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DNA-binding, molecular docking studies and biological activity studies of ruthenium(II) polypyridyl complexes

机译：钌（II）多吡啶基配合物的DNA结合，分子对接研究和生物活性研究

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Anticancer properties of chemically synthesized compounds have been evaluated for efficacy and selectivity. A new ligand PTCP (PTCP = 2-phenanthren-9-yl-1H-1,3,7,8-tetraazacyclopenta[l]phenanthrene) and its three new ruthenium(II) polypyridyl complexes [Ru(N–N)2(PTCP)](ClO4)2 (N–N: phen = 1,10-phenanthroline 1; dmp = 2,9-dimethyl-1,10-phenanthroline 2; ttbpy = 4,4′-di-tert-butyl-2,2′-bipyridine 3) were synthesized and characterized by elemental analysis, ESI-MS, IR, 1H NMR and 13C NMR. In this report, we investigated the cytotoxicity in vitro of the complexes against several cancer cell lines SGC-7901, HepG2, HeLa, SiHa and normal cell NIH3T3. The results show that complexes show highly anti-proliferation activity toward SGC-7901 and low cytotoxic activity against normal cell NIH3T3. The relationship between anti-proliferation and molecular interaction mechanism of the complexes was also elucidated. The apoptosis was assayed by flow cytometry. The changes of mitochondrial membrane potential and the ROS levels were measured by flow cytometry. The cell invasion, cell cycle arrest and the expression of Bcl-2 family proteins were studied in detail. N-Acetylcysteine (NAC) was used in several experiments to testify the effect of the complexes on apoptosis. The results demonstrate that the complexes induce apoptosis in SGC-7901 cells through a ROS-mediated mitochondrial dysfunction pathway, which was accompanied by the regulation of Bcl-2 family proteins. In addition, the interaction of the complexes with calf thymus DNA (CT-DNA) shows that the complexes interact with DNA through partial intercalation mode.
机译：已对化学合成化合物的抗癌特性进行了功效和选择性评估。一种新的配体PTCP（PTCP = 2-phenanthren-9-yl-1 H -1,3,7,8-四氮杂环戊[[em> l ]菲）钌（ II ）聚吡啶配合物[Ru（N–N） 2 （PTCP）]（ClO 4 ） 2 （N–N：phen = 1,10-菲咯啉1; dmp = 2,9-二甲基-1,10-菲咯啉2 ; ttbpy = 4,4'-di- 叔-丁基-2,2'-联吡啶3）的合成并通过元素分析，ESI-MS，IR， 1进行表征 H NMR和 13 C NMR。在本报告中，我们研究了该复合物对几种癌细胞系SGC-7901，HepG2，HeLa，SiHa和正常细胞NIH3T3的细胞毒性。结果表明，复合物显示出对SGC-7901的高度抗增殖活性，对正常细胞NIH3T3的细胞毒活性较低。还阐明了复合物的抗增殖与分子相互作用机理之间的关系。通过流式细胞术测定细胞凋亡。流式细胞仪检测线粒体膜电位和ROS水平的变化。详细研究了细胞侵袭，细胞周期阻滞和Bcl-2家族蛋白的表达。 N -乙酰半胱氨酸（NAC）被用于一些实验中，以证明复合物对细胞凋亡的影响。结果表明，该复合物通过ROS介导的线粒体功能障碍途径诱导SGC-7901细胞凋亡，并伴有Bcl-2家族蛋白的调控。此外，配合物与小胸腺DNA（CT-DNA）的相互作用表明配合物通过部分插入模式与DNA相互作用。

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