摘要
为建立抑制剂与α 葡萄糖苷酶之间的构效关系 ,按照Dixon的方法测定了多种糖及糖衍生物的抑酶性 .共出现 3种Dixon曲线 ,分别代表了 3种不同的酶结合方式 .这些糖和糖衍生物的结构变化 (如羟基构象、C 1位取代基、聚合度等的变化 )都会影响其与酶的结合能力 .结果表明 ,与酶有高结合力的物质需要满足一定的结构要求 ,如恰当的羟基构象、阳离子。
In order to establish the relationship between the structure and function of α glucosidase inhibitors the inhibition ability of some sugars and sugar derivatives toward α glucosidase using method of Dixon was examined. Three kinds of Dixon binding mechanisms have been found. The results also demonstrated that the structural differences of these sugars and sugar derivatives (like the differences of hydroxyl group configuration, C 1 substituent groups and polymerization degree) can affect the interaction between the enzyme and substrates. It also illuminates that an effective α glucosidase inhibitor should possess some structural features, like proper hydroxyl group configuration, positive charge, a half chair or chair like conformation.
出处
《中国生物化学与分子生物学报》
CAS
CSCD
北大核心
2003年第6期780-784,共5页
Chinese Journal of Biochemistry and Molecular Biology
基金
浙江省科技计划项目 (编号 2 0 0 3C2 3 0 3 0 )
国家新药博士基金 (编号2 0 0 3AA2Z3 5 11)资助~~
