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Title 

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

Authors 

D S LeeJ M LeeSung Uk KimKyu Tae ChangS H Lee

Publisher 

Spandidos Publications

Issue Date 

2007

Citation 

International Journal of Molecular Medicine, vol. 20, no. 3, pp. 379-383

Keywords 

animalsanti-bacterial agentsbase sequenceblood glucosecefmenoximeDNA primersdiabetes mellitus, experimentaldrug evaluation, preclinicalmalegene expression

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.

ISSN 

1107-3756

Link 

http://dx.doi.org/10.3892/ijmm.20.3.379

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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