title: In vivo antibacterial activity of vertilmicin, a new aminoglycoside antibiotic.
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.
authors.affiliation: Laboratory of Pharmacology, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. xuefuyou@hotmail.com
authors.forename: Xue-Fu
authors.initials: XF
authors.lastname: You
authors.forename: Cong-Ran
authors.initials: CR
authors.lastname: Li
authors.forename: Xin-Yi
authors.initials: XY
authors.lastname: Yang
authors.forename: Min
authors.initials: M
authors.lastname: Yuan
authors.forename: Wei-Xin
authors.initials: WX
authors.lastname: Zhang
authors.forename: Ren-Hui
authors.initials: RH
authors.lastname: Lou
authors.forename: Yue-Ming
authors.initials: YM
authors.lastname: Wang
authors.forename: Guo-Qing
authors.initials: GQ
authors.lastname: Li
authors.forename: Hui-Zhen
authors.initials: HZ
authors.lastname: Chen
authors.forename: Dan-Qing
authors.initials: DQ
authors.lastname: Song
authors.forename: Cheng-Hang
authors.initials: CH
authors.lastname: Sun
authors.forename: Shan
authors.initials: S
authors.lastname: Cen
authors.forename: Li-Yan
authors.initials: LY
authors.lastname: Yu
authors.forename: Li-Xun
authors.initials: LX
authors.lastname: Zhao
authors.forename: Jian-Dong
authors.initials: JD
authors.lastname: Jiang
mesh_terms: D000617:Aminoglycosides / Q000494:pharmacology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002056:Burns / Q000382:microbiology; D013293:Enterococcus faecalis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D007711:Klebsiella pneumoniae / Q000187:drug effects; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009428:Netilmicin / Q000494:pharmacology; D011817:Rabbits; D012871:Skin Diseases / Q000188:drug therapy / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects; D014552:Urinary Tract Infections / Q000188:drug therapy / Q000382:microbiology
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; C010523:verdamicin; D009428:Netilmicin