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

摘要: 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。

Abstract: AimTo 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. MethodsAccording to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested. ResultsFour new compounds were obtained and confirmed by spectra. ConclusionLipid peroxidation inhibitory effects of cyclovirobuxine D analogues were tested by using TBA method. Some compounds showed better activity than that of cyclovirobuxine D.