School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR China.
Eur J Med Chem. 2013 May;63:603-10. doi: 10.1016/j.ejmech.2013.03.015. Epub 2013 Mar 15.
Two novel ruthenium(II) complexes Ru(dmb)2(addppn)2 (1) and Ru(bpy)2(addppn)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) × 10(5) 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.
合成了两个新型钌（II）配合物Ru(dmb)2(addppn)2（1）和Ru(bpy)2(addppn)2（2）。测定了配合物 1 和 2 与 DNA 的结合常数，分别为 4.78(±0.49)×10(5)和 7.42(±0.53)×10(5)M(-1)。结果表明，配合物 1 和 2 通过嵌入模式与 CT-DNA 相互作用。采用 MTT 法评估了配合物对 BEL-7402、HeLa、MG-63 和 SKBR-3 细胞的体外细胞毒性。通过 Hoechst 33258 染色法和流式细胞术进行细胞凋亡。通过荧光显微镜观察细胞摄取。细胞周期阻滞表明，配合物 1 和 2 对 BEL-7402 细胞的增殖抑制机制是 G0/G1 期阻滞。
