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)Cl] (), with 8-hydroxy-2-methylquinoline as the ligand was synthesized and characterized. Complex exhibited cytotoxicity against BEL-7404, Hep-G2, NCI-H460, T-24, and A549 cell lines with IC values in the micromolar range (6.52-17.86 μM). Various experiments on the Hep-G2 cells showed that complex 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-induced apoptosis was achieved 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 Ca concentration. Taken altogether, complex can trigger cancer cell death by inducing apoptosis through a mitochondrial dysfunction pathway.

Syntheses, Crystal Structures, and Antitumor Activities of Copper(II) and Nickel(II) Complexes with 2-((2-(Pyridin-2-yl)hydrazono)methyl)quinolin-8-ol

“…The mitochondrial membrane potential Δψ can alter the intracellular Ca 2+ level, which has been recognized as a factor in cell death, apoptosis, and injury mediated by various pathways [ 61 , 62 ]. We examined the effects of complex 1 on the mobilization of intracellular Ca 2+ in MGC80-3 cells.…”

Cell nucleus localization and high anticancer activity of quinoline–benzopyran rhodium(iii) metal complexes as therapeutic and fluorescence imaging agents

“…16,27–31 Additionally, a number of researchers have investigated Rh( iii ) complexes based on (iso)quinoline, quinolinone, and 8-hydroxyquinoline ligands. 12,32–44 Some of them have also been tested for their ability to interact with BSA, protein kinases, lysine-specific demethylase 1, DNA, ATP-competitive neural precursor, mitochondria, and other enzymes. 12,32–44 Recently, (iso)quinolone derivative metal complexes have been examined as specific probes and photodynamic therapy reagents, such as 8-hydroxyquinoline Ru( ii )-arene complexes, 45 8-oxychinolin cyclometalated Ir( iii ) complexes, 46 zinc( ii ) phthalocyanine-quinoline derivatives, 47 phenylisoquinoline Ir( iii ) phosphorescent probe, 48,49 near-infrared-emitting Ir( iii ) complexes, 50 luminescent di-2-picolylamine Ir( iii ) complexes, 51 and quinoline–coumarin organoplatinum( ii ) derivatives.…”

“…12,32–44 Some of them have also been tested for their ability to interact with BSA, protein kinases, lysine-specific demethylase 1, DNA, ATP-competitive neural precursor, mitochondria, and other enzymes. 12,32–44 Recently, (iso)quinolone derivative metal complexes have been examined as specific probes and photodynamic therapy reagents, such as 8-hydroxyquinoline Ru( ii )-arene complexes, 45 8-oxychinolin cyclometalated Ir( iii ) complexes, 46 zinc( ii ) phthalocyanine-quinoline derivatives, 47 phenylisoquinoline Ir( iii ) phosphorescent probe, 48,49 near-infrared-emitting Ir( iii ) complexes, 50 luminescent di-2-picolylamine Ir( iii ) complexes, 51 and quinoline–coumarin organoplatinum( ii ) derivatives. 52 a Although a few metal-(iso)quinolone compounds have recently been used in mitochondrial and other imaging experiments, rhodium( iii ) metal complexes bearing quinoline–benzopyran ligands (QB1–QB4) have not yet been studied for such imaging and anticancer therapeutics in cell nucleus fractions, to the best of our knowledge.…”