Abstract
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.
Footnotes
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This work was supported by grants from the Conseil Régional de Bourgogne, from the Ministère de l'Environnement, and from the Institut National de la Recherche Agronomique.
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doi:10.1124/dmd.104.000893.
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ABBREVIATIONS: LC-MS, liquid chromatography-mass spectrometry; GA, glucuronoconjugate(s) of apigenin; SA, sulfoconjugate(s) of apigenin.
- Received June 8, 2004.
- Accepted October 1, 2004.
- The American Society for Pharmacology and Experimental Therapeutics
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