In vitro and in vivo antibacterial activity of modithromycin against streptococci and Haemophilus influenzae.
In vitro and in vivo antibacterial activity of modithromycin against streptococci and Haemophilus influenzae.
复制标题
莫迪霉素对链球菌和流感嗜血杆菌的体外和体内抗菌活性。
DOI：
10.1093/jac/dkr161
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
N.
中科院分区：
文献类型：
--
作者：
Sato;T.;Kawai;Y.;Matsuda;H.;Tateda;K.;Kimura;S.;Ishii;Y.;Yamaguchi;K.;Gotoh;N.
目的研究莫地霉素对肺炎链球菌、化脓性链球菌和流感嗜血杆菌的体外和体内抗菌活性。进行上皮细胞系A549的实验感染，以比较抗菌剂的细胞内活性和持久作用。结果Modithromycin对两种链球菌的所有临床菌株（包括红霉素耐药菌株）的MIC均≤ 1 mg/L。特别是，携带（B）或（A）的莫地霉素的MIC。化脓菌数分别为泰利霉素的16-32倍和2-4倍。对H.对流感病毒的敏感性为8mg/L，是泰利霉素的4倍。Modithromycin和Azithromycin对细胞相关性H.在从顶端培养基中除去试剂后，用泰利霉素和左氧氟沙星对流感病毒进行免疫。在肺部感染模型中，莫地霉素对携带（B）的S表现出更大或相当的疗效。pneumoniae和H.结论：莫地霉素具有最有效的抗S.测试的抗菌剂的化脓性和活性。莫地霉素对S. pneumoniae和H.流感，这可能是由于其持久的细胞内活性。
ObjectivesIn vitroandin vivoantibacterial activities of modithromycin againstStreptococcus pneumoniae,Streptococcus pyogenesandHaemophilus influenzaewere examined.MethodsMICs were determined by the broth microdilution method. Experimental infection of epithelial cell line A549 was performed to compare the intracellular activity and lasting effects of the antimicrobial agents. To evaluatein vivoefficacy, the rat pulmonary infection model was used.ResultsModithromycin had MICs of ≤1 mg/L against all the clinical strains of both streptococci, including erythromycin-resistant strains. In particular, the MICs of modithromycin forerm(B)- ormef(A)-carryingS. pyogeneswere 16–32 times or 2–4 times lower than those of telithromycin, respectively. The MIC90of modithromycin forH. influenzaewas 8 mg/L, which was 4 times higher than that of telithromycin. Modithromycin, as well as azithromycin, showed a lasting inhibitory effect on bacterial growth of cell-associatedH. influenzaecompared with telithromycin and levofloxacin after removal of the agents from the apical medium. In the pulmonary infection model, modithromycin showed greater or comparable efficacy againsterm(B)-carryingS. pneumoniaeandH. influenzae, respectively, than telithromycin, regardless of having an MIC that was 2 or 4 times higher for these strains.ConclusionsModithromycin has the most potent anti-S. pyogenesactivity of the antimicrobial agents tested. Modithromycin also has the betterin vivoefficacy againstS. pneumoniaeandH. influenzae, which might be due to its lasting intracellular activity.