A ruthenium(II) complex binds protein and inhibits proliferation and induces apoptosis in human gastric cancer SGC-7901 cells

A new Ru(II) complex, [Ru(ttbpy)2(NMIP)](ClO4)2 (ttbpy = 4,4′-di-tert butyl-2,2′-bipyridine, NMIP = 2′-(2″-nitro-3″,4″-methylenedioxyphenyl)imidazo[4′,5′-f][1,10]-phenanthroline), has been synthesized and characterized by elemental analysis, ESI-MS and 1H NMR spectroscopy. The complex induces a decrease in fluorescent intensity upon binding to protein bovine serum albumin (BSA). The cytotoxic activity of the ligand and the complex against A549, BEL-7402, HeLa, PC-12, SGC-7901, SiHa and LO2 (normal) cell lines was investigated by the MTT method. The complex show high cytotoxicity toward BEL-7402 (IC50 = 5.0 ± 1.2 μM), HeLa (IC50 = 5.7 ± 1.8 μM) and SGC-7901 (IC50 = 4.9 ± 0.2 μM) cell lines. The cellular uptake indicates that the complex can enter into the cytoplasm and accumulate in the cell nuclei. In addition, the complex can increase the reactive oxygen species levels and induce a decrease in the mitochondrial membrane potential in SGC-7901 cells. The cell cycle arrest shows that the complex inhibited the cell growth in SGC-7901 cells at the G2/M phase.

A new Ru(II) complex, [Ru(ttbpy)2(NMIP)](ClO4)2, was synthesized and characterized. Its effects on protein-binding, cytotoxicity, apoptosis, cellular uptake, cell cycle arrest, ROS and mitochondrial membrane potentials were investigated.Figure optionsDownload as PowerPoint slide