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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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Grape-seed procyanidins prevent the cafeteria-diet-induced decrease of glucagon-like peptide-1 production.

Noemi González-Abuín1, Neus Martínez-Micaelo, Mayte Blay

  • 1Departament de Bioquímica i Biotecnologia, Universitat Rovira i Virgili , 43007 Tarragona, Spain.

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Grape-seed procyanidin extract (GSPE) prevents diet-induced insulin resistance by maintaining glucagon-like peptide-1 (GLP-1) levels. GSPE supports intestinal GLP-1 production and protects against impaired glucose homeostasis.

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Area of Science:

  • Metabolism and Endocrinology
  • Nutritional Science
  • Gastroenterology

Background:

  • Diet-induced insulin resistance impairs glucose homeostasis.
  • Glucagon-like peptide-1 (GLP-1) plays a crucial role in regulating glucose metabolism.
  • Grape-seed procyanidin extract (GSPE) has shown potential in improving insulin resistance.

Purpose of the Study:

  • To investigate the preventive effects of GSPE on GLP-1 production, secretion, and elimination in a diet-induced insulin resistance model.
  • To understand GSPE's impact on intestinal GLP-1 regulation and related enzymes.
  • To explore GSPE's influence on GLP-1 signaling pathways in the hypothalamus.

Main Methods:

  • Rats were fed a cafeteria diet for 12 weeks to induce insulin resistance.
  • GSPE (25 mg/kg) was administered concurrently with the cafeteria diet.
  • Plasma active GLP-1 levels, intestinal GLP-1 production, colonic enteroendocrine cell populations, intestinal dipeptidyl-peptidase 4 (DPP4) activity, and hypothalamic gene expression of GLP-1 and its receptor were assessed.

Main Results:

  • The cafeteria diet significantly decreased active GLP-1 plasma levels, linked to reduced intestinal GLP-1 production and fewer colonic enteroendocrine cells.
  • GSPE administration prevented the decrease in active GLP-1 levels and preserved intestinal GLP-1 production.
  • GSPE maintained intestinal DPP4 activity and modulated the gene expression of GLP-1 and its receptor in the hypothalamus.

Conclusions:

  • GSPE effectively prevents the detrimental effects of a cafeteria diet on intestinal GLP-1 production.
  • GSPE mitigates diet-induced insulin resistance by preserving GLP-1 homeostasis.
  • GSPE demonstrates potential as a preventive strategy against metabolic dysfunction associated with poor diet.