Disposition and metabolism of the flavonoid chrysin in normal volunteers

To describe the oral disposition of the dietary flavonoid chrysin in healthy volunteers. Oral 400 mg doses of chrysin were administered to seven subjects. Chrysin and metabolites were assayed in plasma, urine and faeces by h.p.l.c. Peak plasma chrysin concentrations were only 3-16 ng ml(-1) with AUC...

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Bibliographic Details
Published in:British journal of clinical pharmacology 2001-02, Vol.51 (2), p.143-146
Main Authors: WALLE, T, OTAKE, Y, BRUBAKER, J. A, WALLE, U. K, HALUSHKA, P. V
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Animals
Anti-HIV Agents - metabolism
Anti-HIV Agents - pharmacokinetics
Biological and medical sciences
Flavonoids - metabolism
Flavonoids - pharmacokinetics
General pharmacology
Humans
Male
Medical sciences
Models, Animal
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
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Summary:To describe the oral disposition of the dietary flavonoid chrysin in healthy volunteers. Oral 400 mg doses of chrysin were administered to seven subjects. Chrysin and metabolites were assayed in plasma, urine and faeces by h.p.l.c. Peak plasma chrysin concentrations were only 3-16 ng ml(-1) with AUCs of 5-193 ng ml(-1) h. Plasma chrysin sulphate concentrations were 30-fold higher (AUC 450-4220 ng ml(-1) h). In urine, chrysin and chrysin glucuronide accounted for 0.2-3.1 mg and 2-26 mg, respectively. Most of the dose appeared in faeces as chrysin. Parallel experiments in rats showed high bile concentrations of chrysin conjugates. These findings, together with previous data using Caco-2 cells, suggest that chrysin has low oral bioavailability, mainly due to extensive metabolism and efflux of metabolites back into the intestine for hydrolysis and faecal elimination.
ISSN:0306-5251
1365-2125
DOI:10.1046/j.1365-2125.2001.01317.x