目的对薯蓣皂苷元进行结构改造,从其衍生物中寻找具有抗血栓形成活性的化合物。方法以薯蓣皂苷元为先导化合物,通过酯化反应合成得到目标化合物,选择大鼠动静脉旁路血栓形成模型,评价其体内抗血栓形成活性。结果合成了9个目标化合物,通过波谱学方法(NMR、MS)确证了结构。所合成化合物中连有水杨酰基的化合物(Di-8,9)在抗血栓形成活性筛选试验中显示了较好的活性。结论适当活性基团的引入可以增强薯蓣皂苷元抗血栓形成活性。

Objective To search antithrombotic substances from diosgenin derivatives by structure modification.Methods The target compounds were synthesized by esterification reaction with diosgenin as the leading compound.Antithrombotic activity of these compounds was examined using the thrombogenesis model of arterio-veinous bypass in rats.Results Nine compounds were prepared and their structures were confirmed by spectral methods(NMR and MS).Two compounds(Di-8 and Di-9) containing salicyl group in structure showed promising antithrombotic activity in screening experiment.Conclusion The group of the proper active moiety in structure could improve the antithrombotic activity of diosgenin.

国家重大新药创制大平台子课题(2009ZX09301-008-P-05);天津市自然科学基金资助项目(07TCZDJC05300)