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双(2-取代-3-羟基-4-吡喃酮)合铜(II)配合物的合成和降血糖作用

Synthesis and Anti-hyperglycemic Effect of Copper(II) Bis(2-substituted 3-hydroxy-4-pyronate)

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【作者】 谌喜珠牛艳芬刘伟平李玲王玉天李艳蓉高文桂余尧

【Author】 CHEN, Xi-Zhua NIU, Yan-Fenb LIU, Wei-Ping*,a LI, Lingb WANG, Yu-Tiana LI, Yan-Rongb GAO, Wen-Guia YU, Yaoa (a Kunming Institute of Precious Metals, Kunming 650221) (b Yunnan Pharmacological Laboratories of Natural Products, Kunming 650031)

【机构】 昆明贵金属研究所云南省天然药物药理重点实验室昆明贵金属研究所 昆明650221昆明650031昆明650221

【摘要】 合成了双(2-取代-3-羟基-4-吡喃酮)合铜(II)配合物,采用元素分析、质谱、红外光谱、电子光谱、电子自旋共振谱表征了它们为平面正方型配合物,中心离子和配体的物质的量比为1∶2.在STZ-糖尿病小鼠模型上,其中双(2-乙基-3-羟基-4-吡喃酮)合铜(II)在10mg/kg的剂量下灌胃给药,能增加血清胰岛素的合成和分泌、降低糖尿病小鼠的血糖水平,显示出良好的抗糖尿病的作用.该配合物毒性低,对正常小鼠灌胃给药的半数致死量LD50是855.9mg/kg.

【Abstract】 Copper(II) bis(2-substituted 3-hydroxy-4-pyronate), where the substituent is CH3/C2H5/CH2OH, was synthesized by the reaction between CuCl2 and sodium 2-substituted 3-hydroxy-4-pyronate in aqueous solution, followed by recrystallizaton in water. By using elemental analysis, IR, UV, MS and EPR spectra, their chemical structures were determined to be planar square complexes with 1∶2 molar ratio of Cu to the pyronate in a molecule. The complexes were submitted to the test of preliminary toxicity and anti-hyperglycemic effect on STZ-diabetic mice. The results show that one of the complexes, copper(II) bis(2-ethyl-3-hydroxy-4-pyronate), increased the synthesis and release of the serum insulin, and lowered the blood glucose level in mice at the dose of 10 mg/kg, exhibiting good anti-hyperglycemic activity. The complex was also safe with LD50 of 855.9 mg/kg in healthy mice.

【基金】 国家自然科学基金(No.30260118);云南自然科学基金(No.2002C0019R)资助项目
  • 【文献出处】 化学学报 ,Acta Chimica Sinica , 编辑部邮箱 ,2006年09期
  • 【分类号】R914;R96
  • 【被引频次】2
  • 【下载频次】154
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