Issue 31, 2015

Cytotoxicity in vitro, cell migration and apoptotic mechanism studies induced by ruthenium(ii) complexes

Abstract

Four new ruthenium(II) polypyridyl complexes [Ru(dmb)2(DHBT)](ClO4)2 (1) (DHBT = 12,14-dihydroxyl-4,5,9,10,11,13-hexaazabenzo[b]triphenylene, dmb = 4,4′-dimethyl-2,2′-bipyridine), [Ru(bpy)2(DHBT)](ClO4)2 (2) (bpy = 2,2′-bipyridine), [Ru(phen)2(DHBT)](ClO4)2 (3) (phen = 1,10-phenanthroline) and [Ru(dmp)2(DHBT)](ClO4)2 (4) (dmp = 2,9-dimethyl-1,10-phenanthroline) were synthesized and characterized. The cytotoxicity in vitro of these complexes was evaluated against human HepG-2, HeLa, A549, MG-63 and BEL-7402 cancer cell lines. The IC50 values of the complexes toward selected cell lines range from 14.9 ± 1.1 to 30.1 ± 2.7 μM. The cytotoxicity and the levels of reactive oxygen species were found to increase with increasing concentrations of the complexes. The complexes are sensitive to MG-63 cells and can inhibit the MG-63 cell migration. Morphological and comet assay studies show that the complexes can effectively induce apoptosis in MG-63 cells. Complex 2 inhibits the cell growth at the G0/G1 phase, whereas the other complexes exhibit the antiproliferative mechanism at the S phase in the MG-63 cell line. The complexes can downregulate the expression of Bcl-2 protein and upregulate the levels of Bad protein in MG-63 cells. The complexes induce MG-63 cells apoptosis through a ROS-mediated mitochondrial dysfunction pathway.

Graphical abstract: Cytotoxicity in vitro, cell migration and apoptotic mechanism studies induced by ruthenium(ii) complexes

Article information

Article type
Paper
Submitted
11 Jan 2015
Accepted
26 Feb 2015
First published
02 Mar 2015

RSC Adv., 2015,5, 24534-24543

Cytotoxicity in vitro, cell migration and apoptotic mechanism studies induced by ruthenium(II) complexes

W. Li, B. Han, J. Yao, G. Jiang and Y. Liu, RSC Adv., 2015, 5, 24534 DOI: 10.1039/C5RA00553A

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