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Issue 10, 2015
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Cyclometalated iridium(III) complexes as lysosome-targeted photodynamic anticancer and real-time tracking agents

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Abstract

Stimuli-activatable photosensitizers (PSs) are highly desirable for photodynamic therapy (PDT) to selectively demolish tumor cells. On the other hand, lysosomes are emerging as attractive anticancer targets. Herein, four cyclometalated iridium(III)–β-carboline complexes with pH-responsive singlet oxygen (1O2) production and lysosome-specific imaging properties have been designed and synthesized. Upon visible light (425 nm) irradiation, they show highly selective phototoxicities against cancer cells. Notably, complex 2 ([Ir(N^C)2(N^N)](PF6) in which N^C = 2-phenylpyridine and N^N = 1-(2-benzimidazolyl)-β-carboline) displays a remarkably high phototoxicity index (PI = IC50 in the dark/IC50 in light) of >833 against human lung carcinoma A549 cells. Further studies show that 2-mediated PDT induces caspase-dependent apoptosis through lysosomal damage. The pH-responsive phosphorescence of complex 2 can be utilized to monitor the lysosomal integrity upon PDT, which provides a reliable and convenient method for in situ monitoring of therapeutic effect and real-time assessment of treatment outcome. Our work provides a strategy for the construction of highly effective multifunctional subcellular targeted photodynamic anticancer agents through rational structural modification of phosphorescent metal complexes.

Graphical abstract: Cyclometalated iridium(iii) complexes as lysosome-targeted photodynamic anticancer and real-time tracking agents

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Publication details

The article was received on 01 jún. 2015, accepted on 22 júl. 2015 and first published on 22 júl. 2015


Article type: Edge Article
DOI: 10.1039/C5SC01955A
Citation: Chem. Sci., 2015,6, 5409-5418
  • Open access: Creative Commons BY license
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    Cyclometalated iridium(III) complexes as lysosome-targeted photodynamic anticancer and real-time tracking agents

    L. He, Y. Li, C. Tan, R. Ye, M. Chen, J. Cao, L. Ji and Z. Mao, Chem. Sci., 2015, 6, 5409
    DOI: 10.1039/C5SC01955A

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