The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
In Vitro Microbiological Characterization of Novel Cyclic Homopentapeptides, CP-101, 680 and CP-163, 234, for Animal Health Use
LAURA J. L. NORCIAANNETTE M. SILVIAJOHN P. DIRLAMRODNEY C. SCHNURJAY M. BERGERONJAMES A. RETSEMASHIGERU F. HAYASHI
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1999 Volume 52 Issue 11 Pages 1007-1016

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Abstract

Two cyclic homopentapeptides, CP-101, 680 and CP-163, 234 [6a-(3', 4'-dichlorophenylamino) analogs of viomycin and capreomycin, respectively], were identified as novel antibacterial agents for the treatment of animal disease, especially for livestock respiratory disease. The in vitro microbiological characterization of both CP-101, 680 and CP-163, 234 was carried out using their parent compounds, viomycin and capreomycin, as controls. This characterization included antibacterial spectrum, influence of media, inoculum size, pH, EDTA, polymixin B nonapeptide (PMBN), serum, cell-free protein synthesis inhibition, and time-kill kinetics. Our results indicated that the capreomycin analog, CP-163, 234, showed slightly improved in vitro potency over the viomycin analog, CP-101, 680. Both analogs showed very potent cell-free protein synthesis inhibition activity and were bactericidal against Pasteurella haemolytica, P. multocida and Actinobacillus pleuropneumoniae at the level of 4 times and 8 times MICs. CP-163, 234 was bactericidal at the level of 4× and 8× MIC against E. coli, but re-growth was observed after 24 hours incubation at both concentrations of CP-101, 680.

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