钌（II）多吡啶配合物的合成、DNA 结合和拓扑异构酶抑制活性。
Synthesis, DNA-binding and topoisomerase inhibitory activity of ruthenium(II) polypyridyl complexes.
机构信息
MOE Laboratory of Bioinorganic and Synthetic Chemistry, State Key Laboratory of Optoelectronic Materials and Technologies, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, PR China.
出版信息
Eur J Med Chem. 2011 Apr;46(4):1056-65. doi: 10.1016/j.ejmech.2011.01.019. Epub 2011 Jan 21.
Two ruthenium(II) complexes Ru(bpy)(2)(bfipH) (1) and Ru(phen)(2)(bfipH) (2) have been synthesized and characterized. The DNA-binding behaviors of complexes were studied by using spectroscopic and viscosity measurements. Results suggested that the two complexes bind to DNA in an intercalative mode. Complexes 1 and 2 can efficiently photocleave pBR322 DNA in vitro under irradiation, singlet oxygen ((1)O(2)) was proved to contribute to the DNA photocleavage process. Topoisomerase inhibition and DNA strand passage assay confirmed that two Ru(II) complexes acted as efficient dual inhibitors of topoisomerases I and II. In MTT cytotoxicity studies, two Ru(II) complexes exhibited antitumor activity against BEL-7402, HeLa, MCF-7 tumor cells. The AO/EB staining assay indicated that Ru(II) complexes could induce the apoptosis of HeLa cells.
已经合成并表征了两种钌（II）配合物 Ru(bpy)(2)(bfipH)（1）和Ru(phen)(2)(bfipH)（2）。通过光谱和粘度测量研究了配合物的 DNA 结合行为。结果表明，两种配合物以嵌入模式与 DNA 结合。配合物 1 和 2 在光照下可有效地在体外光解 pBR322 DNA，证明单线态氧（(1)O(2)）有助于 DNA 光解过程。拓扑异构酶抑制和 DNA 链通过实验证实，两种 Ru(II) 配合物是拓扑异构酶 I 和 II 的有效双重抑制剂。在 MTT 细胞毒性研究中，两种 Ru(II) 配合物对 BEL-7402、HeLa、MCF-7 肿瘤细胞表现出抗肿瘤活性。AO/EB 染色实验表明，Ru(II) 配合物可诱导 HeLa 细胞凋亡。
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