Nikaido H, Normark S
Department of Microbiology and Immunology, University of California, Berkeley 94720.
Mol Microbiol. 1987 Jul;1(1):29-36. doi: 10.1111/j.1365-2958.1987.tb00523.x.
In Gram-negative bacteria, beta-lactam antibiotics must overcome two barriers, the outer membrane and the periplasmic beta-lactamase, before they reach the targets of their action, penicillin-binding proteins. Although the barrier property of the outer membrane and catalytic property of the beta-lactamases have been studied and their significance in creating beta-lactam resistance emphasized, the interaction between these two barriers has not been treated quantitatively. Such treatment shows that the sensitivity, to a variety of beta-lactams, of the Escherichia coli K-12 cells containing very different levels of chromosomally coded AmpC beta-lactamase, or a plasmid-coded TEM-type beta-lactamase, can be predicted rather accurately from the penetration rate through the outer membrane and the hydrolysis rate in the periplasm. We further propose a new parameter, 'target access index', which is a quantitative expression of the result of interaction between the two barriers, and reflects the probability of success for the antibiotic to reach the targets.
在革兰氏阴性菌中,β-内酰胺类抗生素在作用于其靶标青霉素结合蛋白之前,必须克服两道屏障,即外膜和周质β-内酰胺酶。虽然外膜的屏障特性和β-内酰胺酶的催化特性已得到研究,且它们在产生β-内酰胺抗性方面的重要性也已得到强调,但这两道屏障之间的相互作用尚未进行定量研究。这种定量研究表明,对于含有不同水平染色体编码的AmpCβ-内酰胺酶或质粒编码的TEM型β-内酰胺酶的大肠杆菌K-12细胞,其对多种β-内酰胺类药物的敏感性,可以根据药物通过外膜的渗透率和在周质中的水解率相当准确地预测出来。我们还提出了一个新参数“靶标可达指数”,它是两道屏障之间相互作用结果的定量表达,反映了抗生素成功到达靶标的概率。