Inhibitory Effect of Validamine, Valienamine and Valiolamine on Activities of Carbohydrases in Rat Small Intestinal Brush Border Membranes

概要

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Three pseudo-aminosugars, validamine, valienamine and valiolamine, produced by Streptomyces hygroscopicus subsp. limoneus showed potent inhibitory action on rat small intestinal carbohydrase activities such as sucrace, maltase, glucoamylase, isomaltase and trehalase activities, but negligible action on lactase activity and pancreatic α-amylase activity. Where inhibition was seen, kinetic analysis showed fully competitive inhibition of the carbohydrase activities by all three inhibitors. Valiolamine has more potent carbohydrase inhibitory activity than validamine or valienamine, and the apparent K_i values of valiolamine for sucrase, maltase, glucoamylase, isomaltase and trehalase activities were 3.2×10^<-7>, 2.9×10^<-6>, 1.2×10^<-6>, 9.1×10^<-7> and 4.9×10^<-5>M, respectively, which are 10^<-5> to 10^<-3> times smaller than the apparent K_m values.
社団法人日本薬学会の論文
1990-07-25