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β-内酰胺类抗生素的细菌外膜通透性

The bacterial outer-membrane permeability of beta-lactam antibiotics.

作者信息

Sawai T, Matsuba K, Tamura A, Yamagishi S

出版信息

J Antibiot (Tokyo). 1979 Jan;32(1):59-65. doi: 10.7164/antibiotics.32.59.

Abstract

Two penicillins and 5 cephalosporins were evaluated for their ability to pass through the outer-membranes of Proteus morganii, Citrobacter freundii and Escherichia coli. Cefazolin, ceftezole and cephaloridine showed high permeability through the outer-membranes of these Gram-negative bacteria. Benzylpenicillin and cephalothin, on the contrary, showed low permeability. The outer-membrane permeability of ampicillin and cephalexin varied from species to species. C. freundii was found to have the highest barrier against both the penicillins and the cephalosporins, and E. coli appeared to have a low barrier against the cephalosporins. The hydrophobic character of the beta-lactam antibiotics, which was estimated by a reversed-phase thin-layer chromatography was closely related to the outer-membrane permeability. In general, the more hydrophilic antibiotic showed the higher outer-membrane permeability. However, cephaloridine, the most lipophilic compound among the antibiotics tested, showed good permeability.

摘要

对两种青霉素和5种头孢菌素透过摩根氏变形杆菌、弗氏柠檬酸杆菌和大肠杆菌外膜的能力进行了评估。头孢唑林、头孢替唑和头孢噻啶对这些革兰氏阴性菌的外膜表现出高通透性。相反,苄青霉素和头孢噻吩的通透性较低。氨苄青霉素和头孢氨苄的外膜通透性因菌种而异。发现弗氏柠檬酸杆菌对青霉素和头孢菌素的屏障作用最强,而大肠杆菌对头孢菌素的屏障作用似乎较弱。通过反相薄层色谱法估算的β-内酰胺抗生素的疏水性与外膜通透性密切相关。一般来说,亲水性越强的抗生素外膜通透性越高。然而,受试抗生素中亲脂性最强的头孢噻啶却表现出良好的通透性。

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