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Benzo[a]phenoselenazine-based NIR photosensitizer for tumor-targeting photodynamic therapy via lysosomal-disruption pathway

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Indexed by:期刊论文

Date of Publication:2019-11-01

Journal:DYES AND PIGMENTS

Included Journals:SCIE、EI

Volume:170

ISSN No.:0143-7208

Key Words:Benzo[a]phenoselenazinium; Photosensitizer; Tumor-targeting; Lysosomes; Photodynamic therapy

Abstract:The ultimate goal of cancer therapy is to develop antitumor agents that will destroy selectively tumor cells while sparing the health cell of the patient. Herein, we reported a novel tumor-specific and lysosome dual-targeted NIR photosensitizer, Se-Biotin, by conjugating a biotin ligand into benzo[a]phenoselenazinium derivative dye for selective destruction of tumor cells. Attractively, co-culture model showed that Se-Biotin could selectively target to and retain in biotin receptor-overexpressed tumor cells, which as a result significantly minimized the side effects toward normal cells. As confinned by the in vitro anticancer mechanism, after cellular internalization, upon irradiation, the effective O-1(2) generation (Phi(Delta) = 0.69)severely disrupted the lysosomalintegrity and subsequently led to apoptotic cell death. Benefiting from these merits, Se-Biotin successfully achieved a superior anticancer performance with the IC50 as low as 85 nM, only under a low light dose irradiation (12 J/cm(2), 660 nm). Therefore, these result demonstrated that Se-Biotin will be a promising PDT agent for targeted cancer photodynamic therapy.

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