Ceftiofur (hydrochloride)

Ceftiofur hydrochloride is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur hydrochloride exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur hydrochloride also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6^[1][2][3]. IC50 & Target:bacterial^[1] In Vitro:Ceftiofur (1, 5, 10 mg/L; pretreatment for 1 h+LPS stimulation for 12 h) hydrochloride can significantly inhibit the secretion of TNF-α, IL-1β, and IL-6 in RAW 264.7 cells, but has no significant effect on the secretion of IL-10^[2].
Ceftiofur hydrochloride (1, 5, 10 mg/L; pretreatment for 1 h+LPS stimulation for 30 min) can significantly inhibit the phosphorylation of ERK, JNK, and p38 and the nuclear translocation of NF-κB p65 in RAW 264.7 cells^[2].
In Vivo:Ceftiofur (20 mg/kg; sc; single dose; 1 h before or 0/1 h after 30 mg/kg LPS challenge) hydrochloride significantly improves the survival rate of mice in the endotoxemia model of female C57BL/6 mice, and reduces the levels of plasma TNF-α, IL-1β, and IL-6, and increases the level of IL-10^[3].