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Protein binding and anticancer activity studies of ruthenium(II) polypyridyl complexes toward BEL-7402 cells

Paper ID Volume ID Publish Year Pages File Format Full-Text
29878 44445 2016 10 PDF Available
Title
Protein binding and anticancer activity studies of ruthenium(II) polypyridyl complexes toward BEL-7402 cells
Abstract

•Four new ruthenium(II) complexes were synthesized and characterized.•Cytotoxicity of complexes toward HepG-2, HeLa, MG-63, A549, BEL-7402 was studied.•The apoptosis, comet assay, cellular uptake, ROS, cell cycle arrest were studied.•The expression of Bcl-2 family proteins was assayed by western blot analysis.•The protein-binding of the complexes with BSA was investigated.

Four new ruthenium(II) polypyridyl complexes [Ru(dmb)2(dqtbt)](ClO4)2 (1) (dqtbt = 12-(2,3-diphenyl-quinoxalin-6-yl)-4,5,10,13-tetraazabenzo[b]triphenylene, dmb = 4,4′-dimethyl-2,2′-bipyridine), [Ru(bpy)2(dqtbt)](ClO4)2 (2) (bpy = 2,2′-bipyridine), [Ru(phen)2(dqtbt)](ClO4)2 (3) (phen = 1,10-phenanthroline) and [Ru(dmp)2(dqtbt)](ClO4)2 (4) (dmp = 2,9-dimethyl-1,10-phenanthroline) were synthesized and characterized. The cytotoxicity in vitro of the complexes was evaluated against human BEL-7402, A549, HeLa, HepG-2 and MG-63 cancer cell lines. These complexes are sensitive to BEL-7402 cells, the IC50 values are 4.9 ± 0.5, 4.6 ± 0.4, 7.7 ± 1.8 and 1.9 ± 0.3 μM toward BEL-7402 cells. The complexes can increase the levels of reactive oxygen species and induce the decrease of mitochondrial membrane potential. Morphological and comet assay studies show that the complexes can effectively induce apoptosis in BEL-7402 cells. Complexes 1–4 inhibit the cell growth at G0/G1 phase in BEL-7402 cell line. The complexes can downregulate the expression of Bcl-2 and Bcl-x proteins and upregulate the levels of Bid protein in BEL-7402 cells. The results show that the complexes induce BEL-7402 cell apoptosis through a ROS-mediated mitochondrial dysfunction pathway. In addition, the complexes show strong protein-binding affinities.

Graphical abstractFour new Ru(II) complexes were synthesized and characterized. The cytotoxicity in vitro, apoptosis, comet assay, ROS, mitochondrial membrane potential, cell cycle arrest, expression of proteins and protein-binding were investigated.Figure optionsDownload full-size imageDownload as PowerPoint slide

Keywords
Ru (II) polypyridyl complexes; Cytotoxicity in vitro; Reactive oxygen species; Mitochondrial membrane potential; Western blot analysis
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Protein binding and anticancer activity studies of ruthenium(II) polypyridyl complexes toward BEL-7402 cells
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 158, May 2016, Pages 39–48
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us