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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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.
Acarbose and miglitol are typically...
Cell Specific Gene Expression01:58

Cell Specific Gene Expression

Multicellular organisms contain a variety of structurally and functionally distinct cell types, but the DNA in all the cells originated from the same parent cells. The differences in the cells can be attributed to the differential gene expression. Liver cells, whose functions include detoxification of blood, production of bile to metabolize fats, and synthesis of proteins essential for metabolism, must express a specific set of genes to perform their functions. Gene expression also varies with...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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 manages...

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Related Experiment Video

Updated: May 19, 2026

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro
12:00

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro

Published on: July 5, 2017

Grape seed-derived procyanidins decrease dipeptidyl-peptidase 4 activity and expression.

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

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

Journal of Agricultural and Food Chemistry
|August 16, 2012
PubMed
Summary

Grape seed procyanidins (GSPes) inhibit dipeptidyl-peptidase 4 (DPP4) activity and gene expression, particularly in the intestine. This modulation may contribute to their glucose-lowering effects in type 2 diabetes.

Related Experiment Videos

Last Updated: May 19, 2026

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro
12:00

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro

Published on: July 5, 2017

Area of Science:

  • Biochemistry
  • Endocrinology
  • Pharmacology

Background:

  • Dipeptidyl-peptidase 4 (DPP4) inhibitors represent a novel therapeutic class for type 2 diabetes.
  • Flavonoids are known to influence DPP4 activity.
  • Grape seed-derived procyanidins (GSPes) exhibit antihyperglycemic properties.

Purpose of the Study:

  • To investigate whether GSPes modulate DPP4 activity and/or expression.
  • To determine the impact of GSPes on glucose homeostasis in vivo.

Main Methods:

  • In vitro enzyme inhibition assays.
  • Cell culture studies using Caco-2 intestinal cells.
  • In vivo studies in healthy and diet-induced obese rats.
  • Measurement of DPP4 activity and gene expression in intestinal and plasma samples.
  • Oral and intraperitoneal glucose tolerance tests.

Main Results:

  • GSPes directly inhibit purified DPP4 in vitro.
  • Chronic GSPE treatment decreased DPP4 activity and gene expression in Caco-2 cells.
  • In vivo, GSPEs reduced intestinal DPP4 activity and gene expression in both healthy and obese rats.
  • Oral glucose tolerance was improved in healthy rats treated with GSPEs.
  • No significant changes in plasmatic DPP4 were observed.
  • Genetically obese rats showed reduced DPP4 gene expression but not activity.

Conclusions:

  • GSPEs inhibit intestinal DPP4 activity through direct inhibition and/or gene expression down-regulation.
  • This inhibition of intestinal DPP4 may contribute to the antihyperglycemic effects of GSPes.
  • Further research is warranted to elucidate the precise mechanisms and therapeutic potential.