Cytotoxic (salen)ruthenium(iii) anticancer complexes exhibit different modes of cell death directed by axial ligands

Cai Li, Kwok-Wa Ip, Wai-Lun Man, Ming-Liang He, Shek-Man Yiu, Tai-Chu Lau, Guangyu Zhu, Dan Song

Research output: Contribution to journalArticlepeer-review

Abstract

Two novel series of (salen)ruthenium(III) complexes bearing guanidine and amidine axial ligands were synthesized, characterized, and evaluated for anticancer activity. In vitro cytotoxicity tests demonstrate that these complexes are cytotoxic against various cancer cell lines and the leading complexes have remarkable cancer-cell selectivity. A detailed study of the guanidine complex 7 and the amidine complex 13 reveals two distinguished modes of action. Complex 7 weakly binds to DNA and induces DNA damage, cell cycle arrest, and typical apoptosis pathways in MCF-7 cells. In contrast, complex 13 induces paraptosis-like cell death hallmarked by massive vacuole formation, mitochondrial swelling, and ER stress, resulting in significant cytotoxicity against human breast cancer cells. Our results provide an extraordinary example of tuning the mechanism of action of (salen)ruthenium(III) anticancer complexes by modifying the structure of the axial ligands.
Original languageEnglish
Pages (from-to)6865-6870
JournalChemical Science
Volume8
Issue number10
DOIs
Publication statusPublished - 31 Jul 2017

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