α-Glucosidase Inhibitors from Glycyrrhiza uralensis Fisch.  

甘草中α-葡萄糖苷酶抑制剂的筛选(英文)

作　　者：许有瑞[1] 倪京满[1] 孟庆刚[1] 张承忠[1] 高燕 王锐[3] 

机构地区：[1]兰州大学药学院,甘肃兰州730000 [2]金川公司医院药剂科,甘肃金昌737100 [3]兰州大学生命科学院,甘肃兰州730000

出　　处：《Journal of Chinese Pharmaceutical Sciences》2006年第1期24-27,共4页中国药学（英文版）

基　　金：MinistryofEducationofChina(No.204142),andNatureScienceFoundationofGansuProvince(No.3ZS051-A25-101).

摘　　要：Aim To screen for α-glucosidase inhibitor from Glyeyrrhiza uralensis Fisch.. Methods Glycyrrhizic acid, glycyrrhetinic acid, flavonoids of glycyrrhiza, alkaloids of glycyrrhiza, and glycyrrhiza polysaccharides were isolated from the root of Glycyrrhiza uralensis Fisch. respectively. Three compounds were isolated from the flavonoids of glycyrrhiza as guided by the α-glucosidase inhibitory test in vitro. Moreover, the characteristics of inhibitory kinetics of glycyrol and glycyrrhetinic acid were investi- gated. Results The flavonoids of glycyrrhiza and glycyrrhetinic acid had the strongest α-glucosidase inhibitory activity. Glycyrol,β-sitosterol and liquifitin were isolated and identified. Glycyrol was a fast- binding, reversible, noncompetitive α-glucosidase inhibitor, showing IC50 at 0.26 μg·mL^-1 Glycyrrhetinic acid was a fast-binding, irreversible α-glucosidase inhibitor, showing IC50 at 102.4 μg·mL^-1. Conclusion Glycyrol is an effective α-glucosidase inhibitor.目的从甘草中筛选α-葡萄糖苷酶抑制剂。方法从甘草中分别提取纯化甘草酸、甘草次酸、甘草黄酮、生物碱和多糖,并进行活性比较。然后以体外α-葡萄糖苷酶抑制试验为指导,从甘草黄酮中提取分离活性成分,并对其抑制动力学特性进行研究。结果甘草黄酮和甘草次酸具有较强的α-葡萄糖苷酶抑制活性,从甘草黄酮中分离鉴定了一活性成分—甘草酚,其表现为快速的非剂量依赖性的非竞争性抑制类型,且IC50=0.26μg·mL-1,而甘草次酸却表现为快速的剂量依赖性的不可逆抑制类型,IC50=102.4μg·mL-1。结论甘草酚可作为一种有效的α-葡萄糖苷酶抑制剂。

关 键 词：α-glucosidase inhibitor Glycyrrhiza uralensis Fisch. glycyrol glycyrrhetinic acid 

分 类 号：R284.1[医药卫生—中药学]