REVIEW Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Using an in vivo streptozotocin-induced mouse model, blood glucose levels decreased by 30% 20 min after ceftezole treatment (10 mg/kg/day). Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-gamma, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following ceftezole treatment.
Noto T, Nehashi T, Endo H, Saito M, Matsubara S. Ceftezole, a new cephalosporin C derivative I. In vitro and in vivo antimicrobial activity. J Antibiot (Tokyo). 1976 Oct;29(10):1058-70.
Minoru Nishida, Takeo Murakawa, Toshiaki Kamimura, Naohiko Okada, Hiroshi Sakamoto, Shigemi Fukada, Shoji Nakamoto, Yoshiko Yokota, and Kazuyo Miki In Vitro and In Vivo Evaluation of Ceftezole, a New Cephalosporin Derivative Antimicrob Agents Chemother. 1976 July; 10(1): 1-13.
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Hirai, Yoshimi; Suzuki, Miyako; Doi, Akemi; Nakazawa, Shozo Bacteriological evaluation of ceftezole, a new synthetic cephalosporin Chemotherapy (Tokyo) (1976), 24(4), 573-83.
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Yotsuji A, Mitsuyama J, Hori R, Yasuda T, Saikawa I, Inoue M, Mitsuhashi S. Mechanism of action of cephalosporins and resistance caused by decreased affinity for penicillin-binding proteins in Bacteroides fragilis. Antimicrob Agents Chemother. 1988 Dec;32(12):1848-53.
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Lee DS, Lee JM, Kim SU, Chang KT, Lee SH. Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity. Int J Mol Med. 2007 Sep;20(3):379-83.
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