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细菌对大环内酯类抗生素耐药多由核糖体改变所致,如对红霉素(EM)耐药系由ereA编码的核糖蛋白改变或由erx编码的rRNA甲基化所造成。由酶促反应引起耐药近年才有零星报道,O’HARA等报告从临床分离的几百株肠杆菌科细菌中有13株(1株大肠杆菌、3株肺炎克雷伯氏菌和9株绿脓杆菌)对EM均高度耐药。为探讨耐药性质,作者将大肠杆菌-Tf481A细胞破碎,得到一种酶能使EM、竹桃霉素(OLM)、螺旋霉素等大环内酯类抗生素失活,以OLM为底物进行试验,钝化产物经结构测定,证明它是2’-
Bacterial resistance to macrolides is mostly caused by changes in ribosomes, such as erythromycin (EM) resistance caused by ereA-encoded ribosomal proteins or erx-encoded rRNA methylation. Drug resistance caused by the enzymatic reaction only sporadically reported in recent years, O’HARA and other reports from the clinical isolation of several hundred strains of Enterobacteriaceae 13 (1 Escherichia coli, Klebsiella pneumoniae and 9 strains of 9 Pseudomonas aeruginosa) are highly resistant to EM. To explore the drug resistance nature, the authors crushed E. coli-Tf481A cells and obtained an enzyme that inactivates macrolide antibiotics such as EM, oleandomycin (OLM), spiramycin and the like, using OLM as a substrate Test, the passivation product was structurally determined to prove it was 2’-