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首页> 外文期刊>Journal of Biomolecular Structure and Dynamics >New binary copper(II) complexes containing intercalating ligands: DNA interactions, an unusual static quenching mechanism of BSA and cytotoxic activities
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New binary copper(II) complexes containing intercalating ligands: DNA interactions, an unusual static quenching mechanism of BSA and cytotoxic activities

机译：含有嵌入配体的新二元铜（II）配合物：DNA相互作用，BSA和细胞毒性活性的不寻常的静态猝灭机理

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摘要

New binary copper(II) complexes - [Cu(4-mphen)2(NO_3)]NO_3-H_2O (1), [Cu(5-mphen)_2 (NO_3)]NO_3-H_2O (2), the known complex [Cu(dmphen)_2(NO_3)]NO_3 (3) and [Cu(tmphen)_2 (NO_3)]NO_3-H_2O (4) - (4-mphen: 4-methyl-l,10-phenanthroline, 5-mphen: 5-methyl-l,10-phenanthroline, dmphen: 4,7-dimethyl-l,10-phenanthroline, tmphen: 3,4,7,8-tetramethyl-l, 10-phenanthroline), have been synthesized and characterized by CHN analysis, ESI-MS, FTIR and single-crystal X-ray diffraction techniques. Interaction of these complexes with calf thymus DNA (CT-DNA) has been investigated by absorption spectral titration, ethidium bromide (EB) and Hoechst 33,258 displacement assay and thermal denaturation measurement. These complexes cleaved pUC19 plasmid DNA in the absence and presence of an external agent. Notably, in the presence of H_2O_2 as an activator, the cleavage abilities of these complexes are obviously enhanced at low concentration. Addition of hydroxyl radical scavengers like DMSO shows significant inhibition of the DNA cleavage activity of these complexes. BSA quenching mechanism was investigated with regard to the type of quenching, binding constant, number of binding locations and the thermodynamic parameters. The experimental results suggested that the probable quenching mechanism was an unusual static process and hydrophobic forces play a dominant role. The CT-DNA and BSA binding efficiencies of these complexes follow the order: 4 >3 >1 >2. Furthermore, in vitro cytotoxicities of these complexes on tumor cells lines (Caco-2, MCF-7 and A549) and healthy cell line (BEAS-2B) showed that these complexes exhibited anticancer activity with low IC_(50) values. The effect of hydrophobicity of the methyl-substituted phenan-throlines on DNA and protein binding activities of these complexes is discussed.
机译：新二元铜（II）配合物 - [Cu（4-Mphen）2（NO_3）] NO_3-H_2O（1），[Cu（5-Mphen）_2（NO_3）] NO_3-H_2O（2），已知复杂[ Cu（Dmphen）_2（NO_3）] NO_3（3）和[Cu（TMPHEN）_2（NO_3）] NO_3-H_2O（4） - （4-MPHEN：4-甲基-1,10-菲咯啉，5门：已经合成了5-甲基-1，10-菲咯啉，Dmphen：4,7-二甲基-1,10-菲林，Tmphen：3,4,7,8-四甲基-1,10-菲咯啉）。分析，ESI-MS，FTIR和单晶X射线衍射技术。通过吸收光谱滴定，溴化乙锭（EB）和Hoechst 33,258位移测定和热变性测量，研究了这些配合物与CALF胸腺DNA（CT-DNA）的相互作用。这些复合物在没有和存在外部剂的情况下切割PUC19质粒DNA。值得注意的是，在H_2O_2作为活化剂的情况下，在低浓度下显着增强了这些配合物的切割能力。羟基自由基的加入羟基自由基，如DMSO显示出这些配合物的DNA切割活性的显着抑制。研究了BSA淬火机构关于淬火，结合常数，结合位置的数量和热力学参数的类型研究。实验结果表明，可能的淬火机制是一种不寻常的静态过程，疏水力起到显着作用。这些配合物的CT-DNA和BSA结合效率遵循顺序：4> 3> 1> 2。此外，在肿瘤细胞系（CaCO-2，MCF-7和A549）和健康的细胞系（BEA-2B）上的这些复合物的体外细胞毒性表明，这些配合物具有低IC_（50）值的抗癌活性。讨论了甲基取代的磷酸血管血管对这些配合物的DNA和蛋白质结合活性的影响。

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