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分别以咪唑(imidazole)、2,2′-联咪唑(2,2′-biimidazole)和邻菲咯啉(phenanthroline)为配体与氯铂酸钾作用合成了三种铂(Ⅳ)二元配合物并进行了表征,确定其化学组成分别为Pt(im)2Cl4.H2O(Ⅰ),PtH2biimCl4.H2O(Ⅱ)和PtPhenCl4.H2O(Ⅲ)(im=imidazole,H2biim=2,2′-biimidazole,Phen=phenanthroline)。抑菌实验结果表明这3种配合物都具有一定的抑菌作用,并以溴化乙锭为荧光探针,研究了配合物与小牛胸腺ct-DNA的相互作用;采用电子吸收光谱法、荧光光谱法、热变性及盐效应等手段探讨了其作用机制并求出了结合常数K、结合位点数n以及热力学参数。实验结果表明:3种配合物均可以嵌插的方式与DNA发生强而稳定的作用,导致DNA双螺旋结构的破坏,使其具有一定的抑菌活性。
Three kinds of platinum (Ⅳ) binary complexes were synthesized by imidazole, 2,2’-biimidazole and phenanthroline as ligands respectively. The chemical composition of Pt (im) 2Cl4.H2O (Ⅰ), PtH2biimCl4.H2O (Ⅱ) and PtPhenCl4.H2O (Ⅲ) were determined and identified as im = imidazole (H2biim = 2,2’-biimidazole, Phen = phenanthroline). The results of antibacterial experiment showed that all three complexes had antibacterial activity. The interaction between the complex and calf thymus ct-DNA was studied by using ethidium bromide as fluorescent probe. The electron absorption spectrometry Fluorescence spectroscopy, thermal denaturation and salt effects and other means to explore its mechanism of action and to find the binding constant K, the number of binding sites n and thermodynamic parameters. The experimental results show that all the three complexes can intercalate with DNA strong and stable, leading to the destruction of DNA double helix structure, which has certain antibacterial activity.