Zimmermann W, Rosselet A
Antimicrob Agents Chemother. 1977 Sep;12(3):368-72. doi: 10.1128/AAC.12.3.368.
On the basis of a simple theoretical model, the ease of penetration of beta-lactam antibiotics through the outer membrane of Escherichia coli was measured. The cell envelope was found to act as a diffusion barrier to both penicillins and cephalosporins. The validity of the model and the cooperative action of cell-bound beta-lactamase and outer membrane were further verified by comparing calculated and experimentally determined velocities of beta-lactam hydrolysis by intact cells and sonically treated cell suspensions. The results showed good correspondence at five different antibiotic concentrations. Similar conclusions could be drawn from a comparison of beta-lactam concentrations on both sides of the outer membrane, calculated from enzyme kinetic measurements and minimal inhibitory concentrations for both a beta-lactamase-producing E. coli and its enzyme-negative variant. in the case of benzylpenicillin and cephalothin, however, no correspondence was found. The joint action of several parameters determining the efficacy of penicillins and cephalosporins against beta-lactamase-producing E. coli is discussed.
基于一个简单的理论模型,测定了β-内酰胺类抗生素穿透大肠杆菌外膜的难易程度。发现细胞包膜对青霉素和头孢菌素均起到扩散屏障的作用。通过比较完整细胞和经超声处理的细胞悬液中β-内酰胺水解的计算速度和实验测定速度,进一步验证了该模型的有效性以及细胞结合型β-内酰胺酶与外膜的协同作用。结果表明,在五种不同抗生素浓度下两者吻合良好。通过比较从酶动力学测量计算得出的外膜两侧β-内酰胺浓度以及产β-内酰胺酶的大肠杆菌及其无酶变体的最低抑菌浓度,也能得出类似结论。然而,对于苄青霉素和头孢噻吩,未发现两者吻合。文中讨论了决定青霉素和头孢菌素对产β-内酰胺酶大肠杆菌疗效的几个参数的联合作用。