Inhibition of Porcine Small Intestinal Sucrase by Validamine  

作　　者：郑裕国 申屠旭萍 沈寅初 

机构地区：[1]Institute of BloengineeringState Key Laboratory Breeding Base of Green Chemistry-Synthesis Technology,Zhejiang University of Technology,Hangzhou 310014,China

出　　处：《Chinese Journal of Chemical Engineering》2005年第3期429-432,共4页中国化学工程学报（英文版）

基　　金：Supported by the National Fund of the Major Basic Research Development Program (973 Project) (No.2003CB716005)the National Natural Science Foundation of China (No. 20176055) the Natural Science Foundation of Zhejiang Province (No. ZB0106).

摘　　要：As an important medicinal intermediate with broad uses, validamine, an aminocyclitol, isolated from the enzymolysis broth of validamycins, has gained more and more attention. The absolute configuration of validamine is similar to that of a-D-glucose, and it demonstrates powerful inhibition activity on glycosidase. In this paper, the inhibitory effect of validamine on porcine small intestinal sucrase was investigated. Validamine was found to be a potent, competitive inhibitor to porcine small intestinal sucrase in vitro with an IC50 value of 6.85 X 10(-4) mol center dot L-1. Validamine exhibited a dose-dependent inhibition effect on porcine small intestinal sucrase, whereby the inhibition interaction of validamine and porcine small intestinal sucrase was a fast binding process. The inhibition of validamine on porcine small intestinal sucrase was pH-dependent.As an important medicinal intermediate with broad uses, validamine, an aminocyclitol, isolated from the enzymolysis broth of validamycins, has gained more and more attention. The absolute configuration of validamine is similar to that of α-D-glucose, and it demonstrates powerful inhibition activity on glycosidase. In this paper, the inhibitory effect of validamine on porcine small intestinal sucrase was investigated. Validamine was found to be a potent, competitive inhibitor to porcine small intestinal sucrase in vitro with an IC50 value of 6.85 × 10^-4 mol·L^-1. Validamine exhibited a dose-dependent inhibition effect on porcine small intestinal sucrase, whereby the inhibition interaction of validamine and porcine small intestinal sucrase was a fast binding process. The inhibition of validamine on porcine small intestinal sucrase was pH-dependent.

关 键 词：validamine enzyme inhibition validamycins porcine small intestinal sucrase 

分 类 号：TQ464[化学工程—制药化工]