Photodynamic Antitumor Activity of 5,15‐Bis(perfluorophenyl)‐10‐(4‐carboxyphenyl)corrole and its Gallium(III) and Phosphorus(V) Complexes

This work reports the preparation and characterization of an A2B corrole 5,15‐bis(perfluorophenyl)‐10‐(4‐carboxyphenyl)corrole and its gallium(III) and phosphorus(V) complexes. Their in‐vitro photodynamic anticancer activities against A549, MDA‐MB‐231, B16, HepG2, and Hela cell lines were also investigated. Among three compounds, phosphorus(V) complexexhibits the best photostability, highest fluorescence quantum yields (ΦF=0.138), and the highest singlet‐oxygen quantum yields (ΦΔ=0.87). Also, the phosphorus(V) complex exhibits the best photodynamic antitumor activity against MDA‐MB‐231 cells with a low IC50 (0.08 μM) upon light irradiation at 625±2 nm, which is much lower than commercial PDT drug Temoporfin (0.1 μM) at the same conditions. The cellular localization assay confirmed that the phosphorus(V) complexis mainly distributed in the cytoplasm and have a good ability to produce reactive oxygen species (ROS) under light illumination, which would further cause oxidative damage to tumor cells and finally result in the apoptosis. After PDT treatment, phosphorus(V) complex may cause tumor cell arrest at the G2/M stage. The preliminary results showed phosphorus(V) corrole complex is a good candidate for photodynamic therapy (PDT) of tumors. 5,15‐Bis(perfluorophenyl)‐10‐(4‐carboxyphenyl)corrole and its gallium (III) and phosphorus(V) complexes were prepared and their in‐vitro photodynamic anticancer activities against A549, MDA‐MB‐231, B16, HepG2, and Hela cell lines were investigated. The phosphorus(V) complex exhibits the highest singlet‐oxygen quantum yields (ΦΔ=0.87) and the best phototoxicity against the MDA‐MB‐231 cell line (IC50=0.08 μM) under (625±2 nm) light illumination.