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Cyclometalated iridium(III) dithioformic acid complexes as mitochondria-targeted imaging and anticancer agents.

Abstract
Four neutral cyclometalated iridium(III) (IrIII) dithioformic acid complexes ([(ppy)2Ir(S^S)], Ir1-Ir4) were designed and synthesized. Toxicity assay revealed that these complexes showed favorable anticancer activity, especially for human non-small cell lung cancer cells (A549). Ir1 exhibited the best anticancer activity (11.0 ± 0.4 μM) was about twice that of cisplatin, meanwhile, which could availably restrain A549 cells migration. Complexes could target mitochondria, induce a decrease in mitochondrial membrane potential (MMP), result in an increase of intracellular reactive oxygen species (ROS) and disruption of the cell cycle, and ultimately generate apoptosis. Western blotting experiment indicated that complexes could inhibit the expression of B cell CLL/lymphoma-2 protein (Bcl-2), induce the expression of BCL2-associated X protein (Bax) and lead to a massive release of Cytochrome C (Cyt-c), which amplified apoptosis signals by activating downstream pathway to promote apoptosis. All these confirmed the existence of mitochondrial anticancer channels for these complexes. Above all, cyclometalated iridium(III) dithioformic acid complexes possess the prospect of becoming a multifunctional cancer therapeutic platform, including mitochondria-targeted imaging, anti-migration, and anticancer agents.
AuthorsYuting Wu, Jinfeng Liu, Mingxiao Shao, Pei Zhang, Shaohua Song, Ge Yang, Xicheng Liu, Zhe Liu
JournalJournal of inorganic biochemistry (J Inorg Biochem) Vol. 233 Pg. 111855 (08 2022) ISSN: 1873-3344 [Electronic] United States
PMID35576884 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2021. Published by Elsevier Inc.
Chemical References
  • Antineoplastic Agents
  • Coordination Complexes
  • Reactive Oxygen Species
  • Iridium
Topics
  • Antineoplastic Agents (metabolism, pharmacology)
  • Apoptosis
  • Carcinoma, Non-Small-Cell Lung (metabolism)
  • Cell Line, Tumor
  • Cell Proliferation
  • Coordination Complexes (metabolism, pharmacology)
  • Humans
  • Iridium (metabolism, pharmacology)
  • Lung Neoplasms (metabolism)
  • Mitochondria (metabolism)
  • Reactive Oxygen Species (metabolism)

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