八厘麻毒素的提取分离、改造及药理作用  

Extraction, chemical modification and pharmacological bioactivity of rhomotoxin

作　　者：易卫平[1] 邱汉婴[1] 郑锦鸿[2] 王锦芝[2] 

机构地区：[1]汕头大学医学院附属第二医院心血管研究室,汕头515041 [2]汕头大学医学院药化研究室,汕头515031

出　　处：《中国新药杂志》2006年第19期1655-1658,共4页Chinese Journal of New Drugs

摘　　要：目的:提取分离并改造八厘麻毒素(RTX)的化学结构及其药理作用研究。方法:经过加热回流、硅胶层析及重结晶获得RTX,再经酸催化、纯化获得八厘麻毒素结构改造物(Rh2),以动脉血压及电生理参数、离体胸主动脉螺旋条生物测定研究其药理作用。结果:获得RTX及Rh2精制品,后者的初步药理作用显示具有收缩血管平滑肌,提高动脉血压的作用,同时不影响心脏的电生理。结论:RTX结构中的2,3-环氧基团被改变后,其降压作用消失而表现为升压作用。Objective： To study the isolation, chemical modification and pharmacological bioactivity of rhomotoxin （RTX）. Methods ： RTX was isolated from Rhododendron molle by hot refluxing, column chromatography on silicon gel and recrystallization. The structure-modified RTX （ Rh2） was obtained by acid catalysis of RTX. Before and after administration of Rh2, arterial blood pressure and cardiac electrophysiological parameters of anesthetic rats were measured; changes in tension were tested by bioassay of spiral strips of isolated rat aorta. Results： Refined Rh2 showed constriction of isolated aorta spiral strips and escalation of systolic blood pressure without impacts of cardiovascular electrophysiological parameters. Conclusion： Vasodilatation was shifted to vasoconstriction when the 2,3-epoxy substitute of RTX was modified.

关 键 词：八厘麻毒素 改造 血管收缩剂 构效关系 

分 类 号：R916.2[医药卫生—药学] R965.1