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 ( 1 O 2) 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)](PF 6) in which N^C = 2-phenylpyridine and N^N = 1-(2-benzimidazolyl)-β-carboline) displays a remarkably high phototoxicity index (PI = IC 50 in the dark/IC 50 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.

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He, L., Li, Y., Tan, C. P., Ye, R. R., Chen, M. H., Cao, J. J., … Mao, Z. W. (2015). Cyclometalated iridium(III) complexes as lysosome-targeted photodynamic anticancer and real-time tracking agents. Chemical Science, 6(10), 5409–5418. https://doi.org/10.1039/c5sc01955a

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