化学学报 ›› 1988, Vol. 46 ›› Issue (4): 398-401. 上一篇    下一篇

研究论文

抗肿瘤活性化合物去甲基斑蟊-5-烯酸的金属配位能力的研究

黄仲贤;杨力伟;周春儿   

  1. 复旦大学化学系
  • 发布日期:1988-04-15

Binding ability of antitumour compound 7-oxabicyclo-(2,2,1)-hept-5-ene-2,3-dicarboxylic acid to metal ions

HUANG ZHONGXIAN;YANG LIWEI;ZHOU CHUNER   

  • Published:1988-04-15

斑蟊类化合物是一种潜在的强有力的螯合剂, 本文研究了去甲斑蝥-5-烯酸(7-氧杂二环[2,2,1]-庚-5-烯-2,3-二羧酸)与一系列生命必需金属元素间结合能力, 与其它二元羧酸比较, 表现出很大的配位能力, 这是环氧原子参与配位所致, 它已由X射线分析证实. 研究了浓度, 酸度的影响, 这关系到一些配位体药物的抗癌活性.

关键词: 抗癌药, 锌络合物, 铁络合物, 铜络合物, 二环庚烯 P, 氧杂环化合物, 钙络合物, 氢络合物, 镁络合物, 铝络合物

The binding ability of the antitumor compound 7-oxabicyclo-[2.2.1]hept-5-ene-2,3-dicarboxylic acid (OHDA) (I) to essential metal ions was studied potentiometrically at 37?and 150 mmol譫m-3 NaCl. Compared to other dicarboxylic acids, OHDA complexes show extra stability implying the binding of the epoxy O atom to metal ions. The coordination of the epoxy O donor was proved by X-ray crystal diffraction measurements of metal2+-OHDA complexes. Speciation studies illustrate that at pH 6-8, the dominant complex species is Zn2+-OHDA, but at low OHDA concentration (10-4-10-7 mol譫m-3), the Mn2+-OHDA complex species shares the predominant position with Zn2+-OHDA in the complex system. This fact may be related to the antitumor activity of some ligand drug mols. by disturbing normal distribution and metabolism of essential metal ions.

Key words: ANTICARCINOGEN, ZINC COMPLEX, IRON COMPLEX, COPPER COMPLEX, BICYCLOHEPTENE P, OXYGEN HETEROCYCLICS, CALCIUM COMPLEX, HYDRIDO COMPLEX, MAGNESIUM COMPLEX, ALUMINIUM COMPLEX

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