Issue 1, 2017

Synthesis, crystal structure, cytotoxicity and action mechanism of a Rh(iii) complex with 8-hydroxy-2-methylquinoline as a ligand

Abstract

A rhodium(III) complex, [Rh(MQ)(DMSO)2Cl2] (1), with 8-hydroxy-2-methylquinoline as the ligand was synthesized and characterized. Complex 1 exhibited cytotoxicity against BEL-7404, Hep-G2, NCI-H460, T-24, and A549 cell lines with IC50 values in the micromolar range (6.52–17.86 μM). Various experiments on the Hep-G2 cells showed that complex 1 caused cell cycle arrest at the S phase, downregulation of cdc25 A, cyclin A, cyclin B and CDK2, and upregulation of p21, p27 and p53. Furthermore, cytotoxicity mechanism studies suggested that complex 1-induced apoptosis was achieved via disruption of the mitochondrial function, which led to a significant loss of the mitochondrial membrane potential, an increase in the cellular levels of reactive oxygen species, cytochrome c, and apaf-1, and a fluctuation of the intracellular Ca2+ concentration. Taken altogether, complex 1 can trigger cancer cell death by inducing apoptosis through a mitochondrial dysfunction pathway.

Graphical abstract: Synthesis, crystal structure, cytotoxicity and action mechanism of a Rh(iii) complex with 8-hydroxy-2-methylquinoline as a ligand

Supplementary files

Article information

Article type
Research Article
Submitted
13 Aug 2016
Accepted
15 Oct 2016
First published
25 Oct 2016

Med. Chem. Commun., 2017,8, 184-190

Synthesis, crystal structure, cytotoxicity and action mechanism of a Rh(III) complex with 8-hydroxy-2-methylquinoline as a ligand

Y. Zhang, Q. Qin, Q. Cao, H. Han, Z. Liu, Y. Liu, H. Liang and Z. Chen, Med. Chem. Commun., 2017, 8, 184 DOI: 10.1039/C6MD00462H

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