Studies on the Action Features between Cefuroxime Axetil and Bovine Serum Albumin
WU Gang-ke1,YAN Cheng-nong2*,LIU Yi2,3
1. Clinical Laboratory,Central Hospital of Jingzhou,Jingzhou 434020, China 2. College of Chemistry and Environmental Engineering, Yangtze University, Jingzhou 434023, China 3. College of Chemistry and Molecule Sciences, Wuhan University, Wuhan 430072, China
Abstract:Under different temperatures and physiological conditions, with cefuroxime axetil concentrations in the range of 1.959×10-6 to 13.71×10-6 mol·L-1, and bovine serum albumin (BSA) concentrations at 2.0×10-6 mol·L-1, the interaction between cefuroxime axetil and BSA was studied by fluorescence spectroscopy, three-dimensional fluorescence spectrum, synchronous fluorescence spectrum and UV-Vis absorption spectroscopy. After analyzing and processing the fluorescence quenching data at different temperatures according to Sterm-Volmer equation,Lineweaver-Burk equation and thermodynamic equation, the average value of the apparent binding constant (KLB: 3.907×106 L·mol-1),and thermodynamics parameters (enthalpy change ΔH:-13.43 kJ·mol-1, entropy change ΔS:81.90 J·K-1 and standard Gibbs free energy change ΔGθ:-38.34 kJ· mol-1)were calculated, and the amounts of binding sites(n: 1.042)were measured. The fluorescence quenching mechanism of BSA after cefuroxime axetil was added was discussed. BSA was bound with cefuroxime axetil and formed a new compound. The quenching belonged to static fluorescence quenching. The thermodynamic parameters agree with ΔH≈0, ΔS>0 and ΔGθ<0, and the binding reaction is mainly entropy-driven and electro-static interaction force plays a major role in the reaction. The maximum emission wavelength of Tyr and Trp had an obvious red shift in the synchronous fluorescence spectra, the fluorescence emission wavelength of two peaks had a blue shift in the three-dimensional fluorescence spectrum of BSA in the presence of cefuroxime axetil and the maximum absorbtion wavelenghs of three systems in the UV-Vis absorption spectra were obviously different. These showed that the changes in the micro-environment of Tyr and Trp and demonstrated that the conformation of BSA changed as cefuroxime axetil had been added. This provides important information for discussing the configuration modification of BSA because of the added cefuroxime axetil, and for elucidating the pharmacological effects of cefuroxime axetil and biological effects in the organism.
吴刚珂1,颜承农2*,刘义2,3. 头孢呋辛酯与牛血清白蛋白相互作用特征研究[J]. 光谱学与光谱分析, 2008, 28(09): 2139-2143.
WU Gang-ke1,YAN Cheng-nong2*,LIU Yi2,3. Studies on the Action Features between Cefuroxime Axetil and Bovine Serum Albumin. SPECTROSCOPY AND SPECTRAL ANALYSIS, 2008, 28(09): 2139-2143.
[1] CHEN Xin-qian, JIN You-yu, TANG Guang(陈新谦, 金有豫, 汤 光). New Medicinal Chemistry(新编药物化学). Beijing:People’s Medical Press(北京:人民卫生出版社),2003. 60. [2] PENG Bo, YAN Zheng-yu, SHAO Xiu-fen, et al(彭 博, 严拯宇, 邵秀芬, 等). Chinese Journal of Spectroscopy Laboratory(光谱实验室),2005,22(5):913. [3] BI Shu-yun, DING Lan, SONG Da-qian, et al(毕淑云, 丁 兰, 宋大千, 等). Acta Chimica Sinica(化学学报),2005,63(23):2169. [4] YAN Cheng-nong, SHANGGUAN Yu-feng, LIU Yi, et al(颜承农, 上官云凤, 刘 义, 等). Spectroscopy and Spectral Analysis(光谱学与光谱分析), 2005, 25(9): 1486. [5] Athina P, Rebecca J G, Richard A F. J. Agric. Food Chem., 2005, 53: 158. [6] Seetharomappa J, Kamat B P. Chem. Pharm. Bull, 2004, 52: 1053. [7] Bhalchandra P K. Journal of Pharmaceutical and Biomedical Analysis, 2005, 38: 1046. [8] YAN Cheng-nong, ZHANG Hua-xun,JU Xiang,et al(颜承农, 张华新, 鞠 香, 等). Chinese Journal Analytical Chemistry(分析化学),2005,33(6):759. [9] YANG Pin, GAO Fei(杨 频, 高 飞). Principle of Bioinorganic Chemistry(生物无机化学原理). Beijing:Science Press(北京:科学出版社),2005. 57. [10] YANG Man-man, YANG Pin, ZHANG Li-wei(杨曼曼, 杨 频, 张立伟). Chinese Science Bulltin(科学通报),1994,39:31. [11] ZHANG Bao-lin, WANG Wen-qing, BAI Feng-lian(张宝林, 王文清, 白凤莲). Chemical Journal of Chinese Universities(高等学校化学学报), 1994, 15:373 [12] Mauricios B, Guilherme L I. J. Phys. Chem. B,1998, 102:4678. [13] Ross D P, Subramanian S. Biochemistry, 1981, 20: 3096. [14] Nemethy G,Scheraga H A. J. Phys. Chem., 1962,66: 1773. [15] Timasheff S V,Peeters H(ED). Protein of Biological Fluids,Oxford:Pergamon Press,1972. 511. [16] Frster T. Modern Quantum Chemistry, New York:Academic Press, 1996. 93. [17] YAN Cheng-nong, MEI Ping, XIONG Dan, et al(颜承农, 梅 平, 熊 丹, 等). Spectroscopy and Spectral Analysis(光谱学与光谱分析), 2006, 26(12): 2306. [18] ZHANG Hai-rong, GUO Si-yuan, LI Lin, et al(张海容, 郭祀远, 李 琳,等). Spectroscopy and Spectral Analysis(光谱学与光谱分析), 2001,21(6):829. [19] YAN Yuan, XU Jin-gou, CHEN Guo-zhen(鄢 远, 许金钩, 陈国珍). Science in China(Series B)(中国科学B辑),1997, 27:16. [20] YAN Cheng-nong, ZHANG Hua-xin, MEI Ping, et al(颜承农, 张华新, 梅 平, 等). Chinese Journal Chemistry(中国化学),2005,23:1151.