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曲古霉素的杀菌活性及抗生素后效应

The bactericidal activity and postantibiotic effect of trospectomycin.

作者信息

Yagi B H, Schaadt R D, Zurenko G E

机构信息

Upjohn Laboratories, Upjohn Company, Kalamazoo, Michigan.

出版信息

Diagn Microbiol Infect Dis. 1992 Jul;15(5):417-23. doi: 10.1016/0732-8893(92)90083-6.

Abstract

Trospectomycin sulfate (trospectomycin, TRS) is a novel, broad-spectrum, aminocyclitol antibiotic that is being developed clinically for the treatment of upper respiratory tract infections, bacterial vaginosis, pelvic inflammatory disease, and gonorrhea. This study investigated the bactericidal activity (by time-kill kinetics) and the postantibiotic effect (PAE) of TRS. Species-dependent bacteriostatic/bactericidal activity was observed for TRS; the antibiotic was bacteriostatic for Staphylococcus epidermidis, Enterococcus faecalis, and Escherichia coli, and bactericidal for Haemophilus influenzae, Neisseria gonorrhoeae, Moraxella catarrhalis, and Bacteroides fragilis (one of two test strains). When TRS was tested at four times its minimum inhibitory concentration or at a maximum test concentration of 32 micrograms/ml, with a 1-hr exposure period, the following PAE values were recorded: S. epidermidis 30032, 1.8 hr, En. faecalis ATCC 29212, 1.6 hr, E. coli UC 311, 1.5 hr, E. coli UC 9451, 1.5 hr, H. influenzae 30063, greater than 4.0 hr, B. fragilis ATCC 25285, 5.2 hr, and B. fragilis UC 12199, 6.7 hr. The broad-spectrum PAE that was observed for TRS is somewhat unique compared with other antibiotics.

摘要

硫酸曲古抑菌素(曲古抑菌素,TRS)是一种新型的广谱氨基环醇类抗生素,目前正处于临床开发阶段,用于治疗上呼吸道感染、细菌性阴道病、盆腔炎和淋病。本研究调查了TRS的杀菌活性(通过时间杀菌动力学)和抗生素后效应(PAE)。观察到TRS具有物种依赖性的抑菌/杀菌活性;该抗生素对表皮葡萄球菌、粪肠球菌和大肠杆菌具有抑菌作用,对流感嗜血杆菌、淋病奈瑟菌、卡他莫拉菌和脆弱拟杆菌(两种测试菌株之一)具有杀菌作用。当以其最低抑菌浓度的四倍或最高测试浓度32微克/毫升测试TRS,暴露1小时时,记录到以下PAE值:表皮葡萄球菌30032为1.8小时,粪肠球菌ATCC 29212为1.6小时,大肠杆菌UC 311为1.5小时,大肠杆菌UC 9451为1.5小时,流感嗜血杆菌30063大于4.0小时,脆弱拟杆菌ATCC 25285为5.2小时,脆弱拟杆菌UC 12199为6.7小时。与其他抗生素相比,TRS观察到的广谱PAE有些独特。

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