Some Anthocyanins Could Be Efficiently Absorbed across the Gastrointestinal Mucosa: Extensive Presystemic Metabolism Reduces Apparent Bioavailability

Despite the accumulating evidence supporting the health effects of anthocyanins, their plasma concentrations were found to be very low. However, 30 and 56% of cyanidin 3-glucoside (Cy-3-glc) and pelargonidin 3-glucoside (Pg-3-glc) were found as protocatechuic acid (PCA) and 4-hydroxybenzoic acid, respectively, in plasma following oral administration in humans. Second, 12.4% of (13)C was recovered from urine and breath following oral ingestion of [(13)C]-Cy-3-glc in humans. The actual percentage of [(13)C]-Cy-3-glc absorbed across the gastrointestinal wall could be higher because of the involvement of enterohepatic recycling in the disposition of anthocyanins. In animal studies, high total urinary recoveries were found following oral ingestion of (14)C-labeled anthocyanins. Third, anthocyanins seem to be efficiently absorbed following in situ gastric and intestinal perfusions in rats. Therefore, some anthocyanins could be efficiently absorbed from the gastrointestinal lumen, undergo extensive first-pass metabolism, and enter the systemic circulation as metabolites.