天然产物研究与开发2006，Vol.18Issue(6)：893-895,3.
Δ5-3β,7β-二羟基甾醇及其C-7差向异构体波谱特征及胆碱酯酶的抑制活性
Spectral Characteristics and Cholinesterase Inhibitory Activities of Some Δ5-3β, 7β-Dihydroxyl Sterols and Their C-7 Epimers
摘要
Abstract
Some NMR spectral characteristics of Δ5-3β,7β-dihydroxyl sterols (1～3) and Δ5-3β,7α-dihydroxyl sterols (4 ～ 6)were correlated. In biological study, compounds 1～6 showed no evident inhibitory activities against acetylcholinesterase (AChE), but they all possessed inhibitory potential in a concentration-dependent manner against butyrylcholinesterase(BuChE). Among them, the most active compound is 24-methylenecholest-5-ene-3β,7α -diol (6) with IC50 value of 9.5 μM.For the title compounds,the configuration of C-7 seemed to be important to the BuChE inhibitory activities. The relationship between inhibitory activities and dihedral angle between the 7-hydroxyl group and tetracyclic plane was discussed.关键词
Δ5-3β,7β-二羟基甾醇/Δ5-3β,7α-二羟基甾醇/胆碱酯酶/二面角Key words
Δ5-3β, 7β-dihydroxyl sterols/Δ5-3β, 7 α-dihydroxyl sterols/AChE/dihedral angle分类
医药卫生引用本文复制引用
陆伟刚,张翠仙,郑康成,苏镜娱,曾陇梅..Δ5-3β,7β-二羟基甾醇及其C-7差向异构体波谱特征及胆碱酯酶的抑制活性[J].天然产物研究与开发,2006,18(6):893-895,3.基金项目
The work was supported by the National High Technology Development Project (2001AA624030), the Natural Science Foundation of Guangdong Province (04300569), and the Youth Teacher Foundation of Sun Yat-Sen University (1131002). （2001AA624030）
