title: Disposition of hop prenylflavonoids in human breast tissue.
abstract: Hop-derived products may contain xanthohumol (XN), isoxanthohumol (IX), and the potent phytoestrogen 8-prenylnaringenin (8-PN). To evaluate the potential health effects of these prenylflavonoids on breast tissue, their concentration, nature of metabolites, and biodistribution were assessed and compared with 17beta-estradiol (E(2)) exposure. In this dietary intervention study, women were randomly allocated to hop (n=11; 2.04 mg XN, 1.20 mg IX, and 0.1 mg 8-PN per supplement) or control (n=10). After a run-in of >or=4 days, three supplements were taken daily for 5 days preceding an aesthetic breast reduction. Blood and breast biopsies were analyzed using HPLC-ESI-MS/MS. Upon hop administration, XN and IX concentrations ranged between 0.72 and 17.65 nmol/L and 3.30 and 31.50 nmol/L, and between 0.26 and 5.14 pmol/g and 1.16 and 83.67 pmol/g in hydrolyzed serum and breast tissue, respectively. 8-PN however, was only detected in samples of moderate and strong 8-PN producers (0.43-7.06 nmol/L and 0.78-4.83 pmol/g). Phase I metabolism appeared to be minor (approximately 10%), whereas extensive glucuronidation was observed (> 90%). Total prenylflavonoids showed a breast adipose/glandular tissue distribution of 38/62 and their derived E(2)-equivalents were negligible compared with E(2) in adipose (384.6+/-118.8 fmol/g, p=0.009) and glandular (241.6+/-93.1 fmol/g, p<0.001) tissue, respectively. Consequently, low doses of prenylflavonoids are unlikely to elicit estrogenic responses in breast tissue.
authors.affiliation: Laboratory of Microbial Ecology and Technology (LabMET), Faculty of Bioscience Engineering, Ghent University-UGent, Belgium.
authors.forename: Selin
authors.initials: S
authors.lastname: Bolca
authors.forename: Jinghu
authors.initials: J
authors.lastname: Li
authors.forename: Dejan
authors.initials: D
authors.lastname: Nikolic
authors.forename: Nathalie
authors.initials: N
authors.lastname: Roche
authors.forename: Phillip
authors.initials: P
authors.lastname: Blondeel
authors.forename: Sam
authors.initials: S
authors.lastname: Possemiers
authors.forename: Denis
authors.initials: D
authors.lastname: De Keukeleire
authors.forename: Marc
authors.initials: M
authors.lastname: Bracke
authors.forename: Arne
authors.initials: A
authors.lastname: Heyerick
authors.forename: Richard B
authors.initials: RB
authors.lastname: van Breemen
authors.forename: Herman
authors.initials: H
authors.lastname: Depypere
mesh_terms: D052436:Adipose Tissue, White / Q000378:metabolism*; D000293:Adolescent; D000328:Adult; D001711:Biotransformation; D001940:Breast; D002851:Chromatography, High Pressure Liquid; D019587:Dietary Supplements; D005260:Female; D044950:Flavanones / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000378:metabolism*; D005419:Flavonoids / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000378:metabolism*; D035264:Flowers / Q000737:chemistry; D006801:Humans; D027582:Humulus / Q000737:chemistry*; D042361:Mammary Glands, Human / Q000378:metabolism*; D008875:Middle Aged; D048789:Phytoestrogens / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000378:metabolism; D011427:Propiophenones / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000378:metabolism*; D021241:Spectrometry, Mass, Electrospray Ionization; D053719:Tandem Mass Spectrometry; D044004:Xanthones / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000378:metabolism*; D055815:Young Adult
chemical_list: C119737:8-prenylnaringenin; D044950:Flavanones; D005419:Flavonoids; D048789:Phytoestrogens; D011427:Propiophenones; D044004:Xanthones; C512910:isoxanthohumol; C104536:xanthohumol