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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Fluorinated cyclometalated iridium(III) complexes as mitochondria-targeted theranostic anticancer agents
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Fluorinated cyclometalated iridium(III) complexes as mitochondria-targeted theranostic anticancer agents

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摘要

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 mu M for HeLa, 1.1 +/- 0.2 mu M for HepG2, 1.5 +/- 0.3 mu M for BEL-7402, 0.8 +/- 0.1 mu M for A549, and 0.7 +/- 0.2 mu M 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.

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