Synthesis, characterization and in vitro antitumor behavior of a vanadium(V) complex with 4′-(3-methoxyphenyl)-2,2′:6′2"-terpyridine

A dioxovanadium(V) complex, [VO2(moptpy)](ClO4) (1, moptpy = 4'-(3-methoxyphenyl)2,2':6' 2 ''-terpyridine), was synthesized and characterized by elemental analysis, ESI-MS, UV-vis, IR, and H-1, C-13, and V-51 NMR. The cytotoxicity in vitro of 1 was evaluated against cancer cell lines HepG-2 (hepatocellular carcinoma), SGC-7901 (gastric carcinoma), SiHa (cervical cancer), BEL-7402 (hepatocellular), and rat PC-12 (pheochromocytoma) by the MTT method. The results demonstrated that 1 exhibits superior anticancer activity in vitro with much lower values of 50% inhibitive concentration (IC50) against the selected cell lines than cisplatin, and 1 shows the highest cytotoxic activity toward SGC-7901 cells (IC50 = 1.3 +/- 0.1 mu M) among the selected cell lines. A series of cellular morphological and staining experiments were carried out, and the results indicated that 1 can effectively induce apoptosis of SGC-7901 cells through a ROS-mediated mitochondrial dysfunction pathway. In addition, cellular incorporation and cell cycle analysis were also performed, and it was concluded from the experimental observations that 1 can efficiently enter into the cell nuclei, and the complex inhibits cell growth in SGC-7901 cell at G0/G1 phase. [GRAPHICS] .