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甘草中α-葡萄糖苷酶抑制剂的筛选

许有瑞, 倪京满*, 孟庆刚, 张承忠, 高燕, 王锐   

  1. 1.兰州大学药学院, 甘肃 兰州 730000;
    2.兰州大学生命科学院, 甘肃 兰州 730000;
    3.金川公司医院药剂科, 甘肃 金昌 737100
  • 收稿日期:2005-12-05 修回日期:2006-02-10 出版日期:2006-03-15 发布日期:2006-03-15
  • 通讯作者: 倪京满*

α-Glucosidase Inhibitors from Glycyrrhiza uralensis Fisch.

XU You-rui, NI Jing-man*, MENG Qing-gang, ZHANG Cheng-zhong, GAO Yan, WANG Rui   

  1. 1.School of Pharmacy, Lanzhou University, Lanzhou 730000, China;
    2.School of Life Science, Lanzhou University, Lanzhou 730000, China;
    3.Hospital of Jinchuan Corporation, Jinchang 737100, China
  • Received:2005-12-05 Revised:2006-02-10 Online:2006-03-15 Published:2006-03-15
  • Contact: NI Jing-man*

摘要: 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, IC50 =0.26 μg·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 = 102.4 μg·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-葡萄糖苷酶抑制剂, α-葡萄糖苷酶抑制剂, α-葡萄糖苷酶抑制剂, 甘草, 甘草, 甘草, 甘草酚, 甘草酚, 甘草酚, 甘草次酸, 甘草次酸, 甘草次酸

Abstract: Aim To screen for α-glucosidase inhibitor from Glycyrrhiza 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 investigated. Results The flavonoids of glycyrrhiza and glycyrrhetinic acid had the strongest α-glucosidase inhibitory activity. Glycyrol, β-sitosterol and liquiritin 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.

Key words: α-glucosidase inhibitor, α-glucosidase inhibitor, Glycyrrhiza uralensis Fisch., Glycyrrhiza uralensis Fisch., glycyrol, glycyrol, glycyrrhetinic acid, glycyrrhetinic acid

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Supporting: Foundation item: Ministry of Education of China (No. 204142 ), and Nature Science Foundation of Gansu Province (No. 3ZS051-A25-101).
*Corresponding author. Tel.: 86-931-8915683; fax: 86-931-8911255