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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 structuralize diosgenin and search for anti-thrombotic compounds from its derivatives. Methods Using diosgenin as the lead compound, the target compound was synthesized by esterification reaction. The model of arteriovenous bypass thrombosis in rats was selected to evaluate the antithrombotic activity in vivo. Results Nine target compounds were synthesized and confirmed by spectroscopic methods (NMR, MS). Among the synthesized compounds, salicyloyl-containing compounds (Di-8,9) showed good activity in antithrombotic activity screening tests. Conclusion The introduction of appropriate active groups can enhance the antithrombotic activity of diosgenin.