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Sample records for active constituents responsible

  1. Analysis of phytochemical constituents of Eucalyptus citriodora L. responsible for antifungal activity against post-harvest fungi.

    PubMed

    Javed, S; Shoaib, A; Mahmood, Z; Mushtaq, S; Iftikhar, S

    2012-01-01

    In vitro antifungal activity and phytochemical constituents of essential oil, aqueous, methanol and chloroform extract of Eucalyptus citriodora Hook leaves were investigated. A qualitative phytochemical analysis was performed for the detection of alkaloids, cardiac glycosides, flavonoids, saponins, sterols, tannins and phenols. Methanolic extract holds all identified biochemical constituents except for the tannin. While these biochemical constituents were found to be absent in essential oil, aqueous and chloroform extracts with the exception of sterols, cardiac glycosides and phenols in essential oil and sterols and phenols in aqueous and chloroform extracts. Antimycotic activity of four fractions of E. citriodora was investigated through agar-well diffusion method against four post-harvest fungi, namely, Aspergillus flavus Link ex Gray, Aspergillus fumigatus Fres., Aspergillus nidulans Eidam ex Win and Aspergillus terreus Thom. The results revealed maximum fungal growth inhibition by methanolic extract (14.5%) followed by essential oil (12.9%), chloroform extract (10.15%) and aqueous extract (10%). PMID:21999598

  2. Mammalian autophagy degrades nuclear constituents in response to tumorigenic stress.

    PubMed

    Dou, Zhixun; Ivanov, Andrejs; Adams, Peter D; Berger, Shelley L

    2016-08-01

    During autophagy, double-membrane autophagosomes are observed in the cytoplasm. Thus, extensive studies have focused on autophagic turnover of cytoplasmic material. Whether autophagy has a role in degrading nuclear constituents is poorly understood. We reveal that the autophagy protein LC3/Atg8 directly interacts with the nuclear lamina protein LMNB1 (lamin B1), and binds to LMN/lamin-associated chromatin domains (LADs). Through these interactions, autophagy specifically mediates destruction of nuclear lamina during tumorigenic stress, such as by activated oncogenes and DNA damage. This nuclear lamina degradation upon aberrant cellular stress impairs cell proliferation by inducing cellular senescence, a stable form of cell-cycle arrest and a tumor-suppressive mechanism. Our findings thus suggest that, in response to cancer-promoting stress, autophagy degrades nuclear material to drive cellular senescence, as a means to restrain tumorigenesis. Our work provokes a new direction in studying the role of autophagy in the nucleus and in tumor suppression. PMID:26654219

  3. Effects of Saffron (Crocus sativus L.) Stigma Extract and its Active Constituent Crocin on Neuropathic Pain Responses in a Rat Model of Chronic Constriction Injury.

    PubMed

    Safakhah, Hossein Ali; Taghavi, Tahereh; Rashidy-Pour, Ali; Vafaei, Abbas Ali; Sokhanvar, Mina; Mohebbi, Narges; Rezaei-Tavirani, Mostafa

    2016-01-01

    This study was designed to investigate the therapeutic effects of saffron (Crocus sativus L.) and its main constituent crocin on neuropathic pain behavioral responses induced by chronic constriction injury (CCI) in rats. Adult male Wistar rats (200 to 250 g) were randomly assigned into 5 groups: Sham + saline, CCI + saline, CCI+ saffron (30 mg/kg), CCI + crocin (15 mg/kg) and CCI + crocin (30 mg/kg). CCI was induced by applying 4 loose ligatures around the sciatic nerve. Two weeks after nerve lesion, injections of saline, saffron or crocin were started and continued until 26(th) day post-surgery. Pain behavioral responses including mechanical allodynia (von Frey filament testing) and thermal hyperalgesia were measured in 14, 17, 20, 23, 26, and 40(th) days after CCI. CCI significantly increased pain behavioral responses. Saffron and crocin (30 mg/kg) decreased thermal hyperalgesia and mechanical allodynia on day 26, and this effect continued until the day 40. Crocin at lower dose (15 mg/kg) was ineffective. These findings indicate that treatment of saffron and crocin after CCI may have a therapeutic effect against neuropathic pain, suggesting that these substances may offer new strategies for the treatment of this highly debilitating condition. PMID:27610166

  4. Effects of Saffron (Crocus sativus L.) Stigma Extract and its Active Constituent Crocin on Neuropathic Pain Responses in a Rat Model of Chronic Constriction Injury

    PubMed Central

    Safakhah, Hossein Ali; Taghavi, Tahereh; Rashidy-Pour, Ali; Vafaei, Abbas Ali; Sokhanvar, Mina; Mohebbi, Narges; Rezaei-Tavirani, Mostafa

    2016-01-01

    This study was designed to investigate the therapeutic effects of saffron (Crocus sativus L.) and its main constituent crocin on neuropathic pain behavioral responses induced by chronic constriction injury (CCI) in rats. Adult male Wistar rats (200 to 250 g) were randomly assigned into 5 groups: Sham + saline, CCI + saline, CCI+ saffron (30 mg/kg), CCI + crocin (15 mg/kg) and CCI + crocin (30 mg/kg). CCI was induced by applying 4 loose ligatures around the sciatic nerve. Two weeks after nerve lesion, injections of saline, saffron or crocin were started and continued until 26th day post-surgery. Pain behavioral responses including mechanical allodynia (von Frey filament testing) and thermal hyperalgesia were measured in 14, 17, 20, 23, 26, and 40th days after CCI. CCI significantly increased pain behavioral responses. Saffron and crocin (30 mg/kg) decreased thermal hyperalgesia and mechanical allodynia on day 26, and this effect continued until the day 40. Crocin at lower dose (15 mg/kg) was ineffective. These findings indicate that treatment of saffron and crocin after CCI may have a therapeutic effect against neuropathic pain, suggesting that these substances may offer new strategies for the treatment of this highly debilitating condition. PMID:27610166

  5. Antiviral activity of constituents of Tamus communis.

    PubMed

    Aquino, R; Conti, C; De Simone, F; Orsi, N; Pizza, C; Stein, M L

    1991-10-01

    The antiviral activity of the phenanthrene derivatives 1-6, of the spyrostane triglycosides dioscin (7) and gracillin (8), of the furostanol tetraglycosides methylprotodioscin (9), its (25S) epimer methylprotoneodioscin (10), and methylprotogracillin 11, have been tested towards two RNA viruses: vesicular stomatitis virus and human rhinovirus type 1B. All these products were extracted from the rizomes of Tamus communis L; compound 11 was isolated also from Asparagus cochinchinesis, together with pseudoprotodioscin (12), a 20 (22)-unsaturated furostanoside, which was also investigated for antiviral activity. The results were of some interest mainly for the phenanthrene derivatives. PMID:1667189

  6. [Active constituents of Commelina communis L].

    PubMed

    Tang, X Y; Zhou, M H; Zhang, Z H; Zhang, Y B

    1994-05-01

    According to the pharmacological results five compounds were isolated from the herb of Commelina communis. Based on physico-chemical constants and spectral data, four of them were identified as n-triacontanol, p-hydroxycinnamic acid, daucosteril and D-mannitol. p-hydroxycinnamic acid shows antibacterial activity and D-mannitol shows antitussive effect. PMID:7945872

  7. Possible relationships between solar activity and atmospheric constituents

    NASA Technical Reports Server (NTRS)

    Roosen, R. G.; Angione, R. J.

    1975-01-01

    The large body of data on solar variations and atmospheric constituents collected between 1902 and 1953 by the Astrophysical Observatory of the Smithsonian Institution (APO) was examined. Short-term variations in amounts of atmospheric aerosols and water vapor due to seasonal changes, volcanic activity, air pollution, and frontal activity are discussed. Preliminary evidence indicates that increased solar activity is at times associated with a decrease in attenuation due to airborne particulates.

  8. Possible relationships between solar activity and atmospheric constituents

    NASA Technical Reports Server (NTRS)

    Roosen, R. G.; Angione, R. J.

    1974-01-01

    The large body of data on solar variations and atmospheric constituents collected between 1902 and 1953 by the Astrophysical Observatory of the Smithsonian Institution (APO) is examined. Short term variations in amounts of atmospheric aerosols and water vapor due to seasonal changes, volcanic activity, air pollution, and frontal activity are discussed. Preliminary evidence indicates that increased solar activity is at times associated with a decrease in attenuation due to airborne particulates.

  9. Nigella sativa and its active constituent thymoquinone in oral health.

    PubMed

    Al-Attass, Safia A; Zahran, Fat'heya M; Turkistany, Shereen A

    2016-03-01

    In this review, we summarized published reports that investigated the role of Nigella sativa (NS) and its active constituent, thymoquinone (TQ) in oral health and disease management. The literature studies were preliminary and scanty, but the results revealed that black seed plants have a potential therapeutic effect for oral and dental diseases. Such results are encouraging for the incorporation of these plants in dental therapeutics and hygiene products. However, further detailed preclinical and clinical studies at the cellular and molecular levels are required to investigate the mechanisms of action of NS and its constituents, particularly TQ. PMID:26905343

  10. Nigella sativa and its active constituent thymoquinone in oral health

    PubMed Central

    AlAttas, Safia A.; Zahran, Fat’heya M.; Turkistany, Shereen A.

    2016-01-01

    In this review, we summarized published reports that investigated the role of Nigella sativa (NS) and its active constituent, thymoquinone (TQ) in oral health and disease management. The literature studies were preliminary and scanty, but the results revealed that black seed plants have a potential therapeutic effect for oral and dental diseases. Such results are encouraging for the incorporation of these plants in dental therapeutics and hygiene products. However, further detailed preclinical and clinical studies at the cellular and molecular levels are required to investigate the mechanisms of action of NS and its constituents, particularly TQ. PMID:26905343

  11. SUMO Ligase Protein Inhibitor of Activated STAT1 (PIAS1) Is a Constituent Promyelocytic Leukemia Nuclear Body Protein That Contributes to the Intrinsic Antiviral Immune Response to Herpes Simplex Virus 1

    PubMed Central

    Brown, James R.; Conn, Kristen L.; Wasson, Peter; Charman, Matthew; Tong, Lily; Grant, Kyle; McFarlane, Steven

    2016-01-01

    ABSTRACT Aspects of intrinsic antiviral immunity are mediated by promyelocytic leukemia nuclear body (PML-NB) constituent proteins. During herpesvirus infection, these antiviral proteins are independently recruited to nuclear domains that contain infecting viral genomes to cooperatively promote viral genome silencing. Central to the execution of this particular antiviral response is the small ubiquitin-like modifier (SUMO) signaling pathway. However, the participating SUMOylation enzymes are not fully characterized. We identify the SUMO ligase protein inhibitor of activated STAT1 (PIAS1) as a constituent PML-NB protein. We show that PIAS1 localizes at PML-NBs in a SUMO interaction motif (SIM)-dependent manner that requires SUMOylated or SUMOylation-competent PML. Following infection with herpes simplex virus 1 (HSV-1), PIAS1 is recruited to nuclear sites associated with viral genome entry in a SIM-dependent manner, consistent with the SIM-dependent recruitment mechanisms of other well-characterized PML-NB proteins. In contrast to that of Daxx and Sp100, however, the recruitment of PIAS1 is enhanced by PML. PIAS1 promotes the stable accumulation of SUMO1 at nuclear sites associated with HSV-1 genome entry, whereas the accumulation of other evaluated PML-NB proteins occurs independently of PIAS1. We show that PIAS1 cooperatively contributes to HSV-1 restriction through mechanisms that are additive to those of PML and cooperative with those of PIAS4. The antiviral mechanisms of PIAS1 are counteracted by ICP0, the HSV-1 SUMO-targeted ubiquitin ligase, which disrupts the recruitment of PIAS1 to nuclear domains that contain infecting HSV-1 genomes through mechanisms that do not directly result in PIAS1 degradation. IMPORTANCE Adaptive, innate, and intrinsic immunity cooperatively and efficiently restrict the propagation of viral pathogens. Intrinsic immunity mediated by constitutively expressed cellular proteins represents the first line of intracellular defense against

  12. [The research on active constituent distribution of rhizoma coptidis pieces].

    PubMed

    Zhao, Jing; Pang, Qi-Chang; Ma, Ji; Hu, Cui-Ying; Wang, Nian-Ping; Wang, Lin; Cui, Dai-Jun

    2011-06-01

    In order to test the distribution of active constituent of traditional Chinese medicine and to evaluate the quality of medicinal part effectively, spectral imaging analysis technology was used, and rhizoma coptidis pieces were tested as an example. First, the fluorescence spectral cube was taken, and the spectral curve of 3 different medicinal parts of the piece was obtained; second, spectral images were reconstructed by principal components analysis method, and the differences of 3 medicinal parts on the first few principal components were focused; third, the first component image was divided by the threshold method, then the distribution and relative content of 3 medicinal parts were obtained. The results show that spectral imaging analysis technology can provide the distribution of the active constituent, which can be used as the criterion of selecting medicinal parts. The testing course is nondestructive and rapid. PMID:21847960

  13. Antiviral and antituberculous activity of Helichrysum melanacme constituents.

    PubMed

    Lall, N; Hussein, A A; Meyer, J J M

    2006-04-01

    Bioassay guided fractionation of the acetonic extract of Helichrysum melanacme using human Influenza virus type A and a drug-sensitive strain of Mycobacterium tuberculosis in vitro resulted in the isolation of 2 4',6'-trihydroxy-3'-prenylchalcone (1) and 4',6',5''-trihydroxy-6'',6''-dimethyldihydropyrano[2'',3''-2',3'] chalcone (2) as active constituents. 3-O-methylquercetin and quercetin were also isolated but were inactive against the microorganisms tested in this study. PMID:16529879

  14. Lotus leaf (Nelumbo nucifera) and its active constituents prevent inflammatory responses in macrophages via JNK/NF-κB signaling pathway.

    PubMed

    Liu, Shing-Hwa; Lu, Tien-Hui; Su, Chin-Chuan; Lay, Ing-Shiow; Lin, Hui-Yi; Fang, Kai-Min; Ho, Tsung-Jung; Chen, Kuo-Liang; Su, Yi-Chang; Chiang, Wen-Chang; Chen, Ya-Wen

    2014-01-01

    Inflammation is a serious health issue worldwide that induces many diseases, such as inflammatory bowel disease (IBD), sepsis, acute pancreatitis and lung injury. Thus, there is a great deal of interest in new methods of limiting inflammation. In this study, we investigated the leaves of Nelumbo nucifera Gaertn, an aquatic perennial plant cultivated in eastern Asia and India, in anti-inflammatory pharmacological effects in the murine macrophage cell line RAW264.7. Results showed that lipopolysaccharide (LPS) increased the protein expression of inducible nitric oxide synthase (iNOS) and COX-2, as well as the mRNA expression and level of IL-6 and TNF-α, while NNE significantly reduced these effects of LPS. LPS also induced phospho-JNK protein expression. The JNK-specific inhibitor SP600125 decreased the proteins expression of phospho-JNK, iNOS, COX-2, and the mRNAs expression and levels of IL-6 and TNF-α. Further, NNE reduced the protein expression of phospho-JNK. LPS was also found to promote the translocation of NF-κB from the cytosol to the nucleus and to decrease the expression of cytosolic IκB. NNE and SP600125 treatment recovered the LPS-induced expression of NF-κB and IκB. While phospho-ERK and phospho-p38 induced by LPS, could not be reversed by NNE. To further investigate the major components of NNE in anti-inflammatory effects, we determined the quercetin and catechin in inflammatory signals. Results showed that quercetin and catechin significantly decreased the proteins expression of iNOS, COX-2 and phospho-JNK. Besides, the mRNAs and levels of IL-6 and TNF-α also decreased by quercetin and catechin treatment in LPS-induced RAW264.7 cells. These results showed that NNE and its major components quercetin and catechin exhibit anti-inflammatory activities by inhibiting the JNK- and NF-κB-regulated pathways and could therefore be an useful anti-inflammatory agent. PMID:25004880

  15. Antibacterial and antifungal activity of aromatic constituents of essential oils.

    PubMed

    Pattnaik, S; Subramanyam, V R; Bapaji, M; Kole, C R

    1997-01-01

    Five aromatic constituents of essential oils (cineole, citral, geraniol, linalool and menthol) were tested for antimicrobial activity against eighteen bacteria (including Gram-positive cocci and rods, and Gram-negative rods) and twelve fungi (three yeast-like and nine filamentous). In terms of antibacterial activity linalool was the most effective and inhibited seventeen bacteria, followed by cineole, geraniol (each of which inhibited sixteen bacteria), menthol and citral aromatic compounds, which inhibited fifteen and fourteen bacteria, respectively. Against fungi the citral and geraniol oils were the most effective (inhibiting all twelve fungi), followed by linalool (inhibiting ten fungi), cineole and menthol (each of which inhibited seven fungi) compounds. PMID:9218354

  16. Chemical constituents of Solanum coagulans and their antimicrobial activities.

    PubMed

    Qin, Xu-Jie; Lunga, Paul-Keilah; Zhao, Yun-Li; Liu, Ya-Ping; Luo, Xiao-Dong

    2016-04-01

    The present study aimed at determining the chemical constituents of Solanum coagulans and their antimicrobial activities. The compounds were isolated by various chromatographic techniques and their structures were elucidated on the basis of extensive spectroscopic analysis, chemical methods, and comparison with reported spectroscopic data. One new phenolic glycoside, methyl salicylate 2-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside (1), together with 12 known compounds (2-13), were isolated from the aerial parts of Solanum coagulans. Compound 1 was a new phenolic glycoside, and 2-6 were isolated from Solanum genus for the first time. The antimicrobial activities of the isolated compounds were also evaluated. Compound 7 showed remarkable antifungal activity against T. mentagrophytes, M. gypseum and E. floccosum with MIC values being 3.13, 1.56 and 3.13 μg·mL(-1), respectively. PMID:27114320

  17. Chemical constituents from Swietenia macrophylla bark and their antioxidant activity.

    PubMed

    Falah, S; Suzuki, T; Katayama, T

    2008-08-15

    Chemical constituents of the bark of Swietenia macrophylla King (Meliaceae) was investigated not only to develop further bark utilization but also to understand the biochemical function of the bark in the forest environment. A new phenylpropanoid-substituted catechin, namely, swietemacrophyllanin [(2R*,3S*,7"R*)-catechin-8,7"-7,2"-epoxy-(methyl 4",5"-dihydroxyphenylpropanoate)] (1) was isolated from the bark of S. macrophylla together with two known compounds, catechin (2) and epicatechin (3). The structure of 1 was elucidated by spectroscopic data and by comparison of the NMR data with those of catiguanins A and B, phenylpropanoid-substituted epicatechins. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity of the isolated compounds indicated that all of the three compounds have strong activity compared with trolox as a reference. Swietemacrophyllanin (1) had the strongest activity with a 50% inhibitory concentration (IC50) value of 56 microg mL(-1). PMID:19266907

  18. [Advances on chemical constituents and pharmacological activity of genus Scilla].

    PubMed

    Fan, Meng-Yang; Wang, Yan-Min; Wang, Zhi-Min; Gao, Hui-Min

    2014-01-01

    The genus Scilla consists of 90 species widely distributed in Europe, Asia and Africa, one and its variant of which can be found in China Some species of the genus have been used in traditional medicine to treat various diseases related to inflammation and pain. Phytochemical studies have demonstrated the presence of triterpene and tritepenoid saponins derived from eucosterol, bufadienolides, alkaloids, stilbenoids and lignan in the plants of this genus. Various bioactivities such as antimicrobial, anti-inflammatory, antioxidant, anti-tumor and glycosidase inhibitory activities, have been reported. In this review, the advance of chemical constituents and pharmacological activities of the Scilla species are summarized for further development and utilization of the resource. PMID:24761625

  19. Rubus fruticosus L.: constituents, biological activities and health related uses.

    PubMed

    Zia-Ul-Haq, Muhammad; Riaz, Muhammad; De Feo, Vincenzo; Jaafar, Hawa Z E; Moga, Marius

    2014-01-01

    Rubus fruticosus L. is a shrub famous for its fruit called blackberry fruit or more commonly blackberry. The fruit has medicinal, cosmetic and nutritive value. It is a concentrated source of valuable nutrients, as well as bioactive constituents of therapeutic interest highlighting its importance as a functional food. Besides use as a fresh fruit, it is also used as ingredient in cooked dishes, salads and bakery products like jams, snacks, desserts, and fruit preserves. R. fruticosus contains vitamins, steroids and lipids in seed oil and minerals, flavonoids, glycosides, terpenes, acids and tannins in aerial parts that possess diverse pharmacological activities such as antioxidant, anti-carcinogenic, anti-inflammatory, antimicrobial anti-diabetic, anti-diarrheal, and antiviral. Various agrogeoclimatological factors like cultivar, environmental conditions of the area, agronomic practices employed, harvest time, post-harvest storage and processing techniques all influence the nutritional composition of blackberry fruit. This review focuses on the nutrients and chemical constituents as well as medicinal properties of different parts of R. fruticosus. Various cultivars and their physicochemical characteristics, polyphenolic content and ascorbic acid content are also discussed. The information in the present work will serve as baseline data and may lead to new biomedical applications of R. fruticosus as functional food. PMID:25072202

  20. Immunocontraceptive activity guided fractionation and characterization of active constituents of neem (Azadirachta indica) seed extracts.

    PubMed

    Garg, S; Talwar, G P; Upadhyay, S N

    1998-04-01

    A novel approach for immunocontraception by intervention of local cell mediated immunity in the reproductive system by using single intrauterine application of neem oil has been described earlier. The reversible block in fertility was reported to last for 107-180 days in female Wistar rats (Upadhyay et al., 1990. Antifertility effects of neem oil by single intrauterine administration: A novel method of contraception. Proceedings Of The Royal Society Of London B 242, 175-180) and 7-11 months in monkeys (Upadhyay et al., 1994. Long term contraceptive effects of intrauterine neem treatment (IUNT) in bonnet monkeys: An alternative to intrauterine contraceptive devices. Contraception 49, 161-167). The present study, describes the identification and characterization of the biologically active fraction from neem seeds (Azadirachta indica A. Juss. Family Meliaceae), responsible for the above activity in adult female Wistar rats. Initial studies with the mechanically extracted oil and solvent extracts of neem seeds have revealed that the antifertility activity was present in constituents of low to intermediate polarity. A hexane extract of neem seeds was reported to be biologically active (Garg et al., 1994. Comparison of extraction procedures on the immunocontraceptive activity of neem seed extracts. Journal of Ethnopharmacology 22, 87-92). Subsequently, hexane extract was sequentially fractionated through the last active fraction using various separation techniques and tested for antifertility activity at each step. Preparative HPLC was used for isolating individual components of the active fraction in quantities, sufficient for characterization. An analytical HPLC method was developed for standardization of the fraction. The active fraction was identified to be a mixture of six components, which comprises of saturated, mono and di-unsaturated free fatty acids and their methyl esters. Dose response study was performed with the last active fractions. The antifertility

  1. Bioactive Constituents and Antioxidant Activity of Some Carpathian Basin honeys.

    PubMed

    Gyergyák, Kinga; Boros, Borbála; Marton, Krisztina; Felinger, Attila; Papp, Nóra; Farkas, Ágnes

    2016-02-01

    Unifloral honeys have a high commercial value and should undergo a strict quality control before marketing. This study aimed at determining floral origin, polyphenolic compounds and antioxidant activity in 7 samples marketed as lavender and thyme honeys. The samples were subjected to pollen analysis to confirm their botanical origin. Coupled chromatographic techniques (HPLC-DAD-ESI-MS) were optimized for the separation and identification of polyphenolic compounds. The antioxidant properties of the samples were determined by spectrophotometric methods. Pollen profile analysis revealed that only 3 out of 5 alleged lavender honeys contained a low percentage (0.6-1.5) of lavender pollen; and there were only traces (0.1-0.6%) of thyme pollen in the alleged thyme honeys. Polyphenolic constituents did not allow for the clear separation of honey samples, revealing no marker compounds previously associated with lavender and thyme honeys. All samples contained large amounts of chlorogenic acid, chrysin, hesperetin, kaempferol and p-coumaric acid; as well as abscisic acid, a plant hormone known to be present in floral nectar and honey. Our results suggest that only one of five alleged lavender honeys and neither of the two alleged thyme honeys are true unifloral honeys. However, they can still provide various health benefits, such as being good sources of antioxidants. There was no relationship between the antioxidant activity and the uni- or multifloral character of the honey samples. Total phenolic content and antioxidant activity was the lowest in the honey sample with lavender and the highest in one of the alleged lavender honeys. Our findings highlight the importance of microscopical and phytochemical analyses of honeys before marketing, to ensure satisfactory quality for customers. PMID:27032212

  2. Antiprotozoal activity of the constituents of Rubus coriifolius.

    PubMed

    Alanís, Alma Delia; Calzada, Fernando; Cedillo-Rivera, Roberto; Meckes, Mariana

    2003-06-01

    Extraction of the aerial parts of Rubus coriifolius, a medicinal plant used by the Maya communities in Southern Mexico to treat bloody diarrhoea, resulted in the isolation of seven known compounds (-)-epicatechin, (+)-catechin, hyperin, nigaichigoside F1, beta-sitosterol 3-O-beta-d-glucopyranoside, gallic acid and ellagic acid. All compounds were tested for their antiprotozoal activity against Entamoeba histolytica and Giardia lambia. Epicatechin was the main responsible for the antiprotozoal activity of the extract against both protozoa, its activity was comparable to emetine, but no exceeded that of metronidazole. PMID:12820241

  3. [Advances in studies on chemical constituents and biological activities of Desmodium species].

    PubMed

    Liu, Chao; Wu, Ying; Zhang, Qian-Jun; Kang, Wen-Yi; Zhang, Long; Zhou, Qing-Di

    2013-12-01

    The chemical constituents isolated from Desmodium species (Leguminosae) included terpenoids, flavonoids, steroids, alkaloids compounds. Modem pharmacological studies have showed that the Desmodium species have antioxidant, antibacterial, anti-inflammatory, hepatoprotective, diuretic, antipyretic, analgesic and choleretic activity. This article mainly has reviewed the research advances of chemical constituents and biological activities of Desmodium species since 2003. PMID:24791478

  4. The Rhizomes of Acorus gramineus and the Constituents Inhibit Allergic Response In vitro and In vivo.

    PubMed

    Lim, Hyun; Lee, Seung Young; Lee, Kang Ro; Kim, Yeong Shik; Kim, Hyun Pyo

    2012-09-01

    The rhizomes of Acorus gramineus have frequently been used in traditional medicine mainly for sedation as well as enhancing brain function. In this study, the anti-allergic activity of A. gramineus was investigated. The 70% ethanol extract of the rhizomes of A. gramineus was found to inhibit the allergic response against 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and β-hexosaminidase release from RBL-2H3 cells with IC50's of 48.9 and >200 μg/ml, respectively. Among the 9 major constituents isolated, β-asarone, (2R,3R,4S,5S)-2,4-dimethyl-1,3-bis (2',4',5'-trimethoxyphenyl)tetrahydrofuran (AF) and 2,3-dihydro-4,5,7-trimethoxy-1-ethyl-2-methyl-3-(2,4,5-trimethoxyphenyl)indene (AI) strongly inhibited 5-LOX-catalyzed LT production in A23187-treated RBL-1 cells, AI being the most potent (IC50=6.7 μM). Against β-hexosaminidase release by antigen-stimulated RBL-2H3 cells, only AI exhibited strong inhibition (IC50=7.3 μM) while β-asarone and AF showed 26.0% and 39.9% inhibition at 50 μM, respectively. In addition, the ethanol extract of A. gramineus showed significant inhibitory action against the hapten-induced delayed hypersensitivity reaction in mice by oral administration at 200 mg/kg. Therefore, it is suggested that A. gramineus possesses anti-allergic activity and the constituents including β-asarone and AI certainly contribute to the anti-allergic activity of the rhizomes of A. gramineus. PMID:24009837

  5. Repellent activity of constituents identified in Foeniculum vulgare fruit against Aedes aegypti (Diptera: Culicidae).

    PubMed

    Kim, Do-Hyoung; Kim, Soon-Il; Chang, Kyu-Sik; Ahn, Young-Joon

    2002-11-20

    The repellent activity of materials derived from the methanol extract of fruits from Foeniculum vulgareagainst hungry Aedes aegypti females was examined using skin and patch tests and compared with that of the commercial N,N-diethyl-m-toluamide (deet) and (Z)-9-octadecenoic acid. The biologically active constituents of the Foeniculum fruits were characterized as (+)-fenchone and (E)-9-octadecenoic acid by spectroscopic analyses. Responses varied according to compound, dose, and exposure time. In a skin test with female mosquitoes, at a dose of 0.4 mg/cm(2), (+)-fenchone and (Z)-9-octadecenoic acid exhibited moderate repellent activity at 30 min after treatment, whereas deet provided >1 h of protection against adult mosquitoes at 0.2 mg/cm(2). (Z)-9-Octadecenoic acid was a more potent repellent agent than (E)-9-octadecenoic acid. (+)-Fenchone and (E)-9-octadecenoic acid merit further study as potential mosquito repellent agents or as lead compounds. PMID:12428949

  6. In Vitro and In Vivo Activities of Chios Mastic Gum Extracts and Constituents against Helicobacter pylori▿

    PubMed Central

    Paraschos, Sotirios; Magiatis, Prokopios; Mitakou, Sofia; Petraki, Kalliopi; Kalliaropoulos, Antonios; Maragkoudakis, Petros; Mentis, Andreas; Sgouras, Dionyssios; Skaltsounis, Alexios-Leandros

    2007-01-01

    The extracts and pure major constituents of Chios mastic gum (resin of Pistacia lentiscus var. chia) were tested for their activities against Helicobacter pylori. A total mastic extract without polymer (TMEWP) was prepared after removal of the contained insoluble polymer in order to ameliorate solubility and enhance in vivo activity. Administration of TMEWP to H. pylori SS1-infected mice over the period of 3 months with an average dose of 0.75 mg/day led to an approximately 30-fold reduction in the H. pylori colonization (1.5 log CFU/g of tissue). However, no attenuation in the H. pylori-associated chronic inflammatory infiltration and the activity of chronic gastritis was observed. To further characterize potential active mastic constituents, the TMEWP was separated into an acidic and a neutral fraction. Both were extensively characterized by nuclear magnetic resonance and mass spectroscopy to elucidate the structure of the components contained within each fraction. After chromatographic separation, the acid fraction gave the major triterpenic acids, while the neutral fraction gave several triterpenic alcohols and aldehydes. Mastic extracts and isolated pure triterpenic acids were tested for in vitro activity against a panel of 11 H. pylori clinical strains. The acid fraction was found to be the most active extract (minimum bactericidal concentration [MBC], 0.139 mg/ml), and the most active pure compound was isomasticadienolic acid (MBC, 0.202 mg/ml [0.443 mM]). Our results show that administration of TMEWP may be effective in reducing H. pylori colonization and that the major triterpenic acids in the acid extract may be responsible for such an activity. PMID:17116667

  7. Screening of Thai medicinal plant extracts and their active constituents for in vitro antimalarial activity.

    PubMed

    Ichino, C; Soonthornchareonnon, N; Chuakul, W; Kiyohara, H; Ishiyama, A; Sekiguchi, H; Namatame, M; Otoguro, K; Omura, S; Yamada, H

    2006-04-01

    To discover antimalarial substances from plants cultivated in Thailand 80%-EtOH extracts from selected plants were screened for in vitro antimalarial activity against the drug resistant K1 strain of Plasmodium falciparum. In total, 86 Thai medicinal plant samples representing 48 species from 35 genera in 16 families were screened and two species (Polyalthia viridis and Goniothalamus marcanii) were found to show notable antimalarial activity (IC50: 10.0 and 6.3 microg/mL). Marcanine A and 16-hydroxycleroda-3,13(14)Z-dien-15,16-olide were identified as the respective major active constituents in P. viridis and G. marcanii, respectively. PMID:16557615

  8. Inhibition of Human Neutrophil Responses by Essential Oil of Artemisia kotuchovii and Its Constituents

    PubMed Central

    Schepetkin, Igor A.; Kushnarenko, Svetlana V.; Özek, Gulmira; Kirpotina, Liliya N.; Utegenova, Gulzhakhan A.; Kotukhov, Yuriy A.; Danilova, Alevtina N.; Özek, Temel; Başer, K. Hüsnü Can; Quinn, Mark T.

    2015-01-01

    Essential oils were obtained by hydrodistillation of the flowers+leaves and stems of Artemisia kotuchovii Kupr. (AKEOf+l and AKEOstm, respectively) and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC/MS). The primary components of the oils were estragole, (E)- and (Z)-β-ocimenes, methyl eugenol, limonene, spathulenol, β-pinene, myrcene, and (E)-methyl cinnamate. Seventy four constituents were present at concentrations from 0.1 to 1.0%, and 34 compounds were identified in trace (<0.1%) amounts in one or both plant components. Screening of the essential oils for biological activity showed that AKEOstm, but not AKEOf+l, inhibited N-formyl-Met-Leu-Phe (fMLF)-stimulated Ca2+ flux and chemotaxis and phorbol-12-myristate-13-acetate (PMA)-induced reactive oxygen species (ROS) production in human neutrophils. Selected pure constituents, representing >96% of the AKEOstm composition, were also tested in human neutrophils and HL-60 cells transfected with N-formyl peptide receptor 1 (FPR1). We found that one component, 6-methyl-3,5-heptadien-2-one (MHDO), inhibited fMLF- and interleukin 8 (IL-8)-stimulated Ca2+ flux, fMLF-induced chemotaxis, and PMA-induced ROS production in human neutrophils. MHDO also inhibited fMLF-induced Ca2+ flux in FPR1-HL60 cells. These results suggest that MHDO may be effective in modulating some innate immune responses, possibly by an inhibition of neutrophil migration and ROS production. PMID:25959257

  9. In vitro serotonergic activity of black cohosh and identification of N(omega)-methylserotonin as a potential active constituent.

    PubMed

    Powell, Sharla L; Gödecke, Tanja; Nikolic, Dejan; Chen, Shao-Nong; Ahn, Soyoun; Dietz, Birgit; Farnsworth, Norman R; van Breemen, Richard B; Lankin, David C; Pauli, Guido F; Bolton, Judy L

    2008-12-24

    Cimicifuga racemosa (L.) Nutt. (syn. Actaea racemosa L., black cohosh) is used to relieve menopausal hot flashes, although clinical studies have provided conflicting data, and the active constituent(s) and mechanism(s) of action remain unknown. Because serotonergic receptors and transporters are involved with thermoregulation, black cohosh and its phytoconstituents were evaluated for serotonergic activity using 5-HT7 receptor binding, cAMP induction, and serotonin selective re-uptake inhibitor (SSRI) assays. Crude extracts displayed 5-HT7 receptor binding activity and induced cAMP production. Fractionation of the methanol extract led to isolation of phenolic acids and identification of N(omega)-methylserotonin by LC-MS/MS. Cimicifuga triterpenoids and phenolic acids bound weakly to the 5-HT7 receptor with no cAMP or SSRI activity. In contrast, N(omega)-methylserotonin showed 5-HT7 receptor binding (IC50 = 23 pM), induced cAMP (EC50 = 22 nM), and blocked serotonin re-uptake (IC50 = 490 nM). These data suggest N(omega)-methylserotonin may be responsible for the serotonergic activity of black cohosh. PMID:19049296

  10. In vitro Serotonergic Activity of Black Cohosh and Identification of Nω-Methylserotonin as a Potential Active Constituent

    PubMed Central

    POWELL, SHARLA L.; GÖDECKE, TANJA; NIKOLIC, DEJAN; CHEN, SHAO-NONG; AHN, SOYOUN; DIETZ, BIRGIT; FARNSWORTH, NORMAN R.; VAN BREEMEN, RICHARD B.; LANKIN, DAVID; PAULI, GUIDO F.; BOLTON, JUDY L.

    2013-01-01

    Cimicifuga racemosa(L.) Nutt. (syn. Actaea racemosa L., black cohosh) is used to relieve menopausal hot flashes, although clinical studies have provided conflicting data, and the active constituent(s) and mechanism(s) of action remain unknown. Since serotonergic receptors and transporters are involved with thermoregulation, black cohosh and its phytoconstituents were evaluated for serotonergic activity using 5-HT7 receptor binding, cAMP induction, and serotonin selective reuptake inhibitor (SSRI) assays. Crude extracts displayed 5-HT7 receptor binding activity and induced cAMP production. Fractionation of the methanol extract lead to isolation of phenolic acids and identification of Nω-methylserotonin by LC/MS-MS. Cimicifuga triterpenoids and phenolic acids bound weakly to the 5-HT7 receptor with no cAMP or SSRI activity. In contrast, Nω-methylserotonin showed 5-HT7 receptor binding (IC50 23 pM), induced cAMP (EC50 22 nM), and blocked serotonin reuptake (IC50 490 nM). These data suggest Nω-methylserotonin may be responsible for the serotonergic activity of black cohosh. PMID:19049296

  11. Chemical constituents and larvicidal activity of Hymenaea courbaril fruit peel.

    PubMed

    Aguiar, José Cláudio D; Santiago, Gilvandete M P; Lavor, Patrícia L; Veras, Helenicy N H; Ferreira, Yana S; Lima, Michele A A; Arriaga, Angela M C; Lemos, Telma L G; Lima, Jefferson Q; de Jesus, Hugo C R; Alves, Péricles B; Braz-Filho, Raimundo

    2010-12-01

    The chemical compositions of the essential oils from the peel of ripe and unripe fruits of Hymenaea courbaril L., obtained by hydrodistillation, were analyzed by GC and GC-MS. The main constituents of the essential oil from the peel of the ripe fruits were the sesquiterpenes alpha-copaene (11.1%), spathulenol (10.1%) and beta-selinene (8.2%), while germacrene-D (31.9%), beta-caryophyllene (27.1%) and bicyclogermacrene (6.5%) were the major compounds in the oil from unripe fruits. The essential oils were tested against Aedes aegypti larvae and showed LC50 values of 14.8 +/- 0.4 microg/mL and 28.4 +/- 0.3 microg/mL for the ripe and unripe fruit peel oils, respectively. From the peel of the ripe fruits, the diterpenes zanzibaric acid and isoozic acid were isolated, along with the sesquiterpene caryolane-1,9beta-diol. To the best of our knowledge, this is the first report of this sesquiterpene in the genus. The structures of all compounds isolated were identified on the basis of their spectral data (IR, MS, 1D- and 2D-NMR) and by comparison with literature spectral data. PMID:21299135

  12. Essential Oil Constituents and Antioxidant Activity of Asplenium Ferns.

    PubMed

    Hammami, Saoussen; Snène, Ali; El Mokni, Ridha; Faidi, Khaled; Falconieri, Danilo; Dhaouadi, Hatem; Piras, Alessandra; Mighri, Zine; Porcedda, Silvia

    2016-09-01

    Two fern species Asplenium adiantum-nigrum L. and Asplenium trichomanes L. collected from the Kroumiria region (Northwest of Tunisia) were individually submitted to hydrodistillation in a Clevenger type apparatus. Volatile organic compounds were identified by GC-MS and GC-FID. Thus, 35 compounds were identified in A. adiantum-nigrum essential oil accounting for 77.5% of the whole constituents dominated by palmitic acid (34.5%); however, only 29 volatiles were identified in A. trichomanes showing a high amount of phytol, an odorous diterpene alcohol, representing 14.4% of the total oil contents. The total phenolic content and the antioxidant effects of crude extracts from both pteridophytes were determined using Folin-Ciocalteu and 2,2'-diphenyl-1-picrylhydrazyl free radical-scavenging assays, respectively. A. adiantum-nigrum ethyl acetate extract is shown to be lower in total phenolic contents (49.3 mg gallic acid equivalent/g) than similar extract from A. trichomanes (55.4 mg GAE/g). PMID:27165574

  13. Isolation and screened neuroprotective active constituents from the roots and rhizomes of Valeriana amurensis.

    PubMed

    Wang, Changfu; Xiao, Yang; Yang, Bingyou; Wang, Zhibin; Wu, Lihua; Su, Xiaolin; Brantner, Adelheid; Kuang, Haixue; Wang, Qiuhong

    2014-07-01

    In previous study, we have screened the effective fraction against Alzheimer's disease (AD-EF) from the extracts of roots and rhizomes of Valeriana amurensis, based on which neuroprotective active constituents from AD-EF were investigated. Six new compounds 1-6, including four iridoids (xiecaoside A-C and xiecaoline A), one pinane-type monoterpeneglucoside (xiecaoside D), and one phenylpropanoid glycoside (xiecaoside E) were isolated together with 11 known compounds 7-17. The structures of 1-6 were elucidated by their spectroscopic data. The protective effects of compounds 1-17 on PC12 cells with neurotoxicity induced by amyloid-beta 1-42 (Aβ(1-42)) was also investigated, respectively. Consequently, compound 6 and lignans 11-17 were responsible for protecting against Aβ-induced toxicity in PC12 cells. PMID:24742562

  14. Phytochemical constituents and antibacterial activity of some green leafy vegetables

    PubMed Central

    Bhat, Ramesa Shafi; Al-Daihan, Sooad

    2014-01-01

    Objective To investigate the antibacterial activity and photochemicals of five green leafy vegetables against a panel of five bacteria strains. Methods Disc diffusion method was used to determine the antibacterial activity, while kanamycin was used as a reference antibiotic. The phytochemical screening of the extracts was performed using standard methods. Results All methanol extracts were found active against all the test bacterial strains. Overall maximum extracts shows antibacterial activity which range from 6 to 15 mm. Proteins and carbohydrates was found in all the green leaves, whereas alkaloid, steroids, saponins, flavonoids, tannins were found in most of the test samples. Conclusions The obtain result suggests that green leafy vegetables have moderate antibacterial activity and contain various pharmacologically active compounds and thus provide the scientific basis for the traditional uses of the studied vegetables in the treatment of bacterial infections. PMID:25182436

  15. Evaluation of PPARa activation by known blueberry constituents

    Technology Transfer Automated Retrieval System (TEKTRAN)

    We previously showed that pterostilbene, a stilbene found in some Vaccinium berries, is an agonist for the nuclear transcription factor peroxisome proliferator activated receptor alpha isoform (PPARa). In the present study, we demonstrate a dose-dependent activation of PPARa by pterostilbene in a r...

  16. Antiproliferative activity of Saponaria vaccaria constituents and related compounds.

    PubMed

    Balsevich, J John; Ramirez-Erosa, Irving; Hickie, Robert A; Dunlop, Donna M; Bishop, Greg G; Deibert, Leah K

    2012-01-01

    Total methanolic extracts of Saponaria vaccaria seed derived from several varieties, as well as various purified components obtained through successive chromatographic separations of total extracts were evaluated for their growth inhibitory activity in WiDr (colon), MDA-MB-231 (breast), NCI-417 (lung) and PC-3 (prostate) human cancer cells as well as the non-tumorigenic fibroblast BJ (CRL-2522) cell line using MTT colorimetric assay. Purified bisdesmosidic saponins segetoside H and I were further examined using microscopy and apoptosis assays. Bisdesmosidic saponins exhibited dose-dependent growth inhibitory and selective apoptosis-inducing activity. Growth inhibitory effects were particularly strong in a breast (MDA-MB-231) and a prostate (PC-3) cancer cell line. Total extracts exhibited a different preference being most active against a colon cancer cell line (WiDr). In a comparison of varieties, all of the total seed extracts exhibited similar dose-dependent activities, but with some variation in potency. Monodesmosidic saponins vaccarosides A and B, phenolic vaccarin, and cyclopeptide segetalin A, co-occurring seed substituents, did not exhibit activity. The non-tumorigenic fibroblast cell line BJ (CRL 2522) was growth inhibited but did not undergo apoptosis when treated with bisdesmosidic saponins at low micromolar concentrations. Saponin-rich extracts from Kochia scoparia seed and Chenopodium quinoa were also evaluated alongside Saponaria saponins but did not exhibit activity. Closely related Quillaja saponins exhibited activity but were less potent. PMID:22056663

  17. Chemical Constituents Antioxidant and Anticholinesterasic Activity of Tabernaemontana catharinensis

    PubMed Central

    Moura, Sidnei; Echeverrigaray, Sergio

    2013-01-01

    The present work aimed to analyze the alkaloid content of the ethanolic extract of Tabernaemontana catharinensis (Apocynaceae family) and its fractions as well as to evaluate their antioxidant and anticholinesterasic activities. The analyses of the ethanolic extract of T. catharinensis by mass spectrometry allowed identifying the presence of the alkaloids 16-epi-affinine, coronaridine-hydroxyindolenine, voachalotine, voacristine-hydroxyindolenine, and 12-methoxy-n-methyl-voachalotine, as well as an alkaloid with m/z 385.21 whose spectrum suggests a derivative of voacristine or voacangine. The extract and its alkaloid rich fractions showed antioxidant activity, especially those that contain the alkaloid m/z 385.21 or 16-epi-affinine with DPPH scavenging activity (IC50) between 37.18 and 74.69 μg/mL. Moreover, the extract and its fractions exhibited anticholinesterasic activity, particularly the fractions characterized by the presence of 12-methoxy-n-methyl-voachalotine, with IC50 = 2.1 to 2.5 μg/mL. Fractions with 16-epi-affinine combined good antioxidant (IC50 = 65.59 to 74.69 μg/mL) and anticholinesterasic (IC50 = 7.7 to 8.3 μg/mL) activities, representing an option for further studies aimed at treating neurodegenerative diseases. PMID:23983637

  18. Chemical constituents and antibacterial activity of Melastoma malabathricum L.

    PubMed

    Wong, Keng-Chong; Hag Ali, Dafaalla Mohamed; Boey, Peng-Lim

    2012-01-01

    The aqueous methanolic extracts of Melastoma malabathricum L. exhibited antibacterial activity when assayed against seven microorganisms by the agar diffusion method. Solvent fractionation afforded active chloroform and ethyl acetate fractions from the leaves and the flowers, respectively. A phytochemical study resulted in the identification of ursolic acid (1), 2α-hydroxyursolic acid (2), asiatic acid (3), β-sitosterol 3-O-β-D-glucopyranoside (4) and the glycolipid glycerol 1,2-dilinolenyl-3-O-β-D-galactopyanoside (5) from the chloroform fraction. Kaempferol (6), kaempferol 3-O-α-L-rhamnopyranoside (7), kaempferol 3-O-β-D-glucopyranoside (8), kaempferol 3-O-β-D-galactopyranoside (9), kaempferol 3-O-(2″,6″-di-O-E-p-coumaryl)-β-D-galactopyranoside (10), quercetin (11) and ellagic acid (12) were found in the ethyl acetate fraction. The structures of these compounds were determined by chemical and spectral analyses. Compounds 1-4, the flavonols (6 and 11) and ellagic acid (12) were found to be active against some of the tested microorganisms, while the kaempferol 3-O-glycosides (7-9) did not show any activity, indicating the role of the free 3-OH for antibacterial activity. Addition of p-coumaryl groups results in mild activity for 10 against Staphylococcus aureus and Bacillus cereus. Compounds 2-5, 7 and 9-12 are reported for the first time from M. malabathricum. Compound 10 is rare, being reported only once before from a plant, without assignment of the double bond geometry in the p-coumaryl moiety. PMID:21834640

  19. Antiprotozoal activity of the constituents of Teloxys graveolens.

    PubMed

    Calzada, Fernando; Velázquez, Claudia; Cedillo-Rivera, Roberto; Esquivel, Baldomero

    2003-08-01

    Antiprotozoal activity-guided fractionation of a methanol extract of the aerial parts of Teloxys graveolens led to the isolation of one coumarinic acid derivative, melilotoside, and five flavonoids, pinocembrine, pinostrobin, chrysin, narcissin and rutin. Among them, melilotoside exhibited the most potent activity toward Entamoeba histolytica and Giardia lamblia (IC(50) 12.5 and 16.8 micro g/mL, respectively). Narcissin showed selectivity against E. histolytlica (IC(50) 17.2 micro g/mL). The results support data for the traditional use of T. graveolens in some gastrointestinal diseases. PMID:12916068

  20. [Progress in study of chemical constituents and anti-tumor activities of Cnidium monnieri].

    PubMed

    Zhou, Ze-wei; Liu, Pei-xun

    2005-09-01

    The main pharmacological constituents of Chinese traditional medicine herb Cnidium monnieri are coumarin compounds and volatile oil. In addition, it contains monoterpene polyols, glucides, as well as recently discovered sesquiterpene components. In recent years, rather active investigations of its anti-tumor were performed at home and abroad. C. monnieri possesses multi-aspect and comprehensive anti-tumor functions, involving directly tumor-inhibitory activity, anti-mutagenicity, reversing multi-drug tolerance of tumor, as well as improving immune functions and so on. In this review, chemical constituents, anti-tumor activities and relevant investigations of Fructus Cnidii were summarized recent decade. PMID:16323535

  1. The anti-thrombotic active constituents from Centella asiatica.

    PubMed

    Satake, Toshiko; Kamiya, Kohei; An, Yin; Oishi Nee Taka, Tomomi; Yamamoto, Junichiro

    2007-05-01

    The in vitro effects of a methanol extract from the aerial parts of Centella asiatica on shear-induced platelet activation and coagulation were assessed after oral administration to rats, by subjecting non-anticoagulated blood to haemostatometry. 3,5-Di-O-caffeoyl quinic acid, 1,5-di-O-caffeoyl quinic acid, 3,4-di-O-caffeoyl quinic acid, 4,5-di-O-caffeoyl quinic acid, and chlorogenic acid, together with asiaticoside, kaempferol, quercetine, kaempferol-3-O-beta-D-glucoside and quercetin-3-O-beta-D-glucoside were all isolated from the methanol extract. Amongst these, only 3,5-di-O-caffeoylquinic acid showed significant inhibition of shear-induced platelet activation and dynamic coagulation. The reactive curve of the inhibitory effect on the platelet reaction and the dynamic coagulation showed a bell-shape. PMID:17473438

  2. [Antidepressant active constituents in the roots of Morinda officinalis How].

    PubMed

    Cui, C; Yang, M; Yao, Z; Cao, B; Luo, Z; Xu, Y; Chen, Y

    1995-01-01

    Five compounds having antidepressant activities have been isolated from the roots of Morinda officinalis, a Chinese traditional Yang-tonic drug. These compounds were identified as succinic acid (1), nystose (2), 1F-fructofuranosylnystose (3), inulin-type hexasaccharide (4) and heptasaccharide (5) by chemical and spectroscopic methods. All of the compounds are isolated from the species of genus Morinda for the first time. PMID:7626209

  3. [Antifungal activity of essential oils and their constituents against Candida spp. and their effects on activity of amphotericin B].

    PubMed

    Nozaki, Akiko; Takahashi, Eizo; Okamoto, Keinosuke; Ito, Hideyuki; Hatano, Tsutomu

    2010-06-01

    Candidiasis is a common opportunistic fungal infection that responds well to amphotericin B (AMPH) treatment. However, AMPH often causes adverse effects such as kidney injury and hypokalemia. Because some essential oils have been reported to have antifungal effects, we investigated the antifungal activity of various essential oils and their major constituents against Candida spp. Most essential oils examined in this study showed antifungal activity, and several enhanced the antifungal effect of AMPH. Clove oil in particular, and its major constituent eugenol, had potent effects. These findings suggest that combining certain essential oils or their constituents with AMPH may be useful for suppressing the adverse effects of AMPH treatment. PMID:20519869

  4. Phenolic Constituents of Medicinal Plants with Activity against Trypanosoma brucei.

    PubMed

    Sun, Ya Nan; No, Joo Hwan; Lee, Ga Young; Li, Wei; Yang, Seo Young; Yang, Gyongseon; Schmidt, Thomas J; Kang, Jong Seong; Kim, Young Ho

    2016-01-01

    Neglected tropical diseases (NTDs) affect over one billion people all over the world. These diseases are classified as neglected because they impact populations in areas with poor financial conditions and hence do not attract sufficient research investment. Human African Trypanosomiasis (HAT or sleeping sickness), caused by the parasite Trypanosoma brucei, is one of the NTDs. The current therapeutic interventions for T. brucei infections often have toxic side effects or require hospitalization so that they are not available in the rural environments where HAT occurs. Furthermore, parasite resistance is increasing, so that there is an urgent need to identify novel lead compounds against this infection. Recognizing the wide structural diversity of natural products, we desired to explore and identify novel antitrypanosomal chemotypes from a collection of natural products obtained from plants. In this study, 440 pure compounds from various medicinal plants were tested against T. brucei by in a screening using whole cell in vitro assays. As the result, twenty-two phenolic compounds exhibited potent activity against cultures of T. brucei. Among them, eight compounds-4, 7, 11, 14, 15, 18, 20, and 21-showed inhibitory activity against T. brucei, with IC50 values below 5 µM, ranging from 0.52 to 4.70 μM. Based on these results, we attempt to establish some general trends with respect to structure-activity relationships, which indicate that further investigation and optimization of these derivatives might enable the preparation of potentially useful compounds for treating HAT. PMID:27077842

  5. [Chemical constituents from Callicarpa nudiflora and their cytotoxic activities].

    PubMed

    Ma, Yan-Chun; Zhang, Min; Xu, Wen-Tong; Feng, Shi-Xiu; Lei, Ming; Yi, Bo

    2014-08-01

    The chemical consitituents from cytotoxic fraction of the Callicarpa nudiflora extract were isolated and purified by a combination of HP-20 macroporous resin, silica gel and Sephadex LH-20 column chromatographies. The structures were elucidated on the basis of the spectroscopic data and comparison of their spectroscopic data with reported data. The cytotoxicity was evaluated by the MTT assay. The 50% and 70% EtOH elutions of EtOH-extract showed significant cytotoxic activities, leading to the isolation of twelve compounds, which were identified as luteoloside(1), lutedin-4'-O-β-D-glucoside(2), 6-hydroxyluteolin-7-O-β-glucoside(3), lutedin-7-O-neohesperidoside(4), rhoifolin (5), luteolin-7, 4'-di-O-glucoside (6), forsythoside B (7), acteoside (8), alyssonoside (9), catalpol(10), nudifloside(11), and leonuride(12). Compounds 3-6, 10 and 12 were isolated from this genus for the first time, and compound 9 was isolated from this plant for the first time. The cytotoxicity assay demonstrated that flavonoids 1-6, in various concentrations, showed monolithic proliferation inhibitory activities against Hela, A549 and MCF-7 cell lines. Compounds 3, 5 and iridoid glycoside 11 possessed higher cytotoxicacivities. In short, flavonoids are the main components of cytotoxic extract from C. nudiflora, while phenylethanoid glycosides are the predominant ingredient but inactive to cancer cell lines. In addition, the minor iridoid glycoside expressed weak cytotoxic activity. PMID:25509294

  6. Anti-Aromatase Activity of the Constituents from Damiana (Turnera diffusa)

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Ethnopharmacological relevance: Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac. Aim of the study: The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from T. diffusa. Material and me...

  7. Potential antimutagenic activity of berberine, a constituent of Mahonia aquifolium

    PubMed Central

    Čerňáková, Marta; Košt'álová, Daniela; Kettmann, Viktor; Plodová, Miriam; Tóth, Jaroslav; Dřímal, Ján

    2002-01-01

    Background As part of a study aimed at developing new pharmaceutical products from natural resources, the purpose of this research was twofold: (1) to fractionate crude extracts from the bark of Mahonia aquifolium and (2) to evaluate the strength of the antimutagenic activity of the separate components against one of the common direct-acting chemical mutagens. Methods The antimutagenic potency was evaluated against acridine orange (AO) by using Euglena gracilis as an eukaryotic test model, based on the ability of the test compound/fraction to prevent the mutagen-induced damage of chloroplast DNA. Results It was found that the antimutagenicity of the crude Mahonia extract resides in both bis-benzylisoquinoline (BBI) and protoberberine alkaloid fractions but only the protoberberine derivatives, jatrorrhizine and berberine, showed significant concentration-dependent inhibitory effect against the AO-induced chloroplast mutagenesis of E. gracilis. Especially berberine elicited, at a very low dose, remarkable suppression of the AO-induced mutagenicity, its antimutagenic potency being almost three orders of magnitude higher when compared to its close analogue, jatrorrhizine. Possible mechanisms of the antimutagenic action are discussed in terms of recent literature data. While the potent antimutagenic activity of the protoberberines most likely results from the inhibition of DNA topoisomerase I, the actual mechanism(s) for the BBI alkaloids is hard to be identified. Conclusions Taken together, the results indicate that berberine possesses promising antimutagenic/anticarcinogenic potential that is worth to be investigated further. PMID:11943071

  8. Chemical constituents of Anacolosa pervilleana and their antiviral activities.

    PubMed

    Bourjot, Mélanie; Leyssen, Pieter; Eydoux, Cécilia; Guillemot, Jean-Claude; Canard, Bruno; Rasoanaivo, Philippe; Guéritte, Françoise; Litaudon, Marc

    2012-09-01

    In an effort to identify novel inhibitors of Chikungunya (CHIKV) and Dengue (DENV) virus replication, a systematic study with 820 ethyl acetate extracts of Madagascan plants was performed in a virus-cell-based assay for CHIKV and a DENV NS5 RNA-dependant RNA polymerase (RdRp) assay. The extract obtained from the leaves of Anacolosa pervilleana was selected for its significant activity in both assays. One new (E)-tridec-2-en-4-ynedioic acid named anacolosine (1), together with three known acetylenic acids, the octadeca-9,11,13-triynoic acid (2), (13E)-octadec-13-en-9,11-diynoic acid (3), (13E)-octadec-13-en-11-ynoic acid (4), two terpenoids, lupenone (5) and β-amyrone (6), and one cyanogenic glycoside, (S)-sambunigrin (7) were isolated. Their structures were elucidated by comprehensive analyses of NMR spectroscopy and mass spectrometry data. The inhibitory potency of these compounds was evaluated on CHIKV, DENV RdRp and West-Nile polymerase virus (WNV RdRp). Both terpenoids showed a moderate activity against CHIKV (EC(50) 77 and 86 μM, respectively) and the acetylenic acids produced IC(50) values around 3 μM in the DENV RdRp assay. PMID:22613073

  9. Withanolides: Biologically Active Constituents in the Treatment of Alzheimer's Disease.

    PubMed

    Khan, Shahid A; Khan, Sher B; Shah, Zarbad; Asiri, Abdullah M

    2016-01-01

    The use of natural products in drug discovery and development have an important history. Several therapeutic agents have been investigated during the biological screenings of natural compounds. It is well documented that plants are possibly the core of novel substances that led to the discovery of new, novel, and effective therapeutic agents. Therefore, in the last few decades, scientists were thoroughly attempting for the search of benevolent drugs to protect mankind from various diseases and discomforts. The diverse chemical structures of natural products are the key element of their success in modern drug discovery. Cholinesterase enzyme inhibitors (ChEI) are chemicals which inhibit the splitting of cholinesterase enzymes (acetylcholinesterase and butyrylcholinesterase). Acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) are two types of cholinesterase enzymes that have been identified in vertebrates that are responsible for Alzheimer's disease and related dementia. Withanolides are affective plant secondary metabolites which inhibit acetylcholinesterase and butyrylcholinesterase enzyme and thus possibly will be the future drug for Alzheimer's disease. By viewing the importance of natural products in drug discovery and development, we present here, the importance of withanolides in the treatment of Alzheimer's disease. In this article, we also describe the classification and structural characterization of withanolides. This review comprises of 114 compounds. PMID:26527154

  10. Anti-arthritic active fraction of Capparis spinosa L. fruits and its chemical constituents.

    PubMed

    Feng, Xiaolu; Lu, Jincai; Xin, Hailiang; Zhang, Lei; Wang, Yuliang; Tang, Kexuan

    2011-03-01

    The aim of this study was to ascertain the anti-arthritic active fraction of Capparis spinosa L. (Capparidaceae) fruits and its chemical constituents. The adjuvant arthritic rat model was developed to evaluate the anti-arthritic effects of different fractions of ethanol extraction from C. spinosa L. The fraction eluted by ethanol-water (50:50, v/v) had the most significant anti-arthritic activity. The chemical constituents of this fraction were therefore studied; seven known compounds were isolated and identified as: P-hydroxy benzoic acid; 5-(hydroxymethyl) furfural; bis(5-formylfurfuryl) ether; daucosterol; α-D-fructofuranosides methyl; uracil; and stachydrine. PMID:21372539

  11. Characterization of antiproliferative activity constituents from Artocarpus heterophyllus.

    PubMed

    Zheng, Zong-Ping; Xu, Yang; Qin, Chuan; Zhang, Shuang; Gu, Xiaohong; Lin, Yingying; Xie, Guobin; Wang, Mingfu; Chen, Jie

    2014-06-18

    Artocarpus heterophyllus is an evergreen fruit tree cultivated in many tropical regions. Previous studies have shown that some of its compositions exhibited potential tyrosinase inhibition activities. This study indentified 8 new phenolic compounds, artoheterophyllins E-J (1-6), 4-geranyl-2',3,4',5-tetrahydroxy-cis-stilbene (7), and 5-methoxymorican M (8) and 2 new natural compounds (9 and 10), 2,3-dihydro-5,7-dihydroxy-2-(2-hydroxy-4-methoxyphenyl)-4H-benzopyran-4-one and 6-[(1S,2S)-1,2-dihydroxy-3-methylbutyl]-2-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-3-(3-methyl-2-buten-1-yl)-4H-1-benzopyran-4-one, together with 23 known compounds (11-33), from the ethanol extract of the wood of A. heterophyllus. The structures of the eight new compounds (1-8) and two new natural compounds were established by extensive 1D- and 2D-NMR experiments. The anticancer effects of the isolated compounds were examined in MCF-7, H460, and SMMC-7721 human cancer cell lines by MTT assay. Compounds 5, 11, 12, and 30 significantly reduced the cell viabilities of these cell lines. Especially, compounds 11 and 30 resulted in more potent cytotoxicity than the positive control, 5-fluorouracil (5-Fu), in SMMC-7721 cell line, with IC50 values of 15.85 and 12.06 μM, whereas compound 30 exhibited more potent cytotoxicity than 5-Fu in NCI-H460 cell line, with an IC50 value of 5.19 μM. In addition, this study suggests that compounds 11 and 30 from the wood of A. heterophyllus have anticancer potential via MAPK pathways. PMID:24854862

  12. Velamo do campo: its volatile constituents, secretory elements, and biological activity.

    PubMed

    El Babili, Fatiha; Roques, Christine; Haddioui, Laila; Bellvert, Floriant; Bertrand, Cédric; Chatelain, Christian

    2012-07-01

    The volatile components from Croton campestris root bark were localized by an anatomical study and analyzed by gas chromatography-mass spectrometry for the first time. The roots of this plant showed secretory cells. These volatile constituents, isolated from the dichloromethane extract by hydrodistillation, were analyzed by gas chromatography-mass spectrometry. We found 69 components. They were characterized, and the major constituents of crude oil root barks were spathulenol (23.3%) and borneol (18.7%). Growth inhibitory activity of the active compounds in solution was evaluated by measuring minimal inhibitory concentrations using a broth micromethod. The minimal inhibitory concentration of root bark volatile constituents was 1.56 μg/mL for Staphylococcus aureus, 3.125 μg/mL for Candida albicans, and 6.25 μg/mL for Aspergillusniger. PMID:22612296

  13. Phytochemical profiling of five medicinally active constituents across 14 Eutrema species.

    PubMed

    Hao, Guoqian; Wang, Qian; Liu, Bingbing; Liu, Jianquan

    2016-04-01

    Wasabi or Japanese horseradish (Eutrema japonicum) is both a traditional condiment and a medicinally important plant with diverse uses. Its medicinally active constituents appear to include five isothiocyanates, but their spatial variations in naturally occurring congeners are unknown. Thus, in this study we measured concentrations of these five active constituents in 20 populations of 14 species of Eutrema and one related species, Yinshania sinuata. Three to five of these constituents were detected in each of the examined species, at concentrations that varied greatly between sampled species and populations of the same species. However, two species, Eutrema tenue and Eutrema deltoideum, had higher total concentrations of the five isothiocyanates and substantially higher concentrations of one or two, than the widely cultivated E. japonicum. Thus, both of these species could be important wild resources for artificial cultivation, in addition to the currently widely cultivated E. japonicum. PMID:26946379

  14. Repellent activity of essential oils and some of their individual constituents against Tribolium castaneum herbst.

    PubMed

    Caballero-Gallardo, Karina; Olivero-Verbel, Jesús; Stashenko, Elena E

    2011-03-01

    A tool for integrated pest management is the use of essential oils (EOs) and plant extracts. In this study, EOs from Tagetes lucida , Lepechinia betonicifolia , Lippia alba , Cananga odorata , and Rosmarinus officinalis , species grown in Colombia, were analyzed by gas chromatography-mass spectrometry. These oils as well as several of their constituents were tested for repellent activity against Tribolium castaneum , using the area preference method. The main components (>10%) found in EOs were methylchavicol, limonene/α-pinene, carvone/limonene, benzyl acetate/linalool/benzyl benzoate, and α-pinene, for T. lucida, L. betonicifolia, L. alba, C. odorata, and R. officinalis, respectively. All EOs were repellent, followed a dose-response relationship, and had bioactivity similar to or better than that of commercial compound IR3535. EOs from C. odorata and L. alba were the most active. Compounds from EOs, such benzyl benzoate, β-myrcene, and carvone, showed good repellent properties. In short, EOs from plants cultivated in Colombia are sources of repellents against T. castaneum. PMID:21291237

  15. Smooth muscle relaxant activity of Crocus sativus (saffron) and its constituents: possible mechanisms.

    PubMed

    Mokhtari-Zaer, Amin; Khazdair, Mohammad Reza; Boskabady, Mohammad Hossein

    2015-01-01

    Saffron, Crocus sativus L. (C. sativus) is rich in carotenoids and used in traditional medicine for treatment of various conditions such as coughs, stomach disorders, amenorrhea, asthma and cardiovascular disorders. These therapeutic effects of the plant are suggested to be due to its relaxant effect on smooth muscles. The effect of C. sativus and its constituents on different smooth muscles and the underlying mechanisms have been studied. Several studies have shown the relaxant effects of C. sativus and its constituents including safranal, crocin, crocetin and kaempferol on blood vessels. In addition, it was reported that saffron stigma lowers systolic blood pressure. The present review highlights the relaxant effects of C. sativus and its constituents on various smooth muscles. The possible mechanisms of this relaxing effect including activation of ß2-adrenoceptors, inhibition of histamine H1 and muscarinic receptors and calcium channels and modulation of nitric oxide (NO) are also reviewed. PMID:26468456

  16. Smooth muscle relaxant activity of Crocus sativus (saffron) and its constituents: possible mechanisms

    PubMed Central

    Mokhtari-Zaer, Amin; Khazdair, Mohammad Reza; Boskabady, Mohammad Hossein

    2015-01-01

    Saffron, Crocus sativus L. (C. sativus) is rich in carotenoids and used in traditional medicine for treatment of various conditions such as coughs, stomach disorders, amenorrhea, asthma and cardiovascular disorders. These therapeutic effects of the plant are suggested to be due to its relaxant effect on smooth muscles. The effect of C. sativus and its constituents on different smooth muscles and the underlying mechanisms have been studied. Several studies have shown the relaxant effects of C. sativus and its constituents including safranal, crocin, crocetin and kaempferol on blood vessels. In addition, it was reported that saffron stigma lowers systolic blood pressure. The present review highlights the relaxant effects of C. sativus and its constituents on various smooth muscles. The possible mechanisms of this relaxing effect including activation of ß2-adrenoceptors, inhibition of histamine H1 and muscarinic receptors and calcium channels and modulation of nitric oxide (NO) are also reviewed. PMID:26468456

  17. Anti-Influenza Virus Activity and Constituents. Characterization of Paeonia delavayi Extracts.

    PubMed

    Li, Jinhua; Yang, Xianying; Huang, Linfang

    2016-01-01

    Paeonia delavayi, an endemic species in southwestern China, has been widely used as a traditional remedy for cardiovascular, extravasated blood, stagnated blood and female diseases in traditional Chinese medicine (TCM). However, there are no reports on the anti-influenza virus activity of this species. Here, the anti-influenza virus activity of P. delavayi root extracts was first evaluated by an influenza virus neuraminidase (NA) inhibition assay. Meantime, constituents in the active extracts were identified using ultra-high performance liquid coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and seven major identified constituents were used to further evaluate the NA inhibitory activity. The results showed that the ethyl acetate fraction (EA) and the ethanol fraction (E) of P. delavayi both presented strong NA inhibitory activity with IC50 values of 75.932 μg/mL and 83.550 μg/mL, respectively. Twenty-seven constituents were characterized in these two active extracts by UPLC-Q-TOF-MS analysis, and seven major identified constituents exhibited high activity against the influenza virus. Among them, Benzoylpaeoniflorin (IC50 = 143.701 µM) and pentagalloylglucose (IC50 = 62.671 µM) exhibited the highest activity against the influenza virus, even far stronger than oseltamivir acid (IC50 = 281.308 µM). This study indicated that P. delavayi was a strong NA inhibitor, but cell-based inhibition, anti-influenza virus activity in vivo and anti-influenza virus mechanism still need to be tested and explored. PMID:27571059

  18. Antifungal activities of major tea leaf volatile constituents toward Colletorichum camelliae Massea.

    PubMed

    Zhang, Zheng-Zhu; Li, Ying-Bo; Qi, Li; Wan, Xiao-Chun

    2006-05-31

    A crude glycosidic fraction was prepared from fresh tea leaves and treated with the crude tea enzyme, fractions of cis-3-hexenol, linalool oxide I (cis-furanoid), linalool oxide II (trans-furanoid), linalool, methyl salicylate, geraniol, benzyl alcohol, and 2-phenylethanol were monitored to be the major aglycone moieties by analyzing the released volatiles. The amount of the released aglycone moieties is 5.8 times higher than those in free form. For investigation of the functions of the glycosidically bound form aroma constituents in tea leaves, their antifungal activities were determined by antifungal assay. Geraniol, linalool, methyl salicylate, benzyl alcohol, and 2-phenylethanol exhibited significant antifungal activities toward Colletorichum camelliae Massea, although cis-3-hexenol and linalool oxides showed weaker activities by comparison. Among them, geraniol was shown to be the most potential antifungal substance with a MIC value of 440 microg/mL. The crude glycosidic fraction prepared from tea leaves also exhibited significant antifungal activities in a wide range of concentrations from 2 to 25 mg/mL in a PDA medium. It was deduced that the glycosidically bound volatiles are formed and stored in the intact tissue of tea leaf and hydrolyzed by the actions of both the endogenous and the exogenous glycosidases to release volatiles as antifungal substances when exposed to Colletorichum camelliae Massea. The results suggested that the higher content of the bound form geraniol in tea leaves of var. sinensis might be responsible for their stronger antipathogen properties toward tea leaf blight, as opposed to those of var. assamica. PMID:16719518

  19. Antidiabetic activity of the chemical constituents of Combretum dolichopetalum root in mice

    PubMed Central

    Uzor, Philip F.; Osadebe, Patience O.

    2016-01-01

    The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present study was designed to evaluate the chemical constituents from the root of C. dolichopetalum with a view to identifying the antidiabetic principles. The constituents include the alkaloids, echinulin (1) and arestrictin B (2), the terpenoids, arjunolic acid (3) and 4'-dihydrophaseic acid (4) as well as the phenolic acids, ellagic acid (5) and 3, 4, 3'-tri-O-methylellagic acid (6). Twenty eight mice (in seven groups, n = 4) were made diabetic using alloxan monohydrate (i.p., 120 mg/kg) and treated orally with either the vehicle (control group), any of the constituents or glibenclamide (standard drug). The fasting blood glucose of the diabetic animals was monitored for nine hours. Results showed that all the chemical constituents (1-6) exhibited significant (p < 0.05) antidiabetic activity comparable to glibenclamide. The alkaloids exhibited the most profound antidiabetic activity. The present study has thus identified the antidiabetic principles of C. dolichopetalum root as echinulin, arestrictin B, arjunolic acid, 4'-dihydrophaseic acid, ellagic acid and 3, 4, 3'-tri-O-methylellagic acid. The study has further validated the ethnomedicinal use of the root of C. dolichopetalum in diabetes. PMID:27298614

  20. Antidiabetic activity of the chemical constituents of Combretum dolichopetalum root in mice.

    PubMed

    Uzor, Philip F; Osadebe, Patience O

    2016-01-01

    The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present study was designed to evaluate the chemical constituents from the root of C. dolichopetalum with a view to identifying the antidiabetic principles. The constituents include the alkaloids, echinulin (1) and arestrictin B (2), the terpenoids, arjunolic acid (3) and 4'-dihydrophaseic acid (4) as well as the phenolic acids, ellagic acid (5) and 3, 4, 3'-tri-O-methylellagic acid (6). Twenty eight mice (in seven groups, n = 4) were made diabetic using alloxan monohydrate (i.p., 120 mg/kg) and treated orally with either the vehicle (control group), any of the constituents or glibenclamide (standard drug). The fasting blood glucose of the diabetic animals was monitored for nine hours. Results showed that all the chemical constituents (1-6) exhibited significant (p < 0.05) antidiabetic activity comparable to glibenclamide. The alkaloids exhibited the most profound antidiabetic activity. The present study has thus identified the antidiabetic principles of C. dolichopetalum root as echinulin, arestrictin B, arjunolic acid, 4'-dihydrophaseic acid, ellagic acid and 3, 4, 3'-tri-O-methylellagic acid. The study has further validated the ethnomedicinal use of the root of C. dolichopetalum in diabetes. PMID:27298614

  1. Hypoglycemic activity of leaf organic extracts from Smallanthus sonchifolius: Constituents of the most active fractions.

    PubMed

    Genta, Susana B; Cabrera, Wilfredo M; Mercado, María I; Grau, Alfredo; Catalán, César A; Sánchez, Sara S

    2010-04-29

    The aim of the present study was to determine the in vivo hypoglycemic activity of five organic extracts and enhydrin obtained from yacon leaves. The main constituents of the most active fraction were identified. Five organic extracts and pure crystalline enhydrin were administered to normoglycemic, transiently hyperglycemic and streptozotocin (STZ)-diabetic rats. The fasting and post-prandial blood glucose, and serum insulin levels were estimated and an oral glucose tolerance test (OGTT) was performed for the evaluation of hypoglycemic activity and dose optimization of each extract. We found that the methanol, butanol and chloroform extracts showed effective hypoglycemic activity at minimum doses of 50, 10 and 20mg/kg body weight, respectively, and were selected for further experiments. Oral administration of a single-dose of each extract produced a slight lowering effect in the fasting blood glucose level of normal healthy rats, whereas each extract tempered significantly the hyperglycemic peak after food ingestion. Daily administration of each extract for 8 weeks produced an effective glycemic control in diabetic animals with an increase in the plasma insulin level. Phytochemical analysis of the most active fraction, the butanol extract, showed that caffeic, chlorogenic and three dicaffeoilquinic acids were significant components. Additionally, enhydrin, the major sesquiterpene lactone of yacon leaves, was also effective to reduce post-prandial glucose and useful in the treatment of diabetic animals (minimum dose: 0.8mg/kg body weight). The results presented here strongly support the notion that the phenolic compounds above as well as enhydrin are important hypoglycemic principles of yacon leaves that could ameliorate the diabetic state. PMID:20211156

  2. Cancer Chemoprevention Effects of Ginger and its Active Constituents: Potential for New Drug Discovery.

    PubMed

    Wang, Chong-Zhi; Qi, Lian-Wen; Yuan, Chun-Su

    2015-01-01

    Ginger is a commonly used spice and herbal medicine worldwide. Besides its extensive use as a condiment, ginger has been used in traditional Chinese medicine for the management of various medical conditions. In recent years, ginger has received wide attention due to its observed antiemetic and anticancer activities. This paper reviews the potential role of ginger and its active constituents in cancer chemoprevention. The phytochemistry, bioactivity, and molecular targets of ginger constituents, especially 6-shogaol, are discussed. The content of 6-shogaol is very low in fresh ginger, but significantly higher after steaming. With reported anti-cancer activities, 6-shogaol can be served as a lead compound for new drug discovery. The lead compound derivative synthesis, bioactivity evaluation, and computational docking provide a promising opportunity to identify novel anticancer compounds originating from ginger. PMID:26477795

  3. Antischistosomal Activity of Two Active Constituents Isolated from the Leaves of Egyptian Medicinal Plants

    PubMed Central

    Ali, Sanaa A; El-Regal, Nagy S; Saeed, Samar M

    2015-01-01

    In this paper, we investigate the role of two active constituents isolated from the leaves of Egyptian medicinal plants. D-mannitol a naturally occurring sugar isolated from the leaves Ixora undulata Roxb., and the pectin a linear chain homogalacturonan (HG) polysaccharide isolated from the leaves of Linum grandiflorum Desf. (scarlet flax). Both are evaluated for their therapeutic effect against schistosomiasis with biochemical and histochemical evaluations and compared with praziquantel, a reference drug. Biochemical studies of hepatic glucose, the glycogen content, and total serum protein were carried out, and histochemical evaluations through serum protein fractions separated by polyacrylamide gel electrophoresis with different molecular weights (260–10 kDa) were made in all groups, in addition to liver and body weight. D-mannitol and pectin show a remarkable effect in enhancing liver and kidney functions through enhancing most protein fractions in the serum of mice infected with Schistosoma mansoni. Also, the glucose and glycogen content in injured liver tissues improved, in addition liver and body weight in the infected groups. Thus they may be of therapeutic potential in the treatment hepatoxicity and nephrotoxicity. PMID:26124666

  4. Chemical Constituents from the Fruiting Bodies of Hexagonia apiaria and Their Anti-inflammatory Activity.

    PubMed

    Thang, Tran Dinh; Kuo, Ping-Chung; Ngoc, Nguyen Thi Bich; Hwang, Tsong-Long; Yang, Mei-Lin; Ta, Shih-Huang; Lee, E-Jian; Kuo, Dai-Huang; Hung, Nguyen Huy; Tuan, Nguyen Ngoc; Wu, Tian-Shung

    2015-11-25

    A chemical investigation of the fruiting bodies of Hexagonia apiaria resulted in the identification of nine compounds including five new triterpenoids, hexagonins A-E (1-5), along with four known compounds. The purified constituents were examined for their anti-inflammatory activity. Among the tested compounds, hexatenuin A displayed the most significant inhibition of superoxide anion generation and elastase release. These triterpenoids may have potentials as anti-inflammatory agents. PMID:26575215

  5. Effects of Thymol and Carvacrol, Constituents of Thymus vulgaris L. Essential Oil, on the Inflammatory Response

    PubMed Central

    Fachini-Queiroz, Fernanda Carolina; Kummer, Raquel; Estevão-Silva, Camila Fernanda; Carvalho, Maria Dalva de Barros; Cunha, Joice Maria; Grespan, Renata; Bersani-Amado, Ciomar Aparecida; Cuman, Roberto Kenji Nakamura

    2012-01-01

    Thyme (Thymus vulgaris L., Lamiaceae) is an aromatic and medicinal plant that has been used in folk medicine, phytopharmaceutical preparations, food preservatives, and as an aromatic ingredient. The effect of Thymus vulgaris essential oil (TEO) and its isolated constituents thymol and cavacrol (CVL) were studied in the following experimental models: ear edema, carrageenan-induced pleurisy, and chemotaxis in vitro. In the pleurisy model, TEO, CVL, and thymol significantly inhibited inflammatory edema. However, only TEO and CVL inhibited leukocyte migration. In the in vitro chemotaxis experiment, CVL inhibited leukocyte migration, whereas thymol exerted a potent chemoattractant effect. In the ear edema model, CVL (10 mg/ear), applied topically, reduced edema formation, exerting a topical anti-inflammatory effect. Thymol did not reduce edema formation but rather presented an irritative response, probably dependent on histamine and prostanoid release. Our data suggest that the antiinflammatory effects of TEO and CVL are attributable to the inhibition of inflammatory edema and leukocyte migration. PMID:22919415

  6. Chemical Constituents and Insecticidal Activities of Ajania fruticulosa Essential Oil.

    PubMed

    Liang, Jun-Yu; Guo, Shan-Shan; You, Chun-Xue; Zhang, Wen-Juan; Wang, Cheng-Fang; Geng, Zhu-Feng; Deng, Zhi-Wei; Du, Shu-Shan; Zhang, Ji

    2016-08-01

    The insecticidal activity and chemical constituents of the essential oil from Ajania fruticulosa were investigated. Twelve constituents representing 91.0% of the essential oil were identified, and the main constituents were 1,8-cineole (41.40%), (+)-camphor (32.10%), and myrtenol (8.15%). The essential oil exhibited contact toxicity against Tribolium castaneum and Liposcelis bostrychophila adults with LD50 values of 105.67 μg/adult and 89.85 μg/cm(2) , respectively. The essential oil also showed fumigant toxicity against two species of insect with LC50 values of 11.52 and 0.65 mg/l, respectively. 1,8-Cineole exhibited excellent fumigant toxicity (LC50  = 5.47 mg/l) against T. castaneum. (+)-Camphor showed obvious fumigant toxicity (LC50  = 0.43 mg/l) against L. bostrychophila. Myrtenol showed contact toxicity (LD50  = 29.40 μg/cm(2) ) and fumigant toxicity (LC50  = 0.50 mg/l) against L. bostrychophila. 1,8-Cineole and (+)-camphor showed strong insecticidal activity to some important insects, and they are main constituents of A. fruticulosa essential oil. The two compounds may be related to insecticidal activity of A. fruticulosa essential oil against T. castaneum and L. bostrychophila. PMID:27482698

  7. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents

    PubMed Central

    Coccimiglio, John; Alipour, Misagh; Jiang, Zi-Hua; Gottardo, Christine

    2016-01-01

    Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s) or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol. PMID:27051475

  8. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents.

    PubMed

    Coccimiglio, John; Alipour, Misagh; Jiang, Zi-Hua; Gottardo, Christine; Suntres, Zacharias

    2016-01-01

    Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s) or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol. PMID:27051475

  9. Chemical constituents and antioxidant activity of the essential oil from leaves of Annona vepretorum Mart. (Annonaceae)

    PubMed Central

    Araújo, Camila de Souza; de Oliveira, Ana Paula; Lima, Rafaely Nascimento; Alves, Péricles Barreto; Diniz, Tâmara Coimbra; da Silva Almeida, Jackson Roberto Guedes

    2015-01-01

    Background: Annona vepretorum (AV) is a native tree from Caatinga biome (semiarid region of Brazil) popularly known as “araticum” and “pinha da Caatinga.” Objective: This study was carried out to evaluate the chemical constituents and antioxidant activity (AA) of the essential oil from the leaves from AV (EO-Av) collected in Petrolina, Pernambuco, Brazil. Materials and Methods: Fresh leaves of AV were cut into pieces, and subjected to distillation for 2 h in a clevenger-type apparatus. Gas chromatograph (GC) analyses were performed using a mass spectrometry/flame ionization detector. The identification of the constituents was assigned on the basis of comparison of their relative retention indices. The antioxidant ability of the EO was investigated through two in vitro models such as radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl method and β-carotene-linoleate-model system. The positive controls (ascorbic acid, butylated hydroxyanisole and butylated hydroxytoluene) were those using the standard solutions. Assays were carried out in triplicate. Results: The oil showed a total of 21 components, and 17 were identified, representing 93.9% of the crude EO. Spathulenol (43.7%), limonene (20.5%), caryophyllene oxide (8.1%) and α-pinene (5.5%) were found to be the major individual constituents. Spathulenol and caryophyllene oxide could be considered chemotaxonomic markers of these genera. The EO demonstrated weak AA. PMID:26246740

  10. Major constituents and anthelmintic activity of volatile oils from leaves and flowers of Cymbopogon martini Roxb.

    PubMed

    Nirmal, S A; Girme, A S; Bhalke, R D

    2007-11-01

    The major volatile constituents of leaves and flowers of Cymbopogon martini from the volatile oil obtained by steam distillation were identified by GC/MS. Five constituents were identified from the volatile oil of leaves and flowers, which constituted about 82.49 and 75.63% of the total amount, respectively. A monoterpene, piperitone (6.00%), was identified in the flowers of C. martini; in addition, flowers were found to contain more olefinic terpenes, namely geraniol (69.63%), compared with leaves (53.41%). Leaves contain bicyclic monoterpene, nerol (24.76%) and alpha-pinene (4.32%). Anthelmintic activity of these oils was evaluated on adult Indian earthworms Pheretima posthuma and results showed that the volatile oil of C. martini flower required less time to cause paralysis and death of the earthworms. PMID:17987504

  11. [Research progress on alkaloids constituents from Zanthoxylum and their pharmacological activities].

    PubMed

    Yuan, Hai-mei; Qiu, Lu; Xie, Zhen-jian; Zou, Liang; Zheng, Jin; Fu, Qiang

    2015-12-01

    There are 250 species of Zanthoxylum (Rutaceae) in the world. This genus distributed in tropical and subtropical regions. Alkaloids are the major and representative ingredients in these plants including quinolines, isoquinolines, and amide alkaloids, with such biological activities as anti-tumor, anti-inflammatory, analgesic, anti-virus, anti-platelet aggregation, anti-bacteria and anti- oxidant. These species have been used for a long time to treat toothache, urinary and venereal diseases, lumbago and rheumatism. This review summarizes the chemical constituents and pharmacological activities from the Z. sppplants, in an effort to the systematic research and application of the alkaloids of this genus. PMID:27141666

  12. Diversity of active constituents in Cichorium endivia and Cynara cornigera extracts.

    PubMed

    Hegazy, Ahmad K; Ezzat, Shahira M; Qasem, Iman B; Ali-Shtayeh, Mohamed S; Basalah, Mohammed O; Ali, Hayssam M; Hatamleh, Ashraf A

    2015-03-01

    The present study attempts to explore the phytochemical constituents of different extracts from Cynara cornigera and Cichorium endivia plant materials. The two species studied are native in Egypt. Five different solvents, viz., aqueous, methylene chloride, petroleum ether, ethyl acetate, and n-butanol were used. Phytochemical analysis revealed the presence of phenols, flavonoids, sterols (stigmasterol and beta-sitosterol), terpenes (α-amyrin, ursolic and oleanolic acid), and hydrocarbons (n-alkane), the latter found in low amount. The ethyl acetate and water extracts of C. cornigera root showed lower mass fractions of phenolic compounds ranged from 20 to 81 g/100 g, and higher amounts in ethyl acetate extract of the inflorescences and butanol extract of the root where values ranged from 195 to 399 g/100 g. The β-sitosterol and stigmasterol were present in all plant extracts. Oleanolic and ursolic acids were detected in roots, leaves and inflorescences of C. cornigera and in C. endivia shoot. The ethyl acetate extracts from C. cornigera leaf and inflorescence attained higher chemical diversity than the other extracts. Alternatively, sterols and triterpenes were the major constituents. The high chemical diversity of active constituents justifies the future potential use of the two species at commercial level. PMID:25740442

  13. Antimicrobial Activity and Phytochemical Constituents of Leaf Extracts of Cassia auriculata.

    PubMed

    Murugan, T; Wins, J Albino; Murugan, M

    2013-01-01

    Plants produce a wide variety of phytochemical constituents, which are secondary metabolites and are used either directly or indirectly in the pharmaceutical industry. 'For centuries, man has effectively used various components of plants or their extracts for the treatment of many diseases, including bacterial infections. In the present study methanol, chloroform and aqueous extracts of Cassia auriculata leaf were subjected for antimicrobial activity by well-diffusion method against six bacterial strains namely Bacillus cereus, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Proteus mirabilis. The results revealed that the methanol and chloroform extracts exhibited strong inhibitory activity against all the tested organisms (zone of inhibition of 12-20 mm), except Pseudomonas aeruginosa (zone of inhibition 10 mm or nil). The aqueous extracts showed moderate activity by 'Zone of inhibition ≤12 or nil). The extracts were screened for their phytochemical constituents by standard protocols' and were shown to contain carbohydrates, proteins, alkaloids, flavonoids, steroids, saponins and tannins. The antibacterial activity of these extracts is possibly linked to the presence of flavonoids, steroid, saponins and/or tannins. Further studies are needed to determine the precise active principles from Cassia auriculata. PMID:23901174

  14. Pachira glabra Pasq. essential oil: chemical constituents, antimicrobial and insecticidal activities.

    PubMed

    Lawal, Oladipupo A; Ogunwande, Isiaka A; Salvador, Atinuke F; Sanni, Adetayo A; Opoku, Andy R

    2014-01-01

    The chemical composition of essential oil obtained by hydrodistillation of the leaves of Pachira glabra Pasq., (PgEO) has been studied by Gas Chromatography (GC) and Gas Chromatography coupled with Mass Spectrometry (GC/MS). Thirty three constituents representing 98.4% of total contents were identified from the essential oil. The major constituents of oil were limonene (23.2%), β-caryophyllene (14.5%), phtyol (8.5%) and β-bisabolene (6.3%). The antimicrobial activity of the PgEO was evaluated against a panel of ten bacteria and three fungal strain using agar diffusion and broth microdilution methods. Results have shown that the PgEO exhibited moderate to strong antimicrobial activity against the tested microorganisms except Citrobacter youagae, Micrococcus spp. and Proteus spp. The activity zones of inhibition (ZI) and minimum inhibitory concentrations (MIC) ranged between 13.7 mm-24.0 mm and 0.3 mg/mL-2.5 mg/mL, respectively. The insecticidal activity of PgEO was assayed against the adult Sitophilus zeamais. The lethal concentrations (LC50 and LC90) of the PgEO showed it to be toxic against adult S. zeamais at 32.2 and 53.7 mg/mL, respectively. This is the first report on the chemical composition and in vitro biological activities of essential oil of P. glabra growing in Nigeria. PMID:24881772

  15. Evaluation of Antiplasmodial activity of extracts and constituents from Ampelozizyphus amazonicus

    PubMed Central

    do Carmo, Dominique F. M.; Amaral, Ana Claudia F.; Machado, Marta; Lopes, Dinora; Echevarria, Aurea; Rosário, Virgílio E.; Silva, Jefferson Rocha de A.

    2015-01-01

    Background: Ampelozizyphus amazonicus Ducke, a plant that is widely used by the population of the Amazonian region to prevent and treat malaria, was investigated in this work, which describes, for the first time, the antiplasmodial activity of its extracts and associates this activity with its isolated constituents. Methods: Different extracts with solvents of increasing polarity (hexane, chloroform, ethanol, and water) were obtained of the root bark. This procedure resulted in extracts that were characterized for their constituents. The cytotoxicity and activity of the extracts against Plasmodium berghei (schizontocidal activity, liver stage) and Plasmodium falciparum (3D7 and Dd2 strains, erythrocyte stage) were assessed in vitro. Results: Of the four extracts assayed against P. berghei, the chloroform extract showed the greatest activity, with an inhibitory concentration 50% (IC50) value of 30.1 µg/mL, followed by the aqueous extract (IC50 = 39.9 µg/mL). The chloroform extract exhibited the highest antiplasmodial activity in the erythrocyte stage of P. falciparum, with an IC50 value lower than 15 µg/mL. Fractionation of this more active extract led to the isolation and elucidation of pentacyclic triterpenes, lupeol, betulin and betulinic acid, which showed antiplasmodial activities with IC50 values ranging from 5.6 to 80.30 µM. The most active of these, betulinic acid, was further quantified in the extracts by high-performance liquid chromatography-photodiode array detector analyzes. The higher amount was found in the chloroform extract, which was the most active one against P. falciparum. Conclusion: The results obtained in this work may partly explain the popular intake of A. amazonicusas an antimalarial remedy in the Amazon region. PMID:26664012

  16. Red American Ginseng: Ginsenoside Constituents and Antiproliferative Activities of Heat-Processed Panax quinquefolius Roots

    PubMed Central

    Wang, Chong-Zhi; Aung, Han H.; Ni, Ming; Wu, Ji-An; Tong, Robin; Wicks, Sheila; He, Tong-Chuan; Yuan, Chun-Su

    2009-01-01

    Red Asian ginseng (Panax ginseng C. A. Meyer, Araliaceae) is used in many Oriental countries. In this study, the saponin constituents and anticancer activities of steamed American ginseng (Panax quinquefolius L.) roots were evaluated. The contents of 12 ginsenosides in the roots were determined using high performance liquid chromatography (HPLC). After the steaming treatment (100 – 120 °C for 1 h and 120 °C for 0.5 – 4 h), the quantity of 7 ginsenosides decreased and that of 5 others increased. The content of ginsenoside Rg3, a previously recognized anticancer compound, increased significantly when the root was steamed at 120 °C for 0.5 – 3 h. The antiproliferative effects of unsteamed and steamed (120 °C for 1 h and 2 h) American ginseng root extracts were assayed by the modified trichrome stain (MTS) method using three cancer cell lines (SW-480, HT-29, NSCLC). Heat-processing increased the antiproliferative effect of American ginseng significantly, and the activity of the extract from roots steamed for 2 h was greater than that of roots steamed for 1 h. Chemical constituents and antiproliferative activities of white and red Asian ginseng have also been evaluated. Five representative ginsenosides, Rb1, Rd, Re, Rg2 and Rg3, were studied. Ginsenoside Rg3 had the most potent effect. The antiproliferative activities of red American ginseng are augmented when ginsenoside Rg3 is increased. PMID:17538869

  17. Chemical constituents and activities of the essential oil from Myristica fragrans against cigarette beetle Lasioderma serricorne.

    PubMed

    Du, Shu-Shan; Yang, Kai; Wang, Cheng-Fang; You, Chun-Xue; Geng, Zhu-Feng; Guo, Shan-Shan; Deng, Zhi-Wei; Liu, Zhi-Long

    2014-09-01

    Essential oil extracted from nutmeg seeds (Myristica fragrans Houtt.) by hydrodistillation was subjected to GC/MS and GC analysis. A total of 27 constituents were identified, of which eugenol (19.9%), methylisoeugenol (16.8%), methyleugenol (16.7%), sabinene (11.8%), and terpinen-4-ol (8.5%) were the major components. The essential oil was tested against Lasioderma serricorne for insecticidal and repellent activity, the LD50 value at the end of 24 h exposure period was 19.3 μg/adult. Six active compounds were isolated by bioassay-guided fractionation. They were identified as eugenol (1), methyleugenol (2), methylisoeugenol (3), elemicin (4), myristicin (5), and safrole (6). Among these isolates, 4 showed the strongest contact toxicity against L. serricorne adults with an LD50 value of 9.8 μg/adult. Repellency of crude oil and active compounds were also determined. Compounds 1, 2, 4, and 5 were strongly repellent against the cigarette beetle and exhibited the same level of repellency compared with the positive control, DEET. The results indicate that the essential oil of M. fragrans and its active constituents have potential for development as natural insecticides and repellents to control L. serricorne. PMID:25238085

  18. Chemical constituents of Phragmanthera austroarabica A. G. Mill and J. A. Nyberg with potent antioxidant activity

    PubMed Central

    Badr, Jihan M.

    2015-01-01

    Background: Phragmanthera austroarabica A.G. Mill. and J. A. Nyberg is a semi parasitic plant belonging to family Loranthaceae. It was collected from Saudi Arabia. It is widely used in folk medicine among the kingdom in treatment of various diseases including diabetes mellitus. Objective: The total alcoholic extract of P. austroarabica collected from Saudi Arabia was investigated for the chemical structure and prominent biological activity of the main constituents. Materials and Methods: Isolation of the active constituents was performed using different chromatographic techniques including column chromatography packed with silica or sephadex and preparative thin layer chromatography. The structures of the isolated compounds were established based on different spectroscopic data as mass spectrum, one-dimensional and two-dimensional nuclear magnetic resonance (correlation spectroscopy, heteronuclear single quantum coherence, and heteronuclear multiple-bond correlation). Results: Phytochemical investigation of the plant resulted in isolation of 12 compounds. The isolated compounds were identified as chrysophanic acid, emodin, chrysophanic acid-8-O-glucoside, emodin-8-O-glucoside, pectolinarigenin, quercetin, dillenetin-3-O-glucoside, catechin, catechin-4’-O-gallate, methyl gallate, lupeol and ursolic acid. All the isolated phenolic compounds revealed significant free radical scavenging activities when tested using 2,2-diphenyl-1-picrylhydrazyl reagent. Conclusion: The antioxidant activities of the isolated compounds can justify the use of P. austroarabica in traditional medicine for treatment of diabetes and verify its possible application as an antihyperglycemic drug. PMID:26692747

  19. Antioxidant, larvicidal and antiacetylcholinesterase activities of cashew nut shell liquid constituents.

    PubMed

    Oliveira, Micheline Soares Costa; Morais, Selene Maia de; Magalhães, Davi Varela; Batista, Williams Pereira; Vieira, Icaro Gusmão Pinto; Craveiro, Afrânio Aragão; de Manezes, Jane Eire Silva Alencar; Carvalho, Ana Fontenelle Urano; de Lima, Glauber Pacelli Gomes

    2011-03-01

    Anacardic acid, cardanol and cardol, the main constituents of natural cashew nut shell liquid (CNSL), were obtained by solvent extraction and assayed for antioxidant, larvicidal and antiacetylcholinesterase activity. Their relative percent composition was obtained by HPLC analysis. Antioxidant activity was assessed using the DPPH and ABTS(+) tests, which showed cardanol as the most active, followed by cardol and anacardic acid. The three CNSL components demonstrated good larvicidal activity against Aedes aegypti (LC(50)=12.40 for anacardic acid, 10.22 for cardol and 14.45 for cardanol) and exhibited inhibition zones for acetylcholinesterase enzymes in the TLC test similar to carbachol, which was used as standard. Based on the results, these multipotent compounds represent promising agents in the control of Ae. aegypti, the main dengue vector in Brazil. PMID:20707981

  20. Antidepressant-like activity of adhyperforin, a novel constituent of Hypericum perforatum L.

    PubMed Central

    Tian, Jingwei; Zhang, Fangxi; Cheng, Jucan; Guo, Shuren; Liu, Pinglan; Wang, Hongbo

    2014-01-01

    Adhyperforin is a novel constituent of Hypericum perforatum L., but its antidepressant-like activity remains unclear. To explore that, several well-validated animal models of depression as well as neurotransmitter reuptake and transporter binding assays were conducted. The results showed adhyperforin could reduce the immobility time of mice in the forced swimming test and tail suspension assay, antagonize the behaviors induced by reserpine, and have no effect on locomotor activity. Furthermore, following establishment of a chronic unpredictable mild stress model, adhyperforin increased the number of crossings and rearings in rats in the open field test and increased the sucrose consumption. Finally, adhyperforin inhibited uptake of serotonin, norepinephrine, and dopamine, and displayed robust binding affinities for the serotonin and norepinephrine transporters. Overall, the current study provides the first evidence that adhyperforin is a novel, active ingredient of Hypericum perforatum L. with robust antidepressant-like activity. PMID:25005489

  1. Black Cumin (Nigella sativa) and Its Active Constituent, Thymoquinone: An Overview on the Analgesic and Anti-inflammatory Effects.

    PubMed

    Amin, Bahareh; Hosseinzadeh, Hossein

    2016-01-01

    For many centuries, seeds of Nigella sativa (black cumin), a dicotyledon of the Ranunculaceae family, have been used as a seasoning spice and food additive in the Middle East and Mediterranean areas. Traditionally, the plant is used for asthma, hypertension, diabetes, inflammation, cough, bronchitis, headache, eczema, fever, dizziness, and gastrointestinal disturbances. The literature regarding the biological activities of seeds of this plant is extensive, citing bronchodilative, anti-inflammatory, antinociceptive, antibacterial, hypotensive, hypolipidemic, cytotoxic, antidiabetic, and hepatoprotective effects. The active ingredients of N. sativa are mainly concentrated in the fixed or essential oil of seeds, which are responsible for most health benefits. This review will provide all updated reported activities of this plant with an emphasis on the antinociceptive and anti-inflammatory effects. Results of various studies have demonstrated that the oil, extracts, and their active ingredients, in particular, thymoquinone, possess antinociceptive and anti-inflammatory effects, supporting the common folk perception of N. Sativa as a potent analgesic and anti-inflammatory agent. Many protective properties are attributed to reproducible radical scavenging activity as well as an interaction with numerous molecular targets involved in inflammation, including proinflammatory enzymes and cytokines. However, there is a need for further investigations to find out the precise mechanisms responsible for the antinociceptive and anti-inflammatory effects of this plant and its active constituents. PMID:26366755

  2. Fractionation and identification of minor and aroma-active constituents in Kangra orthodox black tea.

    PubMed

    Joshi, Robin; Gulati, Ashu

    2015-01-15

    The aroma constituents of Kangra orthodox black tea were isolated by simultaneous distillation extraction (SDE), supercritical fluid extraction and beverage method. The aroma-active compounds were identified using gas chromatography-olfactometry-mass spectrometry. Geraniol, linalool, (Z/E)-linalool oxides, (E)-2-hexenal, phytol, β-ionone, hotrienol, methylpyrazine and methyl salicylate were major volatile constituents in all the extracts. Minor volatile compounds in all the extracts were 2-ethyl-5-methylpyrazine, ethylpyrazine, 2-6,10,14-trimethyl-2-pentadecanone, acetylfuran, hexanoic acid, dihydroactinidiolide and (E/Z)-2,6-nonadienal. The concentrated SDE extract was fractionated into acidic, basic, water-soluble and neutral fractions. The neutral fraction was further chromatographed on a packed silica gel column eluted with pentane and diethyl ether to separate minor compounds. The aroma-active compounds identified using gas chromatography-olfactometry-mass spectrometry were 2-amylfuran, (E/Z)-2,6-nonadienal, 1-pentanol, epoxylinalool, (Z)-jasmone, 2-acetylpyrrole, farnesyl acetone, geranyl acetone, cadinol, cubenol and dihydroactinidiolide. AEDA studies showed 2-hexenal, 3-hexenol, ethylpyrazine, (Z/E)-linalool oxides, linalool, (E/Z)-2,6-nonadienal, geraniol, phenylethanol, β-ionone, hotrienol and dihydroactinidiolide to be odour active components. PMID:25148991

  3. Quantification of Phenolic Constituents and Antioxidant Activity of Pterodon emarginatus Vogel Seeds

    PubMed Central

    Dutra, Rafael C.; Leite, Magda N.; Barbosa, Nádia R.

    2008-01-01

    In the present study the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents and the antioxidant activity of Pterodon emarginatus seeds were investigated in several samples prepared with different extraction procedures: essential oil (EO) using a Clevenger-type apparatus; hexanic (HF), ethyl acetate (EAF), buthanolic (BF) and methanolic (MF) fractions using Soxhlet extraction, and extracts (1 g/extract) obtained from different methods: reflux 80°C/30 min, ultrasound/30 min, static maceration/48 h and heating plate 100°C/45 min. These extracts were prepared using water or ethanol/water at 30:70 v/v, 50:50 v/v or 70:30 v/v. Antioxidant activity [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH)] was tested only in the fractions obtained from Soxhlet extraction. The extract obtained from reflux using ethanol/water (70:30, v/v) showed the highest phenolic constituents level. The EAF, BF and MF showed DPPH scavenging activities with IC50=163.22, 18.89 and 10.15 μg/ml, respectively. PMID:19325773

  4. Quantification of phenolic constituents and antioxidant activity of Pterodon emarginatus vogel seeds.

    PubMed

    Dutra, Rafael C; Leite, Magda N; Barbosa, Nádia R

    2008-04-01

    In the present study the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents and the antioxidant activity of Pterodon emarginatus seeds were investigated in several samples prepared with different extraction procedures: essential oil (EO) using a Clevenger-type apparatus; hexanic (HF), ethyl acetate (EAF), buthanolic (BF) and methanolic (MF) fractions using Soxhlet extraction, and extracts (1 g/extract) obtained from different methods: reflux 80 degrees C/30 min, ultrasound/30 min, static maceration/48 h and heating plate 100 degrees C/45 min. These extracts were prepared using water or ethanol/water at 30:70 v/v, 50:50 v/v or 70:30 v/v. Antioxidant activity [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH)] was tested only in the fractions obtained from Soxhlet extraction. The extract obtained from reflux using ethanol/water (70:30, v/v) showed the highest phenolic constituents level. The EAF, BF and MF showed DPPH scavenging activities with IC(50)=163.22, 18.89 and 10.15 microg/ml, respectively. PMID:19325773

  5. Antibacterial activity of leaf essential oil and its constituents from Cinnamomum longepaniculatum

    PubMed Central

    Li, Li; Li, Zheng-Wen; Yin, Zhong-Qiong; Wei, Qin; Jia, Ren-Yong; Zhou, Li-Jun; Xu, Jiao; Song, Xu; Zhou, Yi; Du, Yong-Hua; Peng, Lian-Ci; Kang, Shuai; Yu, Wang

    2014-01-01

    Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922 and Salmonella enteritidis CMCC (B) 50041, were used in the antibacterial tests of Cinnamomum longepaniculatum leaf essential oil and its five chemical constituents. The effect of 1, 8-cineole on the ultrastructural structure of the bacteria (S. aureus and E. coli) was also investigated by transmission electron microscopy. The C. longepaniculatum leaf essential oil and the five chemical constituents showed variable levels of inhibition. Their MIC ( minimum inhibitory concentration ) and MBC (minimal bacteriocidal concentration) values were all in the range of 0.781 µL/mL~6.25 µL/mL and 0.781 µL/mL~12.5 µL/mL respectively except γ-terpinene. The MIC values of γ-terpinene against E. coli and S. aureus were all higher than 50 µL/mL, but the MIC and MBC values of γ-terpinene against S. enteritidis was only 3.125 µL/mL. Among them, α-terpineol possessed the best antibacterial activity. Under the transmission electron microscope, cell size of treated E. coli decreased, cell wall and cell membrane ruptured, and nucleoplasm was reduced and gathered onto the side. After the S. aureus was treated with 1, 8-cineole, the cell size and shape were damaged and nucleus cytoplasm was concentrated or reduced or agglomerated on the side. These results suggest that C. longepaniculatum leaf essential oil and its constituents have excellent antibacterial activities, the antibacterial mechanism of 1, 8-cineole against E. coli and S. aureus might attributable to its hydrophobicity. PMID:25126170

  6. Antihyperglycemic activity of kinsenoside, a high yielding constituent from Anoectochilus roxburghii in streptozotocin diabetic rats.

    PubMed

    Zhang, Yonghui; Cai, Jinyan; Ruan, Hanli; Pi, Huifang; Wu, Jizhou

    2007-11-01

    Different doses of kinsenoside, a high yielding constituent from Anoectochilus roxburghii, was orally administered to further investigate its biological activity and pharmacological mechanisms that involve in the hypoglycemic effect on streptozotocin (STZ) diabetic rats. Our study showed that this compound exhibited significantly antihyperglycemic activity at the dose of 15mg/kg body weight, which is speculated to be partially attributed to modulating the activity of enzymatic antioxidants, scavenging free radicals, and reducing the content of factor NO. Much more intact beta cells in the islets of Langerhans with denser insulin in kinsenoside-treated groups than the negative control were observed, which greatly supported the morphological and functional elucidation. These results displayed that kinsenoside could be useful for repairing beta cells in pancreatic islet injury as well as improving its function. The OGTT evidenced that this compound could promote the glucose tolerance of acute glucose increase in both diabetic and normal healthy rats. PMID:17869039

  7. Phenolic constituents from the aerial parts of Glycyrrhiza inflata and their antibacterial activities.

    PubMed

    Zhou, Biao; Wan, Chuan-Xing

    2015-01-01

    Chemical investigation on 90% ethanol extracts of the aerial parts of Glycyrrhiza inflata afforded two new phenolic constituents, 2-(3-methyl-2-butenyl)-3,5,4'-trihydroxy-bibenzyl (1) and (2S)-6-[(E)-3-hydroxymethyl-2-butenyl]-3',4',5,7-tetrahydroxy-dihydroflavanone (2) along with seven known dihydroflavanones (3-9). Compounds 1-9 were tested for their minimum inhibitory concentration (MIC) values of inhibiting Staphylococcus aureus and Staphylococcus epidermidis. Compound 1 showed moderate antibacterial activities against both S. aureus (MIC of 50.00 μg/ml) and S. epidermidis (MIC of 12.50 μg/ml). The analysis of structure-activity relationships revealed that the antibacterial activity of dihydroflavanones (2-9) was significantly affected by the position of prenyl group. PMID:25315253

  8. Biological activities of crude extracts and chemical constituents of Bael, Aegle marmelos (L.) Corr.

    PubMed

    Maity, Pallab; Hansda, Dhananjay; Bandyopadhyay, Uday; Mishra, Dipak Kumar

    2009-11-01

    Bael (Aegle marmelos (L.) Corr.) is an important medicinal plant of India. Leaves, fruits, stem and roots of A. marmelos have been used in ethno medicine to exploit its' medicinal properties including astringent, antidiarrheal antidysenteric, demulcent, antipyretic and anti-inflammatory activities. Compounds purified from bael have been proven to be biologically active against several major diseases including cancer, diabetes and cardiovascular diseases. Preclinical studies indicate the therapeutic potential of crude extracts of A. marmelos in the treatment of many microbial diseases, diabetes and gastric ulcer. This review covers the biological activities of some isolated chemical constituents of A. marmelos and preclinical studies on some crude extracts and pure compounds to explore novel bioactive compounds for therapeutic application. PMID:20099458

  9. Chemical constituents, antioxidant and antimocrobial activity of essential oil of Pogostemon paniculatus (Willd.).

    PubMed

    Manoj, Godbole; Manohar, Shiragambi Hanumantagouda; Murthy, Hosakatte Niranjana

    2012-01-01

    The essential oil extracted from the leaves of Pogostemon paniculatus (Willd.) Benth. (Lamiaceae), was analysed by gas chromatography-mass spectrometry (GC-MS). Nineteen compounds constituting 85.36% of the total oil were identified in the oil. Patchouli alcohol (30.65%), α-guaiene (10.67%), β-guaiene (9.09%), caryophyllene (8.64%), eicosene (5.27%) were the major constituents present. The essential oil was analysed for antimicrobial activity by disc diffusion assay and minimum inhibition concentration against six bacteria and three fungi. Results showed inhibitory activity against some of the tested microorganisms. The essential oil was also tested for the DPPH free-radical scavenging activity and had an inhibitory concentration (IC(50)) value of 18.5 µg mL(-1). PMID:22132692

  10. Inhibitory activity of Filipendula ulmaria constituents on recombinant human histidine decarboxylase.

    PubMed

    Nitta, Yoko; Kikuzaki, Hiroe; Azuma, Toshiaki; Ye, Yuan; Sakaue, Motoyoshi; Higuchi, Yoshiki; Komori, Hirohumi; Ueno, Hiroshi

    2013-06-01

    Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine. Agents that control HDC activity are beneficial for treating histamine-mediated symptoms, such as allergies and stomach ulceration. We searched for inhibitors of HDC from the ethyl acetate extract of the petal of Filipendula ulmaria, also called meadowsweet. Rugosin D, rugosin A, rugosin A methyl ester (a novel compound), and tellimagrandin II were the main components; these 4 ellagitannins exhibited a non-competitive type of inhibition, with K(i) values of approximately 0.35-1 μM. These K(i) values are nearly equal to that of histidine methyl ester (K(i)=0.46 μM), an existing substrate analogue inhibitor. Our results show that food products contain potent HDC inhibitors and that these active food constituents might be useful for designing clinically available HDC inhibitors. PMID:23411280

  11. Antimicrobial, antiviral and cytotoxic activity of extracts and constituents from Polygonum spectabile Mart.

    PubMed

    Brandão, Geraldo Célio; Kroon, Erna Gessien; Duarte, Maria Gorette R; Braga, Fernão Castro; de Souza Filho, José Dias; de Oliveira, Alaíde Braga

    2010-10-01

    Polygonum spectabile is used in Brazil for treatment of several infection diseases. Extracts and constituents isolated from this species were evaluated for cytotoxicity and effects on 15 bacterias and yeasts as well on 4 viruses strains (HHV-1, VACV-WR, EMCV, DEN-2). Less polar extracts were effective against Staphylococcus aureus, Bacillus subtillis, Micrococcus luteus, M. canis and Tricophyton mentagrophytes and T. rubrum. Two known chalcones and 3-O-β-D-glucosyl-β-sitosterol were isolated. The ethanol extract was the only one to show antiviral activity (CE50 < 30 μg/ml). One chalcone has inhibited the growth of several bacteria and was significantly active against dermathophytes. The 3 compounds isolated have shown moderate cytotoxicity against Vero and LLCMK(2) cells (CC(50) < 50 μg/ml). These results support the use of P. spectabile as antimicrobial agent. PMID:20382006

  12. Chemical Constituents from the Fruits of Forsythia suspensa and Their Antimicrobial Activity

    PubMed Central

    Chen, Guo-Feng; Yang, Mei-Lin; Lin, Ya-Hua; Peng, Chi-Chung

    2014-01-01

    Lignans and phenylethanoid glycosides purified from Forsythia suspensa were reported to display various bioactivities in the previous literature, including the antimicrobial activity. Therefore, the present research is aimed to purify and identify the chemical constituents of the methanol extracts of fruits of F. suspensa. The methanol extracts of fruits of F. suspensa were fractionated and further purified with the assistance of column chromatography to afford totally thirty-four compounds. Among these isolates, 3β-acetoxy-20α-hydroxyursan-28-oic acid (1) was reported from the natural sources for the first time. Some of the purified principles were subjected to the antimicrobial activity examinations against Escherichia coli to explore new natural lead compounds. PMID:24745011

  13. Antibacterial Activity of Essential Oils and Their Isolated Constituents against Cariogenic Bacteria: A Systematic Review.

    PubMed

    Freires, Irlan Almeida; Denny, Carina; Benso, Bruna; de Alencar, Severino Matias; Rosalen, Pedro Luiz

    2015-01-01

    Dental caries remains the most prevalent and costly oral infectious disease worldwide. Several methods have been employed to prevent this biofilm-dependent disease, including the use of essential oils (EOs). In this systematic review, we discuss the antibacterial activity of EOs and their isolated constituents in view of a potential applicability in novel dental formulations. Seven databases were systematically searched for clinical trials, in situ, in vivo and in vitro studies addressing the topic published up to date. Most of the knowledge in the literature is based on in vitro studies assessing the effects of EOs on caries-related streptococci (mainly Streptococcus mutans) and lactobacilli, and on a limited number of clinical trials. The most promising species with antibacterial potential against cariogenic bacteria are: Achillea ligustica, Baccharis dracunculifolia, Croton cajucara, Cryptomeria japonica, Coriandrum sativum, Eugenia caryophyllata, Lippia sidoides, Ocimum americanum, and Rosmarinus officinalis. In some cases, the major phytochemical compounds determine the biological properties of EOs. Menthol and eugenol were considered outstanding compounds demonstrating an antibacterial potential. Only L. sidoides mouthwash (1%) has shown clinical antimicrobial effects against oral pathogens thus far. This review suggests avenues for further non-clinical and clinical studies with the most promising EOs and their isolated constituents bioprospected worldwide. PMID:25911964

  14. Hydrophobic constituents and their potential anticancer activities from Devil’s Club Oplopanax horridus

    PubMed Central

    Sun, Shi; Du, Guang-Jian; Qi, Lian-Wen; Williams, Stainley; Wang, Chong-Zhi; Yuan, Chun-Su

    2011-01-01

    Ethnopharmacological relevance Devil’s Club Oplopanax horridus (Sm.) Miq. is a widely used folk medicine in the Pacific Northwest such as Alaska and British Columbia for treating a variety of ailments including arthritis, cold, fever, infections, diabetes and cancer. Aim of the study To investigate hydrophobic constituents and their potential anticancer activity from Devil’s Club O. horridus. Materials and methods The root bark of O. horridus (Sm.) Miq was isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods and comparison with published data. The anti-proliferation of isolated hydrophobic constituents in human breast cancer MCF-7 cells, human colon cancer SW-480 and HCT-116 cells were tested. The potential mechanism of anti-proliferation was also investigated using cell cycle and apoptosis assays. Results and discussion Six compounds were isolated and structurally identified as 9,17-octadecadiene-12,14-diyne-1,11,16-triol, 1-acetate (1), oplopandiol acetate (2), falcarindiol (3), oplopandiol (4), trans-nerolidol (5) and t-cadinol (6). These compounds showed potential anticancer activities on human breast cancer and colon cancer cells, of which compound 3 possesses the strongest activity. Further cell cycle and apoptosis test by flow cytometry showed the polyacetylenes 1–4 induced HCT-116 cell arresting in G2/M phase and inhibited proliferation by the induction of apoptosis at both earlier and later stage. Conclusion These results provide promising baseline information for the potential use of O. horridus as well as some of the isolated compounds in the treatment of cancer. PMID:20723598

  15. Comparison of Essential Oil Content, Constituents, and Antioxidant Activity of Nepeta Glomerulosa during Three Developmental Stages

    NASA Astrophysics Data System (ADS)

    Moradi, H.; Azizi, M.; Rowshan, V.

    2014-12-01

    The genus Nepeta with the common Persian name "Pune-Sa" is one of the most important genera of Lamiaceae family. More than 250 species in the world and 67 annual or perennial species in Iran have been reported. Some of these species are valuable in medicine and are used for medicinal purposes. The aim of this study was to identify essential oil content, its chemical composition, and antioxidant activity in the N. glomerulosa during vegetative, flowering and seed set stages. The samples of N. glomerulosa in the three above-mentioned stages were collected from Abade region of Fars Province. The essential oil was obtained though hydrodistillation and was analyzed by GC and GC/MS. Essential oil of the plant in vegetative, flowering and seed set stages were measured to be 55, 53 and 53 components, respectively, with geranyl acetate (16.644%, 18.182% and 24.441%), geraniol (10.797%, 11.372% and 12.389%), caryophyllene oxide (8.302%, 10.515% and 6.661%), humulene epoxide ΙΙ (7.974%, 7.112% and 2.587%), α-pinene (4.743%, 4.126% and 6.724%), limonene (4.086%, 3.848% and 4.711%) and 1,8-cineol (3.397%, 4.609% and 3.759%) being the major components of the essential oil. The results confirmed that phonological stages have a significant effect on essential oils constituents. Geranyl acetate and geraniol increased by development of plant from vegetative to seed set stage and geranyl acetate was the main essential oils constituent of the plants throughout the three phonological stages. Antioxidant activity in flowering and seed set stages was significantly higher than vegetative stage, but compared with Gallic acid, which is a very strong antioxidant substance, had insignificant antioxidant activity.

  16. Chemical Constituents and Antimicrobial Activity of Indian Green Leafy Vegetable Cardiospermum halicacabum.

    PubMed

    Jeyadevi, R; Sivasudha, T; Ilavarasi, A; Thajuddin, N

    2013-06-01

    The present study was carried out to analyze chemical constituents and antibacterial activity of ethanolic leaf extract of Cardiospermum halicacabum (ECH). The FT-IR spectrum confirmed the presence of alcohols, phenols, alkanes, alkynes, aliphatic ester and flavonoids in ECH. The GC-MS analysis revealed that ECH contained about twenty four compounds. The major chemical compounds identified were cyclohexane-1, 4, 5-triol-3-one-1-carboxylic acid, benzene acetic acid, caryophyllene, phytol and neophytadiene. The ECH was screened for its antibacterial activity against different bacterial strains and anti fungal activity against Candida albicans by agar well diffusion and minimum inhibitory concentration (MIC) assay. ECH exhibited antibacterial and antifungal activity. All the tested bacterial strains showed MIC values ranging from 80 to 125 μg of extract/ml and C. albicans showed 190 μg of extract/ml as a MIC. The maximum activity ECH was observed against human pathogen Staphylococcus aureus followed by Escherichia coli and the fish pathogen Aeromonas hydrophila. ECH exhibited moderate activity against some of the tested multidrug resistant strains. PMID:24426110

  17. Active Constituents from Liriope platyphylla Root against Cancer Growth In Vitro

    PubMed Central

    Wu, Chin-Chung; Cheng, Ti-Sheng; Kuo, Ching-Ying; Tsai, Yu-Chi; Chiang, Shang-Yu; Wong, Teng-Song; Wu, Yang-Chang; Chang, Fang-Rong

    2013-01-01

    Liriope spicata is a well-known herb in traditional Chinese medicine, and its root has been clinically demonstrated to be effective in the treatment of metabolic and neural disorders. The constituents isolated from Liriope have also recently been shown to possess anticancer activity, although the mechanism of which remains largely unknown. Here, we illustrate the anticancer activity of LPRP-9, one of the active fractions we fractionated from the Liriope platyphylla root part (LPRP) extract. Treatment with LPRP-9 significantly inhibited proliferation of cancer cell lines MCF-7 and Huh-7 and down-regulated the phosphorylation of AKT. LPRP-9 also activates the stress-activated MPAK, JNK, p38 pathways, the p53 cell-cycle checkpoint pathway, and a series of caspase cascades while downregulating expression of antiapoptotic factors Bcl-2, Bcl-XL, and survivin. Such activities strongly suggest a role for LPRP-9 in apoptosis and autophagy. We further purified and identified the compound (−)-Liriopein B from LPRP-9, which is capable of inhibiting AKT phosphorylation at low concentration. The overall result highlights the anticancer property of LPRP-9, suggests its mechanism for inhibition of proliferation and promotion of cell death for cancer cells via regulation of multitarget pathways, and denotes the importance of purifying components of fraction LPRP-9 to aid cancer therapy. PMID:23762164

  18. Chemical Constituents of the Culture Broth of Phellinus linteus and Their Antioxidant Activity

    PubMed Central

    Lee, Myeong-Seok; Hwang, Byung Soon; Lee, In-Kyoung; Seo, Geon-Sik

    2015-01-01

    The medicinal fungus Phellinus linteus, in the family Hymenochaetaceae, has been used as a traditional medicine for the treatment of various diseases. In this study, the chemical constituents of the culture broth of P. linteus were investigated. P. linteus was cultured in potato dextrose broth medium, and the culture broth was extracted with ethyl acetate. The ethyl acetate-soluble portion was concentrated and subjected to ODS column chromatography, followed by Sephadex LH-20 column chromatography. Six compounds (1~6) were purified by preparative reversed-phase high-performance liquid chromatography. Spectroscopic methods identified their structures as caffeic acid (1), inotilone (2), 4-(3,4-dihydroxyphenyl)-3-buten-2-one (3), phellilane H (4), (2E,4E)-(+)-4'-hydroxy-γ-ionylideneacetic acid (5), and (2E,4E)-γ-ionylideneacetic acid (6). Compounds 1, 2, and 3 exhibited potent dose-dependent antioxidant activity. PMID:25892914

  19. In vitro antiprotozoal activity of triterpenoid constituents of Kleinia odora growing in Saudi Arabia.

    PubMed

    Al Musayeib, Nawal M; Mothana, Ramzi A; Gamal, Ali A El; Al-Massarani, Shaza M; Maes, Louis

    2013-01-01

    Two lupane and four ursane triterpenes, namely epilupeol (1), lupeol acetate (2), ursolic acid (3), brein (4), 3β 11α-dihydroxy urs-12-ene (5) and ursolic acid lactone (6) were isolated from aerial parts of Kleinia odora and identified. Compounds 1 and 3-6 were isolated for the first time from K. odora. The triterpene constituents were investigated for antiprotozoal potential against erythrocytic schizonts of Plasmodium falciparum, intracellular amastigotes of Leishmania infantum and Trypanosoma cruzi and free trypomastigotes of T. brucei. Cytotoxicity was determined against MRC-5 fibroblasts to assess selectivity. The ursane triterpenes were found to be active against more than one type of the tested parasites, with the exception of compound 6. This is also the first report on the occurrence of ursane type triterpenes in the genus Kleinia and their antiprotozoal potential against P. falciparum, L. infantum, T. cruzi, and T. brucei. PMID:23912274

  20. Bioactive constituents of Homalomena aromatica essential oil and its antifungal activity against dermatophytes and yeasts.

    PubMed

    Policegoudra, R S; Goswami, S; Aradhya, S M; Chatterjee, S; Datta, S; Sivaswamy, R; Chattopadhyay, P; Singh, L

    2012-03-01

    Homalomena aromatica rhizomes are rich source of essential oils, which have been attributed for various medicinal uses. In the present investigation, essential oil from H. aromatica rhizomes was isolated and subjected to gas chromatography-mass spectrum (GC-MS) analysis. Fifty-five chemical constituents were reported from H. aromatica rhizomes of which T-muurolol (5.32%), viridiflorol (3.69%), α-selinene (2.19%), M-cymene (2.19%) and γ-Muurolene (1.81%) were identified and reported for the first time. Other major components were identified as linalool (62.5%), terpene-4-ol (7.08%), δ-cadinene (5.57%), α-cadinol (3.71%) and spatulenol (1.81%). H. aromatica rhizome essential oil showed high antimicrobial activity against Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum fulvum, Microsporum gypseum, Trichosporon beigelii and Candida albicans. PMID:23177818

  1. Influence of harvest season on antioxidant activity and constituents of rabbiteye blueberry ( Vaccinium ashei ) leaves.

    PubMed

    Zhu, Liancai; Liu, Xi; Tan, Jun; Wang, Bochu

    2013-11-27

    To select rabbiteye blueberry leaves from an appropriate harvest season to develop functional foods, this paper studied the bioactive secondary metabolites and the antioxidant capacity of rabbiteye blueberry leaves from May, September, and November. The results showed the leaves from May had the highest content of total flavonoids (114.21 mg/g) and the leaves from November had the highest content of total polyphenols and proanthocyanidins (425.24 and 243.29 mg/g, respectively). It was further found that blueberry leaves from different seasons have similar bioactive constituents, but their contents are obviously different by HPLC. The rabbiteye blueberry leaves from November had the highest antioxidant capacity, which was well correlated with their highest proanthocyanidin content. The results clarify that the blueberry leaves from different seasons have different contents of bioactive secondary metabolites and different antioxidant activities, which implied that leaves from November should be selected first for utilization in functional foods. PMID:24175648

  2. Quantitative analysis of major constituents in green tea with different plucking periods and their antioxidant activity.

    PubMed

    Lee, Lan-Sook; Kim, Sang-Hee; Kim, Young-Boong; Kim, Young-Chan

    2014-01-01

    The objective of this study was to determine the relationship between the plucking periods and the major constituents and the antioxidant activity in green tea. Green tea was prepared from leaves plucked from the end of April 2013 to the end of May 2013 at intervals of one week or longer. The contents of theanine, theobromine, caffeine, catechin (C), and gallocatechin gallate (GCg) were significantly decreased, whereas those of epicatechin (EC), epigallocatechin gallate (EGCg) and epigallocatechin (EGC) were significantly increased along with the period of tea leaf plucking. In addition, antioxidant activity of green tea and standard catechins was investigated using ABTS, FRAP and DPPH assays. The highest antioxidant activity was observed in relatively the oldest leaf, regardless of the assay methods used. Additionally, the order of antioxidant activity of standard catechins was as follows: EGCg≥GCg≥ECg>EGC≥GC≥EC≥C. Moreover, the cis-catechins contents were the key factor affecting the antioxidant activity of green tea in all assays employed (ABTS, r=0.731, p<0.01; FRAP, r=0.886, p<0.01; DPPH, r=0.778, p<0.01). PMID:24988187

  3. Antiplasmodial and cytotoxic activities of the constituents of Turraea robusta and Turraea nilotica

    PubMed Central

    Irungu, Beatrice N.; Adipo, Nicholas; Orwa, Jennifer A.; Kimani, Francis; Heydenreich, Matthias; Midiwo, Jacob O.; Martin Björemark, Per; Håkansson, Mikael; Yenesew, Abiy; Erdélyi, Máté

    2015-01-01

    Ethnopharmacological relevance Turraea robusta and Turraea nilotica are African medicinal plants used for the treatment of a wide variety of diseases, including malaria. The genus Turraea is rich in limonoids and other triterpenoids known to possess various biological activities. Materials and methods From the stem bark of T. robusta six compounds, and from various parts of T. nilotica eleven compounds were isolated by the use of a combination of chromatographic techniques. The structures of the isolated compounds were elucidated using NMR and MS, whilst the relative configuration of one of the isolated compounds, toonapubesin F, was established by X-ray crystallography. The antiplasmodial activities of the crude extracts and the isolated constituents against the D6 and W2 strains of Plasmodium falciparum were determined using the semiautomated micro dilution technique that measures the ability of the extracts to inhibit the incorporation of (G-3H, where G is guanine) hypoxanthine into the malaria parasite. The cytotoxicity of the crude extracts and their isolated constituents was evaluated against the mammalian cell lines African monkey kidney (vero), mouse breast cancer (4T1) and human larynx carcinoma (HEp2). Results The extracts showed good to moderate antiplasmodial activities, where the extract of the stem bark of T. robusta was also cytotoxic against the 4T1 and the HEp2 cells (IC50<10 μg/ml). The compounds isolated from these extracts were characterized as limonoids, protolimonoids and phytosterol glucosides. These compounds showed good to moderate activities with the most active one being azadironolide, IC50 2.4±0.03 μM and 1.1±0.01 μM against the D6 and W2 strains of Plasmodium falciparum, respectively; all other compounds possessed IC50 14.4–40.5 μM. None of the compounds showed significant cytotoxicity against vero cells, yet four of them were toxic against the 4T1 and HEp2 cancer cell lines with piscidinol A having IC50 8.0±0.03 and 8.4

  4. Pregnane X receptor-mediated transcriptional activation of UDP-glucuronosyltransferase 1A1 by natural constituents from foods and herbs.

    PubMed

    Wang, Junyan; Huang, Minmin; Hu, Haihong; Yu, Lushan; Zeng, Su

    2014-12-01

    The induction of drug-metabolising enzymes is being increasingly recognised for its clinical importance in drug research and development. In the present study, we used a pregnane X receptor (PXR)-mediated reporter gene assay to evaluate the activating effects of various food, herb, and horticultural plant constituents on the PXR and a UGT1A1 reporter gene DNA construct. The results showed that of 102 naturally occurring constituents tested, 50 activated the PXR signaling pathway and induced expression of the UGT1A1-reporter gene DNA construct. Eleven constituents strongly induced gene expression (a response of >70% compared to that associated with rifampicin), and were further evaluated in in vitro experiments to confirm the induction of UGT1A1 mRNA and protein expression. The results suggest that foods and herbs containing these constituents should be consumed with caution to avoid undesirable drug-drug interactions with co-administered drugs that are substrates for UGT1A1. PMID:24996308

  5. Isolation and identification of chemical constituents from the bacterium Bacillus sp. and their nematicidal activities.

    PubMed

    Zeng, Liming; Jin, Hui; Lu, Dengxue; Yang, Xiaoyan; Pan, Le; Cui, Haiyan; He, Xiaofeng; Qiu, Hongdeng; Qin, Bo

    2015-10-01

    A strain SMrs28 was isolated from the rhizosphere soil of a toxic plant Stellera chamaejasme and identified as Bacillus sp. on the basis of morphological and partial 16S rRNA gene sequence analysis. The crude extract of SMrs28 fermentation broth showed strong nematocidal activities in preliminary test. To define the active nematocidal metabolites of SMrs28, a novel compound (1), 4-oxabicyclo[3.2.2]nona-1(7), 5,8-triene, along with five known compounds (2-6), were isolated from the strain by various column chromatographic techniques and characterized on the basis of spectroscopic analysis. Results of the in vitro nematicidal tests showed that the metabolites presented different levels of activity at certain exposure conditions. Compounds (1-3) displayed LC50 values of 904.12, 451.26, 232.98 µg/ml and 1594.0, 366.62, 206.38 µg/ml against Bursaphelenchus xylophilus and Ditylenchus destructor at 72 h, respectively. This is the first report of the nematicidal activity of the compounds as constituents of Bacillus sp.. Our findings help to find potential chemical structures to develop nematicides from microbial source for the management of nematode-infected plant diseases. PMID:26058971

  6. Antidiabetic activity and chemical constituents of the aerial parts of Heracleum dissectum Ledeb.

    PubMed

    Zhang, Hailong; Su, Yaping; Wang, Xinrui; Mi, Jie; Huo, Yayu; Wang, Zhigang; Liu, Ying; Gao, Yang

    2017-01-01

    Heracleum dissectum Ledeb. has long been used as a wild edible vegetable by local people in China. The purpose of this study is to investigate the antidiabetic potential of aerial part of H. dissectum methanol extract (HdME) and the chemical constituents. Ten compounds including eight coumarins were isolated and four of them were found from H. dissectum for the first time. HdME potently inhibited the elevation of plasma glucose after its oral administration to glucose-loaded mice, and its petroleum ether (PE) fraction exerted the greatest inhibitory activities. Meanwhile, HdME (125 and 250mg/kg) also significantly decreased the blood glucose level in STZ-induced diabetic mice, but had no effect in normoglycemic mice. Additionally, HdME showed weak inhibitory effects on α-glucosidase activity and DPPH free radicals scavenging. In conclusion, HdME has antidiabetic action and PE fraction is the active part where coumarins possibly play an important role in antidiabetic activity. PMID:27507512

  7. [Chemical constituents of Rabdosia japonica var. glaucocalyx and their anti-complementary activity].

    PubMed

    Yao, Shi; Xu, Nai-Yu; Chu, Chun-Jun; Zhang, Jian; Chen, Dao-Feng

    2013-01-01

    To study the chemical constituents of Rabdosia japonica var. glaucocalyx and their anti-complementary activity on the basis of preliminary studies. Target isolation guided by anti-complementary activity test, compounds in the chloroform and n-butanol fractions were isolated and purified by silica gel and Sephadex LH-20 column chromatographies, and preparative HPLC. The structures were identified by various spectroscopic data including ESI-MS, 1H-NMR and 13C-NMR data. The compounds were evaluated for anti-complementary activity in vitro. Eleven compounds were isolated from the chloroform and n-butanol soluble fractions and identified as stigmasterol (1), stigmas-9 (11) -en-3-ol (2), glaucocalyxin D (3), kamebakaurin (4), maslinic acid (5), corosolic acid (6), minheryins I (7), diosmetin (8), caffeic acid ethylene ester (9), caffeic acid (10) and vitexin (11). Isoquercetrin, rutin, quercetin, 3-methylquercetin, luteolin, 7-methylluteolin, and apigenin which were isolated from the preliminary studies together with compounds 9 and 10 showed inhibition of the complement system by the classical pathway. Compounds 2, 4, 6-9 and 11 were obtained from this plant for the first time. Caffeic acid (10) showed the strongest activity in vitro with a CH50 value of 0.041 g x L(-1). PMID:23672041

  8. [Chemical constituents from stems of Hedyotis hedyotidea and their immunosuppressive activity].

    PubMed

    Zhang, Tian-tian; Gao, Sha-sha; Hou, Jun-jie; Zhou, Yong-qin; Zhou, Jie-wen; Wang, Xiao-gang; Qin, Nan; Chen, Jia-chun; Duan, Hong-quan; Fang, Jin-bo

    2015-06-01

    Hedyotis hedyotidea has been traditionally used for the treatment of arthritis, cold, cough, gastro-enteritis, headstroke, etc. But few studies have screened the active compounds from extracts of H. hedyotidea. In this study, the structure of the chemical constituents from stems of H. hedyotidea were determined and the immunosuppressive activity of the compounds was evaluated. The compounds were separated and purified with silica gel, gel column chromatographies and preparative HPLC, and their structures were identified by spectral methods such as MS and NMR. Eleven compounds were obtained and identified as(6S,9S) -vomifoliol (1), betulonic acid (2), betulinic acid (3), betulin(4), 3-epi-betulinic acid (5), ursolic acid (6), β-sitosterol (7), stigmast-4-en-3-one (8), 7β-hydroxysitosterol (9), (3β,7β) -7-methoxystigmast-5-en-3-ol (10) and morindacin (11). This is the first report of compounds 1, 2, 4, 8, 9, 10 and 11 from H. hedyotidea. Compounds 1, 2 and 8-11 were firstly isolated from the genus Hedyotis, and compounds 9 and 10 were isolated from the family Rubiaceae for the first time. The immunosuppressive activity of these compounds was tested using the lymphocyte transsormationtest. Compounds 4, 6 and 9 showed significant immunosuppressive activity. PMID:26591525

  9. Leishmanicidal active constituents from Nepalese medicinal plant Tulsi (Ocimum sanctum L.).

    PubMed

    Suzuki, Akiko; Shirota, Osamu; Mori, Kanami; Sekita, Setsuko; Fuchino, Hiroyuki; Takano, Akihito; Kuroyanagi, Masanori

    2009-03-01

    In the course of screening leishmanicidal active compounds from Asian and South American medicinal plants, a Nepalese medicinal plant, Tulsi (Ocimum sanctum L.), showed strong activity. We therefore studied the isolation and structural elucidation of the active constituents from O. sanctum L. From the ethyl acetate soluble fraction of the plant, seven new novel neolignan derivatives were isolated along with 16 known compounds. The structures of the new compounds (1-7) were elucidated as 6-allyl-3',8-dimethoxy-flavan-3,4'-diol (1), 6-allyl-3-(4-allyl-2-methoxyphenoxy)-3',8-dimethoxyflavan-4'-ol (2), 5-allyl-3-(4-allyl-2-methoxyphenoxymethyl)-2-(4-hydroxy-3-methoxyphenyl)-7-methoxy-2,3-dihydrobenzofuran (3), 1,2-bis(4-allyl-2-methoxyphenoxy)-3-(4-hydroxy-3-methoxyphenyl)-3-methoxypropane (4), 1-(4-hydroxy-3-methoxyphenyl)-1,2,3-tris(4-allyl-2-methoxyphenoxy)propane (5), 1-allyl-4-(5-allyl-2-hydroxy-3-methoxyphenoxy)-3-(4-allyl-2-methoxyphenoxy)-5-methoxybenzene (6), and 3-(5-allyl-2-hydroxy-3-methoxyphenyl)-1-(4-hydroxy-3-methoxyphenoxy)-prop-1-ene (7) by means of (1)H-NMR, (13)C-NMR, and 2D-NMR spectral data. Some of these compounds showed leishmanicidal activity. PMID:19252314

  10. Antiviral Activity and Possible Mechanism of Action of Constituents Identified in Paeonia lactiflora Root toward Human Rhinoviruses

    PubMed Central

    Ngan, Luong Thi My; Jang, Myeong Jin; Kwon, Min Jung; Ahn, Young Joon

    2015-01-01

    Human rhinoviruses (HRVs) are responsible for more than half of all cases of the common cold and cost billions of USD annually in medical visits and missed school and work. An assessment was made of the antiviral activities and mechanisms of action of paeonol (PA) and 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (PGG) from Paeonia lactiflora root toward HRV-2 and HRV-4 in MRC5 cells using a tetrazolium method and real-time quantitative reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay. Results were compared with those of a reference control ribavirin. Based on 50% inhibitory concentration values, PGG was 13.4 and 18.0 times more active toward HRV-2 (17.89 μM) and HRV-4 (17.33 μM) in MRC5 cells, respectively, than ribavirin. The constituents had relatively high selective index values (3.3–>8.5). The 100 μg/mL PA and 20 μg/mL PGG did not interact with the HRV-4 particles. These constituents inhibited HRV-4 infection only when they were added during the virus inoculation (0 h), the adsorption period of HRVs, but not after 1 h or later. Moreover, the RNA replication levels of HRVs were remarkably reduced in the MRC5 cultures treated with these constituents. These findings suggest that PGG and PA may block or reduce the entry of the viruses into the cells to protect the cells from the virus destruction and abate virus replication, which may play an important role in interfering with expressions of rhinovirus receptors (intercellular adhesion molecule-1 and low-density lipoprotein receptor), inflammatory cytokines (interleukin (IL)-6, IL-8, tumor necrosis factor, interferon beta, and IL-1β), and Toll-like receptor, which resulted in diminishing symptoms induced by HRV. Global efforts to reduce the level of synthetic drugs justify further studies on P. lactiflora root-derived materials as potential anti-HRV products or lead molecules for the prevention or treatment of HRV. PMID:25860871

  11. Comparative Studies of Antioxidant Activities and Nutritional Constituents of Persimmon Juice (Diospyros kaki L. cv. Gapjubaekmok)

    PubMed Central

    Lee, Jin Hwan; Lee, Yong Bok; Seo, Woo Duck; Kang, Su Tae; Lim, Jong Woo; Cho, Kye Man

    2012-01-01

    The objectives of this research were to evaluate antioxidant activities and nutritional components, including phenolic acid, catechin, organic acid, sugar, and amino acid, of persimmon juice from persimmons grown in different regions around Korea. Persimmon (Diospyros kaki) exhibits potent antioxidant effects in DPPH, ABTS, reducing power, and FRAP methods of analysis. The levels of nutritional constituents showed significant differences among all the samples. In particular, tartaric acid, glucose, gallic acid, epicatechin gallate and aspartic acid were observed to be the predominant component for each of their general chemical groups, with total average contents of 1876.51 mg/kg, 62.69 g/kg, 12.73 mg/kg, 208.99 mg/kg, and 31.84 mg/100 g, respectively. Interestingly, persimmons from the Hadong region presented the highest sugar (130.60 g/kg), phenolic acid (42.27 mg/kg), and catechin (527.97 mg/kg) contents in comparison with other regional samples. Moreover, this location exhibited the greatest antioxidant activity with highest total phenolic (298.01 mg GAE/kg) and flavonoid (32.11 mg/kg RE) contents. Our results suggest that strong antioxidant activities of persimmons correlate with high phenolic acid and catechin contents, particularly gallic acid and epicatechin gallate. Additionally, these two compounds may be key factors when considering the useful ingredients of persimmon. PMID:24471076

  12. Anti-Inflammatory Activities of Cinnamomum cassia Constituents In Vitro and In Vivo

    PubMed Central

    Liao, Jung-Chun; Deng, Jeng-Shyan; Chiu, Chuan-Sung; Hou, Wen-Chi; Huang, Shyh-Shyun; Shie, Pei-Hsin; Huang, Guang-Jhong

    2012-01-01

    We have investigated the anti-inflammatory effects of Cinnamomum cassia constituents (cinnamic aldehyde, cinnamic alcohol, cinnamic acid, and coumarin) using lipopolysaccharide (LPS)-stimulated mouse macrophage (RAW264.7) and carrageenan (Carr)-induced mouse paw edema model. When RAW264.7 macrophages were treated with cinnamic aldehyde together with LPS, a significant concentration-dependent inhibition of nitric oxide (NO), tumor necrosis factor (TNF-α), and prostaglandin E2 (PGE2) levels productions were detected. Western blotting revealed that cinnamic aldehyde blocked protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), nuclear transcription factor kappa B (NF-κB), and IκBα, significantly. In the anti-inflammatory test, cinnamic aldehyde decreased the paw edema after Carr administration, and increased the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) in the paw tissue. We also demonstrated cinnamic aldehyde attenuated the malondialdehyde (MDA) level and myeloperoxidase (MPO) activity in the edema paw after Carr injection. Cinnamic aldehyde decreased the NO, TNF-α, and PGE2 levels on the serum level after Carr injection. Western blotting revealed that cinnamic aldehyde decreased Carr-induced iNOS, COX-2, and NF-κB expressions in the edema paw. These findings demonstrated that cinnamic aldehyde has excellent anti-inflammatory activities and thus has great potential to be used as a source for natural health products. PMID:22536283

  13. Chemical constituents from Tribulus terrestris and screening of their antioxidant activity.

    PubMed

    Hammoda, Hala M; Ghazy, Nabila M; Harraz, Fathalla M; Radwan, Mohamed M; ElSohly, Mahmoud A; Abdallah, Ingy I

    2013-08-01

    Two oligosaccharides (1,2) and a stereoisomer of di-p-coumaroylquinic acid (3) were isolated from the aerial parts of Tribulus terrestris along with five known compounds (4-8). The structures of the compounds were established as O-β-D-fructofuranosyl-(2→6)-α-D-glucopyranosyl-(1→6)-β-D-fructofuranosyl-(2→6)-β-D-fructofuranosyl-(2→1)-α-D-glucopyranosyl-(6→2)-β-D-fructofuranoside (1), O-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→2)-β-D-fructofuranoside (2), 4,5-di-p-cis-coumaroylquinic acid (3) by different spectroscopic methods including 1D NMR ((1)H, (13)C and DEPT) and 2D NMR (COSY, TOCSY, HMQC and HMBC) experiments as well as ESI-MS analysis. This is the first report for the complete NMR spectral data of the known 4,5-di-p-trans-coumaroylquinic acid (4). The antioxidant activity represented as DPPH free radical scavenging activity was investigated revealing that the di-p-coumaroylquinic acid derivatives possess potent antioxidant activity so considered the major constituents contributing to the antioxidant effect of the plant. PMID:23642392

  14. Chemical constituents and antioxidant and biological activities of the essential oil from leaves of Solanum spirale.

    PubMed

    Keawsa-ard, Sukanya; Liawruangrath, Boonsom; Liawruangrath, Saisunee; Teerawutgulrag, Aphiwat; Pyne, Stephen G

    2012-07-01

    The essential oil of the leaves Solanium spirale Roxb. was isolated by hydrodistillation and analyzed for the first time using GC and GC-MS. Thirty-nine constituents were identified, constituting 73.36% of the total chromatographical oil components. (E)-Phytol (48.10%), n-hexadecanoic acid (7.34%), beta-selinene (3.67%), alpha-selinene (2.74%), octadecanoic acid (2.12%) and hexahydrofarnesyl acetone (2.00%) were the major components of this oil. The antioxidant activity of the essential oil was evaluated by using the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assay. The oil exhibited week antioxidant activity with an IC50 of 41.89 mg/mL. The essential oil showed significant antibacterial activity against both Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus with MIC values of 43.0 microg/mL and 21.5 microg/mL, respectively. It also showed significant cytotoxicity against KB (oral cancer), MCF-7 (breast cancer) and NCI-H187 (small cell lung cancer) with the IC50 values of 26.42, 19.69, and 24.02 microg/mL, respectively. PMID:22908592

  15. Comparative analysis of the constituents in Saposhnikoviae Radix and Glehniae Radix cum Rhizoma by monitoring inhibitory activity of nitric oxide production.

    PubMed

    Kamino, Takuya; Shimokura, Toshihiro; Morita, Yusuke; Tezuka, Yasuhiro; Nishizawa, Mikio; Tanaka, Ken

    2016-04-01

    During the development of natural herbal medicines in Japan, Glehniae Radix cum Rhizoma (Hamabofu in Japanese) has been used as a substitute for Saposhnikoviae Radix (Bofu). Bofu and Hamabofu are blended differently in several Kampo formulae. For example, Bofu is included in Jumihaidokuto by a manufacturer, whereas Hamabofu is included instead of Bofu in the same formula by other manufacturers. Although both Bofu and Hamabofu are used for their expected anti-inflammatory effects, differences in their medicinal properties are not well characterized. In addition, there have been very few reports comparing the pharmacological activities of the constituents in Bofu and Hamabofu. In the present study, we investigated the anti-inflammatory effects of the extracts of Bofu and Hamabofu by monitoring levels of the inflammatory mediator nitric oxide (NO) produced in rat hepatocytes. Moreover, the chemical constituents responsible for the activity were investigated. Our results showed that ethyl acetate fractions of Bofu and Hamabofu extracts contain different compounds, although both fractions suppressed NO production in rat hepatocytes. The linear dihydropyranochromones from the Bofu extract (i.e., 3'-O-angeloylhamaudol, ledebouriellol and hamaudol) suppressed NO production, whereas the coumarins from the Hamabofu extract (i.e., umbelliferone and scopoletin) also suppressed NO production. These results suggest that linear dihydropyranochromones and coumarins are responsible for the anti-inflammatory effects of Bofu and Hamabofu. It is plausible that Bofu and Hamabofu are blended differently in several Kampo formulae due to many constituents with as yet unidentified pharmacological activity. PMID:26833192

  16. Evaluation of Antibacterial Activity, Phytochemical Constituents, and Cytotoxicity Effects of Thai Household Ancient Remedies

    PubMed Central

    Sinvaraphan, Naruephan; Chaipak, Ploypailin; Luxsananuwong, Atita; Voravuthikunchai, Supayang Piyawan

    2014-01-01

    Abstract Aim: Household ancient remedies reported here are described in the National List of Essential Medicines and have traditionally been used in Thailand to treat infection-related ailments. However, the safety and effectiveness of these remedies have been poorly evaluated. The aim of this study was to evaluate the antibacterial properties of these remedies against seven gram-positive and gram-negative multidrug-resistant bacteria species. Phytochemical constituents and cytotoxicity of these remedies were also determined. Methods: Seven remedies, consisting of Um-Ma-Luk-Ka-Wa-Tee, Chan-Ta-Lee-La, Kheaw-Hom, Learng-Pid-Sa-Mud, Pra-Sa-Chan-Dang, Dhart-Ban-Chob, and Tree-Hom, were prepared by a licensed traditional medical doctor using a mixture of medicinal plants. Antibacterial activity of ethanol extracts of the remedies was determined by using a broth microdilution method. Qualitative phytochemical screening analysis was carried out to identify the presence of major components. Cytotoxicity activities of the extracts against Vero cells were assessed by green fluorescent protein–based assay. Results: With the exception of Dhart-Ban-Chob extract, significant minimum inhibitory concentrations (MICs) of <16 to 32 μg/mL were observed for the remedy extracts depending on the bacterial strains. The Um-Ma-Luk-Ka-Wa-Tee extract was noncytotoxic against Vero cells and possessed the highest activity, with MICs of <16 to 31 μg/mL against all methicillin-resistant Staphylococcus aureus isolates. Conclusions: Remarkable antibacterial activities against multidrug-resistant pathogens, as well as low toxicity on Vero cells, of Um-Ma-Luk-Ka-Wa-Tee support the use of this remedy in traditional medicine. Further investigation on other biological activities related to traditional applications, appropriate biomarkers, and treatment mechanisms of the household remedy are required. PMID:25415453

  17. Chemical constituents and biological activities of Galinsoga parviflora cav. (Asteraceae) from Egypt.

    PubMed

    Mostafa, Islam; Abd El-Aziz, Ehsan; Hafez, Samia; El-Shazly, Assem

    2013-01-01

    The phytochemical investigation of an aqueous ethanolic extract of Galinsoga parviflora Cav. (Asteraceae) resulted in the isolation and identification of eleven compounds namely: triacontanol, phytol, beta-sitosterol, stigmasterol, 7-hydroxy-beta-sitosterol, 7-hydroxystigmasterol, beta-sitosterol-3-O-beta-D-glucoside, 3,4-dimethoxycinnamic acid, protocatechuic acid, fumaric acid, and uracil. Furthermore, 48 volatile constituents were identified in the hydrodistilled oil of the aerial parts. The ethanolic extract at a content of 400 mg/kg body weight (BW) exerted 87% reduction in the alanine aminotransferase enzyme level in cirrhotic rats compared with the standard silymarin (150 mg/kg BW) and also exerted a reduction in the blood glucose level equivalent to that of glibenclamide (5 mg/kg BW) in diabetic rats. The ethanolic extract, light petroleum and ethyl acetate fractions exhibited substantial antimicrobial activity against Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Aspergillus niger, and Candida albicans. The ethyl acetate fraction showed strong antioxidant activity at a concentration of 150 mg/mL as compared with 0.1 M ascorbic acid. The cytotoxic effect against the MCF-7 cell line was found to be weak. PMID:24066513

  18. Replacement of inorganic zinc with lower levels of organic zinc (zinc nicotinate) on performance, hematological and serum biochemical constituents, antioxidants status, and immune responses in rats

    PubMed Central

    Nagalakshmi, D.; Sridhar, K.; Parashuramulu, S.

    2015-01-01

    Aim: A study was undertaken to investigate the effect of organic zinc (zinc nicotinate, Zn-nic) supplementation (6, 9, and 12 ppm) compared to inorganic zinc (12 ppm) on growth performance, hematology, serum biochemical constituents oxidative stress, and immunity in weaned female Sprague–Dawley rats. Material and Methods: A 48 weaned rats (285.20±1.95 g) were randomly distributed to 4 dietary treatments with 6 replicates in each and reared in polypropylene cages for 10 weeks. Basal diet (BD) was formulated with purified ingredients without zinc (Zn). Four dietary treatments were prepared by adding 12 ppm Zn from ZnCO3 (control) and 6, 9, and 12 ppm Zn from Zn-nic to the BD. On 42nd day, blood was collected by retro-orbital puncture for analyzing hematological constituents, glucose, cholesterol, alkaline phosphatase, total protein, albumin, and globulin and antioxidant enzyme activities. At 43rd day, rats were antigenically challenged with sheep red blood cell (RBC) to assess humoral immune response and on 70th day cell-mediated immune response. Results: Weekly body weight gains, daily feed intake, blood hematological constituents (white blood cell, RBC, hemoglobin concentration, packed cell volume, mean corpuscular volume, lymphocyte, monocyte, and granulocyte concentration) and serum glucose, total protein levels were comparable among the rats feed Zn from ZnCO3 and Zn-nic (6, 9, and 12 ppm). Serum cholesterol reduced with organic Zn supplementation at either concentration (6-12 ppm). Serum globulin concentration reduced (p<0.05) with 6 ppm Zn-nic supplementation compared to other dietary treatments. Lipid peroxidation lowered (p<0.05) reduced with 12 ppm organic Zn; thiobarbituric acid reacting substances and protein carbonyls concentrations in liver reduced (p<0.05) with 9 and 12 ppm levels of organic Zn supplementation compared to 12 ppm Zn supplementation from inorganic source. RBC catalase and glutathione peroxidase enzymes activities were highest (p<0

  19. Chemical Constituents and Activity of Murraya microphylla Essential Oil against Lasioderma serricorne.

    PubMed

    You, Chun-Xue; Guo, Shan-Shan; Zhang, Wen-Juan; Yang, Kai; Wang, Cheng-Fang; Geng, Zhu-Feng; Du, Shu-Shan; Deng, Zhi-Wei; Wang, Yong-Yan

    2015-09-01

    The chemical composition, contact and repellent activities of the essential oil from Murraya microphylla branches and leaves against Lasioderma serricorne adults were determined and six compounds from the essential oil were isolated as well. The essential oil of M microphylla obtained by hydrodistillation was analyzed by gas chromatography-mass spectrometric (GC-MS) analysis; 22 compounds were identified. The main constituents of the essential oil included β-caryophyllene (18.0%), α-pinene (13.8%), spathulenol (9.5%), α-humulene (6.0%), γ-elemene (5.1%) and zingiberene (4.6%), followed by α-cadinol (3.9%) and caryophyllene oxide (3.8%). Six of these compounds were isolated and fully identified as α-pinene, β-caryophyllene, α-humulene, caryophyllene oxide, spathulenol and α-cadinol. L. serricorne adults had different sensitivities to the crude essential oil and isolated compounds. α-Humulene exhibited the strongest contact activity against L. serricorne, showing an LD50 value of 13.1 µg adult(-1). However, spathulenol, the crude essential oil and α-cadinol showed stronger contact activity against L. serricorne than caryophyllene oxide and β-caryophyllene. The essential oil, α-humulene and spathulenol showed comparable repellency against L. serricorne adults at 2 h after exposure, relative to the positive control, DEET. The results demonstrate that the essential oil and isolated compounds exhibited important contact and repellent activities against L. serricorne. Thus, they could become potential natural insecticides or repellents for control of insects in stored products. PMID:26594776

  20. Evaluation of medicinal value of Epimedium elatum on the basis of pharmacologically active constituents, Icariin and Icariside-II.

    PubMed

    Arief, Zargar Mohmad; Munshi, Abid Hussain; Shawl, Abdul Sami

    2015-09-01

    Epimedium L. is well known medicinal genus of Chinese pharmacopoeia. Various species are ethno-botanically used against diseases of eye and kidney, impotence, asthma, arthritis and hypertension; besides being used as analeptic, expectorant, antibacterial, hypoglycemic, vasodilator and refrigerant. Recent studies have attributed most of these medicinal properties to its flavonoid glycosides, especially Icariin which is the major pharmacologically active constituent. Icariin has been found to possess effective aphrodisiac, antioxidant, immunomodulatory, hepatoprotective, cardioprotective, vasodilatory, antidepressant and anti-osteoporosis activities. Icariside-II, another active constituent, has cytotoxic and cytostatic effects on 6 cancer cell-lines, and immunosuppressive effects on allograft rejection. In this present study, Epimedium elatum Morr. and Decne., the only species of this genus growing in Indian subcontinent, has been investigated for its medicinal value by determining the content of pharmacologically active constituents, Icariin and Icariside-II, by HPLC method. HPLC analysis of alcohol extract of its shade dried parts was performed with reverse phase C-18 column. The mobile phase for Icariin was acetonitrile-water in gradient mode; while for Icariside-II, it was methanol-water. The effluent was monitored at 270 nm. The results have revealed an appreciable content of Icariin and Icariside-II in its aerial and underground parts; the content being higher in populations growing at higher altitudes. The substantial presence of pharmacologically active constituents, Icariin and Icariside-II, in this species of Epimedium, signifies its value as a medicinal plant. PMID:26408886

  1. Synergy and Antagonism of Active Constituents of ADAPT-232 on Transcriptional Level of Metabolic Regulation of Isolated Neuroglial Cells

    PubMed Central

    Panossian, Alexander; Hamm, Rebecca; Kadioglu, Onat; Wikman, Georg; Efferth, Thomas

    2013-01-01

    Gene expression profiling was performed on the human neuroglial cell line T98G after treatment with adaptogen ADAPT-232 and its constituents – extracts of Eleutherococcus senticosus root, Schisandra chinensis berry, and Rhodiola rosea root as well as several constituents individually, namely, eleutheroside E, schizandrin B, salidroside, triandrin, and tyrosol. A common feature for all tested adaptogens was their effect on G-protein-coupled receptor signaling pathways, i.e., cAMP, phospholipase C (PLC), and phosphatidylinositol signal transduction pathways. Adaptogens may reduce the cAMP level in brain cells by down-regulation of adenylate cyclase gene ADC2Y and up-regulation of phosphodiesterase gene PDE4D that is essential for energy homeostasis as well as for switching from catabolic to anabolic states and vice versa. Down-regulation of cAMP by adaptogens may decrease cAMP-dependent protein kinase A activity in various cells resulting in inhibition stress-induced catabolic transformations and saving of ATP for many ATP-dependant metabolic transformations. All tested adaptogens up-regulated the PLCB1 gene, which encodes phosphoinositide-specific PLC and phosphatidylinositol 3-kinases (PI3Ks), key players for the regulation of NF-κB-mediated defense responses. Other common targets of adaptogens included genes encoding ERα estrogen receptor (2.9–22.6 fold down-regulation), cholesterol ester transfer protein (5.1–10.6 fold down-regulation), heat shock protein Hsp70 (3.0–45.0 fold up-regulation), serpin peptidase inhibitor (neuroserpin), and 5-HT3 receptor of serotonin (2.2–6.6 fold down-regulation). These findings can be reconciled with the observed beneficial effects of adaptogens in behavioral, mental, and aging-associated disorders. Combining two or more active substances in one mixture significantly changes deregulated genes profiles: synergetic interactions result in activation of genes that none of the individual substances affected, while

  2. Bryophyllum pinnatum and Related Species Used in Anthroposophic Medicine: Constituents, Pharmacological Activities, and Clinical Efficacy.

    PubMed

    Fürer, Karin; Simões-Wüst, Ana Paula; von Mandach, Ursula; Hamburger, Matthias; Potterat, Olivier

    2016-07-01

    Bryophyllum pinnatum (syn. Kalanchoe pinnata) is a succulent perennial plant native to Madagascar that was introduced in anthroposophic medicine in the early 20th century. In recent years, we conducted a large collaborative project to provide reliable data on the chemical composition, pharmacological properties, and clinical efficacy of Bryophyllum. Here, we comprehensively review the phytochemistry, as well as the pharmacological and clinical data. As to the pharmacology, special emphasis is given to properties related to the use in anthroposophic medicine as a treatment for "hyperactivity diseases", such as preterm labor, restlessness, and sleep disorders. Studies suggesting that B. pinnatum may become a new treatment option for overactive bladder syndrome are also reviewed. Tolerability is addressed, and toxicological data are discussed in conjunction with the presence of potentially toxic bufadienolides in Bryophyllum species. The few data available on two related species with medicinal uses, Bryophyllum daigremontianum and Bryophyllum delagoense, have also been included. Taken together, current data support the use of B. pinnatum for the mentioned indications, but further studies are needed to fully understand the modes of action, and to identify the pharmacologically active constituents. PMID:27220081

  3. Alkenylresorcinols and cytotoxic activity of the constituents isolated from Labisia pumila.

    PubMed

    Al-Mekhlafi, Nabil Ali; Shaari, Khozirah; Abas, Faridah; Kneer, Ralf; Jeyaraj, Ethel Jeyaseela; Stanslas, Johnson; Yamamoto, Naoshi; Honda, Toshio; Lajis, Nordin H

    2012-08-01

    Phytochemical investigation on the leaves of Labisia pumila (Myrsinaceae), an important medicinal herb in Malaysia, has led to the isolation of 1-O-methyl-6-acetoxy-5-(pentadec-10Z-enyl)resorcinol (1), labisiaquinone A (2) and labisiaquinone B (3). Along with these, 16 known compounds including 1-O-methyl-6-acetoxy-5-pentadecylresorcinol (4), 5-(pentadec-10Z-enyl)resorcinol (5), 5-(pentadecyl)resorcinol (6), (-)-loliolide (7), stigmasterol (8), 4-hydroxyphenylethylamine (9), 3,4,5-trihydroxybenzoic acid (10), 3,4-dihydroxybenzoic acid (11), (+)-catechin (12), (-)-epicatechin (13), kaempferol-3-O-α-rhamnopyranosyl-7-O-β-glycopyranoside (14), kaempferol-4'-O-β-glycopyranoside (15), quercetin-3-O-α-rhamnopyranoside (16), kaempferol-3-O-α-rhamnopyranoside (17), (9Z,12Z)-octadeca-9,12-dienoic acid (18) and stigmasterol-3-O-β-glycopyranoside (19) were also isolated. The structures of these compounds were established on the basis of 1D and 2D NMR spectroscopy techniques (¹H, ¹³C, COSY, HSQC, NOESY and HMBC experiments), mass spectrometry and chemical derivatization. Among the constituents tested 1 and 4 exhibited strongest cytotoxic activity against the PC3, HCT116 and MCF-7 cell lines (IC₅₀ values ≤ 10 μM), and they showed selectivity towards the first two-cell lines relative to the last one. PMID:22633846

  4. Polar Constituents and Biological Activity of the Berry-Like Fruits from Hypericum androsaemum L.

    PubMed Central

    Caprioli, Giovanni; Alunno, Alessia; Beghelli, Daniela; Bianco, Armandodoriano; Bramucci, Massimo; Frezza, Claudio; Iannarelli, Romilde; Papa, Fabrizio; Quassinti, Luana; Sagratini, Gianni; Tirillini, Bruno; Venditti, Alessandro; Vittori, Sauro; Maggi, Filippo

    2016-01-01

    Hypericum androsaemum, also known as Tutsan, is a small evergreen shrub common in the Mediterranean basin where it is traditionally used as diuretic and hepatoprotective herbal drug. This plant possesses the peculiarity to produce fleshy and berry-like fruits that ripen from red to shiny black. In the present work, the chemical constituents of methanolic extracts and infusions of red and black fruits were analyzed by HPLC, and correlated with their antioxidant properties which were evaluated by the DPPH, β-Carotene/linoleic acid, and hypochlorous acid tests. In addition, the red pigment of the fruit was isolated by column chromatography and structurally elucidated by NMR. Results showed that H. androsaemum fruits contain high amounts of shikimic and chlorogenic acids, while their color was given by a tetraoxygenated-type xanthone, reported for the first time in Hypericum species. The red berries infusion gave the highest content of total phenolic compounds, DPPH, and hypochlorous acid scavenging activity, and β-carotene bleaching. Cytotoxicity of the berries extracts on three human tumor cell lines (malignant melanoma, breast adenocarcinoma, and colon carcinoma) was evaluated by MTT assay, and relevant inhibition on colon carcinoma cells (IC50 value of 8.4 μg/mL) was found. Finally, the effects of red berries extract on the immune system were evaluated by peripheral blood mononuclear cell (PBMC) proliferation assay that revealed a strong stimulation on lymphocytes at low doses (0.4–6 μg/mL). PMID:26973675

  5. Mentha suaveolens Ehrh. (Lamiaceae) Essential Oil and Its Main Constituent Piperitenone Oxide: Biological Activities and Chemistry.

    PubMed

    Božović, Mijat; Pirolli, Adele; Ragno, Rino

    2015-01-01

    Since herbal medicines play an important role in the treatment of a wide range of diseases, there is a growing need for their quality control and standardization. Mentha suaveolens Ehrh. (MS) is an aromatic herb with fruit and a spearmint flavor, used in the Mediterranean areas as a traditional medicine. It has an extensive range of biological activities, including cytotoxic, antimicrobial, antioxidant, anti-inflammatory, hypotensive and insecticidal properties, among others. This study aims to review the scientific findings and research reported to date on MS that prove many of the remarkable various biological actions, effects and some uses of this species as a source of bioactive natural compounds. On the other hand, piperitenone oxide (PO), the major chemical constituent of the carvone pathway MS essential oil, has been reported to exhibit numerous bioactivities in cells and animals. Thus, this integrated overview also surveys and interprets the present knowledge of chemistry and analysis of this oxygenated monoterpene, as well as its beneficial bioactivities. Areas for future research are suggested. PMID:25985361

  6. Polar Constituents and Biological Activity of the Berry-Like Fruits from Hypericum androsaemum L.

    PubMed

    Caprioli, Giovanni; Alunno, Alessia; Beghelli, Daniela; Bianco, Armandodoriano; Bramucci, Massimo; Frezza, Claudio; Iannarelli, Romilde; Papa, Fabrizio; Quassinti, Luana; Sagratini, Gianni; Tirillini, Bruno; Venditti, Alessandro; Vittori, Sauro; Maggi, Filippo

    2016-01-01

    Hypericum androsaemum, also known as Tutsan, is a small evergreen shrub common in the Mediterranean basin where it is traditionally used as diuretic and hepatoprotective herbal drug. This plant possesses the peculiarity to produce fleshy and berry-like fruits that ripen from red to shiny black. In the present work, the chemical constituents of methanolic extracts and infusions of red and black fruits were analyzed by HPLC, and correlated with their antioxidant properties which were evaluated by the DPPH, β-Carotene/linoleic acid, and hypochlorous acid tests. In addition, the red pigment of the fruit was isolated by column chromatography and structurally elucidated by NMR. Results showed that H. androsaemum fruits contain high amounts of shikimic and chlorogenic acids, while their color was given by a tetraoxygenated-type xanthone, reported for the first time in Hypericum species. The red berries infusion gave the highest content of total phenolic compounds, DPPH, and hypochlorous acid scavenging activity, and β-carotene bleaching. Cytotoxicity of the berries extracts on three human tumor cell lines (malignant melanoma, breast adenocarcinoma, and colon carcinoma) was evaluated by MTT assay, and relevant inhibition on colon carcinoma cells (IC50 value of 8.4 μg/mL) was found. Finally, the effects of red berries extract on the immune system were evaluated by peripheral blood mononuclear cell (PBMC) proliferation assay that revealed a strong stimulation on lymphocytes at low doses (0.4-6 μg/mL). PMID:26973675

  7. 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

  8. Combined experimental and DFT-TDDFT study of photo-active constituents of Canarium odontophyllum for DSSC application

    NASA Astrophysics Data System (ADS)

    Ekanayake, Piyasiri; Kooh, Muhammad Raziq Rahimi; Kumara, N. T. R. N.; Lim, Andery; Petra, Mohammad Iskandar; Voo, Nyuk Yoong; Lim, Chee Ming

    2013-10-01

    The active constituents of Canarium odontophyllum (COP) were investigated experimentally and theoretically for dye sensitized solar cell (DSSC) application. Three main flavonoid pigments (cyanidin, pelargonidin and maritimein) were detected in COP showing photo-energy conversion efficiencies of 1.43%, 0.87% and 0.60%, respectively. The molecular geometries, electronic structures, optical absorption spectra and proton affinity of these molecules were investigated with DFT/TDDFT. All three molecules displayed π→π* transition dominant in HOMO→LUMO transition. The anchoring groups onto TiO2 surface were deduced from combined experimental and calculated data. All the constituents of COP are potential sensitizers for DSSC.

  9. Chemical constituents of Swertia longifolia Boiss. with α-amylase inhibitory activity

    PubMed Central

    Saeidnia, Soodabeh; Ara, Leila; Hajimehdipoor, Homa; Read, Roger W.; Arshadi, Sattar; Nikan, Marjan

    2016-01-01

    α-Amylase inhibitors play a critical role in the control of diabetes and many of medicinal plants have been found to act as α-amylase inhibitors. Swertia genus, belonging to the family Gentianaceae, comprises different species most of which have been used in traditional medicine of several cultures as antidiabetic, anti-pyretic, analgesic, liver and gastrointestinal tonic. Swertia longifolia Boiss. is the only species of Swertia growing in Iran. In the present investigation, phytochemical study of S. longifolia was performed and α-amylase inhibitory effects of the plant fractions and purified compounds were determined. Aerial parts of the plant were extracted with hexane, chloroform, methanol and water, respectively. The components of the hexane and chloroform fractions were isolated by different chromatographic methods and their structures were determined by 1H NMR and 13C NMR data. α-Amylase inhibitory activity was determined by a colorimetric assay using 3,5-dinitro salysilic acid. During phytochemical examination, α-amyrin, β-amyrin and β-sitosterol were purified from the hexane fraction, while ursolic acid, daucosterol and swertiamarin were isolated from chloroform fraction. The results of the biochemical assay revealed α-amylase inhibitory activity of hexane, chloroform, methanol and water fractions, of which the chloroform and methanol fractions were more potent (IC50 16.8 and 18.1 mg/ml, respectively). Among examined compounds, daucosterol was found to be the most potent α-amylase inhibitor (57.5% in concentration 10 mg/ml). With regard to α-amylase inhibitory effects of the plant extracts, purified constituents, and antidiabetic application of the species of Swertia genus in traditional medicine of different countries, S. longifolia seems more appropriate species for further mechanistic antidiabetic evaluations. PMID:27051429

  10. Chemical constituents of Swertia longifolia Boiss. with α-amylase inhibitory activity.

    PubMed

    Saeidnia, Soodabeh; Ara, Leila; Hajimehdipoor, Homa; Read, Roger W; Arshadi, Sattar; Nikan, Marjan

    2016-01-01

    α-Amylase inhibitors play a critical role in the control of diabetes and many of medicinal plants have been found to act as α-amylase inhibitors. Swertia genus, belonging to the family Gentianaceae, comprises different species most of which have been used in traditional medicine of several cultures as antidiabetic, anti-pyretic, analgesic, liver and gastrointestinal tonic. Swertia longifolia Boiss. is the only species of Swertia growing in Iran. In the present investigation, phytochemical study of S. longifolia was performed and α-amylase inhibitory effects of the plant fractions and purified compounds were determined. Aerial parts of the plant were extracted with hexane, chloroform, methanol and water, respectively. The components of the hexane and chloroform fractions were isolated by different chromatographic methods and their structures were determined by (1)H NMR and (13)C NMR data. α-Amylase inhibitory activity was determined by a colorimetric assay using 3,5-dinitro salysilic acid. During phytochemical examination, α-amyrin, β-amyrin and β-sitosterol were purified from the hexane fraction, while ursolic acid, daucosterol and swertiamarin were isolated from chloroform fraction. The results of the biochemical assay revealed α-amylase inhibitory activity of hexane, chloroform, methanol and water fractions, of which the chloroform and methanol fractions were more potent (IC50 16.8 and 18.1 mg/ml, respectively). Among examined compounds, daucosterol was found to be the most potent α-amylase inhibitor (57.5% in concentration 10 mg/ml). With regard to α-amylase inhibitory effects of the plant extracts, purified constituents, and antidiabetic application of the species of Swertia genus in traditional medicine of different countries, S. longifolia seems more appropriate species for further mechanistic antidiabetic evaluations. PMID:27051429

  11. Change in chemical constituents and free radical-scavenging activity during Pear (Pyrus pyrifolia) cultivar fruit development.

    PubMed

    Cho, Jeong-Yong; Lee, Sang-Hyun; Kim, Eun Hee; Yun, Hae Rim; Jeong, Hang Yeon; Lee, Yu Geon; Kim, Wol-Soo; Moon, Jae-Hak

    2015-01-01

    Changes in chemical constituent contents and DPPH radical-scavenging activity in fruits of pear (Pyrus pyrifolia) cultivars during the development were investigated. The fruits of seven cultivars (cv. Niitaka, Chuhwangbae, Wonhwang, Hwangkeumbae, Hwasan, Manpungbae, and Imamuraaki) were collected at 15-day intervals after day 20 of florescence. Vitamins (ascorbic acid and α-tocopherol), arbutin, chlorogenic acid, malaxinic acid, total caffeic acid, total flavonoids, and total phenolics were the highest in immature pear fruit on day 20 after florescence among samples at different growth stages. All of these compounds decreased gradually in the fruit during the development. Immature pear fruit on day 35 or 50 after florescence exhibited higher free radical-scavenging activity than that at other times, although activities were slightly different among cultivars. The chemical constituent contents and free radical-scavenging activity were largely different among immature fruits of the pear cultivars, but small differences were observed when they matured. PMID:25348501

  12. Inhibition of Human Aldehyde Oxidase Activity by Diet-Derived Constituents: Structural Influence, Enzyme-Ligand Interactions, and Clinical Relevance

    PubMed Central

    Barr, John T.; Jones, Jeffrey P.; Oberlies, Nicholas H.

    2015-01-01

    The mechanistic understanding of interactions between diet-derived substances and conventional medications in humans is nascent. Most investigations have examined cytochrome P450–mediated interactions. Interactions mediated by other phase I enzymes are understudied. Aldehyde oxidase (AO) is a phase I hydroxylase that is gaining recognition in drug design and development programs. Taken together, a panel of structurally diverse phytoconstituents (n = 24) was screened for inhibitors of the AO-mediated oxidation of the probe substrate O6-benzylguanine. Based on the estimated IC50 (<100 μM), 17 constituents were advanced for Ki determination. Three constituents were described best by a competitive inhibition model, whereas 14 constituents were described best by a mixed-mode model. The latter model consists of two Ki terms, Kis and Kii, which ranged from 0.26–73 and 0.80–120 μM, respectively. Molecular modeling was used to glean mechanistic insight into AO inhibition. Docking studies indicated that the tested constituents bound within the AO active site and elucidated key enzyme-inhibitor interactions. Quantitative structure-activity relationship modeling identified three structural descriptors that correlated with inhibition potency (r2 = 0.85), providing a framework for developing in silico models to predict the AO inhibitory activity of a xenobiotic based solely on chemical structure. Finally, a simple static model was used to assess potential clinically relevant AO-mediated dietary substance–drug interactions. Epicatechin gallate and epigallocatechin gallate, prominent constituents in green tea, were predicted to have moderate to high risk. Further characterization of this uncharted type of interaction is warranted, including dynamic modeling and, potentially, clinical evaluation. PMID:25326286

  13. Inhibition of human aldehyde oxidase activity by diet-derived constituents: structural influence, enzyme-ligand interactions, and clinical relevance.

    PubMed

    Barr, John T; Jones, Jeffrey P; Oberlies, Nicholas H; Paine, Mary F

    2015-01-01

    The mechanistic understanding of interactions between diet-derived substances and conventional medications in humans is nascent. Most investigations have examined cytochrome P450-mediated interactions. Interactions mediated by other phase I enzymes are understudied. Aldehyde oxidase (AO) is a phase I hydroxylase that is gaining recognition in drug design and development programs. Taken together, a panel of structurally diverse phytoconstituents (n = 24) was screened for inhibitors of the AO-mediated oxidation of the probe substrate O(6)-benzylguanine. Based on the estimated IC50 (<100 μM), 17 constituents were advanced for Ki determination. Three constituents were described best by a competitive inhibition model, whereas 14 constituents were described best by a mixed-mode model. The latter model consists of two Ki terms, Kis and Kii, which ranged from 0.26-73 and 0.80-120 μM, respectively. Molecular modeling was used to glean mechanistic insight into AO inhibition. Docking studies indicated that the tested constituents bound within the AO active site and elucidated key enzyme-inhibitor interactions. Quantitative structure-activity relationship modeling identified three structural descriptors that correlated with inhibition potency (r(2) = 0.85), providing a framework for developing in silico models to predict the AO inhibitory activity of a xenobiotic based solely on chemical structure. Finally, a simple static model was used to assess potential clinically relevant AO-mediated dietary substance-drug interactions. Epicatechin gallate and epigallocatechin gallate, prominent constituents in green tea, were predicted to have moderate to high risk. Further characterization of this uncharted type of interaction is warranted, including dynamic modeling and, potentially, clinical evaluation. PMID:25326286

  14. Jumping the gun: Smoking constituent BaP causes premature primordial follicle activation and impairs oocyte fusibility through oxidative stress

    SciTech Connect

    Sobinoff, A.P.; Pye, V.; Nixon, B.; Roman, S.D.; McLaughlin, E.A.

    2012-04-01

    Benzo(a)pyrene (BaP) is an ovotoxic constituent of cigarette smoke associated with pre-mature ovarian failure and decreased rates of conception in IVF patients. Although the overall effect of BaP on female fertility has been documented, the exact molecular mechanisms behind its ovotoxicity remain elusive. In this study we examined the effects of BaP exposure on the ovarian transcriptome, and observed the effects of in vivo exposure on oocyte dysfunction. Microarray analysis of BaP cultured neonatal ovaries revealed a complex mechanism of ovotoxicity involving a small cohort of genes associated with follicular growth, cell cycle progression, and cell death. Histomorphological and immunohistochemical analysis supported these results, with BaP exposure causing increased primordial follicle activation and developing follicle atresia in vitro and in vivo. Functional analysis of oocytes obtained from adult Swiss mice treated neonatally revealed significantly increased levels of mitochondrial ROS/lipid peroxidation, and severely reduced sperm-egg binding and fusion in both low (1.5 mg/kg/daily) and high (3 mg/kg/daily) dose treatments. Our results reveal a complex mechanism of BaP induced ovotoxicity involving developing follicle atresia and accelerated primordial follicle activation, and suggest short term neonatal BaP exposure causes mitochondrial leakage resulting in reduced oolemma fluidity and impaired fertilisation in adulthood. This study highlights BaP as a key compound which may be partially responsible for the documented effects of cigarette smoke on follicular development and sub-fertility. -- Highlights: ► BaP exposure up-regulates canonical pathways linked with follicular growth/atresia. ► BaP causes primordial follicle activation and developing follicle atresia. ► BaP causes oocyte mitochondrial ROS and lipid peroxidation, impairing fertilisation. ► Short term neonatal BaP exposure compromises adult oocyte quality.

  15. Autoignition response of n-butanol and its blend with primary reference fuel constituents of gasoline.

    DOE PAGESBeta

    Kumar, Kamal; Zhang, Yu; Sung, Chi -Jen; Pitz, William J.

    2015-04-13

    We study the influence of blending n-butanol on the ignition delay times of n-heptane and iso-octane, the primary reference fuels for gasoline. The ignition delay times are measured using a rapid compression machine, with an emphasis on the low-to-intermediate temperature conditions. The experiments are conducted at equivalence ratios of 0.4 and 1.0, for a compressed pressure of 20 bar, with the temperatures at the end of compression ranging from 613 K to 979 K. The effect of n-butanol addition on the development of the two-stage ignition characteristics for the two primary reference fuels is also examined. The experimental results aremore » compared to predictions obtained using a detailed chemical kinetic mechanism, which has been obtained by a systematic merger of previously reported base models for the combustion of the individual fuel constituents. In conclusion, a sensitivity analysis on the base, and the merged models, is also performed to understand the dependence of autoignition delay times on the model parameters.« less

  16. Physiological responses of dogs on exposure to hot, arid conditions. Serum constituents.

    PubMed

    Krausz, S; Marder, J; Eylath, U

    1977-09-16

    Serum electrolytes, metabolites and enzymes were determined in arterial blood of chronically cannulated dogs at room temperature and on exposure to 44-50 degrees C. These dogs were naturally acclimated to hot, arid conditions. In dogs maintaining their rectal temperatures (TR) below 40 degrees C, no significant changes were seen in the levels of Na+, Cl-, cholesterol, uric acid, alkaline phosphatase, lactic dehydrogenase or glutamic-pyruvic transaminase (SGPT). K+, CO2, glucose decreased significantly, and urea nitrogen (BUN) and glutamic-oxaloacetic transaminase (SGOT) showed small but significant increases. In several cases of excitable dogs, in which TR increased above 40 degrees C, we found large, significant increases in uric acid, SGPT and SGOT, and a decrease in cholesterol. The results suggest that in dogs maintaining their TR when exposed to high temperatures, changes in serum constituents indicate merely the presence of respiratory alkalosis and an increased energetic demand. When control of TR is lost, changes occur which suggest liver, and possibly cardiac, tissue damage. PMID:563059

  17. Characterization of volatile constituents of Origanum onites and their antifungal and antibacterical activity

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Essential oils obtained by hydrodistillation (HD) and microwave-assisted hydrodistillaton (MWHD) of Origanum onites aerial parts were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC/MS). Thirty-one constituents representing 98.6% of the water distilled oil and fifty-...

  18. Trypanocidal constituents in plants 5. Evaluation of some Mexican plants for their trypanocidal activity and active constituents in the seeds of Persea americana.

    PubMed

    Abe, Fumiko; Nagafuji, Shinya; Okawa, Masafumi; Kinjo, Junei; Akahane, Hiroshige; Ogura, Tetsuya; Martinez-Alfaro, Miguel Angel; Reyes-Chilpa, Ricardo

    2005-07-01

    Crude extracts of Mexican medicinal plants were screened for trypanocidal activity against Trypanosoma cruzi, which is the etiological agent for Chagas' disease, one of the most serious protozoan diseases in Latin America. There were 71 kinds of methanolic and other organic extracts from 65 plants, which were newly examined by a preliminary screening test to observe immobilization of epimastigotes and trypomastigotes of T. cruzi in vitro. The MeOH extract of seeds of Persea americana (avocado) showed moderate activity against epimastigotes. In order to identify the principal compounds for the activity, the MeOH extract was subjected to bioassay-guided fractionation. From the active fractions, six 1,2,4-trihydroxyheptadecane derivatives and two 1,2,4-trihydroxynonadecane derivatives including a new one were isolated. These compounds showed moderate activity against epimastigotes and trypomastigotes. PMID:15997123

  19. New chemical constituents from Oryza sativa straw and their algicidal activities against blue-green algae.

    PubMed

    Ahmad, Ateeque; Kim, Seung-Hyun; Ali, Mohd; Park, Inmyoung; Kim, Jin-Seog; Kim, Eun-Hye; Lim, Ju-Jin; Kim, Seul-Ki; Chung, Ill-Min

    2013-08-28

    Five new constituents, 5,4'-dihydroxy-7,3'-dimethoxyflavone-4'-O-β-D-xylopyranosyl-(2a→1b)-2a-O-β-D-xylopyranosyl-(2b→1c)-2b-O-β-D-xylopyranosyl-2c-octadecanoate (1), 5,4'-dihydroxy-7,3'-dimethoxyflavone-4'-O-α-D-xylopyranosyl-(2a→1b)-2a-O-α-D-xylopyranosyl-(2b→1c)-2b-O-α-D-xylopyranosyl-(2c→1d)-2c-O-α-D-xylopyranosyl-2d-octadecanoate (2), kaempferol-3-O-α-D-xylopyranosyl-(2a→1b)-2a-O-α-D-xylopyranosyl-(2b→1c)-2b-O-α-D-xylopyranosyl-(2c→1d)-2c-O-α-D-xylopyranosyl-2d-hexadecanoate (3), methyl salicylate-2-O-α-D-xylopyranosyl-(2a→1b)-2a-O-α-D-xylopyranosyl-(2b→1c)-2b-O-α-D-xylopyranosyl-(2c→1d)-2c-O-α-D-xylopyranosyl-(2d→1e)-2d-O-α-D-xylopyranosyl-(2e→1f)-2e-O-α-D-xylopyranosyl-(2f→1g)-2f-O-α-D-xylopyranosyl-(2g→1h)-2g-O-α-D-xylopyranosyl-2h-geranilan-8',10'-dioic acid-1'-oate (4), and oleioyl-β-D-arabinoside (5), along with eight known compounds, were isolated from a methanol extract of Oryza sativa straw. The structures of the new compounds were elucidated using one- and two-dimensional NMR spectroscopies in combination with IR, ESI/MS, and HR-ESI/FTMS. In bioassays with blue-green algae, the efficacies of the algicidal activities of the five new compounds (1-5) were evaluated at concentrations of 1, 10, and 100 mg/L. Compound 5 had the highest growth inhibition (92.6 ± 0.3%) for Microcystis aeruginosa UTEX 2388 at a concentration of 100 ppm (mg/L). Compound 5 has high potential for the ecofriendly control of weeds and algae harmful to water-logged rice. PMID:23889328

  20. Idiosyncratic responses of evergreen broad-leaved forest constituents in China to the late Quaternary climate changes

    PubMed Central

    Fan, Dengmei; Hu, Wan; Li, Bo; Morris, Ashley B.; Zheng, Min; Soltis, Douglas E.; Soltis, Pamela S.; Zhang, Zhiyong

    2016-01-01

    Subtropical evergreen broad-leaved forest (EBLF) is one of the most important vegetation types in China. Inferences from palaeo-biome reconstruction (PBR) and phylogeography regarding range shift history of EBLF during the late Quaternary are controversial and should be reconciled. We compared phylogeographic patterns of three EBLF constituents in China, Castanopsis tibetana, Machilus thunbergii and Schima superba. Contrary to a chorus of previous phylogeographic studies and the results of species distribution modelling (SDM) of this study (in situ survival during the LGM), the three species displayed three different phylogeographic patterns that conform to either an in situ survival model or an expansion-contraction model. These results are partially congruent with the inference of PBR that EBLF was absent to the north of 24° N at the LGM. This study suggests that the constituents of EBLF could have responded idiosyncratically to climate changes during the Late Quaternary. The community assemblages of EBLF could have been changing over time, resulting in no palaeo-analogs to modern-day EBLF, which may be the main reason responsible for the failure of PBR to detect the occurrence of EBLF north of 24° N at the LGM. PMID:27534981

  1. Idiosyncratic responses of evergreen broad-leaved forest constituents in China to the late Quaternary climate changes.

    PubMed

    Fan, Dengmei; Hu, Wan; Li, Bo; Morris, Ashley B; Zheng, Min; Soltis, Douglas E; Soltis, Pamela S; Zhang, Zhiyong

    2016-01-01

    Subtropical evergreen broad-leaved forest (EBLF) is one of the most important vegetation types in China. Inferences from palaeo-biome reconstruction (PBR) and phylogeography regarding range shift history of EBLF during the late Quaternary are controversial and should be reconciled. We compared phylogeographic patterns of three EBLF constituents in China, Castanopsis tibetana, Machilus thunbergii and Schima superba. Contrary to a chorus of previous phylogeographic studies and the results of species distribution modelling (SDM) of this study (in situ survival during the LGM), the three species displayed three different phylogeographic patterns that conform to either an in situ survival model or an expansion-contraction model. These results are partially congruent with the inference of PBR that EBLF was absent to the north of 24° N at the LGM. This study suggests that the constituents of EBLF could have responded idiosyncratically to climate changes during the Late Quaternary. The community assemblages of EBLF could have been changing over time, resulting in no palaeo-analogs to modern-day EBLF, which may be the main reason responsible for the failure of PBR to detect the occurrence of EBLF north of 24° N at the LGM. PMID:27534981

  2. Biological activities and chemical constituents of some mangrove species from Sundarban estuary: An overview

    PubMed Central

    Simlai, Aritra; Roy, Amit

    2013-01-01

    This review represents the studies performed on some beneficial mangrove plants such as Ceriops decandra, Xylocarpus granatum, Xylocarpus moluccensis, Excoecaria agallocha, Sarcolobus globosus, Sonneratia caseolaris and Acanthus ilicifolius from the Sundarban estuary spanning India and Bangladesh with regard to their biological activities and chemical investigations till date. Sundarban is the largest single chunk of mangrove forest in the world. The forest is a source of livelihood to numerous people of the region. Several of its plant species have very large applications in the traditional folk medicine; various parts of these plants are used by the local people as cure for various ailments. Despite such enormous potential, remarkably few reports are available on these species regarding their biological activities and the active principles responsible for such activities. Though some chemical studies have been made on the mangrove plants of this estuary, reports pertaining to their activity-structure relationship are few in number. An attempt has been made in this review to increase the awareness for the medicinal significance as well as conservation and utilization of these mangrove species as natural rich sources of novel bioactive agents. PMID:24347925

  3. Biological activities and chemical constituents of some mangrove species from Sundarban estuary: An overview.

    PubMed

    Simlai, Aritra; Roy, Amit

    2013-07-01

    This review represents the studies performed on some beneficial mangrove plants such as Ceriops decandra, Xylocarpus granatum, Xylocarpus moluccensis, Excoecaria agallocha, Sarcolobus globosus, Sonneratia caseolaris and Acanthus ilicifolius from the Sundarban estuary spanning India and Bangladesh with regard to their biological activities and chemical investigations till date. Sundarban is the largest single chunk of mangrove forest in the world. The forest is a source of livelihood to numerous people of the region. Several of its plant species have very large applications in the traditional folk medicine; various parts of these plants are used by the local people as cure for various ailments. Despite such enormous potential, remarkably few reports are available on these species regarding their biological activities and the active principles responsible for such activities. Though some chemical studies have been made on the mangrove plants of this estuary, reports pertaining to their activity-structure relationship are few in number. An attempt has been made in this review to increase the awareness for the medicinal significance as well as conservation and utilization of these mangrove species as natural rich sources of novel bioactive agents. PMID:24347925

  4. Therapeutics Role of Azadirachta indica (Neem) and Their Active Constituents in Diseases Prevention and Treatment

    PubMed Central

    Alzohairy, Mohammad A.

    2016-01-01

    Neem (Azadirachta indica) is a member of the Meliaceae family and its role as health-promoting effect is attributed because it is rich source of antioxidant. It has been widely used in Chinese, Ayurvedic, and Unani medicines worldwide especially in Indian Subcontinent in the treatment and prevention of various diseases. Earlier finding confirmed that neem and its constituents play role in the scavenging of free radical generation and prevention of disease pathogenesis. The studies based on animal model established that neem and its chief constituents play pivotal role in anticancer management through the modulation of various molecular pathways including p53, pTEN, NF-κB, PI3K/Akt, Bcl-2, and VEGF. It is considered as safe medicinal plants and modulates the numerous biological processes without any adverse effect. In this review, I summarize the role of Azadirachta indica in the prevention and treatment of diseases via the regulation of various biological and physiological pathways. PMID:27034694

  5. Therapeutics Role of Azadirachta indica (Neem) and Their Active Constituents in Diseases Prevention and Treatment.

    PubMed

    Alzohairy, Mohammad A

    2016-01-01

    Neem (Azadirachta indica) is a member of the Meliaceae family and its role as health-promoting effect is attributed because it is rich source of antioxidant. It has been widely used in Chinese, Ayurvedic, and Unani medicines worldwide especially in Indian Subcontinent in the treatment and prevention of various diseases. Earlier finding confirmed that neem and its constituents play role in the scavenging of free radical generation and prevention of disease pathogenesis. The studies based on animal model established that neem and its chief constituents play pivotal role in anticancer management through the modulation of various molecular pathways including p53, pTEN, NF-κB, PI3K/Akt, Bcl-2, and VEGF. It is considered as safe medicinal plants and modulates the numerous biological processes without any adverse effect. In this review, I summarize the role of Azadirachta indica in the prevention and treatment of diseases via the regulation of various biological and physiological pathways. PMID:27034694

  6. Anti-allergic activity of the Morinda citrifolia extract and its constituents

    PubMed Central

    Murata, Kazuya; Abe, Yumi; Shinohara, Kaito; Futamura-Masuda, Megumi; Uwaya, Akemi; Isami, Fumiyuki; Matsuda, Hideaki

    2014-01-01

    Background: Morinda citrifolia (Rubiaceae), commonly known as noni is distributed throughout tropical and sub-tropical regions of the world. Anti-allergic effects of noni have not been reported despite the clinical usage as an anti-allergic agent. Materials and Methods: To investigate the anti-allergic effects of the 50% ethanolic extract of M. citrifolia fruits and leaves (MCF-ext and MCL-ext), dinitrofluorobenzene (DNFB)-induced triphasic cutaneous reaction and picryl chloride-induced contact dermatitis (PC-CD) tests were performed. Results: In DNFB-induced triphasic cutaneous reaction, oral administration of MCF-ext and MCL-ext exhibited dose-dependent inhibition of cutaneous reaction at 1 h (immediate phase response) after the DNFB challenge. MCF-ext also inhibited ear swelling at 24 h (late phase response) and 8 days (very late phase response) after the DNFB challenge. The effect of MCL-ext on the immediate phase response was attributed to the anti-degranulation from RBL-2H3 cells, while MCF-ext had no significant effect on degranulation. The active components of anti-degranulation activity in MCL-ext were determined to be ursolic acid, rutin and kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside. In the PC-CD test, both MCF-ext and MCL-ext showed an anti-swelling effect but the potency of MCF-ext was stronger than MCL-ext. Conclusion: These data suggest that noni fruits and leaves can be a daily consumable material for the prevention of allergic symptoms. PMID:25002809

  7. Pterostilbene, an Active Constituent of Blueberries, Stimulates Nitric Oxide Production via Activation of Endothelial Nitric Oxide Synthase in Human Umbilical Vein Endothelial Cells.

    PubMed

    Park, Seong Hoon; Jeong, Sun-Oh; Chung, Hun-Teag; Pae, Hyun-Ock

    2015-09-01

    Endothelial dysfunction, a key process in development of cardiovascular diseases, is largely due to reduced nitric oxide (NO) derived from endothelial NO synthase (eNOS). Resveratrol has been reported to stimulate NO production via estrogen receptor α (ERα) activation in endothelial cells. Here, we investigated whether two natural methylated analogs of resveratrol, pterostilbene (Pts) and trans-3,5,4'-trimethoxystilbene (TMS), similarly to resveratrol, could influence endothelial NO release in human umbilical vein endothelial cells (HUVECs). In HUVECs exposed to Pts or TMS, NO production and phosphorylation of eNOS, protein kinase B (Akt), and ERα were measured by using a fluorimetric NO assay kit and Western blot analysis, respectively. Dimethylated Pts, but not trimethylated TMS, stimulated dose-dependent NO production via eNOS phosphorylation. Pts also stimulated dose-dependent phosphorylation of Akt, but not of ERα. NO production and eNOS phosphorylation in response to Pts were significantly abolished by the phosphoinositide 3-kinase (PI3K)/Akt inhibitor LY294002, but not by the ERα antagonist ICI182780. Our results suggest that Pts, but not TMS, is capable of inducing eNOS phosphorylation and the subsequent NO release, presumably, by activating PI3K/Akt pathway. The potential efficacy of Pts, an active constituent of blueberries, may aid in the prevention of cardiovascular diseases characterized by endothelial dysfunction. PMID:26008990

  8. Lipid constituents of the edible mushroom, Pleurotus giganteus demonstrate anti-Candida activity.

    PubMed

    Phan, Chia-Wei; Lee, Guan-Serm; Macreadie, Ian G; Malek, Sri Nurestri Abd; Pamela, David; Sabaratnam, Vikineswary

    2013-12-01

    Different solvent extracts of Pleurotus giganteus fruiting bodies were tested for antifungal activities against Candida species responsible for human infections. The lipids extracted from the ethyl acetate fraction significantly inhibited the growth of all the Candida species tested. Analysis by GC/MS revealed lipid components such as fatty acids, fatty acid methyl esters, ergosterol, and ergosterol derivatives. The sample with high amounts of fatty acid methyl esters was the most effective antifungal agent. The samples were not cytotoxic to a mammalian cell line, mouse embryonic fibroblasts BALB/c 3T3 clone A31. To our knowledge, this is the first report of antifungal activity of the lipid components of Pleurotus giganteus against Candida species. PMID:24555294

  9. Relevance of phenolic diterpene constituents to antioxidant activity of supercritical CO(2) extract from the leaves of rosemary.

    PubMed

    Chang, Chi-Huang; Chyau, Charng-Cherng; Hsieh, Chiu-Lan; Wu, Yen-Ying; Ker, Yaw-Bee; Tsen, Hau-Yang; Peng, Robert Y

    2008-01-10

    Isolation of phenolic diterpene constituents from the freeze-dried leaves of Rosmarinus officinalis has been obtained by supercritical extraction with carbon dioxide. To determine the ideal conditions for the maximum yield of extract, nine different conditions using three levels of pressures (3000, 4000 and 5000 psi) in combination with three temperatures at 40, 60 and 80 degrees C, respectively, in combination with the analyses of the corresponding antioxidant activities and constituents which existed in extracts has been investigated. The antioxidant activity of each obtained extract was determined by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals test. GC/MS method was used as an alternative to conventional HPLC method for the determination of the principal antioxidant constituents in extract, including phenolic diterpenes carnosic acid (CA) and carnosol (CAL). The confirmation of CA and CAL in extract was forward performed by subjecting HPLC isolates from extract into an ion trap mass spectrometer through an electrospray ionization (ESI) interface for MS/MS analysis. These results indicate that an ideal extraction process was obtained at 5000 psi and 80 degrees C with an extraction yield of 4.27% (w/w) and rich in phenolic antioxidants CA and CAL as contents of 35.23 and 0.46 mg g(-1) in extract, respectively. PMID:17999341

  10. Effect of Crocus sativus extracts and its active constituent safranal on the harmaline-induced tremor in mice

    PubMed Central

    Amin, Bahareh; Malekzadeh, Mahshad; Heidari, Mahmoud Reza; Hosseinzadeh, Hossein

    2015-01-01

    Objective(s): Due to unsatisfactory response or intolerable side effects of current drugs, treatment of essential tremor remains inadequate. Thus, we aimed to investigate the protective and therapeutic effects of aqueous and ethanolic extracts of Crocus sativus (saffron), and its active consistent, safranal, on the harmaline-induced tremor in mice. Materials and Methods: To induce tremor, harmaline (30 mg/kg) was injected intraperitoneally. Test groups were also given the aqueous and ethanolic extracts of saffron (40, 80, and 160 mg/kg) as well as safranal (0.1, 0.3, and 0.5 ml/kg), intraperitoneally, 10 min before harmaline administration (prophylactic study) or 10 min after the onset of tremors (curative study). The latency of onset, duration, and intensity of tremor were recorded. Results: The extracts (80 and160 mg/kg) dose dependently attenuated duration of harmaline-induced tremors as did reference drug, propranolol (2 and 5 mg/kg). Only the highest dose of extracts (160 mg/kg) attenuated intensity of harmaline-induced tremors throughout the study. Safranal at the doses of (0.1 and 0.3 ml/kg) but not 0.5 ml/kg attenuated duration and intensity of tremor. Onset of tremor increased with the extracts (80 and 160 mg/kg) in prophylactic study, as the effect observed with propranolol at the dose of 5 mg/kg. Safranal did not affect the latency of tremor. Conclusion: Both aqueous and ethanolic extracts of saffron and with a less effect, low doses of safranal, have relatively protective and suppressive effects on the harmaline-induced tremor and different constituents of extracts seem to participate in the protective effects against harmaline induced tremor. PMID:26124930

  11. Anti-inflammatory activities of Gouania leptostachya methanol extract and its constituent resveratrol.

    PubMed

    Dung, To Thi Mai; Lee, Jongsung; Kim, Eunji; Yoo, Byong Chul; Ha, Van Thai; Kim, Yong; Yoon, Deok Hyo; Hong, Sungyoul; Baek, Kwang-Soo; Sung, Nak Yoon; Kim, Tae Woong; Kim, Jong-Hoon; Cho, Jae Youl

    2015-03-01

    Gouania leptostachya DC. var. tonkinensis Pitard. Rhamnaceae is a traditional medicinal plant used in Thailand for treating various inflammatory symptoms. However, no systematic studies have been performed concerning the anti-inflammatory effects or molecular mechanisms of this plant. The immunopharmacological activities of a methanol extract from the leaves and twigs of G. leptostachya (Gl-ME) were elucidated based on the gastritis symptoms of mice treated with HCl/EtOH and the inflammatory responses, such as nitric oxide (NO) release and prostaglandin E2 (PGE2) production, from RAW264.7 cells and peritoneal macrophages. Moreover, inhibitory target molecules were also assessed. Gl-ME dose-dependently diminished the secretion of NO and PGE2 from LPS-stimulated RAW264.7 cells and peritoneal macrophages. The gastritis lesions of HCl/EtOH-treated mice were also attenuated after Gl-ME treatment. The extract (50 and 300 µg/mL) clearly reduced mRNA expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2, nuclear translocation of p65/nuclear factor (NF)-κB, phosphorylation of p65-activating upstream enzymes, such as protein kinase B (AKT), inhibitor of κBα kinase (IKK), and inhibitor of κB (IκBα), and the enzymatic activity of Src. By HPLC analysis, one of the major components in the extract was revealed as resveratrol with NO and Src inhibitory activities. Moreover, this compound suppressed NO production and HCl/EtOH-induced gastric symptoms. Therefore, these results suggest that Gl-ME might be useful as an herbal anti-inflammatory medicine through the inhibition of Src and NF-κB activation pathways. The efficacy data of G. leptostachya also implies that this plant could be further tested to see whether it can be developed as potential anti-inflammatory preparation. PMID:25414115

  12. Chemical constituents of Machaerium hirtum Vell. (Fabaceae) leaves and branches and its anti-inflammatory activity evaluation.

    PubMed

    Ignoato, Marlene C; Fabrão, Rodrigo M; Schuquel, Ivânia T A; Botelho, Marcos F P; Bannwart, Geanderson; Pomini, Armando M; Arruda, Laura L M; Bersani-Amado, Ciomar A; Santin, Silvana M O

    2013-01-01

    Leaves and branches of Machaerium hirtum Vell. (Fabaceae), native to South America, were subjected to phytopharmacological investigation in order to identify its major chemical constituents and evaluate its extracts, fractions and isolated compounds in assays for anti-inflammatory activities. These were performed using mouse ear edema model, pleurisy and myeloperoxidase activity assays. Six compounds were isolated and identified as the flavanones swertisin and isovitexin, the alkaloid 4-hydroxy-N-methylproline, the triterpenes friedelin and lupeol, and the steroids sitosterol and stigmasterol. These compounds were identified by nuclear magnetic resonance of (1)H and (13)C data, in comparison with literature. PMID:23126578

  13. Phytochemical Constituents and Antioxidant and Antimicrobial Activity of Selected Plants Used Traditionally as a Source of Food.

    PubMed

    Tabit, Frederick Tawi; Komolafe, Naomi Tope; Tshikalange, Thilivhali Emmanuel; Nyila, Monde Alfred

    2016-03-01

    Many indigenous plants have also been used as a source of food and medicine in many African rural communities in the past. The study investigated the antimicrobial activity, phytochemical constituent, and antioxidant activity of selected traditional plants used traditionally as a source of food and medicine. The methanol and water extracts of different plant parts were analyzed for phytochemicals using standard phytochemical screening reagents while the broth microdilution assays were used to analyze antimicrobial activities. Alkaloids, phenols, flavonoids, saponins, tannins, and terpenes were found in one or more of the plant extracts, and all the plant extracts demonstrated scavenging activities. The back extracts of Sclerocarya birrea and the leaf extracts of Garcinia livingstonei exhibit the best antioxidant activities, while the water and methanol back extracts of S. birrea and G. livingstonei were the most active against all the tested foodborne bacteria. PMID:26987025

  14. Biofunctional constituent isolated from Citrullus colocynthis fruits and structure-activity relationships of its analogues show acaricidal and insecticidal efficacy.

    PubMed

    Jeon, Ju-Hyun; Lee, Hoi-Seon

    2014-08-27

    The acaricidal and insecticidal potential of the active constituent isolated from Citrullus colocynthis fruits and its structurally related analogues was evaluated by performing leaf disk, contact toxicity, and fumigant toxicity bioassays against Tetranychus urticae, Sitophilus oryzae, and Sitophilus zeamais adults. The active constituent of C. colocynthis fruits was isolated by chromatographic techniques and was identified as 4-methylquinoline on the basis of spectroscopic analyses. To investigate the structure-activity relationships, 4-methylquinoline and its structural analogues were tested against mites and two insect pests. On the basis of the LC50 values, 7,8-benzoquinoline was the most effective against T. urticae. Quinoline, 8-hydroxyquinoline, 2-methylquinoline, 4-methylquinoline, 6-methylquinoline, 8-methylquinoline, and 7,8-benzoquinoline showed high insecticidal activities against S. oryzae and S. zeamais regardless of the application method. These results indicate that introduction of a functional group into the quinoline skeleton and changing the position of the group have an important influence on the acaricidal and insecticidal activities. Furthermore, 4-methylquinoline isolated from C. colocynthis fruits, along with its structural analogues, could be effective natural pesticides for managing spider mites and stored grain weevils. PMID:25110971

  15. Larvicidal activity of the essential oil of Youngia japonica aerial parts and its constituents against Aedes albopictus.

    PubMed

    Liu, Xin Chao; Liu, Qiyong; Chen, Xu Bo; Liu, Qi Zhi; Liu, Zhi Long

    2015-01-01

    The aim of this study was to evaluate the larvicidal activity of the essential oil of Youngia japonica aerial parts against the larvae of Aedes albopictus and to isolate any active compounds from the oil. Gas chromatography-mass spectrometry (GC-MS) analyses revealed the presence of 31 compounds, with menthol (23.53%), α-asarone (21.54%), 1,8-cineole (5.36%), and caryophyllene (4.45%) as the major constituents. Bioactivity-directed chromatographic separation of the oil led to the isolation of menthol and α-asarone as active compounds. The essential oil of Y. japonica exhibited larvicidal activity against the fourth instar larvae of A. albopictus with an LC₅₀ value of 32.45 μg/mL. α-Asarone and menthol possessed larvicidal activity against the fourth instar larvae of A. albopictus with LC₅₀ values of 24.56 μg/mL and 77.97 μg/mL, respectively. The results indicate that the essential oil of Y. japonica aerial parts and the two constituents can be potential sources of natural larvicides. PMID:25854838

  16. The Role of Nigella sativa and Its Active Constituents in Learning and Memory.

    PubMed

    Sahak, Mohamad Khairul Azali; Kabir, Nurul; Abbas, Ghulam; Draman, Suhaimi; Hashim, Noor Hashida; Hasan Adli, Durriyyah Sharifah

    2016-01-01

    The loss of the ability for learning and memory is a prominent feature of dementia, which affects millions of individuals all over the world, due to either neurodegenerative diseases or brain injury. Although a lot of information is known about the pathology involved, treatment remains elusive at best. The Black Seed of Nigella sativa has been historically and religiously used for thousands of years for preventing and treating many different kinds of diseases. This review article looks at Nigella sativa and its potential role in facilitating learning and memory. The possible use of this seed's extract or compounds isolated from it, such as thymoquinone, for treating damaged brain neural tissue is discussed. The evidence presented in this paper appears to be supporting the hypothesis that this plant and/or its bioactive constituents can enhance learning and memory in health and disease in animals and humans. PMID:27022403

  17. The Role of Nigella sativa and Its Active Constituents in Learning and Memory

    PubMed Central

    Sahak, Mohamad Khairul Azali; Kabir, Nurul; Abbas, Ghulam; Draman, Suhaimi; Hashim, Noor Hashida; Hasan Adli, Durriyyah Sharifah

    2016-01-01

    The loss of the ability for learning and memory is a prominent feature of dementia, which affects millions of individuals all over the world, due to either neurodegenerative diseases or brain injury. Although a lot of information is known about the pathology involved, treatment remains elusive at best. The Black Seed of Nigella sativa has been historically and religiously used for thousands of years for preventing and treating many different kinds of diseases. This review article looks at Nigella sativa and its potential role in facilitating learning and memory. The possible use of this seed's extract or compounds isolated from it, such as thymoquinone, for treating damaged brain neural tissue is discussed. The evidence presented in this paper appears to be supporting the hypothesis that this plant and/or its bioactive constituents can enhance learning and memory in health and disease in animals and humans. PMID:27022403

  18. Studies on the constituents of seeds of Pachyrrhizus erosus and their anti herpes simplex virus (HSV) activities.

    PubMed

    Phrutivorapongkul, Ampai; Lipipun, Vimolmas; Ruangrungsi, Nijsiri; Watanabe, Toshiko; Ishikawa, Tsutomu

    2002-04-01

    Studies on the chemical constituents of the seeds of Pachyrrhizus erosus (Leguminosae) resulted in the isolation of nine known components: five rotenoids [dolineone (3), pachyrrhizone (5), 12a-hydroxydolineone (7), 12a-hydroxypachyrrhizone (9), and 12a-hydroxyrotenone (2)], two isoflavonoids [neotenone (4) and dehydroneotenone (8)], one phenylfuranocoumarin [pachyrrhizine (6)], and a monosaccharide (dulcitol). The full 1H- and 13C-NMR assignments for the isolated products except a sugar, including revision of previous assignments in the literature, are reported. Moderate anti herpes simplex virus (HSV) activity was observed in 12a-hydroxydolineone (7) and 12a-hydroxypachyrrhizone (9) among the isolated products. PMID:11964004

  19. Cardiopulmonary responses of intratracheally instilled tire particles and constituent metal components

    USGS Publications Warehouse

    Gottipolu, R.R.; Landa, E.R.; Schladweiler, M.C.; McGee, J.K.; Ledbetter, A.D.; Richards, J.H.; Wallenborn, G.J.; Kodavanti, U.P.

    2008-01-01

    Tire and brake wear particles contain transition metals, and contribute to near-road PM. We hypothesized that acute cardiopulmonary injury from respirable tire particles (TP) will depend on the amount of soluble metals. Respirable fractions of two types of TP (TP1 and TP2) were analyzed for water and acid-leachable metals using ICP-AES. Both TP types contained a variety of transition metals, including zinc (Zn), copper (Cu), aluminum, and iron. Zn and Cu were detected at high levels in water-soluble fractions (TP2 > TP1). Male Wistar Kyoto rats (12-14 wk) were intratracheally instilled, in the first study, with saline, TP1 or TP2 (5 mg/kg), and in the second study, with soluble Zn, Cu (0.5 ??mol/kg), or both. Pulmonary toxicity and cardiac mitochondrial enzymes were analyzed 1 d, 1 wk, or 4 wk later for TP and 4 or 24 h later for metals. Increases in lavage fluid markers of inflammation and injury were observed at d 1 (TP2 > TP1), but these changes reversed by wk 1. No effects on cardiac enzymes were noted with either TP. Exposure of rats to soluble Zn and Cu caused marked pulmonary inflammation and injury but temporal differences were apparent (Cu effects peaked at 4 h and Zn at 24 h). Instillation of Zn, Cu, and Zn+ Cu decreased the activity of cardiac aconitase, isocitrate dehydrogenase, succinate dehydrogenase, cytochrome-c-oxidase and superoxide dismutase suggesting mitochondrial oxidative stress. The observed acute pulmonary toxicity of TP could be due to the presence of water soluble Zn and Cu. At high concentrations these metals may induce cardiac oxidative stress. Copyright ?? Informa Healthcare USA, Inc.

  20. Activity-Guided Isolation of Bioactive Constituents with Antinociceptive Activity from Muntingia calabura L. Leaves Using the Formalin Test

    PubMed Central

    Mohamad Yusof, Mohd. Izwan; Salleh, Mohd. Zaki; Lay Kek, Teh; Ahmat, Norizan; Nik Azmin, Nik Fatini

    2013-01-01

    The present study was conducted to determine the antinociceptive potential of methanol extract of Muntingia calabura L. (MEMC) and to isolate and identify the bioactive compound(s) responsible for the observed antinociceptive activity. The MEMC and its partitions (petroleum ether (PEP), ethyl acetate (EAP), and aqueous (AQP) partitions), in the dose range of 100, 500, and 1000 mg/kg, were tested using the formalin-induced nociceptive test. The PEP, which exerted the most effective activity in the respective early and late phase, was further subjected to the fractionation procedures and yielded seven fractions (labelled A to G). These fractions were tested, at the dose of 300 mg/kg, together with distilled water or 10% DMSO (negative controls); morphine and aspirin (positive controls) for potential antinociceptive activity. Of all fractions, Fraction D showed the most significant antinociceptive activity, which is considered as equieffective to morphine or aspirin in the early or late phase, respectively. Further isolation and identification processes on fraction D led to the identification of three known and one new compounds, namely, 5-hydroxy-3,7,8-trimethoxyflavone (1), 3,7-dimethoxy-5-hydroyflavone (2), 2′,4′-dihydroxy-3′-methoxychalcone (3), and calaburone (4). At the dose of 50 mg/kg, compound 3 exhibited the highest percentage of antinociceptive activity in both phases of the formalin test. In conclusion, the antinociceptive activity of MEMC involved, partly, the synergistic activation of the flavonoid types of compounds. PMID:24348716

  1. Comparative Studies on Bioactive Constituents in Hawk Tea Infusions with Different Maturity Degree and Their Antioxidant Activities

    PubMed Central

    Yuan, Ming; Jia, Xuejing; Ding, Chunbang; Yuan, Shu; Zhang, Zhongwei; Chen, Yanger

    2014-01-01

    Hawk tea (Litsea coreana var. lanuginose) is a very popular herbal tea in the southwest of China. According to the maturity degree of raw materials, Hawk tea can usually be divided into three types: Hawk bud tea (HB), Hawk primary leaf tea (HP), and Hawk mature leaf tea (HM). In this study, some of the bioactive constituents and antioxidant properties of the three kinds of Hawk tea infusions were comparatively investigated. The results showed that the contents of total flavonoids, vitamin C, and carbohydrates in Hawk bud tea infusion (HBI) were higher than those in Hawk primary leaf tea infusion (HPI) and Hawk mature leaf tea infusion (HMI). HPI had higher contents of total polyphenols and exhibited better DPPH radical scavenging activity and ferric reducing activity power. HBI could provide more effective protection against erythrocyte hemolysis. As age is going from bud to mature leaf, the ability to inhibit the formation of low density lipoprotein (LDL) conjugated diene and the loss of tryptophan fluorescence decreased. The bioactive constituents and antioxidant activities of Hawk tea infusions were significantly affected by the maturity degree of the raw material. PMID:25133263

  2. Rapid discovery and identification of anti-inflammatory constituents from traditional Chinese medicine formula by activity index, LC-MS, and NMR

    PubMed Central

    Wang, Shufang; Wang, Haiqiang; Liu, Yining; Wang, Yi; Fan, Xiaohui; Cheng, Yiyu

    2016-01-01

    The traditional activity-guided approach has the shortcoming of low accuracy and efficiency in discovering active compounds from TCM. In this work, an approach was developed by integrating activity index (AI), liquid chromatography – mass spectrometry (LC-MS), and nuclear magnetic resonance (NMR) to rapidly predict and identify the potential active constituents from TCM. This approach was used to discover and identify the anti-inflammatory constituents from a TCM formula, Gui-Zhi-Jia-Shao-Yao-Tang (GZJSYT). The AI results indicated that, among the 903 constituents detected in GZJSYT by LC-MS, 61 constituents with higher AI values were very likely to have anti-inflammatory activities. And eight potential active constituents of them were isolated and validated to have significant inhibitory effects against NO production on LPS-induced RAW 264.7 cell model. Among them, glycyrrhisoflavone (836), glisoflavanone (893) and isoangustone A (902) were reported to have anti-inflammatory effects for the first time. The proposed approach could be generally applicable for rapid and high efficient discovery of anti-inflammatory constituents from other TCM formulae or natural products. PMID:27499135

  3. Rapid discovery and identification of anti-inflammatory constituents from traditional Chinese medicine formula by activity index, LC-MS, and NMR.

    PubMed

    Wang, Shufang; Wang, Haiqiang; Liu, Yining; Wang, Yi; Fan, Xiaohui; Cheng, Yiyu

    2016-01-01

    The traditional activity-guided approach has the shortcoming of low accuracy and efficiency in discovering active compounds from TCM. In this work, an approach was developed by integrating activity index (AI), liquid chromatography - mass spectrometry (LC-MS), and nuclear magnetic resonance (NMR) to rapidly predict and identify the potential active constituents from TCM. This approach was used to discover and identify the anti-inflammatory constituents from a TCM formula, Gui-Zhi-Jia-Shao-Yao-Tang (GZJSYT). The AI results indicated that, among the 903 constituents detected in GZJSYT by LC-MS, 61 constituents with higher AI values were very likely to have anti-inflammatory activities. And eight potential active constituents of them were isolated and validated to have significant inhibitory effects against NO production on LPS-induced RAW 264.7 cell model. Among them, glycyrrhisoflavone (836), glisoflavanone (893) and isoangustone A (902) were reported to have anti-inflammatory effects for the first time. The proposed approach could be generally applicable for rapid and high efficient discovery of anti-inflammatory constituents from other TCM formulae or natural products. PMID:27499135

  4. DIFFERENTIAL GENE EXPRESSION PROFILES IN RAT TRACHAEL EPITHELIAL (RTE) CELLS IN RESPONSE TO COMBUSTION-SOURCE PARTICULATE MATTER (PM) AND VANADIUM (V) A PRIMARY METAL CONSTITUENT

    EPA Science Inventory

    Differential gene expression profiles in rat tracheal epithelial (RTE) cells in response to combustion-source particulate matter (PM) and vanadium (V) a primary metal constituent
    Srikanth S. Nadadur, Janice A. Dye and Daniel L. Costa, US EPA, ORD, NHEERL (ETD, Pulmonary Toxico...

  5. Antifungal Activity of Some Constituents of Origanum vulgare L. Essential Oil Against Postharvest Disease of Peach Fruit.

    PubMed

    Elshafie, Hazem S; Mancini, Emilia; Sakr, Shimaa; De Martino, Laura; Mattia, Carlo Andrea; De Feo, Vincenzo; Camele, Ippolito

    2015-08-01

    Plant essential oils (EOs) can potentially replace synthetic fungicides in the management of postharvest fruit and vegetable diseases. The aim of this study was to evaluate in vitro and in vivo effectiveness of thymol, carvacrol, linalool, and trans-caryophyllene, single constituents of the EO of Origanum vulgare L. ssp. hirtum against Monilinia laxa, M. fructigena, and M. fructicola, which are important phytopathogens and causal agents of brown rot of pome and stone fruits in pre- and postharvest. Moreover, the possible phytotoxic activity of these constituents was assessed and their minimum inhibitory concentration (MIC) was determined. In vitro experiment indicated that thymol and carvacrol possess the highest antifungal activity. Results of in vivo trials confirmed the strong efficacy of thymol and carvacrol against brown rot of peach fruits. The thymol MIC resulted to be 0.16 μg/μL against M. laxa and M. fructigena and 0.12 μg/μL against M. fructicola, whereas for carvacrol they were 0.02 μg/μL against the first two Monilinia species and 0.03 μg/μL against the third. Results of this study indicated that thymol and carvacrol could be used after suitable formulation for controlling postharvest fruit diseases caused by the three studied Monilinia species. PMID:25599273

  6. Essential oil constituents, phenolic content and antioxidant activity of Lavandula stricta Delile growing wild in southern Iran.

    PubMed

    Alizadeh, Ardalan; Aghaee, Zahra

    2016-10-01

    Lavandula stricta belongs to the Lamiaceae family and is considered as an endemic medicinal plant in southern Iran. Essential oil composition, total phenolic content and antioxidant activity from two different populations of L. stricta were studied for the first time. A GC and GC/MS analysis of essential oil isolated from the aerial part of L. stricta identified 31 constituents; the major constituents were α-pinene (58.34-63.52%), linalool (8.85-9.36%), 3-methyl butyl 2-methyl butanoate (7.45-7.70%), sabinene (2.84-3.56%), limonene (2.87-3.21%) and myrcene (2.25%). The total phenolic content of methanolic extracts was determined with the Folin-Ciocalteu reagent and the antioxidant activity of methanolic extract and essential oil were determined with the 2, 2-diphenyl-1-picryl hydrazyl free radical scavenging assay, respectively. Total phenols varied from 61.05 to 64.45 mg GAE/g dry weight, and IC50 values in the radical scavenging assay ranged from 334.11 to 395.23 μg/mL in methanolic extracts and 420-475 μg/mL in essential oil. PMID:26959122

  7. In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri

    PubMed Central

    Ramasamy, Seetha; Chin, Sek Peng; Sukumaran, Sri Devi; Buckle, Michael James Christopher; Kiew, Lik Voon; Chung, Lip Yong

    2015-01-01

    Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bacoside A, a mixture of dammarane-type triterpenoid saponins containing sugar chains linked to a steroid aglycone skeleton. Triterpenoid saponins have been reported to be transformed in vivo to metabolites that give better biological activity and pharmacokinetic characteristics. Thus, the activities of the parent compounds (bacosides), aglycones (jujubogenin and pseudojujubogenin) and their derivatives (ebelin lactone and bacogenin A1) were compared using a combination of in silico and in vitro screening methods. The compounds were docked into 5-HT1A, 5-HT2A, D1, D2, M1 receptors and acetylcholinesterase (AChE) using AutoDock and their central nervous system (CNS) drug-like properties were determined using Discovery Studio molecular properties and ADMET descriptors. The compounds were screened in vitro using radioligand receptor binding and AChE inhibition assays. In silico studies showed that the parent bacosides were not able to dock into the chosen CNS targets and had poor molecular properties as a CNS drug. In contrast, the aglycones and their derivatives showed better binding affinity and good CNS drug-like properties, were well absorbed through the intestines and had good blood brain barrier (BBB) penetration. Among the compounds tested in vitro, ebelin lactone showed binding affinity towards M1 (Ki = 0.45 μM) and 5-HT2A (4.21 μM) receptors. Bacoside A and bacopaside X (9.06 μM) showed binding affinity towards the D1 receptor. None of the compounds showed any inhibitory activity against AChE. Since the stimulation of M1 and 5-HT2A receptors has been implicated in memory and cognition and ebelin lactone was shown to have the strongest binding energy, highest BBB penetration and binding affinity towards M1 and 5-HT2A receptors, we suggest that B. monnieri constituents may be transformed in vivo to the

  8. In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri.

    PubMed

    Ramasamy, Seetha; Chin, Sek Peng; Sukumaran, Sri Devi; Buckle, Michael James Christopher; Kiew, Lik Voon; Chung, Lip Yong

    2015-01-01

    Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bacoside A, a mixture of dammarane-type triterpenoid saponins containing sugar chains linked to a steroid aglycone skeleton. Triterpenoid saponins have been reported to be transformed in vivo to metabolites that give better biological activity and pharmacokinetic characteristics. Thus, the activities of the parent compounds (bacosides), aglycones (jujubogenin and pseudojujubogenin) and their derivatives (ebelin lactone and bacogenin A1) were compared using a combination of in silico and in vitro screening methods. The compounds were docked into 5-HT1A, 5-HT2A, D1, D2, M1 receptors and acetylcholinesterase (AChE) using AutoDock and their central nervous system (CNS) drug-like properties were determined using Discovery Studio molecular properties and ADMET descriptors. The compounds were screened in vitro using radioligand receptor binding and AChE inhibition assays. In silico studies showed that the parent bacosides were not able to dock into the chosen CNS targets and had poor molecular properties as a CNS drug. In contrast, the aglycones and their derivatives showed better binding affinity and good CNS drug-like properties, were well absorbed through the intestines and had good blood brain barrier (BBB) penetration. Among the compounds tested in vitro, ebelin lactone showed binding affinity towards M1 (Ki = 0.45 μM) and 5-HT2A (4.21 μM) receptors. Bacoside A and bacopaside X (9.06 μM) showed binding affinity towards the D1 receptor. None of the compounds showed any inhibitory activity against AChE. Since the stimulation of M1 and 5-HT2A receptors has been implicated in memory and cognition and ebelin lactone was shown to have the strongest binding energy, highest BBB penetration and binding affinity towards M1 and 5-HT2A receptors, we suggest that B. monnieri constituents may be transformed in vivo to the

  9. Activation response of martensitic steels

    SciTech Connect

    Forty, C.B.A.

    1997-09-01

    A hypothetical martensitic steel has been compositionally designed in order to optimize both metallurgical and reduced activation properties. When compared with two other martensitic steels, its activation characteristics are shown to be superior for all activation indices examined. However, these excellent properties are found to be due to the assumed absence of deleterious tramp impurities. When limiting impurity concentrations are determined for the hypothetical steel, they are found to be extremely stringent, and wholly unachievable using industrial scale production methods. It is concluded that only slight improvements can be made to currently available low activation martensitic steels to reduce residual activity responses further. 26 refs., 1 fig., 2 tabs.

  10. Activation Response of Martensitic Steels

    NASA Astrophysics Data System (ADS)

    Forty, C. B. A.

    1997-09-01

    A hypothetical martensitic steel has been compositionally designed in order to optimize both metallurgical and reduced activation properties. When compared with two other martensitic steels, its activation characteristics are shown to be superior for all activation indices examined. However, these excellent properties are found to be due to the assumed absence of deleterious tramp impurities. When limiting impurity concentrations are determined for the hypothetical steel, they are found to be extremely stringent, and wholly unachievable using industrial scale production methods. It is concluded that only slight improvements can be made to currently available low activation martensitic steels to reduce residual activity responses further.

  11. Neural activation during response competition

    NASA Technical Reports Server (NTRS)

    Hazeltine, E.; Poldrack, R.; Gabrieli, J. D.

    2000-01-01

    The flanker task, introduced by Eriksen and Eriksen [Eriksen, B. A., & Eriksen, C. W. (1974). Effects of noise letters upon the identification of a target letter in a nonsearch task. Perception & Psychophysics, 16, 143--149], provides a means to selectively manipulate the presence or absence of response competition while keeping other task demands constant. We measured brain activity using functional magnetic resonance imaging (fMRI) during performance of the flanker task. In accordance with previous behavioral studies, trials in which the flanking stimuli indicated a different response than the central stimulus were performed significantly more slowly than trials in which all the stimuli indicated the same response. This reaction time effect was accompanied by increases in activity in four regions: the right ventrolateral prefrontal cortex, the supplementary motor area, the left superior parietal lobe, and the left anterior parietal cortex. The increases were not due to changes in stimulus complexity or the need to overcome previously learned associations between stimuli and responses. Correspondences between this study and other experiments manipulating response interference suggest that the frontal foci may be related to response inhibition processes whereas the posterior foci may be related to the activation of representations of the inappropriate responses.

  12. Antimycobacterial constituents from Juniperus procera, Ferula communis and Plumbago zeylanica and their in vitro synergistic activity with isonicotinic acid hydrazide.

    PubMed

    Mossa, Jaber S; El-Feraly, Farouk S; Muhammad, Ilias

    2004-11-01

    The synergistic activity of antimycobacterial constituents from Saudi plants was evaluated in combination with isonicotinic acid hydrazide (INH) against four atypical organisms, namely, Mycobacterium intracellulare, M. smegmatis, M. xenopei and M. chelonei. The potency of INH was increased four-fold, using an in vitro checkerboard method, against each mycobacteria when tested with a subtoxic concentration of the totarol, isolated from J. procera. The MIC values of totarol, ferulenol (from Ferula communis) and plumbagin (from Plumbago zeylanica) were thus lowered from 1.25-2.5 to 0.15-0.3 microg/mL due to synergism with INH. When tested against the resistant strain of M. tuberculosis H37Rv, plumbagin and 7beta-hydroxyabieta-8,13-dien-11,12-dione exhibited inhibitory activity at <12.5 microg/mL, while others were inactive at this concentration. PMID:15597311

  13. A Hybrid-Body Containing Constituents of Both P-Bodies and Stress Granules Forms in Response to Hypoosmotic Stress in Saccharomyces cerevisiae

    PubMed Central

    Shah, Khyati H.; Varia, Sapna N.; Cook, Laura A.; Herman, Paul K.

    2016-01-01

    The cytoplasm of the eukaryotic cell is a highly compartmentalized space that contains a variety of ribonucleoprotein (RNP) granules in addition to its complement of membrane-bound organelles. These RNP granules contain specific sets of proteins and mRNAs and form in response to particular environmental and developmental stimuli. Two of the better-characterized of these RNP structures are the stress granule and Processing-body (P-body) that have been conserved from yeast to humans. In this report, we examined the cues regulating stress granule assembly and the relationship between stress granule and P-body foci. These two RNP structures are generally thought to be independent entities in eukaryotic cells. However, we found here that stress granule and P-body proteins were localized to a common or merged granule specifically in response to a hypoosmotic stress. Interestingly, these hybrid-bodies were found to be transient structures that were resolved with time into separate P-body and stress granule foci. In all, these data suggest that the identity of an RNP granule is not absolute and that it can vary depending upon the nature of the induction conditions. Since the activities of a granule are likely influenced by its protein constituency, these observations are consistent with the possibility of RNP granules having distinct functions in different cellular contexts. PMID:27359124

  14. Volatile constituents and antioxidant activity of peel, flowers and leaf oils of Citrus aurantium L. growing in Greece.

    PubMed

    Sarrou, Eirini; Chatzopoulou, Paschalina; Dimassi-Theriou, Kortessa; Therios, Ioannis

    2013-01-01

    The volatile constituents of the essential oils of the peel, flower (neroli) and leaves (petitgrain) of bitter orange (Citrus aurantium L.) growing in Greece were studied by GC-MS. The analytical procedures enabled the quantitative determination of 31 components. More specifically, the components of the essential oils identified were: twelve in the peel, twenty-six in the flowers, and twenty and sixteen in old and young leaves, respectively. The major constituents of the different parts of Citrus aurantium L. essential oils were: β-pinene (0.62%-19.08%), limonene (0.53%-94.67%), trans-β-ocimene (3.11%-6.06%), linalool (0.76%-58.21%), and α-terpineol (0.13%-12.89%). The DPPH test demonstrated that the essential oils in the old leaves had the maximum antioxidant activity, followed by the flowers, young leaves and the peel in that order. This study updates the data in the literature on the essential oils of bitter orange, and provides information on the composition of the oils for a further evaluation of this product. PMID:24002139

  15. Anti-inflammatory activity of constituents isolated from Terminalia chebula ***waiting for publication date

    Technology Transfer Automated Retrieval System (TEKTRAN)

    This study was aimed at the evaluation of the anti-inflammatory activity of twelve compounds isolated from the methanolic extract of fruits of Terminalia chebula. The activity was determined in terms of their ability to inhibit inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in L...

  16. Antibacterial and Anti-Inflammatory Activities of Physalis Alkekengi var. franchetii and Its Main Constituents

    PubMed Central

    Shu, Zunpeng; Xing, Na; Wang, Qiuhong; Li, Xinli; Xu, Bingqing; Li, Zhenyu; Kuang, Haixue

    2016-01-01

    This study was designed to determine whether the 50% EtOH fraction from AB-8 macroporous resin fractionation of a 70% EtOH extract of P. Alkekengi (50-EFP) has antibacterial and/or anti-inflammatory activity both in vivo and in vitro and to investigate the mechanism of 50-EFP anti-inflammatory activity. Additionally, this study sought to define the chemical composition of 50-EFP. Results indicated that 50-EFP showed significant antibacterial activity in vitro and efficacy in vivo. Moreover, 50-EFP significantly reduced nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor alpha (TNF-α), interleukin 1 (IL-1), and interleukin 6 (IL-6) production in lipopolysaccharide- (LPS-) stimulated THP-1 cells. Nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) (examined at the protein level) in THP-1 cells were suppressed by 50-EFP, which inhibited nuclear translocation of p65. Consistent with this anti-inflammatory activity in vitro, 50-EFP reduced inflammation in both animal models. Finally, seventeen compounds (8 physalins and 9 flavones) were isolated as major components of 50-EFP. Our data demonstrate that 50-EFP has antibacterial and anti-inflammatory activities both in vitro and in vivo. The anti-inflammatory effect appears to occur, at least in part, through the inhibition of nuclear translocation of p65. Moreover, physalins and flavones are probably the active components in 50-EFP that exert antibacterial and anti-inflammatory activities. PMID:27057196

  17. Anti-complementary constituents of Houttuynia cordata and their targets in complement activation cascade.

    PubMed

    Jiang, Yun; Lu, Yan; Zhang, Yun-Yi; Chen, Dao-Feng

    2014-01-01

    Activity-guided fractionation for complement inhibitors led to the isolation of 23 known compounds from Houttuynia cordata Thunb. Seven flavonoids, two alkaloids, one coumarin and two phenols showed anti-complementary activity. Preliminary inhibitory mechanism of four flavonoids, including quercitrin, afzelin, isoquercitrin and quercetin in the complement activation cascade were examined for the first time. The results indicated that the target components of flavonols are different from those of flavonosides, and the glycoside moieties may be necessary to block C3 and C4 components. PMID:24423008

  18. Immunomodulatory activities of medicinal mushroom Grifola frondosa extract and its bioactive constituent.

    PubMed

    Wu, Shu-Jing; Lu, Tzy-Ming; Lai, Min-Nan; Ng, Lean-Teik

    2013-01-01

    Grifola frondosa (GF), a high value medicinal mushroom in China and Japan, is popularly consumed as traditional medicines and health foods, especially for enhancing immune functions. In this study, our aim was to examine the immunomodulatory activities of GF and its bioactive compound ergosterol peroxide (EPO) in lipopolysaccharide (LPS)-induced human monocytic (THP-1) cells. At low concentrations, EPO but not other extracts showed a full protection against LPS-induced cell toxicity. EPO significantly blocked MyD88 and VCAM-1 expression, and cytokine (IL-1β, IL-6 and TNF-α) production in LPS-stimulated cells. It also effectively inhibited NF-κB activation, which was further confirmed with siRNA treatment. These results conclude that EPO may play an important role in the immunomodulatory activity of GF through inhibiting the production of pro-inflammatory mediators and activation of NF-κB signaling pathway. PMID:23336512

  19. Analgesic, anti-inflammatory, and CNS depressant activities of new constituents of Nepeta clarkei.

    PubMed

    Hussain, Javid; Ur Rehman, Najeeb; Hussain, Hidayat; Al-Harrasi, Ahmed; Ali, Liaqat; Rizvi, Tania Shamim; Ahmad, Mansoor; Mehjabeen

    2012-04-01

    Two new pentacyclic triterpenes named kirmanoic acid (1) and kurramanoic acid (2) have been isolated from the chloroform-soluble portion of the whole plant of Nepeta clarkei Hook. The structures of the two new compounds were assigned on the basis of their ¹H and ¹³C NMR spectra including two-dimensional NMR techniques such as COSY, HMQC, and HMBC experiments. Kirmanoic acid (1) was investigated for analgesic, anti-inflammatory, and CNS depressant activities. Interestingly kirmanoic acid (1) showed strong analgesic activity than standard drug in acetic induced writhing and formalin tests. Similarly kirmanoic acid (1) also showed strong anti-inflammatory activity than its standard drug. The gross behavioral study of kirmanoic acid (1) revealed that it exhibited mild CNS stimulant and muscle relaxant in the mice. Compound 1 showed a slight increase in Locomotor activity and possesses the antidepressant effect. PMID:22266390

  20. Internal browning disorder of eight pear cultivars affected by bioactive constituents and enzyme activity.

    PubMed

    Koushesh Saba, Mahmoud; Moradi, Samira

    2016-08-15

    Internal browning (IB) is a disorder in pears that is frequently observed in some cultivars. The present research was carried out to study biochemical changes and IB disorder of pear fruit during storage and ripening. Eight pear cultivars harvested and stored at 1°C up to 90 days. IB incidence, some bioactive compounds, polyphenol oxidase (PPO), peroxidase (POX), and superoxide dismutase (SOD) enzymes activities were measured during storage. IB increased during storage time but the susceptibility of cultivars was different. The ascorbic acid (AA), antioxidant capacity (AC) and SOD activity decreased while POX activity increased during storage but the rate of changes were different in studied cultivars. Total phenol (TP) and total flavonoid (TF) average content varied among pear cultivars and the highest TP and TF were observed in 'Bakhi' cultivars during storage. Fruit IB had positive correlation with the PPO activity, but negative correlation with TP, AC and AA. PMID:27006238

  1. Phenolic constituents from the heartwood of Artocapus altilis and their tyrosinase inhibitory activity.

    PubMed

    Nguyen, Mai Ha Khoa; Nguyen, Hai Xuan; Nguyen, Mai Thanh Thi; Nguyen, Nhan Trung

    2012-02-01

    From the MeOH extract of the heartwood of Artocapus altilis, thirteen phenolic compounds have been isolated, namely curcumin (1), desmethoxycurcumin (2), retrodihydrochalcone (3), apigenin (4), tangeretin (5), nobiletin (6), O-methyldehydrodieugenol (7), dehydrodieugenol (8), beta-hydroxypropiovanillone (9), p-coumaric acid (10), p-hydroxybenzaldehyde (11), vanillin (12), and vanillic acid (13). This is the first report on the presence of these compounds in the heartwood of A. altilis. Compounds 1, 2, and 10 showed more potent tyrosinase inhibitory activities, with IC50 values ranging from 2.3 to 42.0 microM, than the positive control kojic acid (IC50, 44.6 microM). The most active compound, p-coumaric acid (10) (IC50, 2.3 microM), was 22 times more active in tyrosinase inhibitory activity than kojic acid. PMID:22474950

  2. Chemical constituents and insecticidal activities of the essential oil from Amomum tsaoko against two stored-product insects.

    PubMed

    Wang, Ying; You, Chun-Xue; Wang, Cheng-Fang; Yang, Kai; Chen, Ran; Zhang, Wen-Juan; Du, Shu-Shan; Geng, Zhu-Feng; Deng, Zhi-Wei

    2014-01-01

    The aim of this research was to determine the chemical constituents and toxicities of the essential oil derived from Amomum tsaoko Crevost et Lemarie fruits against Tribolium castaneum (Herbst) and Lasioderma serricorne (Fabricius). Essential oil of A. tsaoko was obtained from hydrodistillation and was investigated by gas chromatography-mass spectrometry (GC-MS). GC-MS analysis of the essential oil resulted in the identification of 43 components, of which eucalyptol (23.87%), limonene (22.77%), 2-isopropyltoluene (6.66%) and undecane (5.74%) were the major components. With a further isolation, two active constituents were obtained from the essential oil and identified as eucalyptol and limonene. The essential oil and the two isolated compounds exhibited potential insecticidal activities against two storedproduct insects. Limonene showed pronounced contact toxicity against both insect species (LD50 = 14.97 μg/adult for T. castaneum; 13.66 μg/adult for L. serricorne) and was more toxic than eucalyptol (LD50 = 18.83 μg/adult for T. castaneum; 15.58 μg/adult for L. serricorne). The essential oil acting against the two species of insects showed LD50 values of 16.52 and 6.14 μg/adult, respectively. Eucalyptol also possessed strong fumigant toxicity against both insect species (LC50 = 5.47 mg/L air for T. castaneum; 5.18 mg/L air for L. serricorne) and was more toxic than limonene (LC50 = 6.21 mg/L air for T. castaneum; 14.07 mg/L air for L. serricorne), while the crude essential oil acting against the two species of insects showed LC50 values of 5.85 and 8.70 mg/L air, respectively. These results suggested that the essential oil of A. tsaoko and the two compounds may be used in grain storage to combat insect pests. PMID:25213443

  3. Characterization of the Phytochemical Constituents of Taif Rose and Its Antioxidant and Anticancer Activities

    PubMed Central

    Abdel-Hameed, El-Sayed S.; Bazaid, Salih A.; Salman, Mahmood S.

    2013-01-01

    Ward Taifi (Taif rose) is considered one of the most important economic products of Taif, Saudi Arabia. In this study both fresh and dry Taif rose were biologically and phytochemically investigated. The 80% methanol extracts and n-butanol fractions of dry and fresh Taif rose had high radical scavenging activity toward artificial 1,1-diphenyl picrylhydrazyl (DPPH)• radical with SC50 values range 5.86−12.24 µg/ml whereas the aqueous fractions showed weak activity. All samples had in vitro anticancer activity toward HepG2 with IC50 < 20 µg/ml which fall within the criteria of the American Cancer Institute. High positive correlation appeared between the antioxidant activity and total phenolics whereas there is no correlation between total phenolics and anticancer activity. The LC-ESI(− ve)-MS analysis of all extracts indicate the presence of phenolic compounds belonging to hydrolysable tannins and flavonol glycosides. In conclusion, the presence of this is considered to be the first phytochemical report that identifies the major compounds in dry and fresh roses using HPLC-ESI-MS. The methanol extracts and its n-butanol and aqueous fractions for both fresh and dry Taif rose could be used as preventive and therapeutic effective natural agents for diseases in which free radicals involved after more in vitro and in vivo studies. PMID:24282813

  4. Chemical constituents and biological activities of Senecio aegyptius var. discoideus Boiss.

    PubMed

    Hassan, Wafaa; Al-Gendy, Amal; Al-Youssef, Hanan; El-Shazely, Assem

    2012-01-01

    A new eremophilane sesquiterpene, 1-beta-hydroxy-8-oxoeremophila-7,9-dien-12-oic acid (1), in addition to two known flavonol glycosides, rutin (2) and quercetin-3-O-glucoside-7-O-rutinoside (3), was isolated from the ethyl acetate fraction obtained from the aqueous alcoholic extract of the aerial parts of Senecio aegyptius var. discoideus Boiss. (family Asteraceae). The chemical structures of the isolated compounds were established by 1D and 2D NMR analysis (1H, 13C, COSY, HMQC, HMBC), MS and UV data, and through comparison with the literature. The ethyl acetate fraction and the isolated rutin showed significant cytotoxic activity against colorectal carcinoma (HCT 116) and to less extent against brain (U 251) and breast carcinoma (MCF 7). The ethyl acetate fraction showed a significant level of activity against Klebsiella pneumoniae, while the total extract showed the best antifungal activity against Candida albicans and Saccharomyces cerevisiae. DPPH radical scavenging activity of the ethyl acetate fraction was significant (96.7%) when compared to ascorbic acid. It also showed anti-inflammatory activity but no diuretic effect. PMID:22624330

  5. A peroxisome proliferator-activated receptor-gamma agonist and other constituents from Chromolaena odorata.

    PubMed

    Dat, Nguyen Tien; Lee, Kyeong; Hong, Young-Soo; Kim, Young Ho; Minh, Chau Van; Lee, Jung Joon

    2009-06-01

    Peroxisome proliferator-activated receptors (PPARs) are key regulators of lipid and glucose metabolism and have become important therapeutic targets for various diseases. The phytochemical investigation of the chloroform-soluble extract of Chromolaena odorata led to the isolation of a PPAR-gamma agonist, (9 S,13 R)-12-oxo-phytodienoic acid (1), together with 12 other compounds. The structures of chromomoric acid G (2), a new dehydrogenated derivative of 1, and chromolanone (3) were elucidated based on spectroscopic methods. Compound 1 showed a significant effect on PPAR-gamma activation in comparison with rosiglitazone. However, compound 2 was inactive, suggesting that the dehydrogenation of the prostaglandin-like structure in 1 abrogates its PPAR-gamma agonistic activity. PMID:19242902

  6. Antitrypanosomal activity & docking studies of isolated constituents from the lichen Cetraria islandica: possibly multifunctional scaffolds.

    PubMed

    Igoli, John Ogbaji; Gray, Alexander Irvine; Clements, Carol Jean; Kantheti, Poorna; Singla, Rajeev Kumar

    2014-01-01

    Chemical investigation of the lichen Cetraria islandica has led to the isolation of four compounds identified as protolichesterinic acid, lichesterinic acid, protocetraric acid and fumarprotocetraric acid. Their structures were characterized using their physical and spectroscopic data. Using an Alamarblue™ 96 well microplate assay, these compounds were tested to evaluate their trypanocidal activity against Trypanosoma brucei brucei. Protolichesterinic acid (MIC = 6.30 µM) and lichesterinic acid (MIC = 12.5 µM) showed very significant activity against the test organism. Docking studies (GRIP technique) of these molecules revealed their strong affinity towards possible targets of Trypanosoma brucei such as riboflavin kinase, sterol-14α-demethylase (CYP51), rohedsain and glutathione synthetase. Hydrophobicity played a significant role in their antitrypanosomal activity. PMID:24660683

  7. Polysaccharide Constituents of Three Types of Sea Urchin Shells and Their Anti-Inflammatory Activities

    PubMed Central

    Jiao, Heng; Shang, Xiaohui; Dong, Qi; Wang, Shuang; Liu, Xiaoyu; Zheng, Heng; Lu, Xiaoling

    2015-01-01

    As a source of potent anti-inflammatory traditional medicines, the quantitative chromatographic fingerprints of sea urchin shell polysaccharides were well established via pre-column derivatization high performance liquid chromatography (HPLC) analysis. Based on the quantitative results, the content of fucose and glucose could be used as preliminary distinguishing indicators among three sea urchin shell species. Besides, the anti-inflammatory activities of the polysaccharides from sea urchin shells and their gonads were also determined. The gonad polysaccharide of Anthocidaris crassispina showed the most potent anti-inflammatory activity among all samples tested. PMID:26389925

  8. Phytochemical screening and antimicrobial activities of the constituents isolated from Koelreuteria paniculata leaves.

    PubMed

    Ghahari, Somayeh; Alinezhad, Heshmatollah; Nematzadeh, Ghorban Ali; Ghahari, Sajjad

    2015-01-01

    Methanolic extract of Golden rain leaves was fractionated by column chromatography on silica gel and 18 fractions were obtained. Antimicrobial activities of fractions were investigated against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa as quality control bacteria and fungus Pyricularia grisea which causes Blast disease in rice. Fractions showed more antibacterial activity at 0.04 g/mL concentration only on B. subtilis and S. aureus as gram positive bacteria. Also, three fractions indicated excellent antifungal effect on fungus P. grisea. Moreover, in the present study, fractions that showed very good effect on microorganisms were used for gas chromatography-mass spectrometry analysis to identify different phytochemicals. PMID:25813082

  9. Evaluation of biological activities of Alpinia mutica Roxb. and its chemical constituents.

    PubMed

    Mustahil, Noorul Adawiyah; Sukari, Mohd Aspollah; Abdul, Ahmad Bustamam; Ali, Nor Azah; Lian, Gwendoline Ee-Cheng

    2013-03-01

    Phytochemicals investigation on rhizomes of Alpinia mutica has afforded five compounds namely 5,6-dehydrokawain (1), flavokawin B (2), pinostrobin (3) and pinocembrin (4) together with β-sitosterol (5). All crude extracts of the plant demonstrated strong cytotoxicity against CEMss (human T4 lymphoblastoid) cancer cells with IC50 values less than 19 μg/mL, while flavokawin B (2) was the most cytotoxic isolate with IC50 value 1.86±0.37 μg/mL. Most of the crude extracts and isolated compounds showed weak activity in antimicrobial and diphenylpicrylhydrazyl (DPPH) radical scavenging activity tests. PMID:23455212

  10. Ethnobotany, chemical constituents and biological activities of the flowers of Hydnora abyssinica A.Br. (Hydnoraceae).

    PubMed

    Al-Fatimi, M; Ali, N A A; Kilian, N; Franke, K; Arnold, N; Kuhnt, C; Schmidt, J; Lindequist, U

    2016-04-01

    Hydnora abyssinica A.Br. (Hydnoraceae), a holoparasitic herb, is for the first time recorded for Abyan governorate of South Yemen. Flowers of this species were studied for their ethnobotanical, biological and chemical properties for the first time. In South Yemen, they are traditionally used as wild food and to cure stomach diseases, gastric ulcer and cancer. Phytochemical analysis of the extracts showed the presence of terpenes, tannins, phenols, and flavonoids. The volatile components of the air-dried powdered flowers were identified using a static headspace GC/MS analysis as acetic acid, ethyl acetate, sabinene, α-terpinene, (+)-D-limonene and γ-terpinene. These volatile compounds that characterize the odor and taste of the flowers were detected for the first time in a species of the family Hydnoraceae. The flowers were extracted by n-hexane, dichlormethane, ethyl acetate, ethanol, methanol and water. With exception of the water extract all extracts demonstrated activities against Gram-positive bacteria as well as remarkable radical scavenging activities in DPPH assay. Ethyl acetate, methanol and water extracts exhibited good antifungal activities. The cytotoxic activity of the extracts against FL cells, measured in neutral red assay, was only weak (IC50 > 500 μg/mL). The results justify the traditional use of the flowers of Hydnora abyssinica in South Yemen. PMID:27209704

  11. Differential cytotoxic activity of the petroleum ether extract and its furanosesquiterpenoid constituents from Commiphora molmol resin.

    PubMed

    Ayyad, Seif-Eldin N; Hoye, Thomas R; Alarif, Walied M; Al Ahmadi, Sana'a M; Basaif, Salim A; Ghandourah, Mohamed A; Badria, Farid A

    2015-01-01

    This study revealed a differential cytotoxic activity of the petroleum ether extract (IC₅₀ =5 μg/mL) of the resinous exudates of Commiphora molmol against two mouse cell lines KA31T and NIH3T3 (untransformed and transformed mouse fibroblasts, respectively). Four new compounds (1-4) and five known compounds (5-9) were isolated from the petroleum ether extract. The identity of these new compounds was determined as γ-elemane lactone (1), 5-αH,8-βH-eudesma-1,3,7(11)-trien-8,12-olide (2), 2-hydroxy-11,12-dihydrofuranodiene (3), and 2-hydroxyfuranodiene (4). 1 and 2 displayed the highest cytotoxic activity against NIH3T3 cells. 7 and 9 exhibited moderate cytotoxic activity against KA31T cells. Compounds 3-6 showed weak cytotoxic activities against both cell lines. These results may explain the high efficacy of the petroleum ether fraction in several myrrh-derived pharmaceutical preparations. PMID:26020558

  12. Biological activities and volatile constituents of Daucus muricatus L. from Algeria

    PubMed Central

    2012-01-01

    Background In order to find new bioactive natural products, the antimicrobial and antioxidant activities of essential oil components extracted from the separated organs of the Algerian medicinal and aromatic plant Daucus muricatus L. were studied. Results The chemical composition of essential oils obtained by hydrodistillation (HD) was investigated using Gas Chromatography–Retention Indices (GC-RI) and GC–Mass Spectrometry (GC-MS). Two types of essential oils were produced by D. muricatus: (i) The oil from roots is mainly composed by nonterpenic oxygenated compounds (59.8 g/100 g), and (ii) the aerial part oils (i.e., the leaves, stems, flowers, and umbels) was mainly composed by terpenic hydrocarbon compounds (62.3–72.2 g/100 g). The chemical composition of the volatile fraction isolated from different organs of Daucus muricatus were studied by HS–SPME/GC–RI and GC–MS after optimization of Solid Phase MicroExtraction parameters. For all organs studied, the main volatiles emitted by the plant were hydrocarbon compounds (60.7–82.2 g/100 g). Only quantitative differences between the volatiles of the separated organs studied were observed. In addition, the activity of the oil of D. muricatus against eight bacterial strains and one yeast was investigated. The oil from roots revealed active against S. aureus, while the essential oil obtained from the aerial parts was active against the yeast C. albicans. Conclusions Daucus muricatus essential oil seems be a promising source of natural products with potential antimicrobial activity. PMID:22647252

  13. Protective Effects of Rosa damascena and Its Active Constituent on Aβ(25-35)-Induced Neuritic Atrophy.

    PubMed

    Awale, Suresh; Tohda, Chihiro; Tezuka, Yasuhiro; Miyazaki, Makoto; Kadota, Shigetoshi

    2011-01-01

    Dementia is a clinical syndrome characterized by multiple cognitive deficits and causes progressive neurodegeneration leading eventually to death. The incidence of dementia is increasing worldwide with the increase in ageing population. However, no effective treatment is available yet. It has been hypothesized that drugs activating neurite outgrowth might induce neuronal reconstruction and help in the recovery of brain function. Working on this hypothesis, we recently observed that the chloroform extract of the Rosa damascena significantly induced the neurite outgrowth activity and inhibited the Aβ(25-35)-induced atrophy and cell death. Further workup led the isolation of a very long polyunsaturated fatty acid having molecular formula C(37)H(64)O(2) as an active constituent. The structure of this compound was established by extensive analysis of fragmentations observed in EI-MS mode. The isolated compound protected Aβ(25-35)-induced atrophy and displayed strong neurite outgrowth activity. The length of dendrite in the cells treated with this compound were comparable to those of nerve growth factor (NGF) treated cells. PMID:19789212

  14. Antitumor Activity of Kielmeyera Coriacea Leaf Constituents in Experimental Melanoma, Tested in Vitro and in Vivo in Syngeneic Mice

    PubMed Central

    Figueiredo, Carlos Rogério; Matsuo, Alisson Leonardo; Massaoka, Mariana Hiromi; Girola, Natalia; Azevedo, Ricardo Alexandre; Rabaça, Aline Nogueira; Farias, Camyla Fernandes; Pereira, Felipe Valença; Matias, Natalia Silva; Silva, Luciana Pereira; Rodrigues, Elaine Guadelupe; Lago, João Henrique Guilardi; Travassos, Luiz Rodolpho; Silva, Regildo Márcio Gonçalves

    2014-01-01

    Purpose: The antitumor activity of Kielmeyera coriacea (Clusiaceae), a medicinal plant used in the treatment of parasitic, as well as fungal and bacterial infections by the Brazilian Cerrado population, was investigated. Methods: A chloroform extract (CE) of K. coriacea was tested in the murine melanoma cell line (B16F10-Nex2) and a panel of human tumor cell lines. Tumor cell migration was determined by the wound-healing assay and the in vivo antitumor activity of CE was investigated in a melanoma cell metastatic model. 1H NMR and GC/MS were used to determine CE chemical composition. Results: We found that CE exhibited strong cytotoxic activity against murine melanoma cells and a panel of human tumor cell lines in vitro. CE also inhibited growth of B16F10-Nex2 cells at sub lethal concentrations, inducing cell cycle arrest at S phase, and inhibition of tumor cell migration. Most importantly, administration of CE significantly reduced the number of melanoma metastatic nodules in vivo. Chemical analysis of CE indicated the presence of the long chain fatty compounds, 1-eicosanol, 1-docosanol, and 2-nonadecanone as main constituents. Conclusion: These results indicate that K. coriacea is a promising medicinal plant in cancer therapy exhibiting antitumor activity both in vitro and in vivo against different tumor cell lines. PMID:25364658

  15. Phytochemical constituents and antioxidant activities of the whole leaf extract of Aloe ferox Mill

    PubMed Central

    Wintola, Olubunmi Abosebe; Afolayan, Anthony Jide

    2011-01-01

    Background: Aloe ferox Mill. (Asphodelaceae) is used in South Africa for the treatment of constipation among various ailments. Despite the extensive studies conducted on the antioxidant activities of the leaf gel and pulp extract of the plant, there is no information on the antioxidant properties of the whole leaf extract of the species. Materials and Methods: The antioxidant activities of ethanol, acetone, methanol and aqueous extracts of A. ferox were investigated spectrophotometrically against 1,1- diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) diammonium salt, hydrogen peroxide (H2O2), nitric oxide (NO), lipid peroxidation and ferric reducing power. Total phenols, flavonoids, flavonols, proanthocyanidins, tannins, alkaloids and saponins were also determined using the standard methods. Results: The percentage compositions of phenols (70.33), flavonols (35.2), proanthocyanidins (171.06) and alkaloids (60.9) were significantly high in the acetone extract, followed by the ethanol extract with values of 70.24, 12.53, 76.7 and 23.76 respectively, while the least composition was found in the aqueous extract. Moreover, both flavonoids and saponins contents were appreciably high in both methanol and ethanol extracts, while others were very low. Tannins levels were, however, not significantly different (P > 0.05) in all the solvent extracts. At 0.5 mg/ml, the free radical scavenging activity of the methanol, acetone and ethanol extracts showed higher inhibition against ABTS, hydrogen peroxide and nitric oxide radicals. Whereas, scavenging activity of the extracts against DPPH* and lipid peroxidation were observed at a concentration of 0.016 and 0.118 mg/ml respectively in comparison to the butylated hydroxyltoluene (BHT), gallic acid and rutin. The ferric reducing potential of the extracts was concentration dependent and significantly different from that of vitamin C and BHT. Conclusion: The present study showed high

  16. Volatile Constituents of the Leaves of Aniba hostmanniana (Lauraceae) and their Antibacterial Activities.

    PubMed

    De Lima, Wilberto; Rojas-Fermín, Luis B; Koteich-Khatib, Sonia; Lucena, María Eugenia; Arzolad, Juan Carmona

    2015-07-01

    The essential oil of Aniba hostmanniana (Nees) Mez, family Lauraceae, was obtained from fresh leaves by hydrodistillation. The chemical composition of the oil was assessed using gas chromatography with mass spectrometric detection (GC-MS). The antimicrobial activity of the essential oil was tested against Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia) and the Gram-positive bacterium Staphylococcus aureus. GC-MS analysis revealed the presence of 35 compounds in the essential oil, the predominant ones being benzyl benzoate (29.3%), Δ-cadinene (12%), β-caryophyllene (10.5%), bicyclogermacrene (5.9%), and α-copaene (3.9%). The oil showed activity against most of the bacterial strains studied. PMID:26411041

  17. Chemical constituents of Narcissus tazetta var. chinensis and their antioxidant activities.

    PubMed

    Fu, Ka-Li; Li, Xian; Ye, Ji; Lu, Lu; Xu, Xi-Ke; Li, Hui-Liang; Zhang, Wei-Dong; Shen, Yun-Heng

    2016-09-01

    Two new flavan derivatives tazettones C-D (1-2), one new β-coumaranone (tazettone E, 3), one new flavan (tazettone F, 4), and one new phenylpropanoid (tazettone G, 5), together with six known flavonoids (6-11), were isolated from the bulbs of Narcissus tazetta var. chinensis Roem. Their structures were elucidated by spectroscopic analysis. In addition, the structures of 1-3 were confirmed by single crystal X-ray diffraction. All isolated compounds were tested for antioxidant activity by Cell Counting Kit-8 (CCK-8) assay. Compounds 6-8 and 10-11 exhibited potent antioxidant activity against H2O2-induced impairment in human SH-SY5Y neuroblastoma cells at tested concentrations. PMID:27476617

  18. Traditional Uses, Chemical Constituents, and Biological Activities of Bixa orellana L.: A Review

    PubMed Central

    Vilar, Daniela de Araújo; Vilar, Marina Suênia de Araujo; Moura, Túlio Flávio Accioly de Lima e; Raffin, Fernanda Nervo; de Oliveira, Márcia Rosa; Franco, Camilo Flamarion de Oliveira; de Athayde-Filho, Petrônio Filgueiras; Diniz, Margareth de Fátima Formiga Melo; Barbosa-Filho, José Maria

    2014-01-01

    Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent. PMID:25050404

  19. Chemical Constituents of the Rhizomes of Bletilla formosana and Their Potential Anti-inflammatory Activity.

    PubMed

    Lin, Che-Wei; Hwang, Tsong-Long; Chen, Fu-An; Huang, Chia-Hsin; Hung, Hsin-Yi; Wu, Tian-Shung

    2016-08-26

    Nine new phenanthrenes (1-9) and a new benzyl glycoside (10) together with 45 known compounds were isolated from the rhizomes of Bletilla formosana. The structures of 1-10 were elucidated primarily on the basis of their 1D and 2D NMR spectroscopic data. Most of the isolated compounds were evaluated for their anti-inflammatory activities. The results showed that IC50 values for the inhibition of superoxide anion generation and elastase release ranged from 0.2 to 6.5 μM and 0.3 to 5.7 μM, respectively. Structure-activity relationships of the isolated compounds were also investigated. The inhibitory potencies were determined as phenanthrenes > bibenzyls > biphenanthrenes. PMID:27525452

  20. Chemical Constituents of the Underground Parts of Iris florentina and their Cytotoxic Activity.

    PubMed

    Yokosuka, Akihito; Koyama, Yoshikazu; Mimaki, Yoshihiro

    2015-06-01

    Three new isoflavonoid glycosides (1, 5, and 9) and 10 known compounds (2-4, 6-8, and 10-13) were isolated from the underground parts of Iris florentina (Iridaceae). The structures of the new compounds were determined based on extensive spectroscopic data and the results of hydrolytic cleavage. The isolated compounds and the aglycones were evaluated for cytotoxic activity against HL-60 human promyelocytic leukemia cells. Compound 12 induced apoptotic cell death in the HL-60 cells. PMID:26197526

  1. Borreria and Spermacoce species (Rubiaceae): A review of their ethnomedicinal properties, chemical constituents, and biological activities

    PubMed Central

    Conserva, Lucia Maria; Ferreira, Jesu Costa

    2012-01-01

    Borreira and Spermacoce are genera of Rubiaceae widespread in tropical and subtropical America, Africa, Asia, and Europe. Based on its fruits morphology they are considered by many authors to be distinct genera and most others, however, prefer to combine the two taxa under the generic name Spermacoce. Whereas the discussion is still unclear, in this work they were considered as synonyms. Some species of these genera play an important role in traditional medicine in Africa, Asia, Europe, and South America. Some of these uses include the treatment of malaria, diarrheal and other digestive problems, skin diseases, fever, hemorrhage, urinary and respiratory infections, headache, inflammation of eye, and gums. To date, more than 60 compounds have been reported from Borreria and Spermacoce species including alkaloids, iridoids, flavonoids, terpenoids, and other compounds. Studies have confirmed that extracts from Borreria and Spermacoce species as well as their isolated compounds possess diverse biological activities, including anti-inflammatory, antitumor, antimicrobial, larvicidal, antioxidant, gastrointestinal, anti-ulcer, and hepatoprotective, with alkaloids and iridoids as the major active principles. This paper briefly reviews the ethnomedicinal uses, phytochemistry, and biological activities of some isolated compounds and extracts of both genera. PMID:22654404

  2. Comparison of the concentrations of phenolic constituents in cane sugar manufacturing products with their antioxidant activities.

    PubMed

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

    2006-09-20

    Polyphenol content and free radical scavenging capacity of seven kinds of sugar manufacturing products (A sugars, clear juices, syrups, massecuite, and A, B, and C molasses) were studied. Seventy-two samples were collected at different stages of the process during two sugar harvests from a local sugar factory (Bois-Rouge, La Réunion). The total phenolic content of sugar products was determined according to the Folin-Ciocalteu assay. Polyphenols of sugar products were extracted with ethyl acetate and quantified by LC-UV-ESI-MS during all of the process. ABTS and DPPH assays were applied to aqueous solution of sugar products, which exhibited interesting free radical scavenging activity. Comparatively, ethyl acetate extracts exhibited higher antioxidant activity. Multivariate analyses (principal component analysis and canonical discriminant analysis) demonstrated a significant correlation between polyphenols and antioxidant activity. Moreover, it was observed that the sugar process results in an increase of the phenolic content and the free radical scavenging capacity of the different products. These products and especially molasses proved to be a rich source of natural antioxidants and may represent an interesting alternative to synthetic food antioxidants. PMID:16968093

  3. Chemical Constituents Analysis and Antidiabetic Activity Validation of Four Fern Species from Taiwan

    PubMed Central

    Chen, Chen-Yu; Chiu, Fu-Yu; Lin, Yenshou; Huang, Wei-Jan; Hsieh, Po-Shiuan; Hsu, Feng-Lin

    2015-01-01

    Pterosins are abundant in ferns, and pterosin A was considered a novel activator of adenosine monophosphate-activated protein kinase, which is crucial for regulating blood glucose homeostasis. However, the distribution of pterosins in different species of ferns from various places in Taiwan is currently unclear. To address this question, the distribution of pterosins, glucose-uptake efficiency, and protective effects of pterosin A on β-cells were examined. Our results showed that three novel compounds, 13-chloro-spelosin 3-O-β-d-glucopyranoside (1), (3R)-Pterosin D 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (2), and (2R,3R)-Pterosin L 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (3), were isolated for the first time from four fern species (Ceratopteris thalictroides, Hypolepis punctata, Nephrolepis multiflora, and Pteridium revolutum) along with 27 known compounds. We also examined the distribution of these pterosin compounds in the mentioned fern species (except N. multiflora). Although all pterosin analogs exhibited the same effects in glucose uptake assays, pterosin A prevented cell death and reduced reactive oxygen species (ROS) production. This paper is the first report to provide new insights into the distribution of pterosins in ferns from Taiwan. The potential anti-diabetic activity of these novel phytocompounds warrants further functional studies. PMID:25622260

  4. Impact of Wines and Wine Constituents on Cyclooxygenase-1, Cyclooxygenase-2, and 5-Lipoxygenase Catalytic Activity

    PubMed Central

    Temml, Veronika; Maghradze, David; Vanek, Tomas

    2014-01-01

    Cyclooxygenases and lipoxygenases are proinflammatory enzymes; the former affects platelet aggregation, vasoconstriction, vasodilatation and later the development of atherosclerosis. Red wines from Georgia and central and western Europe inhibited cyclooxygenase-1 (COX-1) activity in the range of 63–94%, cyclooxygenase-2 (COX-2) activity in the range of 20–44% (tested at a concentration of 5 mL/L), and 5-lipoxygenase (5-LOX) activity in the range of 72–84% (at a concentration of 18.87 mL/L). White wines inhibited 5-LOX in the range of 41–68% at a concentration of 18.87 mL/L and did not inhibit COX-1 and COX-2. Piceatannol (IC50 = 0.76 μM) was identified as a strong inhibitor of 5-LOX followed by luteolin (IC50 = 2.25 μM), quercetin (IC50 = 3.29 μM), and myricetin (IC50 = 4.02 μM). trans-Resveratrol was identified as an inhibitor of COX-1 (IC50 = 2.27 μM) and COX-2 (IC50 = 3.40 μM). Red wine as a complex mixture is a powerful inhibitor of COX-1, COX-2, and 5-LOX, the enzymes involved in eicosanoid biosynthetic pathway. PMID:24976682

  5. Antimicrobial action of an endophytic fungi from Sophor flavescens and structure identification of its active constituent

    PubMed Central

    Yu, Na; He, Lu; Liu, Na; Wang, Yong; Xu, Hongbo; Liu, Dandan

    2014-01-01

    Endophytic fungus BS002 was isolated and characterized from Sophora flavescens by plate method, which has broad antimicrobial activity. Isolation and trace of a new bioactive compound from the fungus’ culture extracts with the method of column chromatography and TLC biological autoradiography was conducted. Finally, it was identified as 6,7-(2′E) dibutenyl-5,8-dihydroxy-(Z)-cyclooct-2-ene-1,4-dione by nuclear magnetic resonance, infrared and liquid chromatography–mass spectrometry. The compound presented strong antifungal activities for example: Botryosphaeria berengriana f.sp. piricola, Physalospora piricola, Cladosporium cucumerinum Ell. Arthur., Fusarium oxysporum f.sp. cucumerinum, Fusarium moniliforme. The inhibition to Physalospora piricola was the strongest with an antibacterial diameter of 45 mm. This paper is the first report of the antimicrobial activity of endophytic fungi BS002 that was the secondary metabolites extracted from the seeds of Sophora flavescens. The results provide a broad foreground for biopharmaceuticals and biopesticide. PMID:26019517

  6. Chemical constituents from the leaves of Boehmeria rugulosa with antidiabetic and antimicrobial activities.

    PubMed

    Semwal, Deepak Kumar; Rawat, Usha; Semwal, Ravindra; Singh, Randhir; Krishan, Pawan; Singh, Manjeet; Singh, Gur Jas Preet

    2009-12-01

    Three new flavonoid glycosides, named chalcone-6'-hydroxy-2',3,4-trimethoxy-4'-O-beta-D-glucopyranoside (1), isoflavone-3',4',5,6-tetrahydroxy-7-O-[beta-D-glucopyranosyl-(1-->3)-alpha-L-rhamnopyranoside] (2), and isoflavone-3',4',5,6-tetrahydroxy-7-O-[beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-(1-->3)-alpha-L-rhamnopyranoside] (3), were isolated from the leaves of Boehmeria rugulosa, together with five known compounds, beta-sitosterol, quercetin, 3,4-dimethoxy-omega-(2'-piperidyl)-acetophenone (4), boehmeriasin A (5), and quercetin-7-O-beta-D-glucopyranoside. The structures of the isolated compounds were determined by means of chemical and spectral data including 2D NMR experiments. The ethanolic extract of leaves showed significant hypoglycemic activity on alloxan-induced diabetic mice. Glibenclamide, an oral hypoglycemic agent (5 mg/kg, p.o.), was used as a positive control. The ethanolic extract of the plant as well as the isolated compounds 1-3 (25 microg/ml) showed potent antimicrobial activity against two bacterial species (Staphylococcus aureus and Streptococcus mutans) and three fungus pathogens (Microsporum gypseum, Microsporum canis, and Trichophyton rubrum). The activities of the isolated compounds 1-3 have been compared with positive controls, novobiocin, and erythromycin (15 microg/ml). PMID:20183275

  7. Activation of cell-mediated immunity by Morinda citrifolia fruit extract and its constituents.

    PubMed

    Murata, Kazuya; Abe, Yumi; Futamura-Masudaa, Megumi; Uwaya, Akemi; Isami, Fumiyuki; Matsuda, Hideaki

    2014-04-01

    Morinda citrifolia, commonly known as noni, is a traditional natural medicine in French Polynesia and Hawaii. Functional foods derived from M. citrifolia fruit have been marketed to help prevent diseases and promote good health. The objective of this study was to assess the effects of M. citrifolia fruit on cell-mediated immunity. In the picryl chloride-induced contact dermatitis test, M. citrifolia fruit extract (Noni-ext) inhibited the suppression of cell-mediated immunity by immunosuppressive substances isolated from freeze-dried ascites of Ehrlich carcinoma-bearing mice (EC-sup). In addition, Noni-ext inhibited reduction of IL-2 production in EC-sup-treated mice and activated natural killer cells in normal mice. These results suggest that Noni-ext has multiple effects on the recovery of cell-mediated immunity. Furthermore, we investigated the active principles of Noni-ext and identified an iridoid glycoside, deacetylasperulosidic acid. Oral administration of deacetylasperulosidic acid inhibited the reduction of ear swelling, and also cancelled the suppression of IL-2 production along with the activation of natural killer cells in the same manner as that of Noni-ext. PMID:24868850

  8. Biting deterrence, repellency, and larvicidal activity of Ruta chalepensis (Sapindales: Rutaceae) essential oil and its major individual constituents against mosquitoes.

    PubMed

    Ali, Abbas; Demirci, Betul; Kiyan, Hulya Tuba; Bernier, Ulrich R; Tsikolia, Maia; Wedge, David E; Khan, Ikhlas A; Başer, Kemal Husnu Can; Tabanca, Nurhayat

    2013-11-01

    The essential oil from aerial parts of Ruta chalepensis L. (Sapindales: Rutaceae) was obtained by hydrodistillation, and its chemical profile was identified using gas chromatography and gas chromatography-mass spectrometry. Compounds, 2-undecanone (43.2%), 2-nonanone (27.9%), and 2-nonyl acetate (10.6%) were the major constituents of the oil. Biting deterrent activity of R. chalepensis essential oil at 10 and 50 microg/cm2, 2-undecanone at 8.5 microg/cm2, 2-nonanone at 9 microg/cm2, and 2-nonyl acetate at 9.3 microg/cm2 was similar to DEET (N, N-diethyl-meta-toluamide) at 4.8 microg/cm2, against Aedes aegypti L. Biting deterrent activity of R. chalepensis oil at 50 microg/cm2 against Anopheles quadrimaculatus Say was statistically similar to DEET at 4.8 microg/cm2, whereas the activity was lower in the other compounds tested. In cloth patch assay, R. chalepensis essential oil was effective at 187 microg/cm2, whereas 2-undecanone was effective at 108.9 microg/cm2 against Ae. aegypti. In larval bioassays, 2-undecanone showed similar toxicity whereas toxicity of R. chalepensis essential oil and 2-nonanone was higher at 24-h posttreatment at the LD50 in An. quadrimaculatus than Ae. aegypti. This study revealed that R. chalepensis essential oil and its major compounds were active biting deterrents against Ae. aegypti at higher application rates whereas only the essential oil showed activity similar to DEET against An. quadrimaculatus. 2-undecanone was the most active compound in in vivo repellency bioassay against Ae. aegypti. Chemical composition of R. chalepensis essential oil varies because of plant production and harvest practices, and the activity level of the essential oil may depend on the source of the sample. PMID:24843931

  9. Anti-austeric activity of phenolic constituents of seeds of Arctium lappa.

    PubMed

    Tezuka, Yasuhiro; Yamamoto, Keiichi; Awale, Suresh; Lia, Feng; Yomoda, Satoshi; Kadota, Shigetoshi

    2013-04-01

    From seeds of Arctium lappa L. (Asteraceae) we obtained arctigenin (1), arctiin (2), chlorogenic acid (3), 4,5-dicaffeoylquinic acid (4), 3,5-dicaffeoylquinic acid (5), 3,4-dicaffeoylquinic acid (6), matairesinol (11), isolappaol A (12), lappaol F (14), and lappaol B (15), together with 1:1 mixtures of isolappaol C (7) and lappaol C (8), arctignan E (9) and arctignan D (10), and 12 and lappaol A (13), while 3,3',4'-tri-O-demethylarctigenin (16), 3,3'-di-O-demethyl-4'-dehydroxyarctigenin (17), and 3-O-demethylarctigenin (18) were obtained by anaerobic microbiological metabolism of 1. Then, we evaluated the in vitro preferential cytotoxic activity of these pure compounds and 1:1 mixtures, together with enterodiol (19) and enterolactone (20), against human pancreatic cancer PANC-1 cells in nutrient-deprived medium (NDM). Among them, 1 and 18 showed potent activity, with PC50 values of 1.75 and 4.38 microM, respectively, while 11, 15, and 17 showed mild activity with PC50 values of 31.1, 30.9, and 38.7 microM, respectively. By comparing their structures and PC50 values, the following structural moieties could be concluded to be important for the preferential cytotoxicity of 1: 1) the 3-hydroxy-4-methoxyphenyl group at the 2-position on the gamma-butyrolactone ring, 2) the less polar substituent at the 3-position on the gamma-butyrolactone ring, and 3) the gamma-butyrolactone ring. PMID:23738454

  10. Antiproliferative activity and apoptosis-inducing mechanism of constituents from Toona sinensis on human cancer cells

    PubMed Central

    2013-01-01

    Background Natural products, including plants, microorganisms and marines, have been considered as valuable sources for anticancer drug discovery. Many Chinese herbs have been discovered to be potential sources of antitumor drugs. Methods In the present study, we investigated the antitumor efficacy of the compounds isolated from Toona sinensis, an important herbal medicine. The inhibitory activities of these compounds were investigated on MGC-803, PC3, A549, MCF-7, and NIH3T3 cells in vitro by MTT assay. The mechanism of the antitumor action of active compounds was investigated through AO/EB staining, Hoechst 33258 staining, TUNEL assay, flow cytometry analysis, and western blotting analysis. Results Fifteen compounds were isolated from the roots of Toona sinensis. Betulonic acid (BTA) and 3-oxours-12-en-28-oic acid (OEA) isolated from the plant inhibited the proliferation of MGC-803 and PC3 cells, with IC50 values of 17.7 μM and 13.6 μM, 26.5 μM and 21.9 μM, respectively. Both could lead to cell apoptosis, and apoptosis ratios reached 27.3% and 24.5% in MGC-803 cells at 72 h after treatment at 20 μM, respectively. Moreover, the study of cancer cell apoptotic signaling pathway indicated that both of them could induce cancer cell apoptosis through the mitochondrial pathway, involving the expressions of p53, Bax, caspase 9 and caspase 3. Conclusions The study shows that most of the compounds obtained from Toona sinensis could inhibit the growth of human cancer cells. Furthermore, BTA and OEA exhibited potent antitumor activities via induction of cancer cell apoptosis. PMID:23394678

  11. Discovery and antitumor activities of constituents from Cyrtomium fortumei (J.) Smith rhizomes

    PubMed Central

    2013-01-01

    Background Cyrtomium fortumei (J.) Smith is an important Chinese herbal medicine because of its biological functions. However, systematic and comprehensive studies on the phytochemicals from Cyrtomium fortumei (J.) Smith and their bioactivity are limited. Results Using the bioassay-guided technique, the ethyl acetate and n-BuOH extracts of the rhizomes of Cyrtomium fortumei (J.) Smith were shown to exhibit good antitumor activities, consequently leading to the isolation of 23 compounds. All compounds were isolated from the plant for the first time. The inhibitory activities of these compounds were investigated on tumor cells MGC-803, PC3, and A375 in vitro by MTT (thiazolyl blue tetrazolium bromide) assay, and the results showed that pimpinellin (3) had potent cytotoxic activities against the three cell lines, with the IC50 values of 14.4 ± 0.3 μM, 20.4 ± 0.5 μM, and 29.2 ± 0.6 μM, respectively. The mechanism of the antitumor action indicated that pimpinellin inhibited the growth of MGC-803 cells via the induction of tumor cell apoptosis, with apoptosis ratio of 27.44% after 72 h of treatment at 20 μM. Conclusions This study suggests that most of the compounds from the roots of Cyrtomium fortumei (J.) Smith could inhibit the growth of human carcinoma cells. Moreover, pimpinellin inhibited the growth of tumor cells via the induction of tumor cell apoptosis. PMID:23379693

  12. Acute toxicity, antiedematogenic activity, and chemical constituents of Palicourea rigida Kunth.

    PubMed

    Alves, Vanessa G; da Rosa, Elisa A; de Arruda, Laura L M; Rocha, Bruno A; Bersani Amado, Ciomar A; Santin, Silvana M O; Pomini, Armando M; da Silva, Cleuza C

    2016-03-01

    The phytochemical study of the leaves, roots, and flowers of Palicourea rigida led to the isolation of the triterpenes betulinic acid (1) and lupeol (2), the diterpene phytol (3), and the iridoid glycosides sweroside (4) and secoxyloganin (5). These compounds were identified using NMR 1H and 13C and comparing the spectra with published data. We studied the antiedematogenic activity of crude extracts from the organs, and of different fractions, in mice and found that the n-hexane fraction of the leaf extract significantly inhibited the ear edema resulting from croton oil administration. The crude extract from leaves was not acutely toxic to the mice. PMID:26927220

  13. Activity-guided isolation of cytotoxic bis-bibenzyl constituents from Dumortiera hirsuta.

    PubMed

    Toyota, Masao; Ikeda, Risa; Kenmoku, Hiromichi; Asakawa, Yoshinori

    2013-01-01

    Activity-guided fractionation of the ether extract of Dumortiera hirsute (Japanese liverwort), using cytotoxicity testing with cultured HL 60 and KB cells, resulted in the isolation of a new cytotoxic bis-bibenzyl compound, along with the two known bis-bibenzyls: isomarchantin C and isoriccardin C. The structural determination of the new bis-bibenzyl through extensive NMR spectral data indicated a derivative of marchantin A, which has been isolated from the liverwort Marchantia polymorpha. The cytotoxicity of the bis-bibenzyls was evaluated by the MTT (3-(4,5-di-methylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay using cultured HL 60 and KB cells. PMID:23391534

  14. Diterpene Constituents of Euphorbia exigua L. and Multidrug Resistance Reversing Activity of the Isolated Diterpenes.

    PubMed

    Rédei, Dóra; Boros, Klára; Forgo, Peter; Molnár, Joseph; Kele, Zoltán; Pálinkó, István; Pinke, Gyula; Hohmann, Judit

    2015-08-01

    Phytochemical investigation of the MeOH extract obtained from the aerial parts of the annual weed Euphorbia exigua L. resulted in the isolation of two novel (1, 2) and one known (3) jatrophane diterpenes. Their structures were established by extensive 1D- and 2D-NMR spectroscopy and HR-ESI-MS. The isolated compounds were evaluated for multidrug resistance (MDR) reversing activity on human MDR gene-transfected L5178 mouse lymphoma cells; and all three compounds were found to modulate the intracellular drug accumulation. PMID:26265573

  15. Main constituents from the seeds of Vietnamese Cnidium monnieri and cytotoxic activity.

    PubMed

    Dien, Pham Huu; Nhan, Nguyen Thi; Le Thuy, Hoang Thi; Quang, Dang Ngoc

    2012-01-01

    From the ethyl acetate extract of the seeds of Vietnamese Cnidium monnieri L., three coumarins, osthole (1), xanthotoxin (2), imperatorin (3) and a sterol, daucosterol (4) have been purified. Their structures were elucidated by spectroscopic analysis. Furthermore, 8-(3-hidroxy-3-methylbutyl)-7-methoxycoumarin (5) was synthesised from osthole (1) with a good yield (80%). In addition, compound 1 and its synthesis product (5) show moderate and non-selective cytotoxic activities against four cancer cells, KB (a human epidermal carcinoma), MCF7 (human breast carcinoma), SK-LU-1 (human lung carcinoma) and HepG2 (hepatocellular carcinoma). PMID:22017625

  16. [Studies of the active constituents of the Chinese drug "duhuo" Angelica pubescents].

    PubMed

    Li, R Z; He, Y Q; Chiao, M; Xu, Y; Zhang, Q B; Meng, J R; Gu, Y; Ge, L P

    1989-01-01

    Eight coumarins isolated from the alcohol extract of the Chinese drug "Duhuo", the root of Angelica pubescents Maxim. f. biserrata Shan et Yuan (Umbelliferae) were elucidated to be columbianetin (I), columbianetin acetate (II), columbiadin (III), osthol (IV), isoimperatorin (V), bergapten (VI), xanthotoxin (VII), and columbianetin-beta-D-glucopyranoside (VIII), by chemical and spectral analysis, compound VIII was isolated from plant for the first time. All these coumarins were tested on platelet aggregation induced by 2 microns ADP. I, II, III, IV and VIII showed strong inhibiting activity against platelet aggregation. PMID:2618698

  17. Chemical Constituents from Andrographis echioides and Their Anti-Inflammatory Activity

    PubMed Central

    Shen, De-Yang; Juang, Shin-Hun; Kuo, Ping-Chung; Huang, Guan-Jhong; Chan, Yu-Yi; Damu, Amooru G.; Wu, Tian-Shung

    2013-01-01

    Phytochemical investigation of the whole plants of Andrographis echioides afforded two new 2′-oxygenated flavonoids (1) and (2), two new phenyl glycosides (3) and (4), along with 37 known structures. The structures of new compounds were elucidated by spectral analysis and chemical transformation studies. Among the isolated compounds, (1–2) and (6–19) were subjected into the examination for their iNOS inhibitory bioactivity. The structure-activity relationships of the flavonoids for their inhibition of NO production were also discussed. PMID:23271366

  18. Activity against microorganisms affecting cellulosic objects of the volatile constituents of Leonotis nepetaefolia from Nicaragua.

    PubMed

    Casiglia, Simona; Bruno, Maurizio; Senatore, Felice

    2014-11-01

    The chemical composition of the essential oil from aerial parts of L. nepetaefolia (L.) R. Br. collected in Nicaragua was evaluated by GC and GC-MS. The main components were (Z)-phytol (22.8%), caryophyllene oxide (18.9%) and hexahydrofarnesylacetone (9.0%). The antibacterial activity against several Gram + and Gram - bacteria, including Bacillus cereus and B. subtilis, both infesting historical cellulosic material, was also determined. B. cereus, B. subtilis and Staphylococcus epidermis were the most affected by the action of the oil. PMID:25532300

  19. Protein tyrosine phosphatase 1B inhibitory activity of Indonesian herbal medicines and constituents of Cinnamomum burmannii and Zingiber aromaticum.

    PubMed

    Saifudin, Azis; Kadota, Shigetoshi; Tezuka, Yasuhiro

    2013-04-01

    We screened water and methanol extracts of 28 Indonesian medicinal plants for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Nine water extracts, i.e., Alstonia scholaris leaf, Blumea balsamifera, Cinnamomum burmannii, Cymbopogon nardus, Melaleuca leucadendra, Phyllanthus niruri, Piper nigrum, Syzygium aromaticum, and Sy. polyanthum, exhibited ≥70 % inhibition at 25 μg/mL, whereas 11 methanol extracts, i.e., Als. scholaris, Andrographis paniculata, B. balsamifera, Ci. burmannii, Curcuma heyneana, Glycyrrhiza glabra, M. leucadendra, Punica granatum, Rheum palmatum, Sy. polyanthum, and Z. aromaticum, exhibited ≥70 % inhibition at 25 μg/mL. Water extracts of B. balsamifera (IC50, 2.26 μg/mL) and M. leucadendra (IC50, 2.05 μg/mL), and methanol extracts of Ci. burmannii (IC50, 2.47 μg/mL), Pu. granatum (IC50, 2.40 μg/mL), and Sy. polyanthum (IC50, 1.03 μg/mL) exhibited strong inhibitory activity, which was comparable with that of the positive control, RK-682 (IC50, 2.05 μg/mL). The PTP1B inhibitory activity of the constituents of Ci. burmannii and Z. aromaticum was then evaluated. 5'-Hydroxy-5-hydroxymethyl-4″,5″-methylenedioxy-1,2,3,4-dibenzo-1,3,5-cycloheptatriene (2; IC50, 29.7 μM) and trans-cinnamaldehyde (5; IC50, 57.6 μM) were the active constituents of Ci. burmannii, while humulatrien-5-ol-8-one (21; IC50, 27.7 μM), kaempferol-3,4'-di-O-methyl ether (32; IC50, 17.5 μM), and (S)-6-gingerol (33; IC50, 28.1 μM) were those of Z. aromaticum. These results suggest that these medicinal plants may contribute to the treatment and/or prevention of type II diabetes and/or obesity through PTP1B inhibition. PMID:22645080

  20. Odor-active constituents in fresh pineapple (Ananas comosus [L.] Merr.) by quantitative and sensory evaluation.

    PubMed

    Tokitomo, Yukiko; Steinhaus, Martin; Büttner, Andrea; Schieberle, Peter

    2005-07-01

    By application of aroma extract dilution analysis (AEDA) to an aroma distillate prepared from fresh pineapple using solvent-assisted flavor evaporation (SAFE), 29 odor-active compounds were detected in the flavor dilution (FD) factor range of 2 to 4,096. Quantitative measurements performed by stable isotope dilution assays (SIDA) and a calculation of odor activity values (OAVs) of 12 selected odorants revealed the following compounds as key odorants in fresh pineapple flavor: 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDF; sweet, pineapple-like, caramel-like), ethyl 2-methylpropanoate (fruity), ethyl 2-methylbutanoate (fruity) followed by methyl 2-methylbutanoate (fruity, apple-like) and 1-(E,Z)-3,5-undecatriene (fresh, pineapple-like). A mixture of these 12 odorants in concentrations equal to those in the fresh pineapple resulted in an odor profile similar to that of the fresh juice. Furthermore, the results of omission tests using the model mixture showed that HDF and ethyl 2-methylbutanoate are character impact odorants in fresh pineapple. PMID:16041138

  1. Anti-inflammatory Activity of Constituents Isolated from Aerial Part of Angelica acutiloba Kitagawa.

    PubMed

    Uto, Takuhiro; Tung, Nguyen Huu; Taniyama, Risa; Miyanowaki, Tosihide; Morinaga, Osamu; Shoyama, Yukihiro

    2015-12-01

    Recently, the resources of medicinal plants have been exhausting. The root of Angelica acutiloba is one of the most important ingredients in Japanese Kampo medicine for the treatment of gynecological diseases. In our search for alternative medicinal plant resources of the root of A. acutiloba, we found that its aerial part has the anti-inflammatory potency as well as the root. Phytochemical investigation of the aerial part resulted in the isolation of four compounds including a new dimeric phthalide, namely tokiaerialide (2), along with Z-ligustilide (1), falcarindiol (3), and bergaptol (4). Next, we investigated the in vitro anti-inflammatory activity of 1-4 in lipopolysaccharide-stimulated RAW264 macrophages. Among the isolated compounds, 1 exhibited the most potent inhibition against lipopolysaccharide-induced production of prostaglandin E2 , nitric oxide, and pro-inflammatory cytokines (interleukin-6 and tumor necrosis factor-α). Compounds 3 and 4 also inhibited all inflammatory mediators, but their inhibitory abilities were weaker than those of 1. Furthermore, 1, 3, and 4 strongly also induced heme oxygenase-1. These results suggest that 1, 3, and 4 potentially exert anti-inflammatory activity, and the aerial part of A. acutiloba may be considered to be a useful medicinal resource for inflammatory diseases. PMID:26463105

  2. Functional constituents and antioxidant activities of eight Chinese native goji genotypes.

    PubMed

    Zhang, Qiuyun; Chen, Weiwei; Zhao, Jianhua; Xi, Wanpeng

    2016-06-01

    We quantified the levels of polyphenols, carotenoids and polysaccharides in fruits of the eight Chinese native goji genotypes, antioxidant activities of these fruit extracts were also evaluated by DPPH, ABTS and FRAP methods. Quercetin-rhamno-di-hexoside (435-1065 μg/g) and quercetin-3-O-rutinoside (159-629 μg/g) were found to be the predominant flavonoids. Chlorogenic acid was the most abundant phenolic acid (113-526 μg/g), while zeaxanthin (17-9306 μg/g) was the major carotenoid. The total antioxidant activities (TAA) of the berry extracts were significantly correlated with the total polysaccharide and phenolic contents, but not with total carotenoid (TC) levels. Overall, fruits of the Ningxia goji (Lycium barbarum L.) genotypes, DM (Damaye), NJ1 (Ningji No.1), BH (Baihua) and NH (Ningxiahuangguo) were not only rich in polyphenols, carotenoids and polysaccharides, but had significantly higher TAA than those of the other genotypes, suggesting that they represent an excellent source of antioxidants for human nutrition. PMID:26830583

  3. In vivo antioxidant activities of essential oils and their constituents from leaves of the Taiwanese Cinnamomum osmophloeum.

    PubMed

    Hsu, Fu-Lan; Li, Wen-Hsuan; Yu, Chan-Wei; Hsieh, Yi-Chen; Yang, Ying-Fei; Liu, Jui-Tung; Shih, Justin; Chu, Yu-Ju; Yen, Pei-Ling; Chang, Shang-Tzen; Liao, Vivian Hsiu-Chuan

    2012-03-28

    Cinnamomum osmophloeum Kaneh is an indigenous tree species in Taiwan. In this study, phytochemical characteristics and antioxidant activities of the essential oils and key constituents from the leaves of two C. osmophloeum clones were investigated. The two trees possess two chemotypes, which were classified as the cinnamaldehyde type and camphor type. We demonstrated that the essential oils from C. osmophloeum leaves exerted in vivo antioxidant activities in Caenorhabditis elegans. In addition, trans-cinnamaldehyde and D-(+)-camphor, which respectively represent the major compounds in the cinnamaldehyde-type and camphor-type trees, exerted significant in vivo antioxidant activities against juglone-induced oxidative stress in C. elegans. Moreover, expressions of antioxidative-related genes, including superoxide dismutase (SOD) and glutathione S-transferase (GST), were significantly induced by trans-cinnamaldehyde and D-(+)-camphor from C. osmophloeum leaves. Our results showed that the essential oils from C. osmophloeum leaves and their major compounds might have good potential for further development as nutraceuticals or antioxidant remedies. PMID:22380926

  4. Contents of constituents and antioxidant activity of seed and pulp extracts of Annona coriacea and Annona sylvatica.

    PubMed

    Benites, R S R; Formagio, A S N; Argandoña, E J S; Volobuff, C R F; Trevizan, L N F; Vieira, M C; Silva, M S

    2015-08-01

    The antioxidant potential of fruit pulp and seeds of extracts of the Annona coriacea, and A. sylvatica (Annonaceae) were investigated, as well contents total phenolics, flavonoids, condensed tannins and ascorbic acid. Was used to determine the antioxidant activity the 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), β-carotene bleaching and ABTS radical cation method. The total phenol, total flavonoid, condensed tannin, and ascorbic acid contents were measured spectrophotometrically. In this study, the pulp and seeds of the fruits were extracted using methanol/water (8:2) for maceration. The seed extracts of A. coriacea demonstrated a moderate antioxidant effect with free radical scavenging activity of 31.53%, by the DPPH test, 51.59% by the β-carotene bleaching test and 159.50 µM trolx/g of extract in the ABTS assay. We found that the hydromethanolic seed extract of A. coriacea had high total phenol (147.08 ± 4.20 mg of GAE/g of extract) and flavonoid (131.18 ± 2.31 mg of QE/g of extract) content. This indicated that the antioxidant activity of the extracts was related to the contents of these constituents. PMID:26421762

  5. Chemical constituents of Hericium erinaceum associated with the inhibitory activity against cellular senescence in human umbilical vascular endothelial cells.

    PubMed

    Noh, Hyung Jun; Yang, Hyo Hyun; Kim, Geum Soog; Lee, Seung Eun; Lee, Dae Young; Choi, Je Hun; Kim, Seung Yu; Lee, Eun Suk; Ji, Seung Heon; Kang, Ki Sung; Park, Hye-Jin; Kim, Jae-Ryong; Kim, Ki Hyun

    2015-12-01

    Hericium erinaceum is an edible and medicinal mushroom widely used in Korea, Japan, and China. On the search for biologically active compounds supporting the medicinal usage, the MeOH extract of the fruiting bodies of H. erinaceum was investigated for its chemical constituents. Six compounds were isolated and identified as hericenone D (1), (22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol (2), erinacerin B (3), hericenone E (4), hericenone F (5) and isohericerin (6) by comparing their spectroscopic data with previously reported values. The inhibitory effects on adriamycin-induced cellular senescence in human dermal fibroblasts (HDFs) and human umbilical vein endothelial cells (HUVECs) of the isolates (1-6) were studied. Among the isolated compounds, ergosterol peroxide (2) reduced senescence associated β-galactosidase (SA-β-gal) activity increased in HUVECs treated with adriamycin. According to experimental data obtained, the active compound may inspire the development of a new pharmacologically useful substance to be used in the treatment and prevention of age-related diseases. PMID:25676326

  6. Global Gene Expression Alterations as a Crucial Constituent of Human Cell Response to Low Doses of Ionizing Radiation Exposure

    PubMed Central

    Sokolov, Mykyta; Neumann, Ronald

    2015-01-01

    Exposure to ionizing radiation (IR) is inevitable to humans in real-life scenarios; the hazards of IR primarily stem from its mutagenic, carcinogenic, and cell killing ability. For many decades, extensive research has been conducted on the human cell responses to IR delivered at a low dose/low dose (LD) rate. These studies have shown that the molecular-, cellular-, and tissue-level responses are different after low doses of IR (LDIR) compared to those observed after a short-term high-dose IR exposure (HDIR). With the advent of high-throughput technologies in the late 1990s, such as DNA microarrays, changes in gene expression have also been found to be ubiquitous after LDIR. Very limited subset of genes has been shown to be consistently up-regulated by LDIR, including CDKN1A. Further research on the biological effects and mechanisms induced by IR in human cells demonstrated that the molecular and cellular processes, including transcriptional alterations, activated by LDIR are often related to protective responses and, sometimes, hormesis. Following LDIR, some distinct responses were observed, these included bystander effects, and adaptive responses. Changes in gene expression, not only at the level of mRNA, but also miRNA, have been found to crucially underlie these effects having implications for radiation protection purposes. PMID:26729107

  7. A new coumarin and cytotoxic activities of constituents from Cinnamomum cassia.

    PubMed

    Ngoc, Tran Minh; Nhiem, Nguyen Xuan; Khoi, Nguyen Minh; Son, Doan Cao; Hung, Tran Viet; Van Kiem, Phan

    2014-04-01

    A new coumarin derivative, coumacasia (1) and eight known compounds, coumarin (2), cinnamaldehyde (3), 2-methoxycinnamaldehyde (4), 2-hydroxycinnamaldehyde (5), coniferaldehyde (6), cinnamic acid (7), 2-hydroxycinnamic acid (8), and cinnamic alcohol (9), were isolated from the methanol extract of Cinnamomum cassia. Their structures were elucidated by spectral data and by comparison with the reported literature. The cytotoxic activities of compounds 1-9 were evaluated with two human cancer cell lines, HL-60 and A-549. Compound 1 showed growth inhibitory effects in the HL-60 and A-549 cell lines with IC50 values of 8.2 +/- 0.5 and 11.3 +/- 1.1 microM, respectively. Compounds 3-6, and 8 exhibited moderate cytotoxicity with IC50 values ranging from 20.5 to 65.6 microM. PMID:24868863

  8. Chemical constituents of Blumea balsamifera of Indonesia and their protein tyrosine phosphatase 1B inhibitory activity.

    PubMed

    Saifudin, Azis; Tanaka, Ken; Kadota, Shigetoshi; Tezuka, Yasuhiro

    2012-07-01

    A methanol extract of the leaves of Blumea balsamifera (L.) DC. (Asteraceae) afforded a new guaian-type sesquiterpene, epiblumeaene K (1), together with four known guaian-type sesquiterpenes (2-5), three known sesquiterpenes (6-8), and nine known flavonoids (9-17) by a combination of chromatography and preparative TLC techniques. Their structures were elucidated by extensive spectroscopic methods and comparison with the literature data. Among the isolated compounds, a known sesquiterpene, beta-caryophyllene 8R,9R-oxide (6), exhibited a significant PTP1B inhibitory activity in a dose-dependent manner, with an IC50 value of 25.8 microM (5.62 microg/mL). PMID:22908553

  9. Chemical constituents from the root of Polygonum multiflorum and their soluble epoxide hydrolase inhibitory activity.

    PubMed

    Sun, Ya Nan; Li, Wei; Kim, Jang Hoon; Yan, Xi Tao; Kim, Ji Eun; Yang, Seo Young; Kim, Young Ho

    2015-06-01

    Fourteen compounds were isolated from a methanol extract of Polygonum multiflorum roots, and their structures were elucidated by comparing spectroscopic data to published spectra. The inhibitory effects of the isolated compounds on soluble epoxide hydrolase (sEH) were then evaluated. Compounds 1-7 inhibited sEH activity potently, with IC50 values ranging from 6.2 ± 0.5 to 48.6 ± 3.1 μM. Moreover, a kinetic analysis of compounds 1-7 revealed that the inhibitory actions of compounds 1, 3 and 4 were non-competitive, whereas those of compounds 2 and 5-7 were mixed-type. PMID:25413971

  10. Anti-inflammatory activity of linalool and linalyl acetate constituents of essential oils.

    PubMed

    Peana, A T; D'Aquila, P S; Panin, F; Serra, G; Pippia, P; Moretti, M D L

    2002-12-01

    Linalool and linalyl acetate are the principal components of many essential oils known to possess several biological activities, attributable to these monoterpene compounds. In this work, we evaluated individually the anti-inflammatory properties of (-) linalool, that is, the natural occurring enantiomer, and its racemate form, present in various amounts in distilled or extracted essential oils. Because in the linalool-containing essential oils, linalyl acetate, is frequently present, we also examined the anti-inflammatory action of this monoterpene ester. Carrageenin-induced edema in rats was used as a model of inflammation. The experimental data indicate that both the pure enantiomer and its racemate induced, after systemic administration, a reduction of edema. Moreover, the pure enantiomer, at a dose of 25 mg/kg, elicited a delayed and more prolonged effect, while the racemate form induced a significant reduction of the edema only one hour after carrageenin administration. At higher doses, no differences were observed between the (-) enantiomer and the racemate; a further increase in the dose of both forms did not result in an increased effect at any time of observation. The effects of equi-molar doses of linalyl acetate on local edema were less relevant and more delayed than that of the corresponding alcohol. These finding suggest a typical pro-drug behavior of linalyl acetate. The results obtained indicate that linalool and the corresponding acetate play a major role in the anti-inflammatory activity displayed by the essential oils containing them, and provide further evidence suggesting that linalool and linalyl acetate-producing species are potentially anti-inflammatory agents. PMID:12587692

  11. Nootkatone, a characteristic constituent of grapefruit, stimulates energy metabolism and prevents diet-induced obesity by activating AMPK.

    PubMed

    Murase, Takatoshi; Misawa, Koichi; Haramizu, Satoshi; Minegishi, Yoshihiko; Hase, Tadashi

    2010-08-01

    AMP-activated protein kinase (AMPK) is a serine/threonine kinase that is implicated in the control of energy metabolism and is considered to be a molecular target for the suppression of obesity and the treatment of metabolic syndrome. Here, we identified and characterized nootkatone, a constituent of grapefruit, as a naturally occurring AMPK activator. Nootkatone induced an increase in AMPKalpha1 and -alpha2 activity along with an increase in the AMP/ATP ratio and an increase the phosphorylation of AMPKalpha and the downstream target acetyl-CoA carboxylase (ACC), in C(2)C(12) cells. Nootkatone-induced activation of AMPK was possibly mediated both by LKB1 and Ca(2+)/calmodulin-dependent protein kinase kinase. Nootkatone also upregulated PPARgamma coactivator-1alpha in C(2)C(12) cells and C57BL/6J mouse muscle. In addition, administration of nootkatone (200 mg/kg body wt) significantly enhanced AMPK activity, accompanied by LKB1, AMPK, and ACC phosphorylation in the liver and muscle of mice. Whole body energy expenditure evaluated by indirect calorimetry was also increased by nootkatone administration. Long-term intake of diets containing 0.1% to 0.3% (wt/wt) nootkatone significantly reduced high-fat and high-sucrose diet-induced body weight gain, abdominal fat accumulation, and the development of hyperglycemia, hyperinsulinemia, and hyperleptinemia in C57BL/6J mice. Furthermore, endurance capacity, evaluated as swimming time to exhaustion in BALB/c mice, was 21% longer in mice fed 0.2% nootkatone than in control mice. These findings indicate that long-term intake of nootkatone is beneficial toward preventing obesity and improving physical performance and that these effects are due, at least in part, to enhanced energy metabolism through AMPK activation in skeletal muscle and liver. PMID:20501876

  12. Chemical Constituents and Evaluation of Antimicrobial and Cytotoxic Activities of Kielmeyera coriacea Mart. & Zucc. Essential Oils.

    PubMed

    Martins, Carla de M; do Nascimento, Evandro A; de Morais, Sérgio A L; de Oliveira, Alberto; Chang, Roberto; Cunha, Luís C S; Martins, Mário M; Martins, Carlos Henrique G; Moraes, Thaís da S; Rodrigues, Paulla V; da Silva, Cláudio V; de Aquino, Francisco J T

    2015-01-01

    Many essential oils (EOs) of different plant species possess interesting antimicrobial effects on buccal microorganisms and cytotoxic properties. EOs of Kielmeyera coriacea Mart. & Zucc. were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). The EO from leaves is rich in sesquiterpenes hydrocarbons and oxygenated sesquiterpenes. The three major compounds identified were germacrene-D (24.2%), (E)-caryophyllene (15.5%), and bicyclogermacrene (11.6%). The inner bark EO is composed mainly of sesquiterpenes hydrocarbons and the major components are alpha-copaene (14.9%) and alpha-(E)-bergamotene (13.0%). The outer bark EO is composed mainly of oxygenated sesquiterpenes and long-chain alkanes, and the major components are alpha-eudesmol (4.2%) and nonacosane (5.8%). The wood EO is mainly composed of long-chain alkanes and fatty acids, and the major components are nonacosane (9.7%) and palmitic acid (16.2%). The inner bark EO showed the strongest antimicrobial activity against the anaerobic bacteria Prevotella nigrescens (minimum inhibitory concentration-MIC of 50 µg mL(-1)). The outer bark and wood EOs showed MICs of 100 µg mL(-1) for all aerobic microorganisms tested. The EOs presented low toxicity to Vero cells. These results suggest that K. coriacea, a Brazilian plant, provide initial evidence of a new and alternative source of substances with medicinal interest. PMID:25960759

  13. Saffron (its active constituent, crocin) supplementation attenuates lipid peroxidation and protects against tissue injury.

    PubMed

    Altinoz, E; Ozmen, T; Oner, Z; Elbe, H; Erdemli, M E; Bag, H G

    2016-01-01

    The aim of the current study was to investigate the outcomes in a rat model of an acute swimming exercise induced oxidative stress in brain, kidney, liver, skeletal and cardiac muscles using supplementation with crocin. Rats were divided into the eight groups; Normal Control (NC: Untreated and did not swim), Crocin Control (CC: Received crocin and did not swim), Exercise-1 (E-1: Untreated and swam), Exercise-24 (E-24: Untreated and swam), Exercise-48 (E-48: Untreated and swam), Exercise+Crocin-1 (EC-1: Received crocin and swam), Exercise+Crocin-24 (EC-24: Received crocin and swam), Exercise+Crocin-48 (EC-48: Received crocin and swam). The malondialdehyde (MDA) and xanthine oxidase (XO) enzymes levels increased after swimming in untreated and crocin treated groups, but there was a lower increase in crocin treated groups. The highest MDA levels in all tissues were observed in E-1 compared to all other groups. There were significant differences between control and exercise groups in MDA levels of tissues (p < 0.001). In contrast, there were significant differences between control and exercise groups in glutathione (GSH) levels of tissues.In addition, the crocin supplementation significantly increased GSH levels and decreased MDA and XO enzyme levels when compared to untreated exercise groups. Crocin can protect the tissues against exercise induced oxidative stress by enhancing antioxidant activity (Tab. 3, Fig. 1, Ref. 37). PMID:27546539

  14. Antimicrobial activities of Eugenia caryophyllata extract and its major chemical constituent eugenol against Streptococcus pneumoniae.

    PubMed

    Yadav, Mukesh Kumar; Park, Seok-Won; Chae, Sung-Won; Song, Jae-Jun; Kim, Ho Chul

    2013-12-01

    In this study, we investigate the antimicrobial activities of both Eugenia caryophyllata (Ec) extract and its major component eugenol (4-allyl-2-methoxyphenol) against Streptococcus pneumoniae. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined by microdilution method. Pneumococcal biofilms were detected by crystal-violet microtiter plate assay, followed by colony-forming unit counts and visualized by scanning electron microscope (SEM). The synergistic effect of eugenol and penicillin was determined by checker-board method. Both the eugenol and the Ec extract inhibited pneumococcal growth in a concentration-dependent manner. The MIC and MBC of eugenol were 0.06% and 0.12%, respectively. Eugenol at a concentration of 0.12% completely killed S. pneumoniae within 60 min of exposure. The kill rate of planktonic cells was most rapid during the first 15 min of contact with eugenol. The addition of eugenol or Ec extract inhibited in vitro biofilm formation. In already established biofilms, the inhibitory effect of eugenol or Ec extract was more significant in terms of cell viability than in terms of disruption of the biofilm matrix. SEM analysis revealed non-viable and disruptive action of eugenol on the cell membrane of bacteria of biofilms. It was found that eugenol and penicillin produced a synergistic effect against S. pneumoniae. In conclusion, eugenol and Ec extract efficiently inhibited S. pneumoniae in planktonic growth and within biofilms. PMID:23594212

  15. Chemical constituents and in vitro anti-inflammatory activity of Cistanche violacea Desf. (Orobanchaceae) extract.

    PubMed

    Bougandoura, Amina; D'Abrosca, Brigida; Ameddah, Souad; Scognamiglio, Monica; Mekkiou, Ratiba; Fiorentino, Antonio; Benayache, Samir; Benayache, Fadila

    2016-03-01

    A new iridoid (1) and a new phenylethanoid glycoside (4), together with five known compounds (2, 3, 5, 6 and 7), were isolated for the first time from the ethyl acetate soluble part of the hydroalcoholic extract of the aerial parts of Cistanche violacea Desf. (Orobanchaceae), an endemic species of the North of the Sahara. The structures of these compounds have been elucidated on the basis of extensive 2D NMR spectroscopic analysis, including COSY, TOCSY, NOESY, HSQC, CIGAR-HMBC, H2BC and HSQC-TOCSY. All compounds were isolated from C. violacea for the first time. The anti-inflammatory activity of the EtOAc extract of C. violacea, was investigated by using human red blood cell (HRBC) membrane stabilization and inhibition of the albumin denaturation method. This study demonstrates, for the first time the effectiveness of C. violacea in combating inflammation, this might be believed to be influenced by the synergistic action of the above isolated compounds. The present study suggests that C. violacea would serve as a source for the discovery of novel anti-inflammatory agents. PMID:26784519

  16. Chemical Constituents and Evaluation of Antimicrobial and Cytotoxic Activities of Kielmeyera coriacea Mart. & Zucc. Essential Oils

    PubMed Central

    Martins, Carla de M.; do Nascimento, Evandro A.; de Morais, Sérgio A. L.; de Oliveira, Alberto; Chang, Roberto; Cunha, Luís C. S.; Martins, Mário M.; Martins, Carlos Henrique G.; Moraes, Thaís da S.; Rodrigues, Paulla V.; da Silva, Cláudio V.; de Aquino, Francisco J. T.

    2015-01-01

    Many essential oils (EOs) of different plant species possess interesting antimicrobial effects on buccal microorganisms and cytotoxic properties. EOs of Kielmeyera coriacea Mart. & Zucc. were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). The EO from leaves is rich in sesquiterpenes hydrocarbons and oxygenated sesquiterpenes. The three major compounds identified were germacrene-D (24.2%), (E)-caryophyllene (15.5%), and bicyclogermacrene (11.6%). The inner bark EO is composed mainly of sesquiterpenes hydrocarbons and the major components are alpha-copaene (14.9%) and alpha-(E)-bergamotene (13.0%). The outer bark EO is composed mainly of oxygenated sesquiterpenes and long-chain alkanes, and the major components are alpha-eudesmol (4.2%) and nonacosane (5.8%). The wood EO is mainly composed of long-chain alkanes and fatty acids, and the major components are nonacosane (9.7%) and palmitic acid (16.2%). The inner bark EO showed the strongest antimicrobial activity against the anaerobic bacteria Prevotella nigrescens (minimum inhibitory concentration-MIC of 50 µg mL−1). The outer bark and wood EOs showed MICs of 100 µg mL−1 for all aerobic microorganisms tested. The EOs presented low toxicity to Vero cells. These results suggest that K. coriacea, a Brazilian plant, provide initial evidence of a new and alternative source of substances with medicinal interest. PMID:25960759

  17. Aortic relaxant activity of Crataegus gracilior Phipps and identification of some of its chemical constituents.

    PubMed

    Hernández-Pérez, Abigail; Bah, Moustapha; Ibarra-Alvarado, César; Rivero-Cruz, José Fausto; Rojas-Molina, Alejandra; Rojas-Molina, Juana Isela; Cabrera-Luna, José Alejandro

    2014-01-01

    This study focused on the assessment of the vasorelaxant activity of the organic and aqueous extracts obtained from leaves and fruits of a Mexican hawthorn (Crataegus gracilior) on isolated rat aorta, and on the purification and identification of some of their secondary metabolites by the use of chromatographic and spectroscopic techniques. The results obtained showed that the methanol extract has a significantly more potent and effective vasorelaxant effect than the other tested extracts, with an EC50 = 8.69 ± 4.34 µg/mL and an Emax = 94.6% ± 11.30%, values that are close to that of acetylcholine, the positive control. From the same extract, two major triterpenes were isolated and identified as ursolic and corosolic acids by comparison of their experimental NMR spectroscopic data with those reported in the literature. Chlorogenic acid, rutin, quercetin, kaempferol and (+)-catechin were also identified using HPLC coupled with PDAD. All these compounds have already been proven to possess on their own antihypertensive effect and other benefits on cardiovascular diseases and they can support, at least in part, the traditional use of this plant species. PMID:25517338

  18. Chemical constituents of Papulaspora immersa, an endophyte from Smallanthus sonchifolius (Asteraceae), and their cytotoxic activity.

    PubMed

    Gallo, Margareth Borges Coutinho; Cavalcanti, Bruno Coêlho; Barros, Francisco Washington Araújo; Odorico de Moraes, Manoel; Costa-Lotufo, Letícia Veras; Pessoa, Cláudia; Bastos, Jairo Kenupp; Pupo, Mônica Tallarico

    2010-12-01

    Papulaspora immersa H. H. Hotson was isolated from roots and leaves of Smallanthus sonchifolius (Poepp. and Endl.) H. Rob. (Asteraceae), traditionally known as Yacon. The fungus was cultured in rice, and, from the AcOEt fraction, 14 compounds were isolated. Among them, (22E,24R)-8,14-epoxyergosta-4,22-diene-3,6-dione (4), 2,3-epoxy-1,2,3,4-tetrahydronaphthalene-c-1,c-4,8-triol (10), and the chromone papulasporin (13) were new secondary metabolites. The spectral data of the known natural products were compared with the literature data, and their structures were established as the (24R)-stigmast-4-en-3-one (1), 24-methylenecycloartan-3β-ol (2), (22E,24R)-ergosta-4,6,8(14),22-tetraen-3-one (3), (-)-(3R,4R)-4-hydroxymellein (5), (-)-(3R)-5-hydroxymellein (6), 6,8-dihydroxy-3-methylisocoumarin (7), (-)-(4S)-4,8-dihydroxy-α-tetralone (8), naphthalene-1,8-diol (9), 6,7,8-trihydroxy-3-methylisocoumarin (11), 7-hydroxy-2,5-dimethylchromone (12), and tyrosol (14). Compound 4 showed the highest cytotoxic activity against the human tumor cell lines MDA-MB435 (melanoma), HCT-8 (colon), SF295 (glioblastoma), and HL-60 (promyelocytic leukemia), with IC₅₀ values of 3.3, 14.7, 5.0 and 1.6 μM, respectively. Strong synergistic effects were also observed with compound 5 and some of the isolated steroidal compounds. PMID:21162007

  19. Chemical constituents from Sonneratia ovata Backer and their in vitro cytotoxicity and acetylcholinesterase inhibitory activities.

    PubMed

    Nguyen, Thi-Hoai-Thu; Pham, Huu-Viet-Thong; Pham, Nguyen-Kim-Tuyen; Quach, Ngo-Diem-Phuong; Pudhom, Khanitha; Hansen, Poul Erik; Nguyen, Kim-Phi-Phung

    2015-06-01

    Sonneratia ovata Backer, Sonneratiaceae, is a widespread plant in mangrove forests in Vietnam, Cambodia, Thailand, Indonesia. Sonneratia ovata's chemical composition remains mostly unknown. Therefore, we now report on the structural elucidation of three new phenolics, sonnerphenolic A (1), sonnerphenolic B (2), and sonnerphenolic C (23), a new cerebroside, sonnercerebroside (3) together with nineteen known compounds, including nine lignans (5-13), two steroids (14, 15), two triterpenoids (16, 17), three gallic acid derivatives (18-20), two phenolic derivatives (4, 22) and a 1-O-benzyl-β-d-glucopyranose (21) isolated from the leaves of Sonneratia ovata. Their chemical structures were established by spectroscopic data, as well as high resolution mass spectra and comparison with literature data. The in vitro acetylcholinesterase (AChE) inhibition and cytotoxic activities against HeLa (human epithelial carcinoma), NCI-H460 (human lung cancer), MCF-7 (human breast cancer) cancer cell lines and PHF (primary human fibroblast) cell were evaluated on some extracts and purified compounds at a concentration of 100 μg/mL. Compounds (5, 6, 23) exhibited cytotoxicity against the MCF-7 cell line with the IC50 values of 146.9±9.0, 114.5±7.2, and 112.8±9.4 μM, respectively, while they showed nontoxic with the normal cell (PHF) with IC50s >277 μM. Among 15 tested compounds, (S)-rhodolatouchol (22) showed inhibition against AChE with an IC50 value of 96.1±14.5 μM. PMID:25933595

  20. Acaricidal activities against house dust mites of spearmint oil and its constituents.

    PubMed

    Yang, Ji-Yeon; Kim, Min-Gi; Lee, Sung-Eun; Lee, Hoi-Seon

    2014-02-01

    The aim of this study was to evaluate the acaricidal activities of spearmint oil and carvone derivatives against house dust mites using contact and fumigant toxicity bioassays to replace benzyl benzoate as a synthetic acaricide. Based on the LD50 values, the contact toxicity bioassay revealed that dihydrocarvone (0.95 and 0.88 µg/cm2) was 7.7 and 6.8 times more toxic than benzyl benzoate (7.33 and 6.01 µg/cm2) against Dermatophagoides farinae and Dermatophagoides pteronyssinus, respectively, followed by carvone (3.78 and 3.23 µg/cm2), spearmint oil (5.16 and 4.64 µg/cm2), carveol (6.00 and 5.80 µg/cm2), and dihydrocarveol (8.23 and 7.10 µg/cm2). Results of the fumigant toxicity bioassay showed that dihydrocarvone (2.73 and 2.16 µg/cm2) was approximately 4.0 and 4.8 times more effective than benzyl benzoate (11.00 and 10.27 µg/cm2), followed by carvone (6.63 and 5.78 µg/cm2), carveol (7.58 and 7.24 µg/cm2), spearmint oil (9.55 and 8.10 µg/cm2), and dihydrocarveol (9.79 and 8.14 µg/cm2). Taken together, spearmint oil and carvone derivatives are a likely viable alternative to synthetic acaricides for managing house dust mites. PMID:24488719

  1. Chemical composition, antioxidant and antibacterial activities of the leaf essential oil of Juglans regia L. and its constituents.

    PubMed

    Rather, Manzoor A; Dar, Bilal A; Dar, Mohd Yousuf; Wani, Bilal A; Shah, Wajahat A; Bhat, Bilal A; Ganai, Bashir A; Bhat, Khursheed A; Anand, Rajneesh; Qurishi, Mushtaq A

    2012-10-15

    The essential oil from the leaves of Juglans regia L. (Juglandaceae) growing wild in Kashmir (India) was obtained by hydrodistillation and analysed by a combination of capillary GC-FID and GC-MS. A total of 38 compounds, representing 92.7% of the oil, were identified and the major components were found to be α-pinene (15.1%), β-pinene (30.5%), β-caryophyllene (15.5%) germacrene D (14.4%) and limonene (3.6%). The essential oil and the main individual constituents were screened for antibacterial activity and the essential oil evaluated for antioxidant activity. Antibacterial activity was evaluated using the disc diffusion and microdilution methods against a group of clinically significant Gram-positive (Staphylococcus epidermidis MTCC-435, Bacillus subtilis MTCC-441, Staphylococcus aureus) and Gram-negative bacteria (Proteus vulgaris MTCC-321, Pseudomonas aeruginosa MTCC-1688, Salmonella typhi, Shigella dyssenteriae, Klebsiella pneumonia and Escherichia coli). The essential oil and its major components exhibited broad spectrum inhibition against all the bacterial strains with Gram-positive being more susceptible to the oil than Gram-negative bacteria. Antioxidant activity of the oil was evaluated by the scavenging effect on DPPH (2,2-diphenyl-1-picrylhydrazyl) and hydroxyl radicals. In general, the essential oil exhibited high antioxidant activity which was comparable to the reference standards at the same dose (ascorbic acid and butylated hydroxyl toluene, BHT) with IC(50) values of 34.5 and 56.4μg/ml calculated by DPPH and hydroxyl radical scavenging assays respectively. PMID:22951389

  2. Antifungal activity of essential oil and its constituents from Calocedrus macrolepis var. formosana Florin leaf against plant pathogenic fungi.

    PubMed

    Chang, Hui-Ting; Cheng, Ying-Hung; Wu, Chi-Lin; Chang, Shang-Tzen; Chang, Tun-Tschu; Su, Yu-Chang

    2008-09-01

    Resistance to conventional fungicides causes the poor disease control of agriculture. Natural products from plants have great potential as novel fungicide sources for controlling pathogenic fungi. In this study antipathogenic activity of the leaf essential oil and its constituents from Calocedrus macrolepis var. formosana Florin were evaluated in vitro against six plant pathogenic fungi. Chemical analysis of leaf oil by GC/MS allowed identification of alpha-pinene (44.2%), limonene (21.6%), beta-myrcene (8.9%), beta-caryophyllene (8.2%), caryophyllene oxide (2.4%), alpha-cadinol (1.6%), beta-pinene (1.2%), and T-muurolol (1.1%) as main components. Sesquiterpenoid components of the oil were more effective than monoterpenoid components of the oil. In particular, T-muurolol and alpha-cadinol strongly inhibited the growth of Rhizoctonia solani and Fusarium oxysporum, with the IC(50) values < 50 microg ml(-1). These compounds also efficiently inhibited the mycelial growths of Colletotrichum gloeosporioides, P. funerea, Ganoderma australe and F. solani. These results showed that T-muurolol and alpha-cadinol possess antifungal activities against a broad spectrum of tested plant pathogenic fungi and could be used as potential antifungal agents for the control of fungal diseases in plants. PMID:18206367

  3. A First Step in the Quest for the Active Constituents in Filipendula ulmaria (Meadowsweet): Comprehensive Phytochemical Identification by Liquid Chromatography Coupled to Quadrupole-Orbitrap Mass Spectrometry.

    PubMed

    Bijttebier, Sebastiaan; Van der Auwera, Anastasia; Voorspoels, Stefan; Noten, Bart; Hermans, Nina; Pieters, Luc; Apers, Sandra

    2016-04-01

    Filipendula ulmaria (meadowsweet) is traditionally used for the treatment of inflammatory diseases and as a diuretic and antirheumatic. Extracts of Filipendulae herba are on the market in the European Union as food supplements. Nevertheless, its active constituents remain to be revealed. During this study, the phytochemical composition of Filipendulae Ulmariae Herba was comprehensively characterised for the first time with two complementary generic ultrahigh-performance liquid chromatography-photodiode array-accurate mass mass spectrometry methods. Selective ion fragmentation experiments with a hybrid quadrupole-orbital trap mass spectrometer significantly contributed to compound identification: a total of 119 compounds were tentatively identified, 69 new to F. ulmaria. A rich diversity of phenolic constituents was detected and only a few non-phenolic phytochemicals were observed. Metabolisation and pharmacological studies should be conducted to investigate which of these constituents or metabolites there of contribute to the activity of F. ulmaria after oral intake. PMID:26845709

  4. Antibacterial activity and mode of action of the Artemisia capillaris essential oil and its constituents against respiratory tract infection-causing pathogens.

    PubMed

    Yang, Chang; Hu, Dong-Hui; Feng, Yan

    2015-04-01

    Inhalation therapy using essential oils has been used to treat acute and chronic sinusitis and bronchitis. The aim of the present study was to determine the chemical composition of the essential oil of Artemisia capillaris, and evaluate the antibacterial effects of the essential oil and its main components, against common clinically relevant respiratory bacterial pathogens. Gas chromatography and gas chromatography‑mass spectrometry revealed the presence of 25 chemical constituents, the main constituents being: α‑pinene, β‑pinene, limonene, 1,8‑cineole, piperitone, β‑caryophyllene and capillin. The antibacterial activities of the essential oil, and its major constituents, were evaluated against Streptococcus pyogenes, methicillin‑resistant Staphylococcus aureus (MRSA), MRSA (clinical strain), methicillin‑gentamicin resistant Staphylococcus aureus (MGRSA), Streptococcus pneumoniae, Klebsiella pneumoniae, Haemophilus influenzae and Escherichia coli. The essential oil and its constituents exhibited a broad spectrum and variable degree of antibacterial activity against the various strains. The essential oil was observed to be much more potent, as compared with any of its major chemical constituents, exhibiting low minimum inhibitory and bacteriocidal concentration values against all of the bacterial strains. The essential oil was most active against S. pyogenes, MRSA (clinical strain), S. pneumoniae, K. pneumoniae, H. influenzae and E. coli. Piperitone and capillin were the most potent growth inhibitors, among the major chemical constituents. Furthermore, the essential oil of A. capillaris induced significant and dose‑dependent morphological changes in the S. aureus bacterial strain, killing >90% of the bacteria when administered at a higher dose; as determined by scanning electron microscopy. In addition, the essential oil induced a significant leakage of potassium and phosphate ions from the S. aureus bacterial cultures. These results indicate that

  5. Evaluation of larvicidal activity of the essential oil of Allium macrostemon Bunge and its selected major constituent compounds against Aedes albopictus (Diptera: Culicidae)

    PubMed Central

    2014-01-01

    Background During the screening programme for new agrochemicals from Chinese medicinal herbs and local wild plants, the essential oil of dried bulbs of Allium macrostemon Bunge (Liliaceae) was found to possess larvicidal activity against mosquitoes. The aim of this research was to determine the larvicidal activity of the essential oil and its major constituent compounds against the larvae of the Culicidae mosquito, Aedes albopictus. Methods Essential oil of A. macrostemon was obtained by hydrodistillation and analyzed by gas chromatography (GC) and gas chromaotography-mass spectrometry (GC-MS). The activity of the essential oil and its two major constituents were evaluated, using World Health Organization (WHO) procedures, against the fourth instar larvae of Ae. albopictus for 24 h and larval mortalities were recorded at various essential oil/compound concentrations ranging from 9.0 - 150 μg/ml. Results The essential oil of A. macrostemon exhibited larvicidal activity against the early fourth instar larvae of Ae. albopictus with an LC50 value of 72.86 μg/ml. The two constituent compounds, dimethyl trisulfide and methyl propyl disulfide possessed strong larvicidal activity against the early fourth instar larvae of Ae. albopictus with LC50 values of 36.36 μg/ml and 86.16 μg/ml, respectively. Conclusion The results indicated that the essential oil of A. macrostemon and its major constituents have good potential as a source for natural larvicides. PMID:24731297

  6. Stereoselective Effects of Abused "Bath Salt" Constituent 3,4-Methylenedioxypyrovalerone in Mice: Drug Discrimination, Locomotor Activity, and Thermoregulation.

    PubMed

    Gannon, Brenda M; Williamson, Adrian; Suzuki, Masaki; Rice, Kenner C; Fantegrossi, William E

    2016-03-01

    3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of illicit "bath salts" products. MDPV is a chiral molecule, but the contribution of each enantiomer to in vivo effects in mice has not been determined. To address this, mice were trained to discriminate 10 mg/kg cocaine from saline, and substitutions with racemic MDPV, S(+)-MDPV, and R(-)-MDPV were performed. Other mice were implanted with telemetry probes to monitor core temperature and locomotor responses elicited by racemic MDPV, S(+)-MDPV, and R(-)-MDPV under a warm (28°C) or cool (20°C) ambient temperature. Mice reliably discriminated the cocaine training dose from saline, and each form of MDPV fully substituted for cocaine, although marked potency differences were observed such that S(+)-MDPV was most potent, racemic MDPV was less potent than the S(+) enantiomer, and R(-)-MDPV was least potent. At both ambient temperatures, locomotor stimulant effects were observed after doses of S(+)-MDPV and racemic MDPV, but R(-)-MDPV did not elicit locomotor stimulant effects at any tested dose. Interestingly, significant increases in maximum core body temperature were only observed after administration of racemic MDPV in the warm ambient environment; neither MDPV enantiomer altered core temperature at any dose tested, at either ambient temperature. These studies suggest that all three forms of MDPV induce biologic effects, but R(-)-MDPV is less potent than S(+)-MDPV and racemic MDPV. Taken together, these data suggest that the S(+)-MDPV enantiomer is likely responsible for the majority of the biologic effects of the racemate and should be targeted in therapeutic efforts against MDPV overdose and abuse. PMID:26769917

  7. Active Response Gravity Offload System

    NASA Technical Reports Server (NTRS)

    Valle, Paul; Dungan, Larry; Cunningham, Thomas; Lieberman, Asher; Poncia, Dina

    2011-01-01

    The Active Response Gravity Offload System (ARGOS) provides the ability to simulate with one system the gravity effect of planets, moons, comets, asteroids, and microgravity, where the gravity is less than Earth fs gravity. The system works by providing a constant force offload through an overhead hoist system and horizontal motion through a rail and trolley system. The facility covers a 20 by 40-ft (approximately equals 6.1 by 12.2m) horizontal area with 15 ft (approximately equals4.6 m) of lifting vertical range.

  8. Flos Albiziae aqueous extract and its active constituent quercetin potentiate the hypnotic effect of pentobarbital via the serotonergic system

    PubMed Central

    YE, MENG-FEI; LIU, ZHENG; LOU, SHU-FANG; CHEN, ZHEN-YONG; YU, AI-YUE; LIU, CHUN-YAN; YU, CHAO-YANG; ZHANG, HUA-FANG; ZHANG, JIAN

    2015-01-01

    Flos albiziae (FA) is reportedly used for treatment of insomnia and anxiety in traditional medicine. The hypnotic effect of an extract of FA (FAE) and its constituent quercetin [2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one, QR] was examined in mice. QR is a widely distributed natural flavonoid abundant in FA flowers and other tissues. The possible mechanisms underlying the hypnotic effects of FAE and QR were investigated using behavioral pharmacology. FAE and QR significantly potentiated pentobarbital-induced [50 mg/kg, intraperitoneal (ip)] sleep (prolonged sleeping time; shortened sleep latency) in a dose-dependent manner, and these effects were augmented by administration of 5-hydroxytryptophan (5-HTP), a precursor of 5-hydroxytryptamine. With a sub-hypnotic dose of pentobarbital (28 mg/kg, ip), FAE and QR significantly increased the rate of sleep onset and were synergistic with 5-HTP (2.5 mg/kg, ip). Pretreatment with p-chlorophenylalanine, an inhibitor of tryptophan hydroxylase, significantly decreased sleeping time and prolonged sleep latency in pentobarbital-treated mice, whereas FAE and QR significantly reversed this effect. Data show that FAE and QR have hypnotic activity, possibly mediated by the serotonergic system. The present study offers a rationale for the use of FA in treating sleep disorders associated with serotonin system dysfunction. PMID:26623026

  9. Shallominthe Active Antimicrobial Constituent of Persian Shallot in Treatment of Oral Herpes: A Double-Blind Randomized Clinical Trial

    PubMed Central

    Pipelzadeh, Mohammad Hassan; Amin, Mansour; Shiravi Khozani, Abolfazl; Radmanesh, Mohammad

    2014-01-01

    Background: Previous studies showed that shallomin, the active antimicrobial constituent of Persian shallot, has a wide range of antibacterial and antifungal properties. Objectives: The objective of this randomized clinical trial was to evaluate the effectiveness of topical shallomin alcoholic solution in treatment of cold sore. Patients and Methods: A total of 60 volunteers who met the inclusion criteria were randomly allocated to two equal groups to hourly apply topical of either 0.5% shallomin alcoholic solution or placebo within the first 24 hours of developing cold sores. All the cases were reassessed at six-hour intervals. Results: The cold sores were cleared within six hours among 30% of cases who received shallomin solution and the remaining of the cases in this group were cleared between 6six to 24 hours of application. In the placebo group, clearance of the sores occurred in four cases between 48 to 72 hours and the remaining of cases were cleared after 72 hours. Conclusions: The results of this study demonstrated that shallomin is a useful natural remedy in preventing the progression and treatment of cold sores and can significantly reduce the duration of ulceration. PMID:25237646

  10. Effects of herbal products and their constituents on human cytochrome P450(2E1) activity.

    PubMed

    Raner, Gregory M; Cornelious, Sean; Moulick, Kamalika; Wang, Yingqing; Mortenson, Ashley; Cech, Nadja B

    2007-12-01

    Ethanolic extracts from fresh Echinacea purpurea and Spilanthes acmella and dried Hydrastis canadensis were examined with regard to their ability to inhibit cytochrome P450(2E1) mediated oxidation of p-nitrophenol in vitro. In addition, individual constituents of these extracts, including alkylamides from E. purpurea and S. acmella, caffeic acid derivatives from E. purpurea, and several of the major alkaloids from H. canadensis, were tested for inhibition using the same assay. H. canadensis (goldenseal) was a strong inhibitor of the P450(2E1), and the inhibition appeared to be related to the presence of the alkaloids berberine, hydrastine and canadine in the extract. These compounds inhibited 2E1 with K(I) values ranging from 2.8 microM for hydrastine to 18 microM for berberine. The alkylamides present in E. purpurea and S. acmella also showed significant inhibition at concentrations as low as 25 microM, whereas the caffeic acid derivatives had no effect. Commercial green tea preparations, along with four of the individual tea catechins, were also examined and were found to have no effect on the activity of P450(2E1). PMID:17658211

  11. Cortical representation of the constituent structure of sentences

    PubMed Central

    Pallier, Christophe; Devauchelle, Anne-Dominique; Dehaene, Stanislas

    2011-01-01

    Linguistic analyses suggest that sentences are not mere strings of words but possess a hierarchical structure with constituents nested inside each other. We used functional magnetic resonance imaging (fMRI) to search for the cerebral mechanisms of this theoretical construct. We hypothesized that the neural assembly that encodes a constituent grows with its size, which can be approximately indexed by the number of words it encompasses. We therefore searched for brain regions where activation increased parametrically with the size of linguistic constituents, in response to a visual stream always comprising 12 written words or pseudowords. The results isolated a network of left-hemispheric regions that could be dissociated into two major subsets. Inferior frontal and posterior temporal regions showed constituent size effects regardless of whether actual content words were present or were replaced by pseudowords (jabberwocky stimuli). This observation suggests that these areas operate autonomously of other language areas and can extract abstract syntactic frames based on function words and morphological information alone. On the other hand, regions in the temporal pole, anterior superior temporal sulcus and temporo-parietal junction showed constituent size effect only in the presence of lexico-semantic information, suggesting that they may encode semantic constituents. In several inferior frontal and superior temporal regions, activation was delayed in response to the largest constituent structures, suggesting that nested linguistic structures take increasingly longer time to be computed and that these delays can be measured with fMRI. PMID:21224415

  12. Laboratory Evaluation of Larvicidal Activity of the Essential oil of Allium tuberosum Roots and its Selected Major Constituent Compounds Against Aedes albopictus (Diptera: Culicidae).

    PubMed

    Liu, Xin Chao; Zhou, Ligang; Liu, Qiyong; Liu, Zhi Long

    2015-05-01

    The aim of this research was to evaluate larvicidal activity of the essential oil of Allium tuberosum Rottler ex Sprengle roots and its constituents against larval mosquitoes (Aedes albopictus Skuse). Essential oil of A. tuberosum was obtained by hydrodistillation and analyzed by gas chromatography and gas chromatography-mass spectrometry. The major constituents of the oil were found to be sulfur-containing compounds, including allyl methyl trisulfide (35.19%), diallyl disulfide (28.31%), diallyl trisulfide (20.91%), and dimethyl trisulfide (12.33%). The essential oil of A. tuberosum exhibited larvicidal activity against the fourth-instar larvae of Ae. albopictus, with an LC50 value of 18 μg/ml. The constituents compounds-diallyl trisulfide (LC50 = 4 μg/ml) and diallyl disulfide (LC50 = 6 μg/ml)-possessed stronger larvicidal activity than allyl methyl trisulfide (LC50 = 27 μg/ml) and dimethyl trisulfide (LC50 = 35 μg/ml) against the fourth-instar larvae of Ae. albopictus. The results indicated that the essential oil of A. tuberosum and its major constituents have good potential as a source for natural larvicides. PMID:26334818

  13. Optimization of simultaneous ultrasonic-assisted extraction of water-soluble and fat-soluble characteristic constituents from Forsythiae Fructus Using response surface methodology and high-performance liquid chromatography

    PubMed Central

    Xia, Yong-Gang; Yang, Bing-You; Liang, Jun; Wang, Di; Yang, Qi; Kuang, Hai-Xue

    2014-01-01

    Background: The compounds (+)-pinoresinol-β-glucoside (1) forsythiaside, (2) phillyrin (3) and phillygenin (4) were elucidated to be the characteristic constituents for quality control of Forsythiae Fructus extract by chromatographic fingerprint in 2010 edition of Chinese Pharmacopoeia due to their numerous important pharmacological actions. It is of great interest to extract these medicinally active constituents from Forsythiae Fructus simultaneously. Materials and Methods: In this study, a new ultrasound-assisted extraction (UAE) method was developed for the simultaneous extraction of biological components 1-4 in Forsythiae Fructus. The quantitative effects of extraction time, ratio of liquid to solid, extraction temperature, and methanol concentration on yield of these four important biological constituents from Forsythiae Fructus were investigated using response surface methodology with Box-Behnken design. The compounds 1-4 extracted by UAE were quantitative analysis by high-performance liquid chromatography-photodiode array detect (HPLC-PAD), and overall desirability (OD), the geometric mean of the contents of four major biological components, was used as a marker to evaluate the extraction efficiency. Results: By solving the regression equation and analyzing 3-D plots, the optimum condition was at extraction temperature 70°C, time 60 min, ratio of liquid to solid 20, and methanol concentration 76.6%. Under these conditions, extraction yields of compounds 1-4 were 2.92 mg/g, 52.10 mg/g, 0.90 mg/g and 0.57 mg/g, respectively, which were in good agreement with the predicted OD values. In order to achieve a similar yield as UAE, soxhlet extraction required at least 6 h and maceration extraction required much longer time of 24 h. Established UAE method has been successfully applied to sample preparation for the quality control of Forsythiae Fructus. Additionally, a quadrupole time-of-flight mass spectrometry was applied to the structural confirmation of analytes

  14. Chemical Constituents of Malaysian U. cordata var. ferruginea and Their in Vitro α-Glucosidase Inhibitory Activities.

    PubMed

    Abdullah, Nur Hakimah; Salim, Fatimah; Ahmad, Rohaya

    2016-01-01

    Continuing our interest in the Uncaria genus, the phytochemistry and the in-vitro α-glucosidase inhibitory activities of Malaysian Uncaria cordata var. ferruginea were investigated. The phytochemical study of this plant, which employed various chromatographic techniques including recycling preparative HPLC, led to the isolation of ten compounds with diverse structures comprising three phenolic acids, two coumarins, three flavonoids, a terpene and an iridoid glycoside. These constituents were identified as 2-hydroxybenzoic acid or salicylic acid (1), 2,4-dihydroxybenzoic acid (2), 3,4-dihydroxybenzoic acid (3), scopoletin or 7-hydroxy-6-methoxy-coumarin (4), 3,4-dihydroxy-7-methoxycoumarin (5), quercetin (6), kaempferol (7), taxifolin (8), loganin (9) and β-sitosterol (10). Structure elucidation of the compounds was accomplished with the aid of 1D and 2D Nuclear Magnetic Resonance (NMR) spectral data and Ultraviolet-Visible (UV-Vis), Fourier Transform Infrared (FTIR) spectroscopy and mass spectrometry (MS). In the α-glucosidase inhibitory assay, the crude methanolic extract of the stems of the plant and its acetone fraction exhibited strong α-glucosidase inhibition activity of 87.7% and 89.2%, respectively, while its DCM fraction exhibited only moderate inhibition (75.3%) at a concentration of 1 mg/mL. The IC50 values of both fractions were found to be significantly lower than the standard acarbose suggesting the presence of potential α-glucosidase inhibitors. Selected compounds isolated from the active fractions were then subjected to α-glucosidase assay in which 2,4-dihydroxybenzoic acid and quercetin showed strong inhibitory effects against the enzyme with IC50 values of 549 and 556 μg/mL compared to acarbose (IC50 580 μg/mL) while loganin and scopoletin only showed weak α-glucosidase inhibition of 44.9% and 34.5%, respectively. This is the first report of the isolation of 2-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid and loganin from the genus and

  15. Traditional Chinese Nootropic Medicine Radix Polygalae and Its Active Constituent Onjisaponin B Reduce β-Amyloid Production and Improve Cognitive Impairments.

    PubMed

    Li, Xiaohang; Cui, Jin; Yu, Yang; Li, Wei; Hou, Yujun; Wang, Xin; Qin, Dapeng; Zhao, Cun; Yao, Xinsheng; Zhao, Jian; Pei, Gang

    2016-01-01

    Decline of cognitive function is the hallmark of Alzheimer's disease (AD), regardless of the pathological mechanism. Traditional Chinese medicine has been used to combat cognitive impairments and has been shown to improve learning and memory. Radix Polygalae (RAPO) is a typical and widely used herbal medicine. In this study, we aimed to follow the β-amyloid (Aβ) reduction activity to identify active constituent(s) of RAPO. We found that Onjisaponin B of RAPO functioned as RAPO to suppress Aβ production without direct inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) and γ-secretase activities. Our mechanistic study showed that Onjisaponin B promoted the degradation of amyloid precursor protein (APP). Further, oral administration of Onjisaponin B ameliorated Aβ pathology and behavioral defects in APP/PS1 mice. Taken together, our results indicate that Onjisaponin B is effective against AD, providing a new therapeutic agent for further drug discovery. PMID:26954017

  16. Traditional Chinese Nootropic Medicine Radix Polygalae and Its Active Constituent Onjisaponin B Reduce β-Amyloid Production and Improve Cognitive Impairments

    PubMed Central

    Li, Xiaohang; Cui, Jin; Yu, Yang; Li, Wei; Hou, Yujun; Wang, Xin; Qin, Dapeng; Zhao, Cun; Yao, Xinsheng; Zhao, Jian; Pei, Gang

    2016-01-01

    Decline of cognitive function is the hallmark of Alzheimer’s disease (AD), regardless of the pathological mechanism. Traditional Chinese medicine has been used to combat cognitive impairments and has been shown to improve learning and memory. Radix Polygalae (RAPO) is a typical and widely used herbal medicine. In this study, we aimed to follow the β-amyloid (Aβ) reduction activity to identify active constituent(s) of RAPO. We found that Onjisaponin B of RAPO functioned as RAPO to suppress Aβ production without direct inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) and γ-secretase activities. Our mechanistic study showed that Onjisaponin B promoted the degradation of amyloid precursor protein (APP). Further, oral administration of Onjisaponin B ameliorated Aβ pathology and behavioral defects in APP/PS1 mice. Taken together, our results indicate that Onjisaponin B is effective against AD, providing a new therapeutic agent for further drug discovery. PMID:26954017

  17. Antidiabetic Effects of Yam (Dioscorea batatas) and Its Active Constituent, Allantoin, in a Rat Model of Streptozotocin-Induced Diabetes.

    PubMed

    Go, Hyeon-Kyu; Rahman, Md Mahbubur; Kim, Gi-Beum; Na, Chong-Sam; Song, Choon-Ho; Kim, Jin-Shang; Kim, Shang-Jin; Kang, Hyung-Sub

    2015-10-01

    The objective of this study was to investigate the therapeutic efficacies of crude yam (Dioscorea batatas) powder (PY), water extract of yam (EY), and allantoin (the active constituent of yam) in streptozotocin (STZ)-induced diabetic rats with respect to glucose, insulin, glucagon-like peptide-1 (GLP-1), C-peptide, glycated hemoglobin (HbAlc), lipid metabolism, and oxidative stress. For this purpose, 50 rats were divided into five groups: normal control (NC), diabetic control (STZ), and STZ plus treatment groups (STZ + PY, STZ + EY, and STZ + allantoin). After treatment for one-month, there was a decrease in blood glucose: 385 ± 7 in STZ, 231 ± 3 in STZ + PY, 214 ± 11 in STZ + EY, and 243 ± 6 mg/dL in STZ + allantoin, respectively. There were significant statistical differences (p < 0.001) compared to STZ (100%): 60% in STZ + PY, 55% in STZ + EY, and 63% in STZ + allantoin. With groups in the same order, there were significant decreases (p < 0.001) in HbAlc (100% as 24.4 ± 0.6 ng/mL, 78%, 75%, and 77%), total cholesterol (100% as 122 ± 3 mg/dL, 70%, 67%, and 69%), and low-density lipoprotein (100% as 29 ± 1 mg/dL, 45%, 48%, and 38%). There were also significant increases (p < 0.001) in insulin (100% as 0.22 ± 0.00 ng/mL, 173%, 209%, and 177%), GLP-1 (100% as 18.4 ± 0.7 pmol/mL, 160%, 166%, and 162%), and C-peptide (100% as 2.56 ± 0.10 ng/mL, 129%, 132%, and 130%). The treatment effectively ameliorated antioxidant stress as shown by a significant decrease (p < 0.001) in malondialdehyde (100% as 7.25 ± 0.11 nmol/mL, 87%, 86%, and 85%) together with increases (p < 0.01) in superoxide dismutase (100% as 167 ± 6 IU/mL, 147%, 159%, and 145%) and reduced glutathione (100% as 167 ± 6 nmol/mL, 123%, 141%, and 140%). The results indicate that yam and allantoin have antidiabetic effects by modulating antioxidant activities, lipid profiles and by promoting the release of GLP-1, thereby improving the function of β-cells maintaining normal insulin and glucose

  18. Antidiabetic Effects of Yam (Dioscorea batatas) and Its Active Constituent, Allantoin, in a Rat Model of Streptozotocin-Induced Diabetes

    PubMed Central

    Go, Hyeon-Kyu; Rahman, Md. Mahbubur; Kim, Gi-Beum; Na, Chong-Sam; Song, Choon-Ho; Kim, Jin-Shang; Kim, Shang-Jin; Kang, Hyung-Sub

    2015-01-01

    The objective of this study was to investigate the therapeutic efficacies of crude yam (Dioscorea batatas) powder (PY), water extract of yam (EY), and allantoin (the active constituent of yam) in streptozotocin (STZ)-induced diabetic rats with respect to glucose, insulin, glucagon-like peptide-1 (GLP-1), C-peptide, glycated hemoglobin (HbAlc), lipid metabolism, and oxidative stress. For this purpose, 50 rats were divided into five groups: normal control (NC), diabetic control (STZ), and STZ plus treatment groups (STZ + PY, STZ + EY, and STZ + allantoin). After treatment for one-month, there was a decrease in blood glucose: 385 ± 7 in STZ, 231 ± 3 in STZ + PY, 214 ± 11 in STZ + EY, and 243 ± 6 mg/dL in STZ + allantoin, respectively. There were significant statistical differences (p < 0.001) compared to STZ (100%): 60% in STZ + PY, 55% in STZ + EY, and 63% in STZ + allantoin. With groups in the same order, there were significant decreases (p < 0.001) in HbAlc (100% as 24.4 ± 0.6 ng/mL, 78%, 75%, and 77%), total cholesterol (100% as 122 ± 3 mg/dL, 70%, 67%, and 69%), and low-density lipoprotein (100% as 29 ± 1 mg/dL, 45%, 48%, and 38%). There were also significant increases (p < 0.001) in insulin (100% as 0.22 ± 0.00 ng/mL, 173%, 209%, and 177%), GLP-1 (100% as 18.4 ± 0.7 pmol/mL, 160%, 166%, and 162%), and C-peptide (100% as 2.56 ± 0.10 ng/mL, 129%, 132%, and 130%). The treatment effectively ameliorated antioxidant stress as shown by a significant decrease (p < 0.001) in malondialdehyde (100% as 7.25 ± 0.11 nmol/mL, 87%, 86%, and 85%) together with increases (p < 0.01) in superoxide dismutase (100% as 167 ± 6 IU/mL, 147%, 159%, and 145%) and reduced glutathione (100% as 167 ± 6 nmol/mL, 123%, 141%, and 140%). The results indicate that yam and allantoin have antidiabetic effects by modulating antioxidant activities, lipid profiles and by promoting the release of GLP-1, thereby improving the function of β-cells maintaining normal insulin and glucose

  19. Enhancing growth, phytochemical constituents and aphid resistance capacity in cabbage with foliar application of eckol--a biologically active phenolic molecule from brown seaweed.

    PubMed

    Rengasamy, Kannan R R; Kulkarni, Manoj G; Pendota, Srinivasa C; Van Staden, Johannes

    2016-03-25

    Although foliar application of seaweed extracts on plant growth and development has and is extensively studied, reliable knowledge and understanding of the mode of action of particular compound(s) responsible for enhancing plant growth is lacking. A brown seaweed Ecklonia maxima is widely used commercially as a biostimulant to improve plant growth and crop protection. Eckol, a phenolic compound isolated from E. maxima has recently shown stimulatory effects in maize, indicating its potential use as a plant biostimulant. Cabbage is a widely cultivated vegetable crop throughout the world, which requires high input of fertilizers and is susceptible to several aphid borne diseases. This study was conducted to evaluate the effect of foliar application of eckol on the growth, phytochemical constituents and myrosinase activity (aphid resistance capacity) of commercially cultivated cabbage. Foliar application of eckol (10(-6) M) significantly enhanced shoot and root length, shoot and root fresh and dry weight, leaf area and leaf number. This treatment also showed a significant increase in photosynthetic pigments (chlorophyll 'a', chlorophyll 'b', total chlorophyll and carotenoid) compared to the untreated plants. The levels of protein, proline and iridoid glycosides were significantly higher in cabbage leaves with eckol treatment. All the control plants were severely infested with cabbage aphid (Brevicoryne brassicae) but no infestation was observed on the eckol-sprayed plants, which can be attributed to an increase in myrosinase activity. This study reveals dual effects (plant growth promoting and insect repelling) of eckol on cabbage plants that need further investigations both under field conditions and in other brassicaceous species. PMID:26585339

  20. Autoignition response of n-butanol and its blend with primary reference fuel constituents of gasoline.

    SciTech Connect

    Kumar, Kamal; Zhang, Yu; Sung, Chi -Jen; Pitz, William J.

    2015-04-13

    We study the influence of blending n-butanol on the ignition delay times of n-heptane and iso-octane, the primary reference fuels for gasoline. The ignition delay times are measured using a rapid compression machine, with an emphasis on the low-to-intermediate temperature conditions. The experiments are conducted at equivalence ratios of 0.4 and 1.0, for a compressed pressure of 20 bar, with the temperatures at the end of compression ranging from 613 K to 979 K. The effect of n-butanol addition on the development of the two-stage ignition characteristics for the two primary reference fuels is also examined. The experimental results are compared to predictions obtained using a detailed chemical kinetic mechanism, which has been obtained by a systematic merger of previously reported base models for the combustion of the individual fuel constituents. In conclusion, a sensitivity analysis on the base, and the merged models, is also performed to understand the dependence of autoignition delay times on the model parameters.

  1. Search for constituents with neurotrophic factor-potentiating activity from the medicinal plants of paraguay and Thailand.

    PubMed

    Li, Yushan; Ohizumi, Yasushi

    2004-07-01

    20 medicinal plants of Paraguay and 3 medicinal plants of Thailand were examined on nerve growth factor (NGF)-potentiating activities in PC12D cells. The trail results demonstrated that the methanol extracts of four plants, Verbena littoralis, Scoparia dulcis, Artemisia absinthium and Garcinia xanthochymus, markedly enhanced the neurite outgrowth induced by NGF from PC12D cells. Furthermore, utilizing the bioactivity-guided separation we successfully isolated 32, 4 and 5 constituents from V. littoralis, S. dulcis and G. xanthochymus, respectively, including nine iridoid and iridoid glucosides (1-9), two dihydrochalcone dimers (10 and 11), two flavonoids and three flavonoid glycosides (12-16), two sterols (17 and 18), ten triterpenoids (19-28), five xanthones (29-33), one naphthoquinone (34), one benzenepropanamide (35), four phenylethanoid glycosides (36-39) and two other compounds (40 and 41). Among which, 15 compounds (1-4, 10-11, 14-18, 29-31 and 34) were new natural products. The results of pharmacological trails verified that littoralisone (1), gelsemiol (5), 7a-hydroxysemperoside aglucone (6), verbenachalcone (10), littorachalcone (11), stigmast-5-ene 3beta,7alpha,22alpha-triol (18), ursolic acid (19), 3beta-hydroxyurs-11-en-28,13beta-olide (24), oleanolic acid (25), 2alpha,3beta-dihydroxyolean-12-en-28-oic acid (26), 1,4,5,6-tetrahydroxy-7,8-di(3-methylbut-2-enyl)xanthone (29), 1,2,6-trihydroxy-5-methoxy-7-(3-methylbut-2-enyl)xanthone (30), 1,3,5,6-tetrahydroxy-4,7,8-tri(3-methyl-2-butenyl)xanthone (31), 12b-hydroxy-des-D-garcigerrin A (32), garciniaxanthone E (33) and (4R)-4,9-dihydroxy-8-methoxy-alpha-lapachone (34) elicited marked enhancement of NGF-mediated neurite outgrowth in PC12D cells. These substances may contribute to the basic study and the medicinal development for the neurodegenerative disorder. PMID:15235225

  2. Mephedrone interactions with cocaine: prior exposure to ‘bath salt’ constituent enhances cocaine-induced locomotor activation in rats

    PubMed Central

    Gregg, Ryan A.; Tallarida, Christopher S.; Reitz, Allen B.; Rawls, Scott M.

    2014-01-01

    Concurrent use of mephedrone (4-methylmethcathinone) (MEPH) and established drugs of abuse is now commonplace, but knowledge about interactions between these drugs is sparse. The present study was designed to test the hypothesis that prior MEPH exposure enhances the locomotor-stimulant effects of cocaine and methamphetamine (METH). For cocaine experiments, rats pretreated with saline, cocaine (15 mg/kg), or MEPH (15 mg/kg) for 5 days were injected with cocaine after 10 days of drug absence. For METH experiments, rats pretreated with saline, METH (2 mg/kg), or MEPH (15 mg/kg) were injected with METH after 10 days of drug absence. Cocaine challenge produced greater locomotor activity following pretreatment with cocaine or MEPH than following pretreatment with saline. METH challenge produced greater locomotor activity following METH pretreatment than following saline pretreatment; however, locomotor activity in rats pretreated with MEPH or saline and then challenged with METH was not significantly different. The locomotor response to MEPH (15 mg/kg) was not significantly affected by pretreatment with cocaine (15 mg/kg) or METH (0.5, 2 mg/kg). The present demonstration that cocaine-induced locomotor activation is enhanced by prior MEPH exposure suggests that MEPH cross-sensitizes to cocaine and increases cocaine efficacy. Interestingly, MEPH cross-sensitization was not bi-directional and did not extend to METH, suggesting the phenomenon is sensitive to specific psychostimulants. PMID:24126218

  3. Mephedrone interactions with cocaine: prior exposure to the 'bath salt' constituent enhances cocaine-induced locomotor activation in rats.

    PubMed

    Gregg, Ryan A; Tallarida, Christopher S; Reitz, Allen B; Rawls, Scott M

    2013-12-01

    Concurrent use of mephedrone (4-methylmethcathinone; MEPH) and established drugs of abuse is now commonplace, but knowledge about interactions between these drugs is sparse. The present study was designed to test the hypothesis that prior MEPH exposure enhances the locomotor-stimulant effects of cocaine and methamphetamine (METH). For cocaine experiments, rats pretreated with saline, cocaine (15 mg/kg), or MEPH (15 mg/kg) for 5 days were injected with cocaine after 10 days of drug absence. For METH experiments, rats pretreated with saline, METH (2 mg/kg), or MEPH (15 mg/kg) were injected with METH after 10 days of drug absence. Cocaine challenge produced greater locomotor activity after pretreatment with cocaine or MEPH than after pretreatment with saline. METH challenge produced greater locomotor activity after METH pretreatment than after saline pretreatment; however, locomotor activity in rats pretreated with MEPH or saline and then challenged with METH was not significantly different. The locomotor response to MEPH (15 mg/kg) was not significantly affected by pretreatment with cocaine (15 mg/kg) or METH (0.5, 2 mg/kg). The present demonstration that cocaine-induced locomotor activation is enhanced by prior MEPH exposure suggests that MEPH cross-sensitizes to cocaine and increases cocaine efficacy. Interestingly, MEPH cross-sensitization was not bidirectional and did not extend to METH, suggesting that the phenomenon is sensitive to specific psychostimulants. PMID:24126218

  4. Antimicrobial Activity of Tulsi (Ocimum tenuiflorum) Essential Oil and Their Major Constituents against Three Species of Bacteria.

    PubMed

    Yamani, Hanaa A; Pang, Edwin C; Mantri, Nitin; Deighton, Margaret A

    2016-01-01

    In recent years scientists worldwide have realized that the effective life span of any antimicrobial agent is limited, due to increasing development of resistance by microorganisms. Consequently, numerous studies have been conducted to find new alternative sources of antimicrobial agents, especially from plants. The aims of this project were to examine the antimicrobial properties of essential oils distilled from Australian-grown Ocimum tenuiflorum (Tulsi), to quantify the volatile components present in flower spikes, leaves and the essential oil, and to investigate the compounds responsible for any activity. Broth micro-dilution was used to determine the minimum inhibitory concentration (MIC) of Tulsi essential oil against selected microbial pathogens. The oils, at concentrations of 4.5 and 2.25% completely inhibited the growth of Staphylococcus aureus (including MRSA) and Escherichia coli, while the same concentrations only partly inhibited the growth of Pseudomonas aeruginosa. Of 54 compounds identified in Tulsi leaves, flower spikes, or essential oil, three are proposed to be responsible for this activity; camphor, eucalyptol and eugenol. Since S. aureus (including MRSA), P. aeruginosa and E. coli are major pathogens causing skin and soft tissue infections, Tulsi essential oil could be a valuable topical antimicrobial agent for management of skin infections caused by these organisms. PMID:27242708

  5. Antimicrobial Activity of Tulsi (Ocimum tenuiflorum) Essential Oil and Their Major Constituents against Three Species of Bacteria

    PubMed Central

    Yamani, Hanaa A.; Pang, Edwin C.; Mantri, Nitin; Deighton, Margaret A.

    2016-01-01

    In recent years scientists worldwide have realized that the effective life span of any antimicrobial agent is limited, due to increasing development of resistance by microorganisms. Consequently, numerous studies have been conducted to find new alternative sources of antimicrobial agents, especially from plants. The aims of this project were to examine the antimicrobial properties of essential oils distilled from Australian-grown Ocimum tenuiflorum (Tulsi), to quantify the volatile components present in flower spikes, leaves and the essential oil, and to investigate the compounds responsible for any activity. Broth micro-dilution was used to determine the minimum inhibitory concentration (MIC) of Tulsi essential oil against selected microbial pathogens. The oils, at concentrations of 4.5 and 2.25% completely inhibited the growth of Staphylococcus aureus (including MRSA) and Escherichia coli, while the same concentrations only partly inhibited the growth of Pseudomonas aeruginosa. Of 54 compounds identified in Tulsi leaves, flower spikes, or essential oil, three are proposed to be responsible for this activity; camphor, eucalyptol and eugenol. Since S. aureus (including MRSA), P. aeruginosa and E. coli are major pathogens causing skin and soft tissue infections, Tulsi essential oil could be a valuable topical antimicrobial agent for management of skin infections caused by these organisms. PMID:27242708

  6. Antibacterial activity of essential oils, their blends and mixtures of their main constituents against some strains supporting livestock mastitis.

    PubMed

    Fratini, Filippo; Casella, Sergio; Leonardi, Michele; Pisseri, Francesca; Ebani, Valentina Virginia; Pistelli, Laura; Pistelli, Luisa

    2014-07-01

    Ten of the most known and used commercial essential oils (Cinnamomum zeylanicum L., Citrus bergamia Risso, Eucalyptus globulus Labill., Foeniculum vulgare Mill., Origanum majorana L., Origanum vulgare L., Rosmarinus officinalis L., Satureja montana L., Thymus vulgaris L. ct. carvacrol, Thymus vulgaris L. ct. thymol) were tested against six bacteria strains Staphylococcus aureus, Staphylococcus chromogenes, Staphylococcus sciuri, Staphylococcus warneri, Staphylococcus xylosus and Escherichia coli, responsible for mastitis in animals. The best results were achieved by S. montana, T. vulgaris ct. thymol and O. vulgare. Two binary mixtures of essential oils (EOs) were prepared of S. montana and T. vulgaris ct. thymol (ST) and of S. montana and O. vulgare (SO). The ST mixture exhibited the best inhibitory activity against all the tested bacterial strains. Two artificial mixtures of carvacrol/thymol (AB) and carvacrol/thymol/p-cymene (CD) were prepared and tested against all of the bacterial strains used. The results exhibited a general reduction of the inhibitory activity of mixture AB, although not reaching the inhibition of the ST and SO mixtures. However the mixture CD presented an apparent strong inhibition against S. aureus and S. sciuri. The EO mixtures and the mixture CD represent promising phytotherapic approaches against bacteria strains responsible for environmental mastitis. PMID:24727086

  7. Dendrotoxin acceptor from bovine synaptic plasma membranes. Binding properties, purification and subunit composition of a putative constituent of certain voltage-activated K+ channels.

    PubMed Central

    Parcej, D N; Dolly, J O

    1989-01-01

    Dendrotoxin is a snake polypeptide that blocks selectively and potently certain voltage-sensitive, fast-activating K+ channels in the nervous system, where it binds with high affinity to membranous acceptors. Herein, the acceptor protein for dendrotoxin in bovine synaptic membranes is solubilized in active form and its complete purification achieved by affinity chromatography, involving a novel elution procedure. This putative K+-channel constituent is shown to be a large oligomeric glycoprotein containing two major subunits, with Mr values of 75,000 and 37,000. Images Fig. 2. PMID:2930493

  8. Anointing chemicals and ectoparasites: responses by ticks and mosquitoes to Citrus (Rutaceae) peel exudates and monoterpene constituents

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Some birds and mammals rub their feathers or fur with the fruits or leaves of Citrus spp. or other Rutaceae, presumably to deter ectoparasites. We measured avoidance and other responses by the lone star tick (Amblyomma americanum) and the yellow fever mosquito (Aedes aegypti) to lemon peel exudate a...

  9. Anti-herpes virus activities of bioactive fraction and isolated pure constituent of Mallotus peltatus: an ethnomedicine from Andaman Islands

    PubMed Central

    2012-01-01

    Background Viral infections, particularly the infections caused by herpes simplex virus (HSV), represent one of the most serious public health concerns globally because of their devastating impact. The aim of this study was to evaluate the antiviral potential of methanolic crude extract of an ethnomedicine Mallotus peltatus, its active fraction and pure compound, against HSV-1 F and HSV-2 G. Result The cytotoxicity (CC50, the concentration of 50% cellular toxicity), antiviral effective concentration (EC50, the concentration required to achieve 50% protection against virus-induced cytopathic effect), plaque reduction and the selectivity index (SI, the ratio of CC50 and EC50) was determined. Results showed that the crude methanolic extract of M. peltatus possessed weak anti-HSV activity. In contrast, the active fraction A and isolated ursolic acid from fraction A exhibited potent antiherpesvirus activity against both HSV-1 (EC50 = 7.8 and 5.5 μg/ml; SI = 22.3 and 20) and HSV-2 (EC50 = 8.2 and 5.8 μg/ml, and SI = 21.2 and 18.97). The fraction A and isolated ursolic acid (10 μg/ml) inhibited plaque formation of HSV-1 and HSV-2 at more than 80% levels, with a dose dependent antiviral activity, compared to acyclovir. The time response study revealed that the anti-HSV activity of fraction A and isolated ursolic acid is highest at 2–5 h post-infection. Moreover, the time kinetics study by indirect immunofluorescence assay showed a characteristic pattern of small foci of single fluorescent cells in fraction A- treated virus infected cells at 2 h and 4 h post-infection, suggesting drug inhibited viral dissemination. Further, the PCR study with infected cell cultures treated with fraction A and isolated ursolic acid at various time intervals, failed to show amplification at 48–72 h, like acyclovir treated HSV-infected cells. Moreover, fraction A or isolated ursolic acid showed no interaction in combination with acyclovir. Conclusion

  10. Therapeutic Implications of Black Seed and Its Constituent Thymoquinone in the Prevention of Cancer through Inactivation and Activation of Molecular Pathways

    PubMed Central

    Rahmani, Arshad H.; Alzohairy, Mohammad A.; Khan, Masood A.; Aly, Salah M.

    2014-01-01

    The cancer is probably the most dreaded disease in both men and women and also major health problem worldwide. Despite its high prevalence, the exact molecular mechanisms of the development and progression are not fully understood. The current chemotherapy/radiotherapy regime used to treat cancer shows adverse side effect and may alter gene functions. Natural products are generally safe, effective, and less expensive substitutes of anticancer chemotherapeutics. Based on previous studies of their potential therapeutic uses, Nigella sativa and its constituents may be proved as good therapeutic options in the prevention of cancer. Black seeds are used as staple food in the Middle Eastern Countries for thousands of years and also in the treatment of diseases. Earlier studies have shown that N. sativa and its constituent thymoquinone (TQ) have important roles in the prevention and treatment of cancer by modulating cell signaling pathways. In this review, we summarize the role of N. sativa and its constituents TQ in the prevention of cancer through the activation or inactivation of molecular cell signaling pathways. PMID:24959190

  11. Comparison of the anti-inflammatory active constituents and hepatotoxic pyrrolizidine alkaloids in two Senecio plants and their preparations by LC-UV and LC-MS.

    PubMed

    Chen, Pinghong; Wang, Yi; Chen, Lulin; Jiang, Wei; Niu, Yan; Shao, Qing; Gao, Lu; Zhao, Quancheng; Yan, Licheng; Wang, Shufang

    2015-11-10

    Two Senecio plants, Senecio cannabifolius Less. and its variety S. cannabifolius Less. var. integrifolius (Kiodz.) Kidam., were both used as the raw material of Feining granule, a traditional Chinese medicine product for treating respiratory diseases. In this study, the chemical profiles of these two plants were investigated and compared by liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR). A total number of 83 constituents, including 55 organic acids, 11 flavonoids, 4 alkaloids, 3 terpenes and 10 other types of compounds, were characterized. The results indicated that the levels of most flavonoids were higher in S. cannabifolius than in S. cannabifolius var. integrifolius, however, the levels of hepatotoxic pyrrolizidine alkaloids (PAs) were higher in S. cannabifolius var. integrifolius than in S. cannabifolius. Fifteen constituents were evaluated on lipopolysaccharides (LPS) induced RAW 264.7 cells, and eleven of them showed inhibition effect against nitric oxide (NO) production. Finally, the levels of ten major constituents (including seven anti-inflammatory active ones) and two PAs in Feining granule from two Senecio plants were determined and compared by the LC-UV and LC-MS methods, respectively. It was found that one organic acid (homogentisic acid) and two PAs (seneciphylline and senecionine) had higher contents in the preparation of S. cannabifolius var. integrifolius than in that of S. cannabifolius, however, the situations were inverse for the levels of four organic acids and flavonoids (chlorogenic acid, hyperoside, isoquercitrin, and isochlorogenic acid B). Based on the above results, S. cannabifolius might be a better raw material for Feining granule than S. cannabifolius var. integrifolius, because it contained more anti-inflammatory constituents and less hepatotoxic PAs than the latter. However, more pharmacological evaluations should be carried out to support the selection. The results in this study were helpful

  12. Antifungal activity and computational study of constituents from Piper divaricatum essential oil against Fusarium infection in black pepper.

    PubMed

    da Silva, Joyce Kelly R; Silva, José Rogério A; Nascimento, Soelange B; da Luz, Shirlley F M; Meireles, Erisléia N; Alves, Cláudio N; Ramos, Alessandra R; Maia, José Guilherme S

    2014-01-01

    Fusarium disease causes considerable losses in the cultivation of Piper nigrum, the black pepper used in the culinary world. Brazil was the largest producer of black pepper, but in recent years has lost this hegemony, with a significant reduction in its production, due to the ravages produced by the Fusarium solani f. sp. piperis, the fungus which causes this disease. Scientific research seeks new alternatives for the control and the existence of other Piper species in the Brazilian Amazon, resistant to disease, are being considered in this context. The main constituents of the oil of Piper divaricatum are methyleugenol (75.0%) and eugenol (10.0%). The oil and these two main constituents were tested individually at concentrations of 0.25 to 2.5 mg/mL against F. solani f. sp. piperis, exhibiting strong antifungal index, from 18.0% to 100.0%. The 3D structure of the β-glucosidase from Fusarium solani f. sp. piperis, obtained by homology modeling, was used for molecular docking and molecular electrostatic potential calculations in order to determine the binding energy of the natural substrates glucose, methyleugenol and eugenol. The results showed that β-glucosidase (Asp45, Arg113, Lys146, Tyr193, Asp225, Trp226 and Leu99) residues play an important role in the interactions that occur between the protein-substrate and the engenol and methyleugenol inhibitors, justifying the antifungal action of these two phenylpropenes against Fusarium solani f. sp. piperis. PMID:25375334

  13. Variation of the Phytochemical Constituents and Antioxidant Activities of Zingiber officinale var. rubrum Theilade Associated with Different Drying Methods and Polyphenol Oxidase Activity.

    PubMed

    Ghasemzadeh, Ali; Jaafar, Hawa Z E; Rahmat, Asmah

    2016-01-01

    The effects of different drying methods (freeze drying, vacuum oven drying, and shade drying) on the phytochemical constituents associated with the antioxidant activities of Z. officinale var. rubrum Theilade were evaluated to determine the optimal drying process for these rhizomes. Total flavonoid content (TFC), total phenolic content (TPC), and polyphenol oxidase (PPO) activity were measured using the spectrophotometric method. Individual phenolic acids and flavonoids, 6- and 8-gingerol and shogaol were identified by ultra-high performance liquid chromatography method. Ferric reducing antioxidant potential (FRAP) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays were used for the evaluation of antioxidant activities. The highest reduction in moisture content was observed after freeze drying (82.97%), followed by vacuum oven drying (80.43%) and shade drying (72.65%). The highest TPC, TFC, and 6- and 8-shogaol contents were observed in samples dried by the vacuum oven drying method compared to other drying methods. The highest content of 6- and 8-gingerol was observed after freeze drying, followed by vacuum oven drying and shade drying methods. Fresh samples had the highest PPO activity and lowest content of flavonoid and phenolic acid compounds compared to dried samples. Rhizomes dried by the vacuum oven drying method represent the highest DPPH (52.9%) and FRAP activities (566.5 μM of Fe (II)/g DM), followed by freeze drying (48.3% and 527.1 μM of Fe (II)/g DM, respectively) and shade drying methods (37.64% and 471.8 μM of Fe (II)/g DM, respectively) with IC50 values of 27.2, 29.1, and 34.8 μg/mL, respectively. Negative and significant correlations were observed between PPO and antioxidant activity of rhizomes. Vacuum oven dried rhizomes can be utilized as an ingredient for the development of value-added food products as they contain high contents of phytochemicals with valuable antioxidant potential. PMID:27322227

  14. Antihypercholesterolemic and Antioxidative Potential of an Extract of the Plant, Piper betle, and Its Active Constituent, Eugenol, in Triton WR-1339-Induced Hypercholesterolemia in Experimental Rats

    PubMed Central

    Venkadeswaran, Karuppasamy; Muralidharan, Arumugam Ramachandran; Annadurai, Thangaraj; Ruban, Vasanthakumar Vasantha; Sundararajan, Mahalingam; Anandhi, Ramalingam; Thomas, Philip A.; Geraldine, Pitchairaj

    2014-01-01

    Hypercholesterolemia is a dominant risk factor for atherosclerosis and cardiovascular diseases. In the present study, the putative antihypercholesterolemic and antioxidative properties of an ethanolic extract of Piper betle and of its active constituent, eugenol, were evaluated in experimental hypercholesterolemia induced by a single intraperitoneal injection of Triton WR-1339 (300 mg/kg b.wt) in Wistar rats. Saline-treated hypercholesterolemic rats revealed significantly higher mean blood/serum levels of glucose, total cholesterol, triglycerides, low density and very low density lipoprotein cholesterol, and of serum hepatic marker enzymes; in addition, significantly lower mean serum levels of high density lipoprotein cholesterol and significantly lower mean activities of enzymatic antioxidants and nonenzymatic antioxidants were noted in hepatic tissue samples from saline-treated hypercholesterolemic rats, compared to controls. However, in hypercholesterolemic rats receiving the Piper betle extract (500 mg/kg b.wt) or eugenol (5 mg/kg b.wt) for seven days orally, all these parameters were significantly better than those in saline-treated hypercholesterolemic rats. The hypercholesterolemia-ameliorating effect was better defined in eugenol-treated than in Piper betle extract-treated rats, being as effective as that of the standard lipid-lowering drug, lovastatin (10 mg/kg b.wt). These results suggest that eugenol, an active constituent of the Piper betle extract, possesses antihypercholesterolemic and other activities in experimental hypercholesterolemic Wistar rats. PMID:24523820

  15. New Coumarin Derivatives and Other Constituents from the Stem Bark of Zanthoxylum avicennae: Effects on Neutrophil Pro-Inflammatory Responses

    PubMed Central

    Chen, Jih-Jung; Yang, Chieh-Kai; Kuo, Yueh-Hsiung; Hwang, Tsong-Long; Kuo, Wen-Lung; Lim, Yun-Ping; Sung, Ping-Jyun; Chang, Tsung-Hsien; Cheng, Ming-Jen

    2015-01-01

    Three new coumarin derivatives, 8-formylalloxanthoxyletin (1), avicennone (2), and (Z)-avicennone (3), have been isolated from the stem bark of Zanthoxylum avicennae (Z. avicennae), together with 15 known compounds (4–18). The structures of these new compounds were determined through spectroscopic and MS analyses. Compounds 1, 4, 9, 12, and 15 exhibited inhibition (half maximal inhibitory concentration (IC50) values ≤7.65 µg/mL) of superoxide anion generation by human neutrophils in response to formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB). Compounds 1, 2, 4, 8 and 9 inhibited fMLP/CB-induced elastase release with IC50 values ≤8.17 µg/mL. This investigation reveals bioactive isolates (especially 1, 2, 4, 8, 9, 12 and 15) could be further developed as potential candidates for the treatment or prevention of various inflammatory diseases. PMID:25938967

  16. Identification and Molecular Characterization of the Homogentisate Pathway Responsible for Pyomelanin Production, the Major Melanin Constituents in Aeromonas media WS

    PubMed Central

    Wang, He; Qiao, Yunqian; Chai, Baozhong; Qiu, Chenxi; Chen, Xiangdong

    2015-01-01

    The pigmentation of many Aeromonas species has been thought to be due to the production of a L-DOPA (L-3,4-dihydroxyphenylalanine) based melanin. However, in this study we found that although L-DOPA synthesis occurs in the high-melanin-yielding Aeromonas media strain WS, it plays a minor, if any, role in pigmentation. Instead, the pigmentation of A. media strain WS is due to the production of pyomelanin through HGA (homogentisate). Gene products of phhA (encodes phenylalanine hydroxylase), tyrB and aspC (both encode aromatic amino acid aminotransferase), and hppD (encodes 4-hydroxyphenylpyruvate dioxygenase) constitute a linear pathway of converting phenylalanine to HGA and disruption of any one of these genes impairs or blocks pigmentation of A. media strain WS. This HGA biosynthesis pathway is widely distributed in Aeromonas, but HGA is only detectable in the cultures of pigmented Aeromonas species. Heterologous expression of HppD from both pigmented and non-pigmented Aeromonas species in E. coli leads to the production of pyomelanin and thus pigmentation, suggesting that most Aeromonas species have the critical enzymes to produce pyomelanin through HGA. Taken together, we have identified a widely conserved biosynthesis pathway of HGA based pyomelanin in Aeromonas that may be responsible for pigmentation of many Aeromonas species. PMID:25793756

  17. Solar activity, the QBO, and tropospheric responses

    NASA Technical Reports Server (NTRS)

    Tinsley, Brian A.; Brown, Geoffrey M.; Scherrer, Philip H.

    1989-01-01

    The suggestion that galactic cosmic rays (GCR) as modulated by the solar wind are the carriers of the component of solar variability that affects weather and climate has been discussed in the literature for 30 years, and there is now a considerable body of evidence that supports it. Variations of GCR occur with the 11 year solar cycle, matching the time scale of recent results for atmospheric variations, as modulated by the quasibiennial oscillation of equatorial stratospheric winds (the QBO). Variations in GCR occur on the time scale of centuries with a well defined peak in the coldest decade of the little ice age. New evidence is presented on the meteorological responses to GCR variations on the time scale of a few days. These responses include changes in the vertical temperature profile in the troposphere and lower stratosphere in the two days following solar flare related high speed plasma streams and associated GCR decreases, and in decreases in Vorticity Area Index (VAI) following Forbush decreases of GCR. The occurrence of correlations of GCR and meteorological responses on all three time scales strengthens the hypothesis of GCR as carriers of solar variability to the lower atmosphere. Both short and long term tropospheric responses are understandable as changes in the intensity of cyclonic storms initiated by mechanisms involving cloud microphysical and cloud electrification processes, due to changes in local ion production from changes in GCR fluxes and other high energy particles in the MeV to low GeV range. The nature of these mechanisms remains undetermined. Possible stratospheric wind (particularly QBO) effects on the transport of HNO3 and other constituents incorporated in cluster ions and possible condensation and freezing nuclei are considered as relevant to the long term variations.

  18. Cannabidiol, a Major Non-Psychotropic Cannabis Constituent Enhances Fracture Healing and Stimulates Lysyl Hydroxylase Activity in Osteoblasts.

    PubMed

    Kogan, Natalya M; Melamed, Eitan; Wasserman, Elad; Raphael, Bitya; Breuer, Aviva; Stok, Kathryn S; Sondergaard, Rachel; Escudero, Ana V Villarreal; Baraghithy, Saja; Attar-Namdar, Malka; Friedlander-Barenboim, Silvina; Mathavan, Neashan; Isaksson, Hanna; Mechoulam, Raphael; Müller, Ralph; Bajayo, Alon; Gabet, Yankel; Bab, Itai

    2015-10-01

    Cannabinoid ligands regulate bone mass, but skeletal effects of cannabis (marijuana and hashish) have not been reported. Bone fractures are highly prevalent, involving prolonged immobilization and discomfort. Here we report that the major non-psychoactive cannabis constituent, cannabidiol (CBD), enhances the biomechanical properties of healing rat mid-femoral fractures. The maximal load and work-to-failure, but not the stiffness, of femurs from rats given a mixture of CBD and Δ(9) -tetrahydrocannabinol (THC) for 8 weeks were markedly increased by CBD. This effect is not shared by THC (the psychoactive component of cannabis), but THC potentiates the CBD stimulated work-to-failure at 6 weeks postfracture followed by attenuation of the CBD effect at 8 weeks. Using micro-computed tomography (μCT), the fracture callus size was transiently reduced by either CBD or THC 4 weeks after fracture but reached control level after 6 and 8 weeks. The callus material density was unaffected by CBD and/or THC. By contrast, CBD stimulated mRNA expression of Plod1 in primary osteoblast cultures, encoding an enzyme that catalyzes lysine hydroxylation, which is in turn involved in collagen crosslinking and stabilization. Using Fourier transform infrared (FTIR) spectroscopy we confirmed the increase in collagen crosslink ratio by CBD, which is likely to contribute to the improved biomechanical properties of the fracture callus. Taken together, these data show that CBD leads to improvement in fracture healing and demonstrate the critical mechanical role of collagen crosslinking enzymes. PMID:25801536

  19. Compilation of data to estimate groundwater migration potential for constituents in active liquid discharges at the Hanford Site

    SciTech Connect

    Ames, L.L.; Serne, R.J.

    1991-03-01

    A preliminary characterization of the constituents present in the 33 liquid waste streams at the US Department of Energy's Hanford Site has been completed by Westinghouse Hanford Company. In addition, Westinghouse Hanford has summarized the soil characteristics based on drill logs collected at each site that receives these liquid wastes. Literature searches were conducted and available Hanford-specific data were tabulated and reviewed. General literature on organic chemicals present in the liquid waste streams was also reviewed. Using all of this information, Pacific Northwest Laboratory has developed a best estimate of the transport characteristics (water solubility and soil adsorption properties) for those radionuclides and inorganic and organic chemicals identified in the various waste streams. We assume that the potential for transport is qualified through the four geochemical parameters: solubility, distribution coefficient, persistence (radiogenic or biochemical half-life), and volatility. Summary tables of these parameters are presented for more than 50 inorganic and radioactive species and more than 50 organic compounds identified in the liquid waste streams. Brief descriptions of the chemical characteristics of Hanford sediments, solubility, and adsorption processes, and of how geochemical parameters are used to estimate migration in groundwater-sediment environments are also presented. Groundwater monitoring data are tabulated for wells neighboring the facilities that receive the liquid wastes. 91 refs., 16 figs., 23 tabs.

  20. Inhibition of human carcinoma cell growth and DNA synthesis by silibinin, an active constituent of milk thistle: comparison with silymarin.

    PubMed

    Bhatia, N; Zhao, J; Wolf, D M; Agarwal, R

    1999-12-01

    Several studies from our laboratory have shown the cancer chemopreventive and anti-carcinogenic effects of silymarin, a flavonoid antioxidant isolated from milk thistle, in long-term tumorigenesis models and in human prostate, breast and cervical carcinoma cells. Since silymarin is composed mainly of silibinin with small amounts of other stereoisomers of silibinin, in the present communication, studies were performed to assess whether the cancer preventive and anti-carcinogenic effects of silymarin are due to its major component silibinin. Treatment of different prostate, breast, and cervical human carcinoma cells with silibinin resulted in a highly significant inhibition of both cell growth and DNA synthesis in a time-dependent manner with large loss of cell viability only in case of cervical carcinoma cells. When compared with silymarin, these effects of silibinin were consistent and comparable in terms of cell growth and DNA synthesis inhibition, and loss of cell viability. Based on the comparable results of silibinin and silymarin, we suggest that the cancer chemopreventive and anti-carcinogenic effects of silymarin reported earlier are due to the main constituent silibinin. PMID:10660092

  1. Acute Toxicity and Determination of the Active Constituents of Aqueous Extract of Uncaria tomentosa Bark in Hyphessobrycon eques

    PubMed Central

    Claudiano, Gustavo S.; Marcusso, Paulo F.; Ikefuti, Cynthia; Ortega, George G.; Eto, Silas F.; da Cruz, Claudinei; Moraes, Juliet R. E.; Moraes, Flávio R.; Fernandes, João B. K.

    2014-01-01

    Uncaria tomentosa is a medicinal plant used in folk medicine by Amazon tribes. In this study the constituents of aqueous extract of U. tomentosa bark were quantified by chromatographic technique and its lethal concentration 50 (48 h) in Hyphessobrycon eques was determined. The chromatography showed high levels of oxindole alkaloids, quinovic acid glycosides, and low molecular weight polyphenols. The CL50 48 h was 1816 mg/L. Fish showed behavior changes at concentrations above 2000 mg/L, accompanied by a significant decrease of dissolved oxygen. At the highest concentration 100% mortality was observed attributed to oxygen reduction by the amount of oxindole alkaloids, polyphenols accumulation of the extract in the gills, and the interaction of these compounds with dopamine. In conclusion, the aqueous extract of U. tomentosa did not alter the chemical components and it was shown that U. tomentosa has low toxicity to H. eques; therefore, it can be used safely in this species. PMID:24734041

  2. Acute Toxicity and Determination of the Active Constituents of Aqueous Extract of Uncaria tomentosa Bark in Hyphessobrycon eques.

    PubMed

    Yunis Aguinaga, Jefferson; Claudiano, Gustavo S; Marcusso, Paulo F; Ikefuti, Cynthia; Ortega, George G; Eto, Silas F; da Cruz, Claudinei; Moraes, Juliet R E; Moraes, Flávio R; Fernandes, João B K

    2014-01-01

    Uncaria tomentosa is a medicinal plant used in folk medicine by Amazon tribes. In this study the constituents of aqueous extract of U. tomentosa bark were quantified by chromatographic technique and its lethal concentration 50 (48 h) in Hyphessobrycon eques was determined. The chromatography showed high levels of oxindole alkaloids, quinovic acid glycosides, and low molecular weight polyphenols. The CL50 48 h was 1816 mg/L. Fish showed behavior changes at concentrations above 2000 mg/L, accompanied by a significant decrease of dissolved oxygen. At the highest concentration 100% mortality was observed attributed to oxygen reduction by the amount of oxindole alkaloids, polyphenols accumulation of the extract in the gills, and the interaction of these compounds with dopamine. In conclusion, the aqueous extract of U. tomentosa did not alter the chemical components and it was shown that U. tomentosa has low toxicity to H. eques; therefore, it can be used safely in this species. PMID:24734041

  3. Constituents from Cistus salvifolius (Cistaceae) activate peroxisome proliferator-activated receptor-γ but not -δ and stimulate glucose uptake by adipocytes.

    PubMed

    Kühn, Claudia; Arapogianni, Niki Eliza; Halabalaki, Maria; Hempel, Jana; Hunger, Nicole; Wober, Jannette; Skaltsounis, Alexios Leandros; Vollmer, Günter

    2011-03-01

    A number of medicinal/culinary herbs have been reported to improve glucose metabolism and to yield hypoglycemic effects in patients with diabetes. Since stimulation of insulin sensitivity appears to be a potential mechanism, peroxisome proliferator-activated receptor (PPAR) γ is a likely target molecule for small lipophilic compounds derived from endogenous metabolism and nutrition. Functionally, PPAR γ integrates the control of energy, lipid, and glucose homeostasis. In addition, PPAR δ activity is involved in energy expenditure. Therefore the aim of this study was to investigate whether PPAR γ and PPAR δ as well as the stimulation of glucose uptake is activated by botanical products. CISTUS SALVIFOLIUS (Cistaceae) has been identified as a candidate botanical in a preliminary screening of extracts from medicinal plants of Greek flora. In a bioguided approach, crude extracts, fractions and in the end purified compounds have been evaluated for PPAR γ and PPAR δ specific activities using cell-based transactivation assays. Glucose uptake was measured by nonradioactive 2-[ N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxyglucose (2-NBDG) uptake. Concerning PPAR γ several extracts induced reporter gene activity, and clear dose-response patterns (0.1-100 µg/mL) could be established in the case of the cyclohexane and dichloromethane extracts. Isolation of individual compounds from the cyclohexane extract revealed that at least 6 out of 7 compounds isolated were active with TRANS-cinnamic acid showing a clear dose-response pattern. In contrast, they were found to be inactive on PPAR δ. The same compounds, however, were also active in stimulating glucose uptake into 3T3-L1 adipocytes. In summary, the bioguided fractionation of CISTUS SALVIFOLIUS yields PPAR γ stimulating metabolites with differing chemical natures. In conclusion, PPAR γ represents a candidate molecule for the mediation of improvement of glucose metabolism by botanical/nutritional products

  4. Physiological Response to Physical Activity in Children.

    ERIC Educational Resources Information Center

    Gilliam, Thomas B.

    This is a report on research in the field of physical responses of children to strenuous activity. The paper is divided into three subtopics: (1) peak performance measure in children; (2) training effects on children; and (3) importance of physical activity for children. Measurements used are oxygen consumption, ventilation, heart rate, cardiac…

  5. Geochemical evidence of groundwater flow paths and the fate and transport of constituents of concern in the alluvial aquifer at Fort Wingate Depot Activity, New Mexico, 2009

    USGS Publications Warehouse

    Robertson, Andrew J.; Henry, David W.; Langman, Jeffery B.

    2013-01-01

    As part of an environmental investigation at Fort Wingate Depot Activity, New Mexico, the U.S. Geological Survey, in cooperation with the U.S. Army Corps of Engineers, interpreted aqueous geochemical concentrations to better understand the groundwater flow paths and the fate and transport of constituents of concern in the alluvial aquifer underlying the study area. The fine-grained nature of the alluvial matrix creates a highly heterogeneous environment, which adds to the difficulty of characterizing the flow of groundwater and the fate of aqueous constituents of concern. The analysis of the groundwater geochemical data collected in October 2009 provides evidence that is used to identify four groundwater flow paths and their extent in the aquifer and indicates the dominant attenuation processes for the constituents of concern. The extent and interaction of groundwater flow paths were delineated by the major ion concentrations and their relations to each other. Four areas of groundwater recharge to the study area were identified based on groundwater elevations, hydrogeologic characteristics, and geochemical and isotopic evidence. One source of recharge enters the study area from the saturated alluvial deposits underlying the South Fork of the Puerco River to the north of the study area. A second source of recharge is shown to originate from a leaky cistern containing production water from the San Andres-Glorieta aquifer. The other two sources of recharge are shown to enter the study area from the south: one from an arroyo valley draining an area to the south and one from hill-front recharge that passes under the reported release of perchlorate and explosive constituents. The spatial extent and interaction of groundwater originating from these various sources along identified flow paths affect the persistence and attenuation of constituents of concern. It was determined that groundwater originating in the area of a former explosives’ wash-out operation and an

  6. Antioxidant and antibacterial activities of the leaf essential oil and its constituents furanodienone and curzerenone from Lindera pulcherrima (Nees.) Benth. ex hook. f.

    PubMed Central

    Joshi, Subhash C.; Mathela, Chandra S.

    2012-01-01

    Background: Lindera pulcherrima (Nees.) Benth. ex Hook. f. (Family: Lauraceae), an evergreen shrub, is an important medicinal plant distributed in temperate Himalayan regions. The leaves and bark are used as spice in cold, fever, and cough. Materials and Methods: In this study, the terpenoid composition, antioxidant, and antibacterial activities of the leaf essential oil and its major constituents are being analyzed. Conclusion: The in vitro antioxidant activity showed a potent free radical scavenging activity for the essential oil as evidenced by a low IC50 value for DPPH radical followed by furanodienone (0.087 ± 0.03 and 1.164 ± 0.58 mg/ml respectively) and the inhibition of lipid peroxidation for the oil and furanodienone also followed the same order (IC50 0.74 ± 0.13 and 2.12 ± 0.49 mg/ml, respectively). The oil and the constituents were also tested against three Gram negative (Escherichia coli, Salmonella enterica enterica, and (Pasturella multocida) and one Gram positive (Staphylococcus aureus) bacteria. The essential oil was effective against S. aureus (IZ = 19.0 ± 0.34; MIC 3.90 μl/ml) while furanodienone showed potent activity against E. coli and S. enterica enterica (IZ = 18.0 ± 0.14 and 16.0 ± 0.10 respectively). On the other hand, curzerenone was found to be slightly effective against E. coli (IZ = 10.8 ± 0.52). The MIC value of the essential oil was least against S. aureus (MIC = 3.90 μl/ml) and that of furanodienone against E. coli (MIC = 3.90 μl/ml). PMID:22518079

  7. Antiproliferative Activity of Cinnamomum cassia Constituents and Effects of Pifithrin-Alpha on Their Apoptotic Signaling Pathways in Hep G2 Cells

    PubMed Central

    Ng, Lean-Teik; Wu, Shu-Jing

    2011-01-01

    Cinnamaldehyde (Cin), cinnamic acid (Ca) and cinnamyl alcohol (Cal), major constituents of Cinnamomum cassia, have been shown to possess antioxidant, anti-inflammatory, anticancer and other activities. In this study, our aim was to evaluate the antiproliferative activity of these compounds in human hepatoma Hep G2 cells and examine the effects of pifithrin-alpha (PFTα; a specific p53 inhibitor) on their apoptotic signaling transduction mechanism. The antiproliferative activity was measured by XTT assay. Expression of apoptosis-related proteins was detected by western blotting. Results showed that at a concentration of 30 μM, the order of antiproliferative activity in Hep G2 cells was Cin > Ca > Cal. Cin (IC50 9.76 ± 0.67 μM) demonstrated an antiproliferative potency as good as 5-fluorouracil (an anti-cancer drug; IC50 9.57 ± 0.61 μM). Further studies on apoptotic mechanisms of Cin showed that it downregulated the expression of Bcl-XL, upregulated CD95 (APO-1), p53 and Bax proteins, as well as cleaving the poly (ADP-ribose) polymerase (PARP) in a time-dependent pattern. PFTα pre-incubation significantly diminished the effect of Cin-induced apoptosis. It markedly upregulated the anti-apoptotic (Bcl-XL) expression and downregulated the pro-apoptotic (Bax) expression, as well as effectively blocking the CD95 (APO-1) and p53 expression, and PARP cleavage in Cin-treated cells. This study indicates that Cin was the most potent antiproliferative constituent of C. cassia, and its apoptotic mechanism in Hep G2 cells could be mediated through the p53 induction and CD95 (APO-1) signaling pathways. PMID:20038571

  8. [Constituents relating to anti-oxidative and alpha-glucosidase inhibitory activities in Yacon aerial part extract].

    PubMed

    Terada, Sumio; Ito, Kikuo; Yoshimura, Akira; Noguchi, Naoto; Ishida, Takashi

    2006-08-01

    Hot water extract of the aerial part of Yacon (Smallanthus sonchifolia, Compositae) showed potent free radical-scavenging activity and inhibitory effects on lipid peroxidation in rat brain homogenate. The most potent antioxidative activity focused on the 50% MeOH-eluted fraction on DIAION HP-20 column chromatography. The structure of the major component in the fraction was identified as 2,3,5-tricaffeoylaltraric acid (TCAA) based on spectroscopic evidence. The antioxidative activity of TCAA is superior to that of natural antioxidants such as (+/-)-catechin, alpha-tocopherol, and ellagic acid, and TCAA also showed selective maltase-inhibitory activity (IC(50) 49 microg/ml). As the hypoglycemic activity of Yacon extract was described in a previous report, the present results showing that the aerial part of Yacon has strong antioxidative activity may encourage its potential use as a food supplement to prevent type II diabetes. PMID:16880725

  9. Stress Reorganization and Response in Active Solids

    NASA Astrophysics Data System (ADS)

    Hawkins, Rhoda J.; Liverpool, Tanniemola B.

    2014-07-01

    We present a microscopic model of a disordered viscoelastic active solid, i.e., an active material whose long time behavior is elastic as opposed to viscous. It is composed of filaments, passive cross-links, and molecular motors powered by stored chemical energy, e.g., actomyosin powered by adenosine triphosphate. Our model allows us to study the collective behavior of contractile active elements and how their interaction with each other and the passive elastic elements determines the macroscopic mechanical properties of the active material. As a result of the (un)binding dynamics of the active elements, we find that this system provides a highly responsive material with a dynamic mechanical response strongly dependent on the amount of deformation.

  10. Brine shrimp lethality test active constituents and new highly oxygenated seco-prezizaane-type sesquiterpenes from Illicium merrillianum.

    PubMed

    Huang, Jian-Mei; Nakade, Kousuke; Kondo, Mamiko; Yang, Chun-Shu; Fukuyama, Yoshiyasu

    2002-01-01

    In the study of bioactive substances in Illicium plants, the methanol extract of I. merrillianum showed brine shrimp lethality test (BST) activity at 200 microg/ml. Bioassay-guided fractionation of the BST active fractions resulted in the isolation of 4-O-methyleudesm-11-en-4alpha-ol, eudesmol-11-en-4alpha-ol and (-)-hinokinin as potent BST active compounds. On the other hand, four new highly oxygenated seco-prezizaane-type sesquiterpenes, merrilliortholactone (1), 2alpha-hydroxycycloparvifloralone (2), 2alpha-hydroxycycloparviflorolide (3), and 2alpha-hydroxyanisatin (4) were isolated from the BST-inactive polar fractions. The structures of new compounds were elucidated by extensive analyses of spectral data. Furthermore, the absolute configuration of 3 was established by the modified Mosher's method. Compounds 1--4 showed neither BST activity at 100 microg/ml nor neurite outgrowth-promoting activity. PMID:11824575

  11. Biological Activities of Toninia candida and Usnea barbata Together with Their Norstictic Acid and Usnic Acid Constituents

    PubMed Central

    Ranković, Branislav; Kosanić, Marijana; Stanojković, Tatjana; Vasiljević, Perica; Manojlović, Nedeljko

    2012-01-01

    The aim of this study was to investigate the chemical composition of acetone extracts of the lichens Toninia candida and Usnea barbata and in vitro antioxidant, antimicrobial, and anticancer activities of these extracts together with some of their major metabolites. The chemical composition of T. candida and U. barbata extracts was determined using HPLC-UV analysis. The major phenolic compounds in these extracts were norstictic acid (T. candida) and usnic acid (U. barbata). Antioxidant activity was evaluated by free radical scavenging, superoxide anion radical scavenging, reducing power and determination of total phenolic compounds. Results of the study proved that norstictic acid had the largest antioxidant activity. The total content of phenols in the extracts was determined as the pyrocatechol equivalent. The antimicrobial activity was estimated by determination of the minimal inhibitory concentration using the broth microdilution method. The most active was usnic acid with minimum inhibitory concentration values ranging from 0.0008 to 0.5 mg/mL. Anticancer activity was tested against FemX (human melanoma) and LS174 (human colon carcinoma) cell lines using the microculture tetrazolium test. Usnic acid was found to have the strongest anticancer activity towards both cell lines with IC50 values of 12.72 and 15.66 μg/mL. PMID:23203090

  12. Active thermal isolation for temperature responsive sensors

    NASA Technical Reports Server (NTRS)

    Martinson, Scott D. (Inventor); Gray, David L. (Inventor); Carraway, Debra L. (Inventor); Reda, Daniel C. (Inventor)

    1994-01-01

    A temperature responsive sensor is located in the airflow over the specified surface of a body and is maintained at a constant temperature. An active thermal isolator is located between this temperature responsive sensor and the specified surface of the body. The temperature of this isolator is controlled to reduce conductive heat flow from the temperature responsive sensor to the body. This temperature control includes: (1) operating the isolator at the same temperature as the constant temperature of the sensor and (2) establishing a fixed boundary temperature which is either less than or equal to or slightly greater than the sensor constant temperature.

  13. Crocin, the main active saffron constituent, mitigates dichlorvos-induced oxidative stress and apoptosis in HCT-116 cells.

    PubMed

    Ben Salem, Intidhar; Boussabbeh, Manel; Kantaoui, Hiba; Bacha, Hassen; Abid-Essefi, Salwa

    2016-08-01

    The protective effects of Crocin (CRO), a carotenoid with wide spectrum of pharmacological effects, against the cytotoxicity and the apoptosis produced by exposure to Dichlorvos (DDVP) in HCT116 cells were investigated in this work. The cytotoxicity was monitored by cell viability, ROS generation, antioxidant enzymes activities, malondialdehyde (MDA) production and DNA fragmentation. The apoptosis was assessed through the measurement of the mitochondrial transmembrane potential (ΔΨm) and caspases activation. The results indicated that pretreatment of HCT116 cells with CRO, 2h prior to DDVP exposure, significantly increased the survival of cells, inhibited the ROS generation, modulated the activities of catalase (CAT) and superoxide dismutase (SOD) and reduced the MDA level. The reduction in mitochondrial membrane potential, DNA fragmentation and caspases activation were also inhibited by CRO. These findings suggest that CRO can protect HCT116 cells from DDVP-induced oxidative stress and apoptosis. PMID:27470340

  14. Antioxidant Activity of Extract and Its Major Constituents from Okra Seed on Rat Hepatocytes Injured by Carbon Tetrachloride

    PubMed Central

    Hu, Lianmei; Yu, Wenlan; Li, Ying; Tang, Zhaoxin

    2014-01-01

    The antioxidant activities and protective effects of total phenolic extracts (TPE) and their major components from okra seeds on oxidative stress induced by carbon tetrachloride (CCl4) in rat hepatocyte cell line were investigated. The major phenolic compounds were identified as quercetin 3-O-glucosyl (1 → 6) glucoside (QDG) and quercetin 3-O-glucoside (QG). TPE, QG, and QDG from okra seeds exhibited excellent reducing power and free radical scavenging capabilities including α, α-diphenyl-β-picrylhydrazyl (DPPH), superoxide anions, and hydroxyl radical. Overall, DPPH radical scavenging activity and reducing power of QG and QDG were higher than those of TPE while superoxide and hydroxyl radical scavenging activities of QG and TPE were higher than those of QDG. Furthermore, TPE, QG, and QDG pretreatments significantly alleviated the cytotoxicity of CCl4 on rat hepatocytes, with attenuated lipid peroxidation, increased SOD and CAT activities, and decreased GPT and GOT activities. The protective effects of TPE and QG on rat hepatocytes were stronger than those of QDG. However, the cytotoxicity of CCl4 on rat hepatocytes was not affected by TPE, QG, and QDG posttreatments. It was suggested that the protective effects of TPE, QG, and QDG on rat hepatocyte against oxidative stress were related to the direct antioxidant capabilities and the induced antioxidant enzymes activities. PMID:24719856

  15. Anti-glycation activities of phenolic constituents from Silybum marianum (Milk Thistle) flower in vitro and on human explants.

    PubMed

    Shin, Seoungwoo; Lee, Jung-A; Kim, Minkyung; Kum, Hyunwoo; Jung, Eunsun; Park, Deokhoon

    2015-01-01

    Glycation is an ageing reaction of naturally occurring sugars with dermal proteins, with clinical signs appearing in vivo around age 30, and increasing steadily/regularly with age. The suppleness of the dermis is affected by the formation of bridges between proteins and sugars (Maillard's reaction). The accumulation of advanced glycation end products (AGEs) in skin plays a very important role in skin ageing. Therefore, natural compounds or extracts that possess antiglycation activities may have great anti-ageing potential. In the present study, Silybum marianum flower extract (SMFE) was demonstrated to possess antiglycation activity. We found that SMFE inhibits glycation reaction between BSA and glucose. In addition, antiglycation activity of SMFE was confirmed in a human skin explants model. SMFE reduced Nε-(carboxymethyl) lysine (CML) expression, whereas SMFE stimulated fibrillin-1 expression compared to treatment with methyglyoxal. An active ingredient contributing to the observed activities was identified as silibinin. The antiglycation activity of silibinin was dose-dependent. The beneficial effects of silibinin may be applied to prevention or management of AGE-mediated pathologies, targeting in a pleiotropic and complementary way the biochemical and cellular bases of skin aging. PMID:25706757

  16. Comparative investigation of Umbellularia californica and Laurus nobilis leaf essential oils and identification of constituents active against Aedes aegypti.

    PubMed

    Tabanca, Nurhayat; Avonto, Cristina; Wang, Mei; Parcher, Jon F; Ali, Abbas; Demirci, Betul; Raman, Vijayasankar; Khan, Ikhlas A

    2013-12-18

    Umbellularia californica (California bay laurel) and Laurus nobilis (Mediterranean bay laurel) leaves may be mistaken or used as a substitute on the market due to their morphological similarity. In this study, a comparison of anatomical and chemical features and biological activity of both plants is presented. L. nobilis essential oil biting deterrent and larvicidal activity were negligible. On the other hand, U. californica leaf oil showed biting deterrent activity against Aedes aegypti . The identified active repellents was thymol, along with (-)-umbellulone, 1,8-cineole, and (-)-α-terpineol. U. californica essential oil also demonstrated good larvicidal activity against 1-day-old Ae. aegypti larvae with a LD50 value of 52.6 ppm. Thymol (LD50 = 17.6 ppm), p-cymene, (-)-umbellulone, and methyleugenol were the primary larvicidal in this oil. Umbellulone was found as the principal compound (37%) of U. californica essential oil, but was not present in L. nobilis essential oil. Umbellulone mosquito activity is here reported for the first time. PMID:24266426

  17. Antioxidant activity of extract and its major constituents from okra seed on rat hepatocytes injured by carbon tetrachloride.

    PubMed

    Hu, Lianmei; Yu, Wenlan; Li, Ying; Prasad, Nagendra; Tang, Zhaoxin

    2014-01-01

    The antioxidant activities and protective effects of total phenolic extracts (TPE) and their major components from okra seeds on oxidative stress induced by carbon tetrachloride (CCl4) in rat hepatocyte cell line were investigated. The major phenolic compounds were identified as quercetin 3-O-glucosyl (1 → 6) glucoside (QDG) and quercetin 3-O-glucoside (QG). TPE, QG, and QDG from okra seeds exhibited excellent reducing power and free radical scavenging capabilities including α, α-diphenyl-β-picrylhydrazyl (DPPH), superoxide anions, and hydroxyl radical. Overall, DPPH radical scavenging activity and reducing power of QG and QDG were higher than those of TPE while superoxide and hydroxyl radical scavenging activities of QG and TPE were higher than those of QDG. Furthermore, TPE, QG, and QDG pretreatments significantly alleviated the cytotoxicity of CCl4 on rat hepatocytes, with attenuated lipid peroxidation, increased SOD and CAT activities, and decreased GPT and GOT activities. The protective effects of TPE and QG on rat hepatocytes were stronger than those of QDG. However, the cytotoxicity of CCl4 on rat hepatocytes was not affected by TPE, QG, and QDG posttreatments. It was suggested that the protective effects of TPE, QG, and QDG on rat hepatocyte against oxidative stress were related to the direct antioxidant capabilities and the induced antioxidant enzymes activities. PMID:24719856

  18. Effect of Zn2+, Fe3+ and Cr3+ addition to hydroxyapatite for its application as an active constituent of sunscreens

    NASA Astrophysics Data System (ADS)

    de Araujo, T. S.; de Souza, S. O.; de Sousa, E. M. B.

    2010-11-01

    Biocompatible phosphate materials are used in different applications like bone and dental implants, drug delivery systems and others, but could also be applied in inorganic sunscreens. Using sunscreens is extremely necessary, because long time exposure to sun can cause skin cancer. In this work chemical precipitation method has been used to produce hydroxyapatite. Cr3+, Zn2+ and Fe3+ doped samples were characterized using powder X-Ray Diffraction (XRD) and Optical Absorption techniques. X-ray diffraction measurements confirmed the materials were in the expected crystalline structures. The crystallite size as measured from the X-ray pattern was 23-27 nm (±1). The absorption spectra in the ultraviolet and visible ranges indicate that appropriately doped and sized hydroxyapatite particles may have potential applications as active constituents of sunscreens.

  19. Cellular Stress Responses and Monitored Cellular Activities.

    PubMed

    Sawa, Teiji; Naito, Yoshifumi; Kato, Hideya; Amaya, Fumimasa

    2016-08-01

    To survive, organisms require mechanisms that enable them to sense changes in the outside environment, introduce necessary responses, and resist unfavorable distortion. Consequently, through evolutionary adaptation, cells have become equipped with the apparatus required to monitor their fundamental intracellular processes and the mechanisms needed to try to offset malfunction without receiving any direct signals from the outside environment. It has been shown recently that eukaryotic cells are equipped with a special mechanism that monitors their fundamental cellular functions and that some pathogenic proteobacteria can override this monitoring mechanism to cause harm. The monitored cellular activities involved in the stressed intracellular response have been researched extensively in Caenorhabditis elegans, where discovery of an association between key mitochondrial activities and innate immune responses was named "cellular associated detoxification and defenses (cSADD)." This cellular surveillance pathway (cSADD) oversees core cellular activities such as mitochondrial respiration and protein transport into mitochondria, detects xenobiotics and invading pathogens, and activates the endocrine pathways controlling behavior, detoxification, and immunity. The cSADD pathway is probably associated with cellular responses to stress in human inflammatory diseases. In the critical care field, the pathogenesis of lethal inflammatory syndromes (e.g., respiratory distress syndromes and sepsis) involves the disturbance of mitochondrial respiration leading to cell death. Up-to-date knowledge about monitored cellular activities and cSADD, especially focusing on mitochondrial involvement, can probably help fill a knowledge gap regarding the pathogenesis of lethal inflammatory syndromes in the critical care field. PMID:26954943

  20. Constituency Leadership: A Model for School Leaders.

    ERIC Educational Resources Information Center

    Strodl, Peter

    Principals must integrate information originating from many sectors among the schools' constituents. The degree to which constituent groups participate in school activities helps determine the quality of instruction and learning. Crucial to the role of administrator is a network of interactions between people and things, school board pressures and…

  1. The constituents of essential oil: antimicrobial and antioxidant activity of Micromeria congesta Boiss. & Hausskn. ex Boiss. from East Anatolia.

    PubMed

    Herken, Emine Nur; Celik, Ali; Aslan, Mustafa; Aydınlık, Nilüfer

    2012-09-01

    The chemical composition, antimicrobial activity, total phenol content, total antioxidant activity, and total oxidant status of the essential oil from Micromeria congesta Boiss. & Hausskn. ex Boiss. were investigated. Steam distillation was used to obtain the essential oil, and the chemical analyses were performed by gas chromatography-mass spectrometry. The antimicrobial activity was tested by an agar disc diffusion method against the tested microorganisms: Bacillus subtilis NRRL B-744, Bacillus cereus NRRL B-3711, Staphylococcus aureus ATCC 12598, S. aureus ATCC 25923, S. aureus ATCC 25933, Escherichia coli 0157H7, E. coli ATCC25922, Micrococcus luteus NRLL B-4375, Enterococcus faecalis ATCC 19433, Proteus vulgaris RSKK 96026, and Yersinia enterecolitica RSKK 1501. The major compounds found in volatiles of M. congesta were piperitone oxide, linalool oxide, veratrole, pulegone, dihydro carvone, naphthalene, iso-menthone, para-menthone, and cyclohexanone. Compared to that of reference antibiotics, the antibacterial activity of the essential oil is considered as significant. Results showed that M. congesta has the potential for being used in food and medicine depending on its antioxidant and antibacterial activity. PMID:22871061

  2. Study on prevention of two-stage skin carcinogenesis by Hibiscus rosa sinensis extract and the role of its chemical constituent, gentisic acid, in the inhibition of tumour promotion response and oxidative stress in mice.

    PubMed

    Sharma, S; Khan, N; Sultana, S

    2004-02-01

    We designed the present study to investigate the role of gentisic acid in the chemopreventive activity of Hibiscus rosa sinensis extract on 7,12-dimethyl benz(a)anthracene (DMBA)/croton oil-mediated carcinogenesis in mouse skin via 12-O-tetradecanoyl phorbol-13-acetate (TPA)-induced tumour promotion response and oxidative stress. Single topical application of DMBA followed by twice weekly applications of croton oil after one week for 20 weeks resulted in 100% incidence of tumours in animals in 15 weeks. However, application of H. rosa sinensis extract 30 minutes prior to the application of croton oil twice weekly for 20 weeks caused significant reduction in the number of tumours per mouse and the percentage of tumour-bearing mice. Also, the latency period for the appearance of the first tumour was delayed on H. rosa sinensis pretreatment. A single topical application of TPA caused significant depletion in reduced glutathione (GSH) content, activities of its metabolizing and antioxidant enzymes, while malondialdehyde (MDA) formation, H2O2 content, ornithine decarboxylase (ODC) activity and DNA synthesis were significantly increased. Interestingly, pretreatment of H. rosa sinensis extract (3.5 mg and 7 mg/kg body weight) and gentisic acid (2.0 microg and 4.0 microg/0.2 ml acetone per animal) restored the levels of GSH, and its metabolizing and antioxidant enzymes (P<0.05). There was also a statistically significant reduction in MDA formation and H2O2 content (P<0.05) at both doses. Although inhibition of ODC activity by gentisic acid was not dose-dependent, thymidine incorporation in DNA (P<0.05) was dose-dependently recovered by the plant extract and its chemical constituent. We therefore propose that gentisic acid has a role in the modulatory activity of H. rosa sinensis extract. PMID:15075789

  3. Seasonal variations of the phenolic constituents in bilberry (Vaccinium myrtillus L.) leaves, stems and fruits, and their antioxidant activity.

    PubMed

    Bujor, Oana-Crina; Le Bourvellec, Carine; Volf, Irina; Popa, Valentin I; Dufour, Claire

    2016-12-15

    The seasonal variations of the content and diversity of phenolic compounds, as well as the antioxidant activity of leaves, stems and fruits of bilberry collected in May, July and September, were evaluated for two consecutive years. UPLC/MS(n) analyses showed the predominance of anthocyanins in fruits, caffeic acid derivatives in leaves whereas flavanol oligomers represented more than half of the phenolic compounds in stems. Thioacidolysis revealed degrees of polymerization between 2 and 4 and (-)-epicatechin as the main flavanol unit. The sum of the phenolic compounds by UPLC was highly correlated with the total polyphenol content and the antioxidant activity in the DPPH test for all the extracts except for May leaves. The latter were relatively rich in p-coumaric acid derivatives. Seasonal effects were more marked for leaves, which exhibited higher antioxidant activities and phenolic contents in July and September when these parameters were at their highest in July for stems. PMID:27451155

  4. A New Neolignan, and the Cytotoxic and Anti-HIV-1 Activities of Constituents from the Roots of Dasymaschalon sootepense.

    PubMed

    Hongthong, Sakchai; Kuhakarn, Chutima; Jaipetch, Thaworn; Piyachaturawat, Pawinee; Jariyawat, Surawat; Suksen, Kanoknetr; Limthongkul, Jitra; Nuntasaen, Narong; Reutrakul, Vichai

    2016-06-01

    Bioassay-guided isolation from the ethyl acetate extract of Dasymaschalon sootepense roots led to the isolation of twelve compounds including a new dihydrobenzo-furan neolignan, (+)-(2S,3S)-2,3-dihydro-2-(3,4-dimethoxyphenyl)-3-methylbenzofuran-5-carbaldehyde (5), and eleven known compounds (1-4, and 6-12). The chemical structures and stereochemistry of all the isolated compounds were established by spectroscopic techniques. The known compounds 4 and 6 have been fully characterized spectroscopically, including their absolute configurations. Cytotoxic and anti-HIV-1 reverse transcriptase (RT) activities of compounds 1-3, 5 and 8-12 were determined. Among compounds screened, compounds 2, 3 and 10 displayed weak cytotoxic activity with ED50 values ranging from 9.6-47.5 μM and only compound 2 was found weakly active against HIV-1 RT with an IC50 value of 323.2 μM. PMID:27534123

  5. Prenylfuranocoumarin-HMGA-flavonol glucoside conjugates and other constituents of the fruit peels of Citrus hystrix and their anticholinesterase activity.

    PubMed

    Seeka, Chonticha; Sutthivaiyakit, Pakawadee; Youkwan, Juthamanee; Hertkorn, Norbert; Harir, Mourad; Schmitt-Kopplin, Philippe; Sutthivaiyakit, Somyote

    2016-07-01

    Sixteen compounds including dihydroxy prenylfuranocoumarins/3-hydroxy-3-methylglutaric acid conjugates and dihydroxy prenylfuranocoumarins/3-hydroxy-3-methylglutaric acid/1-O-flavonyl-β-d-glucopyranoside conjugates, together with other dihydroxyprenylfuranocoumarins conjugates, were isolated from the ethyl acetate extract of the fruit peels of Citrus hystrix. Some of the isolates were evaluated for their cholinesterase inhibitory activity, but only one compound possessing a 3-O-β-d-glucopyranosyl-3,5,7,4'-tetrahydroxy-6,8,3'-trimethoxyflavonol nucleus in the prenylfuranocoumarin-HMGA conjugate showed strong activity. PMID:26995149

  6. Anti-plasmodial and antioxidant activities of constituents of the seed shells of Symphonia globulifera Linn f.

    PubMed

    Ngouela, Silvère; Lenta, Bruno Ndjakou; Noungoue, Diderot Tchamo; Ngoupayo, Joseph; Boyom, Fabrice Fekam; Tsamo, Etienne; Gut, Jiri; Rosenthal, Philip J; Connolly, Joseph D

    2006-02-01

    A xanthone derivative, named gaboxanthone (1), has been isolated from the seed shells of Symphonia globulifera, together with known compounds, symphonin (2), globuliferin (3), guttiferone A (4), sistosterol, oleanolic acid and methyl citrate. The structure of the compound was assigned as 5,10-dihydroxy-8,9-dimethoxy-2,2-dimethyl-12-(3-methylbut-2-enyl) pyrano [3,2-b]xanthen-6(2H)-one, by means of spectroscopic analysis. The anti-plasmodial and antioxidant activities of the phenolic compounds were evaluated, respectively, in culture against W2 strain of Plasmodium falciparum and using the free radical scavenging activity of the DPPH radical, respectively. Compounds 1-4 were found to be active against the Plasmodium parasites (IC(50) of 3.53, 1.29, 3.86 and 3.17 microM, respectively). Guttiferone A (4) showed a potent free radical scavenging activity compared to the well-known antioxidant caffeic acid. PMID:16368120

  7. Constituents, biological activities and quality control parameters of the crude extract and essential oil from Arracacia tolucensis var. multifida.

    PubMed

    Figueroa, Mario; Rivero-Cruz, Isabel; Rivero-Cruz, Blanca; Bye, Robert; Navarrete, Andrés; Mata, Rachel

    2007-08-15

    Bioassay guided fractionation of an antimycobacterial extract of Arracacia tolucensis var. multifida (Umbelliferae) led to the isolation of isoimperatorin (1), osthol (2), suberosin (3), 8-methoxypsoralen (8-MOP) (4), herniarin (5), scoparone (6), umbelliferone (7), dihydroxypeucedanin (8), 5-methoxypsoralen (5-MOP) (9), isoscopoletin (10) and scopoletin (11). The isolates were tested against Mycobacterium tuberculosis and only 1-4 showed significant activity with MIC values of 64, 32, 16 and 128 microg/mL, respectively. The essential oil showed moderate in vitro antibacterial activity against representative Gram-positive and Gram-negative bacteria. The volatile oil of Arracacia tolucensis var. multifida was analyzed by GC-MS and found to be composed mainly by 2 and 3. The essential oil (IC(50)=116.4+/-23.2 microg/mL) and the extract (IC(50)=1153.1+/-53.2 microg/mL) of the plant provoked concentration dependent inhibition of the tone and amplitude of the guinea-pig ileum spontaneous contractions; the latter activity was related with the high coumarin content of this species. A suitable (novel and rapid) HPLC method to quantify the major active coumarins of the plant was developed. The method provides also a reproducible fingerprint useful for identity tests of this plant. PMID:17582715

  8. Teaching Responsibility through Physical Activity. Second Edition.

    ERIC Educational Resources Information Center

    Hellison, Don

    This book guides teachers in using physical activity to foster personal and social responsibility. Focusing on teaching in school settings, the book features comments from real students to motivate teachers to apply the concept; take-aways that summarize each chapter and help teachers consider their own situations; new chapters on the lesson plan…

  9. Rigor and Responsiveness in Classroom Activity

    ERIC Educational Resources Information Center

    Thomspon, Jessica; Hagenah, Sara; Kang, Hosun; Stroupe, David; Braaten, Melissa; Colley, Carolyn; Windschitl, Mark

    2016-01-01

    Background/Context: There are few examples from classrooms or the literature that provide a clear vision of teaching that simultaneously promotes rigorous disciplinary activity and is responsive to all students. Maintaining rigorous and equitable classroom discourse is a worthy goal, yet there is no clear consensus of how this actually works in a…

  10. Insecticidal and acetylcholine esterase inhibition activity of Asteraceae plant essential oils and their constituents against adults of the German cockroach (Blattella germanica).

    PubMed

    Yeom, Hwa-Jeong; Jung, Chan-Sik; Kang, Jaesoon; Kim, Junheon; Lee, Jae-Hyeon; Kim, Dong-Soo; Kim, Hyun-Seok; Park, Pil-Sun; Kang, Kyu-Suk; Park, Il-Kwon

    2015-03-01

    The fumigant and contact toxicities of 16 Asteraceae plant essential oils and their constituents against adult male and female Blattella germanica were examined. In a fumigant toxicity test, tarragon oil exhibited 100% and 90% fumigant toxicity against adult male German cockroaches at 5 and 2.5 mg/filter paper, respectively. Fumigant toxicities of Artemisia arborescens and santolina oils against adult male German cockroaches were 100% at 20 mg/filter paper, but were reduced to 60% and 22.5% at 10 mg/filter paper, respectively. In contact toxicity tests, tarragon and santolina oils showed potent insecticidal activity against adult male German cockroaches. Components of active oils were analyzed using gas chromatography, gas chromatography-mass spectrometry, or nuclear magnetic resonance spectrometer. Among the identified compounds from active essential oils, estragole demonstrated potent fumigant and contact toxicity against adult German cockroaches. β-Phellandrene exhibited inhibition of male and female German cockroach acetylcholinesterase activity with IC50 values of 0.30 and 0.28 mg/mL, respectively. PMID:25664467

  11. GABA-A Receptor Modulation and Anticonvulsant, Anxiolytic, and Antidepressant Activities of Constituents from Artemisia indica Linn

    PubMed Central

    Khan, Imran; Karim, Nasiara; Ahmad, Waqar; Abdelhalim, Abeer; Chebib, Mary

    2016-01-01

    Artemisia indica, also known as “Mugwort,” has been widely used in traditional medicines. However, few studies have investigated the effects of nonvolatile components of Artemisia indica on central nervous system's function. Fractionation of Artemisia indica led to the isolation of carnosol, ursolic acid, and oleanolic acid which were evaluated for their effects on GABA-A receptors in electrophysiological studies in Xenopus oocytes and were subsequently investigated in mouse models of acute toxicity, convulsions (pentylenetetrazole induced seizures), depression (tail suspension and forced swim tests), and anxiety (elevated plus maze and light/dark box paradigms). Carnosol, ursolic acid, and oleanolic acid were found to be positive modulators of α1β2γ2L GABA-A receptors and the modulation was antagonized by flumazenil. Carnosol, ursolic acid, and oleanolic acid were found to be devoid of any signs of acute toxicity (50–200 mg/kg) but elicited anticonvulsant, antidepressant, and anxiolytic activities. Thus carnosol, ursolic acid, and oleanolic acid demonstrated CNS activity in mouse models of anticonvulsant, antidepressant, and anxiolysis. The anxiolytic activity of all three compounds was ameliorated by flumazenil suggesting a mode of action via the benzodiazepine binding site of GABA-A receptors. PMID:27143980

  12. Constituents and Pharmacological Activities of Myrcia (Myrtaceae): A Review of an Aromatic and Medicinal Group of Plants

    PubMed Central

    Cascaes, Márcia Moraes; Guilhon, Giselle Maria Skelding Pinheiro; Andrade, Eloisa Helena de Aguiar; Zoghbi, Maria das Graças Bichara; Santos, Lourivaldo da Silva

    2015-01-01

    Myrcia is one of the largest genera of the economically important family Myrtaceae. Some of the species are used in folk medicine, such as a group known as “pedra-hume-caá” or “pedra-ume-caá” or “insulina vegetal” (insulin plant) that it is used for the treatment of diabetes. The species are an important source of essential oils, and most of the chemical studies on Myrcia describe the chemical composition of the essential oils, in which mono- and sesquiterpenes are predominant. The non-volatile compounds isolated from Myrcia are usually flavonoids, tannins, acetophenone derivatives and triterpenes. Anti-inflammatory, antinociceptive, antioxidant, antimicrobial activities have been described to Myrcia essential oils, while hypoglycemic, anti-hemorrhagic and antioxidant activities were attributed to the extracts. Flavonoid glucosides and acetophenone derivatives showed aldose reductase and α-glucosidase inhibition, and could explain the traditional use of Myrcia species to treat diabetes. Antimicrobial and anti-inflammatory are some of the activities observed for other isolated compounds from Myrcia. PMID:26473832

  13. Screening of the constituents, antimicrobial and antioxidant activity of endemic Origanum hypericifolium O. Schwartz & P.H. Davis.

    PubMed

    Celik, Ali; Nur Herken, E; Arslan, Idris; Zafer Ozel, M; Mercan, Nazime

    2010-10-01

    The chemical compositions, total phenol content, antioxidant and antimicrobial activities with oxidant status of the essential oil from an endemic Turkish species, Origanum hypericifolium, were investigated. Steam distillation (SD) was used to isolate the essential oils, and the chemical analyses were performed by gas chromatography-mass spectrometry (GC-MS). The antimicrobial activity was tested by agar disc diffusion method against Morganella morganii (clinic isolate), Micrococcus flavus (clinic isolate), Micrococcus luteus NRLL B-4375, Proteus vulgaris RSKK 96026, Escherichia coli ATCC 11230, Escherichia coli ATCC 25922, Yersinia enterecolitica RSKK 1501, Staphylococcus aureus ATCC 25923, S. aureus ATCC 25933, S. aureus ATCC 12598, S. aureus (clinic isolate), MRSA 1 (clinic isolate), MRSA 2 (clinic isolate), MRSA 3 (clinic isolate) and MRSA 4 (clinic isolate). The major compounds found in volatiles of O. hypericifolium were p-cymene, carvacrol and γ-terpinene. Results showed that O. hypericifolium has the potential for being used in food and medicine because of its antioxidant and antibacterial activity. PMID:20835958

  14. Extracts and constituents of Rubus chingii with 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity.

    PubMed

    Ding, Hsiou-Yu

    2011-01-01

    The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity of the fruits of Rubus chingii was studied in vitro. Ethanolic extract, ethyl acetate and n-butanol fractions from dried R. chingii fruits revealed strong DPPH free radical scavenging activity with IC(50) values of 17.9, 3.4 and 4.0 μg/mL, respectively. The ethyl acetate and n-butanol fractions were further purified by a combination of silica gel chromatography, Lobar RP-8 chromatography, and high-pressure liquid chromatography (HPLC). Nine compounds were isolated, where methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), vanillic acid (5), kaempferol (7), and tiliroside (9) showed stronger DPPH free radical scavenging activity than that of ascorbic acid (131.8 μM) with IC(50) values of 45.2, 34.9, 78.5, and 13.7 μM, respectively. In addition, rubusine (1) is a new compound discovered in the present study and methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), methyl dioxindole-3-acetate (3), and 2-oxo-1,2-dihydroquinoline-4-carboxylic acid (4) were isolated from the fruits for the first time. PMID:21747716

  15. Flavonolignans and other constituents from Lepidium meyenii with activities in anti-inflammation and human cancer cell lines.

    PubMed

    Bai, Naisheng; He, Kan; Roller, Marc; Lai, Ching-Shu; Bai, Lu; Pan, Min-Hsiung

    2015-03-11

    From the roots of Lepidium meyenii Walpers (Brassicaceae) have been isolated and identified 2 flavonolignans, tricin 4'-O-[threo-β-guaiacyl-(7″-O-methyl)-glyceryl] ether (1) and tricin 4'-O-(erythro-β-guaiacyl-glyceryl) ether (2), along with 11 other known compounds, tricin (3), pinoresinol (4), 4-hydroxycinnamic acid (5), guanosine (6), glucotropaeolin (7), desulfoglucotropaeolin (8), 3-hydroxybenzylisothiocyanate (9), malic acid benzoate (10), 5-(hydroxymethyl)-2-furfural (11), d-phenylalanine (12), and vanillic acid 4-O-β-d-glucoside (13). Structures were elucidated on the basis of NMR and MS data. Some isolates and previously isolated lepidiline B (14) were tested for cytotoxicity in a small panel of human cancer cell lines (Hep G2, COLO 205, and HL-60) and for anti-inflammatory activities in LPS-treated RAW 264.7 macrophage. Among them, compounds 1 and 14 were modestly active for inhibiting nitrite production in macrophage. Compounds 1, 14, and 3 were demonstrated to be selectively active against HL-60 cells with IC50 values of 40.4, 52.0, and 52.1 μM, respectively. PMID:25667964

  16. Low dielectric response in enzyme active site

    PubMed Central

    Mertz, Edward L.; Krishtalik, Lev I.

    2000-01-01

    The kinetics of charge transfer depend crucially on the dielectric reorganization of the medium. In enzymatic reactions that involve charge transfer, atomic dielectric response of the active site and of its surroundings determines the efficiency of the protein as a catalyst. We report direct spectroscopic measurements of the reorganization energy associated with the dielectric response in the active site of α-chymotrypsin. A chromophoric inhibitor of the enzyme is used as a spectroscopic probe. We find that water strongly affects the dielectric reorganization in the active site of the enzyme in solution. The reorganization energy of the protein matrix in the vicinity of the active site is similar to that of low-polarity solvents. Surprisingly, water exhibits an anomalously high dielectric response that cannot be described in terms of the dielectric continuum theory. As a result, sequestering the active site from the aqueous environment inside low-dielectric enzyme body dramatically reduces the dielectric reorganization. This reduction is particularly important for controlling the rate of enzymatic reactions. PMID:10681440

  17. In vitro cytotoxic activity of extracts and isolated constituents of Salvia leriifolia Benth. against a panel of human cancer cell lines.

    PubMed

    Tundis, Rosa; Loizzo, Monica R; Menichini, Federica; Bonesi, Marco; Colica, Carmela; Menichini, Francesco

    2011-06-01

    In the course of recent efforts to identify new potential antiproliferative active principles, Salvia leriifolia extracts and isolated constituents were evaluated for their cytotoxic activity against a panel of human cancer cell lines, including renal adenocarcinoma (ACHN), amelanotic melanoma (C32), colorectal adenocarcinoma (Caco-2), lung large cell carcinoma (COR-L23), malignant melanoma (A375), lung carcinoma (A549), and hepatocellular carcinoma (Huh-7D12) cells. The hexane and CH(2) Cl(2) extracts showed the strongest cytotoxic activity against the C32 cell line with IC(50) values of 11.2 and 13.6 μg/ml, respectively, and the AcOEt extract was the most active extract against the COR-L23 cell line (IC(50) of 20.9 μg/ml). Buchariol, a sesquiterpene obtained by biofractionation of the CH(2) Cl(2) extract, exhibited a higher activity than the positive control vinblastine against the C32 and A549 cell lines (IC(50) values of 2.1 and 12.6 μM, resp.). Interesting results were also obtained for naringenin, a flavonoid isolated from the AcOEt extract, which exhibited a strong cytotoxic activity against the C32, LNCaP, and COR-L23 cell lines (IC(50) values of 2.2, 7.7, and 33.4 μM, resp.), compared to vinblastine (IC(50) values of 3.3, 32.2, 50.0 μM, resp.). None of the tested compounds affected the proliferation of skin fibroblasts (142BR), suggesting a selective activity against tumor cells. PMID:21674787

  18. Larvicidal and acetylcholinesterase inhibitory activities of apiaceae plant essential oils and their constituents against aedes albopictus and formulation development.

    PubMed

    Seo, Seon-Mi; Jung, Chan-Sik; Kang, Jaesoon; Lee, Hyo-Rim; Kim, Sung-Woong; Hyun, Jinho; Park, Il-Kwon

    2015-11-18

    This study evaluated the larvicidal activity of 12 Apiaceae plant essential oils and their components against the Asian tiger mosquito, Aedes albopictus, and the inhibition of acetylcholine esterase with their components. Of the 12 plant essential oils tested, ajowan (Trachyspermum ammi), caraway seed (Carum carvi), carrot seed (Daucus carota), celery (Apium graveolens), cumin (Cuminum cyminum), dill (Anethum graveolens), and parsley (Petroselinum sativum) resulted in >90% larval mortality when used at 0.1 mg/mL. Of the compounds identified, α-phellandrene, α-terpinene, p-cymene, (-)-limonene, (+)-limonene, γ-terpinene, cuminaldehyde, neral, (S)-+-carvone, trans-anethole, thymol, carvacrol, myristicin, apiol, and carotol resulted in >80% larval mortality when used at 0.1 mg/mL. Two days after treatment, 24.69, 3.64, and 12.43% of the original amounts of the celery, cumin, and parsley oils, respectively, remained in the water. Less than 50% of the original amounts of α-phellandrene, 1,8-cineole, terpinen-4-ol, cuminaldehyde, and trans-antheole were detected in the water at 2 days after treatment. Carvacrol, α-pinene, and β-pinene inhibited the activity of Ae. albopictus acetylcholinesterase with IC50 values of 0.057, 0.062, and 0.190 mg/mL, respectively. A spherical microemulsion of parsley essential oil-loaded poly(vinyl alcohol) (PVA) was prepared, and the larvicidal activity of this formulation was shown to be similar to that of parsley oil. PMID:26500081

  19. Antifungal and cytotoxicity activities of the fresh xylem sap of Hymenaea courbaril L. and its major constituent fisetin

    PubMed Central

    2014-01-01

    Background The great potential of plants as Hymenaea courbaril L (jatoba) has not yet been throughly explored scientifically and therefore it is very important to investigate their pharmacological and toxicological activities to establish their real efficacy and safety. This study investigated the cytotoxicity of xylem sap of Hymenaea courbaril L and its bioactivity against the fungi Cryptococcus neoformans species complex and dermatophytes. Methods The fresh xylem sap of H. courbaril was filtered resulting in an insoluble brown color precipitate and was identified as fisetin. In the filtrate was identified the mixture of fisetinediol, fustin, 3-O-methyl-2,3-trans-fustin and taxifolin, which were evaluated by broth microdilution antifungal susceptibility testing against C. neoformans species complex and dermatophytes. The fresh xylem sap and fisetin were screened for cytotoxicity against the 3T3-A31 cells of Balb/c using neutral red uptake (NRU) assay. Results The fresh xylem sap and the fisetin showed higher in vitro activity than the filtrate. The xylem sap of H. courbaril inhibited the growth of dermatophytes and of C. neoformans with minimal inhibition concentration (MIC) < 256 μg/mL, while the fisetin showed MIC < 128 μg/mL for these fungi. Fisetin showed lower toxicity (IC50 = 158 μg/mL) than the fresh xylem sap (IC50 = 109 μg/mL). Conclusion Naturally occurring fisetin can provide excellent starting points for clinical application and can certainly represent a therapeutic potential against fungal infections, because it showed in vitro antifungal activity and low toxicity on animal cells. PMID:25027026

  20. Anti-inflammatory, free radical scavenging and alpha-glucosidase inhibitory activities of Hamelia patens and its chemical constituents.

    PubMed

    Jiménez-Suárez, Verónica; Nieto-Camacho, Antonio; Jiménez-Estrada, Manuel; Alvarado Sánchez, Brenda

    2016-09-01

    Context Hamelia patens Jacq. (Rubiaceae) is traditionally used to treat wounds, inflammation and diabetes. However, there is still a lack of scientific evidence to support these applications. Objective The objective of this study is to evaluate the anti-inflammatory, antioxidant and antidiabetic activities of Hamelia patens, and identify its bioactive compounds. Materials and methods Four extracts were obtained by maceration and liquid-liquid extraction: HEX, DCM-EtOAc, MeOH-EtOAc and MeOH-Aq. The anti-inflammatory effect was evaluated orally on rat paw carrageenan-induced oedema over 6 h (50, 200 and 500 mg/kg), and topically in mouse ear oedema induced by 12-tetradecanoylphorbol-13-acetate (TPA) after 4 h (0.5 and 1 mg/ear). We also evaluated myeloperoxidase levels in ear tissue, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability, and in vitro α-glucosidase inhibition. The chemical compounds were separated by column chromatography and identified by spectroscopic analysis. Results We found that the oral administration of the HEX extract at 500 and 200 mg/kg significantly decreased the carrageenan-induced inflammation after 1 and 3 h, respectively. The MeOH-EtOAc extract significantly inhibited myeloperoxidase activity (83.5%), followed by the DCM-EtOAc extract (76%), β-sitosterol/stigmasterol (72.7%) and the HEX extract (55%), which significantly decreased oedema induced by TPA at both doses, giving a similar effect to indomethacin. We also found that the MeOH-EtOAc, MeOH-Aq and DCM-EtOAc extracts showed good DPPH scavenging activity (IC50 values of 18.6, 93.9 and 158.2 μg/mL, respectively). The HEX extract showed the lowest α-glucosidase inhibition (an IC50 value of 26.07 μg/mL), followed by the MeOH-EtOAc extract (an IC50 value of 30.18 μg/mL), β-sitosterol/stigmasterol (IC50 34.6 μg/mL) and compound A ((6E,10E,14E,18E)-2,6,10,14,18,23-hexamethyl-2,6,10,14,18,22-tetracosahexaene, an IC50 value of 114.6 μg/mL), which were

  1. Acaricidal activity of Lippia gracilis essential oil and its major constituents on the tick Rhipicephalus (Boophilus) microplus.

    PubMed

    Cruz, Elizangela Mércia de Oliveira; Costa, Livio Martins; Pinto, Jessika Andreza Oliveira; Santos, Darlisson de Alexandria; de Araujo, Sandra Alves; Arrigoni-Blank, Maria de Fátima; Bacci, Leandro; Alves, Péricles Barreto; Cavalcanti, Sócrates Cabral de Holanda; Blank, Arie Fitzgerald

    2013-07-01

    The present study aimed to evaluate the activity of Lippia gracilis Schauer essential oil obtained from different L. gracilis genotypes and their major components, carvacrol and thymol against Rhipicephalus (Boophilus) microplus (cattle tick) larvae and engorged females. The larval test was performed parallel to the adult immersion test for engorged females for four L. gracilis genotypes. Similar tests were further performed for their major compounds carvacrol and thymol. Carvacrol (LC50 of 0.22 and 4.46 mg/mL, to larvae and engorged females, respectively) was more efficient than thymol (LC50 of 3.86 and 5.50 mg/mL, to larvae and engorged females, respectively). The lethal concentrations obtained for the isolated essential oil from genotypes LGRA-201 against larvae (1.31 mg/mL) and LGRA-106 against engorged females (4.66 mg/mL) confirmed the acaricidal activity of L. gracilis essential oil and its effectiveness in controlling the southern cattle tick. PMID:23337330

  2. The hop constituent xanthohumol exhibits hepatoprotective effects and inhibits the activation of hepatic stellate cells at different levels

    PubMed Central

    Weiskirchen, Ralf; Mahli, Abdo; Weiskirchen, Sabine; Hellerbrand, Claus

    2015-01-01

    Xanthohumol is the principal prenylated flavonoid of the female inflorescences of the hop plant. In recent years, various beneficial xanthohumol effects including anti-inflammatory, antioxidant, hypoglycemic activities, and anticancer effects have been revealed. This review summarizes present studies indicating that xanthohumol also inhibits several critical pathophysiological steps during the development and course of chronic liver disease, including the activation and pro-fibrogenic genotype of hepatic stellate cells. Also the various mechanism of action and molecular targets of the beneficial xanthohumol effects will be described. Furthermore, the potential use of xanthohumol or a xanthohumol-enriched hop extract as therapeutic agent to combat the progression of chronic liver disease will be discussed. It is notable that in addition to its hepatoprotective effects, xanthohumol also holds promise as a therapeutic agent for treating obesity, dysregulation of glucose metabolism and other components of the metabolic syndrome including hepatic steatosis. Thus, therapeutic xanthohumol application appears as a promising strategy, particularly in obese patients, to inhibit the development as well as the progression of non-alcoholic fatty liver disease. PMID:25999863

  3. Asparagus cochinchinensis Extract Alleviates Metal Ion-Induced Gut Injury in Drosophila: An In Silico Analysis of Potential Active Constituents

    PubMed Central

    Zhang, Weiyu; Jin, Li Hua

    2016-01-01

    Metal ions and sulfate are components of atmospheric pollutants that have diverse ways of entering the human body. We used Drosophila as a model to investigate the effect of Asparagus cochinchinensis (A. cochinchinensis) extracts on the gut and characterized gut homeostasis following the ingestion of metal ions (copper, zinc, and aluminum). In this study, we found that the aqueous A. cochinchinensis extract increased the survival rate, decreased epithelial cell death, and attenuated metal ion-induced gut morphological changes in flies following chronic exposure to metal ions. In addition, we screened out, by network pharmacology, six natural products (NPs) that could serve as putative active components of A. cochinchinensis that prevented gut injury. Altogether, the results of our study provide evidence that A. cochinchinensis might be an effective phytomedicine for the treatment of metal ion-induced gut injury. PMID:27123034

  4. Asparagus cochinchinensis Extract Alleviates Metal Ion-Induced Gut Injury in Drosophila: An In Silico Analysis of Potential Active Constituents.

    PubMed

    Zhang, Weiyu; Jin, Li Hua

    2016-01-01

    Metal ions and sulfate are components of atmospheric pollutants that have diverse ways of entering the human body. We used Drosophila as a model to investigate the effect of Asparagus cochinchinensis (A. cochinchinensis) extracts on the gut and characterized gut homeostasis following the ingestion of metal ions (copper, zinc, and aluminum). In this study, we found that the aqueous A. cochinchinensis extract increased the survival rate, decreased epithelial cell death, and attenuated metal ion-induced gut morphological changes in flies following chronic exposure to metal ions. In addition, we screened out, by network pharmacology, six natural products (NPs) that could serve as putative active components of A. cochinchinensis that prevented gut injury. Altogether, the results of our study provide evidence that A. cochinchinensis might be an effective phytomedicine for the treatment of metal ion-induced gut injury. PMID:27123034

  5. Constituents of Holothuroidea, 17. Isolation and structure of biologically active monosialo-gangliosides from the sea cucumber Cucumaria echinata.

    PubMed

    Kisa, Fumiaki; Yamada, Koji; Miyamoto, Tomofumi; Inagaki, Masanori; Higuchi, Ryuichi

    2006-07-01

    Three new monosialo-gangliosides, CEG-3 (3), CEG-4 (4), and CEG-5 (5), were obtained, together with two known gangliosides, SJG-1 (1) and CG-1 (2), from the lipid fraction of the chloroform/methanol extract of the sea cucumber Cucumaria echinata. The structures of the new gangliosides were determined on the basis of chemical and spectroscopic evidence to be 1-O-[4-O-acetyl-alpha-L-fucopyranosyl-(1-->11)-(N-glycolyl-alpha-D-neuraminosyl)-(2-->6)-beta-D-glucopyranosyl]-ceramide (3) and 1-O-[alpha-L-fucopyranosyl-(1-->11)-(N-glycolyl-alpha-D-neuraminosyl)-(2-->6)-beta-D-glucopyranosyl]-ceramide (4, 5). The ceramide moieties of each compound were composed of heterogeneous sphingosine or phytosphingosine bases, and 2-hydroxy or nonhydroxylated fatty acid units. These gangliosides showed neuritogenic activity toward the rat pheochromocytoma cell line PC-12 in the presence of nerve growth factor. PMID:16819216

  6. In vitro evaluation of the antioxidant and cytotoxic activities of constituents of the mangrove Lumnitzera racemosa Willd.

    PubMed

    Nguyen, Phuong Thao; Bui, Thi Thuy Luyen; Chau, Ngoc Diep; Bui, Huu Tai; Kim, Eun Ji; Kang, Hee Kyoung; Lee, Sang Hyun; Jang, Hae Dong; Nguyen, The Cuong; Nguyen, Van Thanh; Nguyen, Xuan Cuong; Nguyen, Hoai Nam; Chau, Van Minh; Kim, Young Ho

    2015-04-01

    This study performed phytochemical and bioactive assessments of the mangrove Lumnitzera racemosa Willd. leaves. Bioassay-guided fractionation of the methanolic extracts led to the identification of thirty-six compounds (1-36), their structures were elucidated using detailed NMR spectroscopic and MS analysis. The extracts, fractions, and the isolated compounds were screened for potential antioxidant and cytotoxic activities. Antioxidant assays were performed using peroxyl radical-scavenging and reducing assays, whereas cytotoxicity was measured using MTT assays in HL-60 and Hel-299 cell lines. The methanolic extract, CH2Cl2 and n-BuOH fractions (10.0 μg/mL) exhibited potent antioxidant activity, with Trolox equivalent (TE) values of 24.94 ± 0.59, 28.34 ± 0.20, and 27.09 ± 0.37 (μM), respectively. In addition, the isolated compounds exerted cytotoxic effects in a dose-dependent manner; compounds 1 and 14 exhibited the most potent cytotoxicity in HL-60 cells, with IC50 values of 0.15 ± 0.29 and 0.60 ± 0.16 μM, respectively. To clarify the mechanism(s) behind these cytotoxic effects, we measured the time-dependent changes in apoptotic markers including the condensation and fragmentation of nuclear chromatin, and the downregulation of p-ERK1/2, p-AKT, and c-Myc levels. PMID:25001899

  7. In vivo evaluation of analgesic, anti-inflammatory, and neuropharmacological activities of the chemical constituent from Nepeta clarkei.

    PubMed

    Hussain, Javid; Rehman, Najeeb Ur; Al-Harrasi, Ahmed; Khan, Abdul Latif; Rizvi, Tania Shamim; Mohammad, Faryal Vali; Mehjabeen; Ali, Liaqat

    2015-06-01

    The plant species of genus Nepeta are used to treat various human diseases and for ornamental purposes as well. Nepethalate B (1) was isolated as a result of phytochemical investigations of Nepeta clarkei and was subjected in the present study for investigation of analgesic, anti-inflammatory, and central nervous system (CNS) depressant activities. The percentage inhibition in phase I of the acetic acid induced writhing test of compound 1 (dose of 0.1, 0.2 and 0.4 mg/kg of body weight) was 53.3, 58.0 and 86.7% respectively. These results were found significantly higher (P < 0.01) as compared to the negative control. Moreover, the percentage inhibitions of three phases for 0.1, 0.2 and 0.4 mg/kg were higher than the values obtained for Aspirin (positive control). In formalin test, the percentage pain inhibition between 0 and 5 min (early phase) was 68.0, 25.5, and 75.5% for 0.1, 0.2 and 0.4 mg/kg intra-peritoneal doses of compound 1 respectively. In case of late phase (20-30 min) it was 63.0, 66.7 and 48.1%, respectively. In comparison to aspirin, overall percentage inhibition of compound 1 was significantly higher in early and late phases. Interestingly, at all doses compound 1 showed more potent anti-inflammatory effects in terms of intensity and duration as compared to aspirin. The gross behavioral study of nepethalate B (1) was also carried out and the results revealed that it exhibited CNS depression in the mice and showed a prominent decrease in locomotor activity. PMID:25245563

  8. Antioxidant and α-glucosidase inhibitory activities of cucurbit fruit vegetables and identification of active and major constituents from phenolic-rich extracts of Lagenaria siceraria and Sechium edule.

    PubMed

    Sulaiman, Shaida Fariza; Ooi, Kheng Leong; Supriatno

    2013-10-23

    Antioxidant and α-glucosidase activities and total phenolic contents (TPC) in sequential extracts of dried pulps from seven cucurbit fruit vegetables were determined for the first time. The highest TPC and metal chelating activity were obtained from the chloroform extracts of Luffa acutangula (28.04 ± 0.37 mg GAE/g extract) and Benincasa hispida (EC50 = 0.44 ± 0.03 mg/mL), respectively. The ethyl acetate extract of Sechium edule showed the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity (951.73 ± 29.14 mM TE/g extract). The highest reducing and anti-α-glucosidase activities were shown by the methanol and ethyl acetate extracts of Momordica charantia (692.56 ± 43.38 mM AscAE/g extract; 66.64 ± 2.94%, respectively). The highest correlation (r = 0.99) was observed between the TPC and DPPH values of S. edule. Although caffeic acid was quantified as the major constituent in the methanol extract of Lagenaria siceraria , isoquercetin was found to be the main contributor to the activities. Gallic acid was identified as both the main and most active antioxidant constituent in the ethyl acetate extract of S. edule. PMID:24059845

  9. Volatile constituents of Trifolium pratense spp. nivale quantified at different growth stages, and evaluation of their antimicrobial activity.

    PubMed

    Cecotti, Roberto; Carpana, Emanuele; Bergomi, Patrizia; Tava, Aldo

    2013-11-01

    The composition of the volatile fraction of Trifolium pratense L. ssp. nivale (Sieber) Asch. et Gr. from the southwestern Alps was investigated. Fresh aerial parts were collected in the summer at three different growth stages, namely vegetative, flowering and fruiting. The oils obtained by steam-distillation accounted for 0.006 to 0.011% of the fresh plant material and their composition was determined by GC/FID and GC/MS. Several classes of compounds were found, with a predominance of alcohols in all phases, followed by aldehydes, hydrocarbons, terpenes, phenolics, ketones, acids and esters. The oil composition varied both in quantity and quality; the most abundant compounds were oct-1-en-3-ol and phenylacetaldehyde in the vegetative and flowering phases, and phenylacetaldehyde and 2-phenylethanol in the fruiting phase. The essential oils obtained were tested for activity against two major bee pests, i.e. Paenibacillus larvae and Melissococcus plutonius, and against a reference bacterial species, Bacillus subtilis. PMID:24427957

  10. Evaluation of chemical constituents and free-radical scavenging activity of Swarnabhasma (gold ash), an ayurvedic drug.

    PubMed

    Mitra, A; Chakraborty, S; Auddy, B; Tripathi, P; Sen, S; Saha, A V; Mukherjee, B

    2002-05-01

    From ancient times, Swarnabhasma (gold ash) has been used in several clinical manifestations including loss of memory, defective eyesight, infertility, overall body weakness and incidence of early aging. Swarnabhasma has been used by Ayurvedic physicians to treat different diseases like bronchial asthma, rheumatoid arthritis, diabetes mellitus, nervous disorders, etc. In the present investigation, Swarnabhasma was prepared after proper purification and calcination as per Ayurvedic pharmacy which consisted of Realger (As(2)S(2)), Lead oxide (Pb(3)O(4)), Pure gold (Au) and Latex of Calotropis gigantea. Qualitative analyses indicated that Swarnabhasma contained not only gold but also several microelements (Fe, Al, Cu, Zn, Co, Mg, Ca, As, Pb, etc.). Infrared spectroscopy showed that the material was free from any organic compound. The metal content in the bhasma was determined by atomic absorption spectrometry. Acute oral administration of Swarnabhasma showed no mortality in mice (up to 1 ml /20 g b.w. of Swarnabhasma suspension containing 1mg of drug). Chronic administration of Swarnabhasma also showed no toxicity as judged by SGPT, SGOT, serum creatinine and serum urea level and histological studies. In an experimental animal model, chronic Swarnabhasma-treated animals showed significantly increased superoxide dismutase and catalase activity, two enzymes that reduce free radical concentrations in the body. PMID:12007704

  11. Measurements of thermospheric response to auroral activities

    NASA Technical Reports Server (NTRS)

    Okano, S.; Kim, J. S.

    1986-01-01

    The Joule heating produced by auroral electrojets and its thermospheric response can be studied by monitoring the thermospheric temperatures by optical methods; simultaneously, the concurrent auroral electrojet activities can be investigated by using geomagnetic records obtained from stations along a meridian close to the observation site of optical measurements. The measurements are reported of thermospheric response to auroral activities which were made at Albany (42.68 deg N, 73.82 deg W), New York on September 2, 1978 (UT) when an isolated substorm occured. The thermospheric temperatures were measured by using a high resolution Fabry-Perot interferometer that determines the line profiles of the (OI) 6300A line emission. The intensities and latitudinal positions of auroral electrojets were obtained by the analysis of magnetograms from the IMS Fort Churchill meridian chain stations.

  12. Chemical composition, larvicidal, and biting deterrent activity of essential oils of two subspecies of Tanacetum argenteum (Asterales: Asteraceae) and individual constituents against Aedes aegypti (Diptera: Culicidae).

    PubMed

    Ali, Abbas; Tabanca, Nurhayat; Kurkcuoglu, Mine; Duran, Ahmet; Blythe, Eugene K; Khan, Ikhlas A; Baser, K Husnu Can

    2014-07-01

    Water-distilled essential oils from dried aerial parts of Tanacetum argenteum (Lam.) Willd. subsp. argenteum (Lam.) and T. argenteum (Lam.) Willd. subsp. canum (C. Koch) Grierson were analyzed by gas chromatography and gas chromatography-mass spectrometry. In total, 27 and 32 components were identified representing 97.2 and 98.7% of essential oils of subsp. argenteum and canum, respectively. Main compounds of T. argenteum subsp. argenteum were alpha-pinene (67.9%) and beta-pinene (4.8%), whereas alpha-pinene (53.6%), 1, 8-cineole (14.8%), and camphor (4.7%) were the major constituents of subsp. canum. Essential oil of T. argenteum subsp. canum at 10 microg/cm2 with Biting Deterrent Index (BDI) value of 0.73 showed activity similar to N,N-Diethyl-meta-toluamide (DEET) at 25 mol/cm2, whereas the activity of essential oil of subsp. argenteum was lower (BDI = 0.47) than subsp. canum and DEET. Based on 95% CIs, activity of beta-caryophyllene (BDI value = 0.54) and caryophyllene oxide (BDI = 0.66) were significantly lower than DEET. In larval bioassays, essential oil of T. argenteum subsp. argenteum showed LC50 value of 93.34 ppm, whereas T. argenteum subsp. canum killed only 40% of the larvae at the highest dose of 125 ppm. Among the pure compounds, beta-caryophyllene (LC50 = 26 ppm) was the most potent compound followed by caryophyllene oxide (LC50 = 29 ppm), which was also similar to (-)-beta-pinene (LC50 = 35.9 ppm) against 1-d-old Ae. aegypti larvae at 24-h post treatment. Compounds (-)-alpha-pinene and (+)-beta-pinene showed similar larvicidal activity. Activity of (+)-alpha-pinene with LC50 value of was similar to the essential oil of T. argenteum subsp. argenteum. PMID:25118415

  13. Alkaloid constituents from flower buds and leaves of sacred lotus (Nelumbo nucifera, Nymphaeaceae) with melanogenesis inhibitory activity in B16 melanoma cells.

    PubMed

    Nakamura, Seikou; Nakashima, Souichi; Tanabe, Genzo; Oda, Yoshimi; Yokota, Nami; Fujimoto, Katsuyoshi; Matsumoto, Takahiro; Sakuma, Rika; Ohta, Tomoe; Ogawa, Keiko; Nishida, Shino; Miki, Hisako; Matsuda, Hisashi; Muraoka, Osamu; Yoshikawa, Masayuki

    2013-02-01

    Methanolic extracts from the flower buds and leaves of sacred lotus (Nelumbo nucifera, Nymphaeaceae) were found to show inhibitory effects on melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. From the methanolic extracts, a new alkaloid, N-methylasimilobine N-oxide, was isolated together with eleven benzylisoquinoline alkaloids. The absolute stereostructure of the new alkaloid was determined from chemical and physicochemical evidence. Among the constituents isolated, nuciferine, N-methylasimilobine, (-)-lirinidine, and 2-hydroxy-1-methoxy-6a,7-dehydroaporphine showed potent inhibition of melanogenesis. Comparison of the inhibitory activities of synthetic related alkaloids facilitated characterization of the structure-activity relationships of aporphine- and benzylisoquinoline-type alkaloids. In addition, 3-30 μM nuciferine and N-methylasimilobine inhibited the expression of tyrosinase mRNA, 3-30 μM N-methylasimilobine inhibited the expression of TRP-1 mRNA, and 10-30 μM nuciferine inhibited the expression of TRP-2 mRNA. PMID:23270663

  14. Chemical constituents and antioxidant activity of essential oil and organic extract from the peel and kernel parts of Citrus japonica Thunb. (kumquat) from Iran.

    PubMed

    Nouri, Amrah; Shafaghatlonbar, Ali

    2016-05-01

    The constituents of essential oils and organic extracts from peel and kernels of Citrus japonica were analysed by GC and GC/MS. The content of essential oil in peel and kernel was 1.1 and 0.8% based on dry weight. The essential oil of C. japonica peel and kernel was characterised by a higher amount of limonene (51.0 and 47.1%) and germacrene D (12.1 and 6.3%), and the hexane extracts of its peel and kernel were characterised by a higher amount of dodecanol-1(12.9 and 20.8%) and linolenic acid (13.1 and 16.3%), respectively. The antioxidant activities of oils were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. The results indicate that both oils from different parts of C. japonica possess considerable antioxidant activity. The fruit peel and kernel essential oil could thus be useful in the industries, chiefly in the food and pharmaceutical industries. PMID:26500054

  15. Simultaneous quantification of 25 active constituents in the total flavonoids extract from Herba Desmodii Styracifolii by high-performance liquid chromatography with electrospray ionization tandem mass spectrometry.

    PubMed

    Guo, Panpan; Yan, Wenying; Han, Qingjie; Wang, Chunying; Zhang, Zijian

    2015-04-01

    A sensitive and selective high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry method has been developed and validated for the simultaneous determination of 25 active constituents, including 21 flavonoids and four phenolic acids in the total flavonoids extract from Herba Desmodii Styracifolii for the first time. Among the 25 compounds, seven compounds including caffeic acid, acacetin, genistein, genistin, diosmetin, diosmin and hesperidin were identified and quantified for the first time in Herba Desmodii Styracifolii. Chromatographic separation was accomplished on a ZORBAX SB-C18 (250 mm×4.6 mm, 5.0 μm) column using gradient elution of methanol and 0.1‰ acetic acid v/v at a flow rate of 1.0 mL/min. The identification and quantification of the analytes were achieved using negative electrospray ionization mass spectrometry in multiple-reaction monitoring mode. The method was fully validated in terms of limits of detection and quantification, linearity, precision and accuracy. The results indicated that the developed method is simple, rapid, specific and reliable. Furthermore, the developed method was successfully applied to quantify the 25 active components in six batches of total flavonoids extract from Herba Desmodii Styracifolii. PMID:25620156

  16. Laboratory and Simulated Field Bioassays to Evaluate Larvicidal Activity of Pinus densiflora Hydrodistillate, Its Constituents and Structurally Related Compounds against Aedes albopictus, Aedes aegypti and Culex pipiens pallens in Relation to Their Inhibitory Effects on Acetylcholinesterase Activity.

    PubMed

    Lee, Dong Chan; Ahn, Young-Joon

    2013-01-01

    The toxicity of Pinus densiflora (red pine) hydrodistillate, its 19 constituents and 28 structurally related compounds against early third-instar larvae of Aedes albopictus (Ae. albopictus), Aedes aegypti (Ae. aegypti) and Culex pipiens palles (Cx. p. pallens) was examined using direct-contact bioassays. The efficacy of active compounds was further evaluated in semi-field bioassays using field-collected larval Cx. p. pallens. Results were compared with those of two synthetic larvicides, temephos and fenthion. In laboratory bioassays, Pinus densiflora hydrodistillate was found to have 24 h LC50 values of 20.33, 21.01 and 22.36 mg/L against larval Ae. albopictus, Ae. aegypti and Cx. p. pallens respectively. Among the identified compounds, thymol, δ-3-carene and (+)-limonene exhibited the highest toxicity against all three mosquito species. These active compounds were found to be nearly equally effective in field trials as well. In vitro bioassays were conducted to examine the acetylcholinesterase (AChE) inhibitory activity of 10 selected compounds. Results showed that there is a noticeable correlation between larvicidal activity and AChE inhibitory activity. In light of global efforts to find alternatives for currently used insecticides against disease vector mosquitoes, Pinus densiflora hydrodistillate and its constituents merit further research as potential mosquito larvicides. PMID:26464387

  17. Laboratory and Simulated Field Bioassays to Evaluate Larvicidal Activity of Pinus densiflora Hydrodistillate, Its Constituents and Structurally Related Compounds against Aedes albopictus, Aedes aegypti and Culex pipiens pallens in Relation to Their Inhibitory Effects on Acetylcholinesterase Activity

    PubMed Central

    Lee, Dong Chan; Ahn, Young-Joon

    2013-01-01

    The toxicity of Pinus densiflora (red pine) hydrodistillate, its 19 constituents and 28 structurally related compounds against early third-instar larvae of Aedes albopictus (Ae. albopictus), Aedes aegypti (Ae. aegypti) and Culex pipiens palles (Cx. p. pallens) was examined using direct-contact bioassays. The efficacy of active compounds was further evaluated in semi-field bioassays using field-collected larval Cx. p. pallens. Results were compared with those of two synthetic larvicides, temephos and fenthion. In laboratory bioassays, Pinus densiflora hydrodistillate was found to have 24 h LC50 values of 20.33, 21.01 and 22.36 mg/L against larval Ae. albopictus, Ae. aegypti and Cx. p. pallens respectively. Among the identified compounds, thymol, δ-3-carene and (+)-limonene exhibited the highest toxicity against all three mosquito species. These active compounds were found to be nearly equally effective in field trials as well. In vitro bioassays were conducted to examine the acetylcholinesterase (AChE) inhibitory activity of 10 selected compounds. Results showed that there is a noticeable correlation between larvicidal activity and AChE inhibitory activity. In light of global efforts to find alternatives for currently used insecticides against disease vector mosquitoes, Pinus densiflora hydrodistillate and its constituents merit further research as potential mosquito larvicides. PMID:26464387

  18. Stereoselective Effects of Abused “Bath Salt” Constituent 3,4-Methylenedioxypyrovalerone in Mice: Drug Discrimination, Locomotor Activity, and Thermoregulation

    PubMed Central

    Gannon, Brenda M.; Williamson, Adrian; Suzuki, Masaki; Rice, Kenner C.

    2016-01-01

    3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of illicit “bath salts” products. MDPV is a chiral molecule, but the contribution of each enantiomer to in vivo effects in mice has not been determined. To address this, mice were trained to discriminate 10 mg/kg cocaine from saline, and substitutions with racemic MDPV, S(+)-MDPV, and R(−)-MDPV were performed. Other mice were implanted with telemetry probes to monitor core temperature and locomotor responses elicited by racemic MDPV, S(+)-MDPV, and R(−)-MDPV under a warm (28°C) or cool (20°C) ambient temperature. Mice reliably discriminated the cocaine training dose from saline, and each form of MDPV fully substituted for cocaine, although marked potency differences were observed such that S(+)-MDPV was most potent, racemic MDPV was less potent than the S(+) enantiomer, and R(−)-MDPV was least potent. At both ambient temperatures, locomotor stimulant effects were observed after doses of S(+)-MDPV and racemic MDPV, but R(−)-MDPV did not elicit locomotor stimulant effects at any tested dose. Interestingly, significant increases in maximum core body temperature were only observed after administration of racemic MDPV in the warm ambient environment; neither MDPV enantiomer altered core temperature at any dose tested, at either ambient temperature. These studies suggest that all three forms of MDPV induce biologic effects, but R(−)-MDPV is less potent than S(+)-MDPV and racemic MDPV. Taken together, these data suggest that the S(+)-MDPV enantiomer is likely responsible for the majority of the biologic effects of the racemate and should be targeted in therapeutic efforts against MDPV overdose and abuse. PMID:26769917

  19. Gastroprotective activity of Nigella sativa L oil and its constituent, thymoquinone against acute alcohol-induced gastric mucosal injury in rats

    PubMed Central

    Kanter, Mehmet; Demir, Halit; Karakaya, Cengiz; Ozbek, Hanefi

    2005-01-01

    AIM: To evaluate the role of reactive oxygen species in the pathogenesis of acute ethanol-induced gastric mucosal lesions and the effect of Nigella sativa L oil (NS) and its constituent thymoquinone (TQ) in an exper-imental model. METHODS: Male Wistar albino rats were assigned into 4 groups. Control group was given physiologic saline orally (10 mL/kg body weight) as the vehicle (gavage); ethanol group was administrated 1 mL (per rat) absolute alcohol by gavage; the third and fourth groups were given NS (10 mL/kg body weight) and TQ (10 mg/kg body weight p.o) respectively 1 h prior to alcohol intake. One hour after ethanol administration, stomach tissues were excised for macroscopic examination and biochemical analysis. RESULTS: NS and TQ could protect gastric mucosa against the injurious effect of absolute alcohol and promote ulcer healing as evidenced from the ulcer index (UI) values. NS prevented alcohol-induced increase in thiobarbituric acid-reactive substances (TBARS), an index of lipid peroxidation. NS also increased gastric glutathione content (GSH), enzymatic activities of gastric superoxide dismutase (SOD) and glutathione-S-transferase (GST). Likewise, TQ protected against the ulcerating effect of alcohol and mitigated most of the biochemical adverse effects induced by alcohol in gastric mucosa, but to a lesser extent than NS. Neither NS nor TQ affected catalase activity in gastric tissue. CONCLUSION: Both NS and TQ, particularly NS can partly protect gastric mucosa from acute alcohol-induced mucosal injury, and these gastroprotective effects might be induced, at least partly by their radical scavenging activity. PMID:16425361

  20. Active thermal isolation for temperature responsive sensors

    NASA Technical Reports Server (NTRS)

    Martinson, Scott D. (Inventor); Gray, David L. (Inventor); Carraway, Debra L. (Inventor); Reda, Daniel C. (Inventor)

    1994-01-01

    The detection of flow transition between laminar and turbulent flow and of shear stress or skin friction of airfoils is important in basic research for validation of airfoil theory and design. These values are conventionally measured using hot film nickel sensors deposited on a polyimide substrate. The substrate electrically insulates the sensor and underlying airfoil but is prevented from thermally isolating the sensor by thickness constraints necessary to avoid flow contamination. Proposed heating of the model surface is difficult to control, requires significant energy expenditures, and may alter the basic flow state of the airfoil. A temperature responsive sensor is located in the airflow over the specified surface of a body and is maintained at a constant temperature. An active thermal isolator is located between this temperature responsive sensor and the specific surface of the body. The total thickness of the isolator and sensor avoid any contamination of the flow. The temperature of this isolator is controlled to reduce conductive heat flow from the temperature responsive sensor to the body. This temperature control includes (1) operating the isolator at the same temperature as the constant temperature of the sensor; and (2) establishing a fixed boundary temperature which is either less than or equal to, or slightly greater than the sensor constant temperature. The present invention accordingly thermally isolates a temperature responsive sensor in an energy efficient, controllable manner while avoiding any contamination of the flow.

  1. Constituents of Indonesian medicinal plant Averrhoa bilimbi and their cytochrome P450 3A4 and 2D6 inhibitory activities.

    PubMed

    Auw, Lidyawati; Subehan; Sukrasno; Kadota, Shigetoshi; Tezuka, Yasuhiro

    2015-01-01

    As constituents of Averrhoa bilimbi leaves we identified three new compounds (1-3) together with 12 known ones (4-15); their inhibitory activities on cytochrome P450 3A4 (CYP3A4) and 2D6 (CYP2D6) were examined. Among the isolated compounds, the mixture of 1 and 2, and compounds 4 and 9 showed strong inhibition on CYP3A4, but mild or no inhibition on CYP2D6. These compounds revealed the characteristics of 1) time- and concentration-dependent inhibition, 2) requirement of NADPH for the inhibition, 3) no protection by nucleophiles, and 4) suppression of the inhibition by competitive inhibitor. Thus, they are suggested to be mechanism-based inactivators of CYP3A4 and CYP2D6. The kinetic parameters for the inactivation (k(inact) and K(I)) were 0.19 min(-1) and 36.7 μM for the mixture of 1 and 2, 0.126 min(-1) and 10.5 μM for 4, and 0.29 min(-1) and 23.4 μM for 9. PMID:25920220

  2. Dynamic response of active twist rotor blades

    NASA Astrophysics Data System (ADS)

    Cesnik, Carlos E. S.; Shin, Sang Joon; Wilbur, Matthew L.

    2001-02-01

    Dynamic characteristics of active twist rotor (ATR) blades are investigated analytically and experimentally in this paper. The ATR system is intended for vibration and potentially for noise reductions in helicopters through individual blade control. An aeroelastic model is developed to identify frequency response characteristics of the ATR blade with integral, generally anisotropic, strain actuators embedded in its composite construction. An ATR prototype blade was designed and manufactured to experimentally study the vibration reduction capabilities of such systems. Several bench and hover tests were conducted and those results are presented and discussed here. Selected results on sensitivity of the ATR system to collective setting (i.e. blade loading), blade rpm (i.e. centrifugal force and blade station velocity), and media density (i.e. altitude) are presented. They indicated that the twist actuation authority of the ATR blade is independent of the collective setting up to approximately 10P, and dependent on rotational speed and altitude near the torsional resonance frequency due to its dependency on the aerodynamic damping. The proposed model captures very well the physics and sensitivities to selected test parameters of the ATR system. The numerical result of the blade torsional loads show an average error of 20% in magnitude and virtually no difference in phase for the blade frequency response. Overall, the active blade model is in very good agreement with the experiments and can be used to analyze and design future active helicopter blade systems.

  3. Trisomy 21 consistently activates the interferon response

    PubMed Central

    Sullivan, Kelly D; Lewis, Hannah C; Hill, Amanda A; Pandey, Ahwan; Jackson, Leisa P; Cabral, Joseph M; Smith, Keith P; Liggett, L Alexander; Gomez, Eliana B; Galbraith, Matthew D; DeGregori, James; Espinosa, Joaquín M

    2016-01-01

    Although it is clear that trisomy 21 causes Down syndrome, the molecular events acting downstream of the trisomy remain ill defined. Using complementary genomics analyses, we identified the interferon pathway as the major signaling cascade consistently activated by trisomy 21 in human cells. Transcriptome analysis revealed that trisomy 21 activates the interferon transcriptional response in fibroblast and lymphoblastoid cell lines, as well as circulating monocytes and T cells. Trisomy 21 cells show increased induction of interferon-stimulated genes and decreased expression of ribosomal proteins and translation factors. An shRNA screen determined that the interferon-activated kinases JAK1 and TYK2 suppress proliferation of trisomy 21 fibroblasts, and this defect is rescued by pharmacological JAK inhibition. Therefore, we propose that interferon activation, likely via increased gene dosage of the four interferon receptors encoded on chromosome 21, contributes to many of the clinical impacts of trisomy 21, and that interferon antagonists could have therapeutic benefits. DOI: http://dx.doi.org/10.7554/eLife.16220.001 PMID:27472900

  4. Dynamics of active cellular response under stress

    NASA Astrophysics Data System (ADS)

    de, Rumi; Zemel, Assaf; Safran, Samuel

    2008-03-01

    Forces exerted by and on adherent cells are important for many physiological processes such as wound healing and tissue formation. In addition, recent experiments have shown that stem cell differentiation is controlled, at least in part, by the elasticity of the surrounding matrix. Using a simple theoretical model that includes the forces due to both the mechanosensitive nature of cells and the elastic response of the matrix, we predict the dynamics of orientation of cells. The model predicts many features observed in measurements of cellular forces and orientation including the increase with time of the forces generated by cells in the absence of applied stress and the consequent decrease of the force in the presence of quasi-static stresses. We also explain the puzzling observation of parallel alignment of cells for static and quasi-static stresses and of nearly perpendicular alignment for dynamically varying stresses. In addition, we predict the response of the cellular orientation to a sinusoidally varying applied stress as a function of frequency. The dependence of the cell orientation angle on the Poisson ratio of the surrounding material can be used to distinguish systems in which cell activity is controlled by stress from those where cell activity is controlled by strain. Reference: Nature Physics, vol. 3, pp 655 (2007).

  5. The Protective Effect of α-Hederin, the Active Constituent of Nigella sativa, on Lung Inflammation and Blood Cytokines in Ovalbumin Sensitized Guinea Pigs.

    PubMed

    Keyhanmanesh, Rana; Saadat, Saeideh; Mohammadi, Mostafa; Shahbazfar, Amir-Ali; Fallahi, Maryam

    2015-11-01

    In the present study, the preventive effect of two different concentrations of α-hederin, the active constituent of Nigella sativa, on lung inflammation and blood cytokines in ovalbumin sensitized guinea pigs was examined. Forty eight male adult guinea pigs were divided into control (C), sensitized (S) and sensitized pretreated groups; with thymoquinone (S+TQ), low dose (S+LAH) and high dose of α-hederin (S+HAH) and inhaled fluticasone propionate (S+FP). The lung histopathology and blood levels of IL-4, IFN-γ and IL-17 were assessed. Compared to sensitized animals, all pathological changes improved significantly in pretreated groups (p < 0.001 to p < 0.05). These improvements in α-hederin pretreated groups were similar to S+TQ and S+FP groups except cellular infiltration in S+LAH and S+HAH groups which was lower than S+TQ group (p < 0.05). The blood IL-4 and IL-17 levels in S+HAH groups showed a significant decrease compared to S group (p < 0.05) which were similar to S+TQ and S+FP groups. The level of IFN-γ in S+LAH and S+HAH groups increased significantly compared to S group (p < 0.05) which was higher than S+FP group (p < 0.05). Blood IL-4 in S+HAH group was significantly lower than S+LAH group (p < 0.05). In conclusion, α-hederin could attenuate the lung inflammation and improve the changes of cytokines like thymoquinone and fluticasone in used dosages. PMID:26292851

  6. Identification of the mosquito biting deterrent constituents from the Indian folk remedy plant Jatropha curcas

    Technology Transfer Automated Retrieval System (TEKTRAN)

    An investigation of the Indian folk remedy plant, Jatropha curcas, was performed to specifically identify the constituents responsible for the mosquito biting deterrent activity of the oil as a whole. Jatropha curcas seed oil is burned in oil lamps in India and part of Africa to repel biting insect...

  7. Isolation and identification of kahweol palmitate and cafestol palmitate as active constituents of green coffee beans that enhance glutathione S-transferase activity in the mouse.

    PubMed

    Lam, L K; Sparnins, V L; Wattenberg, L W

    1982-04-01

    Glutathione (GSH) S-transferase is a major detoxification enzyme system that catalyzes the binding of a variety of electrophiles, including reactive forms of chemical carcinogens, to GSH. Green coffee beans fed in the diet induced increased GSH S-transferase activity in the mucosa of the small intestine and in the liver of mice. A potent compound that induces increased GSH S-transferase activity was isolated from green coffee beans and identified as kahweol palmitate. The corresponding free alcohol, kahweol, and its synthetic monoacetate are also potent inducers of the activity of GSH S-transferase. A similar diterpene ester, cafestol palmitate, isolated from green coffee beans was active but less so than was kahweol palmitate. Likewise, the corresponding alcohol, cafestol, and its monoacetate showed moderate potency as inducers of increased GSH S-transferase activity. Kahweol palmitate and cafestol palmitate were extracted from green coffee beans into petroleum ether. The petroleum ether extract was fractionated by preparative normal-phase and reverse-phase liquid chromatographies successively. Final purification with silver nitrate-impregnated thin-layer chromatography yielded the pure palmitates of cafestol and kahweol. The structures were determined by examination of the spectroscopic data of the esters and their parent alcohols and by derivative comparison. PMID:7059995

  8. Hazardous constituent source term. Revision 2

    SciTech Connect

    Not Available

    1994-11-17

    The Department of Energy (DOE) has several facilities that either generate and/or store transuranic (TRU)-waste from weapons program research and production. Much of this waste also contains hazardous waste constituents as regulated under Subtitle C of the Resource Conservation and Recovery Act (RCRA). Toxicity characteristic metals in the waste principally include lead, occurring in leaded rubber gloves and shielding. Other RCRA metals may occur as contaminants in pyrochemical salt, soil, debris, and sludge and solidified liquids, as well as in equipment resulting from decontamination and decommissioning activities. Volatile organic compounds (VOCS) contaminate many waste forms as a residue adsorbed on surfaces or occur in sludge and solidified liquids. Due to the presence of these hazardous constituents, applicable disposal regulations include land disposal restrictions established by Hazardous and Solid Waste Amendments (HSWA). The DOE plans to dispose of TRU-mixed waste from the weapons program in the Waste Isolation Pilot Plant (WIPP) by demonstrating no-migration of hazardous constituents. This paper documents the current technical basis for methodologies proposed to develop a post-closure RCRA hazardous constituent source term. For the purposes of demonstrating no-migration, the hazardous constituent source term is defined as the quantities of hazardous constituents that are available for transport after repository closure. Development of the source term is only one of several activities that will be involved in the no-migration demonstration. The demonstration will also include uncertainty and sensitivity analyses of contaminant transport.

  9. Seaweed extracts and unsaturated fatty acid constituents from the green alga Ulva lactuca as activators of the cytoprotective Nrf2–ARE pathway

    PubMed Central

    Wang, Rui; Paul, Valerie J.; Luesch, Hendrik

    2013-01-01

    Increased amounts of reactive oxygen species (ROS) have been implicated in many pathological conditions, including cancer. The major machinery that the cell employs to neutralize excess ROS is through the activation of the antioxidant-response element (ARE) that controls the activation of many phase II detoxification enzymes. The transcription factor that recognizes the ARE, Nrf2, can be activated by a variety of small molecules, most of which contain an α,β-unsaturated carbonyl system. In the pursuit of chemopreventive agents from marine organisms, we built, fractionated, and screened a library of 30 field-collected eukaryotic algae from Florida. An edible green alga, Ulva lactuca, yielded multiple active fractions by ARE–luciferase reporter assay. We isolated three monounsaturated fatty acid (MUFA) derivatives as active components, including a new keto-type C18 fatty acid (1), the corresponding shorter chain C16 acid (2), and an amide derivative (3) of the C18 acid. Their chemical structures were elucidated by NMR and mass spectrometry. All three contain the conjugated enone motif between C7 and C9, which is thought to be responsible for the ARE activity. Subsequent biological studies focused on 1, the most active and abundant ARE activator isolated. C18 acid 1 induced the expression of ARE-regulated cytoprotective genes, including NAD(P)H:quinone oxidoreductase 1, heme oxygenase 1, thioredoxin reductase 1, both subunits of the glutamate–cysteine ligase (catalytic subunit and modifier subunit), and the cystine/glutamate exchange transporter, in IMR-32 human neuroblastoma cells. Its cellular activity requires the presence of Nrf2 and PI3K function, based on RNA interference and pharmacological inhibitor studies, respectively. Treatment with 1 led only to Nrf2 activation, and not the increase in production of NRF2 mRNA. To test its ARE activity and cytoprotective potential in vivo, we treated mice with a single dose of a U. lactuca fraction that was enriched

  10. Seaweed extracts and unsaturated fatty acid constituents from the green alga Ulva lactuca as activators of the cytoprotective Nrf2-ARE pathway.

    PubMed

    Wang, Rui; Paul, Valerie J; Luesch, Hendrik

    2013-04-01

    Increased amounts of reactive oxygen species (ROS) have been implicated in many pathological conditions, including cancer. The major machinery that the cell employs to neutralize excess ROS is through the activation of the antioxidant-response element (ARE) that controls the activation of many phase II detoxification enzymes. The transcription factor that recognizes the ARE, Nrf2, can be activated by a variety of small molecules, most of which contain an α,β-unsaturated carbonyl system. In the pursuit of chemopreventive agents from marine organisms, we built, fractionated, and screened a library of 30 field-collected eukaryotic algae from Florida. An edible green alga, Ulva lactuca, yielded multiple active fractions by ARE-luciferase reporter assay. We isolated three monounsaturated fatty acid (MUFA) derivatives as active components, including a new keto-type C18 fatty acid (1), the corresponding shorter chain C16 acid (2), and an amide derivative (3) of the C18 acid. Their chemical structures were elucidated by NMR and mass spectrometry. All three contain the conjugated enone motif between C7 and C9, which is thought to be responsible for the ARE activity. Subsequent biological studies focused on 1, the most active and abundant ARE activator isolated. C18 acid 1 induced the expression of ARE-regulated cytoprotective genes, including NAD(P)H:quinone oxidoreductase 1, heme oxygenase 1, thioredoxin reductase 1, both subunits of the glutamate-cysteine ligase (catalytic subunit and modifier subunit), and the cystine/glutamate exchange transporter, in IMR-32 human neuroblastoma cells. Its cellular activity requires the presence of Nrf2 and PI3K function, based on RNA interference and pharmacological inhibitor studies, respectively. Treatment with 1 led only to Nrf2 activation, and not the increase in production of NRF2 mRNA. To test its ARE activity and cytoprotective potential in vivo, we treated mice with a single dose of a U. lactuca fraction that was enriched with

  11. Banisteriopsis caapi, a unique combination of MAO inhibitory and antioxidative constituents for the activities relevant to neurodegenerative disorders and Parkinson’s disease

    PubMed Central

    Samoylenko, Volodymyr; Rahman, Md. Mostafizur; Tekwani, Babu L.; Tripathi, Lalit M.; Wang, Yan-Hong; Khan, Shabana I.; Khan, Ikhlas A.; Miller, Loren S.; Joshi, Vaishali C.; Muhammad, Ilias

    2009-01-01

    Aim of the study Parkinson’s disease is a neurological disorder mostly effecting the elder population of the world. Currently there is no definitive treatment or cure for this disease. Therefore, in this study the composition and constituents of the aqueous extract of B. caapi for monoamine oxidases (MAO) inhibitory and antioxidant activities were assessed, which are relevant to the prevention of neurological disorders, including Parkinsonism. Materials and methods The aqueous extract of B. caapi stems was standardized and then fractionated using reversed-phase (RP) chromatography. Pure compounds were isolated either by reversed-phase (RP) chromatography or centrifugal preparative TLC, using a Chromatotron®. Structure elucidation was carried out by 1D and 2D NMR, Mass, IR and Circular Dichroism spectroscopy and chemical derivatization. Chemical profiling of the extract was carried out with RP-HPLC. The inhibitory activity of MAO-A, MAO-B, acetylcholinesterase, butyrylcholinesterase and catechol-O-methyl transferase enzymes, as well as antioxidant and cytotoxic activities of both B. caapi extract and isolated compounds were evaluated. Results An examination of the aqueous extracts of B. caapi cultivar Da Vine yielded two new alkaloidal glycosides, named banistenoside A (1) and banistenoside B (2), containing “azepino[1,2-a]tetrahydro-β-carboline” unique carbon framework. One additional new natural tetrahydronorharmine (4), four known β-carbolines harmol (3), tetrahydroharmine (5), harmaline (6) and harmine (7), two known proanthocyanidines (−)-epicatechin (8) and (−)-procyanidin B2 (9), and a new disaccharide β-D-fructofuranosyl-(2→5)-fructopyranose (14) together with known sacharose (15) and β-D-glucose (16) were also isolated. In addition, the acetates of 1, 2, 8, 9, 14 and 15 (compounds 10–13, 17, 18) were also prepared. Harmaline (6) and harmine (7) showed potent in vitro inhibitory activity against recombinant human brain monoamine oxidase

  12. Phenolic constituents of the Bangladeshi medicinal plant Pothos scandens and their anti-estrogenic, hyaluronidase inhibition, and histamine release inhibitory activities.

    PubMed

    Muhit, Md Abdul; Izumikawa, Masahiro; Umehara, Kaoru; Noguchi, Hiroshi

    2016-01-01

    Extracts from the stem and roots of the Bangladeshi medicinal plant Pothos scandens L. (Araceae) were isolated, and three hemiterpene glucoside aromatic esters, pothobanosides A (1), B (2), and C (3), and a phenylisobutanoid, pothobanol (4), along with 14 known compounds, were characterized. The isolates were tested for their estrogenic/anti-estrogenic activity using the estrogen-responsive human breast cancer cell lines MCF-7 and T47D, and syringoyl derivatives (2, 3, and canthoside B) showed strong inhibitory activity against both cell lines. Their less oxygenated analogs (1, and markhamioside F) were almost inactive. The isolates were also evaluated for hyaluronidase and histamine release inhibitory activities, and pothobanoside A (1) showed significant hyaluronidase inhibitory activity among the isolated compounds, which was similar to that of the positive control rosmarinic acid. Because hyaluronidase produces an angiogenic response that has been implicated in tumor invasiveness and metastasis, 1 could be valuable as an anti-tumor compound with a different mechanism of action from related compounds (2, 3). Pothobanoside C (3) and pothobanol (4) were also found to inhibit histamine release to a similar degree to the positive control epigallocatechin 3-O-(3"-O-methyl)-gallate. The histamine release inhibitory potency of these isolates may support the traditional uses of this plant in folk medicine. PMID:26542239

  13. Human platelet glycoprotein Ia. One component is only expressed on the surface of activated platelets and may be a granule constituent

    SciTech Connect

    Bienz, D.; Clemetson, K.J.

    1989-01-05

    Glycoprotein Ia (GP Ia) is a relatively minor component of human blood platelets thought to be a receptor involved in collagen-induced platelet activation. However, some difficulties exist with the definition of this glycoprotein. The expression of GP Ia on resting (prostacyclin analogue-treated) and thrombin-activated platelets was compared by surface labeling with /sup 125/I-lactoperoxidase. Intact platelets or platelets solubilized in sodium dodecyl sulfate were labeled with periodate/(/sup 3/H)NaBH/sub 4/. Analysis on two-dimensional isoelectric focusing/sodium dodecyl sulfate-polyacrylamide gel electrophoresis gels showed that GP Ia is very poorly labeled in resting platelets. After activation a new spot (GP Ia*) appears with the same relative molecular mass as GP Ia under reducing conditions. GP Ia and Ia* can be clearly separated by two-dimensional nonreduced/reduced gel electrophoresis. Therefore, two glycoproteins which have been termed GP Ia exist in platelets with similar molecular weight and pI under reducing conditions. One of these (GP Ia*) is only surface-labeled when platelets are activated, indicating that it is only exposed on the surface of activated platelets. Supernatant from activated platelets contains this glycoprotein as well as other granule components. This glycoprotein is missing in platelets from two patients with collagen-response defects.

  14. Thymoquinone, an active constituent of Nigella sativa seeds, binds with bilirubin and protects mice from hyperbilirubinemia and cyclophosphamide-induced hepatotoxicity.

    PubMed

    Laskar, Amaj A; Khan, Masood A; Rahmani, Arshad H; Fatima, Sana; Younus, Hina

    2016-08-01

    Some reports indicate that thymoquinone (TQ), the main constituent of Nigella sativa seeds, is hepatoprotective. The aim of this study was to determine whether TQ is able to bind directly to bilirubin, and whether TQ or liposomal formulation of TQ (Lip-TQ) can reduce cyclophosphamide (CYP)-induced liver toxicity, serum bilirubin level in mice. The binding of TQ with bilirubin was studied by UV-VIS, fluorescence and Near-UV CD spectroscopy. Inhibition of binding of bilirubin to erythrocytes by TQ was also examined. To increase the in vivo efficacy, Lip-TQ was prepared and used against CYP-induced toxicity. The protective role of TQ or Lip-TQ against CYP-induced toxicity was assessed by determining the liver function parameters, the levels of superoxide dismutase (SOD) and catalase (CAT), and histological studies. It was found that TQ binds to bilirubin and significantly inhibits the binding of bilirubin to erythrocytes. Lip-TQ (10 mg/kg) significantly reduced the levels of aspartate transaminase (AST) from 254 ± 48 to 66 ± 18 IU/L (P < 0.001), alanine transaminase (ALT) from 142 ± 28 to 47.8 ± 16 IU/L (P < 0.05) and serum bilirubin from 2.8 ± 0.50 to 1.24 ± 0.30 mg/dl (P < 0.05). Treatment with Lip-TQ reduced the CYP-induced inflammation and hemorrhage in liver tissues. Moreover, treatment with free or Lip-TQ protected the activity of SOD and CAT in CYP-injected mice. Therefore, TQ can reduce the level of bilirubin in systemic circulation in disease conditions that lead to hyperbilirubinemia and liver toxicity and hence may be used as a supplement in the treatment of liver ailments. PMID:27265787

  15. Simultaneous quantification of ten constituents of Xanthoceras sorbifolia Bunge using UHPLC-MS methods and evaluation of their radical scavenging, DNA scission protective, and α-glucosidase inhibitory activities.

    PubMed

    Zhang, Yu; Ma, Jian-Nan; Ma, Chun-Li; Qi, Zhi; Ma, Chao-Mei

    2015-11-01

    The present study was designed to investigate the bioactive constituents of Xanthoceras sorbifolia in terms of amounts and their antioxidant, DNA scission protection, and α-glucosidase inhibitory activities. Simultaneous quantification of 10 X. sorbifolia constituents was carried out by a newly established ultra-high performance liquid chromatography-quadrupole mass spectrometry method (UHPLC-MS). The antioxidant activities were evaluated by measuring DPPH radical scavenging and DNA scission protective activities. The α-glucosidase inhibitory activities were investigated by using an assay with α-glucosidase from Bacillus Stearothermophilus and disaccharidases from mouse intestine. We found that the wood of X. sorbifolia was rich in phenolic compounds with the contents of catechin, epicatechin, myricetin, and dihydromyricetin being 0.12-0.19, 1.94-2.16, 0.77-0.91, and 6.76-7.89 mg·g(-1), respectively. The four constituents strongly scavenged DPPH radicals (with EC50 being 4.2, 3.8 and 5.7 μg·mL(-1), respectively) and remarkably protected peroxyl radical-induced DNA strand scission (92.10%, 94.66%, 75.44% and 89.95% of protection, respectively, at a concentration of 10 μmol·L(-1)). A dimeric flavan 3-ol, epigallocatechin-(4β→8, 2β→O-7)-epicatechin potently inhibited α-glucosidase with an IC50 value being as low as 1.2 μg·mL(-1). The established UHPLC-MS method could serve as a quality control tool for X. sorbifolia. In conclusion, the high contents of antioxidant and α-glucosidase inhibitory constituents in X. sorbifolia support its use as complementation of other therapeutic agents for metabolic disorders, such as diabetes and hypertension. PMID:26614463

  16. Neuritogenic Monoglyceride Derived from the Constituent of a Marine Fish for Activating the PI3K/ERK/CREB Signalling Pathways in PC12 Cells

    PubMed Central

    Yang, Wei; Luo, Yan; Tang, Ruiqi; Zhang, Hui; Ye, Ying; Xiang, Lan; Qi, Jianhua

    2013-01-01

    A neuritogenic monoglyceride, 1-O-(myristoyl) glycerol (MG), was isolated from the head of Ilisha elongate using a PC12 cell bioassay system, and its chemical structure was elucidated using spectroscopic methods. MG significantly induced 42% of the neurite outgrowth of PC12 cells at a concentration of 10 μM. To study the structure-activity relationships of MG, a series of monoglycerides was designed and synthesised. Bioassay results indicated that the alkyl chain length plays a key role in the neuritogenic activity of the monoglycerides. The groups that link the propane-1,2-diol and alkyl chain were also investigated. An ester linkage, rather than an amido one, was found to be optimal for neuritogenic activity. Therefore, 1-O-(stearoyl) glycerol (SG), which induces 57% of the neurite outgrowth of PC12 cells at 10 μM, was determined to be a lead compound for neuritogenic activity. We then investigated the mechanism of action of neurite outgrowth induced by SG on PC12 cells using protein specific inhibitors and Western blot analysis. The mitogen-activated kinase/ERK kinase (MEK) inhibitor U0126 and the phosphatidylinositol-3 kinase (PI3K) inhibitor LY294002 significantly decreased neurite outgrowth. At the same time, SG increased phosphorylation of CREB in protein level. Thus, SG-induced neuritogenic activity depends on the activation of the extracellular-regulated protein kinase (ERK), cAMP responsive element-binding protein (CREB) and PI3K signalling pathways in PC12 cells. PMID:24351811

  17. Cytotoxic activity of secondary metabolites derived from Artemisia annua L. towards cancer cells in comparison to its designated active constituent artemisinin.

    PubMed

    Efferth, Thomas; Herrmann, Florian; Tahrani, Ahmed; Wink, Michael

    2011-08-15

    Artemisia annua L. (sweet wormwood, qinhao) has traditionally been used in Chinese medicine. The isolation of artemisinin from Artemisia annua and its worldwide accepted application in malaria therapy is one of the showcase success stories of phytomedicine during the past decades. Artemisinin-type compounds are also active towards other protozoal or viral diseases as well as cancer cells in vitro and in vivo. Nowadays, Artemisia annua tea is used as a self-reliant treatment in developing countries. The unsupervised use of Artemisia annua tea has been criticized to foster the development of artemisinin resistance in malaria and cancer due to insufficient artemisinin amounts in the plant as compared to standardized tablets with isolated artemisinin or semisynthetic artemisinin derivatives. However, artemisinin is not the only bioactive compound in Artemisia annua. In the present investigation, we analyzed different Artemisia annua extracts. Dichloromethane extracts were more cytotoxic (range of IC₅₀: 1.8-14.4 μg/ml) than methanol extracts towards Trypanosoma b. brucei (TC221 cells). The range of IC₅₀ values for HeLa cancer cells was 54.1-275.5 μg/ml for dichloromethane extracts and 276.3-1540.8 μg/ml for methanol extracts. Cancer and trypanosomal cells did not reveal cross-resistance among other compounds of Artemisia annua, namely the artemisinin-related artemisitene and arteanuine B as well as the unrelated compounds, scopoletin and 1,8-cineole. This indicates that cells resistant to one compound retained sensitivity to another one. These results were also supported by microarray-based mRNA expression profiling showing that molecular determinants of sensitivity and resistance were different between artemisinin and the other phytochemicals investigated. PMID:21831619

  18. Baltimore Supersite: Highly time- and size-resolved concentrations of urban PM 2.5 and its constituents for resolution of sources and immune responses

    NASA Astrophysics Data System (ADS)

    Ondov, J. M.; Buckley, T. J.; Hopke, P. K.; Ogulei, D.; Parlange, M. B.; Rogge, W. F.; Squibb, K. S.; Johnston, M. V.; Wexler, A. S.

    Protection of public health from the effects of air particulate matter (PM) requires measurements and methods that assess the PM chemical constituents, physical properties, and their sources. Sampling was conducted at three sites in the Baltimore area: a source-oriented (industrial) area in south Baltimore (FMC site), and two receptor area sites (Clifton Park and Ponca Street). FMC measurements were made for the initial 1-month of the project; Clifton measurements lasted for about 2 months, while measurements at Ponca Street lasted for about 9.5 months. Pollutant samples were collected at intervals ranging from 5 min to 1 h using semi-continuous monitors for PM 2.5 mass, sulfate, nitrate, elemental and organic carbon, particle number size distributions (10-20,000 nm), CO, NO x, O 3, 11 metals, and mass spectra of individual particles, throughout the project. In addition to standard meteorological measurements, a 3D-sonic anemometer and a LIDAR system were operated during selected periods as were a rotating drum impactor with 3- to 6-h resolution and a filter/PUF sampler for 3-h measurements of organic compounds. Standard speciation and FRM mass measurements were also made. This report describes the types of measurements that were made at the various sites of the Baltimore Supersite program as well as presents the summary statistics for some of the PM measurements that have been made. The measurements of aerosol mass, major components, and size distribution data for the three sites are compared. Results show comparable PM concentrations at Ponca Street and Clifton Park. Increased variability was observed at Ponca Street.

  19. Effect of Alpha-Hederin, the active constituent of Nigella sativa, on miRNA-126, IL-13 mRNA levels and inflammation of lungs in ovalbumin-sensitized male rats

    PubMed Central

    Fallahi, Maryam; Keyhanmanesh, Rana; Khamaneh, Amir Mahdi; Ebrahimi Saadatlou, Mohammad Ali; Saadat, Saeideh; Ebrahimi, Hadi

    2016-01-01

    Objective: In previous studies the therapeutic effects of Nigella sativa have been demonstrated on asthmatic animals. In the present study, the preventive effect of single dose of alpha-hederin, its active constituent, has been evaluated on lung inflammation and some inflammatory mediators in lungs of ovalbumin sensitized rat in order to elicit its mechanism. Materials and Methods: Forty rats were randomly grouped in 4 groups; control (C), sensitized (S), sensitized pretreated groups with thymoquinone (3 mg/kg i.p., S+TQ) and alpha-hederin (0.02 mg/kg i.p., S+AH). Levels of IL-13 mRNA and miRNA-126 in lung tissue and its pathological changes in each group were assessed. Results: Elevated levels of miRNA-126, IL-13 mRNA and pathological changes were observed in the sensitized group compared to the control group (p<0.001 to p<0.05). All of these factors were significantly reduced in S+TQ and S+AH groups in comparison to S group (p<0.001 to p<0.05). Although alpha-hederin decreased the levels of miRNA-126, IL-13 mRNA and pathological changes in comparison with thymoquinone, the results were statistically not significant. Conclusion: The results suggested that alpha-hederin had preventive effect on sensitized rats like thymoquinone. It may intervene in miRNA-126 expression, which consequently could interfere with IL-13 secretion pathway leading to a reduction in inflammatory responses. PMID:27247924

  20. Atranorin and lecanoric acid antagonize TCDD-induced xenobiotic response element-driven activity, but not xenobiotic response element-independent activity.

    PubMed

    Nakashima, Ken-Ichi; Tanabe, Hiroki; Fujii-Kuriyama, Yoshiaki; Hayashi, Hidetoshi; Inoue, Makoto

    2016-07-01

    Lichens are symbiotic organisms that consist of fungi and photosynthetic symbionts (algae and/or cyanobacteria). Previous studies of their constituents suggested lichens produce many kinds of aromatic secondary metabolites, such as depsides, quinones, and dibenzofurans. In this study, we evaluated the aryl hydrocarbon receptor (AhR) antagonistic activity of 17 lichen substances and demonstrated that atranorin (1) and lecanoric acid (2), isolated from Parmotrema tinctorum Hale, showed an inhibitory effect on luciferase activity increased by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), using an XRE-driven pX4TK-Luc reporter gene assay. In addition, CYP1A1 mRNA and protein levels increased by TCDD were also suppressed by 1 and 2. Conversely, neither 1 nor 2 antagonized the suppressive effect of TCDD on interleukin (IL)-1β-induced acute-phase response (APR) gene expression. Thus, we concluded that 1 and 2 were selective AhR modulators that antagonize XRE-dependent activity, but not XRE-independent activity. However, 1 has different characteristics to 2 in that 1 alone showed a suppressive effect on IL-1β-induced APR gene expression in a similar fashion to TCDD. PMID:26979434

  1. 76 FR 19766 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-04-08

    ... From the Federal Register Online via the Government Publishing Office ENVIRONMENTAL PROTECTION AGENCY Agency Information Collection Activities OMB Responses AGENCY: Environmental Protection Agency... 1808.06; Environmental Impact Assessment of Nongovernmental Activities in Antarctica (Renewal); 40...

  2. Inflammasome activation of IL-1 family mediators in response to cutaneous photodamage†

    PubMed Central

    Nasti, Tahseen H; Timares, Laura

    2012-01-01

    Although keratinocytes are relatively resistant to ultraviolet radiation (UVR) induced damage, repeated UVR exposure result in accumulated DNA mutations that can lead to epidermal malignancies. Keratinocytes play a central role in elaborating innate responses that lead to inflammation and influence the generation of adaptive immune responses in skin. Apart from the minor cellular constituents of the epidermis, specifically Langerhans cells and melanocytes, keratinocytes are the major source of cytokines. UVR exposure stimulates keratinocytes to secrete abundant pro-inflammatory IL-1-family proteins, IL-1α, IL-1β, IL-18 and IL-33. Normal skin contains only low levels of inactive precursor forms of IL-1β and IL-18, which require caspase 1-mediated proteolysis for their maturation and secretion. However, caspase-1 activation is not constitutive, but dependents on the UV-induced formation of an active inflammasome complex. IL-1 family cytokines can induce a secondary cascade of mediators and cytokines from keratinocytes and other cells resulting in wide range of innate processes including infiltration of inflammatory leukocytes, induction of immunosuppression, DNA repair or apoptosis. Thus, the ability of keratinocytes to produce a wide repertoire of proinflammatory cytokines can influence the immune response locally as well as systematically, and alter the host response to photodamaged cells. We will highlight differential roles played by each IL-1 family molecule generated by UV-damaged keratinocytes, and reveal their complementary influences in modulating acute inflammatory and immunological events that follow cutaneous UV exposure. PMID:22631445

  3. Synthesis of Amaryllidaceae Constituents and Unnatural Derivatives.

    PubMed

    Ghavre, Mukund; Froese, Jordan; Pour, Milan; Hudlicky, Tomas

    2016-05-01

    This update covers the syntheses of Amaryllidaceae alkaloids since the publication of the last major review in 2008. A short summary of past syntheses and their step count is provided for the major constituents; pancratistatin, 7-deoxypancratistatin, narciclasine, lycoricidine, lycorine, and for other natural constituents, as well as for unnatural derivatives. Discussion of biological activities is provided for unnatural derivatives. Future prospects and further developments in this area are covered at the end of the review. The literature is covered to the end of August 2015. PMID:26969844

  4. Arctigenin but not arctiin acts as the major effective constituent of Arctium lappa L. fruit for attenuating colonic inflammatory response induced by dextran sulfate sodium in mice.

    PubMed

    Wu, Xin; Yang, Yan; Dou, Yannong; Ye, Jun; Bian, Difei; Wei, Zhifeng; Tong, Bei; Kong, Lingyi; Xia, Yufeng; Dai, Yue

    2014-12-01

    The crude powder of the fruit of Arctium lappa L. (ALF) has previously been reported to attenuate experimental colitis in mice. But, its main effective ingredient and underlying mechanisms remain to be identified. In this study, ALF was extracted with ethanol, and then successively fractionated into petroleum ether, ethyl acetate, n-butanol and water fraction. Experimental colitis was induced by dextran sulfate sodium (DSS) in mice. Among the four fractions of ALF, the ethyl acetate fraction showed the most significant inhibition of DSS-induced colitis in mice. The comparative studies of arctigenin and arctiin (the two main ingredients of ethyl acetate fraction) indicated that arctigenin rather than arctiin could reduce the loss of body weight, disease activity index and histological damage in the colon. Arctigenin markedly recovered the loss of intestinal epithelial cells (E-cadherin-positive cells) and decreased the infiltration of neutrophils (MPO-positive cells) and macrophages (CD68-positive cells). Arctigenin could down-regulate the expressions of TNF-α, IL-6, MIP-2, MCP-1, MAdCAM-1, ICAM-1 and VCAM-1 at both protein and mRNA levels in colonic tissues. Also, it markedly decreased the MDA level, but increased SOD activity and the GSH level. Of note, the efficacy of arctigenin was comparable or even superior to that of the positive control mesalazine. Moreover, it significantly suppressed the phosphorylation of MAPKs and the activation of NF-κB, including phosphorylation of IκBα and p65, p65 translocation and DNA binding activity. In conclusion, arctigenin but not arctiin is the main active ingredient of ALF for attenuating colitis via down-regulating the activation of MAPK and NF-κB pathways. PMID:25284342

  5. Ginger and Its Pungent Constituents Non-Competitively Inhibit Serotonin Currents on Visceral Afferent Neurons

    PubMed Central

    Jin, Zhenhua; Lee, Goeun; Kim, Sojin; Park, Cheung-Seog; Park, Yong Seek

    2014-01-01

    Nausea and emesis are a major side effect and obstacle for chemotherapy in cancer patients. Employ of antiemetic drugs help to suppress chemotherapy-induced emesis in some patients but not all patients. Ginger, an herbal medicine, has been traditionally used to treat various kinds of diseases including gastrointestinal symptoms. Ginger is effective in alleviating nausea and emesis, particularly, for cytotoxic chemotherapy drug-induced emesis. Ginger-mediated antiemetic effect has been attributed to its pungent constituents-mediated inhibition of serotonin (5-HT) receptor activity but its cellular mechanism of action is still unclear. Emetogenic chemotherapy drugs increase 5-HT concentration and activate visceral vagal afferent nerve activity. Thus, 5-HT mediated vagal afferent activation is essential to provoke emesis during chemotherapy. In this experiment, water extract of ginger and its three major pungent constituent's effect on 5-HT-evoked responses were tested on acutely dispersed visceral afferent neurons with patch-clamp methods. The ginger extract has similar effects to antiemetic drug ondansetron by blocking 5-HT-evoked responses. Pungent constituents of the ginger, [6]-shogaol, [6]-gingerol, and zingerone inhibited 5-HT responses in a dose dependent manner. The order of inhibitory potency for these compounds were [6]-shogaol>[6]-gingerol>zingerone. Unlike well-known competitive 5-HT3 receptor antagonist ondansetron, all tested ginger constituents acted as non-competitive antagonist. Our results imply that ginger and its pungent constituents exert antiemetic effects by blocking 5-HT-induced emetic signal transmission in vagal afferent neurons. PMID:24757377

  6. Ginger and its pungent constituents non-competitively inhibit serotonin currents on visceral afferent neurons.

    PubMed

    Jin, Zhenhua; Lee, Goeun; Kim, Sojin; Park, Cheung-Seog; Park, Yong Seek; Jin, Young-Ho

    2014-04-01

    Nausea and emesis are a major side effect and obstacle for chemotherapy in cancer patients. Employ of antiemetic drugs help to suppress chemotherapy-induced emesis in some patients but not all patients. Ginger, an herbal medicine, has been traditionally used to treat various kinds of diseases including gastrointestinal symptoms. Ginger is effective in alleviating nausea and emesis, particularly, for cytotoxic chemotherapy drug-induced emesis. Ginger-mediated antiemetic effect has been attributed to its pungent constituents-mediated inhibition of serotonin (5-HT) receptor activity but its cellular mechanism of action is still unclear. Emetogenic chemotherapy drugs increase 5-HT concentration and activate visceral vagal afferent nerve activity. Thus, 5-HT mediated vagal afferent activation is essential to provoke emesis during chemotherapy. In this experiment, water extract of ginger and its three major pungent constituent's effect on 5-HT-evoked responses were tested on acutely dispersed visceral afferent neurons with patch-clamp methods. The ginger extract has similar effects to antiemetic drug ondansetron by blocking 5-HT-evoked responses. Pungent constituents of the ginger, [6]-shogaol, [6]-gingerol, and zingerone inhibited 5-HT responses in a dose dependent manner. The order of inhibitory potency for these compounds were [6]-shogaol>[6]-gingerol>zingerone. Unlike well-known competitive 5-HT3 receptor antagonist ondansetron, all tested ginger constituents acted as non-competitive antagonist. Our results imply that ginger and its pungent constituents exert antiemetic effects by blocking 5-HT-induced emetic signal transmission in vagal afferent neurons. PMID:24757377

  7. HPLC-DAD-ESI-MS analysis of the constituents of aqueous preparations of verbena and lemon verbena and evaluation of the antioxidant activity.

    PubMed

    Bilia, A R; Giomi, M; Innocenti, M; Gallori, S; Vincieri, F F

    2008-02-13

    Verbena and lemon verbena aqueous preparations were investigated for their content of constituents, especially polyphenols by HPLC/DAD/ESI/MS analysis because they are used worldwide as herbal teas. The main class of compounds of these plants were phenylpropanoids (from 16 to 120 mg/g of dried extract), being verbascoside the most abundant in all the preparations up to 97% of the total phenylpropanoids. Also iridoids, hastatoside and verbenalin together with flavonoids, mono- and di-glucuronidic derivatives of luteolin and apigenin were found. These simple preparations, especially that obtained from infusion of lemon verbena, could be lyophilized to obtain a powder having interesting technological properties to be used as ingredients of cosmetics, food supplements and herbal medicinal products do to the many biological properties of verbascoside. In addition, the antioxidant property of the lemon verbena infusion was evaluated by the DPPH test using Trolox as the reference compound. PMID:18155378

  8. Human microsomal cyttrochrome P450-mediated reduction of oxysophocarpine, an active and highly toxic constituent derived from Sophora flavescens species, and its intestinal absorption and metabolism in rat.

    PubMed

    Wu, Lili; Zhong, Wanping; Liu, Junjin; Han, Weichao; Zhong, Shilong; Wei, Qiang; Liu, Shuwen; Tang, Lan

    2015-09-01

    Oxysophocarpine (OSC), an active and toxic quinolizidine alkaloid, is highly valued in Sophora flavescens Ait. and Subprostrate sophora Root. OSC is used to treat inflammation and hepatitis for thousands of years in China. This study aims to investigate the CYP450-mediated reduction responsible for metabolizing OSC and to evaluate the absorption and metabolism of OSC in rat in situ. Four metabolites were identified, with sophocarpine (SC) as the major metabolite. SC formation was rapid in human and rat liver microsomes (HLMs and RLMs, respectively). The reduction rates in the liver are two fold higher than in the intestine, both in humans and rats. In HLMs, inhibitors of CYP2C9, 3A4/5, 2D6, and 2B6 had strong inhibitory effects on SC formation. Meanwhile, inhibitors of CYP3A and CYP2D6 had significant inhibition on SC formation in RLMs. Human recombinant CYP3A4/5, 2B6, 2D6, and 2C9 contributed significantly to SC production. The permeability in rat intestine and the excretion rates of metabolites were highest in the duodenum (p<0.05), and the absorbed amount of OSC in duodenum and jejunum was concentration-dependent. The metabolism could be significantly decreased by CYP3A inhibitor ketoconazole. In conclusion, the liver was the main organ responsible for OSC metabolism. First-pass metabolism via CYP3A4/5, 2B6, 2D6, and 2C9 may be the main reason for the poor OSC bioavailability. PMID:26045316

  9. Macroscopic response in active nonlinear photonic crystals.

    PubMed

    Alagappan, Gandhi; John, Sajeev; Li, Er Ping

    2013-09-15

    We derive macroscopic equations of motion for the slowly varying electric field amplitude in three-dimensional active nonlinear optical nanostructures. We show that the microscopic Maxwell equations and polarization dynamics can be simplified to a macroscopic one-dimensional problem in the direction of group velocity. For a three-level active material, we derive the steady-state equations for normal mode frequency, threshold pumping, nonlinear Bloch mode amplitude, and lasing in photonic crystals. Our analytical results accurately recapture the results of exact numerical methods. PMID:24104802

  10. Rotor Flapping Response to Active Control

    NASA Technical Reports Server (NTRS)

    Nguyen, Khanh; Johnson, Wayne

    2004-01-01

    Rotor active control using higher harmonic blade pitch has been proposed as a means to reduce both rotor radiated noise and airframe vibration and to enhance rotor performance. The higher harmonic input, however, can affect rotor thrust and cyclic flapping - the basic trim characteristics of the rotor. Some of the trim changes can negate the active control benefits. For example, wind tunnel test results of a full scale BO-105 rotor with individual-blade control indicate some rotor performance improvements, accompanied with changes in rotor trim, using two-per-rev blade pitch input. The observed performance benefits could therefore be a simple manifestation of the trim change rather than an efficient redistribution of the rotor airloads. More recently, the flight test of the BO-105 helicopter equip,ped with individual-blade-control actuators also reported trim changes whenever the two-per-rev blade pitch for noise reduction was activated. The pilot had to adjust the trim control to maintain the aircraft under a constant flight path. These two cases highlight the, importance of trim considerations in the application of active control to rotorcraft.

  11. The unpredictability of prolonged activation of stress response pathways

    PubMed Central

    Lamech, Lilian T.

    2015-01-01

    In response to stress, cellular compartments activate signaling pathways that mediate transcriptional programs to promote survival and reestablish homeostasis. Manipulation of the magnitude and duration of the activation of stress responses has been proposed as a strategy to prevent or repair the damage associated with aging or degenerative diseases. However, as these pathways likely evolved to respond specifically to transient perturbations, the unpredictability of prolonged activation should be considered. PMID:26101215

  12. Comparison of two extraction methods for evaluation of volatile constituents patterns in commercial whiskeys Elucidation of the main odour-active compounds.

    PubMed

    Caldeira, M; Rodrigues, F; Perestrelo, R; Marques, J C; Câmara, J S

    2007-11-15

    An analytical procedure based on manual dynamic headspace solid-phase microextraction (HS-SPME) method and the conventional extraction method by liquid-liquid extraction (LLE), were compared for their effectiveness in the extraction and quantification of volatile compounds from commercial whiskey samples. Seven extraction solvents covering a wide range of polarities and two SPME fibres coatings, has been evaluated. The highest amounts extracted, were achieved using dichloromethane (CH2Cl2) by LLE method (LLE(CH2Cl2)) and using a CAR/PDMS fibre (SPME(CAR/PDMS)) in HS-SPME. Each method was used to determine the responses of 25 analytes from whiskeys and calibration standards, in order to provide sensitivity comparisons between the two methods. Calibration curves were established in a synthetic whiskey and linear correlation coefficient (r) were greater than 0.9929 for LLE(CH2Cl2) and 0.9935 for SPME(CAR/PDMS), for all target compounds. Recoveries greater than 80% were achieved. For most compounds, precision (expressed by relative standard deviation, R.S.D.) are very good, with R.S.D. values lower than 14.78% for HS-SPME method and than 19.42% for LLE method. The detection limits ranged from 0.13 to 19.03 microg L(-1) for SPME procedure and from 0.50 to 12.48 microg L(-1) for LLE. A tentative study to estimate the contribution of a specific compound to the aroma of a whiskey, on the basis of their odour activity values (OAV) was made. Ethyl octanoate followed by isoamyl acetate and isobutyl alcohol, were found the most potent odour-active compounds. PMID:18371616

  13. Dynamics of telomerase activity in response to acute psychological stress

    PubMed Central

    Epel, Elissa S.; Lin, Jue; Dhabhar, Firdaus S.; Wolkowitz, Owen M.; Puterman, E; Karan, Lori; Blackburn, Elizabeth H.

    2010-01-01

    Telomerase activity plays an essential role in cel0l survival, by lengthening telomeres and promoting cell growth and longevity. It is now possible to quantify the low levels of telomerase activity in human leukocytes. Low basal telomerase activity has been related to chronic stress in people and to chronic glucocorticoid exposure in vitro. Here we test whether leukocyte telomerase activity changes under acute psychological stress. We exposed 44 elderly women, including 22 high stress dementia caregivers and 22 matched low stress controls, to a brief laboratory psychological stressor, while examining changes in telomerase activity of peripheral blood mononuclear cells (PBMC). At baseline, caregivers had lower telomerase activity levels than controls, but during stress telomerase activity increased similarly in both groups. Across the entire sample, subsequent telomerase activity increased by 18% one hour after the end of the stressor (p<0.01). The increase in telomerase activity was independent of changes in numbers or percentages of monocytes, lymphocytes, and specific T cell types, although we cannot fully rule out some potential contribution from immune cell redistribution in the change in telomerase activity. Telomerase activity increases were associated with greater cortisol increases in response to the stressor. Lastly, psychological response to the tasks (greater threat perception) was also related to greater telomerase activity increases in controls. These findings uncover novel relationships of dynamic telomerase activity with exposure to an acute stressor, and with two classic aspects of the stress response -- perceived psychological stress and neuroendocrine (cortisol) responses to the stressor. PMID:20018236

  14. A new benzoylphloroglucinol derivative with an adamantyl skeleton and other constituents from Garcinia multiflora: effects on neutrophil pro-inflammatory responses.

    PubMed

    Ting, Chia-Wei; Hwang, Tsong-Long; Chen, Ih-Sheng; Yen, Ming-Hong; Chen, Jih-Jung

    2012-01-01

    A novel benzoylphloroglucinol derivative, garcimultiflorone D (1), with an unusual adamantyl-caged skeleton was isolated from the fruits of Garcinia multiflora, together with four known compounds. The structure of 1 was determined through extensive 1D/2D-NMR and mass-spectrometric analyses. Garcimultiflorone D (1) exhibited inhibitory activities with IC(50) values of 7.21±1.07 and 6.01±0.37 μg/ml against fMLP/CB-induced superoxide anion generation and elastase release, respectively. PMID:22253107

  15. A new ferulic acid ester, a new ellagic acid derivative, and other constituents from pachycentria formosana: effects on neutrophil pro-inflammatory responses.

    PubMed

    Cho, Jui-Ying; Lee, Tzong-Huei; Hwang, Tsong-Long; Yang, Sheng-Zehn; Chen, Ih-Sheng; Chou, Tsung-Hsien; Sung, Ping-Jyun; Chen, Jih-Jung

    2011-09-01

    A new ferulic acid ester derivative, tetracosane-1,24-diyl di[(Z)-ferulate] (1), and a new ellagic acid derivative, 3,4 : 3',4'-bis(O,O-methylene)ellagic acid (2), have been isolated from leaves and twigs of Pachycentria formosana, together with eight known compounds. Their structures were determined by in-depth spectroscopic and mass-spectrometric analyses. Among the isolated compounds, oleanolic acid (6), ursolic acid acetate (7), and 3-epibetulinic acid (9) exhibited potent inhibition (IC(50) values ≤ 21.8 μM) of O₂(-) generation by human neutrophils in response to N-formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B (fMLP/CB). In addition, oleanolic acid (6), 3-O-[(E)-feruloyl]ursolic acid (8), 3-epibetulinic acid (9), and lawsonic acid (10) also inhibited fMLP/CB-induced elastase release with IC(50) values ≤ 18.6 μM. PMID:21922659

  16. New Benzo[c]phenanthridine and Benzenoid Derivatives, and Other Constituents from Zanthoxylum ailanthoides: Effects on Neutrophil Pro-Inflammatory Responses

    PubMed Central

    Chung, Ching-Yi; Hwang, Tsong-Long; Kuo, Liang-Mou; Kuo, Wen-Lung; Cheng, Ming-Jen; Wu, Yi-Hsiu; Sung, Ping-Jyun; Chung, Mei-Ing; Chen, Jih-Jung

    2013-01-01

    A new benzo[c]phenanthridine, oxynorchelerythrine (1), and two new benzenoid derivatives, methyl 4-(2-hydroxy-4-methoxy-3-methyl-4-oxobutoxy)benzoate (2) and (E)-methyl 4-(4-((Z)-3-methoxy-3-oxoprop-1-enyl)phenoxy)-2-methylbut-2-enoate (3), have been isolated from the twigs of Zanthoxylum ailanthoides, together with 11 known compounds (4–14). The structures of these new compounds were determined through spectroscopic and MS analyses. Among the isolated compounds, decarine (4), (−)-syringaresinol (6), (+)-episesamin (8), glaberide I (9), (−)-dihydrocubebin (10), and xanthyletin (11) exhibited potent inhibition (IC50 values ≤ 4.79 μg/mL) of superoxide anion generation by human nutrophils in response to N-formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB). Compounds 4, 8, and 11 also inhibited fMLP/CB-induced elastase release with IC50 values ≤ 5.48 μg/mL. PMID:24232457

  17. Chemical constituents of Saniculiphyllum guangxiense.

    PubMed

    Geng, Chang-An; Huang, Xiao-Yan; Lei, Li-Gong; Zhang, Xue-Mei; Chen, Ji-Jun

    2012-08-01

    The first phytochemical investigation on Saniculiphyllum guangxiense resulted in the isolation of two new triterpenoids, 16β-hydroxybryodulcosigenin (3) and 3α-O-feruloylolean-12-en-27-oic acid (6), together with six known compounds, menisdaurin (1), purshianin (2), oleanolic acid (4), 3β-hydroxyolean-12-en-27-oic acid (5), β-sitosterol (7), and daucosterol (8), which were characterized by extensive spectroscopic analyses and in one case by X-ray diffraction. According to this primary investigation, S. guangxiense is rich in nitrile glucosides and triterpenoids, of which menisdaurin (1; 0.06%) and purshianin (2; 0.015%) are the main constituents. Compounds 1-6 were assayed for their anti-hepatitis B virus (HBV) activities against the secretion of HBsAg and HBeAg, as well as HBV DNA replication on Hep G 2.2.15 cell line in vitro. The most active compound, menisdaurin (1), inhibits HBV DNA replication with an IC(50) value of 0.32 mM (SI>11.97). PMID:22899611

  18. Ionospheric Response Due to Seismic Activity

    NASA Astrophysics Data System (ADS)

    Sharma, Dinesh Kumar

    2016-07-01

    Signatures of the seismic activity in the ionospheric F2 region have been studied by analyzing the measurement of electron and ion temperatures during the occurrence of earthquake. The ionospheric electron and ion temperatures data recorded by the RPA payload aboard the Indian SROSS-C2 satellite during the period from January 1995 to December 2000 were used for the altitude range 430-630 km over Indian region. The normal day's electron and ion temperatures have been compared to the temperatures recorded during the seismic activity. The details of seismic events were obtained from USGS earthquake data information website. It has been found that the average electron temperature is enhanced during the occurrence of earthquakes by 1.2 to 1.5 times and this enhancement was for ion temperature ranging from 1.1to 1.3 times over the normal day's average temperatures. The above careful quantitative analysis of ionospheric electron and ion temperatures data shows the consistent enhancement in the ionospheric electron and ion temperatures. It is expected that the seismogenic vertical electrical field propagates up to the ionospheric heights and induces Joule heating that may cause the enhancement in ionospheric temperatures.

  19. Anti-Tumor Action, Clinical Biochemistry Profile and Phytochemical Constituents of a Pharmacologically Active Fraction of S. crispus in NMU-Induced Rat Mammary Tumour Model

    PubMed Central

    Yaacob, Nik Soriani; Yankuzo, Hassan Muhammad; Devaraj, Sutha; Wong, Jimmy Ka Ming; Lai, Choon-Sheen

    2015-01-01

    Cancer patients seek alternative remedies such as traditional medicinal plants for safe and effective treatment and help overcome the side effects of conventional therapy. Current knowledge indicates that extracts of Strobilanthes crispus of the Acanthaceae family exhibit potent anticancer properties in vitro and are non-toxic in vivo. S. crispus was also reported to be protective against chemical hepatocarcinogenesis. We previously showed that a bioactive fraction of S. crispus leaves also synergized with tamoxifen to cause apoptosis of human breast cancer cell lines without damaging non-malignant epithelial cells. The present study aimed to evaluate the antitumor effect of S. crispus dichloromethane fraction (F3) using N-methyl-N-Nitrosourea (NMU)-induced rat mammary tumor model. Tumor regression was observed in 75% of the rats following 8-week oral administration of F3 with no secondary tumour formation and no signs of anemia or infection. However, no improvement in the liver and renal function profiles was observed. Major constituents of F3 were identified as lutein, 131-hydroxy-132-oxo-pheophytin a, campesterol, stigmasterol, β-sitosterol, pheophytin a and 132-hydroxy-pheophytin a. These compounds however, may not significantly contribute to the antitumor effect of F3. PMID:26000968

  20. P-glycoprotein activity and biological response

    SciTech Connect

    Vaalburg, W. . E-mail: w.vaalburg@pet.umcg.nl; Hendrikse, N.H.; Elsinga, P.H.; Bart, J.; Waarde, A. van

    2005-09-01

    P-glycoprotein (P-gp) is a transmembrane drug efflux pump encoded by the MDR-1 gene in humans. Most likely P-gp protects organs against endogenous and exogenous toxins by extruding toxic compounds such as chemotherapeutics and other drugs. Many drugs are substrates for P-gp. Since P-gp is also expressed in the blood-brain barrier, P-gp substrates reach lower concentrations in the brain than in P-gp-negative tissues. Failure of response to chemotherapy of malignancies can be due to intrinsic or acquired drug resistance. Many tumors are multidrug resistant (MDR); resistant to several structurally unrelated chemotherapeutic agents. Several mechanisms are involved in MDR of which P-gp is studied most extensively. P-gp extrudes drugs out of tumor cells resulting in decreased intracellular drug concentrations, leading to the MDR phenotype. Furthermore, the MDR-1 gene exhibits several single nucleotide polymorphisms, some of which result in different transport capabilities. P-gp functionality and the effect of P-gp modulation on the pharmacokinetics of novel and established drugs can be studied in vivo by positron emission tomography (PET) using carbon-11 and fluorine-18-labeled P-gp substrates and modulators. PET may demonstrate the consequences of genetic differences on tissue pharmacokinetics. Inhibitors such as calcium-channel blockers (verapamil), cyclosporin A, ONT-093, and XR9576 can modulate the P-gp functionality. With PET the effect of P-gp modulation on the bioavailability of drugs can be investigated in humans in vivo. PET also allows the measurement of the efficacy of newly developed P-gp modulators.

  1. 77 FR 22776 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-04-17

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  2. 78 FR 68053 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-11-13

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  3. 75 FR 54626 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-09-08

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    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-10-08

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  5. 77 FR 56200 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-09-12

    ... From the Federal Register Online via the Government Publishing Office ENVIRONMENTAL PROTECTION AGENCY Agency Information Collection Activities OMB Responses AGENCY: Environmental Protection Agency... of information unless it displays a currently valid OMB control number. The OMB control numbers...

  6. Pythium infection activates conserved plant defense responses in mosses

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The moss Physcomitrella patens (P. patens) is a useful model to study abiotic stress responses since it is highly tolerant to drought, salt and osmotic stress. However, little is known about the defense mechanisms activated in this moss after pathogen assault. Here the induction of defense responses...

  7. 78 FR 26772 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-05-08

    ... AGENCY Agency Information Collection Activities OMB Responses AGENCY: Environmental Protection Agency.... Seq.). An agency may not conduct or sponsor, and a person is not required to respond to, a collection... Information Collection Request (ICR) Number. SUPPLEMENTARY INFORMATION: OMB Responses to Agency...

  8. Identification of mosquito biting deterrent constituents from the Indian folk remedy plant Jatropha curcas.

    PubMed

    Cantrell, Charles L; Ali, Abbas; Duke, Stephen O; Khan, Ikhlas

    2011-07-01

    An investigation of the Indian folk remedy plant Jatropha curcas L., was performed to identify the constituents responsible for the mosquito biting deterrent activity of the oil. J. curcas seed oil is burned in oil lamps in India and parts of Africa to repel biting insects, primarily mosquitoes. The seed oil was thoroughly analyzed by 1H NMR, 13C NMR, high-performance liquid chromatography-refractive index, and gas chromatography-flame ionization detection to identify the constituents in the oil. Identified constituents, both free fatty acids and triglycerides, were evaluated for activity in Aedes aegypti (L.) (Diptera: Culicidae) biting deterrent assays. Furthermore, an oil condensation trap was used to demonstrate that free fatty acids or triglycerides are partially volatilized during the combustion process. These compounds were found to be responsible for the biting deterrency of the burned oil. Specifically, oleic, palmitic, linoleic, and stearic acids were all active at 25 nmol/cm2 above that of solvent control in Ae. aegypti biting deterrent assays. Oleic, palmitic, and linoleic acids were all more active than stearic acid in the same bioassay. Evaluation of the triglycerides containing each of these fatty acids revealed that tripalmitin, tristearin, trilinolein, and triolein all demonstrated significant activity above a solvent control at 10 microg/cm2, whereas tripalmitin was the most active. Due to literature reports suggesting larvicidal activity of the oil, J. curcas seed oil and its free fatty acid constituents also were evaluated against 1-d-old Ae. aegypti larvae up to 500 ppm. Oleic acid was the only fatty acid having larvicidal activity against 1-d-old Ae. aegypti larvae, with an LD50 of 47.9 ppm. PMID:21845943

  9. Magnetospheric impulse response for many levels of geomagnetic activity

    NASA Technical Reports Server (NTRS)

    Bargatze, L. F.; Baker, D. N.; Hones, E. W., Jr.; Mcpherron, R. L.

    1985-01-01

    The temporal relationship between the solar wind and magnetospheric activity has been studied using 34 intervals of high time resolution IMP 8 solar wind data and the corresponding AL auroral activity index. The median values of the AL index for each interval were utilized to rank the intervals according to geomagnetic activity level. The linear prediction filtering technique was then applied to model magnetospheric response as measured by the AL index to the solar wind input function VB(s). The linear prediction filtering routine produces a filter of time-lagged response coefficients which estimates the most general linear relationship between the chosen input and output parameters of the magnetospheric system. It is found that the filters are composed of two response pulses speaking at time lags of 20 and 60 min. The amplitude of the 60-min pulse is the larger for moderate activity levels, while the 20-min pulse is the larger for strong activity levels. A possible interpretation is that the 20-min pulse represents magnetospheric activity driven directly by solar wind coupling and that the 60-min pulse represents magnetospheric activity driven by the release of energy previously stored in the magnetotail. If this interpretation is correct, the linear filtering results suggest that both the driven and the unloading models of magnetospheric response are important facets of a more comprehensive response model.

  10. Beer constituents as potential cancer chemopreventive agents.

    PubMed

    Gerhäuser, Clarissa

    2005-09-01

    Beer is a complex alcoholic beverage made from barley (malt), hop, water and yeast. Phenolic constituents of beer are derived from malt (70-80%) and hop (20-30%). Structural classes include simple phenols, benzoic- and cinnamic acid derivatives, coumarins, catechins, di-, tri- and oligomeric proanthocyanidins, (prenylated) chalcones and flavonoids as well as alpha- and iso-alpha-acids derived from hop. Compounds belonging to different structural classes have distinct profiles of biological activity in in vitro test systems, and in combination might lead to enhanced effects. Scientific evidence has accumulated over the past 10 years pointing to the cancer preventive potential of selected hop-derived beer constituents, i.e., prenylflavonoids including xanthohumol and isoxanthohumol, and hop bitter acids. Chemopreventive activities observed with these compounds relevant to inhibition of carcinogenesis at the initiation, promotion and progression phases, as well as results from in vivo studies on metabolism, bioavailability and efficacy are summarised in this review. PMID:15953717

  11. Larvicidal constituents of Zingiber officinale (ginger) against Anisakis simplex.

    PubMed

    Lin, Rong-Jyh; Chen, Chung-Yi; Lee, June-Der; Lu, Chin-Mei; Chung, Li-Yu; Yen, Chuan-Min

    2010-11-01

    In this study, we investigated the anthelmintic activity of [10]-shogaol, [6]-shogaol, [10]-gingerol and [6]-gingerol, compounds isolated from the roots of Zingiber officinale L., Zingiberaceae (ginger), against Anisakis simplex. The above compounds kill or reduce spontaneous movement in A. simplex larvae. The maximum lethal efficacy of [10]-shogaol and [10]-gingerol was approximately 80% and 100%, respectively. We further examined the time course of compound-induced loss of mobility in A. simplex. The results showed that various concentrations of [10]-shogaol, [6]-shogaol, [10]-gingerol and [6]-gingerol have maximum effects on loss of spontaneous movement from 24 to 72 h. In addition, the time course of mortality and the percentage of loss of spontaneous movements were ascertained to determine the minimum effective doses of [10]-gingerol and [10]-shogaol. [10]-Gingerol exhibited a larger maximum larvicidal effect and greater loss of spontaneous movement than [10]-shogaol and albendazole. In addition, these constituents of Zingiber officinale showed effects against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and peroxyl radicals. These constituents of Zingiber officinale are responsible for its larvicidal activity against A. simplex. PMID:20533167

  12. Activated oxygen alters cerebral microvascular responses in newborn pigs

    SciTech Connect

    Leffler, C.W.; Busiia, D.W.; Armstead, W.M.; Mirro, R.; Thelin, O. )

    1990-02-26

    In piglets, cerebral ischemia/reperfusion blocks prostanoid dependent cerebral vasodilation to hypercapnia (CO{sub 2}) and hypotension but not prostanoid independent dilation to isoproterenol (Isu) or constriction to norepinephrine (NE). Ischemia/reperfusion increases activated-O{sub 2} production by piglet brains. Using cranial windows in piglets, the authors investigated the hypothesis that activated oxygen can block prostanoid dependent cerebral vasodilator responses to CO{sub 2} and hypotension without altering responses to Isu and NE. Exposure to an activated oxygen generating system of xanthine oxidase, hypoxanthine, and Fe that made about 3 times the activated-O{sub 2} on the brain surface as ischemia/reperfusion caused reversible pial arteriolar dilation. After exposure, pial arteriolar dilation was reduced to CO{sub 2} and hypotension but not to Isu. NE constrictor responses were also unaltered. H{sub 2}O{sub 2} or H{sub 2}O{sub 2} + Fe caused constriction followed by reversible dilation. After exposure, pial arteriolar dilation in response to CO{sub 2} and hypotension was not altered. However, addition of xanthine oxidase and hypoxanthine with H{sub 2}O{sub 2} and Fe totally eliminated pial arteriolar dilator responses to CO{sub 2} and hypotension but did not decrease dilation caused by Isu or constriction caused by NE. The authors conclude that activated oxygen could produce the altered prostanoid dependent pial arteriolar responses observed following ischemia in piglets.

  13. Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities

    PubMed Central

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Liakou, Eleni; Pratsinis, Harris; Kletsas, Dimitris; Chaita, Eliza; Aligiannis, Nektarios; Skaltsounis, Alexios-Leandros; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. PMID:26839809

  14. Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities.

    PubMed

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Liakou, Eleni; Pratsinis, Harris; Kletsas, Dimitris; Chaita, Eliza; Aligiannis, Nektarios; Skaltsounis, Alexios-Leandros; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. PMID:26839809

  15. Ovicidal and adulticidal activities of Origanum majorana essential oil constituents against insecticide-susceptible and pyrethroid/malathion-resistant Pediculus humanus capitis (Anoplura: Pediculidae).

    PubMed

    Yang, Young-Cheol; Lee, Si Hyeock; Clark, J Marshall; Ahn, Young-Joon

    2009-03-25

    The toxicity of essential oil constituents from marjoram, Origanum majorana, to eggs and adult females of the susceptible KR-HL and dual malathion- and permethrin-resistant BR-HL strains of human head louse, Pediculus humanus capitis, was examined using contact + fumigant mortality bioassay. Results were compared with those following treatment with two pyrethroid pediculicides, d-phenothrin or pyrethrum. As judged by the lethal time to 50% mortality (LT(50)) values at the exposure rate of 0.25 mg/cm(2), 1,8-cineole (14.1 min) was the most toxic compound, followed by linalool (15.4 min) to KR-HL females. These compounds were faster acting than either d-phenothrin (24.1 min) or pyrethrum (33.4 min). Based on the lethal concentration causing 50% mortality (LC(50)) values, (-)-camphor (0.022 mg/cm(2)) was the most toxic compound, followed by linalool (0.035 mg/cm(2)), (-)-terpinen-4-ol (0.040 mg/cm(2)), alpha-terpineol (0.045 mg/cm(2)), and 1,8-cineole (0.068 mg/cm(2)) against KR-HL females. These monoterpenoids were less toxic than either d-phenothrin (LC(50), 0.0015 mg/cm(2)) or pyrethrum (0.0013 mg/cm(2)). However, the toxicities of these monoterpenoids were almost identical against females from either of the two strains, even though the BR-HL females exhibited high levels of resistance to d-phenothrin [resistance ratio (RR), 667] and pyrethrum (RR, 754). After a 24 h exposure to linalool, BR-HL egg hatch was inhibited 100 and 84% at 0.25 or 0.125 mg/cm(2), respectively, while (-)-terpinen-4-ol caused 94 and 69% inhibition of egg hatch at 0.25 and 0.125 mg/cm(2). alpha-Terpineol caused 88 and 76% inhibition of egg hatch at 0.5 and 0.25 mg/cm(2), respectively. Thus, certain monoterpenoids from O. majorana essential oil, particularly linalool, (-)-terpinen-4-ol and alpha-terpineol, merit further study as potential pediculicides and ovicides for the control of insecticide-resistant P. h. capitis populations as fumigants with contact action. PMID:19292466

  16. Activation of antioxidant response element (ARE)-dependent genes by roasted coffee extracts.

    PubMed

    Yazheng, Liu; Kitts, David D

    2012-09-01

    Coffee beans contain numerous bioactive components that exhibit antioxidant capacity when assessed using both chemical, cell free, and biological, cell-based model systems. However, the mechanisms underlying the antioxidant effects of coffee in biological systems are not totally understood and in some cases vary considerably from results obtained with simpler in vitro chemical assays. In the present study, the physicochemical characteristics and antioxidant activity of roasted and non-roasted coffee extracts were investigated in both cell free (ORAC(FL)) and cell-based systems. A profile of antioxidant gene expression in cultured human colon adenocarcinoma Caco-2 cells treated with both roasted and non-roasted coffee extracts, respectively, was investigated using Real-Time polymerase chain reaction (PCR) array technology. Results demonstrated that the mechanisms of the antioxidant activity associated with coffee constituents assessed by the ORAC(FL) assay were different to those observed using an intracellular oxidation assay with Caco-2 cells. Moreover, roasted coffee (both light and dark roasted) extracts produced both increased- and decreased-expressions of numerous genes that are involved in the management of oxidative stress via the antioxidant defence system. The selective and specific positive induction of antioxidant response element (ARE)-dependent genes, including gastrointestinal glutathione peroxidase (GPX2), sulfiredoxin (SRXN1), thioredoxin reductase 1 (TXNRD1), peroxiredoxin 1 (PRDX1), peroxiredoxin 4 (PDRX4) and peroxiredoxin 6 (PDRX6) were identified with the activation of the endogenous antioxidant defence system in Caco-2 cells. PMID:22699814

  17. Participation in Peer Response as Activity: An Examination of Peer Response Stances from an Activity Theory Perspective

    ERIC Educational Resources Information Center

    Zhu, Wei; Mitchell, Deborah A.

    2012-01-01

    This article reports a case study that examined English as a Second Language students' peer response stances from an activity theory perspective. More specifically, the study was guided by the constructs of activity and motive/object in Leont'ev's theory. Multiple sources of data were collected from two native Spanish-speaking students enrolled in…

  18. Antioxidant activity and phytochemical constituent of two plants used to manage foot and mouth disease in the Far North Region of Cameroon

    PubMed Central

    Vougat, Ronald Romuald Bebey Ngom; Foyet, Harquin Simplice; Ziebe, Roland; Garabed, Rebecca B.

    2015-01-01

    Aim: Plants used in the Far North Region of Cameroon by livestock farmers to manage foot and mouth disease (FMD) in cattle and the phytochemical composition and antioxidant potentials of two of them (Boscia senegalensis [BS] and Tapinanthus dodoneifolius [TD]) were investigated in this study. Materials and Methods: Ethno veterinary data were collected from 325 livestock farmers using semi-structured interviews from September 2011 to April 2012. The 2,2-diphenyl-picrylhydrazyl radical scavenging activity and total phenolic content (TPC) were first performed with five different solvents to choose the best extract of each plant based on these two factors. To achieve our aim, the ferric iron reducing activity, hydroxyl radical scavenging activity (HRSA), free radical scavenging activity (FRSA), vitamin E and iron content were analyzed on extracts selected using current techniques. Results: The results showed that 12 plants of 8 different families are regularly used by farmers to manage FMD. It also demonstrated that acetone extract of TD and methanolic extract of BS are the extracts which showed the best total antioxidant activity (AA) and the best TPC. In general, TD show the best AA during the HRSA and FRSA analysis compared with BS. Similarly, TD content more phenolic compounds and tannins than BS. Both plants contain proteins, saponins, tannins, phenols, alkaloid, and polyphenols which are known to have many biological activities. Conclusion: These results support the AA of both plants and can justify their use by herders to treat FMD which is often followed by many secondary diseases. PMID:26401383

  19. Veratri Nigri Rhizoma et Radix (Veratrum nigrum L.) and Its Constituent Jervine Prevent Adipogenesis via Activation of the LKB1-AMPKα-ACC Axis In Vivo and In Vitro

    PubMed Central

    Park, Jinbong; Jeon, Yong-Deok; Kim, Hye-Lin; Kim, Dae-Seung; Han, Yo-Han; Jung, Yunu; Youn, Dong-Hyun; Kang, JongWook; Yoon, Daeyeon; Jeong, Mi-Young; Lee, Jong-Hyun; Hong, Seung-Heon; Lee, Junhee; Um, Jae-Young

    2016-01-01

    This study was performed in order to investigate the antiobese effects of the ethanolic extract of Veratri Nigri Rhizoma et Radix (VN), a herb with limited usage, due to its toxicology. An HPLC analysis identified jervine as a constituent of VN. By an Oil Red O assay and a Real-Time RT-PCR assay, VN showed higher antiadipogenic effects than jervine. In high-fat diet- (HFD-) induced obese C57BL/6J mice, VN administration suppressed body weight gain. The levels of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT-enhancer-binding protein alpha (C/EBPα), adipocyte fatty-acid-binding protein (aP2), adiponectin, resistin, and LIPIN1 were suppressed by VN, while SIRT1 was upregulated. Furthermore, VN activated phosphorylation of the liver kinase B1- (LKB1-) AMP-activated protein kinase alpha- (AMPKα-) acetyl CoA carboxylase (ACC) axis. Further investigation of cotreatment of VN with the AMPK agonist AICAR or AMPK inhibitor Compound C showed that VN can activate the phosphorylation of AMPKα in compensation to the inhibition of Compound C. In conclusion, VN shows antiobesity effects in HFD-induced obese C57BL/6J mice. In 3T3-L1 adipocytes, VN has antiadipogenic features, which is due to activating the LKB1-AMPKα-ACC axis. These results suggest that VN has a potential benefit in preventing obesity. PMID:27143989

  20. Water-quality assessment of the Delmarva Peninsula, Delaware, Maryland, and Virginia; effects of agricultural activities on, and distribution of, nitrate and other inorganic constituents in the surficial aquifer

    USGS Publications Warehouse

    Hamilton, P.A.; Denver, J.M.; Phillips, P.J.; Shedlock, R.J.

    1993-01-01

    Agricultural applications of inorganic fertilizers and manure have changed the natural chemical com- position of water in the surficial aquifer through- out the Delmarva Peninsula. Nitrate, derived from nitrification of ammonia in inorganic fertilizers and manure, is the dominant anion in agricultural areas. Concentrations of nitrate in 185 water samples collected in agricultural areas ranged from 0.4 to 48 mg/L as nitrogen, with a median concen- tration of 8.2 mg/L as nitrogen. Nitrate concen- trations exceeded the U.S. Environmental Protection Agency's maximum contaminant level for drinking water of 10 mg/L as nitrogen in about 33% of the 185 water samples. Groundwater affected by agricultural activities contains significantly higher concentrations of dissolved constituents than does natural groundwater. Concentrations of calcium and magnesium are higher because of liming of soils, and concentrations of potassium and chloride are higher because of applications of potash, a supple- ment to the nitrogen-based fertilizers. Alkalinity concentrations commonly are decreased because the bicarbonate ion is consumed in buffering reactions with acid that is produced during nitrification. Effects of agricultural activities on groundwater quality are not limited to the near-surface parts of the aquifer underlying farm fields. Elevated concentrations are common in aerobic water at or near the base of the aquifer, 80 to 100 ft below land surface. The median concentration of nitrate in water beneath agricultural areas collected from 24 wells deeper than 80 ft below land surface was 8.5 mg/L as nitrogen, and concentrations in 9 of these water samples exceeded the maximum contaminant level. Regional variations in concentrations of nitrate and other agriculture related constituents in the surficial aquifer in the Delmarva Peninsula depend on a number of factors that include geomorphology, geology, soils, land use, and groundwater-flow patterns. (USGS)

  1. Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.

    PubMed

    Wang, Jiayi; Pearce, A Norrie; Chan, Susanna T S; Taylor, Richard B; Page, Michael J; Valentin, Alexis; Bourguet-Kondracki, Marie-Lise; Dalton, James P; Wiles, Siouxsie; Copp, Brent R

    2016-03-25

    The first occurrence of an acetylenic 1-amino-2-alcohol, distaminolyne A (1), isolated from the New Zealand ascidian Pseudodistoma opacum, is reported. The isolation and structure elucidation of 1 and assignment of absolute configuration using the exciton coupled circular dichroism technique are described. In addition, a new N-9 hydroxy analogue (2) of the known P. opacum metabolite 7-bromohomotrypargine is also reported. Antimicrobial screening identified modest activity of 1 toward Escherichia coli, Staphylococcus aureus, and Mycobacterim tuberculosis, while 2 exhibited a moderate antimalarial activity (IC50 3.82 μM) toward a chloroquine-resistant strain (FcB1) of Plasmodium falciparum. PMID:26670413

  2. Phenolic constituents from Wissadula periplocifolia (L.) C. Presl. and anti-inflammatory activity of 7,4'-di-O-methylisoscutellarein.

    PubMed

    Teles, Yanna C F; Ribeiro-Filho, Jaime; Bozza, Patrícia T; Agra, Maria de Fátima; Siheri, Weam; Igoli, John O; Gray, Alexander I; Souza, Maria de Fátima V de

    2016-08-01

    This study reports the first phenolics from Wissadula genus (Malvaceae) and the anti-inflammatory activity of 7,4'-di-O-methylisoscutellarein. Using chromatographic methods, five phenolic compounds were isolated from aerial parts of Wissadula periplocifolia (L.) C. Presl. The compounds were identified as 4-hydroxybenzoic acid, 3-hydroxybenzoic acid, trans-cinnamic acid, tamgermanetin and 7,4'-di-O-methylisoscutellarein using spectroscopic methods. The flavone 7,4'-di-O-methylisoscutellarein showed anti-inflammatory activity by inhibiting neutrophils recruitment in a mice model of pleurisy and by decreasing significantly the production of cytokines IL-1β and TNF-α. PMID:27498833

  3. Baseline Brain Activity Predicts Response to Neuromodulatory Pain Treatment

    PubMed Central

    Jensen, Mark P.; Sherlin, Leslie H.; Fregni, Felipe; Gianas, Ann; Howe, Jon D.; Hakimian, Shahin

    2015-01-01

    Objectives The objective of this study was to examine the associations between baseline electroencephalogram (EEG)-assessed brain oscillations and subsequent response to four neuromodulatory treatments. Based on available research, we hypothesized that baseline theta oscillations would prospectively predict response to hypnotic analgesia. Analyses involving other oscillations and the other treatments (meditation, neurofeedback, and both active and sham transcranial direct current stimulation) were viewed as exploratory, given the lack of previous research examining brain oscillations as predictors of response to these other treatments. Design Randomized controlled study of single sessions of four neuromodulatory pain treatments and a control procedure. Methods Thirty individuals with spinal cord injury and chronic pain had their EEG recorded before each session of four active treatments (hypnosis, meditation, EEG biofeedback, transcranial direct current stimulation) and a control procedure (sham transcranial direct stimulation). Results As hypothesized, more presession theta power was associated with greater response to hypnotic analgesia. In exploratory analyses, we found that less baseline alpha power predicted pain reduction with meditation. Conclusions The findings support the idea that different patients respond to different pain treatments and that between-person treatment response differences are related to brain states as measured by EEG. The results have implications for the possibility of enhancing pain treatment response by either 1) better patient/treatment matching or 2) influencing brain activity before treatment is initiated in order to prepare patients to respond. Research is needed to replicate and confirm the findings in additional samples of individuals with chronic pain. PMID:25287554

  4. Patterning of sympathetic nerve activity in response to vestibular stimulation

    NASA Technical Reports Server (NTRS)

    Kerman, I. A.; McAllen, R. M.; Yates, B. J.

    2000-01-01

    Growing evidence suggests a role for the vestibular system in regulation of autonomic outflow during postural adjustments. In the present paper we review evidence for the patterning of sympathetic nerve activity elicited by vestibular stimulation. In response to electrical activation of vestibular afferents, firing of sympathetic nerves located throughout the body is altered. However, activity of the renal nerve is most sensitive to vestibular inputs. In contrast, high-intensity simultaneous activation of cutaneous and muscle inputs elicits equivalent changes in firing of the renal, superior mesenteric and lumbar colonic nerves. Responses of muscle vasoconstrictor (MVC) efferents to vestibular stimulation are either inhibitory (Type I) or are comprised of a combination of excitation and inhibition (Type II). Interestingly, single MVC units located in the hindlimb exhibited predominantly Type I responses while those located in the forelimb and face exhibited Type II responses. Furthermore, brachial and femoral arterial blood flows were dissociated in response to vestibular stimulation, such that brachial vascular resistance increased while femoral resistance decreased. These studies demonstrate that vestibulosympathetic reflexes are patterned according to both the anatomical location and innervation target of a particular sympathetic nerve, and can lead to distinct changes in local blood flow.

  5. Prefrontal Cortex Activity Related to Abstract Response Strategies

    PubMed Central

    Genovesio, Aldo; Brasted, Peter J.; Mitz, Andrew R.; Wise, Steven P.

    2005-01-01

    Overview In monkeys, foraging strategies depend not only on a context established by spatial or symbolic cues, but also on the relations among cues. Genovesio et al. recorded the activity of prefrontal cortex neurons while monkeys chose a strategy based on the relation between consecutive symbolic cues. For the same cues and actions, the monkeys also learned fixed responses to the same symbols. Many neurons had activity selective for a given strategy, others for whether the monkeys’ response choice depended on a symbol or the relation between symbols. These findings indicate that the primate prefrontal cortex contributes to implementing abstract strategies. PMID:16039571

  6. A Comprehensive Review on the Phytochemical Constituents and Pharmacological Activities of Pogostemon cablin Benth.: An Aromatic Medicinal Plant of Industrial Importance.

    PubMed

    Swamy, Mallappa Kumara; Sinniah, Uma Rani

    2015-01-01

    Pogostemon cablin Benth. (patchouli) is an important herb which possesses many therapeutic properties and is widely used in the fragrance industries. In traditional medicinal practices, it is used to treat colds, headaches, fever, nausea, vomiting, diarrhea, abdominal pain, insect and snake bites. In aromatherapy, patchouli oil is used to relieve depression, stress, calm nerves, control appetite and to improve sexual interest. Till now more than 140 compounds, including terpenoids, phytosterols, flavonoids, organic acids, lignins, alkaloids, glycosides, alcohols, aldehydes have been isolated and identified from patchouli. The main phytochemical compounds are patchouli alcohol, α-patchoulene, β-patchoulene, α-bulnesene, seychellene, norpatchoulenol, pogostone, eugenol and pogostol. Modern studies have revealed several biological activities such as antioxidant, analgesic, anti-inflammatory, antiplatelet, antithrombotic, aphrodisiac, antidepressant, antimutagenic, antiemetic, fibrinolytic and cytotoxic activities. However, some of the traditional uses need to be verified and may require standardizing and authenticating the bioactivity of purified compounds through scientific methods. The aim of the present review is to provide comprehensive knowledge on the phytochemistry and pharmacological activities of essential oil and different plant extracts of patchouli based on the available scientific literature. This information will provide a potential guide in exploring the use of main active compounds of patchouli in various medical fields. PMID:25985355

  7. Constituents of the sea cucumber Cucumaria okhotensis. Structures of okhotosides B1-B3 and cytotoxic activities of some glycosides from this species.

    PubMed

    Silchenko, Alexandra S; Avilov, Sergey A; Kalinin, Vladimir I; Kalinovsky, Anatoly I; Dmitrenok, Pavel S; Fedorov, Sergey N; Stepanov, Vadim G; Dong, Zigang; Stonik, Valentin A

    2008-03-01

    Three new triterpene oligoglycosides, okhotosides B 1 ( 1), B 2 ( 2), and B 3 ( 3), have been isolated from the sea cucumber Cucumaria okhotensis along with the known compounds frondoside A ( 4), frondoside A 1, cucumarioside A 2-5, and koreoside A. The structures of 1- 3 were elucidated on the basis of their spectroscopic data (2D NMR and MS). Compounds 1- 3 were moderately toxic against HeLa tumor cells. Frondoside A ( 4) showed more potent cytotoxicity against THP-1 and HeLa tumor cell lines (with IC 50 values of 4.5 and 2.1 microg/mL, respectively) and decreased both the AP-1-dependent trascriptional activities induced by UVB, EGF, or TPA in JB6-LucAP-1 cells and the EGF-induced NF-kappaB-dependent transcriptional activity in JB6-LucNF-kB cells at doses of about 1 microg/mL. At the same doses, it increased the p53-dependent transcriptional activity in nonactivated JB6-Lucp53 cells and inhibited the colony formation of JB6 P (+) Cl 41 cells activated with EGF (INCC 50 = 0.8 microg/mL). PMID:18288810

  8. Anti-adipogenic activity of the edible brown alga Ecklonia stolonifera and its constituent fucosterol in 3T3-L1 adipocytes.

    PubMed

    Jung, Hyun Ah; Jung, Hee Jin; Jeong, Hyun Young; Kwon, Hyun Ju; Kim, Min-Sun; Choi, Jae Sue

    2014-06-01

    Fucosterol is a sterol metabolite of brown algae and regulates genes involved with cholesterol homeostasis. As a part of our continuous search for anti-obesity agents from natural marine sources, the anti-adipogenic activities of Ecklonia stolonifera and its sterol, fucosterol, were evaluated for the inhibition of adipocyte differentiation and lipid formation. Oil Red O staining was used to evaluate triglyceride contents in 3T3-L1 pre-adipocytes primed by differentiation medium (DM) I and DM II. The methanolic extract of E. stolonifera showed strong anti-adipogenic activity, and was thus fractionated with several solvents. Among the tested fractions, the dichloromethane (CH2Cl2) fraction was found to be the most active fraction, with significant inhibition (40.5 %) of intracellular lipid accumulation at a non-toxic concentration, followed by the ethyl acetate fraction (30.2 %) at the same concentration, while the n-butanol and water fractions did not show inhibitory activity within the tested concentrations. The strong anti-adipogenic CH2Cl2-soluble fraction was further purified by a repeated chromatography to yield fucosterol. Fucosterol reduced lipid contents in a concentration-dependent manner without showing any cytotoxicity. Fucosterol treatment also yielded a decrease in the expression of the adipocyte marker proteins peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) in a concentration-dependent manner. Taken together, these results suggest that fucosterol inhibits expression of PPARγ and C/EBPα, resulting in a decrease of lipid accumulation in 3T3-L1 pre-adipocytes, indicating that the potential use of E. stolonifera and its bioactive fucosterol as an anti-obesity agent. PMID:24014306

  9. Comparative analysis of chemical constituents, antimicrobial and antioxidant activities of ethylacetate extracts of Polygonum cuspidatum and its endophytic actinomycete, Streptomyces sp. A0916.

    PubMed

    Wang, Lei; Qiu, Peng; Long, Xiu-Feng; Zhang, Shuai; Zeng, Zhi-Gang; Tian, Yong-Qiang

    2016-02-01

    The present study investigated the chemical composition of ethylacetate extracts from an endophytic actinomycete Streptomyces sp. A0916 and its host Polygonum cuspidatum. A comparative analysis of the antimicrobial and antioxidant properties of the extracts was also conducted. 32 compounds of P. cuspidatum and 23 compounds of Streptomyces sp. A0916 were isolated and identified by GC/MS. Antimicrobial activities of the extracts were evaluated using eight microbial strains (3 Gram-positive bacteria, 3 Gram-negative bacteria, and 2 fungi). The Streptomyces sp. A0916 extracts showed a wide range of antimicrobial activities and presented greater antimicrobial effectiveness than the P. cuspidatum extracts. The minimum inhibitory concentration (MIC) of Streptomyces sp. A0916 extracts against the ampicillin-resistant strain Enterococcus faecium SIIA843 was 32 μg·mL(-1). Furthermore, the extracts had greater antimicrobial effect against Gram-positive bacteria than Gram-negative bacteria. Finally, the antioxidant activity of the Streptomyces sp. A0916 extracts was equal to that of the P. cuspidatum extracts. In conclusion, our results suggest that the endophytic actinomycetes of the medicinal plants are an important source of bioactive substances. PMID:26968677

  10. Chemical constituents of marijuana: the complex mixture of natural cannabinoids.

    PubMed

    Elsohly, Mahmoud A; Slade, Desmond

    2005-12-22

    The cannabis plant (Cannabis sativa L.) and products thereof (such as marijuana, hashish and hash oil) have a long history of use both as a medicinal agent and intoxicant. Over the last few years there have been an active debate regarding the medicinal aspects of cannabis. Currently cannabis products are classified as Schedule I drugs under the Drug Enforcement Administration (DEA) Controlled Substances act, which means that the drug is only available for human use as an investigational drug. In addition to the social aspects of the use of the drug and its abuse potential, the issue of approving it as a medicine is further complicated by the complexity of the chemical make up of the plant. This manuscript discusses the chemical constituents of the plant with particular emphasis on the cannabinoids as the class of compounds responsible for the drug's psychological properties. PMID:16199061

  11. Identification of chemical constituents and larvicidal activity of essential oil from Murraya exotica L. (Rutaceae) against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus (Diptera: Culicidae).

    PubMed

    Krishnamoorthy, Shanmugam; Chandrasekaran, Manivachagam; Raj, Gnanaprakasam Adaikala; Jayaraman, Mahalingam; Venkatesalu, Venugopalan

    2015-05-01

    This study was conducted to evaluate the phytochemical composition and larvicidal effect of leaf essential oil from Murraya exotica against early fourth-instar larvae of Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus. Gas chromatography (GC) and gas chromatography mass spectrometry (GC-MS) analyses revealed that the essential oil contained 27 components. The major chemical components identified were β-humulene (40.62%), benzyl benzoate (23.96%), β-caryophyllene (7.05%) and α-terpinene (5.66%). The larval mortality was observed after 12 and 24 h of exposure period. The results revealed that essential oil showed varied levels of larvicidal activity against A. aegypti, A. stephensi and C. quinquefasciatus. After 12 h of exposure period, the larvicidal activities were LC₅₀ = 74.7 and LC₉₀ = 152.7 ppm (A. aegypti), LC₅₀ = 56.3 and LC₉₀ = 107.8 ppm (A. stephensi ), and LC₅₀ = 74.4 and LC₉₀ = 136.9 ppm (C. quinquefasciatus) and the larvicidal activities after 24 h of exposure period were LC₅₀ = 35.8 and LC₉₀ = 85.4 ppm (A. aegypti), LC₅₀ = 31.3 and LC₉₀ = 75.1 ppm (A. stephensi), and LC₅₀ = 43.2 and LC₉₀ = 103.2 ppm (C. quinquefasciatus). These results suggest that leaf essential oil from M. exotica is a promising and eco-friendly source of natural larvicidal agent against A. aegypti, A. stephensi and C. quinquefasciatus. PMID:25697880

  12. Educating for Political Activity: A Younger Generational Response

    ERIC Educational Resources Information Center

    Mac an Ghaill, Mairtin

    2010-01-01

    This paper is a response to Professor Chitty's "Educational Review" Guest Lecture article, "Educating for political activity". I address the three sections of his paper: a global and national-based politics of war, corporate manipulation and parliamentary scandals. This provides a basis to draw upon empirical material from a recent critical…

  13. Dynamics of lung macrophage activation in response to helminth infection

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Most of our understanding of the development and phenotype of alternatively activated macrophages (AAM) has been obtained from studies investigating the response of bone marrow- and peritoneal-derived cells to IL-4 or IL-13 stimulation. Comparatively little is known about the development of the AAM...

  14. Sensorimotor-Independent Prefrontal Activity During Response Inhibition

    PubMed Central

    Cai, Weidong; Cannistraci, Christopher J.; Gore, John C.; Leung, Hoi-Chung

    2015-01-01

    A network of brain regions involving the ventral inferior frontal gyrus/anterior insula (vIFG/AI), presupplementary motor area (pre-SMA) and basal ganglia has been implicated in stopping impulsive, unwanted responses. However, whether this network plays an equal role in response inhibition under different sensorimotor contexts has not been tested systematically. Here, we conducted an fMRI experiment using the stop signal task, a sensorimotor task requiring occasional withholding of the planned response upon the presentation of a stop signal. We manipulated both the sensory modality of the stop signal (visual versus auditory) and the motor response modality (hand versus eye). Results showed that the vIFG/AI and the preSMA along with the right middle frontal gyrus were commonly activated in response inhibition across the various sensorimotor conditions. Our findings provide direct evidence for a common role of these frontal areas, but not striatal areas in response inhibition independent of the sensorimotor contexts. Nevertheless, these three frontal regions exhibited different activation patterns during successful and unsuccessful stopping. Together with the existing evidence, we suggest that the vIFG/AI is involved in the early stages of stopping such as triggering the stop process while the preSMA may play a role in regulating other cortical and subcortical regions involved in stopping. PMID:23798325

  15. Sensorimotor-independent prefrontal activity during response inhibition.

    PubMed

    Cai, Weidong; Cannistraci, Christopher J; Gore, John C; Leung, Hoi-Chung

    2014-05-01

    A network of brain regions involving the ventral inferior frontal gyrus/anterior insula (vIFG/AI), presupplementary motor area (pre-SMA) and basal ganglia has been implicated in stopping impulsive, unwanted responses. However, whether this network plays an equal role in response inhibition under different sensorimotor contexts has not been tested systematically. Here, we conducted an fMRI experiment using the stop signal task, a sensorimotor task requiring occasional withholding of the planned response upon the presentation of a stop signal. We manipulated both the sensory modality of the stop signal (visual versus auditory) and the motor response modality (hand versus eye). Results showed that the vIFG/AI and the preSMA along with the right middle frontal gyrus were commonly activated in response inhibition across the various sensorimotor conditions. Our findings provide direct evidence for a common role of these frontal areas, but not striatal areas in response inhibition independent of the sensorimotor contexts. Nevertheless, these three frontal regions exhibited different activation patterns during successful and unsuccessful stopping. Together with the existing evidence, we suggest that the vIFG/AI is involved in the early stages of stopping such as triggering the stop process while the preSMA may play a role in regulating other cortical and subcortical regions involved in stopping. PMID:23798325

  16. Potential Antidepressant Constituents of Nigella sativa Seeds

    PubMed Central

    Elkhayat, Ehab S.; Alorainy, Mohammad S.; El-Ashmawy, Ibrahim M.; Fat’hi, Shawkat

    2016-01-01

    Background: Nigella sativa Linn. is well known seed in the Middle East, Asia, and the Far East as a natural remedy for many ailments and as a flavoring agent proclaimed medicinal usage dating back to the ancient Egyptians, Greeks, and Romans. An authentic saying of the Prophet Muhammad (Peace Be Upon Him) about black seed is also quoted in Al-Bukhari. Objective: This study was carried out to evaluate the antidepressant effect and isolate the potential antidepressant constituents of the polar extract of N. sativa seeds. Materials and Methods: The antidepressant effect was evaluated through the immobility duration in tail suspension and forced swim tests (FSTs). Albino mice were orally treated with N. sativa polar extract and its RP-18 column chromatography fractions (50 and 100 mg/kg,). Results: The polar extract and two of its sub-fractions were significantly able to decrease the immobility time of mice when subjected to both tail suspension and FSTs, the effects are comparable to standard drug (Sertraline, 5 mg/kg). However, these treatments did not affect the number of crossings and rearing in the open field test. Phytochemical investigation of the two active fractions led to the isolation of quercetin-3-O-α-L-rhamnopyranoside 1, quercetin-7-O-β-D-gluco- pyranoside 2, tauroside E 3, and sapindoside B as the potential antidepressant constituents. SUMMARY Phytochemical and biological evaluation the antidepressant constituents in Nigella sativa using the tail suspension and forced swim methods afforded the isolation and identification of quercetin-3-O-α-L rhamnopyranoside, quercetin-7-O-β-D gluco pyranoside, tauroside E, and sapindoside B as the potential antidepressant constituents in the polar extract of N. sativa. The isolated compounds were identified through extensive NMR analysis (1D, 2D, ESI MS). Abbreviations used: TST: Tail suspension test, FST: Forced swim test, OFT: An Open field test PMID:27041854

  17. Anti-Ulcerogenic Properties of Lycium chinense Mill Extracts against Ethanol-Induced Acute Gastric Lesion in Animal Models and Its Active Constituents.

    PubMed

    Olatunji, Opeyemi J; Chen, Hongxia; Zhou, Yifeng

    2015-01-01

    The objective of this study was to explore the gastroprotective properties of the aerial part of Lycium chinense Mill (LCA) against ethanol-induced gastric mucosa lesions in mice models. Administration of LCA at doses of 50, 100, 200 and 400 mg/kg body weight prior to ethanol consumption dose dependently inhibited gastric ulcers. The gastric mucosal injury was analyzed by gastric juice acidity, glutathione (GSH), superoxide dismutase (SOD), malondialdehyde (MDA), myeloperoxidase (MPO) activities. Furthermore, the levels of the inflammatory mediators, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β) in serum were also analyzed using ELISA. Pathological changes were also observed with the aid of hematoxylin-eosin (HE) staining. Our results indicated that LCA significantly reduced the levels of MPO, MDA and increased SOD and GSH activities. Furthermore, LCA also significantly inhibited the levels of TNF-α, IL-6, and IL-1β in the serum of ulcerated mice in a dose dependent manner. Immunohistological analysis indicated that LCA also significantly attenuated the overexpression of nuclear factor-κB in pretreated mice models. This findings suggests Lycium chinense Mill possesses gastroprotective properties against ethanol-induced gastric injury and could be a possible therapeutic intervention in the treatment and management of gastric ulcers. PMID:26694339

  18. Procyanidin B2 3,3″-di-O-gallate, a biologically active constituent of grape seed extract, induces apoptosis in human prostate cancer cells via targeting NF-κB, Stat3 and AP1 transcription factors

    PubMed Central

    Tyagi, Alpna; Raina, Komal; Shrestha, Suraj Prakash; Miller, Bettina; Thompson, John A.; Wempe, Michael F.; Agarwal, Rajesh; Agarwal, Chapla

    2014-01-01

    Recently, we identified procyanidin B2 3,3″-di-O-gallate (B2G2) as most active constituent of grape seed extract (GSE) for efficacy against prostate cancer (PCa). Isolating large quantities of B2G2 from total GSE is labor intensive and expensive, thereby limiting both efficacy and mechanistic studies with this novel anti-cancer agent. Accordingly, here we synthesized gram-scale quantities of B2G2, compared it with B2G2 isolated from GSE for possible equivalent biological activity, and conducted mechanistic studies. Both B2G2 preparations inhibited cell growth, decreased clonogenicity, and induced cell cycle arrest and apoptotic death, comparable to each other, in various human PCa cell lines. Mechanistic studies focusing on transcription factors involved in apoptotic and survival pathways revealed that B2G2 significantly inhibits NF-κB and AP1 transcriptional activity and nuclear translocation of Stat3 in PCa cell lines, irrespective of their functional androgen receptor status. B2G2 also decreased survivin expression which is regulated by NF-κB, AP1 and Stat3, and increased cleaved PARP level. In summary, we report B2G2 chemical synthesis at gram-quantity with equivalent biological efficacy against human PCa cell lines and same molecular targeting profiles at key transcription factors level. The synthetic B2G2 will stimulate more research on prostate and possibly other malignancies in preclinical models and clinical translation. PMID:24191894

  19. The grammar of visual narrative: Neural evidence for constituent structure in sequential image comprehension.

    PubMed

    Cohn, Neil; Jackendoff, Ray; Holcomb, Phillip J; Kuperberg, Gina R

    2014-11-01

    Constituent structure has long been established as a central feature of human language. Analogous to how syntax organizes words in sentences, a narrative grammar organizes sequential images into hierarchic constituents. Here we show that the brain draws upon this constituent structure to comprehend wordless visual narratives. We recorded neural responses as participants viewed sequences of visual images (comics strips) in which blank images either disrupted individual narrative constituents or fell at natural constituent boundaries. A disruption of either the first or the second narrative constituent produced a left-lateralized anterior negativity effect between 500 and 700ms. Disruption of the second constituent also elicited a posteriorly-distributed positivity (P600) effect. These neural responses are similar to those associated with structural violations in language and music. These findings provide evidence that comprehenders use a narrative structure to comprehend visual sequences and that the brain engages similar neurocognitive mechanisms to build structure across multiple domains. PMID:25241329

  20. The grammar of visual narrative: Neural evidence for constituent structure in sequential image comprehension

    PubMed Central

    Cohn, Neil; Jackendoff, Ray; Holcomb, Phillip J.; Kuperberg, Gina R.

    2014-01-01

    Constituent structure has long been established as a central feature of human language. Analogous to how syntax organizes words in sentences, a narrative grammar organizes sequential images into hierarchic constituents. Here we show that the brain draws upon this constituent structure to comprehend wordless visual narratives. We recorded neural responses as participants viewed sequences of visual images (comics strips) in which blank images either disrupted individual narrative constituents or fell at natural constituent boundaries. A disruption of either the first or the second narrative constituent produced a left-lateralized anterior negativity effect between 500-700ms. Disruption of the second constituent also elicited a posteriorly-distributed positivity (P600) effect. These neural responses are similar to those associated with structural violations in language and music. These findings provide evidence that comprehenders use a narrative structure to comprehend visual sequences and that the brain engages similar neurocognitive mechanisms to build structure across multiple domains. PMID:25241329

  1. Phase response curves in the characterization of epileptiform activity

    NASA Astrophysics Data System (ADS)

    Perez Velazquez, J. L.; Galán, R. F.; Dominguez, L. Garcia; Leshchenko, Y.; Lo, S.; Belkas, J.; Erra, R. Guevara

    2007-12-01

    Coordinated cellular activity is a major characteristic of nervous system function. Coupled oscillator theory offers unique avenues to address cellular coordination phenomena. In this study, we focus on the characterization of the dynamics of epileptiform activity, based on some seizures that manifest themselves with very periodic rhythmic activity, termed absence seizures. Our approach consists in obtaining experimentally the phase response curves (PRCs) in the neocortex and thalamus, and incorporating these PRCs into a model of coupled oscillators. Phase preferences of the stationary states and their stability are determined, and these results from the model are compared with the experimental recordings, and interpreted in physiological terms.

  2. Bacterial lifestyle shapes the regulation of stringent response activation

    PubMed Central

    Boutte, Cara C.; Crosson, Sean

    2014-01-01

    Bacteria inhabit enormously diverse niches and have a correspondingly large array of regulatory mechanisms to adapt to often inhospitable and variable environments. The stringent response allows bacteria to quickly reprogram transcription in response to changes in nutrient availability. Although the proteins controlling this response are conserved in almost all bacterial species, recent work has illuminated considerable diversity in the starvation cues and regulatory mechanisms that activate stringent signaling proteins in bacteria from different environments. In this review we describe the signals and genetic circuitries that control the stringent signaling systems of a copiotroph, a bacteriovore, an oligotroph and a mammalian pathogen – Escherichia coli, Myxococcus xanthus, Caulobacter crescentus and Mycobacterium tuberculosis, respectively – and discuss how control of the stringent response in these species is adapted to their particular lifestyles. PMID:23419217

  3. Anticipating Human Activities Using Object Affordances for Reactive Robotic Response.

    PubMed

    Koppula, Hema S; Saxena, Ashutosh

    2016-01-01

    An important aspect of human perception is anticipation, which we use extensively in our day-to-day activities when interacting with other humans as well as with our surroundings. Anticipating which activities will a human do next (and how) can enable an assistive robot to plan ahead for reactive responses. Furthermore, anticipation can even improve the detection accuracy of past activities. The challenge, however, is two-fold: We need to capture the rich context for modeling the activities and object affordances, and we need to anticipate the distribution over a large space of future human activities. In this work, we represent each possible future using an anticipatory temporal conditional random field (ATCRF) that models the rich spatial-temporal relations through object affordances. We then consider each ATCRF as a particle and represent the distribution over the potential futures using a set of particles. In extensive evaluation on CAD-120 human activity RGB-D dataset, we first show that anticipation improves the state-of-the-art detection results. We then show that for new subjects (not seen in the training set), we obtain an activity anticipation accuracy (defined as whether one of top three predictions actually happened) of 84.1, 74.4 and 62.2 percent for an anticipation time of 1, 3 and 10 seconds respectively. Finally, we also show a robot using our algorithm for performing a few reactive responses. PMID:26656575

  4. Carbohydrate polymers as constituents of exopolymer substances in seawater, their complexing properties towards copper ions, surface and catalytic activity determined by electrochemical methods.

    PubMed

    Plavšić, Marta; Strmečki, Slađana

    2016-01-01

    The goal of this study was to investigate to which extent polysaccharides (PS) contribute to the complexing capacity for copper ion (LT), to determine their property of surface activity and evaluate their capability to cause the catalytic hydrogen evolution wave (peak "H") due to their adsorption and the catalytic groups in their structure. Complexing capacities and apparent stability constants (Kapp) were measured electrochemically for model polysaccharides (PS): carrageenans (κ-, ι- and λ-), chondroitin sulfate, dextran, dextran sulfate, Na-alginate and humic material. Cu-complexing capacities were determined for Na-alginate (logKapp=8.32) and chondroitin sulphate (logKapp=8.14). PS adsorb on different surfaces due to their amphyphylic properties and on that way they could increase the interaction of copper ions with these surfaces by forming the surface complexes with Cu ions. PMID:26453850

  5. Linking biological activity with herbal constituents by systems biology-based approaches: effects of Panax ginseng in type 2 diabetic Goto-Kakizaki rats.

    PubMed

    Hu, Chunxiu; Wei, Heng; Kong, Hongwei; Bouwman, Jildau; Gonzalez-Covarrubias, Vanessa; van der Heijden, Rob; Reijmers, Theo H; Bao, Xu; Verheij, Elwin R; Hankemeier, Thomas; Xu, Guowang; van der Greef, Jan; Wang, Mei

    2011-11-01

    Although a number of animal experiments and clinical trials have investigated the effects of ginseng roots on diabetes, the relationship between their therapeutic effects on diabetes and the quality and the growth age of this herb have not yet been reported. This study systematically investigated the effects of 3- to 6-year-old ginseng roots on glycemic and plasma lipid control in a rat model of type 2 diabetes. Six groups of male Goto-Kakizaki (GK) rats received either metformin, 3- to 6-year-old ginseng roots, or no treatment. The treatments were administered twice daily for 9 weeks. A combined approach was used that involved applying liquid chromatography-mass spectrometry-based lipidomics, measuring biochemical parameters and profiling the components of ginseng roots of different ages. Compared to the untreated controls, treatment with 4- and 6-year-old ginseng roots significantly improved glucose disposal, and 5-year-old ginseng treatment significantly increased high density lipoprotein cholesterol. Treatment with 6-year-old ginseng significantly decreased total plasma triacylglyceride (TG) and very-low-density lipoprotein cholesterol and improved plasma glycated hemoglobin (HbA1c). In addition, treatment with 4- to 6-year-old ginseng influenced plasma lipidomics in diabetic GK rats by reducing TG lipid species. Metformin significantly reduced fasting blood glucose by 41% and reduced HbA1c by 11%, but showed no effects on the plasma lipid parameters. The present study demonstrates that ginseng roots show growth age-dependent therapeutic effects on hyperlipidemia and hyperglycemia in diabetic GK rats. These age-dependent effects may be linked with the variation in both the ratios and concentrations of specific bioactive ginsenosides in ginseng roots of different growth ages. This study introduced novel systems biology-based approaches for linking biological activities with potential active components in herbal mixtures. PMID:21901208

  6. Focused-ion-beam-fabricated Au nanorods coupled with Ag nanoparticles used as surface-enhanced Raman scattering-active substrate for analyzing trace melamine constituents in solution.

    PubMed

    Sivashanmugan, Kundan; Liao, Jiunn-Der; Liu, Bernard Haochih; Yao, Chih-Kai

    2013-10-24

    A well-ordered Au-nanorod array with a controlled tip ring diameter (Au_NRsd) was fabricated using the focused ion beam method. Au_NRsd was then coupled with Ag nanoparticles (Ag NPs) to bridge the gaps among Au nanorods. The effect of surface-enhanced Raman scattering (SERS) on Au_NRsd and Ag NPs/Au_NRsd was particularly verified using crystal violet (CV) as the molecular probe. Raman intensity obtained from a characteristic peak of CV on Au_NRsd was estimated by an enhancement factor of ≈10(7) in magnitude, which increased ≈10(12) in magnitude for that on Ag NPs/Au_NRsd. A highly SERS-active Ag NPs/Au_NRsd was furthermore applied for the detection of melamine (MEL) at very low concentrations. Raman-active peaks of MEL (10(-3) to 10(-12)M) in water or milk solution upon Au_NRsd or Ag NPs/Au_NRsd were well distinguished. The peaks at 680 and 702 cm(-1) for MEL molecules were found suitable to be used as the index for sensing low-concentration MEL in a varied solution, while that at 1051 cm(-1) was practical to interpret MEL molecules in water or milk solution bonded with Au (i.e., Au_NRsd) or Ag (i.e., Ag NPs/Au_NRsd) surface. At the interface of Ag NPs/Au_NRsd and MEL molecules in milk solution, a laser-induced electromagnetic field or hotspot effect was produced and competent to sense low-concentration MEL molecules interacting with Ag and Au surfaces. Accordingly, Ag NPs/Au_NRsd is very promising to be used as a fast and sensitive tool for screening MEL in complex matrices such as adulteration in e.g., food and pharmaceutical products. PMID:24120168

  7. [Bone marrow stromal damage mediated by immune response activity].

    PubMed

    Vojinović, J; Kamenov, B; Najman, S; Branković, Lj; Dimitrijević, H

    1994-01-01

    The aim of this work was to estimate influence of activated immune response on hematopoiesis in vitro, using the experimental model of BCG immunized BALB/c mice and in patients with chronic immunoactivation: long-lasting infections, autoimmunity or malignancy. We correlated changes in long term bone marrow cultures (Dexter) and NBT reduction with appearance of anemia in patients and experimental model of immunization by BCG. Increased spontaneous NBT reduction pointed out role of macrophage activation in bone marrow stroma damage. Long-term bone marrow cultures showed reduced number of hematopoietic cells, with predomination of fibroblasts and loss of fat cells. This results correlated with anemia and leucocytosis with stimulated myelopoiesis in peripheral blood. Activation of immune response, or acting of any agent that directly changes extracellular matrix and cellularity of bone marrow, may result in microenviroment bone marrow damage that modify hematopoiesis. PMID:18173180

  8. Humpback Dolphin (Genus Sousa) Behavioural Responses to Human Activities.

    PubMed

    Piwetz, Sarah; Lundquist, David; Würsig, Bernd

    2015-01-01

    Humpback dolphins (genus Sousa) use shallow, near-shore waters throughout their range. This coastal distribution makes them vulnerable to recreational and commercial disturbances, especially near heavily populated and industrialized areas. Most research focusing on Sousa and human activities has emphasized direct impacts and threats, involving injury and death, with relatively little focus on indirect effects on dolphins, such as changes in behaviour that may lead to deleterious effects. Understanding behaviour is important in resolving human-wildlife conflict and is an important component of conservation. This chapter gives an overview of animal behavioural responses to human activity with examples from diverse taxa; reviews the scientific literature on behavioural responses of humpback dolphins to human activity throughout their range, including marine vessel traffic, dolphin tourism, cetacean-fishery interactions, noise pollution, and habitat alteration; and highlights information and data gaps for future humpback dolphin research to better inform behaviour-based management decisions that contribute to conservation efforts. PMID:26555621

  9. CD83 Modulates B Cell Activation and Germinal Center Responses.

    PubMed

    Krzyzak, Lena; Seitz, Christine; Urbat, Anne; Hutzler, Stefan; Ostalecki, Christian; Gläsner, Joachim; Hiergeist, Andreas; Gessner, André; Winkler, Thomas H; Steinkasserer, Alexander; Nitschke, Lars

    2016-05-01

    CD83 is a maturation marker for dendritic cells. In the B cell lineage, CD83 is expressed especially on activated B cells and on light zone B cells during the germinal center (GC) reaction. The function of CD83 during GC responses is unclear. CD83(-/-) mice have a strong reduction of CD4(+) T cells, which makes it difficult to analyze a functional role of CD83 on B cells during GC responses. Therefore, in the present study we generated a B cell-specific CD83 conditional knockout (CD83 B-cKO) model. CD83 B-cKO B cells show defective upregulation of MHC class II and CD86 expression and impaired proliferation after different stimuli. Analyses of GC responses after immunization with various Ags revealed a characteristic shift in dark zone and light zone B cell numbers, with an increase of B cells in the dark zone of CD83 B-cKO mice. This effect was not accompanied by alterations in the level of IgG immune responses or by major differences in affinity maturation. However, an enhanced IgE response was observed in CD83 B-cKO mice. Additionally, we observed a strong competitive disadvantage of CD83-cKO B cells in GC responses in mixed bone marrow chimeras. Furthermore, infection of mice with Borrelia burgdorferi revealed a defect in bacterial clearance of CD83 B-cKO mice with a shift toward a Th2 response, indicated by a strong increase in IgE titers. Taken together, our results show that CD83 is important for B cell activation and modulates GC composition and IgE Ab responses in vivo. PMID:26983787

  10. Delphinid behavioral responses to incidental mid-frequency active sonar.

    PubMed

    Henderson, E Elizabeth; Smith, Michael H; Gassmann, Martin; Wiggins, Sean M; Douglas, Annie B; Hildebrand, John A

    2014-10-01

    Opportunistic observations of behavioral responses by delphinids to incidental mid-frequency active (MFA) sonar were recorded in the Southern California Bight from 2004 through 2008 using visual focal follows, static hydrophones, and autonomous recorders. Sound pressure levels were calculated between 2 and 8 kHz. Surface behavioral responses were observed in 26 groups from at least three species of 46 groups out of five species encountered during MFA sonar incidents. Responses included changes in behavioral state or direction of travel, changes in vocalization rates and call intensity, or a lack of vocalizations while MFA sonar occurred. However, 46% of focal groups not exposed to sonar also changed their behavior, and 43% of focal groups exposed to sonar did not change their behavior. Mean peak sound pressure levels when a behavioral response occurred were around 122 dB re: 1 μPa. Acoustic localizations of dolphin groups exhibiting a response gave insight into nighttime movement patterns and provided evidence that impacts of sonar may be mediated by behavioral state. The lack of response in some cases may indicate a tolerance of or habituation to MFA sonar by local populations; however, the responses that occur at lower received levels may point to some sensitization as well. PMID:25324099

  11. Characterizing wind turbine system response to lightning activity

    SciTech Connect

    McNiff, B.; LaWhite, N.; Muljadi, E.

    1998-07-01

    A lightning protection research program was instituted by National Renewable Energy Laboratory to minimize lightning damage to wind turbines and to further the understanding of effective damage mitigation techniques. To that end, a test program is under way to observe lightning activity, protection system response, and damage at a wind power plant in the Department of Energy (DOE) and Electric Power Research Institute (EPRI) Turbine Verification Program. The authors installed Lightning activated surveillance cameras along with a special storm tracking device to observe the activity in the wind plant area. They instrumented the turbines with lightning and ground current detection devices to log direct and indirect strike activity at each unit. They installed a surge monitor on the utility interface to track incoming activity from the transmission lines. Maintenance logs are used to verify damage and determine downtime and repair costs. Actual strikes to turbines were recorded on video and ancillary devices. The test setup and some results are discussed in this paper.

  12. Chemical constituents and antimicrobial activity of the leaf and rhizome oils of Alpinia pahangensis Ridl., an endemic wild ginger from peninsular Malaysia.

    PubMed

    Awang, Khalijah; Ibrahim, Halijah; Rosmy Syamsir, Devi; Mohtar, Mastura; Mat Ali, Rasadah; Azah Mohamad Ali, Nor

    2011-04-01

    The essential oils from the leaves and rhizomes of Alpinia pahangensis Ridl., collected from Pahang, Peninsular Malaysia, were obtained by hydrodistillation, and their chemical compositions were determined by GC and GC/MS analyses. The major components of the rhizome oil were γ-selinene (11.60%), β-pinene (10.87%), (E,E)-farnesyl acetate (8.65%), and α-terpineol (6.38%), while those of the leaf oil were β-pinene (39.61%), α-pinene (7.55%), and limonene (4.89%). The investigation of the antimicrobial activity of the essential oils using the broth microdilution technique revealed that the rhizome oil of A. pahangensis inhibited five Staphylococcus aureus strains with minimum inhibitory concentration (MIC) values between 0.08 and 0.31 μg/μl, and four selected fungi with MIC values between 1.25 and 2.50 μg/μl. PMID:21480512

  13. Sublethal toxicity of commercial formulations of deltamethrin and permethrin on selected biochemical constituents and enzyme activities in liver and muscle tissues of Anabas testudineus.

    PubMed

    Sapana Devi, Maisnam; Gupta, Abhik

    2014-10-01

    The freshwater fish Anabas testudineus was exposed for 21 days to two commercial formulations of synthetic pyrethroids deltamethrin and permethrin at sublethal concentrations of 0.007 and 0.0007 mg L(-1), and 0.093 and 0.0093 mg L(-1), that represented 10% and 1%, respectively, of the 96 h LC50 of these two pesticides for this fish. The glycogen, protein and lactic acid contents, along with succinate dehydrogenase (SDH), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) enzyme activities in liver and muscle tissues of control and pesticide-exposed fish were estimated. When compared with those of control fish, significant depletion of glycogen content was observed in liver, and that of protein in muscle tissue of fish treated with both the pesticides at their higher as well as lower concentrations. Lactic acid reduction was significant only in fish muscle treated with deltamethrin. SDH level was reduced significantly in both liver and muscle tissues except in fish exposed to 0.0093 mg L(-1) permethrin. AST level was reduced significantly in liver and muscle tissues and ALT in muscle tissue of deltamethrin treated fish only. It is concluded that deltamethrin, a type-II pyrethroid, is more toxic to fish than the type-I pyrethroid permethrin and is capable of rendering toxicity at a dose as low as 1% of its LC50 value. PMID:25307465

  14. Constituents of Holothuroidea, 18. Isolation and structure of biologically active disialo- and trisialo-gangliosides from the sea cucumber Cucumaria echinata.

    PubMed

    Kisa, Fumiaki; Yamada, Koji; Miyamoto, Tomofumi; Inagaki, Masanori; Higuchi, Ryuichi

    2006-09-01

    Three new disialo- and trisialo-gangliosides, CEG-6 (6), CEG-8 (8), and CEG-9 (9), were obtained, together with one known ganglioside, HLG-3 (7), from the lipid fraction of the chloroform/methanol extract of the sea cucumber Cucumaria echinata. The structures of the new gangliosides were determined on the basis of chemical and spectroscopic evidence to be 1-O-[alpha-L-fucopyranosyl-(1-->11)-(N-glycolyl-alpha-D-neuraminosyl)-(2-->4)-(N-acetyl-alpha-D-neuraminosyl)-(2-->6)-beta-D-glucopyranosyl]-ceramide (6) and 1-O-[(N-glycolyl-D-neuraminosyl)-(2-->11)-(N-glycolyl-D-neuraminosyl)-(2-->4)-(N-acetyl-D-neuraminosyl)-(2-->6)-D-glucopyranosyl]-ceramide (8, 9). The ceramide moieties of each compound were composed of an homogeneous sphingosine or phytosphingosine base and heterogeneous 2-hydroxy or nonhydroxylated fatty acid units. These gangliosides showed neuritogenic activity toward the rat pheochromocytoma cell line PC-12 in the presence of nerve growth factor. PMID:16946538

  15. The prolactin responses to active and passive heating in man.

    PubMed

    Low, David; Purvis, Alison; Reilly, Thomas; Cable, N Tim

    2005-11-01

    The aim of this study was to compare the prolactin and blood pressure responses at identical core temperatures during active and passive heat stresses, using prolactin as an indirect marker of central fatigue. Twelve male subjects cycled to exhaustion at 60% maximal oxygen uptake (VO2peak) in a room maintained at 33 degrees C (active). In a second trial they were passively heated (passive) in a water bath (41.56 +/- 1.65 degrees C) until core temperature was equal to the core temperature observed at exhaustion during the active trial. Blood samples were taken from an indwelling venous cannula for the determination of serum prolactin during active heating and at corresponding core temperatures during passive heating. Core temperature was not significantly different between the two methods of heating and averaged 38.81 +/- 0.53 and 38.82 +/- 0.70 degrees C (data expressed as means +/- s.d.) at exhaustion during active heating and at the end of passive heating, respectively (P > 0.05). Mean arterial blood pressure was significantly lower throughout passive heating (active, 73 +/- 9 mmHg; passive, 62 +/- 12 mmHg; P < 0.01). Despite the significantly reduced blood pressure responses during passive heating, during both forms of heating the prolactin response was the same (active, 14.9 +/- 12.6 ng ml(-1); passive, 13.3 +/- 9.6 ng ml(-1); n.s.). These results suggest that thermoregulatory, i.e. core temperature, and not cardiovascular afferents provide the key stimulus for the release of prolactin, an indirect marker of central fatigue, during exercise in the heat. PMID:16157657

  16. Changes in thyroid peroxidase activity in response to various chemicals.

    PubMed

    Song, Mee; Kim, Youn-Jung; Park, Yong-Keun; Ryu, Jae-Chun

    2012-08-01

    Thyroperoxidase (TPO) is a large heme-containing glycoprotein that catalyzes the transfer of iodine to thyroglobulin during thyroid hormone (TH) synthesis. Previously, we established an in vitro assay for TPO activity based on human recombinant TPO (hrTPO) stably transfected into human follicular thyroid carcinoma (FTC-238) cells. It is important to determine whether environmental chemicals can disrupt TPO activity because it is an important factor in the TH axis. In this study, we used our assay to examine the changes in TPO activity in response to various chemicals, including benzophenones (BPs), polycyclic aromatic hydrocarbons (PAHs), and persistent organic pollutants (POPs). Overall, BPs, PAHs, and POPs slightly altered TPO activity at low doses, as compared with the positive controls methimazole (MMI), genistein, and 2,2',4,4'-tetrahydroxy BP. Benzophenone, benzhydrol, 3-methylchloranthracene, pyrene, benzo(k)fluoranthene, benzo(e)pyrene, perfluorooctane sulfonate (PFOS), perfluorooctanoic acid (PFOA), and heptachlor decreased TPO activity, while 2,4-dihydroxy BP, 2,2'-dihydroxy-4-methoxy BP, and dibenzo(a,h)anthracene increased TPO activity. From these data, we can predict the disruption of TPO activity by various chemicals as a sensitive TH end point. TPO activity should be considered when enacting measures to regulate environmental exposure to thyroid-disrupting chemicals. PMID:22699773

  17. Response Activation in Overlapping Tasks and the Response-Selection Bottleneck

    ERIC Educational Resources Information Center

    Schubert, Torsten; Fischer, Rico; Stelzel, Christine

    2008-01-01

    The authors investigated the impact of response activation on dual-task performance by presenting a subliminal prime before the stimulus in Task 2 (S2) of a psychological refractory period (PRP) task. Congruence between prime and S2 modulated the reaction times in Task 2 at short stimulus onset asynchrony despite a PRP effect. This Task 2…

  18. [Chemical constituents of Desmodium sambuense].

    PubMed

    Li, Chuankuan; Zhang, Qianjun; Huang, Zhongbi; Chen, Qing; Yao, Rongjun

    2010-09-01

    The chemical constituents of Desmodium sambuense were studied. Chromatographic techniques were applied to isolate and purify the constituents, and the structures were identified on the basis of physico-chemical and spectroscopeic methods. Thirteen compounds were isolated from the 75% ethanol extract of Desmodium sambuens and elucidated as beta-amyrin(1), betulic acid(2), daucosterol(3), triacontanoic acid(4), lup-20(29)-en-3-one(5), tetracosanoic-2,3-dihydroxypropylester(6), stigmast-5-ene-3beta, 7alpha-ol (7),methyl phaeophorbidea(8), o-hydroxy benzoic acid(9),beta-sitosterol(10),d-catechin(11), luteolin (12), epigallocatechin (13). All of the compounds were isolated from this plant for the first time. PMID:21141491

  19. Reduced brain activation in violent adolescents during response inhibition

    PubMed Central

    Qiao, Yi; Mei, Yi; Du, XiaoXia; Xie, Bin; Shao, Yang

    2016-01-01

    Deficits in inhibitory control have been linked to aggression and violent behaviour. This study aimed to observe whether violent adolescents show different brain activation patterns during response inhibition and to ascertain the roles these brain regions play. A self-report method and modified overt aggression scale (MOAS) were used to evaluate violent behaviour. Functional magnetic resonance imaging was performed in 22 violent adolescents and 17 matched healthy subjects aged 12 to 18 years. While scanning, a go/no-go task was performed. Between-group comparisons revealed that activation in the bilateral middle and superior temporal gyrus, hippocampus, and right orbitofrontal area (BA11) regions were significantly reduced in the violent group compared with the control group. Meanwhile, the violent group had more widespread activation in the prefrontal cortex than that observed in the control group. Activation of the prefrontal cortex in the violent group was widespread but lacking in focus, failing to produce intensive activation in some functionally related regions during response inhibition. PMID:26888566

  20. Effects of three activities on annoyance responses to recorded flyovers

    NASA Technical Reports Server (NTRS)

    Gunn, W. J.; Shepherd, W. T.; Fletcher, J. L.

    1975-01-01

    Subjects participated in an experiment in which they were engaged in TV viewing, telephone listening, or reverie (no activity) for a 1/2-hour session. During the session, they were exposed to a series of recorded aircraft sounds at the rate of one flight every 2 minutes. Within each session, four levels of flyover noise, separated by 5dB increments, were presented several times in a Latin Square balanced sequence. The peak level of the noisiest flyover in any session was fixed at 95, 90, 85, 75, or 70 dBA. At the end of the test session, subjects recorded their responses to the aircraft sounds, using a bipolar scale which covered the range from 'very pleasant' to 'extremely annoying'. Responses to aircraft noises were found to be significantly affected by the particular activity in which the subjects were engaged. Furthermore, not all subjects found the aircraft sounds to be annoying.

  1. Activation and Regulation of DNA-Driven Immune Responses

    PubMed Central

    2015-01-01

    SUMMARY The innate immune system provides early defense against infections and also plays a key role in monitoring alterations of homeostasis in the body. DNA is highly immunostimulatory, and recent advances in this field have led to the identification of the innate immune sensors responsible for the recognition of DNA as well as the downstream pathways that are activated. Moreover, information on how cells regulate DNA-driven immune responses to avoid excessive inflammation is now emerging. Finally, several reports have demonstrated how defects in DNA sensing, signaling, and regulation are associated with susceptibility to infections or inflammatory diseases in humans and model organisms. In this review, the current literature on DNA-stimulated innate immune activation is discussed, and important new questions facing this field are proposed. PMID:25926682

  2. Hemodynamic responses to functional activation accessed by optical imaging

    NASA Astrophysics Data System (ADS)

    Ni, Songlin; Li, Pengcheng; Yang, Yuanyuan; Lv, Xiaohua; Luo, Qingming

    2006-01-01

    A multi-wavelength light-emitting diode (LED) and laser diode (LD) based optical imaging system was developed to visualize the changes in cerebral blood flow, oxygenation following functional activation simultaneously in rodent cortex. The 2-D blood flow image was accessed by laser speckle contrast imaging, and the spectroscopic imaging of intrinsic signal was used for the calculation of oxyhemoglobin (HbO), deoxyhemoglobin (Hb) and total hemoglobin (HbT) concentration. The combination of spectroscopic imaging and laser speckle contrast imaging provides the capability to simultaneously investigate the spatial and temporal blood flow and hemoglobin concentration changes with high resolution, which may lead to a better understanding of the coupling between neuronal activation and vascular responses. The optical imaging system been built is compact and convenient to investigators. And it is reliable to acquire raw data. In present study, the hemodynamic responses to cortical spreading depression (CSD) in parietal cortex of ~-chloralose/urethan anesthetized rats were demonstrated.

  3. Photodynamic therapy for cancer and activation of immune response

    NASA Astrophysics Data System (ADS)

    Mroz, Pawel; Huang, Ying-Ying; Hamblin, Michael R.

    2010-02-01

    Anti-tumor immunity is stimulated after PDT for cancer due to the acute inflammatory response, exposure and presentation of tumor-specific antigens, and induction of heat-shock proteins and other danger signals. Nevertheless effective, powerful tumor-specific immune response in both animal models and also in patients treated with PDT for cancer, is the exception rather than the rule. Research in our laboratory and also in others is geared towards identifying reasons for this sub-optimal immune response and discovering ways of maximizing it. Reasons why the immune response after PDT is less than optimal include the fact that tumor-antigens are considered to be self-like and poorly immunogenic, the tumor-mediated induction of CD4+CD25+foxP3+ regulatory T-cells (T-regs), that are able to inhibit both the priming and the effector phases of the cytotoxic CD8 T-cell anti-tumor response and the defects in dendritic cell maturation, activation and antigen-presentation that may also occur. Alternatively-activated macrophages (M2) have also been implicated. Strategies to overcome these immune escape mechanisms employed by different tumors include combination regimens using PDT and immunostimulating treatments such as products obtained from pathogenic microorganisms against which mammals have evolved recognition systems such as PAMPs and toll-like receptors (TLR). This paper will cover the use of CpG oligonucleotides (a TLR9 agonist found in bacterial DNA) to reverse dendritic cell dysfunction and methods to remove the immune suppressor effects of T-regs that are under active study.

  4. Chemical constituents from Abutilon indicum.

    PubMed

    Kuo, Ping-Chung; Yang, Mei-Lin; Wu, Pei-Lin; Shih, Hui-Nung; Thang, Tran Dinh; Dung, Nguyen Xuan; Wu, Tian-Shung

    2008-01-01

    The investigation on the chemical constituents of the whole plant of Abutilon indicum has resulted in the isolation of two new compounds, abutilin A (1) and (R)-N-(1'-methoxycarbonyl-2'-phenylethyl)-4-hydroxybenzamide (2), as well as 28 known compounds. The structures of the two new compounds were established on the basis of the spectroscopic analysis, and the known compounds were identified by comparison of their spectroscopic and physical data with those reported in the literature. PMID:18636384

  5. Autophagic activity dictates the cellular response to oncogenic RAS

    PubMed Central

    Wang, Yihua; Wang, Xiao Dan; Lapi, Eleonora; Sullivan, Alexandra; Jia, Wei; He, You-Wen; Ratnayaka, Indrika; Zhong, Shan; Goldin, Robert D.; Goemans, Christoph G.; Tolkovsky, Aviva M.; Lu, Xin

    2012-01-01

    RAS is frequently mutated in human cancers and has opposing effects on autophagy and tumorigenesis. Identifying determinants of the cellular responses to RAS is therefore vital in cancer research. Here, we show that autophagic activity dictates the cellular response to oncogenic RAS. N-terminal Apoptosis-stimulating of p53 protein 2 (ASPP2) mediates RAS-induced senescence and inhibits autophagy. Oncogenic RAS-expressing ASPP2(Δ3/Δ3) mouse embryonic fibroblasts that escape senescence express a high level of ATG5/ATG12. Consistent with the notion that autophagy levels control the cellular response to oncogenic RAS, overexpressing ATG5, but not autophagy-deficient ATG5 mutant K130R, bypasses RAS-induced senescence, whereas ATG5 or ATG3 deficiency predisposes to it. Mechanistically, ASPP2 inhibits RAS-induced autophagy by competing with ATG16 to bind ATG5/ATG12 and preventing ATG16/ATG5/ATG12 formation. Hence, ASPP2 modulates oncogenic RAS-induced autophagic activity to dictate the cellular response to RAS: to proliferate or senesce. PMID:22847423

  6. Dynamical theory of active cellular response to external stress.

    PubMed

    De, Rumi; Safran, Samuel A

    2008-09-01

    We present a comprehensive, theoretical treatment of the orientational response to external stress of active, contractile cells embedded in a gel-like elastic medium. The theory includes both the forces that arise from the deformation of the matrix as well as forces due to the internal regulation of the stress fibers and focal adhesions of the cell. We calculate the time-dependent response of both the magnitude and the direction of the elastic dipole that characterizes the active forces exerted by the cell, for various situations. For static or quasistatic external stress, cells orient parallel to the stress while for high frequency dynamic external stress, cells orient nearly perpendicular. Both numerical and analytical calculations of these effects are presented. In addition we predict the relaxation time for the cellular response for both slowly and rapidly varying external stresses; several characteristic scaling regimes for the relaxation time as a function of applied frequency are predicted. We also treat the case of cells for which the regulation of the stress fibers and focal adhesions is controlled by strain (instead of stress) and show that the predicted dependence of the cellular orientation on the Poisson ratio of the matrix can differentiate strain vs stress regulation of cellular response. PMID:18851081

  7. Dynamical theory of active cellular response to external stress

    NASA Astrophysics Data System (ADS)

    de, Rumi; Safran, Samuel A.

    2008-09-01

    We present a comprehensive, theoretical treatment of the orientational response to external stress of active, contractile cells embedded in a gel-like elastic medium. The theory includes both the forces that arise from the deformation of the matrix as well as forces due to the internal regulation of the stress fibers and focal adhesions of the cell. We calculate the time-dependent response of both the magnitude and the direction of the elastic dipole that characterizes the active forces exerted by the cell, for various situations. For static or quasistatic external stress, cells orient parallel to the stress while for high frequency dynamic external stress, cells orient nearly perpendicular. Both numerical and analytical calculations of these effects are presented. In addition we predict the relaxation time for the cellular response for both slowly and rapidly varying external stresses; several characteristic scaling regimes for the relaxation time as a function of applied frequency are predicted. We also treat the case of cells for which the regulation of the stress fibers and focal adhesions is controlled by strain (instead of stress) and show that the predicted dependence of the cellular orientation on the Poisson ratio of the matrix can differentiate strain vs stress regulation of cellular response.

  8. Activation of the DNA Damage Response by RNA Viruses.

    PubMed

    Ryan, Ellis L; Hollingworth, Robert; Grand, Roger J

    2016-01-01

    RNA viruses are a genetically diverse group of pathogens that are responsible for some of the most prevalent and lethal human diseases. Numerous viruses introduce DNA damage and genetic instability in host cells during their lifecycles and some species also manipulate components of the DNA damage response (DDR), a complex and sophisticated series of cellular pathways that have evolved to detect and repair DNA lesions. Activation and manipulation of the DDR by DNA viruses has been extensively studied. It is apparent, however, that many RNA viruses can also induce significant DNA damage, even in cases where viral replication takes place exclusively in the cytoplasm. DNA damage can contribute to the pathogenesis of RNA viruses through the triggering of apoptosis, stimulation of inflammatory immune responses and the introduction of deleterious mutations that can increase the risk of tumorigenesis. In addition, activation of DDR pathways can contribute positively to replication of viral RNA genomes. Elucidation of the interactions between RNA viruses and the DDR has provided important insights into modulation of host cell functions by these pathogens. This review summarises the current literature regarding activation and manipulation of the DDR by several medically important RNA viruses. PMID:26751489

  9. Activation of the DNA Damage Response by RNA Viruses

    PubMed Central

    Ryan, Ellis L.; Hollingworth, Robert; Grand, Roger J.

    2016-01-01

    RNA viruses are a genetically diverse group of pathogens that are responsible for some of the most prevalent and lethal human diseases. Numerous viruses introduce DNA damage and genetic instability in host cells during their lifecycles and some species also manipulate components of the DNA damage response (DDR), a complex and sophisticated series of cellular pathways that have evolved to detect and repair DNA lesions. Activation and manipulation of the DDR by DNA viruses has been extensively studied. It is apparent, however, that many RNA viruses can also induce significant DNA damage, even in cases where viral replication takes place exclusively in the cytoplasm. DNA damage can contribute to the pathogenesis of RNA viruses through the triggering of apoptosis, stimulation of inflammatory immune responses and the introduction of deleterious mutations that can increase the risk of tumorigenesis. In addition, activation of DDR pathways can contribute positively to replication of viral RNA genomes. Elucidation of the interactions between RNA viruses and the DDR has provided important insights into modulation of host cell functions by these pathogens. This review summarises the current literature regarding activation and manipulation of the DDR by several medically important RNA viruses. PMID:26751489

  10. Placebo-Activated Neural Systems are Linked to Antidepressant Responses

    PubMed Central

    Peciña, Marta; Bohnert, Amy S. B.; Sikora, Magdalena; Avery, Erich T.; Langenecker, Scott A.; Mickey, Brian J.; Zubieta, Jon-Kar

    2016-01-01

    Importance High placebo responses have been observed across a wide range of pathologies, severely impacting drug development. Objective Here we examined neurochemical mechanisms underlying the formation of placebo effects in patients with Major Depressive Disorder (MDD). Participants Thirty-five medication-free MDD patients. Design and Intervention We performed a single-blinded two-week cross-over randomized controlled trial of two identical oral placebos (described as having either “active” or “inactive” fast-acting antidepressant-like effects) followed by a 10-week open-label treatment with a selective serotonin reuptake inhibitor (SSRI) or in some cases, another agent as clinically indicated. The volunteers were studied with PET and the μ-opioid receptor (MOR)-selective radiotracer [11C]carfentanil after each 1-week “inactive” and “active” oral placebo treatment. In addition, 1 mL of isotonic saline was administered intravenously (i.v.) within sight of the volunteer during PET scanning every 4 min over 20 min only after the 1-week active placebo treatment, with instructions that the compound may be associated with the activation of brain systems involved in mood improvement. This challenge stimulus was utilized to test the individual capacity to acutely activate endogenous opioid neurotransmision under expectations of antidepressant effect. Setting A University Health System. Main Outcomes and Measures Changes in depressive symptoms in response to “active” placebo and antidepressant. Baseline and activation measures of MOR binding. Results Higher baseline MOR binding in the nucleus accumbens (NAc) was associated with better response to antidepressant treatment (r=0.48; p=0.02). Reductions in depressive symptoms after 1-week of “active” placebo treatment, compared to the “inactive”, were associated with increased placebo-induced μ-opioid neurotransmission in a network of regions implicated in emotion, stress regulation, and the

  11. Cinobufagin Modulates Human Innate Immune Responses and Triggers Antibacterial Activity

    PubMed Central

    Xie, Shanshan; Spelmink, Laura; Codemo, Mario; Subramanian, Karthik; Pütsep, Katrin

    2016-01-01

    The traditional Chinese medicine Chan-Su is widely used for treatment of cancer and cardiovascular diseases, but also as a remedy for infections such as furunculosis, tonsillitis and acute pharyngitis. The clinical use of Chan-Su suggests that it has anti-infective effects, however, the mechanism of action is incompletely understood. In particular, the effect on the human immune system is poorly defined. Here, we describe previously unrecognized immunomodulatory activities of cinobufagin (CBG), a major bioactive component of Chan-Su. Using human monocyte-derived dendritic cells (DCs), we show that LPS-induced maturation and production of a number of cytokines was potently inhibited by CBG, which also had a pro-apoptotic effect, associated with activation of caspase-3. Interestingly, CBG triggered caspase-1 activation and significantly enhanced IL-1β production in LPS-stimulated cells. Finally, we demonstrate that CBG upregulates gene expression of the antimicrobial peptides (AMPs) hBD-2 and hBD-3 in DCs, and induces secretion of HNP1-3 and hCAP-18/LL-37 from neutrophils, potentiating neutrophil antibacterial activity. Taken together, our data indicate that CBG modulates the inflammatory phenotype of DCs in response to LPS, and triggers an antibacterial innate immune response, thus proposing possible mechanisms for the clinical effects of Chan-Su in anti-infective therapy. PMID:27529866

  12. Cinobufagin Modulates Human Innate Immune Responses and Triggers Antibacterial Activity.

    PubMed

    Xie, Shanshan; Spelmink, Laura; Codemo, Mario; Subramanian, Karthik; Pütsep, Katrin; Henriques-Normark, Birgitta; Olliver, Marie

    2016-01-01

    The traditional Chinese medicine Chan-Su is widely used for treatment of cancer and cardiovascular diseases, but also as a remedy for infections such as furunculosis, tonsillitis and acute pharyngitis. The clinical use of Chan-Su suggests that it has anti-infective effects, however, the mechanism of action is incompletely understood. In particular, the effect on the human immune system is poorly defined. Here, we describe previously unrecognized immunomodulatory activities of cinobufagin (CBG), a major bioactive component of Chan-Su. Using human monocyte-derived dendritic cells (DCs), we show that LPS-induced maturation and production of a number of cytokines was potently inhibited by CBG, which also had a pro-apoptotic effect, associated with activation of caspase-3. Interestingly, CBG triggered caspase-1 activation and significantly enhanced IL-1β production in LPS-stimulated cells. Finally, we demonstrate that CBG upregulates gene expression of the antimicrobial peptides (AMPs) hBD-2 and hBD-3 in DCs, and induces secretion of HNP1-3 and hCAP-18/LL-37 from neutrophils, potentiating neutrophil antibacterial activity. Taken together, our data indicate that CBG modulates the inflammatory phenotype of DCs in response to LPS, and triggers an antibacterial innate immune response, thus proposing possible mechanisms for the clinical effects of Chan-Su in anti-infective therapy. PMID:27529866

  13. Platelet activation and apoptosis modulate monocyte inflammatory responses in dengue

    PubMed Central

    Hottz, Eugenio D.; Medeiros-de-Moraes, Isabel M.; Vieira-de-Abreu, Adriana; de Assis, Edson F.; Vals-de-Souza, Rogério; Castro-Faria-Neto, Hugo C.; Weyrich, Andrew S.; Zimmerman, Guy A.; Bozza, Fernando A.; Bozza, Patrícia T.

    2014-01-01

    Background Dengue is the most prevalent human arbovirus disease in the world. Dengue infection has a large spectrum of clinical manifestations from self-limited febrile illness to severe syndromes accompanied by bleeding and shock. Thrombocytopenia and vascular leak with altered cytokine profiles in plasma are features of severe dengue. Although monocytes have been recognized as important sources of cytokines in dengue, the contributions of platelet-monocyte interactions to inflammatory responses in dengue have not been addressed. Patients/Methods Patients with dengue were investigated for platelet-monocyte aggregate formation and markers of monocyte activation. Platelet-induced cytokine responses by monocytes and underlying mechanisms were also investigated in vitro. Results We observed increased levels of platelet-monocyte aggregates in blood samples from patients with dengue, especially patients with thrombocytopenia and increased vascular permeability. Moreover, the exposure of monocytes from healthy volunteers to platelets from patients with dengue induced the secretion of the cytokines IL-1β, IL-8, IL-10 and MCP-1, while the exposure to platelets from healthy volunteers only induced the secretion of MCP-1. In addition to the well-established modulation of monocyte cytokine responses by activated platelets through P-selectin binding, we found that interaction of monocytes with apoptotic platelets mediate IL-10 secretion through phosphatidylserine recognition in platelet-monocyte aggregates. Moreover, IL-10 secretion required platelet-monocyte contact but not phagocytosis. Conclusions Together, our results demonstrate that activated and apoptotic platelets aggregate with monocytes during dengue infection and signal specific cytokine responses that may contribute to the pathogenesis of dengue. PMID:25015827

  14. Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.

    PubMed

    Wiel, C; Augert, A; Vincent, D F; Gitenay, D; Vindrieux, D; Le Calvé, B; Arfi, V; Lallet-Daher, H; Reynaud, C; Treilleux, I; Bartholin, L; Lelievre, E; Bernard, D

    2013-01-01

    Cellular senescence, a stable proliferation arrest, is induced in response to various stresses. Oncogenic stress-induced senescence (OIS) results in blocked proliferation and constitutes a fail-safe program counteracting tumorigenesis. The events that enable a tumor in a benign senescent state to escape from OIS and become malignant are largely unknown. We show that lysyl oxidase activity contributes to the decision to maintain senescence. Indeed, in human epithelial cell the constitutive expression of the LOX or LOXL2 protein favored OIS escape, whereas inhibition of lysyl oxidase activity was found to stabilize OIS. The relevance of these in vitro observations is supported by in vivo findings: in a transgenic mouse model of aggressive pancreatic ductal adenocarcinoma (PDAC), increasing lysyl oxidase activity accelerates senescence escape, whereas inhibition of lysyl oxidase activity was found to stabilize senescence, delay tumorigenesis, and increase survival. Mechanistically, we show that lysyl oxidase activity favors the escape of senescence by regulating the focal-adhesion kinase. Altogether, our results demonstrate that lysyl oxidase activity participates in primary tumor growth by directly impacting the senescence stability. PMID:24113189

  15. The unfolded protein response selectively targets active smoothened mutants.

    PubMed

    Marada, Suresh; Stewart, Daniel P; Bodeen, William J; Han, Young-Goo; Ogden, Stacey K

    2013-06-01

    The Hedgehog signaling pathway, an essential regulator of developmental patterning, has been implicated in playing causative and survival roles in a range of human cancers. The signal-transducing component of the pathway, Smoothened, has revealed itself to be an efficacious therapeutic target in combating oncogenic signaling. However, therapeutic challenges remain in cases where tumors acquire resistance to Smoothened antagonists, and also in cases where signaling is driven by active Smoothened mutants that exhibit reduced sensitivity to these compounds. We previously demonstrated that active Smoothened mutants are subjected to prolonged endoplasmic reticulum (ER) retention, likely due to their mutations triggering conformation shifts that are detected by ER quality control. We attempted to exploit this biology and demonstrate that deregulated Hedgehog signaling driven by active Smoothened mutants is specifically attenuated by ER stressors that induce the unfolded protein response (UPR). Upon UPR induction, active Smoothened mutants are targeted by ER-associated degradation, resulting in attenuation of inappropriate pathway activity. Accordingly, we found that the UPR agonist thapsigargin attenuated mutant Smoothened-induced phenotypes in vivo in Drosophila melanogaster. Wild-type Smoothened and physiological Hedgehog patterning were not affected, suggesting that UPR modulation may provide a novel therapeutic window to be evaluated for targeting active Smoothened mutants in disease. PMID:23572559

  16. Library Development Structures in CIC Institutions: The Search for Constituents.

    ERIC Educational Resources Information Center

    Gearhart, G. David; St. Clair, Gloriana

    1994-01-01

    This study determined how the 12 academic libraries in the Council for Interinstitutional Cooperation (CIC) approached the challenge of identifying a constituency for fund-raising development activities. Topics discussed include results of a literature review; university organization for development activities; staffing; examples of achievements;…

  17. A Paradox of Syntactic Priming: Why Response Tendencies Show Priming for Passives, and Response Latencies Show Priming for Actives

    PubMed Central

    Segaert, Katrien; Menenti, Laura; Weber, Kirsten; Hagoort, Peter

    2011-01-01

    Speakers tend to repeat syntactic structures across sentences, a phenomenon called syntactic priming. Although it has been suggested that repeating syntactic structures should result in speeded responses, previous research has focused on effects in response tendencies. We investigated syntactic priming effects simultaneously in response tendencies and response latencies for active and passive transitive sentences in a picture description task. In Experiment 1, there were priming effects in response tendencies for passives and in response latencies for actives. However, when participants' pre-existing preference for actives was altered in Experiment 2, syntactic priming occurred for both actives and passives in response tendencies as well as in response latencies. This is the first investigation of the effects of structure frequency on both response tendencies and latencies in syntactic priming. We discuss the implications of these data for current theories of syntactic processing. PMID:22022352

  18. Optimization of an Active Twist Rotor Blade Planform for Improved Active Response and Forward Flight Performance

    NASA Technical Reports Server (NTRS)

    Sekula, Martin K; Wilbur, Matthew L.

    2014-01-01

    A study was conducted to identify the optimum blade tip planform for a model-scale active twist rotor. The analysis identified blade tip design traits which simultaneously reduce rotor power of an unactuated rotor while leveraging aeromechanical couplings to tailor the active response of the blade. Optimizing the blade tip planform for minimum rotor power in forward flight provided a 5 percent improvement in performance compared to a rectangular blade tip, but reduced the vibration control authority of active twist actuation by 75 percent. Optimizing for maximum blade twist response increased the vibration control authority by 50 percent compared to the rectangular blade tip, with little effect on performance. Combined response and power optimization resulted in a blade tip design which provided similar vibration control authority to the rectangular blade tip, but with a 3.4 percent improvement in rotor performance in forward flight.

  19. Physiologic Responses Produced by Active and Passive Personal Cooling Vests

    NASA Technical Reports Server (NTRS)

    Ku, Yu-Tsuan E.; Lee, Hank C.; Montgomery, Leslie D.; Luna, Bernadette

    2000-01-01

    Personal thermoregulatory systems which provide chest cooling are used in the industrial and aerospace environments to alleviate thermal stress. However, little information is available regarding the physiologic and circulatory changes produced by routine operation of these systems. The objectives of this study were to document and compare the subjects' response to three cooling vests in their recommended configurations. The Life Enhancement Tech (LET) lightweight active cooling vest with cap, the MicroClimate Systems Change of Phase garment (MCS), and the Steele Vest were each used to cool the chest regions of 12 male and 8 female Healthy subjects (21 to 69 yr.) in this study. The subjects, seated in an upright position at normal room temperature (approx. 22 C), were tested for 60 min. with one of the cooling garments. The LET active garment had an initial coolant fluid inlet temperature of 60 F, and was ramped down to 50 F. Oral, right and left ear canal temperatures were logged manually every 5 min. Arm, leg, chest and rectal temperatures; heart rate; and respiration were recorded continuously on a U.F.I., Inc. Biolog ambulatory monitor. For men, all three vests had similar, significant cooling effects. Decreases in the average rectal temperature, oral temperature, and ear canal temperatures were approximately 0.2 C, 0.2 C and 0.1 C, respectively. In contrast to the men, the female subjects wearing the MCS and Steel vests had similar cooling responses in which the core temperature remained elevated and oral and ear canal temperatures did not drop. The LET active garment cooled most of the female subjects in this study; rectal, oral and ear temperature decreased about 0.2 C, 0.3 C and 0.3 C, respectively. These results show that the garment configurations tested do not elicit a similar thermal response in all subjects. A gender difference is evident. The LET active garment configuration was most effective in decreasing temperatures of the female subjects; the MCS

  20. Thermosphere-ionosphere coupling in response to recurrent geomagnetic activity

    NASA Astrophysics Data System (ADS)

    Mukhtarov, Plamen; Pancheva, Dora

    2012-12-01

    The paper presents the global thermosphere-ionosphere response to the high-speed solar wind streams and the subsequent recurrent geomagnetic variations with a period of 9 d during the period of time 1 October 2007-31 March 2009. The COSMIC electron density at fixed heights, as well as the ionospheric parameters foF2 and hmF2, and the two coefficients characterizing the top and bottom side vertical gradients of the electron density profile, are used for investigating the ionospheric 9-d (s=0) wave response. The SABER temperature data are utilized for studying the response of the lower thermosphere to the recurrent auroral heating. The COSMIC and SABER measurements are analyzed by one and the same method where the atmospheric tides and planetary waves which are present in the temperature and electron density measurements are simultaneously extracted from the data. The use of such data analysis approach brings to light additional features of the ionospheric response to a recurrent geomagnetic activity which have not been found before.

  1. Behavioral responses of north American Elk to recreational activity

    USGS Publications Warehouse

    Naylor, L.M.; Wisdom, M.J.; Anthony, R.G.

    2009-01-01

    Off-road recreation on public lands in North America has increased dramatically in recent years. Wild ungulates are sensitive to human activities, but the effect of off-road recreation, both motorized and nonmotorized, is poorly understood. We measured responses of elk (Cervus elaphus) to recreational disturbance in northeast Oregon, USA, from April to October, 2003 and 2004. We subjected elk to 4 types of recreational disturbance: all-terrain vehicle (ATV) riding, mountain biking, hiking, and horseback riding. Motion sensors inside radiocollars worn by 13 female elk recorded resting, feeding, and travel activities at 5-minute intervals throughout disturbance and control periods. Elk fed and rested during control periods, with little time spent traveling. Travel time increased in response to all 4 disturbances and was highest in mornings. Elk travel time was highest during ATV exposure, followed by exposure to mountain biking, hiking, and horseback riding. Feeding time decreased during ATV exposure and resting decreased when we subjected elk to mountain biking and hiking disturbance in 2003. Our results demonstrated that activities of elk can be substantially affected by off-road recreation. Mitigating these effects may be appropriate where elk are a management priority. Balancing management of species like elk with off-road recreation will become increasingly important as off-road recreational uses continue to increase on public lands in North America.

  2. Fibre constituents of some foods.

    PubMed

    Rani, B; Kawatra, A

    1994-06-01

    Some plant foods viz. bottlegourd, carrot, cauliflower, cabbage, green bengalgram, pea, apple, plum, guava, karonda, blackgram husk and lentil husk were analysed for their dietary fibre components. The total dietary fibre contents of these foods varied from 14.68 to 78.21 percent on dry matter basis. As compared to fruits and vegetables, the husks had higher amount of total dietary fibre. Cellulose represented as the major fibre constituent in most of the foods whereas, husks were observed to be good sources of hemicellulose. All foods were low in pectin and lignin contents except guava. PMID:7971775

  3. The visual accommodation response during concurrent mental activity

    NASA Technical Reports Server (NTRS)

    Malmstrom, F. V.; Randle, R. J.; Bendix, J. S.; Weber, R. J.

    1980-01-01

    The direction and magnitude of the human visual accommodation response during concurrent mental activity are investigated. Subject focusing responses to targets at distances of 0.0 D, 3.0 D and an indeterminate distance were monitored by means of an optometer during the performance of a backwards counting task and a visual imagery task (thinking near and thinking far). In both experiments a shift in accommodation towards the visual far point is observed particularly for the near target, which increases with the duration of the task. The results can be interpreted in terms of both the capacity model of Kahneman (1973) and the autonomic arousal model of Hess and Polt (1964), and are not inconsistent with the possibility of an intermediate resting position.

  4. Auditory Cortex Basal Activity Modulates Cochlear Responses in Chinchillas

    PubMed Central

    León, Alex; Elgueda, Diego; Silva, María A.; Hamamé, Carlos M.; Delano, Paul H.

    2012-01-01

    Background The auditory efferent system has unique neuroanatomical pathways that connect the cerebral cortex with sensory receptor cells. Pyramidal neurons located in layers V and VI of the primary auditory cortex constitute descending projections to the thalamus, inferior colliculus, and even directly to the superior olivary complex and to the cochlear nucleus. Efferent pathways are connected to the cochlear receptor by the olivocochlear system, which innervates outer hair cells and auditory nerve fibers. The functional role of the cortico-olivocochlear efferent system remains debated. We hypothesized that auditory cortex basal activity modulates cochlear and auditory-nerve afferent responses through the efferent system. Methodology/Principal Findings Cochlear microphonics (CM), auditory-nerve compound action potentials (CAP) and auditory cortex evoked potentials (ACEP) were recorded in twenty anesthetized chinchillas, before, during and after auditory cortex deactivation by two methods: lidocaine microinjections or cortical cooling with cryoloops. Auditory cortex deactivation induced a transient reduction in ACEP amplitudes in fifteen animals (deactivation experiments) and a permanent reduction in five chinchillas (lesion experiments). We found significant changes in the amplitude of CM in both types of experiments, being the most common effect a CM decrease found in fifteen animals. Concomitantly to CM amplitude changes, we found CAP increases in seven chinchillas and CAP reductions in thirteen animals. Although ACEP amplitudes were completely recovered after ninety minutes in deactivation experiments, only partial recovery was observed in the magnitudes of cochlear responses. Conclusions/Significance These results show that blocking ongoing auditory cortex activity modulates CM and CAP responses, demonstrating that cortico-olivocochlear circuits regulate auditory nerve and cochlear responses through a basal efferent tone. The diversity of the obtained effects

  5. Activity enhances dopaminergic long-duration response in Parkinson disease

    PubMed Central

    Auinger, Peggy; Fahn, Stanley; Oakes, David; Shoulson, Ira; Kieburtz, Karl; Rudolph, Alice; Marek, Kenneth; Seibyl, John; Lang, Anthony; Olanow, C. Warren; Tanner, Caroline; Schifitto, Giovanni; Zhao, Hongwei; Reyes, Lydia; Shinaman, Aileen; Comella, Cynthia L.; Goetz, Christopher; Blasucci, Lucia M.; Samanta, Johan; Stacy, Mark; Williamson, Kelli; Harrigan, Mary; Greene, Paul; Ford, Blair; Moskowitz, Carol; Truong, Daniel D.; Pathak, Mayank; Jankovic, Joseph; Ondo, William; Atassi, Farah; Hunter, Christine; Jacques, Carol; Friedman, Joseph H.; Lannon, Margaret; Russell, David S.; Jennings, Danna; Fussell, Barbara; Standaert, David; Schwarzschild, Michael A.; Growdon, John H.; Tennis, Marsha; Gauthier, Serge; Panisset, Michel; Hall, Jean; Gancher, Stephen; Hammerstad, John P.; Stone, Claudia; Alexander-Brown, Barbara; Factor, Stewart A.; Molho, Eric; Brown, Diane; Evans, Sharon; Clark, Jeffrey; Manyam, Bala; Simpson, Patricia; Wulbrecht, Brian; Whetteckey, Jacqueline; Martin, Wayne; Roberts, Ted; King, Pamela; Hauser, Robert; Zesiewicz, Theresa; Gauger, Lisa; Trugman, Joel; Wooten, G. Frederick; Rost-Ruffner, Elke; Perlmutter, Joel; Racette, Brad A.; Suchowersky, Oksana; Ranawaya, Ranjit; Wood, Susan; Pantella, Carol; Kurlan, Roger; Richard, Irene; Pearson, Nancy; Caviness, John N.; Adler, Charles; Lind, Marlene; Simuni, Tanya; Siderowf, Andrew; Colcher, Amy; Lloyd, Mary; Weiner, William; Shulman, Lisa; Koller, William; Lyons, Kelly; Feldman, Robert G.; Saint-Hilaire, Marie H.; Ellias, Samuel; Thomas, Cathi-Ann; Juncos, Jorge; Watts, Ray; Partlow, Anna; Tetrud, James; Togasaki, Daniel M.; Stewart, Tracy; Mark, Margery H.; Sage, Jacob I.; Caputo, Debbie; Gould, Harry; Rao, Jayaraman; McKendrick, Ann; Brin, Mitchell; Danisi, Fabio; Benabou, Reina; Hubble, Jean; Paulson, George W.; Reider, Carson; Birnbaum, Alex; Miyasaki, Janis; Johnston, Lisa; So, Julie; Pahwa, Rajesh; Dubinsky, Richard M.; Wszolek, Zbigniew; Uitti, Ryan; Turk, Margaret; Tuite, Paul; Rottenberg, David; Hansen, Joy; Ramos, Serrano; Waters, Cheryl; Lew, Mark; Welsh, Mickie; Kawai, Connie; O'Brien, Christopher; Kumar, Rajeev; Seeberger, Lauren; Judd, Deborah; Barclay, C. Lynn; Grimes, David A.; Sutherland, Laura; Dawson, Ted; Reich, Stephen; Dunlop, Rebecca; Albin, Roger; Frey, Kirk; Wernette, Kristine; Fahn, Stanley; Oakes, David; Shoulson, Ira; Kieburtz, Karl; Rudolph, Alice; Marek, Kenneth; Seibyl, John; Lang, Anthony; Olanow, C. Warren; Tanner, Caroline; Schifitto, Giovanni; Zhao, Hongwei; Reyes, Lydia; Shinaman, Aileen; Comella, Cynthia L.; Goetz, Christopher; Blasucci, Lucia M.; Samanta, Johan; Stacy, Mark; Williamson, Kelli; Harrigan, Mary; Greene, Paul; Ford, Blair; Moskowitz, Carol; Truong, Daniel D.; Pathak, Mayank; Jankovic, Joseph; Ondo, William; Atassi, Farah; Hunter, Christine; Jacques, Carol; Friedman, Joseph H.; Lannon, Margaret; Russell, David S.; Jennings, Danna; Fussell, Barbara; Standaert, David; Schwarzschild, Michael A.; Growdon, John H.; Tennis, Marsha; Gauthier, Serge; Panisset, Michel; Hall, Jean; Gancher, Stephen; Hammerstad, John P.; Stone, Claudia; Alexander-Brown, Barbara; Factor, Stewart A.; Molho, Eric; Brown, Diane; Evans, Sharon; Clark, Jeffrey; Manyam, Bala; Simpson, Patricia; Wulbrecht, Brian; Whetteckey, Jacqueline; Martin, Wayne; Roberts, Ted; King, Pamela; Hauser, Robert; Zesiewicz, Theresa; Gauger, Lisa; Trugman, Joel; Wooten, G. Frederick; Rost-Ruffner, Elke; Perlmutter, Joel; Racette, Brad A.; Suchowersky, Oksana; Ranawaya, Ranjit; Wood, Susan; Pantella, Carol; Kurlan, Roger; Richard, Irene; Pearson, Nancy; Caviness, John N.; Adler, Charles; Lind, Marlene; Simuni, Tanya; Siderowf, Andrew; Colcher, Amy; Lloyd, Mary; Weiner, William; Shulman, Lisa; Koller, William; Lyons, Kelly; Feldman, Robert G.; Saint-Hilaire, Marie H.; Ellias, Samuel; Thomas, Cathi-Ann; Juncos, Jorge; Watts, Ray; Partlow, Anna; Tetrud, James; Togasaki, Daniel M.; Stewart, Tracy; Mark, Margery H.; Sage, Jacob I.; Caputo, Debbie; Gould, Harry; Rao, Jayaraman; McKendrick, Ann; Brin, Mitchell; Danisi, Fabio; Benabou, Reina; Hubble, Jean; Paulson, George W.; Reider, Carson; Birnbaum, Alex; Miyasaki, Janis; Johnston, Lisa; So, Julie; Pahwa, Rajesh; Dubinsky, Richard M.; Wszolek, Zbigniew; Uitti, Ryan; Turk, Margaret; Tuite, Paul; Rottenberg, David; Hansen, Joy; Ramos, Serrano; Waters, Cheryl; Lew, Mark; Welsh, Mickie; Kawai, Connie; O'Brien, Christopher; Kumar, Rajeev; Seeberger, Lauren; Judd, Deborah; Barclay, C. Lynn; Grimes, David A.; Sutherland, Laura; Dawson, Ted; Reich, Stephen; Dunlop, Rebecca; Albin, Roger; Frey, Kirk; Wernette, Kristine; Mendis, Tilak

    2012-01-01

    Objective: We tested the hypothesis that dopamine-dependent motor learning mechanism underlies the long-duration response to levodopa in Parkinson disease (PD) based on our studies in a mouse model. By data-mining the motor task performance in dominant and nondominant hands of the subjects in a double-blind randomized trial of levodopa therapy, the effects of activity and dopamine therapy were examined. Methods: We data-mined the Earlier versus Later Levodopa Therapy in Parkinson's Disease (ELLDOPA) study published in 2005 and performed statistical analysis comparing the effects of levodopa and dominance of handedness over 42 weeks. Results: The mean change in finger-tapping counts from baseline before the initiation of therapy to predose at 9 weeks and 40 weeks increased more in the dominant compared to nondominant hand in levodopa-treated subjects in a dose-dependent fashion. There was no significant difference in dominant vs nondominant hands in the placebo group. The short-duration response assessed by the difference of postdose performance compared to predose performance at the same visit did not show any significant difference between dominant vs nondominant hands. Conclusions: Active use of the dominant hand and dopamine replacement therapy produces synergistic effect on long-lasting motor task performance during “off” medication state. Such effect was confined to dopamine-responsive symptoms and not seen in dopamine-resistant symptoms such as gait and balance. We propose that long-lasting motor learning facilitated by activity and dopamine is a form of disease modification that is often seen in trials of medications that have symptomatic effects. PMID:22459675

  6. Responses of cells in plasma-activated medium

    NASA Astrophysics Data System (ADS)

    Tanaka, Hiromasa; Mizuno, Masaaki; Ishikawa, Kenji; Takeda, Keigo; Hashizume, Hiroshi; Nakamura, Kae; Kajiyama, Hiroaki; Kano, Hiroyuki; Okazaki, Yasumasa; Toyokuni, Shinya; Maruyama, Shoichi; Kodera, Yasuhiro; Terasaki, Hiroko; Adachi, Tetsuo; Kato, Masashi; Kikkawa, Fumitaka; Hori, Masaru

    2015-09-01

    Plasma consists of electrons, ions, radicals, and lights, and produces various reactive species in gas and liquid phase. Cells receive various inputs from their circumstances, and induce several physiological outputs. Our goal is to clarify the relationships between plasma inputs and physiological outputs. Plasma-activated medium (PAM) is a circumstance that plasma provides cells and our previous studies suggest that PAM is a promising tool for cancer therapy. However, the mode of actions remains to be elucidated. We propose survival and proliferation signaling networks as well as redox signaling networks are key factors to understand cellular responses of PAM-treated glioblastoma cells.

  7. Current radar responsive tag development activities at Sandia National Laboratories.

    SciTech Connect

    Plummer, Kenneth W.; Ormesher, Richard C.

    2003-09-01

    Over the past ten years, Sandia has developed RF radar responsive tag systems and supporting technologies for various government agencies and industry partners. RF tags can function as RF transmitters or radar transponders that enable tagging, tracking, and location determination functions. Expertise in tag architecture, microwave and radar design, signal analysis and processing techniques, digital design, modeling and simulation, and testing have been directly applicable to these tag programs. In general, the radar responsive tag designs have emphasized low power, small package size, and the ability to be detected by the radar at long ranges. Recently, there has been an interest in using radar responsive tags for Blue Force tracking and Combat ID (CID). The main reason for this interest is to allow airborne surveillance radars to easily distinguish U.S. assets from those of opposing forces. A Blue Force tracking capability would add materially to situational awareness. Combat ID is also an issue, as evidenced by the fact that approximately one-quarter of all U.S. casualties in the Gulf War took the form of ground troops killed by friendly fire. Because the evolution of warfare in the intervening decade has made asymmetric warfare the norm rather than the exception, swarming engagements in which U.S. forces will be freely intermixed with opposing forces is a situation that must be anticipated. Increasing utilization of precision munitions can be expected to drive fires progressively closer to engaged allied troops at times when visual de-confliction is not an option. In view of these trends, it becomes increasingly important that U.S. ground forces have a widely proliferated all-weather radar responsive tag that communicates to all-weather surveillance. The purpose of this paper is to provide an overview of the recent, current, and future radar responsive research and development activities at Sandia National Laboratories that support both the Blue Force Tracking

  8. Active microwave responses - An aid in improved crop classification

    NASA Technical Reports Server (NTRS)

    Rosenthal, W. D.; Blanchard, B. J.

    1984-01-01

    A study determined the feasibility of using visible, infrared, and active microwave data to classify agricultural crops such as corn, sorghum, alfalfa, wheat stubble, millet, shortgrass pasture and bare soil. Visible through microwave data were collected by instruments on board the NASA C-130 aircraft over 40 agricultural fields near Guymon, OK in 1978 and Dalhart, TX in 1980. Results from stepwise and discriminant analysis techniques indicated 4.75 GHz, 1.6 GHz, and 0.4 GHz cross-polarized microwave frequencies were the microwave frequencies most sensitive to crop type differences. Inclusion of microwave data in visible and infrared classification models improved classification accuracy from 73 percent to 92 percent. Despite the results, further studies are needed during different growth stages to validate the visible, infrared, and active microwave responses to vegetation.

  9. [Chemical constituents from Bidens bipinnata].

    PubMed

    Wang, Xiao-Yu; Chen, Guan-Ru; Deng, Zi-Yun; Zhao, Jie; Ge, Jin-Fang; Li, Ning; Chen, Fei-Hu

    2014-05-01

    To investigate the chemical constituents of the whole plants of Bidens bipinnata, the separation and purification of constituents were performed by chromatography on macroporous resin, silica gel, MCI and Sephadex LH-20. Their structures were elucidated by spectroscopic data as quercetin (1), quercetin-3-0-alpha-L-rhamnoside (2), keampferol-3-O-beta-D-glucopyranoside (3), keampferol-3-O-alpha-L-rhamnoside (4), 3', 5-dyhydroxy-3, 6, 4'-trimethoxyl -7-O-beta-D-glucopyranoside flavonoid (5), 7, 8, 3', 4'-tetraflavanone(6), (2S)- and (2R)-isookanin-7-O-beta-D- glucopyranoside (7a/7b), (2S)- and (2R)-3'-methoxy-isookanin-8-O-beta-D-glucopyranoside (8a/8b), 6, 7, 3', 4'-tetrahydroxyaurone(9), maritimetin (10), esculetin (11), 3-O-caffeoyl-2-methyl-d-erythrono-1, 4-lactone (12), (7S, 8R) balanophonin-4-O-beta-D-glucopyranoside (13), eugenyl-O-beta-apiofuranosyl-( 1"-6') -O-beta-glucopyranoside (14), and (+)-syringaresinol-4'-O-beta-D-glucopyranoside (15). Compounds 8, 13, 14, and 15 were isolated from this genus for the first time. Compounds 1 and 6 were potent inhibitors against HSC-T6 cells in vitro and compounds 1, 2, 6, and 7 were capable of decreasing the inflammatory cytokine production of macrophage cells in vitro. PMID:25282892

  10. Scutellarein Reduces Inflammatory Responses by Inhibiting Src Kinase Activity

    PubMed Central

    Sung, Nak Yoon

    2015-01-01

    Flavonoids are plant pigments that have been demonstrated to exert various pharmacological effects including anti-cancer, anti-diabetic, anti-atherosclerotic, anti-bacterial, and anti-inflammatory activities. However, the molecular mechanisms in terms of exact target proteins of flavonoids are not fully elucidated yet. In this study, we aimed to evaluate the anti-inflammatory mechanism of scutellarein (SCT), a flavonoid isolated from Erigeron breviscapus, Clerodendrum phlomidis and Oroxylum indicum Vent that have been traditionally used to treat various inflammatory diseases in China and Brazil. For this purpose, a nitric oxide (NO) assay, polymerase chain reaction (PCR), nuclear fractionation, immunoblot analysis, a kinase assay, and an overexpression strategy were employed. Scutellarein significantly inhibited NO production in a dose-dependent manner and reduced the mRNA expression levels of inducible NO synthase (iNOS) and tumor necrosis factor (TNF)-α in lipopolysaccharide (LPS)-activated RAW264.7 cells. In addition, SCT also dampened nuclear factor (NF)-κB-driven expression of a luciferase reporter gene upon transfection of a TIR-domain-containing adapter-inducing interferon-β (TRIF) construct into Human embryonic kidney 293 (HEK 293) cells; similarly, NF-κ B nuclear translocation was inhibited by SCT. Moreover, the phosphorylation levels of various upstream signaling enzymes involved in NF-κB activation were decreased by SCT treatment in LPS-treated RAW264.7 cells. Finally, SCT strongly inhibited Src kinase activity and also inhibited the autophosphorylation of overexpressed Src. Therefore, our data suggest that SCT can block the inflammatory response by directly inhibiting Src kinase activity linked to NF-κB activation. PMID:26330757

  11. Differences in wearer response to garments for outdoor activity.

    PubMed

    Laing, R M; Sims, S T; Wilson, C A; Niven, B E; Cruthers, N M

    2008-04-01

    The performance of garments for outdoor activity was compared. Three fabrics, each in garments for the upper body, matched garment/wearer dimensions, were worn by 10 athletically 'well-trained' males under controlled conditions (hot 32 +/- 2 degrees C, 20 +/- 2% relative humidity (RH); cold 8 +/- 2 degrees C, 40 +/- 2% RH) with physical (instrumental) and sensory responses obtained during the trials. Differences in human responses to the fabrics/garments included heart rate, core temperature during run (hot, cold), rest (hot) and walk (cold), heat content of the body, humidity under garments during rest and run and time to onset of sweating. No such differences were identified for change in body mass, core temperature during walk (hot) and rest (cold), skin temperature, temperature of skin covered by the garment, humidity under the garments during walk or for any perceptions (thermal sensations, thermal comfort of torso, exertion, wetness). The garment in single jersey wool fabric performed best in both hot and cold conditions. Effects of garments on wearers are often related to properties of the fabrics from which the garments are made. This study shows that only some differences in fabric properties result in measurable thermophysiological and perceptual responses of the garment wearers and underlines the difficulty in predicting performance of garments/persons from laboratory tests on fabrics. PMID:18357537

  12. A supramolecular microgel glutathione peroxidase mimic with temperature responsive activity.

    PubMed

    Yin, Yanzhen; Jiao, Shufei; Lang, Chao; Liu, Junqiu

    2014-05-21

    Glutathione peroxidase (GPx) protects cells from oxidative damage by scavenging surplus reactive oxygen species (ROS). Commonly, an appropriate amount of ROS acts as a signal molecule in the metabolism. A smart artificial GPx exhibits adjustable catalytic activity, which can potentially reduce the amount of ROS to an appropriate degree and maintain its important physiological functions in metabolism. To construct an optimum and excellent smart artificial GPx, a novel supramolecular microgel artificial GPx (SM-Te) was prepared based on the supramolecular host-guest interaction employing the tellurium-containing guest molecule (ADA-Te-ADA) and the cyclodextrin-containing host block copolymer (poly(N-isopropylacrylamide)-b-[polyacrylamides-co-poly(6-o-(triethylene glycol monoacrylate ether)-β-cyclodextrin)], PPAM-CD) as building blocks. Subsequently, based on these building blocks, SM-Te was constructed and the formation of its self-assembled structure was confirmed by dynamic light scattering, NMR, SEM, TEM, etc. Typically, benefitting from the temperature responsive properties of the PNIPAM scaffold, SM-Te also exhibited similar temperature responsive behaviour. Importantly, the GPx catalytic rates of SM-Te displayed a noticeable temperature responsive characteristic. Moreover, SM-Te exhibited the typical saturation kinetics behaviour of a real enzyme catalyst. It was proved that the changes of the hydrophobic microenvironment and the pore size in the supramolecular microgel network of SM-Te played significant roles in altering the temperature responsive catalytic behaviour. The successful construction of SM-Te not only overcomes the insurmountable disadvantages existing in previous covalent bond crosslinked microgel artificial GPx but also bodes well for the development of novel intelligent antioxidant drugs. PMID:24652520

  13. Affective Response to Physical Activity: Testing for Measurement Invariance of the Physical Activity Affect Scale across Active and Non-Active Individuals

    ERIC Educational Resources Information Center

    Carpenter, Laura C.; Tompkins, Sara Anne; Schmiege, Sarah J.; Nilsson, Renea; Bryan, Angela

    2010-01-01

    Affective responses to physical activity are assumed to play a role in exercise initiation and maintenance. The Physical Activity Affect Scale measures four dimensions of an individual's affective response to exercise. Group differences in the interpretation of scale items can impact the interpretability of mean differences, underscoring the need…

  14. GITR Activation Positively Regulates Immune Responses against Toxoplasma gondii

    PubMed Central

    Costa, Frederico R. C.; Mota, Caroline M.; Santiago, Fernanda M.; Silva, Murilo V.; Ferreira, Marcela D.; Fonseca, Denise M.; Silva, João S.; Mineo, José R.; Mineo, Tiago W. P.

    2016-01-01

    Toxoplasma gondii is a widespread parasite responsible for causing clinical diseases especially in pregnant and immunosuppressed individuals. Glucocorticoid-induced TNF receptor (GITR), which is also known as TNFRS18 and belongs to the TNF receptor superfamily, is found to be expressed in various cell types of the immune system and provides an important costimulatory signal for T cells and myeloid cells. However, the precise role of this receptor in the context of T. gondii infection remains elusive. Therefore, the current study investigated the role of GITR activation in the immunoregulation mechanisms induced during the experimental infection of mice with T. gondii. Our data show that T. gondii infection slightly upregulates GITR expression in Treg cells and B cells, but the most robust increment in expression was observed in macrophages and dendritic cells. Interestingly, mice infected and treated with an agonistic antibody anti-GITR (DTA-1) presented a robust increase in pro-inflammatory cytokine production at preferential sites of parasite replication, which was associated with the decrease in latent brain parasitism of mice under treatment with DTA-1. Several in vivo and in vitro analysis were performed to identify the cellular mechanisms involved in GITR activation upon infection, however no clear alterations were detected in the phenotype/function of macrophages, Tregs and B cells under treatment with DTA-1. Therefore, GITR appears as a potential target for intervention during infection by the parasite Toxoplasma gondii, even though further studies are still necessary to better characterize the immune response triggered by GITR activation during T. gondii infection. PMID:27027302

  15. Sulforaphane prevents pulmonary damage in response to inhaled arsenic by activating the Nrf2-defense response

    SciTech Connect

    Zheng, Yi; Tao, Shasha; Lian, Fangru; Chau, Binh T.; Chen, Jie; Sun, Guifan; Fang, Deyu; Lantz, R. Clark; Zhang, Donna D.

    2012-12-15

    Exposure to arsenic is associated with an increased risk of lung disease. Novel strategies are needed to reduce the adverse health effects associated with arsenic exposure in the lung. Nrf2, a transcription factor that mediates an adaptive cellular defense response, is effective in detoxifying environmental insults and prevents a broad spectrum of diseases induced by environmental exposure to harmful substances. In this report, we tested whether Nrf2 activation protects mice from arsenic-induced toxicity. We used an in vivo arsenic inhalation model that is highly relevant to low environmental human exposure to arsenic-containing dusts. Two-week exposure to arsenic-containing dust resulted in pathological alterations, oxidative DNA damage, and mild apoptotic cell death in the lung; all of which were blocked by sulforaphane (SF) in an Nrf2-dependent manner. Mechanistically, SF-mediated activation of Nrf2 alleviated inflammatory responses by modulating cytokine production. This study provides strong evidence that dietary intervention targeting Nrf2 activation is a feasible approach to reduce adverse health effects associated with arsenic exposure. -- Highlights: ► Exposed to arsenic particles and/or SF have elevated Nrf2 and its target genes. ► Sulforaphane prevents pathological alterations, oxidative damage and cell death. ► Sulforaphane alleviates infiltration of inflammatory cells into the lungs. ► Sulforaphane suppresses arsenic-induced proinflammatory cytokine production.

  16. Respiratory responses to passive and active recovery from exercise.

    PubMed

    Takahashi, T; Niizeki, K; Miyamoto, Y

    1997-02-01

    To investigate the effect of the neural components associated with leg movements on the control of ventilation during recovery from exercise, we recorded the minute ventilation (VE), oxygen uptake (VO2), and carbon dioxide output (VCO2) of eight normal volunteers during recovery from moderate, steady-state cycle exercise (170 W). The recovery phases were undergone separately under two different conditions: 5 min of rest (passive recovery) on a bicycle ergometer and 3 min of pedaling at a work rate of 0W (active recovery) followed by 2 min of rest. The phase-1 responses were observed in all the variables studied at the transition of passive recovery but not in the active recovery phase. The kinetics of VCO2, during the off-transition were significantly faster than those of VE in both recoveries, indicating that the decreases in VCO2 could precede the decreases in VE. Although the levels of VE and VCO2 during active recovery were significantly higher than those during passive recovery, the decline in VE was closely proportional to that of VCO2 under both recovery conditions, with resultant indications of similar VE-VCO2 regression lines. These findings suggest that the flux of CO2 to the lungs is an important determinant of ventilatory drive during recovery, and that neither central command nor neural afferents from contracting muscles are requisite for the control of ventilation during recovery from exercise. PMID:9159643

  17. Antimelanoma and Antityrosinase from Alpinia galangal Constituents

    PubMed Central

    Liu, Po-Len; Lin, Li-Ching; Chen, Yen-Ting; Hseu, You-Cheng; Wen, Zhi-Hong

    2013-01-01

    Two compounds, 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (BHPHTO) and bisdemethoxycurcumin (BDMC) they have been isolated from the rhizomes of Alpinia galangal, and the structures of both pure constituents were determined using spectroscopic analyses. The study examined the bioeffectivenesses of the two compounds on the human melanoma A2058 and showed that significantly inhibited the proliferation of melanoma cells in the cell viability assay. This research was also taken on the tests to B16-F10 cell line and showed minor inhibitory consequences of cellular tyrosinase activities and melanin contents. Our results revealed the anticancer effects of A. galangal compounds, and therefore, the target compounds could be potentially applied in the therapeutic application and the food industry. PMID:24027439

  18. Activation of oxidative stress-responsive signaling pathways in early splenotoxic response of aniline

    SciTech Connect

    Wang Jianling; Wang Gangduo; Ansari, G.A.S.; Khan, M. Firoze

    2008-07-15

    Aniline exposure causes toxicity to the spleen, which leads to a variety of sarcomas, and fibrosis appears to be an important preneoplastic lesion. However, early molecular mechanisms in aniline-induced toxicity to the spleen are not known. Previously, we have shown that aniline exposure results in iron overload and induction of oxidative stress in the spleen, which can cause transcriptional upregulation of fibrogenic/inflammatory cytokines via activation of oxidative stress (OS)-responsive signaling pathways. To test this mechanism, male SD rats were treated with aniline (1mmol/kg/day via gavage) for 7days, an experimental condition that precedes the appearance of fibrosis. Significant increases in both NF-{kappa}B and AP-1 binding activity was observed in the nuclear extracts of splenocytes from aniline-treated rats as determined by ELISAs, and supported by Western blot data showing increases in p-I{kappa}B{alpha}, p-p65 and p-c-Jun. To understand the upstream signaling events which could account for the activation of NF-{kappa}B and AP-1, phosphorylation patterns of I{kappa}B kinases (IKK{alpha} and IKK{beta}) and mitogen-activated protein kinases (MAPKs) were pursued. Our data showed remarkable increases in both p-IKK{alpha} and p-IKK{beta} in the splenocytes from aniline-treated rats, suggesting their role in the phosphorylation of both I{kappa}B{alpha} and p65 subunits. Furthermore, aniline exposure led to activation of all three classes of MAPKs, as evident from increased phosphorylation of extracellular-signal-regulated kinase (ERK1/2), c-Jun N-terminal kinase (JNK1/2) and p38 MAPKs, which could potentially contribute to the observed activation of both AP-1 and NF-{kappa}B. Activation of upstream signaling molecules was also associated with simultaneous increases in gene transcription of cytokines IL-1, IL-6 and TNF-{alpha}. The observed sequence of events following aniline exposure could initiate a fibrogenic and/or tumorigenic response in the spleen.

  19. Growing media constituents determine the microbial nitrogen conversions in organic growing media for horticulture.

    PubMed

    Grunert, Oliver; Reheul, Dirk; Van Labeke, Marie-Christine; Perneel, Maaike; Hernandez-Sanabria, Emma; Vlaeminck, Siegfried E; Boon, Nico

    2016-05-01

    Vegetables and fruits are an important part of a healthy food diet, however, the eco-sustainability of the production of these can still be significantly improved. European farmers and consumers spend an estimated €15.5 billion per year on inorganic fertilizers and the production of N-fertilizers results in a high carbon footprint. We investigated if fertilizer type and medium constituents determine microbial nitrogen conversions in organic growing media and can be used as a next step towards a more sustainable horticulture. We demonstrated that growing media constituents showed differences in urea hydrolysis, ammonia and nitrite oxidation and in carbon dioxide respiration rate. Interestingly, mixing of the growing media constituents resulted in a stimulation of the function of the microorganisms. The use of organic fertilizer resulted in an increase in amoA gene copy number by factor 100 compared to inorganic fertilizers. Our results support our hypothesis that the activity of the functional microbial community with respect to nitrogen turnover in an organic growing medium can be improved by selecting and mixing the appropriate growing media components with each other. These findings contribute to the understanding of the functional microbial community in growing media and its potential role towards a more responsible horticulture. PMID:27005434

  20. Integrated and Independent Learning of Hand-Related Constituent Sequences

    ERIC Educational Resources Information Center

    Berner, Michael P.; Hoffmann, Joachim

    2009-01-01

    In almost all daily activities fingers of both hands are used in coordinated succession. The present experiments explored whether learning in such tasks pertains not only to the overall sequence spanning both hands but also to the constituent sequences of each hand. In a serial reaction time task, 2 repeating hand-related sequences were…

  1. Antiparasitic, Nematicidal and Antifouling Constituents from Juniperus Berries

    Technology Transfer Automated Retrieval System (TEKTRAN)

    A bioassay-guided fractionation of Juniperus procera berries yielded antiparasitic, nematicidal and antifouling constituents, including a wide range of known abietane, pimarane and labdane diterpenes. Among these, abieta-7,13-diene (1) demonstrated in vitro antimalarial activity against Plasmodium f...

  2. Effectiveness of classroom response systems within an active learning environment.

    PubMed

    Welch, Susan

    2013-11-01

    In nursing education, the inclusion of pedagogical tools is necessary to transform Millennial classrooms. One such pedagogical tool currently offered is classroom response systems (CRS). The purpose of this study was to evaluate the effectiveness of CRS as a pedagogical tool in improving nursing students' examination performance within an active learning environment. A pretest-posttest design was used to determine whether there was a relationship between the use of CRS (independent variable) and nursing students' examination performance in a first-year Professional Practice course (dependent variable). Paired t tests revealed no greater improvement in posttest scores. Therefore, the use of CRS technology was not effective in increasing nursing students' examination scores in the Professional Practice course. Additional research is needed to provide adequate understanding of the effectiveness of CRS within the nursing education classroom. PMID:24127175

  3. Anti-ulcer effect in rats of bitter cardamon constituents.

    PubMed

    Yamahara, J; Li, Y H; Tamai, Y

    1990-11-01

    The effects of bitter cardamon (the fruit of Alpinia oxphylla), used as a medicine and a condiment, on HCl/ethanol-induced gastric lesions in rats were examined. The acetone extract at 50 mg/kg, p.o. significantly inhibited gastric lesions by 57.0%. An analysis of the active constituents in the acetone extract was performed using column chromatography. Nootkatone at 20 mg/kg, p.o. significantly inhibited gastric lesion. These results suggest that nootkatone, the sesquiterpenoid is an important constituent in stomach medications containing bitter cardamon. PMID:2085887

  4. Active Disaster Response System for a Smart Building

    PubMed Central

    Lin, Chun-Yen; Chu, Edward T.-H; Ku, Lun-Wei; Liu, Jane W. S.

    2014-01-01

    Disaster warning and surveillance systems have been widely applied to help the public be aware of an emergency. However, existing warning systems are unable to cooperate with household appliances or embedded controllers; that is, they cannot provide enough time for preparedness and evacuation, especially for disasters like earthquakes. In addition, the existing warning and surveillance systems are not responsible for collecting sufficient information inside a building for relief workers to conduct a proper rescue action after a disaster happens. In this paper, we describe the design and implementation of a proof of concept prototype, named the active disaster response system (ADRS), which automatically performs emergency tasks when an earthquake happens. ADRS can interpret Common Alerting Protocol (CAP) messages, published by an official agency, and actuate embedded controllers to perform emergency tasks to respond to the alerts. Examples of emergency tasks include opening doors and windows and cutting off power lines and gas valves. In addition, ADRS can maintain a temporary network by utilizing the embedded controllers; hence, victims trapped inside a building are still able to post emergency messages if the original network is disconnected. We conducted a field trial to evaluate the effectiveness of ADRS after an earthquake happened. Our results show that compared to manually operating emergency tasks, ADRS can reduce the operation time by up to 15 s, which is long enough for people to get under sturdy furniture, or to evacuate from the third floor to the first floor, or to run more than 100 m. PMID:25237897

  5. Design of Responsive and Active (Soft) Materials Using Liquid Crystals.

    PubMed

    Bukusoglu, Emre; Bedolla Pantoja, Marco; Mushenheim, Peter C; Wang, Xiaoguang; Abbott, Nicholas L

    2016-06-01

    Liquid crystals (LCs) are widely known for their use in liquid crystal displays (LCDs). Indeed, LCDs represent one of the most successful technologies developed to date using a responsive soft material: An electric field is used to induce a change in ordering of the LC and thus a change in optical appearance. Over the past decade, however, research has revealed the fundamental underpinnings of potentially far broader and more pervasive uses of LCs for the design of responsive soft material systems. These systems involve a delicate interplay of the effects of surface-induced ordering, elastic strain of LCs, and formation of topological defects and are characterized by a chemical complexity and diversity of nano- and micrometer-scale geometry that goes well beyond that previously investigated. As a reflection of this evolution, the community investigating LC-based materials now relies heavily on concepts from colloid and interface science. In this context, this review describes recent advances in colloidal and interfacial phenomena involving LCs that are enabling the design of new classes of soft matter that respond to stimuli as broad as light, airborne pollutants, bacterial toxins in water, mechanical interactions with living cells, molecular chirality, and more. Ongoing efforts hint also that the collective properties of LCs (e.g., LC-dispersed colloids) will, over the coming decade, yield exciting new classes of driven or active soft material systems in which organization (and useful properties) emerges during the dissipation of energy. PMID:26979412

  6. Active disaster response system for a smart building.

    PubMed

    Lin, Chun-Yen; Chu, Edward T-H; Ku, Lun-Wei; Liu, Jane W S

    2014-01-01

    Disaster warning and surveillance systems have been widely applied to help the public be aware of an emergency. However, existing warning systems are unable to cooperate with household appliances or embedded controllers; that is, they cannot provide enough time for preparedness and evacuation, especially for disasters like earthquakes. In addition, the existing warning and surveillance systems are not responsible for collecting sufficient information inside a building for relief workers to conduct a proper rescue action after a disaster happens. In this paper, we describe the design and implementation of a proof of concept prototype, named the active disaster response system (ADRS), which automatically performs emergency tasks when an earthquake happens. ADRS can interpret Common Alerting Protocol (CAP) messages, published by an official agency, and actuate embedded controllers to perform emergency tasks to respond to the alerts. Examples of emergency tasks include opening doors and windows and cutting off power lines and gas valves. In addition, ADRS can maintain a temporary network by utilizing the embedded controllers; hence, victims trapped inside a building are still able to post emergency messages if the original network is disconnected. We conducted a field trial to evaluate the effectiveness of ADRS after an earthquake happened. Our results show that compared to manually operating emergency tasks, ADRS can reduce the operation time by up to 15 s, which is long enough for people to get under sturdy furniture, or to evacuate from the third floor to the first floor, or to run more than 100 m. PMID:25237897

  7. Stress responses in flavivirus-infected cells: activation of unfolded protein response and autophagy

    PubMed Central

    Blázquez, Ana-Belén; Escribano-Romero, Estela; Merino-Ramos, Teresa; Saiz, Juan-Carlos; Martín-Acebes, Miguel A.

    2014-01-01

    The Flavivirus is a genus of RNA viruses that includes multiple long known human, animal, and zoonotic pathogens such as Dengue virus, yellow fever virus, West Nile virus, or Japanese encephalitis virus, as well as other less known viruses that represent potential threats for human and animal health such as Usutu or Zika viruses. Flavivirus replication is based on endoplasmic reticulum-derived structures. Membrane remodeling and accumulation of viral factors induce endoplasmic reticulum stress that results in activation of a cellular signaling response termed unfolded protein response (UPR), which can be modulated by the viruses for their own benefit. Concomitant with the activation of the UPR, an upregulation of the autophagic pathway in cells infected with different flaviviruses has also been described. This review addresses the current knowledge of the relationship between endoplasmic reticulum stress, UPR, and autophagy in flavivirus-infected cells and the growing evidences for an involvement of these cellular pathways in the replication and pathogenesis of these viruses. PMID:24917859

  8. Antioxidant Constituents of Cotoneaster melanocarpus Lodd.

    PubMed

    Holzer, Veronika M D; Lower-Nedza, Agnieszka D; Nandintsetseg, Myagmar; Batkhuu, Javzan; Brantner, Adelheid H

    2013-01-01

    The aim of this study was the evaluation of the antioxidant capacity of Cotoneaster melanocarpus Lodd. and the identification of antioxidant active constituents of this plant. C. melanocarpus Lodd. is a shrub indigenous to Mongolia and used in Traditional Mongolian Medicine as a styptic. Before extraction, the plant material was separated into three parts: young sterile shoots, older stems and leaves. All these parts were extracted with water, methanol, ethyl acetate, dichloromethane and hexane, successively. The methanolic extract of the sterile shoots showed the highest antioxidant activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assay (IC50 30.91 ± 2.97 µg/mL). This active extract was further analyzed with chromatographic methods. TLC fingerprinting and HPLC indicated the presence of the flavonol glycosides quercetin-3-O-rutinoside (rutin), quercetin-3-O-galactoside (hyperoside) and quercetin-3-O-glucoside (isoquercetin), ursolic acid as well as chlorogenic acid, neochlorogenic acid and cryptochlorogenic acid. The findings were substantiated with LC-MS. All identified compounds have antioxidant properties and therefore contribute to the radical scavenging activity of the whole plant. PMID:26784464

  9. Listening as a Perceived and Interactive Activity: Understanding the Impact of Verbal Listening Responses

    ERIC Educational Resources Information Center

    Hall, Bradford

    2012-01-01

    This sequenced activity encourages active engagement with the idea that listening and speaking are not inherently separate or one-way activities. Listening involves both verbal, and nonverbal responses and perceptions of effective listening are tied to these patterns of response. These patterns of response impact both the immediate communication…

  10. Active Ageing in CIS Countries: Semantics, Challenges, and Responses

    PubMed Central

    Sidorenko, Alexandre; Zaidi, Asghar

    2013-01-01

    Although the CIS countries are connected together by the legacy of breaking away from the Soviet Union, they have had a distinctive transition course and are rather diverse in terms of the population ageing challenges and policy responses in place. The commonality is that a comprehensive national strategy on ageing is lacking, and many of necessary reforms were put aside owing to political uncertainties, lack of societal consensus, and financial instability. The notion of active ageing is associated with the term “accelerated ageing,” which is understood to be an individual living a life under harsh living conditions or a society experiencing rapid increases in the relative number of older persons, and therefore it carries a negative connotation. Yet, in the same spirit as the European Year for Active Ageing and Solidarity between Generations 2012, the CIS countries have initiated sectoral programmes towards enhancing employment of older workers, social participation of older people in the society in a wider sense and also measures promoting health and independent living of older persons. PMID:23346109

  11. Physcomitrella patens Activates Defense Responses against the Pathogen Colletotrichum gloeosporioides.

    PubMed

    Reboledo, Guillermo; Del Campo, Raquel; Alvarez, Alfonso; Montesano, Marcos; Mara, Héctor; Ponce de León, Inés

    2015-01-01

    The moss Physcomitrella patens is a suitable model plant to analyze the activation of defense mechanisms after pathogen assault. In this study, we show that Colletotrichum gloeosporioides isolated from symptomatic citrus fruit infects P. patens and cause disease symptoms evidenced by browning and maceration of tissues. After C. gloeosporioides infection, P. patens reinforces the cell wall by the incorporation of phenolic compounds and induces the expression of a Dirigent-protein-like encoding gene that could lead to the formation of lignin-like polymers. C. gloeosporioides-inoculated protonemal cells show cytoplasmic collapse, browning of chloroplasts and modifications of the cell wall. Chloroplasts relocate in cells of infected tissues toward the initially infected C. gloeosporioides cells. P. patens also induces the expression of the defense genes PAL and CHS after fungal colonization. P. patens reporter lines harboring the auxin-inducible promoter from soybean (GmGH3) fused to β-glucuronidase revealed an auxin response in protonemal tissues, cauloids and leaves of C. gloeosporioides-infected moss tissues, indicating the activation of auxin signaling. Thus, P. patens is an interesting plant to gain insight into defense mechanisms that have evolved in primitive land plants to cope with microbial pathogens. PMID:26389888

  12. Physcomitrella patens Activates Defense Responses against the Pathogen Colletotrichum gloeosporioides

    PubMed Central

    Reboledo, Guillermo; del Campo, Raquel; Alvarez, Alfonso; Montesano, Marcos; Mara, Héctor; Ponce de León, Inés

    2015-01-01

    The moss Physcomitrella patens is a suitable model plant to analyze the activation of defense mechanisms after pathogen assault. In this study, we show that Colletotrichum gloeosporioides isolated from symptomatic citrus fruit infects P. patens and cause disease symptoms evidenced by browning and maceration of tissues. After C. gloeosporioides infection, P. patens reinforces the cell wall by the incorporation of phenolic compounds and induces the expression of a Dirigent-protein-like encoding gene that could lead to the formation of lignin-like polymers. C. gloeosporioides-inoculated protonemal cells show cytoplasmic collapse, browning of chloroplasts and modifications of the cell wall. Chloroplasts relocate in cells of infected tissues toward the initially infected C. gloeosporioides cells. P. patens also induces the expression of the defense genes PAL and CHS after fungal colonization. P. patens reporter lines harboring the auxin-inducible promoter from soybean (GmGH3) fused to β-glucuronidase revealed an auxin response in protonemal tissues, cauloids and leaves of C. gloeosporioides-infected moss tissues, indicating the activation of auxin signaling. Thus, P. patens is an interesting plant to gain insight into defense mechanisms that have evolved in primitive land plants to cope with microbial pathogens. PMID:26389888

  13. Cardiovascular responses to active and passive cycling movements.

    PubMed

    Nóbrega, A C; Williamson, J W; Friedman, D B; Araújo, C G; Mitchell, J H

    1994-06-01

    Ten healthy subjects were evaluated at rest and at 5 min of unloaded active (AC) and passive (PC) cycling. Passive limb movements were accomplished using a tandem bicycle with a second rider performing the movements. We measured heart rate (HR), mean arterial pressure (MAP), cardiac output (CO), oxygen uptake (VO2), rating of perceived exertion (RPE), and electrical activity (EMG) of lower limbs muscles. Values for stroke volume (SV) and peripheral vascular resistance (PVR) were calculated. EMG, RPE, and VO2 were higher during AC than during PC (P < 0.001). CO increased during both modes of cycling, but during AC it resulted from a HR acceleration (73 +/- 2 at rest to 82 +/- 2 beats.min-1 at 60 rpm; P < 0.001) with no change in SV whereas during PC, SV increased from rest (65 +/- 4 at rest to 71 +/- 3 ml at 60 rpm; P = 0.003) along with no change in HR. PVR remained constant during PC, but decreased by 13% during AC (P < 0.001) and MAP increased only during PC (93 +/- 2 at rest to 107 +/- 2 mm Hg at 60 rpm). These results supports the concept that central command determines the HR response to dynamic exercise. The increase in SV and consequently in MAP during PC was probably due to increased venous return and/or to muscle mechanoreceptor-evoked increased myocardial contractility. PMID:8052111

  14. Apparatus and method for separating constituents

    DOEpatents

    Maronde, Carl P.; Killmeyer, Jr., Richard P.

    1992-01-01

    A centrifugal separator apparatus and method for improving the efficiency of the separation of constituents in a fluid stream. A cyclone separator includes an assembly for separately discharging both constituents through the same end of the separator housing. A rotary separator includes a rotary housing having a baffle disposed therein for minimizing the differential rotational velocities of the constituents in the housing, thereby decreasing turbulence, and increasing efficiency. The intensity of the centrifugal force and the time which the constituents reside within the housing can be independently controlled to improve efficiency of separation.

  15. A Novel Biological Role of α-Mangostin in Modulating Inflammatory Response Through the Activation of SIRT-1 Signaling Pathway.

    PubMed

    Franceschelli, Sara; Pesce, Mirko; Ferrone, Alessio; Patruno, Antonia; Pasqualone, Livia; Carlucci, Giuseppe; Ferrone, Vincenzo; Carlucci, Maura; de Lutiis, Maria Anna; Grilli, Alfredo; Felaco, Mario; Speranza, Lorenza

    2016-11-01

    Several studies have shown that xanthones obtained from Garcinia Mangostana (GM) have remarkable biological activities. α-mangostin (α-MG) is the main constituent of the fruit hull of the GM. Several findings have suggested that SIRT-1, a nuclear histone deacetylase, could influence cellular function by the inhibition of NF-kB signaling. ROS can inhibit SIRT-1 activity by initiating oxidative modifications on its cysteine residues, and suppression of SIRT-1 enhances the NF-κB signaling resulting in inflammatory responses. The goals of the present study were to evaluate the quantity of α-MG in the methanolic extract of GM (Vithagroup Spa) and to investigate the activity of this xanthone in U937 cell line and in human monocytes from responsive to inflammatory insult analyzing the possible changes on the activation of SIRT-1 protein via NF-Kb. Cells were treated with the methanolic extract of GM and/or LPS. The chromatographic separation of α-MG was performed by an HPLC analysis. EX 527, a specific SIRT-1 inhibitor, was used to determine if SIRT-1/NfkB signaling pathway might be involved in α-MG action on cells. Our results show that α-MG inhibits p65 acetylation and down-regulates the pro-inflammatory gene products as COX-2, iNOS via SIRT-1 activation. Cells treated with EX 527 showed an up-regulation of NFkB acetylation and an over expression of inducible enzymes and their product of catalysis (NO and PGE2). These results suggest that α-MG may be useful for the development of alternative pharmacological strategies aimed at reducing the inflammatory process. J. Cell. Physiol. 231: 2439-2451, 2016. © 2016 Wiley Periodicals, Inc. PMID:26895796

  16. Dermatophytes Activate Skin Keratinocytes via Mitogen-Activated Protein Kinase Signaling and Induce Immune Responses

    PubMed Central

    Achterman, Rebecca R.; Moyes, David L.; Thavaraj, Selvam; Smith, Adam R.; Blair, Kris M.

    2015-01-01

    Dermatophytes cause superficial and cutaneous fungal infections in immunocompetent hosts and invasive disease in immunocompromised hosts. However, the host mechanisms that regulate innate immune responses against these fungi are largely unknown. Here, we utilized commercially available epidermal tissues and primary keratinocytes to assess (i) damage induction by anthropophilic, geophilic, and zoophilic dermatophyte strains and (ii) the keratinocyte signaling pathways, transcription factors, and proinflammatory responses induced by a representative dermatophyte, Trichophyton equinum. Initially, five dermatophyte species were tested for their ability to invade, cause tissue damage, and induce cytokines, with Microsporum gypseum inducing the greatest level of damage and cytokine release. Using T. equinum as a representative dermatophyte, we found that the mitogen-activated protein kinase (MAPK) pathways were predominantly affected, with increased levels of phospho-p38 and phospho-Jun N-terminal protein kinase (JNK) but decreased levels of phospho-extracellular signal-regulated kinases 1 and 2 (ERK1/2). Notably, the NF-κB and PI3K pathways were largely unaffected. T. equinum also significantly increased expression of the AP-1-associated transcription factor, c-Fos, and the MAPK regulatory phosphatase, MKP1. Importantly, the ability of T. equinum to invade, cause tissue damage, activate signaling and transcription factors, and induce proinflammatory responses correlated with germination, indicating that germination may be important for dermatophyte virulence and host immune activation. PMID:25667269

  17. Activated human neutrophil response to perfluorocarbon nanobubbles: oxygen-dependent and -independent cytotoxic responses.

    PubMed

    Hwang, Tsong-Long; Fang, Chia-Lang; Al-Suwayeh, Saleh A; Yang, Li-Jia; Fang, Jia-You

    2011-06-10

    Nanobubbles, a type of nanoparticles with acoustically active properties, are being utilized as diagnostic and therapeutic nanoparticles to better understand, detect, and treat human diseases. The objective of this work was to prepare different nanobubble formulations and investigate their physicochemical characteristics and toxic responses to N-formyl-methionyl-leucyl-phenylalanine (fMLP)-activated human neutrophils. The nanobubbles were prepared using perfluoropentane and coconut oil as the respective core and shell, with soybean phosphatidylcholine (SPC) and/or cationic surfactants as the interfacial layers. The cytotoxic effect of the nanobubbles on neutrophils was determined by extracellular O₂(.)⁻ release, intracellular reactive oxygen species (ROS), lactate dehydrogenase (LDH), and elastase release. Particle sizes of the nanobubbles with different percentages of perfluorocarbon, oil, and surfactants in ranged 186-432 nm. The nanobubbles were demonstrated to inhibit the generation of superoxide and intracellular ROS. The cytotoxicity of nanobubbles may be mainly associated with membrane damage, as indicated by the high LDH leakage. Systems with Forestall (FE), a cationic surfactant, or higher SPC contents exhibited the greatest LDH release by 3-fold compared to the control. The further addition of an oil component reduced the cytotoxicity induced by the nanobubbles. Exposure to most of the nanobubble formulations upregulated elastase release by activated neutrophils. Contrary to this result, stearylamine (SA)-containing systems slightly but significantly suppressed elastase release. FE and SA in a free form caused stronger responses by neutrophils than when they were incorporated into nanobubbles. In summary, exposure to nanobubbles resulted in a formulation-dependent toxicity toward human neutrophils that was associated with both oxygen-dependent and -independent pathways. Clinicians should therefore exercise