Anthocyanin pharmacokinetics and dose-dependent plasma antioxidant pharmacodynamics following whole tart cherry intake in healthy humans

Abstract

Anthocyanin-rich tart cherries may impart health benefits for oxidative stress and inflammation. Anthocyanin (ACN) pharmacokinetic studies often sample plasma and urine within hours of ingestion; these approaches do not reveal enterohepatic metabolites that may be critical for pharmacodynamic bioactivity. This study investigated ACN pharmacokinetics in healthy humans following intake of Montmorency tart cherries (Prunus cerasus). Using a within-subject crossover design, subjects (n = 12) ingested whole frozen tart cherries (45 or 90 cherries), and blood and urine samples were collected over 12 hours. LC-MS/MS identified two unmodified ACN in plasma and two ACN metabolites in urine. Intake of 45 cherries caused a biphasic antioxidant response, while 90 cherries caused a prolonged elevation over the 12 h period. The broad antioxidant peak beyond 8 h suggests that enterohepatic metabolites contribute to antioxidant pharmacodynamics. These findings should encourage extended pharmacokinetic studies with ACN-rich foods to reveal their breadth of bioavailability and bioactivity.