Complexation of fluoroquinolone antibiotics with human serum albumin: A fluorescence quenching study

作者: Neelam Seedher , Pooja Agarwal

DOI: 10.1016/J.JLUMIN.2010.04.020

关键词: StereochemistryQuenching (fluorescence)Ciprofloxacin HydrochlorideSparfloxacinNuclear chemistryFluorescence spectrometryChemistryHydrophobic effectEnrofloxacinHuman serum albuminAntibacterial agent

摘要: Mechanism of interaction and detailed physico-chemical characterization the binding four fluoroquinolones: levofloxacin, sparfloxacin, ciprofloxacin HCl enrofloxacin with human serum albumin has been studied at physiological pH (7.4) using fluorescence spectroscopic technique. The stoichiometry was found to be 1:1 for all drugs used. association constants were order 104 in most cases. At low drug:protein ratios, a significant fraction added drug bound. predominant interactions involved are hydrogen bonding Van der Waal’s case hydrophobic hydrochloride bonding, electrostatic sparfloxacin. The region did not coincide that probe, 1-anilinonaphthalene-8-sulfonate (ANS). From displacement site-specific probes site-marker drugs, it concluded is site II-specific while I-specific drug. Levofloxacin binds both I II equal affinity. Sparfloxacin had higher affinity than I. It also possible sparfloxacin interface between II. Stern–Volmer analysis data showed quenching mechanism predominantly collisional static mechanisms operative levofloxacin sparfloxacin. High magnitude rate constant process entirely diffusion controlled. Circular dichroism (CD) studies presence cause any major changes secondary structure HSA.

参考文章(37)
K. E. Van Holde, W. Curtis Johnson, Pui Shing Ho, Principles of physical biochemistry ,(1998)
Gregorio Weber, Lorna B. Young, FRAGMENTATION OF BOVINE SERUM ALBUMIN BY PEPSIN. I. THE ORIGIN OF THE ACID EXPANSION OF THE ALBUMIN MOLECULE. Journal of Biological Chemistry. ,vol. 239, pp. 1415- 1423 ,(1964) , 10.1016/S0021-9258(18)91331-1
Mohammed Habibur Rahman, Toru Maruyama, Tomoko Okada, Keishi Yamasaki, Masaki Otagiri, Study of interaction of carprofen and its enantiomers with human serum albumin--I. Mechanism of binding studied by dialysis and spectroscopic methods Biochemical Pharmacology. ,vol. 46, pp. 1721- 1731 ,(1993) , 10.1016/0006-2952(93)90576-I
U Kragh-Hansen, Molecular aspects of ligand binding to serum albumin. Pharmacological Reviews. ,vol. 33, pp. 17- 53 ,(1981)
Xiao Min He, Daniel C. Carter, Atomic structure and chemistry of human serum albumin. Nature. ,vol. 358, pp. 209- 215 ,(1992) , 10.1038/358209A0
Chengnong Yan, Jinqiang Tong, Dan Xiong, Yi Liu, Zuting Pan, Study on the Features of the Binding Reaction Between Pefloxacin and Bovine Serum Albumin Using Fluorescence Spectrophotometry Chinese Journal of Analytical Chemistry. ,vol. 34, pp. 796- 800 ,(2006) , 10.1016/S1872-2040(06)60041-8
B. K. MARTIN, Potential Effect of the Plasma Proteins on Drug Distribution Nature. ,vol. 207, pp. 274- 276 ,(1965) , 10.1038/207274A0
David C. Hooper, Mode of Action of Fluoroquinolones Drugs. ,vol. 58, pp. 6- 10 ,(1999) , 10.2165/00003495-199958002-00002