芳香化酶的结构、催化机制及其抑制剂研究进展  

Progress in study of the structure,catalytic mechanism and inhibitors of aromatase

作　　者：付静[1] 沈中华[1] 程飞雄[1] 刘桂霞[1] 李卫华[1] 唐赟[1] 

机构地区：[1]华东理工大学药学院,上海200237

出　　处：《药学学报》2012年第1期18-28,共11页Acta Pharmaceutica Sinica

基　　金：中央高校基本科研业务费专项资金资助项目(WY1014010);新世纪优秀人才支持计划资助项目(NCET-08-0774)

摘　　要：芳香化酶是体内负责雌激素生物转化的限速酶。通过抑制芳香化酶活性调节雌激素水平成为治疗乳腺癌的另一途径。本文首先简要介绍了芳香化酶的结构和催化机制,随后综述了甾体类和非甾体类芳香化酶抑制剂的研究进展,并着重介绍了近年来发现的具有抑制芳香化酶活性的天然产物类抑制剂,包括黄酮类、氧杂蒽酮类、香豆素类及倍半萜烯类化合物,并分析了这些化合物的构效关系。Aromatase is a key enzyme responsible for in vivo estrogen biosynthesis. Inhibition of the activity of the aromatase has become an alterative way for treatment of breast cancer. In this review, the structure and catalytic mechanism of the aromatase is briefly introduced followed by thorough review of the progress in the study of the steroidal and non-steroidal aromatase inhibitors. This review is focused on the natural compounds that exhibit the aromatase inhibition, which include flavonoids, xanthones, coumarins, and sesquiterpenes. The structure-activity relationship of these compounds is also discussed.

关 键 词：雌激素 芳香化酶 芳香化酶抑制剂 天然化合物 构效关系 

分 类 号：R916[医药卫生—药学]