Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops

Leecole Legette, Chanida Karnpracha, Ralph L. Reed, Jaewoo Choi, Gerd Bobe, J. Mark Christensen, Rosita Rodriguez-Proteau, Jonathan Purnell, Jan F. Stevens

Research output: Contribution to journalArticle

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Abstract

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.

Original languageEnglish (US)
Pages (from-to)248-255
Number of pages8
JournalMolecular Nutrition and Food Research
Volume58
Issue number2
DOIs
StatePublished - Feb 2014

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hypoglycemic agents
Humulus
hops
Hypoglycemic Agents
Flavonoids
pharmacokinetics
flavonoids
Pharmacokinetics
dosage
metabolites
half life
xanthohumol
mouth
ingestion
blood
Area Under Curve
Half-Life
Eating

Keywords

  • Flavonoids
  • Hops
  • Human metabolism
  • Pharmacokinetics
  • Xanthohumol

ASJC Scopus subject areas

  • Food Science
  • Biotechnology

Cite this

Legette, L., Karnpracha, C., Reed, R. L., Choi, J., Bobe, G., Christensen, J. M., ... Stevens, J. F. (2014). Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops. Molecular Nutrition and Food Research, 58(2), 248-255. https://doi.org/10.1002/mnfr.201300333

Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops. / Legette, Leecole; Karnpracha, Chanida; Reed, Ralph L.; Choi, Jaewoo; Bobe, Gerd; Christensen, J. Mark; Rodriguez-Proteau, Rosita; Purnell, Jonathan; Stevens, Jan F.

In: Molecular Nutrition and Food Research, Vol. 58, No. 2, 02.2014, p. 248-255.

Research output: Contribution to journalArticle

Legette, L, Karnpracha, C, Reed, RL, Choi, J, Bobe, G, Christensen, JM, Rodriguez-Proteau, R, Purnell, J & Stevens, JF 2014, 'Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops', Molecular Nutrition and Food Research, vol. 58, no. 2, pp. 248-255. https://doi.org/10.1002/mnfr.201300333
Legette, Leecole ; Karnpracha, Chanida ; Reed, Ralph L. ; Choi, Jaewoo ; Bobe, Gerd ; Christensen, J. Mark ; Rodriguez-Proteau, Rosita ; Purnell, Jonathan ; Stevens, Jan F. / Human pharmacokinetics of xanthohumol, an antihyperglycemic flavonoid from hops. In: Molecular Nutrition and Food Research. 2014 ; Vol. 58, No. 2. pp. 248-255.
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abstract = "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.",
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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

AU - Stevens, Jan F.

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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.

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KW - Human metabolism

KW - Pharmacokinetics

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