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Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops
Author(s) -
Legette LeeCole,
Karnpracha Chanida,
Reed Ralph L.,
Choi Jaewoo,
Bobe Gerd,
Christensen J. Mark,
RodriguezProteau Rosita,
Purnell Jonathan Q.,
Stevens Jan F.
Publication year - 2014
Publication title -
molecular nutrition and food research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.495
H-Index - 131
eISSN - 1613-4133
pISSN - 1613-4125
DOI - 10.1002/mnfr.201300333
Subject(s) - xanthohumol , pharmacokinetics , chemistry , flavonoid , ingestion , absorption (acoustics) , pharmacology , zoology , hop (telecommunications) , medicine , biochemistry , antioxidant , biology , computer network , physics , computer science , acoustics
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 (8 PN ), and 6‐prenylnaringenin (6 PN ) were measured by LC ‐ MS / MS . Xanthohumol ( XN ) and IX conjugates were dominant circulating flavonoids among all subjects. Levels of 8 PN and 6 PN 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. Conclusion XN has a distinct biphasic absorption pattern with XN and IX conjugates being the major circulating metabolites.