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Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration

2011; Wiley; Volume: 56; Issue: 3 Linguagem: Inglês

10.1002/mnfr.201100554

1613-4133

LeeCole Legette, Lian Ma, Ralph L. Reed, Cristobal L. Miranda, J. Mark Christensen, Rosita Rodriguez‐Proteau, Jan F. Stevens,

Garlic and Onion Studies

Abstract 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.