Peonidin 3-O-glucoside chloride is an anthocyanin that works as an insulin secretagogue. Peonidin 3-O-glucoside chloride increases glucose uptake by HepG2 cells. Peonidin 3-O-glucoside chloride may be used to be utilized in study/research of comorbidities in type 2 diabetes.
Peonidin 3-O-glucoside chloride (P3G) is a naturally occurring anthocyanin found in red wine, berries, and pigmented rice. It is an agonist of the free fatty acid receptor FFAR1 (GPR40) and glucokinase (GK). It enhances insulin secretion from pancreatic beta-cells and increases glucose uptake in liver cells, making it of interest for diabetes research. Target: FFAR1 (GPR40) and Glucokinase (GK). P3G activates FFAR1, a G-protein coupled receptor expressed on pancreatic beta-cells and enteroendocrine cells, promoting glucose-dependent insulin secretion. It also activates glucokinase in hepatocytes, regulating glucose metabolism and glycolysis. In vitro, in INS-1E pancreatic beta-cells, P3G (1-100 microM, 24 h) significantly increases glucose-stimulated insulin secretion (GSIS) in a dose-dependent manner. It also upregulates phosphorylation of FFAR1 downstream proteins including PLC and PKD. In HepG2 hepatocytes, P3G (100 microM, 24 h) increases glucose uptake, activates GK, and modulates carbohydrate metabolism by increasing p-AMPK and decreasing PEPCK expression. In vivo studies in diabetic animal models are limited. Given its mechanism, oral administration of P3G in mice is expected to improve glucose tolerance and insulin secretion. Direct in vivo efficacy data for this specific compound require further investigation. For cell-free FFAR1 activation assays: membranes prepared from FFAR1-transfected CHO cells are incubated with increasing concentrations of P3G (1-100 microM) in assay buffer containing GDP and 35S-GTPgammaS, incubated, filtered, washed, and bound radioactivity counted. EC50 values can be calculated. For cell assays: INS-1E pancreatic beta-cells seeded in 96-well plates are pretreated with P3G (1-100 microM) for 24 h, then stimulated with 2.8 or 16.7 mM glucose in Krebs-Ringer buffer for 1 h. Supernatants are collected, and insulin concentrations are measured by ELISA. HepG2 cells are treated similarly for glucose uptake assays using 2-NBDG fluorescent glucose analog. No in vivo animal studies have been specifically reported for this compound. Animal studies for related anthocyanins involve oral gavage administration to diabetic mice for 4-8 weeks, monitoring blood glucose, insulin levels, glucose tolerance tests (IPGTT), and insulin tolerance tests (ITT). PK properties: Not well characterized for P3G. Anthocyanins generally have poor oral bioavailability (<2%) due to rapid metabolism and excretion, but can be detected in plasma after consumption. Peak plasma concentrations occur within 1-2 hours post-ingestion. Extensive phase II metabolism (glucuronidation, sulfation) occurs. No significant toxicity has been reported for P3G. As a food-derived compound, it is considered safe at dietary levels. At high doses (>500 mg/kg) in rodent studies, no acute or chronic toxicity was observed. P3G is a natural product found in foods and dietary supplements. It is not FDA-approved as a drug. It is widely studied in nutritional science and as a potential lead for developing novel antidiabetic therapeutics due to its dual mechanism of action (FFAR1 agonist and GK activator) targeting both insulin secretion and glucose metabolism.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.