Cyclometalated Ir(III) Complexes as Lysosome-Targeted Photodynamic Anticancer Agents

We have designed and synthesized two Ir(III) complexes (Ir1 and Ir2) coordinated with an 8-sulfonamidoquinoline derivative ligand as photosensitizers, which exhibit strong red phosphorescence emission and a long phosphorescence lifetime. The Ir(III) complexes exhibit a high population of triplet states, which enable red phosphorescence and efficient singlet oxygen generation. Ir1 and Ir2 rapidly enter the cancer cells and accumulate in lysosomes, producing large amounts of intracellular singlet oxygen when exposed to light irradiation, eventually leading to cancer cell death, and the phototoxic indexes of complexes Ir1 and Ir2 against cancer cells are in the range of 76-228. Overall, our studies indicate that the synthesized Ir(III) complexes with quinoline ligands exhibit photosensitizing properties, effectively inducing cancer cell death when exposed to light. These promising results suggest their potential application in photodynamic therapy.

Automated summary

In this study, we designed and synthesized two complexes as photosensitizers, which exhibited strong phosphorescence and high toxicity against cancer cells. These complexes rapidly accumulated in lysosomes after entering cancer cells, and when exposed to light irradiation, they produced a large amount of oxidizing stress substances, eventually leading to cancer cell death. This provides promising potential application in photodynamic therapy.