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

• The cytotoxicity of complex 1 against BEL-7402, MG-63, A549, SK-BR-3 cells was studied.
• The apoptosis, scratch assay and cellular uptake in BEL-7402 cells were investigated.
• The levels of ROS and the changes of mitochondrial membrane potential were assayed.
• The comet assay and cell cycle arrest was investigated by flow cytometry.
• The expression of caspases and Bcl-1 family proteins were studied.

A Ru(II) polypyridyl complex [Ru(bpy)2(HMSPIP)](ClO4)2 (1) (bpy = 2,2′-bipyridine, HMSPIP = 2-(4-methylsulfonyl)phenyl-1H-imidazo[4,5-f][1,10] phenanthroline) was synthesized. The IC50 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.

The cytotoxicity in vitro, apoptosis, comet assay, scratch assay, ROS, mitochondrial membrane potential, cell cycle arrest and the expression of proteins induced by the Ru(II) complex were investigated.Figure optionsDownload as PowerPoint slide