凝血因子X的活化及活化的凝血因子X的抑制  

Activation of Coagulation Factor X and Inhibition of Activated Coagulation Factor X

作　　者：吴双顶[1,2] 赵超[3] 张萌[3] 刘清亮[1] 

机构地区：[1]中国科学技术大学化学系 [2]中国科学院生态环境研究中心环境水化学国家重点实验室,北京100085 [3]中国科学院生态环境研究中心

出　　处：《中国科学技术大学学报》2000年第6期725-729,共5页JUSTC

基　　金：国家自然科学基金!(2 95 0 5 0 40 )资助项目

摘　　要：凝血因子X(FX)在凝血过程中起重要的作用 .利用鲁氏蝰蛇毒素 (RVV)中的FX活化酶 (RVV X) ,研究了Ca2 + 存在时的FX的活化 .RVV X活化FX有两条路径 :(1 )FX→FXβ→FXaβ;(2 )FX→FXaα→FXaβ.研究表明这两条路径在活化初期呈竞争状态 ,但是随着反应的进行 ,逐渐以第 (2 )种路径为主 ,FXβ 中间体的存在 ,可能有利于FX上的活化肽的脱去 .通过检测酶活性的方法 ,研究了表没食子基儿茶素没食子酸酯 (EGCG)对活化的凝血因子X(FXa)的作用 ,发现EGCG对FXa 有显著的抑制作用 ,其抑制作用随EGCG浓度变化而呈正相关性 ,表明EGCG是一种潜在的抗血栓和抗肿瘤新药 .Coagulation Factor X (FX) is a plasma protein which plays an important role in blood coagulation. The activator of FX, RVV X from Russell's viper venom, can activate FX to a serine protease, activated FX (FX a), in the presence of Ca 2+ , through two activation pathways: (1) FX→FX β→FX aβ , (2) FX→FX aα →FX aβ . These two pathways compete with each other during the initial stage of activation process of FX and two transients are generated as FX β and FX aα . The activation peptide of FX is perhaps removed easier in the presence of FX β than in the absence of FX β. The inhibition effect of (-) epigallocatechin gallate (EGCG) on FX a was studied by determining the activity of FX a. The results show that EGCG can inhibit evidently FX a, which indicates that EGCG is an inhibitor of FX a and a potential new drug of anti thrombosis and tumor antimetastasis.

关 键 词：凝血因子X 活化的凝血因子X 活化 抑制 

分 类 号：R331.1[医药卫生—人体生理学]