石斛酚对诱导型一氧化氮合酶的抑制活性及其机制研究  

Inhibitory Effect of Gigantol on Inducible Nitric Oxide Synthase and Its Mechanism

作　　者：魏小勇[1] 高欣欣[1] 顾琼[2] 王岭[2] 王峥涛 

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

出　　处：《广州中医药大学学报》2011年第4期393-395,457,458,共5页Journal of Guangzhou University of Traditional Chinese Medicine

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

摘　　要：【目的】探讨石斛酚(gigantol)对诱导型一氧化氮合酶(iNOS)的抑制活性及作用位点,阐明石斛酚抗白内障的作用机制。【方法】采用试剂盒方法测定石斛酚对iNOS的体外抑制活性,动力学模拟石斛酚和iNOS的结合方式。【结果】浓度为120μmol/L的石斛酚对iNOS的抑制率为100%,其半数抑制量(IC50)为(32.227±5.73)μmol/L;石斛酚通过对iNOS活性位点的直接作用,进而抑制NO的产生;两者作用氨基酸位点是lle195、Gln257,相互作用力主要为氢键。【结论】石斛酚对iNOS具有良好的抑制作用。Objective To investigate the inhibitory effect of gigantol on inducible nitric oxide synthase（iNOS）,and to explore the therapeutic mechanism of gigantol for treatment of cataract.Methods Inhibitory activity of gigantol against iNOS in vitro was measured by enzymatic method,and the binding mode of gigantol to iNOS was simulated by the program of molecular operating environment（MOE）.Results When the concentration of gigantol was 120μmol/L,the inhibition rate of gigantol against iNOS was 100%,50%inhibiting concentration（IC50） being（32.227±5.73）μmol/L.Gigantol inhibited the production of NO by interacting with the active site of iNOS directly.The amino acid sites of their interaction were at lle195 and Gln257,the mainly binding mode was in hydrogen bonding interaction.Conclusion Gigantol exerts certain inhibition on iNOS activity.

关 键 词：石斛酚/药理学 诱导型一氧化氮合酶 白内障/中药疗法 

分 类 号：R285.5[医药卫生—中药学]