Evaluation of anticancer effect in vitro and in vivo of iridium(III) complexes on gastric carcinoma SGC-7901 cells.

This work mainly introduces the synthesis and characterization of three iridium(III) complexes [Ir(ppy) 2 (adppz)](PF 6) (Ir-1), [Ir(bzq) 2 (addpz)](PF 6) (Ir-2) and [Ir(piq) 2 (adppz)](PF 6) (Ir-3). The complexes are more cytotoxic than cisplatin against tumor cell lines such as SGC-7901, A549, HeLa, Eca-109, HepG2 and BEL-7402. The toxicity test results indicated that complexes Ir-1 , Ir-2 and Ir-3 can effectively inhibit the cell growth of SGC-7901 cells, and the measured IC 50 values are 1.8 ± 0.4, 1.6 ± 0.3 and 0.8 ± 0.1 μM, respectively. AO/EB staining and flow apoptosis confirmed that SGC-7901 cells were caused apoptosis after being treated with the complexes. Along with the increase of endogenous ROS and Ca2+ levels, mitochondrial membrane potential collapse and massive release of cytochrome c , it is fully demonstrated that these complexes induce apoptosis through ROS-mediated mitochondrial pathway. At the same time, the complex Ir-3 is outstanding in the inhibition of tumor growth in vivo. Combined with the above results, it provides a favorable foundation for the future development of more effective anti-tumor drugs. Three new iridium(III) complexes were synthesized and characterized. The cytotoxicity in vitro and in vivo was investigated. The complexes show high anticancer activity in vitro and in vivo. Image 1 • The iridium(III) complexes were synthesized and characterized. • The cytotoxicity in vitro was studied by MTT method. • The apoptosis, cell cycle arrest and intracellular ROS levels were assayed. • The effect of the complex on the tumor growth was evaluated. [ABSTRACT FROM AUTHOR]