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金黄色葡萄球菌中的大环内酯类耐药性:大环内酯类耐药性的诱导因素。

Macrolide resistance in Staphylococcus aureus: inducers of macrolide resistance.

作者信息

Allen N E

出版信息

Antimicrob Agents Chemother. 1977 Apr;11(4):669-74. doi: 10.1128/AAC.11.4.669.

Abstract

Several macrolide-, lincosamide-, and streptogramin B-type (MLS) antibiotics were tested as inducers of erythromycin A (EM)-resistant [(14)C]leucine incorporation. Only 14-membered-ring macrolides having a glycosidically linked 6-deoxy sugar at the C-3 position of the lactone ring and the structurally dissimilar lincosamide, celesticetin, showed inducer activity. Modifications of EM at the C-4'' position of cladinose can apparently destroy the inducer property but do not affect the inhibitory properties of the antibiotic. The findings clearly show that inducer and inhibitor activities can be dissociated and are consistent with the concept that distinct binding/receptor sites are utilized for inhibition of ribosome function and induction of resistance.

摘要

测试了几种大环内酯类、林可酰胺类和链阳菌素B型(MLS)抗生素作为红霉素A(EM)抗性[(14)C]亮氨酸掺入诱导剂的情况。只有在内酯环C-3位具有糖苷键连接的6-脱氧糖的14元环大环内酯类以及结构不同的林可酰胺类药物天青菌素显示出诱导活性。在克拉定糖的C-4''位对EM进行修饰显然会破坏诱导特性,但不影响抗生素的抑制特性。这些发现清楚地表明诱导剂和抑制剂活性可以分离,并且与利用不同的结合/受体位点来抑制核糖体功能和诱导抗性的概念一致。

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