摘要
目的:寻找滇丁香中具有抑制α-葡萄糖苷酶活性的成分.方法:利用体外抑制α-葡萄糖苷酶活性模型进行追踪,采用各种色谱法分离,运用多种谱学技术鉴定结构,并对活性较强的几个单体化合物进行酶抑制动力学研究.结果:滇丁香的醋酸乙酯部分具有较高的活性,从中分离出5个抑制α-葡萄糖苷酶活性的化合物,分别鉴定为:莨菪内酯(1),5-甲氧基-8-羟基香豆素(2),1α,3β,24-三羟基熊果酸(3),熊果酸(4)和齐墩果酸(5),其中化合物4(IC_(50) 3-3 mg·L~(-1)),5(IC_(50)2.88 mg·L~(-1))的活性最好,明显高于阳性对照阿卡波糖(IC_(50) 1081.27 mg·L~(-1)).化合物3为竞争性抑制.结论:化合物1～4为首次报道对α-葡萄糖苷酶有抑制活性.
Abstract
Objective: To search α-glucosidase inhibitors from Luculia pinciana. Method: The α-glucosidase inhibitor was isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetic of the isolations was also investigated. Result: The ethyl acetate extract showed strongest inhibitory activity, and five active compounds were isolated and identified as scopletin (1), 5-methoxy-8-hydroxycoumarin (2), 1α,3β,24-trihydroxyursolic acid (3), ursolic acid (4) and oleanolic acid (5). The IC_(50) values of all compounds were lower than that of acarbose. Four of them shown noncompetitive type manner on a-glucosidase inhibition except that compound 3 is competitive type manner. Conclusion: Compounds 1-4 as the inhibitors of a-glucosidase were reported for the first time.
基金项目
河南省教育厅基础研究计划(2008A360002)
国家科技期刊平台
NSTL
维普
万方数据