Phosphorescent iridium(III)-bis- N -heterocyclic carbene complexes as mitochondria-targeted theranostic and photodynamic anticancer agents

Abstract Mitochondria-targeted compounds represent a promising approach to target tumors selectively and overcome resistance to current anticancer therapies. In this work, three cyclometalated iridium(III) complexes ( 1 – 3 ) containing bis- N -heterocyclic carbene (NHC) ligands have been explored a...

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Bibliographic Details
Published in:Biomaterials 2015-01, Vol.39, p.95-104
Main Authors: Li, Yi, Tan, Cai-Ping, Zhang, Wei, He, Liang, Ji, Liang-Nian, Mao, Zong-Wan
Format: Article
Language:English
Subjects:
Advanced Basic Science
Antineoplastic Agents - chemistry
Biomedical materials
Carbenes
Cell Cycle - drug effects
Cell Line, Tumor
Dentistry
Effectiveness
HeLa Cells
Human
Humans
Iridium - chemistry
Iridium - pharmacology
Iridium - therapeutic use
Iridium(III) complexes
Ligands
Membrane Potential, Mitochondrial - physiology
Methane - analogs & derivatives
Methane - chemistry
Methane - pharmacology
Methane - therapeutic use
Mitochondria
Mitochondria - metabolism
Mitochondrion
Monitoring
N-Heterocyclic carbene
Organometallic Compounds - chemistry
Phosphorescent emission
Photochemotherapy - methods
Surgical implants
Theranostic
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Summary:Abstract Mitochondria-targeted compounds represent a promising approach to target tumors selectively and overcome resistance to current anticancer therapies. In this work, three cyclometalated iridium(III) complexes ( 1 – 3 ) containing bis- N -heterocyclic carbene (NHC) ligands have been explored as theranostic and photodynamic agents targeting mitochondria. These complexes display rich photophysical properties, which greatly facilitates the study of their intracellular fate. All three complexes are more cytotoxic than cisplatin against the cancer cells screened. 1 – 3 can penetrate into human cervical carcinoma (HeLa) cells quickly and efficiently, and they can carry out theranostic functions by simultaneously inducing and monitoring the morphological changes in mitochondria. Mechanism studies show that these complexes exert their anticancer efficacy by initiating a cascade of events related to mitochondrial dysfunction. Additionally, they display up to 3 orders of magnitude higher cytotoxicity upon irradiation at 365 nm, which is so far the highest photocytotoxic responses reported for iridium complexes.
ISSN:0142-9612
1878-5905
DOI:10.1016/j.biomaterials.2014.10.070