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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9.5μM。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。
In this paper, some NMR spectra of Δ5-3β, 7β-dihydroxy sterols (1-3) and Δ5-3β, 7α-dihydroxy sterols (4-6) were compared. The activity test showed that compounds 1-6 had no obvious inhibitory activity on acetylcholinesterase (AChE) and strong inhibitory activity on butyrylcholinesterase (BuChE), among which 24-methylenecholest-5-ene -3β, 7α-diol (6) has an IC50 value of 9.5 μM. By comparing the activity data, we found that the inhibitory activity of 7α-hydroxysterol on butyrylcholinesterase was significantly higher than that of the corresponding 7β-hydroxysterol. We try to explain these differences in activity by calculating the dihedral angles between the 7-hydroxyl and the tetracyclic planes.