氟喹诺酮类药物对大肠杆菌抑制作用量效关系的热化学研究  

Thermochemical Studies on the Quantity-Antibacterial Effect Relationship of Fluoroquinolones

作　　者：沈雪松[1] 刘义[1] 周传佩[2] 赵儒铭[1] 屈松生[1] 

机构地区：[1]武汉大学化学与环境科学学院 [2]湖北药检高等专科学校,武汉430064

出　　处：《化学学报》2000年第11期1463-1466,共4页Acta Chimica Sinica

基　　金：国家自然科学基金(29973030);湖北省自然科学基金(98J052);教育部青年骨干教师计划;武汉大学青年学术骨干专项基金

摘　　要：用LKB-2277生物活性检测系统,测定了洛美沙星、诺氟沙星、培氟沙星三种氟喹诺酮类抗菌素在37℃时,对大肠杆菌的抑制作用过程的热效应变化.根据热动力学模型,拟合了药物的k～c,P_(max)～k,I％～c等关系,定量计算了药物的半抑制浓度Ic_(50),从热动力学角度研究了氟喹诺酮类药物抗菌作用的量效关系,探讨了诺氟沙星和培氟沙星杀菌作用随着药物浓度增加呈双相变化的PE现象和作用机制.Using LKB - 2277 bioactivity monitor, the inhibitory action of three fluoroquinolones on Escherichia coli growth was investigated at 37℃. The three fluoroquinolones were Lomefloxacin, Norfloxacin and Pefloxacin. In accordance with thermokinetic model, the relationships of the drugs, such as k - c, Pmax- k and I% - c, were obtained. Half inhibitory concentrations of the drugs, Ic50, were obtained by quantitative analysis. From the view of thermodynamics, the relationship between quantity and effect of fluoroquinolones was investigated, which showed paradioxical effect (PE) situation. The action mechanism of paradioxical effect was also studied.

关 键 词：氟喹诺酮 量效关系 大肠杆菌 热化学 抗菌作用 

分 类 号：O642[理学—物理化学]