Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration
2012
Legette, LeeCole | Ma, Lian | Reed, Ralph L. | Miranda, Cristobal L. | Christensen, John Mark | Rodriguez‐Proteau, Rosita | Stevens, Jan F.
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.
Show more [+] Less [-]AGROVOC Keywords
Bibliographic information
This bibliographic record has been provided by National Agricultural Library