Anticancer activity studies of a ruthenium(II) polypyridyl complex against human hepatocellular (BEL-7402) cells

Abstract A Ru(II) polypyridyl complex [Ru(bpy) 2 (HMSPIP)](ClO 4 ) 2 ( 1 ) (bpy = 2,2′-bipyridine, HMSPIP = 2-(4-methylsulfonyl)phenyl-1H-imidazo[4,5- f ][1,10] phenanthroline) was synthesized. The IC 50 value of the complex against human hepatocellular cell BEL-7402 is 21.6 ± 2.7 μM. The complex shows no cytotoxic activity toward human lung adenocarcinoma cell A549, human osteosarcoma cell MG-63 and human breast cancer cell SK-BR-3 cells. It is easily for complex 1 to be taken up by BEL-7402 cells. The complex can enhance the reactive oxygen species (ROS) levels and induce the decrease in the mitochondrial membrane potential. The complex inhibits the cell growth in BEL-7402 cells at G2/M phase. Complex 1 can regulate the expression of Bcl-2 family proteins. The results show that the complex induces apoptosis of BEL-7402 cells through a ROS-mediated mitochondrial dysfunction pathway.