A novel phenolate-bridged binuclear copper(II) complex, [Cu 2 II (L-3H)Cl] (1, where L = 2,6-bis[((2-hydroxybenzyl)(2-pyridylmethyl)amino)methyl]-4-methylphenol), have been synthesized and characterized. The antiproliferative activity of the complex has been tested in vitro against the human cervical cancer cell line HeLa, human non-small-cell lung cancer cell line A-549, the human breast cancer cell line MCF-7, and the human hepatic cell line LO2. The results show the complex has the low micromolar range (9.4-11.2 µM) of IC50 values towards the three cancer cell lines, which is markedly comparable to those of cisplatin. However 1 exhibited 10.6-fold less toxicity than cisplatin toward normal cells LO2, suggesting that complex 1 had high selectivity between tumor cells and normal cells. The interactions with DNA were investigated by UV-Vis absorption, fluorescence, circular dichroism, and gel electrophoresis. The results show that the copper(II) complex could strongly bind to DNA mainly by the groove binding mode and efficiently cleave the pBR322 plasmid DNA into its nicked and linear forms in the presence of excessive ascorbic acid. In addition, the evaluation of the protein binding ability shows that complex 1 could bind to human serum albumin (HSA) with a moderate binding affinity and quench the intrinsic fluorescence of HSA.

中文翻译：

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DNA裂解，DNA / HSA结合研究和酚盐桥接双核铜（II）配合物的抗增殖活性。

新型酚盐桥联的双核铜（II）配合物[Cu 2 II（L-3H）Cl]（1，其中L = 2,6-双[（（（2-羟基苄基）（2-吡啶基甲基）氨基）甲基] -4-甲基苯酚），已经合成并表征。该复合物的抗增殖活性已在体外针对人宫颈癌细胞系HeLa，人非小细胞肺癌细胞系A-549，人乳腺癌细胞系MCF-7和人肝细胞系进行了测试LO2。结果表明，该复合物对三种癌细胞系的IC50值具有较低的微摩尔范围（9.4-11.2 µM），与顺铂具有明显的可比性。但是1对正常细胞LO2的毒性比顺铂低10.6倍，表明复合物1在肿瘤细胞和正常细胞之间具有高选择性。通过紫外-可见吸收，荧光，圆二色性和凝胶电泳研究了与DNA的相互作用。结果表明，铜（II）配合物可以主要通过凹槽结合模式牢固地与DNA结合，并在过量抗坏血酸的存在下有效地将pBR322质粒DNA切割成切口和线性形式。此外，对蛋白质结合能力的评估表明，复合物1可以以中等结合亲和力结合人血清白蛋白（HSA），并淬灭HSA的固有荧光。