Linus Pauling Institute, Oregon State University, Corvallis, OR, USA.
Mol Nutr Food Res. 2012 Mar;56(3):466-74. doi: 10.1002/mnfr.201100554. Epub 2011 Dec 7.
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.
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.
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.
黄腐酚（XN）是一种存在于啤酒花中的膳食类黄酮，可能对心血管疾病和 2 型糖尿病有保护作用。然而，XN 的药代动力学（PK）数据有限。本研究提供了 XN 及其在大鼠中的主要代谢物的 PK 参数。
在颈静脉插管的雄性 Sprague-Dawley 大鼠中进行了 PK 研究。大鼠（n = 12/组）分别静脉（IV）注射（1.86mg/kg BW）或口服低（1.86mg/kg BW）、中（5.64mg/kg BW）、高（16.9mg/kg BW）剂量的 XN。使用 LC-MS/MS 分析血浆样品中的 XN 和其代谢物。XN 及其结合物的最大浓度（C(max)）和 AUC(0-96 h)分别为 IV 组 2.9±0.1mg/L 和 2.5±0.3hmg/L，口服低剂量组 0.019±0.002mg/L 和 0.84±0.17hmg/L，口服中剂量组 0.043±0.002mg/L 和 1.03±0.12hmg/L，口服高剂量组 0.15±0.01mg/L 和 2.49±0.10hmg/L。
XN 的生物利用度呈剂量依赖性，大鼠低、中、高剂量组分别约为 0.33、0.13 和 0.11。
