Glycosylated Phosphorous Corrole as effective Photosensitizers for Cancer Photodynamic Therapy via Enhancing cellular Uptake

Developing effective photosensitizers (PSs) is the most important for cancer photodynamic therapy (PDT) treatment. Phosphrous corrole complex is a kind of promising photosensitizer. Herein, we report the synthesis and anticancer activity of a novel glycosylated phosphorous(V) corrole PS 5,15-bis(pentafuorophenyl)-10-(4-glycosyl phenyl) corrole phosphorous complex (2-P) which was prepared from the glycosylation of phosphorous 5,15-bis(pentafuorophenyl)-10-(4-oxhydryl phenyl) corrole (1-P). Experimental results indicate that 2-P exhibits significantly higher uptake in cancer cells than 1-P, leading to an enhanced photo-cytotoxicity toward tumor cells while maintaining low dark or phototoxicity to normal cells such as HEK293T. Upon light exposure, 2-P may remarkably increase the reactive oxygen species (ROS) level of tumor cells, a key factor for enhancing the PDT efficacy. This study demonstrates the potential of 2-P as an effective PS for PDT, highlighting the glycosylation modification is an effective strategy for the design of new phosphorous corrole PDT drugs.