Grape Seed-Derived Procyanidins Decrease Dipeptidyl-peptidase 4 Activity and Expression
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- 作者：Noemi Gonz谩lez-Abu铆n ; Neus Mart铆nez-Micaelo ; Mayte Blay ; Gerard Pujadas ; Santiago Garcia-Vallv茅 ; Montserrat Pinent ; Anna Ard茅vol
- 刊名：Journal of Agricultural and Food Chemistry
- 出版年：2012
- 出版时间：September 12, 2012
- 年：2012
- 卷：60
- 期：36
- 页码：9055-9061
- 全文大小：256K
- 年卷期：v.60,no.36(September 12, 2012)
- ISSN：1520-5118
文摘
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.