从抗蛇毒药探寻内皮素拮抗剂的初步报告

A Preliminary a Study of EndothelinAntagonists from Anti-Snake Venom Herb Medicine

内皮素(endothelin,ET)在许多心血管疾病中具有重要发病学意义,但目前尚无临床可用的有效拮抗剂。ET与某些蛇毒具有同源的结构及相似的生物学效应,因此我们在整体动物及离体血管条上,初步观察了几种抗蛇毒中草药对ET生物学效应的影响。本工作发现:季德胜蛇药水提剂对ET_1收缩的血管有短暂舒张作用;七叶一枝花和半边莲水提剂可部分拮抗ET_1致小鼠死亡作用,抑制ET_1的升压作用和缩血管效应;半边莲和白叶藤有效成份组成的复方三号对ET_1生物学效应无明显拮抗作用。结果提示:从抗蛇毒药中筛选ET拮剂是可行的,有可能为心血管疾病的治疗提供新的途径。

It is well known that endothelin (ET)plays an important role in the patho- genesis of cardiovascular diseases,yet antogonist of ET for clinical application has not been found. Since ET and some snake toxins have homologous structure and similar biological ac- tion,the effect of Chinese anti-snake venom herb medicine on ET bioaction was investigated both in vivo and in vitro,It was found that Ji De Sheng anti-snake venom medicine (季德胜蛇 药)transiently relaxed ET-contracted isolated rat aortic ring;Lobelis radicans Thumb (半边 莲)and Taris polyphylla Smith var. chinensis (French)Hara (七叶一枝花) partly antogo- nized the lethal effect of ET-1 on mice and inhibited blood pressure elevation and vasocon- traction induced by ET-1. However,Compound Ⅲ (复方三号)had no effect on ET-1-bioac- tion. In conclusion, it is feasible to exploit ET antagonists from anti-snake venom herb medicine. In prospects,our work would shed new lights on for treatment of cardiovascular diseases pathogenetically related to ET.