石斛酚对醛糖还原酶的抑制作用及其机制研究  

Inhibition of Gigantol on Aldose Reductase and Its Mechanism

作　　者：魏小勇[1] 高欣欣[1] 顾琼[2] 王岭[2] 方花[1] 戚辉[1] 易艳群[1] 王峥涛 古练权[2] 

机构地区：[1]广州中医药大学,广州510006 [2]中山大学,广州510006 [3]上海中药标准化研究中心,上海201203

出　　处：《中药新药与临床药理》2011年第1期1-4,共4页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然科学基金项目(30850012);广东省自然科学基金项目(06024128);广东省科技计划项目(2009A030100003;2007B020704005;2009B060700070;2009B090300335)

摘　　要：目的探讨石斛酚对醛糖还原酶(AR)的抑制作用及其机制。方法采用紫外分光光度法表征石斛酚对AR的抑制作用及抑制类型;采用分子对接软件Syby17.3中的FlexX预测二者作用残基及结合方式。结果石斛酚对AR的IC50=2.12 mmol/L,抑制类型为非竞争性抑制,并呈显强烈的量-效关系;二者作用残基为Trp111,His110,Tyr48,Trp20,主要结合方式是疏水相互作用、氢键和范得华力。结论石斛酚对AR活性表现出良好的抑制作用。Objective To study the inhibition of gigantol on aldose reductase and its mechanism. Methods We used ultra-violet （UV）speetrophotometry to detect the inhibition and types of inhibition, and used the molecular docking software Sybyl FlexX to predict the residues and the combining method of gigantol and aldose reduetase. Results The 50 % inhibiting concentration （IC50）of gigantol on AR was 2.12 retool/L, and the inhibition belonged to anti-competitive inhibition type in a dose-dependent manner. The residues of gigantol combining with aldose reductase were Trp111, His110, Tyr48, Trp20, the mainly binding mode being hydrophobic interaction, hydrogen bonding and Van der Waals force. Conclusion Gigantol exerts significant inhibition on aldose reductase activity.

关 键 词：石斛酚 醛糖还原酶 抑制 

分 类 号：R285.5[医药卫生—中药学]