RT Journal Article
SR Electronic
T1 PHARMACOKINETICS AND METABOLISM OF APIGENIN IN FEMALE AND MALE RATS AFTER A SINGLE ORAL ADMINISTRATION
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 49
OP 54
DO 10.1124/dmd.104.000893
VO 33
IS 1
A1 Gradolatto, Angéline
A1 Basly, Jean-Philippe
A1 Berges, Raymond
A1 Teyssier, Caroline
A1 Chagnon, Marie-Christine
A1 Siess, Marie-Héléne
A1 Canivenc-Lavier, Marie-Chantal
YR 2005
UL http://dmd.aspetjournals.org/content/33/1/49.abstract
AB 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. The American Society for Pharmacology and Experimental Therapeutics