TY - JOUR
T1 - Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops
AU - Legette, Leecole
AU - Karnpracha, Chanida
AU - Reed, Ralph L.
AU - Choi, Jaewoo
AU - Bobe, Gerd
AU - Christensen, J. Mark
AU - Rodriguez-Proteau, Rosita
AU - Purnell, Jonathan Q.
AU - Stevens, Jan F.
PY - 2014/2
Y1 - 2014/2
N2 - Scope: 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. Methods and results: 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 (Cmax) 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 (AUC0→∞) 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. Conclusion: XN has a distinct biphasic absorption pattern with XN and IX conjugates being the major circulating metabolites.
AB - Scope: 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. Methods and results: 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 (Cmax) 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 (AUC0→∞) 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. Conclusion: XN has a distinct biphasic absorption pattern with XN and IX conjugates being the major circulating metabolites.
KW - Flavonoids
KW - Hops
KW - Human metabolism
KW - Pharmacokinetics
KW - Xanthohumol
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U2 - 10.1002/mnfr.201300333
DO - 10.1002/mnfr.201300333
M3 - Article
C2 - 24038952
AN - SCOPUS:84893397732
SN - 1613-4125
VL - 58
SP - 248
EP - 255
JO - Molecular Nutrition and Food Research
JF - Molecular Nutrition and Food Research
IS - 2
ER -