期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 15, 页码 3226-3230出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.06.040
关键词
Aurone; alpha-Glucosidase inhibitor; Inhibitory mechanism; Docking analysis; Glucose consumption
资金
- Chinese National Natural Science Foundation [21502138]
A series of 6-hydroxyaurones and their analogues have been synthesized and evaluated for their in vitro alpha-glucosidase inhibitory and glucose consumption-promoting activity. These compounds exhibited varying degrees of alpha-glucosidase inhibitory activity, 11 of them showing higher potency than that of the control standard acarbose (IC50 = 50.30 mu M). Surprisingly, analogues devoid of a substituent at C-2 but having an aryl group at C-5 were found to be highly active (e.g., 7f, IC50 = 9.88 mu M). Docking analysis substantiated these findings. The kinetic analysis of compound 7f, the most potent alpha-glucosidase inhibitor of this study, revealed that it inhibited alpha-glucosidase in an irreversible and mixed competitive mode. In addition, compounds 7f and 10c exhibited significant glucose consumption promoting activity at 1 lM. (C) 2017 Elsevier Ltd. All rights reserved.
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