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Cellular uptake, cytotoxicity, apoptosis, DNA-binding, photocleavage and molecular docking studies of ruthenium(II) polypyridyl complexes

Paper ID Volume ID Publish Year Pages File Format Full-Text
29426 44395 2014 13 PDF Available
Title
Cellular uptake, cytotoxicity, apoptosis, DNA-binding, photocleavage and molecular docking studies of ruthenium(II) polypyridyl complexes
Abstract

•DNA binding studies, Ru(II) complexes intercalate between CT-DNA base pairs.•Cellular uptake studies showed effective shrinkage of HeLa cell lines.•Apoptosis results reveal good percentage in late apoptosis region.

Three new mononuclear [Ru (phen)2 ptip]2+ (1), [Ru (bpy)2 ptip]2+ (2) and [Ru (dmb)2 ptip]2+ (3) [ptip = (2-(5-phenylthiophen-2-yl)-1H-imidazo[4, 5-f][1,10 phenanthroline, phen = 1, 10 phenanthroline, bpy = 2, 2′ bipyridine, dmb = 4, 4′-dimethyl 2, 2′ bipyridine] complexes were synthesized and characterised by elemental analysis, IR, NMR and Mass spectra. The DNA-binding behaviours were investigated by electronic absorption titration, luminescence spectra, viscosity measurements and photo-activated cleavage. The DNA-binding constants Kb of complexes 1, 2 and 3 were determined to be 7.0 (±0.06) × 105, 3.87 (±0.04) × 105, 2.79 (±0.07) × 105 respectively. The results showed that these complexes interact with CT-DNA by intercalative mode. Cell viability experiments indicated that the Ru(II) complex showed significant dose-dependent cytotoxicity to HeLa tumour cell lines. Further flow cytometry experiments showed that the cytotoxic Ru(II) complex induced apoptosis of HeLa tumour cell lines. Our data demonstrated that the Ru(II) polypyridyl complex binds to DNA and thereby induces apoptosis in tumor cells, suggesting that anti-tumor activity of the Ru(II) complex could be related to its interaction with DNA. The molecular dynamic simulations and docking methods were used to predict the DNA binding affinity of ruthenium complexes and with good visualisation images supporting with experimental results.

Graphical abstractThe cell viability decreased with increasing concentrations of three complexes. The IC50 values are 21.7%, 22.4% and 23.1% for 1, 2 and 3 complexes towards HeLa cell lines respectively. Our data demonstrated that the Ru(II) polypyridyl complex binds to DNA and thereby induces apoptosis in tumor cells, suggesting that anti-tumor activity of the Ru(II) complex could be related to its interaction with DNA.Figure optionsDownload full-size imageDownload as PowerPoint slide

Keywords
Binding affinity; Anti-tumour activity; Cell viability; Cytocoxicity; Apoptosis and flow cytometry
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Cellular uptake, cytotoxicity, apoptosis, DNA-binding, photocleavage and molecular docking studies of ruthenium(II) polypyridyl complexes
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 132, 5 March 2014, Pages 111–123
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
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Price after discount Only $4.95
100% Money Back Guarantee
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