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Fluorinated cyclometalated iridium(III) complexes as mitochondria-targeted theranostic anticancer agents

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Abstract

Six cyclometalated iridium(III) complexes bearing different numbers of fluorine atoms were synthesized. These complexes demonstrated much better anti-proliferation activities towards five tumour cell lines than the widely used clinical chemotherapeutic agent cisplatin. Moreover, the anti-proliferation activities were correlated to the number of substituted fluorine atoms. Colocalization and inductively coupled plasma-mass spectrometry (ICP-MS) indicated that this series of complexes could penetrate cell membranes rapidly and preferentially target mitochondria. Manifesting high selectivity between tumour cells and normal cells and remarkable sensitivity to a cisplatin-resistant cell line (A549R), complex Ir6 was successfully developed as a novel anticancer agent (with IC50 values of 0.5 ± 0.1 μM for HeLa, 1.1 ± 0.2 μM for HepG2, 1.5 ± 0.3 μM for BEL-7402, 0.8 ± 0.1 μM for A549, and 0.7 ± 0.2 μM for A549R cell lines). Further mechanism studies including mitochondrial membrane potential depolarization and caspase 3/7 activation revealed that Ir6 induced apoptosis via mitochondrial pathways. These results demonstrated that complex Ir6 might be a promising candidate as a mitochondria-targeted theranostic anticancer agent.

Graphical abstract: Fluorinated cyclometalated iridium(iii) complexes as mitochondria-targeted theranostic anticancer agents

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Publication details

The article was received on 23 Mar 2017, accepted on 01 May 2017 and first published on 01 May 2017


Article type: Paper
DOI: 10.1039/C7DT01043E
Citation: Dalton Trans., 2017, Advance Article
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    Fluorinated cyclometalated iridium(III) complexes as mitochondria-targeted theranostic anticancer agents

    M. Ouyang, L. Zeng, H. Huang, C. Jin, J. Liu, Y. Chen, L. Ji and H. Chao, Dalton Trans., 2017, Advance Article , DOI: 10.1039/C7DT01043E

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