Highly efficient singlet oxygen generation, two-photon photodynamic therapy and melanoma ablation by rationally designed mitochondria-specific near-infrared AIEgens

摘要: Photosensitizers (PSs) with multiple characteristics, including efficient singlet oxygen (1O2) generation, cancer cell-selective accumulation and subsequent mitochondrial localization as well near-infrared (NIR) excitation bright NIR emission, are promising candidates for imaging-guided photodynamic therapy (PDT) but rarely concerned. Herein, a simple rational strategy, namely modulation of donor–acceptor (D–A) strength, molecular engineering mitochondria-targeting aggregation-induced emission (AIE) PSs desirable characteristics highly improved 1O2 generation efficiency, (736 nm), high specificity to mitochondria, good biocompatibility, brightness superior photostability is demonstrated. Impressively, upon light irradiation, the optimal AIE PS (DCQu) can generate efficiency much higher than those commercially available PSs. The excellent two-photon absorption properties DCQu allow fluorescence imaging mitochondria excited PDT. selectively differentiate cells from normal without aid extra targeting ligands. Upon ultralow-power irradiation at 4.2 mW cm−2, in situ activation specifically damage vivo melanoma ablation demonstrated, suggesting potency PDT minimal side effects, which future precision medicine.