化学学报 ›› 2004, Vol. 62 ›› Issue (8): 783-788. 上一篇    下一篇

研究论文

Zn2+,Cu2+及Ni2+对二甲双胍的配合作用及降血糖活性研究

朱苗力, 卢丽萍, 杨频   

  1. 山西大学分子科学研究所, 化学生物学与分子工程教育部重点实验室, 太原, 030006
  • 投稿日期:2003-12-12 修回日期:2004-03-08 发布日期:2014-02-18
  • 通讯作者: 杨频,E-mail:yangpin@sxu.edu.cn E-mail:yangpin@sxu.edu.cn
  • 基金资助:
    国家自然科学基金(No.20171031)、山西省青年基金(No.20011007)和2002年山西省归国留学基金资助项目.

Studies on the Structures and Antihyperglycemic Effects of Zn2+, Cu2+, Ni2+-Metformin Complexes

ZHU Miao-Li, LU Li-Ping, YANG Pin   

  1. Institute of Molecular Science, Chemical Biology and Molecular Engineering Laboratory of Education Ministry, Shanxi University, Taiyuan 030006
  • Received:2003-12-12 Revised:2004-03-08 Published:2014-02-18

二甲双胍盐酸盐、硝酸盐及与Zn2+, Cu2+, Ni2+三种金属离子配合物的结构特点、电荷分布和二甲双胍配合物对四氧嘧啶糖尿病小鼠血糖影响的研究表明:Zn2+配合物表现为较为少见的单齿配位,而Cu2+, Ni2+配合物表现为双齿配位.进一步电荷分布计算发现,与端基N原子相比,二甲双胍的桥基N原子具有较高的负电荷.三种金属离子配合物对四氧嘧啶糖尿病小鼠血糖的影响研究显示,桥基N配位掩蔽后,二甲双胍的降血糖功能丧失.说明桥基N对二甲双胍的降血糖作用具有重要意义.

关键词: 二甲双胍金属配合物, 电荷分布, 降血糖活性

The structures and charge distribution as well as antihyperglycemic effects of 1,1-dimethylbiguanide (metformin) metal (Zn2+, Cu2+ and Ni2+) complexes were investigated. Metformin can complex with Zn2+ at bridging N, forming a rare monodentate complex, but complex with Cu2+ and Ni2+ at terminal N atoms, giving rise to bidentate complexes. The charge distribution calculated by DFT and ab initio methods indicates that the bridging N atom has more negative charge than terminal N atoms. The antihyperglycemic effects of metformin metal complexes show that the monodentate complex has no effect and bidentate complexes still keep the activity but less efficient than metformin alone. This result suggests that the bridging N atom of metformin be important for its antihyperglycemic effect.

Key words: complexes of metal-metformin, charge distribution, antihyperglycemic effect