有效胺、井冈胺和1-脱氧野尻霉素对大鼠小肠刷状缘膜中碳水化合物酶活性的抑制作用

Inhibitory effect of validamine, valienamine and valiolamine on activities of carbohydrases in rat small intestinal brush border membranes.

作者信息

Takeuchi M, Takai N, Asano N, Kameda Y, Matsui K

机构信息

Department of Biochemistry, School of Pharmacy, Hokuriku University, Ishikawa, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Jul;38(7):1970-2. doi: 10.1248/cpb.38.1970.

DOI:10.1248/cpb.38.1970

PMID:2268898

Abstract

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 sucrase, maltase, glucoamylase, isomaltase and trehalase activities, but negligible action on lactase activity and pancreatic alpha-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 Ki values of valiolamine for sucrase, maltase, glucoamylase, isomaltase and trehalase activities were 3.2 x 10(-7), 2.9 x 10(-6), 1.2 x 10(-6), 9.1 x 10(-7) and 4.9 x 10(-5) M, respectively, which are 10(-5) to 10(-3) times smaller than the apparent Km values.

摘要

由吸水链霉菌柠檬亚种产生的三种假氨基糖，有效胺、缬氨霉素和伏格列波糖，对大鼠小肠碳水化合物酶活性，如蔗糖酶、麦芽糖酶、葡糖淀粉酶、异麦芽糖酶和海藻糖酶活性，表现出强效抑制作用，但对乳糖酶活性和胰腺α淀粉酶活性的作用可忽略不计。在出现抑制作用的地方，动力学分析表明这三种抑制剂对碳水化合物酶活性均表现为完全竞争性抑制。伏格列波糖比有效胺或缬氨霉素具有更强的碳水化合物酶抑制活性，伏格列波糖对蔗糖酶、麦芽糖酶、葡糖淀粉酶、异麦芽糖酶和海藻糖酶活性的表观Ki值分别为3.2×10⁻⁷、2.9×10⁻⁶、1.2×10⁻⁶、9.1×10⁻⁷和4.9×10⁻⁵ M，比表观Km值小10⁻⁵至10⁻³倍。