|Title||Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration.|
|Publication Type||Journal Article|
|Year of Publication||2012|
|Authors||Legette LC, Ma L, Reed RL, Miranda CL, Christensen JMark, Rodriguez-Proteau R, Stevens JF|
|Journal||Mol Nutr Food Res|
|Date Published||2012 Mar|
|Keywords||Administration, Oral, Animals, Area Under Curve, Biological Availability, Chromatography, Liquid, Dose-Response Relationship, Drug, Dyslipidemias, Flavonoids, Injections, Intravenous, Male, Propiophenones, Rats, Rats, Sprague-Dawley, Tandem Mass Spectrometry|
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 (C(max) ) and area under the curve (AUC(0-96 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.
|Alternate Journal||Mol Nutr Food Res|
|PubMed Central ID||PMC3401605|
|Grant List||P30 ES000210 / ES / NIEHS NIH HHS / United States |
R21 AT005294 / AT / NCCIH NIH HHS / United States
S10 RR022589 / RR / NCRR NIH HHS / United States
R21AT005294 / AT / NCCIH NIH HHS / United States