Evaluation of polyhydroxybenzophenones as α-glucosidase inhibitors.

Xuesen Hu, Yang Xiao, Jianlong Wu, Lin Ma

Index: Arch. Pharm. (Weinheim) 344(2) , 71-7, (2011)

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Abstract

This experiment was designed to synthesize 18 kinds of polyhydroxybenzophenones by using Friedel-Crafts reaction, and to measure the inhibitory activity on α-glucosidase with p-nitrophenyl-β-D-galactopyranoside (PNPG) as a substrate. Here, acarbose (IC(50)  = 1674.75 µmol L(-1) ) was used as the reference inhibitor. The results demonstrated that most of the target compounds had remarkable inhibitory activities on α-glucosidase. Among all these compounds, 2,4,4',6-butahydroxydiphenylketone (11) was found to be the most potent α-glucosidase inhibitor with an IC(50) value of 10.62 µmol L(-1) . In addition, we found these compounds were competitive inhibitors through the kinetic analysis. The results suggested that such compounds might be utilized for the development of new candidates for diabetes treatment.Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.