α-葡萄糖苷酶抑制剂的构效关系

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、共价连接的环形成的半椅状或椅状构型等

Relationship Between Structure and Function of α Glucosidase Inhibitors

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.