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氨基糖苷类抗生素对兔肾皮质切片中碘马尿酸盐蓄积的pH依赖性影响。

The pH-dependent influence of aminoglycoside antibiotics on iodohippurate accumulation in rabbit renal cortical slices.

作者信息

Milman N, Dahlager J

出版信息

J Antibiot (Tokyo). 1978 Nov;31(11):1183-7. doi: 10.7164/antibiotics.31.1183.

Abstract

The effects of aminoglycoside antibiotics on 125I-hippurate (OIH) accumulation in rabbit renal cortical slices were assessed in vitro using incubation media with pH-values ranging from 6.4 to 8.4 and containing streptomycin, kanamycin, amikacin, gentamicin and tobramycin in concentrations ranging from 100 to 2,000 microgram base/ml. The aminoglycoside-induced inhibition of OIH accumulation was clearly pH-dependent and most pronounced at alkaline pH-values. At pH 6.4 and 7.4 the aminoglycosides had either no or only moderate effects on OIH accumulation, while all drugs produced a distinct depression in accumulation at pH 7.9 and 8.4. The microbiologically inert N-acetyl gentamicin had no influence on accumulation. The influence of aminoglycosides on OIH accumulation is probably related to the pKa-values of these drugs and implies the presence of free amino groups.

摘要

使用pH值范围为6.4至8.4且含有浓度范围为100至2000微克碱基/毫升的链霉素、卡那霉素、阿米卡星、庆大霉素和妥布霉素的孵育培养基,在体外评估了氨基糖苷类抗生素对兔肾皮质切片中125I-马尿酸盐(OIH)蓄积的影响。氨基糖苷类药物引起的OIH蓄积抑制明显依赖于pH值,在碱性pH值时最为显著。在pH 6.4和7.4时,氨基糖苷类药物对OIH蓄积要么没有影响,要么只有中等程度的影响,而在pH 7.9和8.4时,所有药物均使蓄积明显降低。微生物学上无活性的N-乙酰庆大霉素对蓄积没有影响。氨基糖苷类药物对OIH蓄积的影响可能与这些药物的pKa值有关,这意味着存在游离氨基。

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