四氮杂轮烯合铜络合物的合成和其瘤细胞灭杀作用

    Synthesis and Tumor Cell Killing Effect of Tetraaza-Annuleno Copper(Ⅱ) Complexes

    • 摘要: 借模板缩聚作用,合成了若干种四氮杂-16-轮烯合铜(Ⅱ)或镍(Ⅱ),以及相应的三氮杂-12-轮烯络合物。其中,用人肺腺癌细胞株在体外,测试了若干种四苯四氮杂-16-轮烯合铜(Ⅱ)盐(TAAB)的瘤细胞灭杀效应。在二甲亚砜中,CU(TAAB)(NO2)2(Ⅰ),Cu(TAAB)Cl2(Ⅱ),Cu(4-Cl-TAAB)Cl2和Cu(4-Br-TAAB)Cl2于黑暗和光照下(括号中为光照)的抑制率分别为:75(85),82(90),64(75),55(57)和85(76)。在水中Ⅰ、Ⅱ的抑制率相应为86(82),和85(76),作为对照物的顺铂在水溶液等当微克分子浓度时,未观察到应答,因此,所有上述试验过的CuTAAB盐,都显示很高的瘤细胞灭杀作用,以二甲亚砜作溶剂时,可以观察到光的增效作用,而在水中测试时,则未发现光的增效作用。

       

      Abstract: Some tetraaza-16-annuleno-, triaza-12 annuleno-copper(Ⅱ) or Ni(Ⅱ) complexes are synthesized by condensed templete polymerization in this paper. The tumor cell killing effects of tetrabenzo-tetraaza-16-annuleno Cu(Ⅱ) salts (RAAB) are tested with human lung adenoma cell in vitro. The inhibition ratios(%), in DMSO, of Cu(TAAB)(NO3)2(Ⅰ), Cu(TAAB)Cl2(Ⅱ), Cu(4-Cl-TAAB)(NO3)2, Cu(4-Cl-TAAB)Cl2 and Cu(4-Br-TAAB)Cl2 in dark and under light (data in brackets) are 75(85), 82(90), 64(75), 55(57) and 33(32), respectively. The inhibition rations, in water, of Ⅰ and n Ⅱ are 86(82) and 85(76), respectively, but the response of cisplatin as comparative object in water is not observed in equivalent micromolecular concentration. Therefore, all of the tested Cu-TAAB salts show very high tumor cell killing effect, The enhancement for this effect under light can be observed in DMSO as solvent, but cannot be detected in water under out experimental condition.

       

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