Yamamoto T, Yokota T
Antimicrob Agents Chemother. 1977 Jun;11(6):936-40. doi: 10.1128/AAC.11.6.936.
Strains of Escherichia coli and Salmonella typhimurium carrying R plasmids, which were obtained from ampicillin-resistant clinical isolates of E. coli and Klebsiella spp. and specified either the type IIIa (TEM-type) or type Va (oxacillin-hydrolyzing) beta-lactamase, are resistant not only to ampicillin but also to carbenicillin and sulbenicillin. The latter two derivatives, however, are poorly hydrolyzed in vitro by the beta-lactamases. Although values of K(m) of the enzymes are lower for sulbenicillin and carbenicillin than for ampicillin, the ratios of V(max) to K(m) for sulbenicillin and carbenicillin are not high enough to explain the high resistance in E. coli bearing the R plasmid. Two mutants of the plasmids conferring a temperature-sensitive ampicillin resistance were induced by nitrosoguanidine treatment. It was confirmed that E. coli CSH2, harboring the mutant plasmid, produces a temperature-sensitive beta-lactamase and is resistant only at low temperatures (below 33 degrees C), but not at 42 degrees C, to ampicillin, sulbenicillin, and carbenicillin simultaneously. It is thus concluded that beta-lactamase itself is responsible for the mechanism of resistance not only to ampicillin but also to sulbenicillin and carbenicillin, even though the enzyme as determined in cell-free extracts hydrolyzes the latter two drugs poorly. An unknown barrier for sulbenicillin and carbenicillin directed by beta-lactamase in E. coli strains carrying R (bla) plasmids is postulated.
从大肠杆菌和肺炎克雷伯菌的耐氨苄西林临床分离株中获得的携带R质粒的大肠杆菌和鼠伤寒沙门氏菌菌株,其指定的IIIa型(TEM型)或Va型(水解苯唑西林)β-内酰胺酶不仅对氨苄西林耐药,而且对羧苄西林和磺苄西林耐药。然而,后两种衍生物在体外被β-内酰胺酶水解的程度很低。虽然该酶对磺苄西林和羧苄西林的米氏常数(K(m))值比对氨苄西林的低,但磺苄西林和羧苄西林的最大反应速度(V(max))与米氏常数的比值不够高,无法解释携带R质粒的大肠杆菌中的高耐药性。通过亚硝基胍处理诱导了两种赋予温度敏感型氨苄西林耐药性的质粒突变体。已证实,携带突变体质粒的大肠杆菌CSH2产生一种温度敏感型β-内酰胺酶,并且仅在低温(低于33℃)下对氨苄西林、磺苄西林和羧苄西林同时耐药,而在42℃时不耐药。因此得出结论,β-内酰胺酶本身不仅是对氨苄西林耐药的机制,也是对磺苄西林和羧苄西林耐药的机制,尽管在无细胞提取物中测定的该酶对后两种药物的水解能力很差。推测在携带R(bla)质粒的大肠杆菌菌株中存在由β-内酰胺酶介导的针对磺苄西林和羧苄西林的未知屏障。