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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 ?M). 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.

SUBMITTER: Zhang YL 

PROVIDER: S-EPMC6072358 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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

Zhang Yun-Liang YL   Qin Qi-Pin QP   Cao Qian-Qian QQ   Han Hong-Hua HH   Liu Zhu-Ling ZL   Liu Yan-Cheng YC   Liang Hong H   Chen Zhen-Feng ZF  

MedChemComm 20161025 1


A rhodium(iii) complex, [Rh(MQ)(DMSO)<sub>2</sub>Cl<sub>2</sub>] (<b>1</b>), with 8-hydroxy-2-methylquinoline as the ligand was synthesized and characterized. Complex <b>1</b> exhibited cytotoxicity against BEL-7404, Hep-G2, NCI-H460, T-24, and A549 cell lines with IC<sub>50</sub> values in the micromolar range (6.52-17.86 μM). Various experiments on the Hep-G2 cells showed that complex <b>1</b> caused cell cycle arrest at the S phase, downregulation of cdc25 A, cyclin A, cyclin B and CDK2, and  ...[more]

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