茜草抑制α-葡萄糖苷酶活性成分研究  

α-Glucosidase inhibitors from Rubia cordifolia

作　　者：康文艺[1] 张丽[1] 宋艳丽[1] 

机构地区：[1]河南大学药学院天然药物研究所,河南开封475004

出　　处：《中国中药杂志》2009年第9期1104-1107,共4页China Journal of Chinese Materia Medica

基　　金：河南省教育厅基础研究计划(2008A360002)

摘　　要：目的：寻找茜草中抑制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,并对活性化合物进行酶抑制动力学研究。结果：茜草三氯甲烷提取物具有很高的活性,从中分离出3个具抑制α-葡萄糖苷酶活性的蒽醌类化合物,分别鉴定为：1,3-二羟基-2-甲基蒽醌（1）,1-羟基-2-甲基蒽醌（2）和1,2-二羟基蒽醌（3）,其中化合物3（IC50=7.97 mg.L^-1）活性最好,与1（IC50=35.96 mg.L^-1）和2（IC50=15.98 mg.L^-1）的活性都明显高于阳性对照阿卡波糖（IC50=1 081.27 mg.L^-1）。化合物1和2为竞争性抑制类型。结论：化合物1-3为首次报道对α-葡萄糖苷酶抑制活性。Objective： To search α-glucosidase inhibitors from Rubia cordifolia. Methed： The α-glucosidase inhibitors were 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 kinetics of the inhibitors were also investigated. Result： The chloroform extract showed high inhibitory activity, and three active compounds were isolated and identified as 1,3-dihydroxy-2-methylanthraquinone （ 1 ）, 1-hydroxy-2-methylanthraquinone （ 2 ） and 1,2-dihydroxyanthraquinone （ 3 ）. The IC50 values of compound 1-3 were all lower than that of acarbose. Compound 1 and 2 shown competitive type manner on α-glucosidase,whereas compound 3 shown noncompetitive type model. Conclusion： Compounds 1-3 as strong inhibitors of α-glucosidase were reported for the first time.

关 键 词：茜草 Α-葡萄糖苷酶 抑制类型 

分 类 号：R284[医药卫生—中药学]