Ceftiofur is a broad-spectrum, third-generation β-lactamase resistant cephalosporin first described in 1987, is commonly used for in vitro veterinary research. Its metabolite (desfurolyceftiofur) also has antibiotic activity. Detection methods to detect the antibiotic activity of Ceftiofur and its metabolite in milk samples are commonly used.
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| Mechanism of Action | Like β-lactams, Cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases. Like many cephalosporins, Ceftiofur is resistant to β-lactamases. |
| Spectrum | Ceftiofur is a broad-spectrum antibiotic targeting a wide variety of Gram-positive and Gram-negative bacteria including β-lactamase producing strains. |
| Microbiology Applications |
Ceftiofur is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram -positive and Gram-negative microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC ranges include: Salmonella spp. 0.5 µg/mL – 2 µg/mL |
| Eukaryotic Cell Culture Applications | Ceftiofur was tested on equine bone marrow-derived mesenchymal stromal cells and found to have no overall effect on cell viability (Parker et al, 2011). The effect of Ceftiofur on cytokine production was examined in vitro and found it can downregulate tumor necrosis factor-alpha (TNF-alpha), interleukin-1beta (IL-1beta), and interleukin-6 (IL-6). It may inhibit LPS-induced production of inflammatory cytokines by blocking NF-kappaB and MAPKs signaling in RAW264.7 cells (Ci et al, 2008) |
| Molecular Formula | C19H17N5O7S3 |
| References |
Ci X et al (2008) Ceftiofur impairs pro-inflammatory cytokine secretion through the inhibition of the activation of NF-kappaB and MAPK. Biochem Biophys Res Commun. 372(1):73-77 PMID 18474228 Georgopapadakou NH (1992) Mechanisms of action of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines in Escherichia coli. Antimicrob. Agents Chemother. 37(3):559-565 PMID 8384817 Holyoak GR, Wang S, Liu S, Bunch TJ, Evans RC and Bunch TD (2009) The effects of Ceftiofur Sodium (axcel) on vovine oocyte and preimplantation embryonic development assessed by in vitro embryo production techniques. J. Vet. Pharmacol. Ther. 21(2):92-98 PMID 9597645 Parker RA, Clegg PD and Taylor SE (2011) The in vitro effects of antibiotics on cell viability and gene expression of equine bone marrow-derived mesenchymal stromal cells. Equine Vet. J. 44(3):355-360 Salmon SA, Watts JL, Yancey RJ (1996) In vitro activity of Ceftiofur and its primary metabolite, desfuroylceftiofur, against organisms of veterinary importance. J Vet Diagn Invest. 8(3):332-6. PMID 8844576 Yancey RJ et al (1987) Ceftiofur sodium, a broad-spectrum Cephalosporin: Evaluation in vitro and in vivo in mice. Am. J. Vet. Res. 48(7): 1050-1053 PMID 3631686 |
