In vivo antibacterial activity of vertilmicin, a new aminoglycoside antibiotic.
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.
You
Xue-Fu
XF
Laboratory of Pharmacology, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. xuefuyou@hotmail.com
Li
Cong-Ran
CR
Yang
Xin-Yi
XY
Yuan
Min
M
Zhang
Wei-Xin
WX
Lou
Ren-Hui
RH
Wang
Yue-Ming
YM
Li
Guo-Qing
GQ
Chen
Hui-Zhen
HZ
Song
Dan-Qing
DQ
Sun
Cheng-Hang
CH
Cen
Shan
S
Yu
Li-Yan
LY
Zhao
Li-Xun
LX
Jiang
Jian-Dong
JD
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
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; C010523:verdamicin; D009428:Netilmicin