DNA-binding and cytotoxicity studies of ruthenium(II) mixed-ligand complexes containing two intercalative ligands
DNA-binding and cytotoxicity studies of ruthenium(II) mixed-ligand complexes containing two intercalative ligands
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含有两个插入配体的钌 (II) 混合配体复合物的 DNA 结合和细胞毒性研究
DOI：
10.1016/j.ica.2012.01.023
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发表时间：
2012-05-30
影响因子：
2.8
通讯作者：
Luan, Fang
中科院分区：
文献类型：
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作者：
Jin, Lianhe;Tan, Lifeng;Luan, Fang
含有两个插入配体的新型 Ru(II) 聚吡啶配合物，[Ru(dppz)(2)phen](2+) (1) (dppz =联吡啶酮-[3,2-a:2',3'-c]吩嗪，phen = 1,10-菲咯啉) 和 [Ru(dppz)(2)dpq](2+) (2) (dpq =已合成并表征了二-吡啶并[3,2-f:2',3'-h]喹喔啉）。通过光谱和粘度测量研究了两种复合物与小牛胸腺 DNA (CT-DNA) 的结合。结果表明，配合物 1 和 2 通过嵌入与 DNA 结合，配合物 2 的 DNA 结合亲和力远强于配合物 1。然而，两种配合物与 DNA 的平衡结合常数均小于具有一种嵌入配体的 [Ru(phen)(2)(dppz)](2+) 和 [Ru(bpy)(2)(dppz)](2+) (bpy = 2,2'-联吡啶)，这可能可以通过两个插入配体 dppz 的空间位阻效应来解释。另一方面，比较复合物1和复合物2，前者可以作为DNA的分子“光开关”，这种差异可能是由于复合物1和2中辅助配体不同所致。此外，两种复合物在体外对选定的肿瘤细胞系表现出不同的抗肿瘤活性，并且可以使细胞凋亡。 (C) 2012 Elsevier B.V. 保留所有权利。
New Ru(II) polypyridyl complexes containing two intercalative ligands, [Ru(dppz)(2)phen](2+) (1) (dppz = dipyrido-[3,2-a:2',3'-c]phenazine, phen = 1,10-phenanthroline) and [Ru(dppz)(2)dpq](2+) (2) (dpq = di-pyrido[3,2-f:2',3'-h]quinoxaline) have been synthesized and characterized. The binding of both complexes with calf thymus DNA (CT-DNA) has been investigated by spectroscopic and viscosity measurement. Results indicate that complexes 1 and 2 bind to DNA through intercalation, and the DNA binding affinity of complex 2 is much stronger than that of complex 1. However, the equilibrium binding constants of both complexes with DNA are smaller than that of [Ru(phen)(2)(dppz)](2+) and [Ru(bpy)(2)(dppz)](2+) (bpy = 2,2'-bipyridine) with one intercalative ligand, which may be interpreted by the steric hindrance effect of the two intercalated ligand dppz. On the other hand, comparing complex 1 with complex 2, the former can serve as a molecular "light switch" for DNA, and this difference may be due to the different ancillary ligands in complexes 1 and 2. In addition, both complexes demonstrate different antitumor activities against selected tumor cell lines in vitro, and can make the cells apoptosis. (C) 2012 Elsevier B.V. All rights reserved.