Institute of Antibiotics, Huashan Hospital, Fudan University, Shanghai, China.
Key Laboratory of Clinical Pharmacology of Antibiotics, National Health and Family Planning Commission of People's Republic of China, Shanghai, China.
J Antimicrob Chemother. 2017 Jul 1;72(7):1930-1936. doi: 10.1093/jac/dkx066.
To investigate mechanisms for the decreased susceptibility to ceftazidime/avibactam in KPC-producing Klebsiella pneumoniae (KPC-KP).
A total of 24 isolates, 8 each with ceftazidime/avibactam MICs of 4-8, 1-2 and ≤0.5 mg/L, were randomly selected from 214 clinical isolates of KPC-KP, and the β-lactamase hydrolysis activity and porin expression profiles were determined. Plasmid profile and relative expression and copy number of the bla KPC gene were also analysed.
Ceftazidime/avibactam MIC 50 and MIC 90 were 2 and 4 mg/L, respectively, for the 214 KPC-KP isolates. The hydrolysis activities of nitrocefin and ceftazidime in both of the ceftazidime/avibactam MIC 4-8 and 1-2 mg/L groups were significantly higher than those of the MIC ≤0.5 mg/L group, while the hydrolysis activities were 4-4.6-fold higher in the MIC 4-8 mg/L group than in the other two groups when 4 mg/L avibactam was added. The relative expression and copy number of the bla KPC gene in the MIC 4-8 mg/L group were 4.2-4.8-fold higher than in the other two groups. Meanwhile, SDS-PAGE showed that all isolates in the two groups with MIC ≥1 mg/L lacked OmpK35, which had either an early frameshift with a premature stop codon ( n = 15, ST11) or overexpression of the negative regulation genes, micF and ompR ( n = 1, ST15), whereas OmpK35 and OmpK36 could both be observed in all isolates with MIC ≤0.5 mg/L.
Decreased ceftazidime/avibactam susceptibility in KPC-KP clinical isolates is caused by high ceftazidime hydrolysis activity and OmpK35 porin deficiency and the majority of isolates belong to ST11.
研究产 KPC 肺炎克雷伯菌(KPC-KP)对头孢他啶/阿维巴坦敏感性降低的机制。
从 214 株 KPC-KP 临床分离株中随机选择 8 株头孢他啶/阿维巴坦 MIC 为 4-8、1-2 和≤0.5mg/L 的菌株,共计 24 株,分别测定β-内酰胺酶水解活性和孔蛋白表达谱。还分析了质粒谱以及 blaKPC 基因的相对表达和拷贝数。
214 株 KPC-KP 分离株的头孢他啶/阿维巴坦 MIC50 和 MIC90 分别为 2 和 4mg/L。头孢他啶/阿维巴坦 MIC 为 4-8 和 1-2mg/L 组的头孢他啶和硝噻吩的水解活性明显高于 MIC≤0.5mg/L 组,而当加入 4mg/L 阿维巴坦时,MIC 为 4-8mg/L 组的水解活性比其他两组高 4-4.6 倍。MIC 为 4-8mg/L 组 blaKPC 基因的相对表达和拷贝数比其他两组高 4.2-4.8 倍。同时,SDS-PAGE 显示,MIC≥1mg/L 的两组分离株均缺失 OmpK35,要么存在提前终止密码子的早期移码突变(n=15,ST11),要么负调控基因 micF 和 ompR 过表达(n=1,ST15),而 MIC≤0.5mg/L 的所有分离株均可观察到 OmpK35 和 OmpK36。
KPC-KP 临床分离株对头孢他啶/阿维巴坦敏感性降低是由于头孢他啶水解活性高和 OmpK35 孔蛋白缺乏所致,大多数分离株属于 ST11。