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Identification, quantitation and biological activity of phytoestrogens in a dietary supplement for breast enhancement
Authors:N G Coldham  M J Sauer
Institution:Department of Risk Research, Veterinary Laboratories Agency, Addlestone, KT15 3NB, Surrey, UK. n.g.coldham@via.maff.gsi.gov.uk
Abstract:A hop-based dietary supplement, marketed for natural breast enhancement, was analysed to determine the identity and biological activity of active constituents and potential biological effects in man. Extracts of the dietary supplement were analysed by LC-MS(n) and phytoestrogens identified and quantitated by reference to appropriate standards. Only hop-associated phytoestrogens were found in the dietary supplement at significant concentrations as follows (mean+/-1 S.D.); 8-prenylnaringenin 10.9+/-0.3, 6-prenylnaringenin 27.4+/-1.2, 6,8-diprenylnaringenin 0.9+/-0.1, xanthohumol 321+/-17 and isoxanthohumol 81.1+/-1.6 microg/g of dietary supplement. The oestrogenic activity of extracts in an ERalpha reporter gene assay was equivalent to 48+/-6.3 ng 17beta-oestradiol/g supplement and consistent with the 8-prenylnaringenin content. The dietary supplement extract also inhibited reductive 17beta-hydroxysteroid oxidoreductase activity, but to a greater extent than a concentration matched reference mixture of hop phytoestrogens. However, the supplement was only weakly active in mouse uterotrophic assays following administration in feed or after subcutaneous injection of extract at doses of 8-PN up to 250 times higher than that recommended for women. These preliminary findings suggest that the dietary supplement is unlikely to produce oestrogenic effects in vivo at the level of the uterus; supporting evidence is still required to demonstrate efficacy.
Keywords:Hops  Phytoestrogens  Breast enhancement  Oestrogen receptor  17β-Hydroxysteroid oxidoreductase  Uterotrophicanhydrosecoisolariciresinol  3  4-bis[(3-methoxy-4-hydroxy-phenyl)methyl] tetrahydrofuran  coumestrol  7  12-dihydroxycoumestan  daidzein  7  4′-dihydroxyisoflavone  daidzin  7-O-glucosyl-4′-hydroxyisoflavone  6  8-diprenylnaringenin  5  7  4′-trihydroxy-6  8-diprenylflavanone  17β-oestradiol  1  3  5-estratriene-3  17β-diol  17α-ethynyloestradiol  17α-ethynyl 1  3  5-estratriene-3  17β-diol  genistein  5  7  4′-trihydroxyisoflavone  genistin  7-O-glucosyl-5  4′-dihydroxyisoflavone  glycitein  7  4′-dihydroxy-6-methoxyisoflavone  isoxanthohumol  7  4′-dihydroxy-5-methoxy-prenylflavanone  matairesinol  dihydro-3  4-bis[(4-hydroxy-3-methoxyphenyl)-methyl]-2-furanone  naringenin  5  7  4′-trihydroxyflavanone  naringin  naringenin-7-rhamnoglucoside  8-prenylnaringenin  5  7  4′-trihydroxy-8-prenylflavanone  6-prenylnaringenin  5  7  4′-trihydroxy-6-prenylflavanone  secoisolariciresinol  2  3-bis[4-hydroxy-3-methoxyphenyl)methyl]-1  4-butanediol  xanthohumol  2′  4′  4-trihydroxy-6′-methoxy-3′-prenylchalcone
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