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Sample records for antidiabetic compound isolated

  1. Antidiabetic Effect of Oral Borapetol B Compound, Isolated from the Plant Tinospora crispa, by Stimulating Insulin Release.

    PubMed

    Lokman, Faradianna E; Gu, Harvest F; Wan Mohamud, Wan Nazaimoon; Yusoff, Mashitah M; Chia, Keh Leong; Ostenson, Claes-Göran

    2013-01-01

    Aims. To evaluate the antidiabetic properties of borapetol B known as compound 1 (C1) isolated from Tinospora crispa in normoglycemic control Wistar (W) and spontaneously type 2 diabetic Goto-Kakizaki (GK) rats. Methods. The effect of C1 on blood glucose and plasma insulin was assessed by an oral glucose tolerance test. The effect of C1 on insulin secretion was assessed by batch incubation and perifusion experiments using isolated pancreatic islets. Results. An acute oral administration of C1 improved blood glucose levels in treated versus placebo groups with areas under glucose curves 0-120 min being 72 ± 17 versus 344 ± 10 mmol/L (P < 0.001) and 492 ± 63 versus 862 ± 55 mmol/L (P < 0.01) in W and GK rats, respectively. Plasma insulin levels were increased by 2-fold in treated W and GK rats versus placebo group at 30 min (P < 0.05). C1 dose-dependently increased insulin secretion from W and GK isolated islets at 3.3 mM and 16.7 mM glucose. The perifusions of isolated islets indicated that C1 did not cause leakage of insulin by damaging islet beta cells (P < 0.001). Conclusion. This study provides evidence that borapetol B (C1) has antidiabetic properties mainly due to its stimulation of insulin release. PMID:24319481

  2. Anti-diabetic activity of active fractions of Stereospermum tetragonum DC and isolation of active principles

    PubMed Central

    Bino Kingsley, Renjit; Mishra, Manisha; Brindha, Pemaiah; Subramoniam, Appian

    2013-01-01

    Objectives To identify the active principles, determine the anti-diabetes activity of fraction of Stereospermum tetragonum root. Materials and Methods The efficacy was evaluated in streptozotocin induced type 2 diabetic rats and the anti-hyperglycemic activity was studied by glucose tolerance test. The major active compounds were isolated by solvent fractionation and chromatographic techniques and characterized with spectral data. Results The active fraction of S. tetragonum showed presence of anti-diabetes mellitus activity in type-2 diabetic rats. It did not significantly influence insulin release from cultured islets. Two active principles (active at 2 mg/kg dose) were isolated and characterized with spectral data. One of them was identified as an iridoid type glycoside and the other one was a lapachol like compound (derivative of naphthoquinone). Conclusions Two active principles from the anti-diabetes fraction of S. tetragonum root were isolated and identified as an iridoid glycoside and a naphthoquinone derivative. PMID:24023445

  3. Fermentation, Isolation, Structure, and antidiabetic activity of NFAT-133 produced by Streptomyces strain PM0324667

    PubMed Central

    2011-01-01

    Type-2 diabetes is mediated by defects in either insulin secretion or insulin action. In an effort to identify extracts that may stimulate glucose uptake, similar to insulin, a high throughput-screening assay for measuring glucose uptake in skeletal muscle cells was established. During the screening studies to discover novel antidiabetic compounds from microbial resources a Streptomyces strain PM0324667 (MTCC 5543, the Strain accession number at Institute of Microbial Technology, Chandigarh, India), an isolate from arid soil was identified which expressed a secondary metabolite that induced glucose uptake in L6 skeletal muscle cells. By employing bioactivity guided fractionation techniques, a tri-substituted simple aromatic compound with anti-diabetic potential was isolated. It was characterized based on MS and 2D NMR spectral data and identified as NFAT-133 which is a known immunosuppressive agent that inhibits NFAT-dependent transcription in vitro. Our investigations revealed the antidiabetic potential of NFAT-133. The compound induced glucose uptake in differentiated L6 myotubes with an EC50 of 6.3 ± 1.8 μM without activating the peroxisome proliferator-activated receptor-γ. Further, NFAT-133 was also efficacious in vivo in diabetic animals and reduced systemic glucose levels. Thus it is a potential lead compound which can be considered for development as a therapeutic for the treatment of type-2 diabetes. We have reported herewith the isolation of the producer microbe, fermentation, purification, in vitro, and in vivo antidiabetic activity of the compound. PMID:22104600

  4. Fermentation, Isolation, Structure, and antidiabetic activity of NFAT-133 produced by Streptomyces strain PM0324667.

    PubMed

    Kulkarni-Almeida, Asha A; Brahma, Manoja K; Padmanabhan, Prabhu; Mishra, Prabhu D; Parab, Rajashri R; Gaikwad, Nitin V; Thakkar, Chandni S; Tokdar, Pradipta; Ranadive, Prafull V; Nair, Amrutha S; Damre, Anagha A; Bahirat, Umakant A; Deshmukh, Nitin J; Doshi, Lalit S; Dixit, Amol V; George, Saji D; Vishwakarma, Ram A; Nemmani, Kumar Vs; Mahajan, Girish B

    2011-11-21

    Type-2 diabetes is mediated by defects in either insulin secretion or insulin action. In an effort to identify extracts that may stimulate glucose uptake, similar to insulin, a high throughput-screening assay for measuring glucose uptake in skeletal muscle cells was established. During the screening studies to discover novel antidiabetic compounds from microbial resources a Streptomyces strain PM0324667 (MTCC 5543, the Strain accession number at Institute of Microbial Technology, Chandigarh, India), an isolate from arid soil was identified which expressed a secondary metabolite that induced glucose uptake in L6 skeletal muscle cells. By employing bioactivity guided fractionation techniques, a tri-substituted simple aromatic compound with anti-diabetic potential was isolated. It was characterized based on MS and 2D NMR spectral data and identified as NFAT-133 which is a known immunosuppressive agent that inhibits NFAT-dependent transcription in vitro. Our investigations revealed the antidiabetic potential of NFAT-133. The compound induced glucose uptake in differentiated L6 myotubes with an EC50 of 6.3 ± 1.8 μM without activating the peroxisome proliferator-activated receptor-γ. Further, NFAT-133 was also efficacious in vivo in diabetic animals and reduced systemic glucose levels. Thus it is a potential lead compound which can be considered for development as a therapeutic for the treatment of type-2 diabetes. We have reported herewith the isolation of the producer microbe, fermentation, purification, in vitro, and in vivo antidiabetic activity of the compound.

  5. Antidiabetic compounds from Sarracenia purpurea used traditionally by the Eeyou Istchee Cree First Nation.

    PubMed

    Muhammad, Asim; Guerrero-Analco, Jose A; Martineau, Louis C; Musallam, Lina; Madiraju, Padma; Nachar, Abir; Saleem, Ammar; Haddad, Pierre S; Arnason, John T

    2012-07-27

    Through ethnobotanical surveys, the CIHR Team in Aboriginal Antidiabetic Medicines identified 17 boreal forest plants stemming from the pharmacopeia of the Cree First Nations of Eeyou Istchee (James Bay region of Northern Quebec) that were used traditionally against diabetes symptoms. The leaves of Sarracenia purpurea (pitcher plant), one of the identified Cree plants, exhibited marked antidiabetic activity in vitro by stimulating glucose uptake in C2C12 mouse muscle cells and by reducing glucose production in H4IIE rat liver cells. Fractionation guided by glucose uptake in C2C12 cells resulted in the isolation of 11 compounds from this plant extract, including a new phenolic glycoside, flavonoid glycosides, and iridoids. Compounds 6 (isorhamnetin-3-O-glucoside), 8 [kaempferol-3-O-(6″-caffeoylglucoside], and 11 (quercetin-3-O-galactoside) potentiated glucose uptake in vitro, which suggests they represent active principles of S. purpurea (EC(50) values of 18.5, 13.8, and 60.5 μM, respectively). This is the first report of potentiation of glucose uptake by compounds 6 and 8, while compound 11 (isolated from Vaccinium vitis) was previously shown to enhance glucose uptake. Treatment of H4IIE liver cells with the new compound 1, 6'-O-caffeoylgoodyeroside, decreased hepatic glucose production by reducing glucose-6-phosphatase enzymatic activity (IC(50) = 13.6 μM), which would contribute to lowering glycemia and to the antidiabetic potential of S. purpurea. PMID:22738356

  6. Antidiabetic compounds from Sarracenia purpurea used traditionally by the Eeyou Istchee Cree First Nation.

    PubMed

    Muhammad, Asim; Guerrero-Analco, Jose A; Martineau, Louis C; Musallam, Lina; Madiraju, Padma; Nachar, Abir; Saleem, Ammar; Haddad, Pierre S; Arnason, John T

    2012-07-27

    Through ethnobotanical surveys, the CIHR Team in Aboriginal Antidiabetic Medicines identified 17 boreal forest plants stemming from the pharmacopeia of the Cree First Nations of Eeyou Istchee (James Bay region of Northern Quebec) that were used traditionally against diabetes symptoms. The leaves of Sarracenia purpurea (pitcher plant), one of the identified Cree plants, exhibited marked antidiabetic activity in vitro by stimulating glucose uptake in C2C12 mouse muscle cells and by reducing glucose production in H4IIE rat liver cells. Fractionation guided by glucose uptake in C2C12 cells resulted in the isolation of 11 compounds from this plant extract, including a new phenolic glycoside, flavonoid glycosides, and iridoids. Compounds 6 (isorhamnetin-3-O-glucoside), 8 [kaempferol-3-O-(6″-caffeoylglucoside], and 11 (quercetin-3-O-galactoside) potentiated glucose uptake in vitro, which suggests they represent active principles of S. purpurea (EC(50) values of 18.5, 13.8, and 60.5 μM, respectively). This is the first report of potentiation of glucose uptake by compounds 6 and 8, while compound 11 (isolated from Vaccinium vitis) was previously shown to enhance glucose uptake. Treatment of H4IIE liver cells with the new compound 1, 6'-O-caffeoylgoodyeroside, decreased hepatic glucose production by reducing glucose-6-phosphatase enzymatic activity (IC(50) = 13.6 μM), which would contribute to lowering glycemia and to the antidiabetic potential of S. purpurea.

  7. Isolation of Antidiabetic Principle from Fruit Rinds of Punica granatum

    PubMed Central

    Jain, Vishal; Viswanatha, G. L.; Manohar, D.; Shivaprasad, H. N.

    2012-01-01

    Present study was aimed to isolate and evaluate the antidiabetic activity of phytoconstituents from fruit rinds of Punica granatum. With the above objectives Valoneic acid dilactone (VAD) was isolated from methanolic fruit rind extracts of Punica granatum (MEPG) and confirmed by 1H-NMR, 13C-NMR, and mass spectral data. Antidiabetic activity was evaluated by Aldose reductase, α-amylase and PTP1B inhibition assays in in vitro and Alloxan-induced diabetes in rats was used as an in vivo model. In bioactivity studies, MEPG and VAD have showed potent antidiabetic activity in α-amylase, aldose reductase, and PTP1B inhibition assays with IC50 values of 1.02, 2.050, 26.25 μg/mL and 0.284, 0.788, 12.41 μg/mL, respectively. Furthermore, in alloxan-induced diabetes model MEPG (200 and 400 mg/kg, p.o.) and VAD (10, 25, and 50 mg/kg, p.o.) have showed significant and dose dependent antidiabetic activity by maintaining the blood glucose levels within the normal limits. Inline with the biochemical findings histopathology of MEPG (200 and 400 mg/kg, p.o.), VAD (10, 25, and 50 mg/kg, p.o.), and glibenclamide (10 mg/kg, p.o.) treated animals showed significant protection against alloxan-induced pancreatic tissue damage. These findings suggest that MEPG and VAD possess significant antidiabetic activity in both in vitro and in vivo models. PMID:22919408

  8. Biguanide related compounds in traditional antidiabetic functional foods.

    PubMed

    Perla, Venu; Jayanty, Sastry S

    2013-06-01

    Biguanides such as metformin are widely used worldwide for the treatment of type-2 diabetes. The identification of guanidine and related compounds in French lilac plant (Galega officinalis L.) led to the development of biguanides. Despite of their plant origin, biguanides have not been reported in plants. The objective of this study was to quantify biguanide related compounds (BRCs) in experimentally or clinically substantiated antidiabetic functional plant foods and potatoes. The corrected results of the Voges-Proskauer (V-P) assay suggest that the highest amounts of BRCs are present in green curry leaves (Murraya koenigii (L.) Sprengel) followed by fenugreek seeds (Trigonella foenum-graecum L.), green bitter gourd (Momordica charantia Descourt.), and potato (Solanum tuberosum L.). Whereas, garlic (Allium sativum L.), and sweet potato (Ipomea batatas (L.) Lam.) contain negligible amounts of BRCs. In addition, the possible biosynthetic routes of biguanide in these plant foods are discussed.

  9. Biguanide related compounds in traditional antidiabetic functional foods.

    PubMed

    Perla, Venu; Jayanty, Sastry S

    2013-06-01

    Biguanides such as metformin are widely used worldwide for the treatment of type-2 diabetes. The identification of guanidine and related compounds in French lilac plant (Galega officinalis L.) led to the development of biguanides. Despite of their plant origin, biguanides have not been reported in plants. The objective of this study was to quantify biguanide related compounds (BRCs) in experimentally or clinically substantiated antidiabetic functional plant foods and potatoes. The corrected results of the Voges-Proskauer (V-P) assay suggest that the highest amounts of BRCs are present in green curry leaves (Murraya koenigii (L.) Sprengel) followed by fenugreek seeds (Trigonella foenum-graecum L.), green bitter gourd (Momordica charantia Descourt.), and potato (Solanum tuberosum L.). Whereas, garlic (Allium sativum L.), and sweet potato (Ipomea batatas (L.) Lam.) contain negligible amounts of BRCs. In addition, the possible biosynthetic routes of biguanide in these plant foods are discussed. PMID:23411283

  10. The Molecular Mechanisms and Rational Design of Anti-Diabetic Vanadium Compounds.

    PubMed

    Niu, Xia; Xiao, Ruyue; Wang, Na; Wang, Ziwei; Zhang, Yue; Xia, Qing; Yang, Xiaoda

    2016-01-01

    Vanadium compounds are promising anti-diabetic agents. Although BEOV was not able to succeed in phase II clinical trial, great progresses have been made in the past three decades on the discovery and development of anti-diabetic vanadium compounds. A vast of knowledge has been obtained on the molecular mechanisms of both the pharmacological and toxicological effects of vanadium complexes. It has been revealed that vanadium compounds exert insulin enhancement effects and cell protection via a multiple mechanism involving inhibition of PTP1B, activation of PPARs- AMPK signaling, regulation of unfolded protein responses (UPRs), and stimulation of antioxidant enzymes, while vanadium-induced oxidative stress and inflammatory response could primarily be attributed to vanadium toxicity. Based on the present results concerning the relationship between structures, biological activities and biochemical properties, the rationale for future design of anti-diabetic vanadium compounds has been discussed.

  11. Screening and design of anti-diabetic compounds sourced from the leaves of neem (Azadirachta indica).

    PubMed

    Jalil, Asma; Ashfaq, Usman Ali; Shahzadi, Samar; Rasul, Ijaz; Rehman, Shahid-Ur; Shah, Masaud; Javed, Muhammad Rizwan; Masoud, Muhammad Shareef

    2013-01-01

    Diabetes Mellitus is affecting people of all age groups worldwide. Many synthetic medicines available for type 2 diabetes mellitus in the market. However, there is a strong requirement for the development of better anti-diabetes compounds sourced especially from natural sources like medicinal plants. The extracts from the leaves of neem (Azadirachta indica) is traditionally known to have anti-diabetes properties. Therefore, there is an increased interest to identify potential compounds identified from neem leaf extracts showing predicted binding property with the known diabetes mellitus type 2 protein enzyme target phosphoenol-pyruvate carboxykinase(PEPCK). The structure data for compounds found in the leaf extract of neem was screened against PEPCK using molecular docking simulation and screening techniques. Results show that the compound 3-Deacetyl-3-cinnamoyl-azadirachtin possesses best binding properties with PEPCK. This observation finds application for further consideration in in vitro and in vivo validation. PMID:24497731

  12. Qualitative variation of anti-diabetic compounds in different tarragon (Artemisia dracunculus L.) cytotypes

    PubMed Central

    Eisenman, Sasha W.; Poulev, Alexander; Struwe, Lena; Raskin, Ilya; Ribnicky, David M.

    2011-01-01

    Ethanolic extracts of diploid Artemisia dracunculus L. (wild tarragon) from populations in the U.S., and polyploid tarragon from a variety of sources, were screened for the anti-diabetic compounds davidigenin; sakuranetin; 2′,4′-dihydroxy-4-methoxydihydrochalcone; 4,5-di-O-caffeoylquinic acid; 5-O-caffeoylquinic acid and 6-demethoxycapillarisin using LC-MS. Only decaploid plants contained all six target compounds and were the only plants that contained davidigenin and 2,4-dihydroxy-4-methoxydihydrochalcone. These results exhibit the importance of germplasm selection and provenance when studying plants for medicinal activity. Relying only on the “right species” for consistent medicinal activities may not be sufficient, as intraspecific variation may be highly significant. PMID:21798321

  13. Antidiabetic oils.

    PubMed

    Berraaouan, Ali; Abid, Sanae; Bnouham, Mohamed

    2013-11-01

    Many studies have demonstrated evidence of the health benefits of natural products. Plant extracts have been tested on a variety of physiological disorders, including diabetes mellitus. Studies have tested aqueous extracts, plant fractions extracts, families of active of compounds, and specific active compounds. In this review, we describe the antidiabetic effects of vegetable oils. Information was collected from ScienceDirect and PubMed databases using the following key words: Diabetes mellitus, Oils, Vegetable oils, Type 1 diabetes, type 2 diabetes, antidiabetic effect, antihyperglycemic, antidiabetic oil. We have compiled approximately ten vegetable oils with including experimental studies that have demonstrated benefits on diabetes mellitus. There are soybean, argan, olive, palm, walnut, black cumin, safflower, Colocynth, Black seed, Rice bran, Cinnamom, and Rocket oils. For each vegetable oil, we investigated on the plant's traditional uses, their pharmacological activities and their antidiabetic effects. It seems that many vegetable oils are really interesting and can be used in the improvement of human health, particularly, to prevent or to treat diabetes mellitus complications.

  14. In vivo potential antidiabetic activity of a novel zinc coordination compound based on 3-carboxy-pyrazole.

    PubMed

    López-Viseras, Marta E; Fernández, Belén; Hilfiker, Sabine; González, Cristina Sánchez; González, Juan Llopis; Calahorro, Antonio J; Colacio, Enrique; Rodríguez-Diéguez, Antonio

    2014-02-01

    A novel Zn mononuclear complex with 3-carboxy-pyrazole ligand has been prepared using conventional routes and characterized by X-ray diffraction. The structure consists of discrete neutral [Zn(C6H3N2O2)2(H2O)2] molecules held together by hydrogen interactions. This compound exhibits a potential in vivo antidiabetic activity and the in vitro toxicity can be considered negligible. PMID:24252384

  15. Mechanism of Antidiabetic Action of Compound GII Purified from Fenugreek (Trigonella foenum graecum) Seeds.

    PubMed

    Puri, D; Prabhu, K M; Dev, G; Agarwal, S; Murthy, P S

    2011-10-01

    To study the mechanism of action of water soluble compound GII purified from fenugreek (Trigonella foenum graecum) seeds which was shown earlier to have antidiabetic effect in the subdiabetic, moderately and severely diabetic rabbits. In rabbits (1-1.5 kg bw) diabetes was induced by intravenous injection of 80 mg/kg bw of alloxan. They were fed with GII at a dose of 50 mg/kg bw daily once in the morning for 15 days in the subdiabetic and moderately diabetic and 30 days in the severely diabetic rabbits. Serum total cholesterol (TC), triglycerides (TG), LDL + VLDL cholesterol [(LDL + VLDL)C], HDL cholesterol [(HDL)C], total tissue lipids, glycogen and enzymes of carbohydrate metabolism (glycolysis, gluconeogenesis, polyol pathway) hexokinase, glucokinase, pyruvate kinase, malic enzyme, glucose-6-phosphatase, glucose-6-phosphate dehydrogenase, aldose reductase and sorbitol dehydrogenase and antioxidant enzymes glutathione peroxidase, glutathione reductase and superoxide dismutase were estimated. Liver and kidney function parameters were also estimated. Treatment with GII for 15 days in the subdiabetic and moderately diabetic rabbits and for 30 days in the severely diabetic rabbits (i) decreased the elevated lipids TC, TG, (LDL + VLDL)C and increased the decreased (HDL)C, (ii) decreased the elevated liver and heart total lipids, TC and TG, (iii) increased the decreased liver and muscle glycogen, (iv) increased the decreased hexokinase, glucokinase, pyruvate kinase, malic enzyme, glucose-6-phosphate dehydrogenase, superoxide dismutase, glutathione peroxidase, (v) decreased the increased glucose-6-phosphatase, sorbitol dehydrogenase, aldose reductase. Results thus show that treatment with GII compound purified from fenugreek seeds for 15 days in the subdiabetic and moderately diabetic and 30 days in the severely diabetic rabbits corrects the altered serum lipids, tissue lipids, glycogen, enzymes of glycolysis, gluconeogenesis, glycogen metabolism, polyol

  16. Antidiabetic Effect of GII Compound Purified from Fenugreek (Trigonella foenum graecum Linn) Seeds in Diabetic Rabbits.

    PubMed

    Puri, D; Prabhu, K M; Murthy, P S

    2012-01-01

    Aim is to study the antidiabetic effect of a compound GII purified earlier from the water extract of fenugreek (Trigonella foenum graecum) seeds by Murthy and his colleagues (patented in India and USA) in diabetic rabbits. Diabetes was induced in rabbits by injecting 80 mg/kg bw of alloxan intravenously into rabiits. Rabbits were subdivided into subdiabetic [fasting blood sugar (FBG) up to 120 mg/dl with abnormal glucose tolerance in glucose tolerance test (GTT)], moderately diabetic (FBG below 250 mg/dl) and severely diabetic (FBG above 250 mg/dl). Blood glucose and glycosylated hemoglobin (HbA1C) were estimated by procedures in the kits of Stangen Immunodiagnostics, Mumbai using, respectively, glucose oxidase method and absorbance at 415 nm. Serum insulin was estimated by the ELISA method as described in the kit of Boehringer Mannheim Immunodiagnostics, Mumbai, India. GII was found to improve blood glucose utilization in GTT and reduced FBG and HbA1C. In the present communication detailed studies were carried out with GII in the subdiabetic, moderately diabetic and severely diabetic rabbits. GII at a dose of 50 mg/kg bw per day brought down the elevated FBG levels in the untreated subdiabetic (FBG 96.6 ± 7 mg/dl), moderately diabetic (150.1 ± 14 mg/dl) and severely diabetic rabbits (427 ± 46 mg/dl) to normal in 12, 15 and 28 days of treatment. It improved serum HbA1C and insulin levels also in these rabbits. Intermittent therapy once a week for 6 weeks with GII at the same dose brought down the FBG values to normal in the subdiabetic (FBG 96.0 ± 2 mg/dl) and in the moderately diabetic rabbits to 133.0 ± 12 mg/dl. After stopping therapy of the subdiabetic and moderately diabetic rabbits whose FBG values came to normal after treatment with GII 50 mg/kg bw, the values remained normal for 1 week and showed a tendency to increase only after 15 days. If these animal studies are applicable to humans these results indicate that a

  17. Interaction of Glucagon G-Protein Coupled Receptor with Known Natural Antidiabetic Compounds: Multiscoring In Silico Approach

    PubMed Central

    Baig, M. H.; Ahmad, K.; Hasan, Q.; Khan, M. K. A.; Rao, N. S.; Kamal, M. A.; Choi, I.

    2015-01-01

    Glucagon receptor (GCGR) is a secretin-like (class B) family of G-protein coupled receptors (GPCRs) in humans that plays an important role in elevating the glucose concentration in blood and has thus become one of the promising therapeutic targets for treatment of type 2 diabetes mellitus. GCGR based inhibitors for the treatment of type 2 diabetes are either glucagon neutralizers or small molecular antagonists. Management of diabetes without any side effects is still a challenge to the medical system, and the search for a new and effective natural GCGR antagonist is an important area for the treatment of type 2 diabetes. In the present study, a number of natural compounds containing antidiabetic properties were selected from the literature and their binding potential against GCGR was determined using molecular docking and other in silico approaches. Among all selected natural compounds, curcumin was found to be the most effective compound against GCGR followed by amorfrutin 1 and 4-hydroxyderricin. These compounds were rescored to confirm the accuracy of binding using another scoring function (x-score). The final conclusions were drawn based on the results obtained from the GOLD and x-score. Further experiments were conducted to identify the atomic level interactions of selected compounds with GCGR. PMID:26236379

  18. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States.

    PubMed

    Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

    2016-05-11

    Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high). The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production.

  19. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States

    PubMed Central

    Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

    2016-01-01

    Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high). The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production. PMID:27187352

  20. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States.

    PubMed

    Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

    2016-01-01

    Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high). The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production. PMID:27187352

  1. Target guided isolation, in-vitro antidiabetic, antioxidant activity and molecular docking studies of some flavonoids from Albizzia Lebbeck Benth. bark

    PubMed Central

    2014-01-01

    Background Albizzia Lebbeck Benth. is traditionally important plant and is reported to possess a variety of pharmacological actions. The present research exertion was undertaken to isolate and characterized the flavonoids from the extract of stem bark of Albizzia Lebbeck Benth. and to evaluate the efficacy of the isolated flavonoids on in-vitro models of type-II diabetes. Furthermore, the results of in-vitro experimentation inveterate by the molecular docking studies of the isolated flavonoids on α-glucosidase and α-amylase enzymes. Methods Isolation of the flavonoids from the methanolic extract of stem bark of A. Lebbeck Benth was executed by the Silica gel (Si) column chromatography to yield different fractions. These fractions were then subjected to purification to obtain three important flavonoids. The isolated flavonoids were then structurally elucidated with the assist of 1H-NMR, 13C-NMR, and Mass spectroscopy. In-vitro experimentation was performed with evaluation of α-glucosidase, α-amylase and DPPH inhibition capacity. Molecular docking study was performed with GLIDE docking software. Results Three flavonoids, (1) 5-deoxyflavone (geraldone), (2) luteolin and (3) Isookanin were isolated from the EtOAc fraction of the methanolic extract of Albizzia lebbeck Benth bark. (ALD). All the compounds revealed to inhibit the α-glucosidase and α-amylase enzymes in in-vitro investigation correlating to reduce the plasma glucose level. Molecular docking study radically corroborates the binding affinity and inhibition of α-glucosidase and α-amylase enzymes. Conclusion The present research exertion demonstrates the anti-diabetic and antioxidant activity of the important isolated flavonoids with inhibition of α-glucosidase, α-amylase and DPPH which is further supported by molecular docking analysis. PMID:24886138

  2. Quinoa seeds leach phytoecdysteroids and other compounds with anti-diabetic properties

    PubMed Central

    Graf, Brittany L.; Poulev, Alexander; Kuhn, Peter; Grace, Mary H.; Lila, Mary Ann; Raskin, Ilya

    2014-01-01

    Quinoa (Chenopodium quinoa Willd.) contains high levels of biologically active phytoecdysteroids, which have been implicated in plant defense from insects, and have shown a range of beneficial pharmacological effects in mammals. We demonstrated that the most prevalent phytoecdysteroid, 20-hydroxyecdysone (20HE), was secreted (leached) from intact quinoa seeds into water during the initial stages of seed germination. Leaching efficiency was optimized by ethanol concentration (70% ethanol), temperature (80°C), time (4 h), and solvent ratio (5 ml/g seed). When compared to extraction of macerated seeds, the leaching procedure released essentially all the 20HE available in the seeds (491 μg/g seed). The optimized quinoa leachate (QL), containing 0.86% 20HE, 1.00% total phytoecdysteroids, 2.59% flavonoid glycosides, 11.9% oil, and 20.4% protein, significantly lowered fasting blood glucose in obese, hyperglycemic mice. Leaching effectively releases and concentrates bioactive phytochemicals from quinoa seeds, providing an efficient means to produce a food-grade mixture that may be useful for anti-diabetic applications. PMID:24912714

  3. Quinoa seeds leach phytoecdysteroids and other compounds with anti-diabetic properties.

    PubMed

    Graf, Brittany L; Poulev, Alexander; Kuhn, Peter; Grace, Mary H; Lila, Mary Ann; Raskin, Ilya

    2014-11-15

    Quinoa (Chenopodium quinoa Willd.) contains high levels of biologically active phytoecdysteroids, which have been implicated in plant defense from insects, and have shown a range of beneficial pharmacological effects in mammals. We demonstrated that the most prevalent phytoecdysteroid, 20-hydroxyecdysone (20HE), was secreted (leached) from intact quinoa seeds into water during the initial stages of seed germination. Leaching efficiency was optimized by ethanol concentration (70% ethanol), temperature (80°C), time (4h), and solvent ratio (5 ml/g seed). When compared to extraction of macerated seeds, the leaching procedure released essentially all the 20HE available in the seeds (491 μg/g seed). The optimized quinoa leachate (QL), containing 0.86% 20HE, 1.00% total phytoecdysteroids, 2.59% flavonoid glycosides, 11.9% oil, and 20.4% protein, significantly lowered fasting blood glucose in obese, hyperglycemic mice. Leaching effectively releases and concentrates bioactive phytochemicals from quinoa seeds, providing an efficient means to produce a food-grade mixture that may be useful for anti-diabetic applications.

  4. An in silico study on antidiabetic activity of bioactive compounds in Euphorbia thymifolia Linn.

    PubMed

    Nguyen Vo, T Hoang; Tran, Ngan; Nguyen, Dat; Le, Ly

    2016-01-01

    Herbal medicines have become strongly preferred treatment to reduce the negative impacts of diabetes mellitus (DM) and its severe complications due to lesser side effects and low cost. Recently, strong anti-hyperglycemic effect of Euphorbia thymifolia Linn. (E. thymifolia) on mice models has reported but the action mechanism of its bioactive compounds has remained unknown. This study aimed to evaluate molecular interactions existing between various bioactive compounds in E. thymifolia and targeted proteins related to Type 2 DM. This process involved the molecular docking of 3D structures of those substances into 4 targeted proteins: 11-β hydroxysteroid dehydrogenase type 1, glutamine: fructose-6-phosphate amidotransferase, protein-tyrosine phosphatase 1B and mono-ADP-ribosyltransferase sirtuin-6. In the next step, LigandScout was applied to evaluate the bonds formed between 20 ligands and the binding sites of each targeted proteins. The results identified seven bioactive compounds with high binding affinity (<-8.0 kcal/mol) to all 4 targeted proteins including β-amyrine, taraxerol, 1-O-galloyl-β-d-glucose, corilagin, cosmosiin, quercetin-3-galactoside and quercitrin. The pharmacophore features were also explained in 2D figures which indicated hydrophobic interactions, hydrogen bond acceptors and hydrogen bond donors forming between carbonyl oxygen molecules of those ligands and active site residues of 4 targeted protein.Graphical abstract Euphorbia thymifolia Linn. is a small prostrate herbaceous annual weed that can positively impact on reducing hyperglycemic effect. In order to clearly understand about molecular level of the its bioactive compounds, in silico approach is performed. PMID:27588252

  5. Antidiabetic Agents.

    ERIC Educational Resources Information Center

    Plummer, Nancy; Michael, Nancy, Ed.

    This module on antidiabetic agents is intended for use in inservice or continuing education programs for persons who administer medications in long-term care facilities. Instructor information, including teaching suggestions, and a listing of recommended audiovisual materials and their sources appear first. The module goal and objectives are then…

  6. Isolation and characterization of a hyperbranched proteoglycan from Ganoderma lucidum for anti-diabetes.

    PubMed

    Pan, Deng; Wang, Linqiang; Chen, Congheng; Hu, Bingwen; Zhou, Ping

    2015-03-01

    Presently, an efficient protein tyrosine phosphatase 1B (PTP1B) inhibitor, named FYGL-n, was isolated from Ganoderma Lucidum and characterized for its structure and bioactivity. Structure and chain conformation of FYGL-n based on both chemical and spectroscopic analysis showed that FYGL-n was a hyperbranched heteropolysaccharide bonded with protein via both serine and threonine residues by O-type glycoside, and showed a sphere observed by AFM. Specifically, monosaccharide composition indicated that FYGL-n consisted of D-arabinose, D-galactose, L-rhamnose and D-glucose in a mole ratio of 0.08:0.21:0.24:0.47, with a molecular mass of 72.9 kDa. The analysis of amino acids in FYGL-n indicated that there were 16 common amino acids, among which aspartic acid, glycine, serine, alanine, glutamic acid and threonine were the dominant components. Also it was demonstrated that FYGL-n could inhibit the PTP1B activity on a competitive mechanism in vitro.

  7. Marine pharmacology in 2009-2011: marine compounds with antibacterial, antidiabetic, antifungal, anti-inflammatory, antiprotozoal, antituberculosis, and antiviral activities; affecting the immune and nervous systems, and other miscellaneous mechanisms of action.

    PubMed

    Mayer, Alejandro M S; Rodríguez, Abimael D; Taglialatela-Scafati, Orazio; Fusetani, Nobuhiro

    2013-07-16

    The peer-reviewed marine pharmacology literature from 2009 to 2011 is presented in this review, following the format used in the 1998-2008 reviews of this series. The pharmacology of structurally-characterized compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, antifungal, antiprotozoal, antituberculosis, and antiviral pharmacological activities were reported for 102 marine natural products. Additionally, 60 marine compounds were observed to affect the immune and nervous system as well as possess antidiabetic and anti-inflammatory effects. Finally, 68 marine metabolites were shown to interact with a variety of receptors and molecular targets, and thus will probably contribute to multiple pharmacological classes upon further mechanism of action studies. Marine pharmacology during 2009-2011 remained a global enterprise, with researchers from 35 countries, and the United States, contributing to the preclinical pharmacology of 262 marine compounds which are part of the preclinical pharmaceutical pipeline. Continued pharmacological research with marine natural products will contribute to enhance the marine pharmaceutical clinical pipeline, which in 2013 consisted of 17 marine natural products, analogs or derivatives targeting a limited number of disease categories.

  8. Marine Pharmacology in 2009–2011: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti-Inflammatory, Antiprotozoal, Antituberculosis, and Antiviral Activities; Affecting the Immune and Nervous Systems, and other Miscellaneous Mechanisms of Action †

    PubMed Central

    Mayer, Alejandro M. S.; Rodríguez, Abimael D.; Taglialatela-Scafati, Orazio; Fusetani, Nobuhiro

    2013-01-01

    The peer-reviewed marine pharmacology literature from 2009 to 2011 is presented in this review, following the format used in the 1998–2008 reviews of this series. The pharmacology of structurally-characterized compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, antifungal, antiprotozoal, antituberculosis, and antiviral pharmacological activities were reported for 102 marine natural products. Additionally, 60 marine compounds were observed to affect the immune and nervous system as well as possess antidiabetic and anti-inflammatory effects. Finally, 68 marine metabolites were shown to interact with a variety of receptors and molecular targets, and thus will probably contribute to multiple pharmacological classes upon further mechanism of action studies. Marine pharmacology during 2009–2011 remained a global enterprise, with researchers from 35 countries, and the United States, contributing to the preclinical pharmacology of 262 marine compounds which are part of the preclinical pharmaceutical pipeline. Continued pharmacological research with marine natural products will contribute to enhance the marine pharmaceutical clinical pipeline, which in 2013 consisted of 17 marine natural products, analogs or derivatives targeting a limited number of disease categories. PMID:23880931

  9. Anti-diabetic property of Tinospora cordifolia and its active compound is mediated through the expression of Glut-4 in L6 myotubes.

    PubMed

    Sangeetha, M K; Priya, C D Mohana; Vasanthi, Hannah R

    2013-02-15

    Tinospora cordifolia is a well reported plant possessing numerous medicinal values including anti-diabetic property. Aim of the present study is to study the mechanism of action of Tinospora cordifolia and its active compound in differentiated myocytes, L6 cells. Key marker of diabetes in cells is the insulin dependent glucose transporter-4 (Glut-4) which also responds to exogenous chemicals, and is over expressed up to 5- and 4-fold, by Tinospora cordifolia and palmatine, respectively. Next to Glut-4, the predominant protein influencing glucose metabolism is PPARα and γ whose expressions were also positively modulated. Further, the inhibitors of insulin pathway prevented glucose uptake mediated by Tinospora cordifolia and palmatine which shows that the activity is majorly mediated through insulin pathway. PMID:23290487

  10. Chemical compounds isolated from Talinum triangulare (Portulacaceae).

    PubMed

    de Oliveira Amorim, Ana Paula; de Carvalho, Almir Ribeiro; Lopes, Norberto Peporine; Castro, Rosane Nora; de Oliveira, Marcia Cristina Campos; de Carvalho, Mário Geraldo

    2014-10-01

    This first phytochemical study of Talinum triangulare Leach (Portulacaceae), also known as 'cariru', which is a commonly consumed food in Northern Brazil, allowed the isolation and structural determination of four new compounds: one acrylamide, 3-N-(acryloyl, N-pentadecanoyl) propanoic acid (5), and three new phaeophytins named (15(1)S, 17R, 18R)-Ficuschlorin D acid (3(1),3(2)-didehydro-7-oxo-17(3)-O-phytyl-rhodochlorin-15-acetic acid), (13), Talichorin A (17R, 18R)-phaeophytin b-15(1)-hidroxy, 15(2),15(3)-acetyl-13(1)-carboxilic acid (14), and (15(1)S, 17R, 18R)-phaeophytin b peroxylactone or (15(1)S, 17R, 18R)-hydroperoxy-ficuschlorin D (16), together with twelve known compounds, including four phaeophytins (11,12, 15 and 17). The structures of the compounds were established on the basis of 1D and 2D NMR, IR, HRESI-MS spectra, including GC-MS, and HPLC-UV analysis, as well as comparisons with the literature data. The CD spectra data analysis were used to define the absolute configuration of phaeophytins 12 (13(2)R, 17R, 18R)-13(2)-hydroxyphaeophytin a, 13 and 16, 15 (15(1)S, 17R, 18R)-3(1),3(2)-didehydro-15(1)-hydroxyrhodochlorin-15-acetic acid δ-lactone-15(2)-methyl-17(3)-phytyl ester and 17 (17R, 18R)-purpurin 18-phytyl ester. PMID:24799228

  11. Bioactivity-guided Isolation of antiosteoporotic compounds from Ligustrum lucidum.

    PubMed

    Chen, Qianfeng; Yang, Lijuan; Zhang, Guolin; Wang, Fei

    2013-07-01

    The fruits of Ligustrum lucidum (FLL) has long been used for the treatment of osteoporosis in China, but the antiosteoporotic compounds in FLL are still poorly understood. In this study, the alkaline phosphatase (ALP) activity-guided isolation of osteogenic components from FLL was carried out by using osteoblast-like UMR-106 cells. Eight compounds, namely tyrosol (1), tyrosyl acetate (2), hydroxytyrosol (3), salidroside (4), oleoside dimethyl ester (5), oleoside-7-ethyl-11-methyl ester (6), nuzhenide (7), and G13 (8), were isolated and identified. Further study showed that compounds 3, 4, 7, and 8 increased ALP activity in UMR-106 cells. Compounds 5, 6, and 7 promoted the proliferation of UMR-106 cells. The aqueous extract of FLL-activated ERα/β-mediated gene transcription, whereas the isolated compounds were inactive. All eight isolated compounds also exhibited antioxidative activity, with compounds 1, 2, and 3 being the most potent. These results indicate that the antiosteoporotic effect of FLL is derived from different compounds together with different mechanisms such as ER-dependent or independent pathways and antioxidative effects. Salidroside (4) and nuzhenide (7) warrant further investigation as new pharmaceutical tools for the prevention and treatment of osteoporosis. PMID:22893624

  12. 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

  13. 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

  14. Antidiabetic and antioxidant effects and phytochemicals of mulberry fruit (Morus alba L.) polyphenol enhanced extract.

    PubMed

    Wang, Yihai; Xiang, Limin; Wang, Chunhua; Tang, Chao; He, Xiangjiu

    2013-01-01

    The antidiabetic and antioxidant activities of the ethyl acetate-soluble extract (MFE) of mulberry fruit (Morus alba L.) were investigated. In vitro, MFE showed potent α-glucosidase inhibitory activity and radical-scavenging activities against DPPH and superoxide anion radicals. In vivo, MFE could significantly decrease fasting blood glucose (FBG) and glycosylated serum protein (GSP), and increase antioxidant enzymatic activities (SOD, CAT, GSH-Px) in streptozotocin (STZ)-induced diabetic mice. Bioactivity-guided fractionation of the MFE led to the isolation of 25 phenolic compounds, and their structures were identified on the basis of MS and NMR data. All the 25 compounds were isolated from mulberry fruit for the first time. Also, the α-glucosidase inhibitory activity and antioxidant activity of the phenolics were evaluated. Potent α-glucosidase inhibitory and radical-scavenging activities of these phenolics suggested that they may be partially responsible for the antidiabetic and antioxidant activities of mulberry fruit.

  15. Antidiabetic and Antioxidant Effects and Phytochemicals of Mulberry Fruit (Morus alba L.) Polyphenol Enhanced Extract

    PubMed Central

    Wang, Yihai; Xiang, Limin; Wang, Chunhua; Tang, Chao; He, Xiangjiu

    2013-01-01

    The antidiabetic and antioxidant activities of the ethyl acetate-soluble extract (MFE) of mulberry fruit (Morus alba L.) were investigated. In vitro, MFE showed potent α-glucosidase inhibitory activity and radical-scavenging activities against DPPH and superoxide anion radicals. In vivo, MFE could significantly decrease fasting blood glucose (FBG) and glycosylated serum protein (GSP), and increase antioxidant enzymatic activities (SOD, CAT, GSH-Px) in streptozotocin (STZ)-induced diabetic mice. Bioactivity-guided fractionation of the MFE led to the isolation of 25 phenolic compounds, and their structures were identified on the basis of MS and NMR data. All the 25 compounds were isolated from mulberry fruit for the first time. Also, the α-glucosidase inhibitory activity and antioxidant activity of the phenolics were evaluated. Potent α-glucosidase inhibitory and radical-scavenging activities of these phenolics suggested that they may be partially responsible for the antidiabetic and antioxidant activities of mulberry fruit. PMID:23936259

  16. Bioassay directed isolation and biological evaluation of compounds isolated from Rubus fairholmianus Gard.

    PubMed

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

    2014-01-01

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

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

    PubMed Central

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

    2014-01-01

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

  18. Isolation of an iron-binding compound from Pseudomonas aeruginosa.

    PubMed Central

    Cox, C D; Graham, R

    1979-01-01

    An iron-binding compound was isolated from ethyl acetate extracts of culture supernatant fluids of Pseudomonas aeruginosa and was purified by successive paper and thin-layer chromatographic procedures. The purified compound was characterized by UV, visible, infrared, and fluorescence spectroscopy. The compound possesses phenolic characteristics, with little or no similarity to dihydroxybenzoates and no indication of a hydroxamate group. P. aeruginosa synthesized the compound during active growth in culture media containing less than 5 X 10(-6) M added FeCl3. When added to iron-poor cultures of P. aeruginosa, the compound promoted the growth of the bacterium and also reversed growth inhibition by the iron chelator ethylenediamine-di-(o-hydroxyphenylacetic acid). PMID:104968

  19. In vivo anti-diabetic, antioxidant and molecular docking studies of 1, 2, 8-trihydroxy-6-methoxy xanthone and 1, 2-dihydroxy-6-methoxyxanthone-8-O-β-D-xylopyranosyl isolated from Swertia corymbosa.

    PubMed

    Mahendran, G; Manoj, M; Murugesh, E; Sathish Kumar, R; Shanmughavel, P; Rajendra Prasad, K J; Narmatha Bai, V

    2014-09-25

    1, 2, 8-trihydroxy-6-methoxy xanthone (1) and 1, 2- dihydroxy-6-methoxyxanthone-8-O-β-d-xylopyranosyl (2) are the main constituents of petroleum ether and ethyl acetate extracts from Swertia corymbosa (Gentinaceae), a medicinal plant used in Indian traditional system for the treatment of diabetes. The present study was designed to examine the antihypoglycemic, antihyperlipidemic and antioxidant effect of compounds 1 and 2 in streptozotocin (STZ) induced diabetic rats. Diabetes was induced in male Wistar rats by a single intraperitoneal injection of STZ (60 mg/kg b.w.). The isolated compounds 1 and 2 at a dose of 50 mg/kg b.w., produced the maximum fall of 83% in the blood glucose level in the diabetic rats after 3h of the treatment. The administration of 1 and 2 (50 mg/kgb.w.) daily for 28 days in STZ induced diabetic rats, resulted in a significant decrease in blood glucose, glycosylated hemoglobin, SGOT, SGPT, ALP serum urea and creatinine with significant rise in plasma insulin level. Test compounds 1 and 2 showed antihyperlipidemic activities as evidenced by significant decrease in serum TC, TG, LDL-C, VLDL-C levels coupled together with elevation of HDL-C level in diabetic treated rats when compared to diabetic untreated rats, indicate the protective role against liver and kidney damage. The results of histopathology also showed 1 and 2 protected tissues (pancreas, liver and kidney) against peroxidation damage and maintained tissue integrity. Further, the molecular interaction study of the ligands 1, 2 and glibenclamide with various diabetes mellitus related protein targets like glucokinase (PDB ID: 1V4S), fructose-1, 6-bisphosphatase 1 (PDB ID: 2JJK) 11-β-hydroxysteroid dehydrogenase (PDB ID: 2BEL) and modeled protein sulfonylurea receptor 1 (SUR1) showed that ligand 1 and 2 possess binding affinity with all protein targets except for 2BEL target protein for which ligand 1 has no interaction. The ligand pose with 2BEL and SUR1 protein target of ligand 2

  20. Red carpeting the newer antidiabetics

    PubMed Central

    Gude, Dilip

    2012-01-01

    The rapidly increasing prevalence of diabetes on a global scale beseeches an urgent need for newer and better treatment options. Our better understanding of the pathophysiology of diabetes has enabled a continual churn out of newer antidiabetic agents with varying modes of action. Sodium-Glucose Transport Proteins-2 inhibitors, dipeptidyl peptidase IV inhibitors, glucagon-like peptide analogues, glucokinase activators, dual peroxisome proliferator-activated receptor agonists, monoclonal antibodies, and dopamine-2 receptor agonists either as monotherapy or combination therapy with the existing oral hypoglycemic agents compound our fight against diabetes. A review of the newer drugs targeting various aspects in the management of diabetes is presented. PMID:22629086

  1. Isolation of a New Homomonoterpene from Madhuca pasquieri and Effect of Isolated Compounds on NO Production.

    PubMed

    Hoang, Le Son; Tran, Manh Hung; Nguyen, Van Thu; Ngo, Quynh Mai Thi; Lee, Joo-Sang; Rho, Seong-Soo; Kim, Jeong Ah; Lee, Jeong-Hyung; Woo, Mi Hee; Min, Byung Sun

    2016-06-01

    A new homomonoterpene, 1,3,3-trimethyl-7-oxabicyclo[3.1.1]hexa-9-en-10-oic acid, named madhusic acid A (1), together with ten known compounds (2-11) were isolated from the methanolic extract of the dried leaves of Madhuca pasquieri (Dubard) H. J. Lam. The structure of the new compound was elucidated on the basis of 1D, 2D NMR (COSY, HMQC, and HMBC) and mass spectral analyses. We examined the effects of the isolated compounds against LPS-induced NO production in macrophage RAW264.7 cells and compound 2 showed effective activity with an IC50 value of 14.5 μM. PMID:27534103

  2. Bioactive sesquiterpene lactones and other compounds isolated from Vernonia cinerea

    PubMed Central

    Youn, Ui Joung; Miklossy, Gabriella; Chai, Xingyun; Wongwiwatthananukit, Supakit; Toyama, Onoomar; Songsak, Thanapat; Turkson, James; Chang, Leng Chee

    2014-01-01

    Four new sesquiterpene lactones, 8α-(2′Z-tigloyloxy)-hirsutinolide (1), 8α-(2′Z-tigloyloxy)-hirsutinolide-13-O-acetate (2), 8α-(4-hydroxytigloyloxy)-hirsutinolide (3), and 8α-hydroxy-13-O-tigloyl-hirsutinolide (4), along with seven known derivatives (5–11), three norisoprenoids (12–14), a flavonoid (15), and a linoleic acid derivative (16), were isolated from the chloroform partition of a methanol extract from the combined leaves and stems of Vernonia cinerea. Their structures were established by 1D and 2D NMR, UV, and MS analyses. Compounds 1–16 were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbour aberrantly-active STAT3, compared to normal NIH3T3 mouse fibroblasts that show no evidence of activated STAT3. Among the isolates, compounds 2 and 7 inhibited the aberrant STAT3 activity in glioblastoma or breast cancer cells. Further, compounds 7 and 8 inhibited viability of all three cell lines, compounds 2, 4, and 9 predominantly inhibited the viability of the U251MG glioblastoma cell line. PMID:24370662

  3. Antileishmanial Activity of Compounds Isolated from Sassafras albidum.

    PubMed

    Pulivarthi, Divya; Steinberg, Kelly Marie; Monzote, Lianet; Piñón, Abel; Setzer, William N

    2015-07-01

    Leishmaniasis is a neglected tropical disease caused by Leishmania parasitic protozoa, which currently lacks efficient treatment. Natural products have shown promise as a potential source for antiprotozoal drugs. This work focuses on the antileishmanial potential of Sassafras albidum (Lauraceae) bark extract. The crude bark extract of S. albidum showed excellent antileishmanial activity with an IC50 value less than 12.5 μg/mL against promastigotes of L. amazonensis. The chloroform stem bark extract of S. albidum was subjected to preparative column chromatography. Five compounds were isolated, purified by recrystallization, and identified as sesamin, spinescin, β-sitosterol, hexatriacontanal, and 1-triacontanol. Antileishmanial and cytotoxic screening were performed on these compounds. Sesamin exhibited the best activity against L. amazonensis with an IC50 of 15.8 μg/mL and was not cytotoxic to mouse macrophage cells (CC50 > 100 μg/mL).

  4. Antibacterial and Cytotoxic Activity of Compounds Isolated from Flourensia oolepis.

    PubMed

    Joray, Mariana Belén; Trucco, Lucas Daniel; González, María Laura; Napal, Georgina Natalia Díaz; Palacios, Sara María; Bocco, José Luis; Carpinella, María Cecilia

    2015-01-01

    The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of Flourensia oolepis were evaluated. Bioguided fractionation led to five flavonoids, identified as 2',4'-dihydroxychalcone (1), isoliquiritigenin (2), pinocembrin (3), 7-hydroxyflavanone (4), and 7,4'-dihydroxy-3'-methoxyflavanone (5). Compound 1 showed the highest antibacterial effect, with minimum inhibitory concentration (MIC) values ranging from 31 to 62 and 62 to 250 μg/mL, against Gram-positive and Gram-negative bacteria, respectively. On further assays, the cytotoxic effect of compounds 1-5 was determined by MTT assay on acute lymphoblastic leukemia (ALL) and chronic myeloid leukemia (CML) cell lines including their multidrug resistant (MDR) phenotypes. Compound 1 induced a remarkable cytotoxic activity toward ALL cells (IC50 = 6.6-9.9 μM) and a lower effect against CML cells (IC50 = 27.5-30.0 μM). Flow cytometry was used to analyze cell cycle distribution and cell death by PI-labeled cells and by Annexin V/PI staining, respectively. Upon treatment, 1 induced cell cycle arrest in the G2/M phase accompanied by a strong induction of apoptosis. These results describe for the first time the antibacterial metabolites of F. oolepis extract, with 1 being the most effective. This chalcone also emerges as a selective cytotoxic agent against sensitive and resistant leukemic cells, highlighting its potential as a lead compound. PMID:26819623

  5. Antibacterial and Cytotoxic Activity of Compounds Isolated from Flourensia oolepis

    PubMed Central

    Joray, Mariana Belén; Trucco, Lucas Daniel; González, María Laura; Napal, Georgina Natalia Díaz; Palacios, Sara María; Bocco, José Luis; Carpinella, María Cecilia

    2015-01-01

    The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of Flourensia oolepis were evaluated. Bioguided fractionation led to five flavonoids, identified as 2′,4′-dihydroxychalcone (1), isoliquiritigenin (2), pinocembrin (3), 7-hydroxyflavanone (4), and 7,4′-dihydroxy-3′-methoxyflavanone (5). Compound 1 showed the highest antibacterial effect, with minimum inhibitory concentration (MIC) values ranging from 31 to 62 and 62 to 250 μg/mL, against Gram-positive and Gram-negative bacteria, respectively. On further assays, the cytotoxic effect of compounds 1–5 was determined by MTT assay on acute lymphoblastic leukemia (ALL) and chronic myeloid leukemia (CML) cell lines including their multidrug resistant (MDR) phenotypes. Compound 1 induced a remarkable cytotoxic activity toward ALL cells (IC50 = 6.6–9.9 μM) and a lower effect against CML cells (IC50 = 27.5–30.0 μM). Flow cytometry was used to analyze cell cycle distribution and cell death by PI-labeled cells and by Annexin V/PI staining, respectively. Upon treatment, 1 induced cell cycle arrest in the G2/M phase accompanied by a strong induction of apoptosis. These results describe for the first time the antibacterial metabolites of F. oolepis extract, with 1 being the most effective. This chalcone also emerges as a selective cytotoxic agent against sensitive and resistant leukemic cells, highlighting its potential as a lead compound. PMID:26819623

  6. Fibrinolytic Compounds Isolated from a Brown Alga, Sargassum fulvellum

    PubMed Central

    Wu, Wenhui; Hasumi, Keiji; Peng, Hui; Hu, Xianwen; Wang, Xichang; Bao, Bin

    2009-01-01

    Two of bioactive natural products were founded in a brown alga, Sargassum fulvellum. After isolation and purification, the molecular structures of these two products were investigated by NMR spectroscopy and GC-mass spectroscopy. The two compounds were identified to be 1-O-palmitoyl-2-O-oleoyl-3-O-(α-D-glucopyranosyl) –glycerol (POGG) and 1-O-myristoyl-2-O-oleoyl-3-O-(α-D-glucopyranosyl) – glycerol (MOGG) which were obtained from Sargassum fulvellum for the first time. POGG and MOGG showed fibrinolytic activity in the reaction system of pro-u-PA and plasminogen. PMID:19597573

  7. Potential antidiabetic and antioxidant activities of Morus indica and Asystasia gangetica in alloxan-induced diabetes mellitus

    PubMed Central

    Kumar, R Pradeep; Sujatha, D; Saleem, TS Mohamed; Chetty, C Madhusudhana; Ranganayakulu, D

    2010-01-01

    Herbal drugs are frequently considered to be less toxic and also free from side effects, than synthetic ones. Hence, the present study was designed to investigate one such combination of herbal drugs, Asystasia gangetica and Morus indica for their antidiabetic and antioxidant potential against alloxan-induced diabetes in albino rats. The effect of both individual and a combination of Asystasia gangetica and Morus indica on blood glucose and liver glycogen were studied in the diabetic rats. The study also assessed for the effect of selected plant extracts for their effect on Superoxide dismutase (SOD), catalase (CAT), reduced glutathione (GSH) and Lipid peroxidation (LPO) in the homogenates of the pancreas. The results of the present study attests significant antidiabetic and antioxidant potential for the selected plants individually and also in combination as a prominent decrease in blood glucose and liver glycogen was observed in the rats treated with the extracts of the selected plants. Similarly, the levels of the protective antioxidant enzymes like SOD, CAT and GSH were increased along with decrease in the LPO levels. The present study provides a scientific evidence for antidiabetic and antioxidant potential of Asystasia gangetica and Morus indica. Further studies to isolate bioactive compounds will pave the way to identify potential lead compounds for developing safe and efficacious antidiabetic agents. PMID:27186088

  8. In vitro antidiabetic potential of the fruits of Crataegus pinnatifida

    PubMed Central

    Chowdhury, S.S.; Islam, M.N.; Jung, H.A.; Choi, J.S.

    2014-01-01

    In an attempt to develop alternative medicine for the treatment of diabetes and related complications, the antidiabetic potential of the fruits of Crataegus pinnatifida was evaluated. The antidiabetic potential of the methanol (MeOH) extract as well as different solvent soluble fractions of the fruits of C. pinnatifida was evaluated via α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), rat lens aldose reductase (RLAR), and advanced glycation end products (AGEs) formation inhibitory assays. The MeOH extract showed potent inhibitory activity against α-glucosidase, PTP1B, and AGEs formation with IC50 values of 122.11, 3.66 and 65.83 μg/ml respectively, while it showed moderate inhibitory activity against RLAR with the IC50 value of 160.54 μg/ml. Among different fractions, the ethyl acetate (EtOAc) and the dichloromethane (CH2Cl2) fractions were found as active fractions exhibiting potential α-glucosidase, PTP1B, RLAR inhibitory, and AGEs formation inhibitory activities. Seven compounds including hyperoside, chlorogenic acid, ursolic acid, oleanolic acid, 3-epicorosolic acid, β-sitosterol, β-sitosterol glucoside were isolated from these two fractions. 3-Epicorosolic acid showed both potent α-glucosidase and PTP1B inhibitory activities with IC50 values of 30.18 and 4.08 μg/ml respectively. Moreover, kinetic study revealed that 3-epicorosolic acid showed mixed type inhibition against PTP1B, while it showed uncompetitive inhibition against α-glucosidase. Therefore, these results suggest that the fruits of C. pinnatifida and its constituents have potential antidiabetic activity which might be used as a functional food for the treatment of diabetes and associated complications. PMID:25598795

  9. Depside derivatives with anti-hepatic fibrosis and anti-diabetic activities from Impatiens balsamina L. flowers.

    PubMed

    Li, Qian; Zhang, Xiaoshu; Cao, Jiaqing; Guo, Zhenghong; Lou, Yuntian; Ding, Meng; Zhao, Yuqing

    2015-09-01

    Eighteen compounds (1-18), seven new (3-9) and eleven previously reported (1, 2, and 10-18), were isolated from the flowers of Impatiens balsamina (Linn). The structures of the isolated compounds were elucidated using different spectroscopic methods, including NMR (1D and 2D), UV, IR, and HR-ESI-MS. Analysis of the bioassay results showed the compounds had notable anti-hepatic fibrosis activity against murine Hepatic Stellate Cells (t-HSC/Cl-6) and anti-diabetics activity against α-glucosidase. Specifically, new compounds 7, 8, 9 showed significant inhibitory activity on t-HSC/Cl-6 cells with IC50 values of 42.12, 109.2, and 34.04 μg/mL respectively, while the IC50 values of positive control Silymarin and Fufang Biejia Ruangan Pian were 202.34 and 231.56 μg/mL, respectively. In addition, compounds 2, 4, 7, 8, 10, 11, 17, and 18 exhibited excellent α-glucosidase inhibitory activity. Among these compounds, 7 exhibited the highest activity with an IC50 value of 0.72 μg/mL, while the IC50 value of the positive control acarbose was 3.36 μg/mL. This is the first study evaluating the anti-hepatic fibrosis and anti-diabetic activities of compounds isolated from the flowers of I. balsamina.

  10. Euonymus alatus: A Review on Its Phytochemistry and Antidiabetic Activity.

    PubMed

    Zhai, Xifeng; Lenon, George Binh; Xue, Charlie C L; Li, Chun-Guang

    2016-01-01

    Euonymus alatus (E. alatus) is a medicinal plant used in some Asian countries for treating various conditions including cancer, hyperglycemia, and diabetic complications. This review outlines the phytochemistry and bioactivities of E. alatus related to antidiabetic actions. More than 100 chemical constituents have been isolated and identified from E. alatus, including flavonoids, terpenoids, steroids, lignans, cardenolides, phenolic acids, and alkaloids. Studies in vitro and in vivo have demonstrated the hypoglycemic activity of E. alatus extracts and its certain constituents. The hypoglycemic activity of E. alatus may be related to regulation of insulin signaling and insulin sensitivity, involving PPARγ and aldose reductase pathways. Further studies on E. alatus and its bioactive compounds may help to develop new agents for treating diabetes and diabetic complications. PMID:27642361

  11. Euonymus alatus: A Review on Its Phytochemistry and Antidiabetic Activity

    PubMed Central

    Zhai, Xifeng

    2016-01-01

    Euonymus alatus (E. alatus) is a medicinal plant used in some Asian countries for treating various conditions including cancer, hyperglycemia, and diabetic complications. This review outlines the phytochemistry and bioactivities of E. alatus related to antidiabetic actions. More than 100 chemical constituents have been isolated and identified from E. alatus, including flavonoids, terpenoids, steroids, lignans, cardenolides, phenolic acids, and alkaloids. Studies in vitro and in vivo have demonstrated the hypoglycemic activity of E. alatus extracts and its certain constituents. The hypoglycemic activity of E. alatus may be related to regulation of insulin signaling and insulin sensitivity, involving PPARγ and aldose reductase pathways. Further studies on E. alatus and its bioactive compounds may help to develop new agents for treating diabetes and diabetic complications. PMID:27642361

  12. Euonymus alatus: A Review on Its Phytochemistry and Antidiabetic Activity

    PubMed Central

    Zhai, Xifeng

    2016-01-01

    Euonymus alatus (E. alatus) is a medicinal plant used in some Asian countries for treating various conditions including cancer, hyperglycemia, and diabetic complications. This review outlines the phytochemistry and bioactivities of E. alatus related to antidiabetic actions. More than 100 chemical constituents have been isolated and identified from E. alatus, including flavonoids, terpenoids, steroids, lignans, cardenolides, phenolic acids, and alkaloids. Studies in vitro and in vivo have demonstrated the hypoglycemic activity of E. alatus extracts and its certain constituents. The hypoglycemic activity of E. alatus may be related to regulation of insulin signaling and insulin sensitivity, involving PPARγ and aldose reductase pathways. Further studies on E. alatus and its bioactive compounds may help to develop new agents for treating diabetes and diabetic complications.

  13. Euonymus alatus: A Review on Its Phytochemistry and Antidiabetic Activity.

    PubMed

    Zhai, Xifeng; Lenon, George Binh; Xue, Charlie C L; Li, Chun-Guang

    2016-01-01

    Euonymus alatus (E. alatus) is a medicinal plant used in some Asian countries for treating various conditions including cancer, hyperglycemia, and diabetic complications. This review outlines the phytochemistry and bioactivities of E. alatus related to antidiabetic actions. More than 100 chemical constituents have been isolated and identified from E. alatus, including flavonoids, terpenoids, steroids, lignans, cardenolides, phenolic acids, and alkaloids. Studies in vitro and in vivo have demonstrated the hypoglycemic activity of E. alatus extracts and its certain constituents. The hypoglycemic activity of E. alatus may be related to regulation of insulin signaling and insulin sensitivity, involving PPARγ and aldose reductase pathways. Further studies on E. alatus and its bioactive compounds may help to develop new agents for treating diabetes and diabetic complications.

  14. Synthesis and Antidiabetic Evaluation of Benzenesulfonamide Derivatives

    PubMed Central

    Hosseinzadeh, Nouraddin; Seraj, Soodeh; Bakhshi-Dezffoli, Mohamad Ebrahim; Hasani, Mohammad; Khoshneviszadeh, Mehdi; Fallah-Bonekohal, Saeed; Abdollahi, Mohammad; Foroumadi, Alireza; Shafiee, Abbas

    2013-01-01

    The complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. Several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. These drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems. A series of seven novel N-(4-phenylthiazol-2-yl)benzenesulfonamides derivatives were synthesized and assayed in-vivo to investigate their antidiabetic activities by streptozotocin-induced model in rat. These derivatives showed considerable biological efficacy when compared to glibenclamide, a potent and well-known antidiabetic agent, as a reference drug. Four of the compounds were effective, amongst which 13 show more prominent activity at 100 mg/Kg p.o. The experimental results are statistically significant at p < 0.05 level. PMID:24250607

  15. Anion Gap Toxicity in Alloxan Induced Type 2 Diabetic Rats Treated with Antidiabetic Noncytotoxic Bioactive Compounds of Ethanolic Extract of Moringa oleifera

    PubMed Central

    2014-01-01

    Moringa oleifera (MO) is used for a number of therapeutic purposes. This raises the question of safety and possible toxicity. The objective of the study was to ascertain the safety and possible metabolic toxicity in comparison with metformin, a known drug associated with acidosis. Animals confirmed with diabetes were grouped into 2 groups. The control group only received oral dose of PBS while the test group was treated with ethanolic extract of MO orally twice daily for 5-6 days. Data showed that the extract significantly lowered glucose level to normal values and did not cause any significant cytotoxicity compared to the control group (P = 0.0698); there was no gain in weight between the MO treated and the control groups (P > 0.8115). However, data showed that treatment with an ethanolic extract of MO caused a decrease in bicarbonate (P < 0.0001), and more than twofold increase in anion gap (P < 0.0001); metformin treatment also decreased bicarbonate (P < 0.0001) and resulted in a threefold increase in anion gap (P < 0.0001). Conclusively, these data show that while MO appears to have antidiabetic and noncytotoxic properties, it is associated with statistically significant anion gap acidosis in alloxan induced type 2 diabetic rats. PMID:25548560

  16. Isolation of antiosteoporotic compounds from seeds of Sophora japonica.

    PubMed

    Abdallah, Hossam M; Al-Abd, Ahmed M; Asaad, Gihan F; Abdel-Naim, Ashraf B; El-halawany, Ali M

    2014-01-01

    Chemical investigation of Sophora japonica seeds resulted in the isolation of seven metabolites identified as: genistin (1), sophoricoside (2), sophorabioside (3), sophoraflavonoloside (4), genistein 7,4'-di-O-β-D-glucopyransoide (5), kaempferol 3-O-α-L-rhamnopyranosyl(1 → 6)β-D-glucopyranosyl(1 → 2)β-D-glucopyranoside (6) and rutin (7). Compounds 1, 2 and 5 showed significant estrogenic proliferative effect in MCF-7 cell in sub-cytotoxic concentration range. Compounds 1 and 2 showed minimal cell membrane damaging effect using LDH leakage assay. Accordingly, compound 2 (sophoricoside, (SPH)) was selected for further in-vivo studies as a potential anti-osteoporosis agent. The anti-osteoporotic effect of SPH was assessed in ovarectomized (OVX) rats after oral administration (15 mg/kg and 30 mg/kg) for 45 days compared to estradiol (10 µg/kg) as a positive control. Only in a dose of 30 mg/kg, SPH regained the original mechanical bone hardness compared to normal non-osteoporotic group. However, SPH (15 mg/kg) significantly increased the level of alkaline phosphatase (ALP) to normal level. Treatment with SPH (30 mg/kg) increased the level of ALP to be higher than normal group. SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX group. On the other hand, treatment with SPH (30 mg/kg) significantly increased the level of OC to 78% higher than normal non-ovarectomized animals group. In addition, SPH (15 mg/kg) decreased the bone resorption marker, acid phosphatase (ACP) to normal level and SPH (30 mg/kg) further diminished the level of serum ACP. Histopathologically, sophoricoside ameliorated the ovarectomy induced osteoporosis in a dose dependent manner. The drug showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group. PMID:24892557

  17. Anti-diabetic Activity.

    PubMed

    2016-01-01

    The hyperglycaemia continues to be a major health problem in India and other developing countries. This imbalance of blood glucose causes serious health problems such as damages to the blood vessel, poor healing of wounds, retinal damage, renal damage--kidney failure. The in vitro enzyme models and evaluation of hypoglycaemic effect of sample on normal and glucose-loaded rats has been used as a prediction experiment in this chapter before going for anti-diabetic experiment using animal models. PMID:26939280

  18. Isolated compounds from Sorghum bicolor L. inhibit the classical pathway of the complement.

    PubMed

    Moon, Hyung-In; Lee, Young-Choon; Lee, Jai-Heon

    2012-04-01

    The present study evaluated the anticomplement effects from isolated compounds of Sorghum bicolor in classical pathway complement system. Using column chromatograph, three compounds; Sorgoleone-362 (1), Sorgoleone-360 (2) and Sorgoleone-386 (3) were isolated and evaluated for in vitro anticomplement activity. Sorgoleone-386 showed inhibitory activity against complement system with 50% inhibitory concentrations (IC(50)) values of 148.3μg/ml. This is the first report of anticomplement activity of isolated compounds from Sorghum bicolor.

  19. Antiproliferative Effect and the Isolated Compounds of Pouzolzia indica

    PubMed Central

    Sangsuwon, Chanyapat; Jiratchariyakul, Weena; U-pratya, Yaowalak; Kummalue, Tanawan

    2013-01-01

    Previous report showed the high potent antiproliferative effect of the methanolic part extracted from the aerial parts of Pouzolzia indica on NB4 and HT93A acute leukemic cell lines with the IC50 values of 28.5 and 49.8 μg/mL, respectively. The bioassay-guided fractionation of the methanolic part gave 5 fractions, that is, FFI–FFV. FFII, FFIII, and FFIV inhibited the above leukemic cell lines with the IC50 values of 15.1 (FFII), 14.4 (FFIII), 32.1 (FFIV), and 31.0 (FFII), 9.7 (FFIII), 10.5 (FFIV) μg/mL, respectively. The compounds in these fractions were isolated using chromatographic technique. FFII contained friedelin 1, 28-hydroxy-3-friedelanone 2, and 7-methoxy-coumarin 3. FFIII contained 6, 7-dimethoxy-coumarin 4, scopoletin 5, methyl caffeate 6. FFIV contained sitosteryl glucoside 7 and a supposed glycosphingolipid 8. The chemical structures were elucidated by spectroscopic methods. PMID:23762121

  20. 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

  1. Effect of stevia and citric acid on the stability of phenolic compounds and in vitro antioxidant and antidiabetic capacity of a roselle (Hibiscus sabdariffa L.) beverage.

    PubMed

    Pérez-Ramírez, Iza F; Castaño-Tostado, Eduardo; Ramírez-de León, José A; Rocha-Guzmán, Nuria E; Reynoso-Camacho, Rosalía

    2015-04-01

    Plant infusions are consumed due to their beneficial effects on health, which is attributed to their bioactive compounds content. However, these compounds are susceptible to degradation during processing and storage. The objective of this research was to evaluate the effect of stevia and citric acid on the stability of phenolic compounds, antioxidant capacity and carbohydrate-hydrolysing enzyme inhibitory activity of roselle beverages during storage. The optimum extraction conditions of roselle polyphenolic compounds was of 95 °C/60 min, which was obtained by a second order experimental design. The incorporation of stevia increased the stability of colour and some polyphenols, such as quercetin, gallic acid and rosmarinic acid, during storage. In addition, stevia decreased the loss of ABTS, DPPH scavenging activity and α-amylase inhibitory capacity, whereas the incorporation of citric acid showed no effect. These results may contribute to the improvement of technological processes for the elaboration of hypocaloric and functional beverages.

  2. A method of isolating organic compounds present in water

    NASA Technical Reports Server (NTRS)

    Calder, G. V.; Fritz, J.; Junk, G. A.

    1972-01-01

    Water sample is passed through a column containing macroreticular resin, which absorbs only nonionic organic compounds. These compounds are selectively separated using aqueous eluents of varying pH, or completely exuded with small amount of an organic eluent.

  3. Effectively designed molecularly imprinted polymers for selective isolation of the antidiabetic drug metformin and its transformation product guanylurea from aqueous media.

    PubMed

    Kyzas, George Z; Nanaki, Stavroula G; Koltsakidou, Anastasia; Papageorgiou, Myrsini; Kechagia, Maria; Bikiaris, Dimitrios N; Lambropoulou, Dimitra A

    2015-03-25

    In the present study, two novel molecularly imprinted polymers (MIPs) with remarkable recognition properties for metformin and its transformation product, guanylurea, have been prepared for their selective, enrichment, isolation and removal from aqueous media. The prepared adsorbents were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and swelling experiments. The performance of the prepared MIPs was evaluated by various parameters including the influence of pH, contact time, temperature and initial compound concentration. The effects on the adsorption behavior of the removal process parameters were studied and the equilibrium data were fitted by the Langmuir and Freundlich models. Due to the imprinting effect, adsorption performance of MIPs was always superior to its corresponding NIP (non-imprinted polymer), with maximum adsorption capacity ∼80 mg g(-1) for both MIPs. Stability and reusability of the MIPs up to the 5th cycle meant that they could be applied repeatedly without losing substantial removal ability. In the next step, the prepared MIP nanoparticles were evaluated as sorbents in a dispersive solid phase extraction (D-SPE) configuration for selective enrichment and determination of metformin and guanylurea in different aqueous matrices. Under the working extraction conditions, the D-SPE method showed good linearity in the range of 50-1000 ng L(-1), repeatability of the extractions (RSD 2.1-5.1%, n=3), and low limits of detection (1.5-3.4 ng L(-1)). The expanded uncertainty of the data obtained was estimated following a bottom-up approach. The proposed method combined the advantages of MIPs and D-SPE, and it could become an alternative tool for analyzing the residues of METF and its transformation product GUA in complex water matrices, such as wastewaters.

  4. A review on antifungal activity of mushroom (basidiomycetes) extracts and isolated compounds.

    PubMed

    Alves, Maria José; Ferreira, Isabel C F R; Dias, Joana; Teixeira, Vânia; Martins, Anabela; Pintado, Manuela

    2013-01-01

    The present review reports the antifungal activity of mushroom extracts and isolated compounds including high (e.g. peptides and proteins) and low (e.g. sesquiterpenes and other terpenes, steroids, organic acids, acylcyclopentenediones and quinolines) molecular weight compounds. Most of the studies available on literature focused on screening of antifungal activity of mushroom extracts, rather than of isolated compounds. Data indicate that mushroom extracts are mainly tested against different Candida species, while mushroom compounds are mostly tested upon other fungi. Therefore, the potential of these compounds might be more useful in food industry than in clinics. Oudemansiella canarii and Agaricus bisporus methanolic extracts proved to be the most active mushroom extracts against Candida spp. Grifolin, isolated from Albatrellus dispansus, seemed to be the most active compound against phytopathogenic fungi. Further studies should be performed in order to better understand the mechanism of action of this and other antifungal compounds as well as safety issues.

  5. Cinnamic acid exerts anti-diabetic activity by improving glucose tolerance in vivo and by stimulating insulin secretion in vitro.

    PubMed

    Hafizur, Rahman M; Hameed, Abdul; Shukrana, Mishkat; Raza, Sayed Ali; Chishti, Sidra; Kabir, Nurul; Siddiqui, Rehan A

    2015-02-15

    Although the anti-diabetic activity of cinnamic acid, a pure compound from cinnamon, has been reported but its mechanism(s) is not yet clear. The present study was designed to explore the possible mechanism(s) of anti-diabetic activity of cinnamic acid in in vitro and in vivo non-obese type 2 diabetic rats. Non-obese type 2 diabetes was developed by injecting 90 mg/kg streptozotocin in 2-day-old Wistar pups. Cinnamic acid and cinnamaldehyde were administered orally to diabetic rats for assessing acute blood glucose lowering effect and improvement of glucose tolerance. Additionally, insulin secretory activity of cinnamic acid and cinnamaldehyde was evaluated in isolated mice islets. Cinnamic acid, but not cinnamaldehyde, decreased blood glucose levels in diabetic rats in a time- and dose-dependent manner. Oral administration of cinnamic acid with 5 and 10 mg/kg doses to diabetic rats improved glucose tolerance in a dose-dependent manner. The improvement by 10 mg/kg cinnamic acid was comparable to that of standard drug glibenclamide (5 mg/kg). Further in vitro studies showed that cinnamaldehyde has little or no effect on glucose-stimulated insulin secretion; however, cinnamic acid significantly enhanced glucose-stimulated insulin secretion in isolated islets. In conclusion, it can be said that cinnamic acid exerts anti-diabetic activity by improving glucose tolerance in vivo and stimulating insulin secretion in vitro.

  6. High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae).

    PubMed

    Silva, Eder Lana E; Lobo, Jonathas Felipe Revoredo; Vinther, Joachim Møllesøe; Borges, Ricardo Moreira; Staerk, Dan

    2016-06-16

    α-Glucosidase inhibitors decrease the cleavage- and absorption rate of monosaccharides from complex dietary carbohydrates, and represent therefore an important class of drugs for management of type 2 diabetes. In this study, a defatted ethyl acetate extract of Eremanthus crotonoides leaves with an inhibitory concentration (IC50) of 34.5 μg/mL towards α-glucosidase was investigated by high-resolution α-glucosidase inhibition profiling combined with HPLC-HRMS-SPE-NMR. This led to identification of six α-glucosidase inhibitors, namely quercetin (16), trans-tiliroside (17), luteolin (19), quercetin-3-methyl ether (20), 3,5-di-O-caffeoylquinic acid n-butyl ester (26) and 4,5-di-O-caffeoylquinic acid n-butyl ester (29). In addition, nineteen other metabolites were identified. The most active compounds were the two regioisomeric di-O-caffeoylquinic acid derivatives 26 and 29, with IC50 values of 5.93 and 5.20 μM, respectively. This is the first report of the α-glucosidase inhibitory activity of compounds 20, 26, and 29, and the findings support the important role of Eremanthus species as novel sources of new drugs and/or herbal remedies for treatment of type 2 diabetes.

  7. An overview on antidiabetic medicinal plants having insulin mimetic property.

    PubMed

    Patel, D K; Prasad, S K; Kumar, R; Hemalatha, S

    2012-04-01

    Diabetes mellitus is one of the common metabolic disorders acquiring around 2.8% of the world's population and is anticipated to cross 5.4% by the year 2025. Since long back herbal medicines have been the highly esteemed source of medicine therefore, they have become a growing part of modern, high-tech medicine. In view of the above aspects the present review provides profiles of plants (65 species) with hypoglycaemic properties, available through literature source from various database with proper categorization according to the parts used, mode of reduction in blood glucose (insulinomimetic or insulin secretagogues activity) and active phytoconstituents having insulin mimetics activity. From the review it was suggested that, plant showing hypoglycemic potential mainly belongs to the family Leguminoseae, Lamiaceae, Liliaceae, Cucurbitaceae, Asteraceae, Moraceae, Rosaceae and Araliaceae. The most active plants are Allium sativum, Gymnema sylvestre, Citrullus colocynthis, Trigonella foenum greacum, Momordica charantia and Ficus bengalensis. The review describes some new bioactive drugs and isolated compounds from plants such as roseoside, epigallocatechin gallate, beta-pyrazol-1-ylalanine, cinchonain Ib, leucocyandin 3-O-beta-d-galactosyl cellobioside, leucopelargonidin-3- O-alpha-L rhamnoside, glycyrrhetinic acid, dehydrotrametenolic acid, strictinin, isostrictinin, pedunculagin, epicatechin and christinin-A showing significant insulinomimetic and antidiabetic activity with more efficacy than conventional hypoglycaemic agents. Thus, from the review majorly, the antidiabetic activity of medicinal plants is attributed to the presence of polyphenols, flavonoids, terpenoids, coumarins and other constituents which show reduction in blood glucose levels. The review also discusses the management aspect of diabetes mellitus using these plants and their active principles.

  8. An overview on antidiabetic medicinal plants having insulin mimetic property

    PubMed Central

    Patel, DK; Prasad, SK; Kumar, R; Hemalatha, S

    2012-01-01

    Diabetes mellitus is one of the common metabolic disorders acquiring around 2.8% of the world's population and is anticipated to cross 5.4% by the year 2025. Since long back herbal medicines have been the highly esteemed source of medicine therefore, they have become a growing part of modern, high-tech medicine. In view of the above aspects the present review provides profiles of plants (65 species) with hypoglycaemic properties, available through literature source from various database with proper categorization according to the parts used, mode of reduction in blood glucose (insulinomimetic or insulin secretagogues activity) and active phytoconstituents having insulin mimetics activity. From the review it was suggested that, plant showing hypoglycemic potential mainly belongs to the family Leguminoseae, Lamiaceae, Liliaceae, Cucurbitaceae, Asteraceae, Moraceae, Rosaceae and Araliaceae. The most active plants are Allium sativum, Gymnema sylvestre, Citrullus colocynthis, Trigonella foenum greacum, Momordica charantia and Ficus bengalensis. The review describes some new bioactive drugs and isolated compounds from plants such as roseoside, epigallocatechin gallate, beta-pyrazol-1-ylalanine, cinchonain Ib, leucocyandin 3-O-beta-d-galactosyl cellobioside, leucopelargonidin-3- O-alpha-L rhamnoside, glycyrrhetinic acid, dehydrotrametenolic acid, strictinin, isostrictinin, pedunculagin, epicatechin and christinin-A showing significant insulinomimetic and antidiabetic activity with more efficacy than conventional hypoglycaemic agents. Thus, from the review majorly, the antidiabetic activity of medicinal plants is attributed to the presence of polyphenols, flavonoids, terpenoids, coumarins and other constituents which show reduction in blood glucose levels. The review also discusses the management aspect of diabetes mellitus using these plants and their active principles. PMID:23569923

  9. Isolation, identification, and quantification of roasted coffee antibacterial compounds.

    PubMed

    Daglia, Maria; Papetti, Adele; Grisoli, Pietro; Aceti, Camilla; Spini, Valentina; Dacarro, Cesare; Gazzani, Gabriella

    2007-12-12

    Coffee brew is a widely consumed beverage with multiple biological activities due both to naturally occurring components and to the hundreds of chemicals that are formed during the roasting process. Roasted coffee extract possesses antibacterial activity against a wide range of microorganisms, including Staphylococcus aureus and Streptococcus mutans, whereas green coffee extract exhibits no such activity. The naturally occurring coffee compounds, such as chlorogenic acids and caffeine, cannot therefore be responsible for the significant antibacterial activity exerted by coffee beverages against both bacteria. The very low minimum inhibitory concentration (MIC) found for standard glyoxal, methylglyoxal, and diacetyl compounds formed during the roasting process points to these alpha-dicarbonyl compounds as the main agents responsible for the antibacterial activity of brewed coffee against Sa. aureus and St. mutans. However, their low concentrations determined in the beverage account for only 50% of its antibacterial activity. The addition of caffeine, which has weak intrinsic antibacterial activity, to a mixture of alpha-dicarbonyl compounds at the concentrations found in coffee demonstrated that caffeine synergistically enhances the antibacterial activity of alpha-dicarbonyl compounds and that glyoxal, methylglyoxal, and diacetyl in the presence of caffeine account for the whole antibacterial activity of roasted coffee.

  10. A Quantum Chemical and Statistical Study of Cytotoxic Activity of Compounds Isolated from Curcuma zedoaria.

    PubMed

    Hamdi, Omer Abdalla Ahmed; Anouar, El Hassane; Shilpi, Jamil A; Trabolsy, Zuhra Bashir Khalifa Al; Zain, Sharifuddin Bin Md; Zakaria, Nur Shahidatul Shida; Zulkefeli, Mohd; Weber, Jean-Frédéric F; Malek, Sri Nurestri A; Rahman, Syarifah Nur Syed Abdul; Awang, Khalijah

    2015-01-01

    A series of 21 compounds isolated from Curcuma zedoaria was subjected to cytotoxicity test against MCF7; Ca Ski; PC3 and HT-29 cancer cell lines; and a normal HUVEC cell line. To rationalize the structure-activity relationships of the isolated compounds; a set of electronic; steric and hydrophobic descriptors were calculated using density functional theory (DFT) method. Statistical analyses were carried out using simple and multiple linear regressions (SLR; MLR); principal component analysis (PCA); and hierarchical cluster analysis (HCA). SLR analyses showed that the cytotoxicity of the isolated compounds against a given cell line depend on certain descriptors; and the corresponding correlation coefficients (R2) vary from 0%-55%. MLR results revealed that the best models can be achieved with a limited number of specific descriptors applicable for compounds having a similar basic skeleton. Based on PCA; HCA and MLR analyses; active compounds were classified into subgroups; which was in agreement with the cell based cytotoxicity assay.

  11. New arylalkanones from Horsfieldia macrobotrys, effective antidiabetic agents concomitantly inhibiting α-glucosidase and free radicals.

    PubMed

    Ramadhan, Rico; Phuwapraisirisan, Preecha

    2015-10-15

    In search of effective antidiabetic agents having therapeutic effect by inhibiting α-glucosidase and preventive effect by scavenging free radicals, Horsfieldia macrobotrys showed promising bioactivity required for the proposed criteria. Bioassay-guided isolation of the stem bark extract resulted in two new arylalkanones named horsfieldone A (1) and maingayone D (2), together with a new flavanone C-glucoside named 8-C-β-d-glucopyranosylpinocembrin (3). Their structures and stereochemistry were determined by spectroscopic techniques as well as Mosher's method. Of isolated compounds, maingayone D (2) was the most potent inhibitors against both α-glucosidases and free radicals. The presence of additional phenolic moieties in 2 clearly indicated their critical roles in inhibitory effects. Further investigation on mechanism underlying α-glucosidase inhibition indicated that maingayone D (2) could retard the enzyme function by both competitive and noncompetitive manners.

  12. In vitro isolation and characterization of biolarvicidal compounds from micropropagated plants of Spilanthes acmella.

    PubMed

    Pandey, Vibha; Chopra, Madhu; Agrawal, Veena

    2011-02-01

    Spilanthes acmella (Family: Asteraceae) commonly known as "toothache plant" is known to possess strong insecticidal and larvicidal properties. Experiments have been conducted to isolate and characterise the biolarvicidal compounds from the flower head extract of micropropagated S. acmella plants employing various tools like FT-IR, TLC, CC, NMR. FT-IR spectroscopy of the crude hexane extract sample revealed the presence of amide (secondary metabolite) as functional group in S. acmella flower heads. The crude extract was separated into 85 fractions (100 ml each) through silica gel column chromatography using hexane-ethyl acetate mobile phase. All fractions were tested for their larvicidal activity against late III/early IV instar Anopheles stephensi larvae and fraction showing maximum bioefficacy against aforesaid larvae was further resolved into three separate bands on Preparative TLC plate, the respective R (f) values being (a) 0.18, (b) 0.23 and (c) 0.27. Based on Proton NMR spectrum of the eluted compounds and their comparison with published results, three different compounds were identified: N-isobutyl-2,6,8-decatrienamide (compound 1), undeca-2E,7Z,9E-trienoic acid isobutylamide (compound 2) from band a and (2E)-N-(2-methylbutyl)-2-undecene-8,10-diynamide (compound 3) from band b. The amount of the compounds obtained were 338 mg (compounds 1 and 2) and 188.4 mg (compound 3), respectively. This is the first report of biolarvicidal compounds isolation and characterisation from micropropagated S. acmella plants. PMID:20859747

  13. Characterization of a fluorescent compound isolated from Legionella pneumophila

    SciTech Connect

    Swanson, S.J.

    1987-01-01

    Legionella pneumophila requires the presence of amino acids for growth and utilizes them for energy. Along with other amino acids, either phenylalanine or tyrosine is essential for the growth of the organism and tyrosine has been identified as an energy source. When L. pneumophila is grown in the presence of tyrosine, a brown melanin-like pigment is produced. A green fluorescent pigment, fg2, was isolated from centrifuged culture fluid after the organism was grown in the presence of tyrosine. Fg2 is water soluble with a molecular weight of 152 as determined by mass spectral analysis. A mutant of L. pneumophila unable to produce fg2 was isolated to assist in elucidation of the biosynthesis of fg2. Radiolabeling experiments were utilized to conclude that neither tyrosine nor any other amino acid was a precursor in the biosynthesis of fg2. Shikimic acid, an intermediate in tyrosine biosynthesis, was found to also be an intermediate in the biosynthesis of fg2. A series of experiments in which L. pneumophila was grown in a chemically defined medium containing various combinations of aromatic amino acids determined that fg2 and the brown pigment always occur in tandem.

  14. Bioassays guided isolation of compounds from Chaetomium globosum.

    PubMed

    Awad, N E; Kassem, H A; Hamed, M A; El-Naggar, M A A; El-Feky, A M M

    2014-06-01

    The aim of the present study was to evaluate different biological activities of the fungus Chaetomium globosum (family Chaetomiaceae). The evaluation was done through testing its antimicrobial, antioxidant and anticancer effects. C. globosum was isolated from the Cucumber soil (rhizosphere) and caused inhibition of the mycelial growth of Fusarium solani, Rhizoctonia solani and Sclerotium rolfsii in the biculture test. Petroleum ether and ethyl acetate extracts of the liquid culture of C. globosum showed potent in vitro antioxidant activity. C. globosum proved potent antibacterial activity against Bacillus subtilis, Escherichia coli and Pseudomonas fluorescens. It also recorded significant antifungal activity against Candida albicans, F. solani, Fusarium oxysporum, R. solani and Pythium ultimum. It exerted cytotoxic effect on human hepatocellular carcinoma cell line (HepG2). Unsaponifiable and saponifiable matters of the petroleum ether extract showed the presence of hydrocarbons, sterols and fatty acids. The ethyl acetate extract showed the presence of prenisatin, chrysophanol, chrysazin, chaetoviridin A and B. The isolated secondary metabolites proved significant antioxidant and antimicrobial activity on B. subtilis, E. coli and R. solani. In conclusion, this fungus showed different biological activities. Further studies must be done to apply its use in the agricultural and medicinal field. PMID:24361402

  15. Composition of concentrates of heterocyclic petroleum compounds isolated by complexformation with titanium tetrachloride

    SciTech Connect

    Nesterenko, V.I.; Alekseyev, A.P.; Plyusnin, A.N.

    1983-01-01

    The group composition of nitrous bases and aromatic sulphur compounds isolated by complex-formation with titanium tetrachloride from Soviet and West Siberian (Fedorov) crude oils was studied. Homologous series of nitrous bases are characterized by practically identical compounds ranging from C /SUB n/ H /SUB 2n-5/ N to C /SUB n/ H /SUB 2n-21/ N. Pyridine and quinoline derivatives with alkyl substituents and naphthene rings predominate. Thiacycloparaffins with a number of naphthene rings in the molecule of 1 to 5 predominate among saturated sulphur compounds. Unsaturated sulphur compounds are represented mainly by homologues of thiophene, benzo- and dibenzothiophene.

  16. Bioactive Compounds Isolated from Microalgae in Chronic Inflammation and Cancer

    PubMed Central

    Talero, Elena; García-Mauriño, Sofía; Ávila-Román, Javier; Rodríguez-Luna, Azahara; Alcaide, Antonio; Motilva, Virginia

    2015-01-01

    The risk of onset of cancer is influenced by poorly controlled chronic inflammatory processes. Inflammatory diseases related to cancer development include inflammatory bowel disease, which can lead to colon cancer, or actinic keratosis, associated with chronic exposure to ultraviolet light, which can progress to squamous cell carcinoma. Chronic inflammatory states expose these patients to a number of signals with tumorigenic effects, including nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) activation, pro-inflammatory cytokines and prostaglandins release and ROS production. In addition, the participation of inflammasomes, autophagy and sirtuins has been demonstrated in pathological processes such as inflammation and cancer. Chemoprevention consists in the use of drugs, vitamins, or nutritional supplements to reduce the risk of developing or having a recurrence of cancer. Numerous in vitro and animal studies have established the potential colon and skin cancer chemopreventive properties of substances from marine environment, including microalgae species and their products (carotenoids, fatty acids, glycolipids, polysaccharides and proteins). This review summarizes the main mechanisms of actions of these compounds in the chemoprevention of these cancers. These actions include suppression of cell proliferation, induction of apoptosis, stimulation of antimetastatic and antiangiogenic responses and increased antioxidant and anti-inflammatory activity. PMID:26437418

  17. Gas chromatographic isolation of individual compounds from complex matrices for radiocarbon dating

    SciTech Connect

    Eglinton, T.I.; Aluwihare, L.I.; McNichol, A.P.; Bauer, J.E.; Druffel, E.R.M.

    1996-03-01

    This paper describes the application of a novel, practical approach for isolation of individual compounds from complex organic matrices for natural abundance radiocarbon measurement. This is achieved through the use of automated pereparative capillary gas chromatography (PCGC) to separate and recover sufficient quantities of individual target compounds for {sup 14}C analysis by accelerator mass spectrometry (AMS). We developed and tested this approach using a suite of samples (plant lipids, petroleums) whose ages spanned the {sup 14}C time scale and which contained a variety of compound types (fatty acids, sterols, hydrocarbons). Comparison of individual compound and bulk radiocarbon signatures for the isotopically homogeneous samples studied revealed that {Delta}{sup 14}C values generally agreed well ({+-}10%). Background contamination was assessed at each stage of the isolation procedure, and incomplete solvent removal prior to combustion was the only significant source of additional carbon. Isotope fractionation was addressed through compound-specific stable carbon isotopic analyses. Fractionation of isotopes during isolation of individual compounds was minimal (<5% for {delta}{sup 13}C), provided the entire peak was collected during PCGC. Trapping of partially coeluting peaks did cause errors, and these results highlight the importance of conducting stable carbon isotopic measurements of each trapped compound in concert with AMS for reliable radiocarbon measurements. 29 refs., 9 figs., 2 tabs.

  18. Characterization of bovine viral diarrhea virus isolates resistant to a novel antiviral compound obtained from persistently infected calves

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this research was to characterize isolates resistant to a novel antiviral compound (DB772) isolated from persistently infected (PI) calves treated with the compound. Viral isolates were obtained from four Angus-cross beef calves (A,B,C,D) persistently infected with BVDV type 1 or 2 ...

  19. Isolation and identification of antimicrobial compound from Mentha longifolia L. leaves grown wild in Iraq

    PubMed Central

    Al-Bayati, Firas A

    2009-01-01

    Background Mentha longifolia L. (Lamiaceae) leaves have been traditionally implemented in the treatment of minor sore throat and minor mouth or throat irritation by the indigenous people of Iraq, although the compounds responsible for the medicinal properties have not been identified. In the present study, an antimicrobial compound was isolated and characterized, and its biological activity was assessed. Methods The compound was isolated and characterized from the extracted essential oil using different spectral techniques: TLC, FTIR spectra and HPLC. Antimicrobial activity of the compound was assessed using both disc diffusion and microdilution method in 96 multi-well microtiter plates. Results A known compound was isolated from the essential oil of the plant and was identified as (-) menthol. The isolated compound was investigated for its antimicrobial activity against seven selected pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Streptococcus mutans, Streptococcus faecalis, Streptococcus pyogenis, Lactobacillus acidophilus, Pseudomonas aeruginosa and the yeast Candida albicans. Menthol at different concentrations (1:1, 1:5, 1:10, 1:20) was active against all tested bacteria except for P. aeruginosa, and the highest inhibitory effect was observed against S. mutans (zone of inhibition: 25.3 mm) using the disc diffusion method. Minimal inhibitory concentration MIC values ranged from 15.6–125.0 μg/ml, and the most promising results were observed against S. aureus and S. mutans (MIC 15.6 μg/ml) while, S. faecalis, S. pyogenis and L. acidophilus ranked next (MIC 31.2 μg/ml). Furthermore, menthol achieved considerable antifungal activity against the yeast C. albicans (zone of inhibition range: 7.1–18.5 mm; MIC: 125.0). Conclusion The isolation of an antimicrobial compound from M. longifolia leaves validates the use of this plant in the treatment of minor sore throat and minor mouth or throat irritation. PMID:19523224

  20. Polyketide and benzopyran compounds of an endophytic fungus isolated from Cinnamomum mollissimum: biological activity and structure

    PubMed Central

    Santiago, Carolina; Sun, Lin; Munro, Murray Herbert Gibson; Santhanam, Jacinta

    2014-01-01

    Objective To study bioactivity and compounds produced by an endophytic Phoma sp. fungus isolated from the medicinal plant Cinnamomum mollissimum. Methods Compounds produced by the fungus were extracted from fungal broth culture with ethyl acetate. This was followed by bioactivity profiling of the crude extract fractions obtained via high performance liquid chromatography. The fractions were tested for cytotoxicity to P388 murine leukemic cells and antimicrobial activity against bacteria and pathogenic fungi. Compounds purified from active fractions which showed antibacterial, antifungal and cytotoxic activities were identified using capillary nuclear magnetic resonance analysis, mass spectrometry and admission to AntiMarin database. Results Three known compounds, namely 4-hydroxymellein, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one and 1-(2,6-dihydroxyphenyl) ethanone, were isolated from the fungus. The polyketide compound 4-hydroxymellein showed high inhibitory activity against P388 murine leukemic cells (94.6%) and the bacteria Bacillus subtilis (97.3%). Meanwhile, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one, a benzopyran compound, demonstrated moderate inhibitory activity against P388 murine leukemic cells (48.8%) and the fungus Aspergillus niger (56.1%). The second polyketide compound, 1 (2,6-dihydroxyphenyl) ethanone was inactive against the tested targets. Conclusions These findings demonstrate the potential of endophytes as producers of pharmacologically important compounds, including polyketides which are major secondary metabolites in fungi. PMID:25183332

  1. Isolation and structural elucidation of novel antimicrobial compounds from maggots of Chrysomyis megacephala Fabricius.

    PubMed

    Gao, Jiayu; Li, Wenyuan; Niu, Lanlan; Cao, Ranran; Yin, Weiping

    2015-02-01

    The excretions/secretions from the maggot of Chrysomyis megacephala Fabricius are traditionally used to treat serious infections in China. In this study, bioassay-guided fractionation led to the isolation of three novel antibacterial compounds (1-3), including important fluorinated compounds (3 and 5), together with other nine known compounds from 70% methanol extract of C. megacephala. The structures of the new compounds were elucidated by NMR spectroscopic analysis and high-resolution mass spectroscopy. The antibacterial activities of the isolated compounds were evaluated using agar disc diffusion method. New compounds 1 and 2 exhibited moderate activity against Bacillus subtilis with a minimum inhibitory concentration (MIC) of 250 μg mL(- 1). The most active compounds 3 and 5 displayed a broad spectrum of antimicrobial activity with an MIC of 125 μg mL(- 1) against G(+) and G(- ) bacteria. The structure of the above-mentioned novel compounds and their antimicrobial activities are herein reported for the first time from the natural product of insects.

  2. Isolation and Identification of Vesicular-Arbuscular Mycorrhiza-Stimulatory Compounds from Clover (Trifolium repens) Roots.

    PubMed

    Nair, M G; Safir, G R; Siqueira, J O

    1991-02-01

    Two isoflavonoids isolated from clover roots grown under phosphate stress were characterized as formononetin (7-hydroxy,4'-methoxy isoflavone) and biochanin A (5,7-dihydroxy,4'-methoxy isoflavone). At 5 ppm, these compounds stimulated hyphal growth in vitro and root colonization of an undescribed vesicular-arbuscular mycorrhiza, a Glomus sp. (INVAM-112). The permethylated products of the two compounds were inactive. These findings suggest that the isoflavonoids studied may act as signal molecules in vesicular-arbuscular mycorrhiza symbiosis.

  3. Gas chromatographic isolation of individual compounds from complex matrices for radiocarbon dating.

    PubMed

    Eglinton, T I; Aluwihare, L I; Bauer, J E; Druffel, E R; McNichol, A P

    1996-03-01

    This paper describes the application of a novel, practical approach for isolation of individual compounds from complex organic matrices for natural abundance radiocarbon measurement. This is achieved through the use of automated preparative capillary gas chromatography (PCGC) to separate and recover sufficient quantities of individual target compounds for (14)C analysis by accelerator mass spectrometry (AMS). We developed and tested this approach using a suite of samples (plant lipids, petroleums) whose ages spanned the (14)C time scale and which contained a variety of compound types (fatty acids, sterols, hydrocarbons). Comparison of individual compound and bulk radiocarbon signatures for the isotopically homogeneous samples studied revealed that Δ(14)C values generally agreed well (±10%). Background contamination was assessed at each stage of the isolation procedure, and incomplete solvent removal prior to combustion was the only significant source of additional carbon. Isotope fractionation was addressed through compound-specific stable carbon isotopic analyses. Fractionation of isotopes during isolation of individual compounds was minimal (<5‰ for δ(13)C), provided the entire peak was collected during PCGC. Trapping of partially coeluting peaks did cause errors, and these results highlight the importance of conducting stable carbon isotopic measurements of each trapped compound in concert with AMS for reliable radiocarbon measurements. The addition of carbon accompanying derivatization of functionalized compounds (e.g., fatty acids and sterols) prior to chromatographic separation represents a further source of potential error. This contribution can be removed using a simple isotopic mass balance approach. Based on these preliminary results, the PCGC-based approach holds promise for accurately determining (14)C ages on compounds specific to a given source within complex, heterogeneous samples.

  4. Preliminary In Vitro and In Vivo Evaluation of Antidiabetic Activity of Ducrosia anethifolia Boiss. and Its Linear Furanocoumarins

    PubMed Central

    Shalaby, Nagwa M. M.; Abd-Alla, Howaida I.; Aly, Hanan F.; Albalawy, Marzougah A.; Shaker, Kamel H.; Bouajila, Jalloul

    2014-01-01

    Aim. Ducrosia anethifolia is used as flavoring additive. There have been little detailed phytochemical reports on this genus and the antidiabetic activity of this plant is not yet evaluated. Method. Structure of compounds was deduced by spectroscopic analyses. Preliminary in vitro evaluation of the antidiabetic activity of crude extract and its furanocoumarins was carried out (α-amylase, α-glucosidase, and β-galactosidase). The in vivo activity was investigated by measuring some oxidative stress markers. Biomarkers of liver injury and kidney were also determined. Results. Eight linear furanocoumarins, psoralen, 5-methoxypsoralen, 8-methoxypsoralen, imperatorin, isooxypeucedanin, pabulenol, oxypeucedanin methanolate, oxypeucedanin hydrate, and 3-O-glucopyranosyl-β-sitosterol, were isolated. All compounds were reported for the first time from the genus Ducrosia except pabulenol. The blood glucose level, liver function enzymes, total protein, lipid, and cholesterol levels were significantly normalized by extract treatment. The antioxidant markers, glucolytic, and gluconeogenic enzymes were significantly ameliorated and the elevated level of kidney biomarkers in the diabetic groups was restored. The compounds showed inhibitory activity in a concentration dependant manner. Imperatorin and 5-methoxypsoralen showed the most potent inhibiting power. Conclusion. D. anethifolia extract showed hypoglycemic, hypolipidemic, and antioxidant effect as well as ameliorating kidney function. This extract and some linear furanocoumarins exhibited carbohydrate metabolizing enzymes inhibitory effect. PMID:24800231

  5. Honey - A Novel Antidiabetic Agent

    PubMed Central

    Erejuwa, Omotayo O.; Sulaiman, Siti A.; Wahab, Mohd S. Ab

    2012-01-01

    Diabetes mellitus remains a burden worldwide in spite of the availability of numerous antidiabetic drugs. Honey is a natural substance produced by bees from nectar. Several evidence-based health benefits have been ascribed to honey in the recent years. In this review article, we highlight findings which demonstrate the beneficial or potential effects of honey in the gastrointestinal tract (GIT), on the gut microbiota, in the liver, in the pancreas and how these effects could improve glycemic control and metabolic derangements. In healthy subjects or patients with impaired glucose tolerance or diabetes mellitus, various studies revealed that honey reduced blood glucose or was more tolerable than most common sugars or sweeteners. Pre-clinical studies provided more convincing evidence in support of honey as a potential antidiabetic agent than clinical studies did. The not-too-impressive clinical data could mainly be attributed to poor study designs or due to the fact that the clinical studies were preliminary. Based on the key constituents of honey, the possible mechanisms of action of antidiabetic effect of honey are proposed. The paper also highlights the potential impacts and future perspectives on the use of honey as an antidiabetic agent. It makes recommendations for further clinical studies on the potential antidiabetic effect of honey. This review provides insight on the potential use of honey, especially as a complementary agent, in the management of diabetes mellitus. Hence, it is very important to have well-designed, randomized controlled clinical trials that investigate the reproducibility (or otherwise) of these experimental data in diabetic human subjects. PMID:22811614

  6. Bioassay-guided isolation and identification of antifungal compounds from ginger.

    PubMed

    Ficker, C; Smith, M L; Akpagana, K; Gbeassor, M; Zhang, J; Durst, T; Assabgui, R; Arnason, J T

    2003-09-01

    A bioassay-guided isolation of antifungal compounds from an African land race of ginger, Zingiber officinale Roscoe, led to the identification of [6], [8] and [10]-gingerols and [6]-gingerdiol as the main antifungal principles. The compounds were active against 13 human pathogens at concentrations of <1 mg/mL. The gingerol content of the African land race was at least 3 x higher than that of typical commercial cultivars of ginger. Therefore, ginger extracts standardized on the basis of the identified compounds, could be considered as antifungal agents for practical therapy. PMID:13680820

  7. New cytotoxic compounds of endophytic fungus Alternaria sp. isolated from Broussonetia papyrifera (L.) Vent.

    PubMed

    Zhang, Naidan; Zhang, Chunyan; Xiao, Xiao; Zhang, Qiaoyan; Huang, Baokang

    2016-04-01

    From the ethyl acetate extract of a culture of the endophytic fungus Alternaria species G7 in Broussonetia papyrifera, a new compound altertoxin IV (1) together with nine known compounds were isolated and identified by means of bioassay-guided fractionation. The structures of these compounds were established on the basis of spectroscopic methods, among which the absolute configuration of compound 1, a new tetrahydroperylenone derivative, was determined by means of X-Ray Crystallographic analysis. The isolated compounds were subjected to cytotoxic activity against three human cancer cell lines (A549, MG-63, and SMMC-7721). Compound 2 showed significant cytotoxic activities against tested cell lines, with IC50 values of 1.47, 2.11 and 7.34 μg/mL, respectively. Additionally, compound 4 also exhibited significant cytotoxic activities against cell lines MG-63 and SMMC-7721, with IC50 values of 0.53 and 2.92 μg/mL. Endophytic fungi Alternaria from B. papyrifera might be promising sources of natural bioactive and novel metabolites.

  8. New cytotoxic compounds of endophytic fungus Alternaria sp. isolated from Broussonetia papyrifera (L.) Vent.

    PubMed

    Zhang, Naidan; Zhang, Chunyan; Xiao, Xiao; Zhang, Qiaoyan; Huang, Baokang

    2016-04-01

    From the ethyl acetate extract of a culture of the endophytic fungus Alternaria species G7 in Broussonetia papyrifera, a new compound altertoxin IV (1) together with nine known compounds were isolated and identified by means of bioassay-guided fractionation. The structures of these compounds were established on the basis of spectroscopic methods, among which the absolute configuration of compound 1, a new tetrahydroperylenone derivative, was determined by means of X-Ray Crystallographic analysis. The isolated compounds were subjected to cytotoxic activity against three human cancer cell lines (A549, MG-63, and SMMC-7721). Compound 2 showed significant cytotoxic activities against tested cell lines, with IC50 values of 1.47, 2.11 and 7.34 μg/mL, respectively. Additionally, compound 4 also exhibited significant cytotoxic activities against cell lines MG-63 and SMMC-7721, with IC50 values of 0.53 and 2.92 μg/mL. Endophytic fungi Alternaria from B. papyrifera might be promising sources of natural bioactive and novel metabolites. PMID:27001249

  9. Bioguided isolation and identification of the nonvolatile antioxidant compounds from fennel (Foeniculum vulgare Mill.) waste.

    PubMed

    Parejo, Irene; Viladomat, Francesc; Bastida, Jaume; Schmeda-Hirschmann, Guillermo; Burillo, Jesús; Codina, Carles

    2004-04-01

    A bioguided isolation of an aqueous extract of fennel waste led to the isolation of 12 major phenolic compounds. Liquid chromatography coupled to atmospheric pressure chemical ionization mass spectrometry (LC/UV/APCI-MS) combined with spectroscopic methods (NMR) was used for compound identification. Radical scavenging activity was tested using three methods: DPPH*, superoxide nitro-blue tetrazolium hypoxanthine/xanthine oxidase, and *OH/luminol chemiluminescence. In addition to products described in the literature, eight antioxidant compounds were isolated and identified for the first time in fennel: 3-caffeoylquinic acid, 4-caffeoylquinic acid, 1,5-O-dicaffeoylquinic acid, rosmarinic acid, eriodictyol-7-O-rutinoside, quercetin-3-O-galactoside, kaempferol-3-O-rutinoside, and kaempferol-3-O-glucoside. The structures of eriodictyol-7-O-rutinoside and quercetin-3-O-glucuronide were completely elucidated by two-dimensional NMR experiments. The isolated compounds exhibited a strong antiradical scavenging activity, which may contribute to the interpretation of the pharmacological effects of fennel.

  10. Biomolecular Characterization of Putative Antidiabetic Herbal Extracts

    PubMed Central

    Stadlbauer, Verena; Haselgrübler, Renate; Lanzerstorfer, Peter; Plochberger, Birgit; Borgmann, Daniela; Jacak, Jaroslaw; Winkler, Stephan M.; Schröder, Klaus; Höglinger, Otmar; Weghuber, Julian

    2016-01-01

    Induction of GLUT4 translocation in the absence of insulin is considered a key concept to decrease elevated blood glucose levels in diabetics. Due to the lack of pharmaceuticals that specifically increase the uptake of glucose from the blood circuit, application of natural compounds might be an alternative strategy. However, the effects and mechanisms of action remain unknown for many of those substances. For this study we investigated extracts prepared from seven different plants, which have been reported to exhibit anti-diabetic effects, for their GLUT4 translocation inducing properties. Quantitation of GLUT4 translocation was determined by total internal reflection fluorescence (TIRF) microscopy in insulin sensitive CHO-K1 cells and adipocytes. Two extracts prepared from purslane (Portulaca oleracea) and tindora (Coccinia grandis) were found to induce GLUT4 translocation, accompanied by an increase of intracellular glucose concentrations. Our results indicate that the PI3K pathway is mainly responsible for the respective translocation process. Atomic force microscopy was used to prove complete plasma membrane insertion. Furthermore, this approach suggested a compound mediated distribution of GLUT4 molecules in the plasma membrane similar to insulin stimulated conditions. Utilizing a fluorescent actin marker, TIRF measurements indicated an impact of purslane and tindora on actin remodeling as observed in insulin treated cells. Finally, in-ovo experiments suggested a significant reduction of blood glucose levels under tindora and purslane treated conditions in a living organism. In conclusion, this study confirms the anti-diabetic properties of tindora and purslane, which stimulate GLUT4 translocation in an insulin-like manner. PMID:26820984

  11. Biomolecular Characterization of Putative Antidiabetic Herbal Extracts.

    PubMed

    Stadlbauer, Verena; Haselgrübler, Renate; Lanzerstorfer, Peter; Plochberger, Birgit; Borgmann, Daniela; Jacak, Jaroslaw; Winkler, Stephan M; Schröder, Klaus; Höglinger, Otmar; Weghuber, Julian

    2016-01-01

    Induction of GLUT4 translocation in the absence of insulin is considered a key concept to decrease elevated blood glucose levels in diabetics. Due to the lack of pharmaceuticals that specifically increase the uptake of glucose from the blood circuit, application of natural compounds might be an alternative strategy. However, the effects and mechanisms of action remain unknown for many of those substances. For this study we investigated extracts prepared from seven different plants, which have been reported to exhibit anti-diabetic effects, for their GLUT4 translocation inducing properties. Quantitation of GLUT4 translocation was determined by total internal reflection fluorescence (TIRF) microscopy in insulin sensitive CHO-K1 cells and adipocytes. Two extracts prepared from purslane (Portulaca oleracea) and tindora (Coccinia grandis) were found to induce GLUT4 translocation, accompanied by an increase of intracellular glucose concentrations. Our results indicate that the PI3K pathway is mainly responsible for the respective translocation process. Atomic force microscopy was used to prove complete plasma membrane insertion. Furthermore, this approach suggested a compound mediated distribution of GLUT4 molecules in the plasma membrane similar to insulin stimulated conditions. Utilizing a fluorescent actin marker, TIRF measurements indicated an impact of purslane and tindora on actin remodeling as observed in insulin treated cells. Finally, in-ovo experiments suggested a significant reduction of blood glucose levels under tindora and purslane treated conditions in a living organism. In conclusion, this study confirms the anti-diabetic properties of tindora and purslane, which stimulate GLUT4 translocation in an insulin-like manner. PMID:26820984

  12. Activity-guided isolation of an antiandrogenic compound of Pygeum africanum.

    PubMed

    Schleich, Sonja; Papaioannou, Maria; Baniahmad, Aria; Matusch, Rudolf

    2006-05-01

    Inactivation of the androgen receptor (AR) through androgen ablation and treatment with antiandrogens is a major goal in the therapy for prostate hyperplasia and prostate cancer. Bioactivity-directed fractionation of a selective dichloromethane extract from the stem bark of Pygeum africanum led to the isolation of the antiandrogenic compound atraric acid. Its activity was examined by an androgen receptor responsive reporter gene assay. For lead structure optimization we transformed the natural occurring compound atraric acid into its ethyl, N-propyl and N-butyl esters and their antiandrogenic activities were examined as well. In addition, benzoic acid was isolated. The structures of all compounds were determined and characterized by means of 1H- and 13C-NMR, HR-EI-mass, IR and UV spectroscopy.

  13. Bonded-phase extraction column isolation of organic compounds in groundwater at a hazardous waste site

    USGS Publications Warehouse

    Rostad, C.E.; Pereira, W.E.; Ratcliff, S.M.

    1984-01-01

    A procedure for isolation of hazardous organic compounds from water for gas chromatography/mass spectrometry analysis Is presented and applied to creosote- and pentachlorophenol-contaminated groundwater resulting from wood-treatment processes. This simple procedure involved passing a 50-100-mL sample through a bonded-phase extraction column, eluting the trapped organic compounds from the column with 2-4 mL of solvent, and evaporating the sample to 100 ??L with a stream of dry nitrogen, after which the sample was ready for gas chromatography/mass spectrometry analysis. Representative compounds indicative of creosote contamination were used for recovery and precision studies from the cyclohexyl-bonded phase. Recovery of these compounds from n-octyl-, n-octadecyl-, cyclohexyl-, and phenyl-bonded phases was compared. The bonded phase that exhibited the best recovery and least bias toward acidic or basic cmpounds was the n-octadecyl phase. Detailed compound Identification Is given for compounds Isolated from creosote- and pentachlorophenol-contaminated groundwater using the cyclohexyl-bonded phase.

  14. Isolation and identification of aromatic compounds in Lion's Mane Mushroom and their anticancer activities.

    PubMed

    Li, Wei; Zhou, Wei; Kim, Eun-Ji; Shim, Sang Hee; Kang, Hee Kyoung; Kim, Young Ho

    2015-03-01

    Lion's Mane Mushroom (Hericium erinaceum) is a traditional edible mushroom widely used in culinary applications and as an herbal medicine in East Asian countries. In the present study, two new aromatic compounds, hericerin A (1) and isohericenone J (5), along with five known compounds, isoericerin (2), hericerin (3), N-De phenylethyl isohericerin (4), hericenone J (6), and 4-[3',7'-dimethyl-2',6'-octadienyl]-2-formyl-3-hydroxy-5-methyoxybenzylalcohol (7), were isolated from a methanol extract of the fruiting bodies of H. erinaceum. The chemical structures of the compounds were determined from mass spectra and 1D- and 2D NMR spectroscopy. The anticancer effects of the isolated compounds were examined in HL-60 human acute promyelocytic leukaemia cells. Hericerin A (1) and hericerin (3) significantly reduced cell proliferation with IC50 values of 3.06 and 5.47 μM, respectively. These same compounds also induced apoptosis of HL-60 cells, accompanied by time-dependent down-regulation of p-AKT and c-myc levels. These data suggest that compounds 1 and 3 from H. erinaceum are suitable for use in potential cancer treatments.

  15. Antifungal activity of schinol and a new biphenyl compound isolated from Schinus terebinthifolius against the pathogenic fungus Paracoccidioides brasiliensis

    PubMed Central

    2010-01-01

    Background The aim of this study was to isolate and identify the antifungal compounds from the extracts of Schinus terebinthifolius (Anacardiaceae) against clinical isolates of the pathogenic fungus Paracoccidioides brasiliensis. Methods The hexane and dichlomethane fractions from leaves and stems of S. terebinthifolius were fractionated using several chromatography techniques to afford four compounds. Results The compounds isolated from S. terebinthifolius were identified as schinol (1), a new biphenyl compound, namely, 4'-ethyl-4-methyl-2,2',6,6'-tetrahydroxy[1,1'-biphenyl]-4,4'-dicarboxylate (2), quercetin (3), and kaempferol (4). Compounds 1 and 2 were active against different strains of P. brasiliensis, showing a minimal inhibitory concentration value against the isolate Pb B339 of 15.6 μg/ml. The isolate Pb 1578 was more sensitive to compound 1 with a MIC value of 7.5 μg/ml. Schinol presented synergistic effect only when combined with itraconazole. The compounds isolated from S. terebinthifolius were not able to inhibit cell wall synthesis or assembly using the sorbitol assay. Conclusion This work reveals for the first time the occurrence of compound 2 and discloses activity of compounds 1 and 2 against several clinical isolates of P. brasiliensis. These results justify further studies to clarify the mechanisms of action of these compounds. PMID:20939907

  16. Sulfated phenolic compounds from Limonium caspium: Isolation, structural elucidation, and biological evaluation

    PubMed Central

    Gadetskaya, Anastassiya V.; Tarawneh, Amer H.; Zhusupova, Galiya E.; Gemejiyeva, Nadezhda G.; Cantrell, Charles L.; Cutler, Stephen J.; Ross, Samir A.

    2016-01-01

    Three new compounds, (2S,3S)-5-methyldihydromyricetin (1), (2S,3S)-5-methyldihydromyricetin-3′-O-sulfate (2) and β-D-glucopyranoside, 3-methyl, but-3-en-1-yl 4-O-α-L-rhamnopyranosyl (3) have been isolated from the Limonium caspium, together with dihydromyricetin (4), dihydromyricetin-3′-O-sulfate (5), myricetin-3′-O-sulfate (6), 5-methylmyricetin (7), myricetin (8), myricetin-3-O-β-glucoside (9), as well as phloridzin (10), and tyramine (11). Compounds 5 and 6 were isolated for the first time as acids. This is the first report of all these compounds from this plant. Their structures were established by extensive NMR studies (1H NMR, 13C NMR, DEPT, 1H–1H COSY, HSQC, HMBC) as well as HRESIMS. All isolated compounds were evaluated for their antibacterial, antifungal, antimalarial and antileishmanial activities. Compounds 7, 8 and 9 exhibited good antifungal activity against Candida glabrata with IC50 values of 6.79, 15.37 and 8.53 μg/mL, respectively. Compound 8 displayed significant antimalarial activity against resistant and sensitive strains of Plasmodium falciparum with IC50 values of 1.82 and 1.51 μg/mL, respectively. Compounds 1, 4, 6, 8 and 9 showed excellent activity against Trypanosoma brucei with IC50 values of 6.93, 9.65, 8.52, 7.67 and 6.31 μg/mL, respectively. To date, this is the first report on the phytochemical and biological activity of secondary metabolites from L. caspium. PMID:26025854

  17. Antidiabetes and Anti-obesity Activity of Lagerstroemia speciosa

    PubMed Central

    Klein, Guy; Kim, Jaekyung; Himmeldirk, Klaus; Cao, Yanyan

    2007-01-01

    The leaves of Lagerstroemia speciosa (Lythraceae), a Southeast Asian tree more commonly known as banaba, have been traditionally consumed in various forms by Philippinos for treatment of diabetes and kidney related diseases. In the 1990s, the popularity of this herbal medicine began to attract the attention of scientists worldwide. Since then, researchers have conducted numerous in vitro and in vivo studies that consistently confirmed the antidiabetic activity of banaba. Scientists have identified different components of banaba to be responsible for its activity. Using tumor cells as a cell model, corosolic acid was isolated from the methanol extract of banaba and shown to be an active compound. More recently, a different cell model and the focus on the water soluble fraction of the extract led to the discovery of other compounds. The ellagitannin Lagerstroemin was identified as an effective component of the banaba extract responsible for the activity. In a different approach, using 3T3-L1 adipocytes as a cell model and a glucose uptake assay as the functional screening method, Chen et al. showed that the banaba water extract exhibited an insulin-like glucose transport inducing activity. Coupling HPLC fractionation with a glucose uptake assay, gallotannins were identified in the banaba extract as components responsible for the activity, not corosolic acid. Penta-O-galloyl-glucopyranose (PGG) was identified as the most potent gallotannin. A comparison of published data with results obtained for PGG indicates that PGG has a significantly higher glucose transport stimulatory activity than Lagerstroemin. Chen et al. have also shown that PGG exhibits anti-adipogenic properties in addition to stimulating the glucose uptake in adipocytes. The combination of glucose uptake and anti-adipogenesis activity is not found in the current insulin mimetic drugs and may indicate a great therapeutic potential of PGG. PMID:18227906

  18. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata

    PubMed Central

    Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Clemente, Edmar

    2012-01-01

    Endophytic microorganisms, defined as fungi or bacteria that colonize the interior of plants without causing any immediate negative effects or damages, have reciprocal relationships with host plants. In some cases their presence is beneficial to the host due to the synthesis of bioactive compounds, among which several alcohols, esters, ketones and others that may react with other compounds and may be lethal to pathogenic microorganisms. Diaporthe helianthi (Phomopsis helianthi in its anamorphic phase) is available worldwide, especially in Europe, Asia and America. Isolated in Europe as an agent of the sunflower stem cancer, it has also been endophytically isolated from tropical and temperate plants. A D. helianthi strain isolated from Luehea divaricata has been employed in current research. An investigation of the secondary metabolite from D. helianthi by CC and NMR of 1H and 13C yielded the separation of 10 fractions and the identification of the phenolic compound 2(-4 hydroxyphenyl)-ethanol (Tyrosol). Its antimicrobial reaction was tested and the ensuing antagonistic effects on the human pathogenic bacteria Enterococcus hirae, Escherichia coli, Micrococcus luteus, Salmonella typhi, Staphylococcus aureus, phytopathogenic Xanthomonas asc. phaseoli and phytopathogenic fungi were demonstrated. Results show that bioactive compounds and Tyrosol produced by D. helianthi have a biotechnological potential. PMID:24031942

  19. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata.

    PubMed

    Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Clemente, Edmar

    2012-07-01

    Endophytic microorganisms, defined as fungi or bacteria that colonize the interior of plants without causing any immediate negative effects or damages, have reciprocal relationships with host plants. In some cases their presence is beneficial to the host due to the synthesis of bioactive compounds, among which several alcohols, esters, ketones and others that may react with other compounds and may be lethal to pathogenic microorganisms. Diaporthe helianthi (Phomopsis helianthi in its anamorphic phase) is available worldwide, especially in Europe, Asia and America. Isolated in Europe as an agent of the sunflower stem cancer, it has also been endophytically isolated from tropical and temperate plants. A D. helianthi strain isolated from Luehea divaricata has been employed in current research. An investigation of the secondary metabolite from D. helianthi by CC and NMR of (1)H and (13)C yielded the separation of 10 fractions and the identification of the phenolic compound 2(-4 hydroxyphenyl)-ethanol (Tyrosol). Its antimicrobial reaction was tested and the ensuing antagonistic effects on the human pathogenic bacteria Enterococcus hirae, Escherichia coli, Micrococcus luteus, Salmonella typhi, Staphylococcus aureus, phytopathogenic Xanthomonas asc. phaseoli and phytopathogenic fungi were demonstrated. Results show that bioactive compounds and Tyrosol produced by D. helianthi have a biotechnological potential. PMID:24031942

  20. Antioxidant activity and mechanisms of action of natural compounds isolated from lichens: a systematic review.

    PubMed

    White, Pollyanna A S; Oliveira, Rita C M; Oliveira, Aldeidia P; Serafini, Mairim R; Araújo, Adriano A S; Gelain, Daniel P; Moreira, Jose C F; Almeida, Jackson R G S; Quintans, Jullyana S S; Quintans-Junior, Lucindo J; Santos, Marcio R V

    2014-09-12

    Chronic diseases such as cancer, diabetes, neurodegenerative and cardiovascular diseases are characterized by an enhanced state of oxidative stress, which may result from the overproduction of reactive species and/or a decrease in antioxidant defenses. The search for new chemical entities with antioxidant profile is still thus an emerging field on ongoing interest. Due to the lack of reviews concerning the antioxidant activity of lichen-derived natural compounds, we performed a review of the antioxidant potential and mechanisms of action of natural compounds isolated from lichens. The search terms "lichens", "antioxidants" and "antioxidant response elements" were used to retrieve articles in LILACS, PubMed and Web of Science published until February 2014. From a total of 319 articles surveyed, 32 met the established inclusion and exclusion criteria. It was observed that the most common isolated compound studied was usnic acid, cited in 14 out of the 32 articles. The most often described antioxidant assays for the study of in vitro antioxidant activity were mainly DPPH, LPO and SOD. The most suggested mechanisms of action were scavenging of reactive species, enzymatic activation and inhibition of iNOS. Thus, compounds isolated from lichens are possible candidates for the management of oxidative stress, and may be useful in the treatment of chronic diseases.

  1. Antiinflammatory and Analgesic Activities of Ethanol Extract and Isolated Compounds from Millettia pulchra.

    PubMed

    Huo, Xiaowei; Zhang, Leilei; Gao, Li; Guo, Yan; Zhang, Lijing; Li, Liyong; Si, Jianyong; Cao, Li

    2015-01-01

    The plant Millettia pulchra was commonly used in folk medicine for the management of inflammation. However, there was no scientific rationale for these effects and the mechanism of action remained incompletely understood. The present study was designed to investigate the antiinflammatory and analgesic activities of an ethanol extract of the stem of M. pulchra (EMP) in vivo, and to explore the antiinflammatory activity of compounds isolated from EMP in vitro. We found that EMP reduced xylene-induced ear edema and relieved both acetic acid-induced pain and pain in the hot plate test. Additionally, a significant decrease in nitric oxide (NO) production was observed in cells treated with the isolated compounds. Lanceolatin B, which showed the greatest inhibition of NO synthesis among the compounds tested, also reduced levels of interleukin-1 beta (IL-1β), IL-6, tumor necrosis factor-alpha (TNF-α), cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), nuclear factor-kappa B (NF-κB), and phosphorylation inhibitory kappa B alpha (p-IκBα) in a dose-dependent manner. These findings provide convincing evidence that EMP and the individual isolated compounds possess significant antiinflammatory and analgesic activities. PMID:26062514

  2. Anti-inflammatory effects of phenolic compounds isolated from the flowers of Nymphaea mexicana Zucc.

    PubMed

    Hsu, Chin-Lin; Fang, Song-Chwan; Yen, Gow-Chin

    2013-08-01

    Nymphaea mexicana Zucc. is an aquatic plant species which belongs to the family Nymphaea and is commonly known as the yellow water lily. The aim of this work was to study the in vitro antiinflammatory effects of phenolic compounds isolated from the flowers of Nymphaea mexicana Zucc. Seven phenolic compounds including vanillic acid, 4-methoxy-3,5-dihydroxybenzoic acid, (2R,3R)-3,7-dihydroxyflavanone, naringenin (4), kaempferol 3-O-(3-O-acetyl-a-L-rhamnopyranoside), kaempferol 3-O-(2-O-acetyl-a-L-rhamnopyranoside), and quercetin 3-(30 0-acetylrhamnoside) (7) were isolated from the flowers of Nymphaea mexicana Zucc. These results revealed that compound 4 has the most prominent inhibitory effect on the LPS-stimulated nitric oxide (NO), monocyte chemotactic protein-1 (MCP-1), and tumor necrosis factor-alpha (TNF-a) production in RAW 264.7 macrophages. In addition, compound 4 also inhibited LPS-mediated induction of protein expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2), and phospho-ERK in RAW 264.7 macrophages. Thus, compound 4 from the flowers of Nymphaea mexicana Zucc. may provide a potential therapeutic approach for inflammation-associated disorders.

  3. Anti-inflammatory effects of phenolic compounds isolated from the flowers of Nymphaea mexicana Zucc.

    PubMed

    Hsu, Chin-Lin; Fang, Song-Chwan; Yen, Gow-Chin

    2013-08-01

    Nymphaea mexicana Zucc. is an aquatic plant species which belongs to the family Nymphaea and is commonly known as the yellow water lily. The aim of this work was to study the in vitro antiinflammatory effects of phenolic compounds isolated from the flowers of Nymphaea mexicana Zucc. Seven phenolic compounds including vanillic acid, 4-methoxy-3,5-dihydroxybenzoic acid, (2R,3R)-3,7-dihydroxyflavanone, naringenin (4), kaempferol 3-O-(3-O-acetyl-a-L-rhamnopyranoside), kaempferol 3-O-(2-O-acetyl-a-L-rhamnopyranoside), and quercetin 3-(30 0-acetylrhamnoside) (7) were isolated from the flowers of Nymphaea mexicana Zucc. These results revealed that compound 4 has the most prominent inhibitory effect on the LPS-stimulated nitric oxide (NO), monocyte chemotactic protein-1 (MCP-1), and tumor necrosis factor-alpha (TNF-a) production in RAW 264.7 macrophages. In addition, compound 4 also inhibited LPS-mediated induction of protein expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2), and phospho-ERK in RAW 264.7 macrophages. Thus, compound 4 from the flowers of Nymphaea mexicana Zucc. may provide a potential therapeutic approach for inflammation-associated disorders. PMID:23727892

  4. In vitro Cytotoxic Activities and Molecular Mechanisms of Angelica shikokiana Extract and its Isolated Compounds

    PubMed Central

    Mira, Amira; Shimizu, Kuniyoshi

    2015-01-01

    Background: Angelica shikokiana is a Japanese medicinal herb that is included among food and drug preparations protecting against cancer; however, there is no previous report about the cytotoxicity of A. shikokiana or its bioactive compounds. Objective: This study was designed to investigate the cytotoxic activities of A. shikokiana methanol extract (AME) and its isolated compounds and to identify the molecular mechanisms of the cytotoxicity. Materials and Methods: Cytotoxicity and selectivity was investigated by measuring the IC50 values on five cancer cell lines; human hepatocellular carcinoma, rhabdomyosarcoma (RD), colorectal carcinoma, human epithelioma and human breast adenocarcinoma and one normal cell line; human lung fibroblasts. The effects on tubulin polymerization and histone deacetylase 8 (HDAC8), were examined to determine the mechanism of cytotoxicity. Docking study was designed to examine the binding affinity to the target molecules. Results: Methanol extract and some of its isolated coumarins and flavonoids showed potent, selective cytotoxicity against cancer cell lines. AME and all isolated compounds inhibited tubulin polymerization. Angelicin and kaempferol-3-O-rutinoside were the most active compounds. Phenolic compounds and furanocoumarins showed binding affinity to colchicine binding site rather than the vinblastine binding site of tubulin microtubules. On the other side, quercetin, kaempferol, luteolin, chlorogenic acid, and methyl chlorogenate exhibited the strongest activity against HDAC8 and the highest affinity to trichostatin A binding site. Conclusion: These findings provide the first scientific evidence of the cytotoxicity of AME through inhibition of tubulin polymerization and HDAC8 activity through its coumarin and flavonoid content. SUMMARY The present study provides for the first time a clue for the cytotoxic activities of the AME. Our results indicate that the cytotoxic activities are partially related to the ability of AME to

  5. Isolation and Identification of Vesicular-Arbuscular Mycorrhiza-Stimulatory Compounds from Clover (Trifolium repens) Roots

    PubMed Central

    Nair, Muraleedharan G.; Safir, Gene R.; Siqueira, Jose O.

    1991-01-01

    Two isoflavonoids isolated from clover roots grown under phosphate stress were characterized as formononetin (7-hydroxy,4′-methoxy isoflavone) and biochanin A (5,7-dihydroxy,4′-methoxy isoflavone). At 5 ppm, these compounds stimulated hyphal growth in vitro and root colonization of an undescribed vesicular-arbuscular mycorrhiza, a Glomus sp. (INVAM-112). The permethylated products of the two compounds were inactive. These findings suggest that the isoflavonoids studied may act as signal molecules in vesicular-arbuscular mycorrhiza symbiosis. PMID:16348409

  6. Determination of the antibacterial activity of crude extracts and compounds isolated from Hortia oreadica (Rutaceae) against oral pathogens

    PubMed Central

    Severino, Vanessa Gisele Pasqualotto; da Silva, Maria Fátima das Graças Fernandes; Lucarini, Rodrigo; Montanari, Lilian Bueno; Cunha, Wilson Roberto; Vinholis, Adriana Helena Chicharo; Martins, Carlos Henrique Gomes

    2009-01-01

    Extracts from Hortia oreadica afforded four dihydrocinnamic acid derivatives, isolated from the n-hexane extract, as well as limonoid guyanin and the furoquinoline alkaloid dictamnine, both isolated from the dichloromethane extract. The extracts and the isolated compounds were tested against some oral pathogens, so as to investigate their antibacterial activity. The results showed that the n-hexane extract and the compound dictamnine are the most active against the selected microorganisms PMID:24031396

  7. Isolation and antimicrobial activity of two phenolic compounds from Pulicaria odora L.

    PubMed

    Ezoubeiri, A; Gadhi, C A; Fdil, N; Benharref, A; Jana, M; Vanhaelen, M

    2005-06-01

    The essential oil of Pulicaria odora, a Moroccan medicinal plant; was analyzed by GC-MS, and subjected to column chromatography on silica gel. Two major constituents were isolated and identified as 2-isopropyl-4-methylphenol (1) and isobutyric acid 2-isopropyl-4-methylphenylester (2), by analysis of spectroscopic data (MS, 1H NMR, 13C NMR, DEPT, COSY, HMQC and HMBC experiments). The isolated compounds are reported for the first time from Pulicaria genus. The essential oil and its major constituents (compounds 1 and 2) were examined for antibacterial and antifungal activity in vitro using the diffusion and dilution methods. Results showed that the essential oil and the 2-isopropyl-4-methylphenol (1) exhibited a very significant antibacterial and antifungal activity, while the isobutyric acid 2-isopropyl-4-methylphenylester (2) was inactive for all tested strains.

  8. Isolation and structural elucidation of a new cyclohexenone compound from Lasiodiplodia theobromae.

    PubMed

    Kitaoka, Naoki; Nabeta, Kensuke; Matsuura, Hideyuki

    2009-08-01

    A new cyclohexenone compound was isolated as a mixture of enantiomers from a culture filtrate of Lasiodiplodia theobromae. The relative structure was determined to be 4,5-dihydroxy-3-methyl-cyclohex-2-enone on the basis of MS, (1)H-NMR, and (13)C-NMR spectroscopic analyses, including 2D-NMR experiments. Resolution of the enantiomers was conducted by a coupling reaction with (S)-MTPA-Cl followed by HPLC separation. PMID:19661717

  9. Isolation of natural compounds from Phlomis stewartii showing α-glucosidase inhibitory activity.

    PubMed

    Jabeen, Bushra; Riaz, Naheed; Saleem, Muhammad; Naveed, Muhammad Akram; Ashraf, Muhammad; Alam, Umber; Rafiq, Hafiza Mehwish; Tareen, Rasool Bakhsh; Jabbar, Abdul

    2013-12-01

    Stewartiiside (1), a phenylethanoid glycoside and three 28-nortriterpenoids: stewertiisins A-C [(17R)-19(18→17)-abeo-3α,18β,23,24-tetrahydroxy-28-norolean-12-ene, 2; (17R)-19(18→17)-abeo-2α,16β,18β,23,24-pentahydroxy-28-norolean-12-en-3-one, 3; (17R)-19(18→17)-abeo-2α,3α,23,24-tetrahydroxy-28-noroleane-11,13-diene, 4] together with eight known compounds: lunariifolioside (5), notohamosin A (6), phlomispentanol (7), isorhamnetin 3-(6-p-coumaroyl)-β-D-glucopyranoside (8), tiliroside (9), caffeic acid (10), p-hydrxybenzoic acid (11) and oleanolic acid (12) were isolated from the ethyl acetate soluble fraction of the methanolic extract of whole plant of Phlomis stewartii. The structures of these isolates (1-12) were elucidated by the combination of 1D ((1)H and (13)C NMR), 2D (HMQC, HMBC COSY, NOESY) NMR spectroscopy and mass spectrometry (EIMS, HREIMS, FABMS, HRFABMS) and in comparison with literature data of related compounds. All the isolates (1-12) showed α-glucosidase inhibitory activity with IC50 values ranging between 14.5 and 355.4 μM, whereas, compounds 1, 5, 9 and 10 showed promising α-glucosidase inhibitory activity with IC50 values below 30 μM.

  10. Purification and characterization of antifungal compounds from Lactobacillus plantarum HD1 isolated from kimchi.

    PubMed

    Ryu, Eun Hye; Yang, Eun Ju; Woo, Eun Rhan; Chang, Hae Choon

    2014-08-01

    Strain HD1 with antifungal activity was isolated from kimchi and identified as Lactobacillus plantarum. Antifungal compounds from Lb. plantarum HD1 were active against food- and feed-borne filamentous fungi and yeasts in a spot-on-the-lawn assay. Antifungal activity of Lb. plantarum HD1 was stronger against filamentous fungi than yeast. Antifungal compounds were purified using solid phase extraction (SPE) and recycling preparative-HPLC. Structures of the antifungal compounds were elucidated by electrospray ionization-mass spectrometry and nuclear magnetic resonance. Active compounds from Lb. plantarum HD1 were identified as 5-oxododecanoic acid (MW 214), 3-hydroxy decanoic acid (MW 188), and 3-hydroxy-5-dodecenoic acid (MW 214). To investigate the potential application of these antifungal compounds for reduction of fungal spoilage in foods, Korean draft rice wine was used as a food model. White film-forming yeasts were observed in control draft rice wine after 11 days of incubation. However, film-forming yeasts were not observed in draft rice wine treated with SPE-prepared culture supernatant of Lb. plantarum HD1 (equivalent to 2.5% addition of culture supernatant) until 27 days of incubation. The addition of antifungal compounds to Korean draft rice wine extended shelf-life up to 27 days at 10 °C without any sterilization process. Therefore, the antifungal activity of Lb. plantarum HD1 may lead to the development of powerful biopreservative systems capable of preventing food- and feed-borne fungal spoilage.

  11. Isolation, partial purification and evaluation of bioactive compounds from leaves of Ageratum houstonianum

    PubMed Central

    Zeeshan, M.; Rizvi, S.M.D.; Khan, M.S.; Kumar, A.

    2012-01-01

    The present study deals with the isolation and partial purification of bioactive compounds from the crude methanol extracts of the leaves of Ageratum houstonianum (Asteraceae). The quantification and the identification of compounds in the crude extract and active bands isolated by preparative TLC were accomplished using GC-MS analysis. The most important compounds identified in the crude extract and active bands (AB-1 and AB-2) were 6-acetyl-7-methoxy-2, 2-dimethylchromene, hexadecanoic acid and squalene, respectively. Crude extract and active bands (AB-1 and AB-2) were investigated for their antibacterial activity against Staphylococcus epidermidis, Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, and Pseudomonas aeruginosa. The crude extract, AB-1 and AB-2 showed maximum zone of inhibition (10-13 mm) against Staphylococcus epidermidis, however, the antibacterial potential of active bands was slightly higher as compared to the crude extract. Dose-dependant increase in antioxidant potential was noticed in crude extract as well as with both active bands measured by DPPH free radicals, ion chelation and total antioxidants capacity. Our study reports various bioactive compounds in the leaves of the A. houstonianum with significant antioxidant and antibacterial potential. PMID:27350770

  12. Anti-inflammatory effects of phenolic compounds isolated from the fruits of Artocarpus heterophyllus.

    PubMed

    Fang, Song-Chwan; Hsu, Chin-Lin; Yen, Gow-Chin

    2008-06-25

    Artocarpus heterophyllus Lam is a large evergreen tree cultivated throughout Southeast Asia for its fruits. Its leaves and roots have been used for medicinal purposes. The aim of this work was to study the in vitro anti-inflammatory effects of phenolic compounds isolated from the ethyl acetate extracts of the fruits of Artocarpus heterophyllus. Three phenolic compounds were characterized as artocarpesin [5,7,2',4'-tetrahydroxy-6-(3-methylbut-3-enyl) flavone] ( 1), norartocarpetin (5,7,2',4'-tetrahydroxyflavone) ( 2), and oxyresveratrol [ trans-2,4,3',5'-tetrahydroxystilbene] ( 3) by spectroscopic methods and through comparison with data reported in the literatures. The anti-inflammatory effects of the isolated compounds ( 1- 3) were evaluated by determining their inhibitory effects on the production of proinflammatory mediators in lipopolysaccharide (LPS)-activated RAW 264.7 murine macrophage cells. These three compounds exhibited potent anti-inflammatory activity. The results indicated that artocarpesin ( 1) suppressed the LPS-induced production of nitric oxide (NO) and prostaglandin E 2 (PGE 2) through the down-regulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) protein expressions. Thus, artocarpesin ( 1) may provide a potential therapeutic approach for inflammation-associated disorders.

  13. Anti-inflammatory effects of phenolic compounds isolated from the fruits of Artocarpus heterophyllus.

    PubMed

    Fang, Song-Chwan; Hsu, Chin-Lin; Yen, Gow-Chin

    2008-06-25

    Artocarpus heterophyllus Lam is a large evergreen tree cultivated throughout Southeast Asia for its fruits. Its leaves and roots have been used for medicinal purposes. The aim of this work was to study the in vitro anti-inflammatory effects of phenolic compounds isolated from the ethyl acetate extracts of the fruits of Artocarpus heterophyllus. Three phenolic compounds were characterized as artocarpesin [5,7,2',4'-tetrahydroxy-6-(3-methylbut-3-enyl) flavone] ( 1), norartocarpetin (5,7,2',4'-tetrahydroxyflavone) ( 2), and oxyresveratrol [ trans-2,4,3',5'-tetrahydroxystilbene] ( 3) by spectroscopic methods and through comparison with data reported in the literatures. The anti-inflammatory effects of the isolated compounds ( 1- 3) were evaluated by determining their inhibitory effects on the production of proinflammatory mediators in lipopolysaccharide (LPS)-activated RAW 264.7 murine macrophage cells. These three compounds exhibited potent anti-inflammatory activity. The results indicated that artocarpesin ( 1) suppressed the LPS-induced production of nitric oxide (NO) and prostaglandin E 2 (PGE 2) through the down-regulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) protein expressions. Thus, artocarpesin ( 1) may provide a potential therapeutic approach for inflammation-associated disorders. PMID:18500810

  14. Isolation and identification of plant phenolic compounds in birch leaves: Air pollution stress and leaf phenolics

    NASA Astrophysics Data System (ADS)

    Loponen, Jyrki Mikael

    Chromatographic (analytical and preparative HPLC), chemical (hydrolysis) and spectroscopic (UV, 1H NMR, 13C NMR and MS) techniques proved to be suitable tools for the structure identification of plant phenolic compounds. More than 30 individual phenolic compounds were detected and quantified. Detailed information of the structures of individual compounds was determined after isolation from birch leaves. Ten flavonoid glycosides were identified. Two of them, myricetin-3-O-α-L-(acetyl)-rhamnopyranoside and quercetin-3-O-α-L-(4/prime'-O-acetyl)- rhamnopyranoside, have been rarely found in birch leaves. Further, some characterized major phenolics with non- flavonoid structures in our study were 1-O-galloyl- β-D-(2-O-acetyl)-glucopyranose, gallic, chlorogenic, neochlorogenic, cis- and trans-forms of 3- and 5-p-coumaroylquinic acids. The presence of gallotannin group was evidenced by strong positive correlations between concentrations of these gallotannins (preliminary identified by HPLC and UV spectra) and the protein precipitation capacity of extracts. Content of gallotannins decreased with leaf growth and maturation. It is known that concentrations of phenolic compounds regularly increase in slowly growing stressed plants and therefore, it is natural that they are also sensitive to different forms of air pollution. Total content and the contents of some individual phenolics correlated negatively with the distance from the pollution source in our study area. In addition to comparing absolute concentrations of compounds in question, the within-tree correlations or within-tree variations of the relevant compounds between polluted and control areas were an alternative approach. Differences in pairwise correlations between the investigated leaf phenolic compounds indicated the competition between some gallotannins and p-coumaroylquinic acids on the polluted but not on the control site. Air pollution seems to be a stress factor for birch trees associated with

  15. Inhibition effects of isolated compounds from Artemisia rubripes Nakai of the classical pathway on the complement system.

    PubMed

    Jung, Seil; Lee, Jai-Heon; Lee, Young-Choon; Moon, Hyung-In

    2012-04-01

    The study evaluated the anticomplement activity from isolated compounds from Artemisia rubripes Nakai from South Korea on the classical pathway. In the previous works, Artemisia rubripes chloroform extracts showed inhibitory activity against complement system. The chromatographic separation of a chloroform chloride extract of Artemisia rubripes led to the isolation of three compounds. Their structures were characterized to be scopoletin (1), 11,(13)-triene-6,12-olide (2), and 1β,6α-dihydroxy-4(15)-eudesmene (3) by spectroscopic data. This is the first report of anticomplement activity of isolated compounds from Artemisia rubripes.

  16. Isolation of cholinesterase and β-secretase 1 inhibiting compounds from Lycopodiella cernua.

    PubMed

    Nguyen, Van Thu; To, Dao Cuong; Tran, Manh Hung; Oh, Sang Ho; Kim, Jeong Ah; Ali, Md Yousof; Woo, Mi-Hee; Choi, Jae Sue; Min, Byung Sun

    2015-07-01

    Three new serratene-type triterpenoids (1-3) and a new hydroxy unsaturated fatty acid (13) together with nine known compounds (4-12) were isolated from Lycopodiella cernua. The chemical structures were established using NMR, MS, and Mosher's method. Compound 13 showed the most potent inhibitory activity against acetylcholinesterase (AChE) with an IC50 value of 0.22μM. For butyrylcholinesterase (BChE) inhibitory activity, 5 showed the most potent activity with an IC50 value of 0.42μM. Compound 2 showed the most potent activity with an IC50 of 0.23μM for BACE-1 inhibitory activity. The kinetic activities were investigated to determine the type of enzyme inhibition involved. The types of AChE inhibition shown by compounds 4, 5, and 13 were mixed; BChE inhibition by 5 was competitive, while 2 and 6 showed mixed-types. In addition, molecular docking studies were performed to investigate the interaction of these compounds with the pocket sites of AChE. The docking results revealed that the tested inhibitors 3, 4, and 13 were stably present in several pocket domains of the AChE residue. PMID:26003344

  17. Identification of PPARgamma Partial Agonists of Natural Origin (II): In Silico Prediction in Natural Extracts with Known Antidiabetic Activity

    PubMed Central

    Guasch, Laura; Sala, Esther; Mulero, Miquel; Valls, Cristina; Salvadó, Maria Josepa; Pujadas, Gerard; Garcia-Vallvé, Santiago

    2013-01-01

    Background Natural extracts have played an important role in the prevention and treatment of diseases and are important sources for drug discovery. However, to be effectively used in these processes, natural extracts must be characterized through the identification of their active compounds and their modes of action. Methodology/Principal Findings From an initial set of 29,779 natural products that are annotated with their natural source and using a previously developed virtual screening procedure (carefully validated experimentally), we have predicted as potential peroxisome proliferators-activated receptor gamma (PPARγ) partial agonists 12 molecules from 11 extracts known to have antidiabetic activity. Six of these molecules are similar to molecules with described antidiabetic activity but whose mechanism of action is unknown. Therefore, it is plausible that these 12 molecules could be the bioactive molecules responsible, at least in part, for the antidiabetic activity of the extracts containing them. In addition, we have also identified as potential PPARγ partial agonists 10 molecules from 16 plants with undescribed antidiabetic activity but that are related (i.e., they are from the same genus) to plants with known antidiabetic properties. None of the 22 molecules that we predict as PPARγ partial agonists show chemical similarity with a group of 211 known PPARγ partial agonists obtained from the literature. Conclusions/Significance Our results provide a new hypothesis about the active molecules of natural extracts with antidiabetic properties and their mode of action. We also suggest plants with undescribed antidiabetic activity that may contain PPARγ partial agonists. These plants represent a new source of potential antidiabetic extracts. Consequently, our work opens the door to the discovery of new antidiabetic extracts and molecules that can be of use, for instance, in the design of new antidiabetic drugs or functional foods focused towards the

  18. Isolation of phenolic compounds from iceberg lettuce and impact on enzymatic browning.

    PubMed

    Mai, Franziska; Glomb, Marcus A

    2013-03-20

    Enzymatic browning is generally reported as the reaction between phenolic substances and enzymes. The quality of iceberg lettuce is directly linked to this discoloration. In particular, the color change of lettuce stems considerably reduces consumer acceptance and thus decreases sales revenue of iceberg lettuce. Ten phenolic compounds (caffeic acid, chlorogenic acid, phaseolic acid, chicoric acid, isochlorogenic acid, luteolin-7-O-glucuronide, quercetin-3-O-glucuronide, quercetin-3-O-galactoside, quercetin-3-O-glucoside, and quercetin-3-O-(6″-malonyl)-glucoside) were isolated from Lactuca sativa var. capitata by multilayer countercurrent chromatography (MLCCC) and preparative high-performance liquid chromatography (HPLC). In addition, syringin was identified for the first time in iceberg lettuce. This polyphenolic ingredient was previously not mentioned for the family of Cichorieae in general. The purity and identity of isolated compounds were confirmed by different NMR experiments, HPLC-DAD-MS, and HR-MS techniques. Furthermore, the relationship between discoloration of iceberg lettuce and enzymatic browning was thoroughly investigated. Unexpectedly, the total concentration of phenolic compounds and the activity of polyphenol oxidase were not directly related to the browning processes. Results of model incubation experiments of plant extract solutions led to the conclusion that in addition to the typical enzymatic browning induced by polyphenol oxidases, further mechanisms must be involved to explain total browning of lettuce.

  19. Isolation and identification of compounds responsible for antioxidant capacity of Euryale ferox seeds.

    PubMed

    Song, Chang-Wei; Wang, Shu-Mei; Zhou, Li-Li; Hou, Fan-Fan; Wang, Kai-Jin; Han, Quan-Bin; Li, Ning; Cheng, Yong-Xian

    2011-02-23

    Euryale ferox seed is consumed medicinally or for food in China. The present study revealed it to contain significant antioxidant activity, which may be associated with its medical applications as a proteinuria inhibitor of diabetic nephropathy. This study resulted in the identification of 3 new sesquineolignans, named euryalins A-C (1-3), and 16 known compounds, which were all first isolated from this plant apart from 5,7,4-trihydroxy-flavanone. The antioxidant potential of the partial isolates was evaluated using the DPPH radical scavenging assay and mesangial cellular assay. Compounds 2, rel-(2α,3β)-7-O-methylcedrusin (4), syringylglycerol-8-O-4-(sinapyl alcohol) ether (5), and (+)-syringaresinol (7) were found to be most active on DPPH assay, whereas compounds 2, 4, 7, (1R,2R,5R,6S)-2-(3,4-dimethoxyphenyl)-6-(3,4-dihydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane, and buddlenol E could significantly inhibit high glucose-stimulated reactive oxygen species production in mesangial cells. The results suggested that E. ferox seed could be considered as an excellent source of natural antioxidants and is useful in the prevention of diabetic nephropathy.

  20. Isolation and identification of compounds responsible for antioxidant capacity of Euryale ferox seeds.

    PubMed

    Song, Chang-Wei; Wang, Shu-Mei; Zhou, Li-Li; Hou, Fan-Fan; Wang, Kai-Jin; Han, Quan-Bin; Li, Ning; Cheng, Yong-Xian

    2011-02-23

    Euryale ferox seed is consumed medicinally or for food in China. The present study revealed it to contain significant antioxidant activity, which may be associated with its medical applications as a proteinuria inhibitor of diabetic nephropathy. This study resulted in the identification of 3 new sesquineolignans, named euryalins A-C (1-3), and 16 known compounds, which were all first isolated from this plant apart from 5,7,4-trihydroxy-flavanone. The antioxidant potential of the partial isolates was evaluated using the DPPH radical scavenging assay and mesangial cellular assay. Compounds 2, rel-(2α,3β)-7-O-methylcedrusin (4), syringylglycerol-8-O-4-(sinapyl alcohol) ether (5), and (+)-syringaresinol (7) were found to be most active on DPPH assay, whereas compounds 2, 4, 7, (1R,2R,5R,6S)-2-(3,4-dimethoxyphenyl)-6-(3,4-dihydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane, and buddlenol E could significantly inhibit high glucose-stimulated reactive oxygen species production in mesangial cells. The results suggested that E. ferox seed could be considered as an excellent source of natural antioxidants and is useful in the prevention of diabetic nephropathy. PMID:21280632

  1. Isolation of phenolic compounds from iceberg lettuce and impact on enzymatic browning.

    PubMed

    Mai, Franziska; Glomb, Marcus A

    2013-03-20

    Enzymatic browning is generally reported as the reaction between phenolic substances and enzymes. The quality of iceberg lettuce is directly linked to this discoloration. In particular, the color change of lettuce stems considerably reduces consumer acceptance and thus decreases sales revenue of iceberg lettuce. Ten phenolic compounds (caffeic acid, chlorogenic acid, phaseolic acid, chicoric acid, isochlorogenic acid, luteolin-7-O-glucuronide, quercetin-3-O-glucuronide, quercetin-3-O-galactoside, quercetin-3-O-glucoside, and quercetin-3-O-(6″-malonyl)-glucoside) were isolated from Lactuca sativa var. capitata by multilayer countercurrent chromatography (MLCCC) and preparative high-performance liquid chromatography (HPLC). In addition, syringin was identified for the first time in iceberg lettuce. This polyphenolic ingredient was previously not mentioned for the family of Cichorieae in general. The purity and identity of isolated compounds were confirmed by different NMR experiments, HPLC-DAD-MS, and HR-MS techniques. Furthermore, the relationship between discoloration of iceberg lettuce and enzymatic browning was thoroughly investigated. Unexpectedly, the total concentration of phenolic compounds and the activity of polyphenol oxidase were not directly related to the browning processes. Results of model incubation experiments of plant extract solutions led to the conclusion that in addition to the typical enzymatic browning induced by polyphenol oxidases, further mechanisms must be involved to explain total browning of lettuce. PMID:23473017

  2. Antimicrobial compounds produced by Actinomadura sp. AC104 isolated from an Algerian Saharan soil.

    PubMed

    Badji, B; Zitouni, A; Mathieu, F; Lebrihi, A; Sabaou, N

    2006-04-01

    During a search for nonpolyenic antifungal antibiotics, an actinomycete designated AC104 was isolated from a Saharan soil sample by a dilution agar plating method using a chitin - vitamins B medium supplemented with rifampicin. Isolate AC104 presented the morphological and the chemical characteristics of the genus Actinomadura. On the basis of 76 physiological tests and 16S rDNA analysis, this isolate was determined to be quite different from the known species of Actinomadura. It is active against filamentous fungi and both Gram-positive and Gram-negative bacteria. The production of antibiotic substances was investigated using several culture media. The highest antimicrobial activities were obtained on ISP2 medium. The benzenic extract contained five bioactive spots detected on thin layer chromatography plates. Among these antibiotics, a complex called 104A, which showed the more interesting antifungal activity, was selected and purified by reverse-phase high-pressure liquid chromatography. This complex is composed of four compounds. Ultraviolet-visible, infrared, mass, and 1H nuclear magnetic resonance spectroscopy studies showed that these molecules contain an aromatic ring substituted by aliphatic chains. These compounds differ from the known antibiotics produced by Actinomadura species.

  3. In vitro screening of compounds against laboratory and field isolates of human hookworm reveals quantitative differences in anthelmintic susceptibility.

    PubMed

    Treger, Rebecca S; Otchere, Joseph; Keil, Martin F; Quagraine, Josephine E; Rai, Ganesha; Mott, Bryan T; Humphries, Debbie L; Wilson, Michael; Cappello, Michael; Vermeire, Jon J

    2014-01-01

    A panel of 80 compounds was screened for anthelmintic activity against a laboratory strain of Ancylostoma ceylanicum and field isolates of hookworm obtained from school children in the Kintampo North District of the Brong Ahafo Region of Ghana. Although the laboratory strain of A. ceylanicum was more susceptible to the compounds tested than the field isolates of hookworm, a twofold increase in compound concentration resulted in comparable egg hatch percent inhibition for select compounds. These data provide evidence that the efficacy of anthelmintic compounds may be species-dependent and that field and laboratory strains of hookworm differ in their sensitivities to the anthelmintics tested. These data also suggest that both compound concentration and hookworm species must be considered when screening to identify novel anthelmintic compounds.

  4. In vitro Screening of Compounds against Laboratory and Field Isolates of Human Hookworm Reveals Quantitative Differences in Anthelmintic Susceptibility

    PubMed Central

    Treger, Rebecca S.; Otchere, Joseph; Keil, Martin F.; Quagraine, Josephine E.; Rai, Ganesha; Mott, Bryan T.; Humphries, Debbie L.; Wilson, Michael; Cappello, Michael; Vermeire, Jon J.

    2014-01-01

    A panel of 80 compounds was screened for anthelmintic activity against a laboratory strain of Ancylostoma ceylanicum and field isolates of hookworm obtained from school children in the Kintampo North District of the Brong Ahafo Region of Ghana. Although the laboratory strain of A. ceylanicum was more susceptible to the compounds tested than the field isolates of hookworm, a twofold increase in compound concentration resulted in comparable egg hatch percent inhibition for select compounds. These data provide evidence that the efficacy of anthelmintic compounds may be species-dependent and that field and laboratory strains of hookworm differ in their sensitivities to the anthelmintics tested. These data also suggest that both compound concentration and hookworm species must be considered when screening to identify novel anthelmintic compounds. PMID:24297811

  5. Antidiabetic properties of germinated brown rice: a systematic review.

    PubMed

    Imam, Mustapha Umar; Azmi, Nur Hanisah; Bhanger, Muhammad Iqbal; Ismail, Norsharina; Ismail, Maznah

    2012-01-01

    Diet is an important variable in the course of type 2 diabetes, which has generated interest in dietary options like germinated brown rice (GBR) for effective management of the disease among rice-consuming populations. In vitro data and animal experiments show that GBR has potentials as a functional diet for managing this disease, and short-term clinical studies indicate encouraging results. Mechanisms for antidiabetic effects of GBR due to bioactive compounds like γ-aminobutyric acid (GABA), γ-oryzanol, dietary fibre, phenolics, vitamins, acylated steryl β-glucoside, and minerals include antihyperglycemia, low insulin index, antioxidative effect, antithrombosis, antihypertensive effect, hypocholesterolemia, and neuroprotective effects. The evidence so far suggests that there may be enormous benefits for diabetics in rice-consuming populations if white rice is replaced with GBR. However, long-term clinical studies are still needed to verify these findings on antidiabetic effects of GBR. Thus, we present a review on the antidiabetic properties of GBR from relevant preclinical and clinical studies, in order to provide detailed information on this subject for researchers to review the potential of GBR in combating this disease.

  6. Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan.

    PubMed

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

    2015-01-22

    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.

  7. 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

  8. Anti-diabetic effect of a traditional Chinese medicine formula.

    PubMed

    Wang, Hsiu-Ju; Chiang, Been-Huang

    2012-11-01

    An anti-diabetic TCM formula consisting of Schizandra chinensis Baill. (SC), Coptis chinensis (CC), Psidium guajava L. leaves (PG) and Morus alba L. leaves (MA) was developed based on its α-glucosidase, DPP-4 and AGE inhibitory activities in vitro using response surface methodology (RSM). Then, the in vivo study was carried out to confirm the anti-diabetic function of the formula. RSM results showed that the optimum anti-diabetic TCM formula is the combination SC (3000 μg mL(-1)), CC (80 μg mL(-1)), PG (374.56 μg mL(-1)) and MA (480 μg mL(-1)). For the in vivo study, insulin resistant mice were induced by high-fat/high-sucrose (HF/HS) feeding for 6 weeks. Administration of the developed formula significantly decreased non-fasting blood glucose in the HF/HS diet mice. Moreover, the formula decreased blood glucose levels in the insulin tolerance test. These results indicated that the anti-diabetic mechanism of the formula might be due to decreased insulin resistance. The serum fructosamine level in the high dose group was significantly lower than the HF/HS and normal control groups, indicating that the formula could improve middle term glucose levels and reduce the risk of complications. The contents of berberine and 1-deoxynojirimycin in the formula were 4.7 ± 0.4 and 77.1 ± 1.1 μg mL(-1), respectively. These two compounds can be used as indicators for quality control during production. PMID:22899105

  9. Bioactivity-guided isolation of new antiproliferative compounds from Juniperus foetidissima Willd.

    PubMed

    Rafieian-Kopaei, Mahmood; Suleimani Dehkordi, Ibrahim; Ghanadian, Mustafa; Shokrollahi, Ardeshir; Aghaei, Mahmoud; Syed Majid, Ayatollahi; Choudhary, M Iqbal

    2016-09-01

    Based on a literature survey on cytotoxic medicinal plants, Juniper species were identified as interesting source of antitumor compounds. Using bioassay-guided fractionation against Caov-4 cancer cells on acetone extract of leaves and branchlets of Juniperus foetidissima led to the isolation of a new 3H-benzofuaran-2-one: 4-methyl-3-methoxy-3H-benzofuaran-2-one (1), a new sesquiterpene: 4,9(α)-dihydroxy-nardosin-6-en (2) and an already known labdane-type diterpene: 15-hydroxy-8(17),13(E)-labdadiene-19-carboxilic acid (3). Compounds 1-3 exhibited cytotoxic effects, with moderate cytotoxicity against the EJ-138 bladder and CAOV-4 ovary cancer cell lines.

  10. Isolation of Bioactive Compounds from Sunflower Leaves (Helianthus annuus L.) Extracted with Supercritical Carbon Dioxide.

    PubMed

    El Marsni, Zouhir; Torres, Ascension; Varela, Rosa M; Molinillo, José M G; Casas, Lourdes; Mantell, Casimiro; Martinez de la Ossa, Enrique J; Macias, Francisco A

    2015-07-22

    The work described herein is a continuation of our initial studies on the supercritical fluid extraction (SFE) with CO2 of bioactive substances from Helianthus annuus L. var. Arianna. The selected SFE extract showed high activity in the wheat coleoptile bioassay, in Petri dish phytotoxicity bioassays, and in the hydroponic culture of tomato seeds. Chromatographic fractionations of the extracts and a spectroscopic analysis of the isolated compounds showed 52 substances belonging to 10 different chemical classes, which were mainly sesquiterpene lactones, diterpenes, and flavonoids. Heliannuol M (31), helivypolides K and L (36, 37), and helieudesmanolide B (38) are described for the first time in the literature. Metabolites have been tested in the etiolated wheat coleoptile bioassay with good results in a noteworthy effect on germination. The most active compounds were also tested on tomato seeds, heliannuol A (30) and leptocarpin (45) being the most active, with values similar to those of the commercial herbicide.

  11. Bioassay-Guided Isolation of Compounds from Datura stramonium with TRAIL-Resistance Overcoming Activity.

    PubMed

    Karmakar, Utpal K; Toume, Kazufumi; Ishikawa, Naoki; Arai, Midori A; Sadhu, Samir K; Ahmed, Firoj; Ishibashi, Masami

    2016-02-01

    TRAIL is a potent inducer of apoptosis in most cancer cells, but not in normal cells, and therefore has deserved intense interest as a promising agent for cancer therapy. In the search for bioactive natural products for overcoming TRAIL-resistance, we previously reported a number of active compounds. In our screening program on natural resources targeting overcoming TRAIL-resistance, activity-guided fractionation of the MeOH extract of Datura stramonium leaves led to the isolation of three alkaloids--scopolamine (1), trigonelline (2), and tyramine (3). Compounds 1, 2, and 3 exhibited TRAIL-resistance overcoming activity at 50, 150, and 100 µM, respectively in TRAIL-resistant AGS cells. PMID:27032197

  12. Elusive 2H-1,2-oxasiletes through reactions of an isolable dialkylsilylene with diazocarbonyl compounds.

    PubMed

    Dong, Zhaowen; Xiao, Xu-Qiong; Li, Zhifang; Lu, Qiong; Lai, Guoqiao; Kira, Mitsuo

    2015-09-28

    The reactions of isolable dialkysilylene 1 with 2-diazo-1,2-diphenylethanone and ethyl 2-diazo-2-phenylacetate gave elusive silacycles, 2H-1,2-oxasiletes 2 and 3, respectively, in high yields. Because these reactions occur at low temperatures of ca.-30 °C, initial complexation of the silylene to the carbonyl oxygen of the diazocarbonyl compounds is suggested to trigger dinitrogen elimination followed by cyclization. In contrast, a six-membered cyclic diazo compound 8 and 1-sila-2,3-diazabicyclo[3.3.0]oct-3-ene 10 were obtained in good yields by the reaction of 1 with less reactive ethyl 2-diazo-3-oxo-3-phenylpropanoate 7 and trimethylsilyldiazomethane 9. Molecular structures of 2, 3, 8 and 10 were determined by X-ray crystallography.

  13. Mosquito larvicidal activity of isolated compounds from the rhizome of Zingiber officinale.

    PubMed

    Rahuman, A Abdul; Gopalakrishnan, Geetha; Venkatesan, P; Geetha, Kannappan; Bagavan, A

    2008-08-01

    The larvicidal activity of a petroleum ether extract of Zingiber officinale Roscoe (Zingiberaceae) was evaluated against Aedes aegypti L. and Culex quinquefasciatus Say (Diptera). Bioassay-guided fractionation led to the isolation of 4-gingerol (1), (6)-dehydrogingerdione (2) and (6)-dihydrogingerdione (3); the latter has not previously been reported from Z. officinale. The structures were established from infrared (IR), ultraviolet (UV), (1)H-nuclear magnetic resonance (NMR), (13)C-NMR and mass spectral data. Following a 24 h exposure, compounds 1-3 exhibited larvicidal activities against fourth instar larvae of A. aegypti (LC(50) 4.25, 9.80, 18.20 ppm) and C. quinquefasciatus (LC50 5.52, 7.66, 27.24 ppm), respectively. The results show that the most effective compound was 4-gingerol. PMID:18618523

  14. Isolation of Bioactive Compounds from Sunflower Leaves (Helianthus annuus L.) Extracted with Supercritical Carbon Dioxide.

    PubMed

    El Marsni, Zouhir; Torres, Ascension; Varela, Rosa M; Molinillo, José M G; Casas, Lourdes; Mantell, Casimiro; Martinez de la Ossa, Enrique J; Macias, Francisco A

    2015-07-22

    The work described herein is a continuation of our initial studies on the supercritical fluid extraction (SFE) with CO2 of bioactive substances from Helianthus annuus L. var. Arianna. The selected SFE extract showed high activity in the wheat coleoptile bioassay, in Petri dish phytotoxicity bioassays, and in the hydroponic culture of tomato seeds. Chromatographic fractionations of the extracts and a spectroscopic analysis of the isolated compounds showed 52 substances belonging to 10 different chemical classes, which were mainly sesquiterpene lactones, diterpenes, and flavonoids. Heliannuol M (31), helivypolides K and L (36, 37), and helieudesmanolide B (38) are described for the first time in the literature. Metabolites have been tested in the etiolated wheat coleoptile bioassay with good results in a noteworthy effect on germination. The most active compounds were also tested on tomato seeds, heliannuol A (30) and leptocarpin (45) being the most active, with values similar to those of the commercial herbicide. PMID:26151222

  15. Molecular detection and isolation from antarctica of methylotrophic bacteria able to grow with methylated sulfur compounds.

    PubMed

    Moosvi, S Azra; McDonald, Ian R; Pearce, David A; Kelly, Donovan P; Wood, Ann P

    2005-08-01

    This study is the first demonstration that a diverse facultatively methylotrophic microbiota exists in some Antarctic locations. PCR amplification of genes diagnostic for methylotrophs was carried out with bacterial DNA isolated from 14 soil and sediment samples from ten locations on Signy Island, South Orkney Islands, Antarctica. Genes encoding the mxaF of methanol dehydrogenase, the fdxA for Afipia ferredoxin, the msmA of methanesulfonate monooxygenase, and the 16S rRNA gene of Methylobacterium were detected in all samples tested. The mxaF gene sequences corresponded to those of Hyphomicrobium, Methylobacterium, and Methylomonas. Over 30 pure cultures of methylotrophs were isolated on methanesulfonate, dimethylsulfone, or dimethylsulfide from ten Signy Island lakes. Some were identified from 16S rRNA gene sequences (and morphology) as Hyphomicrobium species, strains of Afipia felis, and a methylotrophic Flavobacterium strain. Antarctic environments thus contain diverse methylotrophic bacteria, growing on various C1-substrates, including C1-sulfur compounds. PMID:16104352

  16. Antimutagenic Compounds of White Shrimp (Litopenaeus vannamei): Isolation and Structural Elucidation.

    PubMed

    López-Saiz, Carmen-María; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Velázquez, Carlos; Ocaño-Higuera, Víctor-Manuel; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2016-01-01

    According to the World Health Organization, cancer is the main cause of mortality worldwide; thus, the search of chemopreventive compounds to prevent the disease has become a priority. White shrimp (Litopenaeus vannamei) has been reported as a source of compounds with chemopreventive activities. In this study, shrimp lipids were extracted and then fractionated in order to isolate those compounds responsible for the antimutagenic activity. The antimutagenic activity was assessed by the inhibition of the mutagenic effect of aflatoxin B1 on TA98 and TA100 Salmonella tester strains using the Ames test. Methanolic fraction was responsible for the highest antimutagenic activity (95.6 and 95.9% for TA98 and TA100, resp.) and was further separated into fifteen different subfractions (M1-M15). Fraction M8 exerted the highest inhibition of AFB1 mutation (96.5 and 101.6% for TA98 and TA100, resp.) and, after further fractionation, four subfractions M8a, M8b, M8c, and M8d were obtained. Data from (1)H and (13)C NMR, and mass spectrometry analysis of fraction M8a (the one with the highest antimutagenic activity), suggest that the compound responsible for its antimutagenicity is an apocarotenoid.

  17. Antimutagenic Compounds of White Shrimp (Litopenaeus vannamei): Isolation and Structural Elucidation

    PubMed Central

    López-Saiz, Carmen-María; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Velázquez, Carlos; Ocaño-Higuera, Víctor-Manuel; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2016-01-01

    According to the World Health Organization, cancer is the main cause of mortality worldwide; thus, the search of chemopreventive compounds to prevent the disease has become a priority. White shrimp (Litopenaeus vannamei) has been reported as a source of compounds with chemopreventive activities. In this study, shrimp lipids were extracted and then fractionated in order to isolate those compounds responsible for the antimutagenic activity. The antimutagenic activity was assessed by the inhibition of the mutagenic effect of aflatoxin B1 on TA98 and TA100 Salmonella tester strains using the Ames test. Methanolic fraction was responsible for the highest antimutagenic activity (95.6 and 95.9% for TA98 and TA100, resp.) and was further separated into fifteen different subfractions (M1–M15). Fraction M8 exerted the highest inhibition of AFB1 mutation (96.5 and 101.6% for TA98 and TA100, resp.) and, after further fractionation, four subfractions M8a, M8b, M8c, and M8d were obtained. Data from 1H and 13C NMR, and mass spectrometry analysis of fraction M8a (the one with the highest antimutagenic activity), suggest that the compound responsible for its antimutagenicity is an apocarotenoid. PMID:27006678

  18. Antimutagenic Compounds of White Shrimp (Litopenaeus vannamei): Isolation and Structural Elucidation.

    PubMed

    López-Saiz, Carmen-María; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Velázquez, Carlos; Ocaño-Higuera, Víctor-Manuel; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2016-01-01

    According to the World Health Organization, cancer is the main cause of mortality worldwide; thus, the search of chemopreventive compounds to prevent the disease has become a priority. White shrimp (Litopenaeus vannamei) has been reported as a source of compounds with chemopreventive activities. In this study, shrimp lipids were extracted and then fractionated in order to isolate those compounds responsible for the antimutagenic activity. The antimutagenic activity was assessed by the inhibition of the mutagenic effect of aflatoxin B1 on TA98 and TA100 Salmonella tester strains using the Ames test. Methanolic fraction was responsible for the highest antimutagenic activity (95.6 and 95.9% for TA98 and TA100, resp.) and was further separated into fifteen different subfractions (M1-M15). Fraction M8 exerted the highest inhibition of AFB1 mutation (96.5 and 101.6% for TA98 and TA100, resp.) and, after further fractionation, four subfractions M8a, M8b, M8c, and M8d were obtained. Data from (1)H and (13)C NMR, and mass spectrometry analysis of fraction M8a (the one with the highest antimutagenic activity), suggest that the compound responsible for its antimutagenicity is an apocarotenoid. PMID:27006678

  19. Identification of a bioactive compound isolated from Brazilian propolis type 6.

    PubMed

    Castro, Myrella Lessio; do Nascimento, Andréa Mendes; Ikegaki, Masaharu; Costa-Neto, Cláudio M; Alencar, Severino M; Rosalen, Pedro L

    2009-07-15

    A prenylated benzophenone, hyperibone A, was isolated from the hexane fraction of Brazilian propolis type 6. Its structure was determined by spectral analysis including 2D NMR. This compound exhibited cytotoxic activity against HeLa tumor cells (IC(50)=0.1756microM), strong antimicrobial activity (MIC range-0.73-6.6microg/mL; MBC range-2.92-106microg/mL) against Streptococcus mutans, Streptococcus sobrinus, Streptococcus oralis, Staphylococcus aureus, and Actinomyces naeslundii, and the results of its cytotoxic and antimicrobial activities were considered good.

  20. Identification of a methicillin-resistant Staphylococcus aureus inhibitory compound isolated from Serratia marcescens

    PubMed Central

    Kadouri, Daniel E.; Shanks, Robert M.Q.

    2013-01-01

    In this study, we identified an antimicrobial compound produced by the Gram-negative bacterium Serratia marcescens. Colonies of S. marcescens inhibited the growth of nine different methicillin-resistant Staphylococcus aureus (MRSA) isolates and several other tested Gram-positive bacterial species, but not Gram-negative bacteria. Genetic analysis revealed the requirement for the swrW gene which codes for a non-ribosomal peptide synthetase that generates the cyclodepsipeptide antibiotic serratamolide, also known as serrawettin W1. This is the first report describing the anti-MRSA properties of serratamolide. PMID:23791620

  1. Anticancer activity of new depsipeptide compound isolated from an endophytic fungus.

    PubMed

    Verekar, Shilpa Amit; Mishra, Prabhu Dutt; Sreekumar, Eyyammadichiyil Sankaranarayanan; Deshmukh, Sunil Kumar; Fiebig, Heinz-Herbert; Kelter, Gerhard; Maier, Armin

    2014-10-01

    A novel depsipeptide (PM181110) was purified from an endophytic fungus Phomopsis glabrae isolated from the leaves of Pongamia pinnata (family Fabaceae). The chemical structure of PM181110 was elucidated using physiochemical properties, 2D NMR and other spectroscopic methods. PM181110 is very close in structure to FE399. The compound exhibited in vitro anticancer activity against 40 human cancer cell lines with a mean IC50 value of 0.089 μM and ex vivo efficacy towards 24 human tumor xenografts (mean IC50=0.245 μM). PMID:24824817

  2. New Polyprenylated Phloroglucinol and Other Compounds Isolated from the Fruits of Clusia nemorosa (Clusiaceae).

    PubMed

    Ferreira, Rafaela Oliveira; da Silva, Tania Maria Sarmento; de Carvalho, Mário Geraldo

    2015-01-01

    Clusia nemorosa has been widely used in folk medicine to treat various ailments, including headaches and inflammation. Investigation of the fruits of Clusia nemorosa (Clusiaceae) led to the isolation and characterization of a new phloroglucinol derivative, named 6S,8S,28S-nemorosic acid (1), together with seven known compounds: friedelin (2), β-sitosterol (3), stigmasterol (4), β-sitosterol glycoside (5), kaempferol (6), quercetin (7) and dimethyl citrate (8). The structures were determined by extensive 1D- and 2D-NMR, CD and MS spectroscopic analyses. PMID:26287129

  3. [Pharmacogenetics of oral antidiabetic treatment].

    PubMed

    Tkáč, Ivan

    2016-03-01

    Pharmacogenetics is the study of how genes (individual genotypes) affect a persons response to drugs. At present, recommendations made about the treatment of some monogenic forms of diabetes are based on genetic diagnostics. The first studies in the field of pharmacogenetics of oral antidiabetics have now been published which have identified associations of individual genetic variants with response to treatment. The response to sulfonylurea derivatives was significantly associated with the variants KCNJ11/ABCC8, TCF7L2 and CYP2C9. The response to metformin treatment was associated with the genetic variants ATM and SLC47A1. The response to treatment with glitazones was associated with the genetic variant PPARG. The therapeutic response to the treatment with gliptins was associated with the genetic variants TCF7L2 and CTRB1/2. It may be expected that in the near future pharmacogenetic knowledge will also be used within personalized treatment of type 2 diabetes. PMID:27180666

  4. Pharmacogenetics of oral antidiabetic treatment.

    PubMed

    Schroner, Z; Javorsky, M; Kozarova, M; Tkac, I

    2011-01-01

    In the majority of patients with type 2 diabetes (T2D), oral antidiabetic drug (OAD) treatment is the first line treatment after lifestyle measures fail. Two major groups of OAD are used in clinical practice--insulin secretagogues and insulin sensitisers. Sulphonyluea (SU) derivatives are insulin secretagogues and stimulate insulin secretion by inhibiting ATP-sensitive potassium channels. Genes KCNJ11 and ABCC8 encode potassium channel proteins. KCNJ11 gene Glu23Lys polymorphism was associated with an increased risk of SU secondary failure, while Ser1369Ala polymorphism of ABCC8 gene had influence antidiabetic efficacy of SU drug gliclazide. In addition, the polymorphism of TCF7L2 gene, which has the strongest association with T2D, also influenced secondary SU drug failure. Insulin sensitisers include both metformin and glitazones. Some drug-genotype associations were observed for metformin in patients with T2D. Several genes influenced the effect of glitazone treatment. Rosiglitazone was more effective in diabetes control in carriers of Prol2Ala polymorphism of PPARG gene encoding the PPARg-receptor--the target of this drug. Rosiglitazone treatment had less effect on glycemic control and adiponectin increase in T2D patients with GG-genotypes of adiponectin (APM1) polymorphism. Pioglitazone treatment had smaller effect on glycemic control in patients with LPL Ser447X polymorphism. Identification of drug-genotype interactions in pharmacogenetic studies of the OAD treatment might have clinical implications in the near future resulting in selection of more specific "patient-tailored therapy" in T2D (Tab. 1, Ref. 58).

  5. Isolation and partial characterization of antimicrobial compounds from a new strain Nonomuraea sp. NM94.

    PubMed

    Badji, Boubekeur; Mostefaoui, Abdellah; Sabaou, Nasserdine; Lebrihi, Ahmed; Mathieu, Florence; Seguin, Elisabeth; Tillequin, François

    2007-06-01

    An actinomycete strain NM94 was isolated from a Saharan soil sample by a dilution agar plating method using chitin-vitamins B medium supplemented with penicillin. The strain presented the morphological and chemical characteristics of the genus Nonomuraea. On the basis of 16S rDNA analysis and physiological tests, this isolate was found to be quite different from the known species of Nonomuraea and might be new. The strain NM94 secreted several antibiotics on yeast extract malt extract glucose medium that were active against some Gram-positive bacteria, yeast, and fungi. The antibiotics were extracted with dichloromethane and detected by bioautography on silica gel plates using Mucor ramannianus and Bacillus subtilis as the test organisms. Among these antibiotics, a complex called 94A showed interesting antifungal activity. It was selected and purified by reverse-phase HPLC. This complex was composed of five compounds. Spectroscopic studies by infrared, mass, and (1)H NMR of the compounds were carried out. Initial results showed that these molecules differed from the known antibiotics produced by other Nonomuraea species. PMID:17318487

  6. Microsphaerol and seimatorone: two new compounds isolated from the endophytic fungi, Microsphaeropsis sp. and Seimatosporium sp.

    PubMed

    Hussain, Hidayat; Root, Natalia; Jabeen, Farah; Al-Harrasi, Ahmed; Ahmad, Manzoor; Mabood, Fazal; Hassan, Zahid; Shah, Afzal; Green, Ivan R; Schulz, Barbara; Krohn, Karsten

    2015-02-01

    A new polychlorinated triphenyl diether named microsphaerol (1), has been isolated from the endophtic fungus Microsphaeropsis sp. An intensive phytochemical investigation of the endophytic fungus Seimatosporium sp., led to the isolation of a new naphthalene derivative named seimatorone (2) and eight known compounds, i.e., 1-(2,6-dihydroxyphenyl)-3-hydroxybutan-1-one (3), 1-(2,6-dihydroxyphenyl)butan-1-one (4), 1-(2-hydroxy-6-methoxyphenyl)butan-1-one (5), 5-hydroxy-2-methyl-4H-chromen-4-one (6), 2,3-dihydro-5-hydroxy-2-methyl-4H-chromen-4-one (7), 8-methoxynaphthalen-1-ol (8), nodulisporins A and B (9 and 10, resp.), and daldinol (11). The structures of 1 and 2 were elucidated by detailed spectroscopic analysis including (1) H- and (13) C-NMR, COSY, HMQC, HMBC, and HR-EI-MS, while the structures of the known compounds were deduced from comparison of their spectral data with those in the literature. Preliminary studies revealed that microsphaerol (1) showed good antibacterial activities against B. Megaterium and E. coli, and good antilagal and antifungal activities against C. fusca, M. violaceum, respectively. On the other hand, seimatorone (2) exhibited moderate antibacterial, antialgal, and antifungal activities.

  7. Natural antifouling compounds produced by a novel fungus Aureobasidium pullulans HN isolated from marine biofilm.

    PubMed

    Gao, Min; Su, Rongguo; Wang, Ke; Li, Xuzhao; Lu, Wei

    2013-12-15

    A fungus, Aureobasidium pullulans, was isolated from marine biofilm and identified. A bioassay-guided fractionation procedure was developed to isolate and purify antifouling compounds from A. pullulans HN. The procedure was: fermentation broth-aeration and addition of sodium thiosulfate-graduated pH and liquid-liquid extraction-SPE purification-GC-MS analysis. Firstly, the fermentation broth was tested for its toxicity. Then it was treated with aeration and addition of sodium thiosulfate, and its toxicity was almost not changed. Lastly, antifouling compounds were extracted at different pH, the extract had high toxicity at pH 2 but almost no toxicity at pH 10, which suggested the toxicants should be fatty acids. The EC50 of the extract against Skeletonema costatum was 90.9 μg ml(-1), and its LC50 against Balanus amphitrete larvae was 22.2 μg ml(-1). After purified by HLB SPE column, the EC50 of the extract against S. costatum was 49.4 μg ml(-1). The myristic and palmitic acids were found as the main toxicants by GC-MS. PMID:24210009

  8. Antihistamine Effect of a Pure Bioactive Compound Isolated from Slug (Diplosolenodes occidentalis) Material

    PubMed Central

    Jacob, AS; Simon, OR; Wheatle, D; Ruddock, P; McCook, K

    2014-01-01

    ABSTRACT Objective: Folklore claims of the therapeutic effect of garden slug (Diplosolenodes occidentalis) extract used to relieve bronchoconstriction in asthmatic individuals were never validated scientifically. The aim of this study was to isolate the pure bioactive compound from slug extract causing this effect. Methods: The crude ground material was prepared in ethanol and after filtration, separation by flash column chromatography method was done. The structure was elucidated by data from hydrogen and carbon nuclear magnetic resonance (NMR) profiles. The bioactive compound was assessed for dose dependent response effects on guinea pig tracheal smooth muscle pre-contracted with histamine. Receptor specificity studies were done by using HTMT dimaleate (H1 agonist). The type of antagonism was also identified. Results: The pure component isolated from garden slug material was identified by spectral studies as glyceryl trilinolenate. It caused dose-dependent relaxation in guinea pig tracheal smooth muscle strips pre-contracted with histamine, it acted via H1 type receptors and showed non-competitive antagonism. Conclusion: Glyceryl trilinolenate produced dose-dependent relaxation in tracheal smooth muscle strips in the presence of the agonist histamine. Glyceryl trilinolenate displayed non-competitive antagonism at H1 receptors in the trachea. This agent was able to alleviate bronchoconstriction in individuals presenting with atopic asthma in rural agricultural areas in Jamaica (verbal communications). It is possible that glyceryl trilinolenate can be used therapeutically to produce tracheal smooth muscle relaxation in individuals presenting with atopic asthma. PMID:25781274

  9. Antibacterial activity of isolated phenolic compounds from cranberry (Vaccinium macrocarpon) against Escherichia coli.

    PubMed

    Rodríguez-Pérez, Celia; Quirantes-Piné, Rosa; Uberos, José; Jiménez-Sánchez, Cecilia; Peña, Alejandro; Segura-Carretero, Antonio

    2016-03-01

    Phenolic compounds from a cranberry extract were isolated in order to assess their contribution to the antibacterial activity against uropathogenic strains of Escherichia coli (UPEC). With this purpose, a total of 25 fractions from a cranberry extract were isolated using semipreparative high performance liquid chromatography (HPLC) and characterized based on the results obtained by reversed-phase HPLC coupled to mass spectrometry detection. Then, the effects on UPEC surface hydrophobicity and biofilm formation of the cranberry extract as well as the purest fractions (a total of 13) were tested. As expected, the whole extract presented a powerful antibacterial activity against UPEC while the selected fractions presented a different behavior. Myricetin and quercitrin significantly decreased (p < 0.05) E. coli biofilm formation compared with the control, while dihydroferulic acid glucuronide, procyanidin A dimer, quercetin glucoside, myricetin and prodelphinidin B led to a significant decrease of the surface hydrophobicity compared with the control. The results suggest that apart from proanthocyanidins, other compounds, mainly flavonoids, can act against E. coli biofilm formation and also modify UPEC surface hydrophobicity in vitro, one of the first steps of adhesion. PMID:26902395

  10. Isolation and partial characterization of antimicrobial compounds from a new strain Nonomuraea sp. NM94.

    PubMed

    Badji, Boubekeur; Mostefaoui, Abdellah; Sabaou, Nasserdine; Lebrihi, Ahmed; Mathieu, Florence; Seguin, Elisabeth; Tillequin, François

    2007-06-01

    An actinomycete strain NM94 was isolated from a Saharan soil sample by a dilution agar plating method using chitin-vitamins B medium supplemented with penicillin. The strain presented the morphological and chemical characteristics of the genus Nonomuraea. On the basis of 16S rDNA analysis and physiological tests, this isolate was found to be quite different from the known species of Nonomuraea and might be new. The strain NM94 secreted several antibiotics on yeast extract malt extract glucose medium that were active against some Gram-positive bacteria, yeast, and fungi. The antibiotics were extracted with dichloromethane and detected by bioautography on silica gel plates using Mucor ramannianus and Bacillus subtilis as the test organisms. Among these antibiotics, a complex called 94A showed interesting antifungal activity. It was selected and purified by reverse-phase HPLC. This complex was composed of five compounds. Spectroscopic studies by infrared, mass, and (1)H NMR of the compounds were carried out. Initial results showed that these molecules differed from the known antibiotics produced by other Nonomuraea species.

  11. Antibacterial activity of isolated phenolic compounds from cranberry (Vaccinium macrocarpon) against Escherichia coli.

    PubMed

    Rodríguez-Pérez, Celia; Quirantes-Piné, Rosa; Uberos, José; Jiménez-Sánchez, Cecilia; Peña, Alejandro; Segura-Carretero, Antonio

    2016-03-01

    Phenolic compounds from a cranberry extract were isolated in order to assess their contribution to the antibacterial activity against uropathogenic strains of Escherichia coli (UPEC). With this purpose, a total of 25 fractions from a cranberry extract were isolated using semipreparative high performance liquid chromatography (HPLC) and characterized based on the results obtained by reversed-phase HPLC coupled to mass spectrometry detection. Then, the effects on UPEC surface hydrophobicity and biofilm formation of the cranberry extract as well as the purest fractions (a total of 13) were tested. As expected, the whole extract presented a powerful antibacterial activity against UPEC while the selected fractions presented a different behavior. Myricetin and quercitrin significantly decreased (p < 0.05) E. coli biofilm formation compared with the control, while dihydroferulic acid glucuronide, procyanidin A dimer, quercetin glucoside, myricetin and prodelphinidin B led to a significant decrease of the surface hydrophobicity compared with the control. The results suggest that apart from proanthocyanidins, other compounds, mainly flavonoids, can act against E. coli biofilm formation and also modify UPEC surface hydrophobicity in vitro, one of the first steps of adhesion.

  12. Antinociceptive and anti-inflammatory effects of compounds isolated from Scaphyglottis livida and Maxillaria densa.

    PubMed

    Déciga-Campos, Myrna; Palacios-Espinosa, Juan Francisco; Reyes-Ramírez, Adelfo; Mata, Rachel

    2007-11-01

    Oral administration of a CH(2)Cl(2)-MeOH (1:1) extract of Scaphyglottis livida produced dose-dependent antinociceptive and anti-inflammatory effects when tested in mice and rats using the hot-plate (150-600 mg/kg) and carrageenan-induced inflammation (150-600 mg/kg) models, respectively. Morphine (1.5-6 mg/kg, p.o.) and indomethacin (10-40 mg/kg, p.o.) were used as positive controls, respectively. Four compounds were isolated from the active extract of Scaphyglottis livida, namely 5alpha-lanosta-24,24-dimethyl-9(11),25-dien-3beta-ol (LDD), 24,24,dimethyl-9,19-cyclolanosta-9(11),25-dien-3-one (cyclobalanone), gigantol and 3,4'-dihydroxy-3',4,5-trimethoxybibenzyl (DTB). LDD and gigantol (25-100 mg/kg, p.o.) significantly increased the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenan-induced inflammation in rats. The antinociception provoked by LDD and gigantol was partially blocked by naloxone (1mg/kg, i.p.). However, pretreatment with L-NAME (100 mg/kg, i.p.) and glibenclamide (10 mg/kg, i.p.) did not affect the antinociceptive response induced by LDD or gigantol suggesting that their pharmacological effect could be partially due to activation of opioid receptors. Moreover, a CH(2)Cl(2)-MeOH (1:1) extract of Maxillaria densa reduced acetic acid-induced abdominal writhes but was not able to produce antinociception in the hot-plate assay. Two compounds were isolated from the active extract of Maxillaria densa, namely fimbriol A and erianthridin. Both compounds partially reduced acetic acid-induced writhes. The results tend to support the popular use of this species in folk medicine for treatment of painful complaints.

  13. Isolation, Partial Purification and Characterization of an Antimicrobial Compound, Produced by Bacillus atrophaeus

    PubMed Central

    Ebrahimipour, Gholam Hossein; Khosravibabadi, Zahra; Sadeghi, Hossein; Aliahmadi, Atusa

    2014-01-01

    Background: Antibiotics are usually assumed as secondary metabolites produced during the idiophase of microbial growth, which can kill or inhibit the growth of other microorganisms. Nowadays, indiscriminate use of antibiotics has resulted in resistant microorganisms. Therefore, screening researches on products with antimicrobial activities are necessary. Objectives: To find new antibiotics to defend against pathogenic microorganisms resistant to common antibiotics, the bacterium isolated from skin of the frog called Rana ridibunda was studied for its antimicrobial activities. Materials and Methods: An antibiotic-producing bacterium was isolated from the frog skin. The bacterium was identified based on 16SrDNA sequencing and biochemical and morphological characteristics. Antimicrobial activity of the culture supernatant was examined against laboratorial standard bacteria by disc diffusion and minimum inhibitory concentration (MIC) methods. To characterize the produced antimicrobial compound, the culture supernatant of the bacterium was washed by chloroform and dried at 40°C; then, the antimicrobial substance was extracted by methanol and acetone and detected by bioautography on silica gel plates. Dialysis tube was used to find the molecular weight of this substance. Results: The isolated bacterium was identified as a new strain of Bacillus atrophaeus. The antimicrobial substance exhibited heat stability between 25ºC and 100ºC and was active in a broad pH range from 2.0 to 11.0. The bioautography assay showed that methanol was the optimum solvent for the extraction of antimicrobial substance. The dialysis tube indicated that the antimicrobial substance weight was less than 1 kDa and the compound did not precipitate with ammonium sulfate. Conclusions: This study showed that some properties of antimicrobial substances produced by the GA strain differed from other peptide antibiotics produced by the genus Bacillus such as bacitracin, which increases the likelihood of

  14. Isolation of an antimicrobial compound produced by bacteria associated with reef-building corals

    PubMed Central

    Tapiolas, Dianne; Motti, Cherie A.; Foret, Sylvain; Tebben, Jan; Willis, Bette L.; Bourne, David G.

    2016-01-01

    Bacterial communities associated with healthy corals produce antimicrobial compounds that inhibit the colonization and growth of invasive microbes and potential pathogens. To date, however, bacteria-derived antimicrobial molecules have not been identified in reef-building corals. Here, we report the isolation of an antimicrobial compound produced by Pseudovibrio sp. P12, a common and abundant coral-associated bacterium. This strain was capable of metabolizing dimethylsulfoniopropionate (DMSP), a sulfur molecule produced in high concentrations by reef-building corals and playing a role in structuring their bacterial communities. Bioassay-guided fractionation coupled with nuclear magnetic resonance (NMR) and mass spectrometry (MS), identified the antimicrobial as tropodithietic acid (TDA), a sulfur-containing compound likely derived from DMSP catabolism. TDA was produced in large quantities by Pseudovibrio sp., and prevented the growth of two previously identified coral pathogens, Vibrio coralliilyticus and V. owensii, at very low concentrations (0.5 μg/mL) in agar diffusion assays. Genome sequencing of Pseudovibrio sp. P12 identified gene homologs likely involved in the metabolism of DMSP and production of TDA. These results provide additional evidence for the integral role of DMSP in structuring coral-associated bacterial communities and underline the potential of these DMSP-metabolizing microbes to contribute to coral disease prevention.

  15. Isolation of an antimicrobial compound produced by bacteria associated with reef-building corals

    PubMed Central

    Tapiolas, Dianne; Motti, Cherie A.; Foret, Sylvain; Tebben, Jan; Willis, Bette L.; Bourne, David G.

    2016-01-01

    Bacterial communities associated with healthy corals produce antimicrobial compounds that inhibit the colonization and growth of invasive microbes and potential pathogens. To date, however, bacteria-derived antimicrobial molecules have not been identified in reef-building corals. Here, we report the isolation of an antimicrobial compound produced by Pseudovibrio sp. P12, a common and abundant coral-associated bacterium. This strain was capable of metabolizing dimethylsulfoniopropionate (DMSP), a sulfur molecule produced in high concentrations by reef-building corals and playing a role in structuring their bacterial communities. Bioassay-guided fractionation coupled with nuclear magnetic resonance (NMR) and mass spectrometry (MS), identified the antimicrobial as tropodithietic acid (TDA), a sulfur-containing compound likely derived from DMSP catabolism. TDA was produced in large quantities by Pseudovibrio sp., and prevented the growth of two previously identified coral pathogens, Vibrio coralliilyticus and V. owensii, at very low concentrations (0.5 μg/mL) in agar diffusion assays. Genome sequencing of Pseudovibrio sp. P12 identified gene homologs likely involved in the metabolism of DMSP and production of TDA. These results provide additional evidence for the integral role of DMSP in structuring coral-associated bacterial communities and underline the potential of these DMSP-metabolizing microbes to contribute to coral disease prevention. PMID:27602265

  16. Isolation of an antimicrobial compound produced by bacteria associated with reef-building corals.

    PubMed

    Raina, Jean-Baptiste; Tapiolas, Dianne; Motti, Cherie A; Foret, Sylvain; Seemann, Torsten; Tebben, Jan; Willis, Bette L; Bourne, David G

    2016-01-01

    Bacterial communities associated with healthy corals produce antimicrobial compounds that inhibit the colonization and growth of invasive microbes and potential pathogens. To date, however, bacteria-derived antimicrobial molecules have not been identified in reef-building corals. Here, we report the isolation of an antimicrobial compound produced by Pseudovibrio sp. P12, a common and abundant coral-associated bacterium. This strain was capable of metabolizing dimethylsulfoniopropionate (DMSP), a sulfur molecule produced in high concentrations by reef-building corals and playing a role in structuring their bacterial communities. Bioassay-guided fractionation coupled with nuclear magnetic resonance (NMR) and mass spectrometry (MS), identified the antimicrobial as tropodithietic acid (TDA), a sulfur-containing compound likely derived from DMSP catabolism. TDA was produced in large quantities by Pseudovibrio sp., and prevented the growth of two previously identified coral pathogens, Vibrio coralliilyticus and V. owensii, at very low concentrations (0.5 μg/mL) in agar diffusion assays. Genome sequencing of Pseudovibrio sp. P12 identified gene homologs likely involved in the metabolism of DMSP and production of TDA. These results provide additional evidence for the integral role of DMSP in structuring coral-associated bacterial communities and underline the potential of these DMSP-metabolizing microbes to contribute to coral disease prevention. PMID:27602265

  17. Isolation and Identification of Cytotoxic Compounds from Aeschynomene fascicularis, a Mayan Medicinal Plant.

    PubMed

    Caamal-Fuentes, Edgar E; Peraza-Sánchez, Sergio R; Torres-Tapia, Luis W; Moo-Puc, Rosa E

    2015-07-24

    The plant Aeschynomene fascicularis (Fabaceae) has been used in Mayan traditional medicine in the Yucatan peninsula. However, the compounds present in the plant responsible for its curative properties have not yet been investigated. Aeschynomene fascicularis root bark was extracted with 100% methanol to obtain a crude extract. The methanol extract was partitioned successively with solvents with increasing polarity to obtain the corresponding hexane (Hx), dichloromethane (DCM) and ethyl acetate fractions (EtOAc), as well as a residual water-alcoholic fraction. These fractions were tested for their cytotoxic activities using an MTT assay against Hep-2 cancer cell lines. The Hx fraction led to the isolation of spinochalcone C (1), spinochalcone A (2), isocordoin (3) and secundiflorol G (4). Their structures were identified based on spectroscopic evidence and chemical properties. All compounds were subjected to cytotoxicity and antiproliferative assays against a panel of seven cell lines, including one normal-type cell line. Spinochalcone A (2) exhibited cytotoxic activity against DU-145 cell line and antiproliferative activity against the KB cell line. Secundiflorol G (4) showed strong cytotoxic activity towards KB and Hep-2 cell lines. In addition, isocordoin (3) showed moderate activity on KB, Hep-2 and DU-145 cell lines. The active Compounds 2, 3 and 4 are potential therapeutic entities against cancer.

  18. A Systematic Review of the Anticancer Properties of Compounds Isolated from Licorice (Gancao).

    PubMed

    Tang, Zheng-Hai; Li, Ting; Tong, Yun-Guang; Chen, Xiao-Jia; Chen, Xiu-Ping; Wang, Yi-Tao; Lu, Jin-Jian

    2015-12-01

    Licorice (Gancao in Chinese) has been used worldwide as a botanical source in medicine and as a sweetening agent in food products for thousands of years. Triterpene saponins and flavonoids are its main ingredients that exhibit a variety of biological activities, including hepatoprotective, antiulcer, anti-inflammatory, antiviral and anticancer effects among others. This review attempts to summarize the current knowledge on the anticancer properties and mechanisms of the compounds isolated from licorice and obtain new insights for further research and development of licorice. A broad spectrum of in vitro and in vivo studies have recently demonstrated that the mixed extracts and purified compounds from licorice exhibit evident anticancer properties by inhibition of proliferation, induction of cell cycle arrest, apoptosis, autophagy, differentiation, suppression of metastasis, angiogenesis, and sensitization of chemotherapy or radiotherapy. A combined treatment of licorice compounds and clinical chemotherapy drugs remarkably enhances anticancer effects and reduces the side effects of chemotherapeutics. Furthermore, glycyrrhizic acid and glycyrrhetinic acid in licorice have been indicated to present obvious liver-targeting effects in targeted drug delivery systems for hepatocellular carcinoma treatment.

  19. Reduction of nitroaromatic compounds by anaerobic bacteria isolated from the human gastrointestinal tract.

    PubMed Central

    Rafil, F; Franklin, W; Heflich, R H; Cerniglia, C E

    1991-01-01

    Human intestinal microbial flora were screened for their abilities to reduce nitroaromatic compounds by growing them on brain heart infusion agar plates containing 1-nitropyrene. Bacteria metabolizing 1-nitropyrene, detected by the appearance of clear zones around the colonies, were identified as Clostridium leptum, Clostridium paraputrificum, Clostridium clostridiiforme, another Clostridium sp., and a Eubacterium sp. These bacteria produced aromatic amines from nitroaromatic compounds, as shown by thin-layer chromatography, high-pressure liquid chromatography, and biochemical tests. Incubation of three of these bacteria with 1-nitropyrene, 1,3-dinitropyrene, and 1,6-dinitropyrene inactivated the direct-acting mutagenicity associated with these compounds. Menadione and o-iodosobenzoic acid inhibited nitroreductase activity in all of the isolates, indicating the involvement of sulfhydryl groups in the active site of the enzyme. The optimum pH for nitroreductase activity was 8.0. Only the Clostridium sp. required added flavin adenine dinucleotide for nitroreductase activity. The nitroreductases were constitutive and extracellular. An activity stain for the detection of nitroreductase on anaerobic native polyacrylamide gels was developed. This activity stain revealed only one isozyme in each bacterium but showed that the nitroreductases from different bacteria had distinct electrophoretic mobilities. Images PMID:2059053

  20. Antiherpetic Plants: A Review of Active Extracts, Isolated Compounds, and Bioassays.

    PubMed

    Silva-Mares, David; Torres-López, Ernesto; Rivas-Galindo, Verónica M

    2016-04-01

    Herpes simplex is a disease that is widely distributed throughout the world. It is caused by herpes simplex virus type 1 (HSV-1) and simplex virus type 2 (HSV-2). The drugs of choice for treatment are acyclovir (ACV), Penciclovir (PCV) and other guanine analogues, which have the same mechanism of action. However, due to the constant increase of ACV-resistant strains in immunocompromised patients, it is necessary to find new treatment alternatives. It has been shown that natural products are a good alternative for the treatment of these diseases as well as being an excellent source of compounds with anti-herpetic activity, which may be useful for the development of new drugs and act through a mechanism of action different from ACV and PCV. This paper compiles reports on extracts and compounds isolated from plants that have anti-herpetic activity. We present an analysis of the solvents most widely used for extraction from plants as well as cells and commonly used methods for evaluating cytotoxic and anti-herpetic activity. Families that have a higher number of plants with anti-herpetic activity are evaluated, and we also highlight the importance of studies of mechanisms of action of extracts and compounds with anti-herpetic activity. PMID:27396217

  1. Isolation of antibacterial compounds from Quercus dilatata L. through bioassay guided fractionation

    PubMed Central

    2012-01-01

    Background Four medicinal plants (Chrozophora hierosolymitana Spreng, Chrysanthemum leucanthemum L., Ephedra gerardiana Wall. ex Stapf, and Quercus dilatata L.) used by indigenous healers to treat various infectious diseases were selected for the present study. The major objective of the present study was isolation and characterization of antimicrobial components from the crude plant extracts using bioassay guided fractionation. Methods Seven methanolic extracts of the four plants were screened to identify any antimicrobial agents present in them. The active crude plant extract was fractionated first by solvent partitioning and then by HPLC. Characterization of the active fractions was done by using spectrophotometer. Results All the seven methanolic extracts showed low antifungal activity, however, when these extracts were tested for antibacterial activity, significant activity was exhibited by two extracts. The extract of aerial parts of Q. dilatata was most active and therefore, was selected for further analysis. Initially fractionation was done by solvent-solvent partitioning and out of six partitioned fractions, ethanol fraction was selected on the basis of results of antibacterial activity and phytochemical analysis. Further, fractionation was carried out by RP- HPLC and purified active subfractions were characterized by comparing their absorption spectra with that of the known natural products isolated from the plants of Quercus genus. Discussion and conclusion The results suggest that this is the first report of the isolated antibacterial compounds from this genus. PMID:22554280

  2. Antidiabetic and antihyperlipemic effects of Clemeo felina.

    PubMed

    Nagarajan, N S; Murugesh, N; Thirupathy Kumaresan, P; Radha, N; Murali, A

    2005-06-01

    Petroleum ether and benzene extracts of Clemeo felina, given orally at doses of 300 mg kg(-1) day(-1) for 30 days, were found to be antidiabetic and antihyperlipemic on alloxan diabetic rats. Moreover, a significant decrease in the activities of serum enzymes like alkaline phosphatase, acid phosphatase and HMGCoA reductase activity in the liver was observed. However, treatment of rats with the extracts as well as standard antidiabetic drugs increased liver hexakinase activity and serum LDH activity.

  3. Synthesis and biological activity of trans-tiliroside derivatives as potent anti-diabetic agents.

    PubMed

    Zhu, Yujin; Zhang, Yanjun; Liu, Yi; Chu, Hongwan; Duan, Hongquan

    2010-12-10

    A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents.

  4. Screening and isolation of the algicidal compounds from marine green alga Ulva intestinalis

    NASA Astrophysics Data System (ADS)

    Sun, Xue; Jin, Haoliang; Zhang, Lin; Hu, Wei; Li, Yahe; Xu, Nianjun

    2016-07-01

    Twenty species of seaweed were collected from the coast of Zhejiang, China, extracted with ethanol, and screened for algicidal activity against red tide microalgae Heterosigma akashiwo and Prorocentrum micans. Inhibitory effects of fresh and dried tißsues of green alga Ulva intestinalis were assessed and the main algicidal compounds were isolated, purified, and identified. Five seaweed species, U. intestinalis, U. fasciata, Grateloupia romosissima, Chondria crassicaulis, and Gracilariopsis lemaneiformis, were investigated for their algicidal activities. Fresh tissues of 8.0 and 16.0 mg/mL of U. intestinalis dissolved in media significantly inhibited growth of H. akashiwo and P. micans, respectively. Dried tissue and ethyl acetate (EtOAc) extracts of U. intestinalis at greater than 1.2 and 0.04 mg/mL, respectively, were fatal to H. akashiwo, while its water and EtOAc extracts in excess of 0.96 and 0.32 mg/mL, respectively, were lethal to P. micans. Three algicidal compounds in the EtOAc extracts were identified as 15-ethoxy-(6z,9z,12z)-hexadecatrienoic acid (I), (6E,9E,12E)-(2-acetoxy- β-D-glucose)-octadecatrienoic acid ester (II) and hexadecanoic acid (III). Of these, compound II displayed the most potent algicidal activity with IC50 values of 4.9 and 14.1 µg/mL for H. akashiwo and P. micans, respectively. Compound I showed moderate algicidal activity with IC50 values of 13.4 and 24.7 µg/mL for H. akashiwo and P. micans, respectively. These findings suggested that certain macroalgae or products therefrom could be used as effective biological control agents against red tide algae.

  5. Isolation, characterisation and antibacterial activity of new compounds from methanolic extract of seeds of Caesalpinia crista L. (Caesalpinaceae).

    PubMed

    Kumar, Ankit; Garg, Vikas; Chaudhary, Anurag; Jain, Pankaj Kumar; Tomar, Praveen Kumar

    2014-01-01

    Phytochemical study on the methanolic extract of Caesalpinia crista afforded two novel compounds, 2-hydroxytrideca-3,6-dienyl-pentanoate and octacosa-12,15-diene along with known compounds 3-O-methylellagic acid 3'O-α-rhamnopyranoside, β-sitosterol and sucrose. Compound 3-O-methylellagic acid 3'O-α-rhamnopyranoside is reported for the first time from the plant. Molecular structures, of isolated compounds, were elucidated by using the NMR spectroscopy in combination with IR and mass spectral data. All isolated compounds, extract and fractions were evaluated for in vitro antibacterial activity against various Gram-positive and Gram-negative bacterial strains and found to be significantly active against Staphylococcus aureus and methicillin-resistant S. aureus (minimum inhibitory concentration: 64-512 μg mL(- 1)).

  6. Isolation and Characterization of the Anticancer Compound Piceatannol from Sophora Interrupta Bedd

    PubMed Central

    Mathi, Pardhasaradhi; Das, Snehasish; Nikhil, Kumar; Roy, Partha; Yerra, Srikanth; Ravada, Suryachandra Rao; Bokka, Venkata Raman; Botlagunta, Mahendran

    2015-01-01

    Background: Sophora belongs to the family of Fabaceae and the species in this genus are currently used as a folklore medicine for preventing a variety of ailments including cancer. Our aim was to identify and validate an anticancer compound from Sophora interrupta using multi-spectroscopic, anticancer screening, and molecular docking approach. Methods: The cytotoxicity of the various solvent extracts, petroleum ether, n-butanol, and ethyl acetate (EtOAc) of the S. interrupta root powder was evaluated in a breast cancer cell lines (MCF-7). The extract that had anticancer activity was subjected to column chromatography based on the polarity of the solvents. The anticancer activity of the elution fractions was validated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The isolated metabolite fraction with anticancer activity was run through a C18 column isocratic and gradient high-performance liquid chromatography (HPLC). The structure of the isolated compound was characterized using 1H nuclear magnetic resonance (NMR), 13C-NMR, Fourier transform infrared spectroscopy, and liquid chromatography-mass spectrometer methods. Results: The crude EtAOc extract effectively inhibited the proliferation of MCF-7 cells. The column eluted chloroform and EtOAc (4:6) fraction of the EtOAc extract showed significant anticancer activity in the MCF-7 cells compared with normal mesenchymal stem cells. This fraction showed three major peaks in the HPLC chromatogram and the first major peak with a retention time (RT) of 7.153 was purified using preparative-HPLC. The structure of the compound is a piceatannol, which is a metabolic product of resveratrol. Piceatannol formed direct two hydrogen bond interactions between Cys912 (2H), and Glu878 of vascular endothelial growth factor receptor 1 (VEGFR1) with a glide-score (G-score) of −10.193, and two hydrogen bond interactions between Cys919, and Asp1046 of VEGFR2, with a G-score of −8.359. The structure is

  7. Apoptosis mediated anti-proliferative effect of compound isolated from Cassia auriculata leaves against human colon cancer cell line

    NASA Astrophysics Data System (ADS)

    Esakkirajan, M.; Prabhu, N. M.; Manikandan, R.; Beulaja, M.; Prabhu, D.; Govindaraju, K.; Thiagarajan, R.; Arulvasu, C.; Dhanasekaran, G.; Dinesh, D.; Babu, G.

    2014-06-01

    A compound was isolated from Cassia auriculata leaves and characterized by high-performance liquid chromatography (HPLC), liquid chromatography mass spectrometry (LC-MS), UV-vis spectroscopy (UV-vis), Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). The in vitro anticancer effect of the compound isolated from C. auriculata was evaluated in human colon cancer cells HCT 15 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cytotoxicity, nuclear morphology analysis and measurement of lactate dehydrogenase. The isolated compound 4-(2,5 dichlorobenzyl)-2,3,4,5,6,7 hexahydro7(4 methoxyphenyl)benzo[h][1,4,7] triazecin8(1H)-one showed 50% inhibition of HCT 15 cells when tested at 20 μg/ml after 24 h incubation. Cytotoxicity, nuclear morphology and lactate dehydrogenase assays clearly show potent anticancer activity of the isolated compound against colon cancer. Thus, the in vitro findings suggest that the compound isolated from C. auriculata leaves have potent anti-cancer properties with possible clinical applications.

  8. Fishing for Nature's Hits: Establishment of the Zebrafish as a Model for Screening Antidiabetic Natural Products.

    PubMed

    Tabassum, Nadia; Tai, Hongmei; Jung, Da-Woon; Williams, Darren R

    2015-01-01

    Diabetes mellitus affects millions of people worldwide and significantly impacts their quality of life. Moreover, life threatening diseases, such as myocardial infarction, blindness, and renal disorders, increase the morbidity rate associated with diabetes. Various natural products from medicinal plants have shown potential as antidiabetes agents in cell-based screening systems. However, many of these potential "hits" fail in mammalian tests, due to issues such as poor pharmacokinetics and/or toxic side effects. To address this problem, the zebrafish (Danio rerio) model has been developed as a "bridge" to provide an experimentally convenient animal-based screening system to identify drug candidates that are active in vivo. In this review, we discuss the application of zebrafish to drug screening technologies for diabetes research. Specifically, the discovery of natural product-based antidiabetes compounds using zebrafish will be described. For example, it has recently been demonstrated that antidiabetic natural compounds can be identified in zebrafish using activity guided fractionation of crude plant extracts. Moreover, the development of fluorescent-tagged glucose bioprobes has allowed the screening of natural product-based modulators of glucose homeostasis in zebrafish. We hope that the discussion of these advances will illustrate the value and simplicity of establishing zebrafish-based assays for antidiabetic compounds in natural products-based laboratories.

  9. Fishing for Nature's Hits: Establishment of the Zebrafish as a Model for Screening Antidiabetic Natural Products

    PubMed Central

    Tabassum, Nadia; Tai, Hongmei; Jung, Da-Woon; Williams, Darren R.

    2015-01-01

    Diabetes mellitus affects millions of people worldwide and significantly impacts their quality of life. Moreover, life threatening diseases, such as myocardial infarction, blindness, and renal disorders, increase the morbidity rate associated with diabetes. Various natural products from medicinal plants have shown potential as antidiabetes agents in cell-based screening systems. However, many of these potential “hits” fail in mammalian tests, due to issues such as poor pharmacokinetics and/or toxic side effects. To address this problem, the zebrafish (Danio rerio) model has been developed as a “bridge” to provide an experimentally convenient animal-based screening system to identify drug candidates that are active in vivo. In this review, we discuss the application of zebrafish to drug screening technologies for diabetes research. Specifically, the discovery of natural product-based antidiabetes compounds using zebrafish will be described. For example, it has recently been demonstrated that antidiabetic natural compounds can be identified in zebrafish using activity guided fractionation of crude plant extracts. Moreover, the development of fluorescent-tagged glucose bioprobes has allowed the screening of natural product-based modulators of glucose homeostasis in zebrafish. We hope that the discussion of these advances will illustrate the value and simplicity of establishing zebrafish-based assays for antidiabetic compounds in natural products-based laboratories. PMID:26681965

  10. Review of clinical studies of Polygonum multiflorum Thunb. and its isolated bioactive compounds

    PubMed Central

    Bounda, Guy-Armel; Feng, YU

    2015-01-01

    Polygonum multiflorum Thunb. (PMT), officially listed in the Chinese Pharmacopoeia, is one of the most popular perennial Chinese traditional medicines known as He shou wu in China and East Asia, and as Fo-ti in North America. Mounting pharmacological studies have stressed out its key benefice for the treatment of various diseases and medical conditions such as liver injury, cancer, diabetes, alopecia, atherosclerosis, and neurodegenerative diseases as well. International databases such as PubMed/Medline, Science citation Index and Google Scholar were searched for clinical studies recently published on P. multiflorum. Various clinical studies published articles were retrieved, providing information relevant to pharmacokinetics-pharmacodynamics analysis, sleep disorders, dyslipidemia treatment, and neurodegenerative diseases. This review is an effort to update the clinical picture of investigations ever carried on PMT and/or its isolated bio-compounds and to enlighten its therapeutic assessment. PMID:26130933

  11. Review of clinical studies of Polygonum multiflorum Thunb. and its isolated bioactive compounds.

    PubMed

    Bounda, Guy-Armel; Feng, Y U

    2015-01-01

    Polygonum multiflorum Thunb. (PMT), officially listed in the Chinese Pharmacopoeia, is one of the most popular perennial Chinese traditional medicines known as He shou wu in China and East Asia, and as Fo-ti in North America. Mounting pharmacological studies have stressed out its key benefice for the treatment of various diseases and medical conditions such as liver injury, cancer, diabetes, alopecia, atherosclerosis, and neurodegenerative diseases as well. International databases such as PubMed/Medline, Science citation Index and Google Scholar were searched for clinical studies recently published on P. multiflorum. Various clinical studies published articles were retrieved, providing information relevant to pharmacokinetics-pharmacodynamics analysis, sleep disorders, dyslipidemia treatment, and neurodegenerative diseases. This review is an effort to update the clinical picture of investigations ever carried on PMT and/or its isolated bio-compounds and to enlighten its therapeutic assessment. PMID:26130933

  12. [Synthesis and investigation on antidiabetic activity of 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamide].

    PubMed

    Yang, Da-Cheng; Yan, Ju-Fang; Xu, Jin; Ye, Fei; Zhou, Zu-Wen; Zhang, Wei-Yu; Fan, Li; Chen, Xin

    2010-01-01

    Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily. PMID:21351452

  13. Pharmacogenetics of Oral Antidiabetic Drugs

    PubMed Central

    Becker, Matthijs L.; Pearson, Ewan R.; Tkáč, Ivan

    2013-01-01

    Oral antidiabetic drugs (OADs) are used for more than a half-century in the treatment of type 2 diabetes. Only in the last five years, intensive research has been conducted in the pharmacogenetics of these drugs based mainly on the retrospective register studies, but only a handful of associations detected in these studies were replicated. The gene variants in CYP2C9, ABCC8/KCNJ11, and TCF7L2 were associated with the effect of sulfonylureas. CYP2C9 encodes sulfonylurea metabolizing cytochrome P450 isoenzyme 2C9, ABCC8 and KCNJ11 genes encode proteins constituting ATP-sensitive K+ channel which is a therapeutic target for sulfonylureas, and TCF7L2 is a gene with the strongest association with type 2 diabetes. SLC22A1, SLC47A1, and ATM gene variants were repeatedly associated with the response to metformin. SLC22A1 and SLC47A1 encode metformin transporters OCT1 and MATE1, respectively. The function of a gene variant near ATM gene identified by a genome-wide association study is not elucidated so far. The first variant associated with the response to gliptins is a polymorphism in the proximity of CTRB1/2 gene which encodes chymotrypsinogen. Establishment of diabetes pharmacogenetics consortia and reduction in costs of genomics might lead to some significant clinical breakthroughs in this field in a near future. PMID:24324494

  14. Isolation and identification of bioactive compounds from chloroform fraction of methanolic extract of Carissa opaca roots.

    PubMed

    Ahmed, Dildar; Fatima, Khaizran; Saeed, Ramsha; Masih, Rashid

    2016-09-01

    Carissa opaca is a shrub known for its variety of medicinal applications. This study reports isolation and identification of four chemical compounds from its roots for the first time. The methanolic extract of the roots was fractionated into various solvents with increasing polarity. Chloroform fraction was subjected to column and thin layer chromatography to ultimately yield 2H-cyclopropanaphthalene-2-one, 7-hydroxy-6-methoxy-2H-1-benzopyran-2-one, 3-(4-methoxyphenyl)-2,6-dimethylbenzofuran and 5(1H)-azulenone, 2,4,6,7,8,8a-hexahydro-3,8-dimethyl-4-(1-methylethylidene)-,(8S-cis). They were identified by GC-MS analysis. The compounds exhibited considerable antimicrobial activities against Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger with zones of inhibition ranging from 10 to 13 mm as compared to the standard drug amoxicillin with zones of inhibition 13-17 mm under the similar conditions. In conclusion, the roots of C. opaca can provide new leads for future antimicrobial drugs.

  15. Effects-driven chemical fractionation of heavy fuel oil to isolate compounds toxic to trout embryos.

    PubMed

    Bornstein, Jason M; Adams, Julie; Hollebone, Bruce; King, Thomas; Hodson, Peter V; Brown, R Stephen

    2014-04-01

    Heavy fuel oil (HFO) spills account for approximately 60% of ship-source oil spills and are up to 50 times more toxic than medium and light crude oils. Heavy fuel oils contain elevated concentrations of polycyclic aromatic hydrocarbons (PAHs) and alkyl-PAHs, known to be toxic to fish; however, little direct characterization of HFO toxicity has been reported. An effects-driven chemical fractionation was conducted on HFO 7102 to separate compounds with similar chemical and physical properties, including toxicity, to isolate the groups of compounds most toxic to trout embryos. After each separation, toxicity tests directed the next phase of fractionation, and gas chromatography-mass spectrometry analysis correlated composition with toxicity, with a focus on PAHs. Low-temperature vacuum distillation permitted the separation of HFO into 3 fractions based on boiling point ranges. The most toxic of these fractions underwent wax precipitation to remove long-chain n-alkanes. The remaining PAH-rich extract was further separated using open column chromatography, which provided distinct fractions that were grouped according to increasing aromatic ring count. The most toxic of these fractions was richest in PAHs and alkyl-PAHs. The results of the present study were consistent with previous crude oil studies that identified PAH-rich fractions as the most toxic. PMID:24375845

  16. Effects-driven chemical fractionation of heavy fuel oil to isolate compounds toxic to trout embryos.

    PubMed

    Bornstein, Jason M; Adams, Julie; Hollebone, Bruce; King, Thomas; Hodson, Peter V; Brown, R Stephen

    2014-04-01

    Heavy fuel oil (HFO) spills account for approximately 60% of ship-source oil spills and are up to 50 times more toxic than medium and light crude oils. Heavy fuel oils contain elevated concentrations of polycyclic aromatic hydrocarbons (PAHs) and alkyl-PAHs, known to be toxic to fish; however, little direct characterization of HFO toxicity has been reported. An effects-driven chemical fractionation was conducted on HFO 7102 to separate compounds with similar chemical and physical properties, including toxicity, to isolate the groups of compounds most toxic to trout embryos. After each separation, toxicity tests directed the next phase of fractionation, and gas chromatography-mass spectrometry analysis correlated composition with toxicity, with a focus on PAHs. Low-temperature vacuum distillation permitted the separation of HFO into 3 fractions based on boiling point ranges. The most toxic of these fractions underwent wax precipitation to remove long-chain n-alkanes. The remaining PAH-rich extract was further separated using open column chromatography, which provided distinct fractions that were grouped according to increasing aromatic ring count. The most toxic of these fractions was richest in PAHs and alkyl-PAHs. The results of the present study were consistent with previous crude oil studies that identified PAH-rich fractions as the most toxic.

  17. In vitro antitumoral activity of compounds isolated from Artemisia gorgonum Webb.

    PubMed

    Martins, Alice; Mignon, Rukmini; Bastos, Marina; Batista, Daniela; Neng, Nuno R; Nogueira, José M F; Vizetto-Duarte, Catarina; Custódio, Luísa; Varela, João; Rauter, Amélia P

    2014-09-01

    Artemisia gorgonum (Asteraceae) is an endemic plant to the Cape Verde islands and plays an important role in traditional medicine. The chloroform extract of the plant aerial parts afforded six sesquiterpene lactones, two methoxylated flavonoids, two lignans, and one tetracyclic triterpene, which were isolated by chromatographic methods and their structure established by physical and spectroscopic techniques. The cytotoxic activity of the three major constituents, namely, arborescin, artemetin, and sesamin, was evaluated on neuroblastoma (SH-SY5Y), hepatocarcinoma (HepG2), and nontumoral bone marrow stromal (S17) cell lines. The application of different concentrations of the compounds significantly decreased tumor cells viability at different extents, especially at the highest concentrations tested. Arborescin is the most promising compound as it was able to reduce tumoral cell viability with an IC50 significantly lower (229-233 μM; p < 0.01) than that of S17 cells (445 μM). Arborescin and artemetin were less toxic to nontumoral cells than the antitumoral drug tested, etoposide. Our results indicate that arborescin has a significant cytotoxic activity in vitro, more pronounced on the cancer cell lines, confirming A. gorgonum as a source of potential antitumoral molecules. PMID:24633846

  18. Membrane filtration of agro-industrial wastewaters and isolation of organic compounds with high added values.

    PubMed

    Zagklis, Dimitris P; Paraskeva, Christakis A

    2014-01-01

    The aim of the current study was the exploitation of agro-industrial wastes or by-products such as olive mill wastewater (OMW) and defective wines. A cost-effective system for their maximum exploitation is suggested, using a combined process of membrane filtration and other physicochemical processes. Wastewaters are first treated in a membrane system (prefiltration, ultrafiltration, nanofiltration, and reverse osmosis) where pure water and other organic fractions (by-products) are obtained. Organic fractions, called hereafter byproducts and not wastes, are further treated for the separation of organic compounds and isolation of high added value products. Experiments were performed with OMW and defective wines as characteristic agro-industrial wastewaters. Profit from the exploitation of agro-industrial wastewaters can readily help the depreciation of the indeed high cost process of membrane filtration. The simple phenolic fraction of the OMW was successfully isolated from the rest of the waste, and problems occurring during winemaking, such as high volatile acidity and odours, were tackled.

  19. Membrane filtration of agro-industrial wastewaters and isolation of organic compounds with high added values.

    PubMed

    Zagklis, Dimitris P; Paraskeva, Christakis A

    2014-01-01

    The aim of the current study was the exploitation of agro-industrial wastes or by-products such as olive mill wastewater (OMW) and defective wines. A cost-effective system for their maximum exploitation is suggested, using a combined process of membrane filtration and other physicochemical processes. Wastewaters are first treated in a membrane system (prefiltration, ultrafiltration, nanofiltration, and reverse osmosis) where pure water and other organic fractions (by-products) are obtained. Organic fractions, called hereafter byproducts and not wastes, are further treated for the separation of organic compounds and isolation of high added value products. Experiments were performed with OMW and defective wines as characteristic agro-industrial wastewaters. Profit from the exploitation of agro-industrial wastewaters can readily help the depreciation of the indeed high cost process of membrane filtration. The simple phenolic fraction of the OMW was successfully isolated from the rest of the waste, and problems occurring during winemaking, such as high volatile acidity and odours, were tackled. PMID:24434988

  20. Antitumour compounds from a saline soil isolate, Streptomyces griseoincarnatus CTF15.

    PubMed

    Sajid, Imran; Shaaban, Khaled A; Hasnain, Shahida

    2011-03-01

    A new actinomycete strain designated as Streptomyces sp. CTF15 was isolated from a saline soil using casein-KNO(3) agar medium. The strain Streptomyces sp. CTF15 exhibited promising antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Streptomyces viridochromogens Tu57 and high cytotoxicity (91.2% mortality) against Artimia salina in biological screening. The cultivation of this strain in a 50 L lab fermenter and subsequent isolation and purification by a series of chromatographic techniques and structure elucidation by MS and NMR analysis of the active metabolites revealed that it is a highly stable producer of resistomycin (1), tetracenomycin D (2) and actinomycin D (3), even under non-optimised culture conditions. The morphological, microscopic, biochemical and physiological characterisation suggested that the strain CTF15 belongs to the genus Streptomyces. A partial 16S rRNA gene sequence (1429 bp) from the strain CTF15 was determined and found to have high identity (99%) with Streptomyces griseoincarnatus. As such, this is the first report of a strain of S. griseoincarnatus capable of producing these three bioactive compounds simultaneously.

  1. Isolation and Structural Elucidation of Antiproliferative Compounds of Lipidic Fractions from White Shrimp Muscle (Litopenaeus vannamei)

    PubMed Central

    López-Saiz, Carmen-María; Velázquez, Carlos; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2014-01-01

    Shrimp is one of the most popular seafood items worldwide, and has been reported as a source of chemopreventive compounds. In this study, shrimp lipids were separated by solvent partition and further fractionated by semi-preparative RP-HPLC and finally by open column chromatography in order to obtain isolated antiproliferative compounds. Antiproliferative activity was assessed by inhibition of M12.C3.F6 murine cell growth using the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide) assay. The methanolic fraction showed the highest antiproliferative activity; this fraction was separated into 15 different sub-fractions (M1–M15). Fractions M8, M9, M10, M12, and M13 were antiproliferative at 100 µg/mL and they were further tested at lower concentrations. Fractions M12 and M13 exerted the highest growth inhibition with an IC50 of 19.5 ± 8.6 and 34.9 ± 7.3 µg/mL, respectively. Fraction M12 was further fractionated in three sub-fractions M12a, M12b, and M12c. Fraction M12a was identified as di-ethyl-hexyl-phthalate, fraction M12b as a triglyceride substituted by at least two fatty acids (predominantly oleic acid accompanied with eicosapentaenoic acid) and fraction M12c as another triglyceride substituted with eicosapentaenoic acid and saturated fatty acids. Bioactive triglyceride contained in M12c exerted the highest antiproliferative activity with an IC50 of 11.33 ± 5.6 µg/mL. Biological activity in shrimp had been previously attributed to astaxanthin; this study demonstrated that polyunsaturated fatty acids are the main compounds responsible for antiproliferative activity. PMID:25526568

  2. Isolation and structural elucidation of antiproliferative compounds of lipidic fractions from white shrimp muscle (Litopenaeus vannamei).

    PubMed

    López-Saiz, Carmen-María; Velázquez, Carlos; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2014-01-01

    Shrimp is one of the most popular seafood items worldwide, and has been reported as a source of chemopreventive compounds. In this study, shrimp lipids were separated by solvent partition and further fractionated by semi-preparative RP-HPLC and finally by open column chromatography in order to obtain isolated antiproliferative compounds. Antiproliferative activity was assessed by inhibition of M12.C3.F6 murine cell growth using the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide) assay. The methanolic fraction showed the highest antiproliferative activity; this fraction was separated into 15 different sub-fractions (M1-M15). Fractions M8, M9, M10, M12, and M13 were antiproliferative at 100 µg/mL and they were further tested at lower concentrations. Fractions M12 and M13 exerted the highest growth inhibition with an IC50 of 19.5 ± 8.6 and 34.9 ± 7.3 µg/mL, respectively. Fraction M12 was further fractionated in three sub-fractions M12a, M12b, and M12c. Fraction M12a was identified as di-ethyl-hexyl-phthalate, fraction M12b as a triglyceride substituted by at least two fatty acids (predominantly oleic acid accompanied with eicosapentaenoic acid) and fraction M12c as another triglyceride substituted with eicosapentaenoic acid and saturated fatty acids. Bioactive triglyceride contained in M12c exerted the highest antiproliferative activity with an IC50 of 11.33 ± 5.6 µg/mL. Biological activity in shrimp had been previously attributed to astaxanthin; this study demonstrated that polyunsaturated fatty acids are the main compounds responsible for antiproliferative activity. PMID:25526568

  3. Isolation, structure elucidation and enzyme inhibition studies of a new hydroxy ester and other compounds from Berberis jaeschkeana Schneid stem.

    PubMed

    Alamzeb, Muhammad; Khan, M Rafiullah; Mamoon-Ur-Rashid; Ali, Saqib; Khan, Ashfaq Ahmad

    2015-01-01

    Bioassay-guided isolation and fractionation of Berberis jaeschkeana Schneid var. jaeschkeana stem resulted in the isolation and characterisation of a new long chain hydroxy ester named as berberinol (1) along with six known compounds (2-7). All the structures were established from 1D and 2D spectroscopic data. Crude extract, sub-fractions and all the isolated compounds were evaluated for their anti-fungal and urease enzyme inhibition properties. All of the sub-fractions and compounds showed good anti-fungal and urease enzyme inhibition properties. Minimum inhibitory concentrations (MICs) were calculated for all active samples in case of urease enzyme inhibition. MICs values were found to be in the range of 39.03-49.78 μg/mL for urease enzyme inhibition.

  4. Isolation and Identification of Antifungal Compounds from Bacillus subtilis C9 Inhibiting the Growth of Plant Pathogenic Fungi

    PubMed Central

    Islam, Md. Rezuanul; Jeong, Yong Tae; Lee, Yong Se

    2012-01-01

    Antagonistic microorganisms against Rhizoctonia solani were isolated and their antifungal activities were investigated. Two hundred sixteen bacterial isolates were isolated from various soil samples and 19 isolates were found to antagonize the selected plant pathogenic fungi with varying degrees. Among them, isolate C9 was selected as an antagonistic microorganism with potential for use in further studies. Treatment with the selected isolate C9 resulted in significantly reduced incidence of stem-segment colonization by R. solani AG2-2(IV) in Zoysia grass and enhanced growth of grass. Through its biochemical, physiological, and 16S rDNA characteristics, the selected bacterium was identified as Bacillus subtilis subsp. subtilis. Mannitol (1%) and soytone (1%) were found to be the best carbon and nitrogen sources, respectively, for use in antibiotic production. An antibiotic compound, designated as DG4, was separated and purified from ethyl acetate extract of the culture broth of isolate C9. On the basis of spectral data, including proton nuclear magneric resonance (1H NMR), carbon nuclear magneric resonance (13C NMR), and mass analyses, its chemical structure was established as a stereoisomer of acetylbutanediol. Application of the ethyl acetate extract of isolate C9 to several plant pathogens resulted in dose-dependent inhibition. Treatment with the purified compound (an isomer of acetylbuanediol) resulted in significantly inhibited growth of tested pathogens. The cell free culture supernatant of isolate C9 showed a chitinase effect on chitin medium. Results from the present study demonstrated the significant potential of the purified compound from isolate C9 for use as a biocontrol agent as well as a plant growth promoter with the ability to trigger induced systemic resistance of plants. PMID:22783136

  5. A new iridoid glycoside and potential MRB inhibitory activity of isolated compounds from the rhizomes of Cyperus rotundus L.

    PubMed

    Zhou, Zhongliu; Yin, Wenqing; Zhang, Hualin; Feng, Zongcai; Xia, Jingmin

    2013-01-01

    A new iridoid glycoside, rotunduside (1), along with four known iridoid glycosides, 10-O-p-hydroxybenzoyltheviridoside (2), 10-O-vanilloyltheviridoside (3), 6″-O-(trans-p-coumaroyl)-procumbide (4) and loganic acid (5), was isolated from the rhizomes of Cyperus rotundus L. Their chemical structures were elucidated on the basis of UV, IR, MS and NMR spectroscopic analyses. In addition, the macrophages respiratory burst (MRB) inhibitory activity of the isolated compounds was reported. Compound 2 exhibited considerable MRB inhibitory activity in the test with IC50 value of ~37 μM. PMID:23356789

  6. Bis(4-hydroxybenzyl)sulfide: a sulfur compound inhibitor of histone deacetylase isolated from root extract of Pleuropterus ciliinervis.

    PubMed

    Son, Il Hong; Lee, Sung Ik; Yang, Hyun Duk; Moon, Hyung-In

    2007-01-01

    A sulfur compound, bis(4-hydroxybenzyl)sulfide (1) was isolated from the root extract of Pleuropterus ciliinervis. Its structure was elucidated using NMR spectroscopic techniques and mass spectrometric analysis. Compound 1 showed potent inhibitory activity in a histone deacetylase (HDAC) enzyme assay. It also exhibited growth inhibitory activity on five human tumor cell lines and more sensitive inhibitory activity on the MDA-MB-231 breast tumor cell line. PMID:17851433

  7. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.

    PubMed

    Ammirati, Mark; Bagley, Scott W; Bhattacharya, Samit K; Buckbinder, Leonard; Carlo, Anthony A; Conrad, Rebecca; Cortes, Christian; Dow, Robert L; Dowling, Matthew S; El-Kattan, Ayman; Ford, Kristen; Guimarães, Cristiano R W; Hepworth, David; Jiao, Wenhua; LaPerle, Jennifer; Liu, Shenping; Londregan, Allyn; Loria, Paula M; Mathiowetz, Alan M; Munchhof, Michael; Orr, Suvi T M; Petersen, Donna N; Price, David A; Skoura, Athanasia; Smith, Aaron C; Wang, Jian

    2015-11-12

    Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, a tool compound, 16 (PF-6260933) and a lead 17 possessing excellent kinome selectivity and suitable properties were delivered to establish proof of concept in vivo. The medicinal chemistry effort that led to the discovery of these lead compounds is described herein together with in vivo pharmacokinetic properties and activity in a model of insulin resistance. PMID:26617966

  8. Isolation and identification of mosquito larvicidal compound from Abutilon indicum (Linn.) Sweet.

    PubMed

    Abdul Rahuman, A; Gopalakrishnan, Geetha; Venkatesan, P; Geetha, Kannappan

    2008-04-01

    Larvicidal activity of crude hexane, ethyl acetate, petroleum ether, acetone and methanol extracts of five medicinal plants, Abutilon indicum, Aegle marmelos, Euphorbia thymifolia, Jatropha gossypifolia and Solanum torvum were assayed for their toxicity against the early fourth-instar larvae of Culex quinquefasciatus. The larval mortality was observed after 24 h exposure. All extracts showed moderate larvicidal effects; however, the highest larval mortality was found in petroleum ether extract of A. indicum. In the present study, bioassay-guided fractionation of A. indicum led to the separation and identification of a beta-sitosterol as a potential new mosquito larvicidal compound with LC50 value of 11.49, 3.58 and 26.67 ppm against Aedes aegypti L, Anopheles stephensi Liston and C. quinquefasciatus Say (Diptera: Culicidae), respectively. 1H NMR, 13C NMR and mass spectral data confirmed the identification of the active compound. beta-sitosterol has been recognized as the active ingredient of many medicinal plant extracts. All the crude extracts when screened for their larvicidal activities indicated toxicity against the larvae of C. quinquefasciatus. This article reports the isolation and identification of the beta-sitosterol as well as bioassay data for the crude extracts. There are no reports of beta-sitosterol in the genus A. indicum, and their larvicidal activities are being evaluated for the first time. Results of this study show that the petroleum ether extract of A. indicum may be considered as a potent source and beta-sitosterol as a new natural mosquito larvicidal agent. PMID:18176816

  9. Immunomodulatory Effects of a Bioactive Compound Isolated from Dryopteris crassirhizoma on the Grass Carp Ctenopharyngodon idella

    PubMed Central

    Chi, Cheng; Giri, Sib Sankar; Jun, Jin Woo; Kim, Hyoun Joong; Yun, Saekil; Kim, Sang Guen

    2016-01-01

    In the present study, we investigated effects of compound kaempferol 3-a-L-(4-O-acetyl)rhamnopyranoside-7-a-L-rhamnopyranoside (SA) isolated from Dryopteris crassirhizoma during immune-related gene expression in Ctenopharyngodon idella head kidney macrophages (CIHKM). The expression of immune-related genes (IL-1β, TNF-α, MyD88, and Mx1) were investigated using real-time PCR at 2 h, 8 h, 12 h, and 24 h after incubation with 1, 10, and 50 μg mL−1 of SA. Furthermore, fish were injected intraperitoneally with 100 μL of SA, and immune parameters such as lysozyme activity, complement C3, SOD, phagocytic activity, and IgM level were examined at 1, 2, and 3 weeks after injection. The differential expression of cytokines was observed after exposure to SA. IL-1β genes displayed significant expression at 2 and 8 h after exposure to 1–10 μg mL−1 of SA. SA also induced gene expression of cytokines such as MyD88, Mx1, and TNF-α. Furthermore, enhanced immune parameters in grass carp confirmed the immunomodulatory activity of SA. Interestingly, this compound has no toxic effect on CIHKM cells as tested by MTT assay. In addition, fish immunised with 10 μg mL−1 of SA exhibited maximum resistance against Aeromonas hydrophila infection. These results suggest that SA has the potential to stimulate immune responses in grass carp. PMID:27294155

  10. Antidiabetic potential of oleanolic acid from Ligustrum lucidum Ait.

    PubMed

    Gao, Dawei; Li, Qingwang; Li, Ying; Liu, Zhihua; Liu, Zhiwei; Fan, Yusheng; Han, Zengsheng; Li, Jian; Li, Kun

    2007-11-01

    Ligustrum lucidum Ait. has been used in traditional Chinese medicine for over 1000 years because of its anti-tumor, antimutagenic, antidiabetic, and hepatoprotective properties. The aim of this study was to determine whether oleanolic acid (OA) is the principal active compound of L. lucidum responsible for its antidiabetic properties, and to examine its effect on the expression of thyroid hormones and insulin secretion, thus revealing the mechanism by which L. lucidum modulates insulin levels in diabetes. When rats with streptozotocin-induced diabetes were treated with OA (100 and 200 mg/kg body mass per day, for 40 days), the changes in blood glucose levels and in oral glucose tolerance tests showed that hypoglycemia was more pronounced in OA-treated groups than in the diabetic control rats, and that the levels of triglyceride, total cholesterol, and low-density lipoportein cholesterol in OA-treated rats were lower than those in the diabetic control rats, whose high-density lipoprotein cholesterol increased. OA-treated rats also gained weight, and exhibited increased serum insulin levels. In contrast, OA treatment did not effect the levels of thyroid hormone or TSH in rats with streptozotocin-induced diabetes. These results indicate that OA has hypoglycemic and hypolipidemic effects. OA treatment might stimulate insulin release, and consequently, results in the modulation of glucose levels and regulation of lipid metabolism. PMID:18066109

  11. Anti-oxidative and cholinesterase inhibitory effects of leaf extracts and their isolated compounds from two closely related Croton species.

    PubMed

    Ndhlala, Ashwell R; Aderogba, Mutalib A; Ncube, Bhekumthetho; Van Staden, Johannes

    2013-02-01

    A comparative evaluation of the antioxidant and acetylcholinesterase inhibitory activity of the leaf extracts of Croton gratissimus and Croton zambesicus (subgratissimus) and compounds isolated from the extracts was carried out to determine their potential and suitability or otherwise as a substitute for each other in the management of oxidative and neurodegenerative conditions. Different antioxidant assays (DPPH, FRAP, β-carotene-linoleic and the lipid peroxidation models) and the microplate assay for acetylcholinesterase (AChE) inhibition were carried out separately to study the activities of the crude leaf extracts and four solvent fractions from each of the two Croton species. Bioassay guided fractionation was used to target antioxidant constituents of the crude extracts and ethyl acetate fractions of 20% aqueous methanol extract of C. gratissimus on silica gel and Sephadex LH-20 columns resulted in the isolation of kaempferol-3-O-β-6''(p-coumaroyl) glucopyranoside (tiliroside, 2), apigenin-6-C-glucoside (isovitexin, 3) and kampferol (4). The extract of C. zambesicus yielded quercetin-3-O-β-6''(p-coumaroyl) glucopyranoside-3'-methyl ether (helichrysoside- 3'-methyl ether, 1), kaempferol-3-O-β-6''(p-coumaroyl) glucopyranoside (tiliroside, 2) and apigenin-6-C-glucoside (isovitexin, 3). Three of the isolated compounds and their different combinations were also included in the bioassays. In all the assays performed, the antioxidant capacity and AChE inhibitory effects of C. zambesicus extracts were weaker than those of C. gratissimus. This suggests that C. gratissimus may not be substituted by C. zambesicus, despite the similarity in some of their constituents. Generally, the combinations made from the isolated compounds showed better activities in most of the assays compared to the individual isolated compounds. This suggests mechanisms such as synergism and/or additive effects to be taking place. This study established low, moderate and high antioxidant

  12. Investigation of gastroprotective compounds at subcellular level in isolated gastric mucosal cells.

    PubMed

    Nagy, L; Morales, R E; Beinborn, M; Vattay, P; Szabo, S

    2000-12-01

    We tested the hypothesis that recognized gastroprotective agents exert direct protection against ethanol-induced injury in isolated rat gastric mucosal cells in vitro. If protection exists, we also wanted to identify subcellular targets in the reversible and/or irreversible stages of cell injury. Ethanol-induced cell injury was quantified by measuring plasma membrane leakage (trypan blue exclusion and lactate dehydrogenase release), mitochondrial integrity (succinic dehydrogenase), and nuclear damage (ethidium bromide-DNA fluorescence). Initial cell viability and responsiveness were estimated by the effects of carbachol, carbachol + atropine, or 16,16-dimethyl-PGE(2) on chief cell pepsinogen secretion. Enriched parietal cells were stimulated by histamine, carbachol, or histamine + IBMX. Preincubation of cells with PG, sucrose octasulfate, or the sulfhydryl compounds N-acetylcysteine, taurine, or cysteamine increased cell resistance

  13. Antipoliovirus Activity of the Organic Extract of Eupatorium buniifolium: Isolation of Euparin as an Active Compound

    PubMed Central

    Visintini Jaime, María Florencia; Campos, Rodolfo H.; Martino, Virginia S.; Cavallaro, Lucía V.; Muschietti, Liliana V.

    2013-01-01

    The antiviral activity of the organic extract (OE) of Eupatorium buniifolium against poliovirus type 1 was determined by in vitro assays with an effective concentration 50 (EC50) of 23.3 ± 3.3 µg/mL. Bioassay-guided fractionation of the OE allowed the isolation of an active principle that was identified by spectroscopic methods (1H- and 13C-NMR, EI-MS, UV, and IR spectroscopy) as the benzofuran euparin. The plaque reduction assay in Vero cells was used to assess the antiviral activity of euparin against poliovirus types 1, 2, and 3 with EC50 values of 0.47, 0.12, and 0.15 µg/mL, respectively. Moreover, this compound showed high selectivity indexes of 284.9, 1068, and 854.7, respectively. In order to identify the mechanism by which euparin exerts its antiviral activity, the virucidal effect, the pretreatment of Vero cells, and the time of action on one viral replication cycle were evaluated. Results obtained demonstrated that euparin exerts its effect during the early events of the replication cycle, from the virus adsorption to cells up to the first twenty minutes after infection. This is the first report on the presence of euparin in E. buniifolium and its antiviral activity. PMID:23956770

  14. Isolation and characterization of indigenous Streptomyces and Lentzea strains from soils containing boron compounds in Argentina.

    PubMed

    Moraga, Norma Beatriz; Poma, Hugo Ramiro; Amoroso, María Julia; Rajal, Verónica Beatriz

    2014-06-01

    The Salta Province - in the northwest of Argentina - is the main worldwide producer of hydroboracite and leads in exports of boron mineral and its derivatives in Latin America. In addition to the natural presence of boron compounds in the soils, there are others contaminated due to the boron mining industry. Although some bacteria are known to require boron for their growth or to be capable of storing boron, no studies have been published about Streptomyces or Lentzea genera's capacity to tolerate high boron concentrations, or about their metabolic capacities in boron contaminated environments. The results of this research show the isolation and molecular characterization of eight strains belonging to the actinobacteria phylum collected from different soils contaminated with high boron concentration in Salta state. The boron tolerance assays, which show that three of the strains were able to tolerate up 60-80 mM boron, demonstrate the potential capability of this group of bacteria to grow and maybe to remove boron from the environment. They appear to be promising, considering that these microorganisms are infrequent pathogens, are metabolically versatile and many Streptomyces can synthesize boron containing metabolites. PMID:23686918

  15. Compound-specific chlorine isotope analysis of polychlorinated biphenyls isolated from Aroclor and Clophen technical mixtures.

    PubMed

    Mandalakis, Manolis; Holmstrand, Henry; Andersson, Per; Gustafsson, Orjan

    2008-03-01

    Compound-specific chlorine isotope analysis (CSIA-Cl) is promising as a novel and powerful method for monitoring in situ degradation of organochlorines in the environment and for source fingerprinting purposes. In order to apply CSIA-Cl in field studies of polychlorinated biphenyls (PCBs), the chlorine isotopic composition (delta(37)Cl) of individual PCB congeners in source materials must be known. In the present study, we determined delta(37)Cl of 18 congeners isolated from three widely produced technical mixtures. All congeners provided delta(37)Cl ranging between -1.9 per thousand and -3.5 per thousand. Although the comparable products Aroclor 1242 (-2.0 per thousand to -2.5 per thousand) and Clophen A30 (-1.9 per thousand to -3.0 per thousand) were synthesized by different industries, they provided similar delta(37)Cl for the same type of congeners. On the contrary, the more chlorinated congeners present in Aroclor 1254 (-2.1 to -3.5 per thousand) were more (37)Cl depleted compared to Aroclor 1242 manufactured by the same company. Overall, delta(37)Cl of PCB congeners decreased by -0.26 per thousand for each additional chlorine atom.

  16. Identification and bioactivity of compounds from the fungus Penicillium sp. CYE-87 isolated from a marine tunicate.

    PubMed

    Shaala, Lamiaa A; Youssef, Diaa T A

    2015-04-01

    In the course of our continuous interest in identifying bioactive compounds from marine microbes, we have investigated a tunicate-derived fungus, Penicillium sp. CYE-87. A new compound with the 1,4-diazepane skeleton, terretrione D (2), together with the known compounds, methyl-2-([2-(1H-indol-3-yl)ethyl]carbamoyl)acetate (1), tryptamine (3), indole-3-carbaldehyde (4), 3,6-diisobutylpyrazin-2(1H)-one (5) and terretrione C (6), were isolated from Penicillium sp. CYE-87. The structures of the isolated compounds were established by spectral analysis, including 1D (1H, 13C) and 2D (COSY, multiplicity edited-HSQC and HMBC) NMR and HRESIMS, as well as comparison of their NMR data with those in the literature. The compounds were evaluated for their antimigratory activity against the human breast cancer cell line (MDA-MB-231) and their antiproliferation activity against HeLa cells. Compounds 2 and 6 showed significant antimigratory activity against MDA-MB-231, as well as antifungal activity against C. albicans. PMID:25815893

  17. Characterization of an Antibacterial Compound, 2-Hydroxyl Indole-3-Propanamide, Produced by Lactic Acid Bacteria Isolated from Fermented Batter.

    PubMed

    Jeevaratnam, Kadirvelu; Vidhyasagar, Venkatasubramanian; Agaliya, Perumal Jayaprabha; Saraniya, Appukuttan; Umaiyaparvathy, Muthukandan

    2015-09-01

    Lactic acid bacteria are known to produce numerous antimicrobial compounds that are active against various pathogens. Here, we have purified and characterized a novel low-molecular-weight (LMW) antimicrobial compound produced by Lactobacillus and Pediococcus isolated from fermented idly and uttapam batter. The LMW compound was extracted from cell-free supernatant using ice-cold acetone, purified by gel permeation and hydrophobic interaction chromatography. It exhibited antimicrobial activity against Gram-positive and Gram-negative pathogenic bacteria sparing the probiotic strains like Lactobacillus rhamnosus. The molecular weight of the LMW compound was identified as 204 Da using LC-MS-ESI. In addition, the structure of the compound was predicted using spectroscopic methods like FTIR and NMR and identified as 2-hydroxyl indole-3-propanamide. The LMW compound was differentiated from its related compound, tryptophan, by Salkowski reaction and thin-layer chromatography. This novel LMW compound, 2-hydroxyl indole-3-propanamide, may have an effective application as an antibiotic which can spare prevailing probiotic organisms but target only the pathogenic strains.

  18. Why Antidiabetic Vanadium Complexes are Not in the Pipeline of “Big Pharma” Drug Research? A Critical Review

    PubMed Central

    Scior, Thomas; Guevara-Garcia, Jose Antonio; Do, Quoc-Tuan; Bernard, Philippe; Laufer, Stefan

    2016-01-01

    Public academic research sites, private institutions as well as small companies have made substantial contributions to the ongoing development of antidiabetic vanadium compounds. But why is this endeavor not echoed by the globally operating pharmaceutical companies, also known as “Big Pharma”? Intriguingly, today’s clinical practice is in great need to improve or replace insulin treatment against Diabetes Mellitus (DM). Insulin is the mainstay therapeutically and economically. So, why do those companies develop potential antidiabetic drug candidates without vanadium (vanadium-free)? We gathered information about physicochemical and pharmacological properties of known vanadium-containing antidiabetic compounds from the specialized literature, and converted the data into explanations (arguments, the “pros and cons”) about the underpinnings of antidiabetic vanadium. Some discoveries were embedded in chronological order while seminal reviews of the last decade about the Medicinal chemistry of vanadium and its history were also listed for further understanding. In particular, the concepts of so-called “noncomplexed or free” vanadium species (i.e. inorganic oxido-coordinated species) and “biogenic speciation” of antidiabetic vanadium complexes were found critical and subsequently documented in more details to answer the question. PMID:26997154

  19. Antioxidant Activity of Marine Algal Polyphenolic Compounds: A Mechanistic Approach.

    PubMed

    Fernando, I P Shanura; Kim, Misook; Son, Kwang-Tae; Jeong, Yoonhwa; Jeon, You-Jin

    2016-07-01

    Polyphenolic compounds isolated from marine algae exhibit a broad spectrum of beneficial biological properties, including antioxidant, anticancer, antimicrobial, anti-inflammatory, and antidiabetic activities, along with several other bioactivities centered on their antioxidant properties. Consequently, polyphenolic compounds are increasingly being investigated for their potential use in food, cosmetic, and pharmaceutical applications. The antioxidant activities of these compounds have been explored widely through experimental studies. Nonetheless, a theoretical understanding of the structural and electronic properties could broaden research perspectives, leading to the identification and synthesis of efficient structural analogs with prophylactic uses. This review briefly summarizes the current state of knowledge regarding antioxidant polyphenolic compounds in marine algae with an attempt to describe the structure-activity relationship. PMID:27332715

  20. Novel Antiphytopathogenic Compound 2-Heptyl-5-Hexylfuran-3-Carboxylic Acid, Produced by Newly Isolated Pseudomonas sp. Strain SJT25 ▿†

    PubMed Central

    Wang, Xiao-Ying; Xu, Yu-Quan; Lin, Shuang-Jun; Liu, Zhen-Zhen; Zhong, Jian-Jiang

    2011-01-01

    Pseudomonas sp. strain SJT25, which strongly antagonizes plant pathogens, was isolated from rice rhizosphere soil by a bioactivity-guided approach. A novel antiphytopathogenic compound was isolated from the fermentation broth of Pseudomonas sp. SJT25 and identified as 2-heptyl-5-hexylfuran-3-carboxylic acid. This compound showed antimicrobial activities both in vitro and in vivo. PMID:21742907

  1. Interaction of mouse intestinal P-glycoprotein with oral antidiabetic drugs and its inhibitors.

    PubMed

    Kalsi, Harman; Grewal, Ravneet K

    2015-09-01

    Type 2 diabetes (T2DM) is a progressive insulin secretory defect accompanied by resistance to insulin, and thereby making glycemic control a major concern in the treatment of these patients. Oral drug administration, though a popular option for its non-invasiveness, suffer from poor bioavailability. It could be related to the efflux transport of intestinal P-glycoprotein (Pgp). In the present study, we explored the binding interactions of antidiabetic drugs i.e., sulfonylurea drugs (glimepiride, glipizide, glyburide) and rapid acting insulin secretagogues viz., nateglinide, repaglinide and rosiglitazone; and Pgp inhibitors i.e., Generation I (verapamil and tamoxifen), III (tetradrine and tariquidar), and natural inhibitors (fumagillin and piperine) in mouse Pgp model. Our results revealed that fumagillin piperine and verapamil possess maximum interaction energies with Pgp compared to antidiabetic drugs. These observations elucidate the role of fumagillin and piperine as potential natural compounds which could intervene in the efflux action of Pgp in extruding the antidiabetic drugs and may have implications for increasing efficacy of oral antidiabetic therapy. PMID:26548081

  2. Botanical, Pharmacological, Phytochemical, and Toxicological Aspects of the Antidiabetic Plant Bidens pilosa L.

    PubMed Central

    2014-01-01

    Bidens pilosa L. is an easy-to-grow, widespread, and palatable perennial on earth. Hence, it has traditionally been used as foods and medicines without noticeable adverse effects. Despite significant advancement in chemical and biological studies of B. pilosa over the past few years, comprehensive and critical reviews on its anti-diabetic properties are missing. The present review is to summarize up-to-date information on the pharmacology, phytochemistry, and toxicology of B. pilosa, in regard to type 1 diabetes and type 2 diabetes from the literature. In addition to botanical studies and records of the traditional use of B. pilosa in diabetes, scientific studies investigating antidiabetic action of this species and its active phytochemicals are presented and discussed. The structure and biosynthesis of B. pilosa and its polyynes in relation to their anti-diabetic action and mechanism are emphasized. Although some progress has been made, rigorous efforts are further required to unlock the molecular basis and structure-activity relationship of the polyynes isolated from B. pilosa before their clinical applications. The present review provides preliminary information and gives guidance for further anti-diabetic research and development of this plant. PMID:24616740

  3. Evaluation of Mixed Probiotic Starter Cultures Isolated from Kimchi on Physicochemical and Functional Properties, and Volatile Compounds of Fermented Hams

    PubMed Central

    Yoo, Seung Seok

    2016-01-01

    The objective of this study was to investigate the effects of mixed starter cultures isolated from kimchi on physicochemical properties, functionality and flavors of fermented ham. Physicochemical properties, microbial counts, shear force, cholesterol contents and volatile compounds of fermented ham were investigated during processing (curing and ripening time). Curing process for 7 d increased saltiness, however, decreased hunter color values (L, a, and b values). Ripening process for 21 d increased most parameters, such as saltiness, color values, weight loss, shear force and cholesterol content due to the drying process. The mixed starter culture had higher lactic acid bacteria than the commercial one. While eight volatile compounds were identified from fermented hams during curing process, total fiftyeight volatile compounds were identified from fermented hams during ripening process. The main volatile compounds were alcohols, esters and furans. However, no differences in volatile compounds were observed between two batches. Fermented hams (batch B) manufactured with probiotic starter culture (LPP) had higher sensory score in texture, color and overall acceptability than counterparts (batch A), while the opposite trend was observed in flavor. Therefore, mixed probiotic starter culture isolated from kimchi might be used as a starter culture to be able to replace with commercial starter culture (LK-30 plus) for the manufacture of fermented ham. PMID:27499673

  4. Evaluation of Mixed Probiotic Starter Cultures Isolated from Kimchi on Physicochemical and Functional Properties, and Volatile Compounds of Fermented Hams.

    PubMed

    Kim, Young Joo; Park, Sung Yong; Lee, Hong Chul; Yoo, Seung Seok; Oh, Sejong; Kim, Kwang Hyun; Chin, Koo Bok

    2016-01-01

    The objective of this study was to investigate the effects of mixed starter cultures isolated from kimchi on physicochemical properties, functionality and flavors of fermented ham. Physicochemical properties, microbial counts, shear force, cholesterol contents and volatile compounds of fermented ham were investigated during processing (curing and ripening time). Curing process for 7 d increased saltiness, however, decreased hunter color values (L, a, and b values). Ripening process for 21 d increased most parameters, such as saltiness, color values, weight loss, shear force and cholesterol content due to the drying process. The mixed starter culture had higher lactic acid bacteria than the commercial one. While eight volatile compounds were identified from fermented hams during curing process, total fiftyeight volatile compounds were identified from fermented hams during ripening process. The main volatile compounds were alcohols, esters and furans. However, no differences in volatile compounds were observed between two batches. Fermented hams (batch B) manufactured with probiotic starter culture (LPP) had higher sensory score in texture, color and overall acceptability than counterparts (batch A), while the opposite trend was observed in flavor. Therefore, mixed probiotic starter culture isolated from kimchi might be used as a starter culture to be able to replace with commercial starter culture (LK-30 plus) for the manufacture of fermented ham. PMID:27499673

  5. Anti-Trichomonas vaginalis activity of Hypericum polyanthemum extract obtained by supercritical fluid extraction and isolated compounds.

    PubMed

    Cargnin, Simone Tasca; Vieira, Patrícia de Brum; Cibulski, Samuel; Cassel, Eduardo; Vargas, Rubem Mário Figueiró; Montanha, Jarbas; Roehe, Paulo; Tasca, Tiana; von Poser, Gilsane Lino

    2013-04-01

    The anti-Trichomonas vaginalis activity of Hypericum polyanthemum extract obtained by supercritical fluid extraction (50°C, 150bar) and the chemical compounds isolated and purified from this extract (benzopyrans HP1, HP2, HP3, and phloroglucinol derivative uliginosin B) were assessed. All samples had anti-T. vaginalis activity; however, HP1 demonstrated the best selectivity against this protozoan (metronidazole-resistant and susceptible isolates), with no cytotoxicity on mammalian cells (selectivity index of 73.97). Moreover, HP1 had activity against a metronidazole-resistant isolate (52% of viable trophozoites), and this effect was higher when tested with a low concentration of metronidazole (23% of viable trophozoites). Experiments demonstrated that all isolated compounds caused damage to the parasites' membrane (>90% of LDH release) and do not present a notable hemolytic effect, although HP2 and uliginosin B exhibited cytotoxicity against mammalian cells. Therefore, the analyzed molecules are promising prototypes for new antiprotozoal drugs, especially HP1, which seems to improve metronidazole's effect on a resistant T. vaginalis isolate.

  6. A new dammarane saponin and other triterpenoids from Siolmatra brasiliensis and evaluation of the antidiabetic activity of its extract.

    PubMed

    Dos Santos, Carlos Henrique Corrêa; Borges, Izabeau Pontes; da Silva, Virgínia Claudia; de Sousa, Paulo Teixeira; Kawashita, Nair Honda; Baviera, Amanda Martins; Carvalho, Mario Geraldo de

    2016-09-01

    Context Siolmatra brasiliensis (Cogn.) Baill (Cucurbitaceae) is a climbing plant widely used for the treatment of diabetes mellitus symptoms. Objective This work evaluates the antidiabetic activity of an extract of S. brasiliensis in streptozotocin-diabetic rats and promotes the phytochemical investigation to isolate the major compounds of the same extract. Materials and methods Male Wistar rats were divided into normal (N) and diabetic rats (DC) treated with water; diabetic rats treated with 3U insulin (DI) or with 250 (DSb250) or 500 mg/kg (DSb500) of hydroalcoholic extract of the stalks of S. brasiliensis, via oral gavage, for 21 days. Physiological and biochemical parameters classically altered in diabetes were monitored. The triterpenoids were isolated from the ethyl acetate fraction under silica gel column chromatography and Sephadex-LH20 methods and their structures were determined by NMR, HR-ESI-MS and DC analysis. Results When compared with DC, DSb250 rats showed a reduction in the hyperglycemia (DC: 26.46 ± 0.69 versus DSb250: 19.67 ± 1.06 mmol/L) and glycosuria (DC: 43.02 ± 3.19 versus DSb250: 28.46 ± 2.14 mmol/24 h) and increase in hepatic glycogen (DC: 14.44 ± 1.26 versus DSb250: 22.08 ± 4.26 mg/g). Three known cucurbitacins were isolated from a hydroalcoholic extract of S. brasiliensis, i.e., cayaponosides A1, B4, D, and a new dammarane saponin 3-O-β-d-gentiobiosyl-26-O-β-d-glucopyranosyl-20-hydroxydammar-24-ene. The structures of these compounds were elucidated by spectral data analysis of the natural products and their acetyl derivatives. Discussion and conclusion The known cucurbitacins and/or the new identified saponin may be related with the antidiabetic activity of S. brasiliensis. PMID:26810155

  7. Tanjungides A and B: new antitumoral bromoindole derived compounds from Diazona cf formosa. isolation and total synthesis.

    PubMed

    Murcia, Carmen; Coello, Laura; Fernández, Rogelio; Martín, María Jesús; Reyes, Fernando; Francesch, Andrés; Munt, Simon; Cuevas, Carmen

    2014-02-21

    Tanjungides A (1) (Z isomer) and B (2) (E isomer), two novel dibrominated indole enamides, have been isolated from the tunicate Diazona cf formosa. Their structures were determined by spectroscopic methods including HRMS, and extensive 1D and 2D NMR. The stereochemistry of the cyclised cystine present in both compounds was determined by Marfey's analysis after chemical degradation and hydrolysis. We also report the first total synthesis of these compounds using methyl 1H-indole-3-carboxylate as starting material and a linear sequence of 11 chemical steps. Tanjungides A and B exhibit significant cytotoxicity against human tumor cell lines.

  8. Anti microbial and anti-oxidant properties of the isolated compounds from the methanolic extract from the leaves of Tectona grandis

    PubMed Central

    Nayeem, Naira; Karvekar, MD

    2011-01-01

    The compounds Gallic acid (GA), rutin(R), quercitin (Q), ellagic acid (EA) and sitosterol(S) were isolated from the methanolic extract of the leaves of Tectona grandis. These compounds were subjected to antimicrobial and antioxidant activity. The zone of inhibition of isolated compounds was evaluated by cup plate method against bacteria i.e. Staphylococcus aureus, Bacillus subtilis, Eschericia coli, Klebsiella pneumoniae and fungi Candida albicans. The anti oxidant activity of the extract and the isolated compounds were evaluated by using 1, 1-Diphenyl-2-picryl-hydrazyl (DPPH). Rutin has shown significant anti microbial activity against both the gram positive and gram negative bacteria when compared to the other compounds. The results of the anti oxidant activity revealed that quercitin showed good activity followed by rutin gallic acid, ellagic acid and sitosterol. The difference in both these activities of the isolated compounds was attributed to the number and position of the phenolic OH groups PMID:24826018

  9. Natural Phyto-Bioactive Compounds for the Treatment of Type 2 Diabetes: Inflammation as a Target

    PubMed Central

    Gothai, Sivapragasam; Ganesan, Palanivel; Park, Shin-Young; Fakurazi, Sharida; Choi, Dong-Kug; Arulselvan, Palanisamy

    2016-01-01

    Diabetes is a metabolic, endocrine disorder which is characterized by hyperglycemia and glucose intolerance due to insulin resistance. Extensive research has confirmed that inflammation is closely involved in the pathogenesis of diabetes and its complications. Patients with diabetes display typical features of an inflammatory process characterized by the presence of cytokines, immune cell infiltration, impaired function and tissue destruction. Numerous anti-diabetic drugs are often prescribed to diabetic patients, to reduce the risk of diabetes through modulation of inflammation. However, those anti-diabetic drugs are often not successful as a result of side effects; therefore, researchers are searching for efficient natural therapeutic targets with less or no side effects. Natural products’ derived bioactive molecules have been proven to improve insulin resistance and associated complications through suppression of inflammatory signaling pathways. In this review article, we described the extraction, isolation and identification of bioactive compounds and its molecular mechanisms in the prevention of diabetes associated complications. PMID:27527213

  10. Natural Phyto-Bioactive Compounds for the Treatment of Type 2 Diabetes: Inflammation as a Target.

    PubMed

    Gothai, Sivapragasam; Ganesan, Palanivel; Park, Shin-Young; Fakurazi, Sharida; Choi, Dong-Kug; Arulselvan, Palanisamy

    2016-01-01

    Diabetes is a metabolic, endocrine disorder which is characterized by hyperglycemia and glucose intolerance due to insulin resistance. Extensive research has confirmed that inflammation is closely involved in the pathogenesis of diabetes and its complications. Patients with diabetes display typical features of an inflammatory process characterized by the presence of cytokines, immune cell infiltration, impaired function and tissue destruction. Numerous anti-diabetic drugs are often prescribed to diabetic patients, to reduce the risk of diabetes through modulation of inflammation. However, those anti-diabetic drugs are often not successful as a result of side effects; therefore, researchers are searching for efficient natural therapeutic targets with less or no side effects. Natural products' derived bioactive molecules have been proven to improve insulin resistance and associated complications through suppression of inflammatory signaling pathways. In this review article, we described the extraction, isolation and identification of bioactive compounds and its molecular mechanisms in the prevention of diabetes associated complications. PMID:27527213

  11. [Screening and identification of low temperature-adapted antagonistic Bacillus isolated from Kekexili region of West China and the analysis of the isolates lipopeptide compounds].

    PubMed

    Xie, Yong-Li; Gao, Xue-Wen

    2013-01-01

    The research and exploitation of special microbial resources in extreme environment is of scientific significance and has broad applied prospect. In this paper, eight Bacillus strains isolated from the vegetation rhizospheres in Kekexili extreme region of Qinghai Province and presented good growth status at low temperature 4 and 10 degrees C were identified. Through physiological and biochemical analysis, rep-PCR fingerprinting, and 16S rDNA and gyrB partial sequence analyses, the eight strains were identified as Bacillus mojavensis (3 isolates), Bacillus amyloliquefaciens (1 isolate), and Bacillus simplex (4 isolates). The agar plate antagonistic test showed that four of the isolates presented distinct antagonistic activity to Sclerotinia sclerotiorum and Xanthomonas oryzae pv. oryzae. The MALDI-TOF-MS analysis showed that the strain KKD1 (B. mojavensis) produced fengycin and surfactin, whereas the strain KKD2 (B. amyloliquefaciens) produced iturin A, surfactin and fengycin, suggesting that the bio-control efficacy of the Bacillus strains could be related to the synthesis and excretion of the antifungal lipopeptide compounds. This study provided the bacterial resources for the research and exploitation of low temperature-adapted Bacillus bio-fertilizers and bio-pesticides. PMID:23718003

  12. Isolation, structural characterization and in silico drug-like properties prediction of a natural compound from the ethanolic extract of Cayratia trifolia (L.)

    PubMed Central

    Perumal, Palanisamy Chella; Sowmya, Sundaram; Pratibha, Prabhakaran; Vidya, Balasubramanian; Anusooriya, Palanirajan; Starlin, Thangarajan; Ravi, Subban; Gopalakrishnan, Velliyur Kanniappan

    2015-01-01

    Background: Natural products have continually played an important role in drug discovery because it serves as active principles in drugs as well as templates for synthesis of new drugs. Cayratia trifolia (L.) is a medicinal plant, which has been reported to have antiviral, antibacterial, antiprotozoal, hypoglycemic, anticancer and diuretic activities. Objective: Therefore, the objective of this study is to isolate and identify the natural compound from the ethanolic extract of Cayratia trifolia (L.) and to predict the Absorption, Distribution, Metabolism and Excretion (ADME) properties of isolated natural compound. Materials and Methods: Column chromatography and thin layer chromatography were used to isolate the natural compound and Fourier-transform infrared (FTIR) spectroscopy was used to predict the functional groups present in the isolated natural compound. The structural characterization studies were functionally carried out using 1H, 13C, two-dimensional nuclear magnetic resonance (NMR) and mass spectrometry methods. Results: FTIR showed that, the groups of OH, C-H, C = C may be present in the isolated natural compound. 1H, 13C, two-dimensional NMR and mass spectrometry data suggests that the isolated natural compound probably like linoleic acid. In silico ADME properties, prediction of the compound was under acceptable range. Conclusion: Based on the results, it can be concluded that, the isolated natural compound of linoleic acid that has been exhibited good medicinal properties. PMID:25598646

  13. Antidermatophytic and Toxicological Evaluations of Dichloromethane-Methanol Extract, Fractions and Compounds Isolated from Coula edulis

    PubMed Central

    Tamokou, Jean De Dieu; Kuiate, Jules Roger; Gatsing, Donatien; Efouet, Alango Pépin Nken; Njouendou, Abdel Jélil

    2011-01-01

    Background: Coula edulis Bail (Olacaceae), is an evergreen tree growing to a height of 25. This study aimed at evaluating the antidermatophytic and toxicological properties of the stem bark of C. edulis extract as well as fractions and compounds isolated from it. Methods: The plant extract was prepared by maceration in CH2Cl2-MeOH (1:1 v/v). The fractionation of this extract was done by silica gel column chromatography. Antidermatophytic activities were assayed using agar dilution method. The acute and sub-acute toxicities of oral administrations of the extract were studied in rodents. Results: The crude extract of C. edulis displayed antidermatophytic activity against the tested microorganisms with highest activity against Microsporum audouinii and Trichophyton mentagrophytes. The fractionation enhanced the antidermatophytic activity in fraction F3 (MIC=0.62-1.25 mg/ml) compared to the crude extract (MIC=1.25-5 mg/ml). Further fractionation and purification of the fractions F2 and F3 gave respectively 3-O-β-D-glucopyranoside of sitosterol (MIC=0.20-0.40 mg/ml) and a mixture of β-sitosterol, stigmasterol and n-hexadecanoid acid (MIC=0.80 mg/ml). The median lethal doses (LD50) of the crude extract were 16.8 and 19.6 g/kg body weight (BW) in male and female mice, respectively. At 200 mg/kg BW, there was a decrease in body weight gain, food and water consumptions. Gross anatomical analysis revealed white vesicles on the liver of the rats treated with the extract at 200 mg/kg BW. This dose also induced significant (P<0.05) changes on hematological and biochemical parameters in rats after 28 days of treatment. Conclusion: These data suggest that the CH2Cl2-MeOH (1:1 v/v) extract of C. edulis stem bark possesses antidermatophytic properties. They also show that at high doses (≥ 200 mg/kg BW), the extract has significant hepatotoxic and nephrotoxic activities. PMID:23357938

  14. Toxic Compound, Anti-Nutritional Factors and Functional Properties of Protein Isolated from Detoxified Jatropha curcas Seed Cake

    PubMed Central

    Saetae, Donlaporn; Suntornsuk, Worapot

    2011-01-01

    Jatropha curcas is a multipurpose tree, which has potential as an alternative source for biodiesel. All of its parts can also be used for human food, animal feed, fertilizer, fuel and traditional medicine. J. curcas seed cake is a low-value by-product obtained from biodiesel production. The seed cake, however, has a high amount of protein, with the presence of a main toxic compound: phorbol esters as well as anti-nutritional factors: trypsin inhibitors, phytic acid, lectin and saponin. The objective of this work was to detoxify J. curcas seed cake and study the toxin, anti-nutritional factors and also functional properties of the protein isolated from the detoxified seed cake. The yield of protein isolate was approximately 70.9%. The protein isolate was obtained without a detectable level of phorbol esters. The solubility of the protein isolate was maximal at pH 12.0 and minimal at pH 4.0. The water and oil binding capacities of the protein isolate were 1.76 g water/g protein and 1.07 mL oil/g protein, respectively. The foam capacity and stability, including emulsion activity and stability of protein isolate, had higher values in a range of basic pHs, while foam and emulsion stabilities decreased with increasing time. The results suggest that the detoxified J. curcas seed cake has potential to be exploited as a novel source of functional protein for food applications. PMID:21339978

  15. Isolation and Chemical Structural Characterisation of a Compound with Antioxidant Activity from the Roots of Senna italica

    PubMed Central

    Mokgotho, Matlou Phineas; Gololo, Stanley Sechene; Masoko, Peter; Shai, Leshwene Jeremiah; Bagla, Victor Patrick; Eloff, Jacobus Nicolaas

    2013-01-01

    Senna italica, a member of the Fabaceae family (subfamily Caesalpiniaceae), is widely used in South African traditional medicine to treat a number of disease conditions. Aqueous extracts of the plant are mainly used to treat sexually transmitted infections and intestinal complications. The roots of S. italica were ground to a fine powder and sequentially extracted with n-hexane, dichloromethane, acetone, and methanol using serial exhaustive extraction (SEE) method. Thin layer chromatography was used to analyse the phytochemical composition of the extracts and DPPH radical scavenging method to detect the presence of antioxidant compounds. The bioassay guided fractionation of the acetone fraction afforded an antioxidant compound with free radical scavenging activity. The isolated compound was subsequently identified as 3,4′,5-trihydroxystilbene (resveratrol). This study represents the first report of the stilbene resveratrol in S. italica. PMID:23843877

  16. Inhibitory Activities of Phenolic Compounds Isolated from Adina rubella Leaves Against 5α-Reductase Associated with Benign Prostatic Hypertrophy.

    PubMed

    Yin, Jun; Heo, Jun Hyeok; Hwang, Yoon Jeong; Le, Thi Tam; Lee, Min Won

    2016-01-01

    Adina rubella Hance (AR), a plant native to Korea, has been used as traditional medicine for dysentery, eczema, intoxication, and external hemorrhages. Previous phytochemical studies of AR have reported several components, including terpenoids, phenolics, and alkaloids. The current study evaluated the anti-oxidative and anti-inflammatory activities and 5α-reductase inhibition of isolated compounds of AR leaves to find a potential therapeutic agent for benign prostatic hypertrophy (BPH). Repeated chromatographic isolation of an 80% acetone extract of AR leaves yielded seven phenolic compounds: caffeic acid (1), chlorogenic acid (2), methyl chlorogenate (3), quercetin-3-rutinoside (4), kaempferol-3-O-α-l-rhamnopyranosyl-(1→6)-β-d-glucopyranoside (5), hyperoside (6), and grandifloroside (7). Compound 7 is a novel compound in AR. Caffeoyl derivatives 1-3 and 7 showed good anti-oxidative activities. In particular, caffeic acid (1) and grandifloroside (7) showed potent anti-inflammatory activities, and 7 also exhibited potent inhibitory activity against TNF-α and 5α-reductase. Our results show that the extract and grandifloroside (7) from leaves of AR might be developed as a source of potent anti-oxidative and anti-inflammatory agents and therapeutic agent for BPH. PMID:27399661

  17. Optimal dosing regimen of nitric oxide donor compounds for the reduction of Pseudomonas aeruginosa biofilm and isolates from wastewater membranes.

    PubMed

    Barnes, Robert J; Bandi, Ratnaharika R; Wong, Wee Seng; Barraud, Nicolas; McDougald, Diane; Fane, Anthony; Kjelleberg, Staffan; Rice, Scott A

    2013-01-01

    Membrane fouling by bacterial biofilms remains a key challenge for membrane-based water purification systems. Here, the optimal biofilm dispersal potential of three nitric oxide (NO) donor compounds, viz. sodium nitroprusside, 6-(2-hydroxy-1-methyl-2-nitrosohydrazino)-N-methyl-1-hexanamine (MAHMA NONOate) and 1-(hydroxy-NNO-azoxy)-L-proline, disodium salt, was investigated using Pseudomonas aeruginosa PAO1 as a model organism. Dispersal was quantitatively assessed by confocal microscopy [bacterial cells and the components of the extracellular polymeric substances (EPS) (polysaccharides and extracellular DNA)] and colony-forming unit counts. The three NO donor compounds had different optimal exposure times and concentrations, with MAHMA NONOate being the optimal NO donor compound. Biofilm dispersal correlated with a reduction in both bacterial cells and EPS. MAHMA NONOate also reduced single species biofilms formed by bacteria isolated from industrial membrane bioreactor and reverse osmosis membranes, as well as in isolates combined to generate mixed species biofilms. The data present strong evidence for the application of these NO donor compounds for prevention of biofouling in an industrial setting. PMID:23368407

  18. Optimal dosing regimen of nitric oxide donor compounds for the reduction of Pseudomonas aeruginosa biofilm and isolates from wastewater membranes.

    PubMed

    Barnes, Robert J; Bandi, Ratnaharika R; Wong, Wee Seng; Barraud, Nicolas; McDougald, Diane; Fane, Anthony; Kjelleberg, Staffan; Rice, Scott A

    2013-01-01

    Membrane fouling by bacterial biofilms remains a key challenge for membrane-based water purification systems. Here, the optimal biofilm dispersal potential of three nitric oxide (NO) donor compounds, viz. sodium nitroprusside, 6-(2-hydroxy-1-methyl-2-nitrosohydrazino)-N-methyl-1-hexanamine (MAHMA NONOate) and 1-(hydroxy-NNO-azoxy)-L-proline, disodium salt, was investigated using Pseudomonas aeruginosa PAO1 as a model organism. Dispersal was quantitatively assessed by confocal microscopy [bacterial cells and the components of the extracellular polymeric substances (EPS) (polysaccharides and extracellular DNA)] and colony-forming unit counts. The three NO donor compounds had different optimal exposure times and concentrations, with MAHMA NONOate being the optimal NO donor compound. Biofilm dispersal correlated with a reduction in both bacterial cells and EPS. MAHMA NONOate also reduced single species biofilms formed by bacteria isolated from industrial membrane bioreactor and reverse osmosis membranes, as well as in isolates combined to generate mixed species biofilms. The data present strong evidence for the application of these NO donor compounds for prevention of biofouling in an industrial setting.

  19. Finding Needles in a Haystack: Application of Network Analysis and Target Enrichment Studies for the Identification of Potential Anti-Diabetic Phytochemicals

    PubMed Central

    Fayaz, Shaik M.; Suvanish Kumar, Valsala S.; Rajanikant, Krishnamurthy G.

    2014-01-01

    Diabetes mellitus is a debilitating metabolic disorder and remains a significant threat to public health. Herbal medicines have been proven to be effective anti-diabetic agents compared to synthetic drugs in terms of side effects. However, the complexity in their chemical constituents and mechanism of action, hinder the effort to discover novel anti-diabetic drugs. Hence, understanding the biological and chemical basis of pharmacological action of phytochemicals is essential for the discovery of potential anti-diabetic drugs. Identifying important active compounds, their protein targets and the pathways involved in diabetes would serve this purpose. In this context, the present study was aimed at exploring the mechanism of action of anti-diabetic plants phytochemicals through network and chemical-based approaches. This study also involves a focused and constructive strategy for preparing new effective anti-diabetic formulations. Further, a protocol for target enrichment was proposed, to identify novel protein targets for important active compounds. Therefore, the successive use of network analysis combined with target enrichment studies would accelerate the discovery of potential anti-diabetic phytochemicals. PMID:25396726

  20. Methanobactin: a copper binding compound having antibiotic and antioxidant activity isolated from methanotrophic bacteria

    DOEpatents

    DiSpirito, Alan A.; Zahn, James A.; Graham, David W.; Kim, Hyung J.; Alterman, Michail; Larive, Cynthia

    2007-04-03

    A means and method for treating bacterial infection, providing antioxidant activity, and chelating copper using a copper binding compound produced by methanotrophic bacteria is described. The compound, known as methanobactin, is the first of a new class of antibiotics having gram-positive activity. Methanobactin has been sequenced, and its structural formula determined.

  1. Isolation, Purification, and Structural Identification of an Antifungal Compound from a Trichoderma Strain.

    PubMed

    Li, Chong-Wei; Song, Rui-Qing; Yang, Li-Bin; Deng, Xun

    2015-08-01

    Trichoderma strain T-33 has been demonstrated to have inhibitory effect on the fungus species Cytospora chrysosperma. Here, an active antifungal compound was obtained from Trichoderma strain T-33 extract via combined separation technologies, including organic solvent extraction, liquid chromatography, and thin-layer chromatography. The purified compound was further characterized by advanced analytical technologies to elucidate its chemical structure. Results indicated that the active antifungal compound in Trichoderma strain T-33 extract is 2,5- cyclohexadiene-1,4-dione-2,6-bis (1,1-dimethylethyl). PMID:25876599

  2. Isolation, Purification, and Structural Identification of an Antifungal Compound from a Trichoderma Strain.

    PubMed

    Li, Chong-Wei; Song, Rui-Qing; Yang, Li-Bin; Deng, Xun

    2015-08-01

    Trichoderma strain T-33 has been demonstrated to have inhibitory effect on the fungus species Cytospora chrysosperma. Here, an active antifungal compound was obtained from Trichoderma strain T-33 extract via combined separation technologies, including organic solvent extraction, liquid chromatography, and thin-layer chromatography. The purified compound was further characterized by advanced analytical technologies to elucidate its chemical structure. Results indicated that the active antifungal compound in Trichoderma strain T-33 extract is 2,5- cyclohexadiene-1,4-dione-2,6-bis (1,1-dimethylethyl).

  3. Occurrence of UV-Absorbing, Mycosporine-Like Compounds among Cyanobacterial Isolates and an Estimate of Their Screening Capacity

    PubMed Central

    Garcia-Pichel, Ferran; Castenholz, Richard W.

    1993-01-01

    A survey of 20 strains of cyanobacteria (belonging to 13 genera) isolated from habitats exposed to strong insolation revealed that 13 strains contained one or more water-soluble, UV-absorbing, mycosporine amino acid (MAA)-like compounds. Some of the compounds were identical in several strains. In all, 13 distinct compounds were found. The UV absorption spectra of MAAs complemented well that of the extracellular sunscreen pigment scytonemin, which many of the strains also produced. Even though the specific MAA contents were variable among strains, they were invariably higher when the cultures were grown with UV radiation than when it was absent. In five strains tested, the MAA complement accumulated as a solute in the cytoplasmic cell fraction. The sunscreen capacities of MAA and scytonemin and their combined capacity were estimated for each strain and condition on the basis of the specific contents, cell size, and cellular location of the compounds. The estimates suggested that significant, albeit not complete, protection from UV photodamage could be gained from the possession of either MAA or scytonemin but especially from simultaneous screening by both types of compounds. PMID:16348839

  4. In vitro evaluation of anti-diabetic activity and cytotoxicity of chemically analysed Ocimum basilicum extracts.

    PubMed

    Kadan, Sleman; Saad, Bashar; Sasson, Yoel; Zaid, Hilal

    2016-04-01

    The aim of this study was to evaluate the role of glucose transporter-4 (GLUT4) in the anti-diabetic effects of methanol, hexane and dichloromethane extracts of the aerial parts of Ocimum basilicum (OB) and to analyze their phytochemical composition. Phytochemical analysis of the three extracts by GC/MS using the silylation derivatization technique revealed 53 compounds, 17 of them were found for the first time in OB. Cytotoxic and anti-diabetic properties of the extracts were evaluated using L6-GLUT4myc muscle cells stably expressing myc epitope at the exofacial loop (GLUT4). No cytotoxic effects were observed in treated cells up to 0.25 mg/ml extract as measured with MTT and LDH-leakage assays. GLUT4 translocation to the plasma membrane was elevated by 3.5 and 7 folds (-/+ insulin) after treatment with OB extracts for 20 h. Our findings suggest that the observed anti-diabetic properties of OB extracts are possibly mediated in part through one or more of the 17 new identified compound.

  5. In vitro evaluation of anti-diabetic activity and cytotoxicity of chemically analysed Ocimum basilicum extracts.

    PubMed

    Kadan, Sleman; Saad, Bashar; Sasson, Yoel; Zaid, Hilal

    2016-04-01

    The aim of this study was to evaluate the role of glucose transporter-4 (GLUT4) in the anti-diabetic effects of methanol, hexane and dichloromethane extracts of the aerial parts of Ocimum basilicum (OB) and to analyze their phytochemical composition. Phytochemical analysis of the three extracts by GC/MS using the silylation derivatization technique revealed 53 compounds, 17 of them were found for the first time in OB. Cytotoxic and anti-diabetic properties of the extracts were evaluated using L6-GLUT4myc muscle cells stably expressing myc epitope at the exofacial loop (GLUT4). No cytotoxic effects were observed in treated cells up to 0.25 mg/ml extract as measured with MTT and LDH-leakage assays. GLUT4 translocation to the plasma membrane was elevated by 3.5 and 7 folds (-/+ insulin) after treatment with OB extracts for 20 h. Our findings suggest that the observed anti-diabetic properties of OB extracts are possibly mediated in part through one or more of the 17 new identified compound. PMID:26593590

  6. Recent advances in understanding the anti-diabetic actions of dietary flavonoids.

    PubMed

    Babu, Pon Velayutham Anandh; Liu, Dongmin; Gilbert, Elizabeth R

    2013-11-01

    Flavonoids are polyphenolic compounds that are abundant in fruits and vegetables, and increasing evidence demonstrates a positive relationship between consumption of flavonoid-rich foods and disease prevention. Epidemiological, in vitro and animal studies support the beneficial effects of dietary flavonoids on glucose and lipid homeostasis. It is encouraging that the beneficial effects of some flavonoids are at physiological concentrations and comparable to clinically-used anti-diabetic drugs; however, clinical research in this field and studies on the anti-diabetic effects of flavonoid metabolites are limited. Flavonoids act on various molecular targets and regulate different signaling pathways in pancreatic β-cells, hepatocytes, adipocytes and skeletal myofibers. Flavonoids may exert beneficial effects in diabetes by (i) enhancing insulin secretion and reducing apoptosis and promoting proliferation of pancreatic β-cells; (ii) improving hyperglycemia through regulation of glucose metabolism in hepatocytes; (iii) reducing insulin resistance, inflammation and oxidative stress in muscle and fat and (iv) increasing glucose uptake in skeletal muscle and white adipose tissue. This review highlights recent findings on the anti-diabetic effects of dietary flavonoids, including flavan-3-ols, flavanones, flavonols, anthocyanidins, flavones and isoflavones, with particular emphasis on the studies that investigated the cellular and molecular mechanisms involved in the beneficial effects of the compounds.

  7. Recent advances in understanding the anti-diabetic actions of dietary flavonoids

    PubMed Central

    Babu, Pon Velayutham Anandh; Liu, Dongmin; Gilbert, Elizabeth R.

    2013-01-01

    Flavonoids are polyphenolic compounds that are abundant in fruits and vegetables and increasing evidence demonstrates a positive relationship between consumption of flavonoid-rich foods and disease prevention. Epidemiological, in vitro and animal studies support the beneficial effects of dietary flavonoids on glucose and lipid homeostasis. It is encouraging that the beneficial effects of some flavonoids are at physiological concentrations and comparable to clinically-used anti-diabetic drugs; however, clinical research in this field and studies on the anti-diabetic effects of flavonoid metabolites are limited. Flavonoids act on various molecular targets and regulate different signaling pathways in pancreatic β-cells, hepatocytes, adipocytes, and skeletal myofibers. Flavonoids may exert beneficial effects in diabetes by (i) enhancing insulin secretion and reducing apoptosis and promoting proliferation of pancreatic β-cells, (ii) improving hyperglycemia through regulation of glucose metabolism in hepatocytes, (iii) reducing insulin resistance, inflammation and oxidative stress in muscle and fat, and (iv) increasing glucose uptake in skeletal muscle and white adipose tissue. This review highlights recent findings on the anti-diabetic effects of dietary flavonoids, including flavan-3-ols, flavanones, flavonols, anthocyanidins, flavones, and isoflavones, with particular emphasis on the studies that investigated the cellular and molecular mechanisms involved in the beneficial effects of the compounds. PMID:24029069

  8. Mosquitocidal properties of natural product compounds isolated from Chinese herbs and synthetic analogs of curcumin.

    PubMed

    Anstrom, David M; Zhou, Xia; Kalk, Cody N; Song, Baoan; Lan, Que

    2012-03-01

    Because of resistance to current insecticides and to environmental, health, and regulatory concerns, naturally occurring compounds and their derivatives are of increasing interest for the development of new insecticidal compounds against vectors of disease-causing pathogens. Fifty-eight compounds, either extracted and purified from plants native to China or synthetic analogs of curcumin, were evaluated for both their larvicidal activity against Aedes aegypti (L.) and their ability to inhibit binding of cholesterol to Ae. aegypti sterol carrier protein-2 in vitro. Of the compounds tested, curcumin analogs seem especially promising in that of 24 compounds tested five were inhibitors of Ae. aegypti sterol carrier protein-2 with EC50 values ranging from 0.65 to 62.87 microM, and three curcumin analogs exhibited larvicidal activity against fourth instar Ae. aegypti larvae with LC50 values ranging from 17.29 to 27.90 microM. Adding to the attractiveness of synthetic curcumin analogs is the relative ease of synthesizing a large diversity of compounds; only a small fraction of such diversity has been sampled in this study.

  9. Mosquitocidal Properties of Natural Product Compounds Isolated From Chinese Herbs and Synthetic Analogs of Curcumin

    PubMed Central

    ANSTROM, DAVID M.; ZHOU, XIA; KALK, CODY N.; SONG, BAOAN; LAN, QUE

    2012-01-01

    Because of resistance to current insecticides and to environmental, health, and regulatory concerns, naturally occurring compounds and their derivatives are of increasing interest for the development of new insecticidal compounds against vectors of disease-causing pathogens. Fifty-eight compounds, either extracted and purified from plants native to China or synthetic analogs of curcumin, were evaluated for both their larvicidal activity against Aedes aegypti (L.) and their ability to inhibit binding of cholesterol to Ae. aegypti sterol carrier protein-2 in vitro. Of the compounds tested, curcumin analogs seem especially promising in that of 24 compounds tested five were inhibitors of Ae. aegyptisterol carrier protein-2 with EC50 values ranging from 0.65 to 62.87 μM, and three curcumin analogs exhibited larvicidal activity against fourth instar Ae. aegypti larvae with LC50 values ranging from 17.29 to 27.90 μM. Adding to the attractiveness of synthetic curcumin analogs is the relative ease of synthesizing a large diversity of compounds; only a small fraction of such diversity has been sampled in this study. PMID:22493854

  10. Detoxification of corn antimicrobial compounds as the basis for isolating Fusarium verticillioides and some other Fusarium species from corn.

    PubMed

    Glenn, A E; Hinton, D M; Yates, I E; Bacon, C W

    2001-07-01

    The preformed antimicrobial compounds produced by maize, 2,4-dihydroxy-7-methoxy-2H-1,4-benzoxazin-3-one and its desmethoxy derivative 2,4-dihydroxy-2H-1,4-benzoxazin-3-one, are highly reactive benzoxazinoids that quickly degrade to the antimicrobials 6-methoxy-2-benzoxazolinone (MBOA) and 2-benzoxazolinone (BOA), respectively. Fusarium verticillioides (= F. moniliforme) is highly tolerant to MBOA and BOA and can actively transform these compounds to nontoxic metabolites. Eleven of 29 Fusarium species had some level of tolerance to MBOA and BOA; the most tolerant, in decreasing order, were F. verticillioides, F. subglutinans, F. cerealis (= F. crookwellense), and F. graminearum. The difference in tolerance among species was due to their ability to detoxify the antimicrobials. The limited number of species having tolerance suggested the potential utility of these compounds as biologically active agents for inclusion within a semiselective isolation medium. By replacing the pentachloronitrobenzene in Nash-Snyder medium with 1.0 mg of BOA per ml, we developed a medium that resulted in superior frequencies of isolation of F. verticillioides from corn while effectively suppressing competing fungi. Since the BOA medium provided consistent, quantitative results with reduced in vitro and taxonomic efforts, it should prove useful for surveys of F. verticillioides infection in field samples.

  11. Ethanolic extracts and isolated compounds from small-leaf grape (Vitis thunbergii var. taiwaniana) with antihypertensive activities.

    PubMed

    Lin, Yin-Shiou; Lu, Yeh-Lin; Wang, Guei-Jane; Chen, Lih-Geeng; Wen, Chi-Luan; Hou, Wen-Chi

    2012-08-01

    This study aimed to investigate the antihypertensive effects of ethanolic extracts (EE) and compounds isolated from the small-leaf grape (Vitis thunbergii var. taiwaniana, VTT). The highest antiangiotensin-converting enzyme (anti-ACE) was found in stem-EE (IC50 was 69.5 μg/mL). In spontaneously hypertensive rats (SHRs), stem-EE effectively reduced blood pressure 24 h after administration of a single oral dose or when administered daily for 4 weeks. The isolated compounds, including (+)-vitisin A, ampelopsin C, and (+)-ε-viniferin, were shown to have anti-ACE and vasodilating effects against phenylephrine-induced tensions in an endothelium-intact aortic ring, with (+)-vitisin A being the most effective compound. Compared to control rats, SHRs showed significantly reduced systolic and diastolic blood pressures 24 h after a single oral dose of (+)-vitisin A (10 mg/kg) or captopril (2 mg/kg). These results suggest that the development of functional foods with VTT extracts may be beneficial for regulating blood pressure.

  12. Bioassay-Guided Isolation and Antioxidant Evaluation of Flavonoid Compound from Aerial Parts of Lippia nodiflora L.

    PubMed Central

    Sudha, A.; Srinivasan, P.

    2014-01-01

    The present study was designed to identify the DPPH (2, 2-diphenyl-1-picrylhydrazyl) free-radical scavenging constituents from methanol extract of L. nodiflora using bioassay-guided fractionation. The ethyl acetate fraction (EAF) revealed a strong antioxidant activity, compared to other fractions through in vitro DPPH radical-scavenging assay. The repeated fractionation of active EAF by silica gel column chromatography yielded a compound with strong antioxidant potential. The isolated bioactive compound was determined as 2-(3, 4-dimethoxyphenyl)-5-hydroxy-7-methoxy-4H-chromen-4-one (5-hydroxy-3′, 4′, 7-trimethoxyflavone), by comparing spectral data (UV, IR, 1H NMR, 13C NMR, and MS) with literature reports. The isolated compound demonstrated an excellent antioxidant activity through all antioxidant assays and also significantly inhibited lipid peroxidation at a concentration of 50 μg/mL. The results obtained suggested that extracts from L. nodiflora or its derived phytocompound can be used potentially as a bioactive source of natural antioxidants by contributing beneficial health effects. PMID:24967379

  13. A pharmacological perspective on the use of Brazilian Red Propolis and its isolated compounds against human diseases.

    PubMed

    Freires, Irlan Almeida; de Alencar, Severino Matias; Rosalen, Pedro Luiz

    2016-03-01

    Propolis is a complex resinous mixture collected by bees, with high medicinal, historical and economic value. The nutraceutical and pharmacological benefits of propolis have been extensively explored in several fields of medicine as an important resource for prevention and treatment of oral and systemic diseases. A relatively new type of propolis, named red propolis (in Brazil, Brazilian Red Propolis - BRP), has been arousing attention for the promising pharmacological properties of some of its isolated compounds (vestitol, neovestitol, quercetin, medicarpin, formononetin, etc). Due to a distinct chemical composition, BRP and its isolated compounds (mainly isoflavones) affect a wide range of biological targets and could have an impact against numerous diseases as an antimicrobial, anti-inflammatory and immunomodulatory, antioxidant and antiproliferative agent. In this review, we comprehensively address the main aspects related to BRP bioprospection, chemistry and therapeutic potential. Further information is provided on mechanisms of action discovered thus far as well as clinical use in humans and regulatory aspects. As of now, BRP and its isolated molecules remain a fascinating topic for further research and application in biomedical areas and dentistry. PMID:26840367

  14. Isolation, identification, and antibacterial activity of chemical compounds from ethanolic extract of suji leaf (Pleomele angusifolia NE Brown)

    NASA Astrophysics Data System (ADS)

    Faridah; Natalia; Lina, Maria; W, Hendig

    2014-03-01

    Suji (Pleomele angustifolia NE Brown) is one of the medicinal plants of the tribe of Liliaceae, empirically useful to treat coughs and respiratory diseases such as tuberculosis (TB) and pneumonia. In this study, ethanolic extract of suji leaves was tested its activity against bacteria that attacks the respiratory organs, namely Mycobacterium tuberculosis and Streptococcus pneumoniae, using a paper disc diffusion and dilution agar method. These extracts have activity in inhibiting the growth of M. tuberculosis at a concentration of 8 mg and against S. pneumoniae at a concentration of 4 mg. The fractions were tested their antibacterial activity against Streptococcus pneumoniae using paper disc diffusion method. The most active fraction was chosen based on the inhibition diameter. The fractions contained flavonoids, steroids, and essential oils. The precipitate isolated from the extraction process shows needle-shaped, white, cold and tasteless crystals. Moreover, the HPLC analysis of isolate revealed a single peak with a retention time of 7.183 minutes. The exact compounds in the isolate could not be determined but it was known the compounds contained the functional groups of alkene, alkane, C=O, -OH. Test results obtained from UV-Vis spectrophotometer provides maximum absorption at a wavelength of 203.0 nm.

  15. A pharmacological perspective on the use of Brazilian Red Propolis and its isolated compounds against human diseases.

    PubMed

    Freires, Irlan Almeida; de Alencar, Severino Matias; Rosalen, Pedro Luiz

    2016-03-01

    Propolis is a complex resinous mixture collected by bees, with high medicinal, historical and economic value. The nutraceutical and pharmacological benefits of propolis have been extensively explored in several fields of medicine as an important resource for prevention and treatment of oral and systemic diseases. A relatively new type of propolis, named red propolis (in Brazil, Brazilian Red Propolis - BRP), has been arousing attention for the promising pharmacological properties of some of its isolated compounds (vestitol, neovestitol, quercetin, medicarpin, formononetin, etc). Due to a distinct chemical composition, BRP and its isolated compounds (mainly isoflavones) affect a wide range of biological targets and could have an impact against numerous diseases as an antimicrobial, anti-inflammatory and immunomodulatory, antioxidant and antiproliferative agent. In this review, we comprehensively address the main aspects related to BRP bioprospection, chemistry and therapeutic potential. Further information is provided on mechanisms of action discovered thus far as well as clinical use in humans and regulatory aspects. As of now, BRP and its isolated molecules remain a fascinating topic for further research and application in biomedical areas and dentistry.

  16. Garlic as an anti-diabetic agent: recent progress and patent reviews.

    PubMed

    Padiya, Raju; Banerjee, Sanjay K

    2013-08-01

    This article reviews recent literature on the usage and relevance of garlic and its bioactive components in controlling diabetes and diabetes-associated pathologies; and also updates recent patents on the subject. Antidiabetic effect of garlic is well documented even in ancient medical literature. Garlic and its active ingredients have been extensively studied for their antidiabetic efficacies in either experimentally induced or genetic animal models of diabetes. Human studies are also available where hypoglycemic effect of garlic was reported. The beneficial effects of garlic are mainly attributed to the presence of volatile sulfur compounds like alliin, allicin, diallyl disulfide, diallyl trisulfide, diallyl sulfide, S-allyl cysteine, ajoene and allyl mercaptan. Garlic and garlic extracts have been shown to be effective in reducing insulin resistance. Therefore, considering the importance of garlic in controlling diabetic complications, several preparations and food processes containing garlic have been patented. This review discusses some of the recent progresses made in this field and consolidates the results.

  17. Antidiabetic actions of cocoa flavanols.

    PubMed

    Martin, Maria Ángeles; Goya, Luis; Ramos, Sonia

    2016-08-01

    Prevention of diabetes mellitus type 2 (DMT2) through the diet is receiving a growing interest and cocoa because of its polyphenolic compounds, mainly flavanols, has become an important potential chemopreventive natural agent. Cocoa and its main flavanols might contribute to prevent or delay diabetes mellitus type 2 by modulating insulin secretion in β-pancreatic cells and targeting insulin-sensitive tissues because of their insulin-like activity or through the regulation of key proteins of the insulin signaling route. Among other actions, cocoa flavanols have been proved to enhance glucose uptake through the promotion of glucose transport, to repress glucose production, or to improve lipid metabolism. Nevertheless, the molecular mechanisms of action involved in these effects are not fully understood and many points remain to be clarified. This review provides insights into the molecular machinery of the chemopreventive activity of cocoa and its flavanols by compiling cell culture and animal models studies, as well as evidence from human interventional trials. PMID:26824673

  18. Novel Piperine Derivatives with Antidiabetic Effect as PPAR-γ Agonists.

    PubMed

    Kharbanda, Chetna; Alam, Mohammad Sarwar; Hamid, Hinna; Javed, Kalim; Bano, Sameena; Ali, Yakub; Dhulap, Abhijeet; Alam, Perwez; Pasha, M A Qadar

    2016-09-01

    Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ-induced diabetic model. It was observed that nine of twenty novel piperine analogues (5b, 6a-h), showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR-γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead molecules for treatment of diabetes with lesser side-effects. PMID:27037532

  19. Chemical compounds toxic to invertebrates isolated from marine cyanobacteria of potential relevance to the agricultural industry.

    PubMed

    Essack, Magbubah; Alzubaidy, Hanin S; Bajic, Vladimir B; Archer, John A C

    2014-10-29

    In spite of advances in invertebrate pest management, the agricultural industry is suffering from impeded pest control exacerbated by global climate changes that have altered rain patterns to favour opportunistic breeding. Thus, novel naturally derived chemical compounds toxic to both terrestrial and aquatic invertebrates are of interest, as potential pesticides. In this regard, marine cyanobacterium-derived metabolites that are toxic to both terrestrial and aquatic invertebrates continue to be a promising, but neglected, source of potential pesticides. A PubMed query combined with hand-curation of the information from retrieved articles allowed for the identification of 36 cyanobacteria-derived chemical compounds experimentally confirmed as being toxic to invertebrates. These compounds are discussed in this review.

  20. Theobroma cacao: Review of the Extraction, Isolation, and Bioassay of Its Potential Anti-cancer Compounds

    PubMed Central

    Baharum, Zainal; Akim, Abdah Md; Hin, Taufiq Yap Yun; Hamid, Roslida Abdul; Kasran, Rosmin

    2016-01-01

    Plants have been a good source of therapeutic agents for thousands of years; an impressive number of modern drugs used for treating human diseases are derived from natural sources. The Theobroma cacao tree, or cocoa, has recently garnered increasing attention and become the subject of research due to its antioxidant properties, which are related to potential anti-cancer effects. In the past few years, identifying and developing active compounds or extracts from the cocoa bean that might exert anti-cancer effects have become an important area of health- and biomedicine-related research. This review provides an updated overview of T. cacao in terms of its potential anti-cancer compounds and their extraction, in vitro bioassay, purification, and identification. This article also discusses the advantages and disadvantages of the techniques described and reviews the processes for future perspectives of analytical methods from the viewpoint of anti-cancer compound discovery. PMID:27019680

  1. Chemical Compounds Toxic to Invertebrates Isolated from Marine Cyanobacteria of Potential Relevance to the Agricultural Industry

    PubMed Central

    Essack, Magbubah; Alzubaidy, Hanin S.; Bajic, Vladimir B.; Archer, John A. C.

    2014-01-01

    In spite of advances in invertebrate pest management, the agricultural industry is suffering from impeded pest control exacerbated by global climate changes that have altered rain patterns to favour opportunistic breeding. Thus, novel naturally derived chemical compounds toxic to both terrestrial and aquatic invertebrates are of interest, as potential pesticides. In this regard, marine cyanobacterium-derived metabolites that are toxic to both terrestrial and aquatic invertebrates continue to be a promising, but neglected, source of potential pesticides. A PubMed query combined with hand-curation of the information from retrieved articles allowed for the identification of 36 cyanobacteria-derived chemical compounds experimentally confirmed as being toxic to invertebrates. These compounds are discussed in this review. PMID:25356733

  2. Theobroma cacao: Review of the Extraction, Isolation, and Bioassay of Its Potential Anti-cancer Compounds.

    PubMed

    Baharum, Zainal; Akim, Abdah Md; Hin, Taufiq Yap Yun; Hamid, Roslida Abdul; Kasran, Rosmin

    2016-02-01

    Plants have been a good source of therapeutic agents for thousands of years; an impressive number of modern drugs used for treating human diseases are derived from natural sources. The Theobroma cacao tree, or cocoa, has recently garnered increasing attention and become the subject of research due to its antioxidant properties, which are related to potential anti-cancer effects. In the past few years, identifying and developing active compounds or extracts from the cocoa bean that might exert anti-cancer effects have become an important area of health- and biomedicine-related research. This review provides an updated overview of T. cacao in terms of its potential anti-cancer compounds and their extraction, in vitro bioassay, purification, and identification. This article also discusses the advantages and disadvantages of the techniques described and reviews the processes for future perspectives of analytical methods from the viewpoint of anti-cancer compound discovery. PMID:27019680

  3. Occurrence of UV-absorbing, mycosporine-like compounds among cyanobacterial isolates and an estimate of their screening capacity

    SciTech Connect

    Garcia-Pichel, F.; Castenholz, R.W. )

    1993-01-01

    Many cyanobacteria inhabit environments with intense solar radiation. Among the mechanisms to prevent UV photodamage are negative photomovements and the synthesis of UV sunscreen compounds. To assess how common and diverse UV sunscreen substances are among cyanobacteria living under intense solar radiation, the researchers analysed isolates of cyanobacteria for mycosporine amino acids (MAAs)-like, UV-absorbing, water-soluable substances. The cellular locations and the effect of UV radiation on their specific contents were also investigated. MAAs are common but diverse among terrestrial cyanobacteria, most often occuring in species with extracellular scytonemin. The spectral complementation suggests that the combined action of scytonemin and MAA may be responsible for sunscreen effects at shorter UV wavelengths, while the effect at longer wavelenths must be due solely to scytonemin. The authors conclude that these compounds have a significant effect in preventing UV radiation damage. 34 refs., 2 figs., 4 tabs.

  4. Melanin biosynthesis inhibitory activity of a compound isolated from young green barley (Hordeum vulgare L.) in B16 melanoma cells.

    PubMed

    Meng, Tian Xiao; Irino, Nobuto; Kondo, Ryuichiro

    2015-07-01

    In the course to find compounds that inhibit melanin biosynthesis (i.e., whitening agents), we evaluated the effects of the methanol-soluble fraction (i.e., the water-soluble portion of methanol extracts-CHP20P-MeOH eluted fraction) from young green barley leaves on melanin production in B16 melanoma cells. Activity-guided fractionation led to an isolate called tricin (compound 1) as an inhibitory compound of melanin production in B16 melanoma cells. Furthermore, tricin analogs such as tricetin, tricetin trimethyl ether, luteolin, and apigenin were used for analyzing the structure-activity relationships (SAR) of 5,7-dihydroxyflavones studies. Tricin demonstrated stronger inhibitory activity compared to three other compounds. The results suggest that a hydroxyl group at the C-4' position and methoxy groups at the C-3',5' positions of the tricin skeleton may have important roles in this inhibitory activity in B16 melanoma cells. Our results suggest that tricin inhibits melanin biosynthesis with higher efficacy than arbutin, and it could be used as a whitening agent. PMID:25827948

  5. Melanin biosynthesis inhibitory activity of a compound isolated from young green barley (Hordeum vulgare L.) in B16 melanoma cells.

    PubMed

    Meng, Tian Xiao; Irino, Nobuto; Kondo, Ryuichiro

    2015-07-01

    In the course to find compounds that inhibit melanin biosynthesis (i.e., whitening agents), we evaluated the effects of the methanol-soluble fraction (i.e., the water-soluble portion of methanol extracts-CHP20P-MeOH eluted fraction) from young green barley leaves on melanin production in B16 melanoma cells. Activity-guided fractionation led to an isolate called tricin (compound 1) as an inhibitory compound of melanin production in B16 melanoma cells. Furthermore, tricin analogs such as tricetin, tricetin trimethyl ether, luteolin, and apigenin were used for analyzing the structure-activity relationships (SAR) of 5,7-dihydroxyflavones studies. Tricin demonstrated stronger inhibitory activity compared to three other compounds. The results suggest that a hydroxyl group at the C-4' position and methoxy groups at the C-3',5' positions of the tricin skeleton may have important roles in this inhibitory activity in B16 melanoma cells. Our results suggest that tricin inhibits melanin biosynthesis with higher efficacy than arbutin, and it could be used as a whitening agent.

  6. Isolation and characterization of new phenolic compounds with estrogen biosynthesis-inhibiting and antioxidation activities from Broussonetia papyrifera leaves.

    PubMed

    Yang, Chunyan; Li, Fu; Du, Baowen; Chen, Bin; Wang, Fei; Wang, Mingkui

    2014-01-01

    Broussonetia papyrifera leaves (BPL) as a traditional Chinese medicine are also used in livestock feed for stimulating reproduction, adipose tissue and muscle development; however, the mechanism of their action is still unknown. Through estrogen biosynthesis-guided fractionation in human ovarian granulosa-like KGN cells, five new phenolic glycosides, broussoside A-E(1-5), along with fifteen known dietary phenolic compounds, were isolated from the n-butanol extract of BPL, and their structures were elucidated on the basis of NMR spectra analysis and chemical evidence. New compounds 3, 4, 5 and the known compounds 9 and 10 were found to potently inhibit estrogen biosynthesis in KGN cells. In addition, compounds 9, 17, 18, and 20 showed strong antioxidant activity against ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and DPPH (1, 1'-diphenyl -2-picryl-hydrazyl radical) assays. These findings suggest that BPL may improve meat quality through the regulation of estrogen biosynthesis. Furthermore, they may be useful for the discovery of potential aromatase modulators from natural products. Finally, they could be considered as a new source for natural antioxidants.

  7. Isolation and Characterization of New Phenolic Compounds with Estrogen Biosynthesis-Inhibiting and Antioxidation Activities from Broussonetia papyrifera Leaves

    PubMed Central

    Yang, Chunyan; Li, Fu; Du, Baowen; Chen, Bin; Wang, Fei; Wang, Mingkui

    2014-01-01

    Broussonetia papyrifera leaves (BPL) as a traditional Chinese medicine are also used in livestock feed for stimulating reproduction, adipose tissue and muscle development; however, the mechanism of their action is still unknown. Through estrogen biosynthesis-guided fractionation in human ovarian granulosa-like KGN cells, five new phenolic glycosides, broussoside A–E(1–5), along with fifteen known dietary phenolic compounds, were isolated from the n-butanol extract of BPL, and their structures were elucidated on the basis of NMR spectra analysis and chemical evidence. New compounds 3, 4, 5 and the known compounds 9 and 10 were found to potently inhibit estrogen biosynthesis in KGN cells. In addition, compounds 9, 17, 18, and 20 showed strong antioxidant activity against ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and DPPH (1, 1′-diphenyl -2-picryl-hydrazyl radical) assays. These findings suggest that BPL may improve meat quality through the regulation of estrogen biosynthesis. Furthermore, they may be useful for the discovery of potential aromatase modulators from natural products. Finally, they could be considered as a new source for natural antioxidants. PMID:24714659

  8. Bioactivity guided isolation of antifungal compounds from the liverwort Bazzania trilobata (L.) S.F. Gray.

    PubMed

    Scher, Jochen M; Speakman, John-Bryan; Zapp, Josef; Becker, Hans

    2004-09-01

    A dichloromethane and a methanol extract of the liverwort Bazzania trilobata showed antifungal activity against the phytopathogenic fungi Botrytis cinerea, Cladosporium cucumerinum, Phythophthora infestans, Pyricularia oryzae and Septoria tritici. Bioautography on thin-layer chromatograms was used to isolate six antifungal sesquiterpenes: 5- and 7-hydroxycalamenene, drimenol, drimenal, viridiflorol, gymnomitrol and three bisbibenzyls: 6 ',8'-dichloroisoplagiochin C, isoplagiochin D and 6'-chloroisoplagiochin D. Furthermore we report the isolation of gymnomitr-8(12)-en-4-one and the new coumarin 7,8-dihydroxycoumarin-7-O-beta-D-glucuronide. Their structures have been elucidated based on extensive NMR spectral evidence. PMID:15451321

  9. Compounds isolated from Ageratum houstonianum inhibit the activity of matrix metalloproteinases (MMP-2 and MMP-9): An oncoinformatics study

    PubMed Central

    Verma, Anupriya; Rizvi, Syed Mohd. Danish; Shaikh, Sibhghatulla; Ansari, Mohd. Afaque; Shakil, Shazi; Ghazal, Fauzia; Siddiqui, Mohd. Haris; Haneef, Mohd.; Rehman, Ajijur

    2014-01-01

    Background: In osteosarcoma tissue, both MMP-2 and MMP-9 are over expressed compared to their expression in non-affected stromal tissue. Hence, gelatinases are attractive targets for anti-osteosarcoma drugs. Objective: To study the inhibitory activity of compounds isolated from Ageratum houstonianum against MMP-2 and MMP-9 by in-silico approach. Material and Methods: We performed docking study using ‘Autodock 4.2’ between 1,2-benzenedicarboxylic acid-bis (2-ethylhexyl) ester; squalene; 3,5-bis (1,1-dimethylethyl) phenol; pentamethyl tetrahydro-5H-chromene; (1, 4-cyclohexylphenyl) ethanone and 6-vinyl-7-methoxy-2,2-dimethylchromene with MMP-2 and MMP-9. Results: Among all six compounds isolated from Ageratum houstonianum, (1, 4-cyclohexylphenyl) ethanone showed the maximum potential as a putative inhibitor of both MMP-2 and MMP-9 enzymes with reference to ΔG (−7.95 and −8.2 kcal/mol, respectively) and Ki (1.48 and 0.98 μM, respectively) values. Total intermolecular energy of docking for (1, 4-cyclohexylphenyl) ethanone-MMP catalytic domain-interaction was found to be −8.55 kcal/mol for MMP-2 and −9.21 kcal/mol for MMP-9. Conclusion: This study explores molecular interactions between human MMPs (MMP-2 and MMP-9) and six natural compounds. This study predicts that (1,4-cyclohexylphenyl) ethanone is a more efficient inhibitor of human MMP-2 and MMP-9 enzymes compared to the other natural compounds used in this study with reference to Ki and ΔG values. PMID:24695379

  10. Antibacterial and anti-inflammatory effects of Syzygium jambos L. (Alston) and isolated compounds on acne vulgaris

    PubMed Central

    2013-01-01

    Background Acne vulgaris is a chronic skin disorder leading to inflammation as a result of the production of reactive oxygen species due to the active involvement of Propionibacterium acnes (P. acnes) in the infection site of the skin. The current study was designed to assess the potential of the leaf extract of Syzygium jambos L. (Alston) and its compounds for antibacterial and anti-inflammatory activity against the pathogenic P. acnes. Methods The broth dilution method was used to assess the antibacterial activity. The cytotoxicity investigation on mouse melanocyte (B16-F10) and human leukemic monocyte lymphoma (U937) cells was done using sodium 3’-[1-(phenyl amino-carbonyl)-3,4-tetrazolium]-bis-[4-methoxy-6-nitrobenzene sulfonic acid hydrate (XTT) reagent. The non-toxic concentrations of the samples was investigated for the suppression of cytokines interleukin 8 (IL 8) and tumour necrosis factor (TNF α) by testing the supernatants in the co-culture of the human U937 cells and heat killed P. acnes using enzyme immunoassay kits (ELISA). The statistical analysis was done using the Graph Pad Prism 4 program. Results Bioassay guided isolation of ethanol extract of the leaves of S. jambos led to the isolation of three known compounds namely; squalene, an anacardic acid analogue and ursolic acid which are reported for the first time from this plant. The ethanol extract of S. jambos and one of the isolated compound namely, anacardic acid analogue were able to inhibit the growth of P. acnes with a noteworthy minimum inhibitory concentration (MIC) value of 31.3 and 7.9 μg/ml, respectively. The ethanol extract and three commercially acquired compounds namely; myricetin, myricitrin, gallic acid exhibited significant antioxidant activity with fifty percent inhibitory concentration (IC50) ranging between 0.8-1.9 μg/ml which was comparable to that of vitamin C, the reference antioxidant agent. The plant extract, compounds ursolic acid and myricitrin (commercially

  11. Insulin and longevity: antidiabetic biguanides as geroprotectors.

    PubMed

    Anisimov, Vladimir N; Semenchenko, Anna V; Yashin, Anatoli I

    2003-01-01

    The results of previous experimental studies of effects of antidiabetic biguanides (phenformin and buformin) on life span and spontaneous tumor incidence in mice and rats were recalculated and reanalyzed using standard demographic models of mortality. The chronic treatment of female C3H/Sn mice with phenformin prolonged the mean life span by 21.1% (P < 0.05), the mean life span of the last 10% survivors by 28.4% and the maximum life span by 5.5 months (by 26%) in comparison with the control. The demographic aging rate represented by the estimate of respective Gompertz's parameter decreased by 31.2% and MRDT increased 1.45-fold. The treatment significantly inhibited (4.0-fold, P < 0.01) the incidence of mammary adenocarcinomas in mice. Administration of phenformin to female LIO rats failed to influence the mean life span. At the same time, the mean life span of the last 10% survivors increased by 10.1% (P < 0.05), and maximum life span increased by 3 months (+9.8%). Phenformin attenuated the development of spontaneous tumors in comparison to the control. The treatment of female rats with another antidiabetic biguanide, buformin, slightly increased their mean life span (by 7.3%; P > 0.05). The mean life span of the last 10% survivors increased by 12% (P < 0.05) and the maximum life span increased by 2 months (+5.5%) as compared with controls. The population aging rate decreased by 18.1% (P < 0.05) and MRDT increased 1.22-fold under the influence of buformin (P < 0.05). The total tumor incidence decreased by 49.5% in buformin-treated rats. Both antidiabetic biguanides slightly decreased the body weight, slowed down the age-related decline of the reproductive function in female rats. The results of our experiments provide evidence that antidiabetic biguanides are promising geroprotectors as well as drugs which can be used in the prevention of cancer.

  12. Isolation and characterization of an utero-active compound from Agave americana.

    PubMed

    Basilio, C M; Seyler, L; Bernstein, J; Castro de la Mata, R

    1989-12-01

    Crude extracts of Agave americana contain two utero-active compounds. One of these, tentatively named "Fraction B", has been purified to chromatographic homogeneity. Its pharmacological actions are similar to those of acetylcholine. However its chromatographic and electrophoretic mobilities are different. Some chemical properties of fraction B are compatible with the structure of an acyl derivative of choline different from acetylcholine.

  13. SEPARATION AND ISOLATION OF VOLATILE ORGANIC COMPOUNDS USING VACUUM DISTILLATION WITH GC/MS DETERMINATION

    EPA Science Inventory

    Vacuum distillation of water, soil, oil, and fish samples is presented as an alternative technique for determining volatile organic compounds (VOCs). Analyses of samples containing VOCs and non-VOCs at 50ppb concentrations were performed to evaluate method limitations. Analyte re...

  14. Infrared Matrix-Isolation Study of New Noble-Gas Compounds

    NASA Astrophysics Data System (ADS)

    Zhu, Cheng; Räsänen, Markku; Khriachtchev, Leonid

    2016-06-01

    We identify new noble-gas compounds in solid matrices using IR spectroscopy. The compounds under study belong to two types: HNgY and YNgY' where Ng is a noble-gas atom and Y and Y' are electronegative fragments. The experimental assignments are supported by ab initio calculations at the MP2(full) and CCSD(T) levels of theory with the def2-TZVPPD basis set. We have prepared and characterized two new HNgY compounds (noble-gas hydrides): HKrCCCl in a Kr matrix and HXeCCCl in a Xe matrix.I The synthesis of these compounds includes two steps: UV photolysis of HCCCl in a noble-gas matrix to form the H + CCCl fragments and annealing of the matrix to mobilize H atoms and to promote the H + Ng + CCCl = HNgCCCl reaction. An interesting observation in the experiments on HXeCCCl in a Xe matrix is the temperature-induced transformation of the three H-Xe stretching bands. This observation is explained by temperature-induced changes of local matrix morphology around the embedded HXeCCCl molecule. In these experiments, we have also obtained the IR spectrum of the CCCl radical, which is produced by photodecomposition of HCCCl. We have identified three new YNgY' compounds (fluorinated noble-gas cyanides): FKrCN in a Kr matrix and FXeCN and FXeNC in a Xe matrix.II These molecule are formed by photolysis of FCN in a noble-gas matrix due to locality of this process. The amount of these molecules increases upon thermal mobilization of the F atoms in the photolyzed matrix featuring the F + Ng + CN reaction.

  15. Bio-guided isolation of antioxidant compounds from Chrysophyllum perpulchrum, a plant used in the Ivory Coast pharmacopeia.

    PubMed

    Philippe, Bidie Alain; Karine, Ndjoko; Barthélemy, Attioua Koffi; Noél, Zirihi Guédé; David, N'guessan Jean; Joseph, Djaman Allico; Hosttetmann, Kurt

    2010-09-13

    Chrysophyllum perpulchrum (Sapotaceae) is used in the traditional Ivory Coast pharmacopeia to cure fevers. The extract of C. perpulchrum used for this study was the powdered form obtained from the maceration of the dried plant bark in 96% methanol, followed by evaporation to dryness. In the present study, the antioxidative and radical-scavenging activities of the methanolic extract were studied with three standard biological tests: DPPH reduction, ferric thiocyanate (FTC) lipidic peroxidation inhibition and thiobarbituric acid reacting substances (TBARS). Gallic acid and quercetin were used as references. The total amount of phenolic compounds in the extract was determined by ultraviolet (UV) spectrometry and calculated as gallic acid equivalents. Catechin and two dimeric procyanidins were found to be the compounds responsible for the activities. They were chemically dereplicated in the extract by LC-MS. For quantitation purposes, they were isolated by successive chromatographic methods and characterized by mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectrometry. The quantities of these compounds in C. perpulchrum were 5.4% for catechin (P1), and 5.6 and 9.2% for dimers (compounds 2 (P2) and 3 (P3)), respectively. They displayed antioxidant activity with IC(50) values of 2.50 ± 0.15 µg/mL (P1), 2.10 ± 0.2 µg/mL (P2) and 2.10 ± 0.1 µg/mL (P3). The total extract, the active fractions and the pure compounds inhibited the lipid peroxidation by the FTC method and the TBARS method in the range of 60%. These values were comparable to those seen for quercetin.

  16. Isolation and characterization of phytotoxic compounds produced by Streptomyces sp. AMC 23 from red mangrove (Rhizophora mangle).

    PubMed

    Crevelin, Eduardo José; Canova, Sarah Pigato; Melo, Itamar Soares; Zucchi, Tiago Domingues; da Silva, Rafael Eduardo; Moraes, Luiz Alberto Beraldo

    2013-12-01

    Natural products produced by microorganisms have been utilized as sources of new drugs possessing a wide range of agrochemical and pharmacological activities. During our research on Actinomycetes from Brazilian mangroves, the ethyl acetate extract of Streptomyces sp. AMC 23 isolated from the red mangrove (Rhizophora mangle) rhizosphere produced a highly active compound against the microalga Chlorella vulgaris, often used to assess the phytotoxic activity. As a result, the bioassay-guided fractionation led to the isolation of the mixture of the known compounds bafilomycin B1 and bafilomycin B2. The chemical structures of bafilomycin B1 and bafilomycin B2 were established based on their spectroscopic data by infrared (IR), mass spectrometry (MS), (1)H nuclear magnetic resonance (NMR), gradient-enhanced heteronuclear multiple quantum coherence (gHMQC), and gradient-enhanced heteronuclear multiple-bond connectivity (gHMBC) as well as comparison with reference data from the literature. Moreover, it was also possible to identify other bafilomycins using non-chromatographic-dependent techniques (Tandem mass spectrometry). Additionally, this is the first report on the phytotoxic activity of bafilomycin B1.

  17. Isolation and characterization of phytotoxic compounds produced by Streptomyces sp. AMC 23 from red mangrove (Rhizophora mangle).

    PubMed

    Crevelin, Eduardo José; Canova, Sarah Pigato; Melo, Itamar Soares; Zucchi, Tiago Domingues; da Silva, Rafael Eduardo; Moraes, Luiz Alberto Beraldo

    2013-12-01

    Natural products produced by microorganisms have been utilized as sources of new drugs possessing a wide range of agrochemical and pharmacological activities. During our research on Actinomycetes from Brazilian mangroves, the ethyl acetate extract of Streptomyces sp. AMC 23 isolated from the red mangrove (Rhizophora mangle) rhizosphere produced a highly active compound against the microalga Chlorella vulgaris, often used to assess the phytotoxic activity. As a result, the bioassay-guided fractionation led to the isolation of the mixture of the known compounds bafilomycin B1 and bafilomycin B2. The chemical structures of bafilomycin B1 and bafilomycin B2 were established based on their spectroscopic data by infrared (IR), mass spectrometry (MS), (1)H nuclear magnetic resonance (NMR), gradient-enhanced heteronuclear multiple quantum coherence (gHMQC), and gradient-enhanced heteronuclear multiple-bond connectivity (gHMBC) as well as comparison with reference data from the literature. Moreover, it was also possible to identify other bafilomycins using non-chromatographic-dependent techniques (Tandem mass spectrometry). Additionally, this is the first report on the phytotoxic activity of bafilomycin B1. PMID:23979946

  18. Morphological and molecular identification of filamentous Aspergillus flavus and Aspergillus parasiticus isolated from compound feeds in South Africa.

    PubMed

    Iheanacho, Henry E; Njobeh, Patrick B; Dutton, Francis M; Steenkamp, Paul A; Steenkamp, Lucia; Mthombeni, Julian Q; Daru, Barnabas H; Makun, Anthony H

    2014-12-01

    Isolation of filamentous species of two Aspergillum genera from compound feeds produced in South Africa, and subsequent extraction of their individual DNA in this study, presents a simple but rapid molecular procedure for high through-put analysis of the individual morphological forms. DNA was successfully isolated from the Aspergillus spp. from agar cultures by use of a commercial kit. Agarose gel electrophoresis fractionation of the fungi DNA, showed distinct bands. The DNA extracted by this procedure appears to be relatively pure with a ratio absorbance at 260 and 280 nm. However, the overall morphological and molecular data indicated that 67.5 and 51.1% of feed samples were found to be contaminated with Aspergillus flavus and Aspergillus parasiticus, respectively, with poultry feed having the highest contamination mean level of 5.7 × 105 CFU/g when compared to cattle (mean: 4.0 × 106 CFU/g), pig (mean: 2.7 × 104 CFU/g) and horse (1.0 × 102 CFU) feed. This technique presents a readily achievable, easy to use method in the extraction of filamentous fungal DNA and it's identification. Hence serves as an important tool towards molecular study of these organisms for routine analysis check in monitoring and improving compound feed quality against fungal contamination.

  19. Isolation and first total synthesis of PM050489 and PM060184, two new marine anticancer compounds.

    PubMed

    Martín, María Jesús; Coello, Laura; Fernández, Rogelio; Reyes, Fernando; Rodríguez, Alberto; Murcia, Carmen; Garranzo, María; Mateo, Cristina; Sánchez-Sancho, Francisco; Bueno, Santiago; de Eguilior, Carlos; Francesch, Andrés; Munt, Simon; Cuevas, Carmen

    2013-07-10

    Microtubules continue to be one of the most successful anticancer drug targets and a favorite hit for many naturally occurring molecules. While two of the most successful representative agents in clinical use, the taxanes and the vinca alkaloids, come from terrestrial sources, the sea has also proven to be a rich source of new tubulin-binding molecules. We describe herein the first isolation, structural elucidation and total synthesis of two totally new polyketides isolated from the Madagascan sponge Lithoplocamia lithistoides . Both PM050489 and PM060184 show antimitotic properties in human tumor cells lines at subnanomolar concentrations and display a distinct inhibition mechanism on microtubules. The development of an efficient synthetic procedure has solved the supply problem and, following pharmaceutical development, has allowed PM060184 to start clinical studies as a promising new drug for cancer treatment.

  20. Actions of a versatile fluorene-degrading bacterial isolate on polycyclic aromatic compounds.

    PubMed Central

    Grifoll, M; Selifonov, S A; Gatlin, C V; Chapman, P J

    1995-01-01

    Pseudomonas cepacia F297 grew with fluorene as a sole source of carbon and energy; its growth yield corresponded to an assimilation of about 40% of fluorene carbon. The accumulation of a ring meta-cleavage product during growth and the identification of 1-indanone in growth media and washed-cell suspensions suggest that strain F297 metabolizes fluorene by mechanisms analogous to those of naphthalene degradation. In addition to fluorene, strain F297 utilized for growth a wide variety of polycyclic aromatic compounds (PACs), including naphthalene, 2,3-dimethylnaphthalene, phenanthrene, anthracene, and dibenzothiophene. Fluorene-induced cells of the strain also transformed 2,6-dimethylnaphthalene, biphenyl, dibenzofuran, acenaphthene, and acenaphthylene. The identification of products formed from those substrates (by gas chromatography-mass spectrometry) in washed-cell suspensions indicates that P. cepacia F297 carries out the following reactions: (i) aromatic ring oxidation and cleavage, apparently using the pyruvate released for growth, (ii) methyl group oxidations, (iii) methylenic oxidations, and (iv) S oxidations of aromatic sulfur heterocycles. Strain F297 grew with a creosote-PAC mixture, producing an almost complete removal of all aromatic compounds containing 2 to 3 rings in 14 days, as demonstrated by gas chromatography analysis of the remaining PACs recovered from cultures. The identification of key chemicals confirmed that not only are certain compounds depleted but also the anticipated reaction products are found. PMID:7487007

  1. Contrasting ex vivo efficacies of "reversed chloroquine" compounds in chloroquine-resistant Plasmodium falciparum and P. vivax isolates.

    PubMed

    Wirjanata, Grennady; Sebayang, Boni F; Chalfein, Ferryanto; Prayoga; Handayuni, Irene; Noviyanti, Rintis; Kenangalem, Enny; Poespoprodjo, Jeanne Rini; Burgess, Steven J; Peyton, David H; Price, Ric N; Marfurt, Jutta

    2015-09-01

    Chloroquine (CQ) has been the mainstay of malaria treatment for more than 60 years. However, the emergence and spread of CQ resistance now restrict its use to only a few areas where malaria is endemic. The aim of the present study was to investigate whether a novel combination of a CQ-like moiety and an imipramine-like pharmacophore can reverse CQ resistance ex vivo. Between March to October 2011 and January to September 2013, two "reversed chloroquine" (RCQ) compounds (PL69 and PL106) were tested against multidrug-resistant field isolates of Plasmodium falciparum (n = 41) and Plasmodium vivax (n = 45) in Papua, Indonesia, using a modified ex vivo schizont maturation assay. The RCQ compounds showed high efficacy against both CQ-resistant P. falciparum and P. vivax field isolates. For P. falciparum, the median 50% inhibitory concentrations (IC50s) were 23.2 nM for PL69 and 26.6 nM for PL106, compared to 79.4 nM for unmodified CQ (P < 0.001 and P = 0.036, respectively). The corresponding values for P. vivax were 19.0, 60.0, and 60.9 nM (P < 0.001 and P = 0.018, respectively). There was a significant correlation between IC50s of CQ and PL69 (Spearman's rank correlation coefficient [r s] = 0.727, P < 0.001) and PL106 (rs = 0.830, P < 0.001) in P. vivax but not in P. falciparum. Both RCQs were equally active against the ring and trophozoite stages of P. falciparum, but in P. vivax, PL69 and PL106 showed less potent activity against trophozoite stages (median IC50s, 130.2 and 172.5 nM) compared to ring stages (median IC50s, 17.6 and 91.3 nM). RCQ compounds have enhanced ex vivo activity against CQ-resistant clinical isolates of P. falciparum and P. vivax, suggesting the potential use of reversal agents in antimalarial drug development. Interspecies differences in RCQ compound activity may indicate differences in CQ pharmacokinetics between the two Plasmodium species.

  2. Pharmacogenetics of Anti-Diabetes Drugs

    PubMed Central

    DiStefano, Johanna K.; Watanabe, Richard M.

    2010-01-01

    A variety of treatment modalities exist for individuals with type 2 diabetes mellitus (T2D). In addition to dietary and physical activity interventions, T2D is also treated pharmacologically with nine major classes of approved drugs. These medications include insulin and its analogues, sulfonylureas, biguanides, thiazolidinediones (TZDs), meglitinides, α-glucosidase inhibitors, amylin analogues, incretin hormone mimetics, and dipeptidyl peptidase 4 (DPP4) inhibitors. Pharmacological treatment strategies for T2D are typically based on efficacy, yet favorable responses to such therapeutics are oftentimes variable and difficult to predict. Characterization of drug response is expected to substantially enhance our ability to provide patients with the most effective treatment strategy given their individual backgrounds, yet pharmacogenetic study of diabetes medications is still in its infancy. To date, major pharmacogenetic studies have focused on response to sulfonylureas, biguanides, and TZDs. Here, we provide a comprehensive review of pharmacogenetics investigations of these specific anti-diabetes medications. We focus not only on the results of these studies, but also on how experimental design, study sample issues, and definition of ‘response’ can significantly impact our interpretation of findings. Understanding the pharmacogenetics of anti-diabetes medications will provide critical baseline information for the development and implementation of genetic screening into therapeutic decision making, and lay the foundation for “individualized medicine” for patients with T2D. PMID:20936101

  3. [Anti-diabetics and chronic kidney disease].

    PubMed

    Garofalo, Carlo; Iazzetta, Nicolangelo; Camocardi, Andrea; Pacilio, Mario; Iodice, Carmela; Minutolo, Roberto; De Nicola, Luca; Conte, Giuseppe

    2015-01-01

    Diabetes mellitus (DM) is the most important non-communicable disease after hypertension. Prevalence of type 2 DM has progressively increased over the last decades. In Italy, 11.8% of the general adult population can be identified as diabetic. The major complication of DM is diabetic nephropathy (DM-CKD), which develops in approximately one-third of diabetics. Achieving optimal glycemic control is the first therapeutic goal in the management of DM-CKD. In recent years, new antidiabetic drugs have been marketed (GLP1 analogues, DPP-4 inhibitors, SGLT-2 inhibitors) to ameliorate glycemia in patients nave or treated by means of traditional agents, such as sulfonylureas, metformin, glinides, insulin. However, use of these drugs in DM-CKD should be evaluated carefully, mainly because of the higher risk of hypoglycemia that requires dosing adjustments. Metformin still represents an adequate choice if proper dose adjustments are made on the basis of renal function. Sulfonylureas with limited renal clearance, i.e., gliquidone, glipizide and gliclazide are an alternative to metformin and more effective than repaglinide on glycemic control. Other antidiabetic agents with potential nephroprotective effects, namely DPP-4 inhibitors, incretin analogues and SGLT-2 inhibitors, may allow nephroprotective effects independent of glycemic control. Insulin remains the cornerstone of therapy when oral therapy is no longer effective.

  4. Cardiovascular safety of anti-diabetic drugs.

    PubMed

    Kumar, R; Kerins, D M; Walther, T

    2016-01-01

    Cardiovascular disease is the leading cause of morbidity and mortality among patients with diabetes, underscoring the importance of choosing anti-diabetic drugs that do not increase cardiovascular risk but might reduce the risk of cardiovascular events. Most type 2 diabetic patients die from cardiovascular causes despite the beneficial effects of blood pressure (BP) and lipid-lowering medications. The prevalence of patients with cardiovascular disease and diabetes mellitus is growing exponentially. Approximately 40% of patients hospitalized with heart failure and reduced ejection fraction have diabetes mellitus. The recent trials conducted in patients with heart failure who had diabetes showed a different response to standard medication, with these patients being more prone to develop side effects than patients with the same degree of heart failure but without diabetes mellitus. Therefore, careful selection of drug therapy paying particular attention to cardiovascular safety is important in optimizing diabetic therapy. This review discusses the efficacy and safety of the most commonly prescribed anti-diabetic drugs in the context of cardiovascular impact. PMID:27533060

  5. Newer antidiabetic drugs and calorie restriction mimicry

    PubMed Central

    Kalra, Sanjay; Jacob, Jubbin Jagan; Gupta, Yashdeep

    2016-01-01

    De-acceleration of aging and delayed development of age-related morbidity accompanies the restriction of calories (without malnutrition) in laboratory mice, nematodes, yeast, fish, and dogs. Recent results from long-term longitudinal studies conducted on primates have suggested longevity benefits of a 30% restriction of calories in rhesus monkeys as well. Among calorie restricted rhesus monkeys one of the mechanisms for the improvement in lifespan was the reduction in the development of glucose intolerance and cardiovascular disease. Although there are no comparable human studies, it is likely that metabolic and longevity benefits will accompany a reduction in calories in humans as well. However, considering the difficulties in getting healthy adults to limit food intake science has focused on understanding the biochemical processes that accompany calorie restriction (CR) to formulate drugs that would mimic the effects of CR without the need to actually restrict calories. Drugs in this emerging therapeutic field are called CR mimetics. Some of the currently used anti-diabetic agents may have some CR mimetic like effects. This review focuses on the CR mimetic properties of the currently available anti-diabetic agents. PMID:26904485

  6. Biotransformation of Momordica charantia fresh juice by Lactobacillus plantarum BET003 and its putative anti-diabetic potential.

    PubMed

    Mazlan, Farhaneen Afzal; Annuar, M Suffian M; Sharifuddin, Yusrizam

    2015-01-01

    Lactobacillus plantarum BET003 isolated from Momordica charantia fruit was used to ferment its juice. Momordica charantia fresh juice was able to support good growth of the lactic acid bacterium. High growth rate and cell viability were obtained without further nutrient supplementation. In stirred tank reactor batch fermentation, agitation rate showed significant effect on specific growth rate of the bacterium in the fruit juice. After the fermentation, initially abundant momordicoside 23-O-β-Allopyranosyle-cucurbita-5,24-dien-7α,3β,22(R),23(S)-tetraol-3-O-β-allopyranoside was transformed into its corresponding aglycone in addition to the emergence of new metabolites. The fermented M. charantia juice consistently reduced glucose production by 27.2%, 14.5%, 17.1% and 19.2% at 15-minute intervals respectively, when compared against the negative control. This putative anti-diabetic activity can be attributed to the increase in availability and concentration of aglycones as well as other phenolic compounds resulting from degradation of glycosidic momordicoside. Biotransformation of M. charantia fruit juice via lactic acid bacterium fermentation reduced its bitterness, reduced its sugar content, produced aglycones and other metabolites as well as improved its inhibition of α-glucosidase activity compared with the fresh, non-fermented juice.

  7. Biotransformation of Momordica charantia fresh juice by Lactobacillus plantarum BET003 and its putative anti-diabetic potential

    PubMed Central

    Mazlan, Farhaneen Afzal; Annuar, M. Suffian M.

    2015-01-01

    Lactobacillus plantarum BET003 isolated from Momordica charantia fruit was used to ferment its juice. Momordica charantia fresh juice was able to support good growth of the lactic acid bacterium. High growth rate and cell viability were obtained without further nutrient supplementation. In stirred tank reactor batch fermentation, agitation rate showed significant effect on specific growth rate of the bacterium in the fruit juice. After the fermentation, initially abundant momordicoside 23-O-β-Allopyranosyle-cucurbita-5,24-dien-7α,3β,22(R),23(S)-tetraol-3-O-β-allopyranoside was transformed into its corresponding aglycone in addition to the emergence of new metabolites. The fermented M. charantia juice consistently reduced glucose production by 27.2%, 14.5%, 17.1% and 19.2% at 15-minute intervals respectively, when compared against the negative control. This putative anti-diabetic activity can be attributed to the increase in availability and concentration of aglycones as well as other phenolic compounds resulting from degradation of glycosidic momordicoside. Biotransformation of M. charantia fruit juice via lactic acid bacterium fermentation reduced its bitterness, reduced its sugar content, produced aglycones and other metabolites as well as improved its inhibition of α-glucosidase activity compared with the fresh, non-fermented juice. PMID:26539336

  8. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis

    PubMed Central

    Karunaratne, D. Nedra

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means. PMID:27594892

  9. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis

    PubMed Central

    Karunaratne, D. Nedra

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means.

  10. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis.

    PubMed

    Pamunuwa, Geethi; Karunaratne, D Nedra; Waisundara, Viduranga Y

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means. PMID:27594892

  11. A comparative study on the potential of epiphytic yeasts isolated from tropical fruits to produce flavoring compounds.

    PubMed

    Grondin, Eric; Shum Cheong Sing, Alain; Caro, Yanis; Raherimandimby, Marson; Randrianierenana, Ando Lalaniaina; James, Steve; Nueno-Palop, Carmen; François, Jean Marie; Petit, Thomas

    2015-06-16

    In recent years, there has been an increasing interest in identifying and characterizing the yeast flora associated with diverse types of habitat because of the many potential desirable technological properties of these microorganisms, especially in food applications. In this study, a total of 101 yeast strains were isolated from the skins of tropical fruits collected in several locations in the South West Indian Ocean. Sequence analysis of the D1/D2 domains of the large subunit (LSU) ribosomal RNA gene identified 26 different species. Among them, two species isolated from the skins of Cape gooseberry and cocoa beans appeared to represent putative new yeast species, as their LSU D1/D2 sequence was only 97.1% and 97.4% identical to that of the yeasts Rhodotorula mucilaginosa and Candida pararugosa, respectively. A total of 52 Volatile Organic Compounds (VOCs) were detected by Head Space Solid Phase Micro Extraction coupled to Gas Chromatography and Mass Spectroscopy (HS-SPME-GC/MS) from the 26 yeast species cultivated on a glucose rich medium. Among these VOCs, 6 uncommon compounds were identified, namely ethyl but-2-enoate, ethyl 2-methylbut-2-enoate (ethyl tiglate), ethyl 3-methylbut-2-enoate, 2-methylpropyl 2-methylbut-2-enoate, butyl 2-methylbut-2-enoate and 3-methylbutyl 2-methylbut-2-enoate, making them possible yeast species-specific markers. In addition, statistical methods such as Principal Component Analysis allowed to associate each yeast species with a specific flavor profile. Among them, Saprochaete suaveolens (syn: Geotrichum fragrans) turned to be the best producer of flavor compounds, with a total of 32 out of the 52 identified VOCs in its flavor profile.

  12. Protective effects of the compounds isolated from the seed of Psoralea corylifolia on oxidative stress-induced retinal damage

    SciTech Connect

    Kim, Kyung-A; Shim, Sang Hee; Ahn, Hong Ryul; Jung, Sang Hoon

    2013-06-01

    The mechanism underlying glaucoma remains controversial, but apoptosis caused by increased levels of reactive oxygen species (ROS) is thought to play a role in its pathogenesis. We investigated the effects of compounds isolated from Psoralea corylifolia on oxidative stress-induced cell death in vitro and in vivo. Transformed retinal ganglion cells (RGC-5) were treated with L-buthione-(S,R)-sulfoximine (BSO) and glutamate in the presence or with pre-treatment with compound 6, bakuchiol isolated from P. corylifolia. We observed reduced cell death in cells pre-treated with bakuchiol. Moreover, bakuchiol inhibited the oxidative stress-induced decrease of mitochondrial membrane potential (MMP, ΔΨm). Furthermore, while intracellular Ca{sup 2+} was high in RGC-5 cells after exposure to oxidative stress, bakuchiol reduced these levels. In an in vivo study, in which rat retinal damage was induced by intravitreal injection of N-methyl-D-aspartate (NMDA), bakuchiol markedly reduced translocation of AIF and release of cytochrome c, and inhibited up-regulation of cleaved caspase-3, cleaved caspase-9, and cleaved PARP. The survival rate of retinal ganglion cells (RGCs) 7 days after optic nerve crush (ONC) in mice was significantly decreased; however, bakuchiol attenuated the loss of RGCs. Moreover, bakuchiol attenuated ONC-induced up-regulation of apoptotic proteins, including cleaved PARP, cleaved caspase-3, and cleaved caspase-9. Bakuchiol also significantly inhibited translocation of mitochondrial AIF into the nuclear fraction and release of mitochondrial cytochrome c into the cytosol. These results demonstrate that bakuchiol isolated from P. corylifolia has protective effects against oxidative stress-induced retinal damage, and may be considered as an agent for treating or preventing retinal degeneration. - Highlights: • Psoralea corylifolia have neuroprotective effects in vitro and in vivo. • Bakuchiol attenuated the increase of apoptotic proteins induced by oxidative

  13. Identification and Characterization of an Anti-Fibrotic Benzopyran Compound Isolated from Mangrove-Derived Streptomyces xiamenensis

    PubMed Central

    Xu, Min-Juan; Liu, Xiao-Jin; Zhao, Yi-Lei; Liu, Dong; Xu, Zhen-Hao; Lang, Xiao-Meng; Ao, Ping; Lin, Wen-Han; Yang, Song-Lin; Zhang, Zhi-Gang; Xu, Jun

    2012-01-01

    An anti-fibrotic compound produced by Streptomycesn xiamenensis, found in mangrove sediments, was investigated for possible therapeutic effects against fibrosis. The compound, N-[[3,4-dihydro-3S-hydroxy-2S-methyl-2-(4′R-methyl-3′S-pentenyl)-2H-1-benzopyran-6-yl]carbonyl]-threonine (1), was isolated from crude extracts and its structure, including the absolute configuration was determined by extensive spectroscopic data analyses, Mosher’s method, Marfey’s reagent and quantum mechanical calculations. In terms of biological effects, this compound inhibits the proliferation of human lung fibroblasts (WI26), blocks adhesion of human acute monocytic leukemia cells (THP-1) to a monolayer of WI26 cells, and reduces the contractile capacity of WI26 cells in three-dimensional free-floating collagen gels. Altogether, these data indicate that we have identified a bioactive alkaloid (1) with multiple inhibitory biological effects on lung excessive fibrotic characteristics, that are likely involved in fibrosis, suggesting that this molecule might indeed have therapeutic potential against fibrosis. PMID:22611360

  14. Effect-Directed Discovery of Bioactive Compounds Followed by Highly Targeted Characterization, Isolation and Identification, Exemplarily Shown for Solidago virgaurea.

    PubMed

    Móricz, Ágnes M; Ott, Péter G; Häbe, Tim T; Darcsi, András; Böszörményi, Andrea; Alberti, Ágnes; Krüzselyi, Dániel; Csontos, Péter; Béni, Szabolcs; Morlock, Gertrud E

    2016-08-16

    A nontargeted, effect-directed screening (bioprofiling) and a subsequent highly targeted characterization of antibacterial compounds from plant matrices is demonstrated on the example of Solidago virgaurea root extracts. The procedure comprises high-performance thin-layer chromatography (HPTLC) coupled with six bacterial bioassays including two plant pathogens, a radical scavenging assay, an acetylcholinesterase assay as well as in situ and ex situ mass spectrometric analyses. In situ mass spectra were directly recorded from the adsorbent using the Direct Analysis in Real Time interface (HPTLC-DART-MS), whereas ex situ mass spectra were recorded using an elution head-based interface (HPTLC-ESI-MS). For further bioassay-guided isolation of the main antimicrobial compounds, flash chromatographic fractionation and semipreparative high-performance liquid chromatographic purification were used and nuclear magnetic resonance data allowed the identification of the unknown antimicrobial compounds as 2Z,8Z- and 2E,8Z-matricaria esters. The discovered antibacterial activity was confirmed and specified by a luminometric assay and as minimal inhibitory concentration in the liquid phase. PMID:27433973

  15. Cytotoxic and Antifungal Activities of 5-Hydroxyramulosin, a Compound Produced by an Endophytic Fungus Isolated from Cinnamomum mollisimum

    PubMed Central

    Santiago, Carolina; Fitchett, Chris; Munro, Murray H. G.; Jalil, Juriyati; Santhanam, Jacinta

    2012-01-01

    An endophytic fungus isolated from the plant Cinnamomum mollissimum was investigated for the bioactivity of its metabolites. The fungus, similar to a Phoma sp., was cultured in potato dextrose broth for two weeks, followed by extraction with ethyl acetate. The crude extract obtained was fractionated by high-performance liquid chromatography. Both crude extract and fractions were assayed for cytotoxicity against P388 murine leukemic cells and inhibition of bacterial and fungal pathogens. The bioactive extract fraction was purified further and characterized by nuclear magnetic resonance, mass spectral and X-ray crystallography analysis. A polyketide compound, 5-hydroxyramulosin, was identified as the constituent of the bioactive fungal extract fraction. This compound inhibited the fungal pathogen Aspergillus niger (IC50 1.56 μg/mL) and was cytotoxic against murine leukemia cells (IC50 2.10 μg/mL). 5-Hydroxyramulosin was the major compound produced by the endophytic fungus. This research suggests that fungal endophytes are a good source of bioactive metabolites which have potential applications in medicine. PMID:22454674

  16. Alpha-Glucosidase Enzyme Biosensor for the Electrochemical Measurement of Antidiabetic Potential of Medicinal Plants.

    PubMed

    Mohiuddin, M; Arbain, D; Islam, A K M Shafiqul; Ahmad, M S; Ahmad, M N

    2016-12-01

    A biosensor for measuring the antidiabetic potential of medicinal plants was developed by covalent immobilization of α-glucosidase (AG) enzyme onto amine-functionalized multi-walled carbon nanotubes (MWCNTs-NH2). The immobilized enzyme was entrapped in freeze-thawed polyvinyl alcohol (PVA) together with p-nitrophenyl-α-D-glucopyranoside (PNPG) on the screen-printed carbon electrode at low pH to prevent the premature reaction between PNPG and AG enzyme. The enzymatic reaction within the biosensor is inhibited by bioactive compounds in the medicinal plant extracts. The capability of medicinal plants to inhibit the AG enzyme on the electrode correlates to the potential of the medicinal plants to inhibit the production of glucose from the carbohydrate in the human body. Thus, the inhibition indicates the antidiabetic potential of the medicinal plants. The performance of the biosensor was evaluated to measure the antidiabetic potential of three medicinal plants such as Tebengau (Ehretis laevis), Cemumar (Micromelum pubescens), and Kedondong (Spondias dulcis) and acarbose (commercial antidiabetic drug) via cyclic voltammetry, amperometry, and spectrophotometry. The cyclic voltammetry (CV) response for the inhibition of the AG enzyme activity by Tebengau plant extracts showed a linear relation in the range from 0.423-8.29 μA, and the inhibition detection limit was 0.253 μA. The biosensor exhibited good sensitivity (0.422 μA/mg Tebengau plant extracts) and rapid response (22 s). The biosensor retains approximately 82.16 % of its initial activity even after 30 days of storage at 4 °C. PMID:26887579

  17. Alpha-Glucosidase Enzyme Biosensor for the Electrochemical Measurement of Antidiabetic Potential of Medicinal Plants.

    PubMed

    Mohiuddin, M; Arbain, D; Islam, A K M Shafiqul; Ahmad, M S; Ahmad, M N

    2016-12-01

    A biosensor for measuring the antidiabetic potential of medicinal plants was developed by covalent immobilization of α-glucosidase (AG) enzyme onto amine-functionalized multi-walled carbon nanotubes (MWCNTs-NH2). The immobilized enzyme was entrapped in freeze-thawed polyvinyl alcohol (PVA) together with p-nitrophenyl-α-D-glucopyranoside (PNPG) on the screen-printed carbon electrode at low pH to prevent the premature reaction between PNPG and AG enzyme. The enzymatic reaction within the biosensor is inhibited by bioactive compounds in the medicinal plant extracts. The capability of medicinal plants to inhibit the AG enzyme on the electrode correlates to the potential of the medicinal plants to inhibit the production of glucose from the carbohydrate in the human body. Thus, the inhibition indicates the antidiabetic potential of the medicinal plants. The performance of the biosensor was evaluated to measure the antidiabetic potential of three medicinal plants such as Tebengau (Ehretis laevis), Cemumar (Micromelum pubescens), and Kedondong (Spondias dulcis) and acarbose (commercial antidiabetic drug) via cyclic voltammetry, amperometry, and spectrophotometry. The cyclic voltammetry (CV) response for the inhibition of the AG enzyme activity by Tebengau plant extracts showed a linear relation in the range from 0.423-8.29 μA, and the inhibition detection limit was 0.253 μA. The biosensor exhibited good sensitivity (0.422 μA/mg Tebengau plant extracts) and rapid response (22 s). The biosensor retains approximately 82.16 % of its initial activity even after 30 days of storage at 4 °C.

  18. Alpha-Glucosidase Enzyme Biosensor for the Electrochemical Measurement of Antidiabetic Potential of Medicinal Plants

    NASA Astrophysics Data System (ADS)

    Mohiuddin, M.; Arbain, D.; Islam, A. K. M. Shafiqul; Ahmad, M. S.; Ahmad, M. N.

    2016-02-01

    A biosensor for measuring the antidiabetic potential of medicinal plants was developed by covalent immobilization of α-glucosidase (AG) enzyme onto amine-functionalized multi-walled carbon nanotubes (MWCNTs-NH2). The immobilized enzyme was entrapped in freeze-thawed polyvinyl alcohol (PVA) together with p-nitrophenyl-α- d-glucopyranoside (PNPG) on the screen-printed carbon electrode at low pH to prevent the premature reaction between PNPG and AG enzyme. The enzymatic reaction within the biosensor is inhibited by bioactive compounds in the medicinal plant extracts. The capability of medicinal plants to inhibit the AG enzyme on the electrode correlates to the potential of the medicinal plants to inhibit the production of glucose from the carbohydrate in the human body. Thus, the inhibition indicates the antidiabetic potential of the medicinal plants. The performance of the biosensor was evaluated to measure the antidiabetic potential of three medicinal plants such as Tebengau ( Ehretis laevis), Cemumar ( Micromelum pubescens), and Kedondong ( Spondias dulcis) and acarbose (commercial antidiabetic drug) via cyclic voltammetry, amperometry, and spectrophotometry. The cyclic voltammetry (CV) response for the inhibition of the AG enzyme activity by Tebengau plant extracts showed a linear relation in the range from 0.423-8.29 μA, and the inhibition detection limit was 0.253 μA. The biosensor exhibited good sensitivity (0.422 μA/mg Tebengau plant extracts) and rapid response (22 s). The biosensor retains approximately 82.16 % of its initial activity even after 30 days of storage at 4 °C.

  19. Evaluation of medicinal plant extracts and isolated compound epicatechin from Ricinus communis against Paramphistomum cervi.

    PubMed

    Zahir, Abdul Abduz; Rahuman, Abdul Abdul; Bagavan, Asokan; Geetha, Kannappan; Kamaraj, Chinnaperumal; Elango, Gandhi

    2012-10-01

    The purpose of this study is to determine the efficacies of hexane, chloroform, ethyl acetate, acetone, and methanol leaf extracts of Euphorbia hirta L., Psidium guajava L., Ricinus communis L., Solanum trilobatum L., and Tridax procumbens L. against sheep fluke Paramphistomum cervi (Digenea: Paramphistomatidae). All plant extracts showed moderate effects after 24 h of exposure; however, the highest parasite mortality was found in the methanol extract of R. communis. In the present study, bioassay-guided fractionation of methanol extract of R. communis led to the separation and identification of epicatechin as a potential new compound (LC(50) = 31.2; LC(90) = 105.0 ppm) against P. cervi. The structures were established from infrared, ultraviolet, (1)H-nuclear magnetic resonance (NMR), (13)C-NMR, and mass spectral data which confirmed the identification of the compound epicatechin from R. communis. Results of this study showed that the methanol extract of R. communis may be considered as a potent source and epicatechin as a new natural parasitic agent.

  20. In vitro immunocompetence of two compounds isolated from Polygala tenuifolia and development of resistance against grass carp reovirus (GCRV) and Dactylogyrus intermedius in respective host.

    PubMed

    Yu, Xiao-Bo; Liu, Guang-Lu; Zhu, Bin; Hao, Kai; Ling, Fei; Wang, Gao-Xue

    2014-12-01

    The present study was undertaken to isolate some compounds from methanol extract of Polygala tenuifolia and evaluate their immunostimulatory properties and antiviral activity using grass carp Ctenopharyngodon idella kidney (CIK) cells and GCRV. By applying insecticidal bioassay-guided, chromatography techniques and successive recrystallization, two purified compounds were obtained. The changes of expression of selected immune genes (Mx1, IL-1β, TNFα, MyD88 and IgM) in C. idella kidney cell lines were evaluated after exposure to these isolated compounds. The results showed that compound 1 and 2 up-regulated to varying degrees of Mx1, IL-1β, TNFα, and MyD88 in C. idella kidney cells. WST-8 kit assay verified the two compounds has no toxic effects on CIK cell, and furthermore, have in vitro antivirus activity. Especially, that there is keeping 79% cell viability when exposure to compound 2 (100 mg L(-1)). According to in vivo insecticidal assays against Dactylogyrus intermedius, compound 2 exhibited higher efficacy than compound 1, which was found to be 87.2% effective at the concentrations of 5 mg L(-1) and safe to goldfish (Carassius auratus). Besides, the purified compounds were identified by spectral data as: (1) 1,5-Anhydro-D-glucitol and (2) 3,4,5-trimethoxy cinnamic acid. Overall, the results indicate that bath administration of these compounds modulates the immune related genes in C. idella kidney cells and to some extent, eliminate the virus and parasitic infections.

  1. Antidiabetic Activity of Polyherbal Formulation in Streptozotocin – Nicotinamide Induced Diabetic Wistar Rats

    PubMed Central

    Petchi, Rajendran Ramesh; Vijaya, Chockalingam; Parasuraman, Subramani

    2014-01-01

    Glycosmis pentaphylla, Tridax procumbens, and Mangifera indica are well-known plants available throughout India and they are commonly used for the treatment of various diseases including diabetes mellitus. The antidiabetic activity of the individual plant parts is well known, but the synergistic or combined effects are unclear. The concept of polyherbalism has been highlighted in Sharangdhar Samhita, an Ayurvedic literature dating back to 1300 AD. Polyherbal formulations enhance the therapeutic action and reduce the concentrations of single herbs, thereby reducing adverse events. The aim of the present study is to formulate a polyherbal formulation and evaluate its antidiabetic potential in animals. The polyherbal formulation was formulated using the ethanol extracts of the stem bark of G. pentaphylla, whole plant of T. procumbens, and leaves of M. indica. The polyherbal formulation contains the ethanol extracts of G. pentaphylla, T. procumbens, and M. indica in the ratio of 2:2:1. The quality of the finished product was evaluated as per the World Health Organization's guidelines for the quality control of herbal materials. The quality testing parameters of the polyherbal formulation were within the limits. Fingerprint analysis of the polyherbal formulation showed effective separation at 366 nm, and it revealed that the active compound present in the polyherbal formulation and the active compounds present in all the three extracts were the same. The acute toxicity studies of the polyherbal formulation did not show any toxic symptoms in doses up to 2000 mg/kg over 14 days. The oral antidiabetic activity of the polyherbal formulation (250 and 500 mg/kg) was screened against streptozotocin (50 mg/kg; i.p.) + nicotinamide (120 mg/kg; i.p.) induced diabetes mellitus in rats. The investigational drug was administered for 21 consecutive days, and the effect of the polyherbal formulation on blood glucose levels was studied at regular intervals. At the end of the study, the

  2. Antidiabetic activity of polyherbal formulation in streptozotocin - nicotinamide induced diabetic wistar rats.

    PubMed

    Petchi, Rajendran Ramesh; Vijaya, Chockalingam; Parasuraman, Subramani

    2014-04-01

    Glycosmis pentaphylla, Tridax procumbens, and Mangifera indica are well-known plants available throughout India and they are commonly used for the treatment of various diseases including diabetes mellitus. The antidiabetic activity of the individual plant parts is well known, but the synergistic or combined effects are unclear. The concept of polyherbalism has been highlighted in Sharangdhar Samhita, an Ayurvedic literature dating back to 1300 AD. Polyherbal formulations enhance the therapeutic action and reduce the concentrations of single herbs, thereby reducing adverse events. The aim of the present study is to formulate a polyherbal formulation and evaluate its antidiabetic potential in animals. The polyherbal formulation was formulated using the ethanol extracts of the stem bark of G. pentaphylla, whole plant of T. procumbens, and leaves of M. indica. The polyherbal formulation contains the ethanol extracts of G. pentaphylla, T. procumbens, and M. indica in the ratio of 2:2:1. The quality of the finished product was evaluated as per the World Health Organization's guidelines for the quality control of herbal materials. The quality testing parameters of the polyherbal formulation were within the limits. Fingerprint analysis of the polyherbal formulation showed effective separation at 366 nm, and it revealed that the active compound present in the polyherbal formulation and the active compounds present in all the three extracts were the same. The acute toxicity studies of the polyherbal formulation did not show any toxic symptoms in doses up to 2000 mg/kg over 14 days. The oral antidiabetic activity of the polyherbal formulation (250 and 500 mg/kg) was screened against streptozotocin (50 mg/kg; i.p.) + nicotinamide (120 mg/kg; i.p.) induced diabetes mellitus in rats. The investigational drug was administered for 21 consecutive days, and the effect of the polyherbal formulation on blood glucose levels was studied at regular intervals. At the end of the study, the

  3. Isofuranodiene: A neuritogenic compound isolated from wild celery (Smyrnium olusatrum L., Apiaceae).

    PubMed

    Mustafa, Ahmed M; Maggi, Filippo; Papa, Fabrizio; Kaya, Elif; Dikmen, Miris; Öztürk, Yusuf

    2016-02-01

    In the search for neuroactive compounds that mimic the nerve growth factor (NGF) activity for the protection against neurodegenerative diseases, the potential medicinal values of foods and plants attracts intense interest. Isofuranodiene is the major constituent of the essential oil of wild celery (Smyrnium olusatrum L., Apiaceae). The cytotoxic effects of isofuranodiene towards rat neuronal PC-12 pheochromocytoma cells were determined by MTT assay, while the cell differentiation was evaluated with xCELLigence real time cell analysis system (RTCA DP), and the neuritogenic activity was assessed by neurite outgrowth image analysis. Isofuranodiene at concentrations of 25 and 12.5 μM alone, or in combination with 50 nM NGF, showed a marked stimulation of neuritogenesis, but it was more effective at 12.5 μM with or without NGF. The present study reports the first evidence of the neuritogenic effects of isofuranodiene, which appears to be a promising neurotrophic and neuroprotective agent deserving further investigation.

  4. A REVIEW ON SOME ANTIDIABETIC PLANTS OF INDIA

    PubMed Central

    Rai, M.K.

    1995-01-01

    The control over diabetes mellitus depends upon the availability of insulin. Various efforts have been made in the recent past to control / check it. There is an increasing demand to use the natural antidiabetic agents. The literature pertaining to antidiabetic herbs is scattered. The present article is a conglomeration of available indigenous literature. It gives an additional information of list of antidiabetic plants which have not been discussed by Nagarajan et al76 and Handa et al45. It also presents some common plants used in diabetes, and the future of hypoglycaemic herbal drugs. PMID:22556695

  5. Actinobacteria Isolated from an Underground Lake and Moonmilk Speleothem from the Biggest Conglomeratic Karstic Cave in Siberia as Sources of Novel Biologically Active Compounds

    PubMed Central

    Tokovenko, Bogdan T.; Protasov, Eugeniy S.; Gamaiunov, Stanislav V.; Rebets, Yuriy V.; Luzhetskyy, Andriy N.; Timofeyev, Maxim A.

    2016-01-01

    Actinobacteria isolated from unstudied ecosystems are one of the most interesting and promising sources of novel biologically active compounds. Cave ecosystems are unusual and rarely studied. Here, we report the isolation and characterization of ten new actinobacteria strains isolated from an ancient underground lake and moonmilk speleothem from the biggest conglomeratic karstic cave in Siberia with a focus on the biological activity of the obtained strains and the metabolite dereplication of one active strain. Streptomyces genera isolates from moonmilk speleothem demonstrated antibacterial and antifungal activities. Some of the strains were able to inhibit the growth of pathogenic Candida albicans. PMID:26901168

  6. Actinobacteria Isolated from an Underground Lake and Moonmilk Speleothem from the Biggest Conglomeratic Karstic Cave in Siberia as Sources of Novel Biologically Active Compounds.

    PubMed

    Axenov-Gribanov, Denis V; Axenov-Gibanov, Denis V; Voytsekhovskaya, Irina V; Tokovenko, Bogdan T; Protasov, Eugeniy S; Gamaiunov, Stanislav V; Rebets, Yuriy V; Luzhetskyy, Andriy N; Timofeyev, Maxim A

    2016-01-01

    Actinobacteria isolated from unstudied ecosystems are one of the most interesting and promising sources of novel biologically active compounds. Cave ecosystems are unusual and rarely studied. Here, we report the isolation and characterization of ten new actinobacteria strains isolated from an ancient underground lake and moonmilk speleothem from the biggest conglomeratic karstic cave in Siberia with a focus on the biological activity of the obtained strains and the metabolite dereplication of one active strain. Streptomyces genera isolates from moonmilk speleothem demonstrated antibacterial and antifungal activities. Some of the strains were able to inhibit the growth of pathogenic Candida albicans. PMID:26901168

  7. Antidiabetic Indian plants: a good source of potent amylase inhibitors.

    PubMed

    Bhat, Menakshi; Zinjarde, Smita S; Bhargava, Shobha Y; Kumar, Ameeta Ravi; Joshi, Bimba N

    2011-01-01

    Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly α-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having antidiabetic property namely, Azadirachta indica Adr. Juss.; Murraya koenigii (L.) Sprengel; Ocimum tenuflorum (L.) (syn: Sanctum); Syzygium cumini (L.) Skeels (syn: Eugenia jambolana); Linum usitatissimum (L.) and Bougainvillea spectabilis were tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract of O. tenuflorum; B. spectabilis; M. koenigii and S. cumini have significant α-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts of O. tenuflorum and chloroform extract of M. koenigi showed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor. PMID:18955350

  8. Bioassay-guided antidiabetic study of Phaleria macrocarpa fruit extract.

    PubMed

    Ali, Rabyah B; Atangwho, Item J; Kaur, Navneet; Abraika, Omar Saad; Ahmad, Mariam; Mahmud, Roziahanim; Asmawi, Mohd Z

    2012-01-01

    An earlier anti-hyperglycemic study with serial crude extracts of Phaleria macrocarpa (PM) fruit indicated methanol extract (ME) as the most effective. In the present investigation, the methanol extract was further fractionated to obtain chloroform (CF), ethyl acetate (EAF), n-butanol (NBF) and aqueous (AF) fractions, which were tested for antidiabetic activity. The NBF reduced blood glucose (p < 0.05) 15 min after administration, in an intraperitoneal glucose tolerance test (IPGTT) similar to metformin. Moreover, it lowered blood glucose in diabetic rats by 66.67% (p < 0.05), similar to metformin (51.11%), glibenclamide (66.67%) and insulin (71.43%) after a 12-day treatment, hence considered to be the most active fraction. Further fractionation of NBF yielded sub-fractions I (SFI) and II (SFII), and only SFI lowered blood glucose (p < 0.05), in IPGTT similar to glibenclamide. The ME, NBF, and SFI correspondingly lowered plasma insulin (p < 0.05) and dose-dependently inhibited glucose transport across isolated rat jejunum implying an extra-pancreatic mechanism. Phytochemical screening showed the presence of flavonoids, terpenes and tannins, in ME, NBF and SFI, and LC-MS analyses revealed 9.52%, 33.30% and 22.50% mangiferin respectively. PM fruit possesses anti-hyperglycemic effect, exerted probably through extra-pancreatic action. Magniferin, contained therein may be responsible for this reported activity. PMID:22547320

  9. Isolation of Coralmycins A and B, Potent Anti-Gram Negative Compounds from the Myxobacteria Corallococcus coralloides M23.

    PubMed

    Kim, Yu Jin; Kim, Hyun-Ju; Kim, Geon-Woo; Cho, Kyungyun; Takahashi, Shunya; Koshino, Hiroyuki; Kim, Won-Gon

    2016-09-23

    Two new potent anti-Gram negative compounds, coralmycins A (1) and B (2), were isolated from cultures of the myxobacteria Corallococcus coralloides M23, together with another derivative (3) that was identified as the very recently reported cystobactamid 919-2. Their structures including the relative stereochemistry were elucidated by interpretation of spectroscopic, optical rotation, and CD data. The relative stereochemistry of 3 was revised to "S*R*" by NMR analysis. The antibacterial activity of 1 was most potent against Gram-negative pathogens, including Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumanii, and Klebsiella pneumoniae, with MICs of 0.1-4 μg/mL; these MICs were 4-10 and 40-100 times stronger than the antibacterial activities of 3 and 2, respectively. Thus, these data indicated that the β-methoxyasparagine unit and the hydroxy group of the benzoic acid unit were critical for antibacterial activity. PMID:27598688

  10. Recently Confirmed Apoptosis-Inducing Lead Compounds Isolated from Marine Sponge of Potential Relevance in Cancer Treatment

    PubMed Central

    Essack, Magbubah; Bajic, Vladimir B.; Archer, John A.C.

    2011-01-01

    Despite intense efforts to develop non-cytotoxic anticancer treatments, effective agents are still not available. Therefore, novel apoptosis-inducing drug leads that may be developed into effective targeted cancer therapies are of interest to the cancer research community. Targeted cancer therapies affect specific aberrant apoptotic pathways that characterize different cancer types and, for this reason, it is a more desirable type of therapy than chemotherapy or radiotherapy, as it is less harmful to normal cells. In this regard, marine sponge derived metabolites that induce apoptosis continue to be a promising source of new drug leads for cancer treatments. A PubMed query from 01/01/2005 to 31/01/2011 combined with hand-curation of the retrieved articles allowed for the identification of 39 recently confirmed apoptosis-inducing anticancer lead compounds isolated from the marine sponge that are selectively discussed in this review. PMID:22131960

  11. Anti-methicillin Resistant Staphylococcus aureus Compound Isolation from Halophilic Bacillus amyloliquefaciens MHB1 and Determination of Its Mode of Action Using Electron Microscope and Flow Cytometry Analysis.

    PubMed

    Jeyanthi, Venkadapathi; Velusamy, Palaniyandi

    2016-06-01

    The aim of this study was to purify, characterize and evaluate the antibacterial activity of bioactive compound against methicillin-resistant Staphylococcus aureus (MRSA). The anti-MRSA compound was produced by a halophilic bacterial strain designated as MHB1. The MHB1 strain exhibited 99 % similarity to Bacillus amyloliquefaciens based on 16S rRNA gene analysis. The culture conditions of Bacillus amyloliquefaciens MHB1 were optimized using nutritional and environmental parameters for enhanced anti-MRSA compound production. The pure bioactive compound was isolated using silica gel column chromatography and Semi-preparative High-performance liquid chromatography (Semi-preparative HPLC). The Thin layer chromatography, Fourier transform infrared spectroscopy and proton NMR ((1)H NMR) analysis indicated the phenolic nature of the compound. The molecular mass of the purified compound was 507 Da as revealed by Liquid chromatography-mass spectrometry (LC-MS) analysis. The compound inhibited the growth of MRSA with minimum inhibitory concentration (MIC) of 62.5 µg mL(-1). MRSA bacteria exposed to 4× MIC of the compound and the cell viability was determined using flow cytometric analysis. Scanning electron microscope and Transmission electron microscope analysis was used to determine the ultrastructural changes in bacteria. This is the first report on isolation of anti-MRSA compound from halophilic B. amyloliquefaciens MHB1 and could act as a promising biocontrol agent. PMID:27570306

  12. Antibacterial and anti-inflammatory activities of an extract, fractions, and compounds isolated from Gochnatia pulchra aerial parts

    PubMed Central

    Lucarini, R.; Tozatti, M.G.; Silva, M.L.A.; Gimenez, V.M.M.; Pauletti, P.M.; Groppo, M.; Turatti, I.C.C.; Cunha, W.R.; Martins, C.H.G.

    2015-01-01

    This paper reports on the in vitro antibacterial and in vivo anti-inflammatory properties of a hydroethanolic extract of the aerial parts of Gochnatia pulchra (HEGP). It also describes the antibacterial activity of HEGP fractions and of the isolated compounds genkwanin, scutellarin, apigenin, and 3,5-O-dicaffeoylquinic acid, as evaluated by a broth microdilution method. While HEGP and its fractions did not provide promising results, the isolated compounds exhibited pronounced antibacterial activity. The most sensitive microorganism was Streptococcus pyogenes, with minimum inhibitory concentration (MIC) values of 100, 50 and 25 µg/mL for genkwanin and the flavonoids apigenin and scutellarin, respectively. Genkwanin produced an MIC value of 25 µg/mL against Enterococcus faecalis. A paw edema model in rats and a pleurisy inflammation model in mice aided investigation of the anti-inflammatory effects of HEGP. This study also evaluated the ability of HEGP to modulate carrageenan-induced interleukin-1 beta (IL-1β), tumor necrosis factor alpha (TNF-α), and monocyte chemoattractant protein-1 (MCP-1) production. Orally administered HEGP (250 and 500 mg/kg) inhibited carrageenan-induced paw edema. Regarding carrageenan-induced pleurisy, HEGP at 50, 100, and 250 mg/kg diminished leukocyte migration by 71.43%, 69.24%, and 73.34% (P<0.05), respectively. HEGP suppressed IL-1β and MCP-1 production by 55% and 50% at 50 mg/kg (P<0.05) and 60% and 25% at 100 mg/kg (P<0.05), respectively. HEGP abated TNF-α production by macrophages by 6.6%, 33.3%, and 53.3% at 100, 250, and 500 mg/kg (P<0.05), respectively. HEGP probably exerts anti-inflammatory effects by inhibiting production of the pro-inflammatory cytokines TNF-α, IL-1β, and MCP-1. PMID:26200228

  13. Isofuranodiene: A neuritogenic compound isolated from wild celery (Smyrnium olusatrum L., Apiaceae).

    PubMed

    Mustafa, Ahmed M; Maggi, Filippo; Papa, Fabrizio; Kaya, Elif; Dikmen, Miris; Öztürk, Yusuf

    2016-02-01

    In the search for neuroactive compounds that mimic the nerve growth factor (NGF) activity for the protection against neurodegenerative diseases, the potential medicinal values of foods and plants attracts intense interest. Isofuranodiene is the major constituent of the essential oil of wild celery (Smyrnium olusatrum L., Apiaceae). The cytotoxic effects of isofuranodiene towards rat neuronal PC-12 pheochromocytoma cells were determined by MTT assay, while the cell differentiation was evaluated with xCELLigence real time cell analysis system (RTCA DP), and the neuritogenic activity was assessed by neurite outgrowth image analysis. Isofuranodiene at concentrations of 25 and 12.5 μM alone, or in combination with 50 nM NGF, showed a marked stimulation of neuritogenesis, but it was more effective at 12.5 μM with or without NGF. The present study reports the first evidence of the neuritogenic effects of isofuranodiene, which appears to be a promising neurotrophic and neuroprotective agent deserving further investigation. PMID:26304411

  14. Antioxidant activities and determination of phenolic compounds isolated from oriental plums (Soldam, Oishiwase and Formosa)

    PubMed Central

    Kim, Mee-Ree; Cho, Soo-Muk; Kim, So-Young; Kim, Jung-Bong; Cho, Young-Sook

    2012-01-01

    The purposes of this study were to determine phenolic compounds and to evaluate antioxidant activities of plums (Soldam, Oishiwase and Formosa). Soldam contains the highest amount of total phenolics among cultivars (Formosa: 4.0%, Oishiwase: 3.3%, Soldam: 6.4% for total phenolic) as well as the total flavonoids of which constituents were mainly myricetin and anthocyanidin. The antioxidant activities were measured by DPPH, ABTS radical scavenging, and SOD-like activities. The DPPH radical scavenging activity of Korean plum extracts (200 µg/mL) showed more than 43%, and the Soldam turned out to be the highest : ID50 value: 160-177 µg/mL for Formosa and Oishiwase; 58-64 µg/mL for Soldam. The ABTS radical scavenging activity of Korean plum extracts (200 µg/mL) was found to be more than 50%. The SOD-like activity of Korean plum extracts (200 µg/mL) showed more than 70%. Among three kinds of cultivars, Soldam had the highest antioxidant activity. The nitrite scavenging activity of Soldam was 61.5%, which is the highest, compared with that of the other cultivars, about 50%. From these results, Korean plums turned out to be phytochemical rich fruit as well as to show high antioxidant activities. PMID:22977680

  15. 1,2,3,4,6 Penta-O-galloyl-β-d-glucose, a bioactivity guided isolated compound from Mangifera indica inhibits 11β-HSD-1 and ameliorates high fat diet-induced diabetes in C57BL/6 mice.

    PubMed

    Mohan, C G; Viswanatha, G L; Savinay, G; Rajendra, C E; Halemani, Praveen D

    2013-03-15

    Methanolic leaf extract of Mangifera indica (MEMI) was subjected to bioactivity guided fractionation in order to identify the active antidiabetic constituent. 32 fractions were evaluated for possible 11β-HSD-1 inhibition activity under in vitro conditions. The EA-7/8-9/10-4 fraction was evolved as a most potent fraction among all the fractions and it was identified as well known gallotannin compound 1,2,3,4,6 penta-O-galloyl-β-d-glucose (PGG) by spectral analysis. Based on these results the PGG was further evaluated in ex vivo 11β-HSD-1 inhibition assay and high fat diet (HFD)-induced diabetes in male C57BL/6 mice. Single dose (10, 25, 50 and 100mg/kg) of PGG and carbenoxolone (CBX) have dose dependently inhibited the 11β-HSD-1 activity in liver and adipose tissue. Furthermore, HFD appraisal to male C57BL/6 mice caused severe hyperglycemia, hypertriglyceridemia, elevated levels of plasma corticosterone and insulin, increased liver and white adipose mass with increase in body weight was observed compare to normal control. Also, oral glucose tolerance was significantly impaired compare to normal control. Interestingly, post-treatment with PGG for 21 days had alleviated the HFD-induced biochemical alterations and improved oral glucose tolerance compare to HFD-control. In conclusion, the PGG isolated from MEMI inhibits 11β-HSD-1 activity and ameliorates HFD-induced diabetes in male C57BL/6 mice.

  16. Bioassay-Guided Isolation of Neuroprotective Compounds from Uncaria rhynchophylla against Beta-Amyloid-Induced Neurotoxicity

    PubMed Central

    Xian, Yan-Fang; Lin, Zhi-Xiu; Mao, Qing-Qiu; Hu, Zhen; Zhao, Ming; Che, Chun-Tao; Ip, Siu-Po

    2012-01-01

    Uncaria rhynchophylla is a component herb of many Chinese herbal formulae for the treatment of neurodegenerative diseases. Previous study in our laboratory has demonstrated that an ethanol extract of Uncaria rhynchophylla ameliorated cognitive deficits in a mouse model of Alzheimer's disease induced by D-galactose. However, the active ingredients of Uncaria rhynchophylla responsible for the anti-Alzheimer's disease activity have not been identified. This study aims to identify the active ingredients of Uncaria rhynchophylla by a bioassay-guided fractionation approach and explore the acting mechanism of these active ingredients by using a well-established cellular model of Alzheimer's disease, beta-amyloid- (Aβ-) induced neurotoxicity in PC12 cells. The results showed that six alkaloids, namely, corynoxine, corynoxine B, corynoxeine, isorhynchophylline, isocorynoxeine, and rhynchophylline were isolated from the extract of Uncaria rhynchophylla. Among them, rhynchophylline and isorhynchophylline significantly decreased Aβ-induced cell death, intracellular calcium overloading, and tau protein hyperphosphorylation in PC12 cells. These results suggest that rhynchophylline and isorhynchophylline are the major active ingredients responsible for the protective action of Uncaria rhynchophylla against Aβ-induced neuronal toxicity, and their neuroprotective effect may be mediated, at least in part, by inhibiting intracellular calcium overloading and tau protein hyperphosphorylation. PMID:22778778

  17. Isolation and characterization of alkyl peroxy radical scavenging compound from leaves of Laurus nobilis.

    PubMed

    Kang, Hye Won; Yu, Kwang Won; Jun, Woo Jin; Chang, Ih Seop; Han, Sang Bae; Kim, Hee Yun; Cho, Hong Yon

    2002-01-01

    EtOH-soluble fraction from leaves of Laurus nobilis (bay leaves) possessed the highest alkyl peroxy radical (ROO*) scavenging activity among 120 kinds of herbs and edible plants, using the bioassay system which could determine the viability of Staphylococcus aureus 209p by ROO* cytotoxicity. After EtOH-soluble fraction was partitioned with chloroform, ethylacetate, n-butanol and water, the ethylacetate-soluble fraction (L-EA) possessing the highest scavenging activity was further fractionated by Silica gel, Sephadex LH-20 and semi-preparative HPLC analysis on micro-Bondapak C18 reverse phase, and a major flavonol (L-EA-IIa-3-H2) in leaves of L. nobilis was isolated. According to the ultraviolet-visible absorption spectra, L-EA-IIa-3-H2 was thought to be 3,5,7,3'-OH or 3(5),7,3',4'-OH flavonol. After acid hydrolysis of the fraction, L-EA-IIa-3-H2 was found to consist of quercetin and glucose, and was confirmed by one- or two-dimensional (1D or 2D)-NMR to be isoquercitrin. In addition, the ROO* scavenging activity of L-EA-IIa-3-H2 was supported by ESR and its activity was found to be comparable to that of other well-known antioxidants such as epigallocatechin and resveratrol, and higher than that of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT) and ascorbic acid.

  18. Antimicrobial compounds produced by Lactobacillus sakei subsp. sakei 2a, a bacteriocinogenic strain isolated from a Brazilian meat product.

    PubMed

    de Carvalho, Kátia G; Bambirra, Felipe H S; Kruger, Monika F; Barbosa, Matheus S; Oliveira, Jamil S; Santos, Alexandre M C; Nicoli, Jacques R; Bemquerer, Marcelo P; de Miranda, Antonio; Salvucci, Emiliano J; Sesma, Fernando J M; Franco, Bernadette D G M

    2010-04-01

    Bacteriocins produced by lactic acid bacteria are gaining increased importance due to their activity against undesirable microorganisms in foods. In this study, a concentrated acid extract of a culture of Lactobacillus sakei subsp. sakei 2a, a bacteriocinogenic strain isolated from a Brazilian pork product, was purified by cation exchange and reversed-phase chromatographic methods. The amino acid sequences of the active antimicrobial compounds determined by Edman degradation were compared to known protein sequences using the BLAST-P software. Three different antimicrobial compounds were obtained, P1, P2 and P3, and mass spectrometry indicated molecular masses of 4.4, 6.8 and 9.5 kDa, respectively. P1 corresponds to classical sakacin P, P2 is identical to the 30S ribosomal protein S21 of L. sakei subsp. sakei 23 K, and P3 is identical to a histone-like DNA-binding protein HV produced by L. sakei subsp. sakei 23 K. Total genomic DNA was extracted and used as target DNA for PCR amplification of the genes sak, lis and his involved in the synthesis of P1, P2 and P3. The fragments were cloned in pET28b expression vector and the resulting plasmids transformed in E. coli KRX competent cells. The transformants were active against Listeria monocytogenes, indicating that the activity of the classical sakacin P produced by L. sakei 2a can be complemented by other antimicrobial proteins.

  19. Weak hybridization and isolated localized magnetic moments in the compounds CeT2Cd20 (T = Ni, Pd)

    NASA Astrophysics Data System (ADS)

    White, B. D.; Yazici, D.; Ho, P.-C.; Kanchanavatee, N.; Pouse, N.; Fang, Y.; Breindel, A. J.; Friedman, A. J.; Maple, M. B.

    2015-08-01

    We report the physical properties of single crystals of the compounds CeT2Cd20 (T = Ni, Pd) that were grown in a molten Cd flux. Large separations of  ˜6.7-6.8 Å between Ce ions favor the localized magnetic moments that are observed in measurements of the magnetization. The strength of the Ruderman-Kittel-Kasuya-Yosida magnetic exchange interaction between the localized moments is severely limited by the large Ce-Ce separations and by weak hybridization between localized Ce 4 f and itinerant electron states. Measurements of electrical resistivity performed down to 0.138 K were unable to observe evidence for the emergence of magnetic order; however, magnetically-ordered ground states with very low transition temperatures are still expected in these compounds despite the isolated nature of the localized magnetic moments. Such a fragile magnetic order could be highly susceptible to tuning via applied pressure, but evidence for the emergence of magnetic order has not been observed so far in our measurements up to 2.5 GPa.

  20. Weak hybridization and isolated localized magnetic moments in the compounds CeT2Cd20 (T = Ni, Pd)

    DOE PAGES

    White, B. D.; Yazici, D.; Ho, P. -C.; Kanchanavatee, N.; Pouse, N.; Fang, Y.; Breindel, A. J.; Friedman, A. J.; Maple, M. B.

    2015-07-20

    Here, we report the physical properties of single crystals of the compounds CeT2Cd20 (T = Ni, Pd) that were grown in a molten Cd flux. Large separations of ~6.7- 6.8 Å between Ce ions favor the localized magnetic moments that are observed in measurements of the magnetization. The strength of the Ruderman-Kittel-Kasuya- Yosida magnetic exchange interaction between the localized moments is severely limited by the large Ce-Ce separations and by weak hybridization between localized Ce 4f and itinerant electron states. Measurements of electrical resistivity performed down to 0.138 K were unable to observe evidence for the emergence of magnetic order;more » however, magnetically-ordered ground states with very low transition temperatures are still expected in these compounds despite the isolated nature of the localized magnetic moments. Such a fragile magnetic order could be highly susceptible to tuning via applied pressure, but evidence for the emergence of magnetic order has not been observed so far in our measurements up to 2.5 GPa.« less

  1. The isolation and identification of two compounds with predominant radical scavenging activity in hempseed (seed of Cannabis sativa L.).

    PubMed

    Chen, Tianpeng; He, Jinfeng; Zhang, Jianchun; Li, Xiaohui; Zhang, Hua; Hao, Jianxiong; Li, Lite

    2012-09-15

    Forty samples were extracted from defatted kernels and hulls of two varieties of hempseed (Bama and Yunma No. 1) using 10 different polar solvent systems. The radical scavenging capacity of the extracts was evaluated using 2,2-diphenyl-1-pikrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays and the total phenolic content was determined by Folin-Ciocalteu's phenol reagent. The correlation analysis indicated that the antioxidants in hempseed belonged to phenolic and DPPH() assay was suitable for evaluating the radical scavenging activity. Two compounds, with predominant antiradical activity, were isolated in 60% ethanol extract of hempseed hull using macroporous resin absorption, LH-20 gel chromatography, and high performance liquid chromatography methods, which were identified as N-trans-caffeoyltyramine and cannabisin B by high-resolution mass spectra, nuclear magnetic resonance spectra, and ultraviolet data. The two compounds exhibited significant high DPPH() scavenging activity and protective effect against in vitro oxidation of human low-density lipoprotein compared with extracts from flaxseed, grape seed, and soybean. This suggests that hempseed hull extract is a potential source of natural antioxidants, which could be added to dietary supplements to help prevent oxidative stress.

  2. Multivalent dendrimeric compounds containing carbohydrates expressed on immune cells inhibit infection by primary isolates of HIV-1

    SciTech Connect

    Rosa Borges, Andrew; Wieczorek, Lindsay; Johnson, Benitra; Benesi, Alan J.; Brown, Bruce K.; Kensinger, Richard D.; Krebs, Fred C.; Wigdahl, Brian; Blumenthal, Robert; Puri, Anu; McCutchan, Francine E.; Birx, Deborah L.; Polonis, Victoria R.; Schengrund, Cara-Lynne

    2010-12-05

    Specific glycosphingolipids (GSL), found on the surface of target immune cells, are recognized as alternate cell surface receptors by the human immunodeficiency virus type 1 (HIV-1) external envelope glycoprotein. In this study, the globotriose and 3'-sialyllactose carbohydrate head groups found on two GSL were covalently attached to a dendrimer core to produce two types of unique multivalent carbohydrates (MVC). These MVC inhibited HIV-1 infection of T cell lines and primary peripheral blood mononuclear cells (PBMC) by T cell line-adapted viruses or primary isolates, with IC{sub 50}s ranging from 0.1 to 7.4 {mu}g/ml. Inhibition of Env-mediated membrane fusion by MVC was also observed using a dye-transfer assay. These carbohydrate compounds warrant further investigation as a potential new class of HIV-1 entry inhibitors. The data presented also shed light on the role of carbohydrate moieties in HIV-1 virus-host cell interactions. -- Research Highlights: {yields}Multivalent carbohydrates (MVCs) inhibited infection of PBMCs by HIV-1. {yields}MVCs inhibited infection by T cell line-adapted viruses. {yields}MVCs inhibited infection by primary isolates of HIV-1. {yields}MVCs inhibited Env-mediated membrane fusion.

  3. Bioassay-guided isolation and identification of anti-platelet-active compounds from the root of Ashitaba (Angelica keiskei Koidz.).

    PubMed

    Son, Dong Ju; Park, Ye Oak; Yu, Chengguang; Lee, Sung Eun; Park, Young Hyun

    2014-01-01

    Platelet aggregation is fundamental to a wide range of physiological and pathological processes, including the induction of thrombosis and arteriosclerosis. Anti-platelet activity of a crude methanol extract and solvent fractions of Ashitaba roots (Angelica keiskei Koidz.) was evaluated using a turbidimetric method using washed rabbit platelets. We identified the anti-platelet activities of two chalcones, 4-hydroxyderricin and xanthoangelol, isolated from the ethyl acetate-soluble fraction of Ashitaba roots by using a bioassay-guided isolation method. 4-Hydroxyderricin and xanthoangelol effectively inhibited platelet aggregation induced by collagen (IC50 of 41.9 and 35.9 μM, respectively), platelet-activating factor (IC50 of 46.1 and 42.3 μM, respectively) and phorbol 12-myristate 13-acetate (IC50 of 16.5 and 45.9 μM, respectively). These compounds did not inhibit thrombin-induced platelet aggregation (IC50 of>80 μM). The results suggest that the chalcones 4-hydroxyderricin and xanthoangelol may be potent anti-thrombotic components of A. keiskei Koidz.

  4. Characterization of Ocular Iontophoretic Drug Transport of Ionic and Non-ionic Compounds in Isolated Rabbit Cornea and Conjunctiva.

    PubMed

    Sekijima, Hidehisa; Ehara, Junya; Hanabata, Yusuke; Suzuki, Takumi; Kimura, Soichiro; Lee, Vincent H L; Morimoto, Yasunori; Ueda, Hideo

    2016-06-01

    Ocular iontophoresis (IP) in isolated rabbit cornea and conjunctiva was examined in terms of transport enhancement, tissue viability and integrity using electrophysiological parameters by the Ussing-type chamber technique. Lidocaine hydrochloride (LC, a cationic compound), sodium benzoate (BA, anionic compound), and fluorescein isothiocyanate labeled dextran (molecular weight 4400 Da, FD-4, hydrophilic large compound) were used as model permeants. Direct electric current was applied at 0.5-5.0 mA/cm(2) for the cornea and 0.5-20 mA/cm(2) for the conjunctiva for 30 min. LC and BA fluxes across the cornea and conjunctiva were significantly increased by the application of electric current up to 2.3- and 2.5-fold and 4.0- and 3.4-fold, respectively, and returned to their baseline level on stopping the current. Furthermore, a much higher increase by IP application was obtained for the FD-4 transport. The increased FD-4 flux in the conjunctiva returned to baseline on stopping the current, whereas the flux in the cornea was sustained at a higher level after stopping the current. The transepithelial electric resistance of the cornea and conjunctiva was lowered by electric current application but fully recovered after stopping the current up to 2.0 mA/cm(2) for the cornea and 10 mA/cm(2) for the conjunctiva, suggesting that the corneal and conjunctival viability and integrity are maintained even after application of these current densities. These results indicate that ocular IP may be a useful non-invasive technique to achieve drug delivery of hydrophilic large molecules into the eyes. PMID:27040754

  5. The antidiabetic compound 2-dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione, isolated from averrhoa carambola L., demonstrates significant antitumor potential against human breast cancer cells

    PubMed Central

    Gao, Ying; Huang, Renbin; Gong, Yixuan; Park, Hyo Sim; Wen, Qingwei; Almosnid, Nadin Marwan; Chippada-Venkata, Uma D.; Hosain, Najlaa Abdulrhman; Vick, Eric; Farone, Anthony; Altman, Elliot

    2015-01-01

    2-Dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione (DMDD) is a cyclohexanedione found in the roots of Averrhoa carambola L., commonly known as starfruit. Researchers have shown that DMDD has significant therapeutic potential for the treatment of diabetes; however, the effects of DMDD on human cancers have never been reported. We investigated the cytotoxic effects of DMDD against human breast, lung and bone cancer cells in vitro and further examined the molecular mechanisms of DMDD-induced apoptosis in human breast cancer cells. DMDD suppressed the growth of breast carcinoma cells, but not normal mammary epithelial cells, via induction of G1 phase cell cycle arrest, oxidative stress and apoptosis. DMDD increased the level of intracellular reactive oxygen species (ROS) and DMDD-induced ROS generation was found to be associated with the mitochondrial activity. The cytotoxicity that was induced by DMDD was attenuated by co-treatment with the antioxidant N-acetyl-L-cysteine (NAC). DMDD-induced cell apoptosis involved the activation of both the intrinsic mitochondrial pathway and the extrinsic receptor pathway. In addition, DMDD inhibited the canonical NF-κB signaling pathway at all steps, including TNF-α production, phosphorylation of NF-κB p65 and IκBα, as well as TNF-α activated NF-κB p65 nuclear translocation. Collectively, our studies indicate that DMDD has significant potential as a safe and efficient therapeutic agent for the treatment of breast cancer. PMID:26203774

  6. The antidiabetic compound 2-dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione, isolated from Averrhoa carambola L., demonstrates significant antitumor potential against human breast cancer cells.

    PubMed

    Gao, Ying; Huang, Renbin; Gong, Yixuan; Park, Hyo Sim; Wen, Qingwei; Almosnid, Nadin Marwan; Chippada-Venkata, Uma D; Hosain, Najlaa Abdulrhman; Vick, Eric; Farone, Anthony; Altman, Elliot

    2015-09-15

    2-Dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione (DMDD) is a cyclohexanedione found in the roots of Averrhoa carambola L., commonly known as starfruit. Researchers have shown that DMDD has significant therapeutic potential for the treatment of diabetes; however, the effects of DMDD on human cancers have never been reported. We investigated the cytotoxic effects of DMDD against human breast, lung and bone cancer cells in vitro and further examined the molecular mechanisms of DMDD-induced apoptosis in human breast cancer cells. DMDD suppressed the growth of breast carcinoma cells, but not normal mammary epithelial cells, via induction of G1 phase cell cycle arrest, oxidative stress and apoptosis. DMDD increased the level of intracellular reactive oxygen species (ROS) and DMDD-induced ROS generation was found to be associated with the mitochondrial activity. The cytotoxicity that was induced by DMDD was attenuated by co-treatment with the antioxidant N-acetyl-L-cysteine (NAC). DMDD-induced cell apoptosis involved the activation of both the intrinsic mitochondrial pathway and the extrinsic receptor pathway. In addition, DMDD inhibited the canonical NF-κB signaling pathway at all steps, including TNF-α production, phosphorylation of NF-κB p65 and IκBα, as well as TNF-α activated NF-κB p65 nuclear translocation.Collectively, our studies indicate that DMDD has significant potential as a safe and efficient therapeutic agent for the treatment of breast cancer.

  7. Antidiabetic activity of 3-hydroxyflavone analogues in high fructose fed insulin resistant rats

    PubMed Central

    Nayak, Yogendra; Venkatachalam, H.; Daroji, Vijay Kumar; Mathew, Geetha; Jayashree, B.S.; Unnikrishnan, M.K.

    2014-01-01

    Synthetic 3-hydroxyflavone analogues (JY-1, JY-2, JY-3, JY-4), were tested for antidiabetic activity in high-fructose-diet-fed (66 %, for 6 weeks) insulin-resistant Wistar rats (FD-fed rats). The fasting blood glucose, insulin, creatinine and AGEs were decreased to near normal upon treatment with test compounds. Insulin resistance markers such as HOMA-IR, K-ITT, plasma triglycerides, lipids, endogenous antioxidant defense and glycogen were restored in FD-fed rats after treatment with 3-hydroxyflavones. It is known that insulin resistance is partly because of oxidative stress and hence antioxidant activity was determined. They exhibited significant in vitro DPPH and ABTS radical scavenging activity (IC50: 10.66-66.63 µM). Test compounds inhibited ROS and NO production in RAW 264.7 cells (IC50: 10.39–42.63 µM) and they were found as potent as quercetin. Further, the test compounds inhibited lipid peroxidation at low concentrations (IC50: 99.61-217.47 µM). All test compounds at concentrations 100-200 µM protected calf thymus DNA-damage by Fenton reaction. In addition, test compounds inhibited protein glycation in different in vitro antiglycation assays. JY-2 showed maximum potency in all the stages of glycation which was comparable to the standard quercetin and aminoguanidine. Test compounds also enhanced the glucose uptake by L6 myotubes at an EC50 much lower than that of quercetin. Thus the synthetic 3-hydroxyflavones were found to have good antidiabetic activity by pleotropic and multimodal suppression of insulin resistance and enhancement of glucose uptake by skeletal muscles. These compounds are non-toxic at the doses tested. Further, the combined antioxidant and antiglycation activities of these molecules have complementary benefits in management of diabetes. PMID:26417321

  8. [The vanadium compounds: chemistry, synthesis, insulinomimetic properties].

    PubMed

    Fedorova, E V; Buriakina, A V; Vorob'eva, N M; Baranova, N I

    2014-01-01

    The review considers the biological role of vanadium, its participation in various processes in humans and other mammals, and the anti-diabetic effect of its compounds. Vanadium salts have persistent hypoglycemic and antihyperlipidemic effects and reduce the probability of secondary complications in animals with experimental diabetes. The review contains a detailed description of all major synthesized vanadium complexes having antidiabetic activity. Currently, vanadium complexes with organic ligands are more effective and safer than the inorganic salts. Despite the proven efficacy of these compounds as the anti-diabetic agents in animal models, only one organic complex of vanadium is currently under the second phase of clinical trials. All of the considered data suggest that vanadium compound are a new promising class of drugs in modern pharmacotherapy of diabetes.

  9. Bromophenols from marine algae with potential anti-diabetic activities

    NASA Astrophysics Data System (ADS)

    Lin, Xiukun; Liu, Ming

    2012-12-01

    Marine algae contain various bromophenols with a variety of biological activities, including antimicrobial, anticancer, and anti-diabetic effects. Here, we briefly review the recent progress in researches on the biomaterials from marine algae, emphasizing the relationship between the structure and the potential anti-diabetic applications. Bromophenols from marine algae display their hyperglycemic effects by inhibiting the activities of protein tyrosine phosphatase 1B, α-glucosidase, as well as other mechanisms.

  10. A New Method for the Isolation of Ergosterol and Peroxyergosterol as Active Compounds of Hygrophoropsis aurantiaca and in Vitro Antiproliferative Activity of Isolated Ergosterol Peroxide.

    PubMed

    Nowak, Renata; Drozd, Marta; Mendyk, Ewaryst; Lemieszek, Marta; Krakowiak, Olga; Kisiel, Wanda; Rzeski, Wojciech; Szewczyk, Katarzyna

    2016-01-01

    In the present study, ergosterol peroxide and ergosterol were isolated for the first time from fresh fruit bodies of Hygrophoropsis aurantiaca (False Chanterelle). The substances were characterized mainly by spectroscopic methods (¹H-NMR, (13)C-NMR, DEPT-45, DEPT-90, DEPT-135, 2D-NMR). In our study, a new specific thin layer chromatographic method was developed for determination of ergosterol and ergosterol peroxide in H. aurantiaca extract. The method is based on the separation of n-hexane extract on silica gel (Silica Gel G) TLC plates using the optimized solvent system toluene/ethyl acetate (3:1; v/v). The main advantages of the developed method are the simplicity of operation and the low cost. The in vitro study results revealed the antiproliferative properties of ergosterol peroxide against LS180 human colon cancer cells. The described effect was attributed both to altered mitochondrial activity and decreased DNA synthesis. Additionally, in the same concentration range the investigated compound was not toxic to CCD 841 CoTr human colon epithelial cells. The present study suggests that fruit bodies of H. aurantiaca have great potential for producing substances and extracts with potential applications in medicine. PMID:27455215

  11. The effects of purine compounds on the isolated aorta of the frog Rana temporaria.

    PubMed Central

    Knight, G. E.; Burnstock, G.

    1996-01-01

    1. In the isolated aorta of the frog, Rana temporaria, adenosine concentration-dependently, endothelium-independently relaxed adrenaline pre-constricted vessels. None of the adenosine analogues including D-5'-(N-ethylcarboxamide) adenosine (NECA), R- and S-N6-(2-phenylisopropyl) adenosine (R-and S-PIA) and 2-chloroadenosine (2-CA), or the more selective A1, A2 and A3 agonists cyclopentyladenosine (CPA), CGS 21680 and N6-(3-iodobenzyl) adenosine-5'-N-methylcarboxamide (IB-MECA) respectively, had any effect. 2. The non-selective adenosine antagonist, 8-p-sulphophenyl-theophylline (8-pSPT; 30 microM) failed to inhibit adenosine relaxations, as did NG-nitro-L-arginine methyl ester (L-NAME; 0.1 mM) and indomethacin (30 microM). 3. Adenosine 5'-triphosphate (ATP), alpha, beta-methylene ATP (alpha, beta-MeATP), beta, gamma-methylene ATP (beta, gamma-MeATP), 2-methylthio ATP (2-MeSATP) and uridine 5'-triphosphate (UTP) all concentration-dependently contracted the frog aorta. ATP and alpha, beta-MeATP were equipotent and more potent than UTP and beta, gamma-MeATP; 2-MeSATP had little activity. 4. The P2-purinoceptor antagonist, suramin (0.1 mM) inhibited contractions to alpha, beta-MeATP but not to ATP. Pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS; 30 microM) also inhibited contractions to alpha, beta-MeATP but not to ATP. Contractions to ATP were, however, inhibited by indomethacin (30 microM). 5. In conclusion, in the frog aorta there appears to be a novel subclass of P1-purinoceptor mediating vasodilatation, although like the A3 subclass it is not blocked by methylxanthines; a P2-purinoceptor mediates vasconstriction which resembles a P2x subtype, based on the agonist potency of alpha, beta-MeATP being more potent than 2-MeSATP (UTP has moderate activity) and PPADS is an effective antagonist. There is no evidence for the presence of a P2y-purinoceptor, mediating vasodilatation, in this preparation. PMID:8851504

  12. Detection of antidiabetic activity by crude paratoid gland secretions from common Indian toad (bufomelano stictus)

    PubMed Central

    Neerati, Prasad

    2015-01-01

    Background: Amphibians have provided a remarkable array of biological active compounds, which are secreted from socalled granular skin glands which serve to protect the amphibians from predators due to its noxious effects on buccal tissue and at least in the case of some peptides, to protect from bacterial (or) protozoan infections. Given the respiratory and antimicrobial functions of amphibian skin, it is likely that some of the novel molecules found in amphibian granular gland secretions might be of use in the treatment of skin and respiratory infections. Secretions from common Indian toad (Bufo melanostictus) a member of Bufonidae family has the history of medicinal use however the anti-diabetic activity is not reported. The present study is aimed to determine whether paratoid gland extract have any influence on the diabetes and the pharmacokinetics and pharmacodynamics of glimepiride (GLM) in normal and diabetic rats. Materials and Methods: An aqueous and methanolic extracts of paratoid glandular secretions were prepared, air dried and used to determine the antidiabetic activity in rats. The blood sampling was done at preset time intervals between 0, 0.5, 1, 2, 4, 6, 8 and 12 h, using heparinized capillaries. The blood glucose levels are estimated by glucose oxidase-peroxidase method, and reversed-phase high-performance liquid chromatography is used to determine the pharmacokinetic parameters of GLM using glibenclamide as an internal standard. Results: Both the aqueous and methanolic extracts produced better glycemic control in diabetic rats, and methanolic extract is better than the aqueous extract. Serum concentrations of GLM increased at 2nd h, and the percentage glucose reduction is maximal at the 4th h with both aqueous and methanolic extracts of paratoid secretions of common Indian toad. Conclusions: Paratoid gland secretions of the common Indian toad is antidiabetic, in addition it has beneficial effects in combination with GLM. Further, it requires the

  13. Acerogenin A, a natural compound isolated from Acer nikoense Maxim, stimulates osteoblast differentiation through bone morphogenetic protein action

    SciTech Connect

    Kihara, Tasuku; Ichikawa, Saki; Yonezawa, Takayuki; Lee, Ji-Won; Akihisa, Toshihiro; Woo, Je Tae; Michi, Yasuyuki; Amagasa, Teruo; Yamaguchi, Akira

    2011-03-11

    Research highlights: {yields} Acerogenin A stimulated osteoblast differentiation in osteogenic cells. {yields} Acerogenin A-induced osteoblast differentiation was inhibited by noggin. {yields} Acerogenin A increased Bmp-2, Bmp-4 and Bmp-7 mRNA expression in MC3T3-E1 cells. {yields} Acerogenin A is a candidate agent for stimulating bone formation. -- Abstract: We investigated the effects of acerogenin A, a natural compound isolated from Acer nikoense Maxim, on osteoblast differentiation by using osteoblastic cells. Acerogenin A stimulated the cell proliferation of MC3T3-E1 osteoblastic cells and RD-C6 osteoblastic cells (Runx2-deficient cell line). It also increased alkaline phosphatase activity in MC3T3-E1 and RD-C6 cells and calvarial osteoblastic cells isolated from the calvariae of newborn mice. Acerogenin A also increased the expression of mRNAs related to osteoblast differentiation, including Osteocalcin, Osterix and Runx2 in MC3T3-E1 cells and primary osteoblasts: it also stimulated Osteocalcin and Osterix mRNA expression in RD-C6 cells. The acerogenin A treatment for 3 days increased Bmp-2, Bmp-4, and Bmp-7 mRNA expression levels in MC3T3-E1 cells. Adding noggin, a BMP specific-antagonist, inhibited the acerogenin A-induced increase in the Osteocalcin, Osterix and Runx2 mRNA expression levels. These results indicated that acerogenin A stimulates osteoblast differentiation through BMP action, which is mediated by Runx2-dependent and Runx2-independent pathways.

  14. Bioassay-Guided Chromatographic Isolation and Identification of Antibacterial Compounds from Artemisia annua L. That Inhibit Clostridium perfringens Growth.

    PubMed

    Ivarsen, Elise; Fretté, Xavier C; Christensen, Kathrine B; Christensen, Lars P; Engberg, Ricarda M; Grevsen, Kai; Kjaer, Anders

    2014-01-01

    Clostridium perfringens is the causative agent of necrotic enteritis leading to significant losses in the poultry industry. Dichloromethane and n-hexane extracts of aerial parts of Artemisia annua (Asteraceae) exhibited activity against C. perfringens with minimum inhibitory concentrations (MIC) of 185 and 270 μg/mL, respectively. Bioassay-guided fractionation of the extracts gave several active fractions (MIC between 75 and 600 μg/mL). Investigations of the most active fractions resulted in the isolation and characterization of the polyacetylene ponticaepoxide (MIC between 100 and 200 μg/mL) and (+)-threo-(5E)-trideca-1,5-dien-7,9,11-triyne-3,4-diol (MIC between 400 and 800 μg/mL), the flavonols chrysosplenol D (MIC between 200 and 400 μg/mL) and casticin (slight inhibition at 800 μg/mL), and 2,4-dihydroxy-6-methoxyacetophenone (slight inhibition at 800 μg/mL). Also, the coumarin scopoletin and the sesquiterpene lactone artemisinin were isolated from active fractions but showed no inhibition of C. perfringens growth at 800 and 2000 μg/mL, respectively. Fractions containing essential oil components with camphor constituting >60% did not show inhibition of C. perfringens up to 1600 μg/mL. Extracts and some active fractions showed higher antibacterial effect than individual bioactive compounds, suggesting that synergistic effects may underlie the observed antibacterial effect. The present study adds new valuable information on the antibacterial effect of A. annua against C. perfringens. PMID:25902977

  15. Oral anti-diabetics in Ramadan.

    PubMed

    Islam, Najmul

    2015-05-01

    A large proportion of Muslim patients with type 2 diabetes fast during the month of Ramadan worldwide. Hypoglycaemia is one of the major complications associated with long periods without food during the fasting hours. There is also a risk of hyperglycaemia due to over indulgence in food during the two main meals of Suhur and Iftar. Healthcare providers need to be cognizant of the risk of fasting and be competent to provide Ramadan adjusted diabetes care particularly adjustment of oral anti diabetics. This review article has taken into consideration observational studies, randomized trial data, pathophysiology and practical experience in recommending adjustment in oral anti-diabetics during fasting in type-2 diabetics. Metformin and Thiazolidinediones (TZD'S) being insulin sensitizers need minimum adjustment with low risk of hypoglycaemia. Older generation Sulphonylureas (SU) pose a high risk of hypoglycaemia but the newer generations of Sulphonylureas have a reasonable safety profile. Alpha- Glucosidase inhibitors are safe during fasting but their use is limited due to the side effects.

  16. Apelin receptors: From signaling to antidiabetic strategy.

    PubMed

    Chaves-Almagro, C; Castan-Laurell, I; Dray, C; Knauf, C; Valet, P; Masri, B

    2015-09-15

    The G protein-coupled receptor APJ and its cognate ligand, apelin, are widely expressed throughout human body. They are implicated in different key physiological processes such as angiogenesis, cardiovascular functions, fluid homeostasis and energy metabolism regulation. On the other hand, this couple ligand-receptor is also involved in the development and progression of different pathologies including diabetes, obesity, cardiovascular disease and cancer. Recently, a new endogenous peptidic ligand of APJ, named Elabela/Toddler, has been identified and shown to play a crucial role in embryonic development. Whereas nothing is yet known regarding Elabela/Toddler functions in adulthood, apelin has been extensively described as a beneficial adipokine regarding to glucose and lipid metabolism and is endowed with anti-diabetic and anti-obesity properties. Indeed, there is a growing body of evidence supporting apelin signaling as a novel promising therapeutic target for metabolic disorders (obesity, type 2 diabetes). In this review, we provide an overview of the pharmacological properties of APJ and its endogenous ligands. We also report the activity of peptidic and non-peptidic agonists and antagonists targeting APJ described in the literature. Finally, we highlight the important role of this signaling pathway in the control of energy metabolism at the peripheral level and in the central nervous system in both physiological conditions and during obesity or diabetes. PMID:26007641

  17. Synthesis and antidiabetic performance of β-amino ketone containing nabumetone moiety.

    PubMed

    Wang, Hang; Yan, Ju-fang; Song, Xiao-li; Fan, Li; Xu, Jin; Zhou, Guang-ming; Jiang, Li; Yang, Da-cheng

    2012-03-15

    We wish to report the further design and improved synthesis that resulted in two series of target molecules, TM-1 and TM-2, with remarkably simplified structures containing β-amino ketone of discrete nabumetone moiety. These were obtained via a 'one-pot, two-step, three-component' protocol of Mannich reaction with yield up to 97%. A total of 28 out of 31 new compounds were characterized using (1)H NMR, (13)C NMR, ESI MS and HRMS techniques. Studies on their antidiabetic activities, screened in vitro at 10 μg mL(-1) level, indicate that TM-2 possesses peroxisome proliferator-activated receptor activation and α-glucosidase inhibition activity significantly stronger than that of TM-1, and also that of the series B compounds that were previously synthesized by the group. Analysis of the structure-activity relationship points to the sulfanilamide unit as the most probable potent group of β-amino ketone and, on the basis of which, a tangible strategy is presented for the development of new antidiabetic drugs. PMID:22364952

  18. Draft Genome Sequence of Pseudomonas sp. EpS/L25, Isolated from the Medicinal Plant Echinacea purpurea and Able To Synthesize Antimicrobial Compounds

    PubMed Central

    Presta, Luana; Bosi, Emanuele; Fondi, Marco; Maida, Isabel; Perrin, Elena; Miceli, Elisangela; Maggini, Valentina; Bogani, Patrizia; Firenzuoli, Fabio; Di Pilato, Vincenzo; Rossolini, Gian Maria; Mengoni, Alessio

    2016-01-01

    We announce here the draft genome sequence of Pseudomonas sp. strain EpS/L25, isolated from the stem/leaves of the medicinal plant Echinacea purpurea. This genome will allow for comparative genomics in order to identify genes associated with the production of bioactive compounds and antibiotic resistance. PMID:27151804

  19. Draft Genome Sequence of Pseudomonas sp. EpS/L25, Isolated from the Medicinal Plant Echinacea purpurea and Able To Synthesize Antimicrobial Compounds.

    PubMed

    Presta, Luana; Bosi, Emanuele; Fondi, Marco; Maida, Isabel; Perrin, Elena; Miceli, Elisangela; Maggini, Valentina; Bogani, Patrizia; Firenzuoli, Fabio; Di Pilato, Vincenzo; Rossolini, Gian Maria; Mengoni, Alessio; Fani, Renato

    2016-01-01

    We announce here the draft genome sequence of Pseudomonas sp. strain EpS/L25, isolated from the stem/leaves of the medicinal plant Echinacea purpurea This genome will allow for comparative genomics in order to identify genes associated with the production of bioactive compounds and antibiotic resistance. PMID:27151804

  20. Volatile organic compounds from fungi isolated after hurricane katrina induce developmental defects and apoptosis in a Drosophila melanogaster model.

    PubMed

    Inamdar, Arati A; Bennett, Joan W

    2015-05-01

    In previous work, our laboratory developed a Drosophila model for studying the adverse effects of fungal volatile organic compounds (VOCs) emitted by growing cultures of molds. In this report, we have extended these studies and compared the toxic effects of fungal VOCs emitted from living cultures of four molds isolated after Hurricane Katrina from a flooded home in New Orleans. Strains of Aspergillus, Mucor, Penicillium, and Trichoderma were grown with wild-type larvae and the toxic effects of volatile products on the developmental stages of Drosophila larvae were evaluated. Furthermore, heterozygous mutants of Drosophila carrying the apoptotic genes, reaper and dronc, were used to assess the role of apoptosis in fungal VOCs mediated toxicity. Third-instar larvae of Drosophila carrying these apoptotic genes were exposed to fungal VOCs emitted from growing mold cultures for 10 days. The larval strains carrying apoptopic genes survived longer than the control wild type larvae; moreover, of those that survived, heterozygous reaper and dronc strains progressed to pupae and adult phases more rapidly, suggesting that fungal VOCs may induce apoptotic changes in flies. These data lend support to the use of Drosophila as an inexpensive and genetically versatile toxicological model to investigate the mechanistic basis for some of the human illnesses/symptoms associated with exposure to mold-contaminated indoor air, especially after hurricanes.

  1. Volatile organic compounds from fungi isolated after hurricane katrina induce developmental defects and apoptosis in a Drosophila melanogaster model.

    PubMed

    Inamdar, Arati A; Bennett, Joan W

    2015-05-01

    In previous work, our laboratory developed a Drosophila model for studying the adverse effects of fungal volatile organic compounds (VOCs) emitted by growing cultures of molds. In this report, we have extended these studies and compared the toxic effects of fungal VOCs emitted from living cultures of four molds isolated after Hurricane Katrina from a flooded home in New Orleans. Strains of Aspergillus, Mucor, Penicillium, and Trichoderma were grown with wild-type larvae and the toxic effects of volatile products on the developmental stages of Drosophila larvae were evaluated. Furthermore, heterozygous mutants of Drosophila carrying the apoptotic genes, reaper and dronc, were used to assess the role of apoptosis in fungal VOCs mediated toxicity. Third-instar larvae of Drosophila carrying these apoptotic genes were exposed to fungal VOCs emitted from growing mold cultures for 10 days. The larval strains carrying apoptopic genes survived longer than the control wild type larvae; moreover, of those that survived, heterozygous reaper and dronc strains progressed to pupae and adult phases more rapidly, suggesting that fungal VOCs may induce apoptotic changes in flies. These data lend support to the use of Drosophila as an inexpensive and genetically versatile toxicological model to investigate the mechanistic basis for some of the human illnesses/symptoms associated with exposure to mold-contaminated indoor air, especially after hurricanes. PMID:24307503

  2. Central Antinociceptive and Mechanism of Action of Pereskia bleo Kunth Leaves Crude Extract, Fractions, and Isolated Compounds

    PubMed Central

    Guilhon, Carolina Carvalho; Abdul Wahab, Ikarastika Rahayu; Boylan, Fabio; Fernandes, Patricia Dias

    2015-01-01

    Pereskia bleo (Kunth) DC. (Cactaceae) is a plant commonly used in popular medicine in Malaysia. In this work, we evaluate the antinociceptive effect of P. bleo leaf extracts and isolated compounds in central antinociceptive model. Ethanol extract (E), hexane (H), ethyl acetate (EA), or butanol (B) fractions (30, 50, or 100 mg/kg, p.o.), sitosterol (from hexane) and vitexin (from ethyl acetate), were administered to mice. Antinociceptive effect was evaluated in the hot plate and capsaicin- or glutamate-induced licking models. Morphine (1 mg/kg, p.o.) was used as reference drug. Naloxone (1 mg/kg, i.p.), atropine (1 mg/kg, i.p.), and L-nitro arginine methyl ester (L-NAME, 3 mg/kg, i.p.) were administered 30 min earlier (100 mg/kg, p.o.) in order to evaluate the mechanism of the antinociceptive action. Higher dose of B developed an effect significantly superior to morphine-treated group. Naloxone prevented the antinociceptive effect of all fractions. L-NAME demonstrated effect against E, EA, and B. In all fractions, sitosterol and vitexin reduced the licking time after capsaicin injection. Glutamate-induced licking response was blocked by H, EA, and B. Our results indicate that Pereskia bleo fractions, sitosterol and vitexin, possessed a central antinociceptive effect. Part of this effect is mediated by opioid receptors and nitrergic pathway. PMID:26273315

  3. From an Isolable Acyclic Phosphinosilylene Adduct to Donor-Stabilized Si=E Compounds (E=O, S, Se).

    PubMed

    Hansen, Kerstin; Szilvási, Tibor; Blom, Burgert; Irran, Elisabeth; Driess, Matthias

    2015-12-21

    Reaction of the arylchlorosilylene-NHC adduct ArSi(NHC)Cl [Ar=2,6-Trip2C6H3; NHC=(MeC)2(NMe)2C:] 1 with one molar equiv of lithium diphenylphosphanide affords the first stable NHC-stabilized acyclic phosphinosilylene adduct 2 (ArSi(NHC)PPh2), which could be structurally characterized. Compound 2, when reacted with one molar equiv selenium and sulfur, affords the silanechalcogenones 4 a and 4 b (ArSi(NHC)(=E)PPh2, 4 a: E=Se, 4 b: E=S), respectively. Conversion of 2 with an excess of Se and S, through additional insertion of one chalcogen atom into the Si=P bond, leads to 3 a and 3 b (ArSi(NHC)(=E)-E-P(=E)Ph2, 3 a: E=Se, 3 b: E=S), respectively. Additionally, the exposure of 2 to N2O or CO2 yielded the isolable NHC-stabilized silanone 4 c, Ar(NHC)(Ph2P)Si=O. PMID:26592863

  4. Inhibition of matrix metalloproteinase-1 and type-I procollagen expression by phenolic compounds isolated from the leaves of Quercus mongolica in ultraviolet-irradiated human fibroblast cells.

    PubMed

    Kim, Han Hyuk; Kim, Dong Hee; Oh, Myeong Hwan; Park, Kwang Jun; Heo, Jun Hyeok; Lee, Min Won

    2015-01-01

    The aim of this study was to investigate the effect of Quercus mongolica (QM) which induce anti-photoaging process of skin in vitro. Bioassay-guided isolation of 80 % Me2CO extract of the leaves of QM led to the isolation and identification of six known phenolic compounds: pedunculagin (1), (-)-epigallocatechin (2), (+)-catechin (3), quercetin 3-O-(6″-O-galloyl)-β-D-glucopyranoside (4), kaempferol-3-O-β-D-glucopyranoside-7-O-α-L-rhamnopyranoside (5) and kaempferol 3-O-(6″-galloyl)-β-D-glucopyranoside (6). The effects of compounds 1-6 on expression of matrix metalloproteinase-1 (MMP-1) and type-I procollagen were further evaluated. Among them, compound 1 showed potent inhibitory effect on MMP-1 and the increased type-I procollagen synthesis in ultraviolet B-induced human fibroblast. These results suggest that pedunculagin, an ellagitannin, is a potential candidate for the prevention and treatment of skin aging.

  5. Isolation and identification of colourless caffeoyl compounds in purple sweet potato by HPLC-DAD-ESI/MS and their antioxidant activities.

    PubMed

    Zhao, Jin-Ge; Yan, Qian-Qian; Xue, Ren-Yu; Zhang, Jian; Zhang, Yu-Qing

    2014-10-15

    More than 10 red anthocyanins and related glucosides have been isolated and identified from purple sweet potato (Ipomoea batatas, Ayamurasaki) in the recent decades. This paper reports the isolation of colourless caffeoyl compounds from purple sweet potato using AB-8 macroresin absorption and semi-preparative HPLC-DAD. The structures of the five isolated monomers were identified as: 5-caffeoylquinic acid (1), 6-O-caffeoyl-β-d-fructofuranosyl-(2-1)-α-d-glucopyranoside (2) and trans-4,5-dicaffeoylquinic acid (3), 3,5-dicaffeoylquinic acid (4), 4,5-dicaffeoylquinic acid (5), and by ESI/MS and NMR. Compounds 1, 4 and 5 were reported previously in combination with anthocyanins in purple sweet potato, whereas 2 and 3 were found for the first time. In vitro antioxidant assay showed trans-4,5-dicaffeoylquinic acid has significant antioxidant activities. These results should lay the groundwork for further work identifying purple sweet potato as a healthy food.

  6. Synthesis and Evaluation of 1-Substituted-Biguanide Derivatives as Anti-Diabetic Agents for Type II Diabetes Insulin Resistant.

    PubMed

    Abbas, S Y; Basyouni, W M; El-Bayouki, K A M; Abdel-Rahman, R F

    2016-07-01

    New 1-substituted-biguanide derivatives 1-3 were synthesized by the reaction of 2,4-dimethoxyaniline, hydrazine and methylhydrazine with dicyandiamide in diluted hydrochloric acid. The resulting biguanide salts were fully characterized by spectroscopic methods. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives (200 mg/kg/day) for 2 weeks significantly decreased the elevated blood glucose level. Oral administration of biguanide derivative 2 significantly decreased the level of total cholesterol. While, the triglycerides level was little decreased following administration of biguanide 1 as compared to hyperglycemic rats. Additionally, anti-diabetic properties towards liver function enzyme activities (AST and ALT) and kidney functions (urea and critinine) as well as histopathological studies relative to metformin hydrochloride were investigated and discussed. PMID:27191826

  7. Antidiabetic treatment with gliptins: focus on cardiovascular effects and outcomes.

    PubMed

    Fisman, Enrique Z; Tenenbaum, Alexander

    2015-01-01

    The traditional oral pharmacological therapy for type 2 diabetes mellitus (T2DM) has been based on the prescription of metformin, a biguanide, as first line antihyperglycemic agent world over. It has been demonstrated that after 3 years of treatment, approximately 50% of diabetic patients could achieve acceptable glucose levels with monotherapy; but by 9 years this had declined to only 25%. Therefore, the implementation of a combined pharmacological therapy acting via different pathways becomes necessary, and its combination with a compound of the sulfonylurea group was along decades the most frequently employed prescription in routine clinical practice. Meglitinides, glitazones and alpha-glucosidase inhibitors were subsequently developed, but the five mentioned groups of oral antihyperglycemic agents are associated with variable degrees of undesirable or even severe cardiovascular events. The gliptins-also called dipeptidyl peptidase 4 (DPP4) inhibitors--are an additional group of antidiabetic compounds with increasing clinical use. We review the status of the gliptins with emphasis on their capabilities to positively or negatively affect the cardiovascular system, and their potential involvement in major adverse cardiovascular events (MACE). Alogliptin, anagliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin and vildagliptin are the compounds currently in clinical use. Regardless differences in chemical structure and metabolic pathways, gliptins as a group exert favorable changes in experimental models. These changes, as an almost general rule, include improved endothelial function, reduction of inflammatory markers, oxidative stress ischemia/reperfusion injury and atherogenesis. In addition, increased adiponectin levels and modest decreases in lipidemia and blood pressure were reported. In clinical settings, several trials--notably the longer one, employing sitagliptin, with a mean follow-up period of 3 years--did not show an increased risk for ischemic

  8. Antidiabetic treatment with gliptins: focus on cardiovascular effects and outcomes.

    PubMed

    Fisman, Enrique Z; Tenenbaum, Alexander

    2015-01-01

    The traditional oral pharmacological therapy for type 2 diabetes mellitus (T2DM) has been based on the prescription of metformin, a biguanide, as first line antihyperglycemic agent world over. It has been demonstrated that after 3 years of treatment, approximately 50% of diabetic patients could achieve acceptable glucose levels with monotherapy; but by 9 years this had declined to only 25%. Therefore, the implementation of a combined pharmacological therapy acting via different pathways becomes necessary, and its combination with a compound of the sulfonylurea group was along decades the most frequently employed prescription in routine clinical practice. Meglitinides, glitazones and alpha-glucosidase inhibitors were subsequently developed, but the five mentioned groups of oral antihyperglycemic agents are associated with variable degrees of undesirable or even severe cardiovascular events. The gliptins-also called dipeptidyl peptidase 4 (DPP4) inhibitors--are an additional group of antidiabetic compounds with increasing clinical use. We review the status of the gliptins with emphasis on their capabilities to positively or negatively affect the cardiovascular system, and their potential involvement in major adverse cardiovascular events (MACE). Alogliptin, anagliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin and vildagliptin are the compounds currently in clinical use. Regardless differences in chemical structure and metabolic pathways, gliptins as a group exert favorable changes in experimental models. These changes, as an almost general rule, include improved endothelial function, reduction of inflammatory markers, oxidative stress ischemia/reperfusion injury and atherogenesis. In addition, increased adiponectin levels and modest decreases in lipidemia and blood pressure were reported. In clinical settings, several trials--notably the longer one, employing sitagliptin, with a mean follow-up period of 3 years--did not show an increased risk for ischemic

  9. Synthesis, characterization and anti-diabetic therapeutic potential of a new benzyl acid-derivatized kojic acid vanadyl complex.

    PubMed

    Wei, Yong-Biao; Yang, Xiao-Da

    2012-12-01

    Vanadium complexes are potent hypoglycemic agents and of great potential for therapeutical treatment of diabetes. In the present work, a novel vanadium compound, bis ((5-hydroxy-4-oxo-4H-pyran-2-yl)methyl benzoatato) oxovanadium (IV) (BBOV) has been synthesized. Treatment of STZ-induced diabetic rats with BBOV restored the blood glucose to normal level and ameliorated glucose tolerance. The hypoglycemic effect of BBOV is similar to that of bis (maltolato) oxovanadium but is less toxic in median lethal dose. Overall, the present work will provide useful information for further development of new anti-diabetic vanadium compounds.

  10. Potent Antidiabetic Activity and Metabolite Profiling of Melicope Lunu-ankenda Leaves.

    PubMed

    Al-Zuaidy, Mizher Hezam; Hamid, Azizah Abdul; Ismail, Amin; Mohamed, Suhaila; Abdul Razis, Ahmad Faizal; Mumtaz, Muhammad Waseem; Salleh, Syafiq Zikri

    2016-05-01

    Diabetes mellitus is normally characterized by chronic hyperglycemia associated with disturbances in the fat, carbohydrate, and protein metabolism. There is an increasing trend of using natural products instead of synthetic agents as alternative therapy for disorders due to their fewer side effects. In this study, antidiabetic and antioxidant activities of different Melicope lunu-ankenda (ML) ethanolic extracts were evaluated using inhibition of α-glucosidase and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals scavenging activity, respectively; whereas, proton nuclear magnetic resonance ((1) H NMR) and ultra-high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) techniques were used for metabolite profiling of ML leaf extracts at different concentrations of ethanol and water. Sixty percent of ethanolic ML extract showed highest inhibitory effect against α-glucosidase enzyme (IC50 of 37 μg/mL) and DPPH scavenging activity (IC50 of 48 μg/mL). Antidiabetic effect of ML extracts was also evaluated in vivo and it was found that the high doses (400 mg/Kg BW) of ML extract exhibited high suppression in fasting blood glucose level by 62.75%. The metabolites responsible for variation among ML samples with variable ethanolic levels have been evaluated successfully using (1) H-NMR-based metabolomics. The principal component analysis (PCA) and partial least squares(PLS) analysis scores depicted clear and distinct separations into 4 clusters representing the 4 ethanolic concentrations by PC1 and PC2, with an eigenvalue of 69.9%. Various (1) H-NMR chemical shifts related to the metabolites responsible for sample difference were also ascribed. The main bioactive compounds identified attributing toward the separation included: isorhamnetin, skimmianine, scopoletin, and melicarpinone. Hence, ML may be used as promising medicinal plant for the development of new functional foods, new generation antidiabetic drugs, as a single entity phytomedicine or in

  11. Potent Antidiabetic Activity and Metabolite Profiling of Melicope Lunu-ankenda Leaves.

    PubMed

    Al-Zuaidy, Mizher Hezam; Hamid, Azizah Abdul; Ismail, Amin; Mohamed, Suhaila; Abdul Razis, Ahmad Faizal; Mumtaz, Muhammad Waseem; Salleh, Syafiq Zikri

    2016-05-01

    Diabetes mellitus is normally characterized by chronic hyperglycemia associated with disturbances in the fat, carbohydrate, and protein metabolism. There is an increasing trend of using natural products instead of synthetic agents as alternative therapy for disorders due to their fewer side effects. In this study, antidiabetic and antioxidant activities of different Melicope lunu-ankenda (ML) ethanolic extracts were evaluated using inhibition of α-glucosidase and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals scavenging activity, respectively; whereas, proton nuclear magnetic resonance ((1) H NMR) and ultra-high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) techniques were used for metabolite profiling of ML leaf extracts at different concentrations of ethanol and water. Sixty percent of ethanolic ML extract showed highest inhibitory effect against α-glucosidase enzyme (IC50 of 37 μg/mL) and DPPH scavenging activity (IC50 of 48 μg/mL). Antidiabetic effect of ML extracts was also evaluated in vivo and it was found that the high doses (400 mg/Kg BW) of ML extract exhibited high suppression in fasting blood glucose level by 62.75%. The metabolites responsible for variation among ML samples with variable ethanolic levels have been evaluated successfully using (1) H-NMR-based metabolomics. The principal component analysis (PCA) and partial least squares(PLS) analysis scores depicted clear and distinct separations into 4 clusters representing the 4 ethanolic concentrations by PC1 and PC2, with an eigenvalue of 69.9%. Various (1) H-NMR chemical shifts related to the metabolites responsible for sample difference were also ascribed. The main bioactive compounds identified attributing toward the separation included: isorhamnetin, skimmianine, scopoletin, and melicarpinone. Hence, ML may be used as promising medicinal plant for the development of new functional foods, new generation antidiabetic drugs, as a single entity phytomedicine or in

  12. Isolation of pure compound R/J/3 from Pluchea indica (L.) Less. and its anti-amoebic activities against Entamoeba histolytica.

    PubMed

    Biswas, Ria; Dutta, P K; Achari, B; Bandyopadhyay, Durba; Mishra, Moumita; Pramanik, K C; Chatterjee, T K

    2007-08-01

    The plant Pluchea indica is known for its anti-inflammatory, anti-ulcer, anti-pyretic, hypoglycemic, diuretic and anti-microbial activities besides many other pharmacological activities. We have isolated and purified seven compounds from the methanolic root extract of this plant by column chromatography. The compounds were identified by spectroscopic analyses. The anti-amoebic activities of the pure compound R/J/3 was investigated against the HM1 strain of Entamoeba histolytica. The compound, R/J/3 showed the most pronounced anti-proliferative activity at a dose of 50 microg/ml. It also showed a marked activity on cell lysis of trophozoites, 4h after administration. The cell lytic activity was compared with metronidazole (5 microg/ml) as positive control. PMID:17174538

  13. Bioassay-guided isolation and identification of bioactive compound from aerial parts of Luffa acutangula against lung cancer cell line NCI-H460.

    PubMed

    Vanajothi, Ramar; Srinivasan, Pappu

    2015-01-01

    Luffa acutangula (Cucurbitaceae) is widely used as a traditional medicine in India and was reported to possess various pharmacological activities including its anti-proliferative effects. In this study, the bioactive compound of ethanolic extract of L. acutangula (LA) was isolated using bioassay-guided approach. Five major fractions were collected and evaluated for their anti-proliferative activity against non-small cell lung cancer cells (NCI-H460). Among the test fractions, the fraction LA/FII effectively decreased the growth of cancer cells with IC50 values of 10 µg/ml concentration. Furthermore, it significantly increased intracellular reactive oxygen species and decreased the mitochondrial membrane potential. The apoptogenic activity of fraction LA/FII was confirmed by cell shrinkage, membrane blebbing and formation of apoptotic bodies. A single bioactive compound was isolated from the active faction, LA/FII and subsequently identified as 1,8 dihydroxy-4-methylanthracene 9,10-dione (compound 1) by comparing its spectral data [Ultraviolet (UV), Infrared (IR), Nuclear magnetic resonance (NMR) and Electrospray Ionization-Mass Spectroscopy (ESI-MS)] with literature values. This is the first report on the isolation of compound 1 from this plant.

  14. Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones.

    PubMed Central

    Yakushiji, T.; Fukuda, T.; Oyama, Y.; Akaike, N.

    1989-01-01

    1. The effects of benzodiazepines and non-benzodiazepine compounds on the gamma-aminobutyric acid (GABA)-induced chloride current (ICl) were studied in frog isolated sensory neurones by use of a concentration-jump (termed 'concentration-clamp') technique, under single-electrode voltage-clamp conditions. The drugs used were classified into four categories as follows: full benzodiazepine receptor agonists (diazepam, clonazepam, nitrazepam, midazolam, clotiazepam and etizolam), partial agonists (CL 218,872, Ro 16-6028, Ro 17-1812 and Ro 23-0364), inverse agonists (Ro 15-3505, FG 7142 and beta-CCE) and a benzodiazepine receptor antagonist, Ro 15-1788 (flumazenil). 2. All full agonists at concentrations of 3 x 10(-6) M or less increased dose-dependently the peak amplitude of ICl elicited by 3 x 10(-6) M GABA to twice to three times larger than the control. However, no further augmentation of the GABA response was observed at concentrations of 1 x 10(-5) M or higher. Partial agonists also showed a dose-dependent augmentation of the GABA response at concentrations ranging from 3 x 10(-8) M to 3 x 10(-5) M, but their efficacies of augmentation of the GABA response were only about half or less of those of full agonists. Of the inverse agonists, beta-CCE had a unique dose-dependent effect on the GABA response. Beta-CCE reduced dose-dependently the GABA response at concentrations of less than 3 x 10(-6) M, but augmented it at concentrations of 3 x 10(-5) M and 6 x 10(-5) M. The inverse agonists reduced dose-dependently the GABA response.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2574062

  15. Anti-inflammatory activity of compounds isolated from Astragalus sinicus L. in cytokine-induced keratinocytes and skin

    PubMed Central

    Kim, Byung-Hak; Oh, Ikhoon; Kim, Jung-Ho; Jeon, Ju-eun; Jeon, Byeongwook; Shin, Jongheon; Kim, Tae-Yoon

    2014-01-01

    Inflammation is a part of the complex biological responses of a tissue to injury that protect the organ by removing injurious stimuli and initiating the healing process, and is considered as a mechanism of innate immunity. To identify biologically active compounds against pathogenic inflammatory and immune responses, we fractionated water, aqueous methanol and n-hexane layers from nine kinds of leguminosae and examined anti-inflammatory activity of the fractions in human keratinocytes and mouse skin. Among the fractions, rf3 and rf4, isolated from the aqueous methanol layer of Astragalus sinicus L., exhibited the strongest reactive oxygen species (ROS)-scavenging and anti-inflammatory activities as measured by inhibition of the intracellular ROS production, nuclear factor-kappaB (NF-κB), janus kinase (JAK)/signal transducer and activator of transcription (STAT), and phosphatidylinositol 3-kinase/Akt signaling in cytokine-stimulated human keratinocytes, as well as by effects on T-cell differentiation in mouse CD4+ T cells. In addition, topical application of rf3 and rf4 suppressed the progression of psoriasis-like dermatitis and expression of pro-inflammatory mediators in interleukin (IL)-23-injected mouse ears. Our results suggest that Astragalus sinicus L. may ameliorate chronic inflammatory skin diseases due to its antioxidant and anti-inflammatory activities via regulation of the intracellular ROS production, NF-κB, JAK/STAT and PI3/Akt signaling cascades as well as immune responses, and these results are the first report that Astragalus sinicus L. exhibits pharmacological activity. PMID:24651533

  16. Infrared Spectroscopy of Matrix-Isolated Polycyclic Aromatic Compounds and their Ions. 6; Polycyclic Aromatic Nitrogen Heterocycles

    NASA Technical Reports Server (NTRS)

    Mattioda, A. L.; Hudgins, Douglas M.; Bauschlicher, C. W., Jr.; Rosi, M.; Allamandola, L. J.; DeVincenzi, D. (Technical Monitor)

    2002-01-01

    The matrix-isolation technique has been employed to measure the mid-infrared spectra of several polycyclic aromatic nitrogen heterocycles in both neutral and cationic forms. The species studied include: 7,8 benzoquinoline (C13H9N); 2-azapyrene (C15H9N); 1- and 2-azabenz(a)anthracene (C17H11N); and 1-, 2-, and 4-azachrysene (also C17H11N). The experimentally measured band frequencies and intensities for each molecule are tabulated and compared with their theoretically calculated values computed using density functional theory at the B3LYP/4-31G level. The overall agreement between experiment and theory is quite good, in keeping with previous investigations involving the parent aromatic hydrocarbons. Several interesting spectroscopic trends are found to accompany nitrogen substitution into the aromatic framework of these compounds. First, for the neutral species, the nitrogen atom produces a significant increase in the total integrated infrared intensity across the 1600 - 1100/cm region and plays an essential role in the molecular vibration that underlies an uncharacteristically intense, discrete feature that is observed near 1400/cm in the spectra of 7,8 benzoquinoline, 1-azabenz(a)anthracene, and 4-azachrysene. The origin of this enhanced infrared activity and the nature of the new 1400/cm vibrational mode are explored. Finally, in contrast to the parent hydrocarbon species, these aromatic nitrogen heterocycles possess a significant permanent dipole moment. Consequently, these dipole moments and the rotational constants are reported for these species in their neutral and ionized forms.

  17. Anti-inflammatory activity of compounds isolated from Astragalus sinicus L. in cytokine-induced keratinocytes and skin.

    PubMed

    Kim, Byung-Hak; Oh, Ikhoon; Kim, Jung-Ho; Jeon, Ju-Eun; Jeon, Byeongwook; Shin, Jongheon; Kim, Tae-Yoon

    2014-03-21

    Inflammation is a part of the complex biological responses of a tissue to injury that protect the organ by removing injurious stimuli and initiating the healing process, and is considered as a mechanism of innate immunity. To identify biologically active compounds against pathogenic inflammatory and immune responses, we fractionated water, aqueous methanol and n-hexane layers from nine kinds of leguminosae and examined anti-inflammatory activity of the fractions in human keratinocytes and mouse skin. Among the fractions, rf3 and rf4, isolated from the aqueous methanol layer of Astragalus sinicus L., exhibited the strongest reactive oxygen species (ROS)-scavenging and anti-inflammatory activities as measured by inhibition of the intracellular ROS production, nuclear factor-kappaB (NF-κB), janus kinase (JAK)/signal transducer and activator of transcription (STAT), and phosphatidylinositol 3-kinase/Akt signaling in cytokine-stimulated human keratinocytes, as well as by effects on T-cell differentiation in mouse CD4(+) T cells. In addition, topical application of rf3 and rf4 suppressed the progression of psoriasis-like dermatitis and expression of pro-inflammatory mediators in interleukin (IL)-23-injected mouse ears. Our results suggest that Astragalus sinicus L. may ameliorate chronic inflammatory skin diseases due to its antioxidant and anti-inflammatory activities via regulation of the intracellular ROS production, NF-κB, JAK/STAT and PI3/Akt signaling cascades as well as immune responses, and these results are the first report that Astragalus sinicus L. exhibits pharmacological activity.

  18. Isolation, Characterization, Crystal Structure Elucidation of Two Flavanones and Simultaneous RP-HPLC Determination of Five Major Compounds from Syzygium campanulatum Korth.

    PubMed

    Memon, Abdul Hakeem; Ismail, Zhari; Al-Suede, Fouad Saleih Resq; Aisha, Abdalrahim F A; Hamil, Mohammad Shahrul Ridzuan; Saeed, Mohammed Ali Ahmed; Laghari, Madeeha; Majid, Amin Malik Shah Abdul

    2015-08-04

    Two flavanones named (2S)-7-Hydroxy-5-methoxy-6,8-dimethyl flavanone (1), (S)-5,7-dihydroxy-6,8-dimethyl-flavanone (2), along with known chalcone, namely, (E)-2',4'- dihydroxy-6'-methoxy-3',5'-dimethylchalcone (3) and two triterpenoids, namely, betulinic and ursolic acids (4 and 5), were isolated from the leaves of Syzygium campanulatum Korth (Myrtaceae). The structures of compounds (1 and 2) were determined on the basis of UV-visible, FTIR, NMR spectroscopies and LC-EIMS analytical techniques. Furthermore, new, simple, precise, selective, accurate, highly sensitive, efficient and reproducible RP-HPLC method was developed and validated for the quantitative analysis of the compounds (1-5) from S. campanulatum plants of five different age. RP-HPLC method was validated in terms of specificity, linearity (r2 ≤ 0.999), precision (2.0% RSD), and recoveries (94.4%-105%). The LOD and LOQ of these compounds ranged from 0.13-0.38 and 0.10-2.23 μg·mL-1, OPEN ACCESS respectively. Anti-proliferative activity of isolated flavanones (1 and 2) and standardized extract of S. campanulatum was evaluated on human colon cancer (HCT 116) cell line. Compounds (1 and 2) and extract revealed potent and dose-dependent activity with IC50 67.6, 132.9 and 93.4 μg·mL-1, respectively. To the best of our knowledge, this is the first study on isolation, characterization, X-ray crystallographic analysis of compounds (1 and 2) and simultaneous RP-HPLC determination of five major compounds (1-5) from different age of S. campanulatum plants.

  19. Molecular Modeling Studies of Thiophenyl C-Aryl Glucoside SGLT2 Inhibitors as Potential Antidiabetic Agents

    PubMed Central

    Sharma, Mukesh C.; Sharma, Smita

    2014-01-01

    A QSAR study on thiophenyl derivatives as SGLT2 inhibitors as potential antidiabetic agents was performed with thirty-three compounds. Comparison of the obtained results indicated the superiority of the genetic algorithm over the simulated annealing and stepwise forward-backward variable method for feature selection. The best 2D QSAR model showed satisfactory statistical parameters for the data set (r2 = 0.8499, q2 = 0.8267, and pred_r2 = 0.7729) with four descriptors describing the nature of substituent groups and the environment of the substitution site. Evaluation of the model implied that electron-rich substitution position improves the inhibitory activity. The good predictive 3D-QSAR models by k-nearest neighbor (kNN) method for molecular field analysis (MFA) have cross-validated coefficient q2 value of 0.7663 and predicted r2 value of 0.7386. The results have showed that thiophenyl groups are necessary for activity and halogen, bulky, and less bulky groups in thiophenyl nucleus enhanced the biological activity. These studies are promising for the development of novel SGLT2 inhibitor, which may have potent antidiabetic activity. PMID:25574393

  20. Evaluation of Antioxidative and Antidiabetic Activity of Bark of Holarrhena Pubescens Wall

    PubMed Central

    Jamarkattel, Nirmala; Shrestha, Aasmin; Lamsal, Nisha Kiran; Shakya, Sangam; Rajbhandari, Sneha

    2014-01-01

    Objective: The objectives of the study are to screen out various phytochemicals and to evaluate the antioxidant and antidiabetic potential of the stem bark of Holarrhena pubescens Wall (Holarrhena antidysenterica). Materials and Methods: The antioxidant activity was determined by the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity where ascorbic acid was taken as positive control. The antioxidant property was later exploited and the methanolic extract of plant was tested for antihyperglycemic activity in glucose overloaded hyperglycemic mice. The extract was tested for its hypoglycemic activity at two-dose levels, 250 and 500 mg/kg respectively where Glipizide 5 mg/kg was taken as standard reference drug. All results are presented as mean ± SD (Standard Deviation). Significant differences between experimental groups were determined by Student’s t-test. Results: The methanolic and water extract showed strong antioxidant activity with inhibition of more than 90% DPPH free radicals at the concentration of 100μg/mL. The hypoglycemic activity of methanolic extract on glucose tolerance test were significant (p <0.05) for the effects of 500 mg/kg after 120 min of treatment and (p <0.01) for 250 mg/kg of extract after half hour of treatment compared to control. Conclusion: The presence of flavonoides, phenolic compounds suggested that they may be partially responsible for antioxidant and antidiabetic activity. PMID:25386454

  1. Anti-Diabetic Potential of Noni: The Yin and the Yang.

    PubMed

    Nerurkar, Pratibha V; Hwang, Phoebe W; Saksa, Erik

    2015-01-01

    Escalating trends of chronic diseases such as type-2 diabetes (T2D) have sparked a renewed interest in complementary and alternative medicine, including herbal products. Morinda citrifolia (noni) has been used for centuries by Pacific Islanders to treat various ailments. Commercial noni fruit juice has been marketed as a dietary supplement since 1996. In 2003, the European Commission approved Tahitian noni juice as a novel food by the Health and Consumer Protection Directorate General. Among noni's several health benefits, others and we have demonstrated the anti-diabetic effects of fermented noni fruit juice in animal models. Unfortunately, noni's exciting journey from Polynesian medicine to the research bench does not reach its final destination of successful clinical outcomes when translated into commercial products. Noni products are perceived to be safe due to their "natural" origin. However, inadequate evidence regarding bioactive compounds, molecular targets, mechanism of action, pharmacokinetics, long-term safety, effective dosages, and/or unanticipated side effects are major roadblocks to successful translation "from bench side to bedside". In this review we summarize the anti-diabetic potential of noni, differences between traditional and modern use of noni, along with beneficial clinical studies of noni products and challenges in clinical translation of noni's health benefits.

  2. Antioxidant versus anti-diabetic properties of leaves from Vernonia amygdalina Del. growing in Malaysia.

    PubMed

    Atangwho, Item J; Egbung, Godwin E; Ahmad, Mariam; Yam, Mun F; Asmawi, Mohd Z

    2013-12-15

    The antioxidant and anti-diabetic properties of the sequential extracts of Vernonia amygdalina based on the chemical composition of the most effective anti-diabetic extract were studied. Using DPPH and ABTS radical scavenging as well as FRAP assays, the extracts showed a consistent dose-dependent trend of potent antioxidant activity in the following solvents: water extract>methanol extract>chloroform extract>and petroleum ether extracts. In the oral glucose tolerance test, the chloroform extract exerted the highest response (33.3%), similar to metformin (27.2%), after 2h compared to the control (50.8%, P<0.05). After a 14-day administration in diabetic rats, the chloroform extract recorded the highest blood (23.5%) and serum (21.4%) glucose-lowering effects (P<0.05). GC-MS analysis of the chloroform extract revealed high levels of linoleic acid (4.72%), α-linolenic acid (10.8%) and phytols (12.0%), as well as other compounds. PMID:23993503

  3. Synthesis and Evaluation of Novel Triterpene Analogues of Ursolic Acid as Potential Antidiabetic Agent.

    PubMed

    Wu, Panpan; Zheng, Jie; Huang, Tianming; Li, Dianmeng; Hu, Qingqing; Cheng, Anming; Jiang, Zhengyun; Jiao, Luoying; Zhao, Suqing; Zhang, Kun

    2015-01-01

    Ursolic acid (UA) is a naturally bioactive compound that possesses potential anti-diabetic activity. The relatively safe and effective molecule intrigued us to further explore and to improve its anti-diabetic activity. In the present study, a series of novel UA analogues was synthesized and their structures were characterized. Their bioactivities against the α-glucosidase from baker's yeast were determined in vitro. The results suggested that most of the analogues exhibited significant inhibitory activity, especially analogues 8b and 9b with the IC50 values of 1.27 ± 0.27 μM (8b) and 1.28 ± 0.27 μM (9b), which were lower than the other analogues and the positive control. The molecular docking and 2D-QSAR studies were carried out to prove that the C-3 hydroxyl could interact with the hydrophobic region of the active pocket and form hydrogen bonds to increase the binding affinity of ligand and the homology modelling protein. Thus, these results will be helpful for understanding the relationship between binding mode and bioactivity and for designing better inhibitors from UA analogues. PMID:26406581

  4. Synthesis and Evaluation of Novel Triterpene Analogues of Ursolic Acid as Potential Antidiabetic Agent

    PubMed Central

    Wu, Panpan; Zheng, Jie; Huang, Tianming; Li, Dianmeng; Hu, Qingqing; Cheng, Anming; Jiang, Zhengyun; Jiao, Luoying; Zhao, Suqing; Zhang, Kun

    2015-01-01

    Ursolic acid (UA) is a naturally bioactive compound that possesses potential anti-diabetic activity. The relatively safe and effective molecule intrigued us to further explore and to improve its anti-diabetic activity. In the present study, a series of novel UA analogues was synthesized and their structures were characterized. Their bioactivities against the α-glucosidase from baker's yeast were determined in vitro. The results suggested that most of the analogues exhibited significant inhibitory activity, especially analogues 8b and 9b with the IC50 values of 1.27 ± 0.27 μM (8b) and 1.28 ± 0.27 μM (9b), which were lower than the other analogues and the positive control. The molecular docking and 2D-QSAR studies were carried out to prove that the C-3 hydroxyl could interact with the hydrophobic region of the active pocket and form hydrogen bonds to increase the binding affinity of ligand and the homology modelling protein. Thus, these results will be helpful for understanding the relationship between binding mode and bioactivity and for designing better inhibitors from UA analogues. PMID:26406581

  5. Standardization of Unani Antidiabetic Tablet - Qurse Tabasheer

    PubMed Central

    Ali, Waris; Shaikh, Hamiduddin; Ansari, Abdullah; Khanam, Salma

    2016-01-01

    established for poly herbal formulation QT, which may be used as reference for preparation and standardization of QT. SUMMARY In this work Standardization of anti-diabetic tablet Qurse Tabasheer with diverse ingredients including herbal and mineral origin drugs has been attempted with identification of its ingredients, formulation, physicochemical evaluation and HPTLC finger printing, which may help in preparing consistent and better efficacious formulations. Abbreviations Used: QT: Qurse Tabasheer TLC: thin layer chromatography HPTLC: high-performance thin layer chromatography WHO: World health organization FRLHT: Foundation for Revitalization of Local Health Traditions Fe2O3: Iron oxide Sio2: Silica CaCo3: Calcium carbonate, Tio2: Titanium Oxide NIUM: National Institute of Unani Medicine #: Mesh size LOD: Loss of weight on drying USP: United state Pharmacopeia UV: Ultra Violet λ: Lambda θ: theta CFU: Colony-forming unit PMID:27034607

  6. The isolation, Characterization and Preclinical Studies of Metal Complex of Thespesia populnea for the Potential Peroxisome Proliferator-activated Receptors-γ Agonist Activity

    PubMed Central

    Phanse, Mohini Ashok; Patil, Manohar Janardhan; Abbulu, Konde

    2015-01-01

    Background: Diabetes mellitus is an international public health problem since ancient days. The condition is predominantly more severe in developing countries like India where, life is more sedentary due to the even changing lifestyles in this fast-paced global scenario. Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes mellitus in India for years. The aim of this work is to explore the anti-diabetic activity of the isolated compound. Materials and Methods: The sesquiterpene isolated from hexane fraction of bark of T. populnea modified synthetically then identified by using analytical techniques such as electron paramagnetic resonance spectra for confirmation and the anti-diabetic activity was evaluated by anti-hyperglycemic, hypoglycemic potential. Result: In the present work, we have studied the anti-hyperglycemic and hypoglycemic activity of the vanadium complex in glucose loaded and normal animals were shown significantly decreased in plasma blood glucose level. The results derived from preclinical studies confirm the potential of new sesquiterpene. Conclusion: The findings could provide evidence regarding the anti-diabetic potential of T. populnea by lowering blood glucose level. SUMMARY Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes in India. Present study aimed to explore the anti diabetic potential of isolated compound. Isolation of sesquiterpene from hexane fraction of bark of Thespesia populnea and modified synthetically then authenticated by using analytical techniques such as electron paramagnetic resonance spectra for confirmation. The modified complex was further assessed for its anti diabetic property in glucose loaded rats. Vanadium complex demonstrated significant reduction in plasma blood glucose level in glucose loaded animals. The results derived from preclinical studies confirm the potential of new sesquiterpene. The present findings conclude that

  7. Evaluation of Antioxidant, Antidiabetic and Anticholinesterase Activities of Smallanthus sonchifolius Landraces and Correlation with Their Phytochemical Profiles.

    PubMed

    Russo, Daniela; Valentão, Patrícia; Andrade, Paula B; Fernandez, Eloy C; Milella, Luigi

    2015-01-01

    The present study aimed to investigate the phytochemical profile of leaf methanol extracts of fourteen Smallanthus sonchifolius (yacon) landraces and their antioxidant, anticholinesterase and antidiabetic activities that could lead to the finding of more effective agents for the treatment and management of Alzheimer's disease and diabetes. For this purpose, antioxidant activity was assessed using different tests: ferric reducing ability power (FRAP), 2,2-diphenyl-1-picryl hydrazyl (DPPH), nitric oxide (˙NO) and superoxide (O2˙-) scavenging and lipid peroxidation inhibition assays. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, whereas antidiabetic activity was investigated by α-amylase and α-glucosidase inhibition tests. To understand the contribution of metabolites, phytochemical screening was also performed by high performance liquid chromatography-diode array detector (HPLC-DAD) system. Among all, methanol extract of PER09, PER04 and ECU44 landraces exhibited the highest relative antioxidant capacity index (RACI). ECU44 was found to be rich in 4,5-di-O-caffeoylquinic acid (CQA) and 3,5-di-O-CQA and displayed a good α-amylase and α-glucosidase inhibition, showing the lowest IC50 values. Flavonoids, instead, seem to be involved in the AChE and BChE inhibition. The results of this study revealed that the bioactive compound content differences could be determinant for the medicinal properties of this plant especially for antioxidant and antidiabetic activities. PMID:26263984

  8. Evaluation of Antioxidant, Antidiabetic and Anticholinesterase Activities of Smallanthus sonchifolius Landraces and Correlation with Their Phytochemical Profiles

    PubMed Central

    Russo, Daniela; Valentão, Patrícia; Andrade, Paula B.; Fernandez, Eloy C.; Milella, Luigi

    2015-01-01

    The present study aimed to investigate the phytochemical profile of leaf methanol extracts of fourteen Smallanthus sonchifolius (yacon) landraces and their antioxidant, anticholinesterase and antidiabetic activities that could lead to the finding of more effective agents for the treatment and management of Alzheimer’s disease and diabetes. For this purpose, antioxidant activity was assessed using different tests: ferric reducing ability power (FRAP), 2,2-diphenyl-1-picryl hydrazyl (DPPH), nitric oxide (˙NO) and superoxide (O2˙−) scavenging and lipid peroxidation inhibition assays. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, whereas antidiabetic activity was investigated by α-amylase and α-glucosidase inhibition tests. To understand the contribution of metabolites, phytochemical screening was also performed by high performance liquid chromatography-diode array detector (HPLC-DAD) system. Among all, methanol extract of PER09, PER04 and ECU44 landraces exhibited the highest relative antioxidant capacity index (RACI). ECU44 was found to be rich in 4,5-di-O-caffeoylquinic acid (CQA) and 3,5-di-O-CQA and displayed a good α-amylase and α-glucosidase inhibition, showing the lowest IC50 values. Flavonoids, instead, seem to be involved in the AChE and BChE inhibition. The results of this study revealed that the bioactive compound content differences could be determinant for the medicinal properties of this plant especially for antioxidant and antidiabetic activities. PMID:26263984

  9. Isolation of nematicidal compounds from Tagetes patula L. yellow flowers: structure-activity relationship studies against cyst nematode Heterodera zeae infective stage larvae.

    PubMed

    Faizi, Shaheen; Fayyaz, Shahina; Bano, Samina; Iqbal, Erum Yawar; Lubna; Siddiqi, Humaira; Naz, Aneela

    2011-09-14

    Bioassay-guided isolation studies on the extracts of yellow flowers of Tagetes patula L. against the Heterodera zeae were carried out to identify phytochemicals lethal to this economically important cyst nematode. In vitro investigation of a polar extract and fractions showing activity led to the isolation of phenolic compounds (flavonoids and phenolic acids). In the nonpolar extract, a few fatty acids, their methyl esters, and thiophenes (including α-terthienyl) were detected. In studies of compounds obtained commercially, α-terthienyl and gallic and linoleic acids showed 100% mortality at concentrations of 0.125% after 24 h. Assessment of structure-activity relationships revealed that an increase in the number of hydroxyl groups in phenolic acids increased the activity; with fatty acids, activity depended on chain length and the number and position of double bonds. Crude extracts of the flowers of different colors also have promising activity. PMID:21780738

  10. Recent advances in structure and reactivity of dissolved organic matter: radiation chemistry of non-isolated natural organic matter and selected model compounds.

    PubMed

    Ayatollahi, Shakiba; Kalnina, Daina; Song, Weihua; Cottrell, Barbara A; Gonsior, Michael; Cooper, William J

    2012-01-01

    The importance of natural organic matter (NOM) as a source of carbon in natural waters, as the source of reactive oxygen species, or for the complications its presence causes in treatment of natural waters, is undeniable. Recent studies have also pointed to the major photochemical role of triplet excited state of natural organic matter in the environmental fate of pharmaceutical and personal care products (PPCPs) in waters. However, the characterization of NOM is problematic due to its complex molecular structure. One approach to better understand NOM chemistry is the use of model compounds. As the condensation of a plant's phenolic compounds leads to humification and the formation of NOM, a structurally broad group of nine phenolic compounds were selected as model compounds for this study. With methods used in the discipline of radiation chemistry, the oxidative chemistry and transient spectra of these phenols were studied. In addition, the oxidative chemistry and transient spectra of a sample of NOM from the Black River, North Carolina, USA, was characterized. This natural water sample was used as received and represents the first studies of non-isolated NOM by pulsed radiolysis. The results of the transient spectra of the NOM revealed that the radical intermediates were very long lived. This phenomenon was not captured using the nine model compounds suggesting that more complex compounds are needed to further our understanding of the oxidation chemistry of NOM.

  11. Thailandins A and B, New Polyene Macrolactone Compounds Isolated from Actinokineospora bangkokensis Strain 44EHW(T), Possessing Antifungal Activity against Anthracnose Fungi and Pathogenic Yeasts.

    PubMed

    Intra, Bungonsiri; Greule, Anja; Bechthold, Andreas; Euanorasetr, Jirayut; Paululat, Thomas; Panbangred, Watanalai

    2016-06-29

    Two new polyene macrolactone antibiotics, thailandins A, 1, and B, 2, were isolated from the fermentation broth of rhizosphere soil-associated Actinokineospora bangkokensis strain 44EHW(T). The new compounds from this strain were purified using semipreparative HPLC and Sephadex LH-20 gel filtration while following an antifungal activity guided fractionation. Their structures were elucidated through spectroscopic techniques including UV, HR-ESI-MS, and NMR. These compounds demonstrated broad spectrum antifungal activity against fungi causing anthracnose disease (Colletotrichum gloeosporioides DoA d0762, Colletotrichum gloeosporiodes DoA c1060, and Colletotrichum capsici DoA c1511) as well as pathogenic yeasts (Candida albicans MT 2013/1, Candida parasilopsis DKMU 434, and Cryptococcus neoformans MT 2013/2) with minimum inhibitory concentrations ranging between 16 and 32 μg/mL. This is the first report of polyene antibiotics produced by Actinokineospora species as bioactive compounds against anthracnose fungi and pathogenic yeast strains. PMID:27267862

  12. Isolation, Chemical Fingerprinting and Simultaneous Quantification of Four Compounds from Tanacetum gracile Using a Validated HPLC-ESI-QTOF-Mass Spectrometry Method.

    PubMed

    Sharma, Neha; Kumar, Chetan; Dutt, Prabhu; Gupta, Suphla; Satti, Naresh K; Chandra, Suresh; Kitchlu, Surinder; Paul, Satya; Vishwakarma, Ram A; Verma, Mahendra K

    2016-01-01

    The present study was conducted to carry out the phytochemical investigation of Tanacetum gracile Hook. f. & Thomson and to develop a method for the simultaneous quantification of the isolated compounds in the extracts ofT. gracile growing in different locations. Cluster analysis rectangular similarity matrix was performed to understand the chemical fingerprinting variations in the extracts. High-performance liquid chromatography-electrospray ionization-quadrupole-time-of-flight-mass spectrometry (HPLC-ESI-QTOF-MS) was used to quantify four bioactive compounds, and separation of the compounds was achieved on a reverse-phase C8 column using a mobile phase of acetonitrile: 0.1% formic acid in water with a gradient elution by maintaining the flow rate of 300 μL/min. The QTOF-MS was operated using the electro-spray ionization technique with the positive ion polarity mode. The calibration curves of four marker compounds were linear over the concentration range of 3.12-100 ng/µL (R(2)> 0.996). A specific, accurate and precise HPLC-ESI-QTOF-MS method was optimized for the determination of kaempferol, ketoplenolide, tetramethoxyflavone and artemetin both individually and simultaneously. Quantification of these chemical markers in different extracts was carried out using this validated method. Kaempferol was isolated for the first time from T. gracile. PMID:26951542

  13. Decomposition of plant-sourced carbon compounds by heterotrophic betaproteobacteria isolated from a tropical Costa Rican bromeliad.

    PubMed

    Klann, Jane; McHenry, Alexandra; Montelongo, Carin; Goffredi, Shana K

    2016-06-01

    Betaproteobacteria were the most common isolates from the water-filled tank of a Costa Rican bromeliad. Isolates included eight species from the orders Neisseriales and Burkholderiales, with close relatives recovered previously from tropical soils, wetlands, freshwater, or in association with plants. Compared to close relatives, the isolates displayed high temperature and comparatively low pH optima, reflecting the tropical, acidic nature of the bromeliad tank. Bromeliad-associated bacteria most closely related to Chromobacterium, Herbaspirillum, and Aquitalea were all isolated exclusively at pH 6, while Ralstonia, Cupriavidus, and three species of Burkholderia were isolated mostly at pH 4. Activity profiles for the isolates suggest pervasive capabilities for the breakdown of plant-sourced organics, including d-galacturonic acid, mannitol, d-xylose, and l-phenylalanine, also reflecting a niche dominated by decomposition of leaves from the overlying canopy, which become entrained in the tanks. Metabolic activity profiles were overlapping between the Burkholderiales, isolated at pH 4, and the Neisseriales, isolated at pH 6, suggesting that plant material decomposition, which is presumably the underlying process sustaining the tank community and possibly the plant itself, occurs in the tanks at both pH extremes. These results suggest that bromeliad-associated betaproteobacteria may play an important role in the cycling of carbon in this unusual aquatic habitat. PMID:26918550

  14. Variable emissions of microbial volatile organic compounds (MVOCs) from root-associated fungi isolated from Scots pine

    NASA Astrophysics Data System (ADS)

    Bäck, Jaana; Aaltonen, Hermanni; Hellén, Heidi; Kajos, Maija K.; Patokoski, Johanna; Taipale, Risto; Pumpanen, Jukka; Heinonsalo, Jussi

    2010-09-01

    Soils emit a large variety of volatile organic compounds. In natural ecosystems, measurements of microbial volatile organic compound (MVOC) exchange rates between soil and atmosphere are difficult due to e.g. the spatial heterogeneity of the belowground organisms, and due to the many potential sources for the same compounds. We measured in laboratory conditions the MVOC emission rates and spectra of eight typical fungi occurring in boreal forest soils. The studied species are decomposers ( Gymnopilus penetrans, Ophiostoma abietinum), ectomycorrhizal ( Cenococcum geophilum, Piloderma olivaceum, Suillus variegatus, Tomentellopsis submollis) and endophytic fungi ( Meliniomyces variabilis, Phialocephala fortinii). The MVOC emissions contained altogether 21 known and 6 unidentified compounds whose emission rates were >0.1 μg g(DW) -1 h -1. The most abundant compounds were the short-chain carbonyl compounds (acetone and acetaldehyde). The greatest carbonyl emissions were measured from P. olivaceum (1.9 mg acetone g(DW) -1 h -1) and P. fortinii (0.114 mg acetaldehyde g(DW) -1 h -1). Terpenoid emissions (isoprene, mono- and sesquiterpenes) were detected from some fungal cultures, but in relatively small amounts. We conclude that soil micro-organisms can potentially be responsible for significant emissions of volatiles, especially short-chain oxygenated compounds, to the below-canopy atmosphere.

  15. Isolation and identification of an anti-bolting compound, hexadecatrienoic acid monoglyceride, responsible for inhibition of bolting and maintenance of the leaf rosette in radish plants.

    PubMed

    Yoshida, Yuko; Takada, Noboru; Koda, Yasunori

    2010-08-01

    Generally, the bolting (stem elongation from rosette plants) of winter annuals is believed to be induced by an increase in the levels of gibberellin that occurs after a certain period of chilling (vernalization), and a deficiency of gibberellin allows the plant to maintain a rosette style. Lack of direct evidence proving the above assumption in radish plants (Raphanus sativus L.) encouraged us to assume the presence of an anti-bolting compound actively maintaining the rosette habit through inhibition of bolting. Anti-bolting activity was detected in an extract of rosette shoots of radish plants by an assay using seedlings cultured in vitro. The causal compound that strongly inhibited bolting was isolated and identified as alpha-(7Z,10Z,13Z)-hexadecatrienoic acid monoglyceride (16:3 monoglyceride). This compound did not inhibit leaf production at the apical meristem, indicating that it merely inhibits growth at the internode. The compound disappeared completely after vernalization, and bolting occurred thereafter. The results suggest that the release from inhibition by 16:3 monoglyceride induces the initiation of bolting. The possible mechanism by which the compound exerts the activity is discussed. PMID:20601431

  16. Continuous-Flow Synthesis of Deuterium-Labeled Antidiabetic Chalcones: Studies towards the Selective Deuteration of the Alkynone Core.

    PubMed

    Ötvös, Sándor B; Hsieh, Chi-Ting; Wu, Yang-Chang; Li, Jih-Heng; Chang, Fang-Rong; Fülöp, Ferenc

    2016-01-01

    Flow chemistry-based syntheses of deuterium-labeled analogs of important antidiabetic chalcones were achieved via highly controlled partial C≡C bond deuteration of the corresponding 1,3-diphenylalkynones. The benefits of a scalable continuous process in combination with on-demand electrolytic D2 gas generation were exploited to suppress undesired over-reactions and to maximize reaction rates simultaneously. The novel deuterium-containing chalcone derivatives may have interesting biological effects and improved metabolic properties as compared with the parent compounds. PMID:26959006

  17. Preparative isolation and purification of flavone compounds from sophora japonica L. by high-speed counter-current chromatography combined with macroporous resin column separation.

    PubMed

    Sun, Ailing; Sun, Qinghua; Liu, Renmin

    2007-05-01

    High-speed counter-current chromatography combined with macroporous resin column separation was applied to the isolation and purification of genistein-7,4'-di-O-beta-D-glucoside (I), genistein-7-O-beta-D-glucopyranoside-4'-O-[(alpha-L-rhamnopyransoyl)-(1-2)-beta-D-glucopyranoside] (II), kaempferol-3-O-beta-D-sophoroside(III), quercetin-3-O-beta-L-ramnopyranosyl-(1 - 6)-beta-D-glucopyranoside (IV), genistein-4'-beta-L-rhamnopyransoyl-(1 - 2)-alpha-D-glucopyranoside (V), and kaempferol-3-O-beta-L-ramnopyranosyl-(1 - 6)-beta-D-glucopyranoside (VI) from the Chinese medicinal herb Sophora japonica L. The crude extracts from the pericarps of Sophora japonica L. were pre-separated on a D-101 macroporous resin column and divided into two parts as sample 1 and sample 2. An 80-mg portion of sample 1 was separated by using n-butanol-acetic acid (1%) (5:5, v/v) as the two-phase solvent system and yielded 30.1 mg of compound I, 23.3 mg of compound II. A 120 mg portion of sample 2 was separated by using ethyl acetate-n-butanol-acetic acid (1%) (5:0.8:5, v/v) as the two-phase solvent system and yielded 5.5 mg of compound III, 31.7 mg of compound IV, 37.4 mg of compound V, and 6.2 mg of compound VI. The purities of compounds I, II, III, IV, V, and VI were 98.7, 98.2, 97.8, 98.5, 99.3, and 98.9%, respectively, as determined by HPLC. The chemical structures of these components were identified by 1H-NMR and 13C-NMR. PMID:17566335

  18. Antioxidant, α-glucosidase and xanthine oxidase inhibitory activity of bioactive compounds from maize (Zea mays L.).

    PubMed

    Nile, Shivraj H; Park, Se W

    2014-01-01

    Chemical investigations into maize (Zea mays L.) kernels yielded phenolic compounds, which were structurally established using chromatographic and spectroscopic methods. The isolated phenolic compounds from maize kernel were examined in vitro for their antioxidant abilities by DPPH (2,2-diphenyl-1-picryl hydrazine) radical, OH radical scavenging activity, and reducing ability, along with α-glucosidase and xanthine oxidase (XO) inhibition. The isolated maize phenolics revealed significant xanthine oxidase and α-glucosidase inhibitory activity to that of allopurinol and acarbose in vitro and in vivo, respectively. The kinetics study with xanthine oxidase revealed competitive type of inhibition by isolated maize vanillic acid (M2), ferulic acid (M5), 3'-methoxyhirsutrin (M7), and peonidin-3-glucoside (M10) as compared to control allopurinol. Overall, with few exceptions, all the phenolic compounds from maize kernel revealed significant biological activities with all parameters examined. Also, the phenolic compounds from maize were found to be more reactive toward DPPH radical and had considerable reducing ability and OH radical scavenging activity. These findings suggest that maize kernel phenolic compounds can be considered as potential antioxidant, α-glucosidase, and XO inhibitory agents those might be further explored for the design of lead antioxidant, antidiabetic and antigout drug candidates using in vivo trials. PMID:23957301

  19. Antidiabetic and Antilipidemic Effect of Musa balbisiana Root Extract: A Potent Agent for Glucose Homeostasis in Streptozotocin-Induced Diabetic Rat.

    PubMed

    Kalita, Himadri; Boruah, Dulal C; Deori, Meetali; Hazarika, Ankita; Sarma, Rahul; Kumari, Sima; Kandimalla, Raghuram; Kotoky, Jibon; Devi, Rajlakshmi

    2016-01-01

    Folklore studies have revealed that Musa balbisiana Colla (MB; Family: Musaceae) has high medicinal properties. The purpose of the present study is to evaluate antihyperglycemic, and antioxidant activity of MB extracts in streptozotocin (STZ) induced diabetic rats. In vitro antioxidant and antidiabetic activity of MB extracts, i.e., root extract (RE), shoot extract and inflorescence extract were determined by using various methods viz 1,-1-diphenyl-2-picrylhydrazyl (DPPH) and a method to assess their possible effect on glucose diffusion across gastrointestinal tract and identify bioactive compound of potent extract. In vivo antilipidemic and antidiabetic activity was evaluated by administrating oral dose of RE for 15 days on STZ- induced diabetic rat. RE showed highest antioxidant activity by scavenging DPPH radical (IC50 32.96 μg/ml) and inhibit 30% glucose movement in vitro. The methanol extract of root showed the presence of calyx [4] arene category of the compound. Furthermore, RE treated rat revealed a reduction in fasting blood glucose (62.5%), serum total cholesterol (36.2%), triglyceride (54.5%), and low-density lipoprotein (50.94%) after 15 days as compared to STZ treated animal. There was an initiation of regenerative structures of the affected organs after 15 days of RE treatment. Histopathological observations clearly differentiate the structural changes in pancreas, liver, and kidney of STZ and RE treated group. The presence of calyx [4] arene class of compound may be responsible for its antioxidant and antidiabetic properties by absorbing glucose in vivo. PMID:27199747

  20. Antidiabetic and Antilipidemic Effect of Musa balbisiana Root Extract: A Potent Agent for Glucose Homeostasis in Streptozotocin-Induced Diabetic Rat

    PubMed Central

    Kalita, Himadri; Boruah, Dulal C.; Deori, Meetali; Hazarika, Ankita; Sarma, Rahul; Kumari, Sima; Kandimalla, Raghuram; Kotoky, Jibon; Devi, Rajlakshmi

    2016-01-01

    Folklore studies have revealed that Musa balbisiana Colla (MB; Family: Musaceae) has high medicinal properties. The purpose of the present study is to evaluate antihyperglycemic, and antioxidant activity of MB extracts in streptozotocin (STZ) induced diabetic rats. In vitro antioxidant and antidiabetic activity of MB extracts, i.e., root extract (RE), shoot extract and inflorescence extract were determined by using various methods viz 1,-1-diphenyl-2-picrylhydrazyl (DPPH) and a method to assess their possible effect on glucose diffusion across gastrointestinal tract and identify bioactive compound of potent extract. In vivo antilipidemic and antidiabetic activity was evaluated by administrating oral dose of RE for 15 days on STZ- induced diabetic rat. RE showed highest antioxidant activity by scavenging DPPH radical (IC50 32.96 μg/ml) and inhibit 30% glucose movement in vitro. The methanol extract of root showed the presence of calyx [4] arene category of the compound. Furthermore, RE treated rat revealed a reduction in fasting blood glucose (62.5%), serum total cholesterol (36.2%), triglyceride (54.5%), and low-density lipoprotein (50.94%) after 15 days as compared to STZ treated animal. There was an initiation of regenerative structures of the affected organs after 15 days of RE treatment. Histopathological observations clearly differentiate the structural changes in pancreas, liver, and kidney of STZ and RE treated group. The presence of calyx [4] arene class of compound may be responsible for its antioxidant and antidiabetic properties by absorbing glucose in vivo. PMID:27199747

  1. Antioxidant and antidiabetic activities of extracts from Cirsium japonicum roots

    PubMed Central

    Yin, Jie; Heo, Seong-Il

    2008-01-01

    This study investigated the antioxidant activity of methanol (MeOH) and water extracts from roots of Cirsium japonicum in vitro. MeOH extract showed a stronger free radical scavenging activity than water extract. However, both of extracts showed a concentration dependent hydroxyl radical scavenging activity, reducing power and metal chelating ability. MeOH extract had greater phenolic and flavonoid contents than water extract. The antidiabetic activity of these two extracts was evaluated by the α-glucosidase inhibition assay. The water extract showed a considerable α-glucosidase inhibitory activity. To our knowledge, this may be the first time to report the antioxidant and antidiabetic activities in Cirsium japonicum roots. PMID:20016726

  2. Antidiabetic Effects of Simple Phenolic Acids: A Comprehensive Review.

    PubMed

    Vinayagam, Ramachandran; Jayachandran, Muthukumaran; Xu, Baojun

    2016-02-01

    Diabetes mellitus (DM) has become a major public health threat across the globe. Current antidiabetic therapies are based on synthetic drugs that very often have side effects. It has been widely acknowledged that diet plays an important role in the management of diabetes. Phenolic acids are widely found in daily foods such as fruits, vegetables, cereals, legumes, and wine and they provide biological, medicinal, and health properties. Simple phenolic acids have been shown to increase glucose uptake and glycogen synthesis, improve glucose and lipid profiles of certain diseases (obesity, cardiovascular diseases, DM, and its complication). The current review is an attempt to list out the antidiabetic effects of simple phenolic acids from medicinal plants and botanical foods. PMID:26634804

  3. Isolation and purification of flavonoid and isoflavonoid compounds from the pericarp of Sophora japonica L. by adsorption chromatography on 12% cross-linked agarose gel media.

    PubMed

    Qi, Yuanying; Sun, Ailing; Liu, Renmin; Meng, Zhaoling; Xie, Hongyan

    2007-01-26

    A method for isolation and purification of flavonoid and isoflavonoid compounds in extracts of the pericarp of Sophora japonica L. was established by adsorption chromatography on the 12% cross-linked agarose gel Superose 12. The crude extracts were pre-separated to two parts, sample A and sample B, on a D-101 macroporous resin column by elution with 20% ethanol and 40% ethanol, respectively. Samples A and B were then separated by adsorption chromatography on Superose 12 with 40% methanol as the mobile phase. Eight compounds including four kinds of flavonoids and four kinds of isoflavonoids were obtained by the proposed method. The adsorption mechanisms of flavonoids and isoflavonoids on Superose 12 were also discussed. PMID:17174318

  4. Oblongifolin M, an active compound isolated from a Chinese medical herb Garcinia oblongifolia, potently inhibits enterovirus 71 reproduction through downregulation of ERp57

    PubMed Central

    Wang, Hua; He, Yaqing; Chen, Ying; Zhang, Hong; Wu, Rong; Chen, Xinchun; Zhou, Boping; He, Jason; Kung, Hsiang-Fu; Huang, Canhua; Wei, Yuquan; Huang, Jian-dong; Xu, Hongxi; He, Ming-Liang

    2016-01-01

    There is no effective drug to treat EV71 infection yet. Traditional Chinese herbs are great resources for novel antiviral compounds. Here we showed that Oblongifolin M (OM), an active compound isolated from Garcinia oblongifolia, potently inhibited EV71 infection in a dose dependent manner. To identify its potential effectors in the host cells, we successfully identified 18 proteins from 52 differentially expressed spots by comparative proteomics studies. Further studies showed that knockdown of ERp57 inhibited viral replication through downregulating viral IRES (internal ribosome entry site) activities, whereas ectopic expression of ERp57 increased IRES activity and partly rescued the inhibitory effects of OM on viral replication. We demonstrated that OM is an effective antiviral agent; and that ERp57 is one of its cellular effectors against EV71 infection. PMID:26848777

  5. Isolation and identification of unique marker compounds from the Tasmanian poppy Papaver somniferum N. Implications for the identification of illicit heroin of Tasmanian origin.

    PubMed

    Odell, Luke R; Skopec, Jana; McCluskey, Adam

    2008-03-01

    Tasmanian opium accounts for 25% of the world's legal supply of opium straw, and in 1998-99 sufficient numbers of flower pods (66,013) to manufacture ca 500 kg of heroin were stolen. Whilst the heroin signature program has been developed to determine the origin of heroin from other key producers, no such signature currently exists for Tasmanian derived heroin. Tasmanian poppies contain a unique alkaloid, oripavine, which is the source of 'marker' impurities in illicit heroin produced from Tasmanian poppy straw. Treatment of oripavine (500mg) under Thiboumery and Mohr heroin processing conditions, followed by simple evaporative workup afforded 613 mg of a dark orange residue, which upon extensive chromatographic purification yielded oripavine 3-acetate (2) 22 mg; 3-acetyl-N-acetyldesthebaine (3) 35 mg; 3-acetyl-6-methoxy-4,5-epoxyphenanthrene (4) 5.8 mg; 3,4-diacetyl-6-methoxyphenanthrene (5) 27 mg; and 3,4,6-methoxy-5-[2(N-methylacetamido)]ethylphenanthrene (6) 52 mg. Compounds (2-6) are derived from oripavine and are unique to heroin derived from the Tasmanian poppy Papaver somniferum N. Analysis of illicit heroin samples seized from Turkey, Pakistan, Columbia and Myanmar did not reveal any of the aforementioned marker compounds. We have, however, identified four of these marker compounds (3-6) in seized heroin samples from Australia suggesting that they are of Tasmanian origin. Complete details of the isolation and identification of these compounds are provided.

  6. In vitro Cytotoxicity and Anti-herpes Simplex Virus Type 1 Activity of Hydroethanolic Extract, Fractions, and Isolated Compounds from Stem Bark of Schinus terebinthifolius Raddi

    PubMed Central

    Nocchi, Samara Requena; de Moura-Costa, Gislaine Franco; Novello, Claudio Roberto; Rodrigues, Juliana; Longhini, Renata; de Mello, João Carlos Palazzo; Filho, Benedito Prado Dias; Nakamura, Celso Vataru; Ueda-Nakamura, Tânia

    2016-01-01

    Background: Herpes simplex virus type 1 (HSV-1) is associated with orofacial infections and is transmitted by direct contact with infected secretions. Several efforts have been expended in the search for drugs to the treatment for herpes. Schinus terebinthifolius is used in several illnesses and among them, for the topical treatment of skin wounds, especially wounds of mucous membranes, whether infected or not. Objective: To evaluate the cytotoxicity and anti-HSV-1 activity of the crude hydroethanolic extract (CHE) from the stem bark of S. terebinthifolius, as well as its fractions and isolated compounds. Materials and Methods: The CHE was subjected to bioguided fractionation. The anti-HSV-1 activity and the cytotoxicity of the CHE, its fractions, and isolated compounds were evaluated in vitro by SRB method. A preliminar investigation of the action of CHE in the virus–host interaction was conducted by the same assay. Results: CHE presented flavan-3-ols and showed anti-HSV-1 activity, better than its fractions and isolated compounds. The class of substances found in CHE can bind to proteins to form unstable complexes and enveloped viruses, as HSV-1 may be vulnerable to this action. Our results suggest that the CHE interfered with virion envelope structures, masking viral receptors that are necessary for adsorption or entry into host cells. Conclusion: The plant investigated exhibited potential for future development treatment against HSV-1, but further tests are necessary, especially to elucidate the mechanism of action of CHE, as well as preclinical and clinical studies to confirm its safety and efficacy. SUMMARY Crude hydroethanolic extract (CHE) presents promising activity against herpes simplex virus type 1 (HSV 1), with selectivity index (SI) = 22.50CHE has flavan-3-ols in its composition, such as catechin and gallocatechinThe fractions and isolated compounds obtained from CHE by bioguided fractionation are less active than the CHE against HSV-1CHE interferes

  7. Isolation and Characterization of Bacteria That Grow on Methane and Organic Compounds as Sole Sources of Carbon and Energy

    PubMed Central

    Patt, Tom E.; Cole, Gloria C.; Bland, Judith; Hanson, R. S.

    1974-01-01

    Bacteria capable of growth on methane and a variety of complex organic substrates as sole sources of carbon and energy have been isolated. Conditions used to rigorously establish the purity of the cultures are described. One facultative methylotroph has been studied in detail. This organism has peripherally arranged pairs of intracytoplasmic membranes characteristic of obligate methylotrophs. This isolate apparently utilizes the serine pathway of formaldehyde fixation. The location of methane oxidizers in a dimictic lake indicates that these organisms prefer less than saturating levels of dissolved oxygen. Laboratory experiments confirmed the preference of these organisms for atmospheres containing less oxygen than air. Images PMID:4142033

  8. Citrus fruit flavor and aroma biosynthesis: isolation, functional characterization, and developmental regulation of Cstps1, a key gene in the production of the sesquiterpene aroma compound valencene.

    PubMed

    Sharon-Asa, Liat; Shalit, Moshe; Frydman, Ahuva; Bar, Einat; Holland, Doron; Or, Etti; Lavi, Uri; Lewinsohn, Efraim; Eyal, Yoram

    2003-12-01

    Citrus fruits possess unique aromas rarely found in other fruit species. While fruit flavor is composed of complex combinations of soluble and volatile compounds, several low-abundance sesquiterpenes, such as valencene, nootkatone, alpha-sinensal, and beta-sinensal, stand out in citrus as important flavor and aroma compounds. The profile of terpenoid volatiles in various citrus species and their importance as aroma compounds have been studied in detail, but much is still lacking in our understanding of the physiological, biochemical, and genetic regulation of their production. Here, we report on the isolation, functional expression, and developmental regulation of Cstps1, a sesquiterpene synthase-encoding gene, involved in citrus aroma formation. The recombinant enzyme encoded by Cstps1 was shown to convert farnesyl diphosphate to a single sesquiterpene product identified as valencene by gas chromatography-mass spectrometry (GC-MS). Phylogenetic analysis of plant terpene synthase genes localized Cstps1 to the group of angiosperm sesquiterpene synthases. Within this group, Cstps1 belongs to a subgroup of citrus sesquiterpene synthases. Cstps1 was found to be developmentally regulated: transcript was found to accumulate only towards fruit maturation, corresponding well with the timing of valencene accumulation in fruit. Although citrus fruits are non-climacteric, valencene accumulation and Cstps1 expression were found to be responsive to ethylene, providing further evidence for the role of ethylene in the final stages of citrus fruit ripening. Isolation of the gene encoding valencene synthase provides a tool for an in-depth study of the regulation of aroma compound biosynthesis in citrus and for metabolic engineering for fruit flavor characteristics. PMID:14617067

  9. Phytotoxic Potential of Secondary Metabolites and Semisynthetic Compounds from Endophytic Fungus Xylaria feejeensis Strain SM3e-1b Isolated from Sapium macrocarpum.

    PubMed

    García-Méndez, Marbella Claudia; Macías-Ruvalcaba, Norma A; Lappe-Oliveras, Patricia; Hernández-Ortega, Simón; Macías-Rubalcava, Martha Lydia

    2016-06-01

    Bioactivity-directed fractionation of the combined culture medium and mycelium extract of the endophytic fungus Xylaria feejeensis strain SM3e-1b, isolated from Sapium macrocarpum, led to the isolation of three known natural products: (4S,5S,6S)-4-hydroxy-3-methoxy-5-methyl-5,6-epoxycyclohex-2-enone or coriloxine, 1; 2-hydroxy-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione, 2; and 2,6-dihydroxy-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione or fumiquinone B, 3. This is the first report of compound 3 being isolated from this species. Additionally, four new derivatives of coriloxine were prepared: (4R,5S,6R)-6-chloro-4,5-dihydroxy-3-methoxy-5-methylcyclohex-2-enone, 4; 6-hydroxy-5-methyl-3-(methylamino)cyclohexa-2,5- diene-1,4-dione, 5; (4R,5R,6R)-4,5-dihydroxy-3-methoxy-5-methyl-6-(phenylamino)cyclohex-2-enone, 6; and 2-((4-butylphenyl)amino)-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione, 7. X-ray analysis allowed us to unambiguously determine the structures and absolute configuration of semisynthetic derivatives 4, 5, and 6. The phytotoxic activity of the three isolated natural products and the coriloxine derivatives is reported. Germination of the seed, root growth, and oxygen uptake of the seedlings of Trifolium pratense, Medicago sativa, Panicum miliaceum, and Amaranthus hypochondriacus were significantly inhibited by all of the tested compounds. In general, they were more effective inhibiting root elongation than suppressing the germination and seedling oxygen uptake processes as shown by their IC50 values.

  10. Phytotoxic Potential of Secondary Metabolites and Semisynthetic Compounds from Endophytic Fungus Xylaria feejeensis Strain SM3e-1b Isolated from Sapium macrocarpum.

    PubMed

    García-Méndez, Marbella Claudia; Macías-Ruvalcaba, Norma A; Lappe-Oliveras, Patricia; Hernández-Ortega, Simón; Macías-Rubalcava, Martha Lydia

    2016-06-01

    Bioactivity-directed fractionation of the combined culture medium and mycelium extract of the endophytic fungus Xylaria feejeensis strain SM3e-1b, isolated from Sapium macrocarpum, led to the isolation of three known natural products: (4S,5S,6S)-4-hydroxy-3-methoxy-5-methyl-5,6-epoxycyclohex-2-enone or coriloxine, 1; 2-hydroxy-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione, 2; and 2,6-dihydroxy-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione or fumiquinone B, 3. This is the first report of compound 3 being isolated from this species. Additionally, four new derivatives of coriloxine were prepared: (4R,5S,6R)-6-chloro-4,5-dihydroxy-3-methoxy-5-methylcyclohex-2-enone, 4; 6-hydroxy-5-methyl-3-(methylamino)cyclohexa-2,5- diene-1,4-dione, 5; (4R,5R,6R)-4,5-dihydroxy-3-methoxy-5-methyl-6-(phenylamino)cyclohex-2-enone, 6; and 2-((4-butylphenyl)amino)-5-methoxy-3-methylcyclohexa-2,5-diene-1,4-dione, 7. X-ray analysis allowed us to unambiguously determine the structures and absolute configuration of semisynthetic derivatives 4, 5, and 6. The phytotoxic activity of the three isolated natural products and the coriloxine derivatives is reported. Germination of the seed, root growth, and oxygen uptake of the seedlings of Trifolium pratense, Medicago sativa, Panicum miliaceum, and Amaranthus hypochondriacus were significantly inhibited by all of the tested compounds. In general, they were more effective inhibiting root elongation than suppressing the germination and seedling oxygen uptake processes as shown by their IC50 values. PMID:27159617

  11. Antidiabetic Effect of Sida cordata in Alloxan Induced Diabetic Rats

    PubMed Central

    Shah, Naseer Ali; Khan, Muhammad Rashid

    2014-01-01

    Medicinal plants are efficient ameliorator of oxidative stress associated with diabetes mellitus. In this study, ethyl acetate fraction (SCEE) of Sida cordata was investigated for scientific validation of its folk use in diabetes. Antidiabetic effect of SCEE was confirmed by antihyperglycemic activity in normal glucose loaded and diabetic glucose loaded animals as well as normal off feed animals. Confirmation of antidiabetic activity and toxicity ameliorative role of S. cordata was investigated in a chronic multiple dose treatment study of fifteen days. A single dose of alloxan (120 mg/kg) produced a decrease in insulin level, hyperglycemia, elevated total lipids, triglycerides, and cholesterol and decreased the high-density lipoproteins. Concurrent with these changes, there was an increase in the concentration of lipid peroxidation (TBARS), H2O2, and nitrite in pancreas, liver, and testis. This oxidative stress was related to a decrease in glutathione content (GSH) and antioxidant enzymes. Administration of SCEE for 15 days after diabetes induction ameliorated hyperglycemia, restored lipid profile, blunted the increase in TBARS, H2O2, and nitrite content, and stimulated the GSH production in the organs of alloxan-treated rats. We suggested that SCEE could be used as antidiabetic component in case of diabetes mellitus. This may be related to its antioxidative properties. PMID:25114914

  12. Antidiabetic effect of Sida cordata in alloxan induced diabetic rats.

    PubMed

    Shah, Naseer Ali; Khan, Muhammad Rashid

    2014-01-01

    Medicinal plants are efficient ameliorator of oxidative stress associated with diabetes mellitus. In this study, ethyl acetate fraction (SCEE) of Sida cordata was investigated for scientific validation of its folk use in diabetes. Antidiabetic effect of SCEE was confirmed by antihyperglycemic activity in normal glucose loaded and diabetic glucose loaded animals as well as normal off feed animals. Confirmation of antidiabetic activity and toxicity ameliorative role of S. cordata was investigated in a chronic multiple dose treatment study of fifteen days. A single dose of alloxan (120 mg/kg) produced a decrease in insulin level, hyperglycemia, elevated total lipids, triglycerides, and cholesterol and decreased the high-density lipoproteins. Concurrent with these changes, there was an increase in the concentration of lipid peroxidation (TBARS), H2O2, and nitrite in pancreas, liver, and testis. This oxidative stress was related to a decrease in glutathione content (GSH) and antioxidant enzymes. Administration of SCEE for 15 days after diabetes induction ameliorated hyperglycemia, restored lipid profile, blunted the increase in TBARS, H2O2, and nitrite content, and stimulated the GSH production in the organs of alloxan-treated rats. We suggested that SCEE could be used as antidiabetic component in case of diabetes mellitus. This may be related to its antioxidative properties.

  13. Mechanisms and Clinical Application of Tetramethylpyrazine (an Interesting Natural Compound Isolated from Ligusticum Wallichii): Current Status and Perspective

    PubMed Central

    Chen, Keji

    2016-01-01

    Tetramethylpyrazine, a natural compound from Ligusticum wallichii (Chuan Xiong), has been extensively used in China for cardiovascular and cerebrovascular diseases for about 40 years. Because of its effectiveness in multisystems, especially in cardiovascular, its pharmacological action, clinical application, and the structural modification have attracted broad attention. In this paper its mechanisms of action, the clinical status, and synthetic derivatives will be reviewed briefly.

  14. Weak hybridization and isolated localized magnetic moments in the compounds CeT2Cd20 (T = Ni, Pd)

    NASA Astrophysics Data System (ADS)

    White, Benjamin; Yazici, Duygu; Ho, Pei-Chun; Kanchanavatee, Noravee; Pouse, Naveen; Friedman, Aaron; Maple, M. Brian

    2015-03-01

    Large Ce-Ce distances of 6.7-6.8 Åand weak hybridization between Ce 4 f and itinerant electron states act to promote stable localized magnetic moments in the compounds CeT2Cd20 (T = Ni, Pd), but also conspire to severely limit the strength of the Ruderman-Kittel-Kasuya-Yosida (RKKY) magnetic exchange interaction that couples them. As a consequence, measurements of electrical resistivity, performed on single-crystalline samples of these new Cd-based compounds down to 0.138 K, were unable to resolve any evidence for magnetic order. In this presentation, we will compare measurements of the physical properties of CeT2Cd20 (T = Ni, Pd) under ambient and applied pressures with the reported properties of the isostructural compounds CeT2X20 (T = transition metal; X = Al, Zn). We will use these comparisons to discuss the interplay of unit cell volume, hybridization, and the RKKY interaction and its role in establishing the ground states of the Ce-based ``1-2-20'' compounds. Sample synthesis and physical properties measurements were supported by the U.S. DOE under Grant No. DE-FG02-04-ER46105. Measurements of electrical resistivity below 1 K were supported by the NSF under Grants No. DMR-1206553 and No. DMR-1104544.

  15. Non-insulin antidiabetic therapy in cardiac patients: current problems and future prospects.

    PubMed

    Fisman, Enrique Z; Motro, Michael; Tenenbaum, Alexander

    2008-01-01

    ) these hazards are not mere 'side effects' but are deeply rooted in the drugs' mechanisms of action; (3) current data indicate that combined glibenclamide/metformin therapy seems to present a special risk and should be avoided in the long-term management of type 2 diabetics with proven CAD, and (4) Non-Insulin Antidiabetic Therapy in Diabetic Cardiac Patients 155 customized antihyperglycemic pharmacological approaches should be investigated for the optimal treatment of diabetic patients with heart disease. New possibilities are represented by incretin mimetic compounds, dipeptidyl peptidase (DPP)-4 inhibitors, inhaled insulin and eventually oral insulin. PMID:18230961

  16. A Novel Diphenylthiosemicarbazide Is a Potential Insulin Secretagogue for Anti-Diabetic Agen

    PubMed Central

    Sugawara, Kenji; Honda, Kohei; Reien, Yoshie; Yokoi, Norihide; Seki, Chihiro; Takahashi, Harumi; Minami, Kohtaro; Mori, Ichiro; Matsumoto, Akio; Nakaya, Haruaki; Seino, Susumu

    2016-01-01

    Insulin secretagogues are used for treatment of type 2 diabetes. We attempted to discover novel small molecules to stimulate insulin secretion by using in silico similarity search using sulfonylureas as query, followed by measurement of insulin secretion. Among 38 compounds selected by in silico similarity search, we found three diphenylsemicarbazides and one quinolone that stimulate insulin secretion. We focused on compound 8 (C8), which had the strongest insulin-secreting effect. Based on the structure-activity relationship of C8-derivatives, we identified diphenylthiosemicarbazide (DSC) 108 as the most potent secretagogue. DSC108 increased the intracellular Ca2+ level in MIN6-K8 cells. Competitive inhibition experiment and electrophysiological analysis revealed sulfonylurea receptor 1 (SUR1) to be the target of DSC108 and that this diphenylthiosemicarbazide directly inhibits ATP-sensitive K+ (KATP) channels. Pharmacokinetic analysis showed that DSC108 has a short half-life in vivo. Oral administration of DSC108 significantly suppressed the rises in blood glucose levels after glucose load in wild-type mice and improved glucose tolerance in the Goto-Kakizaki (GK) rat, a model of type 2 diabetes with impaired insulin secretion. Our data indicate that DSC108 is a novel insulin secretagogue, and is a lead compound for development of a new anti-diabetic agent. PMID:27764176

  17. Evaluation of anti-diabetic and alpha glucosidase inhibitory action of anthraquinones from Rheum emodi.

    PubMed

    Arvindekar, Aditya; More, Tanaji; Payghan, Pavan V; Laddha, Kirti; Ghoshal, Nanda; Arvindekar, Akalpita

    2015-08-01

    Rheum emodi is used as a culinary plant across the world and finds an eminent role in the Ayurvedic and traditional Chinese systems of medicine. The plant is known to principally contain 1,8-dihydroxyanthraquinones (DHAQs) like rhein, aloe emodin, emodin, chrysophanol and physcion that possess diverse pharmacological and therapeutic actions. The present work deals with developing a platform technology for isolation of these DHAQs and evaluating their anti-diabetic potential. Herein, we report the anti-hyperglycemic activity and alpha glucosidase (AG) inhibitory actions of five isolated DHAQs from R. emodi. All the five isolated DHAQs showed good anti-hyperglycemic activity with aloe emodin exhibiting maximum lowering of blood glucose in an oral glucose tolerance test. However, on evaluation of the AG inhibitory potential of the DHAQs only emodin exhibited potent intestinal AG inhibition (93 ± 2.16%) with an IC50 notably lower than acarbose. Subsequent kinetic studies indicated a mixed type of inhibition for emodin. In vivo studies using oral maltose load showed almost total inhibition for emodin when compared to acarbose. Molecular docking studies revealed the presence of an allosteric topographically distinct 'quinone binding site' and showed that interaction with Ser 74 occurs exclusively with emodin, which is vital for AG inhibition. The net benefit from the glucose lowering effect and mixed type inhibition by emodin would enable the administration of a small dosage that is safe and non-toxic in the case of prolonged use in treating diabetes. PMID:26145710

  18. High performance thin layer chromatography fingerprinting, phytochemical and physico-chemical studies of anti-diabetic herbal extracts

    PubMed Central

    Itankar, Prakash R.; Sawant, Dattatray B.; Tauqeer, Mohd.; Charde, Sonal S.

    2015-01-01

    Introduction: Herbal medicines have gained increasing popularity in the last few decades, and this global resurgence of herbal medicines increases their commercial value. However, this increasing demand has resulted in a decline in their quality, primarily due to a lack of adequate regulations pertaining to herbal medicines. Aim: To develop an optimized methodology for the standardization of herbal raw materials. Materials and Methods: The present study has been designed to examine each of the five herbal anti-diabetic drugs, Gymnema sylvester R. Br., Pterocarpus marsupium Roxburgh., Enicostema littorale Blume., Syzygium cumini (L.) Skeels. and Emblica officinalis Gaertn. The in-house extracts and marketed extracts were evaluated using physicochemical parameters, preliminary phytochemical screening, quantification of polyphenols (Folin–Ciocalteu colorimetric method) and high performance thin layer chromatography (HPTLC) fingerprint profiling with reference to marker compounds in plant extracts. Results: All the plants mainly contain polyphenolic compounds and are quantified in the range of 3.6–21.72% w/w. E. officinalis contain the highest and E. littorale contain the lowest content of polyphenol among plant extracts analyzed. HPTLC fingerprinting showed that the in-house extracts were of better quality than marketed extracts. Conclusion: The results obtained from the study could be utilized for setting limits for the reference phytoconstituents (biomarker) for the quality control and quality assurance of these anti-diabetic drugs. PMID:27011722

  19. Evaluation of antidiabetic, antioxidant and antiglycating activities of the Eysenhardtia polystachya

    PubMed Central

    Gutierrez, Rosa Martha Perez; Baez, Efren Garcia

    2014-01-01

    Background: Many diseases are associated with oxidative stress caused by free radicals. The aim of the present study was to evaluate the antidiabetic, antioxidant and antiglycation properties of Eysenhardtia polystachya (EP) bark methanol-water extract. Materials and Methods : The antioxidant capacities were evaluated by studying in vitro the scavenging of DPPH and ABTS free radical, reactive oxygen species such as RO2, O2·-, H2O2, OH., H2O2, ONOO-, NO, HOCl,1 O2, chelating ability, ORAC, β-carotene-bleaching and lipid peroxidation. The antiglycation activities of EP were evaluated by haemoglobin, bovine serum albumin (BSA)-glucose, BSA-methylglyoxal and BSA-glucose assays. Oral administration of EP at the doses of 100 mg/kg, 200 mg/kg and 400 mg/g was studied in normal, glucose-loaded and antidiabetic effects on streptozotocin-induced mildly diabetic (MD) and severely diabetic (SD) mice. Results: EP showed Hdonor activity, free radical scavenging activity, metal chelating ability and lipid peroxidation Antioxidant activity may be attributed to the presence of phenolic and flavonoid compounds. EP is an inhibitor of fluorescent AGE, methylglyoxal and the glycation of haemoglobin. In STZ-induced diabetic mice, EP reduced the blood glucose, increased serum insulin, body weight, marker enzymes of hepatic function, glycogen, HDL, GK and HK while there was reduction in the levels of triglyceride, cholesterol, TBARS, LDL and G6Pase. Conclusions: Eysenhardtia polystachya possesses considerable antioxidant activity with reactive oxygen species (ROS) scavenging activity and demonstrated an anti-AGEs and hepatoprotective role, inhibits hyperglycemic, hyperlipidemic and oxidative stress indicating that these effects may be mediated by interacting with multiple targets operating in diabetes mellitus. PMID:24991120

  20. [Preparative isolation and purification of five non-volatile compounds from Fructus caryophylli and Flos caryophylli by high-speed counter-current chromatography].

    PubMed

    Gao, Lu; Yu, Bo; Yang, Hong

    2011-11-01

    A high-speed counter-current chromatographic (HSCCC) method was successfully developed for the isolation of three non-volatile compounds from Fructus Caryophylli and two chromone compounds from Flos Caryophylli. The optimum separation solution systems included system A (n-hexane-ethyl acetate-methanol-water (5:8:6: 13, v/v/v/v) and system B (n-hexane-ethyl acetate-methanol-water (5: 8: 9: 10, v/v/v/v). The upper phase of the system A was used as the stationary phase, and the lower phases of the systems A and B as the mobile phases were operated at a flow of 1.2 mL/min, while the apparatus rotated at 880 r/min. The 12.3 mg of ellagic acid, 9.6 mg of rhamnetin, 17.2 mg of quercetin were successfully purified from 70 mg of the crude extract of Fructus Caryophylli by a two-step separation. In the same way, 10.2 mg of 5,7-dimethoxy-2-methylchromone, 8.6 mg of 5,7-dimethoxy-2,6-dimethyl-chromone were purified from 50 mg of the crude extract of Flos Caryophylli. The purities of the compounds were all over 96% as determined by high performance liquid chromatography (HPLC). The five compounds were indentified by mass spectrometry (MS), 1H-nuclear magnetic resonance (NMR) and 13C-NMR. The results indicate that HSCCC is a powerful technique for the purification of non-volatile compounds from different parts of Eugenia caryophylla Thunb.

  1. Antidiabetic and antioxidative effects of Annona squamosa leaves are possibly mediated through quercetin-3-O-glucoside.

    PubMed

    Panda, Sunanda; Kar, Anand

    2007-01-01

    Present investigation was made to reveal the involvement of a quercetin in the antidiabetic and antiperoxidative effects of Annona squamosa leaf extract. Quercetin-3-O-glucoside (characterized by UV, IR, MS and NMR analyses) was isolated from Annona squamosa leaves and examined for its potential to regulate alloxan-induced hyperglycemia and lipid peroxidation (LPO) in rats. While in alloxan treated animals, an increase in the concentration of serum glucose with a parallel decrease in insulin level was observed, administration of 15 mg/kg/day of isolated quercetin-3-O-glucoside for 10 consecutive days to the hyperglycemic animals reversed these effects and simultaneously inhibited the activity of hepatic glucose-6-phosphatase. It further decreased the hepatic and renal LPO with a concomitant increase in the activities of antioxidative enzymes, such as catalase (CAT) and superoxide dismutase (SOD) and in glutathione (GSH) content, indicating its safe and antiperoxidative effects. These findings suggest the potential of quercetin-3-O-glucoside in the amelioration of diabetes mellitus and tissue lipid peroxidation. It also appears that the antidiabetic effects of A. squamosa leaf extract is possibly mediated through the insulin stimulating and/or free radical scavenging properties of its active constituent, quercetin-3-O-glucoside. PMID:18997283

  2. A micro-Raman spectroscopic investigation of leukemic U-937 cells treated with Crotalaria agatiflora Schweinf and the isolated compound madurensine

    NASA Astrophysics Data System (ADS)

    le Roux, Karlien; Prinsloo, Linda C.; Hussein, Ahmed A.; Lall, Namrita

    In South Africa traditional medicine plays an important role in primary health care and therefore it is very important that the medicinal use of plants is scientifically tested for toxicity and effectiveness. It was established that the ethanolic extract of the leaves of Crotalaria agatiflora, as well as the isolated compound madurensine, is moderately toxic against leukemic U-937 cells. Light microscopic investigations indicated that symptoms of cell death are induced during treatments, but flow cytometry analysis of treated cells, using annexin-V and propidium iodide, showed that apoptosis and necrosis are insignificantly induced. The Raman results suggested that protein extraction and DNA melting occur in the cells during treatment with the ethanolic extracts (IC50 value 73.9 μg/mL), drastically changing the molecular content of the cells. In contrast, treatment with madurensine (IC50 value 136.5 μg/mL), an isolated pyrrolizidine alkaloid from the ethanolic extract of the leaves, did not have the same effect. The results are also compared to that of cells treated with actinomycin D, a compound known to induce apoptosis. The investigation showed that micro-Raman spectroscopy has great promise to be used for initial screening of samples to determine the effects of different treatments on cancerous cell lines together with conventional methods. The results highlight the fact that for many natural products used for medicinal purposes, the therapeutic effect of the crude plant extract tends to be significantly more effective than the particular action of its individual constituents.

  3. Characterization of kinetic parameters and the formation of volatile compounds during the tequila fermentation by wild yeasts isolated from agave juice.

    PubMed

    Arellano, Melchor; Pelayo, Carlos; Ramírez, Jesús; Rodriguez, Ingrid

    2008-08-01

    The production of aroma compounds during tequila fermentation using four native yeast strains isolated from agave juice was quantified at controlled (35 degrees C) and uncontrolled temperatures (room temperature) by gas chromatography (FID). Three of the four strains were identified as Saccharomyces cerevisiae (MTLI 1, MALI 1 and MGLI 1) and one as Kloeckera apiculata (MALI 2). Among the aroma compounds produced, acetaldehyde has the highest accumulation at the controlled temperature and before 50% of sugar was consumed. The S. cerevisiae strains produced ethyl acetate in almost the same quantity at a concentration of 5 mg/L and the K. apiculata produced six-times more (30 mg/L) than the S. cerevisiae strains, independent of the fermentation temperature. The rate and amount of 1-propanol, amyl alcohols and isobutanol production were affected by the type of yeast used. The K. apiculate strain produced 50% less of the higher alcohols than the Saccharomyces strains. The results obtained showed that indigenous isolated yeasts play an important role in the tequila flavor and suggest that mixtures of these yeasts may be used to produce tequila with a unique and desirable aroma.

  4. Identification of compounds from high-fat and extra virgin olive oil-supplemented diets in whole mouse liver extracts and isolated mitochondria using mass spectrometry.

    PubMed

    dos Santos, Gustavo Aparecido; Ferreira, Mônica Siqueira; de Oliveira, Diogo Noin; de Oliveira, Vanessa; Siqueira-Santos, Edilene S; Cintra, Dennys Esper Corrêa; Castilho, Roger Frigério; Velloso, Lício Augusto; Catharino, Rodrigo Ramos

    2015-07-01

    Nonalcoholic steatohepatitis (NASH) is a fatty liver disorder that could be improved with extra virgin olive oil (EVOO) supplementation in diet. We propose the monitoring, in whole mouse liver extracts and in isolated mitochondria, of the absorption of compounds from three different diets: standard (CT), high-fat (HFD) and high-fat supplemented with EVOO (HFSO). Male mice were submitted to one of the following three diets: CT or HFD for 16 weeks or HFD for 8 weeks followed by additional 8 weeks with HFSO. Following this period, liver was extracted for histological evaluation, mitochondria isolation and mass spectrometry analyses. Diets, liver extracts and Percoll-purified mitochondria were analyzed using ESI-MS and the lipidomics approach. Morphological, histological and spectrometric results indicated a decrease in NASH severity with EVOO supplementation in comparison with animals maintained with HFD. Spectrometric data also demonstrated that some compounds presented on the diets are absorbed by the mitochondria. EVOO was shown to be a potential therapeutic alternative in food for NASH. Our results are in accordance with the proposition that the major factor that influences different responses to diets is their composition - and not only calories - especially when it comes to studies on obesity.

  5. Mechanisms and Clinical Application of Tetramethylpyrazine (an Interesting Natural Compound Isolated from Ligusticum Wallichii): Current Status and Perspective

    PubMed Central

    Chen, Keji

    2016-01-01

    Tetramethylpyrazine, a natural compound from Ligusticum wallichii (Chuan Xiong), has been extensively used in China for cardiovascular and cerebrovascular diseases for about 40 years. Because of its effectiveness in multisystems, especially in cardiovascular, its pharmacological action, clinical application, and the structural modification have attracted broad attention. In this paper its mechanisms of action, the clinical status, and synthetic derivatives will be reviewed briefly. PMID:27668034

  6. Isolation, identification, and quantification of potential defensive compounds in the viceroy butterfly and its larval host-plant, Carolina willow.

    PubMed

    Prudic, Kathleen L; Khera, Smriti; Sólyom, Anikó; Timmermann, Barbara N

    2007-06-01

    The viceroy-monarch and viceroy-queen butterfly associations are classic examples of mimicry. These relationships were originally classified as Batesian, or parasitic, but were later reclassified as Müllerian, or mutalistic, based on predator bioassays. The Müllerian reclassification implies that viceroy is unpalatable because it too is chemically defended like the queen and the monarch. However, unlike the queen and the monarch, the viceroy defensive chemistry has remained uncharacterized. We demonstrate that the viceroy butterfly (Limenitis archippus, Nymphalidae) not only sequesters nonvolatile defensive compounds from its larval host-plant, the Carolina willow (Salix caroliniana, Salicaceae), but also secretes volatile defensive compounds when disturbed. We developed liquid chromatography-mass spectrometry-mass spectrometry methods to identify a set of phenolic glycosides shared between the adult viceroy butterfly and the Carolina willow, and solid phase microextraction and gas chromatography-mass spectrometry methods to identify volatile phenolic compounds released from stressed viceroy butterflies. In both approaches, all structures were characterized based on their mass spectral fragmentation patterns and confirmed with authentic standards. The phenolics we found are known to deter predator attack in other prey systems, including other willow-feeding insect species. Because these compounds have a generalized defensive function at the concentrations we described, our results are consistent with the Müllerian reclassification put forth by other researchers based on bioassay results. It seems that the viceroy butterfly possesses chemical defenses different from its monarch and queen butterfly counterparts (phenolic glycosides vs. cardiac glycosides, respectively), an unusual phenomenon in mimicry warranting future study.

  7. Isolation and characterization of nanosheets containing few layers of the Aurivillius family of oxides and metal-organic compounds

    SciTech Connect

    Sreedhara, M.B.; Prasad, B.E.; Moirangthem, Monali; Murugavel, R.; Rao, C.N.R.

    2015-04-15

    Nanosheets containing few-layers of ferroelectric Aurivillius family of oxides, Bi{sub 2}A{sub n−1}B{sub n}O{sub 3n+3} (where A=Bi{sup 3+}, Ba{sup 2+} etc. and B=Ti{sup 4+}, Fe{sup 3+} etc.) with n=3, 4, 5, 6 and 7 have been prepared by reaction with n-butyllithium, followed by exfoliation in water. The few-layer samples have been characterized by Tyndall cones, atomic force microscopy, optical spectroscopy and other techniques. The few-layer species have a thickness corresponding to a fraction of the c-parameter along which axis the perovskite layers are stacked. Magnetization measurements have been carried out on the few-layer samples containing iron. Few-layer species of a few layered metal-organic compounds have been obtained by ultrasonication and characterized by Tyndall cones, atomic force microscopy, optical spectroscopy and magnetic measurements. Significant changes in the optical spectra and magnetic properties are found in the few-layer species compared to the bulk samples. Few-layer species of the Aurivillius family of oxides may find uses as thin layer dielectrics in photovoltaics and other applications. - Graphical abstract: Exfoliation of the layered Aurivillius oxides into few-layer nanosheets by chemical Li intercalation using n-BuLi followed by reaction in water. Exfoliation of the layered metal-organic compounds into few-layer nanosheets by ultrasonication. - Highlights: • Few-layer nanosheets of Aurivillius family of oxides with perovskite layers have been generated by lithium intercalation. • Few-layer nanosheets of few layered metal-organic compounds have been generated by ultrasonication. • Few-layer nanosheets of the Aurivillius oxides have been characterized by AFM, TEM and optical spectroscopy. • Aurivillius oxides containing Fe show layer dependent magnetic properties. • Exfoliated few-layer metal-organic compounds show changes in spectroscopic and magnetic properties compared with bulk materials.

  8. Isolation and characterization of phenolic compounds and anthocyanins from Murta (Ugni molinae Turcz.) fruits. Assessment of antioxidant and antibacterial activity.

    PubMed

    Junqueira-Gonçalves, Maria Paula; Yáñez, Lina; Morales, Carolina; Navarro, Muriel; A Contreras, Rodrigo; Zúñiga, Gustavo E

    2015-01-01

    Berry fruit consumption has become important in the promotion of human health, mainly due to their phenolic compounds, which have been associated with protection against different pathologies, as well as antimicrobial and other biological activities. Consequently, there has been a growing interest in identifying natural antioxidants and antimicrobials from these plants. This study aimed to characterize the phenolic chemical composition and anthocyanin profile of murta (Ugni molinae Turcz.) fruit, and to evaluate the antioxidant and antimicrobial activity of its extracts (ethanolic and methanolic). LC/MS of the ethanolic extracts showed the presence of three major compounds: caffeic acid 3-glu, quercetin-3-glu and quercetin, while in the methanolic acid extract they were cyanidin-3-glucoside, pelargonidin-3-arabinose and delphinidin-3-glucoside. The antioxidant activity of ethanolic extracts (DPPH· and ORAC assays) was higher than that of methanol acid extracts or purified anthocynins. Furthermore, the methanol acid extract showed an inhibitory activity against the bacteria E. coli and S. typhi similar to that of standard antibiotics. The results suggest that the antioxidant activity of the ethanolic extract is regulated by the high content of phenolic compounds and the fruit's characteristic color is due to the content of pelargonidin-3-arabinose and delphinidin-3-glucoside. The obtained results demonstrated the appreciable antioxidant and antibacterial activities, providing opportunities to explore murta extracts as biopreservatives. PMID:25838172

  9. Isolation and characterization of phenolic compounds and anthocyanins from Murta (Ugni molinae Turcz.) fruits. Assessment of antioxidant and antibacterial activity.

    PubMed

    Junqueira-Gonçalves, Maria Paula; Yáñez, Lina; Morales, Carolina; Navarro, Muriel; A Contreras, Rodrigo; Zúñiga, Gustavo E

    2015-03-31

    Berry fruit consumption has become important in the promotion of human health, mainly due to their phenolic compounds, which have been associated with protection against different pathologies, as well as antimicrobial and other biological activities. Consequently, there has been a growing interest in identifying natural antioxidants and antimicrobials from these plants. This study aimed to characterize the phenolic chemical composition and anthocyanin profile of murta (Ugni molinae Turcz.) fruit, and to evaluate the antioxidant and antimicrobial activity of its extracts (ethanolic and methanolic). LC/MS of the ethanolic extracts showed the presence of three major compounds: caffeic acid 3-glu, quercetin-3-glu and quercetin, while in the methanolic acid extract they were cyanidin-3-glucoside, pelargonidin-3-arabinose and delphinidin-3-glucoside. The antioxidant activity of ethanolic extracts (DPPH· and ORAC assays) was higher than that of methanol acid extracts or purified anthocynins. Furthermore, the methanol acid extract showed an inhibitory activity against the bacteria E. coli and S. typhi similar to that of standard antibiotics. The results suggest that the antioxidant activity of the ethanolic extract is regulated by the high content of phenolic compounds and the fruit's characteristic color is due to the content of pelargonidin-3-arabinose and delphinidin-3-glucoside. The obtained results demonstrated the appreciable antioxidant and antibacterial activities, providing opportunities to explore murta extracts as biopreservatives.

  10. Insect growth inhibition, antifeedant and antifungal activity of compounds isolated/derived from Zingiber officinale Roscoe (ginger) rhizomes.

    PubMed

    Agarwal, M; Walia, S; Dhingra, S; Khambay, B P

    2001-03-01

    Fresh rhizomes of Zingiber officinale (ginger), when subjected to steam distillation, yielded ginger oil in which curcumene was found to be the major constituent. The thermally labile zingiberene-rich fraction was obtained from its diethyl ether extract. Column chromatography of ginger oleoresin furnished a fraction from which [6]-gingerol was obtained by preparative TLC. Naturally occurring [6]-dehydroshogaol was synthesised following condensation of dehydrozingerone with hexanal, whereas zingerone and 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)butane were obtained by hydrogenation of dehydrozingerone with 10% Pd/C. The structures of the compounds were established by 1H NMR, 13C NMR and mass (EI-MS and ES-MS) spectral analysis. The test compounds exhibited moderate insect growth regulatory (IGR) and antifeedant activity against Spilosoma obliqua, and significant antifungal activity against Rhizoctonia solani. Among the various compounds, [6]-dehydroshogaol exhibited maximum IGR activity (EC50 3.55 mg ml-1), while dehydrozingerone imparted maximum antifungal activity (EC50 86.49 mg litre-1).

  11. Exploring Bioactive Properties of Marine Cyanobacteria Isolated from the Portuguese Coast: High Potential as a Source of Anticancer Compounds

    PubMed Central

    Costa, Margarida; Garcia, Mónica; Costa-Rodrigues, João; Costa, Maria Sofia; Ribeiro, Maria João; Fernandes, Maria Helena; Barros, Piedade; Barreiro, Aldo; Vasconcelos, Vitor; Martins, Rosário

    2013-01-01

    The oceans remain a major source of natural compounds with potential in pharmacology. In particular, during the last few decades, marine cyanobacteria have been in focus as producers of interesting bioactive compounds, especially for the treatment of cancer. In this study, the anticancer potential of extracts from twenty eight marine cyanobacteria strains, belonging to the underexplored picoplanktonic genera, Cyanobium, Synechocystis and Synechococcus, and the filamentous genera, Nodosilinea, Leptolyngbya, Pseudanabaena and Romeria, were assessed in eight human tumor cell lines. First, a crude extract was obtained by dichloromethane:methanol extraction, and from it, three fractions were separated in a Si column chromatography. The crude extract and fractions were tested in eight human cancer cell lines for cell viability/toxicity, accessed with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and lactic dehydrogenase release (LDH) assays. Eight point nine percent of the strains revealed strong cytotoxicity; 17.8% showed moderate cytotoxicity, and 14.3% assays showed low toxicity. The results obtained revealed that the studied genera of marine cyanobacteria are a promising source of novel compounds with potential anticancer activity and highlight the interest in also exploring the smaller filamentous and picoplanktonic genera of cyanobacteria. PMID:24384871

  12. Isolation of the four methyl jasmonate stereoisomers and their effects on selected chiral volatile compounds in red raspberries.

    PubMed

    Flores, Gema; Blanch, Gracia Patricia; Ruiz del Castillo, Maria Luisa

    2013-12-01

    The four stereoisomers present in a commercial sample of methyl jasmonate (MJ) were isolated at semi-preparative scale by HPLC, using a permethylated β-cyclodextrin column. This allowed the baseline resolution and collection of both major (methyl jasmonates) and minor (epi-methyl jasmonates) stereoisomers. When 1.5 mL of a 5mg per mL MJ solution were injected, isolated amounts were 3.56 mg for (-) and (+)-methyl jasmonates, with respective purities of 96.1% and 99.9%, and 0.18 mg for (-)- and (+)-epi-methyl jasmonates, with 98.6% and 91.6% respective purities. The post-harvest treatment of red raspberry fruits with the pure methyl jasmonate stereoisomers isolated proved that (-)-epi-MJ either promotes the bioformation of (+)-limonene or inhibits that of (-)-limonene to a greater extent than the other three MJ stereoisomers, while the biosynthesis of the (+)-enantiomer of α-ionone is favoured equally, whichever MJ stereoisomer used. The results obtained in the present study might be used to obtain food products with improved sensory characteristics.

  13. Functionalization of gold nanoparticles as antidiabetic nanomaterial

    NASA Astrophysics Data System (ADS)

    Venkatachalam, M.; Govindaraju, K.; Mohamed Sadiq, A.; Tamilselvan, S.; Ganesh Kumar, V.; Singaravelu, G.

    2013-12-01

    In the present investigation, functionalization of gold nanoparticles synthesized using propanoic acid 2-(3-acetoxy-4,4,14-trimethylandrost-8-en-17-yl) (PAT) an active biocomponent isolated from Cassia auriculata is studied in detail. On reaction of PAT with aqueous HAuCl4, rapid formation of stable gold nanoparticles was achieved. Formation of gold nanoparticles was confirmed by UV-vis spectroscopy, XRD, GC-MS, FTIR, TEM and SEM with EDAX. Gold nanoparticles mostly were monodisperse, spherical in shape and ranged in size 12-41 nm. Gold nanoparticles synthesised using PAT was administered to alloxan (150 mg/kg body weight) induced diabetic male albino rats at different doses (0.25, 0.5, 0.75 and 1.0 mg/kg body weight) for 28 days. Plasma glucose level, cholesterol and triglyceride were significantly (p < 0.001) reduced in experimental animals treated with gold nanoparticles at dosage of 0.5 mg/kg body weight and plasma insulin increased significantly. The newly genre green gold nanoparticles exhibit remarkable protein tyrosine phosphatase 1B inhibitory activity.

  14. Inhibitory effect of glycoprotein isolated from Opuntia ficus-indica var. saboten MAKINO on activities of allergy-mediators in compound 48/80-stimulated mast cells.

    PubMed

    Lim, Kye-Taek

    2010-01-01

    The present study was performed to investigate the anti-allergy potentials of glycoprotein (90kDa) isolated from Opuntia ficus-indica var. saboten MAKINO (OFI glycoprotein) in vivo (ICR mice) and in vitro (RBL-2H3 cells). At first, to know whether the OFI glycoprotein has an inhibitory ability for allergy in vivo, we evaluated the activities of allergy-related factors such as histamine and beta-hexosaminidase release, lactate dehydrogenase (LDH), and interleukin 4 (IL-4) in compound 48/80 (8 ml/kg BW)-treated ICR mice. After that, we studied to found the effect for anti-allergy in vitro such as nuclear factor kappa B (NF-kappaB) and inducible nitric oxide synthase (iNOS), extracellular signal-regulated kinase (ERK) 1/2, arachidonic acid, and cyclooxygenase-2 (COX-2) in compound 48/80 (5 microg/ml)-treated RBL-2H3 cells. Our results showed that the OFI glycoprotein (5 mg/kg) inhibited histamine and beta-hexosaminidase release, lactate dehydrogenase (LDH), and interleukin 4 (IL-4) in mice serum. Also OFI glycoprotein (25 microg/ml) has suppressive effects on the expression of MAPK (ERK1/2), and on protein expression of anti-allergic proteins (iNOS and COX-2). Thus, we speculate that the OFI glycoprotein is an example of natural compound that blocks anti-allergic signal transduction pathways.

  15. Optimization of extraction parameters on the isolation of phenolic compounds from sour cherry (Prunus cerasus L.) pomace.

    PubMed

    Yılmaz, Fatih Mehmet; Karaaslan, Mehmet; Vardin, Hasan

    2015-05-01

    There is an increasing interest to bio-components obtained from fruit & vegetable wastes. Anthocyanin is one of the components regained from fruits especially from red ones. Sour cherry is considered as industrial fruit since most of the grown fruit is processed into juice and hence considerable amount of pomace is removed from process. The influences of process parameters on the extraction of phenolic compounds from sour cherry pomace were investigated. Fifty-one percent ethanol concentration, 75 °C temperature and 12 mL/g solvent to solid ratio were selected as optimum process parameters. Time effect on the process efficiency was monitored at three different temperatures (25, 50 and 75 °C) and total phenolic and total anthocyanin contents were found to reach equilibrium concentrations between 80 and 100 min time intervals. Ethanol concentrations affected differently extraction yield of anthocyanins and non-anthocyanin phenolics. Various individual phenolic compounds present in sour cherry pomace were identified and quantified by HPLC equipped with UV/Vis PDA. Of the phenolic compounds, cyanidin-3-glucosylrutinoside, neochlorogenic acid and catechin were the most abundant ones found in the pomace. 14.23 ± 0.38 mg/g total phenolic, 0.41 ± 0.02 mg/g total anthocyanin, 0.19 ± 0.02 mg/g cyanidin-3-glucosylrutinoside, 0.22 ± 0.01 mg/g neochlorogenic acid and 0.22 ± 0.02 mg/g catechin contents (dry weight) were determined in the pomace at optimum extraction conditions. PMID:25892783

  16. The Hypoglycemic and Synergistic Effect of Loganin, Morroniside, and Ursolic Acid Isolated from the Fruits of Cornus officinalis.

    PubMed

    He, Kai; Song, Shanghua; Zou, Zongyao; Feng, Min; Wang, Dezhen; Wang, Yanzhi; Li, Xuegang; Ye, Xiaoli

    2016-02-01

    Hypoglycemic activity-guided separation of ethanol extracts from the fruits of Cornus officinalis Sieb. et Zucc (CO) led to the isolation of loganin, morroniside, and ursolic acid. The antidiabetic capacity of CO extracts and related compounds was further investigated in diabetes mellitus mice. The results suggested that both CO extracts and pure compounds could ameliorate diabetes-associated damages and complications. Oral administration of loganin and morroniside decreased fasting blood glucose levels in diabetes mellitus mice. Ursolic acid exhibited the highest reactive oxygen species scavenging activity and α-glucosidase inhibitory activity. Notably, we noticed an interesting synergistic effect between loganin and ursolic acid. Given these favorable hypoglycemic properties, C. officinalis, a food and medicinal plant in China, may be used as a valuable food supplement for the treatment of diabetes mellitus.

  17. The Hypoglycemic and Synergistic Effect of Loganin, Morroniside, and Ursolic Acid Isolated from the Fruits of Cornus officinalis.

    PubMed

    He, Kai; Song, Shanghua; Zou, Zongyao; Feng, Min; Wang, Dezhen; Wang, Yanzhi; Li, Xuegang; Ye, Xiaoli

    2016-02-01

    Hypoglycemic activity-guided separation of ethanol extracts from the fruits of Cornus officinalis Sieb. et Zucc (CO) led to the isolation of loganin, morroniside, and ursolic acid. The antidiabetic capacity of CO extracts and related compounds was further investigated in diabetes mellitus mice. The results suggested that both CO extracts and pure compounds could ameliorate diabetes-associated damages and complications. Oral administration of loganin and morroniside decreased fasting blood glucose levels in diabetes mellitus mice. Ursolic acid exhibited the highest reactive oxygen species scavenging activity and α-glucosidase inhibitory activity. Notably, we noticed an interesting synergistic effect between loganin and ursolic acid. Given these favorable hypoglycemic properties, C. officinalis, a food and medicinal plant in China, may be used as a valuable food supplement for the treatment of diabetes mellitus. PMID:26619955

  18. Antidiabetic Effects of Aqueous Infusions of Artemisia herba-alba and Ajuga iva in Alloxan-Induced Diabetic Rats.

    PubMed

    Boudjelal, Amel; Siracusa, Laura; Henchiri, Cherifa; Sarri, Madani; Abderrahim, Benkhaled; Baali, Faiza; Ruberto, Giuseppe

    2015-06-01

    The aqueous infusions of the aerial parts of Artemisia herba-alba Asso and Ajuga iva Schreber, prepared in accordance with the traditional procedure used in the local folk medicine, have been analysed for their composition and content of phytochemical constituents and examined for their antidiabetic effectiveness in alloxan-induced diabetic rats. Oral administration of A. herba-alba and A. iva infusions was studied in normal and alloxan-induced diabetic rats, which were randomly divided into nine groups, each group consisting of six animals. The drug preparations (100, 200, and 300 mg/kg b. w.) of each plant were given orally to the rats of each group twice daily for 15 days. Compositional analysis of the aqueous infusions revealed the presence of several polyphenols as main components. A. herba-alba infusion was characterised by mono- and di-cinnamoylquinic acids, with 5-caffeoylquinic (chlorogenic) acid being the main compound, followed by 3,5-dicaffeoylquinic acid. Vicenin-2 (apigenin 6,8-di-C-glucoside) appeared to be the most abundant among flavonoids. On the other hand, A. iva showed the exclusive presence of flavonoids, with the flavanone naringin present in relatively high levels together with several apigenin (flavone) derivatives. Oral administration of 300 mg/kg b. w. of the aqueous infusions of A. herba-alba and A. iva exhibited a significant reduction in blood glucose content, showing a much more efficient antidiabetic activity compared to glibenclamide, the oral hypoglycaemic agent used as a positive control in this study. These results suggest that A. herba-alba and A. iva possess significant antidiabetic activity, as they were able to improve the biochemical damage in alloxan-induced diabetes in rats.

  19. Antioxidant and antidiabetic properties of condensed tannins in acetonic extract of selected raw and processed indigenous food ingredients from Kenya.

    PubMed

    Kunyanga, Catherine Nkirote; Imungi, Jasper Kathenya; Okoth, Michael; Momanyi, Clare; Biesalski, Han Konrad; Vadivel, Vellingiri

    2011-05-01

    Recently, tannins have received considerable attention as health-promoting component in various plant foods and several studies have reported on its nutraceutical properties. However, no study has established the role of condensed tannins in indigenous foods of Kenya. Therefore, this study was designed to evaluate the antioxidant activity (DPPH and FRAP) and antidiabetic effects (α-amylase and α-glucosidase inhibition activities) of condensed tannins in some selected raw and traditionally processed indigenous cereals, legumes, oil seeds, and vegetables. The condensed tannin content of the grains and vegetables ranged between 2.55 and 4.35 g/100 g DM and 1.53 and 5.73 g/100 g DM, respectively. The scavenging effect of acetonic extract on DPPH radical ranged from 77% to 90% while the reducing power was found to be 31 to 574 mmol Fe(II)/g DM in all the investigated food ingredients. The condensed tannin extracts of the analyzed samples showed promising antidiabetic effects with potential α-amylase and α-glucosidase inhibition activities of 23% to 44% and 58% to 88%, respectively. Condensed tannins extracted from the amaranth grain, finger millet, field bean, sunflower seeds, drumstick, and amaranth leaves exerted significantly higher antioxidant and antidiabetic activities than other food ingredients. Among the traditional processing methods, roasting of grains and cooking of vegetables were found to be more suitable mild treatments for preserving the tannin compound and its functional properties as opposed to soaking + cooking and blanching treatments. The identified elite sources of optimally processed indigenous food ingredients with promising results could be used as health-promoting ingredients through formulation of therapeutic diets.

  20. Potent antifungal activity of extracts and pure compound isolated from pomegranate peels and synergism with fluconazole against Candida albicans.

    PubMed

    Endo, Eliana Harue; Cortez, Diógenes Aparício Garcia; Ueda-Nakamura, Tânia; Nakamura, Celso Vataru; Dias Filho, Benedito Prado

    2010-09-01

    Activity-guided repeated fractionation of crude hydro alcoholic extract prepared from the fruit peel of Punica granatum on a silica-gel column yielded a compound that exhibited strong antifungal activity against Candida spp. Based on spectral analyses, the compound was identified as punicalagin. Punicalagin showed strong activity against Candida albicans and Candida parapsilosis, with MICs of 3.9 and 1.9 microg/ml, respectively. The combination of punicalagin and fluconazole showed a synergistic interaction. MIC for fluconazole decreased twofold when combined with the extract. The FIC index was 0.25. The synergism observed in disk-diffusion and checkerboard assays was confirmed in time-kill curves. The effect of punicalagin on the morphology and ultrastructure in treated yeast cells was examined by scanning and transmission electron microscopy. An irregular budding pattern and pseudohyphae were seen in treated yeasts. By transmission electron microscopy, treated cells showed a thickened cell wall, changes in the space between cell wall and the plasma membrane, vacuoles, and a reduction in cytoplasmic content. Since the punicalagin concentration effective in vitro is achievable in vivo, the combination of this agent with fluconazole represents an attractive prospect for the development of new management strategies for candidiasis, and should be investigated further in in vivo models. PMID:20541606

  1. Antidiabetic effect of some medicinal plants of Oriental Morocco in neonatal non-insulin-dependent diabetes mellitus rats.

    PubMed

    Bnouham, Mohamed; Merhfour, Fatima Zahra; Ziyyat, Abderrahim; Aziz, Mohamed; Legssyer, Abdelkhaleq; Mekhfi, Hassane

    2010-10-01

    The goal of the present study is to test the effect of water extract (WE) of four medicinal plants used as antidiabetics in Eastern Morocco (Arbutus unedo: Au, Ammoïdes pusilla: Ap, Thymelaea hirsuta: Th, and Urtica dioïca: Ud). These plants are used in cooking to bring out the flavor in a dish or to complement it. The first experiment was realized in order to determine the antidiabetic effect of the WE of these plants during 5 weeks' treatment. Seven groups of Wistar rats were used: Healthy controls, neonatal streptozotocin (n-stz) induced-diabetic rats (90 mg/kg; intraperitoneally [i.p.]), n-stz + tolbutamide (400 mg/l), and 4 groups n-stz + WE of plants (400 mg/l, drink water). The percentages of Plasma glucose lowering effect were, respectively for Au, Ap, Th, Ud and tolbutamide: 31.6 % p<0.01, 27.4 % p<0.05, 38.2 % p<0.01, 13 % and 33.9 % p<0.05 when compared with untreated diabetic controls. In a second experiment, oral glucose tolerance tests were carried out in n-stz induced-diabetic rats. The i.p. administration of the water extract (WE) of Ap and Ud (150 mg/kg) 30 minutes before the glucose overload (2 g/kg) showed a significant reduction glycemia, respectively of 36 % at 60 min (p<0.05) and 50 % at 180 min (p<0.05) after glucose overload compared with controls. In contrast, the effect of WE of Au and Th (150 mg/kg, i.p.) was not significant. The in vitro study of glucose utilization by isolated rat hemidiaphragm suggests that these extracts in combination with insulin potentiate its activity and enhance the utilization of glucose. In conclusion, it seems that these plants possess antidiabetic activity.

  2. Antidiabetic effect of some medicinal plants of Oriental Morocco in neonatal non-insulin-dependent diabetes mellitus rats.

    PubMed

    Bnouham, Mohamed; Merhfour, Fatima Zahra; Ziyyat, Abderrahim; Aziz, Mohamed; Legssyer, Abdelkhaleq; Mekhfi, Hassane

    2010-10-01

    The goal of the present study is to test the effect of water extract (WE) of four medicinal plants used as antidiabetics in Eastern Morocco (Arbutus unedo: Au, Ammoïdes pusilla: Ap, Thymelaea hirsuta: Th, and Urtica dioïca: Ud). These plants are used in cooking to bring out the flavor in a dish or to complement it. The first experiment was realized in order to determine the antidiabetic effect of the WE of these plants during 5 weeks' treatment. Seven groups of Wistar rats were used: Healthy controls, neonatal streptozotocin (n-stz) induced-diabetic rats (90 mg/kg; intraperitoneally [i.p.]), n-stz + tolbutamide (400 mg/l), and 4 groups n-stz + WE of plants (400 mg/l, drink water). The percentages of Plasma glucose lowering effect were, respectively for Au, Ap, Th, Ud and tolbutamide: 31.6 % p<0.01, 27.4 % p<0.05, 38.2 % p<0.01, 13 % and 33.9 % p<0.05 when compared with untreated diabetic controls. In a second experiment, oral glucose tolerance tests were carried out in n-stz induced-diabetic rats. The i.p. administration of the water extract (WE) of Ap and Ud (150 mg/kg) 30 minutes before the glucose overload (2 g/kg) showed a significant reduction glycemia, respectively of 36 % at 60 min (p<0.05) and 50 % at 180 min (p<0.05) after glucose overload compared with controls. In contrast, the effect of WE of Au and Th (150 mg/kg, i.p.) was not significant. The in vitro study of glucose utilization by isolated rat hemidiaphragm suggests that these extracts in combination with insulin potentiate its activity and enhance the utilization of glucose. In conclusion, it seems that these plants possess antidiabetic activity. PMID:20154101

  3. A Novel Compound Rasatiol Isolated from Raphanus sativus Has a Potential to Enhance Extracellular Matrix Synthesis in Dermal Fibroblasts

    PubMed Central

    Roh, Seok-Seon; Park, Seung-Bae; Park, Seong-Mo; Choi, Byoung Wook; Lee, Min-Ho; Hwang, Yul-Lye; Kim, Chang Hun; Jeong, Hyun-Ah; Kim, Chang Deok

    2013-01-01

    Background The fibrous proteins of extracellular matrix (ECM) produced by dermal fibroblast contributes to the maintenance of connective tissue integrity. Objective This study is carried out to identify the bioactive ingredient from natural products that enhances ECM production in dermal fibroblasts. Methods Bioassay-directed fractionation was used to isolate the active ingredient from natural extracts. The effects of rasatiol (isolated from Raphanus sativus) on ECM production in primary cultured human dermal fibroblasts was investigated by enzyme linked immunosorbent assay and western blot analysis. Results Rasatiol accelerated fibroblast growth in a dose-dependent manner and increased the production of type 1 collagen, fibronectin and elastin. Phosphorylation of p42/44 extracellular signal-regulated kinase, p38 mitogen-activated protein kinase, and Akt was remarkably increased by rasatiol, indicating that enhanced ECM production is linked to the activation of intracellular signaling cascades. Conclusion These results indicate that rasatiol stimulates the fibrous components of ECM production, and may be applied to the maintenance of skin texture. PMID:24003274

  4. In Silico Molecular Docking and In Vitro Antidiabetic Studies of Dihydropyrimido[4,5-a]acridin-2-amines

    PubMed Central

    Bharathi, A.; Roopan, Selvaraj Mohana; Vasavi, C. S.; Munusami, Punnagai; Gayathri, G. A.; Gayathri, M.

    2014-01-01

    An in vitro antidiabetic activity on α-amylase and α–glucosidase activity of novel 10-chloro-4-(2-chlorophenyl)-12-phenyl-5,6-dihydropyrimido[4,5-a]acridin-2-amines (3a–3f) were evaluated. Structures of the synthesized molecules were studied by FT-IR, 1H NMR, 13C NMR, EI-MS, and single crystal X-ray structural analysis data. An in silico molecular docking was performed on synthesized molecules (3a–3f). Overall studies indicate that compound 3e is a promising compound leading to the development of selective inhibition of α-amylase and α-glucosidase. PMID:24991576

  5. Isolation, purification and characterization of novel antimicrobial compound 7-methoxy-2,2-dimethyl-4-octa-4',6'-dienyl-2H-napthalene-1-one from Penicillium sp. and its cytotoxicity studies.

    PubMed

    Kaur, Harpreet; Onsare, Jemimah Gesare; Sharma, Vishal; Arora, Daljit Singh

    2015-12-01

    Fungus isolated from soil has been evaluated for its antimicrobial activity which showed broad spectrum antimicrobial activity against all the pathogenic microorganisms used. Optimization was done by response surface methodology (RSM) to further optimize the medium which could further enhance the antimicrobial activity by 1.1-1.9 folds. Column chromatography was used to isolate the active compound which was characterized to be by various spectroscopic techniques such NMR, IR and LCMS and it was found to be apparently novel compound 7-methoxy-2,2-dimethyl-4-octa-4',6'-dienyl-2 H -napthalene-1-one. MIC of the active compound ranged from (0.5-15 µg/mL which was found to be comparable with the standard antibiotics. Viable cell count studies of the active compound showed it to be bactericidal in nature. Further, the compound when tested for its biosafety was found neither to be cytotoxic nor mutagenic. Cytotoxicity studies of the compound on cancer cell lines showed a valuable cytotoxic potential against all tested human cancer cell lines. Further, the compound induces apoptosis in lung cancer (A549) cells reveled by increase the distribution of nuclear DNA in Sub G1 phase as observed in flow cytometry. The study demonstrated that an apparently novel compound isolated from Penicillium sp. seems to be a stable and potent antimicrobial.

  6. Purple corn (Zea mays L.) phenolic compounds profile and its assessment as an agent against oxidative stress in isolated mouse organs.

    PubMed

    Ramos-Escudero, Fernando; Muñoz, Ana María; Alvarado-Ortíz, Carlos; Alvarado, Ángel; Yáñez, Jaime A

    2012-02-01

    This study was designed to determine the contents of total polyphenols, flavonoids, flavonols, flavanols, and anthocyanins of purple corn (Zea mays L.) extracts obtained with different methanol:water concentrations, acidified with 1% HCl (1 N). Another objective was to determine the antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and deoxyribose assay, individual phenolic compounds by high-performance liquid chromatography (HPLC), and endogenous antioxidant enzyme (superoxide dismutase [SOD], catalase [CAT], and total peroxidase [TPX]) activity and lipid peroxidation activity (thiobarbituric acid-reactive substances [TBARS] assay) in isolated mouse organs. Overall, the highest total content of polyphenols, anthocyanins, flavonoids, flavonols, and flavanols was obtained with the 80:20 methanol:water extract, acidified with 1% HCl (1 N). The 50% inhibitory concentration values obtained by the DPPH and ABTS assays with this extract were 66.3 μg/mL and 250 μg/mL, respectively. The antioxidant activity by the FRAP assay was 26.1 μM Trolox equivalents/g, whereas the deoxyribose assay presented 93.6% inhibition. Because of these results, the 80:20 methanol:water extract, acidified with 1% HCl (1 N), was used for the remaining tests. Eight phenolic compounds were identified by HPLC: chlorogenic acid, caffeic acid, rutin, ferulic acid, morin, quercetin, naringenin, and kaempferol. Furthermore, it was observed that the purple corn extract was capable of significantly reducing lipid peroxidation (lower malondialdehyde [MDA] concentrations by the TBARS assay) and at the same time increasing endogenous antioxidant enzyme (CAT, TPX, and SOD) activities in isolated mouse kidney, liver, and brain. On the basis of the results, it was concluded that the purple corn extract contained various bioactive phenolic compounds that exhibited considerable in vitro

  7. Purple corn (Zea mays L.) phenolic compounds profile and its assessment as an agent against oxidative stress in isolated mouse organs.

    PubMed

    Ramos-Escudero, Fernando; Muñoz, Ana María; Alvarado-Ortíz, Carlos; Alvarado, Ángel; Yáñez, Jaime A

    2012-02-01

    This study was designed to determine the contents of total polyphenols, flavonoids, flavonols, flavanols, and anthocyanins of purple corn (Zea mays L.) extracts obtained with different methanol:water concentrations, acidified with 1% HCl (1 N). Another objective was to determine the antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and deoxyribose assay, individual phenolic compounds by high-performance liquid chromatography (HPLC), and endogenous antioxidant enzyme (superoxide dismutase [SOD], catalase [CAT], and total peroxidase [TPX]) activity and lipid peroxidation activity (thiobarbituric acid-reactive substances [TBARS] assay) in isolated mouse organs. Overall, the highest total content of polyphenols, anthocyanins, flavonoids, flavonols, and flavanols was obtained with the 80:20 methanol:water extract, acidified with 1% HCl (1 N). The 50% inhibitory concentration values obtained by the DPPH and ABTS assays with this extract were 66.3 μg/mL and 250 μg/mL, respectively. The antioxidant activity by the FRAP assay was 26.1 μM Trolox equivalents/g, whereas the deoxyribose assay presented 93.6% inhibition. Because of these results, the 80:20 methanol:water extract, acidified with 1% HCl (1 N), was used for the remaining tests. Eight phenolic compounds were identified by HPLC: chlorogenic acid, caffeic acid, rutin, ferulic acid, morin, quercetin, naringenin, and kaempferol. Furthermore, it was observed that the purple corn extract was capable of significantly reducing lipid peroxidation (lower malondialdehyde [MDA] concentrations by the TBARS assay) and at the same time increasing endogenous antioxidant enzyme (CAT, TPX, and SOD) activities in isolated mouse kidney, liver, and brain. On the basis of the results, it was concluded that the purple corn extract contained various bioactive phenolic compounds that exhibited considerable in vitro

  8. Purple Corn (Zea mays L.) Phenolic Compounds Profile and Its Assessment as an Agent Against Oxidative Stress in Isolated Mouse Organs

    PubMed Central

    Ramos-Escudero, Fernando; Muñoz, Ana María; Alvarado-Ortíz, Carlos; Alvarado, Ángel

    2012-01-01

    Abstract This study was designed to determine the contents of total polyphenols, flavonoids, flavonols, flavanols, and anthocyanins of purple corn (Zea mays L.) extracts obtained with different methanol:water concentrations, acidified with 1% HCl (1 N). Another objective was to determine the antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and deoxyribose assay, individual phenolic compounds by high-performance liquid chromatography (HPLC), and endogenous antioxidant enzyme (superoxide dismutase [SOD], catalase [CAT], and total peroxidase [TPX]) activity and lipid peroxidation activity (thiobarbituric acid–reactive substances [TBARS] assay) in isolated mouse organs. Overall, the highest total content of polyphenols, anthocyanins, flavonoids, flavonols, and flavanols was obtained with the 80:20 methanol:water extract, acidified with 1% HCl (1 N). The 50% inhibitory concentration values obtained by the DPPH and ABTS assays with this extract were 66.3 μg/mL and 250 μg/mL, respectively. The antioxidant activity by the FRAP assay was 26.1 μM Trolox equivalents/g, whereas the deoxyribose assay presented 93.6% inhibition. Because of these results, the 80:20 methanol:water extract, acidified with 1% HCl (1 N), was used for the remaining tests. Eight phenolic compounds were identified by HPLC: chlorogenic acid, caffeic acid, rutin, ferulic acid, morin, quercetin, naringenin, and kaempferol. Furthermore, it was observed that the purple corn extract was capable of significantly reducing lipid peroxidation (lower malondialdehyde [MDA] concentrations by the TBARS assay) and at the same time increasing endogenous antioxidant enzyme (CAT, TPX, and SOD) activities in isolated mouse kidney, liver, and brain. On the basis of the results, it was concluded that the purple corn extract contained various bioactive phenolic compounds that exhibited

  9. [Primary combined oral antidiabetic therapy in type-2 diabetes mellitus].

    PubMed

    Winkler, Gábor; Baranyi, Eva

    2002-10-27

    New target values of the metabolic control and recent directions in the therapeutic strategies of type 2 diabetes mellitus are overviewed. Attention is called to the atherogenic effect of blood glucose elevations exceeding physiological level, even when only post-prandial and with short duration. The significance of early phase prandial insulin secretion in the metabolic state is underlined, and the related new therapeutic possibilities are discussed. Practical guidelines are given to the introduction of oral antidiabetic therapy, and the importance of the early, aggressive, combined treatment with a complex mechanism of action is emphasized.

  10. Pain‑relieving effect of a compound isolated from white peony root oral liquid on acute radiation‑induced esophagitis.

    PubMed

    Wang, Zhiyu; Shen, Li; Li, Xing; Shu, Xin; Shan, Baoen; Zhang, Li; Gong, Yanjun; Dong, Zhiming

    2013-06-01

    Acute radiation‑induced esophagitis (ARIE) is a common complication of radiotherapy. The aim of this study was to clarify the molecular mechanism of pain relief by the compound of white peony root oral liquid (cWPROL) in ARIE. An animal model of ARIE was established and either cWPROL or a mixture of lidocaine, dexamethasone and gentamycin (mLDG) was administered. We indirectly observed rat symptoms of pain by recording the weight of food and the volume of water consumed by the rats, along with changes in body weight. Additionally, the expression levels of substance P (SP) in the esophageal tissues were detected by immunohistochemistry. It was demonstrated that cWPROL was able to release the pain of ARIE by decreasing the expression of SP; this may be one of the molecular mechanisms via which cWPROL induces pain relief.

  11. Phytotoxic Effects and Phytochemical Fingerprinting of Hydrodistilled Oil, Enriched Fractions, and Isolated Compounds Obtained from Cryptocarya massoy (Oken) Kosterm. Bark.

    PubMed

    Rolli, Enrico; Marieschi, Matteo; Maietti, Silvia; Guerrini, Alessandra; Grandini, Alessandro; Sacchetti, Gianni; Bruni, Renato

    2016-01-01

    The hydrodistilled oil of Cryptocarya massoy bark was characterized by GC-FID and GC/MS analyses, allowing the identification of unusual C10 massoia lactone (3, 56.2%), C12 massoia lactone (4, 16.5%), benzyl benzoate (1, 12.7%), C8 massoia lactone (3.4%), δ-decalactone (5, 1.5%), and benzyl salicylate (2, 1.8%) as main constituents. The phytotoxic activities of the oil, three enriched fractions (lactone-rich, ester-rich, and sesquiterpene-rich), and four constituents (compounds 1, 2, 5, and δ-dodecalactone (6)) against Lycopersicon esculentum and Cucumis sativus seeds and seedlings were screened. At a concentration of 1000 μl/l, the essential oil and the massoia lactone-rich fraction caused a complete inhibition of the germination of both seeds, and, when applied on tomato plantlets, they induced an 85 and 100% dieback, respectively. These performances exceeded those of the well-known phytotoxic essential oils of Syzygium aromaticum and Cymbopogon citratus, already used in commercial products for the weed and pest management. The same substances were also evaluated against four phytopathogenic bacteria and ten phytopathogenic fungi, providing EC50 values against the most susceptible strains in the 100-500 μl/l range for the essential oil and in the 10-50 μl/l range for compound 6 and the lactone-rich fraction. The phytotoxic behavior was related mainly to massoia lactones and benzyl esters, while a greater amount of 6 may infer a good activity against some phytopathogenic fungi. Further investigations of these secondary metabolites are warranted, to evaluate their use as natural herbicides. PMID:26765353

  12. Design, Synthesis and Pharmacological Evaluation of Novel Vanadium-Containing Complexes as Antidiabetic Agents

    PubMed Central

    Fedorova, Elena V.; Buryakina, Anna V.; Zakharov, Alexey V.; Filimonov, Dmitry A.; Lagunin, Alexey A.; Poroikov, Vladimir V.

    2014-01-01

    Based on the data about structure and antidiabetic activity of twenty seven vanadium and zinc coordination complexes collected from literature we developed QSAR models using the GUSAR program. These QSAR models were applied to 10 novel vanadium coordination complexes designed in silico in order to predict their hypoglycemic action. The five most promising substances with predicted potent hypoglycemic action were selected for chemical synthesis and pharmacological evaluation. The selected coordination vanadium complexes were synthesized and tested in vitro and in vivo for their hypoglycemic activities and acute rat toxicity. Estimation of acute rat toxicity of these five vanadium complexes was performed using a freely available web-resource (http://way2drug.com/GUSAR/acutoxpredict.html). It has shown that the selected compounds belong to the class of moderate toxic pharmaceutical agents, according to the scale of Hodge and Sterner. Comparison with the predicted data has demonstrated a reasonable correspondence between the experimental and predicted values of hypoglycemic activity and toxicity. Bis{tert-butyl[amino(imino)methyl]carbamato}oxovanadium (IV) and sodium(2,2′-Bipyridyl)oxo-diperoxovanadate(V) octahydrate were identified as the most potent hypoglycemic agents among the synthesized compounds. PMID:25057899

  13. In vivo Studies on Antidiabetic Plants Used in South African Herbal Medicine

    PubMed Central

    J. Afolayan, Anthony; O. Sunmonu, Taofik

    2010-01-01

    Diabetes is one of the most common metabolic disorders worldwide. It is a major health problem with its frequency increasing every day in most countries. The disease is generally believed to be incurable; and the few orthodox drugs available to manage the disease are not readily affordable to the poor. Based on the historical success of natural products as antidiabetic agents and the ever increasing need for new antidiabetics, a number of South African medicinal plants have been evaluated for their antidiabetic properties. In this article, we review the major studies conducted based on ethnobotanical surveys carried out between 2005 and 2008 in South Africa on plants that are traditionally used for the treatment of diabetes. Overall, the results of the studies conducted confirmed the potential of South African medicinal plants in antidiabetic drug discovery and identified a number of promising taxa for further in vivo investigation as plant-based antidiabetic agents. PMID:20838564

  14. Therapeutic Phytogenic Compounds for Obesity and Diabetes

    PubMed Central

    Jung, Hee Soong; Lim, Yun; Kim, Eun-Kyoung

    2014-01-01

    Natural compounds have been used to develop drugs for many decades. Vast diversities and minimum side effects make natural compounds a good source for drug development. However, the composition and concentrations of natural compounds can vary. Despite this inconsistency, half of the Food and Drug Administration (FDA)-approved pharmaceuticals are natural compounds or their derivatives. Therefore, it is essential to continuously investigate natural compounds as sources of new pharmaceuticals. This review provides comprehensive information and analysis on natural compounds from plants (phytogenic compounds) that may serve as anti-obesity and/or anti-diabetes therapeutics. Our growing understanding and further exploration of the mechanisms of action of the phytogenic compounds may afford opportunities for development of therapeutic interventions in metabolic diseases. PMID:25421245

  15. Potent block of potassium currents in rat isolated sympathetic neurones by the uncharged form of amitriptyline and related tricyclic compounds.

    PubMed Central

    Wooltorton, J. R.; Mathie, A.

    1995-01-01

    1. The block of K+ currents by amitriptyline and the related tricyclic compounds cyproheptadine and dizocilpine was studied in dissociated rat sympathetic neurones by whole-cell voltage-clamp recording. 2. Cyproheptadine (30 microM) inhibited the delayed-rectifier current (Kv) by 92% and the transient current (KA) by 43%. For inhibition of Kv, cyproheptaidine had a KD of 2.2 microM. Dizocilpine (30 microM) inhibited Kv by 26% and KA by 22%. The stereoisomers of dizocilpine were equally potent at blocking Kv and KA. 3. Amitriptyline, a weak base, was significantly more effective in blocking Kv at pH 9.4 (KD = 0.46 microM) where the ratio of charged to uncharged drug was 50:50 compared with pH 7.4 (KD = 11.9 microM) where the ratio was 99:1. 4. N-methylamitriptyline (10 microM), the permanently charged analogue of amitriptyline, inhibited Kv by only 2% whereas in the same cells amitriptyline (10 microM) inhibited Kv by 36%. 5. Neither amitriptyline nor N-methylamitriptyline had a detectable effect on Kv when added to the intracellular solution. 6. It is concluded that the uncharged form of amitriptyline is approximately one hundred times more potent in blocking Kv than the charged form. However, this does not seem to be due to uncharged amitriptyline having better access to an intracellular binding site. PMID:8564248

  16. Isolation and characterization of nanosheets containing few layers of the Aurivillius family of oxides and metal-organic compounds

    NASA Astrophysics Data System (ADS)

    Sreedhara, M. B.; Prasad, B. E.; Moirangthem, Monali; Murugavel, R.; Rao, C. N. R.

    2015-04-01

    Nanosheets containing few-layers of ferroelectric Aurivillius family of oxides, Bi2An-1BnO3n+3 (where A=Bi3+, Ba2+ etc. and B=Ti4+, Fe3+ etc.) with n=3, 4, 5, 6 and 7 have been prepared by reaction with n-butyllithium, followed by exfoliation in water. The few-layer samples have been characterized by Tyndall cones, atomic force microscopy, optical spectroscopy and other techniques. The few-layer species have a thickness corresponding to a fraction of the c-parameter along which axis the perovskite layers are stacked. Magnetization measurements have been carried out on the few-layer samples containing iron. Few-layer species of a few layered metal-organic compounds have been obtained by ultrasonication and characterized by Tyndall cones, atomic force microscopy, optical spectroscopy and magnetic measurements. Significant changes in the optical spectra and magnetic properties are found in the few-layer species compared to the bulk samples. Few-layer species of the Aurivillius family of oxides may find uses as thin layer dielectrics in photovoltaics and other applications.

  17. Increased Flavonoid Compounds from Fermented Houttuynia cordata using Isolated Six of Bacillus from Traditionally Fermented Houttuynia cordata.

    PubMed

    Kwon, Ryun Hee; Ha, Bae Jin

    2012-06-01

    Flavonoids, which form a major component in Houttuynia cordata Thunb., display a wide range of pharmacological activities. The expression of plant flavonoids is partly regulated by fermentation. Therefore, we studied the effects of fermentation on H. cordata in order to identify the strains present during the fermentation process, and to determine whether fermented H. cordata could be used as a probiotic. Our results showed that all 6 of the bacterial strains isolated from fermented H. cordata (FHC) belonged to the genus Bacillus. As expected, fermenting H cordata also increased the flavonoid content as increases were observed in the levels of rutin, quercitrin, and quercetin. To test the effects of fermentation, we treated LPS-stimulated RAW264.7 cells with non-fermented H. cordata extracts (HCE) or FHC extracts (FHCE). Compared to the HCE-treated cells, the FHCE-treated cells showed increased viability. No cytotoxic effects were detected in the FHCE-treated groups in the 2 cell lines used in the study, namely, RAW264.7 and RBL-2H3. FHCE-treated HepG2 cells showed decreased growth, compared to HCE-treated HepG2 cells. These results indicate that the fermented H. cordata predominantly contained Bacillus strains. Furthermore, FHCE are able to prevent LPS-induced inflammatory effects and inhibit the growth of HepG2 cells. PMID:24278599

  18. Roles of obese-insulin resistance and anti-diabetic drugs on the heart with ischemia-reperfusion injury.

    PubMed

    Apaijai, Nattayaporn; Chattipakorn, Siriporn C; Chattipakorn, Nipon

    2014-12-01

    The incidence of obesity with insulin resistance is increasing worldwide. This condition is also known as a risk factor of coronary artery disease and associated with increased arrhythmias, impaired left ventricular function, and increased infarct size during cardiac ischemia-reperfusion (I/R) injury. The proposed mechanisms are due to impaired glucose utilization and pro-survival signaling molecules, and increased inflammatory cytokines, which have been demonstrated in the I/R hearts in various models of obese-insulin resistance. However, the cardiac effects of diets in the I/R heart are still unsettled since several studies reported that high-caloric diet consumption might protect the heart from I/R injury. Although several therapeutic strategies such as anti-diabetic drugs, natural compounds as well as treadmill exercise have been proposed to exert cardioprotection in the I/R heart in obese-insulin resistant animals, some interventions including ischemic post-conditioning failed to protect the heart from I/R injury. In this comprehensive review, reports from both genetic deletion and dietary-induced obese-insulin resistant animal models regarding the effects of obese-insulin resistance on metabolic parameters, cardiac function, infarct size, and molecular mechanisms under I/R injury are summarized. Moreover, the effects of anti-diabetic drugs and other pharmacological interventions on these parameters in an obese-insulin resistant model under I/R injury are also comprehensively summarized and discussed.

  19. Antidiabetic activity of flower buds of Michelia champaca Linn

    PubMed Central

    Jarald, E. Edwin; Joshi, S.B.; Jain, D.C.

    2008-01-01

    Objective: To identify the antihyperglycemic activity of various extracts, petroleum ether (60-80°), chloroform, acetone, ethanol, aqueous and crude aqueous, of the flower buds of Michelia champaca, and to identify the antidiabetic activity of active antihyperglycemic extract. Materials and Methods: Plant extracts were tested for antihyperglycemic activity in glucose overloaded hyperglycemic rats. The effective antihyperglycemic extract was tested for its hypoglycemic activity at two-dose levels, 200 and 400 mg/kg respectively. To confirm its utility in the higher model, the effective extract of M. champaca was subjected to antidiabetic study in alloxan induced diabetic model at two dose levels, 200 and 400 mg/kg respectively. The biochemical parameters, glucose, urea, creatinine, serum cholesterol, serum triglyceride, high density lipoprotein, low density lipoprotein, hemoglobin and glycosylated hemoglobin were also assessed in the experimental animals. Results: The ethanolic extract of M. champaca exhibited significant antihyperglycemic activity but did not produce hypoglycemia in fasted normal rats. Apart from this extract, the crude aqueous and petroleum ether extracts were found active only at the end of the first hour. Treatment of diabetic rats with ethanolic extract of this plant restored the elevated biochemical parameters significantly (P<0.05) (P<0.01) and the activity was found dose dependent. Conclusion: This study supports the traditional claim and the ethanolic extract of this plant could be added in traditional preparations for the ailment of various diabetes-associated complications. PMID:21279181

  20. Antidiabetic therapy in post kidney transplantation diabetes mellitus.

    PubMed

    Werzowa, Johannes; Säemann, Marcus; Haidinger, Michael; Krebs, Michael; Hecking, Manfred

    2015-07-01

    Post-transplantation diabetes mellitus (PTDM) is a common complication after kidney transplantation that affects up to 40% of kidney transplant recipients. By pathogenesis, PTDM is a diabetes form of its own, and may be characterised by a sudden, drug-induced deficiency in insulin secretion rather than worsening of insulin resistance over time. In the context of deteriorating allograft function leading to a re-occurrence of chronic kidney disease after transplantation, pharmacological interventions in PTDM patients deserve special attention. In the present review, we aim at presenting the current evidence regarding efficacy and safety of the modern antidiabetic armamentarium. Specifically, we focus on incretin-based therapies and insulin treatment, besides metformin and glitazones, and discuss their respective advantages and pitfalls. Although recent pilot trials are available in both prediabetes and PTDM, further studies are warranted to elucidate the ideal timing of various antidiabetics as well as its long-term impact on safety, glucose metabolism and cardiovascular outcomes in kidney transplant recipients.

  1. Anti-Diabetic Effects of Madecassic Acid and Rotundic Acid.

    PubMed

    Hsu, Yuan-Man; Hung, Yi-chih; Hu, Lihong; Lee, Yi-ju; Yin, Mei-chin

    2015-12-01

    Anti-diabetic effects of madecassic acid (MEA) and rotundic acid (RA) were examined. MEA or RA at 0.05% or 0.1% was supplied to diabetic mice for six weeks. The intake of MEA, not RA, dose-dependently lowered plasma glucose level and increased plasma insulin level. MEA, not RA, intake dose-dependently reduced plasminogen activator inhibitor-1 activity and fibrinogen level; as well as restored antithrombin-III and protein C activities in plasma of diabetic mice. MEA or RA intake decreased triglyceride and cholesterol levels in plasma and liver. Histological data agreed that MEA or RA intake lowered hepatic lipid droplets, determined by ORO stain. MEA intake dose-dependently declined reactive oxygen species (ROS) and oxidized glutathione levels, increased glutathione content and maintained the activity of glutathione reductase and catalase in the heart and kidneys of diabetic mice. MEA intake dose-dependently reduced interleukin (IL)-1β, IL-6, tumor necrosis factor-α and monocyte chemoattractant protein-1 levels in the heart and kidneys of diabetic mice. RA intake at 0.1% declined cardiac and renal levels of these inflammatory factors. These data indicated that MEA improved glycemic control and hemostatic imbalance, lowered lipid accumulation, and attenuated oxidative and inflammatory stress in diabetic mice. Thus, madecassic acid could be considered as an anti-diabetic agent. PMID:26633490

  2. Medicinal plants of India with anti-diabetic potential.

    PubMed

    Grover, J K; Yadav, S; Vats, V

    2002-06-01

    Since ancient times, plants have been an exemplary source of medicine. Ayurveda and other Indian literature mention the use of plants in treatment of various human ailments. India has about 45000 plant species and among them, several thousands have been claimed to possess medicinal properties. Research conducted in last few decades on plants mentioned in ancient literature or used traditionally for diabetes have shown anti-diabetic property. The present paper reviews 45 such plants and their products (active, natural principles and crude extracts) that have been mentioned/used in the Indian traditional system of medicine and have shown experimental or clinical anti-diabetic activity. Indian plants which are most effective and the most commonly studied in relation to diabetes and their complications are: Allium cepa, Allium sativum, Aloe vera, Cajanus cajan, Coccinia indica, Caesalpinia bonducella, Ficus bengalenesis, Gymnema sylvestre, Momordica charantia, Ocimum sanctum, Pterocarpus marsupium, Swertia chirayita, Syzigium cumini, Tinospora cordifolia and Trigonella foenum graecum. Among these we have evaluated M. charantia, Eugenia jambolana, Mucuna pruriens, T. cordifolia, T. foenum graecum, O. sanctum, P. marsupium, Murraya koeingii and Brassica juncea. All plants have shown varying degree of hypoglycemic and anti-hyperglycemic activity. PMID:12020931

  3. A pharmacological appraisal of medicinal plants with antidiabetic potential

    PubMed Central

    Khan, Vasim; Najmi, Abul Kalam; Akhtar, Mohd.; Aqil, Mohd.; Mujeeb, Mohd.; Pillai, K. K.

    2012-01-01

    Diabetes mellitus is a complicated metabolic disorder that has gravely troubled the human health and quality of life. Conventional agents are being used to control diabetes along with lifestyle management. However, they are not entirely effective and no one has ever been reported to have fully recovered from diabetes. Numerous medicinal plants have been used for the management of diabetes mellitus in various traditional systems of medicine worldwide as they are a great source of biological constituents and many of them are known to be effective against diabetes. Medicinal plants with antihyperglycemic activities are being more desired, owing to lesser side-effects and low cost. This review focuses on the various plants that have been reported to be effective in diabetes. A record of various medicinal plants with their established antidiabetic and other health benefits has been reported. These include Allium sativa, Eugenia jambolana, Panax ginseng, Gymnema sylvestre, Momrodica charantia, Ocimum sanctum, Phyllanthus amarus, Pterocarpus marsupium, Trigonella foenum graecum and Tinospora cordifolia. All of them have shown a certain degree of antidiabetic activity by different mechanisms of action. PMID:22368396

  4. Important Aspects of Post-Prandial Antidiabetic Drug, Acarbose.

    PubMed

    Singla, Rajeev Kumar; Singh, Radha; Dubey, Ashok Kumar

    2016-01-01

    Acarbose, a well known and efficacious α-amylase and α-glucosidase inhibitor, is a postprandial acting antidiabetic drug. DNS-based α-amylase inhibitory assays showed that use of acarbose at concentrations above 125 µg/ml resulted in release of reducing sugar in the reaction, an unexpected observation. Objective of the present study was to design experimental strategies to address this unusual finding. Acarbose was found to be susceptible to thermo-lysis. Further, besides being an inhibitor, it could also be hydrolyzed by porcine pancreatic α-amylase, but had weaker affinity for α - amylase compared to starch. GRIP docking was done for the mechanistic analysis of the active site in the enzyme for substrate, inhibitor and, inhibitor's metabolite (K2). Interaction between acarbose and α-amylase involved significant hydrogen binding compared to that of starch, producing a stronger enzyme-inhibitor complex. Further, docking analysis led us to predict the site on α-amylase where the inhibitor (acarbose) bound more tightly, which possibly affected the binding and hydrolysis of starch exerting its effective anti-diabetic function. PMID:27086787

  5. Anti-Diabetic Effects of Madecassic Acid and Rotundic Acid

    PubMed Central

    Hsu, Yuan-Man; Hung, Yi-chih; Hu, Lihong; Lee, Yi-ju; Yin, Mei-chin

    2015-01-01

    Anti-diabetic effects of madecassic acid (MEA) and rotundic acid (RA) were examined. MEA or RA at 0.05% or 0.1% was supplied to diabetic mice for six weeks. The intake of MEA, not RA, dose-dependently lowered plasma glucose level and increased plasma insulin level. MEA, not RA, intake dose-dependently reduced plasminogen activator inhibitor-1 activity and fibrinogen level; as well as restored antithrombin-III and protein C activities in plasma of diabetic mice. MEA or RA intake decreased triglyceride and cholesterol levels in plasma and liver. Histological data agreed that MEA or RA intake lowered hepatic lipid droplets, determined by ORO stain. MEA intake dose-dependently declined reactive oxygen species (ROS) and oxidized glutathione levels, increased glutathione content and maintained the activity of glutathione reductase and catalase in the heart and kidneys of diabetic mice. MEA intake dose-dependently reduced interleukin (IL)-1β, IL-6, tumor necrosis factor-α and monocyte chemoattractant protein-1 levels in the heart and kidneys of diabetic mice. RA intake at 0.1% declined cardiac and renal levels of these inflammatory factors. These data indicated that MEA improved glycemic control and hemostatic imbalance, lowered lipid accumulation, and attenuated oxidative and inflammatory stress in diabetic mice. Thus, madecassic acid could be considered as an anti-diabetic agent. PMID:26633490

  6. Antidiabetic and Antioxidant Activity of Scoparia dulcis Linn.

    PubMed

    Mishra, M R; Mishra, A; Pradhan, D K; Panda, A K; Behera, R K; Jha, S

    2013-09-01

    The hypoglycaemic activity of methanol extract of Scoparia dulcis was performed on both in vitro and in vivo models along with determination of total extractable polyphenol. Methanol extract of Scoparia dulcis contains 4.9% and water extract contains 3.2% of total extractable polyphenol. The antioxidant activity showed very promising result in both the tested methods that is 2,2-diphenyl-1-picrylhydrazyl and ferric ion reducing capacity. The antioxidant activity is directly correlated to the antidiabetic potential of drug. The two enzymes (amylase and glycosidase) found in intestine are responsible for the increasing postprandial glucose in body. In vitro model was performed on these enzymes and the results showed that methanol extract of Scoparia dulcis was effective to check the postprandial glucose level. The in vivo hypoglycaemic activity of methanol extract of Scoparia dulcis was performed on streptozotocin-induced diabetes mellitus showed significant inhibition of blood glucose level as compared to control and similar to that of standard glibenclamide. The overall data potentiates the traditional value of Scoparia dulcis as an antidiabetic drug. PMID:24403665

  7. Antidiabetic activity of a polyherbal formulation (DRF/AY/5001).

    PubMed

    Mandlik, Rahul V; Desai, Sandya K; Naik, Suresh R; Sharma, Gaurav; Kohli, R K

    2008-08-01

    The herbal formulation, DRF/AY/5001, elicits hypoglycemic/antidiabetic effects in both normal and experimentally induced hyperglycemic (epinephrine and alloxan) rats. Further, herbal formulation treatment can significantly alter the pattern of glucose tolerance in normal and diabetic rats. It is possible that the herbal formulation may act through both, pancreatic and extra-pancreatic mechanism(s). The DRF/AY/5001 also elicited a significant antioxidant effect in alloxan diabetic rats as reflected by its ability to inhibit lipid peroxidation and to elevate the enzymatic antioxidants in pancreatic tissue. The histopathological studies during the long-term treatment have shown to ameliorate the alloxan induced histological damage of islets of Langerhans. The inhibitory effects on biochemical and histological parameters induced by herbal formulation at a dose of 600 mg/kg were almost comparable to that of standard drug, glibenclamide (4 mg/kg). The present study demonstrates that herbal formulation exhibits promisisng antidiabetic activity and helps to maintain good glycemic and metabolic control.

  8. Antidiabetic Evaluation of Momordica charantia L Fruit Extracts

    PubMed Central

    Tahira, S; Hussain, F

    2014-01-01

    To investigate hypoglycaemic, hypolipidaemic and pancreatic beta cell regeneration activities of Momordica charantia L fruits (MC). Alloxan-induced diabetic rabbits were treated with methanolic and ethanolic MC extract. Effects of plant extracts and the drug glibenclamide on serum glucose, lipid profile and pancreatic beta cell were determined after two weeks of treatment. Serum glucose and lipid profiles were assayed by kit methods. Pancreatic tissue histopathology was performed to study pancreatic beta cell regeneration. Momordica charantia extracts produced significant hypoglycaemic effects (p < 0.05). Hypolipidaemic activity of MC was negligible. Momordica charantia supplementations were unable to normalize glucose and lipid profiles. Glibenclamide, a standard drug, not only lowered hyperglycaemia and hyperlipidaemia but also restored the normal levels. Regeneration of pancreatic beta cells by MC extracts was minimal, with fractional improvement produced by glibenclamide. The most significant finding of the present study was a 28% reduction in hyperglycaemia by MC ethanol extracts. To determine reliable antidiabetic potentials of MC, identification of the relevant antidiabetic components and underlying mechanisms is warranted. PMID:25429471

  9. Neuroprotective activity of parawixin 10, a compound isolated from Parawixia bistriata spider venom (Araneidae: Araneae) in rats undergoing intrahippocampal NMDA microinjection

    PubMed Central

    Fachim, Helene Aparecida; Mortari, Marcia Renata; Gobbo-Netto, Leonardo; dos Santos, Wagner Ferreira

    2015-01-01

    Background: Parawixia bistriata is a semi-colonial spider found mainly in southeastern of Brazil. Parawixin 10 (Pwx 10) a compound isolated from this spider venom has been demonstrated to act as neuroprotective in models of injury regulating the glutamatergic neurotransmission through glutamate transporters. Objectives: The aim of this work was to evaluate the neuroprotective effect of Pwx 10 in a rat model of excitotoxic brain injury by N-methyl-D-aspartate (NMDA) injection. Material and Methods: Male Wistar rats have been used, submitted to stereotaxic surgery for saline or NMDA microinjection into dorsal hippocampus. Two groups of animals were treated with Pwx 10. These treated groups received a daily injection of the Pwx 10 (2.5 mg/μL) in the right lateral ventricle into rats pretreated with NMDA, always at the same time, each one starting the treatment 1 h or 24 h. Nissl staining was performed for evaluating the extension and efficacy of the NMDA injury and the neuroprotective effect of Pwx 10. Results: The treatment with Pwx 10 showed neuroprotective effect, being most pronounced when the compound was administrated from 1 h after NMDA in all hippocampal subfields analyzed (CA1, CA3 and hilus). Conclusion: These results indicated that Pwx 10 may be a good template to develop therapeutic drugs for treating neurodegenerative diseases, reinforcing the importance of continuing studies on its effects in the central nervous system. PMID:26246735

  10. In vitro and in vivo assessment of the effect of antiprotozoal compounds isolated from Psoralea corylifolia against Ichthyophthirius multifiliis in fish

    PubMed Central

    Song, Kaige; Ling, Fei; Huang, Aiguo; Dong, Wenjing; Liu, Guanglu; Jiang, Chao; Zhang, Qizhong; Wang, Gaoxue

    2015-01-01

    Ichthyophthirius multifiliis, an external fish parasite, often causes significant economic damage to the aquaculture industry. Since the use of malachite green was banned, the search of alternative substance to control I. multifiliis infections becomes stringent. In present study, in vitro and in vivo anti-ich efficacies of isopsoralen and psoralidin, two active compounds isolated from methanol extract of Psoralea corylifolia by bioassay-guided fractionation based on the efficacy of anti-ich encysted tomonts, were evaluated. In vitro antiprotozoal efficacy of psoralidin is much better than that of isopsoralen. Psoralidin can kill all theronts at concentrations of 0.8 mg/L or more during 4 h exposure; and terminate reproduction of I. multifiliis post 6 h exposure of protomonts to 0.9 mg/L and encysted tomonts to 1.2 mg/L. In vivo trials showed that 5 h exposure of infected fish to 2.5 mg/L of psoralidin significantly reduced the number of theronts released from tomonts. Furthermore, we observed that a part of protomonts, collected from infected fish post treatment, presented characteristic morphological changes of apoptosis after staining with Annexin V-EGFP/propidium iodide, indicating the possible mechanism of psoralidin against I. multifiliis trophont in situ. On the basis of these results, psoralidin can be used as a potential lead compound for the development of commercial drug against I. multifiliis. PMID:26042195

  11. Centrifugal partition extraction in the pH-zone-refining displacement mode: an efficient strategy for the screening and isolation of biologically active phenolic compounds.

    PubMed

    Hamzaoui, Mahmoud; Renault, Jean-Hugues; Reynaud, Romain; Hubert, Jane

    2013-10-15

    Centrifugal partition extraction (CPE) was developed for the first time in the pH-zone-refining mode to fractionate a crude bark extract of the African tree Anogeissus leiocarpus Guill. & Perr. (Combretaceae). The fractionation process was performed at a flow rate of 20mL/min using a biphasic solvent system composed of methyl tert-butyl ether/acetonitrile/water (4:1:5, v/v/v) in the ascending mode. Sodium hydroxide (40mM) and trifluoroacetic acid (30mM) were used as retainer and displacer agents, respectively. In a single run of 67min, 3g of the initial crude extract were successfully separated into fractions selectively enriched in ionizable triterpenes, ellagic acid derivatives and flavonoids. The antioxidant potential of the initial crude extract, isolated compounds and fraction pools was also evaluated by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable free radical scavenging assay, providing an interesting view about the effect of the degree of substitution of ellagic acid derivatives on their radical scavenging activity. This study will demonstrate that centrifugal partition extraction used in the pH-zone-refining mode can be proposed as an efficient strategy for the rapid screening of natural phenolic compounds.

  12. Weak hybridization and isolated localized magnetic moments in the compounds CeT2Cd20 (T = Ni, Pd)

    SciTech Connect

    White, B. D.; Yazici, D.; Ho, P. -C.; Kanchanavatee, N.; Pouse, N.; Fang, Y.; Breindel, A. J.; Friedman, A. J.; Maple, M. B.

    2015-07-20

    Here, we report the physical properties of single crystals of the compounds CeT2Cd20 (T = Ni, Pd) that were grown in a molten Cd flux. Large separations of ~6.7- 6.8 Å between Ce ions favor the localized magnetic moments that are observed in measurements of the magnetization. The strength of the Ruderman-Kittel-Kasuya- Yosida magnetic exchange interaction between the localized moments is severely limited by the large Ce-Ce separations and by weak hybridization between localized Ce 4f and itinerant electron states. Measurements of electrical resistivity performed down to 0.138 K were unable to observe evidence for the emergence of magnetic order; however, magnetically-ordered ground states with very low transition temperatures are still expected in these compounds despite the isolated nature of the localized magnetic moments. Such a fragile magnetic order could be highly susceptible to tuning via applied pressure, but evidence for the emergence of magnetic order has not been observed so far in our measurements up to 2.5 GPa.

  13. Moracin C, A Phenolic Compound Isolated from Artocarpus heterophyllus, Suppresses Lipopolysaccharide-Activated Inflammatory Responses in Murine Raw264.7 Macrophages.

    PubMed

    Yao, Xue; Wu, Dang; Dong, Ningning; Ouyang, Ping; Pu, Jiaqian; Hu, Qian; Wang, Jingyuan; Lu, Weiqiang; Huang, Jin

    2016-07-25

    Artocarpus heterophyllus, a popular tropical fruit commonly known as the jackfruit tree, is normally planted in subtropical or tropical areas. Since a variety of phytochemicals isolated from A. heterophyllus have been found to possess potently anti-inflammatory, antiviral and antimalarial activities, researchers have devoted much interest to its potential pharmaceutical value. However, the exact mechanism underlying its anti-inflammatory activity is not well characterized. In this study, seven natural products isolated from A. heterophyllus, including 25-Hydroxycycloart-23-en-3-one (HY), Artocarpin (AR), Dadahol A (DA), Morachalcone A (MA), Artoheterophyllin B (AB), Cycloheterophyllin (CY) and Moracin C (MC) were collected. Lipopolysaccharide (LPS)-stimulated inflammatory response in RAW264.7 macrophages were used in this study. Among these compounds, MC significantly inhibited LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release without marked cytotoxicity. Furthermore, MC effectively reduced LPS stimulated up-regulation of mRNA and protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and serval pro-inflammatory cytokines (interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor α (TNF-α)). Mechanistic studies revealed that the anti-inflammatory effect of MC was associated with the activation of the mitogen activated protein kinases (MAPKs) (including p38, ERK and JNK) and nuclear factor-κB (NF-κB) pathways, especially reducing the nuclear translocation of NF-κB p65 subunit as revealed by nuclear separation experiment and confocal microscopy.

  14. Isolation of an extremely halophilic arhaeon Natrialba sp. C21 able to degrade aromatic compounds and to produce stable biosurfactant at high salinity.

    PubMed

    Khemili-Talbi, Souad; Kebbouche-Gana, Salima; Akmoussi-Toumi, Siham; Angar, Yassmina; Gana, Mohamed Lamine

    2015-11-01

    Natrialba sp. strain C21 was isolated from oil contaminated saline water in Ain Salah (Algeria) and has exhibited a good potential for degrading phenol (3% v/v), naphthalene (3% v/v), and pyrene (3% v/v) at high salinity with high growth, enzymatic activity and biosurfactant production. Successful metabolism of aromatic hydrocarbon compounds of the strain Natrialba sp. C21 appears to require the ortho-cleavage pathway. Indeed, assays of the key enzymes involved in the ring cleavage of catechol 1, 2-dioxygenase indicated that degradation of the phenol, naphthalene and pyrene by strain Natrialba sp. C21 was via the ortho-cleavage pathway. Cells grown on aromatic hydrocarbons displayed greater ortho-activities mainly towards catechol, while the meta-activity was very low. Besides, biosurfactants derived from the strain C21 were capable of effectively emulsifying both aromatic and aliphatic hydrocarbons and seem to be particularly promising since they have particular adaptations like the increased stability at high temperature and salinity conditions. This study clearly demonstrates for the first time that strain belonging to the genera Natrialba is able to grow at 25% (w/v) NaCl, utilizing phenol, naphthalene, and pyrene as the sole carbon sources. The results suggest that the isolated halophilic archaeon could be a good candidate for the remediation process in extreme environments polluted by aromatic hydrocarbons. Moreover, the produced biosurfactant offers a multitude of interesting potential applications in various fields of biotechnology.

  15. Screening alpha-glucosidase and alpha-amylase inhibitors from natural compounds by molecular docking in silico.

    PubMed

    Jhong, Chien-Hung; Riyaphan, Jirawat; Lin, Shih-Hung; Chia, Yi-Chen; Weng, Ching-Feng

    2015-01-01

    The alpha-glucosidase inhibitor is a common oral anti-diabetic drug used for controlling carbohydrates normally converted into simple sugars and absorbed by the intestines. However, some adverse clinical effects have been observed. The present study seeks an alternative drug that can regulate the hyperglycemia by down-regulating alpha-glucosidase and alpha-amylase activity by molecular docking approach to screen the hyperglycemia antagonist against alpha-glucosidase and alpha-amylase activities from the 47 natural compounds. The docking data showed that Curcumin, 16-hydroxy-cleroda-3,13-dine-16,15-olide (16-H), Docosanol, Tetracosanol, Antroquinonol, Berberine, Catechin, Quercetin, Actinodaphnine, and Rutin from 47 natural compounds had binding ability towards alpha-amylase and alpha-glucosidase as well. Curcumin had a better biding ability of alpha-amylase than the other natural compounds. Analyzed alpha-glucosidase activity reveals natural compound inhibitors (below 0.5 mM) are Curcumin, Actinodaphnine, 16-H, Quercetin, Berberine, and Catechin when compared to the commercial drug Acarbose (3 mM). A natural compound with alpha-amylase inhibitors (below 0.5 mM) includes Curcumin, Berberine, Docosanol, 16-H, Actinodaphnine/Tetracosanol, Catechin, and Quercetin when compared to Acarbose (1 mM). When taken together, the implication is that molecular docking is a fast and effective way to screen alpha-glucosidase and alpha-amylase inhibitors as lead compounds of natural sources isolated from medicinal plants.

  16. Analysis of Plant Growth-Promoting Effects of Fluorescent Pseudomonas Strains Isolated from Mentha piperita Rhizosphere and Effects of Their Volatile Organic Compounds on Essential Oil Composition.

    PubMed

    Santoro, Maricel V; Bogino, Pablo C; Nocelli, Natalia; Cappellari, Lorena Del Rosario; Giordano, Walter F; Banchio, Erika

    2016-01-01

    Many species or strains of the genus Pseudomonas have been characterized as plant growth promoting rhizobacteria (PGPR). We used a combination of phenotypic and genotypic techniques to analyze the community of fluorescent Pseudomonas strains in the rhizosphere of commercially grown Mentha piperita (peppermint). Biochemical techniques, Amplified rDNA Restriction Analysis (ARDRA), and 16S rRNA gene sequence analysis revealed that the majority of the isolated native fluorescent strains were P. putida. Use of two Repetitive Sequence-based PCR (rep-PCR) techniques, BOX-PCR and ERIC-PCR, allowed us to evaluate diversity among the native strains and to more effectively distinguish among them. PGPR activity was tested for the native strains and reference strain P. fluorescens WCS417r. Micropropagated M. piperita plantlets were exposed to microbial volatile organic compounds (mVOCs) emitted by the bacterial strains, and plant biomass parameters and production of essential oils (EOs) were measured. mVOCs from 11 of the native strains caused an increase in shoot fresh weight. mVOCs from three native strains (SJ04, SJ25, SJ48) induced changes in M. pierita EO composition. The mVOCs caused a reduction of metabolites in the monoterpene pathway, for example menthofuran, and an increase in menthol production. Menthol production is the primary indicator of EO quality. The mVOCs produced by native strains SJ04, SJ25, SJ48, and strain WCS417r were analyzed. The obtained mVOC chromatographic profiles were unique for each of the three native strains analyzed, containing varying hydrocarbon, aromatic, and alogenic compounds. The differential effects of the strains were most likely due to the specific mixtures of mVOCs emitted by each strain, suggesting a synergistic effect occurs among the compounds present.

  17. Analysis of Plant Growth-Promoting Effects of Fluorescent Pseudomonas Strains Isolated from Mentha piperita Rhizosphere and Effects of Their Volatile Organic Compounds on Essential Oil Composition.

    PubMed

    Santoro, Maricel V; Bogino, Pablo C; Nocelli, Natalia; Cappellari, Lorena Del Rosario; Giordano, Walter F; Banchio, Erika

    2016-01-01

    Many species or strains of the genus Pseudomonas have been characterized as plant growth promoting rhizobacteria (PGPR). We used a combination of phenotypic and genotypic techniques to analyze the community of fluorescent Pseudomonas strains in the rhizosphere of commercially grown Mentha piperita (peppermint). Biochemical techniques, Amplified rDNA Restriction Analysis (ARDRA), and 16S rRNA gene sequence analysis revealed that the majority of the isolated native fluorescent strains were P. putida. Use of two Repetitive Sequence-based PCR (rep-PCR) techniques, BOX-PCR and ERIC-PCR, allowed us to evaluate diversity among the native strains and to more effectively distinguish among them. PGPR activity was tested for the native strains and reference strain P. fluorescens WCS417r. Micropropagated M. piperita plantlets were exposed to microbial volatile organic compounds (mVOCs) emitted by the bacterial strains, and plant biomass parameters and production of essential oils (EOs) were measured. mVOCs from 11 of the native strains caused an increase in shoot fresh weight. mVOCs from three native strains (SJ04, SJ25, SJ48) induced changes in M. pierita EO composition. The mVOCs caused a reduction of metabolites in the monoterpene pathway, for example menthofuran, and an increase in menthol production. Menthol production is the primary indicator of EO quality. The mVOCs produced by native strains SJ04, SJ25, SJ48, and strain WCS417r were analyzed. The obtained mVOC chromatographic profiles were unique for each of the three native strains analyzed, containing varying hydrocarbon, aromatic, and alogenic compounds. The differential effects of the strains were most likely due to the specific mixtures of mVOCs emitted by each strain, suggesting a synergistic effect occurs among the compounds present. PMID:27486441

  18. Determination of the phenolic content and antioxidant potential of crude extracts and isolated compounds from leaves of Cordia multispicata and Tournefortia bicolor.

    PubMed

    Correia Da Silva, Thiago B; Souza, Vivian Karoline T; Da Silva, Ana Paula F; Lyra Lemos, Rosangela P; Conserva, Lucia M

    2010-01-01

    In this work, the total phenolic content and antioxidant activity of extracts and four flavonoids isolated from leaves of two Boraginaceae species (Cordia multispicata Cham. and Tournefortia bicolor Sw.) were evaluated using Folin-Ciocalteu reagent, DPPH free radical scavenging and inhibition of peroxidation of linoleic acid by FTC method. For comparison, ascorbic acid, alpha-tocopherol and BHT were used. In general, extracts from T. bicolor (68.8 +/- 0.001 to > 1000 mg/g) showed higher phenolic content than C. multispicata (66.1 +/- 0.009 to 231 +/- 0.07 mg/g), and also scavenged radicals (IC(50) 12.8 +/- 2.5 to 437 +/- 3.5 mg/L) and inhibited lipid peroxide formation (IC(50) 51.2 +/- 2.29 to 89 +/- 0.59 mg/L). For these extracts a good correlation between the phenolic content and antioxidant activity was observed, suggesting that T. bicolor is richer in phenolic compounds and that it could serve as a new source of natural antioxidants or nutraceuticals with potential applications. Chromatographic procedures monitored by antioxidant assays afforded seven compounds, which were identified by spectral analyses (IR, MS and 1D and 2D NMR) and comparison with reported data as being trans-phytol (1), taraxerol (2), 3,7,4'-trimethoxyflavone (3), 5,3'-dihydroxy-3,7,4'-trimethoxyflavone (4), quercetin (5), tiliroside (6), and rutin (7). Compounds (4-7) were also evaluated and were effective as DPPH quenching (IC(50) 7.7 +/- 3.6 to 79.3 +/- 3.4 mg/L) and as inhibition of lipid peroxidation (IC(50) 80.1 +/- 0.98 to 88.7 +/- 3.62 mg/L). This is the first report on the total phenolic content, radical-scavenging and antioxidant activities of these species.

  19. Analysis of Plant Growth-Promoting Effects of Fluorescent Pseudomonas Strains Isolated from Mentha piperita Rhizosphere and Effects of Their Volatile Organic Compounds on Essential Oil Composition

    PubMed Central

    Santoro, Maricel V.; Bogino, Pablo C.; Nocelli, Natalia; Cappellari, Lorena del Rosario; Giordano, Walter F.; Banchio, Erika

    2016-01-01

    Many species or strains of the genus Pseudomonas have been characterized as plant growth promoting rhizobacteria (PGPR). We used a combination of phenotypic and genotypic techniques to analyze the community of fluorescent Pseudomonas strains in the rhizosphere of commercially grown Mentha piperita (peppermint). Biochemical techniques, Amplified rDNA Restriction Analysis (ARDRA), and 16S rRNA gene sequence analysis revealed that the majority of the isolated native fluorescent strains were P. putida. Use of two Repetitive Sequence-based PCR (rep-PCR) techniques, BOX-PCR and ERIC-PCR, allowed us to evaluate diversity among the native strains and to more effectively distinguish among them. PGPR activity was tested for the native strains and reference strain P. fluorescens WCS417r. Micropropagated M. piperita plantlets were exposed to microbial volatile organic compounds (mVOCs) emitted by the bacterial strains, and plant biomass parameters and production of essential oils (EOs) were measured. mVOCs from 11 of the native strains caused an increase in shoot fresh weight. mVOCs from three native strains (SJ04, SJ25, SJ48) induced changes in M. pierita EO composition. The mVOCs caused a reduction of metabolites in the monoterpene pathway, for example menthofuran, and an increase in menthol production. Menthol production is the primary indicator of EO quality. The mVOCs produced by native strains SJ04, SJ25, SJ48, and strain WCS417r were analyzed. The obtained mVOC chromatographic profiles were unique for each of the three native strains analyzed, containing varying hydrocarbon, aromatic, and alogenic compounds. The differential effects of the strains were most likely due to the specific mixtures of mVOCs emitted by each strain, suggesting a synergistic effect occurs among the compounds present. PMID:27486441

  20. Inhibition of phosphatidylcholine biosynthesis and cell proliferation in Trypanosoma cruzi by ajoene, an antiplatelet compound isolated from garlic.

    PubMed

    Urbina, J A; Marchan, E; Lazardi, K; Visbal, G; Apitz-Castro, R; Gil, F; Aguirre, T; Piras, M M; Piras, R

    1993-06-22

    Ajoene [(E,Z)-4,5,9-trithiadodeca-1,6,11-triene 9-oxide], a potent antiplatelet compound derived from garlic, inhibits the proliferation of both epimastigotes and amastigotes of Trypanosoma cruzi, the causative agent of Chagas' disease. The growth of the epimastigote form was immediately arrested by 80 microM ajoene, while 100 microM induced cell lysis in 24 hr. In the amastigote form proliferating inside VERO cells, 40 microM ajoene was sufficient to eradicate the parasite from the host cells in 96 hr. Growth inhibition of the epimastigotes was accompanied by a gross alteration of the phospholipid composition of the treated cells in which phosphatidylcholine (PC), the major phospholipid class present in control cells, dropped to the least abundant phospholipid in cells treated with 60 microM ajoene for 96 hr, while its immediate precursor, phosphatidylethanolamine (PE), became the predominant species; this was correlated with a marked drop in the incorporation of [14C-U]acetate in PC and a corresponding increase in PE. Concomitant with the change in the phospholipid headgroup composition of the cells, the fatty acids esterified to this lipid fraction underwent a dramatic alteration due to the increase in the content of saturated fatty acids and a marked reduction in the content of linoleic (18:2) acid, which is the predominant fatty acid in control cells. We also found that ajoene inhibited the de novo synthesis of neutral lipids and, in particular, of sterols in the epimastigotes, but the resultant changes in the sterol composition were not sufficient to explain the antiproliferative effects of the drug. Electron-microscopy showed a concentration-dependent alteration of intracellular membranous structures, particularly the mitochondrion and endoplasmatic reticulum. The results suggest that one important factor associated with the antiproliferative effects of ajoene against T. cruzi is its specific alteration of the phospholipid composition of these cells.

  1. Pharmacological properties of beta-amyrin palmitate, a novel centrally acting compound, isolated from Lobelia inflata leaves.

    PubMed

    Subarnas, A; Tadano, T; Oshima, Y; Kisara, K; Ohizumi, Y

    1993-06-01

    Effects of beta-amyrin palmitate isolated from the leaves of Lobelia inflata were studied on the central nervous system of mice and were compared with those of antidepressant drugs, mianserin and imipramine. In the forced swimming test, beta-amyrin palmitate, like mianserin and imipramine, reduced the duration of immobility of mice significantly in a dose-dependent manner (5, 10 and 20 mg kg-1). beta-Amyrin palmitate (5, 10 and 20 mg kg-1) or mianserin (5, 10 and 20 mg kg-1) elicited a dose-related reduction in locomotor activity of mice and antagonized locomotor stimulation induced by methamphetamine. In contrast, imipramine (5, 10 and 20 mg kg-1) increased locomotor activity and potentiated methamphetamine-induced hyperactivity. beta-Amyrin palmitate showed no effect on reserpine-induced hypothermia, whilst mianserin (10 mg kg-1) and imipramine (10 and 20 mg kg-1) antagonized the reserpine-induced effect. Unlike imipramine, beta-amyrin palmitate and mianserin did not affect haloperidol-induced catalepsy, tetrabenazine-induced ptosis and apomorphine-induced stereotypy. beta-Amyrin palmitate and imipramine had no effects on the head-twitch response induced by 5-hydroxytryptophan, whereas mianserin (5, 10 and 20 mg kg-1) decreased it in a dose-dependent manner. A potentiating effect of beta-amyrin palmitate (5, 10 and 20 mg kg-1) on narcosis induced by sodium pentobarbitone was stronger than that of imipramine (10, 20 and 40 mg kg-1) but weaker than that of mianserin (2.5, 5 and 10 mg kg-1). These results suggest that beta-amyrin palmitate has similar properties in some respects to mianserin and might possess a sedative action.(ABSTRACT TRUNCATED AT 250 WORDS)

  2. Antimalarial drug interactions of compounds isolated from Kigelia africana (Bignoniaceae) and their synergism with artemether, against the multidrug-resistant W2mef Plasmodium falciparum strain.

    PubMed

    Zofou, Denis; Tene, Mathieu; Tane, Pierre; Titanji, Vincent P K

    2012-02-01

    For decades, drug resistance has been the major obstacle in the fight against malaria, and the search for new drugs together with the combination therapy constitutes the major approach in responding to this situation. The present study aims at assessing the in vitro antimalarial activity of four compounds isolated from Kigelia africana stem bark (atranorin - KAE1, specicoside - KAE7, 2β,3β,19α-trihydroxy-urs-12-20-en-28-oic acid - KAE3, and p-hydroxy-cinnamic acid - KAE10) and their drug interactions among themselves and their combination effects with quinine and artemether. The antiplasmodial activity and drug interactions were evaluated against the multidrug-resistant W2mef strain of Plasmodium falciparum using the parasite lactate dehydrogenase assay. Three of the four compounds tested were significantly active against W2mef: specicoside (IC(50) = 1.02 ± 0.17 μM), 2β,3β,19α-trihydroxy-urs-12-en-28-oic acid (IC(50) = 1.86 ± 0.15 μM) and atranorin (IC(50) = 1.78 ± 0.18 μM), whereas p-hydroxy-cinnamic acid showed a weak activity (IC(50) = 12.89 ± 0.87 μM). A slight synergistic effect was observed between atranorin and 2β,3β,19α-trihydroxy-urs-12-en-28-oic acid (Combination index, CI = 0.82) whereas the interaction between specicoside and p-hydroxy-cinnamic acid were instead antagonistic (CI = 2.67). All the three compounds showed synergistic effects with artemether, unlike the slight antagonistic interactions of atranorin and 2β,3β,19α-trihydroxy-urs-12-en-28-oic acid in combination with quinine. K. africana compounds are therefore likely to serve as leads in the development of new partner drugs in artemether-based combination therapy. PMID:21814840

  3. Isolation, purification, and characterization of antimicrobial compound 6-[1,2-dimethyl-6-(2-methyl-allyloxy)-hexyl]-3-(2-methoxy-phenyl)-chromen-4-one from Penicillium sp. HT-28.

    PubMed

    Kaur, Harpreet; Arora, Daljit Singh; Sharma, Vishal

    2014-08-01

    A fungal culture (Penicillium sp., HT-28), isolated from soil has been evaluated for its bioactivity, which showed broad spectrum antimicrobial activity and was effective against methicillin-resistant Staphylococcus aureus (MRSA) also. Statistical optimization of the medium by response surface methodology (RSM) enhanced the antimicrobial activity up to 1.8-fold. Column chromatography was used to isolate the active compound (A), which was characterized to be 6-[1,2-dimethyl-6-(2-methyl-allyloxy)-hexyl]-3-(2-methoxy-phenyl)-chromen-4-one by various spectroscopic techniques such as infrared (IR), (1)H and (13)C nuclear magnetic resonance (NMR) spectra, and mass spectroscopy. Minimum inhibitory concentration (MIC) of the active compound (A) ranged from 0.5 to 15 μg/mL. Viable cell count studies of the active compound (A) showed S. aureus, Escherichia coli, Staphylococcus epidermidis, and Salmonella typhimurium 1 to be the most sensitive. The compound retained its bioactivity after treating it at 100 °C for 1 h. Furthermore, the compound (A) when tested for its biosafety was found neither to be cytotoxic nor mutagenic. The study demonstrated that an apparently novel compound isolated from Penicillium sp. (HT-28) seems to be a stable and potent antimicrobial.

  4. Evaluation of anti-diabetic drugs by using silkworm, Bombyx mori.

    PubMed

    Matsumoto, Yasuhiko; Sekimizu, Kazuhisa

    2016-02-01

    Since diabetes patients are increasing in the world, establishment of a novel method for development of anti-diabetic drugs is desired. In this review, we describe recent results of our studies regarding diabetic model using silkworms for evaluation of anti-diabetic drugs for patients of both type I and type II diabetes. The use of the evaluation systems using silkworms is expected to contribute to reduction in cost and in the number of mammals sacrificed for screening of anti-diabetic drugs.

  5. Development and Phytochemical Characterization of High Polyphenol Red Lettuce with Anti-Diabetic Properties

    PubMed Central

    Cheng, Diana M.; Pogrebnyak, Natalia; Kuhn, Peter; Krueger, Christian G.; Johnson, William D.; Raskin, Ilya

    2014-01-01

    Polyphenol-rich Rutgers Scarlet Lettuce (RSL) (Lactuca sativa L.) was developed through somaclonal variation and selection in tissue culture. RSL may contain among the highest reported contents of polyphenols and antioxidants in the category of common fruits and vegetables (95.6 mg/g dry weight and 8.7 mg/g fresh weight gallic acid equivalents and 2721 µmol/g dry weight and 223 µmol/g fresh weight Trolox equivalents). Three main compounds accumulate at particularly high levels in RSL: chlorogenic acid, up to 27.6 mg/g dry weight, cyanidin malonyl-glucoside, up to 20.5 mg/g dry weight, and quercetin malonyl-glucoside, up to 35.7 mg/g dry weight. Major polyphenolic constituents of RSL have been associated with health promotion as well as anti-diabetic and/or anti-inflammatory activities. Daily oral administration of RSL (100 or 300 mg/kg) for up to eight days acutely reduced hyperglycemia and improved insulin sensitivity in high fat diet-induced obese hyperglycemic mice compared to vehicle (water) control. Data presented here support possible use of RSL as a functional food for the dietary management of diabetes. PMID:24637790

  6. Flavonoid derivative exerts an antidiabetic effect via AMPK activation in diet-induced obesity mice.

    PubMed

    Chen, Ying; Zhang, Chang; Jin, Mei-Na; Qin, Nan; Qiao, Wei; Yue, Xiao-Long; Duan, Hong-Quan; Niu, Wen-Yan

    2016-09-01

    In our previous study, a derivative of tiliroside, 3-O-[(E)-4-(4-ethoxyphenyl)-2-oxobut-3-en-1-yl]kaempferol (Fla-OEt) significantly enhanced glucose consumption in insulin resistant HepG2 cells. This article deals with the antihyperglycemic and antihyperlipidemic effects of Fla-OEt in diet-induced obesity (DIO) mice. Daily administration of Fla-OEt significantly decreased oral glucose tolerance test, intraperitoneal insulin tolerance test and serum lipids. Hyperinsulinemic-euglycemic clamp and the ratio of high-density-lipoprotein/low-density-lipoprotein with Fla-OEt treatment were increased comparing with high-fat diet (HFD) group, so lipid metabolism was improved. Histopathology examination showed that the Fla-OEt restored the damage of adipose tissues and liver in DIO mice. Moreover, compared with HFD group, Fla-OEt treatment significantly increased the phosphorylation of AMPK and ACC in adiposity tissues, liver, and muscles. The mechanism of its action might be the activation of AMPK pathway. It appears that Fla-OEt is worth further study for development as a lead compound for a potential antidiabetic agent.

  7. Uptake, translocation and possible biodegradation of the antidiabetic agent metformin by hydroponically grown Typha latifolia.

    PubMed

    Cui, Hao; Schröder, Peter

    2016-05-01

    The increasing load of pharmaceutical compounds has raised concerns about their potential residues in aquatic environments and ecotoxicity. Metformin (MET), a widely prescribed antidiabetic II medicine, has been detected in high concentration in sewage and in wastewater treatment effluents. An uptake and translocation study was carried out to assess the ultimate fate of MET in phytoremediation. MET was removed from media by Typha latifolia, and the removal processes followed first order kinetics. After 28 days, the removal efficiencies were in a range of 74.0±4.1-81.1±3.3%. In roots, MET concentration was increasing during the first two weeks of the experiment but thereafter decreasing. In contrast, MET concentration was continuously increasing in rhizomes and leaves. Bioaccumulation of MET in roots was much higher than in leaves and rhizomes. As degradation product of metformin in the plant, methylbiguanide (MBG) was detected whereas guanylurea was undetectable. Moreover, MBG concentration in roots was increasing with exposure time. An enzymatic degradation experiment showed the degradation rate followed the order of MET

  8. Antidiabetic Activity of Gnidia glauca and Dioscorea bulbifera: Potent Amylase and Glucosidase Inhibitors

    PubMed Central

    Ghosh, Sougata; Ahire, Mehul; Patil, Sumersing; Jabgunde, Amit; Bhat Dusane, Meenakshi; Joshi, Bimba N.; Pardesi, Karishma; Jachak, Sanjay; Dhavale, Dilip D.; Chopade, Balu A.

    2012-01-01

    Diabetes is a metabolic disorder affecting about 220 million people worldwide. One of the most critical complications of diabetes is post-prandial hyper-glycemia (PPHG). Glucosidase inhibitor and α-amylase inhibitors are class of compounds that help in managing PPHG. Low-cost herbal treatment is recommended due to their lesser side effect for treatment of diabetes. Two plants with significant traditional therapeutic potential, namely, Gnidia glauca and Dioscorea bulbifera, were tested for their efficiency to inhibit α-amylase and α-glucosidase. Stem, leaf, and flower of G. glauca and bulb of D. bulbifera were sequentially extracted with petroleum ether, ethyl acetate, and methanol as well as separately with 70% ethanol. Petroleum ether extract of flower of G. glauca was found to inhibit α-amylase significantly (78.56%). Extracts were further tested against crude murine pancreatic, small intestinal, and liver glucosidase enzyme which revealed excellent inhibitory properties. α-glucosidase inhibition provided a strong in vitro evidence for confirmation of both G. glauca and D. bulbifera as excellent antidiabetic remedy. This is the first report of its kind that provides a strong biochemical basis for management of type II diabetes using G. glauca and D. bulbifera. These results provide intense rationale for further in vivo and clinical study. PMID:21785651

  9. In vitro antidiabetic activity of various crude extracts of Boletus variipes

    NASA Astrophysics Data System (ADS)

    Muniandy, Sutha; Fazry, Shazrul; Daud, Fauzi; Senafi, Sahidan

    2015-09-01

    Diabetes mellitus is a complex metabolic disease that progressively spread worldwide and difficult to treat due to various physical and metabolic complications. Current treatment using synthetic drugs has lead to various undesirable side effects. Here we determined the effect of Boletus variipes extracts on diabetes related enzymes. In this study, hot water, cold water and methanol extracts of B. variipes were utilized in order to assess their in vitro antidiabetic activity by measuring the effect on α-amylase and α-glucosidase enzyme. Hot water extract possessed the highest inhibition activity of α-amylase and α-glucosidase in a concentration dependent manner with the IC50 value 87 mg/mL and 89 mg/mL respectively. The methanol extract also showed inhibition activity of α-amylase and α-glucosidase but significantly lower than the hot water extract. Whereas cold water extract did not show any inhibition activity towards both the enzymes. Therefore, it is hypothesized that the hot water extract of Boletus variipes contains bioactive compound that can inhibit alpha-amylase and alpha-glucosidase enzyme activity. At the request of all authors of the paper an updated version was published on 11 May 2016. The original version identified the species of mushroom as Boletus variipes, but new findings have proved the species of mushroom to be Boletus qriseipurpureus. The species name has been updated throughout the revised version of this paper.

  10. Comparative effects of sulfhydryl compounds on target organellae, nuclei and mitochondria, of hydroxylated fullerene-induced cytotoxicity in isolated rat hepatocytes.

    PubMed

    Nakagawa, Yoshio; Inomata, Akiko; Ogata, Akio; Nakae, Dai

    2015-12-01

    DNA damage and cytotoxicity induced by a hydroxylated fullerene [C60 (OH)24 ], which is a spherical nanomaterial and/or a water-soluble fullerene derivative, and their protection by sulfhydryl compounds were studied in freshly isolated rat hepatocytes. The exposure of hepatocytes to C60 (OH)24 at a concentration of 50 μM caused time (0 to 3 h)-dependent cell death accompanied by the formation of cell surface blebs, the loss of cellular levels of ATP and reduced glutathione, accumulation of glutathione disulfide, and induction of DNA fragmentation assayed using alkali single-cell agarose-gel electrophoresis. C60 (OH)24 -induced cytotoxicity was effectively prevented by pretreatment with sulfhydryl compounds. N-acetyl-L-cysteine (NAC), L-cysteine and L-methionine, at a concentration of 2.5 mM, ameliorated cell death, accompanied by a decrease in cellular ATP levels, formation of cell surface blebs, induction of reactive oxygen species (ROS) and loss of mitochondrial membrane potential caused by C60 (OH)24 . In addition, DNA fragmentation caused by C60 (OH)24 was also inhibited by NAC, whereas an antioxidant ascorbic acid did not affect C60 (OH)24 -induced cell death and DNA damage in rat hepatocytes. Taken collectively, these results indicate that incubation of rat hepatocytes with C60 (OH)24 elicits DNA damage, suggesting that nuclei as well as mitochondria are target sites of the hydroxylated fullerene; and induction of DNA damage and oxidative stress is ameliorated by an increase in cellular GSH levels, suggesting that the onset of toxic effects may be partially attributable to a thiol redox-state imbalance caused by C60 (OH)24 .

  11. Bioactivity-guided isolation of beta-sitosterol and some fatty acids as active compounds in the anxiolytic and sedative effects of Tilia americana var. mexicana.

    PubMed

    Aguirre-Hernández, Eva; Rosas-Acevedo, Hortensia; Soto-Hernández, Marcos; Martínez, Ana Laura; Moreno, Julia; González-Trujano, Ma Eva

    2007-09-01

    Tilia species have been used as anxiolytics for many years. In a previous study anxiolytic-like effects of a hexane extract of Tilia americana var. mexicana inflorescences were observed in experimental models in mice. To get additional insights into the neuroactive actions of this particular Tilia species, in this study we report a bioactivity guided-fractionation of the extract and separation by column chromatographic methods to isolate three fatty acids and a triterpene identified as beta-sitosterol as major constituents. Our results revealed that the crude extract at 10 and 30 mg/kg I. P. and some pooled fractions at the same dosages potentiated sodium pentobarbital-induced sleeping time and caused a significant increase in the time spent at the open-arm sides in the plus-maze test. A reduction in the exploratory behavioral pattern manifested as ambulatory activity, as well as head dipping and rearing tests was also observed. Further fractionation and purification yielded four major fractions containing fatty acids and beta-sitosterol as the active compounds. A dose-response curve of beta-sitosterol in the range 1 to 30 mg/kg doses indicated that this compound produced an anxiolytic-like action from 1 to 10 mg/kg and a sedative response when the dose was increased to 30 mg/kg, these effects resemble those produced by diazepam (0.1 mg/kg). Our results suggest that hexane extract of Tilia americana var. mexicana produces depressant actions on the central nervous system, at least in part, because of the presence of beta-sitosterol and some fatty acids that remain to be identified.

  12. Moracin C, A Phenolic Compound Isolated from Artocarpus heterophyllus, Suppresses Lipopolysaccharide-Activated Inflammatory Responses in Murine Raw264.7 Macrophages

    PubMed Central

    Yao, Xue; Wu, Dang; Dong, Ningning; Ouyang, Ping; Pu, Jiaqian; Hu, Qian; Wang, Jingyuan; Lu, Weiqiang; Huang, Jin

    2016-01-01

    Artocarpus heterophyllus, a popular tropical fruit commonly known as the jackfruit tree, is normally planted in subtropical or tropical areas. Since a variety of phytochemicals isolated from A. heterophyllus have been found to possess potently anti-inflammatory, antiviral and antimalarial activities, researchers have devoted much interest to its potential pharmaceutical value. However, the exact mechanism underlying its anti-inflammatory activity is not well characterized. In this study, seven natural products isolated from A. heterophyllus, including 25-Hydroxycycloart-23-en-3-one (HY), Artocarpin (AR), Dadahol A (DA), Morachalcone A (MA), Artoheterophyllin B (AB), Cycloheterophyllin (CY) and Moracin C (MC) were collected. Lipopolysaccharide (LPS)-stimulated inflammatory response in RAW264.7 macrophages were used in this study. Among these compounds, MC significantly inhibited LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release without marked cytotoxicity. Furthermore, MC effectively reduced LPS stimulated up-regulation of mRNA and protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and serval pro-inflammatory cytokines (interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor α (TNF-α)). Mechanistic studies revealed that the anti-inflammatory effect of MC was associated with the activation of the mitogen activated protein kinases (MAPKs) (including p38, ERK and JNK) and nuclear factor-κB (NF-κB) pathways, especially reducing the nuclear translocation of NF-κB p65 subunit as revealed by nuclear separation experiment and confocal microscopy. PMID:27463712

  13. Moracin C, A Phenolic Compound Isolated from Artocarpus heterophyllus, Suppresses Lipopolysaccharide-Activated Inflammatory Responses in Murine Raw264.7 Macrophages.

    PubMed

    Yao, Xue; Wu, Dang; Dong, Ningning; Ouyang, Ping; Pu, Jiaqian; Hu, Qian; Wang, Jingyuan; Lu, Weiqiang; Huang, Jin

    2016-01-01

    Artocarpus heterophyllus, a popular tropical fruit commonly known as the jackfruit tree, is normally planted in subtropical or tropical areas. Since a variety of phytochemicals isolated from A. heterophyllus have been found to possess potently anti-inflammatory, antiviral and antimalarial activities, researchers have devoted much interest to its potential pharmaceutical value. However, the exact mechanism underlying its anti-inflammatory activity is not well characterized. In this study, seven natural products isolated from A. heterophyllus, including 25-Hydroxycycloart-23-en-3-one (HY), Artocarpin (AR), Dadahol A (DA), Morachalcone A (MA), Artoheterophyllin B (AB), Cycloheterophyllin (CY) and Moracin C (MC) were collected. Lipopolysaccharide (LPS)-stimulated inflammatory response in RAW264.7 macrophages were used in this study. Among these compounds, MC significantly inhibited LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release without marked cytotoxicity. Furthermore, MC effectively reduced LPS stimulated up-regulation of mRNA and protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and serval pro-inflammatory cytokines (interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor α (TNF-α)). Mechanistic studies revealed that the anti-inflammatory effect of MC was associated with the activation of the mitogen activated protein kinases (MAPKs) (including p38, ERK and JNK) and nuclear factor-κB (NF-κB) pathways, especially reducing the nuclear translocation of NF-κB p65 subunit as revealed by nuclear separation experiment and confocal microscopy. PMID:27463712

  14. Determination of in vitro antidiabetic effects, antioxidant activities and phenol contents of some herbal teas.

    PubMed

    Büyükbalci, Aynur; El, Sedef Nehir

    2008-03-01

    In this research, some herbal teas and infusions traditionally used in the treatment of diabetes in Turkey, have been studied for their antidiabetic effects on in vitro glucose diffusion and phenolic contents and antioxidant activities. Ten aqueous herbal tea extracts were examined using an in vitro method to determine their effects on glucose movement across the gastrointestinal tract. Total phenol content of herbal teas was analyzed by Folin-Ciocalteu's procedure. Antioxidant activities of herbal teas were evaluated by the effect of extracts on DPPH radical and hydrogen peroxide scavenging. Antioxidant activity was defined as the amount of the sample to decrease the initial DPPH concentration by 50% as efficient concentration, EC50. Antiradical activity [AE] was calculated as 1/EC50. Values were evaluated statistically. Results support the view that none of the herbal teas showed antidiabetic effect on glucose diffusion using in vitro model glucose absorption. Teas were arranged in the order of green tea > peppermint > thyme > black tea > relax tea > absinthium > shrubby blackberry > sage > roselle > olive leaves according to their total phenol contents. Among ten herbal teas, green tea had the highest hydrogen-donating capacity against to DPPH radical. Ranking of the herbal teas with respect to their DPPH radical scavenging activity were green tea > peppermint > black tea > thyme > relax tea > absinthium > roselle > olive leaves > sage > shrubby blackberry. It was determined that adding flavoring substances such as lemon, bergamot, clove and cinnamon, which are commonly used in preparation of black tea in Turkey resulted to have synergistic effect on total antioxidant activities of black and peppermint teas. The highest hydrogen peroxide inhibition value (65.50%) was obtained for green tea at a 250 microl/ml concentration. The H2O2 scavenging activity of herbal teas decreased in the order green tea > peppermint > relax tea > black tea > thyme > olive leaves

  15. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

    NASA Astrophysics Data System (ADS)

    Lloyd, David J.; St Jean, David J.; Kurzeja, Robert J. M.; Wahl, Robert C.; Michelsen, Klaus; Cupples, Rod; Chen, Michelle; Wu, John; Sivits, Glenn; Helmering, Joan; Komorowski, Renée; Ashton, Kate S.; Pennington, Lewis D.; Fotsch, Christopher; Vazir, Mukta; Chen, Kui; Chmait, Samer; Zhang, Jiandong; Liu, Longbin; Norman, Mark H.; Andrews, Kristin L.; Bartberger, Michael D.; van, Gwyneth; Galbreath, Elizabeth J.; Vonderfecht, Steven L.; Wang, Minghan; Jordan, Steven R.; Véniant, Murielle M.; Hale, Clarence

    2013-12-01

    Glucose homeostasis is a vital and complex process, and its disruption can cause hyperglycaemia and type II diabetes mellitus. Glucokinase (GK), a key enzyme that regulates glucose homeostasis, converts glucose to glucose-6-phosphate in pancreatic β-cells, liver hepatocytes, specific hypothalamic neurons, and gut enterocytes. In hepatocytes, GK regulates glucose uptake and glycogen synthesis, suppresses glucose production, and is subject to the endogenous inhibitor GK regulatory protein (GKRP). During fasting, GKRP binds, inactivates and sequesters GK in the nucleus, which removes GK from the gluconeogenic process and prevents a futile cycle of glucose phosphorylation. Compounds that directly hyperactivate GK (GK activators) lower blood glucose levels and are being evaluated clinically as potential therapeutics for the treatment of type II diabetes mellitus. However, initial reports indicate that an increased risk of hypoglycaemia is associated with some GK activators. To mitigate the risk of hypoglycaemia, we sought to increase GK activity by blocking GKRP. Here we describe the identification of two potent small-molecule GK-GKRP disruptors (AMG-1694 and AMG-3969) that normalized blood glucose levels in several rodent models of diabetes. These compounds potently reversed the inhibitory effect of GKRP on GK activity and promoted GK translocation both in vitro (isolated hepatocytes) and in vivo (liver). A co-crystal structure of full-length human GKRP in complex with AMG-1694 revealed a previously unknown binding pocket in GKRP distinct from that of the phosphofructose-binding site. Furthermore, with AMG-1694 and AMG-3969 (but not GK activators), blood glucose lowering was restricted to diabetic and not normoglycaemic animals. These findings exploit a new cellular mechanism for lowering blood glucose levels with reduced potential for hypoglycaemic risk in patients with type II diabetes mellitus.

  16. Discovery of a long-chain carbamoyl aminocarnitine derivative, a reversible carnitine palmitoyltransferase inhibitor with antiketotic and antidiabetic activity.

    PubMed

    Giannessi, Fabio; Pessotto, Pompeo; Tassoni, Emanuela; Chiodi, Piero; Conti, Roberto; De Angelis, Francesco; Dell'Uomo, Natalina; Catini, Roberto; Deias, Roberto; Tinti, Maria Ornella; Carminati, Paolo; Arduini, Arduino

    2003-01-16

    The synthesis and pharmacological activity of reversible CPT I inhibitors as potential antiketotic and antidiabetic drugs are reported. Such inhibitors constitute a series of enantiomerically pure aminocarnitine derivatives having the general formula (CH3)3N+CH2CH(ZR)CH2COO- (with Z = ureido, carbamate, sulfonamide, and sulfamide moieties; R = C7-C14 linear alkyl chains). A primary pharmacological screening based on the evaluation of CPT I activity in intact rat liver (L-CPT I) mitochondria revealed the best activity for the (R) forms of ureidic derivative 17 (ZR = NHCONHR, R = C14), sulfonamidic derivative 7 (ZR = NHSO2R, R = C12), and sulfamidic derivative 9 (ZR = NHSO2NHR, R = C11). The IC50 values are 1.1, 0.7, and 0.8 microM, respectively. For the carbamic derivative 11 (ZR = NHCOOR, R = C8), an IC50 of 9.5 microM was observed. In addition, an extraordinarily high selectivity toward the liver isoform with respect to the heart isoform (muscle-CPT I identical with M-CPT I) was found for the ureidic compound 17 (IC50(M-CPT I) vs IC50(L-CPTI) = 39.4), as well as for other ureidic or carbamic compounds. Diabetic db/db mice treated orally with 17 and 7 for 45 days at a dose of 50 mg/kg twice a day showed a good reduction of serum glucose levels with respect to the untreated db/db mice (p < 0.01). In addition, 17 showed antiketotic activity in normal fasted rats. 17 has been selected for development as a potential antiketotic and antidiabetic drug. PMID:12519067

  17. Pharmacological investigations of the anti-diabetic effect of Cortex Moutan and its active component paeonol.

    PubMed

    Lau, C H; Chan, C M; Chan, Y W; Lau, K M; Lau, T W; Lam, F C; Law, W T; Che, C T; Leung, P C; Fung, K P; Ho, Y Y; Lau, C B S

    2007-11-01

    Cortex Moutan (CM, root bark of Paeonia suffruticosa Andr.) is one of the common herbs found in anti-diabetic traditional Chinese medicine formulae. To study the potential anti-diabetic mechanisms of CM, four in vitro models (intestinal brush border membrane vesicles (BBMV), rat hepatoma cell line H4IIE, human skin fibroblasts cell line Hs68 and mouse adipocytes 3T3-L1) were used. CM showed significant in vitro anti-diabetic effects by inhibiting glucose uptake of BBMV and enhancing glucose uptake into Hs68 and 3T3-L1 cells. Using bioassay-guided fractionation, paeonol was confirmed to be one of the active constituents for inhibiting BBMV glucose uptake. With neonatal-streptozotocin diabetic rats, paeonol (200 and 400mg/kgbody wt.) was found to improve oral glucose tolerance in vivo. To the best of our knowledge, this is the first report on the anti-diabetic effect of paeonol.

  18. [Cardiovascular safety of non-insulin anti-diabetic drugs. Scientific position statement of SEMERGEN].

    PubMed

    Prieto, M Á; Comas Samper, J M; Escobar Cervantes, C; Gasull Molinera, V

    2014-01-01

    Diabetes increases the risk of both microvascular and macrovascular complications. Although reducing plasma glucose levels to recommended targets decreases the risk of microvascular outcomes, the effects of anti-diabetic drugs on macrovascular complications and cardiovascular death are of concern. In fact, it has been suggested that some anti-diabetic agents could even be harmful for cardiovascular outcomes. In this context, several health care regulatory agencies have established the need for performing clinical trials specifically designed to assess the cardiovascular safety of anti-diabetic drugs. The results of 2 clinical trials have recently been published that provide important information on the cardiovascular safety of dipeptidyl peptidase 4 (DPP-4) inhibitors. The aim of this document was to review the available evidence on the cardiovascular safety of non-insulin anti-diabetic drugs and provide practical recommendations on their use in this context.

  19. Analytical interferences of mercuric chloride preservative in environmental water samples: Determination of organic compounds isolated by continuous liquid-liquid extraction or closed-loop stripping

    USGS Publications Warehouse

    Foreman, W.T.; Zaugg, S.D.; Falres, L.M.; Werner, M.G.; Leiker, T.J.; Rogerson, P.F.

    1992-01-01

    Analytical interferences were observed during the determination of organic compounds in groundwater samples preserved with mercuric chloride. The nature of the interference was different depending on the analytical isolation technique employed. (1) Water samples extracted with dichloromethane by continuous liquid-liquid extraction (CLLE) and analyzed by gas chromatography/mass spectrometry revealed a broad HgCl2 'peak' eluting over a 3-5-min span which interfered with the determination of coeluting organic analytes. Substitution of CLLE for separatory funnel extraction in EPA method 508 also resulted in analytical interferences from the use of HgCl2 preservative. (2) Mercuric chloride was purged, along with organic contaminants, during closed-loop stripping (CLS) of groundwater samples and absorbed onto the activated charcoal trap. Competitive sorption of the HgCl2 by the trap appeared to contribute to the observed poor recoveries for spiked organic contaminants. The HgCl2 was not displaced from the charcoal with the dichloromethane elution solvent and required strong nitric acid to achieve rapid, complete displacement. Similar competitive sorption mechanisms might also occur in other purge and trap methods when this preservative is used.

  20. Antidiabetic activity of Aloe vera L. juice. I. Clinical trial in new cases of diabetes mellitus.

    PubMed

    Yongchaiyudha, S; Rungpitarangsi, V; Bunyapraphatsara, N; Chokechaijaroenporn, O

    1996-11-01

    Aloe vera gel has been claimed to have antidiabetic activity but not all published results are consistent. We investigated the effect of oral administration of one tablespoonful of Aloe vera juice, twice a day for at least 2 weeks in patients with diabetes. Blood sugar and triglyceride levels in the treated group fell; cholesterol levels were not affected. The results suggest the potential of aloe vera juice for use as an antidiabetic agent.

  1. Adjuvant effects and antiserum action potentiation by a (herbal) compound 2-hydroxy-4-methoxy benzoic acid isolated from the root extract of the Indian medicinal plant 'sarsaparilla' (Hemidesmus indicus R. Br.).

    PubMed

    Alam, M I; Gomes, A

    1998-10-01

    The adjuvant effect and antiserum potentiation of a compound 2-hydroxy-4-methoxy benzoic acid were explored in the present investigation. This compound, isolated and purified from the Indian medicinal plant Hemidesmus indicus R. Br, possessed antisnake venom activity. Rabbits immunized with Vipera russellii venom in the presence and absence of the compound along with Freund's complete adjuvant, produced a precipitating band in immunogel diffusion and immunogel electrophoresis. The venom neutralizing capacity of this antiserum showed positive adjuvant effects as evident by the higher neutralization capacity (lethal and hemorrhage) when compared with the antiserum raised with venom alone. The pure compound potentiated the lethal action neutralization of venom by commercial equine polyvalent snake venom antiserum in experimental models. These observations raised the possibility of the use of chemical antagonists (from herbs) against snake bite, which may provide a better protection in presence of antiserum, especially in the rural parts of India.

  2. An enzoinformatics study targeting polo-like kinases-1 enzyme: Comparative assessment of anticancer potential of compounds isolated from leaves of Ageratum houstonianum

    PubMed Central

    Rizvi, Syed Mohd. Danish; Shakil, Shazi; Zeeshan, Mohd.; Khan, Mohd. Sajid; Shaikh, Sibhghatulla; Biswas, Deboshree; Ahmad, Adnan; Kamal, Mohammad Amjad

    2014-01-01

    Natural products from plant sources, embracing inherently ample structural diversity than synthetic ones are the major sources of anticancer agents and will constantly play as protagonists for discovering new drugs. Polo-like kinases (PLKs) play a leading role in the ordered execution of mitotic events and 4 mammalian PLK family members have been identified. PLK1 is an attractive target for anticancer drugs in mammalian cells, among the four members of PLKs. The present study expresses the molecular interaction of compounds (1,2-Benzenedicarboxylic acid bis (2 ethylhexyl) ester, squalene, 3,5-bis (1,1-dimethylethyl) phenol, Pentamethyl tetrahydro-5H-chromene, (1,4-Cyclohexylphenyl) ethanone and 6-Vinyl-7-methoxy-2,2-dimethylchromene) isolated from methanolic extract of leaves of Ageratum houstonianum with PLK1 enzyme. Docking between PLK1 and each of these compounds (separately) was performed using “Auto dock 4.2.” (1,4-Cyclohexylphenyl) ethanone showed the maximum potential as a promising inhibitor of PLK1 enzyme with reference to ∆G (−6.84 kcal/mol) and Ki (9.77 μM) values. This was sequentially followed by Pentamethyl tetrahydro-5H-chromene (∆G = −6.60 kcal/mol; Ki = 14.58 μM), squalene (∆G = −6.17 kcal/mol; Ki = 30.12 μM), 6-Vinyl-7-methoxy-2,2-dimethylchromene (∆G = −5.91 kcal/mol; Ki = 46.68 μM), 3, 5-bis (1,1-dimethylethyl) phenol (∆G = −5.70 kcal/mol; Ki = 66.68 μM) and 1,2-Benzenedicarboxylic acid bis (2 ethylhexyl) ester (∆G = −5.58 kcal/mol; Ki = 80.80 μM). These results suggest that (1,4-Cyclohexylphenyl) ethanone might be a potent PLK1 inhibitor. Further, in vitro and in vivo rumination are warranted to validate the anticancer potential of (1,4-Cyclohexylphenyl) ethanone. PMID:24914294

  3. Inhibitory Effects of Chemical Compounds Isolated from the Rhizome of Smilax glabra on Nitric Oxide and Tumor Necrosis Factor-α Production in Lipopolysaccharide-Induced RAW264.7 Cell

    PubMed Central

    Lu, Chuan-li; Zhu, Wei; Wang, Dong-mei; Chen, Wen-long; Hu, Meng-mei; Wang, Min; Xu, Xiao-jie

    2015-01-01

    The rhizome of Smilax glabra has been used for a long time as both food and folk medicine in many countries. The present study focused on the active constituents from the rhizome of S. glabra, which possess potential anti-inflammatory activities. As a result, nine known compounds were isolated from the rhizome of S. glabra with the bioassay-guiding, and were identified as syringaresinol (1), lasiodiplodin (2), de-O-methyllasiodiplodin (3), syringic acid (4), 1,4-bis(4-hydroxy-3,5-dimethoxyphenyl)-2,3-bis(hydroxymethyl)-1,4-butanediol (5), lyoniresinol (6), trans-resveratrol (7), trans-caffeic acid methyl ester (8), and dihydrokaempferol (9). Among these compounds, 2 and 3 were isolated for the first time from S. glabra. In addition, the potential anti-inflammatory activities of the isolated compounds were evaluated in vitro in lipopolysaccharide- (LPS-) induced RAW264.7 cells. Results indicated that 4 and 7 showed significant inhibitory effects on NO production of RAW264.7 cells, and 1, 2, 3, and 5 showed moderate suppression effects on induced NO production. 1, 7, and 5 exhibited high inhibitory effects on TNF-α production, with the IC50 values less than 2.3, 4.4, and 16.6 μM, respectively. These findings strongly suggest that compounds 1, 2, 3, 4, 5, 7, and 9 were the potential anti-inflammatory active compositions of S. glabra. PMID:25821492

  4. [Sulfonylureas in today's blood glucose lowering therapy. New data on advantages and potential barriers of an "old" antidiabetic group].

    PubMed

    Winkler, Gábor

    2015-03-29

    Sulfonylurea compounds have been basic elements of antidiabetic treatment in type 2 diabetes for a long time. However, with the introduction of incretin type insulin secretagogues it is often arises, whether is still there a place for sulfonylureas in the today's therapy. To answer this question the author overviews general pharmaceutical characteristics of the sulfonylurea compounds as well as individual particularities of the second generation derivatives used at present in Hungary. The author details also the most important differences between incretin type drugs - first of all dipeptidyl peptidase-4 inhibitors - and sulfonylureas. On the basis of available data it can be concluded in accordance with the latest international guidelines, that sulfonylureas have still role in the blood glucose lowering therapy of type 2 diabetes, though they became somewhat pushed back among insulin secretagogue type drugs. If a sulfonylurea compound is the drug of choice, it is important to select the appropriate molecule (in case of normal renal function gliclazide or glimepiride). It is also important to re-educate the patient, as well as to apply the minimal dose providing the desired glycaemic effect. PMID:25796278

  5. Adsorption and biodegradation of antidiabetic pharmaceuticals in soils.

    PubMed

    Mrozik, Wojciech; Stefańska, Justyna

    2014-01-01

    Pharmaceuticals are emerging contaminants in the natural environment. Most studies of the environmental fate of these chemicals focus on their behavior in wastewater treatment processes and in sewage sludge. Little is known about their behavior in soils. In this study adsorption and biodegradation of four antidiabetic pharmaceuticals - glimepiride, glibenclamide, gliclazide and metformin - were examined in three natural soils. The sorption of sulfonylurea derivatives was high (higher than sulfonylurea herbicides for example), whereas metformin showed high mobility. Desorption rates were highest for metformin. Sorption isotherms in two of three soils fitted best to the Freundlich model. Despite their high affinity to for soil surfaces, biodegradation studies revealed that transformation of the drugs occurred. Biodegradation results were described by pseudo-first order kinetics with half-life values from 5 to over 120 d (under aerobic conditions) and indicate that none of the tested drugs can be classified as quickly biodegradable. Biodegradation under anoxic conditions was much slower; often degrading by less than 50% during time of the experiment.

  6. Antihyperlipidemic and antidiabetic effects of umbelliferone in streptozotocin diabetic rats.

    PubMed Central

    Ramesh, B.; Pugalendi, K. V.

    2005-01-01

    The aim of the study was to evaluate blood glucose and lipid lowering effects of Umbelliferone (UMB) in streptozotocin (STZ) diabetic rats. Male albino Wistar rats (180 to 200 g) were induced diabetes by administration of STZ (40 mg/kg) intraperitonially. Normal and diabetic rats were treated with UMB in 10 percent dimethyl sulfoxide (DMSO) for 45 days. Diabetic rats had increased plasma glucose and decreased insulin, total proteins (TP), and albumin in addition to decreased food intake and body weight. Elevation in total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), very low density lipoprotein cholesterol (VLDL-C), triglycerides (TG), free fatty acids (FFA), and phospholipids (PL), and reduction in high density lipoprotein cholesterol (HDL-C) in the plasma were observed. Liver and kidney tissues of diabetic rats had elevation in the levels of TC, TG, FFA, and PL. Treatment with UMB decreased plasma glucose and increased insulin, TP, and albumin apart from food intake and body weight. In UMB-treated diabetic rats, plasma and tissue TC, TG, PL and FFA, and plasma LDL-C, VLDL-C, and HDL-C reversed to near normal. Thus, reduction of blood glucose and lipid profiles indicates that UMB has antidiabetic and antihyperlipidemic effects in diabetic rats. PMID:16720013

  7. Pharmacogenomics in type 2 diabetes: oral antidiabetic drugs.

    PubMed

    Daniels, M A; Kan, C; Willmes, D M; Ismail, K; Pistrosch, F; Hopkins, D; Mingrone, G; Bornstein, S R; Birkenfeld, A L

    2016-10-01

    Type 2 diabetes mellitus (T2DM) is a fast progressing disease reaching pandemic proportions. T2DM is specifically harmful because of its severe secondary complications. In the course of the disease, most patients require treatment with oral antidiabetic drugs (OADs), for which a relatively large number of different options are available. The growing number of individuals affected by T2DM as well as marked interindividual differences in the response to treatment call for individualized therapeutic regimens that can maximize treatment efficacy and thus reduce side effects and costs. A large number of genetic polymorphisms have been described affecting the response to treatment with OADs; in this review, we summarize the most recent advances in this area of research. Extensive evidence exists for polymorphisms affecting pharmacokinetics and pharmacodynamics of biguanides and sulfonylureas. Data on incretin-based medications as well as the new class of sodium/glucose cotransporter 2 (SGLT2) inhibitors are just starting to emerge. With diabetes being a known comorbidity of several psychiatric disorders, we also review genetic polymorphisms possibly responsible for a common treatment response in both conditions. For all drug classes reviewed here, large prospective trials are necessary in order to consolidate the existing evidence and derive treatment schemes based on individual genetic traits.

  8. Severe hypoglycemia in users of sulfonylurea antidiabetic agents and antihyperlipidemics.

    PubMed

    Leonard, C E; Bilker, W B; Brensinger, C M; Han, X; Flory, J H; Flockhart, D A; Gagne, J J; Cardillo, S; Hennessy, S

    2016-05-01

    Drug-drug interactions causing severe hypoglycemia due to antidiabetic drugs is a major clinical and public health problem. We assessed whether sulfonylurea use with a statin or fibrate was associated with severe hypoglycemia. We conducted cohort studies of users of glyburide, glipizide, and glimepiride plus a statin or fibrate within a Medicaid population. The outcome was a validated, diagnosis-based algorithm for severe hypoglycemia. Among 592,872 persons newly exposed to a sulfonylurea+antihyperlipidemic, the incidence of severe hypoglycemia was 5.8/100 person-years. Adjusted hazard ratios (HRs) for sulfonylurea+statins were consistent with no association. Most overall HRs for sulfonylurea+fibrate were elevated, with sulfonylurea-specific adjusted HRs as large as 1.50 (95% confidence interval (CI): 1.24-1.81) for glyburide+gemfibrozil, 1.37 (95% CI: 1.11-1.69) for glipizide+gemfibrozil, and 1.63 (95% CI: 1.29-2.06) for glimepiride+fenofibrate. Concomitant therapy with a sulfonylurea and fibrate is associated with an often delayed increased rate of severe hypoglycemia. PMID:26566262

  9. NRF2 activation by antioxidant antidiabetic agents accelerates tumor metastasis.

    PubMed

    Wang, Hui; Liu, Xiufei; Long, Min; Huang, Yi; Zhang, Linlin; Zhang, Rui; Zheng, Yi; Liao, Xiaoyu; Wang, Yuren; Liao, Qian; Li, Wenjie; Tang, Zili; Tong, Qiang; Wang, Xiaocui; Fang, Fang; Rojo de la Vega, Montserrat; Ouyang, Qin; Zhang, Donna D; Yu, Shicang; Zheng, Hongting

    2016-04-13

    Cancer is a common comorbidity of diabetic patients; however, little is known about the effects that antidiabetic drugs have on tumors. We discovered that common classes of drugs used in type 2 diabetes mellitus, the hypoglycemic dipeptidyl peptidase-4 inhibitors (DPP-4i) saxagliptin and sitagliptin, as well as the antineuropathic α-lipoic acid (ALA), do not increase tumor incidence but increase the risk of metastasis of existing tumors. Specifically, these drugs induce prolonged activation of the nuclear factor E2-related factor 2 (NRF2)-mediated antioxidant response through inhibition of KEAP1-C151-dependent ubiquitination and subsequent degradation of NRF2, resulting in up-regulated expression of metastasis-associated proteins, increased cancer cell migration, and promotion of metastasis in xenograft mouse models. Accordingly, knockdown of NRF2 attenuated naturally occurring and DPP-4i-induced tumor metastasis, whereas NRF2 activation accelerated metastasis. Furthermore, in human liver cancer tissue samples, increased NRF2 expression correlated with metastasis. Our findings suggest that antioxidants that activate NRF2 signaling may need to be administered with caution in cancer patients, such as diabetic patients with cancer. Moreover, NRF2 may be a potential biomarker and therapeutic target for tumor metastasis. PMID:27075625

  10. Salicylic acid elicitation during cultivation of the peppermint plant improves anti-diabetic effects of its infusions.

    PubMed

    Figueroa-Pérez, Marely G; Gallegos-Corona, Marco A; Ramos-Gomez, Minerva; Reynoso-Camacho, Rosalía

    2015-06-01

    Peppermint (Mentha piperita) infusions represent an important source of bioactive compounds with health benefits, which can be enhanced by applying salicylic acid (SA) during plant cultivation. The aim of this study was to evaluate the effect of SA (0, 0.5 and 2 mM) during peppermint cultivation on the chemical profile of saponins and alkaloids, as well as the anti-diabetic properties of the resulting infusions. The results showed that a 2 mM SA treatment significantly improved the chemical profiles of the infusions. Furthermore, the administration of 2 mM SA-treated peppermint infusions for 4 weeks to a high-fat diet/streptozotocin-induced diabetic rats decreased serum glucose levels (up to 25%) and increased serum insulin levels (up to 75%) as compared with the diabetic control. This can be related to the observed protection on pancreatic β-cells. Furthermore, 0.5 and 2 mM SA-treated peppermint infusions decreased LDL (24 and 47%, respectively) and increased HDL levels (18 and 37%, respectively). In addition, all groups treated with peppermint infusions had lower serum and liver triglyceride contents, where 2 mM SA peppermint infusion showed the highest effect (44% and 56%, respectively). This is probably caused by its higher capacity to inhibit pancreatic lipase activity and lipid absorption. Moreover, SA-treated peppermint infusions improved the steatosis score in diabetic rat liver and decreased serum transaminase levels, probably as a result of the increase in steroidal saponins and alkaloids, such as trigonellin. Therefore, the application of 2 mM SA during cultivation of peppermint could be used to improve the anti-diabetic properties of peppermint infusions.

  11. In Vitro Antioxidant, Anti-Diabetes, Anti-Dementia, and Inflammation Inhibitory Effect of Trametes pubescens Fruiting Body Extracts.

    PubMed

    Im, Kyung Hoan; Nguyen, Trung Kien; Choi, Jaehyuk; Lee, Tae Soo

    2016-01-01

    Trametes pubescens, white rot fungus, has been used for folk medicine in Asian countries to treat ailments such as cancer and gastrointestinal diseases. This study was initiated to evaluate the in vitro antioxidant, anti-diabetes, anti-dementia, and anti-inflammatory activities of T. pubescens fruiting bodies. The 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging activities of T. pubescens methanol (ME) and hot water (HWE) extracts (2.0 mg/mL) were comparable to butylated hydroxytoluene (BHT), the positive control. However, the chelating effects of ME and HWE were significantly higher than that of BHT. The HWE (6 mg/mL) also showed comparable reducing power to BHT. Eleven phenol compounds were detected by high performance liquid chromatography (HPLC) analysis. The α-amylase and α-glucosidase inhibitory activities of the ME and HWE of the mushroom were lower than Acarbose, the standard reference; however, the inhibitory effects of the mushroom extracts at 2.0 mg/mL were moderate. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects of ME and HWE were moderate and comparable with galanthamine, the standard drug to treat early stages of Alzheimer's disease (AD). The ME had a neuroprotective effect against glutamate-induced PC-12 cell cytotoxicity at the concentration range of 2-40 μg/mL. The mushroom extracts also showed inflammation inhibitory activities such as production of nitric oxide (NO) and expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced murine macrophage-like cell lines (RAW 264.7) and significantly suppressed the carrageenan-induced rat paw-edema. Therefore, fruiting body extracts of T. pubescens demonstrated antioxidant related anti-diabetes, anti-dementia and anti-inflammatory activities. PMID:27196881

  12. Prevalence, Trends, and Patterns of Use of Antidiabetic Medications Among Pregnant Women, 2001–2007

    PubMed Central

    Lawrence, Jean M.; Andrade, Susan E.; Avalos, Lyndsay A.; Beaton, Sarah J.; Chiu, Vicki Y.; Davis, Robert L.; Dublin, Sascha; Pawloski, Pamala A.; Raebel, Marsha A.; Smith, David H.; Toh, Sengwee; Wang, Jean Q.; Kaplan, Sigal; Amini, Thushi; Hampp, Christian; Hammad, Tarek A.; Scott, Pamela E.; Cheetham, T. Craig

    2013-01-01

    Objective To describe the prevalence, trends, and patterns in use of antidiabetic medications to treat hyperglycemia and insulin resistance prior to and during pregnancy in a large U.S. cohort of insured pregnant women. Methods Pregnancies resulting in livebirths were identified (N=437,950) from 2001–2007 among 372,543 women 12–50 years of age at delivery from 10 health maintenance organizations participating in the Medication Exposure in Pregnancy Risk Evaluation Program. Information for these descriptive analyses, including all antidiabetic medications dispensed during this period, was extracted from electronic health records and infant birth certificates. Results Just over one percent (1.21%) of deliveries were to women dispensed antidiabetic medication(s) in the 120 days before pregnancy. Use of antidiabetic medications before pregnancy increased from 0.66% of deliveries in 2001 to 1.66% of deliveries in 2007 (p<0.001) due to a rise in metformin use. Most women using metformin before pregnancy had a diagnosis code for polycystic ovaries or female infertility (67.2%) while only 13.6% had a diagnosis code for diabetes. The use of antidiabetic medications during the second or third trimester of pregnancy increased from 2.8% of deliveries in 2001 to 3.6% in 2007 (p <0.001). Approximately two-thirds (68%) of women using metformin before pregnancy did not use any antidiabetic medications during pregnancy. Conclusions Antidiabetic medication use prior to and during pregnancy rose from 2001–2007, possibly due to increasing prevalence of gestational diabetes mellitus, type 1 and type 2 diabetes, and other conditions associated with insulin resistance. PMID:23262934

  13. Gedunin and Azadiradione: Human Pancreatic Alpha-Amylase Inhibiting Limonoids from Neem (Azadirachta indica) as Anti-Diabetic Agents.

    PubMed

    Ponnusamy, Sudha; Haldar, Saikat; Mulani, Fayaj; Zinjarde, Smita; Thulasiram, Hirekodathakallu; RaviKumar, Ameeta

    2015-01-01

    Human pancreatic α-amylase (HPA) inhibitors offer an effective strategy to lower postprandial hyperglycemia via control of starch breakdown. Limonoids from Azadirachta indica known for their therapeutic potential were screened for pancreatic α-amylase inhibition, a known anti-diabetic target. Studies were carried out to reveal their mode of action so as to justify their hypoglycemic potential. Of the nine limonoids isolated/semi-synthesized from A.indica and screened for α-amylase inhibition, azadiradione and exhibited potential inhibition with an IC50 value of 74.17 and 68.38 μM, respectively against HPA under in vitro conditions. Further screening on AR42J α-amylase secretory cell line for cytotoxicity and bioactivity revealed that azadiradione and gedunin exhibited cytotoxicity with IC50 of 11.1 and 13.4μM. Maximal secreted α-amylase inhibition of 41.8% and 53.4% was seen at 3.5 and 3.3μM, respectively. Michaelis-Menten kinetics suggested a mixed mode of inhibition with maltopentaose (Ki 42.2, 18.6 μM) and starch (Ki' 75.8, 37.4 μM) as substrate with a stiochiometry of 1:1 for both azadiradione and gedunin, respectively. The molecular docking simulation indicated plausible π-alkyl and alkyl-alkyl interactions between the aromatic amino acids and inhibitors. Fluorescence and CD confirmed the involvement of tryptophan and tyrosine in ligand binding to HPA. Thermodynamic parameters suggested that binding is enthalpically and entropically driven with ΔG° of -21.25 kJ mol-1 and -21.16 kJ mol-1 for azadiradione and gedunin, respectively. Thus, the limonoids azadiradione and gedunin could bind and inactivate HPA (anti-diabetic target) and may prove to be lead drug candidates to reduce/control post-prandial hyperglycemia. PMID:26469405

  14. Gedunin and Azadiradione: Human Pancreatic Alpha-Amylase Inhibiting Limonoids from Neem (Azadirachta indica) as Anti-Diabetic Agents

    PubMed Central

    Zinjarde, Smita; Thulasiram, Hirekodathakallu; RaviKumar, Ameeta

    2015-01-01

    Human pancreatic α-amylase (HPA) inhibitors offer an effective strategy to lower postprandial hyperglycemia via control of starch breakdown. Limonoids from Azadirachta indica known for their therapeutic potential were screened for pancreatic α-amylase inhibition, a known anti-diabetic target. Studies were carried out to reveal their mode of action so as to justify their hypoglycemic potential. Of the nine limonoids isolated/semi-synthesized from A.indica and screened for α-amylase inhibition, azadiradione and exhibited potential inhibition with an IC50 value of 74.17 and 68.38 μM, respectively against HPA under in vitro conditions. Further screening on AR42J α-amylase secretory cell line for cytotoxicity and bioactivity revealed that azadiradione and gedunin exhibited cytotoxicity with IC50 of 11.1 and 13.4μM. Maximal secreted α-amylase inhibition of 41.8% and 53.4% was seen at 3.5 and 3.3μM, respectively. Michaelis-Menten kinetics suggested a mixed mode of inhibition with maltopentaose (Ki 42.2, 18.6 μM) and starch (Ki′ 75.8, 37.4 μM) as substrate with a stiochiometry of 1:1 for both azadiradione and gedunin, respectively. The molecular docking simulation indicated plausible π-alkyl and alkyl-alkyl interactions between the aromatic amino acids and inhibitors. Fluorescence and CD confirmed the involvement of tryptophan and tyrosine in ligand binding to HPA. Thermodynamic parameters suggested that binding is enthalpically and entropically driven with ΔG° of -21.25 kJ mol-1 and -21.16 kJ mol-1 for azadiradione and gedunin, respectively. Thus, the limonoids azadiradione and gedunin could bind and inactivate HPA (anti-diabetic target) and may prove to be lead drug candidates to reduce/control post-prandial hyperglycemia. PMID:26469405

  15. 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

  16. Comparing DNA extraction methods for analysis of botanical materials found in anti-diabetic supplements.

    PubMed

    Llongueras, Jose P; Nair, Saraswathy; Salas-Leiva, Dayana; Schwarzbach, Andrea E

    2013-03-01

    A comparative performance evaluation of DNA extraction methods from anti-diabetic botanical supplements using various commercial kits was conducted, to determine which produces the best quality DNA suitable for PCR amplification, sequencing and species identification. All plant materials involved were of suboptimal quality showing various levels of degradation and therefore representing real conditions for testing herbal supplements. Eight different DNA extraction methods were used to isolate genomic DNA from 13 medicinal plant products. Two methods for evaluation, DNA concentration measurements that included absorbance ratios as well as PCR amplifiability, were used to determine quantity and quality of extracted DNA. We found that neither DNA concentrations nor commonly used UV absorbance ratio measurements at A(260)/A(280) between 1.7 and 1.9 are suitable for globally predicting PCR success in these plant samples, and that PCR amplifiablity itself was the best indicator of extracted product quality. However, our results suggest that A(260)/A(280) ratios below about 1.3 and above 2.3 indicated a DNA quality too poor to amplify. Therefore, A(260)/A(280) measurements are not useful to identify samples that likely will amplify but can be used to exclude samples that likely will not amplify reducing the cost for unnecessarily subjecting samples to PCR. The two Nucleospin(®) plant II kit extraction methods produced the most pure and amplifiable genomic DNA extracts. Our results suggest that there are clear, discernable differences between extraction methods for low quality plant samples in terms of producing contamination-free, high-quality genomic DNA to be used for further analysis. PMID:22403012

  17. Isolation of an unknown compound, from both blood of Bhopal aerosol disaster victims and residue of tank E-610 of Union Carbide India Limited--chemical characterization of the structure.

    PubMed

    Chandra, H; Saraf, A K; Jadhav, R K; Rao, G J; Sharma, V K; Sriramachari, S; Vairamani, M

    1994-04-01

    A total of more than 28 chemical entities/reaction products in the form of gases, vapour and particulate matter were reported from the tank E-610 of methyl isocyanate (MIC) storage tank of Union Carbide India Limited on the night of 2/3 December 1984 in Bhopal. In earlier studies, methyl isocyanate and its trimer, with a few other compounds, were reported in the human victims preserved in deep freeze. Randomly selected samples were analysed by gas chromatograph coupled with mass spectrometer (ITD-800, Finnigan MAT, UK). Four of the cases showed the peaks and fragmentation pattern identified with one of the unidentified compound of molecular weight 269 amu in the Tank Residue, which constituted about 0.2 area per cent on GC-ITD. After isolation by column chromatography and being exposed to characterization, it was identified as a Spiro compound. It was possibly formed by the polymerization of five molecules of methyl isocyanate.

  18. Plant-Derived Compounds Targeting Pancreatic Beta Cells for the Treatment of Diabetes

    PubMed Central

    Oh, Yoon Sin

    2015-01-01

    Diabetes is a global health problem and a national economic burden. Although several antidiabetic drugs are available, the need for novel therapeutic agents with improved efficacy and few side effects remains. Drugs derived from natural compounds are more attractive than synthetic drugs because of their diversity and minimal side effects. This review summarizes the most relevant effects of various plant-derived natural compounds on the functionality of pancreatic beta cells. Published data suggest that natural compounds directly enhance insulin secretion, prevent pancreatic beta cell apoptosis, and modulate pancreatic beta cell differentiation and proliferation. It is essential to continuously investigate natural compounds as sources of novel pharmaceuticals. Therefore, more studies into these compounds' mechanisms of action are warranted for their development as potential anti-diabetics. PMID:26587047

  19. Rodent carcinogenicity with the thiazolidinedione antidiabetic agent troglitazone.

    PubMed

    Herman, J R; Dethloff, L A; McGuire, E J; Parker, R F; Walsh, K M; Gough, A W; Masuda, H; de la Iglesia, F A

    2002-07-01

    Carcinogenic potential of the thiazolidinedione antidiabetic troglitazone was assessed in 104-week studies in mice and rats. Mice were given 50, 400, or 800 mg/kg, male rats 100, 400, or 800 mg/kg, and female rats 25, 50, or 200 mg/kg. Vehicle and placebo controls were included. Survival was significantly decreased in both sexes of both species at high doses, but was adequate for valid evaluation of carcinogenicity. Hypertrophy and hyperplasia of brown adipose tissue was observed in both species at all doses, and fatty change and hypocellularity of bone marrow was noted in mice at all doses and in female rats at 50 and 200 mg/kg. Hepatocellular vacuolation was observed in mice at 400 and 800 mg/kg, and centrilobular hepatocellular hypertrophy occurred in rats at > or = 200 mg/kg. Ventricular dilatation, myocardial fibrosis, and atrial myocyte karyomegaly in male rats at 400 and 800 mg/kg and female rats at all doses were morphologically similar to spontaneous lesions, but incidence and severity were increased compared with controls. In mice, the incidence of hemangiosarcoma was increased in females at 400 mg/kg and in both sexes at 800 mg/kg. The incidence of hepatocellular carcinoma was increased in female mice at 800 mg/kg. Troglitazone exposure [AUC((0-24))] at the lowest dose associated with increased tumor incidence in mice was 16 times human therapeutic exposure at 400 mg daily. No tumors of any type were increased in rats at exposures up to 47 times therapeutic exposure.

  20. Molecular approach to identify antidiabetic potential of Azadirachta indica

    PubMed Central

    Satyanarayana, K.; Sravanthi, K.; Shaker, I. Anand; Ponnulakshmi, R.

    2015-01-01

    Background: Azadirachta indica (Neem) is a medicinal plant, used in Ayurveda for treating various diseases, one of which is diabetes mellitus. It is known to possess antiinflammatory, antipyretic, antimicrobial, antidiabetic and diverse pharmacological properties. However, the molecular mechanism underlying the effect of A. indica on insulin signal transduction and glucose homeostasis is obscure. Objective: The aim was to study the effects of A. indica aqueous leaf extract on the expression of insulin signaling molecules and glucose oxidation in target tissue of high-fat and fructose-induced type-2 diabetic male rat. Materials and Methods: The oral effective dose of A. indica leaf extract (400 mg/kg body weight [b.wt]) was given once daily for 30 days to high-fat diet-induced diabetic rats. At the end of the experimental period, fasting blood glucose, oral glucose tolerance, serum lipid profile, and the levels of insulin signaling molecules, glycogen, glucose oxidation in gastrocnemius muscle were assessed. Results: Diabetic rats showed impaired glucose tolerance and impairment in insulin signaling molecules (insulin receptor, insulin receptor substrate-1, phospho-IRS-1Tyr632, phospho-IRS-1Ser636, phospho-AktSer473, and glucose transporter 4 [GLUT4] proteins), glycogen concentration and glucose oxidation. The treatment with A. indica leaf extract normalized the altered levels of blood glucose, serum insulin, lipid profile and insulin signaling molecules as well as GLUT4 proteins at 400 mg/kg b.wt dose. Conclusion: It is concluded from the present study that A. indica may play a significant role in the management of type-2 diabetes mellitus, by improving the insulin signaling molecules and glucose utilization in the skeletal muscle. PMID:26604551

  1. [Antidiabetic fixed-dose combination tablet for the management of type 2 diabetes].

    PubMed

    Sakane, Naoki

    2012-01-01

    How to use oral antidiabetic fixed-dose combination tablet for the management of type 2 diabetes (T2DM)? In addition to diet and exercise, the majority of diabetic patients need drug therapy to achieve optimal glycemic control. Monotherapy with oral antidiabetic agent is the firstline pharmacologic treatment option. However, in order to maintain glycemic control, additional oral antidiabetic agents are often added to monotherapies resulting in dual therapy. Dual therapy can be prescribed as separate pills, or as a single pill containing two agents. Randomized controlled trials of patients requiring dual therapy, have shown fixed-dose combination therapies to have superior efficacy when compared to loose-pills combination therapies. T2DM patients treated with fixed-dose combination therapies may have better adherence, improved satisfaction, and lower direct costs, compared to those treated with loose-pill combination therapies. PMID:22413513

  2. Antidiabetic effect of taurine in cultured rat skeletal l6 myotubes.

    PubMed

    Cheong, Sun Hee; Chang, Kyung Ja

    2013-01-01

    Taurine (2-aminoethanesulfonic acid), a sulfur-containing β-amino acid, is found in all animal cells at millimolar concentrations and has been reported to show various health promoting activities including antidiabetic properties. The beneficial effects of taurine in diabetes mellitus have been known. However, the exact mechanism of hypoglycemic action of taurine is not properly defined. In this study, we investigated antidiabetic effect of taurine in the cell culture system using rat skeletal muscle cells. In cultured rat skeletal L6 myotubes, we studied the effect of taurine (0-100 μM) on glucose uptake to plasma membrane from the aspects of AMP-activated protein kinase (AMPK) signaling. Taurine stimulated glucose uptake in a dose-dependent manner by activating AMPK signaling. From these results, it may suggest that taurine show antidiabetic effect by stimulating insulin-independent glucose uptake in rat skeletal muscle.

  3. Compositional Studies: Antioxidant and Antidiabetic Activities of Capparis decidua (Forsk.) Edgew

    PubMed Central

    Zia-Ul-Haq, Muhammad; Ćavar, Sanja; Qayum, Mughal; Imran, Imran; de Feo, Vincenzo

    2011-01-01

    Capparis decidua is one of the traditional remedies used for various medicinal treatments in Pakistan. This study presents the determination of proximate composition, amino acids, fatty acids, tocopherols, sterols, glucosinolate and phenolic content in extracts obtained from different aerial parts of C. decidua, as well as their antidiabetic and antioxidant activity. All examined extracts were prominently rich in phenolics and glucosinates, and they showed potent antidiabetic and antihemolytic activity. The present study could be helpful in developing medicinal preparations for the treatment of diabetes and related symptoms. PMID:22272107

  4. Insilico docking study of compounds elucidated from helicteres isora fruits with ampkinase- insulin receptor.

    PubMed

    Vennila, Subramanium; Bupesh, Giridharan; Saravanamurali, Krishnan; SenthilKumar, Viajayan; SenthilRaja, Ramalingam; Saran, Natarajan; Magesh, Sachidanandam

    2014-01-01

    Insulin receptor (IR) proteins were essential intracellular signaling peptides in the insulin action cascade. Insulin receptor substrate proteins (IRS-1and IRS-2) serve and regulate the insulin level in the normal insulin action. The broad role of IRS-1 and IRS-2 in cell growth and survival reveals a common regulatory pathway linking development, somatic growth, fertility, neuronal proliferation, and aging to the core mechanisms used by vertebrates for nutrient sensing. Such type of proteins were cyclic adenosine monophosphate-activated protein kinase, this proteins play a key role in the insulin response and regulation. Type -2 Diabetes mellitus occurs during prolonged periods of peripheral insulin resistance due to inactivation of IRS proteins. The compounds isolated from the medicinal plants were safer than synthetic drugs and possess high bio activity. In the present study, four compounds were elucidated from fruits of Helicteres isora. The elucidated compounds were evaluated for the antidiabetic activity using in silico docking study. The receptor was analyzed for the active site and pocket finder tools. The aminoacids such as Phenylalanine, Lysine, Glutamic acid and Asparigine were predicted as active site binding residues. Docking studies were done through Autodock 4 software. All the compounds from fruits of Helicteres isora showed good docking profiles with AMP Kinase, except compound-3 (1,2,3,4-tetrahydro-1,5,6,8-tetramethyl-7-(2-methylprop-1-enylnaphthalene-4-ylpivalate). Finally the result from the study demonstrates that the HS-1, HS-2 and HS-4 posses potent anti diabetic activity against type-2 diabetes mellitus through drug action on AMP kinase cascade system. PMID:24966532

  5. Insilico docking study of compounds elucidated from helicteres isora fruits with ampkinase- insulin receptor

    PubMed Central

    Vennila, Subramanium; Bupesh, Giridharan; Saravanamurali, Krishnan; SenthilKumar, Viajayan; SenthilRaja, Ramalingam; Saran, Natarajan; Magesh, Sachidanandam

    2014-01-01

    Insulin receptor (IR) proteins were essential intracellular signaling peptides in the insulin action cascade. Insulin receptor substrate proteins (IRS-1and IRS-2) serve and regulate the insulin level in the normal insulin action. The broad role of IRS-1 and IRS-2 in cell growth and survival reveals a common regulatory pathway linking development, somatic growth, fertility, neuronal proliferation, and aging to the core mechanisms used by vertebrates for nutrient sensing. Such type of proteins were cyclic adenosine monophosphate-activated protein kinase, this proteins play a key role in the insulin response and regulation. Type -2 Diabetes mellitus occurs during prolonged periods of peripheral insulin resistance due to inactivation of IRS proteins. The compounds isolated from the medicinal plants were safer than synthetic drugs and possess high bio activity. In the present study, four compounds were elucidated from fruits of Helicteres isora. The elucidated compounds were evaluated for the antidiabetic activity using in silico docking study. The receptor was analyzed for the active site and pocket finder tools. The aminoacids such as Phenylalanine, Lysine, Glutamic acid and Asparigine were predicted as active site binding residues. Docking studies were done through Autodock 4 software. All the compounds from fruits of Helicteres isora showed good docking profiles with AMP Kinase, except compound-3 (1,2,3,4-tetrahydro-1,5,6,8-tetramethyl-7-(2-methylprop-1-enylnaphthalene-4-ylpivalate). Finally the result from the study demonstrates that the HS-1, HS-2 and HS-4 posses potent anti diabetic activity against type-2 diabetes mellitus through drug action on AMP kinase cascade system. PMID:24966532

  6. Potential influence of organic compounds on the transport of radionuclides from a geologic repository. Assessment of effectiveness of geologic isolation systems

    SciTech Connect

    Silviera, D.J.

    1981-03-01

    This study identifies organic compounds that may be present in a repository and outlines plausible interactions and mechanisms that may influence the forms and chemical behavior of these compounds. A review of the literature indicates that large quantities of organic radioactive wastes are generated by the nuclear industry and if placed in a repository could increase or decrease the leach rate and sorption characteristics of waste radionuclides. The association of radionuclides with organic matter can render the nuclides soluble or insoluble depending on the particular nuclide and such parameters as the pH, Eh, and temperature of the hydrogeologic system as well as the properties of the organic compounds themselves. 44 references.

  7. 18F9 (4-(3,6-bis (ethoxycarbonyl)-4,5,6,7-tetrahydrothieno (2,3-c) pyridin-2-ylamino)-4-oxobutanoic acid) enhances insulin-mediated glucose uptake in vitro and exhibits antidiabetic activity in vivo in db/db mice.

    PubMed

    Anandharajan, Rathinasabapathy; Sayyed, Sufyan G; Doshi, Lalit S; Dixit, Pooja; Chandak, Prakash G; Dixit, Amol V; Brahma, Manoja K; Deshmukh, Nitin J; Gupte, Ravindra; Damre, Anagha; Suthar, Jaspreet; Padigaru, Muralidhara; Sharma, Somesh D; Nemmani, Kumar V S

    2009-10-01

    Insulin resistance is central to the pathogenesis of type 2 diabetes mellitus. Previous studies have demonstrated that compounds that cause adipogenesis and improve glucose uptake in 3T3-L1 cells are potential insulin sensitizers. Therefore, we evaluated one such compound, 18F9, for (1) adipogenesis in human subcutaneous preadipocyte (SQ) cells, (2) glucose uptake in human skeletal muscle myotubes and SQ cells, and (3) antidiabetic activity in db/db mice. We also investigated its effect on ex vivo glucose uptake in soleus muscle isolated from continuously treated db/db mice. Gene expression profiling in soleus muscle and epididymal fat of db/db mice was performed to understand its effect on glucose metabolism, lipid metabolism, and thermogenesis. 18F9 enhanced adipogenesis in SQ cells and increased glucose uptake in SQ and human skeletal muscle myotubes cells. In db/db mice, 18F9 exhibited dose-dependent reduction in plasma glucose and insulin level. Interestingly, 18F9 was as efficacious as rosiglitazone but did not cause body weight gain and hepatic adverse effects. In addition, 18F9 demonstrated no change in plasma volume in Wistar rats. Furthermore, it enhanced ex vivo glucose uptake in soleus muscles in these mice, which substantiates our in vitro findings. Human peroxisome proliferator activated receptor-gamma transactivation assay revealed a weak peroxisome proliferator activated receptor-gamma transactivation potential (44% of rosiglitazone at 10 mumol/L) of 18F9. Gene expression profiling indicated that 18F9 increased insulin sensitivity mainly through a phosphoinositide 3-kinase-dependent mechanism. 18F9 also up-regulated genes involved in lipid transport and synthesis at par with rosiglitazone. Unlike rosiglitazone, 18F9 elevated the expression of Pdk4. In addition, 18F9 elevated the expression of glycogen synthase and adiponectin significantly higher than rosiglitazone. Taken