Kang Anthony D, Smith Kenneth P, Eliopoulos George M, Berg Anders H, McCoy Christopher, Kirby James E
Department of Pathology, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA; U.S. Army Medical Department Center and School, Fort Sam Houston, TX.
Department of Pathology, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA.
Diagn Microbiol Infect Dis. 2017 Jun;88(2):188-191. doi: 10.1016/j.diagmicrobio.2017.03.006. Epub 2017 Mar 16.
The in vitro activity of apramycin was compared to that of amikacin, gentamicin, and tobramycin against multidrug-resistant, extensively drug-resistant, and pandrug-resistant Acinetobacter baumannii and Pseudomonas aeruginosa. Apramycin demonstrated an MIC/MIC of 8/32μg/ml for A. baumannii and 16/32μg/ml for P. aeruginosa. Only 2% of A. baumannii and P. aeruginosa had an MIC greater than an epidemiological cutoff value of 64μg/ml. In contrast, the MIC/MIC for amikacin, gentamicin, and tobramycin were ≥64/>256μg/ml for A. baumannii with 57%, 95%, and 74% of isolates demonstrating resistance, respectively, and the MIC/MIC were ≥8/256μg/ml for P. aeruginosa with 27%, 50%, and 57% of strains demonstrating resistance, respectively. Apramycin appears to offer promising in vitro activity against highly resistant pathogens. It therefore may warrant further pre-clinical study to assess potential for repurposing as a human therapeutic and relevance as a scaffold for further medicinal chemistry exploration.
将阿泊霉素与阿米卡星、庆大霉素和妥布霉素对多重耐药、广泛耐药和全耐药鲍曼不动杆菌及铜绿假单胞菌的体外活性进行了比较。阿泊霉素对鲍曼不动杆菌的MIC/MIC为8/32μg/ml，对铜绿假单胞菌为16/32μg/ml。只有2%的鲍曼不动杆菌和铜绿假单胞菌的MIC大于64μg/ml的流行病学临界值。相比之下，阿米卡星、庆大霉素和妥布霉素对鲍曼不动杆菌的MIC/MIC分别为≥64/>256μg/ml，分别有57%、95%和74%的分离株显示耐药，对铜绿假单胞菌的MIC/MIC分别为≥8/256μg/ml，分别有27%、50%和57%的菌株显示耐药。阿泊霉素似乎对高度耐药病原体具有有前景的体外活性。因此，它可能值得进一步进行临床前研究，以评估其作为人类治疗药物重新利用的潜力以及作为进一步药物化学探索支架的相关性。
