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细菌对磺胺类药物摄取的pH依赖性

pH dependency in uptake of sulfonamides by bacteria.

作者信息

Büttner D, Büttner H

出版信息

Chemotherapy. 1980;26(3):153-63. doi: 10.1159/000237899.

Abstract

Sulfonamide-sensitive cells of Escherichia coli were incubated under standarized conditions with various sulfonamides and the quantity of sulfonamide uptake into the bacteria measured. The test substances reached a higher concentration inside the bacteria than in the incubation medium, the degree of accumulation varying for the individual substances despite uniformly applied incubation conditions. In all cases a pH dependency was detected which varied with the pKa values of the substances tested. On the basis of the pKa dependency of the pH effect, the sulfonamide uptake can be interpreted as being a passive diffusion process. Knowing the intracellular pH value, which was determined by the DMO method, it was then possible to calculate the theoretically expected value for the accumulation as a concentration coefficient. Since the calculated and experimentally determined values differ approximately by a factor of 2, an intracellular binding of the sulfonamides is assumed. The same results were obtained in cells of sulfonamide-resistant E. coli strains.

摘要

将大肠杆菌的磺胺敏感细胞在标准化条件下与各种磺胺类药物一起孵育,并测定细菌摄取磺胺类药物的量。测试物质在细菌内部达到的浓度高于孵育培养基中的浓度,尽管孵育条件一致,但各个物质的积累程度有所不同。在所有情况下都检测到了pH依赖性,其随测试物质的pKa值而变化。基于pH效应的pKa依赖性,磺胺类药物的摄取可解释为被动扩散过程。通过DMO方法确定了细胞内pH值后,就有可能计算出作为浓度系数的积累的理论预期值。由于计算值和实验测定值相差约2倍,因此假定磺胺类药物存在细胞内结合。在耐磺胺类药物的大肠杆菌菌株的细胞中也获得了相同的结果。

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