AI Article Synopsis
- Cyclometalated iridium(III) complexes, specifically Ir1-Ir3, show promise as new anticancer drugs, outperforming cisplatin in anticancer activity with IC values between 0.23 to 5.6 μM.
- These complexes are primarily located in mitochondria and cause mitochondrial dysfunction, which is crucial for their anticancer effects.
- The mechanism involves depolarizing the mitochondrial membrane, increasing reactive oxygen species (ROS), and triggering apoptosis via activated caspases.
Article 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 IC 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.
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| http://dx.doi.org/10.1007/s00775-020-01783-2 | DOI Listing |
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