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新型氨基糖苷类抗生素维替米星的体内抗菌活性

In vivo antibacterial activity of vertilmicin, a new aminoglycoside antibiotic.

作者信息

You Xue-Fu, Li Cong-Ran, Yang Xin-Yi, Yuan Min, Zhang Wei-Xin, Lou Ren-Hui, Wang Yue-Ming, Li Guo-Qing, Chen Hui-Zhen, Song Dan-Qing, Sun Cheng-Hang, Cen Shan, Yu Li-Yan, Zhao Li-Xun, Jiang Jian-Dong

机构信息

Laboratory of Pharmacology, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

出版信息

Antimicrob Agents Chemother. 2009 Oct;53(10):4525-8. doi: 10.1128/AAC.00223-09. Epub 2009 Jul 27.

DOI:10.1128/AAC.00223-09
PMID:19635958
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2764209/
Abstract

Vertilmicin is a novel aminoglycoside antibiotic with potent activity against gram-negative and -positive bacteria in vitro. In this study, we further evaluated the efficacy of vertilmicin in vivo in systemic and local infection animal models. We demonstrated that vertilmicin had relatively high and broad-spectrum activities against mouse systemic infections caused by Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, and Enterococcus faecalis. The 50% effective doses of subcutaneously administered vertilmicin were 0.63 to 0.82 mg/kg, 0.18 to 0.29 mg/kg, 0.25 to 0.99 mg/kg, and 4.35 to 7.11 mg/kg against E. coli, K. pneumoniae, S. aureus, and E. faecalis infections, respectively. The therapeutic efficacy of vertilmicin was generally similar to that of netimicin, better than that of gentamicin in all the isolates tested, and better than that of verdamicin against E. coli 9612 and E. faecalis HH22 infections. The therapeutic efficacy of vertilmicin was further confirmed in local infection models of rabbit skin burn infection and mouse ascending urinary tract infection.

摘要

维替米星是一种新型氨基糖苷类抗生素,在体外对革兰氏阴性菌和阳性菌具有强大活性。在本研究中,我们进一步评估了维替米星在全身和局部感染动物模型中的体内疗效。我们证明,维替米星对由大肠杆菌、肺炎克雷伯菌、金黄色葡萄球菌和粪肠球菌引起的小鼠全身感染具有相对较高的广谱活性。皮下注射维替米星针对大肠杆菌、肺炎克雷伯菌、金黄色葡萄球菌和粪肠球菌感染的50%有效剂量分别为0.63至0.82mg/kg、0.18至0.29mg/kg、0.25至0.99mg/kg和4.35至7.11mg/kg。维替米星的治疗效果总体上与奈替米星相似,在所有测试分离株中优于庆大霉素,在针对大肠杆菌9612和粪肠球菌HH22感染方面优于弗氏米星。维替米星的治疗效果在兔皮肤烧伤感染和小鼠上行性尿路感染的局部感染模型中得到进一步证实。

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In vivo antibacterial activity of vertilmicin, a new aminoglycoside antibiotic.新型氨基糖苷类抗生素维替米星的体内抗菌活性
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本文引用的文献

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In vitro antibacterial activity of vertilmicin and its susceptibility to modifications by the recombinant AAC6'-APH2'' enzyme.韦替米星的体外抗菌活性及其对重组 AAC6'-APH2'' 酶修饰的敏感性。
Antimicrob Agents Chemother. 2008 Nov;52(11):3875-82. doi: 10.1128/AAC.01400-07. Epub 2008 Aug 18.
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Acquired gentamicin resistance by permeability impairment in Enterococcus faecalis.粪肠球菌通过通透性受损获得庆大霉素耐药性。
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Development of a long-term ascending urinary tract infection mouse model for antibiotic treatment studies.用于抗生素治疗研究的长期上行性尿路感染小鼠模型的建立。
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Aminoglycosides: activity and resistance.氨基糖苷类:活性与耐药性。
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