Grape Seed-Derived Procyanidins Decrease Dipeptidyl-peptidase 4 Activity and Expression

Dipeptidyl-peptidase 4 (DPP4) inhibitors are among the newest treatments against type 2 diabetes. Since some flavonoids modulate DPP4 activity, we evaluated whether grape seed-derived procyanidins (GSPEs), which are antihyperglycemic, modulate DPP4 activity and/or expression. In vitro inhibition ass...

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Bibliographic Details
Published in:Journal of agricultural and food chemistry 2012-09, Vol.60 (36), p.9055-9061
Main Authors: González-Abuín, Noemi, Martínez-Micaelo, Neus, Blay, Mayte, Pujadas, Gerard, Garcia-Vallvé, Santiago, Pinent, Montserrat, Ardévol, Anna
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
blood glucose
Blood Glucose - metabolism
Caco-2 Cells
Diabetes Mellitus, Type 2 - drug therapy
Diabetes Mellitus, Type 2 - enzymology
Diabetes Mellitus, Type 2 - genetics
Diabetes Mellitus, Type 2 - metabolism
Dipeptidyl Peptidase 4 - genetics
Dipeptidyl Peptidase 4 - metabolism
Down-Regulation - drug effects
Female
flavonoids
Food industries
Fruit and vegetable industries
Fundamental and applied biological sciences. Psychology
gene expression
Gene Expression - drug effects
gene expression regulation
glucose
Grape Seed Extract - pharmacology
grapes
homeostasis
Humans
noninsulin-dependent diabetes mellitus
Proanthocyanidins - pharmacology
procyanidins
Rats
Rats, Wistar
Rats, Zucker
Vitis - chemistry
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Summary:Dipeptidyl-peptidase 4 (DPP4) inhibitors are among the newest treatments against type 2 diabetes. Since some flavonoids modulate DPP4 activity, we evaluated whether grape seed-derived procyanidins (GSPEs), which are antihyperglycemic, modulate DPP4 activity and/or expression. In vitro inhibition assays showed that GSPEs inhibit pure DPP4. Chronic GSPE treatments in intestinal human cells (Caco-2) showed a decrease of DPP4 activity and gene expression. GSPE was also assayed in vivo. Intestinal but not plasmatic DPP4 activity and gene expression were decreased by GSPE in healthy and diet-induced obese animals. Healthy rats also showed glycemia improvement after oral glucose consumption but not after an intraperitoneal glucose challenge. In genetically obese rats, only DPP4 gene expression was down-regulated. Thus, procyanidin inhibition of intestinal DPP4 activity, either directly and/or via gene expression down-regulation, could be responsible for some of their effects in glucose homeostasis.
ISSN:0021-8561
1520-5118
DOI:10.1021/jf3010349