Linus Pauling Institute, Oregon State University, Corvallis, OR, USA; College of Pharmacy, Oregon State University, Corvallis, OR, USA.
Mol Nutr Food Res. 2014 Feb;58(2):248-55. doi: 10.1002/mnfr.201300333. Epub 2013 Aug 27.
Xanthohumol (XN) is a bioactive prenylflavonoid from hops. A single-dose pharmacokinetic (PK) study was conducted in men (n = 24) and women (n = 24) to determine dose-concentration relationships.
Subjects received a single oral dose of 20, 60, or 180 mg XN. Blood was collected at 0, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 120 h. Plasma levels of XN and its metabolites, isoxanthohumol (IX), 8-prenylnaringenin (8PN), and 6-prenylnaringenin (6PN) were measured by LC-MS/MS. Xanthohumol (XN) and IX conjugates were dominant circulating flavonoids among all subjects. Levels of 8PN and 6PN were undetectable in most subjects. The XN PK profile showed peak concentrations around 1 h and between 4-5 h after ingestion. The maximum XN concentrations (C(max)) were 33 ± 7 mg/L, 48 ± 11 mg/L, and 120 ± 24 mg/L for the 20, 60, and 180 mg dose, respectively. Using noncompartmental modeling, the area under the curves (AUC(0→∞)) for XN were 92 ± 68 h × μg/L, 323 ± 160 h × μg/L, and 863 ± 388 h × μg/L for the 20, 60, and 180 mg dose, respectively. The mean half-life of XN was 20 h for the 60 and 18 h for the 180 mg dose.
XN has a distinct biphasic absorption pattern with XN and IX conjugates being the major circulating metabolites.
黄腐酚（XN）是一种来自啤酒花的生物活性类异戊二烯黄酮。在男性（n=24）和女性（n=24）中进行了单次剂量药代动力学（PK）研究，以确定剂量-浓度关系。
受试者单次口服 20、60 或 180mgXN。在 0、0.25、0.5、1、2、4、8、12、24、48、72、96 和 120h 采集血样。通过 LC-MS/MS 测量 XN 及其代谢物异黄腐酚（IX）、8-异戊烯基柚皮素（8PN）和 6-异戊烯基柚皮素（6PN）的血浆水平。在所有受试者中，XN 和 IX 缀合物是主要的循环类黄酮。大多数受试者的 8PN 和 6PN 水平无法检测到。XN PK 特征显示摄入后约 1 小时和 4-5 小时达到峰值浓度。20、60 和 180mg 剂量的 XN 最大浓度（C(max)）分别为 33±7mg/L、48±11mg/L 和 120±24mg/L。使用非房室模型，XN 的曲线下面积（AUC(0→∞)）分别为 92±68h×μg/L、323±160h×μg/L 和 863±388h×μg/L。XN 的平均半衰期为 60mg 剂量的 20h 和 180mg 剂量的 18h。
XN 具有明显的双相吸收模式，XN 和 IX 缀合物是主要的循环代谢物。
