate (0.771). The peptide fraction from a protein preparation from the locust S. gregaria exhibited the most significant lipoxygenase and cyclooxygenase-2 inhibitory activity (IC 50 value 3.13 µg/mL and 5.05 µg/mL, respectively).

Enzyme inhibitory and radical scavenging effects of some antidiabetic plants of Turkey

PubMed Central

Orhan, Nilüfer; Hoçbaç, Sanem; Orhan, Didem Deliorman; Asian, Mustafa; Ergun, Fatma

2014-01-01

Objective(s): Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum), are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. Materials and Methods: α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. Results: H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2) on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml). Conclusion: Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes. PMID:25140204

Extraction of polyphenols from processed black currant (Ribes nigrum L.) residues.

PubMed

Kapasakalidis, Petros G; Rastall, Robert A; Gordon, Michael H

2006-05-31

The total phenol and anthocyanin contents of black currant pomace and black currant press residue (BPR) extracts, extracted with formic acid in methanol or with methanol/water/acetic acid, were studied. Anthocyanins and other phenols were identified by means of reversed phase HPLC, and differences between the two plant materials were monitored. In all BPR extracts, phenol levels, determined by the Folin-Ciocalteu method, were 8-9 times higher than in the pomace extracts. Acid hydrolysis liberated a much higher concentration of phenols from the pomace than from the black currant press residue. HPLC analysis revealed that delphinidin-3-O-glucoside, delphinidin-3-O-rutinoside, cyanidin-3-O-glucoside, and cyanidin-3-O-rutinoside were the major anthocyanins and constituted the main phenol class ( approximately 90%) in both types of black currant tissues tested. However, anthocyanins were present in considerably lower amounts in the pomace than in the BPR. In accordance with the total phenol content, the antioxidant activity determined by scavenging of 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation, the ABTS(*)(+) assay, showed that BPR extracts prepared by solvent extraction exhibited significantly higher (7-10 times) radical scavenging activity than the pomace extracts, and BPR anthocyanins contributed significantly (74 and 77%) to the observed high radical scavenging capacity of the corresponding extracts.

Highly galloylated tannin fractions from witch hazel (Hamamelis virginiana) bark: electron transfer capacity, in vitro antioxidant activity, and effects on skin-related cells.

PubMed

Touriño, Sonia; Lizárraga, Daneida; Carreras, Anna; Lorenzo, Sonia; Ugartondo, Vanessa; Mitjans, Montserrat; Vinardell, María Pilar; Juliá, Luis; Cascante, Marta; Torres, Josep Lluís

2008-03-01

Witch hazel ( Hammamelis virginiana) bark is a rich source of both condensed and hydrolizable oligomeric tannins. From a polyphenolic extract soluble in both ethyl acetate and water, we have generated fractions rich in pyrogallol-containing polyphenols (proanthocyanidins, gallotannins, and gallates). The mixtures were highly active as free radical scavengers against ABTS, DPPH (hydrogen donation and electron transfer), and HNTTM (electron transfer). They were also able to reduce the newly introduced TNPTM radical, meaning that they included some highly reactive components. Witch hazel phenolics protected red blood cells from free radical-induced hemolysis and were mildly cytotoxic to 3T3 fibroblasts and HaCat keratinocytes. They also inhibited the proliferation of tumoral SK-Mel 28 melanoma cells at lower concentrations than grape and pine procyanidins. The high content in pyrogallol moieties may be behind the effect of witch hazel phenolics on skin cells. Because the most cytotoxic and antiproliferative mixtures were also the most efficient as electron transfer agents, we hypothesize that the final putative antioxidant effect of polyphenols may be in part attributed to the stimulation of defense systems by mild prooxidant challenges provided by reactive oxygen species generated through redox cycling.

The isolation and identification of two compounds with predominant radical scavenging activity in hempseed (seed of Cannabis sativa L.).

PubMed

Chen, Tianpeng; He, Jinfeng; Zhang, Jianchun; Li, Xiaohui; Zhang, Hua; Hao, Jianxiong; Li, Lite

2012-09-15

Forty samples were extracted from defatted kernels and hulls of two varieties of hempseed (Bama and Yunma No. 1) using 10 different polar solvent systems. The radical scavenging capacity of the extracts was evaluated using 2,2-diphenyl-1-pikrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays and the total phenolic content was determined by Folin-Ciocalteu's phenol reagent. The correlation analysis indicated that the antioxidants in hempseed belonged to phenolic and DPPH() assay was suitable for evaluating the radical scavenging activity. Two compounds, with predominant antiradical activity, were isolated in 60% ethanol extract of hempseed hull using macroporous resin absorption, LH-20 gel chromatography, and high performance liquid chromatography methods, which were identified as N-trans-caffeoyltyramine and cannabisin B by high-resolution mass spectra, nuclear magnetic resonance spectra, and ultraviolet data. The two compounds exhibited significant high DPPH() scavenging activity and protective effect against in vitro oxidation of human low-density lipoprotein compared with extracts from flaxseed, grape seed, and soybean. This suggests that hempseed hull extract is a potential source of natural antioxidants, which could be added to dietary supplements to help prevent oxidative stress. Copyright © 2012 Elsevier Ltd. All rights reserved.

Oxidative DNA damage preventive activity and antioxidant potential of Stevia rebaudiana (Bertoni) Bertoni, a natural sweetener.

PubMed

Ghanta, Srijani; Banerjee, Anindita; Poddar, Avijit; Chattopadhyay, Sharmila

2007-12-26

At 0.1 mg/mL, the ethyl acetate extract (EAE) of the crude 85% methanolic extract (CAE) of Stevia rebaudiana leaves exhibited preventive activity against DNA strand scission by *OH generated in Fenton's reaction on pBluescript II SK (-) DNA. Its efficacy is better than that of quercetin. The radical scavenging capacity of CAE was evaluated by the DPPH test (IC50=47.66+/-1.04 microg/mL). EAE was derived from CAE scavenged DPPH (IC50=9.26+/-0.04 microg/mL), ABTS+ (IC50=3.04+/-0.22 microg/mL) and *OH (IC50=3.08+/-0.19 microg/mL). Additionally, inhibition of lipid peroxidation induced with 25 mM FeSO 4 on rat liver homogenate as a lipid source was noted with CAE (IC50=2.1+/-1.07 mg/mL). The total polyphenols and total flavonoids of EAE were 0.86 mg gallic acid equivalents/mg and 0.83 mg of quercetin equivalents/mg, respectively. Flavonoids, isolated from EAE, were characterized as quercetin-3-O-arabinoside, quercitrin, apigenin, apigenin-4-O-glucoside, luteolin, and kaempferol-3-O-rhamnoside by LC-MS and NMR analysis. These results indicate that Stevia rebaudiana may be useful as a potential source of natural antioxidants.

Helichrysum monizii Lowe: phenolic composition and antioxidant potential.

PubMed

Gouveia, Sandra; Castilho, Paula C

2012-01-01

In Madeira Archipelago there are four endemic Helichyrsum species and three of them are used in the traditional medicine. Helichrysum monizii is a rare endemism with very scarce information available concerning its uses in the local traditional medicine. The aim of this work was to study for the first time Helichrysum monizii in terms of its antioxidant capacity and the identification of the phenolic compounds to which that activity is due. Three different methods of extraction were performed and total phenolic and flavonoid contents of extracts were correlated to radical scavenging and antioxidant capacity by DPPH, ABTS, FRAP and β-carotene assays. An HPLC-DAD-ESI/MS(n) method was employed for the separation and identification of the phenolic and flavonoid components. The results revealed a high antioxidant potential mainly related to the phenolic profile of the plant. Polar components of methanol extracts of Helichrsyum monizii were detected by a high-performance liquid chromatography/electrospray ionisation tandem mass spectrometry (HPLC-DAD-ESI/MS(n) ) method. Thirty-three compounds were identified and 19 of them were identified as quinic acid derivatives. The high antioxidant potential Helichrysum monizii was for the first time established. Dicaffeoylquinic acids are the main responsible for that activity. Copyright © 2011 John Wiley & Sons, Ltd.

Phytochemical Profile and Evaluation of the Biological Activities of Essential Oils Derived from the Greek Aromatic Plant Species Ocimum basilicum, Mentha spicata, Pimpinella anisum and Fortunella margarita.

PubMed

Fitsiou, Eleni; Mitropoulou, Gregoria; Spyridopoulou, Katerina; Tiptiri-Kourpeti, Angeliki; Vamvakias, Manolis; Bardouki, Haido; Panayiotidis, Mihalis Ι; Galanis, Alex; Kourkoutas, Yiannis; Chlichlia, Katerina; Pappa, Aglaia

2016-08-16

Natural products, known for their medicinal properties since antiquity, are continuously being studied for their biological properties. In the present study, we analyzed the composition of the volatile preparations of essential oils of the Greek plants Ocimum basilicum (sweet basil), Mentha spicata (spearmint), Pimpinella anisum (anise) and Fortunella margarita (kumquat). GC/MS analyses revealed that the major components in the essential oil fractions, were carvone (85.4%) in spearmint, methyl chavicol (74.9%) in sweet basil, trans-anethole (88.1%) in anise, and limonene (93.8%) in kumquat. We further explored their biological potential by studying their antimicrobial, antioxidant and antiproliferative activities. Only the essential oils from spearmint and sweet basil demonstrated cytotoxicity against common foodborne bacteria, while all preparations were active against the fungi Saccharomyces cerevisiae and Aspergillus niger. Antioxidant evaluation by DPPH and ABTS radical scavenging activity assays revealed a variable degree of antioxidant potency. Finally, their antiproliferative potential was tested against a panel of human cancer cell lines and evaluated by using the sulforhodamine B (SRB) assay. All essential oil preparations exhibited a variable degree of antiproliferative activity, depending on the cancer model used, with the most potent one being sweet basil against an in vitro model of human colon carcinoma.

Comparative pharmacodynamics of the new fluoroquinolone ABT492 and ciprofloxacin with Escherichia coli and Pseudomonas aeruginosa in an in vitro dynamic model.

PubMed

Zinner, Stephen H; Vostrov, Sergey N; Alferova, Irene V; Lubenko, Irene Yu; Portnoy, Yury A; Firsov, Alexander A

2004-08-01

The killing kinetics of Escherichia coli and Pseudomonas aeruginosa were compared when exposed to ABT492 and ciprofloxacin. E. coli ATCC 25922 and a clinical isolate of P. aeruginosa 4226 were exposed to ABT492 (single dose) and ciprofloxacin (two 12 h doses) at the ratios of area under the curve (AUC) to MIC varying from 60 to 480 h and at clinically achievable AUC/MIC ratios of ABT492 (1,740 and 140 h, respectively) and ciprofloxacin (2,200 and 120 h, respectively) that correspond to a 400 mg dose of ABT492 and two 500 mg doses of ciprofloxacin. In addition, a double dose of ABT492 (800 mg; AUC/MIC 280 h) and two 12 h doses of ABT492 (2 x 400 mg) were used with P. aeruginosa. Maximal reductions in the starting inoculum of E. coli and P. aeruginosa were greater with ABT492 than with ciprofloxacin at a given AUC/MIC ratio (60-480 h), whereas the times to regrowth were shorter with ABT492. A specific AUC/MIC relationship of the antimicrobial effect was inherent in each quinolone-pathogen pair. With both E. coli and P. aeruginosa, AUC/MIC plots of the area between the control growth and the time-kill curves (I(E)) were steeper for ciprofloxacin than ABT492 and they were species-independent. The effect of ABT492 on E. coli at the clinically achievable AUC/MIC ratio (1740h) was more pronounced than the respective AUC/MIC of ciprofloxacin (2,200 h). With P. aeruginosa, a 140 h AUC/MIC of ABT492 (400 mg as a single dose) provided 1.8-fold less effect than a 120 h AUC/MIC of ciprofloxacin (2 x 500 mg). However, two 12 h doses of ABT492 (AUC/MIC 2 x 140 h) but not a double single dose (800 mg) were more efficient than ciprofloxacin. These findings predict comparable efficacies of clinically achievable AUC/MICs of ABT492 and ciprofloxacin against E. coli (q.d. versus b.i.d. quinolone dosing) and P. aeruginosa at b.i.d. but not at q.d. ABT492.

GDC-0941 sensitizes breast cancer to ABT-737 in vitro and in vivo through promoting the degradation of Mcl-1.

PubMed

Zheng, Lin; Yang, Wei; Zhang, Chong; Ding, Wan-jing; Zhu, Hong; Lin, Neng-ming; Wu, Hong-hai; He, Qiao-jun; Yang, Bo

2011-10-01

The present study showed that GDC-0941 potently sensitized breast cancer to ABT-737 in vitro and in vivo. ABT-737 exhibited limited lethality in breast cancer cells; however, when combined with GDC-0941, it displayed strong synergistic cytotoxicity and enhanced caspase-mediated apoptosis. GDC-0941 promoted proteasomal degradation of Mcl-1, of which the overexpression has been validated to confer ABT-737 resistance, thereby enhanced the anticancer efficacy of ABT-737. Furthermore, the combination of GDC-0941 and ABT-737 exerted increased anti-tumor efficacy on MDA-MB-231 xenograft models. Overall, our data described unprecedentedly the promising therapeutic potential and underlying mechanisms of combining GDC-0941 with ABT-737 in treating breast cancer. Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.

Lycopene inhibits the isomerization of β-carotene during quenching of singlet oxygen and free radicals.

PubMed

Heymann, Thomas; Heinz, Philipp; Glomb, Marcus A

2015-04-01

The present study aimed to investigate the influence of singlet oxygen and radical species on the isomerization of carotenoids. On the one hand, lycopene and β-carotene standards were incubated with 1,4-dimethylnaphthalene-1,4-endoperoxide that produced singlet oxygen in situ. (13Z)- and (15Z)-β-carotene were preferentially generated at low concentrations of singlet oxygen, while high concentrations resulted in formation of (9Z)-β-carotene. The addition of different concentrations of lycopene led to the same isomerization progress of β-carotene, but resulted in a decreased formation of (9Z)-β-carotene and retarded degradation of (all-E)-β-carotene. On the other hand, isomerization of β-carotene and lycopene was induced by ABTS-radicals, too. As expected from the literature, chemical quenching was observed especially for lycopene, while physical quenching was preferred for β-carotene. Mixtures of β-carotene and lycopene resulted in a different isomerization progress compared to the separate β-carotene model. As long as lycopene was present, almost no isomerization of β-carotene was triggered; after that, strong formation of (13Z)-, (9Z)-, and (15Z)-β-carotene was initiated. In summary, lycopene protected β-carotene against isomerization during reactions with singlet oxygen and radicals. These findings can explain the pattern of carotenoid isomers analyzed in fruits and vegetables, where lycopene containing samples showed higher (all-E)/(9Z)-β-carotene ratios, and also in in vivo samples such as human blood plasma.

In vitro evaluation of antioxidant and cytotoxic activities of lignin fractions extracted from Acacia nilotica.

PubMed

Barapatre, Anand; Meena, Avtar Singh; Mekala, Sowmya; Das, Amitava; Jha, Harit

2016-05-01

Lignin is one of the most important phytomacromolecule with diverse therapeutic properties such as anticancer, antimicrobial, anti-inflammatory and immune-stimulatory. The present study was carried out to evaluate the in vitro antioxidant, free radical scavenging and anti-proliferative/cytotoxic activities of eleven different lignin fractions, extracted from the wood of Acacia nilotica by pressurized solvent extraction (PSE) and successive solvent extraction (SSE) methods. Results indicate that the PSE fractions have high polyphenolic content and reducing power. However, the antioxidant efficiency examined by DPPH and ABTS radical scavenging assay was higher in SSE fractions. All lignin fractions revealed a significant ability to scavenge nitric oxide, hydroxyl and superoxide radicals. The extracted lignin fractions display high ferric ion reducing capacity and also possess excellent antioxidant potential in the hydrophobic (linoleic acid) system. Fractions extracted by polar solvent has the highest iron (Fe(2+)) chelating activity as compared to other factions, indicating their effect on the redox cycling of iron. Four lignin fractions depicted higher cytotoxic potential (IC50: 2-15 μg/mL) towards breast cancer cell line (MCF-7) but were ineffective (IC50: ≥ 100 μg/mL) against normal primary human hepatic stellate cells (HHSteCs). These findings suggest that the lignin extracts of A. nilotica wood has a remarkable potential to prevent disease caused by the overproduction of radicals and also seem to be a promising candidate as natural antioxidant and anti-cancer agents. Copyright © 2016 Elsevier B.V. All rights reserved.

A phase I study assessing the safety and pharmacokinetics of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 with gemcitabine and cisplatin in patients with solid tumors.

PubMed

Gietema, J A; Hoekstra, R; de Vos, F Y F L; Uges, D R A; van der Gaast, A; Groen, H J M; Loos, W J; Knight, R A; Carr, R A; Humerickhouse, R A; Eskens, F A L M

2006-08-01

The aim of the study was to determine the safety profile, pharmacokinetics and potential drug interactions of the angiogenesis inhibitor ABT-510 combined with gemcitabine-cisplatin chemotherapy in patients with solid tumors. Patients with advanced solid tumors received gemcitabine 1250 mg/m2 intravenously (i.v.) on days 1 and 8 and cisplatin 80 mg/m2 on day 1 of a 3-week cycle in combination with ABT-510. ABT-510 was administered subcutaneously twice daily at doses of 50 mg or 100 mg. Plasma samples for pharmacokinetics were obtained on days 1 (gemcitabine, cisplatin as single agents), 15 (ABT-510 as single agent) and 22 (gemcitabine, cisplatin and ABT-510 as combination). Thirteen patients received ABT-510 as either 50 mg b.i.d. (seven patients) or 100 mg b.i.d. (six patients) in combination with gemcitabine-cisplatin. The most common reported adverse events reflected the known toxicity profile induced by gemcitabine-cisplatin without ABT-510. One episode of hemoptysis occurred in a patient with non-small-cell lung cancer (NSCLC) after 13 days of treatment. No clinically significant pharmacokinetic interactions between ABT-510, gemcitabine and platinum were observed. Three partial responses were observed in 12 evaluable patients (one head and neck cancer, one melanoma and one NSCLC). Combining ABT-510 at doses of 50 mg and 100 mg with gemcitabine-cisplatin is feasible. Pharmacokinetic interactions were not observed and adding ABT-510 does not appear to increase toxicity.

Felsic plutonism in the Al Amar—Idsas area, Kingdom of Saudi Arabia

NASA Astrophysics Data System (ADS)

Le Bel, L.; Laval, M.

A tonalite—trondhjemite suite, calc-alkalic plutons and alkali-feldspar granites dated 670 and 580 Ma, intrude thick volcano-sedimentary rocks of the Al Amar group E of the Al Amar fault and the Abt schist W of the fault. The tonalite—trondhjemite suite (group I) is characterized by low Rb (50 ppm) and Sr (100-400 ppm) and by weakly fractionated rare-earth patterns (La/Yb Nca 2-3) with a weak negative Eu anomaly. Calc-alkalic plutons (group II) are richer in Rb (50-150 ppm), contain variable Sr (50-1000 ppm), and have strongly fractionated rare-earth patterns (La/Yb Nca 6-22) with no Eu anomaly. Alkali-feldspar granite (group III) is characterized by high Rb (150-200 ppm) and shows fractionated rare-earth patterns (La/Yb Nca 6-18) with a well-developed Eu anomaly. Group III includes 'specialized granites' with high Rb (300-400 ppm) and Sn (28-66 ppm), and rare-earth patterns showing a distinctive 'sea gull' profile with a very strong Eu anomaly (Eu*/Eu = 20). Oxygen isotope geochemistry suggests that group I rocks (¯x δ18O ca 7.0) were mantle-derived, and that group II and III rocks intruding the Al Amar group ( δ18O ca 7.9 and 8.8 respectively) were derived by remelting of group I, whereas those intruding Abt schist ( δ18O ca 8.7 and 10.8 respectively) were partially derived by anatexis of the Afif block. Magmatogenesis reflects an island-arc development. Rocks of group I represent the initial subduction phase. Syn- to late-tectonic plutons of group II intruded the arc east of the Al Amar fault and the accretionary prism (Abt schist) to the west, which was in collision with the older Afif block. Post-tectonic group III rocks were emplaced in an already cratonized area.

Hepatoprotective potential of Fagonia olivieri DC. against acetaminophen induced toxicity in rat.

PubMed

Rashid, Umbreen; Khan, Muhammad Rashid; Sajid, Moniba

2016-11-09

Fagonia olivieri (DC) being used for the treatment of diabetes, cancer, fever and claimed to be effective in many other stress related disorders. In this study we have evaluated the F. olivieri whole methanol extract and its derived fractions for various in vitro and in vivo antioxidant studies. The crude methanol extract of the whole plant of F. olivieri (FOM) and its derived fractions; n-hexane (FOH), chloroform (FOC), ethyl acetate (FOE), n-butanol (FOB) and aqueous (FOA) were evaluated for the total phenolic and flavonoid content and in vitro antioxidant abilities. The antioxidant effect of FOM was determined by acetaminophen-induced hepatotoxicity in Sprague-Dawley (Rattus novergicus) male rats. The methanol/fractions were also analysed by HPLC analysis for the presence of polyphenolics. The total phenolic content of the samples ranged from 19.3 ± 0.529 to 106.2 ± 0.892 mg GAE/g extract while total flavonoid content 16.2 ± 0.881 to 50.1 ± 1.764 mg RTE/g extract, respectively. FOA showed highest radical scavenging activity for DPPH (IC 50  = 55.2 ± 1.212 μg/ml), ABTS (IC 50  = 90.2 ± 1.232 μg/ml) superoxide (IC 50  = 37.1 ± 0.643 μg/ml) and for H 2 O 2 (IC 50  = 64 ± 1.463 μg/ml). FOE exhibited the highest antioxidant activities for phosphomolybdenum (IC 50  = 78.2 ± 0.883 μg/ml) and for hydroxyl radical scavenging (IC 50  = 82 ± 2.603 μg/ml). HPLC analysis of FOM and its derived fractions showed the presence of rutin, catechin and gallic acid. Elevated levels of AST, ALT, ALP, LDH and lipid profile in serum and lipid peroxidation and DNA damages in liver; while decreased activity level of CAT, SOD, GSH-Px, GR and reduced glutathione (GSH) concentration induced with acetaminophen in rat were reverted towards the control group with co-administration of FOM. Our results showed that F. olivieri is a potential source of natural antioxidants, which justifies its use in folklore medicine.

[Abatacept].

PubMed

Iwamoto, Naoki; Kawakami, Atsushi

2016-06-01

Abatacept (ABT) is a recombinant fusion protein comprising the extracellular domain of human CTLA4, which inhibits the activation of T cells. Several clinical trials have provided evidence of efficacy and safety of ABT in the patients with rheumatoid athritis (RA) with various clinical characteristics such as MTX inadequate responders (IR), TNF inhibitor-IR. Moreover, indirect comparison of ABT to other biologics reported in Cochrane review revealed that ABT has better safety profile in serious adverse events and serious infection Thus the features of ABT in the treatment of RA have gradually become apparent and knowledge of these features is helpful for better use of biologics. In this review we will discuss the efficacy and safety of ABT in the management of RA.

Effect of cold storage on total phenolics content, antioxidant activity and vitamin C level of selected potato clones.

PubMed

Külen, Oktay; Stushnoff, Cecil; Holm, David G

2013-08-15

Twelve Colorado-grown specialty potato clones were evaluated for total phenolic content, antioxidant activity and ascorbic acid content at harvest and after 2, 4, 6 and 7 months cold storage at 4 °C. Potato clones were categorized as pigmented ('CO97226-2R/R', 'CO99364-3R/R', 'CO97215-2P/P', 'CO97216-3P/P', 'CO97227-2P/P', 'CO97222-1R/R', 'Purple Majesty', 'Mountain Rose' and 'All Blue'), yellow ('Yukon Gold') and white fleshed ('Russet Nugget', 'Russet Burbank'). Folin-Ciocalteu reagent was used to estimate total phenolic content, and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS(•+) ) and 2,2-diphenyl-1-picrylhydrazyl (DPPH(•) ) radical scavenging assays were used to estimate antioxidant capacity. Pigmented potato genotypes had significantly higher total phenolic content and antioxidant activity at all data points than yellow- and white-fleshed cultivars. Vitamin C content was higher in 'Yukon Gold' than in the other clones. The highest level of vitamin C in all clones was at harvest and after 2 months in cold storage. Vitamin C content in all potato clones dropped rapidly with longer intervals of cold storage. Although total phenolic content and antioxidant activity fluctuated during cold storage, after 7 months of cold storage their levels were slightly higher than at harvest. Total phenolic content was better correlated with Trolox equivalent antioxidant capacity (TEAC)/ABTS(•+) than the TEAC/DPPH(•) radical scavenging assay. Pigmented potato clones had significantly higher total phenolic content and antioxidant activity, while the yellow-fleshed potato cultivar 'Yukon Gold' had significantly higher vitamin C content. Vitamin C content decreased in all potato clones during cold storage, while total phenolics increased in pigmented clones. © 2013 Society of Chemical Industry.

Use of Different Proteases to Obtain Flaxseed Protein Hydrolysates with Antioxidant Activity.

PubMed

Karamać, Magdalena; Kosińska-Cagnazzo, Agnieszka; Kulczyk, Anna

2016-06-29

The antioxidant activity of flaxseed protein hydrolysates obtained using five different enzymes was evaluated. Proteins were isolated from flaxseed cake and were separately treated with papain, trypsin, pancreatin, Alcalase and Flavourzyme. The degree of hydrolysis (DH) was determined as the percentage of cleaved peptide bonds using a spectrophotometric method with o-phthaldialdehyde. The distribution of the molecular weights (MW) of the hydrolysis products was profiled using Tricine-sodium dodecyl sulfate-polyacrylamide gel electrophoresis (Tricine-SDS-PAGE) and size exclusion-high performance liquid chromatography (SE-HPLC) separations. The antioxidant activities of the protein isolate and hydrolysates were probed for their radical scavenging activity using 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) radical cation (ABTS(•+)) and photochemiluminescence (PCL-ACL) assays, and for their ferric reducing antioxidant power (FRAP) and ability to bind Fe(2+). The hydrolysates were more effective as antioxidants than the protein isolate in all systems. The PCL-ACL values of the hydrolysates ranged from 7.2 to 35.7 μmol Trolox/g. Both the FRAP and ABTS(•+) scavenging activity differed among the hydrolysates to a lower extent, with the ranges of 0.20-0.24 mmol Fe(2+)/g and 0.17-0.22 mmol Trolox/g, respectively. The highest chelating activity (71.5%) was noted for the pancreatin hydrolysate. In general, the hydrolysates obtained using Alcalase and pancreatin had the highest antioxidant activity, even though their DH (15.4% and 29.3%, respectively) and the MW profiles of the peptides varied substantially. The O₂(•-) scavenging activity and the ability to chelate Fe(2+) of the Flavourzyme hydrolysate were lower than those of the Alcalase and pancreatin hydrolysates. Papain was the least effective in releasing the peptides with antioxidant activity. The study showed that the type of enzyme used for flaxseed protein hydrolysis determines the antioxidant activity of the hydrolysates.

Antioxidant activity of ethanolic extract of inflorescence of Ormenis Africana in vitro and in cell cultures.

PubMed

Ben Mansour, Riadh; Gargouri, Bochra; Bouaziz, Mohamed; Elloumi, Nésrine; Belhadj Jilani, Imtinène; Ghrabi, Zaineb; Lassoued, Saloua

2011-05-16

The antioxidant potency of the hydroethanolic extract of Ormenis Africana (HEOA), Asteraceae was evaluated with regards to total polyphenol, flavonoid and anthocyanins content. Antioxidant activity has been assessed chemically and biologically. First, the free radical scavenging ability of HEOA was evaluated using two commonly in vitro tests: ABTS and DPPH radicals. Then, the protection effect of this extract against oxidative stress was conducted in HeLa cells treated with Fe2+ or H2O2. Oxidative stress was evaluated by measuring the lipid peroxidation levels (TBARs and DC) and the antioxidant enzymes activities (catalase and Superoxide dismutase). Cytotoxic effect of HEOA was prealably determined against HeLa cell line by MTT assay. HEOA contain considerable levels of antioxidant compound as evidenced by high amount of polyphenols (312.07 mg GAE/g dray matter), flavonoids (73.72 ± 1.98 mg QE/g dray matterl) and anthocyanins (0.28 ± 0.09 mg Cy-3-glu E/g dray matter). DPPH and ABTS assays showed a high antioxidant activity (IC50 = 24 μg/ml; TEAC = 2.137 mM) which was comparable to BHT.In biological system, HEOA exhibited a 50% cytotoxic concentration evaluated as 16.52 μg/ml. Incubation of HeLa cell line with no cytotoxic concentrations resulted in a remarkable protection from oxidative stress induced by Fe2+ or H2O2 which was evidenced by a decrease of MDA and CD levels as well as a diminution of antioxidant enzymes activities (Catalase and SOD) as compared to cells treated with Fe2+ or H2O2 alone. The hydroethanolic extract of O. Africana could thus be considered as a source of potential antioxidants. The results of this study will promote the reasonable usage of this plant in food and pharmacy industries as well as in alternative medicine and natural therapy.

Acute toxicity evaluation, antibacterial, antioxidant and immunomodulatory effects of Melastoma malabathricum.

PubMed

Alnajar, Zahra A Amin; Abdulla, Mahmood A; Ali, Hapipah M; Alshawsh, Mohammed A; Hadi, A Hamid A

2012-03-20

Melastoma malabathricum (MM) is a well-known plant in Malaysian traditional medicine, locally known as senduduk. Its ethanol and aqueous extracts have been used in the present investigation to study the immunomodulatory role on human peripheral blood mononuclear cell (PBMC), and the DPPH, ABTS and FRAP free radical scavenging activities were also measured. Total flavonoids and total phenolic contents were assayed and the antibacterial effect was tested against four species of bacteria; two Gram-positive (Staphylococcus aureus and Streptococcus agalactiae) and two Gram-negative (Escherichia coli and Klebsilla pneumonia). The tests were carried out using the disc diffusion, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methods. Moreover, the acute toxicity was evaluated in vivo on the ethanol extract of MM to establish its safety when administered orally. In our results, both extracts of MM showed abilities to scavenge DPPH and ABTS free radicals, IC(50) values: (11.599 ± 0.84, 10.573 ± 0.58 µmol/L) and (62.657 ± 0.78, 63.939 ± 0.48 µmol/L) for ethanol and aqueous extracts respectively. Indeed the ethanol extract evidenced high phenolic content (384.33 ± 0.005 mg/g), flavonoids contents (85.8 ± 0.009 mg/g) and ferric reducing antioxidant power (33,590 ± 0.038 mmol/g), with high activity against S. aureus and S. agalactiae (11 ± 0.3 and 12 ± 0.6 mm inhibition zones). Likewise, the percentage of peripheral blood mononuclear cells (PBMC) viability was increased in response to MM, IC(50) values (1.781 ± 1.2 and 6.545 ± 0.93 µg/mL) for ethanol and aqueous extracts, respectively. In addition, our results showed that the MM extract is safe even at a high dose of 5,000 mg/kg and has no oral toxicity. These findings suggest the excellent medicinal bioactivity of MM and explain the popularity of this plant in the folk medicine as a remedy for different illnesses.

Antioxidant and immunomodulatory properties of polysaccharides from Allanblackia floribunda Oliv stem bark and Chromolaena odorata (L.) King and H.E. Robins leaves.

PubMed

Boudjeko, Thaddée; Megnekou, Rosette; Woguia, Alice Louise; Kegne, Francine Mediesse; Ngomoyogoli, Judith Emery Kanemoto; Tchapoum, Christiane Danielle Nounga; Koum, Olga

2015-12-09

Many plant polysaccharides have shown high antioxidant and immunostimulating properties and can be explored as novel molecules with biological properties that can potentially improve immune function. The objective of this work was to characterize soluble and cell wall polysaccharides isolated from the stem bark of Allanblackia floribunda and Chromolaena odorata leaves and to evaluate their antioxidant and immunomodulatory properties. Three polysaccharide fractions: soluble polysaccharides (PoS), pectins (Pec) and hemicelluloses (Hem) were extracted from A. floribunda stem bark and C. odorata leaves. These samples were analysed for their proteins, phenolic compounds and total sugar contents. The monosaccharide composition was determined by gas chromatography and arabinogalactan proteins content in PoS was evaluated by rocket electrophoresis. The in vitro antioxidant activities were evaluated by 1, 1-diphenyl-2-picryl hydrazyl (DPPH) and 2,2'-azino-bis-3-éthylbenzylthiazoline-6-sulphonic acid (ABTS) radical scavenging assays and ferrous ions chelating activity. Immunomodulatory activities were performed on the peripheral blood mononuclear cells (PBMCs) using proliferation and enzyme linked immunospot (ELISPOT) method to determine the production of an interferon-gamma. The characterization of the various fractions showed varied metabolites in each plant. In PoS fractions, Ara and Gal were the major monosaccharides found, indicating that arabinogalactans are the primary macromolecules. Hem fractions contained predominantly Xyl and GalA for A. floribunda and Xyl (upto 80 %) for and C. odorata. A. floribunda Hem fraction and C. odorata PoS fraction showed significant DPPH and ABTS radical scavenging activities and immunostimulatory activity via stimulation of PBMC and production of IFN-γ in a dose-dependent manner. The results obtained from this study support the ethnomedicinal use of the stem bark of A. floribunda and leaves of C. odorata. Further research is necessary to have supporting evidence that the antioxidative and immunomodulative activities of these fractions are really connected to the polysaccharides and not polyphenols.

Antioxidant activity of ethanolic extract of inflorescence of Ormenis Africana in vitro and in cell cultures

PubMed Central

2011-01-01

Background The antioxidant potency of the hydroethanolic extract of Ormenis Africana (HEOA), Asteraceae was evaluated with regards to total polyphenol, flavonoid and anthocyanins content. Antioxidant activity has been assessed chemically and biologically. First, the free radical scavenging ability of HEOA was evaluated using two commonly in vitro tests: ABTS and DPPH radicals. Then, the protection effect of this extract against oxidative stress was conducted in HeLa cells treated with Fe2+ or H2O2. Oxidative stress was evaluated by measuring the lipid peroxidation levels (TBARs and DC) and the antioxidant enzymes activities (catalase and Superoxide dismutase). Cytotoxic effect of HEOA was prealably determined against HeLa cell line by MTT assay. Results HEOA contain considerable levels of antioxidant compound as evidenced by high amount of polyphenols (312.07 mg GAE/g dray matter), flavonoids (73.72 ± 1.98 mg QE/g dray matterl) and anthocyanins (0.28 ± 0.09 mg Cy-3-glu E/g dray matter). DPPH and ABTS assays showed a high antioxidant activity (IC50 = 24 μg/ml; TEAC = 2.137 mM) which was comparable to BHT. In biological system, HEOA exhibited a 50% cytotoxic concentration evaluated as 16.52 μg/ml. Incubation of HeLa cell line with no cytotoxic concentrations resulted in a remarkable protection from oxidative stress induced by Fe2+ or H2O2 which was evidenced by a decrease of MDA and CD levels as well as a diminution of antioxidant enzymes activities (Catalase and SOD) as compared to cells treated with Fe2+ or H2O2 alone. Conclusion The hydroethanolic extract of O. Africana could thus be considered as a source of potential antioxidants. The results of this study will promote the reasonable usage of this plant in food and pharmacy industries as well as in alternative medicine and natural therapy. PMID:21575256

Composition and antioxidant, antibacterial, and anti-HepG2 cell activities of polyphenols from seed coat of Amygdalus pedunculata Pall.

PubMed

Lu, Cairui; Li, Cong; Chen, Bang; Shen, Yehua

2018-11-01

This study aims at identifying the composition of polyphenols present in Amygdalus pedunculata Pall seed coat (APSC), and characterizing their antioxidant, antibacterial, and anticancer activities. The polyphenols from APSC were composed of 32 compounds. The compounds with important biological activities included apigenin 7-O-glucoside (the main component; 34.53 mg/100 g), quercitrin (23.43 mg/100 g), kaempferol (10.28 mg/100 g), naringenin (6.27 mg/100 g), cyanidin 3-rutinoside (5.76 mg/100 g), cyanidin 3-O-galactoside (5.19 mg/100 g), and quercetin (2.50 mg/100 g), as well as a variety of phenolic acids (gentisic acid, 23.13 mg/100 g; salicylic acid, 18.79 mg/100 g; gallic acid, 2.55 mg/100 g; etc.). Characterization of the identified polyphenols indicated that APSC possessed high antioxidant activity, due to its ability to reduce Fe 3+ and scavenge ABTS, DPPH, OH, O 2 - , and H 2 O 2 free radicals. The ability of APSC to reduce Fe 3+ and scavenge ABTS radical, and H 2 O 2 was stronger than that of control group ascorbic acid (Vc). The data from bacteriostatic test showed that polyphenols from APSC had good antibacterial activity against Escherichia coli, Staphylococcus aureus, Bacillus cereus, and Bacillus subtilis, but showed no activity against Aspergillus niger. Cell viability assays using HepG2 cell illustrated that polyphenols from APSC significantly inhibited cell proliferation and induced cell apoptosis. The findings demonstrate that polyphenols from APSC may be utilized as is or further developed into natural antioxidant, antibacterial, and anticancer agents. This work also provides a basis for the development and utilization of Amygdalus pedunculata Pall. Copyright © 2018 Elsevier Ltd. All rights reserved.

Antioxidant capacities, phenolic contents, and GC/MS analysis of Rhodiola imbricata Edgew. root extracts from Trans-Himalaya.

PubMed

Tayade, A B; Dhar, P; Sharma, M; Chauhan, R S; Chaurasia, O P; Srivastava, R B

2013-03-01

Our aim was to assess the antioxidant capacities and phenolic constituents of methanol and aqueous extracts of Rhodiola imbricata Edgew. root from Trans-Himalayan cold desert of Ladakh. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging capacity of the root extracts increased in a dose-dependent manner (up to 0.1 mg/mL) and root extract concentrations required for 50% inhibition of radical scavenging effect (IC50 ) were recorded as 0.013 and 0.014 mg/mL (for DPPH) and 0.016 and 0.017 mg/mL (for ABTS) for methanol and aqueous extracts, respectively. The total antioxidant power of the extract was determined by ferric reducing antioxidant power (FRAP) assay. Total polyphenol and phenolic acid content of methanol and aqueous extracts were 112.24, 59.06, 39.02, and 16.95 mg gallic acid equivalent/g of extract, respectively. Total flavonoid and flavonol contents were estimated to be 30.2, 17.67, 20.68, and 7.38 mg quercetin equivalent/g of extract, respectively. In all antioxidant capacity assays, the methanol extract exhibited significantly higher antioxidant capacity than that of aqueous extract due to the presence of significantly higher amount of vital phytoconstitiuents, viz. polyphenol, phenolic acid, and flavonol. GC/MS analysis showed that phytosterols, alkyl halide, phenols, and fatty acid esters were major phytochemical clusters. On the other hand, monoterpenes, fatty acids, tocopherols, aliphatic hydrocarbons, and ethers were found to be present in comparatively less amount in the methanol extract. Hence, our study signifies that this high-altitude medicinal herb could be used as the natural source of antioxidants and supports its use in traditional system of medicine to ameliorate oxidative stress and high-altitude maladies. © 2013 Institute of Food Technologists®

Antioxidant activities and phenolic contents of three red seaweeds (Division: Rhodophyta) harvested from the Gulf of Mannar of Peninsular India.

PubMed

Chakraborty, Kajal; Joseph, Deepu; Praveen, Nammunayathuputhenkotta Krishnankartha

2015-04-01

The antioxidant activities of methanol extract and its solvent fractions (n-hexane, dichloromethane and ethyl acetate) of three red seaweeds (Hypnea musciformis, H. valentiae, and Jania rubens) collected from the Gulf of Mannar of South eastern coast of India were evaluated, using different in vitro systems, viz., DPPH, ABTS, HO radical scavenging activities, H2O2 scavenging ability, Fe(2+) ion chelating ability and reducing potential. Folin-Ciocalteu method was used to determine the total phenolic content of the extracts/fractions, and the results were expressed as mg of gallic acid equivalent (GAE)/g of the seaweed extracts/fractions. Thiobarbituric acid-reactive substances (TBARS) inhibition assay was employed to assess the ability of the seaweed extracts/fractions to inhibit lipid oxidation. Ethyl acetate (EtOAc) fractions of H. musciformis exhibited significantly higher total phenolic content (205.5 mg GAE/g), DPPH· scavenging activity (IC50 0.6 mg/mL), ABTS(.+) scavenging activity (IC50 0.51 μg/mL), Fe(2+) chelating ability (IC50 0.70 mg/mL), H2O2 scavenging activity (IC50 0.39 mg/mL), reducing ability (Abs700 nm 1.46) and lipid peroxidation inhibitory ability (2.71 MDAEC/kg) (P < 0.05) compared to its n-hexane, DCM fractions, crude MeOH extract and MeOH extracts/fractions of H. valentiae and J. rubens. DCM fraction of J. rubens showed significantly higher hydroxyl radical scavenging activity (IC50 0.55 mg/mL) compared with H. musciformis and H. valentiae (P < 0.05). This study indicated the potential use of red seaweeds, in particular, H. musciformis as candidate species to be used as food supplement for increasing the shelf-life of food industry, and candidates in combating carcinogenesis and inflammatory diseases.

ABT-089, but not ABT-107, ameliorates nicotine withdrawal-induced cognitive deficits in C57BL6/J mice

PubMed Central

Yildirim, Emre; Connor, David A.; Gould, Thomas J.

2015-01-01

Nicotine withdrawal produces cognitive deficits that can predict relapse. Amelioration of these cognitive deficits emerges as a target in current smoking cessation therapies. In rodents, withdrawal from chronic nicotine disrupts contextual fear conditioning (CFC), whereas acute nicotine enhances this hippocampus-specific learning and memory. These modifications are mediated by β2-subunit-containing (β2*) nicotinic acetylcholine receptors in the hippocampus. We aimed to test ABT-089, a partial agonist of α4β2*, and ABT-107, an α7 nicotinic acetylcholine receptor agonist, for amelioration of cognitive deficits induced by withdrawal from chronic nicotine in mice. Mice underwent chronic nicotine administration (12.6 mg/kg/day or saline for 12 days), followed by 24 h of withdrawal. At the end of withdrawal, mice received 0.3 or 0.6 mg/kg ABT-089 or 0.3 mg/kg ABT-107 (doses were determined through initial dose–response experiments and prior studies) and were trained and tested for CFC. Nicotine withdrawal produced deficits in CFC that were reversed by acute ABT-089, but not ABT-107. Cued conditioning was not affected. Taken together, our results suggest that modulation of hippocampal learning and memory using ABT-089 may be an effective component of novel therapeutic strategies for nicotine addiction. PMID:25426579

Binding of released Bim to Mcl-1 is a mechanism of intrinsic resistance to ABT-199 which can be overcome by combination with daunorubicin or cytarabine in AML cells

PubMed Central

Niu, Xiaojia; Zhao, Jianyun; Ma, Jun; Xie, Chengzhi; Edwards, Holly; Wang, Guan; Caldwell, J. Timothy; Xiang, Shengyan; Zhang, Xiaohong; Chu, Roland; Wang, Zhihong; Lin, Hai; Taub, Jeffrey W.; Ge, Yubin

2016-01-01

Purpose To investigate the molecular mechanism underlying intrinsic resistance to ABT-199. Experimental Design Western blots and real-time RT-PCR were used to determine levels of Mcl-1 after ABT-199 treatment alone or in combination with cytarabine or daunorubicin. Immunoprecipitation of Bim and Mcl-1 were used to determine the effect of ABT-199 treatment on their interactions with Bcl-2 family members. Lentiviral shRNA knockdown of Bim and CRISPR knockdown of Mcl-1 were used to confirm their role in resistance to ABT-199. JC-1 assays and flow cytometry were used to determine drug-induced apoptosis. Results Immunoprecipitation of Bim from ABT-199 treated cell lines and a primary patient sample demonstrated decreased association with Bcl-2, but increased association with Mcl-1 without corresponding change in mitochondrial outer membrane potential. ABT-199 treatment resulted in increased levels of Mcl-1 protein, unchanged or decreased Mcl-1 transcript levels, and increased Mcl-1 protein half-life, suggesting that the association with Bim plays a role in stabilizing Mcl-1 protein. Combining conventional chemotherapeutic agent cytarabine or daunorubicin with ABT-199 resulted in increased DNA damage along with decreased Mcl-1 protein levels, compared to ABT-199 alone, and synergistic induction of cell death in both AML cell lines and primary patient samples obtained from AML patients at diagnosis. Conclusions Our results demonstrate that sequestration of Bim by Mcl-1 is a mechanism of intrinsic ABT-199 resistance and supports the clinical development of ABT-199 in combination with cytarabine or daunorubicin for the treatment of AML. PMID:27103402

Angiotensin receptor blockade: a novel approach for symptomatic radiation necrosis after stereotactic radiosurgery

PubMed Central

Okwan-Duodu, Derick; Switchenko, Jeffrey M.; Press, Robert H.; Jhaveri, Jaymin; Buchwald, Zachary S.; Zhong, Jim; Chapman, Bhavana V.; Bindra, Ranjit S.; Contessa, Joseph N.; Park, Henry S.; Yu, James B.; Decker, Roy H.; Olson, Jeffrey J.; Oyesiku, Nelson M.; Abrams, Ross A.; Shu, Hui-Kuo G.; Curran, Walter J.; Crocker, Ian R.

2018-01-01

Preclinical evidence suggests angiotensin blockade therapy (ABT) decreases late radiation toxicities. This study aims to investigate the association between ABT and symptomatic radiation necrosis (SRN) following stereotactic radiosurgery (SRS). Resected brain metastases (rBM) and arteriovenous malformation (AVM) patients treated with SRS from 2002 to 2015 were identified. Patients in the ABT cohort were on therapy during SRS and at 1-month follow up. Kaplan Meier method and cumulative incidence model were used to analyze overall survival (OS) and intracranial outcomes. 228 consecutive patients were treated with SRS: 111 with rBM and 117 with AVM. Overall, 51 (22.4%) patients were in the ABT group: 32 (28.8%) in the rBM and 19 (16.2%) in AVM cohorts. Baseline characteristics were similar, except for higher Graded Prognostic Analysis (3–4) in the rBM (ABT: 25.0% vs. non-ABT: 49.0%, p = 0.033) and median age in the AVM (ABT: 51.4 vs. non-ABT: 35.4, p < 0.001) cohorts. In both populations, OS and intracranial efficacy (rBM—local control; AVM—obliteration rates) were statistically similar between the cohorts. ABT was associated with lower 1-year SRN rates in both populations: rBM, 3.1 versus 25.3% (p = 0.003); AVM, 6.7 vs. 14.6% (p = 0.063). On multivariate analysis, ABT was a significant predictive factor for rBM (HR: 0.17; 95% CI 0.03–0.88, p = 0.035), but did not reach statistical significance for AVM (HR: 0.36; 95% CI 0.09–1.52, p = 0.165). ABT use appears to be associated with a reduced risk of SRN following SRS, without detriment to OS or intracranial efficacy. A prospective trial to validate these findings is warranted. PMID:29124649

Angiotensin receptor blockade: a novel approach for symptomatic radiation necrosis after stereotactic radiosurgery.

PubMed

Chowdhary, Mudit; Okwan-Duodu, Derick; Switchenko, Jeffrey M; Press, Robert H; Jhaveri, Jaymin; Buchwald, Zachary S; Zhong, Jim; Chapman, Bhavana V; Bindra, Ranjit S; Contessa, Joseph N; Park, Henry S; Yu, James B; Decker, Roy H; Olson, Jeffrey J; Oyesiku, Nelson M; Abrams, Ross A; Shu, Hui-Kuo G; Curran, Walter J; Crocker, Ian R; Patel, Kirtesh R

2018-01-01

Preclinical evidence suggests angiotensin blockade therapy (ABT) decreases late radiation toxicities. This study aims to investigate the association between ABT and symptomatic radiation necrosis (SRN) following stereotactic radiosurgery (SRS). Resected brain metastases (rBM) and arteriovenous malformation (AVM) patients treated with SRS from 2002 to 2015 were identified. Patients in the ABT cohort were on therapy during SRS and at 1-month follow up. Kaplan Meier method and cumulative incidence model were used to analyze overall survival (OS) and intracranial outcomes. 228 consecutive patients were treated with SRS: 111 with rBM and 117 with AVM. Overall, 51 (22.4%) patients were in the ABT group: 32 (28.8%) in the rBM and 19 (16.2%) in AVM cohorts. Baseline characteristics were similar, except for higher Graded Prognostic Analysis (3-4) in the rBM (ABT: 25.0% vs. non-ABT: 49.0%, p = 0.033) and median age in the AVM (ABT: 51.4 vs. non-ABT: 35.4, p < 0.001) cohorts. In both populations, OS and intracranial efficacy (rBM-local control; AVM-obliteration rates) were statistically similar between the cohorts. ABT was associated with lower 1-year SRN rates in both populations: rBM, 3.1 versus 25.3% (p = 0.003); AVM, 6.7 vs. 14.6% (p = 0.063). On multivariate analysis, ABT was a significant predictive factor for rBM (HR: 0.17; 95% CI 0.03-0.88, p = 0.035), but did not reach statistical significance for AVM (HR: 0.36; 95% CI 0.09-1.52, p = 0.165). ABT use appears to be associated with a reduced risk of SRN following SRS, without detriment to OS or intracranial efficacy. A prospective trial to validate these findings is warranted.

Binding of Released Bim to Mcl-1 is a Mechanism of Intrinsic Resistance to ABT-199 which can be Overcome by Combination with Daunorubicin or Cytarabine in AML Cells.

PubMed

Niu, Xiaojia; Zhao, Jianyun; Ma, Jun; Xie, Chengzhi; Edwards, Holly; Wang, Guan; Caldwell, J Timothy; Xiang, Shengyan; Zhang, Xiaohong; Chu, Roland; Wang, Zhihong J; Lin, Hai; Taub, Jeffrey W; Ge, Yubin

2016-09-01

To investigate the molecular mechanism underlying intrinsic resistance to ABT-199. Western blots and real-time RT-PCR were used to determine levels of Mcl-1 after ABT-199 treatment alone or in combination with cytarabine or daunorubicin. Immunoprecipitation of Bim and Mcl-1 were used to determine the effect of ABT-199 treatment on their interactions with Bcl-2 family members. Lentiviral short hairpin RNA knockdown of Bim and CRISPR knockdown of Mcl-1 were used to confirm their role in resistance to ABT-199. JC-1 assays and flow cytometry were used to determine drug-induced apoptosis. Immunoprecipitation of Bim from ABT-199-treated cell lines and a primary patient sample demonstrated decreased association with Bcl-2, but increased association with Mcl-1 without corresponding change in mitochondrial outer membrane potential. ABT-199 treatment resulted in increased levels of Mcl-1 protein, unchanged or decreased Mcl-1 transcript levels, and increased Mcl-1 protein half-life, suggesting that the association with Bim plays a role in stabilizing Mcl-1 protein. Combining conventional chemotherapeutic agent cytarabine or daunorubicin with ABT-199 resulted in increased DNA damage along with decreased Mcl-1 protein levels, compared with ABT-199 alone, and synergistic induction of cell death in both AML cell lines and primary patient samples obtained from AML patients at diagnosis. Our results demonstrate that sequestration of Bim by Mcl-1 is a mechanism of intrinsic ABT-199 resistance and supports the clinical development of ABT-199 in combination with cytarabine or daunorubicin for the treatment of AML. Clin Cancer Res; 22(17); 4440-51. ©2016 AACR. ©2016 American Association for Cancer Research.

Population pharmacokinetics and exposure-uric acid analyses after single and multiple doses of ABT-639, a calcium channel blocker, in healthy volunteers.

PubMed

An, Guohua; Liu, Wei; Duan, W Rachel; Nothaft, Wolfram; Awni, Walid; Dutta, Sandeep

2015-03-01

ABT-639 is a selective T-type calcium channel blocker with efficacy in a wide range of preclinical models of nociceptive and neuropathic pain. In the current first-in-human (FIH) study, the pharmacokinetics, tolerability, and safety of ABT-639 after single- (up to 170 mg) and multiple doses (up to 160 mg BID) were evaluated in healthy volunteers in a randomized, double-blinded, placebo-controlled manner. ABT-639 demonstrated acceptable safety and pharmacokinetic profiles in human. Results from assessment of the routine laboratory variables showed an unexpected statistically significant and clinically relevant decrease in blood uric acid with the increase in ABT-639 dose, which is possibly due to inhibition in URAT1 transporter. Pharmacokinetic/pharmacodynamic models were constructed to characterize the relationship between ABT-639 exposure and uric acid response. The final model was a mechanism-based indirect response pharmacodynamic model with the stimulation of uric acid elimination by ABT-639. The model estimated K in values in males and females were 10.2 and 7.13 μmol/h, respectively. The model estimated K out was 0.033 1/h. ABT-639 concentration that can produce 50% stimulation in uric acid elimination was estimated to be 8,070 ng/mL. Based on the final model, further simulations were conducted to predict the effect of ABT-639 on uric acid in gout patients. The simulation results indicated that, if the urate-lowering response to ABT-639 in gout patients is similar to that in healthy subjects, ABT-639 BID doses of 140 mg or higher would be expected to provide clinically meaningful lowering of blood uric acid levels below the 380 μmol/L solubility limit of monosodium urate.

In Vitro and In Vivo Enhancement of Chemoradiation Using the Oral PARP Inhibitor ABT-888 in Colorectal Cancer Cells

DOE Office of Scientific and Technical Information (OSTI.GOV)

Shelton, Joseph W., E-mail: jwshelt@emory.edu; Waxweiler, Timothy V.; Landry, Jerome

2013-07-01

Purpose: Poly(ADP-ribose) polymerase plays a critical role in the recognition and repair of DNA single-strand breaks and double-strand breaks (DSBs). ABT-888 is an orally available inhibitor of this enzyme. This study seeks to evaluate the use of ABT-888 combined with chemotherapy and radiation therapy (RT) in colorectal carcinoma models. Methods and Materials: RT clonogenic assays were performed on HCT116 and HT29 cells treated with 5-fluorouracil, irinotecan, or oxaliplatin with or without ABT. The surviving fraction at 2 Gy and dose-modifying factor at 10% survival were analyzed. Synergism was assessed by isobologram analysis for combination therapies. γH2AX and neutral comet assaysmore » were performed to assess the effect of therapy on DSB formation/repair. In vivo assessments were made by use of HCT116 cells in a xenograft mouse model. Tumor growth delay was measured at a volume of 500 mm{sup 3}. Results: Both lines were radiosensitized by ABT alone, and ABT further increased chemotherapy dose-modifying factors to the 1.6 to 1.8 range. All combinations were synergistic (combination indices <0.9). ABT treatment significantly increased DSB after RT (γH2AX, 69% vs 43%; P=.017) and delayed repair. We found tumor growth delays of 7.22 days for RT; 11.90 days for RT and ABT; 13.5 days for oxaliplatin, RT, and ABT; 14.17 days for 5-fluorouracil, RT, and ABT; and 23.81 days for irinotecan, RT, and ABT. Conclusion: ABT-888 radiosensitizes at similar or higher levels compared with classic chemotherapies and acts synergistically with these chemotherapies to enhance RT effects. In vivo confirmation of these results indicates a potential role for combining its use with existing chemoradiation regimens.« less

Phytochemical Composition and Antioxidant Activities of Dianthus Thunbergii Hooper and Hypoxis Argentea Harv Ex Baker: Plants Used for the Management of Diabetes Mellitus in Eastern Cape, South Africa.

PubMed

Akinrinde, Akinleye Stephen; Afolayan, Anthony Jide; Bradley, Graeme

2018-01-01

Inhabitants of the Eastern Cape Province of South Africa use the roots of Dianthus thunbergii and corms of Hypoxis argentea to treat diabetes mellitus and other ailments. The objective of this study was to analyze the phytochemical composition and antioxidant activities of the aqueous and ethanol extracts of the roots and corms of two plants. Total phenolics, flavonoids, flavonols, proanthocyanidins, tannins, and alkaloids were determined by standard methods. The scavenging activities of the extracts against 1,1 diphenyl-2-picrylhydrazyl (DPPH), 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid (ABTS), nitric oxide (NO), hydrogen peroxide (H 2 O 2 ), and their ferric-reducing antioxidant potentials (FRAPs) were measured. The ethanol extract of H. argentea had the highest content of phenolics (66.71 ± 2.71 mg gallic acid equivalent/g) and tannins (1.18 ± 0.07 mg TAE/g), while the ethanol extract of D. thunbergii gave higher contents of flavonoids and proanthocyanidins (62.21 ± 1.75 mg Qe/g and 432.62 ± 2.43 mg Ca/g, respectively). Flavonols were the most predominant in the aqueous extract of H. argentea (25.51 ± 1.92 mg Qe/g). We observed a concentration-dependent response in the ABTS- and H 2 O 2 -scavenging activities and FRAP values of the extracts and standards (Vitamin C, butylated hydroxytoluene, and rutin). The ethanol extracts of both plants generally demonstrated better antioxidant activities against H 2 O 2 , NO, and ABTS while also possessing better reducing power than the aqueous extracts. The aqueous extract of D. thunbergii , however, showed the best DPPH scavenging activity. The higher content of phytochemicals and antioxidant capacity obtained for the ethanol extracts of D. thunbergii and H. argentea may prove to be valuable information in selecting suitable extraction solvents for the medicinal applications of both plants. Ethanol extracts of Hypoxis argentea had the highest levels of phenolics and tanninsEthanol extracts of Dianthus thunbergii had the highest levels of flavonoids and proanthocyanidinsEthanol extracts of both plants possess better antioxidant activityagainst hydrogen peroxide, nitric oxide, and ABTS as well as higher reducingpower than the aqueous extractsAqueous extract of Dianthus thunbergii had the highest free radical scavenging activity as measured with DPPH. Abbreviations used: ABTS: 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid); BHT: Butylated hydroxytoluene; DPPH: 1,1 diphenyl-2-picrylhydrazyl; DTA: Dianthus thunbergii aqueous extract (16.6%); DTE: Dianthus thunbergii ethanol extract (2.4%); Fe 3+ -TPTZ: Ferric tripyridyltriazine; FRAP: Ferric-reducing antioxidant potentials; GAE: Gallic acid equivalent; HAA: Hypoxis argentea aqueous extract (3.2%); HAE: Hypoxis argentea ethanol extract (1.8%); Qe: Quercetin equivalence; ROS: Reactive oxygen species; TBA: Thiobarbituric acid;TCA: Trichloroacetic acid.

In vitro antioxidant properties, free radicals scavenging activities of extracts and polyphenol composition of a non-timber forest product used as spice: Monodora myristica.

PubMed

Moukette, Bruno Moukette; Pieme, Constant Anatole; Njimou, Jacques Romain; Biapa, Cabral Prosper Nya; Marco, Bravi; Ngogang, Jeanne Yonkeu

2015-03-14

Excessive production of free radicals causes direct damage to biological molecules such as DNA, proteins, lipids, carbohydrates leading to tumor development and progression. Natural antioxidant molecules from phytochemicals of plant origin may directly inhibit either their production or limit their propagation or destroy them to protect the system. In the present study, Monodora myristica a non-timber forest product consumed in Cameroon as spice was screened for its free radical scavenging properties, antioxidant and enzymes protective activities. Its phenolic compound profile was also realized by HPLC. This study demonstrated that M. myristica has scavenging properties against DPPH(•), OH(•), NO(•), and ABTS(•) radicals which vary in a dose depending manner. It also showed an antioxidant potential that was comparable with that of Butylated Hydroxytoluene (BHT) and vitamin C used as standard. The aqueous ethanol extract of M. myristica barks (AEH); showed a significantly higher content in polyphenolic compounds (21.44 ± 0.24 mg caffeic acid/g dried extract) and flavonoid (5.69 ± 0.07 quercetin equivalent mg/g of dried weight) as compared to the other studied extracts. The HPLC analysis of the barks and leaves revealed the presence of several polyphenols. The acids (3,4-OH-benzoic, caffeic, gallic, O- and P- coumaric, syringic, vanillic), alcohols (tyrosol and OH-tyrosol), theobromine, quercetin, rutin, catechine and apigenin were the identified and quantified polyphenols. All the tested extracts demonstrated a high protective potential on the superoxide dismutase (SOD), catalase and peroxidase activities. Finally, the different extracts from M. myristica and specifically the aqueous ethanol extract reveal several properties such as higher free radical scavenging properties, significant antioxidant capacities and protective potential effects on liver enzymes.

Effects of Extraction and Processing Methods on Antioxidant Compound Contents and Radical Scavenging Activities of Laver (Porphyra tenera)

PubMed Central

Hwang, Eun-Sun; Thi, Nhuan Do

2014-01-01

Laver is one of the most consumed edible red algae seaweeds in the genus Porphyra. Laver is primarily prepared in the form of dried, roasted, and seasoned products. We investigated the total polyphenol and flavonoid contents of laver products, and evaluated the in vitro antioxidant properties of solvent extracts from commercially processed laver products. Significant differences in the concentration of phenolic compounds were found among differently processed laver. The total phenolic content for laver extracts ranged from 10.81 mg gallic acid equivalent (GAE)/g extract to 32.14 mg GAE/g extract, depending on extraction solvent and temperature. Laver extracts contained very few flavonoids (0.55 mg catechin equivalent/g extracts to 1.75 mg catechin equivalent/g extracts). 2,2-Diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), hydroxyl radical, and superoxide anion scavenging assays were used to determine the radical scavenging capacities of laver extracts. These assays revealed that the processing method and extraction condition affected the antioxidant potentials of laver. Antioxidant activity of dried laver, roasted laver, and seasoned laver increased in a concentration-dependent manner (100~1,000 μg/mL). The radical scavenging activities of 37°C and 100°C water extracts were lower than that of a 37°C 70% ethanol extract. The highest radical scavenging capacity was observed in the 37°C 70% ethanol extracts of dried laver, roasted laver, and seasoned laver. Overall, these results support that notion that laver contains bioactive compounds, such as polyphenols and flavonoids, which may have a positive effect on health. PMID:24772408

Effects of Extraction and Processing Methods on Antioxidant Compound Contents and Radical Scavenging Activities of Laver (Porphyra tenera).

PubMed

Hwang, Eun-Sun; Thi, Nhuan Do

2014-01-01

Laver is one of the most consumed edible red algae seaweeds in the genus Porphyra. Laver is primarily prepared in the form of dried, roasted, and seasoned products. We investigated the total polyphenol and flavonoid contents of laver products, and evaluated the in vitro antioxidant properties of solvent extracts from commercially processed laver products. Significant differences in the concentration of phenolic compounds were found among differently processed laver. The total phenolic content for laver extracts ranged from 10.81 mg gallic acid equivalent (GAE)/g extract to 32.14 mg GAE/g extract, depending on extraction solvent and temperature. Laver extracts contained very few flavonoids (0.55 mg catechin equivalent/g extracts to 1.75 mg catechin equivalent/g extracts). 2,2-Diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), hydroxyl radical, and superoxide anion scavenging assays were used to determine the radical scavenging capacities of laver extracts. These assays revealed that the processing method and extraction condition affected the antioxidant potentials of laver. Antioxidant activity of dried laver, roasted laver, and seasoned laver increased in a concentration-dependent manner (100~1,000 μg/mL). The radical scavenging activities of 37°C and 100°C water extracts were lower than that of a 37°C 70% ethanol extract. The highest radical scavenging capacity was observed in the 37°C 70% ethanol extracts of dried laver, roasted laver, and seasoned laver. Overall, these results support that notion that laver contains bioactive compounds, such as polyphenols and flavonoids, which may have a positive effect on health.

Exploration of avocado by-products as natural sources of bioactive compounds.

PubMed

Tremocoldi, Maria Augusta; Rosalen, Pedro Luiz; Franchin, Marcelo; Massarioli, Adna Prado; Denny, Carina; Daiuto, Érica Regina; Paschoal, Jonas Augusto Rizzato; Melo, Priscilla Siqueira; Alencar, Severino Matias de

2018-01-01

This study aimed to evaluate the antioxidant, anti-inflammatory, and cytotoxic properties and phenolic composition of peel and seed of avocado varieties Hass and Fuerte using green solvents. Ethanol soluble compounds were identified in peel and seed of both varieties using HPLC-MS/MS and quantified using HPLC-DAD. Agro-industrial by-products of both varieties exhibited high radical scavenging activity against synthetic free radicals (DPPH and ABTS) and reactive oxygen species (peroxyl, superoxide, and hypochlorous acid) and high ability to reduce Fe3+ to Fe2+. The main compounds with significant contribution to the antioxidant activity determined by online HPLC-ABTS●+ analyses were procyanidin B2 and epicatechin in the peel and trans-5-O-caffeoyl-D-quinic acid, procyanidin B1, catechin, and epicatechin in the seed. Peel of Fuerte significantly suppressed TNF-α and nitric oxide (NO) release (459.3 pg/mL and 8.5 μM, respectively), possibly because of the high phenolic content and antioxidant activity detected. Avocado agro-industrial by-products can be used for food and pharmaceutical purposes due to their antioxidant and anti-inflammatory properties.

Non-enzymatic browning reaction of glucosamine at mild conditions: Relationship between colour formation, radical scavenging activity and α-dicarbonyl compounds production.

PubMed

Hong, Pui Khoon; Betti, Mirko

2016-12-01

Glucosamine (GlcN, 5% w/v) was incubated in either phosphate buffer or ammonium hydroxide solutions at 40 and 60°C for up to 48h in order to yield caramel solutions. Non-enzymatic browning was monitored via changes in absorption at 280, 320 and 420nm and the physico-chemical properties as well as the generation of short chain α-dicarbonyl compounds were evaluated. Accumulation of GlcN autocondensation products (280nm) proceeded in parallel with the development of pre-melanoidins (320nm) and melanoidins (420nm). The reactive α-dicarbonyls were detected at temperature as low as 40°C within 3h with a maximum level of diacetyl recorded at 6h. The caramel solutions showed a high efficacy in scavenging DPPH and ABTS radicals in accordance with the increasing browning intensity. The results suggest that GlcN browning can be modulated according to the specific desired properties to produce a multi-functional food ingredient that has health-promoting effects. Copyright © 2016 Elsevier Ltd. All rights reserved.

Monoterpenes: Novel insights into their biological effects and roles on glucose uptake and lipid metabolism in 3T3-L1 adipocytes.

PubMed

Tan, X C; Chua, K H; Ravishankar Ram, M; Kuppusamy, U R

2016-04-01

Various strategies have been adopted to combat complications caused by Type 2 diabetes mellitus and controlled diet is one of them. Monoterpenes, major constituents of essential oils, are synthesized and widely used as artificial food flavors. A series of twelve monoterpenes were assessed in the present study. Monoterpenes, exhibited low 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity even at high concentrations. Some monoterpenes inhibited α-amylase and α-glucosidase activity and stimulated glucose uptake and lipolysis. Monoterpenes such as (R)-(+)-limonene stimulated both glucose uptake (17.4%) and lipolysis (17.7%); the mRNA expression of glucose transporter 1 (GLUT1) was upregulated but glucose transporter 4 (GLUT4) was unaffected, and adipose triglyceride lipase (ATGL) was suppressed. Taken together, the selected monoterpenes may not confer strong protection against free radicals but nevertheless, their positive influence on lipid and glucose metabolism may have potential in the control of obesity and Type 2 diabetes mellitus. Copyright © 2015 Elsevier Ltd. All rights reserved.

Exploration of avocado by-products as natural sources of bioactive compounds

PubMed Central

Tremocoldi, Maria Augusta; Rosalen, Pedro Luiz; Franchin, Marcelo; Massarioli, Adna Prado; Denny, Carina; Daiuto, Érica Regina; Paschoal, Jonas Augusto Rizzato; Melo, Priscilla Siqueira

2018-01-01

This study aimed to evaluate the antioxidant, anti-inflammatory, and cytotoxic properties and phenolic composition of peel and seed of avocado varieties Hass and Fuerte using green solvents. Ethanol soluble compounds were identified in peel and seed of both varieties using HPLC-MS/MS and quantified using HPLC-DAD. Agro-industrial by-products of both varieties exhibited high radical scavenging activity against synthetic free radicals (DPPH and ABTS) and reactive oxygen species (peroxyl, superoxide, and hypochlorous acid) and high ability to reduce Fe3+ to Fe2+. The main compounds with significant contribution to the antioxidant activity determined by online HPLC-ABTS●+ analyses were procyanidin B2 and epicatechin in the peel and trans-5-O-caffeoyl-D-quinic acid, procyanidin B1, catechin, and epicatechin in the seed. Peel of Fuerte significantly suppressed TNF-α and nitric oxide (NO) release (459.3 pg/mL and 8.5 μM, respectively), possibly because of the high phenolic content and antioxidant activity detected. Avocado agro-industrial by-products can be used for food and pharmaceutical purposes due to their antioxidant and anti-inflammatory properties. PMID:29444125

Phenolic acids and flavonoids of peanut by-products: Antioxidant capacity and antimicrobial effects.

PubMed

de Camargo, Adriano Costa; Regitano-d'Arce, Marisa Aparecida Bismara; Rasera, Gabriela Boscariol; Canniatti-Brazaca, Solange Guidolin; do Prado-Silva, Leonardo; Alvarenga, Verônica Ortiz; Sant'Ana, Anderson S; Shahidi, Fereidoon

2017-12-15

Peanut skin (PS) and meal from dry-blanched peanuts (MDBP) were evaluated as sources of phenolic compounds. PS rendered the highest total phenolic content, antioxidant capacity towards ABTS radical cation, DPPH and hydroxyl radicals as well as reducing power. Phenolic acids were present in PS and MDBP whereas proanthocyanidins and monomeric flavonoids were found only in PS as identified by HPLC-DAD-ESI-MS n . Procyanidin-rich extracts prevented oxidation in non-irradiated and gamma-irradiated fish model system. Both extracts inhibited the growth of gram-positive (Bacillus cereus, Staphylococcus aureus, Listeria monocytogenes, Geobacillus stearothermophilus) and gram-negative bacteria (Pseudomonas aeruginosa, Pseudomonas fluorescens, Salmonella Enteritidis, Salmonella Typhimurium, Escherichia coli). Regardless of the strain, phenolic acid-rich extracts showed the lowest minimum inhibitory capacity (MIC); therefore presenting higher antibacterial effect. The MIC of phenolic acid-rich extracts (24-49μgphenolics/mL) was higher but comparable to Ampicillin (10μg/mL). Thus, phenolics in PS and MDBP may serve as antioxidants and antimicrobial compounds. Copyright © 2017. Published by Elsevier Ltd.

Starch-based bio-elastomers functionalized with red beetroot natural antioxidant.

PubMed

Tran, Thi Nga; Athanassiou, Athanassia; Basit, Abdul; Bayer, Ilker S

2017-02-01

Red beetroot (RB) powder was incorporated into starch-based bio-elastomers to obtain flexible biocomposites with tunable antioxidant properties. Starch granules within the bio-elastomers affected the release of the antioxidant molecule betanin in the RB powder. The bio-elastomers were hydrophobic and resisted dissolution in water, hence the release of betanin was due to diffusion rather than polymer matrix disintegration. Hydrophobicity was maintained even after water immersion. Released betanin demonstrated highly efficient antioxidant scavenging activity against 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS(+)). RB powder was also found to increase the Young's modulus of the bio-elastomers without compromising their elongation ability. Infrared spectral analysis indicated weak interactions through hydrogen bonding among starch granules, RB powder and PDMS polymer within the bio-elastomers. Hence, as a simple but intelligent biomaterial consisting of mainly edible starch and RB powder the present bio-elastomers can be used in active packaging for a variety of pharmaceutical, medical, and food applications. Copyright © 2016 Elsevier Ltd. All rights reserved.

ANTIOXIDANT ACTIVITY AND A-AMYLASE INHIBITORY POTENTIAL OF ROSA CANINA L

PubMed Central

Jemaa, Houda Ben; Jemia, Amani Ben; Khlifi, Sarra; Ahmed, Halima Ben; Slama, Fethi Ben; Benzarti, Anis; Elati, Jalila; Aouidet, Abdallah

2017-01-01

Background: Diabetes mellitus is one of the most common endocrinal disorders and medicinal plants continue to play an important role in the management of this disease. In this study, Rosa canina was investigated for the antioxidant and α-amylase inhibition activities. Materials and Methods: Methanolic extract of Rosa canina was investigated for its potential antioxidant activity. The extracts’ total phenolic and flavonoid contents and scavenging capacity for free radicals were evaluated. The α-amylase inhibition assay was also carried. Results: Rosa canina extract exhibits a total Phenolic and flavonoid levels respectively (21.918 mg GAE/g and 2.647mg ER/g). The free radical scavenging activity was found to be prominent against DPPH with an IC50 of 0.668 mg/ml and against ABTS with an IC50 of 0.467 mg/ml. Extract showed a significant ferric ion reducing activities with an IC50 of4.962 mg/ml. Conclusion: Rosa canina exerted a higher inhibitory activity against α-amylase. The obtained results support the antidiabetic use of rosa canina. PMID:28573216

Fish skin gelatin hydrolysates produced by visceral peptidase and bovine trypsin: Bioactivity and stability.

PubMed

Ketnawa, Sunantha; Benjakul, Soottawat; Martínez-Alvarez, Oscar; Rawdkuen, Saroat

2017-01-15

The peptidase from the viscera of farmed giant catfish was used for producing gelatin hydrolysates (HG) and compared with those produced from commercial bovine trypsin (HB). The degree of hydrolysis (DH) observed suggests that proteolytic cleavage rapidly occurred within the first 120min of incubation, and there was higher DH in HG than in HB. HG demonstrated the highest ACE-inhibitory activity, DPPH, ABTS radical scavenging activity, and FRAP. HB showed the highest FRAP activity. The DPPH radical scavenging activity of HG was quite stable over the pH range of 1-11, but it increased slightly when the heating duration time reached 240min at 100°C. The ACE-inhibitory activity of HG showed the highest stability at a pH of 7, and it remained very stable at 100°C for over 15-240min. The visceral peptidase from farmed giant catfish could be an alternative protease for generating protein hydrolysates with desirable bioactivities. The resulting hydrolysates showed good stability, making them potential functional ingredients for food formulations. Copyright © 2016 Elsevier Ltd. All rights reserved.

Chemical composition, fatty acid content and antioxidant potential of meat from goats supplemented with Moringa (Moringa oleifera) leaves, sunflower cake and grass hay.

PubMed

Qwele, K; Hugo, A; Oyedemi, S O; Moyo, B; Masika, P J; Muchenje, V

2013-03-01

The present study determined the chemical composition, fatty acid (FA) content and antioxidant capacity of meat from goats supplemented with Moringa oleifera leaves (MOL) or sunflower cake (SC) or grass hay (GH). The meat from goat supplemented with MOL had higher concentrations of total phenolic content (10.62±0.27 mg tannic acid equivalent E/g). The MOL significantly scavenged 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic-acid (ABTS) radical to 93.51±0.19% (93.51±0.19%) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical to 58.95±0.3% than other supplements. The antioxidative effect of MOL supplemented meat on catalase (CAT), reduced glutathione (GSH), superoxide dismutase (SOD) and lipid oxidation (LO) was significantly (P<0.05) higher than other meat from goat feed on grass hay or those supplemented with sunflower seed cake. The present study indicated that the anti-oxidative potential of MOL may play a role in improving meat quality (chemical composition, colour and lipid stability). Copyright © 2012 Elsevier Ltd. All rights reserved.

Carotenoids, Phenolic Compounds and Tocopherols Contribute to the Antioxidative Properties of Some Microalgae Species Grown on Industrial Wastewater.

PubMed

Safafar, Hamed; van Wagenen, Jonathan; Møller, Per; Jacobsen, Charlotte

2015-12-11

This study aimed at investigating the potential of microalgae species grown on industrial waste water as a new source of natural antioxidants. Six microalgae from different classes, including Phaeodactylum sp. (Bacillariophyceae), Nannochloropsis sp. (Eustigmatophyceae), Chlorella sp., Dunaniella sp., and Desmodesmus sp. (Chlorophyta), were screened for their antioxidant properties using different in vitro assays. Natural antioxidants, including pigments, phenolics, and tocopherols, were measured in methanolic extracts of microalgae biomass. Highest and lowest concentrations of pigments, phenolic compounds, and tocopherols were found in Desmodesmus sp. and Phaeodactylum tricornuotom microalgae species, respectively. The results of each assay were correlated to the content of natural antioxidants in microalgae biomass. Phenolic compounds were found as major contributors to the antioxidant activity in all antioxidant tests while carotenoids were found to contribute to the 1,1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging activity, ferrous reduction power (FRAP), and ABTS-radical scavenging capacity activity. Desmodesmus sp. biomass represented a potentially rich source of natural antioxidants, such as carotenoids (lutein), tocopherols, and phenolic compounds when cultivated on industrial waste water as the main nutrient source.

Carotenoids, Phenolic Compounds and Tocopherols Contribute to the Antioxidative Properties of Some Microalgae Species Grown on Industrial Wastewater

PubMed Central

Safafar, Hamed; van Wagenen, Jonathan; Møller, Per; Jacobsen, Charlotte

2015-01-01

This study aimed at investigating the potential of microalgae species grown on industrial waste water as a new source of natural antioxidants. Six microalgae from different classes, including Phaeodactylum sp. (Bacillariophyceae), Nannochloropsis sp. (Eustigmatophyceae), Chlorella sp., Dunaniella sp., and Desmodesmus sp. (Chlorophyta), were screened for their antioxidant properties using different in vitro assays. Natural antioxidants, including pigments, phenolics, and tocopherols, were measured in methanolic extracts of microalgae biomass. Highest and lowest concentrations of pigments, phenolic compounds, and tocopherols were found in Desmodesmus sp. and Phaeodactylum tricornuotom microalgae species, respectively. The results of each assay were correlated to the content of natural antioxidants in microalgae biomass. Phenolic compounds were found as major contributors to the antioxidant activity in all antioxidant tests while carotenoids were found to contribute to the 1,1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging activity, ferrous reduction power (FRAP), and ABTS-radical scavenging capacity activity. Desmodesmus sp. biomass represented a potentially rich source of natural antioxidants, such as carotenoids (lutein), tocopherols, and phenolic compounds when cultivated on industrial waste water as the main nutrient source. PMID:26690454

Hydrogen sulfide inhibits enzymatic browning of fresh-cut lotus root slices by regulating phenolic metabolism.

PubMed

Sun, Ying; Zhang, Wei; Zeng, Tao; Nie, Qixing; Zhang, Fengying; Zhu, Liqin

2015-06-15

The effect of fumigation with hydrogen sulfide (H2S) gas on inhibiting enzymatic browning of fresh-cut lotus root slices was investigated. Browning degree, changes in color, total phenol content, superoxide anion production rate (O2(-)), H2O2 content, antioxidant capacities (DPPH radical scavenging ability, ABTS radical scavenging activity and the reducing power) and activities of the phenol metabolism-associated enzymes including phenylalanine ammonialyase (PAL), catalase (CAT), peroxidase (POD), polyphenol oxidase (PPO) were evaluated. The results showed that treatment with 15 μl L(-1) H2S significantly inhibited the browning of fresh-cut lotus root slices (P<0.05), reduced significantly O2(-) production rate and H2O2 content, and enhanced antioxidant capacities (P<0.05). PPO and POD activities in the fresh-cut lotus root slices were also significantly inhibited by treatment with H2S (P<0.05). This study suggested that treatment with exogenous H2S could inhibit the browning of fresh-cut lotus root slices by enhancing antioxidant capacities to alleviate the oxidative damage. Copyright © 2015 Elsevier Ltd. All rights reserved.

Phytochemical analysis with free radical scavenging, nitric oxide inhibition and antiproliferative activity of Sarcocephalus pobeguinii extracts.

PubMed

Mfotie Njoya, Emmanuel; Munvera, Aristide Mfifen; Mkounga, Pierre; Nkengfack, Augustin Ephrem; McGaw, Lyndy Joy

2017-04-04

Free radicals have been implicated in the pathogenesis of diverse metabolic disorders including cancer. Therefore, fighting against free radicals has become an important strategy in the prevention or treatment of such diseases, in addition to direct or indirect anticancer chemotherapy. Sarcocephalus pobeguinii has been used traditionally to treat various diseases in which excess production of free radicals is implicated, warranting investigation of its free radical scavenging, anticancer and anti-inflammatory activity. In the present study, extracts from leaves, fruits, roots and bark of Sarcocephalus pobeguinii were evaluated on four human cancer cell lines (MCF-7, HeLa, Caco-2 and A549 cells) and a non-cancerous cell line for their antiproliferative potential. The cells were incubated with the plant extracts for 48 h at 37 °C in a 5% CO 2 humidified environment and their cytotoxic effect was determined using the tetrazolium-based colorimetric (MTT) assay. The radical inhibition was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) scavenging techniques. The nitric oxide inhibitory activity was determined using LPS-activated RAW 264.7 macrophages. The correlation between radical scavenging capacity and antiproliferative activity was also analysed. The extract from leaves of Sarcocephalus pobeguinii (LSP) exhibited the highest cytotoxic effect on all four of the human cancer cell lines but with some cytotoxicity to the normal Vero cells. However, the LSP extract had the best selectivity index, ranging from 3.15 to 18.28. Also, antioxidant and anti-inflammatory assays indicated that the LSP extract had the highest radical scavenging capacity of all the extracts. A positive linear correlation was found between free radical scavenging ability and antiproliferative activity against the four cancer cell lines, with the highest correlation factor (R 2  = 0.9914) obtained between DPPH inhibition and antiproliferative activity against A549 cells. The high selectivity index of the Sarcocephalus pobeguinii leaf extract indicates the potential of using this extract in cancer therapy. Furthermore, the positive correlation between free radical scavenging and antiproliferative activity suggests that the radical scavenging capacity of extracts may contribute to a prediction of their anticancer property.

In vitro antibacterial potency and spectrum of ABT-492, a new fluoroquinolone.

PubMed

Nilius, Angela M; Shen, Linus L; Hensey-Rudloff, Dena; Almer, Laurel S; Beyer, Jill M; Balli, Darlene J; Cai, Yingna; Flamm, Robert K

2003-10-01

ABT-492 demonstrated potent antibacterial activity against most quinolone-susceptible pathogens. The rank order of potency was ABT-492 > trovafloxacin > levofloxacin > ciprofloxacin against quinolone-susceptible staphylococci, streptococci, and enterococci. ABT-492 had activity comparable to those of trovafloxacin, levofloxacin, and ciprofloxacin against seven species of quinolone-susceptible members of the family Enterobacteriaceae, although it was less active than the comparators against Citrobacter freundii and Serratia marcescens. The activity of ABT-492 was greater than those of the comparators against fastidious gram-negative species, including Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Legionella spp. and against Pseudomonas aeruginosa and Helicobacter pylori. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity. In particular, ABT-492 was more active than trovafloxacin and levofloxacin against multidrug-resistant Streptococcus pneumoniae, including strains resistant to penicillin and macrolides, and H. influenzae, including beta-lactam-resistant strains. It retained greater in vitro activity than the comparators against S. pneumoniae and H. influenzae strains resistant to other quinolones due to amino acid alterations in the quinolone resistance-determining regions of the target topoisomerases. ABT-492 was a potent inhibitor of bacterial topoisomerases, and unlike the comparators, DNA gyrase and topoisomerase IV from either Staphylococcus aureus or Escherichia coli were almost equally sensitive to ABT-492. The profile of ABT-492 suggested that it may be a useful agent for the treatment of community-acquired respiratory tract infections, as well as infections of the urinary tract, bloodstream, and skin and skin structure and nosocomial lung infections.

In Vitro Antibacterial Potency and Spectrum of ABT-492, a New Fluoroquinolone

PubMed Central

Nilius, Angela M.; Shen, Linus L.; Hensey-Rudloff, Dena; Almer, Laurel S.; Beyer, Jill M.; Balli, Darlene J.; Cai, Yingna; Flamm, Robert K.

2003-01-01

ABT-492 demonstrated potent antibacterial activity against most quinolone-susceptible pathogens. The rank order of potency was ABT-492 > trovafloxacin > levofloxacin > ciprofloxacin against quinolone-susceptible staphylococci, streptococci, and enterococci. ABT-492 had activity comparable to those of trovafloxacin, levofloxacin, and ciprofloxacin against seven species of quinolone-susceptible members of the family Enterobacteriaceae, although it was less active than the comparators against Citrobacter freundii and Serratia marcescens. The activity of ABT-492 was greater than those of the comparators against fastidious gram-negative species, including Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Legionella spp. and against Pseudomonas aeruginosa and Helicobacter pylori. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity. In particular, ABT-492 was more active than trovafloxacin and levofloxacin against multidrug-resistant Streptococcus pneumoniae, including strains resistant to penicillin and macrolides, and H. influenzae, including β-lactam-resistant strains. It retained greater in vitro activity than the comparators against S. pneumoniae and H. influenzae strains resistant to other quinolones due to amino acid alterations in the quinolone resistance-determining regions of the target topoisomerases. ABT-492 was a potent inhibitor of bacterial topoisomerases, and unlike the comparators, DNA gyrase and topoisomerase IV from either Staphylococcus aureus or Escherichia coli were almost equally sensitive to ABT-492. The profile of ABT-492 suggested that it may be a useful agent for the treatment of community-acquired respiratory tract infections, as well as infections of the urinary tract, bloodstream, and skin and skin structure and nosocomial lung infections. PMID:14506039

Thrombospondin-1 (TSP-1) Analogs ABT-510 and ABT-898 Inhibit Prolactinoma Growth and Recover Active Pituitary Transforming Growth Factor-β1 (TGF-β1)

PubMed Central

Recouvreux, M. Victoria; Camilletti, M. Andrea; Rifkin, Daniel B.; Becu-Villalobos, Damasia

2012-01-01

Prolactinomas are the most prevalent type of secreting pituitary tumors in humans and generally respond well to a medical therapy with dopamine agonists. However, for patients exhibiting resistance to dopaminergic drugs, alternative treatments are desired. Antiangiogenic strategies might represent a potential therapy for these tumors. Thrombospondin 1 (TSP-1) is a large multifunctional glycoprotein involved in multiple biological processes including angiogenesis, apoptosis, and activation of TGF-β1. Because tumors that overexpress TSP-1 grow more slowly, have fewer metastases, and have decreased angiogenesis, TSP-1 provides a novel target for cancer treatment. ABT-510 and ABT-898 are TSP-1 synthetic analogs that mimic its antiangiogenic action. In the present study, we explored the potential effect of ABT-510 and ABT-898 on experimental prolactinomas induced by chronic diethylstilbestrol (DES) treatment in female rats. We demonstrated that a 2-wk treatment with ABT-510 and ABT-898 counteracted the increase in pituitary size and serum prolactin levels as well as the pituitary proliferation rate induced by DES. These inhibitory effects on tumor growth could be mediated by the antiangiogenic properties of the drugs. We also demonstrated that ABT-510 and ABT-898, in addition to their described antiangiogenic effects, increased active TGF-β1 level in the tumors. We postulate that the recovery of the local cytokine activation participates in the inhibition of lactotrope function. These results place these synthetic TSP-1 analogs as potential alternative or complementary treatments in dopamine agonist-resistant prolactinomas. PMID:22700773

Thrombospondin-1 (TSP-1) analogs ABT-510 and ABT-898 inhibit prolactinoma growth and recover active pituitary transforming growth factor-β1 (TGF-β1).

PubMed

Recouvreux, M Victoria; Camilletti, M Andrea; Rifkin, Daniel B; Becu-Villalobos, Damasia; Díaz-Torga, Graciela

2012-08-01

Prolactinomas are the most prevalent type of secreting pituitary tumors in humans and generally respond well to a medical therapy with dopamine agonists. However, for patients exhibiting resistance to dopaminergic drugs, alternative treatments are desired. Antiangiogenic strategies might represent a potential therapy for these tumors. Thrombospondin 1 (TSP-1) is a large multifunctional glycoprotein involved in multiple biological processes including angiogenesis, apoptosis, and activation of TGF-β1. Because tumors that overexpress TSP-1 grow more slowly, have fewer metastases, and have decreased angiogenesis, TSP-1 provides a novel target for cancer treatment. ABT-510 and ABT-898 are TSP-1 synthetic analogs that mimic its antiangiogenic action. In the present study, we explored the potential effect of ABT-510 and ABT-898 on experimental prolactinomas induced by chronic diethylstilbestrol (DES) treatment in female rats. We demonstrated that a 2-wk treatment with ABT-510 and ABT-898 counteracted the increase in pituitary size and serum prolactin levels as well as the pituitary proliferation rate induced by DES. These inhibitory effects on tumor growth could be mediated by the antiangiogenic properties of the drugs. We also demonstrated that ABT-510 and ABT-898, in addition to their described antiangiogenic effects, increased active TGF-β1 level in the tumors. We postulate that the recovery of the local cytokine activation participates in the inhibition of lactotrope function. These results place these synthetic TSP-1 analogs as potential alternative or complementary treatments in dopamine agonist-resistant prolactinomas.

The Stress Protein BAG3 Stabilizes Mcl-1 Protein and Promotes Survival of Cancer Cells and Resistance to Antagonist ABT-737*

PubMed Central

Boiani, Mariana; Daniel, Cristina; Liu, Xueyuan; Hogarty, Michael D.; Marnett, Lawrence J.

2013-01-01

Members of the Bcl-2 family of proteins are important inhibitors of apoptosis in human cancer and are targets for novel anticancer agents such as the Bcl-2 antagonists, ABT-263 (Navitoclax), and its analog ABT-737. Unlike Bcl-2, Mcl-1 is not antagonized by ABT-263 or ABT-737 and is considered to be a major factor in resistance. Also, Mcl-1 exhibits differential regulation when compared with other Bcl-2 family members and is a target for anticancer drug discovery. Here, we demonstrate that BAG3, an Hsp70 co-chaperone, protects Mcl-1 from proteasomal degradation, thereby promoting its antiapoptotic activity. Using neuroblastoma cell lines, with a defined Bcl-2 family dependence, we found that BAG3 expression correlated with Mcl-1 dependence and ABT-737 resistance. RNA silencing of BAG3 led to a marked reduction in Mcl-1 protein levels and overcame ABT-737 resistance in Mcl-1-dependent cells. In ABT-737-resistant cells, Mcl-1 co-immunoprecipitated with BAG3, and loss of Mcl-1 after BAG3 silencing was prevented by proteasome inhibition. BAG3 and Mcl-1 were co-expressed in a panel of diverse cancer cell lines resistant to ABT-737. Silencing BAG3 reduced Mcl-1 protein levels and overcame ABT-737 resistance in several of the cell lines, including triple-negative breast cancer (MDA-MB231) and androgen receptor-negative prostate cancer (PC3) cells. These studies identify BAG3-mediated Mcl-1 stabilization as a potential target for cancer drug discovery. PMID:23341456

The stress protein BAG3 stabilizes Mcl-1 protein and promotes survival of cancer cells and resistance to antagonist ABT-737.

PubMed

Boiani, Mariana; Daniel, Cristina; Liu, Xueyuan; Hogarty, Michael D; Marnett, Lawrence J

2013-03-08

Members of the Bcl-2 family of proteins are important inhibitors of apoptosis in human cancer and are targets for novel anticancer agents such as the Bcl-2 antagonists, ABT-263 (Navitoclax), and its analog ABT-737. Unlike Bcl-2, Mcl-1 is not antagonized by ABT-263 or ABT-737 and is considered to be a major factor in resistance. Also, Mcl-1 exhibits differential regulation when compared with other Bcl-2 family members and is a target for anticancer drug discovery. Here, we demonstrate that BAG3, an Hsp70 co-chaperone, protects Mcl-1 from proteasomal degradation, thereby promoting its antiapoptotic activity. Using neuroblastoma cell lines, with a defined Bcl-2 family dependence, we found that BAG3 expression correlated with Mcl-1 dependence and ABT-737 resistance. RNA silencing of BAG3 led to a marked reduction in Mcl-1 protein levels and overcame ABT-737 resistance in Mcl-1-dependent cells. In ABT-737-resistant cells, Mcl-1 co-immunoprecipitated with BAG3, and loss of Mcl-1 after BAG3 silencing was prevented by proteasome inhibition. BAG3 and Mcl-1 were co-expressed in a panel of diverse cancer cell lines resistant to ABT-737. Silencing BAG3 reduced Mcl-1 protein levels and overcame ABT-737 resistance in several of the cell lines, including triple-negative breast cancer (MDA-MB231) and androgen receptor-negative prostate cancer (PC3) cells. These studies identify BAG3-mediated Mcl-1 stabilization as a potential target for cancer drug discovery.

Free-radical chemistry of sulfite.

PubMed Central

Neta, P; Huie, R E

1985-01-01

The free-radical chemistry of sulfite oxidation is reviewed. Chemical transformations of organic and biological molecules induced by sulfite oxidation are summarized. The kinetics of the free-radical oxidations of sulfite are discussed, as are the kinetics of the reactions of the sulfite-derived radicals SO3 and the peroxy derivative SO5 with organic compounds. PMID:3830699

Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.

PubMed

Peng, Ying; Lou, Li-Li; Liu, Si-Fan; Zhou, Le; Huang, Xiao-Xiao; Song, Shao-Jiang

2016-11-15

Seven new neolignans (1-2, 7-11) and five known compounds (3-6, 12) were isolated from the 70% EtOH extract of hawthorn seeds. Their structures were determined by spectroscopic analyses. The antioxidant and anti-inflammatory activities of all the isolates were investigated. Most of the isolates showed moderate radical scavenging activity in the DPPH assay and significant activities in the ABTS and FRAP assays. Furthermore, compounds 7-12 exhibited marked nitric oxide (NO) inhibition and compounds 1-4 had a potent necrosis factor-α (TNF-α) inhibitory effect. The results we obtained showed that hawthorn seeds can be regarded as a potential new and cheap source of antioxidants and inflammation inhibitors. Copyright © 2016 Elsevier Ltd. All rights reserved.

The scavenging reactions of nitrogen dioxide radical and carbonate radical by tea polyphenol derivatives: a pulse radiolysis study

NASA Astrophysics Data System (ADS)

Miao, Jin-Ling; Wang, Wen-Feng; Pan, Jing-Xi; Lu, Chang-Yuan; Li, Rong-Qun; Yao, Si-De

2001-02-01

The reactions of tea polyphenol derivatives, including epicatechin (EC) and epigallocatechin gallate (EGCG), with nitrogen dioxide radical (NO 2rad ) and carbonate radical (CO 3rad - ) have been studied in detail using time-resolved pulse radiolysis technique. In all the cases, the corresponding phenoxyl radical was formed through electron transfer reaction. From the build-up kinetics of the phenoxyl radicals and the decay kinetics of CO 3rad - radical, the reaction rate constants of EC, EGCG with NO 2rad and CO 3rad - were determined to be 9.0×10 7, 1.2×10 8 and 5.6×10 8, 6.6×10 8 dm 3 mol -1 s -1, respectively. Therefore, tea polyphenol derivatives proved to be efficient scavengers of NO 2rad and CO 3rad - radicals.

Free and Bound Phenolic Compound Content and Antioxidant Activity of Different Cultivated Blue Highland Barley Varieties from the Qinghai-Tibet Plateau.

PubMed

Yang, Xi-Juan; Dang, Bin; Fan, Ming-Tao

2018-04-11

In this study, the polyphenols composition and antioxidant properties of 12 blue highland barley varieties planted on the Qinghai-Tibet Plateau area were measured. The contents of the free, bound and total phenolic acids varied between 166.20-237.60, 170.10-240.75 and 336.29-453.94 mg of gallic acid equivalents per 100 g of dry weight (DW) blue highland barley grains, while the free and bound phenolic acids accounted for 50.09% and 49.91% of the total phenolic acids, respectively. The contents of the free, bound and total flavones varied among 20.61-25.59, 14.91-22.38 and 37.91-47.98 mg of catechin equivalents per 100 g of dry weight (DW) of blue highland barley grains, while the free and bound flavones accounted for 55.90% and 44.10% of the total flavones, respectively. The prominent phenolic compounds in the blue hulless barley grains were gallic acid, benzoic acid, syringic acid, 4-coumaric acid, naringenin, hesperidin, rutin, (+)-catechin and quercetin. Among these, protocatechuic acid, chlorogenic acid and (+)-catechin were the major phenolic compounds in the free phenolics extract. The most abundant bound phenolics were gallic acid, benzoic acid, syringic acid, 4-coumaric acid, benzoic acid, dimethoxybenzoic acid, naringenin, hesperidin, quercetin and rutin. The average contribution of the bound phenolic extract to the DPPH • free radical scavenging capacity was higher than 86%, that of free phenolic extract to the ABTS •+ free radical scavenging capacity was higher than 79%, and that of free phenolic (53%) to the FRAP antioxidant activity was equivalent to that of the bound phenol extract (47%). In addition, the planting environment exerts a very important influence on the polyphenol composition, content and antioxidant activity of blue highland barley. The correlation analysis showed that 2,4-hydroxybenzoic acid and protocatechuic acid were the main contributors to the DPPH • and ABTS •+ free radical scavenging capacity in the free phenolic extract, while chlorogenic acid, vanillic acid, ferulic acid and quercetin were the main contributors to the free radical scavenging capacity in the bound phenol extract. The study results show that the blue highland barley grains have rich phenolic compounds and high antioxidant activity, as well as significant varietal differences. The free and bound phenolic extracts in the blue hulless barley grains have an equivalent proportion in the total phenol, and co-exist in two forms. They can be used as a potential valuable source of natural antioxidants, and can aid in enhancing the development and daily consumption of foods relating to blue highland barley.

Antioxidant and anticholinesterase investigations of Rumex hastatus D. Don: potential effectiveness in oxidative stress and neurological disorders.

PubMed

Ahmad, Sajjad; Ullah, Farhat; Ayaz, Muhammad; Sadiq, Abdul; Imran, Muhammad

2015-03-26

Rumex species are traditionally used for the treatment of neurological disorders including headache, migraine, depression, paralysis etc. Several species have been scientifically validated for antioxidant and anticholinestrase potentials. This study aims to investigate Rumex hastatus D. Don crude methanolic extract, subsequent fractions, saponins and flavonoids for acetylcholinestrase, butyrylcholinestrase inhibition and diverse antioxidant activities to validate its folkloric uses in neurological disorders. Rumex hastatus crude methanolic extract (Rh. Cr), subsequent fractions; n-hexane (Rh. Hex), chloroform (Rh. Chf), ethyl acetate (Rh. EtAc), aqueous fraction (Rh. Aq), crude saponins (Rh. Sp) and flavonoids (Rh. Fl) were investigated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) at various concentrations (125, 250, 500, 1000 μg/mL) using Ellman's spectrophotometric analysis. Antioxidant potentials of Rh. Sp and Rh. Fl were evaluated using DPPH, H2O2 and ABTS free radical scavenging assays at 62.5, 125, 250, 500, 1000 μg/mL. All the test samples showed concentration dependent cholinesterase inhibition and radicals scavenging activity. The AChE inhibition potential of Rh. Sp and Rh. Fl were most prominent i.e., 81.67 ± 0.88 and 91.62 ± 1.67 at highest concentration with IC50 135 and 20 μg/mL respectively. All the subsequent fractions exhibited moderate to high AChE inhibition i.e., Rh. Cr, Rh. Hex, Rh. Chf, Rh. EtAc and Rh. Aq showed IC50 218, 1420, 75, 115 and 1210 μg/mL respectively. Similarly, against BChE various plant extracts i.e., Rh. Sp, Rh. Fl, Rh. Cr, Rh. Hex, Rh. Chf, Rh. EtAc and Rh. Aq resulted IC50 165, 175, 265, 890, 92, 115 and 220 μg/mL respectively. In DPPH free radical scavenging assay, Rh. Sp and Rh. Fl showed comparable results with the positive control i.e., 63.34 ± 0.98 and 76.93 ± 1.13% scavenging at 1 mg/mL concentration (IC50 312 and 104 μg/mL) respectively. The percent ABTS radical scavenging potential exhibited by Rh. Sp and Rh. Fl (1000 μg/mL) were 82.58 ± 0.52 and 88.25 ± 0.67 with IC50 18 and 9 μg/mL respectively. Similarly in H2O2 scavenging assay, the Rh. Sp and Rh. Fl exhibited IC50 175 and 275 μg/mL respectively. The strong anticholinesterase and antioxidant activities of Rh. Sp, Rh. Fl and various fractions of R. hastatus support the purported ethnomedicinal uses and recommend R. hastatus as a possible remedy for the treatment of AD and neurodegenerative disorders.

Comparative pharmacodynamics of the new fluoroquinolone ABT492 and levofloxacin with Streptococcus pneumoniae in an in vitro dynamic model.

PubMed

Firsov, Alexander A; Alferova, Irene V; Smirnova, Maria V; Lubenko, Irene Yu; Portnoy, Yury A; Zinner, Stephen H

2005-05-01

The kinetics of killing of Streptococcus pneumoniae exposed to ABT492 or levofloxacin were compared. S. pneumoniae ATCC 49619 and four ciprofloxacin-resistant clinical isolates, S. pneumoniae 1149, 391, 79 and 804, were exposed to ABT492 and levofloxacin as a single dose in a dynamic model that simulates human pharmacokinetics of the quinolones. With S. pneumoniae ATCC 49619 eight-fold ranging AUC/MIC ratios (60-500 h) were simulated for each quinolone. In addition, two larger AUC/MICs, i.e., 1080 and 2150 h for ABT492 and 1460 and 3660 h for levofloxacin which correspond to 100 and 200 mg doses of ABT492 and 200 and 500 mg doses of levofloxacin, respectively, were mimicked. Each ciprofloxacin-resistant organism was exposed to the clinical doses of ABT492 (400 mg) and levofloxacin (500 mg); the respective AUC/MIC ratios were from 580 to 3470 h and from 28 to 110 h. At comparable AUC/MICs (from 60 to 500 h), regrowth of S. pneumoniae ATCC 49619 followed initial killing, and the times to regrowth were longer with levofloxacin than ABT492. However, no regrowth of S. pneumoniae ATCC 49619 occurred at the higher AUC/MICs of ABT492 (1080 and 2150 h) and levofloxacin (1460 and 3660 h). Killing of S. pneumoniae 1149, 391 and 79 without bacterial regrowth, was provided by ABT492 (AUC/MIC 3470, 2310 and 1160 h, respectively) but not levofloxacin (AUC/MIC 55, 110 and 28 h, respectively). Regrowth of S. pneumoniae 804 was observed with both ABT492 and levofloxacin (AUC/MIC 580 and 55 h, respectively). Areas between the control growth curve and the time-kill curve (ABBCs) for ABT492 against S. pneumoniae 1149, 391 and 79 were 2.6-4.2 times larger than the respective ABBCs for levofloxacin, whereas similar ABBCs were found with S. pneumoniae 804 exposed to both quinolones. These findings predict significantly greater efficacy of ABT492 than levofloxacin at clinically achievable AUC/MIC ratios against ciprofloxacin-resistant S. pneumoniae and similar efficacies of the two quinolones against susceptible organisms.

Molecular and biochemical characterization of a highly stable bacterial laccase that occurs as a structural component of the Bacillus subtilis endospore coat.

PubMed

Martins, Ligia O; Soares, Claudio M; Pereira, Manuela M; Teixeira, Miguel; Costa, Teresa; Jones, George H; Henriques, Adriano O

2002-05-24

The Bacillus subtilis endospore coat protein CotA shows laccase activity. By using comparative modeling techniques, we were able to derive a model for CotA based on the known x-ray structures of zucchini ascorbate oxidase and Cuprinus cereneus laccase. This model of CotA contains all the structural features of a laccase, including the reactive surface-exposed copper center (T1) and two buried copper centers (T2 and T3). Single amino acid substitutions in the CotA T1 copper center (H497A, or M502L) did not prevent assembly of the mutant proteins into the coat and did not alter the pattern of extractable coat polypeptides. However, in contrast to a wild type strain, both mutants produced unpigmented colonies and spores unable to oxidize syringaldazine (SGZ) and 2'2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). The CotA protein was purified to homogeneity from an overproducing Escherichia coli strain. The purified CotA shows an absorbance and a EPR spectra typical of blue multicopper oxidases. Optimal enzymatic activity was found at < or =pH 3.0 and at pH 7.0 for ABTS or SGZ oxidation, respectively. The apparent K(m) values for ABTS and SGZ at 37 degrees C were of 106 +/- 11 and 26 +/- 2 microm, respectively, with corresponding k(cat) values of 16.8 +/- 0.8 and 3.7 +/- 0.1 s(-1). Maximal enzyme activity was observed at 75 degrees C with ABTS as substrate. Remarkably, the coat-associated or the purified enzyme showed a half-life of inactivation at 80 degrees C of about 4 and 2 h, respectively, indicating that CotA is intrinsically highly thermostable.

Activation of α4β2*/α6β2* nicotinic receptors alleviates anxiety during nicotine withdrawal without upregulating nicotinic receptors.

PubMed

Yohn, Nicole L; Turner, Jill R; Blendy, Julie A

2014-05-01

Although nicotine mediates its effects through several nicotinic acetylcholine receptor (nAChR) subtypes, it remains to be determined which nAChR subtypes directly mediate heightened anxiety during withdrawal. Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Therefore, it is hypothesized that success can be found by the repurposing of other nAChR partial agonists for cessation therapies that target anxiety. It is noteworthy that the selective partial agonists for α4β2, ABT-089 [2-methyl-3-[2(S)-pyrrolidinylmethoxy]pyridine], and α7, ABT-107 [5-(6-[(3R)-1-azabicyclo[2.2.2]oct-3-yloxy] pyridazin-3-yl)-1H-indole] (AbbVie, North Chicago, IL), have not been evaluated as possible therapeutics for nicotine cessation. Therefore, we examined the effect of ABT-089 and ABT-107 on anxiety during withdrawal from nicotine in the novelty-induced hypophagia (NIH) paradigm. We found that short-term administration of ABT-089 and ABT-107 alleviate anxiety-like behavior during withdrawal from nicotine while long-term administration of ABT-089 but not ABT-107 reduces anxiety-like behavior during withdrawal. After behavioral testing, brains were harvested and β2-containing nAChRs were measured using [(3)H]epibaditine. ABT-089 and ABT-107 do not upregulate nAChRs, which is in contrast to the upregulation of nAChRs observed after nicotine. Furthermore, ABT-089 is anxiogenic in nicotine naive animals, suggesting that the effects on anxiety are specifically related to the nicotine-dependent state. Together, these studies identify additional nAChR partial agonists that may aid in the rational development of smoking cessation aids.

Safety, tolerability and pharmacokinetics of the histamine H3 receptor antagonist, ABT-288, in healthy young adults and elderly volunteers

PubMed Central

Othman, Ahmed A; Haig, George; Florian, Hana; Locke, Charles; Zhang, Jun; Dutta, Sandeep

2013-01-01

Aim The objective of this work was to characterize the safety, tolerability and pharmacokinetics of ABT-288, a highly selective histamine H3 receptor antagonist, in healthy young adults and elderly subjects following single and multiple dosing in a phase 1 setting. Methods Single doses (0.1, 0.3, 1, 3, 10, 20 and 40 mg ABT-288) and multiple doses (0.5, 1.5, 3 and 6 mg ABT-288 once-daily for 14 days) were evaluated in young adults and multiple doses (0.5, 1.5, 3 and 5 mg ABT-288 once-daily for 12 days) were evaluated in elderly subjects using randomized, double-blind, placebo-controlled, dose-escalating study designs. The effect of food on ABT-288 pharmacokinetics (5 mg single dose) was evaluated using an open label, randomized, crossover design. Results ABT-288 safety, tolerability and pharmacokinetics were comparable in young and elderly subjects. Single doses up to 40 mg and multiple doses up to 3 mg once-daily were generally safe and well tolerated. The most frequently reported adverse events were hot flush, headache, abnormal dreams, insomnia, nausea and dizziness. ABT-288 exposure (AUC) was dose-proportional over the evaluated dose ranges. The mean elimination half-life ranged from 40 to 61 h across dose groups. Steady state was achieved by day 10 of once-daily dosing with 3.4- to 4.2-fold accumulation. Food did not have a clinically meaningful effect on ABT-288 exposure. Conclusions Based on the above results, 1 and 3 mg once-daily doses of ABT-288 were advanced to phase 2 evaluation in Alzheimer's patients. PMID:23016924

Safety, tolerability and pharmacokinetics of the histamine H3 receptor antagonist, ABT-288, in healthy young adults and elderly volunteers.

PubMed

Othman, Ahmed A; Haig, George; Florian, Hana; Locke, Charles; Zhang, Jun; Dutta, Sandeep

2013-05-01

The objective of this work was to characterize the safety, tolerability and pharmacokinetics of ABT-288, a highly selective histamine H3 receptor antagonist, in healthy young adults and elderly subjects following single and multiple dosing in a phase 1 setting. Single doses (0.1, 0.3, 1, 3, 10, 20 and 40 mg ABT-288) and multiple doses (0.5, 1.5, 3 and 6 mg ABT-288 once-daily for 14 days) were evaluated in young adults and multiple doses (0.5, 1.5, 3 and 5 mg ABT-288 once-daily for 12 days) were evaluated in elderly subjects using randomized, double-blind, placebo-controlled, dose-escalating study designs. The effect of food on ABT-288 pharmacokinetics (5 mg single dose) was evaluated using an open label, randomized, crossover design. ABT-288 safety, tolerability and pharmacokinetics were comparable in young and elderly subjects. Single doses up to 40 mg and multiple doses up to 3 mg once-daily were generally safe and well tolerated. The most frequently reported adverse events were hot flush, headache, abnormal dreams, insomnia, nausea and dizziness. ABT-288 exposure (AUC) was dose-proportional over the evaluated dose ranges. The mean elimination half-life ranged from 40 to 61 h across dose groups. Steady state was achieved by day 10 of once-daily dosing with 3.4- to 4.2-fold accumulation. Food did not have a clinically meaningful effect on ABT-288 exposure. Based on the above results, 1 and 3 mg once-daily doses of ABT-288 were advanced to phase 2 evaluation in Alzheimer's patients. © 2012 Abbott Laboratories. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.

ABT-510 induces tumor cell apoptosis and inhibits ovarian tumor growth in an orthotopic, syngeneic model of epithelial ovarian cancer

PubMed Central

Greenaway, James; Henkin, Jack; Lawler, Jack; Moorehead, Roger; Petrik, Jim

2012-01-01

Epithelial ovarian cancer (EOC) is the fifth most common cancer in women and is characterized by a low 5-year survival rate. One strategy that can potentially improve the overall survival rate in ovarian cancer is the use of antitumor agents such as ABT-510. ABT-510 is a small mimetic peptide of the naturally occurring antiangiogenic compound thrombospondin-1 and has been shown to significantly reduce tumor growth and burden in preclinical mouse models and in naturally occurring tumors in dogs. This is the first evaluation of ABT-510 in a preclinical model of human EOC. Tumorigenic mouse surface epithelial cells were injected into the bursa of C57BL/6 mice that were treated with either 100 mg/kg ABT-510 or an equivalent amount of PBS. ABT-510 caused a significant reduction in tumor size, ascites fluid volume, and secondary lesion dissemination when compared with PBS controls. Analysis of the vasculature of ABT-510-treated mice revealed vascular remodeling with smaller diameter vessels and lower overall area, increased number of mature vessels, and decreased tissue hypoxia. Tumors of ABT-510-treated mice had a significantly higher proportion of apoptotic tumor cells compared with the PBS-treated controls. Immunoblot analysis of cell lysates revealed a reduction in vascular endothelial growth factor, vascular endothelial growth factor receptor-2, and proliferating cell nuclear antigen protein expression as well as expression of members of the phosphatidylinositol 3-kinase and mitogen-activated protein kinase survival pathways. In vitro, ABT-510 induced tumor cell apoptosis in mouse and human ovarian cancer cells. This study shows ABT-510 as a promising candidate for inhibiting tumor growth and ascites formation in human EOC. PMID:19139114

Preclinical evaluation of antiangiogenic thrombospondin-1 peptide mimetics, ABT-526 and ABT-510, in companion dogs with naturally occurring cancers.

PubMed

Rusk, Anthony; McKeegan, Evelyn; Haviv, Fortuna; Majest, Sandra; Henkin, Jack; Khanna, Chand

2006-12-15

The angiogenic phenotype of malignant cancers has been established as a target for cancer therapy. ABT-526 and ABT-510, two peptide mimetics of thrombospondin-1 (TSP-1), block angiogenesis in vitro and in vivo and slow tumor growth in mice. To guide the clinical development of these drugs, translational studies in dogs with naturally occurring cancers were initiated. A prospective open-label trial using ABT-510 or ABT-526 in pet dogs with measurable malignant spontaneously arising tumors. Endpoints included safety, pharmacokinetics, antitumor activity, and preliminary assessment of changes in circulating endothelial cell populations. Two-hundred and forty-two dogs were sequentially entered to this open-label trial. The elimination half-life for ABT-510 and ABT-526 was 0.7 and 0.8 h, respectively (range, 0.5-1 h). No dose-limiting toxicities were seen in any dogs (N = 242). Forty-two dogs receiving peptide had objective responses (>50% reduction in tumor size; n = 6) or significant disease stabilization. Most objective responses were seen after 60 days of exposure to the TSP-1 peptide. Antitumor activity was similar for both peptides and was seen in several histologies, including mammary carcinoma, head and neck carcinoma, soft tissue sarcoma, cutaneous T-cell lymphoma, and non-Hodgkin's lymphoma. Assessment of circulating endothelial cell populations in a small subset of dogs suggested that effective exposure to TSP-1 peptides may be associated with reductions in circulating endothelial cells. These results support the safety and activity of ABT-526 and ABT-510 in dogs with naturally occurring malignant cancers. Data from this preclinical trial support the development of TSP-1 mimetic peptides as anticancer agents.

ABT-510 induces tumor cell apoptosis and inhibits ovarian tumor growth in an orthotopic, syngeneic model of epithelial ovarian cancer.

PubMed

Greenaway, James; Henkin, Jack; Lawler, Jack; Moorehead, Roger; Petrik, Jim

2009-01-01

Epithelial ovarian cancer (EOC) is the fifth most common cancer in women and is characterized by a low 5-year survival rate. One strategy that can potentially improve the overall survival rate in ovarian cancer is the use of antitumor agents such as ABT-510. ABT-510 is a small mimetic peptide of the naturally occurring antiangiogenic compound thrombospondin-1 and has been shown to significantly reduce tumor growth and burden in preclinical mouse models and in naturally occurring tumors in dogs. This is the first evaluation of ABT-510 in a preclinical model of human EOC. Tumorigenic mouse surface epithelial cells were injected into the bursa of C57BL/6 mice that were treated with either 100 mg/kg ABT-510 or an equivalent amount of PBS. ABT-510 caused a significant reduction in tumor size, ascites fluid volume, and secondary lesion dissemination when compared with PBS controls. Analysis of the vasculature of ABT-510-treated mice revealed vascular remodeling with smaller diameter vessels and lower overall area, increased number of mature vessels, and decreased tissue hypoxia. Tumors of ABT-510-treated mice had a significantly higher proportion of apoptotic tumor cells compared with the PBS-treated controls. Immunoblot analysis of cell lysates revealed a reduction in vascular endothelial growth factor, vascular endothelial growth factor receptor-2, and proliferating cell nuclear antigen protein expression as well as expression of members of the phosphatidylinositol 3-kinase and mitogen-activated protein kinase survival pathways. In vitro, ABT-510 induced tumor cell apoptosis in mouse and human ovarian cancer cells. This study shows ABT-510 as a promising candidate for inhibiting tumor growth and ascites formation in human EOC.

Concomitant methotrexate and tacrolimus augment the clinical response to abatacept in patients with rheumatoid arthritis with a prior history of biological DMARD use.

PubMed

Takahashi, Nobunori; Fujibayashi, Takayoshi; Kida, Daihei; Hirano, Yuji; Kato, Takefumi; Kato, Daizo; Saito, Kiwamu; Kaneko, Atsushi; Yabe, Yuichiro; Takagi, Hideki; Oguchi, Takeshi; Miyake, Hiroyuki; Watanabe, Tsuyoshi; Hayashi, Masatoshi; Kanayama, Yasuhide; Funahashi, Koji; Hanabayashi, Masahiro; Hirabara, Shinya; Asai, Shuji; Takemoto, Toki; Terabe, Kenya; Asai, Nobuyuki; Yoshioka, Yutaka; Ishiguro, Naoki; Kojima, Toshihisa

2015-10-01

This observational retrospective study examined whether abatacept efficacy could be augmented with concomitant methotrexate (MTX) or tacrolimus (TAC) in patients with rheumatoid arthritis (RA) who experienced failure with prior biological disease-modifying antirheumatic drugs (DMARDs) and in whom favorable therapeutic efficacy is difficult to achieve. All patients with a prior biological DMARD history who were treated with abatacept for 52 weeks and registered in a Japanese multicentre registry were included. Clinical efficacy and safety of abatacept according to the concomitant drug used, i.e., none (ABT-mono), MTX (ABT-MTX), and TAC (ABT-TAC), were compared. A greater mean percent change of DAS28-ESR was observed in the ABT-TAC group compared with the ABT-mono group at weeks 12 (-20.5 vs. -5.4 %, p = 0.035) and 24 (-25.0 vs. -11.0 %, p = 0.036). ABT-MTX and ABT-TAC groups had a significantly higher proportion of patients who achieved low disease activity (LDA) within 52 weeks compared with the respective baselines, while no significant change was observed in the ABT-mono group. A higher proportion of patients in the ABT-TAC group achieved EULAR moderate response compared with the ABT-mono group at week 52 (66.7 vs. 35.0 %, p = 0.025). Multivariate logistic regression analysis revealed that concomitant TAC use was independently associated with the achievement of LDA and EULAR response at 52 weeks, while concomitant MTX use was not. Concomitant TAC use may offer a suitable option for RA patients treated with abatacept after prior biological DMARD failure, likely because both abatacept and TAC affect T cell activation.

The IGF-1 receptor inhibitor picropodophyllin potentiates the anti-myeloma activity of a BH3-mimetic

PubMed Central

Bieghs, Liesbeth; Lub, Susanne; Fostier, Karel; Maes, Ken; Van Valckenborgh, Els; Menu, Eline; Johnsen, Hans E.; Overgaard, Michael T.; Larsson, Olle; Axelson, Magnus; Nyegaard, Mette; Schots, Rik; Jernberg-Wiklund, Helena

2014-01-01

The ABT-analogous 737, 263 and 199 are BH3 mimetics showing potent anti-myeloma (MM) activity, but only on defined molecular subgroups of MM patients presenting a Bcl-2high/Mcl-1low profile. IGF-1 is a major survival factor in MM regulating the expression of Bcl-2 proteins and might therefore be a resistance factor to these ABT-analogous. We first show that IGF-1 protected human MM cell lines (HMCLs) against ABT-737. Concurrently, the IGF-1 receptor inhibitor picropodophyllin (PPP) synergistically sensitized HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. Knockdown of Bcl-2 by shRNA protected MM cells to ABT-737, while Mcl-1 shRNA sensitized the cells. PPP overcame the Bcl-2 dependency of ABT-737, but failed to completely overcome the protective effect of Mcl-1. In vivo, co-treatment of 5T33MM bearing mice significantly decreased tumor burden and prolonged overall survival both in a prophylactic and therapeutic setting. Interestingly, proteasome inhibitor resistant CD138− 5T33MM cells were more sensitive to ABT-737, whereas PPP alone targeted the CD138+ cells more effectively. After co-treatment, both subpopulations were targeted equally. Together, the combination of an IGF-1R inhibitor and an ABT-analogue displays synergistic anti-myeloma activity providing the rational for further (pre)clinical testing. PMID:25008202

Inhibition of Mcl-1 enhances cell death induced by the Bcl-2-selective inhibitor ABT-199 in acute myeloid leukemia cells.

PubMed

Luedtke, Daniel A; Niu, Xiaojia; Pan, Yihang; Zhao, Jianyun; Liu, Shuang; Edwards, Holly; Chen, Kang; Lin, Hai; Taub, Jeffrey W; Ge, Yubin

2017-01-01

Acute myeloid leukemia (AML) is a serious disease. The 5-year survival rates remain frustratingly low (65% for children and 26% for adults). Resistance to frontline chemotherapy (usually cytarabine) often develops; therefore a new treatment modality is needed. Bcl-2 family proteins play an important role in balancing cell survival and apoptosis. The antiapoptotic Bcl-2 family proteins have been found to be dysregulated in AML. ABT-199, a BH3 mimetic, was developed to target antiapoptotic protein Bcl-2. Although ABT-199 has demonstrated promising results, resistance occurs. Previous studies in AML show that ABT-199 alone decreases the association of proapoptotic protein Bim with Bcl-2, but this is compensated by increased association of Bim with prosurvival protein Mcl-1, stabilizing Mcl-1, resulting in resistance to ABT-199. In this study, we investigated the antileukemic activity of the Mcl-1-selective inhibitor A-1210477 in combination with ABT-199 in AML cells. We found that A-1210477 synergistically induced apoptosis with ABT-199 in AML cell lines and primary patient samples. The synergistic induction of apoptosis was decreased upon Bak, Bax and Bim knockdown. While A-1210477 treatment alone also increased Mcl-1 protein levels, combination with ABT-199 reduced binding of Bim to Mcl-1. Our results demonstrate that sequestration of Bim by Mcl-1, a mechanism of ABT-199 resistance, can be abrogated by combined treatment with the Mcl-1 inhibitor A-1201477.

Topical Formulation Containing Naringenin: Efficacy against Ultraviolet B Irradiation-Induced Skin Inflammation and Oxidative Stress in Mice

PubMed Central

Martinez, Renata M.; Pinho-Ribeiro, Felipe A.; Steffen, Vinicius S.; Silva, Thais C. C.; Caviglione, Carla V.; Bottura, Carolina; Fonseca, Maria J. V.; Vicentini, Fabiana T. M. C.; Vignoli, Josiane A.; Baracat, Marcela M.; Georgetti, Sandra R.; Verri, Waldiceu A.; Casagrande, Rubia

2016-01-01

Naringenin (NGN) exhibits anti-inflammatory and antioxidant activities, but it remains undetermined its topical actions against ultraviolet B (UVB)-induced inflammation and oxidative stress in vivo. The purpose of this study was to evaluate the physicochemical and functional antioxidant stability of NGN containing formulations, and the effects of selected NGN containing formulation on UVB irradiation-induced skin inflammation and oxidative damage in hairless mice. NGN presented ferric reducing power, ability to scavenge 2,2′-azinobis (3-ethylbenzothiazoline- 6-sulfonic acid) (ABTS) and hydroxyl radical, and inhibited iron-independent and dependent lipid peroxidation. Among the three formulations containing NGN, only the F3 kept its physicochemical and functional stability over 180 days. Topical application of F3 in mice protected from UVB-induced skin damage by inhibiting edema and cytokine production (TNF-α, IL-1β, IL-6, and IL-10). Furthermore, F3 inhibited superoxide anion and lipid hydroperoxides production and maintained ferric reducing and ABTS scavenging abilities, catalase activity, and reduced glutathione levels. In addition, F3 maintained mRNA expression of cellular antioxidants glutathione peroxidase 1, glutathione reductase and transcription factor Nrf2 (nuclear factor erythroid 2-related factor 2), and induced mRNA expression of heme oxygenase-1. In conclusion, a formulation containing NGN may be a promising approach to protecting the skin from the deleterious effects of UVB irradiation. PMID:26741806

Antioxidant, antiproliferative and antimicrobial activities of the volatile oil from the wild pepper Piper capense used in Cameroon as a culinary spice.

PubMed

Woguem, Verlaine; Maggi, Filippo; Fogang, Hervet P D; Tapondjoua, Léon A; Womeni, Hilaire M; Luana, Quassinti; Bramuccic, Massimo; Vitali, Luca A; Petrelli, Dezemona; Lupidi, Giulio; Papa, Fabrizio; Vittori, Sauro; Barboni, Luciano

2013-12-01

Wild pepper (Piper capense L.f., Piperaceae) is a spice traditionally used in western Cameroon to make soups called 'Nkui' and 'Nah poh'. In the present work, the essential oil hydrodistilled from fruits was analyzed by GC-FID and GC-MS, and for in vitro biological activities, namely cytotoxic, antioxidant and antimicrobial, by MTT, DPPH, ABTS and agar disc diffusion methods. The oil composition was dominated by monoterpene hydrocarbons (56.5%) responsible for the pepper odor, such as (beta-pinene (33.2%), sabinene (10.0%) and alpha-pinene (8.9%). The oil induced a concentration-dependent inhibitory effect on human tumor cells MDA-MB 231 (breast adenocarcinoma), A375 (malignant melanoma) and HCT116 (colon carcinoma), showing IC50 values of 26.3, 76.0 and 22.7 microg/ml, respectively. The oil showed total antioxidant activity with a Trolox equivalent antioxidant concentration (TEAC) value of 140 micromol/g. The essential oil of P. capense proved to be an effective scavenger of the ABTS+ radical, with an activity only about 30 times lower than that of Trolox. Moderate activity was observed against the Gram-positive species Staphylococcos aureus and Enterococcusfaecalis, and the yeast Candida albicans. The notable inhibition of some human tumor cells is worthy of further investigation to discover the possible mechanisms of action responsible for the observed cytotoxic effect of this essential oil.

Flavonoid and Antioxidant Capacity of Propolis Prediction Using Near Infrared Spectroscopy.

PubMed

Betances-Salcedo, Eddy; Revilla, Isabel; Vivar-Quintana, Ana M; González-Martín, M Inmaculada

2017-07-18

The use of propolis as a dietary supplement or as an ingredient in different food products is increasing, due to its antioxidant and bactericidal properties. These nutritional properties directly depend on its phenolic composition. For this reason, this study analysed the total contents of flavones and flavonols, flavanones and dihydroflavonols, and the antioxidant capacity by using the methods of ABTS and linoleic acid/ β -carotene in 99 samples of propolis from Spain and Chile. A rapid method was developed for quantifying these parameters in raw propolis using near infrared (NIR) spectroscopy with a remote reflectance fibre-optic probe applied directly to the ground-up sample. The models developed allow for the determination of the total flavones and flavonols (0-183 mg quercetin/g propolis and 0-72 mg rutin/g propolis), of the total flavanones and dihydroflavonols (9-109 mg pinocembrin/g propolis extract), and of its antioxidant capacity by the ABTS method based on the reduction of the 2.2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation(0-3212.6 nmol Trolox/mg of propolis) and of linoleic acid/ β -carotene (22-86% inhibition). The NIR spectroscopy models were applied in external validation to different samples of the calibration group, which led to the conclusion that the methods developed provide significantly identical data to the initial chemical data of reference.

Label-free colorimetric sensor for sensitive detection of choline based on DNAzyme-choline oxidase coupling.

PubMed

Nikzad, Nasrin; Karami, Zahra

2018-04-14

Changes in choline levels can be associated with diseases such as Alzheimer, Parkinson, Huntington, fatty liver, interstitial lung abnormalities, autism and so on. Therefore, quantitative determination of choline is important in the biological and clinical analysis. So far, several methods have been investigated for measuring choline in the body fluids, each of which has disadvantages such as the need for specialist ability, complexity, and high cost. For this purpose, a facile and sensitive colorimetric biosensor based on DNAzyme-choline oxidase coupling used for the determination of choline. In this method, the first, choline oxidase produces H 2 O 2 and betaine in the presence of choline and oxygen, then, the DNAzyme converts colorless ABTS into green ABTS + radicals. Compared to the previous methods, the linear range and the limit of detection of this talented biosensor were 0.1-25 μM and 22 nM. Choline measurement using this biosensor has shown satisfactory selectivity and repeatability. Its recovery was 96.9-103.7%, which shows the reliability of biosensor assay in biological samples. Simplicity, low cost, naked eye, high sensitivity, and precision are the benefits of this biosensor. Taken to gather, the proposed system can be considered as a great biosensor for measuring choline levels especially in point of care diagnostic. Copyright © 2018 Elsevier B.V. All rights reserved.

Antioxidant and chelating capacity of Maillard reaction products in amino acid-sugar model systems: applications for food processing.

PubMed

Mondaca-Navarro, Blanca A; Ávila-Villa, Luz A; González-Córdova, Aarón F; López-Cervantes, Jaime; Sánchez-Machado, Dalia I; Campas-Baypoli, Olga N; Rodríguez-Ramírez, Roberto

2017-08-01

Maillard reaction products (MRP) have gained increasing interest owing to their both positive and negative effects on human health. Aqueous amino acid-sugar model systems were studied in order to evaluate the antioxidant and chelating activity of MRP under conditions similar to those of food processing. Amino acids (cysteine, glycine, isoleucine and lysine) combined with different sugars (fructose or glucose) were heated to 100 and 130 °C for 30, 60 and 90 min. Antioxidant capacity was evaluated via ABTS and DPPH free radical scavenging assays, in addition to Fe 2+ and Cu 2+ ion chelating capacity. In the ABTS assay, the cysteine-fructose model system presented the highest antioxidant activity at 7.05 µmol mL -1 (130 °C, 60 min), expressed in Trolox equivalents. In the DPPH assay, the cysteine-glucose system presented the highest antioxidant activity at 3.79 µmol mL -1 (100 °C, 90 min). The maximum rate of chelation of Fe 2+ and Cu 2+ was 96.31 and 59.44% respectively in the lysine-fructose and cysteine-glucose systems (100 °C, 30 min). The model systems presented antioxidant and chelating activity under the analyzed temperatures and heating times, which are similar to the processing conditions of some foods. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Chemical Composition, Antioxidant and Antimicrobial Activities of Thymus capitata Essential Oil with Its Preservative Effect against Listeria monocytogenes Inoculated in Minced Beef Meat

PubMed Central

El Abed, Nariman; Kaabi, Belhassen; Smaali, Mohamed Issam; Chabbouh, Meriem; Habibi, Kamel; Mejri, Mondher; Marzouki, Mohamed Nejib; Ben Hadj Ahmed, Sami

2014-01-01

The chemical composition, antioxidant and antimicrobial activities, and the preservative effect of Thymus capitata essential oil against Listeria monocytogenes inoculated in minced beef meat were evaluated. The essential oil extracted was chemically analyzed by gas chromatography-mass spectrometry. Nineteen components were identified, of which carvacrol represented (88.89%) of the oil. The antioxidant activity was assessed in vitro by using both the DPPH and the ABTS assays. The findings showed that the essential oil exhibited high antioxidant activity, which was comparable to the reference standards (BHT and ascorbic acid) with IC50 values of 44.16 and 0.463 μg/mL determined by the free-radical scavenging DPPH and ABTS assays, respectively. Furthermore, the essential oil was evaluated for its antimicrobial activity using disc agar diffusion and microdilution methods. The results demonstrated that the zone of inhibition varied from moderate to strong (15–80 mm) and the minimum inhibition concentration values ranged from 0.32 to 20 mg/mL. In addition, essential oil evaluated in vivo against Listeria monocytogenes showed clear and strong inhibitory effect. The application of 0.25 or 1% (v/w) essential oil of T. capitata to minced beef significantly reduced the L. monocytogenes population when compared to those of control samples (P-value  <0.01). PMID:24719640

Properties of Flavonoids Isolated from the Bark of Eysenhardtia polystachya and Their Effect on Oxidative Stress in Streptozotocin-Induced Diabetes Mellitus in Mice.

PubMed

Perez-Gutierrez, Rosa Martha; Garcia-Campoy, Abraham Heriberto; Muñiz-Ramirez, Alethia

Six new flavonoids 2',4'-dihydroxychalcone-6'-O- β -d-glucopyranoside ( 1 ), α ,3,2',4'-tetrahydroxy-4-methoxy-dihydrochalcone-3'-C- β -glucopyranosy-6'-O- β -d-glucopyranoside ( 2 ), 7-hydroxy-5,8'-dimethoxy-6' α -l-rhamnopyranosyl-8-(3-phenyl-trans-acryloyl)-1-benzopyran-2-one ( 3 ), 6'7-dihydroxy-5,8-dimethoxy-8(3-phenyl-trans-acryloyl)-1-benzopyran-2-one ( 4 ), 9-hydroxy-3,8-dimethoxy-4-prenylpterocarpan ( 5 ), and α ,4,4'-trihydroxydihydrochalcone-2'-O- β -d-glucopyranoside ( 6 ) were isolated from bark of Eysenhardtia polystachya. Antidiabetic activity of compounds 1 - 5 in terms of their cellular antioxidant and free radical scavenging and also in streptozotocin- (STZ-) induced diabetic mice was evaluated on liver transaminases, lipid peroxidation, total bilirubin, total protein, superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (CSH-Px), and glutathione reductase (GSH). Results indicated that 1 - 5 scavenged 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl ( ∙ OH), nitric oxide radicals (NO ∙ ), superoxide anion radical (O 2 ∙- ), radical cation (ABTS ∙+ ), and hydrogen peroxide (H 2 O 2 ) radical, and protection against H 2 O 2 induced BSA damage was also observed. Furthermore, 1 - 5 showed ability to decrease the oxidative stress in H9c2 cell. Diabetic mice present high levels of lipid peroxide, total protein, SGPT, SGOT, ALP, and TB. However, treatment of STZ-induced diabetes in mice with 1 - 5 reduced levels of these enzymes leading to protector effect of liver. In addition, with treatment with 1 - 5 , increases in radical scavenging enzymes of CSH-Px, SOD, GSH, and CAT have also been observed in diabetic mice. The antioxidant properties of compounds 1 - 5 are a promising strategy for ameliorating therapeutic effects by avoiding disorders in the normal redox reactions in healthy cells which consequently could alleviate complications of diabetes.

Chemical Composition and Antioxidant and Antibacterial Activities of an Essential Oil Extracted from an Edible Seaweed, Laminaria japonica L.

PubMed

Patra, Jayanta Kumar; Das, Gitishree; Baek, Kwang-Hyun

2015-07-02

Laminaria japonica L. is among the most commonly consumed seaweeds in northeast Asia. In the present study, L. japonica essential oil (LJEO) was extracted by microwave-hydrodistillation and analyzed by gas chromatography and mass spectroscopy. LJEO contained 21 volatile compounds, comprising 99.76% of the total volume of the essential oil, primarily tetradeconoic acid (51.75%), hexadecanoic acid (16.57%), (9Z,12Z)-9,12-Octadecadienoic acid (12.09%), and (9Z)-hexadec-9-enoic acid (9.25%). Evaluation of the antibacterial potential against three foodborne pathogens, Bacillus cereus ATCC 10876, Escherichia coli O157:H7 ATCC 43890, and Staphylococcus aureus ATCC 49444, revealed that LJEO at a concentration of 25 mg/paper disc exerted high antibacterial activity against S. aureus (11.5 ± 0.58 mm inhibition zone) and B. cereus (10.5 ± 0.57 mm inhibition zone), but no inhibition of E. coli O157:H7. LJEO also displayed DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging activity (80.45%), superoxide anion scavenging activity (54.03%), and ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical and hydroxyl radical scavenging at 500 µg/mL. Finally, LJEO showed high inhibition of lipid peroxidation with strong reducing power. In conclusion, LJEO from edible seaweed is an inexpensive but favorable resource with strong antibacterial capacity as well as free radical scavenging and antioxidant activity; therefore, it has the potential for use in the food, cosmetics, and pharmaceutical industries.

Enzyme-Assisted Extraction Optimization, Characterization and Antioxidant Activity of Polysaccharides from Sea Cucumber Phyllophorus proteus.

PubMed

Qin, Yujing; Yuan, Qingxia; Zhang, Yuexing; Li, Jialu; Zhu, Xinjiao; Zhao, Lingling; Wen, Jing; Liu, Jikai; Zhao, Longyan; Zhao, Jinhua

2018-03-06

Enzyme-assisted extraction optimization, characterization and in vitro antioxidant activity of polysaccharides from sea cucumber Phyllophorus proteus (PPP) were investigated in the present study. The optimal extraction conditions with a yield of 6.44 ± 0.06% for PPP were determined as follows: Extraction time of 2.89 h, ratio of extraction solvent to raw material of 16.26 mL/g, extraction pH of 6.83, exraction temperature of 50 °C and papain concentration of 0.15%. Three purified fractions, PPP-1a, PPP-1b and PPP-2 with molecular weights of 369.60, 41.73 and 57.76 kDa, respectively, were obtained from PPP by chromatography of FPA98Cl and Sepharose CL-6B columns. Analysis of monosaccharide compositions showed that PPP-1a consisted of N -acetyl-galactosamine (GalNAc), galactose (Gal) and fucose (Fuc), PPP-1b of Fuc as the only monosaccharide and PPP-2 of glucuronic acid, GalNAc and Fuc. Sulfate contents of PPP, PPP-1a, PPP-1b and PPP-2 were determined to be 21.9%, 20.6%, 25.2% and 28.0% ( w / w ), respectively. PPP and PPP-1a had higher molecular weight and intrinsic viscosity than those of the PPP-1b and PPP-2. PPP, PPP-1a, PPP-1b and PPP-2 exhibited obvious activities of scavenging 1,1-diphenyl-2-picrylhydrazyl radical, hydroxyl radical, superoxide radical and ABTS radical in different extent, which suggested that the polysaccharides from Phyllophorus proteus may be novel agents having potential value for antioxidation.

Screening and identification of antioxidants in biological samples using high-performance liquid chromatography-mass spectrometry and its application on Salacca edulis Reinw.

PubMed

Shui, Guanghou; Leong, Lai Peng

2005-02-23

In this study, a new approach was developed for screening and identifying antioxidants in biological samples. The approach was based on significant decreases of the intensities of ion peaks obtained from high-performance liquid chromatography (HPLC) coupled with mass spectrometry (MS) upon reaction with 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals. HPLC-MS/MS was further applied to elucidate structures of antioxidant peaks characterized in a spiking test. The new approach could also be used to monitor the reactivity of antioxidants in biological sample with free radicals. The approach was successfully applied to the identification of antioxidants in salak (Salacca edulis Reinw), a tropical fruit that is reported to be a very good source of natural antioxidants, but it was still not clear which compounds were responsible for its antioxidant property. The antioxidants in salak were identified to be chlorogenic acid, (-)-epicatechin, and singly linked proanthocyanidins that mainly existed as dimers through hexamers of catechin or epicatechin. In salak, chlorogenic acid was identified to be an antioxidant of the slow reaction type as it reacted with free radicals much more slowly than either (-)-epicatechin or proanthocyanidins. The new approach was proved to be useful for the characterization and identification of antioxidants in biological samples as a mass detector combined with an HPLC separation system not only serves as an ideal tool to monitor free radical active components but also provides their possible chemical structures in a biological sample.

Comparative in vitro susceptibilities and bactericidal activities of investigational fluoroquinolone ABT-492 and other antimicrobial agents against human mycoplasmas and ureaplasmas.

PubMed

Waites, Ken B; Crabb, Donna M; Duffy, Lynn B

2003-12-01

We determined in vitro susceptibilities for ABT-492 and other antimicrobials against Mycoplasma pneumoniae, Mycoplasma fermentans, Mycoplasma hominis, and Ureaplasma species. ABT-492 MICs were < or =1 microg/ml, and the agent was bactericidal against selected isolates of M. pneumoniae and M. hominis. ABT-492 has potential for treatment of infections due to these microorganisms.

In vitro and bactericidal activities of ABT-492, a novel fluoroquinolone, against Gram-positive and Gram-negative organisms.

PubMed

Almer, Laurel S; Hoffrage, Jennifer B; Keller, Erika L; Flamm, Robert K; Shortridge, Virginia D

2004-07-01

In vitro activities of ABT-492, ciprofloxacin, levofloxacin, trovafloxacin, moxifloxacin, gatifloxacin, and gemifloxacin were compared. ABT-492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms. Bactericidal activity of ABT-492 was also evaluated.

In vitro activity of ABT-492 against anaerobic bacteria.

PubMed

Sillerström, E; Wahlund, E; Nord, C E

2004-06-01

The purpose of the study was to determine the in vitro activity of ABT-492 compared with that of other antimicrobial agents against anaerobic bacteria. The activity of ABT-492 was investigated against 369 clinical isolates of anaerobic bacteria by the agar dilution method and was compared with that of moxifloxacin, piperacillin, cefoxitin, imipenem, clindamycin and metronidazole. ABT-492 and imipenem were the most active antimicrobial agents tested.

Comparative In Vitro Susceptibilities and Bactericidal Activities of Investigational Fluoroquinolone ABT-492 and Other Antimicrobial Agents against Human Mycoplasmas and Ureaplasmas

PubMed Central

Waites, Ken B.; Crabb, Donna M.; Duffy, Lynn B.

2003-01-01

We determined in vitro susceptibilities for ABT-492 and other antimicrobials against Mycoplasma pneumoniae, Mycoplasma fermentans, Mycoplasma hominis, and Ureaplasma species. ABT-492 MICs were ≤1 μg/ml, and the agent was bactericidal against selected isolates of M. pneumoniae and M. hominis. ABT-492 has potential for treatment of infections due to these microorganisms. PMID:14638513

Extraction optimization and influences of drying methods on antioxidant activities of polysaccharide from cup plant (Silphium perfoliatum L.)

PubMed Central

Li, Ran; Duan, Meng-Ying; Wu, Hong-Xin

2017-01-01

Response surface methodology (RSM) was used to investigate the extraction condition of polysaccharide from cup plant (Silphium perfoliatum L.) (named CPP). Water to raw material ratio (10–30 mL/g), extraction time (40–80 min) and extraction temperature (60–100°C) were set as the 3 independent variables, and their effects on the extraction yield of CPP were measured. In addition, the effects of drying methods including hot air drying (HD), vacuum drying (VD) and freeze drying (FD) on the antioxidant activities of CPP were evaluated. The results showed that the optimal condition to extract CPP was: water to raw material ratio (15 mL/g), extraction time (61 min), and extraction temperature (97°C), a maximum CPP yield of 6.49% was obtained under this condition. CPP drying with FD method showed stronger reducing power (0.943 at 6 mg/mL) and radical scavenging capacities against DPPH radical (75.71% at 1.2 mg/mL) and ABTS radical (98.06 at 1.6 mg/mL) than CPP drying with HD and VD methods. Therefore, freeze drying served as a good method for keeping the antioxidant activities of polysaccharide from cup plant. The polysaccharide from cup plant has potential to use as a natural antioxidant. PMID:28837625

Chemical Composition and Antioxidant Properties of Juniper Berry (Juniperus communis L.) Essential Oil. Action of the Essential Oil on the Antioxidant Protection of Saccharomyces cerevisiae Model Organism

PubMed Central

Höferl, Martina; Stoilova, Ivanka; Schmidt, Erich; Wanner, Jürgen; Jirovetz, Leopold; Trifonova, Dora; Krastev, Lutsian; Krastanov, Albert

2014-01-01

The essential oil of juniper berries (Juniperus communis L., Cupressaceae) is traditionally used for medicinal and flavoring purposes. As elucidated by gas chromatography/flame ionization detector (GC/FID) and gas chromatography/mass spectrometry (GC/MS methods), the juniper berry oil from Bulgaria is largely comprised of monoterpene hydrocarbons such as α-pinene (51.4%), myrcene (8.3%), sabinene (5.8%), limonene (5.1%) and β-pinene (5.0%). The antioxidant capacity of the essential oil was evaluated in vitro by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging, 2,2-azino-bis-3-ethylbenzothiazoline-6 sulfonic acid (ABTS) radical cation scavenging, hydroxyl radical (ОН•) scavenging and chelating capacity, superoxide radical (•O2−) scavenging and xanthine oxidase inhibitory effects, hydrogen peroxide scavenging. The antioxidant activity of the oil attributable to electron transfer made juniper berry essential oil a strong antioxidant, whereas the antioxidant activity attributable to hydrogen atom transfer was lower. Lipid peroxidation inhibition by the essential oil in both stages, i.e., hydroperoxide formation and malondialdehyde formation, was less efficient than the inhibition by butylated hydroxytoluene (BHT). In vivo studies confirmed these effects of the oil which created the possibility of blocking the oxidation processes in yeast cells by increasing activity of the antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). PMID:26784665

Chemical Composition and Antioxidant Properties of Juniper Berry (Juniperus communis L.) Essential Oil. Action of the Essential Oil on the Antioxidant Protection of Saccharomyces cerevisiae Model Organism.

PubMed

Höferl, Martina; Stoilova, Ivanka; Schmidt, Erich; Wanner, Jürgen; Jirovetz, Leopold; Trifonova, Dora; Krastev, Lutsian; Krastanov, Albert

2014-02-24

The essential oil of juniper berries (Juniperus communis L., Cupressaceae) is traditionally used for medicinal and flavoring purposes. As elucidated by gas chromatography/flame ionization detector (GC/FID) and gas chromatography/mass spectrometry (GC/MS methods), the juniper berry oil from Bulgaria is largely comprised of monoterpene hydrocarbons such as α-pinene (51.4%), myrcene (8.3%), sabinene (5.8%), limonene (5.1%) and β-pinene (5.0%). The antioxidant capacity of the essential oil was evaluated in vitro by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging, 2,2-azino-bis-3-ethylbenzothiazoline-6 sulfonic acid (ABTS) radical cation scavenging, hydroxyl radical (ОН(•)) scavenging and chelating capacity, superoxide radical ((•)O₂(-)) scavenging and xanthine oxidase inhibitory effects, hydrogen peroxide scavenging. The antioxidant activity of the oil attributable to electron transfer made juniper berry essential oil a strong antioxidant, whereas the antioxidant activity attributable to hydrogen atom transfer was lower. Lipid peroxidation inhibition by the essential oil in both stages, i.e., hydroperoxide formation and malondialdehyde formation, was less efficient than the inhibition by butylated hydroxytoluene (BHT). In vivo studies confirmed these effects of the oil which created the possibility of blocking the oxidation processes in yeast cells by increasing activity of the antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx).

Protective role of quercetin against copper(II)-induced oxidative stress: A spectroscopic, theoretical and DNA damage study.

PubMed

Jomova, Klaudia; Lawson, Michael; Drostinova, Lenka; Lauro, Peter; Poprac, Patrik; Brezova, Vlasta; Michalik, Martin; Lukes, Vladimir; Valko, Marian

2017-12-01

The radical scavenging and metal chelating properties of flavonoids indicate that they may play a protective role in diseases with perturbed metal homeostasis such as Alzheimer's disease. In this work we investigated the effect of the coordination of quercetin to copper(II) in view of the formation of ROS in Cu-catalyzed Fenton reaction. ABTS and DPPH assays confirmed that the copper(II)-quercetin complex exhibits a stronger radical scavenging activity than does quercetin alone. EPR spin trapping experiments have shown that chelation of quercetin to copper significantly suppressed the formation of hydroxyl radicals in the Cu(II)-Fenton reaction. DNA damage experiments revealed a protective effect for quercetin, but only at higher stoichiometric ratios of quercetin relative to copper. DNA protective effect of quercetin against ROS attack was described by two mechanisms. The first mechanism lies in suppressed formation of ROS due to the decreased catalytic action of copper in the Fenton reaction, as a consequence of its chelation and direct scavenging of ROS by free quercetin. Since the Cu-quercetin complex intercalates into DNA, the second mechanism was attributed to a suppressed intercalating ability of the Cu-quercetin complex due to the mildly intercalating free quercetin into DNA, thus creating a protective wall against stronger intercalators. Copyright © 2017 Elsevier Ltd. All rights reserved.

Antioxidant ability and mechanism of rhizoma Atractylodes macrocephala.

PubMed

Li, Xican; Lin, Jian; Han, Weijuan; Mai, Wenqiong; Wang, Li; Li, Qiang; Lin, Miaofang; Bai, Mingsong; Zhang, Lishan; Chen, Dongfeng

2012-11-13

Rhizoma Atractylodes macrocephala (AM) has been used in Traditional Chinese Medicine (TCM) for about 2,000 years. In the study, we firstly determined the antioxidant levels of five AM extracts by •OH-scavenging, •O2−-scavenging, Fe2+-chelating, Cu2+-chelating, DPPH·-scavenging, and ABTS+·-scavenging assays. After measurement of the chemical contents in five AM extracts, we quantitatively analyzed the correlations between antioxidant levels and chemical contents. It was observed that total phenolics and total flavonoids had significant positive correlations with antioxidant levels (R = 0.685 and 0.479, respectively). In contrast, total sugars and total saponins presented lower correlations with antioxidant levels (R=−0.272 and 0.244, respectively). It means that antioxidant activity of AM should be attributed to total phenolics (including phenolic acids and flavonoids), and not total sugars and total saponins. Further analysis indicated that phenolic acids exhibited higher R values with radical-scavenging assays (R=0.32–1.00), while flavonoids showed higher R values with metal-chelating assays (R=0.86 and 0.90). In conclusion, AM exerts its antioxidant effect through metal-chelating, and radical-scavenging which is via donating hydrogen atom and donating electron. Its metal-chelating may result from flavonoids, while its radical-scavenging can be attributed to phenolic acids, especially caffeic acid, ferulic acid, and protocatechuic acid.

Antioxidant Activity and Total Phenolic and Flavonoid Content of Various Solvent Extracts from In Vivo and In Vitro Grown Trifolium pratense L. (Red Clover)

PubMed Central

Mat Taha, Rosna; Banisalam, Behrooz

2015-01-01

In the present study the extracts of in vivo and in vitro grown plants as well as callus tissue of red clover were tested for their antioxidant activities, using different extraction solvent and different antioxidant assays. The total flavonoid and phenolic contents as well as extraction yield of the extracts were also investigated to determine their correlation with the antioxidant activity of the extracts. Among all the tested extracts the highest amounts of total phenolic and total flavonoids content were found in methanol extract of in vivo grown plants. The antioxidant activity of tested samples followed the order in vivo plant extract > callus extract > in vitro extract. The highest reducing power, 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging, and chelating power were found in methanol extracts of in vivo grown red clover, while the chloroform fraction of in vivo grown plants showed the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, superoxide anion radical scavenging and hydrogen peroxide scavenging compared to the other tested extracts. A significant correlation was found between the antioxidant activity of extracts and their total phenolic and total flavonoid content. According to the findings, the extract of in vitro culture of red clover especially the callus tissue possesses a comparable antioxidant activity to the in vivo cultured plants' extract. PMID:26064936

The PARP inhibitor ABT-888 potentiates dacarbazine-induced cell death in carcinoids.

PubMed

Somnay, Y; Lubner, S; Gill, H; Matsumura, J B; Chen, H

2016-10-01

Monoagent DNA-alkylating chemotherapies like dacarbazine are among a paucity of medical treatments for advanced carcinoid tumors, but are limited by host toxicity and intrinsic chemoresistance through the base excision repair (BER) pathway via poly (ADP-ribose) polymerase (PARP). Hence, inhibitors of PARP may potentiate DNA-damaging agents by blocking BER and DNA restoration. We show that the PARP inhibitor ABT-888 (Veliparib) enhances the cytotoxic effects of dacarbazine in carcinoids. Two human carcinoid cell lines (BON and H727) treated with a combination of ABT-888 and dacarbazine resulted in synergistic growth inhibition signified by combination indices <1 on the Chou-Talalay scale. ABT-888 administered prior to varying dacarbazine doses promoted the suppression of neuroendocrine biomarkers of malignancy, ASCL1 and chromogranin A, as shown by western analysis. Ataxia telangiectasia mitogen factor phosphorylation and p21 Waf1/Cip1 activation, indicative of DNA damage, were increased by ABT-888 when combined with dacarbazine treatment, suggesting BER pathway attenuation by ABT-888. PE Annexin V/7-AAD staining and sorting revealed a profound induction of apoptosis following combination treatment, which was further confirmed by increased PARP cleavage. These results demonstrate that ABT-888 synergizes dacarbazine treatment in carcinoids. Therefore, ABT-888 may help treat carcinoids unresponsive or refractory to mainstay therapies.

RNAi screening uncovers Dhx9 as a modifier of ABT-737 resistance in an Eμ-myc/Bcl-2 mouse model

PubMed Central

Mills, John R.; Malina, Abba; Lee, Teresa; Di Paola, Domenic; Larsson, Ola; Miething, Cornelius; Grosse, Frank; Tang, Hengli; Zannis-Hadjopoulos, Maria; Lowe, Scott W.

2013-01-01

ABT-737 is a promising chemotherapeutic agent that promotes apoptosis by acting as a selective BH3 mimetic to neutralize Bcl-2–like family members. One shortcoming with its use is that Mcl-1, a member of the Bcl-2 family, is poorly inhibited by ABT-737 and thus is a major cause of resistance. We performed a short hairpin RNA (shRNA)-based drop-out screen to identify novel genes and pathways that could reverse resistance to ABT-737 treatment in Eµ-myc/Bcl-2 lymphoma cells engineered to rely on endogenous Mcl-1 for survival. Several drug-sensitive shRNAs were identified that were selectively depleted in the presence of ABT-737. Of these, 2 independent shRNAs targeting the RNA/DNA helicase Dhx9 were found to sensitize lymphomas to ABT-737 to an extent comparable to control Mcl-1 shRNAs. Although Dhx9 suppression sensitized both mouse and human cells to ABT-737 treatment, it did so without altering MCL-1 levels. Rather, loss of Dhx9 appeared to activate a p53-dependent apoptotic program, through aggravation of replicative stress, which was found to be both necessary and sufficient for the ABT-737–shDhx9 synthetic lethal relationship. PMID:23440244

ABT-773: Pharmacokinetics and Interactions with Ranitidine and Sucralfate

PubMed Central

Pletz, M. W.; Preechachatchaval, V.; Bulitta, J.; Allewelt, M.; Burkhardt, O.; Lode, H.

2003-01-01

We assessed the pharmacokinetics and interaction of ABT-773 in 12 volunteers receiving ABT-773 alone or concomitantly with ranitidine or sucralfate. Data for 150 mg of ABT-773 were as follows: the maximum concentration of the drug in plasma (Cmax) was 318 ng/ml, its half-life was 5.66 h, and its area under the plasma concentration-time curve from 0 h to ∞ (AUC0-∞) was 1,662 ng · h/ml. Coadministration of ranitidine, reduced the Cmax (−25.7%) and AUC0-∞ (−15.8%) significantly. Sucralfate had no impact on the bioavailability of ABT-773. PMID:12604553

Combined microplate-ABTS and HPLC-ABTS analysis of tomato and pepper extracts reveals synergetic and antagonist effects of their lipophilic antioxidative components.

PubMed

Le Grandois, Julie; Guffond, Delphine; Hamon, Erwann; Marchioni, Eric; Werner, Dalal

2017-05-15

The antioxidant capacity of 9 pure lipophilic compounds was examined by microplate-ABTS and HPLC-ABTS, using similar experimental conditions. Results obtained showed that HPLC-ABTS method can be used for a rapid determination of individual antioxidant capacity of compounds in standard solutions or complex mixtures. The application of both methods to real lipophilic extracts from tomato (Solanum lycopersicum L.), green and red peppers (Capsicum annuum) reveals possible interactions between antioxidants. Thus, synthetic mixtures of two compounds identified in tomato and peppers were measured using microplate-ABTS and HPLC-ABTS. Synergistic effects were observed between (β-carotene-capsanthin) (1:9) and (1:1), (α-tocopherol-capsanthin) (1:9), (lutein-lycopene) (9:1) and (capsanthin-δ-tocopherol) (9:1). On the contrary, antagonistic effects were observed for (lutein-δ-tocopherol) and (α-tocopherol-δ-tocopherol). The interactions observed with two-compound mixtures are not systematically observed in the natural lipophilic extracts from tomato, green and red peppers, probably since extracts are more complex and are susceptible to cause interferences. Copyright © 2016 Elsevier Ltd. All rights reserved.

Novel Water Soluble Chitosan Derivatives with 1,2,3-Triazolium and Their Free Radical-Scavenging Activity

PubMed Central

Li, Qing; Sun, Xueqi; Gu, Guodong

2018-01-01

Chitosan is an abundant and renewable polysaccharide, which exhibits attractive bioactivities and natural properties. Improvement such as chemical modification of chitosan is often performed for its potential of providing high bioactivity and good water solubility. A new class of chitosan derivatives possessing 1,2,3-triazolium charged units by associating “click reaction” with efficient 1,2,3-triazole quaternization were designed and synthesized. Their free radical-scavenging activity against three free radicals was tested. The inhibitory property and water solubility of the synthesized chitosan derivatives exhibited a remarkable improvement over chitosan. It is hypothesized that triazole or triazolium groups enable the synthesized chitosan to possess obviously better radical-scavenging activity. Moreover, the scavenging activity against superoxide radical of chitosan derivatives with triazolium (IC50 < 0.01 mg mL−1) was more efficient than that of derivatives with triazole and Vitamin C. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl radical-scavenging assay, the same pattern were observed, which should be related to the triazolium grafted at the periphery of molecular chains. PMID:29597269

Novel Water Soluble Chitosan Derivatives with 1,2,3-Triazolium and Their Free Radical-Scavenging Activity.

PubMed

Li, Qing; Sun, Xueqi; Gu, Guodong; Guo, Zhanyong

2018-03-28

Chitosan is an abundant and renewable polysaccharide, which exhibits attractive bioactivities and natural properties. Improvement such as chemical modification of chitosan is often performed for its potential of providing high bioactivity and good water solubility. A new class of chitosan derivatives possessing 1,2,3-triazolium charged units by associating "click reaction" with efficient 1,2,3-triazole quaternization were designed and synthesized. Their free radical-scavenging activity against three free radicals was tested. The inhibitory property and water solubility of the synthesized chitosan derivatives exhibited a remarkable improvement over chitosan. It is hypothesized that triazole or triazolium groups enable the synthesized chitosan to possess obviously better radical-scavenging activity. Moreover, the scavenging activity against superoxide radical of chitosan derivatives with triazolium (IC 50 < 0.01 mg mL -1 ) was more efficient than that of derivatives with triazole and Vitamin C. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl radical-scavenging assay, the same pattern were observed, which should be related to the triazolium grafted at the periphery of molecular chains.

A new expression for computing the bottomside thickness parameter and comparisons with the NeQuick and IRI-2012 models during declining phase of solar cycle 23 at equatorial latitude station, Chumphon, Thailand

NASA Astrophysics Data System (ADS)

Jamjareegulgarn, Punyawi; Supnithi, Pornchai; Watthanasangmechai, Kornyanat; Yokoyama, Tatsuhiro; Tsugawa, Takuya; Ishii, Mamoru

2017-07-01

This paper proposes a new expression for computing the bottomside thickness parameter at equatorial latitude station, Chumphon (10.72°N, 99.37°E), Thailand. Its diurnal variations from 2004 to 2006 at this location are then studied. The proposed expression is derived based on two experimental data sources: FMCW ionosonde and dual-frequency GPS system, and some expressions of the NeQuick 2 model. Hence, after both the bottomside thickness parameter computed by the proposed equation, B2bot_Pro, and the bottomside shape parameter (namely, B1_Pro in this work) are computed, the bottomside electron density and the height where the bottomside electron density drops down to be 24% of the NmF2 (namely, h0.24) can be computed and shown in this work using the analytical functions of the IRI model. Moreover, the diurnal variations of the B2bot_Pro are compared with those computed from the NeQuick model, B2bot_NeQ, and the predicted B0 of the IRI-2012 model with ABT-2009 and Bil-2000 options (namely, ;B0_ABT; and ;B0_Bil;, respectively). The averaged, minimum, and maximum values of percentage deviations among these bottomside thickness parameters are also computed and shown in this work. Our results show that the diurnal variations of B2bot_Pro at Chumphon station have the following patterns: they start to increase during nighttime to the first peaks during pre-sunrise hours, and then decrease abruptly to their minimum values during sunrise hours. Afterward, they increase again to reach the second peaks around local noontime and fall gradually to their starting times during 20-04 LT. The diurnal variations of B2bot_Pro follow generally the same trends as those of the B2bot_NeQ and the B0_ABT, except pre-sunrise hours. The pre-sunrise peaks and sunrise collapses in both the B2bot_NeQ and the B0_ABT can be found occasionally. On the other hand, the diurnal variations in B2bot_Pro differ from those in B0_Bil due to the flattened variation in B0_Bil and the pre-sunrise peaks as well as sunrise collapses in B0_Bil disappear. The pre-sunrise peaks of the B2bot_Pro at the Chumphon station are higher than those of the B2bot_NeQ, the B0_ABT, and the observed B0 at other regions. Furthermore, the percentage deviations between the B2bot_Pro and the B0_ABT (PD_B2B0ABT) are mostly lower than 30% for all seasons of the studied years, opposite to the other percentage deviations studied in this work. The proposed B2bot_Pro parameters in this work follow a similar trend to the B2bot_NeQ and the B0_ABT, but it is not conclusive that the proposed values are equivalent to them.

ESR studies on reactivity of protein-derived tyrosyl radicals formed by prostaglandin H synthase and ribonucleotide reductase.

PubMed

Lassmann, G; Curtis, J; Liermann, B; Mason, R P; Eling, T E

1993-01-01

Using ESR spectroscopy, the ability of enzyme inhibitors to quench protein-derived tyrosyl radicals was studied in two different enzymes, prostaglandin H synthase and ribonucleotide reductase. The prostaglandin H synthase inhibitors indomethacin, eugenol, and MK-410 effectively prevent the formation of tyrosyl radicals during the oxidation of arachidonic acid by prostaglandin H synthase from ram seminal vesicles. A direct reaction with preformed tyrosyl radicals was observed only with eugenol. The other prostaglandin H synthase inhibitors were ineffective. The ribonucleotide reductase inhibitors hydroxyurea and 4-hydroxyanisole, which effectively inactivate the tyrosyl radical in the active site of ribonucleotide reductase present in tumor cells, exhibit a different reactivity with tyrosyl radicals formed by prostaglandin H synthase. Hydroxyurea quenches preformed tyrosyl radicals in prostaglandin H synthase weakly, whereas 4-hydroxyanisole does not quench tyrosyl radicals in prostaglandin H synthase at all. Eugenol, which quenches preformed prostaglandin H synthase-derived tyrosyl radicals, also quenches the tyrosyl radical in ribonucleotide reductase. The results suggest that the reactivity of protein-linked tyrosyl radicals in ribonucleotide reductase and those formed during prostaglandin H synthase catalysis are very different and have unrelated roles in enzyme catalysis.

In Vitro and Bactericidal Activities of ABT-492, a Novel Fluoroquinolone, against Gram-Positive and Gram-Negative Organisms

PubMed Central

Almer, Laurel S.; Hoffrage, Jennifer B.; Keller, Erika L.; Flamm, Robert K.; Shortridge, Virginia D.

2004-01-01

In vitro activities of ABT-492, ciprofloxacin, levofloxacin, trovafloxacin, moxifloxacin, gatifloxacin, and gemifloxacin were compared. ABT-492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms. Bactericidal activity of ABT-492 was also evaluated. PMID:15215148

Identification of Antidiabetic Compounds from Polyphenolic-rich Fractions of Bulbine abyssinica A. Rich Leaves

PubMed Central

Odeyemi, Samuel Wale; Afolayan, Anthony Jiede

2018-01-01

Background: Bulbine abyssinica has been reported to possess a variety of pharmacological activities traditionally. Previous work suggested its antidiabetic properties, but information on the antidiabetic compounds is still lacking. Objective: The present research exertion was aimed to isolate and identify biologically active polyphenols from B. abyssinica leaves and to evaluate their efficacy on carbohydrate digesting enzymes. Materials and Methods: Fractionation of the polyphenolic contents from the methanolic extract of B. abyssinica leaves was executed by the silica gel column chromatography to yield different fractions. The antioxidant activities of these fractions were carried out against 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazyl radicals, and ferric ion-reducing antioxidant power (FRAP). In vitro antidiabetic experimentation was performed by evaluating the α-amylase and α-glucosidase inhibitory capacity. The isolated polyphenols were then identified using liquid chromatography and mass spectroscopy (LC/MS). Results: Out of the eight polyphenolic fractions (BAL 1–8), BAL-4 has the highest inhibitory activity against ABTS radicals whereas BAL-6 showed potent ferric ion-reducing capacity. BAL-5 was the most effective fraction with antidiabetic activity with IC50of 140.0 and 68.58 ± 3.2 μg/ml for α-amylase and α-glucosidase inhibitory activities, respectively. All the fractions competitively inhibited α-amylase, BAL-5 and BAL-6 also inhibited α-glucosidase competitively, while BAL-4 and BAL-1 exhibited noncompetitive and near competitive inhibitions against α-glucosidase, respectively. The LC/MS analysis revealed the presence of carvone in all the fractions. Conclusions: The present study demonstrates the antioxidant and antidiabetic activities of the isolated polyphenols from B. abyssinica. SUMMARY Polyphenols were successfully isolated and identified from Bulbine abyssinica leavesThe isolated polyphenols are biologically active with high antioxidant as well as inhibitor of carbohydrate-digesting enzymesB. abyssinica can be a good source of amylase and glucosidase inhibitorsB. abyssinica can be used as complementary or alternative therapeutic agents especially for the treatment of diabetesCarvone, quercetin, and psoralen could be the compounds responsible for the α-amylase and α-glucosidase inhibitory activities. Abbreviations Used: ABTS: 2,2'-Azino-bis (3-ethylbenzthiazoline-6-sulfonic acid), DPPH: 2,2-diphenyl-1-picrylhydrazyl, FRAP: Ferric ion-reducing antioxidant power, LC/MS: Liquid chromatography and mass spectroscopy, AGEs: Advanced glycation end products, TLC: Thin-layer chromatography, MeOH: Methanol, PNP-G: ρ-Nitrophenyl-α-D-Glucoside, R2: Coefficient of determination, mgQE: Milligram quercetin equivalent, mgTAE: Milligram tannic acid equivalent, mgCE: Milligram catechin equivalent, g: Gram PMID:29568191

Ethylene glycol modified 2-(2‧-aminophenyl)benzothiazoles at the amino site: the excited-state N-H proton transfer reactions in aqueous solution, micelles and potential application in live-cell imaging

NASA Astrophysics Data System (ADS)

Liu, Bo-Qing; Chen, Yi-Ting; Chen, Yu-Wei; Chung, Kun-You; Tsai, Yi-Hsuan; Li, Yi-Jhen; Chao, Chi-Min; Liu, Kuan-Miao; Tseng, Huan-Wei; Chou, Pi-Tai

2016-03-01

Triethylene glycol monomethyl ether and poly(ethylene glycol) monomethyl ether modified 2-(2‧-aminophenyl)benzothiazoles, namely ABT-P3EG, ABT-P7EG and ABT-P12EG varied by different chain length of poly(ethylene glycol) at the amino site, were synthesized to probe their photophysical and bio-imaging properties. In polar, aprotic solvents such as CH2Cl2 ultrafast excited-state intramolecular proton transfer (ESIPT) takes place, resulting in a large Stokes shifted tautomer emission in the green-yellow (550 nm) region. In neutral water, ABT-P12EG forms micelles with diameters of 15  ±  3 nm under a critical micelle concentration (CMC) of ~80 μM, in which the tautomer emission is greatly enhanced free from water perturbation. Cytotoxicity experiments showed that all ABT-PnEGs have negligible cytotoxicity against HeLa cells even at doses as high as 1 mM. Live-cell imaging experiments were also performed, the results indicate that all ABT-PnEGs are able to enter HeLa cells. While the two-photon excitation emission of ABT-P3EG in cells cytoplasm shows concentration independence and is dominated by the anion blue fluorescence, ABT-P7EG and ABT-P12EG exhibit prominent green tautomer emission at  >  CMC and in part penetrate to the nuclei, adding an additional advantage for the cell imaging.

A Derivative Method with Free Radical Oxidation to Predict Resveratrol Metabolites by Tandem Mass Spectrometry

PubMed Central

Liu, Wangta; Shiue, Yow-Ling; Lin, Yi-Reng; Lin, Hugo You-Hsien; Liang, Shih-Shin

2015-01-01

In this study, we demonstrated an oxidative method with free radical to generate 3,5,4′-trihydroxy-trans-stilbene (trans-resveratrol) metabolites and detect sequentially by an autosampler coupling with liquid chromatography electrospray ionization tandem mass spectrometer (LC-ESI–MS/MS). In this oxidative method, the free radical initiator, ammonium persulfate (APS), was placed in a sample bottle containing resveratrol to produce oxidative derivatives, and the reaction progress was tracked by autosampler sequencing. Resveratrol, a natural product with purported cancer preventative qualities, produces metabolites including dihydroresveratrol, 3,4′-dihydroxy-trans-stilbene, lunularin, resveratrol monosulfate, and dihydroresveratrol monosulfate by free radical oxidation. Using APS free radical, the concentrations of resveratrol derivatives differ as a function of time. Besides simple, convenient and time- and labor saving, the advantages of free radical oxidative method of its in situ generation of oxidative derivatives followed by LC-ESI–MS/MS can be utilized to evaluate different metabolites in various conditions. PMID:27594817

A Derivative Method with Free Radical Oxidation to Predict Resveratrol Metabolites by Tandem Mass Spectrometry.

PubMed

Liu, Wangta; Shiue, Yow-Ling; Lin, Yi-Reng; Lin, Hugo You-Hsien; Liang, Shih-Shin

2015-10-01

In this study, we demonstrated an oxidative method with free radical to generate 3,5,4'-trihydroxy- trans -stilbene ( trans -resveratrol) metabolites and detect sequentially by an autosampler coupling with liquid chromatography electrospray ionization tandem mass spectrometer (LC-ESI-MS/MS). In this oxidative method, the free radical initiator, ammonium persulfate (APS), was placed in a sample bottle containing resveratrol to produce oxidative derivatives, and the reaction progress was tracked by autosampler sequencing. Resveratrol, a natural product with purported cancer preventative qualities, produces metabolites including dihydroresveratrol, 3,4'-dihydroxy- trans -stilbene, lunularin, resveratrol monosulfate, and dihydroresveratrol monosulfate by free radical oxidation. Using APS free radical, the concentrations of resveratrol derivatives differ as a function of time. Besides simple, convenient and time- and labor saving, the advantages of free radical oxidative method of its in situ generation of oxidative derivatives followed by LC-ESI-MS/MS can be utilized to evaluate different metabolites in various conditions.

Combined treatment with ABT-737 and VX-680 induces apoptosis in Bcl-2- and c-FLIP-overexpressing breast carcinoma cells.

PubMed

Choi, Jung Eun; Woo, Seon Min; Min, Kyoung-Jin; Kang, Su Hwan; Lee, Soo Jung; Kwon, Taeg Kyu

2015-03-01

ABT-737, a BH3-mimetic small-molecule inhibitor, binds with very high affinity to Bcl-2, Bcl-xL and Bcl-w, and inhibits their activity. Aurora kinase is one of the serine/threonine kinase family members and is a vital and critical regulator of mitosis and meiosis. In the present study, we investigated the effects and mechanisms of a combined treatment of ABT-737 and VX-680 (Aurora kinase inhibitor) in human breast cancer MDA-MB‑435S cells. ABT-737 plus VX-680 induced caspase-dependent apoptosis in the human breast cancer cells. Combined treatment with ABT-737 and VX-680 led to the downregulation of Bcl-2 expression at the transcriptional level and the downregulation of c-FLIP and Mcl-1 expression at the post-transcriptional level. Overexpression of Bcl-2 or c-FLIP could not block the induction of apoptosis caused by the combined treatment with ABT-737 and VX-680. However, overexpression of Mcl-1 partially inhibited the induction of apoptosis. In contrast, the combined treatment with ABT-737 and VX680 had no effect on the apoptosis in normal cells. Taken together, our study demonstrated that combined treatment with ABT-737 and VX-680 induced apoptosis in anti‑apoptotic protein (Bcl-2 or c-FLIP)-overexpressing cells.

Antioxidant and antidiabetic properties of tartary buckwheat rice flavonoids after in vitro digestion*

PubMed Central

Bao, Tao; Wang, Ye; Li, Yu-ting; Gowd, Vemana; Niu, Xin-he; Yang, Hai-ying; Chen, Li-shui; Chen, Wei; Sun, Chong-de

2016-01-01

Oxidative stress and diabetes have a tendency to alter protein, lipid, and DNA moieties. One of the strategic methods used to reduce diabetes-associated oxidative stress is to inhibit the carbohydrate-digesting enzymes, thereby decreasing gastrointestinal glucose production. Plant-derived natural antioxidant molecules are considered a therapeutic tool in the treatment of oxidative stress and diabetes. The objective of this study was to identify tartary buckwheat rice flavonoids and evaluate the effect of in vitro digestion on their antioxidant and antidiabetic properties. High performance liquid chromatography (HPLC) analysis indicated the presence of rutin as a major component and quercitrin as a minor component of both digested and non-digested flavonoids. Both extracts showed a significant antioxidant capacity, but digested flavonoids showed reduced activity compared to non-digested. There were some decreases of the antioxidant activities (2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazy (DPPH) radical, and ferric reducing antioxidant power (FRAP)) of digested tartary buckwheat rice flavonoids compared with non-digested. Flavonoids from both groups significantly inhibited reactive oxygen species (ROS) production and α-glucosidase activity. Both digested and non-digested flavonoids markedly increased glucose consumption and glycogen content in HepG2 cells. Tartary buckwheat rice flavonoids showed appreciable antioxidant and antidiabetic properties, even after digestion. Tartary buckwheat rice appears to be a promising functional food with potent antioxidant and antidiabetic properties. PMID:27921399

Red-fleshed Apples: Old Autochthonous Fruits as a Novel Source of Anthocyanin Antioxidants.

PubMed

Faramarzi, Shadab; Pacifico, Severina; Yadollahi, Abbas; Lettieri, Annamaria; Nocera, Paola; Piccolella, Simona

2015-09-01

In order to promote breeding programs and a full reintroduction into production of two local red-fleshed apple varieties grown in Bekran and Bastam (Iran), the evaluation of their antioxidant properties was of interest. LC-MS(n) based metabolic fingerprinting analyses were applied to investigate the anthocyanin content of both peel and flesh components of the fruits. Cyanidin-3-O-hexoside isomers were present in both 'Bekran' and 'Bastam' apples, whereas 'Bekran' apple was a valuable source of anthocyanin rutinose derivatives. Employing DPPH(•), ABTS(•+), and ORAC methods, the antiradical efficacy was evaluated. The ability of the investigated fruit components to scavenge OH(•), and O(2) (•-) reactive species was also assessed. ID(50) values highlighted the massive antioxidant response of 'Bekran' peel component, able to counteract by 50 % OH(•), and O(2) (•-) at 130.3 and 91.6 μg/mL, respectively. The cytoprotective screening towards HeLa, HepG2, A549, SH-5YSY, and SK-N-BE(2)-C cell lines evidenced that the investigated Iranian red-fleshed apple fruits were able to exert a significant antioxidant response in hydrogen peroxide oxidized cell systems. Data collected suggested that the revaluation of 'Bekran' and 'Bastam' apple cultivars could represent a precious source of antioxidant compounds whose dietary intake could improve the human well-being reducing risks of free radical related chronic and degenerative diseases.

ABT492 and levofloxacin: comparison of their pharmacodynamics and their abilities to prevent the selection of resistant Staphylococcus aureus in an in vitro dynamic model.

PubMed

Firsov, Alexander A; Vostrov, Sergey N; Lubenko, Irene Yu; Arzamastsev, Alexander P; Portnoy, Yury A; Zinner, Stephen H

2004-07-01

To compare the kinetics of killing/regrowth of differentially susceptible clinical isolates of Staphylococcus aureus exposed to ABT492 and levofloxacin and to explore their relative abilities to prevent the selection of resistant mutants. Three clinical isolates of S. aureus--including two ciprofloxacin-susceptible S. aureus, 201 and 480--and a ciprofloxacin-resistant S. aureus 866, were exposed to clinically achievable ratios of area under the curve (AUC) to MIC in a dynamic model that simulated human pharmacokinetics of ABT492 (400 mg) and levofloxacin (500 mg) as a single dose. In addition, S. aureus 201 was exposed to single and multiple doses of ABT492 and levofloxacin (both once daily for 3 days) over wide ranges of 24 h AUC/MIC (AUC24/MIC) including clinically achievable AUC24/MIC ratios. With each isolate, ABT492 at clinically achievable AUC/MICs produced greater anti-staphylococcal effects than levofloxacin. Areas between the control growth and the time--kill curves (ABBC in single dose simulations and the sum of ABBCs determined after the first, second and third dosing in multiple dose simulations--ABBC(1+2+3)) were higher with ABT492 than levofloxacin. Moreover, at comparable AUC/MICs and AUC24/MICs, the maximal reductions in the starting inoculum of ABT492-exposed S. aureus were more pronounced than with levofloxacin. Loss in susceptibility of S. aureus 201 exposed to ABT492 or levofloxacin depended on the simulated AUC24/MIC. Although the maximal increase in MIC (MICfinal) related to its initial value (MICinitial) was seen at a higher AUC24/MIC ratio of ABT492 (120 h) than levofloxacin (50 h), similar AUC24/MICs (240 and 200 h, respectively) were protective against the selection of resistant S. aureus. These threshold values are readily achievable with 400 mg ABT492 (AUC24/MIC 870 h) but not with 500 mg levofloxacin (AUC24/MIC 70 h). Overall, these findings predict greater efficacy of clinically achievable AUC/MIC (or AUC24/MIC) of ABT492 both in terms of the anti-staphylococcal effect and prevention of the selection of resistant mutants.

Increased lymphocyte apoptosis in mouse models of colitis upon ABT-737 treatment is dependent upon BIM expression.

PubMed

Lutz, C; Mozaffari, M; Tosevski, V; Caj, M; Cippà, P; McRae, B L; Graff, C L; Rogler, G; Fried, M; Hausmann, M

2015-08-01

Exaggerated activation of lymphocytes contributes to the pathogenesis of inflammatory bowel disease (IBD). Medical therapies are linked to the BCL-2 family-mediated apoptosis. Imbalance in BCL-2 family proteins may cause failure in therapeutic responses. We investigated the role of BCL-2 inhibitor ABT-737 for lymphocyte apoptosis in mice under inflammatory conditions. B.6129P2-interleukin (IL)-10(tm1Cgn) /J (IL-10(-/-) ) weighing 25-30 g with ongoing colitis were used. Fifty mg/kg/day ABT-737 was injected intraperitoneally (i.p.). Haematological analyses were performed with an ADVIA 2120 flow cytometer and mass cytometry with a CyTOF 2. Following i.p. administration, ABT-737 was detected in both spontaneous and acute colitis in peripheral blood (PBL) and colon tissue. Treatment led to lymphopenia. CD4(+) CD44(+) CD62L(+) central memory and CD8(+) , CD44(+) CD62L(-) central memory T cells were decreased in PBL upon ABT-737 compared to vehicle-receiving controls. Increased apoptosis upon ABT-737 was determined in blood lymphocytes, splenocytes and Peyer's patches and was accompanied by a decrease in TNF and IL-1B. ABT-737 positively altered the colonic mucosa and ameliorated inflammation, as shown by colonoscopy, histology and colon length. A decreased BIM/BCL-2 ratio or absence of BIM in both Bim(-) (/) (-) and Il10(-) (/) (-) × Bim(-) (/) (-) impeded the protective effect of ABT-737. The BIM/BCL-2 ratio decreased with age and during the course of treatment. Thus, long-term treatment resulted in adapted TNF levels and macroscopic mucosal damage. ABT-737 was efficacious in diminishing lymphocytes and ameliorating colitis in a BIM-dependent manner. Regulation of inappropriate survival of lymphocytes by ABT-737 may provide a therapeutic strategy in IBD. © 2015 British Society for Immunology.

An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UV(B)-inflamed and normal skin.

PubMed

Schaffler, Klaus; Reeh, Peter; Duan, W Rachel; Best, Andrea E; Othman, Ahmed A; Faltynek, Connie R; Locke, Charles; Nothaft, Wolfram

2013-02-01

Laser (radiant-heat) evoked potentials (LEPs) from vertex-EEG peak-to-peak (PtP) amplitude were used to determine acute antinociceptive/antihyperalgesic efficacy of ABT-102, a novel TRPV1 antagonist efficacious in preclinical pain models, compared with active controls and placebo in normal and UV(B)-inflamed skin. This was a randomized, placebo- and active-controlled, double-blind, intra-individual, crossover trial. Twenty-four healthy subjects received six sequences of single doses of ABT-102 (0.5, 2, 6 mg), etoricoxib 90 mg, tramadol 100 mg and placebo. Painful stimuli were induced by CO(2) -laser on normal and UV(B) -inflamed skin. LEPs and visual analogue scale (VAS-pain) ratings were taken at baseline and hourly up to 8 h post-dose from both skin types. Compared with placebo, significant mean decreases in the primary variable of LEP PtP-amplitude from UV(B)-inflamed skin were observed with ABT-102 6 mg (P < 0.001), ABT-102 2 mg (P = 0.002), tramadol 100 mg (P < 0.001), and etoricoxib 90 mg (P = 0.001) over the 8 h period; ABT-102 0.5 mg was similar to placebo. ABT-102 6 mg was superior to active controls over the 8 h period (P < 0.05) whereas ABT-102 2 mg was comparable. Improvements in VAS scores compared with placebo were observed with ABT-102 6 mg (P < 0.001) and ABT-102 2 mg (P = 0.002). ABT-102 average plasma concentrations were 1.3, 4.4 and 9.4 ng ml(-1) for the 0.5, 2 and 6 mg doses, respectively. There were no clinically significant safety findings. TRPV-1 antagonism appears promising in the management of clinical pain, but requires further investigation. © 2012 Abbott. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.

Radiosensitization of Pancreatic Cancer Cells In Vitro and In Vivo through Poly (ADP-ribose) Polymerase Inhibition with ABT-888.

PubMed

Tuli, Richard; Surmak, Andrew J; Reyes, Juvenal; Armour, Michael; Hacker-Prietz, Amy; Wong, John; DeWeese, Theodore L; Herman, Joseph M

2014-05-13

To determine whether poly (ADP-ribose) polymerase-1/2 (PARP-1/2) inhibition enhances radiation-induced cytotoxicity of pancreatic adenocarcinoma in vitro and in vivo, and the mechanism by which this occurs. Pancreatic carcinoma cells were treated with ABT-888, radiation, or both. In vitro cell viability, apoptosis, and PARP activity were measured. Orthotopic xenografts were generated in athymic mice and treated with ABT-888 (25mg/kg), radiation (5Gy), both, or no treatment. Mice were monitored with bioluminescence imaging. In vitro, treatment with ABT-888 and radiation led to higher rates of cell death after 8days (P < .01). Co-treatment with 5Gy and 1, 10 or 100μmol/l of ABT-888 led to dose enhancement factors of 1.29, 1.41 and 2.36, respectively. Caspase activity was not significantly increased when treated with ABT-888 (10 μmol/l) alone (1.28-fold, P = .08), but became significant when radiation was added (2.03-fold, P < .01). PARP activity increased post-radiation and was abrogated following co-treatment with ABT-888. In vivo, treatment with ABT-888, radiation or both led to tumor growth inhibition (TGI) of 8, 30 and 39days, and survival at 60days of 0%, 0% and 40%, respectively. ABT-888 with radiation significantly enhanced tumor response in vitro and in vivo. ABT-888 inhibited PAR protein polymerization resulting in dose-dependent feedback up-regulation of PARP and p-ATM suggesting increased DNA damage. This translated into enhancement in TGI and survival with radiation in vivo. In vitro PAR levels correlated with levels of tumor apoptosis suggesting potential as a predictive biomarker. These data are being used to support a Phase I study in locally advanced pancreatic cancer. Copyright © 2014 Elsevier Inc. All rights reserved.

ABT-263 induces G1/G0-phase arrest, apoptosis and autophagy in human esophageal cancer cells in vitro.

PubMed

Lin, Qing-Huan; Que, Fu-Chang; Gu, Chun-Ping; Zhong, De-Sheng; Zhou, Dan; Kong, Yi; Yu, Le; Liu, Shu-Wen

2017-12-01

Both the anti- and pro-apoptotic members of the Bcl-2 family are regulated by a conserved Bcl-2 homology (BH3) domain. ABT-263 (Navitoclax), a novel BH3 mimetic and orally bioavailable Bcl-2 family inhibitor with high affinity for Bcl-xL, Bcl-2 and Bcl-w has entered clinical trials for cancer treatment. But the anticancer mechanisms of ABT-263 have not been fully elucidated. In this study we investigated the effects of ABT-263 on human esophageal cancer cells in vitro and to explore its anticancer mechanisms. Treatment with ABT-263 dose-dependently suppressed the viability of 3 human esophageal cancer cells with IC 50 values of 10.7±1.4, 7.1±1.5 and 8.2±1.6 μmol/L, in EC109, HKESC-2 and CaES-17 cells, respectively. ABT-263 (5-20 μmol/L) dose-dependently induced G 1 /G 0 -phase arrest in the 3 cancer cell lines and induced apoptosis evidenced by increased the Annexin V-positive cell population and elevated levels of cleaved caspase 3, cleaved caspase 9 and PARP. We further demonstrated that ABT-263 treatment markedly increased the expression of p21 Waf1/Cip1 and decreased the expression of cyclin D1 and phospho-Rb (retinoblastoma tumor suppressor protein) (Ser780) proteins that contributed to the G 1 /G 0 -phase arrest. Knockdown of p21 Waf1/Cip1 attenuated ABT-263-induced G 1 /G 0 -phase arrest. Moreover, ABT-263 treatment enhanced pro-survival autophagy, shown as the increased LC3-II levels and decreased p62 levels, which counteracted its anticancer activity. Our results suggest that ABT-263 exerts cytostatic and cytotoxic effects on human esophageal cancer cells in vitro and enhances pro-survival autophagy, which counteracts its anticancer activity.

An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin

PubMed Central

Schaffler, Klaus; Reeh, Peter; Duan, W Rachel; Best, Andrea E; Othman, Ahmed A; Faltynek, Connie R; Locke, Charles; Nothaft, Wolfram

2013-01-01

Aims Laser (radiant-heat) evoked potentials (LEPs) from vertex-EEG peak-to-peak (PtP) amplitude were used to determine acute antinociceptive/antihyperalgesic efficacy of ABT-102, a novel TRPV1 antagonist efficacious in preclinical pain models, compared with active controls and placebo in normal and UVB-inflamed skin. Methods This was a randomized, placebo- and active-controlled, double-blind, intra-individual, crossover trial. Twenty-four healthy subjects received six sequences of single doses of ABT-102 (0.5, 2, 6 mg), etoricoxib 90 mg, tramadol 100 mg and placebo. Painful stimuli were induced by CO2-laser on normal and UVB-inflamed skin. LEPs and visual analogue scale (VAS-pain) ratings were taken at baseline and hourly up to 8 h post-dose from both skin types. Results Compared with placebo, significant mean decreases in the primary variable of LEP PtP-amplitude from UVB-inflamed skin were observed with ABT-102 6 mg (P < 0.001), ABT-102 2 mg (P = 0.002), tramadol 100 mg (P < 0.001), and etoricoxib 90 mg (P = 0.001) over the 8 h period; ABT-102 0.5 mg was similar to placebo. ABT-102 6 mg was superior to active controls over the 8 h period (P < 0.05) whereas ABT-102 2 mg was comparable. Improvements in VAS scores compared with placebo were observed with ABT-102 6 mg (P < 0.001) and ABT-102 2 mg (P = 0.002). ABT-102 average plasma concentrations were 1.3, 4.4 and 9.4 ng ml−1 for the 0.5, 2 and 6 mg doses, respectively. There were no clinically significant safety findings. Conclusions TRPV-1 antagonism appears promising in the management of clinical pain, but requires further investigation. PMID:22775239

Phytochemical Composition and Antioxidant Activities of Dianthus Thunbergii Hooper and Hypoxis Argentea Harv Ex Baker: Plants Used for the Management of Diabetes Mellitus in Eastern Cape, South Africa

PubMed Central

Akinrinde, Akinleye Stephen; Afolayan, Anthony Jide; Bradley, Graeme

2018-01-01

Background: Inhabitants of the Eastern Cape Province of South Africa use the roots of Dianthus thunbergii and corms of Hypoxis argentea to treat diabetes mellitus and other ailments. Objective: The objective of this study was to analyze the phytochemical composition and antioxidant activities of the aqueous and ethanol extracts of the roots and corms of two plants. Materials and Methods: Total phenolics, flavonoids, flavonols, proanthocyanidins, tannins, and alkaloids were determined by standard methods. The scavenging activities of the extracts against 1,1 diphenyl-2-picrylhydrazyl (DPPH), 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid (ABTS), nitric oxide (NO), hydrogen peroxide (H2O2), and their ferric-reducing antioxidant potentials (FRAPs) were measured. Results: The ethanol extract of H. argentea had the highest content of phenolics (66.71 ± 2.71 mg gallic acid equivalent/g) and tannins (1.18 ± 0.07 mg TAE/g), while the ethanol extract of D. thunbergii gave higher contents of flavonoids and proanthocyanidins (62.21 ± 1.75 mg Qe/g and 432.62 ± 2.43 mg Ca/g, respectively). Flavonols were the most predominant in the aqueous extract of H. argentea (25.51 ± 1.92 mg Qe/g). We observed a concentration-dependent response in the ABTS- and H2O2-scavenging activities and FRAP values of the extracts and standards (Vitamin C, butylated hydroxytoluene, and rutin). The ethanol extracts of both plants generally demonstrated better antioxidant activities against H2O2, NO, and ABTS while also possessing better reducing power than the aqueous extracts. The aqueous extract of D. thunbergii, however, showed the best DPPH scavenging activity. Conclusion: The higher content of phytochemicals and antioxidant capacity obtained for the ethanol extracts of D. thunbergii and H. argentea may prove to be valuable information in selecting suitable extraction solvents for the medicinal applications of both plants. SUMMARY Ethanol extracts of Hypoxis argentea had the highest levels of phenolics and tanninsEthanol extracts of Dianthus thunbergii had the highest levels of flavonoids and proanthocyanidinsEthanol extracts of both plants possess better antioxidant activityagainst hydrogen peroxide, nitric oxide, and ABTS as well as higher reducingpower than the aqueous extractsAqueous extract of Dianthus thunbergii had the highest free radical scavenging activity as measured with DPPH. Abbreviations used: ABTS: 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid); BHT: Butylated hydroxytoluene; DPPH: 1,1 diphenyl-2-picrylhydrazyl; DTA: Dianthus thunbergii aqueous extract (16.6%); DTE: Dianthus thunbergii ethanol extract (2.4%); Fe3+-TPTZ: Ferric tripyridyltriazine; FRAP: Ferric-reducing antioxidant potentials; GAE: Gallic acid equivalent; HAA: Hypoxis argentea aqueous extract (3.2%); HAE: Hypoxis argentea ethanol extract (1.8%); Qe: Quercetin equivalence; ROS: Reactive oxygen species; TBA: Thiobarbituric acid;TCA: Trichloroacetic acid. PMID:29720831

Comparative study of the in vitro activity of a new fluoroquinolone, ABT-492.

PubMed

Harnett, S J; Fraise, A P; Andrews, J M; Jevons, G; Brenwald, N P; Wise, R

2004-05-01

The in vitro activity of a new fluoroquinolone, ABT-492, was determined. MICs were compared with those of two beta-lactams, telithromycin, ciprofloxacin and four later generation fluoroquinolones. The effects of human serum and of inoculum concentration were also investigated. MIC data indicate that ABT-492 has potent activity against Gram-positive organisms with enhanced anti-staphylococcal activity compared with earlier fluoroquinolones, in addition to activity against beta-haemolytic streptococci, pneumococci including penicillin- and fluoroquinolone-resistant strains and vancomycin-susceptible and -resistant Enterococcus faecalis but not Enterococcus faecium. ABT-492 was the most active agent tested against Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitidis, fluoroquinolone-susceptible Neisseria gonorrhoeae and anaerobes. Good activity was observed for ABT-492 amongst the Enterobacteriaceae and anaerobes tested, but ciprofloxacin showed superior activity for species of Proteus, Morganella and Providencia, as well as for Pseudomonas spp. In common with the other fluoroquinolones tested, organisms with reduced susceptibility to ciprofloxacin had raised MIC(90)s to ABT-492. The one isolate of H. influenzae tested with reduced fluoroquinolone susceptibility had an ABT-492 MIC close to that of the population lacking a mechanism of quinolone resistance. ABT-492 was more active than ciprofloxacin against Chlamydia spp. An inoculum effect was observed with a number of isolates of Staphylococcus aureus, Streptococcus pneumoniae, E. faecium, Klebsiella spp. and Escherichia coli, in addition to moderately raised MICs in the presence of 70% serum protein. The clinical significance of these findings is yet to be determined. ABT-492 is a new fluoroquinolone with excellent activity against both Gram-positive and Gram-negative organisms, with many potential clinical uses.

A Phase 2, Double-Blind, Placebo-Controlled Randomized Trial Assessing the Efficacy of ABT-436, a Novel V1b Receptor Antagonist, for Alcohol Dependence

PubMed Central

Ryan, Megan L; Falk, Daniel E; Fertig, Joanne B; Rendenbach-Mueller, Beatrice; Katz, David A; Tracy, Katherine A; Strain, Eric C; Dunn, Kelly E; Kampman, Kyle; Mahoney, Elizabeth; Ciraulo, Domenic A; Sickles-Colaneri, Laurie; Ait-Daoud, Nassima; Johnson, Bankole A; Ransom, Janet; Scott, Charles; Koob, George F; Litten, Raye Z

2017-01-01

Alcohol use disorder has been linked to dysregulation of the brain stress systems, producing a negative emotional state leading to chronic relapsing behavior. Vasopressin receptors appear to have a regulatory role in stress, anxiety, and alcohol. This study evaluated the novel compound, ABT-436, a V1b receptor antagonist, in alcohol-dependent participants in a 12-week clinical trial. Men and women (n=150) who met criteria for DSM–IV alcohol dependence were recruited across four sites. Participants received double-blind ABT-436 or placebo, and a computerized behavioral intervention. ABT-436 was titrated to 800 mg/day during weeks 2–12. Although the primary outcome, percentage of heavy drinking days, was lower in participants receiving ABT-436 compared with placebo, this difference was not statistically significant (31.3 vs 37.6, respectively; p=0.172; d=0.20). However, participants receiving ABT-436 had significantly greater percentage of days abstinent than those receiving placebo (51.2 vs 41.6, respectively; p=0.037; d=0.31). No significant differences were found between treatment groups on any other measures of drinking, alcohol craving, or alcohol-related consequences. Smokers receiving ABT-436 smoked significantly fewer cigarettes per week than those receiving placebo (p=0.046). ABT-436 was well tolerated, with diarrhea (mild-to-moderate severity) being the most common side effect. In subgroup analyses, participants with relatively higher baseline levels of stress responded better to ABT-436 than placebo on select drinking outcomes, suggesting there may be value in testing medications targeting the vasopressin receptor in high stress, alcohol-dependent patients. PMID:27658483

Realistic intake of a flavanol-rich soluble cocoa product increases HDL-cholesterol without inducing anthropometric changes in healthy and moderately hypercholesterolemic subjects.

PubMed

Martínez-López, Sara; Sarriá, Beatriz; Sierra-Cinos, José Luis; Goya, Luis; Mateos, Raquel; Bravo, Laura

2014-02-01

To assess whether antioxidant, anti-inflammatory and other cardio-protective effects attributed to cocoa are achieved when regularly consuming moderate amounts of a flavanol-rich soluble cocoa product, a non-randomized, controlled, crossover, free-living study was carried out in healthy (n = 24; 25.9 ± 5.6 years) and moderately hypercholesterolemic (200-240 mg dL(-1); n = 20; 30.0 ± 10.3 years) volunteers. Participants consumed two servings per day (7.5 g per serving) of a soluble cocoa product (providing 45.3 mg flavanols per day) in milk, which was compared with consuming only milk during a 4 week period. The effects on systolic and diastolic blood pressure and heart rate were determined, as well as on serum lipid and lipoprotein profiles, interleukins (IL)-1β, IL-6, IL-8, IL-10, tumor necrosis factor-α (TNF-α), monocyte chemoattractant protein-1 (MCP-1), vascular (VCAM-1) and intercellular cell adhesion molecules (ICAM-1), serum malondialdehyde (MDA), carbonyl groups (CG), ferric reducing/antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and free radical scavenging capacity (ABTS). During the study, the volunteers' diets and physical activity were also evaluated, as well as any changes in weight, skin folds, circumferences and related anthropometric parameters. Cocoa and certain polyphenol-rich fruits and vegetables and their derivatives were restricted. After consuming the cocoa product positive effects were observed such as an increase in serum HDL-C (p < 0.001) and dietary fiber intake (p = 0.050), whereas IL-10 decreased (p = 0.022). Other cardiovascular-related biomarkers and anthropometric parameters were unaffected. We have therefore concluded that regular consumption of this cocoa product in a Spanish-Mediterranean diet may protect against cardiovascular disease in healthy and hypercholesterolemic subjects without producing any weight gain or other anthropometric changes.

High efficacy of the BCL-2 inhibitor ABT199 (venetoclax) in BCL-2 high-expressing neuroblastoma cell lines and xenografts and rational for combination with MCL-1 inhibition

PubMed Central

Bate-Eya, Laurel T.; den Hartog, Ilona J.M.; van der Ploeg, Ida; Schild, Linda; Koster, Jan; Santo, Evan E.; Westerhout, Ellen M.; Versteeg, Rogier; Caron, Huib N.; Molenaar, Jan J.; Dolman, M. Emmy M.

2016-01-01

The anti-apoptotic protein B cell lymphoma/leukaemia 2 (BCL-2) is highly expressed in neuroblastoma and plays an important role in oncogenesis. In this study, the selective BCL-2 inhibitor ABT199 was tested in a panel of neuroblastoma cell lines with diverse expression levels of BCL-2 and other BCL-2 family proteins. ABT199 caused apoptosis more potently in neuroblastoma cell lines expressing high BCL-2 and BIM/BCL-2 complex levels than low expressing cell lines. Effects on cell viability correlated with effects on BIM displacement from BCL-2 and cytochrome c release from the mitochondria. ABT199 treatment of mice with neuroblastoma tumors expressing high BCL-2 levels only resulted in growth inhibition, despite maximum BIM displacement from BCL-2 and the induction of a strong apoptotic response. We showed that neuroblastoma cells might survive ABT199 treatment due to its acute upregulation of the anti-apoptotic BCL-2 family protein myeloid cell leukaemia sequence 1 (MCL-1) and BIM sequestration by MCL-1. In vitro inhibition of MCL-1 sensitized neuroblastoma cell lines to ABT199, confirming the pivotal role of MCL-1 in ABT199 resistance. Our findings suggest that neuroblastoma patients with high BCL-2 and BIM/BCL-2 complex levels might benefit from combination treatment with ABT199 and compounds that inhibit MCL-1 expression. PMID:27056887

Biological rational for sequential targeting of Bruton tyrosine kinase and Bcl-2 to overcome CD40-induced ABT-199 resistance in mantle cell lymphoma.

PubMed

Chiron, David; Dousset, Christelle; Brosseau, Carole; Touzeau, Cyrille; Maïga, Sophie; Moreau, Philippe; Pellat-Deceunynck, Catherine; Le Gouill, Steven; Amiot, Martine

2015-04-20

The aggressive biological behavior of mantle cell lymphoma (MCL) and its short response to current treatment highlight a great need for better rational therapy. Herein, we investigate the ability of ABT-199, the Bcl-2-selective BH3 mimetic, to kill MCL cells. Among MCL cell lines tested (n = 8), only three were sensitive (LD50 < 200 nM). In contrast, all primary MCL samples tested (n = 11) were highly sensitive to ABT-199 (LD50 < 10 nM). Mcl-1 and Bcl-xL both confer resistance to ABT-199-specific killing and BCL2/(BCLXL+MCL1) mRNA ratio is a strong predictor of sensitivity. By mimicking the microenvironment through CD40 stimulation, we show that ABT-199 sensitivity is impaired through activation of NF-kB pathway and Bcl-x(L) up-regulation. We further demonstrate that resistance is rapidly lost when MCL cells detach from CD40L-expressing fibroblasts. It has been reported that ibrutinib induces lymphocytosis in vivo holding off malignant cells from their protective microenvironment. We show here for two patients undergoing ibrutinib therapy that mobilized MCL cells are highly sensitive to ABT-199. These results provide evidence that in situ ABT-199 resistance can be overcome when MCL cells escape from the lymph nodes. Altogether, our data support the clinical application of ABT-199 therapy both as a single agent and in sequential combination with BTK inhibitors.

Individual and collective modes of surface magnetoplasmon in thiolate-protected silver nanoparticles studied by MCD spectroscopy

NASA Astrophysics Data System (ADS)

Yao, Hiroshi; Shiratsu, Taisuke

2016-05-01

Large magneto-optical (MO) responses at the energy of localized surface plasmon resonance (LSPR), namely, surface magnetoplasmons, are demonstrated for the first time in thiolate-protected silver nanoparticles with magnetic circular dichroism (MCD) spectroscopy. The samples examined are decanethiol (DT)-, azobenzenethiol (ABT)-, and ABT/DT mixed-monolayer-protected Ag nanoparticles. ABT-protected Ag nanoparticles are somewhat aggregated and thus exhibit a broad, collective mode of plasmonic absorption, whereas other samples with highly-dispersed nanoparticles show an individual mode of LSPR absorption. In all Ag nanoparticles, a derivative-like MCD signal is observed under an applied magnetic field of 1.6 T, which can be explained in terms of two circular modes of magnetoplasmon caused by the increase (or decrease) in the Lorentz force imparted on the free electrons that oscillate in the left (or right) circular orbits in the nanosphere. For the Ag nanoparticles exhibiting an individual LSPR mode, in particular, simultaneous deconvolution analysis of UV-vis absorption and MCD spectra reveal that (i) the amplitude of the magnetoplasmonic component with lower frequency (ω-), resulting from the reduction in the confinement strength of collective electrons by the Lorentz force, is stronger than that with a higher frequency (ω+) (ii) the accurate shift or cyclotron frequency between two magnetoplasmonic modes (ωc = ω+ - ω-) is size-dependent, and presents a very large value with implications for the apparent enhancement of the local magnetic-field in the Ag nanoparticles. These results strongly suggest that the Ag-thiolate layer or Ag-S bonding on the nanoparticle surface plays a significant role in the MO enhancement.Large magneto-optical (MO) responses at the energy of localized surface plasmon resonance (LSPR), namely, surface magnetoplasmons, are demonstrated for the first time in thiolate-protected silver nanoparticles with magnetic circular dichroism (MCD) spectroscopy. The samples examined are decanethiol (DT)-, azobenzenethiol (ABT)-, and ABT/DT mixed-monolayer-protected Ag nanoparticles. ABT-protected Ag nanoparticles are somewhat aggregated and thus exhibit a broad, collective mode of plasmonic absorption, whereas other samples with highly-dispersed nanoparticles show an individual mode of LSPR absorption. In all Ag nanoparticles, a derivative-like MCD signal is observed under an applied magnetic field of 1.6 T, which can be explained in terms of two circular modes of magnetoplasmon caused by the increase (or decrease) in the Lorentz force imparted on the free electrons that oscillate in the left (or right) circular orbits in the nanosphere. For the Ag nanoparticles exhibiting an individual LSPR mode, in particular, simultaneous deconvolution analysis of UV-vis absorption and MCD spectra reveal that (i) the amplitude of the magnetoplasmonic component with lower frequency (ω-), resulting from the reduction in the confinement strength of collective electrons by the Lorentz force, is stronger than that with a higher frequency (ω+) (ii) the accurate shift or cyclotron frequency between two magnetoplasmonic modes (ωc = ω+ - ω-) is size-dependent, and presents a very large value with implications for the apparent enhancement of the local magnetic-field in the Ag nanoparticles. These results strongly suggest that the Ag-thiolate layer or Ag-S bonding on the nanoparticle surface plays a significant role in the MO enhancement. Electronic supplementary information (ESI) available: EDX spectroscopic analysis of various Ag nanoparticle samples; MCD signals normalized to absorbance for the Ag(DT)L and Ag(DT)S samples; deconvolution of UV-vis absorption and MCD spectra using three Lorentzian components; IR spectral changes upon photoisomerization; thermal cis-to-trans relaxation of azobenzene in the Ag(ABT) sample; UV-vis absorption spectra of Ag nanoparticle samples in the presence/absence of a magnetic field of 1.6 T. See DOI: 10.1039/c6nr00631k

Identification and quantification of phenolic compounds of selected fruits from Madeira Island by HPLC-DAD-ESI-MS(n) and screening for their antioxidant activity.

PubMed

Spínola, Vítor; Pinto, Joana; Castilho, Paula C

2015-04-15

Five fruits species commonly cultivated and consumed in Madeira Island (Portugal) were investigated for their phenolic profile by means of reversed phase high-performance liquid chromatography coupled to diode array detection and electrospray ionisation mass spectrometry (HPLC-DAD-ESI/MS(n)) and antioxidant potential. A large number of compounds were characterised, flavonoids and phenolic acids being the major components found in target samples, 39 compounds (flavonoids, phenolic acids, terpenoids, cyanogenic glycosides and organic acids) were identified in cherimoyas, lemons, papayas, passion-fruits and strawberries for the first time. Furthermore, all samples were systematically analysed for their total phenolic and flavonoid contents along with two radical scavenging methods (ABTS and ORAC) for antioxidant activity measurement. Target fruits presented high phenolic contents which is responsible for most of the antioxidant activity against radical reactive species (R(2)>0.80). Quantitative data showed that anthocyanins, in particular pelargonidin-3-O-hexoside (>300 mg/100 mL), present only in strawberries were the compounds in largest amounts but are the ones which contribute less to the antioxidant activity. Copyright © 2014 Elsevier Ltd. All rights reserved.

Combating oxidative stress as a hallmark of cancer and aging: Computational modeling and synthesis of phenylene diamine analogs as potential antioxidant.

PubMed

Abou-Zeid, Laila; Baraka, Hany N

2014-07-01

The cross talk between the over expression of oxygen-free radicals is known as reactive oxygen species (ROS) that is associated with the excessive telomerase activity (TA). Telomerase activity is an invariable finding where human telomerase (hTERT) has been implicated in tumor oxidative stress and redox-mediated malignancy. The hTERT over expression is a novel tumor marker and is promising as a novel class of therapeutic weapons to fight against cancer. A new series of phenylene diamines were designed, synthesized, and evaluated for their in vitro antioxidant as an indicator of inhibiting the oxidative stress tumor. Compounds 3b and 7b proved to be the most active antioxidants with high percentage ABTS inhibition ranged from 89.40% to 88.59% respectively. Molecular modeling studies indicated that the crest configuration of phenylene diamine nucleus with substitutions of trimethoxy benzamido functional proved to be crucial for enhancing the free radical scavenging activity. Molecular modeling exploration indicated the proper binding selectivity of the 3b and 7b to the 3KYL pocket with promising hTERT inhibitors as a hallmark of cancer.

A new ultra-high pressure liquid chromatography method for the determination of antioxidant flavonol aglycones in six Lysimachia species.

PubMed

Tóth, Anita; Végh, Krisztina; Alberti, Ágnes; Béni, Szabolcs; Kéry, Ágnes

2016-10-01

UPLC-DAD method was developed and validated for the quantitative determination of free flavonol aglycones (kaempferol, quercetin and myricetin) after acidic hydrolysis in six Lysimachia species. Quantitative analyses showed that the amounts of various flavonol aglycones were significantly different in Lysimachia vulgaris, Lysimachia nummularia, Lysimachia punctata, Lysimachia christinae, Lysimachia ciliata and Lysimachia clethroides. The L. clethroides sample was found to be the richest in kaempferol (25.77 ± 1.29 μg/mg extract) and quercetin (97.67 ± 4.61 μg/mg extract), while the L. nummularia sample contained the highest amount of myricetin (20.79 ± 1.00 μg/mg extract). The antioxidant capacity of hydrolysed extracts was evaluated using in vitro DPPH(•) (2,2-diphenyl-1-picrylhydrazyl) and ABTS(•+) [2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid)] decolourisation tests. The observed radical scavenging capacities of the extracts showed a relationship with the measured flavonol aglycone content and composition. The acidic treatment resulted in an increased free radical scavenging activity compared to the untreated methanol extract.

Phytochemicals and Antioxidant Capacity from Nypa fruticans Wurmb. Fruit

PubMed Central

Prasad, Nagendra; Yang, Bao; Kong, Kin Weng; Khoo, Hock Eng; Sun, Jian; Azlan, Azrina; Ismail, Amin; Romli, Zulfiki Bin

2013-01-01

Nypa fruticans Wurmb. is one of the important underutilized fruit of Malaysia, which lacks scientific attention. Total phenolics, flavonoid content, and antioxidant capacities from endosperm extracts of Nypa fruticans (unripe and ripe fruits) were evaluated. Endosperm extract of unripe fruits (EEU) exhibited the highest phenolics (135.6 ± 4.5 mg GAE/g), flavonoid content (68.6 ± 3.1 RE/g), and antioxidant capacity. Free radical scavenging capacity of EEU as assessed by 2-2′-azino-bis (3-ethylbenz-thiazoline-6-sulfonic acid (ABTS) and 1,1-diphenyl-2-picryl hydrazyl (DPPH) radicals showed inhibitory activity of 78 ± 1.2% and 85 ± 2.6%, respectively. Beta carotene bleaching coefficient of EEU was higher (2550 ± 123), when compared to endosperm extract of ripe fruits (1729 ± 172). Additionally, EEU exhibited high antioxidant capacity by phosphomolybdenum method and ferric reducing antioxidant power values. Eight phenolic compounds from Nypa fruticans endosperm extracts were identified and quantified by ultra-high-performance liquid chromatography. Chlorogenic acid, protocatechuic acid, and kaempferol were the major phenolic compounds. Thus this fruit could be used as a potential source of natural antioxidant. PMID:23710209

Antioxidant and hypoglycemic effects of Diospyros lotus fruit fermented with Microbacterium flavum and Lactobacillus plantarum.

PubMed

Zhang, Zhi-Peng; Ma, Jun; He, Yuan-Yuan; Lu, Jun; Ren, Di-Feng

2018-06-01

Diospyros lotus, a member of the Ebenaceae family, has long been used as a traditional sedative in China. In this study, the antioxidant and hypoglycemic effects of non-fermented and microorganism-fermented D. lotus were explored. The total phenolic and vitamin C contents of microorganism-fermented D. lotus for 24-72 h were less than those of non-fermented. High-performance liquid chromatography showed that the tannic, catechinic, and ellagic acid contents increased significantly upon fermentation for 24 h. D. lotus fermented with Microbacterium flavum for 24 h exhibited the highest DPPH radical scavenging activity (IC 50  = 4.18 μg mL -1 ), and the highest ABTS radical scavenging activity was exhibited at 72 h of fermentation (IC 50  = 29.18 μg mL -1 ). The anti-α-glucosidase activity of fermented D. lotus was higher (2.06-4.73-fold) than that of non-fermented one. Thus, fermented D. lotus is a useful source of natural antioxidants, and a valuable food, exhibiting antioxidant and hypoglycemic properties. Copyright © 2018 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

Structure elucidation and antioxidant activity of a novel polysaccharide isolated from Boletus speciosus Forst.

PubMed

Ding, Xiang; Hou, Yi-ling; Hou, Wan-ru

2012-04-01

In this study, a novel heteropolysaccharide was isolated from the fruiting bodies of Boletus speciosus Forst through DEAE-cellulose column and Sephadex G-200 column. The Boletus speciosus Forst polysaccharide (BSFP-1) had a molecular weight of 1.33×10(4) Da and was mainly composed of l-Man and d-Gal which ratios were 2:1. Structural features of Boletus speciosus Forst polysaccharide (BSFP-1) were investigated by a combination of total hydrolysis, methylation analysis, gas chromatography-mass spectrometry (GC-MS), infrared (IR) spectra and nuclear magnetic resonance (NMR) spectroscopy. The results indicated that Boletus speciosus Forst polysaccharide (BSFP-1) had a backbone of (1→4)-α-l-mannopyranose residues which branches at O-6 based on the experimental results. The branches were mainly composed of one with →1)-α-d-galactopyranose residue. The antioxidant activity of BSFP-1 was evaluated with two biochemical methods, including 1,1-diphenyl-2-picrylhydrazyl (DPPH(-)) radical scavenging, scavenging activity of 2,2'-azino-bis(3-ethylbenzthiazoline-6-suphonic acid)diammonium (ABTS(+)) radical. The results indicated that BSFP-1 showed strong antioxidant. Copyright © 2012 Elsevier B.V. All rights reserved.

Crocus cancellatus subsp. damascenus stigmas: chemical profile, and inhibition of α-amylase, α-glucosidase and lipase, key enzymes related to type 2 diabetes and obesity.

PubMed

Loizzo, Monica R; Marrelli, Mariangela; Pugliese, Alessandro; Conforti, Filomena; Nadjafi, Farsad; Menichini, Francesco; Tundis, Rosa

2016-01-01

Spices are appreciated for their medicinal properties besides their use as food adjuncts to enhance the sensory quality of food. In this study, Crocus cancellatus subsp. damascenus was investigated for its antioxidant activities employing different in vitro systems. Stigma extract demonstrated a radical scavenging activity against both 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals with IC50 values of 34.6 and 21.6 µg/mL and a good ferric reducing ability (53.9 µM Fe(II)/g). In order to clarify the potential functional properties of this spice, the carbohydrate-hydrolysing enzymes and pancreatic lipase inhibitory properties were investigated. Crocus cancellatus subsp. damascenus extract inhibited α-amylase and α-glucosidase with IC50 values of 57.1 and 68.6 µg/mL, respectively. The bioactivity was discussed in terms of phytochemicals content. The obtained results may be of interest from a functional point of view or as food additive and to promote the revalorization of this species.

Purification, Characterization, and Antioxidant Activity of Polysaccharides Isolated from Cortex Periplocae.

PubMed

Wang, Xiaoli; Zhang, Yifei; Liu, Zhikai; Zhao, Mingqin; Liu, Pengfei

2017-10-31

In this study, crude Cortex Periplocae polysaccharides (CCPPs) were extracted with water. CCPPs were decolored with AB-8 resin and deproteinated using papain-Sevage methods. Then, they were further purified and separated through DEAE-52 anion exchange chromatography and Sephadex G-100 gel filtration chromatography, respectively. Three main fractions-CPP1, CPP2, and CPP3, (CPPs)-were obtained. The average molecular weights, monosaccharide analysis, surface morphology, and chemical compositions of the CPPs were investigated by high-performance gel permeation chromatography (HPGPC), gas chromatography-mass spectrometry (GC/MS), UV-vis spectroscopy, Fourier transform infrared (FT-IR) spectrum, and nuclear magnetic resonance (NMR). In addition, the antioxidant activities of these three polysaccharides were investigated. The results indicated that all of the CPPs were composed of rhamnose, arabinose, mannose, glucose, and galactose. These three polysaccharides exhibited antioxidant activities in four assays including 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethyl-benzthiazoline-6-sulfonic acid) (ABTS) radical, reducing power, and total antioxidant activity in vitro. The data indicated that these three polysaccharides could be utilized as potential natural sources of alternative additives in the functional food, cosmetics, and pharmaceutical industries.

Influence of the Toothpaste with Brazilian Ethanol Extract Propolis on the Oral Cavity Health

PubMed Central

Skaba, Dariusz; Morawiec, Tadeusz; Tanasiewicz, Marta; Bobela, Elżbieta; Skucha-Nowak, Małgorzata; Dawiec, Monika; Yamamoto, Rindai; Makita, Yuki; Redzynia, Małgorzata; Janoszka, Beata; Niedzielska, Iwona; Król, Wojciech

2013-01-01

Propolis-based therapeutic agents represent this potential for the development of new drugs in dental care. The aim of a clinical-cohort study was to determine the influence of application of toothpaste enriched with Brazilian extract of propolis (EEP) on health status of oral cavity. Laboratory analysis was conducted in order to assess the chemical composition of EEP including total phenolic compounds, the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging activity, ABTS radical cation scavenging activity, and FRAP assay. Clinical research involved two groups of subjects comprising 32 adult patients, with assessment based on the preliminary evaluation of the state of their marginal periodontium. The investigation of oral health indices API, OHI, and SBI and microbiological examination of oral microflora were also carried out. Results obtained indicated time-dependent microbial action of EEP at 50 mg/L concentration, with antimicrobial activity against Gram-positive bacteria. The total decrease of API, OHI, and SBI mean values was observed. Hygienic preparations with 3% content of Brazilian ethanol extract of green propolis (EEP) efficiently support removal of dental plaque and improve the state of marginal periodontium. PMID:23861699

Color, bioactive compounds and morphological characteristics of encapsulated Asian pear juice powder during spray drying.

PubMed

Lee, Chang-Gon; Ahmed, Maruf; Jiang, Gui-Hun; Eun, Jong-Bang

2017-08-01

Encapsulated Asian pear juice powder was produced through spray drying using three maltodextrin levels (15, 20, and 25% w/v) and three inlet air temperatures (130, 150, and 170 °C). The impact of maltodextrin concentrations and inlet air temperatures on color, bioactive compounds, and morphological characteristics of encapsulated Asian pear juice powder were investigated. Maltodextrin concentrations and inlet air temperatures significantly influenced L * and b * values of encapsulated Asian pear juice powder. Increasing inlet air temperatures increased total phenolic content, whereas the vitamin C content decreased. Vitamin C content was strongly correlated with particle size, inlet air temperature, and maltodextrin concentration. ABTS + radical-scavenging activity was highly correlated with total phenol content while DPPH radical-scavenging activity was highly correlated with vitamin C content. Encapsulated powders made with higher inlet air temperature and higher maltodextrin concentration had lowest median particle diameter with a smoother, more regular and rounded outer surface than those of encapsulated powders produced with lower inlet air temperature and lower maltodextrin concentration. Therefore, the results demonstrate that high-quality encapsulated Asian pear juice powder could be manufactured by adding 15% (w/v) maltodextrin and spray-drying at 170 °C.

Addition products of alpha-tocopherol with lipid-derived free radicals.

PubMed

Yamauchi, Ryo

2007-01-01

The addition products of alpha-tocopherol with lipid-derived free radicals have been reviewed. Free radical scavenging reactions of alpha-tocopherol take place via the alpha-tocopheroxyl radical as an intermediate. If a suitable free radical is present, an addition product can be formed from the coupling of the free radical with the alpha-tocopheroxyl radical. The addition products of alpha-tocopherol with lipid-peroxyl radicals are 8a-(lipid-dioxy)-alpha-tocopherones, which are hydrolyzed to alpha-tocopherylquinone. On the other hand, the carbon-centered radicals of lipids prefer to react with the phenoxyl radical of alpha-tocopherol to form 6-O-lipid-alpha-tocopherol under anaerobic conditions. The addition products of alpha-tocopherol with peroxyl radicals (epoxylinoleoyl-peroxyl radicals) produced from cholesteryl ester and phosphatidylcholine were detected in the peroxidized human plasma using a high-sensitive HPLC procedure with postcolumn reduction and electrochemical detection. Thus, the formation of these addition products provides us with much information on the antioxidant function of vitamin E in biological systems.

Anticholinesterase and antioxidant potentials of Nonea micrantha Bioss. & Reut along with GC-MS analysis.

PubMed

Imran, Muhammad; Ullah, Farhat; Ayaz, Muhammad; Sadiq, Abdul; Shah, Muhammad Raza; Jan, Muhammad Saeed; Ullah, Farman

2017-11-23

Nonea micrantha Boiss. & Reut . being an unexplored member of Boraginaceae was investigated for GC/MS analysis, acetylcholinesterase (AChE), butyrylcholinesterase (BChE) inhibitory and antioxidant activities in an attempt to find its effectiveness in neurological disorders. The AChE and BChE inhibitory activities of crude methanolic extract (Nm.Cr), subsequent fractions; n-hexane (Nm.Hex), chloroform (Nm.Cf), ethyl acetate (Nm.EtAc), aqueous (Nm.Aq) and crude saponins (Nm.Sp) from N. micrantha were conducted using Ellman's assay. The antioxidant activity of the plant samples using DPPH and ABTS free radical scavenging potential following quantitative spectrophotometric and qualitative TLC method were also studied. Moreover the total reducing power (TRP) of all the samples was also figured out. The GC/Ms analysis confirmed that the plant is rich in bioactive molecules. Among different fractions, Nm.Hex, Nm.EtAc and Nm.Cf exhibited highest AChE inhibitory activities causing 75.51 ± 0.73, 68.54 ± 0.59 and 63.48 ± 0.59% enzyme inhibition respectively and IC 50 of 44, 100 and 144 μg/mL respectively. In BChE inhibiton assay, Nm.Aq, Nm.Sp and Nm.Cr showed highest activity causing 83.49 ± 0.27, 81.49 ± 0.89 and 75.31 ± 0.56% enzyme inhibition with IC 50 of 90, 110 and 44 μg/mL respectively. In DPPH assay, Nm.Aq, Nm.Cf, Nm.Hex and Nm.Cr were most potent exhibiting IC 50 values of 3, 5, 93 and 120 μg/ml respectively. In ABTS assay Nm.EtAc, Nm.Aq, Nm.Sp and Nm.Cr showed IC 50 values of 60, 95, 100 and 150 μg/mL respectively. Likewise ABTS inhibition was most prominent for Nm.Sp, Nm.EtAc and Nm.Aq causing 78.26 ± 0.49, 67.67 ± 0.73 and 63.58 ± 0.45% inhibition respectively at 1 mg/mL. These results were further confirmed by qualitative screening using DPPH and ABTS staining. Our anticholinesterase and antioxidant results signify the N. micrantha as a potential source of natural bioactive compounds. Moreover isolation of natural bioactive compounds from this plant may lead to novel drug candidates against neurodegenerative disorders.

New derivatives of 3,4-dihydroisoquinoline-3-carboxylic acid with free-radical scavenging, D-amino acid oxidase, acetylcholinesterase and butyrylcholinesterase inhibitory activity.

PubMed

Solecka, Jolanta; Guśpiel, Adam; Postek, Magdalena; Ziemska, Joanna; Kawęcki, Robert; Lęczycka, Katarzyna; Osior, Agnieszka; Pietrzak, Bartłomiej; Pypowski, Krzysztof; Wyrzykowska, Agata

2014-09-30

A series of 3,4-dihydroisoquinoline-3-carboxylic acid derivatives were synthesised and tested for their free-radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH·), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical (ABTS·+), superoxide anion radical (O2·-) and nitric oxide radical (·NO) assays. We also studied d-amino acid oxidase (DAAO), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. Almost each of newly synthesised compounds exhibited radical scavenging capabilities. Moreover, several compounds showed moderate inhibitory activities against DAAO, AChE and BuChE. Compounds with significant free-radical scavenging activity may be potential candidates for therapeutics used in oxidative-stress-related diseases.

Free radical reactions of isoxazole and pyrazole derivatives of hispolon: kinetics correlated with molecular descriptors.

PubMed

Shaikh, Shaukat Ali M; Barik, Atanu; Singh, Beena G; Modukuri, Ramani V; Balaji, Neduri V; Subbaraju, Gottumukkala V; Naik, Devidas B; Priyadarsini, K Indira

2016-12-01

Hispolon (HS), a natural polyphenol found in medicinal mushrooms, and its isoxazole (HI) and pyrazole (HP) derivatives have been examined for free radical reactions and in vitro antioxidant activity. Reaction of these compounds with one-electron oxidant, azide radicals ([Formula: see text]) and trichloromethyl peroxyl radicals ([Formula: see text]), model peroxyl radicals, studied by nanosecond pulse radiolysis technique, indicated formation of phenoxyl radicals absorbing at 420 nm with half life of few hundred microseconds (μs). The formation of phenoxyl radicals confirmed that the phenolic OH is the active centre for free radical reactions. Rate constant for the reaction of these radicals with these compounds were in the order k HI ≅ k HP  >   k HS . Further the compounds were examined for their ability to inhibit lipid peroxidation in model membranes and also for the scavenging of 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical and superoxide ([Formula: see text]) radicals. The results suggested that HP and HI are less efficient than HS towards these radical reactions. Quantum chemical calculations were performed on these compounds to understand the mechanism of reaction with different radicals. Lower values of adiabatic ionization potential (AIP) and elevated highest occupied molecular orbital (HOMO) for HI and HP compared with HS controlled their activity towards [Formula: see text] and [Formula: see text] radicals, whereas the contribution of overall anion concentration was responsible for higher activity of HS for DPPH, [Formula: see text], and lipid peroxyl radical. The results confirm the role of different structural moieties on the antioxidant activity of hispolon derivatives.

40 CFR 1037.730 - ABT reports.

Code of Federal Regulations, 2014 CFR

2014-07-01

... identification number for the first vehicle covered by the new FEL. In this case, identify each applicable FEL... EMISSIONS FROM NEW HEAVY-DUTY MOTOR VEHICLES Averaging, Banking, and Trading for Certification § 1037.730 ABT reports. (a) If any of your vehicle families are certified using the ABT provisions of this...

Chemotherapeutic drugs sensitize human renal cell carcinoma cells to ABT-737 by a mechanism involving the Noxa-dependent inactivation of Mcl-1 or A1.

PubMed

Zall, Henry; Weber, Arnim; Besch, Robert; Zantl, Niko; Häcker, Georg

2010-06-24

Human renal cell carcinoma (RCC) is very resistant to chemotherapy. ABT-737 is a novel inhibitor of anti-apoptotic proteins of the Bcl-2 family that has shown promise in various preclinical tumour models. We here report a strong over-additive pro-apoptotic effect of ABT-737 and etoposide, vinblastine or paclitaxel but not 5-fluorouracil in cell lines from human RCC. ABT-737 showed very little activity as a single agent but killed RCC cells potently when anti-apoptotic Mcl-1 or, unexpectedly, A1 was targeted by RNAi. This potent augmentation required endogenous Noxa protein since RNAi directed against Noxa but not against Bim or Puma reduced apoptosis induction by the combination of ABT-737 and etoposide or vinblastine. At the level of mitochondria, etoposide-treatment had a similar sensitizing activity and allowed for ABT-737-induced release of cytochrome c. Chemotherapeutic drugs can overcome protection afforded by Mcl-1 and A1 through endogenous Noxa protein in RCC cells, and the combination of such drugs with ABT-737 may be a promising strategy in RCC. Strikingly, A1 emerged in RCC cell lines as a protein of similar importance as the well-established Mcl-1 in protection against apoptosis in these cells.

The development of CotA mediator cocktail system for dyes decolorization.

PubMed

Luo, S; Xie, T; Liu, Z; Sun, F; Wang, G

2018-05-01

The increasing use of dyes leads to serious environmental concerns, it is significant to explore eco-friendly and economic approaches for dye decolorization. This study aimed to develop mediator cocktail (AS and ABTS) for enhancing the capability of laccase-mediator system in the removal of dyes. By mediator screening, the mediators of ABTS and AS (ABTS, 2, 2'-azino-bis-(3-ethylbenzothiazo-thiazoline-6-sulphonic acid); AS, acetosyringone) were combined for dyes decolorization. The Box-Behnken Design and response surface analysis was performed to optimize experiment conditions. Comparing the CotA-ABTS-AS cocktail system with CotA-single mediator system showed that the coupling of ABTS and AS could increase the decolorization rate 15 times higher, save a third of the cost and shorten the reaction time by 50%. In addition, our studies revealed that sequential oxidation may occur in CotA-ABTS-AS system. Compared with CotA laccase-single mediator system, the CotA-ABTS-AS cocktail system showed advantages including higher efficiency, lower cost and shorter reaction time. This was the first report on the dyes decolorization by laccase mediator cocktail system. These results paved the curb for the application of laccase mediator system in various industrial processes. © 2018 The Society for Applied Microbiology.

Descriptive sensory analysis of Aceto Balsamico Tradizionale di Modena DOP and Aceto Balsamico Tradizionale di Reggio Emilia DOP.

PubMed

Zeppa, Giuseppe; Gambigliani Zoccoli, Mario; Nasi, Enrico; Masini, Giovanni; Meglioli, Giuseppe; Zappino, Matteo

2013-12-01

Aceto Balsamico Tradizionale (ABT) is a typical Italian vinegar available in two different forms: Aceto Balsamico Tradizionale di Modena DOP (ABTM) and Aceto Balsamico Tradizionale di Reggio Emilia DOP (ABTRE). ABT is obtained by alcoholic fermentation and acetic bio-oxidation of cooked grape must and aged at least 12 years in wooden casks and is known and sold around the world. Despite this widespread recognition, data on sensory characteristics of these products are very scarce. Therefore a descriptive analysis was conducted to define a lexicon for the ABT sensory profile and to create a simple, stable and reproducible synthetic ABT for training panellists. A lexicon of 20 sensory parameters was defined and validated and a synthetic ABT was prepared as standard reference. Simple standards for panellist training were also defined and the sensory profiles of ABTM and ABTRE were obtained. The obtained results confirm that descriptive analysis can be used for the sensory characterisation of ABT and that the sensory profiles of ABTM and ABTRE are very different. Furthermore, the results demonstrate that a lexicon and proper standard references are essential for describing the sensory qualities of ABT both for technical purposes and to protect the product from commercial fraud. © 2013 Society of Chemical Industry.

Improved production of poly-γ-glutamic acid by Bacillus subtilis D7 isolated from Doenjang, a Korean traditional fermented food, and its antioxidant activity.

PubMed

Lee, Na-Ri; Lee, Sang-Mee; Cho, Kwang-Sik; Jeong, Seong-Yun; Hwang, Dae-Youn; Kim, Dong-Seob; Hong, Chang-Oh; Son, Hong-Joo

2014-06-01

The objectives of this study was to improve poly-γ-glutamic acid (γ-PGA) production by Bacillus subtilis D7 isolated from a Korean traditional fermented food and to assess its antioxidant activity for applications in the cosmetics and pharmaceutical industries. Strain D7 produced γ-PGA in the absence of L-glutamic acid, indicating L-glutamic acid-independent production. However, the addition of L-glutamic acid increased γ-PGA production. Several tricarboxylic acid cycle intermediates and amino acids could serve as the metabolic precursors for γ-PGA production, and the addition of pyruvic acid and D-glutamic acid to culture medium improved the yield of γ-PGA markedly. The maximum yield of γ-PGA obtained was 24.93 ± 0.64 g/l in improved medium, which was about 5.4-fold higher than the yield obtained in basal medium. γ-PGA was found to have 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (46.8 ± 1.5 %), hydroxyl radical scavenging activity (52.0 ± 1.8 %), 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonate (ABTS) radical scavenging activity (42.1 ± 1.8 %), nitric oxide scavenging activity (35.1 ± 1.3 %), reducing power (0.304 ± 0.008), and metal chelating activity (91.3 ± 3.5 %). These results indicate that γ-PGA has a potential use in the food, cosmetics, and biomedical industries for the development of novel products with radical scavenging activity. As far as we are aware, this is the first report to describe the antioxidant activityof γ-PGA produced by bacteria.

Effect of hydroalcoholic extract of Aegle marmelos fruit on radical scavenging activity and exercise-endurance capacity in mice.

PubMed

Nallamuthu, Ilaiyaraja; Tamatam, Anand; Khanum, Farhath

2014-05-01

Aegle marmelos L. Corr (Rutaceae) is an important Indian Ayurvedic medicinal plant used for the treatment of various ailments. However, little information is available on the anti-fatigue properties of its fruit. Evaluation of the physical endurance and exercise-induced oxidative stress modulating properties of A. marmelos fruit in mice. Radical scavenging activity of the fruit hydroalcoholic extract was evaluated using in vitro systems. The extract was further evaluated for its endurance-enhancing properties at three oral doses (100, 200 and 400 mg/kg b.wt) in BALB/c mice for 21 d using a swimming test. The extract exhibited significant scavenging activity against DPPH (IC₅₀, 351 ± 37 µg/ml) and ABTS radicals (IC₅₀, 228 ± 25 µg/ml), respectively, with the polyphenol content of 95 µg/mg extract. It also inhibited AAPH radical-induced oxidation of biomolecules such as BSA protein (63%), plasmid DNA (81%) and lipids (80.5%). Administration of extract resulted in an increase in the duration of swimming time to exhaustion by 23.4 and 47.5% for medium and higher doses, respectively. The extract significantly normalized the fatigue-related biochemical parameters and also down-regulated the swim stress-induced over-expression of heat shock protein-70 and up-regulated the skeletal muscle metabolic regulators (GLUT-4 and AMPK1-α) by 2- and 3-fold, respectively, at the higher dose in muscle tissues. Our study demonstrates the anti-fatigue properties of A. marmelos fruit, most probably manifested by delaying the accumulation of serum lactic acid, increasing the fat utilization and up-regulating the skeletal muscle metabolic regulators.

Preparation of A-type proanthocyanidin dimers from peanut skins and persimmon pulp and comparison of the antioxidant activity of A-type and B-type dimers.

PubMed

Dong, Xiao-qian; Zou, Bo; Zhang, Ying; Ge, Zhen-zhen; Du, Jing; Li, Chun-mei

2013-12-01

We have established a simple method for preparing large quantities of A-type dimers from peanut skin and persimmon for further structure-activity relationship study. Peanut skins were defatted with hexane and oligomeric proanthocyanidins were extracted from it with 20% of methanol, and the extract was fractionated with ethyl acetate. Persimmon tannin was extracted from persimmon with methanol acidified with 1% hydrochloric acid, after removing the sugar and small phenols, the high molecular weight persimmon tannin was partially cleaved with 6.25% hydrochloric acid in methanol. The ethyl acetate fraction from peanut skins and persimmon tannin cleaved products was chromatographed on AB-8 macroporous resin followed by Toyopearl HW-50F resin to yield about 378.3mg of A-type (epi)catechin (EC) dimer from 1 kg dry peanut skins and 34.3mg of A-type (epi)catechin-3-O-gallate (ECG) dimer and 37.7 mg of A-type (epi)gallocatechin-3-O-gallate (EGCG) dimer from 1 kg fresh persimmon fruit. The antioxidant properties of the A-type and B-type dimers were compared in five different assays, namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical, hydroxyl radical, lipid peroxidation in mice liver homogenate and erythrocyte hemolysis in rat blood. Our results showed that both A-type and B-type dimers showed high antioxidant potency in a dose-dependent manner. In general, B-type dimers showed higher radical scavenging potency than A-type ones with the same subunits in aqueous systems. But in tissue or lipid systems, A-type dimers showed similar or even higher antioxidant potency than B-type ones. © 2013.

Evaluation of radical scavenging activity, intestinal cell viability and antifungal activity of Brazilian propolis by-product.

PubMed

de Francisco, Lizziane; Pinto, Diana; Rosseto, Hélen; Toledo, Lucas; Santos, Rafaela; Tobaldini-Valério, Flávia; Svidzinski, Terezinha; Bruschi, Marcos; Sarmento, Bruno; Oliveira, M Beatriz P P; Rodrigues, Francisca

2018-03-01

Propolis is a natural adhesive resinous compound produced by honeybees to protect hives from bacteria and fungi, being extremely expensive for food industry. During propolis production, a resinous by-product is formed. This resinous waste is currently undervalued and underexploited. Accordingly, in this study the proximate physical and chemical quality, as well as the antioxidant activity, radical scavenging activity and cell viability of this by-product were evaluated and compared with propolis in order to boost new applications in food and pharmaceutical industries. The results revealed that the by-product meets the physical and chemical quality standards expected and showed that the propolis waste contains similar amounts of total phenolic content (TPC) and total flavonoid content (TFC) to propolis. Also, a good scavenging activity against reactive oxygen and nitrogen species (ROS and RNS, respectively) determined by the assays of superoxide anion radical (O 2 - ), hydrogen peroxide (H 2 O 2 ), hypochlorous acid (HOCl), nitric oxide (NO) and peroxyl radical (ROO) were determined. Linear positive correlations were established between the TPC of both samples and the antioxidant activity evaluated by three different methods (DPPH, ABTS and FRAP assays). The extracts were also screened for cell viability assays in two different intestinal cell lines (HT29-MTX and Caco-2), showing a viability concentration-dependent. Similarly, the Artemia salina assay, used to assess toxicity, demonstrated the concentration influence on results. Finally, the antifungal activity against ATCC species of Candida was demonstrated. These results suggest that propolis by-product can be used as a new rich source of bioactive compounds for different areas, such as food or pharmaceutical. Copyright © 2017 Elsevier Ltd. All rights reserved.

Profiling of anthocyanins in transgenic purple-fleshed sweet potatoes by HPLC-MS/MS.

PubMed

Ge, Jingqiu; Hu, Yijie; Wang, Hongxia; Huang, Yuanshe; Zhang, Peng; Liao, Zhihua; Chen, Min

2017-11-01

Anthocyanins in purple-fleshed sweet potato (PSP) are beneficial to human health. The leaf color (Lc) gene is a transcription factor involved in regulating anthocyanin biosynthesis. The anthocyanin profiles of wild-type PSP of Ayamurasaki and its three Lc-transgenic lines were investigated by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). In vitro antioxidant activities of wild-type and Lc-transgenic lines, including reducing power activity, DPPH radical scavenging activity, hydroxyl radical scavenging activity, linoleic acid autoxidation inhibition activity, ABTS free radical scavenging activity and oxygen radical absorbance capacity activity, were measured. The results showed that the total anthocyanin contents increased 1.5-1.9 times in three transgenic lines compared with that in wild-type PSP. Seventeen anthocyanins were found in wild-type PSP, while 19 in Lc-transgenic lines including cyanidin-based, peonidin-based and pelargonidin-based anthocyanins. Three pelargonidin-based anthocyanins were detected in three Lc-transgenic lines. Among them, the relative contents of cyanidin-based and pelargonidin-based anthocyanins increased 1.9-2.0 and 3.4-4.5 times respectively, while peonidin-based anthocyanins decreased 1.8-1.9 times in Lc-transgenic lines, compared with wild-type PSP. PSP from wild-type Ayamurasaki and three Lc-transgenic lines exhibited potent antioxidant activities, whereas there was no distinct difference among them. The transgene Lc significantly increased the content of total anthocyanins and remarkably changed the anthocyanin profiles in Ayamurasaki. Such novel and high content of anthocyanins obtained in the Lc-transgenic lines with potent antioxidant activities may provide unique functional products with potential helpful for human health. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Scavenging of free-radical metabolites of aniline xenobiotics and drugs by amino acid derivatives: toxicological implications of radical-transfer reactions.

PubMed

Michail, Karim; Baghdasarian, Argishti; Narwaley, Malyaj; Aljuhani, Naif; Siraki, Arno G

2013-12-16

We investigated a novel scavenging mechanism of arylamine free radicals by poly- and monoaminocarboxylates. Free radicals of arylamine xenobiotics and drugs did not react with oxygen in peroxidase-catalyzed reactions; however, they showed marked oxygen uptake in the presence of an aminocarboxylate. These free-radical intermediates were identified using the spin trap 5,5-dimethyl-1-pyrroline-N-oxide (DMPO) and electron paramagnetic resonance (EPR) spectrometry. Diethylenetriaminepentaacetic acid (DTPA), a polyaminocarboxylate, caused a concentration-dependent attenuation of N-centered radicals produced by the peroxidative metabolism of arylamines with the subsequent formation of secondary aliphatic carbon-centered radicals stemming from the cosubstrate molecule. Analogously, N,N-dimethylglycine (DMG) and N-methyliminodiacetate (MIDA), but not iminodiacetic acid (IDA), demonstrated a similar scavenging effect of arylamine-derived free radicals in a horseradish peroxidase/H2O2 system. Using human promyelocytic leukemia (HL-60) cell lysate as a model of human neutrophils, DTPA, MIDA, and DMG readily reduced anilinium cation radicals derived from the arylamines and gave rise to the corresponding carbon radicals. The rate of peroxidase-triggered polymerization of aniline was studied as a measure of nitrogen-radical scavenging. Although, IDA had no effect on the rate of aniline polymerization, this was almost nullified in the presence of DTPA and MIDA at half of the molar concentration of the aniline substrate, whereas a 20 molar excess of DMPO caused only a partial inhibition. Furthermore, the yield of formaldehyde, a specific reaction endproduct of the oxidation of aminocarboxylates by aniline free-radical metabolites, was quantitatively determined. Azobenzene, a specific reaction product of peroxidase-catalyzed free-radical dimerization of aniline, was fully abrogated in the presence of DTPA, as confirmed by GC/MS. Under aerobic conditions, a radical-transfer reaction is proposed between aminocarboxylates and arylamine free radicals via the carboxylic group-linked tertiary nitrogen of the deprotonated amino acid derivatives. These findings may have significant implications for the biological fate of arylamine xenobiotic and drug free-radical metabolites.

Evaluation of enzymatically treated Artemisia annua L. on growth performance, meat quality, and oxidative stability of breast and thigh muscles in broilers.

PubMed

Wan, X L; Song, Z H; Niu, Y; Cheng, K; Zhang, J F; Ahmad, H; Zhang, L L; Wang, T

2017-04-01

An experiment was conducted to evaluate the effects of including enzymatically treated Artemisia annua L. (EA) in broiler diets on growth performance, meat quality, and oxidative stability of breast and thigh muscles. A total of 256 one-d-old Arbor Acres broiler chicks were randomly allotted into four groups with eight replicates of eight birds each. Broilers in the four groups were offered basal diet supplemented with 0.0, 0.5, 1.0, and 1.5 g/kg EA during the 42-d experiment, respectively. The ADG, ADFI, and feed/gain ratio (F:G) were measured at 42 d of age. Breast and thigh muscle samples from eight birds per treatment were obtained at 42 d to determine meat quality, free radical scavenging activity, and lipid peroxidation. All treatment groups had similar ADG, ADFI, and F:G during the 42 d experiment (P > 0.05). Drip loss at 24 h and shearing force of breast muscle were linearly (P < 0.05) and quadratically (P < 0.05) decreased by EA addition. The drip loss at 24 h and 48 h, cooking loss and shearing force of thigh muscle followed the same fashion. The supplementation of EA quadratically increased 2, 2-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) (P = 0.004) and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) (P = 0.035) free radical scavenging activities in breast muscle, and linearly (P < 0.05) and quadratically (P < 0.05) increased ABTS and DPPH scavenging activities of thigh muscle. Increasing levels of EA linearly (P < 0.05) or quadratically (P < 0.05) or both decreased the malondialdehyde (MDA) concentrations in breast and thigh muscle samples during 15 d of storage at 4°C. The results indicated that EA supplementation improved meat quality and oxidative stability of breast and thigh muscles in broilers. The inclusion level of 1.0 g/kg EA in broiler diet was recommended. © 2016 Poultry Science Association Inc.

Antibacterial and antioxidant properties of the methanol extracts of the leaves and stems of Calpurnia aurea

PubMed Central

Adedapo, Adeolu A; Jimoh, Florence O; Koduru, Srinivas; Afolayan, Anthony J; Masika, Patrick J

2008-01-01

Background In South Africa, Calpurnia aurea (Ait.) Benth is used to destroy lice and to relieve itches, to destroy maggots and to treat allergic rashes, particularly those caused by caterpillars. Antioxidants play an important role protecting against damage by reactive oxygen species. Plants containing flavonoids have been reported to possess strong antioxidant properties. Methods The antibacterial, antioxidant activities and phenolic contents of the methanol extracts of the leaves and stems of Calpurnia aurea were evaluated using in vitro standard methods. Spectrophotometry was the basis for the determinations of total phenol, total flavonoids, flavonols, and proanthocyanidins. Tannins, quercetin and catechin equivalents were used for these parameters. The antioxidant activities of the stem extract of Calpurnia aurea were determined by ABTS, DPPH, and ferrous reducing antioxidant property (FRAP) methods. Laboratory isolates of 10 bacteria species which included five Gram-positive and five Gram-negative strains were used to assay for antibacterial activity of this plant. Results The results from this study showed that the antioxidant activities of the stem extract of Calpurnia aurea as determined by the total phenol, flavonoids, and FRAP methods were higher than that of the leaves. On the other hand, the leaf extract of the plant has higher level of total flavonols and proanthocyanidins. The leaf extract also has higher radical scavenging activity as shown in 1, 1-Diphenyl-2-picrylhydrazyl (DPPH), and 2,2¿-azinobis-3- ethylbenzothiazoline-6-sulfonic acid (ABTS) assay. The leaf extract showed activity against seven of the bacterial organisms. Conclusion The results from this study indicate that the leaves and stem extracts of Calpurnia aurea possess antioxidant properties and could serve as free radical inhibitors or scavenger or, acting possibly as primary antioxidants. Although, the antibacterial properties of Calpurnia aurea are not as effective as the standard drugs- Chloramphenicol and Streptomycin, they still possess some activity against bacterial strains used in this study. Calpurnia aurea may therefore be a good candidate for functional foods as well as pharmaceutical plant-based products. PMID:18803865

Hepatoprotective effects and antioxidant, antityrosinase activities of phloretin and phloretin isonicotinyl hydrazone.

PubMed

Zuo, Ai-Ren; Yu, Yan-Ying; Shu, Qing-Long; Zheng, Li-Xiang; Wang, Xiao-Min; Peng, Shu-Hong; Xie, Yan-Fei; Cao, Shu-Wen

2014-06-01

Acute liver damage is primarily induced by one of several causes, among them viral exposure, alcohol consumption, and drug and immune system issues. Agents with the ability to inhibit tyrosinase and protect against DNA damage caused by reactive oxygen species (ROS) may be therapeutically useful for the prevention or treatment of ROS-related diseases. This investigation examined the hepatoprotective effects of phloretin and phloretin isonicotinyl hydrazone (PIH) on d-galactosamine (D-GalN)-induced acute liver damage in Kunming mice, as well as the possible mechanisms. The serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), γ-glutamyl transferase (γ-GT), alkaline phosphatase (ALP), and total bilirubin (TB) as well as the histopathological changes in mouse liver sections were determined. The antioxidant effects of phloretin, quercetin, and PIH on lipid peroxidation in rat liver mitochondria in vitro, 1,1-diphenyl-2-picrylhydrazyl (DPPH) or 2,2-azino-bis-(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) free radical scavenging activity in vitro, and supercoiled pBR322 plasmid DNA were confirmed. The experiment also examined the antityrosinase activity, inhibition type, and inhibition constant of phloretin and PIH. Phloretin, quercetin, or PIH significantly prevented the increase in serum ALT, AST, γ-GT, ALP, and TB in acute liver damage induced by D-GalN, and produced a marked reduction in the histopathological hepatic lesions. Phloretin, quercetin, or PIH also exhibited antioxidant effects on lipid peroxidation in rat liver mitochondria in vitro, DPPH or ABTS free radical scavenging activity in vitro, and supercoiled pBR322 plasmid DNA. Phloretin, quercetin, or PIH also exhibited good antityrosinase activity. To the best of our knowledge, this was the first study of the hepatoprotective effects of phloretin and PIH on D-GalN-induced acute liver damage in Kunming mice as well as the possible mechanisms. This was also the first study of the lipid peroxidation inhibition activity of phloretin and PIH in liver mitochondria induced by the Fe(2+)/vitamin C (Vc) system in vitro, the protective effects on supercoiled pBR322 plasmid DNA, and the antityrosinase activity of phloretin and PIH. Copyright © 2014. Published by Elsevier B.V.

Effect of Alpinia zerumbet components on antioxidant and skin diseases-related enzymes

PubMed Central

2012-01-01

Background The skin is chronically exposed to endogenous and environmental pro-oxidant agents, leading to the harmful generation of reactive oxygen species. Antioxidant is vital substances which possess the ability to protect the body from damage cause by free radicals induce oxidative stress. Alpinia zerumbet, a traditionally important economic plant in Okinawa, contains several interesting bioactive constituents and possesses health promoting properties. In this regard, we carried out to test the inhibitory effect of crude extracts and isolated compounds from A. zerumbet on antioxidant and skin diseases-related enzymes. Methods The antioxidant activities were examined by DPPH, ABTS and PMS-NADH radical scavenging. Collagenase, elastase, hyaluronidase and tyrosinase were designed for enzymatic activities to investigate the inhibitory properties of test samples using a continuous spectrophotometric assay. The inhibitory capacity of test samples was presented at half maximal inhibitory concentration (IC50). Results The results showed that aqueous extract of the rhizome was found to have greater inhibitory effects than the others on both of antioxidant and skin diseases-related enzymes. Furthermore, 5,6-dehydrokawain (DK), dihydro-5,6-dehydrokawain (DDK) and 8(17),12-labdadiene-15,16-dial (labdadiene), isolated from rhizome, were tested for antioxidant and enzyme inhibitions. We found that DK showed higher inhibitory activities on DPPH, ABTS and PMS-NADH scavenging (IC50 = 122.14 ± 1.40, 110.08 ± 3.34 and 127.78 ± 4.75 μg/ml, respectively). It also had stronger inhibitory activities against collagenase, elastase, hyaluronidase and tyrosinase (IC50 = 24.93 ± 0.97, 19.41 ± 0.61, 19.48 ± 0.24 and 76.67 ± 0.50 μg/ml, respectively) than DDK and labdadiene. Conclusion Our results indicate that the rhizome aqueous extract proved to be the source of bioactive compounds against enzymes responsible for causing skin diseases. Moreover, DK could be used as a potent inhibitor and be further exploited to be used in anti-skin disease formulations. PMID:22827920

Chlorophytum borivilianum as potential terminator of free radicals in various in vitro oxidation systems.

PubMed

Visavadiya, Nishant P; Soni, Badrish; Dalwadi, Nirav; Madamwar, Datta

2010-04-01

Chlorophytum borivilianum is a very popular herb in traditional Indian medicine and used as a potent "Rasayana" drug in "Ayurveda" as a rejuvenator. Currently, a large body of evidence supports the key role of free radicals in diverse pathological conditions such as aging and atherosclerosis. The present investigation essentially focuses on the comprehensive account of in vitro antioxidant activity exerted by C.borivilianum root extracts (i.e., aqueous and ethanolic), to clarify the pharmacological antagonism of chemicals/metals-mediated oxidation. Graded-dose (25 to 1000 microg/ml) of aqueous extract exhibited higher antioxidant potency as evidenced by powerful nitric oxide, superoxide, hydroxyl, DPPH and ABTS(*+) radicals scavenging activity along with reducing capacity (Fe(3+)/ferricyanide complex and FRAP assays), metal chelating ability, as well as markedly suppressed the lipid peroxidation in mitochondrial fractions as compared to ethanolic extract. Further, aqueous extract significantly decreased (P < 0.05) copper-mediated human serum and kinetics of LDL oxidation, as demonstrated by prolongation of lag phase time with decline of oxidation rate, conjugated dienes, lipid hydroperoxides and thiobarbituric acid reactive substances. In addition, the total polyphenol and flavonoid contents of aqueous extract were higher than that of ethanolic extract, which indicated a positive correlation between antioxidant activity and contents of total phenols. The IC(50) values of both extracts were also compared with appropriate antioxidant standards. Overall, aqueous extract of C.borivilianum root has significant powerful antioxidant activity and may favorably affect atherosclerosis risk status by reducing LDL oxidation susceptibility.

In Vitro Ion Chelating, Antioxidative Mechanism of Extracts from Fruits and Barks of Tetrapleura tetraptera and Their Protective Effects against Fenton Mediated Toxicity of Metal Ions on Liver Homogenates

PubMed Central

Moukette, Bruno Moukette; Pieme, Anatole Constant; Biapa, Prosper Cabral Nya; Njimou, Jacques Romain; Bravi, Marco; Yonkeu Ngogang, Jeanne

2015-01-01

The aim of the present study was to investigate the antioxidant activity and protective potential of T. tetraptera extracts against ion toxicity. The antioxidant activity of the extracts was investigated spectrophotometrically against several radicals (1,1-diphenyl-2-picrylhydrazyl (DPPH•), 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS•), hydroxyl radical (HO•), and nitric oxide (NO•)), followed by the ferric reducing power, total phenols, flavonoid, and flavonol contents. The effects of the extracts on catalase (CAT), superoxide dismutase (SOD), and peroxidase activities were also determined using the standard methods as well as the polyphenol profile using HPLC. The results showed that the hydroethanolic extract of T. tetraptera (CFH) has the lowest IC50 value with the DPPH, ABTS, OH, and NO radicals. The same extract also exhibited the significantly higher level of total phenols (37.24 ± 2.00 CAE/g dried extract); flavonoids (11.36 ± 1.88 QE/g dried extract); and flavonols contents (3.95 ± 0.39 QE/g dried extract). The HPLC profile of T. tetraptera revealed that eugenol (958.81 ± 00 mg/g DW), quercetin (353.78 ± 00 mg/g DW), and rutin (210.54 ± 00 mg/g DW) were higher in the fruit than the bark extracts. In conclusion, extracts from T. tetraptera may act as a protector against oxidative mediated ion toxicity. PMID:26356679

Ramalina capitata (Ach.) Nyl. acetone extract: HPLC analysis, genotoxicity, cholinesterase, antioxidant and antibacterial activity.

PubMed

Zrnzevic, Ivana; Stankovic, Miroslava; Stankov Jovanovic, Vesna; Mitic, Violeta; Dordevic, Aleksandra; Zlatanovic, Ivana; Stojanovic, Gordana

2017-01-01

In the present investigation, effects of Ramalina capitata acetone extract on micronucleus distribution on human lymphocytes, on cholinesterase activity and antioxidant activity (by the CUPRAC method) were examined, for the first time as well as its HPLC profile. Additionally, total phenolic compounds (TPC), antioxidant properties (estimated via DPPH, ABTS and TRP assays) and antibacterial activity were determined. The predominant phenolic compounds in this extract were evernic, everninic and obtusatic acids. Acetone extract of R. capitata at concentration of 2 μg mL -1 decreased a frequency of micronuclei (MN) for 14.8 %. The extract reduces the concentration of DPPH and ABTS radicals for 21.2 and 36.1 % (respectively). Values for total reducing power (TRP) and cupric reducing capacity (CUPRAC) were 0.4624 ± 0.1064 μg ascorbic acid equivalents (AAE) per mg of dry extract, and 6.1176 ± 0.2964 μg Trolox equivalents (TE) per mg of dry extract, respectively. The total phenol content was 670.6376 ± 66.554 μg galic acid equivalents (GAE) per mg of dry extract. Tested extract at concentration of 2 mg mL -1 exhibited inhibition effect (5.2 %) on pooled human serum cholinesterase. The antimicrobial assay showed that acetone extract had inhibition effect towards Gram-positive strains. The results of manifested antioxidant activity, reducing the number of micronuclei in human lymphocytes, and antibacterial activity recommends R. capitata extract for further in vivo studies.

Antioxidative activities of 62 wild mushrooms from Nepal and the phenolic profile of some selected species.

PubMed

Tamrakar, Sonam; Tran, Hai Bang; Nishida, Marina; Kaifuchi, Satoru; Suhara, Hiroto; Doi, Katsumi; Fukami, Katsuya; Parajuli, Gopal Prasad; Shimizu, Kuniyoshi

2016-10-01

Mushrooms have garnered immense popularity for their nutritional as well as medicinal values. The therapeutic potential of mushrooms in Nepal, a country well known for its biodiversity and natural medicinal resources, remains largely unstudied. Therefore, this study attempts to unveil the antioxidative properties of Nepalese wild mushrooms. Sixty-two wild mushroom samples were collected from several forests in different parts of Nepal. Ethanol and water extracts of the dried samples were tested for their antioxidative activities using total phenolic content (TPC), oxygen radical absorbance capacity (ORAC) assay, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and reducing power (RP) assays. Ethanol extracts of samples belonging to the order Hymenochaetales showed significantly high activity in all the assays. Inonotus clemensiae had an exceptionally high TPC of 643.2 mg gallic acid equivalent (GAE)/g extract and also exhibited the lowest EC50 values in DPPH (0.081 mg/mL), ABTS (0.409 mg/mL), and EC0.5 value in reducing power (RP; 0.031 mg/mL) assays. High-performance liquid chromatography (HPLC) analysis of the top ten samples with the highest TPC was done to identify the phenolic compounds in the extracts, followed by liquid chromatography-mass spectrometry (LC-MS) analysis for some unknown compounds. These findings highlight the very strong antioxidative activity of Nepalese mushrooms, and paves the way for further research to explore their economic potential.

DOE Office of Scientific and Technical Information (OSTI.GOV)

Carraher, Jack M.; Bakac, Andreja

Laser flash photolysis of 4-benzoylpyridine N-oxide (BPyO) at 308 nm in aqueous solutions generates a triplet excited state 3BPyO* that absorbs strongly in the visible, λ max 490 and 380 nm. 3BPyO* decays with the rate law k decay/s -1 = (3.3 ± 0.9) × 10 4 + (1.5 ± 0.2) × 10 9 [BPyO] to generate a mixture of isomeric hydroxylated benzoylpyridines, BPy(OH), in addition to small amounts of oxygen atoms, O( 3P). Molecular oxygen quenches 3BPyO*, k Q = 1.4 × 10 9 M -1 s -1, but the yields of O( 3P) increase in O 2-saturated solutionsmore » to 36%. Other triplet quenchers have a similar effect, which rules out the observed 3BPyO* as a source of O( 3P). It is concluded that O( 3P) is produced from either 1BPyO* or a short-lived, unobserved, higher energy triplet generated directly from 1BPyO*. 3BPyO* is reduced by Fe 2+ and by ABTS 2- to the radical anion BPyO .- which exhibits a maximum at 510 nm, ε = 2200 M -1 cm -1. The anion engages in back electron transfer with ABTS .- with k = 1.7 × 109 M -1 s -1. The same species can be generated by reducing ground state BPyO with .C(CH 3) 2OH. The photochemistry of BPyO in acetonitrile is similar to that in aqueous solutions.« less

Development and validation of an algorithm to establish a total antioxidant capacity database of the US diet.

PubMed

Floegel, Anna; Kim, Dae-Ok; Chung, Sang-Jin; Song, Won O; Fernandez, Maria Luz; Bruno, Richard S; Koo, Sung I; Chun, Ock K

2010-09-01

Estimation of total antioxidant intake is the first step to investigate the protective effects of antioxidants on oxidative stress-mediated disease. The present study was designed to develop an algorithm to estimate total antioxidant capacity (TAC) of the US diet. TAC of individual antioxidants and 50 popular antioxidant-rich food items in the US diet were determined by 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) assay and the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Theoretical TAC of foods was calculated as the sum of individual antioxidant capacities of compounds. The top 10 TAC food items in the US diet according to standard serving size were blueberry > plum > green tea > strawberry > green tea (decaffeinated) > red wine > grape juice > black tea > cherry > grape. Major contributors to TAC were the total phenolic content (r = 0.952, P < 0.001) and flavonoid content (r = 0.827, P < 0.001) of 50 foods. Theoretical TAC was positively correlated to experimental TAC of 50 foods determined by the ABTS assay (r = 0.833, P < 0.001) and the DPPH assay (r = 0.696, P < 0.001), and to TAC from the USDA database for the oxygen radical absorbance capacity (r = 0.484, P = 0.001, n = 44). The TAC database of the US diet has been established and validated. In future studies, TAC of the US diet can be linked to biomarkers of chronic disease.

Thai plants with high antioxidant levels, free radical scavenging activity, anti-tyrosinase and anti-collagenase activity.

PubMed

Chatatikun, Moragot; Chiabchalard, Anchalee

2017-11-09

Ultraviolet radiation from sunlight induces overproduction of reactive oxygen species (ROS) resulting in skin photoaging and hyperpigmentation disorders. Novel whitening and anti-wrinkle compounds from natural products have recently become of increasing interest. The purpose of this study was to find products that reduce ROS in 14 Thai plant extracts. To determine total phenolic and flavonoid content, antioxidant activity, anti-tyrosinase activity and anti-collagenase activity, we compared extracts of 14 Thai plants prepared using different solvents (petroleum ether, dichloromethane and ethanol). Antioxidant activities were determined by DPPH and ABTS assays. Total phenolic content of the 14 Thai plants extracts was found at the highest levels in ethanol followed by dichloromethane and petroleum ether extracts, respectively, while flavonoid content was normally found in the dichloromethane fraction. Scavenging activity ranged from 7 to 99% scavenging as assessed by DPPH and ABTS assays. The ethanol leaf extract of Ardisia elliptica Thunb. had the highest phenolic content, antioxidant activity and collagenase inhibition, while Cassia alata (L.) Roxb. extract had the richest flavonoid content. Interestingly, three plants extracts, which were the ethanolic fractions of Annona squamosa L., Ardisia elliptica Thunb. and Senna alata (L.) Roxb., had high antioxidant content and activity, and significantly inhibited both tyrosinase and collagenase. Our finding show that the ethanol fractions of Annona squamosa L., Ardisia elliptica Thunb. and Senna alata (L.) Roxb. show promise as potential ingredients for cosmetic products such as anti-wrinkle agents and skin whitening products.

In Vitro Pharmacodynamic Activities of ABT-492, a Novel Quinolone, Compared to Those of Levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis

PubMed Central

Gunderson, Shana M.; Hayes, Robert A.; Quinn, John P.; Danziger, Larry H.

2004-01-01

ABT-492 is a novel quinolone with potent activity against gram-positive, gram-negative, and atypical pathogens, making this compound an ideal candidate for the treatment of community-acquired pneumonia. We therefore compared the in vitro pharmacodynamic activity of ABT-492 to that of levofloxacin, an antibiotic commonly used for the treatment of pneumonia, through MIC determination and time-kill kinetic analysis. ABT-492 demonstrated potent activity against penicillin-sensitive, penicillin-resistant, and levofloxacin-resistant Streptococcus pneumoniae strains (MICs ranging from 0.0078 to 0.125 μg/ml); β-lactamase-positive and β-lactamase-negative Haemophilus influenzae strains (MICs ranging from 0.000313 to 0.00125 μg/ml); and β-lactamase-positive and β-lactamase-negative Moraxella catarrhalis strains (MICs ranging from 0.001 to 0.0025 μg/ml), with MICs being much lower than those of levofloxacin. Both ABT-492 and levofloxacin demonstrated concentration-dependent bactericidal activities in time-kill kinetics studies at four and eight times the MIC with 10 of 12 bacterial isolates exposed to ABT-492 and with 12 of 12 bacterial isolates exposed to levofloxacin. Sigmoidal maximal-effect models support concentration-dependent bactericidal activity. The model predicts that 50% of maximal activity can be achieved with concentrations ranging from one to two times the MIC for both ABT-492 and levofloxacin and that near-maximal activity (90% effective concentration) can be achieved at concentrations ranging from two to five times the MIC for ABT-492 and one to six times the MIC for levofloxacin. PMID:14693540

In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.

PubMed

Gunderson, Shana M; Hayes, Robert A; Quinn, John P; Danziger, Larry H

2004-01-01

ABT-492 is a novel quinolone with potent activity against gram-positive, gram-negative, and atypical pathogens, making this compound an ideal candidate for the treatment of community-acquired pneumonia. We therefore compared the in vitro pharmacodynamic activity of ABT-492 to that of levofloxacin, an antibiotic commonly used for the treatment of pneumonia, through MIC determination and time-kill kinetic analysis. ABT-492 demonstrated potent activity against penicillin-sensitive, penicillin-resistant, and levofloxacin-resistant Streptococcus pneumoniae strains (MICs ranging from 0.0078 to 0.125 micro g/ml); beta-lactamase-positive and beta-lactamase-negative Haemophilus influenzae strains (MICs ranging from 0.000313 to 0.00125 micro g/ml); and beta-lactamase-positive and beta-lactamase-negative Moraxella catarrhalis strains (MICs ranging from 0.001 to 0.0025 micro g/ml), with MICs being much lower than those of levofloxacin. Both ABT-492 and levofloxacin demonstrated concentration-dependent bactericidal activities in time-kill kinetics studies at four and eight times the MIC with 10 of 12 bacterial isolates exposed to ABT-492 and with 12 of 12 bacterial isolates exposed to levofloxacin. Sigmoidal maximal-effect models support concentration-dependent bactericidal activity. The model predicts that 50% of maximal activity can be achieved with concentrations ranging from one to two times the MIC for both ABT-492 and levofloxacin and that near-maximal activity (90% effective concentration) can be achieved at concentrations ranging from two to five times the MIC for ABT-492 and one to six times the MIC for levofloxacin.

Lipid metabolism-related gene expression pattern of Atlantic bluefin tuna (Thunnus thynnus L.) larvae fed on live prey.

PubMed

Betancor, Mónica B; Ortega, Aurelio; de la Gándara, Fernando; Tocher, Douglas R; Mourente, Gabriel

2017-04-01

The present study is the first to evaluate lipid metabolism in first-feeding Atlantic bluefin tuna (ABT; Thunnus thynnus L.) larvae fed different live prey including enriched rotifers Brachionus plicatilis and Acartia sp. copepod nauplii from 2 days after hatch. Understanding the molecular basis of lipid metabolism and regulation in ABT will provide insights to optimize diet formulations for this high-value species new to aquaculture. To this end, we investigated the effect of dietary lipid on whole larvae lipid class and fatty acid compositions and the expression of key genes involved in lipid metabolism in first feeding ABT larvae fed different live prey. Additionally, the expression of lipid metabolism genes in tissues of adult broodstock ABT was evaluated. Growth and survival data indicated that copepods were the best live prey for first feeding ABT and that differences in growth performance and lipid metabolism observed between larvae from different year classes could be a consequence of broodstock nutrition. In addition, expression patterns of lipid metabolic genes observed in ABT larvae in the trials could reflect differences in lipid class and fatty acid compositions of the live prey. The lipid nutritional requirements, including essential fatty acid requirements of larval ABT during the early feeding stages, are unknown, and the present study represents a first step in addressing these highly relevant issues. However, further studies are required to determine nutritional requirements and understand lipid metabolism during development of ABT larvae and to apply the knowledge to the commercial culture of this iconic species.

Prospective study of thrombospondin-1 mimetic peptides, ABT-510 and ABT-898, in dogs with soft tissue sarcoma.

PubMed

Sahora, A I; Rusk, A W; Henkin, J; McKeegan, E M; Shi, Y; Khanna, C

2012-01-01

Exposure to anti-angiogenic thrombospondin-1 (TSP-1) mimetic peptides (MPs) has resulted in sporadic anti-tumor activity in humans and dogs. Novel TSP-1 MPs formulations will be safe, tolerated, and clinically active in soft tissue sarcoma (STS) in dogs. Sixty-two client-owned dogs with measurable STS were enrolled, excluding hemangiosarcoma. A prospective, single agent, multicenter, open-label study assessing ABT-510 bolus, ABT-898 bolus, or ABT-898 depot formulations of TSP-1 in dogs. Endpoints included tolerability, antitumor activity, and the assessment of ability of clinical covariates and circulating endothelial cells (CEC) concentration to predict tumor response. Two non-dose-limiting toxicoses possibly attributed to treatment were observed (keratitis and osteoarthritis). Antitumor activity (10/44 = 23% responses) was observed in study subjects who received treatment for >28 days (n = 44) including both partial (7) and minimal responses (3). Responses were disproportionately seen in dogs receiving ABT-898 formulations (9/28 = 32%) versus those receiving ABT-510 (1/16 = 6%; P < .045). Disease stabilization for >84 days was also documented (8/44 = 18%). Slow rates of tumor progression before study entry correlated with anti-tumor activity in treated dogs, whereas no significant association was found between changes in total CEC concentration and tumor response (P = .28) or time to progression (P = .42). Safely achieved antitumor activity was documented with TSP-1 MPs in dogs with STS. The most notable activity was achieved with the ABT-898 formulations. Copyright © 2012 by the American College of Veterinary Internal Medicine.

Endogenous Noxa Determines the Strong Proapoptotic Synergism of the BH3-Mimetic ABT-737 with Chemotherapeutic Agents in Human Melanoma Cells12

PubMed Central

Weber, Arnim; Kirejczyk, Zofia; Potthoff, Stephanie; Ploner, Christian; Häcker, Georg

2009-01-01

Human melanoma cells are very resistant to treatment with chemotherapeutic agents, and melanoma shows poor response to chemotherapeutic therapy. We describe a strong synergistic proapoptotic effect of the Bcl-2 family inhibitor ABT-737 and the standard antimelanoma drugs, namely, dacarbazine and fotemustine, and the experimental agent, imiquimod. Experiments with human melanoma cells, keratinocytes, and embryonic fibroblasts showed that all three agents activated the mitochondrial apoptosis pathway. ABT-737 on its own was ineffective in melanoma cells unless Mcl-1 was experimentally downregulated. However, ABT-737 strongly enhanced the proapoptotic activity of the chemotherapeutic drugs. Whereas cell death induction by all three agents involved the activity of both BH3-only proteins, Bim and Noxa, the combination with ABT-737 overcame the requirement for Bim. However, the synergism between ABT-737 and imiquimod or dacarbazine required endogenous Noxa, as demonstrated by experiments with Noxa-specific RNAi. Surprisingly, although Bim was activated, it was unable to replace Noxa. Studies of mitochondrial cytochrome c release using BH3 peptides confirmed that a main effect of dacarbazine, fotemustine, and imiquimod was to neutralize Mcl-1, thereby sensitizing mitochondria to the inhibition of other Bcl-2 family members through ABT-737. ABT-737 is thus a promising agent for combination therapy for human melanoma. Importantly, the efficacy of this therapy depends on endogenous Noxa, and the ability of chemotherapeutic drugs to activate Noxa may be a valuable predictor of their synergism with Bcl-2-targeting drugs. PMID:19412422

Anticancer compound ABT-263 accelerates apoptosis in virus-infected cells and imbalances cytokine production and lowers survival rates of infected mice.

PubMed

Kakkola, L; Denisova, O V; Tynell, J; Viiliäinen, J; Ysenbaert, T; Matos, R C; Nagaraj, A; Ohman, T; Kuivanen, S; Paavilainen, H; Feng, L; Yadav, B; Julkunen, I; Vapalahti, O; Hukkanen, V; Stenman, J; Aittokallio, T; Verschuren, E W; Ojala, P M; Nyman, T; Saelens, X; Dzeyk, K; Kainov, D E

2013-07-25

ABT-263 and its structural analogues ABT-199 and ABT-737 inhibit B-cell lymphoma 2 (Bcl-2), BCL2L1 long isoform (Bcl-xL) and BCL2L2 (Bcl-w) proteins and promote cancer cell death. Here, we show that at non-cytotoxic concentrations, these small molecules accelerate the deaths of non-cancerous cells infected with influenza A virus (IAV) or other viruses. In particular, we demonstrate that ABT-263 altered Bcl-xL interactions with Bcl-2 antagonist of cell death (Bad), Bcl-2-associated X protein (Bax), uveal autoantigen with coiled-coil domains and ankyrin repeats protein (UACA). ABT-263 thereby activated the caspase-9-mediated mitochondria-initiated apoptosis pathway, which, together with the IAV-initiated caspase-8-mediated apoptosis pathway, triggered the deaths of IAV-infected cells. Our results also indicate that Bcl-xL, Bcl-2 and Bcl-w interact with pattern recognition receptors (PRRs) that sense virus constituents to regulate cellular apoptosis. Importantly, premature killing of IAV-infected cells by ABT-263 attenuated the production of key pro-inflammatory and antiviral cytokines. The imbalance in cytokine production was also observed in ABT-263-treated IAV-infected mice, which resulted in an inability of the immune system to clear the virus and eventually lowered the survival rates of infected animals. Thus, the results suggest that the chemical inhibition of Bcl-xL, Bcl-2 and Bcl-w could potentially be hazardous for cancer patients with viral infections.

Curcumin enhances the antitumor effect of ABT-737 via activation of the ROS-ASK1-JNK pathway in hepatocellular carcinoma cells

PubMed Central

ZHENG, RUINIAN; YOU, ZHIJIAN; JIA, JUN; LIN, SHUNHUAN; HAN, SHUAI; LIU, AIXUE; LONG, HUIDONG; WANG, SENMING

2016-01-01

At present, the therapeutic treatment strategies for patients with hepatocellular carcinoma (HCC) remain unsatisfactory, and novel methods are urgently required to treat this disease. Members of the B cell lymphoma (Bcl)-2 family are anti-apoptotic proteins, which are commonly expressed at high levels in certain HCC tissues and positively correlate with the treatment resistance of patients with HCC. ABT-737, an inhibitor of Bcl-2 anti-apoptotic proteins, has been demonstrated to exhibit potent antitumor effects in several types of tumor, including HCC. However, treatment with ABT-737 alone also activates certain pro-survival signaling pathways, which attenuate the antitumor validity of ABT-737. Curcumin, which is obtained from Curcuma longa, is also an antitumor potentiator in multiple types of cancer. In the present study, the synergistic effect of curcumin and ABT-737 on HCC cells was investigated for the first time, to the best of our knowledge. It was found that curcumin markedly enhanced the antitumor effects of ABT-737 on HepG2 cells, which was partially dependent on the induction of apoptosis, according to western blot analysis and flow cytometric apoptosis analysis. In addition, the sustained activation of the ROS-ASK1-c-Jun N-terminal kinase pathway may be an important mediator of the synergistic effect of curcumin and ABT-737. Collectively, these results indicated that the combination of curcumin and ABT-737 can efficaciously induce the death of HCC cells, and may offer a potential treatment strategy for patients with HCC. PMID:26707143

Diastereoselective radical addition to γ-alkyl-α-methylene-γ-butyrolactams and the synthesis of a chiral pyroglutamic acid derivative.

PubMed

Yajima, Tomoko; Yoshida, Eriko; Hamano, Masako

2013-01-01

The cis- and trans-stereoselective radical additions to α-methylene-γ-alkyl- γ-lactams were investigated and the scope and limitation of the reaction were also revealed. This stereoselective radical reaction was used for synthesis of chiral pyroglutamic acid derivatives starting from a commercially available chiral amino acid.

Protection of ionizing radiation-induced cytogenetic damage by hydroalcoholic extract of Cynodon dactylon in Chinese hamster lung fibroblast cells and human peripheral blood lymphocytes.

PubMed

Rao, Bola Sadashiva Satish; Upadhya, Dinesh; Adiga, Satish Kumar

2008-01-01

The radiomodulatory potential of hydroalcoholic extract of a medicinal plant Cynodon dactylon (family: Poaceae) against radiation-induced cytogenetic damage was analyzed using Chinese hamster lung fibroblast (V79) cells and human peripheral blood lymphocytes (HPBLs) growing in vitro. Induction of micronuclei was used as an index of cytogenetic damage, evaluated in cytokinesis blocked binucleate cells. The hydroalcoholic Cynodon dactylon extract (CDE) rendered protection against the radiation-induced DNA damage, as evidenced by the significant (p<0.001) reduction in micronucleated binucleate cells (MNBNC%) after various doses of CDE treatment in V79 cells and HPBLs. The optimum dose of CDE (40 and 50 microg/ml in HPBLs and V79 cells, respectively) with the greatest reduction in micronuclei was further used in combination with various doses of gamma radiation (0.5, 1, 2, 3, and 4 Gy) exposed 1 h after CDE treatment. A linear dose-dependent MNBNC% increase in radiation alone group was observed, while 40/50 microg/ml CDE significantly resulted in the reduction of MNBNC%, compared to the respective radiation alone groups. CDE resulted in a dose-dependent increase in free radical scavenging ability against various free radicals, viz., 2, 2-diphenyl-2-picryl-hydrazyl (DPPH); 2, 2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS); superoxide anion (O2*-); hydroxyl radical (OH*) and nitric oxide radical (NO*) generated in vitro. Also, an excellent (70%) inhibition of lipid peroxidation in vitro was observed at a dose of 300 microg/ml CDE, attaining the saturation point at higher doses. The present findings demonstrated the radioprotective effect of CDE, also rendering protection against radiation-induced genomic instability and DNA damage. The observed radioprotective effect may be partly attributed to the free radical scavenging and antilipid peroxidative potential of CDE.

Following Through on Follow Through.

ERIC Educational Resources Information Center

Edwards, Roger H.; Bridewell, Joy L.

Possible causes for the discrepancy between the ABT report on the national Project Follow Through and the Saint Louis, Missouri program were discussed: (1) ABT data were positively biased because of non-random, differential attrition from the program and control groups; (2) positive ABT data were due to use of a particular cohort group; or (3)…

40 CFR 80.1270 - Who may generate benzene credits under the ABT program?

Code of Federal Regulations, 2012 CFR

2012-07-01

... 40 Protection of Environment 17 2012-07-01 2012-07-01 false Who may generate benzene credits under... (CONTINUED) AIR PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1270 Who may generate benzene credits under the ABT program? (a...

40 CFR 80.1270 - Who may generate benzene credits under the ABT program?

Code of Federal Regulations, 2014 CFR

2014-07-01

... 40 Protection of Environment 17 2014-07-01 2014-07-01 false Who may generate benzene credits under... (CONTINUED) AIR PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1270 Who may generate benzene credits under the ABT program? (a...

40 CFR 80.1270 - Who may generate benzene credits under the ABT program?

Code of Federal Regulations, 2013 CFR

2013-07-01

... 40 Protection of Environment 17 2013-07-01 2013-07-01 false Who may generate benzene credits under... (CONTINUED) AIR PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1270 Who may generate benzene credits under the ABT program? (a...

40 CFR 80.1270 - Who may generate benzene credits under the ABT program?

Code of Federal Regulations, 2010 CFR

2010-07-01

... 40 Protection of Environment 16 2010-07-01 2010-07-01 false Who may generate benzene credits under... (CONTINUED) AIR PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1270 Who may generate benzene credits under the ABT program? (a...

40 CFR 80.1270 - Who may generate benzene credits under the ABT program?

Code of Federal Regulations, 2011 CFR

2011-07-01

... 40 Protection of Environment 16 2011-07-01 2011-07-01 false Who may generate benzene credits under... (CONTINUED) AIR PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1270 Who may generate benzene credits under the ABT program? (a...

Availability Based Tariff and its impact On different Industry Players-A Review

NASA Astrophysics Data System (ADS)

Holmukhe, R. M.; Pawar, Yogini; Desai, R. S.; Hasarmani, T. S.

2010-10-01

ABT is a performance-based tariff for the supply of electricity by generators owned and controlled by the central government. It is also a new system of scheduling and dispatch, which requires both generators and beneficiaries to commit to day-ahead schedules. It is a system of rewards and penalties seeking to enforce day ahead pre-committed schedules, though variations are permitted if notified One and one half hours in advance. The order emphasizes prompt payment of dues. ABT (Availability Based Tariff) along with the Electricity Act of 2003 is perhaps the most significant and definitive step taken in the Indian power sector so far to bring more efficiency and focus to this vital infrastructure. The ABT mechanism is based on financial principles. ABT scheme is for unscheduled interchange of power. The paper reviews ABT issues, its components, clauses, mechanism, benefits and the impact of grid on different players like generation utilities, grid operator, consumers involved in power generation, transmission and distribution. While the proposed tariff structure has wide implications for each player, this deals exclusively with the technology challenges/opportunities thrown up by ABT.

Phase I study of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 with 5-fluorouracil and leucovorin: a safe combination.

PubMed

Hoekstra, R; de Vos, F Y F L; Eskens, F A L M; de Vries, E G E; Uges, D R A; Knight, R; Carr, R A; Humerickhouse, R; Verweij, J; Gietema, J A

2006-03-01

We performed a phase I study with the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 combined with 5-fluorouracil and leucovorin (5-FU/LV) to determine safety profile and assess pharmacokinetic interactions. Patients with advanced solid malignancies received LV 20 mg/m(2) followed by 5-FU 425 mg/m(2) both administered intravenously in 15 min daily for 5 days every 4 weeks. ABT-510 was administered subcutaneously twice daily continuously from day 2 onwards. Blood and urine samples for pharmacokinetic analyses were collected at days 1, 5 and 22. Twelve patients received a total of 45 cycles of 5-FU/LV combined with ABT-510. ABT-510 dose levels studied were 50 and 100 mg. The combination was well tolerated, with a toxicity profile comparable to that of 5-FU/LV alone. At the dose levels studied no significant pharmacokinetic interactions were observed. These data indicate that ABT-510 administered twice daily subcutaneously can be safely combined with 5-FU/LV administered daily for 5 days, every 4 weeks.

Hemin-Graphene Derivatives with Increased Peroxidase Activities Restrain Protein Tyrosine Nitration.

PubMed

Xu, Huan; Yang, Zhen; Li, Hailing; Gao, Zhonghong

2017-12-14

Protein tyrosine nitration is implicated in the occurrence and progression of pathological conditions involving free radical reactions. It is well recognized that hemin can catalyze protein tyrosine nitration in the presence of nitrite and hydrogen peroxide. Generally, the catalytic efficiency is positively correlated to its peroxidase activity. In this study, however, it is found that the efficiency of hemin in catalyzing protein tyrosine nitration is largely suppressed after functionalization with graphene derivatives, even though its peroxidase-like activity is more than quadrupled. Further studies show that the oxidation of tyrosine is still observed for these composites; dityrosine formation, however, is greatly inhibited. Furthermore, these composites also exhibit strong effects on the oxidation of nitrite into nitrate. Therefore, we propose a mechanism in which hemin-graphene derivatives facilitate the oxidation of tyrosine and nitrite to produce tyrosyl radicals and nitrogen dioxide radicals in the presence of hydrogen peroxide, but graphene interlayers serve as barriers that hinder radical-radical coupling reactions; consequently, protein tyrosine nitration is restrained. This property of hemin-graphene derivatives, by which they catalyze substrate oxidation but suppress radical-radical coupling reactions, shows their great potential in selective oxidation procedures for byproduct removal. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Antioxidative properties of hydroxycinnamic acid derivatives and a phenylpropanoid glycoside. A pulse radiolysis study

NASA Astrophysics Data System (ADS)

Lin, Weizhen; Navaratnam, Suppiah; Yao, Side; Lin, Nianyun

1998-10-01

Spectral and redox properties of the phenoxyl radicals from hydroxycinnamic acid derivatives and one selected component of phenylpropanoid glycosides, verbascoside, were studied using pulse radiolysis techniques. On the basis of the pH dependence of phenoxyl radical absorptions, the p Ka values for deprotonation of sinapic acid radical and ferulic acid radical are 4.9 and 5.2. The rate constants of one electron oxidation of those antioxidants by azide radical and bromide radical ion were determined at pH 7. The redox potentials of those antioxidants were determined as 0.59-0.71 V vs NHE at pH 7 with reference standard 4-methoxyphenol and resorcinol.

Autologous blood transfusion in dogs with thoracic or abdominal hemorrhage: 25 cases (2007-2012).

PubMed

Higgs, Veronica A; Rudloff, Elke; Kirby, Rebecca; Linklater, Andrew K J

2015-01-01

To describe the use and outcome following autologous blood transfusion (ABT) in dogs. Retrospective study (January 2007-July 2012). Private veterinary referral center. Twenty-five dogs that underwent ABT secondary to thoracic or abdominal hemorrhage. None. The hospital transaction database was searched using the keyword "autotransfusion" from January 2007 to July 2012. Data collected included signalment, body weight, etiology of hemorrhage, source and method of collection, volumes and method of ABT administration, use of anticoagulant, reported complications, and outcome. Twenty-five dogs were included for a total of 27 ABTs. Causes of hemorrhage included vascular trauma (14/25 dogs, 56%), ruptured tumor (8/25, 32%), and coagulopathy attributed to brodifacoum toxicosis (3/25, 12%). Autologous blood was collected from the abdominal (19/25, 76%), thoracic (5/25, 20%), or abdominal and thoracic cavities (1/25, 4%). Anticoagulant was added to the ABT blood in 13 of 25 (52%) cases. A median ABT volume of 29.3 mL/kg (range 2.9-406.9 mL/kg) was infused through either a 210 μm blood administration filter (21/27, 78%) or an 18 μm hemonate filter (6/27, 22%). Reported complications that may have been associated with ABT included hypocalcemia (4/17, 24%), hemolyzed serum (5/19, 26%), and prolonged coagulation times (4/5, 80%). These complications were considered of minimal clinical significance. Additional blood products were administered in 17 of 25 (68%) dogs. Seventeen (68%) dogs survived to discharge. Cause of death in the remaining cases was euthanasia or cardiac arrest secondary to uncontrollable hemorrhage. ABT is an adjunct to volume replacement in dogs with thoracic or abdominal hemorrhage secondary to vascular trauma, ruptured tumor, or anticoagulant rodenticide toxicosis. ABT may be used as bridge to definitive hemorrhage control, particularly when other blood products are not available or affordable. Complications may include hypocalcemia, prolonged coagulation times, and hemolysis. © Veterinary Emergency and Critical Care Society 2015.

Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639

PubMed Central

2015-01-01

The discovery of a novel peripherally acting and selective Cav3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bioavailability. Modification of 4 to further improve ADME properties led to the discovery of ABT-639. Following oral administration, ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat. PMID:26101566

Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.

PubMed

Zhang, Qingwei; Xia, Zhiren; Joshi, Shailen; Scott, Victoria E; Jarvis, Michael F

2015-06-11

The discovery of a novel peripherally acting and selective Cav3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bioavailability. Modification of 4 to further improve ADME properties led to the discovery of ABT-639. Following oral administration, ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat.

Free Radical Reactions in Food.

ERIC Educational Resources Information Center

Taub, Irwin A.

1984-01-01

Discusses reactions of free radicals that determine the chemistry of many fresh, processed, and stored foods. Focuses on reactions involving ascorbic acid, myoglobin, and palmitate radicals as representative radicals derived from a vitamin, metallo-protein, and saturated lipid. Basic concepts related to free radical structure, formation, and…

Postoperative blood salvage versus allogeneic blood transfusion in total knee and hip arthroplasty: a literature review.

PubMed

Leigheb, Massimiliano; Pogliacomi, Francesco; Bosetti, Michela; Boccafoschi, Francesca; Sabbatini, Maurizio; Cannas, Mario; Grassi, Federico

2016-04-15

We aimed to compare Postoperative Blood Salvage (PBS) with Allogeneic Blood Transfusion (ABT) in patients undergoing Total Hip and Knee Arthroplasty (THA, TKA).  A bibliographic research was carried out in order to review the literature dedicated to postoperative blood salvage in major orthopaedic surgery, excluding papers dealing exclusively with preoperative autologous donation, intraoperative blood salvage and ABT. PBS and ABT were compared according to complications, costs and duration of hospitalization. PBS effectiveness in reducing ABT was also assessed. PBS system is useful for reducing the complication rate and the length of hospital stay if compared to ABT. Costs for the reinfusion of unwashed shed blood, washed blood, and allogeneic transfusion are controversial among the different authors. Several papers demonstrate that PBS significantly reduces the need of postoperative ABT in both THA and TKA, while there is low evidence that PBS does not affect the risk of surgical wound complications. To reduce potential risks related to PBS, including non-hemolytic febrile reaction, the reinfusion of saved blood should begin within 4-6 hours after the start of collection through the wound drainage. According to literature, PBS appears to be a valid alternative to ABT, which is the standard treatment for postoperative anemia in THA and TKA. Contraindications to PBS must be ruled out before recommending it to patients undergoing major orthopaedic procedures.

Methylphenidate and Memory and Attention Adaptation Training for Persistent Cognitive Symptoms after Traumatic Brain Injury: A Randomized, Placebo-Controlled Trial.

PubMed

McDonald, Brenna C; Flashman, Laura A; Arciniegas, David B; Ferguson, Robert J; Xing, Li; Harezlak, Jaroslaw; Sprehn, Gwen C; Hammond, Flora M; Maerlender, Arthur C; Kruck, Carrie L; Gillock, Karen L; Frey, Kim; Wall, Rachel N; Saykin, Andrew J; McAllister, Thomas W

2017-08-01

The purpose of this multicenter, prospective, randomized, placebo-controlled study was to evaluate and compare the efficacy of two cognitive rehabilitation interventions (Memory and Attention Adaptation Training (MAAT) and Attention Builders Training (ABT)), with and without pharmacological enhancement (ie, with methylphenidate (MPH) or placebo), for treating persistent cognitive problems after traumatic brain injury (TBI). Adults with a history of TBI at least 4 months before study enrollment with either objective cognitive deficits or subjective cognitive complaints were randomized to receive MPH or placebo and MAAT or ABT, yielding four treatment combinations: MAAT/MPH (N=17), ABT/MPH (N=19), MAAT/placebo (N=17), and ABT/placebo (N=18). Assessments were conducted pre-treatment (baseline) and after 6 weeks of treatment (post treatment). Outcome measures included scores on neuropsychological measures and subjective rating scales. Statistical analyses used linear regression models to predict post-treatment scores for each outcome variable by treatment type, adjusting for relevant covariates. Statistically significant (P<0.05) treatment-related improvements in cognitive functioning were found for word-list learning (MAAT/placebo>ABT/placebo), nonverbal learning (MAAT/MPH>MAAT/placebo and MAAT/MPH>ABT/MPH), and auditory working memory and divided attention (MAAT/MPH>ABT/MPH). These results suggest that combined treatment with metacognitive rehabilitation (MAAT) and pharmacotherapy (MPH) can improve aspects of attention, episodic and working memory, and executive functioning after TBI.

Factors Influencing the ABT Phenomenon among Graduate Students in a Master Program in Mexico

ERIC Educational Resources Information Center

Gonzalez-Castillo, Vicente; Cisneros-Cohernour, Edith J.

2007-01-01

This paper presents the findings of a study examining the factors that influence the ABT phenomenon (all but thesis) among graduate students of a Master in Education program in the Southeast of Mexico. Findings of the study identified individual and organizational factors influencing ABT. The study allowed for a better understanding about how…

Diastereoselective radical addition to γ-alkyl-α-methylene-γ-butyrolactams and the synthesis of a chiral pyroglutamic acid derivative

PubMed Central

Yoshida, Eriko; Hamano, Masako

2013-01-01

Summary The cis- and trans-stereoselective radical additions to α-methylene-γ-alkyl- γ-lactams were investigated and the scope and limitation of the reaction were also revealed. This stereoselective radical reaction was used for synthesis of chiral pyroglutamic acid derivatives starting from a commercially available chiral amino acid. PMID:23946839

Multifunctional properties of polysaccharides from Dalbergia sissoo, Tectona grandis and Mimosa diplotricha.

PubMed

Rana, Vikas; Das, Manuj K; Gogoi, Satyabrat; Kumar, Vineet

2014-02-15

Three water-soluble polysaccharides were isolated and purified from the leaves of Dalbergia sissoo Roxb. (DSLP), bark of Tectona grandis L. f (TGBP) and seeds of Mimosa diplotricha var. diplotricha Sauvalle (MDSP). Antioxidant and moisture preserving activities of these three polysaccharides were investigated using in vitro methods. The antioxidant activities studied include superoxide (O2(*-)), 1,1-diphenyl-2-picrylhydrazyl (DPPH*), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS(*+)), hydroxyl (OH(-)), nitric oxide (NO*), N,N-dimethyl-p-phenylenediamine (DMPD(+)) radical scavenging activities, ferric ion (Fe(3+)) reducing ability, ferrous ion (Fe(2+)) chelating and lipid peroxidation activities. The study revealed higher activity of TGBP in all antioxidant assays than DSLP and MDSP. Further, the three polysaccharides showed effective moisture retention properties in comparison with hyaluronic acid and glycerol. Copyright © 2013 Elsevier Ltd. All rights reserved.

New amides from seeds of Silybum marianum with potential antioxidant and antidiabetic activities.

PubMed

Qin, Ning-Bo; Jia, Cui-Cui; Xu, Jun; Li, Da-Hong; Xu, Fan-Xing; Bai, Jiao; Li, Zhan-Lin; Hua, Hui-Ming

2017-06-01

Two new amide compounds, mariamides A and B (1-2), were obtained together with fourteen known compounds from the seeds of milk thistle (Silybum marianum). Their structures were established on the basis of extensive 1D and 2D NMR analyses, as well as HR-ESI-MS data. Most of the compounds showed significant antioxidant activities than positive control in ABTS and FRAP assays. However, only amide compounds 1-4 showed moderate DPPH radical scavenging activity and compounds 7 and 16 showed the most potent activity against DPPH. Most of the compounds showed moderate to stronger α-glucosidase inhibitory activities. Nevertheless, only flavonoids showed strong PTP1B inhibitory activities. These results indicate a use of milk thistle seed extracts as promising antioxidant and antidiabetic agents. Copyright © 2017 Elsevier B.V. All rights reserved.

Optimization of subcritical water extraction parameters of antioxidant polyphenols from sea buckthorn (Hippophaë rhamnoides L.) seed residue.

PubMed

Gong, Ying; Zhang, Xiaofei; He, Li; Yan, Qiuli; Yuan, Fang; Gao, Yanxiang

2015-03-01

Polyphenols was extracted with subcritical water from the sea buckthorn seed residue (after oil recovery), and the extraction parameters were optimized using response surface methodology (RSM). The independent processing variables were extraction temperature, extraction time and the ratio of water to solid. The optimal extraction parameters for the extracts with highest ABTS radical scavenging activity were 120 °C, 36 min and the water to solid ratio of 20, and the maximize antioxidant capacity value was 32.42 mmol Trolox equivalent (TE)/100 g. Under the optimal conditions, the yield of total phenolics, total flavonoids and proanthocyanidins was 36.62 mg gallic acid equivalents (GAE)/g, 19.98 mg rutin equivalent (RE)/g and 10.76 mg catechin equivalents (CE)/g, respectively.

The thrombospondin-1 mimetic ABT-510 increases the uptake and effectiveness of cisplatin and paclitaxel in a mouse model of epithelial ovarian cancer.

PubMed

Campbell, Nicole E; Greenaway, James; Henkin, Jack; Moorehead, Roger A; Petrik, Jim

2010-03-01

Epithelial ovarian cancer (EOC) comprises approximately 90% of ovarian cancers and arises from the surface epithelium. Typical treatment of EOC involves cytoreductive surgery combined with chemotherapy. More recent therapies have targeted the tumor vasculature using antiangiogenic compounds such as thrombospondin-1 (TSP-1). TSP-1 mimetic peptides such as ABT-510 have been created and have been in various clinical trials. We have previously shown that ABT-510 reduces abnormal vasculature associated with tumor tissue and increases the presence of mature blood vessels. It has been hypothesized that treatment with antiangiogenic compounds would allow increased delivery of cytotoxic agents and enhance treatment. In this study, we evaluated the potential role of ABT-510 and various chemotherapeutics (cisplatin and paclitaxel) on tumor progression, angiogenesis, and the benefits of combinational treatments on tissue uptake and perfusion using an orthotopic syngeneic mouse model of EOC. Animals were treated with ABT-510 (100 mg/kg per day) alone or in combination with cisplatin (2 mg/kg per 3 days) or paclitaxel (10 mg/kg per 2 days) at 60 days after tumor induction. Radiolabeled and fluorescently labeled paclitaxel demonstrated a significant increase in tumor uptake after ABT-510 treatment. Combined treatment with ABT-510 and cisplatin or paclitaxel resulted in a significant increase in tumor cell and tumor endothelial cell apoptosis and a resultant decrease in ovarian tumor size. Combined treatment also regressed secondary lesions and eliminated the presence of abdominal ascites. The results from this study show that through vessel normalization, ABT-510 increases uptake of chemotherapy drugs and can induce regression of advanced ovarian cancer.

The Thrombospondin-1 Mimetic ABT-510 Increases the Uptake and Effectiveness of Cisplatin and Paclitaxel in a Mouse Model of Epithelial Ovarian Cancer

PubMed Central

Campbell, Nicole E; Greenaway, James; Henkin, Jack; Moorehead, Roger A; Petrik, Jim

2010-01-01

Epithelial ovarian cancer (EOC) comprises approximately 90% of ovarian cancers and arises from the surface epithelium. Typical treatment of EOC involves cytoreductive surgery combined with chemotherapy. More recent therapies have targeted the tumor vasculature using antiangiogenic compounds such as thrombospondin-1 (TSP-1). TSP-1 mimetic peptides such as ABT-510 have been created and have been in various clinical trials. We have previously shown that ABT-510 reduces abnormal vasculature associated with tumor tissue and increases the presence of mature blood vessels. It has been hypothesized that treatment with antiangiogenic compounds would allow increased delivery of cytotoxic agents and enhance treatment. In this study, we evaluated the potential role of ABT-510 and various chemotherapeutics (cisplatin and paclitaxel) on tumor progression, angiogenesis, and the benefits of combinational treatments on tissue uptake and perfusion using an orthotopic syngeneic mouse model of EOC. Animals were treated with ABT-510 (100 mg/kg per day) alone or in combination with cisplatin (2 mg/kg per 3 days) or paclitaxel (10 mg/kg per 2 days) at 60 days after tumor induction. Radiolabeled and fluorescently labeled paclitaxel demonstrated a significant increase in tumor uptake after ABT-510 treatment. Combined treatment with ABT-510 and cisplatin or paclitaxel resulted in a significant increase in tumor cell and tumor endothelial cell apoptosis and a resultant decrease in ovarian tumor size. Combined treatment also regressed secondary lesions and eliminated the presence of abdominal ascites. The results from this study show that through vessel normalization, ABT-510 increases uptake of chemotherapy drugs and can induce regression of advanced ovarian cancer. PMID:20234821

Targeting the unmet medical need: the Abbott Laboratories oncology approach.

PubMed

Carlson, Dawn M; Steinberg, Joyce L; Gordon, Gary

2005-09-01

While significant advances in the treatment of cancer occured during the last half of the twentieth century, parallel decreases in overall cancer death rates were not observed. Cancer therapy remains an area of significant unmet medical need. Abbott's oncology research programs are focused on pioneering trageted, less toxic therapies, aimed at different aspects of tumor growth and development. Oncology drugs in development at Abbott target several mechanisms of cancer progression by interfering with multiple processes necessary for tumor growth: recruitment of a blood supply, cell proliferation, and the development of metastases. They include a selective endothelin A-receptor antagonist (atrasentan/Xinlay), 3 angiogenesis inhibitors (ABT 510, a thrombospondin mimetic: ABT-869, a multitargeted receptor tyrosine kinase inhibitor; and ABT 828, recombinant human plasminogen kringle 5), a cell proliferation inhibitor (ABT-751, an antimitotic agent), an apoptosis inducer (ABT 737, a Bcl-2 family inhibitor), and a poly(ADP-ribose)polymerase inhibitor.

Evaluation of Concurrent Radiation, Temozolomide and ABT-888 Treatment Followed by Maintenance Therapy with Temozolomide and ABT-888 in a Genetically Engineered Glioblastoma Mouse Model.

PubMed

Lemasson, Benjamin; Wang, Hanxiao; Galbán, Stefanie; Li, Yinghua; Zhu, Yuan; Heist, Kevin A; Tsein, Christina; Chenevert, Thomas L; Rehemtulla, Alnawaz; Galbán, Craig J; Holland, Eric C; Ross, Brian D

2016-02-01

Despite the use of ionizing radiation (IR) and temozolomide (TMZ), outcome for glioblastoma (GBM) patients remains dismal. Poly (ADP-ribose) polymerase (PARP) is important in repair pathways for IR-induced DNA damage and TMZ-induced alkylation at N7-methylguanine and N3-methyldenine. However, optimized protocols for administration of PARP inhibitors have not been delineated. In this study, the PARP inhibitor ABT-888 was evaluated in combination with and compared to current standard-of-care in a genetically engineered mouse GBM model. Results demonstrated that concomitant TMZ/IR/ABT-888 with adjuvant TMZ/ABT-888 was more effective in inducing apoptosis and reducing proliferation with significant tumor growth delay and improved overall survival over concomitant TMZ/IR with adjuvant TMZ. Diffusion-weighted MRI, an early translatable response biomarker detected changes in tumors reflecting response at 1 day post TMZ/IR/ABT-888 treatment. This study provides strong scientific rationale for the development of an optimized dosing regimen for a PARP inhibitor with TMZ/IR for upfront treatment of GBM. Copyright © 2015 The Authors. Published by Elsevier Inc. All rights reserved.