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β-内酰胺酶产生菌及其相应转接合子中β-内酰胺类药物的β-内酰胺酶稳定性与抗菌活性的相关性

Correlation of beta-lactamase stability and antibacterial activity of beta-lactams in beta-lactamase-producing bacteria and respective transconjugants.

作者信息

Esposito S, Galante D, Barba D, Pennucci C, Limauro D

出版信息

Drugs Exp Clin Res. 1986;12(4):329-33.

PMID:3522155
Abstract

A total of 343 Gram-negative bacteria were isolated and identified from urine specimens of patients with urinary tract infections. All the bacteria were investigated for their production of beta-lactamases by the nitrocefin test. beta-lactamase-producing strains were tested by the Datta method to detect any transfer of beta-lactamase production to a receiving E. coli K12 RN-strain. MICs of six beta-lactamase-stable compounds (ceftazidime, ceftriaxone, cefamandole, cefoxitin, cefotaxime, cefuroxime) were determined against all the beta-lactamase transferring bacteria and their respective transconjugants by a miniaturized dilution broth method. beta-lactamases produced by donors and transconjugants were purified and identified by determination of the isoelectric point by focusing; their hydrolytic activity was assessed by a spectrophotometric method using cytochrome c reduction. A total of 129 bacteria out of 343 produced beta-lactamases and 27 of these transferred the beta-lactamase production by conjugation. The beta-lactamases isolated from donors and transconjugants had the same pl and the same substrate profile. Ceftazidime was more stable to all the beta-lactamases isolated and more active against all the bacteria examined than the other compounds.

摘要

从尿路感染患者的尿液标本中分离并鉴定出343株革兰氏阴性菌。通过硝基头孢菌素试验研究所有细菌的β-内酰胺酶产生情况。对产生β-内酰胺酶的菌株采用达塔方法进行检测,以检测β-内酰胺酶产生是否转移至受体大肠杆菌K12 RN菌株。采用微量稀释肉汤法测定六种β-内酰胺酶稳定化合物(头孢他啶、头孢曲松、头孢孟多、头孢西丁、头孢噻肟、头孢呋辛)对所有β-内酰胺酶转移菌及其各自的接合子的最低抑菌浓度(MIC)。通过聚焦法测定等电点对供体菌和接合子产生的β-内酰胺酶进行纯化和鉴定;使用细胞色素c还原的分光光度法评估其水解活性。343株细菌中共有129株产生β-内酰胺酶,其中27株通过接合转移β-内酰胺酶产生。从供体菌和接合子中分离出的β-内酰胺酶具有相同的等电点和相同的底物谱。与其他化合物相比,头孢他啶对所有分离出的β-内酰胺酶更稳定,对所有检测的细菌活性更强。

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