Pharmacokinetics and metabolism of apigenin in female and male rats after a single oral administration.
The metabolism of apigenin, a weak estrogenic flavonoid phytochemical, was investigated in the rat. After a single oral administration of radiolabeled apigenin, 51.0% of radioactivity was recovered in urine, 12.0% in feces, 1.2% in the blood, 0.4% in the kidneys, 9.4% in the intestine, 1.2% in the liver, and 24.8% in the rest of the body within 10 days. Sex differences appear with regard to the nature of compounds eliminated via the urinary route: immature male and female rats, like mature female rats, excreted a higher percentage of the mono-glucuronoconjugate of apigenin than the mono-sulfoconjugate of apigenin (10.0-31.6% versus 2.0-3.6%, respectively). Mature male rats excreted the same compounds in an inverse ratio (4.9% and 13.9%, respectively). Radioactivity appeared in the blood only 24 h after oral administration. Blood kinetics showed a high elimination half-time (91.8 h), a distribution volume of 259 ml, and a plasmatic clearance of 1.95 ml/h. All of the parameters calculated from these experiments suggested a slow metabolism of apigenin, with a slow absorption and a slow elimination phase. Thus, a possible accumulation of this flavonoid in the body can be hypothesized.
Unité Mixte de Recherche de Toxicologie Alimentaire, INRA, 17 rue Sully, BP 86510, 21065 Dijon cedex, France.
Angéline
A
Gradolatto
Jean-Philippe
JP
Basly
Raymond
R
Berges
Caroline
C
Teyssier
Marie-Christine
MC
Chagnon
Marie-Héléne
MH
Siess
Marie-Chantal
MC
Canivenc-Lavier
D000284:Administration, Oral; D000367:Age Factors; D000818:Animals; D047310:Apigenin / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000652:urine; D005260:Female; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012727:Sex Characteristics
D047310:Apigenin