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

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Title
Ceftezole, a cephem antibiotic, is an α-glucosidase inhibitor with in vivo anti-diabetic activity
Author(s)
D S Lee; J M Lee; Sung Uk Kim; Kyu Tae Chang; S H Lee
Bibliographic Citation
International Journal of Molecular Medicine, vol. 20, no. 3, pp. 379-383
Publication Year
2007
Abstract
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 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. Taken together, these in vivo and in vitro results suggest that ceftezole may be a clinically useful anti-diabetic compound.
Keyword
α-glucosidaseAnti-diabeticCeftezoleIn vitroIn vivoInhibitor
ISSN
1107-3756
Publisher
Spandidos Publ Ltd
DOI
http://dx.doi.org/10.3892/ijmm.20.3.379
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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