红景天苷糖碳苷类似物的合成及心肌保护活性研究  

The C-glycoside analogues of salidroside:synthesis and their protective effects on myocardial cells

作　　者：彭涛[1] 王林[1] 韩凤昭[1] 张首国[1] 温晓雪[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所药物化学研究室,北京100850

出　　处：《中国药物化学杂志》2009年第2期89-93,共5页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30472081);北京市科技计划项目(D080802002908010)

摘　　要：目的设计合成具有心肌保护作用的糖碳苷化合物。方法针对红景天苷可被糖苷水解酶水解的缺点,将其改造为糖碳苷并改变苯环上的取代基进行新药设计,获得红景天苷的糖碳苷类似物。通过体外心肌细胞的缺氧-复氧损伤模型评价其心肌保护活性。结果与结论合成了10个糖碳苷类新化合物。初步药理评价表明,大多数化合物对缺氧-复氧损伤心肌具有明显的保护作用,其中5个化合物的活性强于红景天苷,并呈剂量依赖关系。Aim To design and synthesize C-glycoside compounds with protection effects on myocardial cells. Methods Target compounds were designed to improve the resistant on glycosidase,including replacement of the anomeric oxygen of salidroside by carbon and changing the substitution groups on the benzene ring. The target compounds＇ activities were evaluated in vitro on anoxia/reoxygenation injuries model of myocardial cells. Results and conclusion Ten novel C-glycoside compounds were synthesized. The results of primary pharmacological tests indicate that most target compounds have protective effects on anoxia/reoxygenation injuries model of myocardial cells obviously. Five compounds have stronger effects compared with salidroside, and significant dosage-dependent relationship were observed.

关 键 词：糖碳苷 合成 心肌保护作用 红景天苷 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]