Cefazedone (Refosporen, Cefazedonum) is a semisynthetic first-generation cephalosporin with antibacterial activity.
Ceftezole exhibited potent α-glucosidase inhibitory activity. In in vitro α-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast α-glucosidase with a Ki value of 5.78×10?7 M when the enzyme mixture was pretreated with ceftezole[2].
In mice, dogs, and rabbits, cefazedone produced high and prolonged serum levels. It does not penetrate the CSF or brain tissue[1]. Ceftezole inhibits the blood glucose increase that occurs following glucose uptake. Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-γ, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following ceftezole treatment. It exhibits anti-diabetic activity in vivo[2].
[1] Dingeldein E, et al. Arzneimittelforschung. 1979, 29(2a):400-3. [2] Lee DS, et al. Int J Mol Med. 2007, 20(3):379-83.