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评价双价过渡金属腙配合物的 DNA 结合、DNA 切割、蛋白质结合和体外细胞毒性活性。

Evaluation of DNA binding, DNA cleavage, protein binding and in vitro cytotoxic activities of bivalent transition metal hydrazone complexes.

机构信息

Department of Chemistry, Bharathiar University, Coimbatore 641 046, India.

出版信息

Eur J Med Chem. 2011 Aug;46(8):3376-87. doi: 10.1016/j.ejmech.2011.05.001. Epub 2011 May 8.

DOI:10.1016/j.ejmech.2011.05.001
PMID:21600679
Abstract

Divalent Co, Ni and Cu hydrazone complexes containing [N'-(phenyl(pyridine-2-yl)methylidene) benzohydrazide] ligand were synthesised and characterised. Interactions of these complexes with DNA revealed an intercalative mode of binding between them. Further, all the hydrazone chelates showed moderate ability to cleave pUC19 DNA. Synchronous fluorescence spectra proved that the interaction of metal complexes with bovine serum albumin (BSA) resulted in a conformational change of the latter. Assay on the cytotoxicity of the above complexes against HeLa tumor cells and NIH 3T3 normal cells revealed that the complexes are toxic only against tumor cells but not to normal cells. In all the biological assays, the complex with copper ion as the metal center showed enhanced activities than the other two.

摘要

二价 Co、Ni 和 Cu 腙配合物,含有[N'-(苯(吡啶-2-基)亚甲基)苯甲酰肼]配体,被合成并进行了表征。这些配合物与 DNA 的相互作用表明它们之间存在一种嵌入结合模式。此外,所有的腙螯合物都显示出适度的切割 pUC19 DNA 的能力。同步荧光光谱证明,金属配合物与牛血清白蛋白(BSA)的相互作用导致后者构象发生变化。对上述配合物对 HeLa 肿瘤细胞和 NIH 3T3 正常细胞的细胞毒性进行的测定表明,这些配合物仅对肿瘤细胞有毒,而对正常细胞无毒。在所有的生物学测定中,以铜离子为金属中心的配合物显示出比其他两种配合物更高的活性。

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