Yano Hisakazu, Kobayashi Toshimitsu, Okitsu Naohiro, Aoki Akiko, Toriya Minoru, Nakada Yukiko, Sagai Hitoshi, Iyobe Shizuko, Inoue Matsuhisa
Department of Otolaryngology-Head and Neck Surgery, Tohoku University Graduate School of Medicine.
Jpn J Antibiot. 2007 Feb;60(1):31-46.
We examined antibacterial activities of 4 kinds of macrolides (MLs), erythromycin (EM), clarithromycin (CAM), azithromycin (AZM) and rokitamycin (RKM), against 4 bacterial species of clinical strains isolated in 2004. Bacterial isolates used were 51 strains of methicillin-susceptible Staphylococcus aureus (MSSA), 20 of Streptococcus pyogenes, 68 of Streptococcus agalactiae, and 120 of Streptococcus pneumoniae. Macrolide resistance genes, ermB and mefE, in macrolide-resistant S. pyogenes and S. agalactiae, and all of pneumococci were analyzed by PCR. Antimicrobial activities against macrolide-susceptible MSSA of EM and CAM, were more potent than those of RKM. By contrast, against S. pneumoniae, RKM was more effective than EM, CAM and AZM. Against S. pyogenes and S. agalactiae, 4 antibiotics showed similar antimicrobial activities. Twelve, 1 and 2 strains of MSSA, S. pyogenes and S. agalactiae, respectively, were resistant to EM, CAM and AZM, whereas RKM was active to almost, but not quite, of them. Among 120 strains of S. pneumoniae, 76 (63.3%) were resistant to EM (MIC; > or = 0.5 microg/mL), and 23, 15 and 28 strains were highly resistant (MIC; > 128 microg/mL) to EM, CAM and AZM, respectively. By contrast, for RKM, there were far fewer resistant strains, and there was no highly resistant strain. PCR analyses of macrolide-resistant genes revealed that 1 resistant strain of S. pyogenes and 2 of S. agalactiae carried mefE and ermB, respectively. In the case of S. pneumoniae, 59, 19 and 5 strains, respectively, carried ermB, mefE and both ermB and mefe. We also studied about bactericidal activities and postantibiotic effects (PAE) of MLs using macrolide-susceptible, and ermB- and mefE-carrying S. pneumoniae, and observed morphological alterations of the strains treated with the drugs by a scanning electron microscope. It was demonstrated that RKM had superior bactericidal activities and PAE than other 3 drugs, and potent destructive effects to all of 3 strains.
我们检测了4种大环内酯类药物（MLs），即红霉素（EM）、克拉霉素（CAM）、阿奇霉素（AZM）和罗他霉素（RKM）对2004年分离出的4种临床菌株的抗菌活性。所用的细菌分离株包括51株甲氧西林敏感金黄色葡萄球菌（MSSA）、20株化脓性链球菌、68株无乳链球菌和120株肺炎链球菌。采用聚合酶链反应（PCR）分析了耐大环内酯类的化脓性链球菌、无乳链球菌及所有肺炎链球菌中的大环内酯抗性基因ermB和mefE。EM和CAM对大环内酯敏感的MSSA的抗菌活性比RKM更强。相比之下，对于肺炎链球菌，RKM比EM、CAM和AZM更有效。对于化脓性链球菌和无乳链球菌，4种抗生素显示出相似的抗菌活性。分别有12株MSSA、1株化脓性链球菌和2株无乳链球菌对EM、CAM和AZM耐药，而RKM对几乎所有这些菌株都有活性，但并非全部。在120株肺炎链球菌中，76株（63.3%）对EM耐药（最低抑菌浓度；≥0.5μg/mL），分别有23株、15株和28株对EM、CAM和AZM高度耐药（最低抑菌浓度；>128μg/mL）。相比之下，对于RKM，耐药菌株要少得多，且没有高度耐药菌株。对大环内酯抗性基因的PCR分析显示，1株耐大环内酯的化脓性链球菌和2株无乳链球菌分别携带mefE和ermB。在肺炎链球菌中，分别有59株、19株和5株携带ermB、mefE以及ermB和mefE。我们还研究了MLs对大环内酯敏感、携带ermB和mefE的肺炎链球菌的杀菌活性和抗生素后效应（PAE），并通过扫描电子显微镜观察了用药物处理的菌株的形态变化。结果表明，RKM比其他3种药物具有更强的杀菌活性和PAE，对所有3种菌株都有强大的破坏作用。
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