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A new iridium(III) complex, [Ir(ppy)2(FBPIP)]PF6 (Ir-1), was synthesized and characterized. The cytotoxic activity of this complex against SGC-7901, PC-12, SiHa, HepG2, BEL-7402, A549, HeLa and normal LO2 cells was investigated using the MTT method. The complex showed no cytotoxic activity against the selected cell lines. However, upon irradiation, the complex displayed potent anti-proliferative activity toward SGC-7901 cells, with a low IC50 value of 6.1 ± 0.6 μM, and showed selectivity between cancer and normal cells. Apoptosis was assayed using the AO/EB staining method. The level of reactive oxygen species (ROS), mitochondrial membrane potential, autophagy and cell invasion were studied under a fluorescence microscope. The cell cycle distribution was studied by flow cytometry. The expression of caspase and Bcl-2 family proteins was investigated by western blot. Complex Ir-1 was shown to accumulate preferentially in the mitochondria of SGC-7901 cells and induced apoptosis via the mitochondrial pathway, which involved ROS generation, mitochondrial membrane potential depolarization, and Bcl-2 and caspase family member activation. These results demonstrate that the complex induces cancer cell apoptosis by acting on mitochondrial pathways.

Photoinduced ROS regulation of apoptosis and mechanism studies of iridium(iii) complex against SGC-7901 cells