The HSA affinity of warfarin and flurbiprofen determined by fluorescence anisotropy measurements of camptothecin

Bio Systems
Tomasz WybranowskiStefan Kruszewski

Abstract

The determination of affinity of warfarin and flurbiprofen to human serum albumin (HSA) by fluorescence anisotropy measurements of carboxylate form of camptothecin (CPT-C) is the subject of this paper. A simple method based on measurements of fluorescence anisotropy of CPT-C allows to determine the affinity constant of CPT-C to HSA by computation of the fraction of bound CPT-C molecules with HSA It was observed, that adding of competing drug to plasma significant reduces the rate of increase of CPT-C fluorescence anisotropy with increase of albumin concentration and, the affinity constant of CPT-C to HSA decreases. The hypothesis of interactions between competing drug and CPT-C is presented. The results of these studies suggest that CPT-C displaces other drug from protein binding site and the degree of this displacement depends on concentration of drug and drug-HSA binding affinity. The presented in this paper biosystems research allows to estimate the affinity constant of warfarin and flurbiprofen. It was also confirmed that despite that most of drugs bind predominantly to Site I or Site II of HSA (only one of these sites is high-affinity site), at elevated concentrations, part of drug molecules can be bound to low-affinity si...Continue Reading

References

Apr 10, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·C BertucciV Cavrini
Jun 26, 2002·Biological & Pharmaceutical Bulletin·Ulrich Kragh-HansenMasaki Otagiri
Jan 18, 2006·The Journal of Pharmacology and Experimental Therapeutics·Haritha MandulaQuentin R Smith
Sep 28, 2007·Combinatorial Chemistry & High Throughput Screening·Blanka ZiomkowskaStefan Kruszewski
Nov 17, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Gabor PatonayLucjan Strekowski

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Citations

May 27, 2010·The Journal of Chemical Physics·Jacek SiódmiakAdam Gadomski
Mar 19, 2014·Chemical Society Reviews·Ignacio VayáMiguel A Miranda
Sep 6, 2012·Journal of Pharmaceutical and Biomedical Analysis·Juan M Pallicer, Stefanie D Krämer
Jul 9, 2013·Luminescence : the Journal of Biological and Chemical Luminescence·Maryam Mahmoodian MoghaddamJamshidkhan Chamani
Sep 4, 2015·European Journal of Drug Metabolism and Pharmacokinetics·Nooshin AbdollahpourJamshidkhan Chamani
Apr 13, 2015·Journal of Photochemistry and Photobiology. B, Biology·Fei DingYu-Kui Peng
Oct 16, 2013·Journal of Biomolecular Structure & Dynamics·Mahboobeh ZolfagharzadehJamshidkhan Chamani

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