Document Detail

In vitro and in vivo antioxidant properties of gliclazide.
MedLine Citation:
PMID:  11004429     Owner:  NLM     Status:  MEDLINE    
Diabetes is a state of increased oxidant stress and there is evidence that oxidation may play a role in the genesis of complications. Gliclazide, a sulfonylurea hypoglycemic drug, has been shown to possess free radical scavenging properties. This study examined the effects of in vitro supplementation with gliclazide and other sulfonylureas as on low-density lipoprotein (LDL) oxidation and the total plasma antioxidant capacity (TPAC). In a separate study, the effects of 10 months of oral gliclazide therapy on oxidative parameters were assessed in 44 type 2 diabetic patients. Gliclazide, but not glibenclamide, glimepiride, glipizide or tolbutamide, inhibited LDL oxidation and enhanced TPAC. With the addition of 1 microM gliclazide, oxidation lag time increased from 53.6+/-2.6 to 113.6+/-5.1 min (p<0.001), and TPAC increased from 1. 09+/-0.11 to 1.23+/-0.11 mM (p<0.01). Administration of either modified release or standard gliclazide to type 2 diabetic patients resulted in a fall in 8-isoprostanes, a marker of lipid oxidation, and an increase in the antioxidant parameters TPAC, SOD and thiols. These studies show that gliclazide possesses antioxidant properties that produce measurable clinical effects at therapeutic doses.
R C O'Brien; M Luo; N Balazs; J Mercuri
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of diabetes and its complications     Volume:  14     ISSN:  1056-8727     ISO Abbreviation:  J. Diabetes Complicat.     Publication Date:    2000 Jul-Aug
Date Detail:
Created Date:  2000-10-17     Completed Date:  2000-10-17     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  9204583     Medline TA:  J Diabetes Complications     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  201-6     Citation Subset:  IM    
Department of Medicine, Monash University, Victoria 3168, Clayton, Australia.
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MeSH Terms
Antioxidants / pharmacology,  therapeutic use*
Blood Glucose / analysis
Diabetes Mellitus, Type 2 / blood,  drug therapy*
Dinoprost / analogs & derivatives,  blood
Free Radical Scavengers
Gliclazide / pharmacology,  therapeutic use*
Hemoglobin A, Glycosylated / analysis
Hypoglycemic Agents / therapeutic use
Lipid Peroxidation
Lipoproteins, LDL / blood
Middle Aged
Oxidative Stress
Superoxide Dismutase / blood
Reg. No./Substance:
0/Antioxidants; 0/Blood Glucose; 0/F2-Isoprostanes; 0/Free Radical Scavengers; 0/Hemoglobin A, Glycosylated; 0/Hypoglycemic Agents; 0/Lipoproteins, LDL; 21187-98-4/Gliclazide; 27415-26-5/8-epi-prostaglandin F2alpha; 551-11-1/Dinoprost; EC Dismutase

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