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Mysore, India

Zameer F.,University of Mysore | Naidu A.,Indian Central Food Technological Research Institute | M. N. N.P.,JSS Institution Camp | Dhananjaya B.L.,Global University | Hegdekatte R.,University of Mysore
Pharmaceutical Biology | Year: 2015

Context Withania somnifera (L.) Dunal is traditionally used for treating various ailments, but lacks scientific evaluation. Objective This study evaluates Withania somnifera (WS) for its effect on platelet activity and inflammatory enzymes. Materials and methods Aqueous and ethanolic (1:1) leaf extracts were subjected to in vitro indirect haemolytic activity using Naja naja venom, human platelet aggregation was quantified for lipid peroxidation using arachidonic acid (AA) as agonist and 5-lipoxygenase (5-LOX) levels were determined using standard spectrometric assays. Further, molecular docking was performed by the ligand fit method using molegro software package (Molegro ApS, Aarhus, Denmark). Results The study found that aqueous and ethanol extracts have very negligible effect (15%) with an IC50 value of 13.8 mg/mL on PLA2 from Naja naja venom. Further, extracts of WS also had very little effect (18%) with an IC50 value of 16.6 mg/mL on malondialdehyde (MDA) formation. However, a 65% inhibition of 5-LOX with an IC50 value of 0.92 mg/mL was observed in 1:1 ethanol extracts. The same was evident from SAR model with the active ingredient withaferin A binding predominantly on Phe 77, Tyr 98, Arg 99, Asp 164, Leu 168, Ser 382, Arg 395, Tyr 396 and Tyr 614 with an atomic contact energy value of −128.96 compared to standard phenidone (−103.61). Thus, the current study validates the application of WS for inflammatory diseases. Conclusion This study reveals the inhibitory potential of W. somnifera on inflammatory enzymes and platelet aggregation. Thus, WS can serve as a newer, safer and affordable medicine for inflammatory diseases. © 2015 Taylor & Francis Source

Ramu R.,JSS Institution Camp | Shirahatti P.S.,JSS Institution Camp | Zameer F.,Mahajana Life Science Research Center | Nagendra Prasad M.N.,JSS Institution Camp
Journal of the Science of Food and Agriculture | Year: 2015

BACKGROUND: Postprandial hyperglycaemia in diabetes could be ameliorated by inhibiting intestinal α-glucosidases, responsible for starch hydrolysis and its absorption. Different parts of banana have been in use in conventional medicinal formulations since ancient times. Its role as an antihyperglycaemic agent has also been studied. This study was aimed at explaining the mechanism of hypoglycaemic effect by ethanol extract of banana pseudostem (EE). Additionally, studies on the active components involved in the effect have also been attempted. RESULTS: EE significantly inhibited mammalian intestinal α-glucosidases and yeast α-glucosidase (IC50, 8.11 ± 0.10 μg mL-1). The kinetic studies showed that EE inhibited sucrase, maltase and and p-nitrophenyl-α-d-glucopyranoside hydrolysis by mixed-type inhibition. Further, in vivo studies identified that the oral administration (100-200 mg kg-1 body weight) of EE significantly suppressed the maltose/glucose-induced postprandial plasma glucose elevation and wielded an antihyperglycaemic effect in normal and alloxan-induced diabetic rats. GC-MS analysis of EE revealed high levels of β-sitosterol (29.62%), stigmasterol (21.91%), campesterol (10.85%) and other compounds. CONCLUSION: These findings suggest that EE might exert an anti-diabetic effect by inhibition of α-glucosidases from the intestine, in turn suppressing the carbohydrate absorption into the bloodstream. Hence the results extend a foundation to the future prospects of the food-derived enzyme inhibitors in treatment of diabetes. © 2014 Society of Chemical Industry. Source

Ramu R.,JSS Institution Camp | Shirahatti P.S.,JSS Institution Camp | Zameer F.,Mahajana Life Science Research Center | Ranganatha L.V.,University of Mysore | Nagendra Prasad M.N.,JSS Institution Camp
South African Journal of Botany | Year: 2014

Postprandial hyperglycaemia is characterized as the earliest symptom of diabetes and its management attenuates several of the associated secondary complications. In this context, we investigated the role of ethanol extract of banana flower (EF) for its antihyperglycaemic effects. The EF showed a strong inhibition towards α-glucosidase and pancreatic amylase which play a vital role in clinical management of postprandial hyperglycaemia. The major active compounds present in EF were identified as Umbelliferone (C1) and Lupeol (C2) using various spectroscopic methods. C1 (IC50: 7.08±0.17μg/ml) and C2 (IC50: 7.18±0.14μg/ml) were found to inhibit α-glucosidase in a non-competitive mode of inhibition, with low Ki values. Further, in vitro glycation assays showed that EF and its compounds prevented each stage of protein glycation and formation of its intermediary compounds. EF, C1 and C2 also exhibited a potent inhibition on aldose reductase with IC50 values of 2.25±0.29, 1.32±0.22 & 1.53±0.29μg/ml respectively. Our results suggest that, the observed potential of EF in antihyperglycaemic activity via inhibition of α-glucosidase and in antidiabetogenic effect by inhibition of polyol pathway and protein glycation is more likely to be attributed to the presence of C1 and C2. © 2014 South African Association of Botanists. Source

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