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Scientific Name:
Humulus lupulus
Family Name:
Common Name:
hop, hops
Evidence of Activity
Pharmacokinetics (ADME)
A study presents a validation report for a method of quantitative xanthohumol determination in rat plasma, with the reported percentage recovery greater than 95%. Harish 2022
A study presents a synthetic approach to obtaining reference standards for the identification of human xanthohumol metabolites, matching them to a human blood sample obtained following consumption of xanthohumol. Buckett 2022
A study presents the data on the pharmacokinetics and tissue distribution (including liver, muscles, lungs, pancreas, kidneys, heart, spleen, and brain) of 8-prenylnaringenin following 22-day administration, in mice, as well as the binding affinity to human serum albumin and cellular uptake, as compared to naringenin. Tanaka 2022
A pharmacokinetic study identified 6 major metabolites of xanthohumol, isoxanthohumol being the major one, with rapid absorption, metabolism, and elimination following oral administration, in rats. Bai 2021
An in-vitro/in-vivo (mouse) study reports on the phase I and II metabolites of α- and β- bitter acids from hops (Humulus lupulus), including oxidized metabolites of humulones, glucuronide conjugates, and glucuronide derivatives of oxidized phase I metabolites. Salviati 2021
A pharmacokinetic study characterized metabolic transformations of 8-prenylnaringenin, found in hops, by human liver microsomes and 11 recombinant human UDP-glucuronosyltransferases. Fang 2019
Several microbial metabolites of isoxanthohumol, a major hop prenylflavanone, were discovered. Kim 2019
Eubacterium ramulus (an intestinal bacterium) converted xanthohumol to α,β-dihydroxanthohumol and metabolized 8-prenylnaringenin to two related chalcones, in vitro. Paraiso 2018
Prenylation was found to enhance muscular accumulation of 8-prenyl naringenin, as compared with naringenin, in mice, resulting in potential benefits in prevention of disuse muscle atrophy. Mukai 2018
Urinary humulinone and 2,3-dihydroxy-3-methylvaleric acid were shown to be potential biomarkers of beer consumption in human subjects. Urinary stearoylcarnitine concentrations decreased after beer consumption, indicating increased rates of fat oxidation. Quifer-Rada 2017
The sum of iso-α-acids and tricyclohumols was selected as one of the compliance biomarkers of beer intake, to boost investigation into health effects of beer. Gürdeniz 2016
One hundred phase I glucuronyl and sulfate metabolites of eleven prenylated flavonoids and isoflavonoids from hop and licorice were identified, using pork liver preparations, in vitro. Van de Schans 2015
Enantiospecific pharmacokinetics of isoxanthohumol, including its metabolite 8-prenylnaringenin, was studied in the rat. Martinez 2015
Iso-α-acids were detected in blood, serum, vitreous humor, and urine of human subjects postmortem. Rodda 2015
Pharmacokinetics of hop-derived iso-α-acids after the consumption of beer is studied. Rodda 2014
The pharmacokinetics of hop prenylflavanoids was studied in menopausal women with a standardized hop extract. Apart from those findings, the administration of the extract caused no acute toxicity. van Breemen 2014
Volatile compounds from hops (sesquiterpenes and β-myrcene) showed almost complete bioavailability in the intestinal epithelial Caco-2 cells in vitro, while the α,β-unsaturated alcohols likely undergo first-pass metabolism. Heinlein 2014
Enantiospecific resolution of 8-prenylnaringenin, a prenylflavonoid from hops, was achieved in rat serum and urine by a novel and simple liquid chromatographic-electrospray ionization-mass spectrometry method. Martinez 2014
The pharmacokinetics of xanthohumol is investigated in human subjects. Legette 2014
The metabolites of hop-derived α-, β-, and iso-α- bitter acids were identified. The most important metabolites of α-acids were identified as humulinones and hulupones. Iso-α-acids were found to be primarly metabolized into cis- and trans-humulinic acids, next to oxidized alloiso-α-acids. Cattoor 2013
The pharmacokinetics of 8-prenylnaringenin was mimicked in a microbe. Bartmańska 2013
This article reports on the validation of a novel UHPLC-MS/MS method for the detection of hop-derived beer ingredients in blood. Rodda 2013
The pharmacokinetics of xanthohumol in rats is studied. Legette 2012
The uptake of xanthohumol into cells in vitro is inhibited by high concentration of fetal bovine serum. Motyl 2012
Biotransformation of hop oil compounds was assessed in an in vitro digestion model. The results of this study show that gastrointestinal processes can modulate the chemical composition of ingested aroma constituents and might even influence the bioactivity of essential oils. Heinlein 2012
Bioavailability of hop-derived iso-α-acids and reduced derivatives was determined in New Zealand white rabbits and Caco-2 cell monolayers. Cattoor 2011
The uptake and intracellular kinetics of xanthohumol in hepatocytes, hepatic stellate cells, and intestinal cells were studied. Wolff 2011
This article reports on the analysis of polyphenolic compounds from hop and their phase I and II metabolites in rat in vivo. Jirásko 2010
Hop alpha-acids are absorbed with significantly higher efficiency by Caco-2 cell monolayers than beta-acids. Cattoor 2010
Xanthohumol undergoes partial metabolism by human gut microbiota. Hanske 2010
Hop prenylflavonoids localize to the breast tissue, but their concentration is negligible compared with that of 17beta-estradiol (E2) to elicit an estrogenic effect. Bolca 2010
Microbial metabolites of 8-prenylnaringenin were identified. Kim 2008
A probiotic intestinal bacteria Eubacterium limosum converts isoxanthohumol to the potent phytoestrogen 8-prenylnaringenin and co-administration in rats normalized the differences in conversion rates between different rats. Possemiers 2008
Variations in 8-prenylnaringenin production from isoxanthohumol by intestinal bacteria was investigated in intestinal content samples from 100 individuals. Possemiers 2007
Isoxanthohumol conversion into 8-prenylnaringenin in 50 healthy post-menopausal Caucasian women was found to correlate positively with the isoxanthohumol:8-prenylnaringenin ratio, intestinal methane production, theobromine intake and negatively with alcohol intake and recent antibiotic therapy. Bolca 2007
Xanthohumol accumulated in the cytosol of human intestinal epithelial cells apparently bound to cytosolic proteins. Pang 2007
The pharmacokinetics of 8-prenylnaringenin was investigated in postmenopausal women. Rad 2006
8-Prenylnaringenin was absorbed by intestinal epithelial Caco-2 cells via passiva diffusion, with further formation of 4'-O-glucuronide, 7-O-sulfate, and 4'-O-sulfate by the cells, and both phase I and II metabolites by human hepatocytes, with 7-O-glucuronide being the most abundant of the latter. Nikolic 2006
In vitro experiments with the dynamic SHIME model showed that hop prenylflavonoids pass unaltered through the stomach and small intestine and that activation of isoxanthohumol into 8-prenylnaringenin (up to 80% conversion) occurs only in the distal colon. Possemiers 2006
Microbial metabolism of xanthohumol, a prenylated chalcone from hops, was investigated. Kim 2006
Conversion of isoxanthohumol to 8-prenylnaringenin and the their excretion was studied in men consuming various brands of beer. Schaefer 2005
Isoxanthohumol was converted into 8-prenylnaringenin by the intestinal microbiota, with different efficiency, depending on the individual; and Eubacterium limosum was identified to be capable of this conversion. Possemiers 2005
In vitro phase II metabolism of xanthohumol by human recombinant UDP-glucuronosyltransferases and sulfotransferases was studied. Ruefer 2005
The rate of isomerization of alpha acids to iso-alpha acids of hops was determined across a range of temperatures (90-130 degrees C) to characterize the rate at which iso-alpha acids are formed during kettle boiling. Malowicki 2005
Xanthohumol (XN) was measured by HPLC in rat plasma, urine, and fecal samples after oral or intravenous (iv) administration. Plasma levels of XN fell rapidly within 60 min after iv administration. XN and its metabolites were excreted mainly in the feces within 24 h of administration. Avula 2004
The in vitro metabolism of 8-prenylnaringenin, an estrogenic compound from hops, by human liver microsomes was investigated. Nikolic 2004
Bio-activation of isoxanthohumol, a hop compound, to the potently estrogenic 8-prenylnaringenin was studied in rat liver microsomes expressing the human estrogen receptor alpha. Coldham 2002
The biotransformation of Xanthohumol, the major prenylated flavonoid of the female inflorescences of the hop plant (Humulus lupulus) by rat liver microsomes was investigated. Yilmazer 2001
Glucuronidation of xanthohumol with the formation of its C-4' and C-4 monoglucuronides was observed in rat and human liver microsomes. Yilmazer 2001
Antagonistic effect of serum on bacteriostatic action of lupulone. [No abstract] Sacks 1951
History of Record
November 1999
MAJOR REVISION BY: Michael C. Tims, PhD. candidate
June 2001
March 2023