摘要
本文对△^5-3β，7β-二羟基甾醇（1—3）和△^5-3β，7α-二羟基甾醇（4～6）的一些核磁共振波谱特征进行了比较。活性测试表明化合物1—6对乙酰胆碱酯酶（AChE）无明显的抑制活性，对丁酰胆碱酯酶（BuChE）则有较强的抑制活性，其中24-亚甲基胆甾-5-烯-3β，7α-二醇（6）的IC50值为9．5μM。通过活性数据比较我们发现7α-羟基甾醇对丁酰胆碱酯酶的抑制活性明显比相应的7β-羟基甾醇高。我们通过计算7位羟基和四环平面之间的二面角角度来尝试解释这些活性差别。
Some NMR spectral characteristics of △^5-3β,7β-dihydroxyl sterols （1 - 3） and △^5-3β,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.
出处
《天然产物研究与开发》
CAS
CSCD
2006年第6期893-895,共3页
Natural Product Research and Development
基金
The work was supported bythe 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).
