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

  • Authors:
    • Dong-Sun Lee
    • Jin-Man Lee
    • Sung-Uk Kim
    • Kyu-Tae Chang
    • Sang-Han Lee
  • View Affiliations

  • Published online on: September 1, 2007     https://doi.org/10.3892/ijmm.20.3.379
  • Pages: 379-383
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Abstract

Using a high throughput-compatible assay to screen for potential α-glucosidase inhibitors, we found that the β-lactam antibiotic 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 5.78x10−7 M when the enzyme mixture was pretreated with ceftezole. Using an in vivo streptozotocin-induced mouse model, we confirmed that 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-γ, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following ceftezole treatment. Taken together, these in vivo and in vitro results suggest that ceftezole may be a clinically useful anti-diabetic compound.

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September 2007
Volume 20 Issue 3

Print ISSN: 1107-3756
Online ISSN:1791-244X

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APA
Lee, D., Lee, J., Kim, S., Chang, K., & Lee, S. (2007). Ceftezole, a cephem antibiotic, is an α-glucosidase inhibitor with in vivo anti-diabetic activity. International Journal of Molecular Medicine, 20, 379-383. https://doi.org/10.3892/ijmm.20.3.379
MLA
Lee, D., Lee, J., Kim, S., Chang, K., Lee, S."Ceftezole, a cephem antibiotic, is an α-glucosidase inhibitor with in vivo anti-diabetic activity". International Journal of Molecular Medicine 20.3 (2007): 379-383.
Chicago
Lee, D., Lee, J., Kim, S., Chang, K., Lee, S."Ceftezole, a cephem antibiotic, is an α-glucosidase inhibitor with in vivo anti-diabetic activity". International Journal of Molecular Medicine 20, no. 3 (2007): 379-383. https://doi.org/10.3892/ijmm.20.3.379