Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.

@article{Lee2007CeftezoleAC,
  title={Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.},
  author={D S Lee and Jin-Man Lee and Sung-Uk Kim and Kyu-Tae Chang and Sang-Han Lee},
  journal={International journal of molecular medicine},
  year={2007},
  volume={20 3},
  pages={379-83}
}
Using a high throughput-compatible assay to screen for potential alpha-glucosidase inhibitors, we found that the beta-lactam antibiotic ceftezole exhibited 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, we confirmed that blood… CONTINUE READING