首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Activity of the Novel Macrolide BAL19403 against Ribosomes from Erythromycin-Resistant Propionibacterium acnes
【2h】

Activity of the Novel Macrolide BAL19403 against Ribosomes from Erythromycin-Resistant Propionibacterium acnes

机译:新型大环内酯BAL19403对抗红霉素痤疮丙酸杆菌核糖体的活性

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务,本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文,但由于OA文献来源多样且变更频繁,仍可能出现获取不到、文献不完整或与标题不符等情况,如果获取不到我们将提供退款服务。请知悉。

摘要

is a macrolide antibiotic from a novel structural class with potent activity against propionibacteria in vitro. The antibacterial spectrum of covers clinical isolates with mutations in the 2057 to 2059 region of 23S rRNA that confer resistance to erythromycin and clindamycin. The basis of this improved activity was investigated by ribosome binding assays and by a coupled transcription and translation assay. The latter was specifically developed for the use of ribosomes from Propionibacterium acnes. inhibited protein expression by ribosomes from erythromycin-sensitive and erythromycin-resistant P. acnes with similar potencies if the resistance was due to G2057A or A2058G mutations. showed a >10-fold higher activity than erythromycin against ribosomes from a strain with the erm(X) gene. Erm(X) confers high levels of macrolide and lincosamide resistance by dimethylation of A2058. Assays with such ribosomes showed that was potent enough to inhibit half of the total activity with a 50% inhibitory concentration very close to the value measured with erythromycin-sensitive ribosomes. We concluded from our data that the P. acnes strain with the erm(X) gene had a mixed population of ribosomes, with macrolide-sensitive and macrolide-resistant species.
机译:是一种来自新型结构类的大环内酯类抗生素,在体外具有对丙酸杆菌的强效活性。涵盖23S rRNA在2057至2059区域具有突变的临床分离株的抗菌谱,这些突变赋予了对红霉素和克林霉素的抗性。通过核糖体结合测定以及偶联的转录和翻译测定研究了这种提高的活性的基础。后者是专门为使用痤疮丙酸杆菌的核糖体而开发的。如果耐药是由于G2057A或A2058G突变引起的,则抑制核糖体对红霉素敏感和红霉素耐药的痤疮丙酸杆菌的蛋白表达具有相似的效力。对具有erm(X)基因的菌株的核糖体显示出比红霉素高10倍以上的活性。 Erm(X)通过A2058的二甲基化赋予高水平的大环内酯和林可酰胺抗性。用此类核糖体进行的测定表明,这种活性足以抑制总活性的一半,而50%的抑制浓度非常接近用红霉素敏感的核糖体测得的值。从我们的数据得出的结论是,带有erm(X)基因的痤疮丙酸杆菌菌株具有核糖体的混合种群,具有对大环内酯敏感和对大环内酯具有抵抗力的物种。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号