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[新型喹诺酮类药物T-3761的体外抗分枝杆菌活性]

[In vitro antimycobacterial activity of a new quinolone, T-3761].

作者信息

Tomioka H, Sato K, Saito H

机构信息

Department of Microbiology and Immunology, Shimane Medical University, Izumo, Japan.

出版信息

Kekkaku. 1995 Feb;70(2):97-101.

PMID:7699982
Abstract

We evaluated the in vitro antimicrobial activity of T-3761 and ofloxacin against representative pathogenic mycobacteria by the agar dilution method, using 7H11 agar medium. T-3761 showed appreciable antimicrobial activity against Mycobacterium tuberculosis (MIC90: 3.13 micrograms/ml), M. kansasii (MIC90: 6.25 micrograms/ml) and M. fortuitum (MIC90: 3.13 micrograms/ml), whereas the agent was not active against M. marinum (MIC90: 25 micrograms/ml), M. scrofulaceum (MIC90: 50 micrograms/ml), M. avium (MIC90: > 100 micrograms/ml), M. intracellulare (MIC90: > 100 micrograms/ml), M. chelonae subsp. abscessus (MIC90: > 100 micrograms/ml) and M. chelonae subsp. chelonae (MIC90: 50 micrograms/ml). The in vitro antimicrobial activity of T-3761 against M. fortuitum was a little more potent than that of ofloxacin, whereas the activity of T-3761 against the other mycobacteria was slightly inferior to that of ofloxacin. The antimycobacterial activity of T-3761 against M. tuberculosis H37Rv (MIC in vitro: T-3761 = 3.13 micrograms/ml, OFLX = 0.78 micrograms/ml) phagocytosed in murine peritoneal macrophages was less active than that of ofloxacin, when the macrophages were cultured in RPMI-1640 medium containing 1 microgram/ml or 10 micrograms/ml of these agents for up to 5 days. The activity of 10 micrograms/ml of T-3761 was equivalent to that of 1 microgram/ml of ofloxacin.

摘要

我们采用琼脂稀释法,使用7H11琼脂培养基,评估了T-3761和氧氟沙星对代表性致病性分枝杆菌的体外抗菌活性。T-3761对结核分枝杆菌(MIC90:3.13微克/毫升)、堪萨斯分枝杆菌(MIC90:6.25微克/毫升)和偶然分枝杆菌(MIC90:3.13微克/毫升)显示出明显的抗菌活性,而该药物对海分枝杆菌(MIC90:25微克/毫升)、瘰疬分枝杆菌(MIC90:50微克/毫升)、鸟分枝杆菌(MIC90:>100微克/毫升)、胞内分枝杆菌(MIC90:>100微克/毫升)脓肿分枝杆菌亚种(MIC90:>100微克/毫升)和龟分枝杆菌亚种(MIC90:50微克/毫升)无活性。T-3761对偶然分枝杆菌的体外抗菌活性比氧氟沙星略强,而T-3761对其他分枝杆菌的活性略低于氧氟沙星。当巨噬细胞在含有1微克/毫升或10微克/毫升这些药物的RPMI-1640培养基中培养长达5天时,T-3761对小鼠腹腔巨噬细胞吞噬的结核分枝杆菌H37Rv(体外MIC:T-3761 = 3.13微克/毫升,OFLX = 0.78微克/毫升)的抗分枝杆菌活性低于氧氟沙星。10微克/毫升的T-3761活性与1微克/毫升的氧氟沙星相当。

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