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- Title
Mitochondria-targeted phosphorescent cyclometalated iridium(III) complexes: synthesis, characterization, and anticancer properties.
- Authors
Li, Yi; Liu, Ben; Xu, Cui-Xia; He, Liang; Wan, Yi-Chao; Ji, Liang-Nian; Mao, Zong-Wan
- Abstract
Cyclometalated iridium(III) complexes represent a promising approach to developing new anticancer metallodrugs. In this work, three phosphorescent cyclometalated iridium(III) complexes Ir1–Ir3 have been explored as mitochondria-targeted anticancer agents. All three complexes display higher antiproliferative activity than cisplatin against the cancer cells screened, and with the IC50 values ranging from 0.23 to 5.6 μM. Colocalization studies showed that these complexes are mainly localized in the mitochondria. Mechanism studies show that these complexes exert their anticancer efficacy through initiating a series of events related to mitochondrial dysfunction, including depolarization of mitochondrial membrane potential (MMP), elevation of intracellular reactive oxygen species (ROS) levels, and induction of apoptosis. Mitochondria-targted cyclometalated iridium complexes induce apoptosis through depolarized mitochondria, elevation of intracellular ROS and activated caspase.
- Subjects
IRIDIUM; MEMBRANE potential; MITOCHONDRIAL membranes; REACTIVE oxygen species; CANCER cells; TUBULINS
- Publication
Journal of Biological Inorganic Chemistry (JBIC), 2020, Vol 25, Issue 4, p597
- ISSN
0949-8257
- Publication type
Article
- DOI
10.1007/s00775-020-01783-2