Effects of a grapeseed procyanidin extract (GSPE) on insulin resistance

Gemma Montagut1, Cinta Bladé, Mayte Blay

  • 1Department of Biochemistry and Biotechnology, Rovira i Virgili University, Tarragona, 43007 Spain.

Insights

Grape seed procyanidin extract (GSPE) shows promise for improving glucose homeostasis and insulin resistance. A daily dose of 25 mg/kg GSPE positively impacts metabolic health, particularly in adipose tissue.

Area of Science:

  • Biochemistry
  • Metabolic Syndrome Research
  • Nutraceuticals

Background:

  • Flavonoids, like those in grape seed procyanidin extract (GSPE), are recognized for potential benefits against metabolic syndrome risk factors.
  • However, their precise mechanisms in modulating glucose homeostasis remain incompletely understood.

Purpose of the Study:

  • To investigate the efficacy of GSPE in stimulating glucose uptake in insulin-resistant cells.
  • To evaluate the effects of GSPE on glucose metabolism and insulin resistance in hyperinsulinemic animal models.

Main Methods:

  • Assessed GSPE's glucose uptake stimulation in 3T3-L1 adipocytes resistant to insulin or dexamethasone.
  • Administered varying doses of GSPE to hyperinsulinemic rats fed a cafeteria diet for 30 days.
  • Analyzed plasma insulin, Homeostasis Model Assessment-insulin resistance (HOMA-IR) index, and gene expression (Pparg2, Glut4, Irs1) in adipose tissue.

Main Results:

  • GSPE demonstrated higher glucose uptake stimulation than insulin in insulin-resistant adipocytes, but was less effective when resistance was induced by dexamethasone.
  • GSPE treatment reduced plasma insulin levels and improved the HOMA-IR index in hyperinsulinemic rats.
  • A daily dose of 25 mg/kg GSPE down-regulated key adipocyte markers (Pparg2, Glut4, Irs1) in mesenteric white adipose tissue, while preserving acute glucose uptake responsiveness.

Conclusions:

  • A daily dose of 25 mg/kg GSPE exerts a positive long-term effect on glucose homeostasis, potentially by targeting adipose tissue for direct glucose uptake stimulation.
  • The study underscores the importance of considering bioactive dosage, as higher concentrations do not invariably yield greater benefits.

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...
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: 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...
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: 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...
Hormones Regulating Blood Glucose01:16

Hormones Regulating Blood Glucose

Insulin is released by beta cells of the pancreas when blood glucose levels are high. It facilitates glucose absorption and utilization in insulin-dependent cells with insulin receptors on their plasma membranes. Insulin promotes glucose uptake by increasing the number of glucose transport proteins in the cell membrane, allowing glucose to enter the cell. As a result, glucose utilization and ATP production are enhanced.
In addition to accelerating glucose uptake and utilization, insulin has...