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Disposition and Metabolism of the Flavonoid Chrysin in Normal Volunteers

Overview
Journal Br J Clin Pharmacol
Specialty Pharmacology
Date 2001 Mar 22
PMID 11259985
Citations 73
Authors
T Walle
Y Otake
J A Brubaker
U K Walle
P V Halushka
Affiliations
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Abstract

Aims: To describe the oral disposition of the dietary flavonoid chrysin in healthy volunteers.

Methods: 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.

Results: 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.

Conclusions: 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.

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