Abstract
Ethnopharmacological relevance Gynostemma pentaphyllum (Thunb.) tea was used in Vietnamese folk medicine as anti-diabetic agent. Aim of the study This study was aimed to investigate the inhibitory activities of fractions and constituents isolated from Gynostemma pentaphyllum on protein tyrosine phosphatase 1B (PTP1B) since it has been proposed as a treatment therapy for type 2 diabetes and obesity. Materials and methods The 70% EtOH extract, CHCl 3 fraction, EtOAc fraction, BuOH fraction, and seven isolated dammarane triterpenes were evaluated for their inhibitory activity in protein phosphatase enzymes (PTP1B and VHR). Results CHCl 3-soluble fraction showed a dose-dependent inhibitory activity of the PTP1B enzyme with the IC 50 value of 30.5 μg/mL. Among seven tested compounds, compounds 6 showed the most potent PTP1B inhibitory activity with IC 50 value of 5.3 ± 0.4 μM compared to a range 15.7–28.5 μM for the other six compounds. The inhibition mode of 6 was competitive toward p-NPP with a K i value of 2.8 μM. Conclusion These study results suggested that the PTP1B inhibitory activity of these dammaranes may enable this plant to play an important role in the treatment of diabetes.
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