Asian Pacific Journal of Tropical Biomedicine · 2015 · 72 citations · 12 references
Life SciencesBotanyPharmacologyBiochemical PharmacologyPlant BiochemistryStructure-activity RelationshipsDiabetes PharmacotherapyEnzyme InhibitionMedicinal Plant KnowledgeMedicinal PlantsStructure-activity Relationship AnalysisAntidiabetic ActivityDipeptidyl PeptidasesLeaf Extract AssaysLiquid Chromatography-mass SpectrometryLiquid Chromatography-mass Spectrometry AnalysisMicroplate ScreeningPharmacological ScreeningPlant Extract Inhibitors
Objective To evaluate the anti-diabetic potential of leaf extract from Urena lobata ( U. lobata ) through dipeptidyl peptidase IV (DPP-IV) inhibitory activity. Methods U. lobata leaf was extracted in hot water and ethanol. The activity of DPP-IV inhibitor was tested by in vitro study using gly-pro-p-nitroanilide as substrat of DPP-IV and vildagliptin , as standard reference. A product of the reactions between gly-pro-p-nitroanilide and DPP-IV, was observed by microplate readers with λ = 405 nm. All data were expressed as mean ± SD and the IC 50 value was determined by non linear regression curve fit. Active substances in leaf extract of U. lobata was analyzed by liquid chromatography-mass spectrometry. DPP-IV inhibitory activity of active compounds was evaluated in silico using docking server. Results The ethanolic extract of U. lobata showed stronger DPP-IV inhibitor activity than water extract with the IC 50 values of 1 654.64 and 6 489.88 μg/mL, respectively. Vildagliptin, based on standard reference for DPP-IV inhibitor activity, has IC 50 value of 57.44 μg/mL. Based on in silico analysis, mangiferin , stigmasterol and β-sitosterol in U. lobata extract have a strong inhibitory activity on DPP-IV. Conclusions The results showed that DPP-IV inhibitory activity of U. lobata is related to its active compounds such as mangiferin, stigmasterol and β-sitosterol.
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