首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >DNA-binding, photocleavage, cytotoxicity in vitro, apoptosis and cell cycle arrest studies of symmetric ruthenium(II) complexes
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DNA-binding, photocleavage, cytotoxicity in vitro, apoptosis and cell cycle arrest studies of symmetric ruthenium(II) complexes

机译:对称钌(II)配合物的DNA结合,光裂解,体外细胞毒性,细胞凋亡和细胞周期阻滞研究

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摘要

Two novel ruthenium(II) complexes [Ru(dmb)2(addppn)](ClO 4)2 (1) and [Ru(bpy)2(addppn)](ClO 4)2 (2) were synthesized. The DNA-binding constants of complexes 1 and 2 were determined to be 4.78 (±0.49) × 10 5 and 7.42 (±0.53) × 105 M-1. The results indicate that complexes 1 and 2 interact with CT DNA through intercalative mode. The cytotoxicity in vitro of the complexes toward BEL-7402, HeLa, MG-63 and SKBR-3 cells was assessed by MTT assay. The apoptosis was carried out with Hoechst 33258 staining method and flow cytometry. The cellular uptake was observed under fluorescence microscope. The cell cycle arrest shows that the antiproliferative mechanism induced by complexes 1 and 2 on BEL-7402 cells is G0/G1 phase arrest.
机译:合成了两种新型钌(II)配合物[Ru(dmb)2(addppn)](ClO 4)2(1)和[Ru(bpy)2(addppn)](ClO 4)2(2)。测定复合物1和2的DNA结合常数为4.78(±0.49)×10 5和7.42(±0.53)×105M-1。结果表明,配合物1和2通过插入模式与CT DNA相互作用。通过MTT分析评估复合物对BEL-7402,HeLa,MG-63和SKBR-3细胞的体外细胞毒性。用Hoechst 33258染色法和流式细胞仪进行细胞凋亡。在荧光显微镜下观察细胞摄取。细胞周期停滞表明,复合物1和2在BEL-7402细胞上诱导的抗增殖机制是G0 / G1期停滞。

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