环维黄杨星D的结构改造及抗脂质氧化活性研究

Structural modification of cyclovirobuxine D and their inhibition activity on lipid peroxidation

目的以20或21-氨基甾体化合物为先导化合物,对植物活性单体———环维黄杨星D进行结构改造,以寻求抗脂质氧化活性更强的心脑血管药物。方法根据合理药物设计原理,设计合成目标化合物,并研究其抗脂质氧化活性。结果获得4个环维黄杨星D新衍生物,并经光谱证明了结构。结论采用硫代巴比妥酸(TBA)法测定脂质过氧化物(MDA),结果表明,部分化合物药理效果优于环维黄杨星D。

Aim To search for compounds through structural modification of cyclovirobuxine D, using 20 or 21-aminosteroids as lead compound for the treatment of cerebrovascular diseases with better lipid peroxidation inhibitory activity. Methods According to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested. Results Four new compounds were obtained and confirmed by spectra. Conclusion Lipid peroxidation inhibitory effects of cyclovirobuxine D analogues were tested by using TBA method. Some compounds showed better activity than that of cyclovirobuxine D.