Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration
Version of Record online: 7 DEC 2011
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Molecular Nutrition & Food Research
Volume 56, Issue 3, pages 466–474, March 2012
How to Cite
Legette, L., Ma, L., Reed, R. L., Miranda, C. L., Christensen, J. M., Rodriguez-Proteau, R. and Stevens, J. F. (2012), Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration. Mol. Nutr. Food Res., 56: 466–474. doi: 10.1002/mnfr.201100554
- Issue online: 28 MAR 2012
- Version of Record online: 7 DEC 2011
- Manuscript Accepted: 22 SEP 2011
- Manuscript Revised: 9 SEP 2011
- Manuscript Received: 9 AUG 2011
- National Institutes of Health. Grant Numbers: R21AT005294, S10 RR022589, P30 ES000210
- USANA Health Sciences, Inc., Salt Lake City, UT
- Anheuser-Busch Companies, Inc., St. Louis, MO
- Hopsteiner Inc., New York
Scope Xanthohumol (XN), a dietary flavonoid found in hops, may have health-protective actions against cardiovascular disease and type 2 diabetes. Yet, there are limited data on the pharmacokinetics (PK) of XN. This study provides PK parameters for XN and its major metabolites in rats.
Methods and results A PK study was conducted in male jugular vein-cannulated Sprague-Dawley rats. Rats (n = 12/group) received an intravenous (IV) injection (1.86 mg/kg BW) or an oral gavage of a low (1.86 mg/kg BW), medium (5.64 mg/kg BW), or high (16.9 mg/kg BW) dose of XN. Plasma samples were analyzed for XN and its metabolites using LC-MS/MS. The maximum concentration (Cmax) and area under the curve (AUC0-96 h) of total XN (free and conjugated) were 2.9±0.1 mg/L and 2.5±0.3 h* mg/L in IV group, 0.019±0.002 mg/L and 0.84±0.17 h* mg/L in the oral low group, 0.043±0.002 mg/L and 1.03±0.12 h* mg/L in the oral medium group, and 0.15±0.01 mg/L and 2.49±0.10 h* mg/L in the oral high group.
Conclusion The bioavailability of XN is dose-dependent and approximately 0.33, 0.13, and 0.11 in rats, for the low-, medium-, and high-dose groups, respectively.