DNA-binding, photocleavage, cytotoxicity in vitro, apoptosis and cell cycle arrest studies of symmetric ruthenium(II) complexes

• Two new ruthenium (II) complexes [Ru(dmb)2(addppn)](ClO4)2 and [Ru(bpy)2(addppn)](ClO4)2 were synthesized.
• The DNA-binding behaviors were studies by absorption titration, viscosity measurements and photocleavage.
• The cytotoxicity of these complexes was evaluated by MTT method.
• The apoptosis was investigated by Hoechst 33258 staining method and flow cytometry.
• The cellular uptake and cell cycle arrest were investigated with fluorescence microscope and flow cytometry.

Two novel ruthenium(II) complexes [Ru(dmb)2(addppn)](ClO4)2 (1) and [Ru(bpy)2(addppn)](ClO4)2 (2) were synthesized. The DNA-binding constants of complexes 1 and 2 were determined to be 4.78 (±0.49) × 105 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.

Complexes [Ru(dmb)2(addppn)](ClO4)2 (1) and [Ru(bpy)2(addppn)](ClO4)2 (2) were synthesized. The DNA-binding behaviors were investigated. The cytotoxicity was assessed by MTT method. The apoptosis, cellular uptake and cell cycle arrest was also studied.Figure optionsDownload as PowerPoint slide