头孢哌酮和乳酸环丙沙星与人血清白蛋白相互作用的荧光光谱研究  

Study on Interaction of Cefoperazone and Ciprofloxacin Lactate with Human Serum Albumin by Fluorescence Spectrum

作　　者：麻能轩[1] 慕丽晓[1] 李瑞金[2] 周叶红[2] 双少敏[1] 

机构地区：[1]山西大学化学化工学院,太原030006 [2]山西大学环境科学研究所,太原030006

出　　处：《中国药房》2013年第33期3084-3086,共3页China Pharmacy

基　　金：国家自然科学基金资助项目(No.21175087)

摘　　要：目的:探讨头孢哌酮(CPZ)、乳酸环丙沙星(CFLX)单独和同时存在时与人血清白蛋白(HSA)的相互作用。方法:采用荧光光谱法研究CPZ、CFLX单独和同时存在时对HSA的荧光猝灭作用,通过Stern-Volmer方程计算猝灭常数(Kq),判断猝灭机制;计算结合常数(KA)和结合位点数。结果:20、37℃时,HSA-CPZ体系的Kq分别为1.1×1012、0.87×1012L(/mol·s);HSA-CFLX体系Kq分别为2.67×1012、1.75×1012L(/mol·s)。CPZ和CFLX对HSA的内源性荧光均因形成复合物而产生静态猝灭。20、37℃时HSA-CPZ和HSA-CFLX体系的KA为0.11×103～1.79×103L/mol,结合位点数为0.57～0.75。37℃时,HSA-CFLX-CPZ体系的KA值为3.47×103L/mol,与HSA-CPZ体系KA值之比为31.55;HSA-CPZ-CFLX体系的KA值为3.59×103L/mol,与HSA-CFLX体系KA值之比为8.55。结论:CPZ和CFLX同时存在时,一种药物的存在会使另外一种药物与HSA的KA增大、结合稳定性增强,从而致使游离药物的浓度降低,药效下降。OBJECTIVE： To investigate the interaction of cefoperazone （CPZ） and ciprofloxacin lactate （CFLX） alone or com- bination with human serum albumin （HSA）. METHODS： Fluorescence spectrum was used to investigate the fluorescence quench- ing effect of CPZ and CFLX alone or combination on HSA. The quenching constants （Kq） were calculated by using Stern-Volmer equation to determine quenching mechanism, and the binding constant （KA） and the number of binding site were obtained. RE- SULTS： At 20 ℃ and 37 ℃, Kq of HSA-CPZ were 1.1×10^12, 0.87×10^12 L/（mol-s）; Kq of HSA-CFLX were 2.67×10^12, 1.75×10^2 L/（mol-s）. CPZ and CFLX could cause the static quenching of HSA endogenous fluorescence due to forming compound. At 20 ℃ and 37 ℃, KA of HSA-CPZ and HSA-CFLX were 0.11×10^3-1.79×10^3 L/mol and binding sites of them were 0.57-0.75. At 37 ℃, KA of HSA-CFLX-CPZ was 3.47×10^3 L/mol, and ratio of it to KA of HSA-CPZ was 31.55; KA of HSA-CPZ-CFLX was 3.59×10^3 L/mol, and ratio of it to KA of HSA-CFLX was 8.55. CONCLUSIONS： CPZ and CFLX in the ternary system, the presence of one drug would enhance the binding constant and stability of the other drug with HSA, which induces the concentration of free drug decreasing and the efficacy of the drugs could be reduced.

关 键 词：头孢哌酮 乳酸环丙沙星 人血清白蛋白 静态猝灭 荧光光谱 

分 类 号：R917[医药卫生—药物分析学] R913[医药卫生—药学]