| 三元混配铜(Ⅱ)配合物的晶体结构、DNA作用及其生物活性 |
| Crystal Structure, DNA Binding Properties and Biological Activities of a Ternary Mixed-Ligand Copper(Ⅱ) Complex |
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| 摘要: 利用溶剂缓慢挥发法合成了以5-氯-2-（2'-吡啶基）苯并咪唑为主配体、L-苯丙氨酸根为辅助配体的三元混配铜（Ⅱ）配合物：[Cu（HPBC）（L-Phe）（H2O）]ClO4（简称为1，HPBC=5-氯-2-（2'-吡啶基）苯并咪唑，L-Phe=L-苯丙氨酸根）。采用元素分析、红外光谱、紫外可见光谱、摩尔电导率测定和电喷雾质谱等手段对配合物1进行了表征，利用X射线单晶衍射确定配合物具有五配位的变形四方锥构型，并通过电子吸收光谱、荧光光谱、粘度测定及分子对接等方法揭示了配合物主要以插入作用的方式与小牛胸腺DNA（CT-DNA）结合。配合物对被测微生物（李斯特菌、金黄色葡萄球菌和大肠杆菌）及癌细胞（SGC-7901、Bel-7402、HeLa和A549）显示出良好的抗菌和细胞毒活性（IC50=1.69~2.50 μmol·L-1）。最重要的是，通过确定细胞的形态变化（AO/EB双染法）及细胞周期测定分析，揭示了配合物1通过DNA结合的途径诱导SGC-7901细胞凋亡。 |
| 关键词: 铜(Ⅱ)配合物 5-氯-2-(2'-吡啶基)苯并咪唑 L-苯丙氨酸 DNA作用 抗菌 抗肿瘤活性 |
| 基金项目: 国家自然科学基金（No.21701195）和广东省自然科学基金（No.2015A030313423）资助。 |
| Abstract: A new ternary Cu(Ⅱ) complex[Cu(HPBC)(L-Phe)(H2O)]ClO4 (1) was synthesized with 5-chloro-2-(2'-pyridyl) benzimidazole (HPBC) as the main ligand and L-phenylalaninate (L-Phe) as the auxiliary ligand. Complex 1 was characterized by elemental analysis, various spectroscopic methods and molar conductivity measurement, and the X-ray crystallographic study was used to determine the crystallographic structure of the complex, which exhibits a five-coordinated distorted square-pyramidal geometry. The binding property of the complex toward calf thymus DNA (CT-DNA) was studied by electronic absorption, competitive fluorescence titration, viscosity measurement and molecular docking technology, revealing that the complex mainly bound to DNA by an intercalative mode. The antibacterial activities (Listeria monocytogenes, Staphylococcus aureus and Escherichia coli) of Cu(ClO4)2, HPBC and the complex were tested by Oxford Cup method. In addition, the complex displayed favorable cytotoxic activities toward all the tested cancer cells such as SGC-7901, Bel-7402, HeLa and A549 with IC50 values of 1.69~2.50 μmol·L-1. Most importantly, the possible anticancer mechanism of the complex was explored by determining the morphological changes of cells (AO/EB double staining method) and cell cycle measurement analyses. The results revealed that the complex could induce apoptosis through the DNA binding pathway. CCDC:2032899. |
| Keywords: copper(Ⅱ) complex 5-chloro-2-(2'-pyridyl)benzimidazole L-phenylalanine DNA interaction antimicrobial anticancer activity |
| 投稿时间：2020-07-06 修订日期：2020-10-28 |
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| 蔡戴宏,莫慧雯,何良,乐学义.三元混配铜(Ⅱ)配合物的晶体结构、DNA作用及其生物活性[J].无机化学学报,2021,37(1):74-84. |
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