intestinal absorption

human intestinal

carotene

drug metabolism

oral administration

grapefruit juice

drug absorption

pharmacokinetic model

Free Radical Biology and Medicine

The bioavailability of apigenin and its O -glycosides in humans was investigated with apigenin-4′-glucuronide (Ap-4′-GlcUA), apigenin-7-glucuronide and apigenin-7-sulfate being identified as in vivo metabolites. Apigenin per se was poorly absorbed with metabolites equivalent to 0.5% of intake excreted in urine 0–24 h post-intake. Consumption of a parsley drink containing apigenin-7- O -(2″- O -apiosyl)glucoside resulted in the peak plasma concentration ( C max ) of Ap-4′-GlcUA occurring after 4 h, indicative of absorption in the lower gastrointestinal tract (GIT). Urinary excretion of the three metabolites corresponded to 11.2% of intake. Ingestion of dried powdered parsley leaves with yogurt extended the C max of Ap-4′-GlcUA to 6 h. Consumption of chamomile tea containing apigenin-7′- O -glucoside resulted in a 2 h C max of Ap-4′-GlcUA, in keeping with absorption in the upper GIT. Urinary excretion was equivalent to 34% of intake. Intake of the parsley drink provided information on intra- and inter-individual variations in the level of excretion of the apigenin metabolites. This trail was registered at clinicaltrials.gov as NCT03526081. • Human absorption and metabolism of apigenin and its glycosides. • Identification of apigenin metabolites in plasma and urine. • Plasma pharmacokinetics and urinary excretion of apigenin metabolites. • Impact of sugar moiety on apigenin absorption. • Essential data for ex vivo tissue studies using apigenin metabolites.

Absorption, distribution, metabolism and excretion of apigenin and its glycosides in healthy male adults