Photodynamic antitumor activity of dihydroxyl A2B triaryl corrole and its gallium(III) and phosphorus(V) complexes

Two new dihydroxyl A2B triaryl corroles 10-(2,4-dihydroxyphenyl)-5,15-bis(pentafluorophenyl)corrole (1) and 10-(3,4-dihydroxyphenyl)-5,15-bis(pentafluorophenyl)corrole (2) and their gallium(III) and phosphorus(V) complexes (1-Ga, 2-Ga, 1-P and 2-P) were synthesized and investigated as photodynamic antitumor agents. All synthesized corrole derivatives could generate singlet oxygen smoothly under illumination at 620-625 nm and showed remarkable in vitro photodynamic antitumor activity. Excited, phosphorus(V) corrole 1-P even exhibited better phototoxicity towards A549 and MDA-MB-231 tumor cell line (IC50, 0.08 and 0.12 mu M) than clinical drug Foscan (R) (IC50, 0.27 mu M). The laser confocal microscopy results showed that the cellular absorbed 1-P was located in the cytoplasm. Under illumination, intracellular reactive oxygen species (ROS) could be detected, which would triger the destruction of the mitochondrial membrane potential and finally lead to apoptosis. Furthermore, the 1-P photodynamic treatment would cause the cancer cells arrested at sub-G1 stage.