The studies on bioactivity in vitro of ruthenium(II) polypyridyl complexes towards human lung carcinoma A549 cells

Three Ru(II) polypyridyl complexes [Ru(dmb)(2)(HDPIP)](ClO4)(2) (1), [Ru(bpy)(2)(HDPIP)](ClO4)(2) (2) and [Ru(phen)(2)(HDPIP)](ClO4)(2) (3) were synthesized and characterized. The IC50 values of the complexes against BEL-7402, A549, MG-63 and SK-BR-3 cells range from 20.8 +/- 1.6 to 7.3 +/- 1.0 mu M. Complexes 1, 2 and 3 can enhance the ROS levels and enter into the cytoplasm and accumulate in the cell nuclei. All the complexes can induce a decrease of the mitochondrial membrane potential and inhibit the cell growth in A549 cells in the G0/G1 phase. Complex 3 has no obvious impact on the expression of the anti-apoptotic protein Bcl-2, and increases the levels of the pro-apoptotic proteins Bax and Bid. Complex 3 induces apoptosis of A549 cells through a ROS-mediated mitochondrial dysfunction pathway.