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

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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Original languageEnglish
Pages (from-to)6865-6870
Journal / PublicationChemical Science
Volume8
Issue number10
Online published31 Jul 2017
Publication statusPublished - 1 Oct 2017

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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.

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Cytotoxic (salen)ruthenium(III) anticancer complexes exhibit different modes of cell death directed by axial ligands. / Li, Cai; Ip, Kwok-Wa; Man, Wai-Lun; Song, Dan; He, Ming-Liang; Yiu, Shek-Man; Lau, Tai-Chu; Zhu, Guangyu.

In: Chemical Science, Vol. 8, No. 10, 01.10.2017, p. 6865-6870.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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