Article ID Journal Published Year Pages File Type
5546595 Acta Pharmaceutica Sinica B 2017 5 Pages PDF
Abstract

α-Glucosidase and lipase inhibitors play important roles in the treatment of hyperglycaemia and dyslipidemia. To identify novel naturally occurring inhibitors, a bioactivity-guided phytochemical research was performed on the pu-erh tea. One new flavanol, named (-)-epicatechin-3-O-(Z)-coumarate (1), and 16 known analogs (217) were isolated from the aqueous extract of the pu-erh tea. Their structures were determined by spectroscopic and chemical methods. Furthermore, the water extract of pu-erh tea and its fractions exhibited inhibitory activities against α-glucosidases and lipases in vitro; compound 15 showed moderate inhibitory effect against sucrase with an IC50 value of 32.5 μmol/L and significant inhibitory effect against maltase with an IC50 value of 1.3 μmol/L. Compounds 8, 10, 11 and 15 displayed moderate activity against a lipase with IC50 values of 16.0, 13.6, 19.8, and 13.3 μmol/L, respectively.

Graphical abstractOne new flavanol, named (-)-epicatechin-3-O-(Z)-coumarate (1), and 16 known analogs (217) were isolated from the aqueous extract of the pu-erh tea. Compound 15 showed moderate inhibitory effect on sucrase with an IC50 value of 32.5 μmol/L and significant inhibitory effect on maltase in vitro with an IC50 value of 1.3 μmol/L; compounds 8, 10, 11 and 15 displayed moderate activity against a lipase with IC50 values of 16.0, 13.6, 19.8, and 13.3 μmol/L, respectively.Download high-res image (147KB)Download full-size image

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