CAJ | 학술논문

本文对Δ5-3β,7β-二羟基甾醇(1～3)和Δ5-3β,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9.5 μM.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.
본문대Δ5-3β,7β-이간기치순(1～3)화Δ5-3β,7α-이간기치순(4～6)적일사핵자공진파보특정진행료비교.활성측시표명화합물1～6대을선담감지매(AChE)무명현적억제활성,대정선담감지매(BuChE)칙유교강적억제활성,기중24-아갑기담치-5-희-3β,7α-이순(6)적IC50치위9.5 μM.통과활성수거비교아문발현7α-간기치순대정선담감지매적억제활성명현비상응적7β-간기치순고.아문통과계산7위간기화사배평면지간적이면각각도래상시해석저사활성차별.
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.