FR2893848A1 - Phytohormonal composition, useful as hormonal substitute to treat premenopausal, menopausal and androposal disorders, comprises a combination of lignan-rich plant extracts and chaste tree extract - Google Patents

Phytohormonal composition, useful as hormonal substitute to treat premenopausal, menopausal and androposal disorders, comprises a combination of lignan-rich plant extracts and chaste tree extract Download PDF

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FR2893848A1
FR2893848A1 FR0553611A FR0553611A FR2893848A1 FR 2893848 A1 FR2893848 A1 FR 2893848A1 FR 0553611 A FR0553611 A FR 0553611A FR 0553611 A FR0553611 A FR 0553611A FR 2893848 A1 FR2893848 A1 FR 2893848A1
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Jean Luc Charagnac
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Laboratoires Nutreov SAS
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PHYSCIENCE SOC PAR ACTIONS SIM
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    • AHUMAN NECESSITIES
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    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/07Retinol compounds, e.g. vitamin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415Pyridoxine, i.e. Vitamin B6
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • AHUMAN NECESSITIES
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    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/537Salvia (sage)
    • AHUMAN NECESSITIES
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    • A61K36/55Linaceae (Flax family), e.g. Linum
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Abstract

Phytohormonal composition (C1) comprises a combination of lignan-rich plant extracts and chaste tree i.e. Vitex agnus castusextract. ACTIVITY : Gynecological; Endocrine-Gen; Vasotropic. No biological data given. MECHANISM OF ACTION : None given.

Description

L'invention concerne une composition phytohormonale et son utilisationThe invention relates to a phytohormonal composition and its use

comme substitutif hormonal, comprenant une combinaison d'extraits de végétaux riches en lignanes ou en isoflavones et d'extrait de gattilier, et son utilisation pour le traitement des troubles de la préménopause et de la ménopause, ainsi que de l'andropause. Les troubles de la préménopause et de la ménopause, notamment bouffées de chaleur, sueurs nocturnes, fatigabilité, troubles de l'humeur et du sommeil, sont généralement traités par administration d'un substitut hormonal associant des estrogènes et des progestatifs mais l'administration de telles hormones peut entraîner des effets secondaires indésirables. Par ailleurs, l'andropause s'accompagne de certaines manifestations gênantes comme une augmentation de volume de la prostate entraînant des difficultés mictionnelles, une alopécie andogénique ou encore des problèmes d'érection. Il serait souhaitable de disposer d'un substitut hormonal présentant des effets secondaires moindres et de préférence très limités et ayant une efficacité réelle sur les troubles de la préménopause, de la ménopause et de l'andropause.  as a hormonal substitute, comprising a combination of plant extracts rich in lignans or isoflavones and chaste tree extract, and its use for the treatment of menopausal and menopausal disorders, as well as andropause. Premenopausal and menopausal disorders, including hot flushes, night sweats, fatigability, mood and sleep disorders, are generally treated by administering a hormone substitute combining estrogens and progestins, but the administration of such hormones can cause unwanted side effects. In addition, andropause is accompanied by some annoying manifestations such as an increase in the volume of the prostate causing difficulty micturition, alopecia andogenic or erection problems. It would be desirable to have a hormone substitute with lesser and preferably very limited side effects and with real efficacy on premenopausal, menopausal and andropause disorders.

Ceci est obtenu de façon surprenante par l'association d'extraits végétaux donnant une composition phytohormonale permettant de réaliser un traitement substitutif complet de la préménopause, de la ménopause et de l'andropause. L'invention fournit donc une composition phytohormonale comprenant une combinaison d'extraits de végétaux riches en lignanes ou en isoflavones et d'extrait de gattilier (Vitex agnus castus). De manière préférée, cette composition phytohormonale contient en outre un sel de magnésium et de la vitamine B6. De préférence encore, cette composition phytohormonale 30 colide 35 Les lignanes dont les métabolites enterolignanes) sont les phyto-est e -s pt ù t .. c trou-ver sous , lire ou pilée. Ils sont présents dans c s non fruits et l café. C rt 1 fines, en lier la grain la source Tans 1( qui en con , T 4.0 star,"•.r,l i r1111AF L ri rr9I . L , , , . , , 3 6,11 ma11519 (411%,,,, T.&%.,11 -• '= t du métabolisme des l'effet de la flore intestinale de l'organisme. Les entérolignanes peuvent exister sous forme d'oligoméres et de dimères, en tant qu'aglycones ou hétérosides. Les lignanes les plus connus sont le séco-isolaricï-résinol et le matairésinol. Ils sont métabolisés par la flore intestinale en entérodiol et entérolactone qui eux seuls répondent à la définition des phytoestrogénes. Ainsi, les essais portant sur l'activité estrogénique sont-ils faits ar- ès métabolisation des lignanes. Les formules développées de ces cornpc ont données ci s. 20 15 25 30 fruits secs qui en contiennent, en particulier la graine de soja qui est la source la plus employée. Leurs structures sont proches de celle de l'estradiol, un système plan qui inclut un noyau aromatiuqe substitué en para. Les isoflavones peuvent exister sous forme d'aglycones, mais le plus souvent dans les plantes elles se présentent à l'état de glycosides. Dans le tractus gastro-intestinal, la daidzéine est métabolisée en dihydrodaidzéine puis en équol, métabolite hautement estrogénique et la génistéine est métabolisée en dihydrogénistéine, puis en 6'-hydro 0-déméthyl Io angolensine, pour donner le p-éthyl phénol et le tri hydroxy-benzène. Le gattilier (Vitex agnus castus) est un arbuste originaire de Grèce et d'Italie, répandu dans les régions méditerranéennes. Les extraits sont obtenus à partir des baies séchées et contiennent deux flavonoides spécifiques à cette plante, la casticine et l'agnuside. On trouve dans le 15 commerce des extraits standardisés soit en casticine (rapport pondéral de l'extrait à la casticine de 6 à 12 :1) soit en agnuside (de 0,5 % à 6 % en poids d'agnuside dans l'extrait sec), qui se présentent sous forme de teintures, d'extraits liquides ou d'extraits secs. On connaît l'utilisation d'extrait de gattilier pour traiter 20 certains syndromes prémenstruels mais il n'a jusqu'à présent pas été préconisé pour traiter les troubles de la préménopause, de la ménopause et de l'andropause. On a maintenant trouvé de manière surprenante que l'association lignanes ou isoflavones/flavonoïdes du gattilier fournit un 25 subtitut phytohormonal complet traitant de manière efficace et sûre les troubles de la préménopause et de la ménopause. On a également trouvé de manière surprenante que l'association lignanes et flavonoïdes du gattilier pouvait constituer un substitut hormonal pour améliorer certaines manifestations de 30 l'a ,)IIO( tni toii-a- (,fai-i a.1-1 n.r%  This is surprisingly obtained by the combination of plant extracts giving a phytohormonal composition for performing a complete replacement treatment for premenopause, menopause and andropause. The invention thus provides a phytohormonal composition comprising a combination of plant extracts rich in lignans or isoflavones and chaste tree extract (Vitex agnus castus). Preferably, this phytohormonal composition further contains a magnesium salt and vitamin B6. More preferably, this phytohormonal 30 colide composition (lignans whose enterolignan metabolites) are phyto-is e -s pt-t .. c hole-ver under, read or crushed. They are present in these fruits and coffee. C tt 1 fines, bind the grain to the source Tans 1 (which in con t? The metabolism of the intestinal flora effect of the organism, enterolignans can exist in the form of oligomers and dimers, as aglycones or glycosides. The most well-known lignans are seco-isolarinic-resinol and matairésinol, which are metabolized by the intestinal flora to enterodiol and enterolactone, which alone meet the definition of phytoestrogens, so that the tests on estrogen activity are The developed formulas of these cornpcs have given dry fruits which contain them, in particular the soybean which is the most widely used source. estradiol, a flat system that includes a para-substituted aromatic ring. They may exist as aglycones, but most often in plants they occur as glycosides. In the gastrointestinal tract, daidzein is metabolized to dihydrodaidzein and then to equol, a highly estrogenic metabolite, and genistein is metabolized to dihydrogenistein and then to 6'-hydro-0-demethyl Io angolensin to give p-ethyl phenol and sorting. hydroxy benzene. Chaste tree (Vitex agnus castus) is a shrub native to Greece and Italy, widespread in the Mediterranean regions. The extracts are obtained from dried berries and contain two flavonoids specific to this plant, casticine and agnuside. Standardized extracts are commercially available either in casticin (weight ratio of the extract to casticin of 6 to 12: 1) or in agnuside (from 0.5% to 6% by weight of agnuside in the extract). dry), which are in the form of dyes, liquid extracts or dry extracts. The use of Chasteberry extract is known to treat some premenstrual syndromes but has not heretofore been advocated for the treatment of premenopausal, menopausal and andropause disorders. It has now surprisingly been found that the lignans or isoflavones / flavonoids combination of chaste tree provides a complete phytohormonal subtitut which effectively and safely addresses premenopausal and menopausal disorders. It has also surprisingly been found that the combination of lignans and flavonoids in the chaste tree can be a hormone substitute for improving certain manifestations of the disease. %

4 de 10 mg à 40 mg d'extrait de gattilier standardisé à 0,5 % - 6 % en poids d'agnuside ou standardisé à 6-12:1 de casticine (rapport pondéral extrait : casticine), de 25 mg à 100 mg d'extrait de sauge standardisé à 15 % en poids d'acide carnosique, de 100 . 300 mg d'Vi-sv-crelACUL, z, magnésium mg 111 • de 2 mg à 4 mg de vitamine B6, • de 50 mg à 100 mg de vitamine C, de 5 mg à 15 mg de sélénium, de 1 mg à 2 mg de vitamine A, de 5 mg à 15 mg de vitamine E. Elle fournit également une composition phytohormonale contenant en poids sec de 50 mg à 200 mg d'extrait de graines de soja contenant de 10 à 30 % en poids d'isoflanones, de 10 mg à 40 mg d'extrait de gattilier standardisé à 0,5 % - 6 % en poids d'agnusides ou standardisé à 6-12:1 de casticine (rapport pondéral extrait :casticine) de 25 mg à 100 mg d'extrait de sauge standardié à 15 % en poids d'acide carnosique, • de 100 mg à 300 mg d'oxyde de magnésium, • de 2 mg à 4 mg de vitamine B6, • de 50 mg à 100 mg de vitamine C, • de 5 mg à 15 mg de sélénium, • de 1 mg à 2 mg de vitamine A, • de 5 mg à 15 mg de vitamine E. De telles compositions sont, selon l'invention, utilisées comme substitutif hormonal dans le traitement des troubles de la préménopause, d- la ménopause et p opause. 35 être présentés séparément, en combinaison de deux ou plusieurs éléments ou dans une seule préparation posologique. 1. Exemple de composition lignagnes/flavonoïdes de gattilier (en poids sec) pour une dose quotidienne 5 105 mg d'extrait de graines de lin à 20 % en poids de lignanes exprimés en SDG (SecoisolarieirésinolDiGlucoside), 20 mg d'extrait de gattilier à 0,6 % de casticine, 50 mg d'extrait de sauge standardisé à 15 % en acide carnosique, 290 mg d'oxyde de magnésium, 3,18 mg de vitamine B6 à 82 % de produit actif, 87,00 mg de vitamine C à 90 % de produit actif, 10 mg de sélénite de sodium, 12 mg d'acétate de rétinol à 10 % de vitamine A, 32,00 mg de préparation de vitamine E contenant 37,00 % de produit actif, 2. Exemple de composition isoflavones/flavonoïdes de gattilier (en poids sec) pour une dose quotidienne 100 mg d'extrait de graines de soja à 20 % en poids d'isoflavo~ es, 20 mg d'extrait de gattilier à 0,6 % de casticine, 50 mg d'extrait de sauge standardisé à 15 % en acide carnosique, 290 mg d'oxyde de magnésium, 3,18 mg de vitamine B6 à 82 % de produit actif, 87,00 mg de vitamine C à 90 % de produit actif, 10 mg de sélénite de sodium, 12 mg d'acétate de rétinol à 10 % de vitamine A, 32,00 mg de préparation de vitamine E contenant 37,00 % de produit actif,  4 from 10 mg to 40 mg standardized 0.5% - 6% by weight agnuside or standardized 6-12: 1 casticin extract extract (extracted weight ratio: casticin), from 25 mg to 100 mg of sage extract standardized to 15% by weight of carnosic acid, of 100. 300 mg Vi-sv-crelACUL, z magnesium mg 111 • 2 mg to 4 mg vitamin B6, • 50 mg to 100 mg vitamin C, 5 mg to 15 mg selenium, 1 mg to 2 mg of vitamin A, from 5 mg to 15 mg of vitamin E. It also provides a phytohormonal composition containing in dry weight from 50 mg to 200 mg of soybean extract containing from 10 to 30% by weight of isoflanones , from 10 mg to 40 mg of chasteberry extract standardized to 0.5% - 6% by weight of agnusides or standardized to 6-12: 1 of casticin (extracted weight ratio: casticin) of 25 mg to 100 mg of sage extract standardized to 15% by weight of carnosic acid, • from 100 mg to 300 mg of magnesium oxide, • from 2 mg to 4 mg of vitamin B6, • from 50 mg to 100 mg of vitamin C, From 5 mg to 15 mg of selenium, from 1 mg to 2 mg of vitamin A, from 5 mg to 15 mg of vitamin E. Such compositions are, according to the invention, used as a hormonal substitute in the treatment of disorders of the meadow menopause, d- menopause and p opause. Be presented separately, in combination of two or more elements or in a single dosage preparation. 1. Example of lignain / flavonoid composition of Chasteberry (dry weight) for a daily dose 105 mg of linseed extract containing 20% by weight of lignans expressed in SDG (secoisolarieirésinolDiGlucoside), 20 mg of chaste tree extract 0.6% casticin, 50 mg standardized sage extract 15% carnosic acid, 290 mg magnesium oxide, 3.18 mg vitamin B6 82% active, 87.00 mg of vitamin C 90% active, 10 mg sodium selenite, 12 mg retinol acetate 10% vitamin A, 32.00 mg vitamin E preparation containing 37.00% active product, 2. Example of isoflavone / flavonoid composition of Chasteberry (dry weight) for a daily dose 100 mg of soybean extract with 20% by weight of isoflavo ~ es, 20 mg of chaste extract with 0.6% of casticin, 50 mg of standardized sage extract with 15% carnosic acid, 290 mg of magnesium oxide, 3.18 mg of vitamin B6 with 82% of active product, 8 7.00 mg vitamin C 90% active, 10 mg sodium selenite, 12 mg retinol acetate 10% vitamin A, 32.00 mg vitamin E preparation containing 37.00% of active product,

Claims (4)

REVENDICATIONS 1. Composition phytohormonale comprenant une combinaison d'extraits de végétaux riches en lignanes ou en isoflavones et d'extrait de gattilier (Vitez agnus castus).  1. Phytohormonal composition comprising a combination of plant extracts rich in lignans or isoflavones and chaste tree extract (Vitez agnus castus). 2. Composition phytohormonale selon la revendication 1, caractérisée en ce qu'elle contient en outre un sel de magnésium et de la vitamine B6.  2. phytohormonal composition according to claim 1, characterized in that it further contains a magnesium salt and vitamin B6. 3. Composition phytohormonale selon l'une ou l'autre des revendications 1 et 2, caractérisée en ce qu'elle contient un extrait de sauge.  3. phytohormonal composition according to either of claims 1 and 2, characterized in that it contains a sage extract. 4. Composition phytohormonale selon l'une quelconque des revendications 1 à 3, caractérisée en ce qu'elle contient un extrait de valériane, de passiflore et/ou de camomille. Composition phytohormonale selon l'une quelconque des revendications 1 à 4, caractérisé en ce qu'elle contient des agents anti-âge et anti-oxydants du type vitamines A, C et E et sélénium. 6. Composition phytohormonale selon la revendication 1, caractérisée en qu'elle contient, en poids sec, de 50 mg à 200 mg d'extrait de graines de lin contenant de 10 à 30 % en poids de lignanes, de 10 mg à 40 mg d'extrait de gattilier standardisé à 0,5 % - 6 % en poids d'agnuside ou standardisé à 6-12 :1 de casticine (rapport pondéral extrait : casticine), de 25 mg à 100 mg d'extrait de sauge standardisé à 15 % en poids d'acide camosique, • de 100 mg à 300 mg d'oxyde de magnésium, • de 2 mg à 4 mg de vitamine B6, • de 50 mg à 100 mg de vitamine C, • de 5 mct à rs mg de sélénium, da d ;4- A, 7 • 50 mg d'extrait de sauge standardisé à 15 % en acide carnosique, ^ 290 mg d'oxyde de magnésium, • 3,18 mg de vitamine B6 à 82 % de produit actif, • 87,00 mg de vitamine C à 90 % de produit actif, . 10 mg de sélénite de sodium, ^ 12 mg d'acétate de rétinol à 10 % de vitamine A, • 32,00 mg de préparation de vitamine E contenant 37,00 % de produit actif. 8. Composition selon la revendication 1, caractérisée en ce 10 qu'elle contient en poids sec : de 50 mg à 200 mg d'extrait de graines de soja contenant de 10 à 30 % en poids d'isoflanones, de 10 mg à 40 mg d'extrait de gattilier standardisé à 0,5 % - 6 % en poids d'agnusides ou standardisé à 6-12 :1 de casticine (rapport 15 pondéral extrait :casticine) de 25 mg à 100 mg d'extrait de sauge standardisé à 15 % en poids d'acide carnosique, de 100 mg à 300 mg d'oxyde de magnésium, ^ de 2 mg à 4 mg de vitamine B6, 20 . de 50 mg à 100 mg de vitamine C, ^ de 5 mg à 15 mg de sélénium, • de 1 mg à 2 mg de vitamine A, de 5 mg à 15 mg de vitamine E. 9. Composition selon la revendication 8, caractérisé en ce 25 qu'elle contient en poids : 100 mg d'extrait de graines de soja à 20 % en poids d'isoflavones, 20 mg d'extrait de gattilier à 0,6 % de casticine, 50 mg d'extrait de sauge standardisé à 15 % en acide carnosique, 290 mg d'oxyde de magnésium, 30 3,18 mg de vitamine B6 à 82 % de produit actif, 87,00 mg de vitamine C à 90 % de produit actif, mg de sélénite de sodium, 12 mg d'acétate de rétinol à 10 % de vitamine A, 32,00 mg de préparation de vitamine E contenant 37,00 % de produit 35 actif.10. Composition phytohormonale selon l'une quelconque des revendications 1 à 8, utilisée comme substitutif hormonal dans le traitement des troubles de la préménopause, de la ménopause et de andropause.  4. phytohormonal composition according to any one of claims 1 to 3, characterized in that it contains an extract of valerian, passionflower and / or chamomile. Phytohormonal composition according to any one of Claims 1 to 4, characterized in that it contains anti-aging and antioxidant agents of vitamin A, C and E and selenium type. 6. phytohormonal composition according to claim 1, characterized in that it contains, in dry weight, from 50 mg to 200 mg of flaxseed extract containing from 10 to 30% by weight of lignans, from 10 mg to 40 mg of chasteberry extract standardized to 0.5% - 6% by weight of agnuside or standardized to 6-12: 1 of casticin (extracted weight ratio: casticin), from 25 mg to 100 mg of sage extract standardized to 15% by weight of camosic acid, • from 100 mg to 300 mg of magnesium oxide, • from 2 mg to 4 mg of vitamin B6, • from 50 mg to 100 mg of vitamin C, • from 5 mct to rs mg selenium, da d; 4- A, 7 • 50 mg standardized sage extract 15% carnosic acid, 290 mg magnesium oxide, • 3.18 mg vitamin B6 82% product active, • 87.00 mg vitamin C at 90% active product,. 10 mg of sodium selenite, 12 mg of retinol acetate containing 10% of vitamin A, 32.00 mg of vitamin E preparation containing 37.00% of active product. 8. Composition according to claim 1, characterized in that it contains in dry weight: from 50 mg to 200 mg of soybean extract containing from 10 to 30% by weight of isoflanones, from 10 mg to 40 mg of chasteberry extract standardized to 0.5% - 6% by weight of agnusides or standardized to 6-12: 1 of casticin (extracted weight ratio: casticin) from 25 mg to 100 mg of standardized sage extract 15% by weight carnosic acid, 100 mg to 300 mg magnesium oxide, 2 mg to 4 mg vitamin B6, 20. from 50 mg to 100 mg of vitamin C, from 5 mg to 15 mg of selenium, from 1 mg to 2 mg of vitamin A, from 5 mg to 15 mg of vitamin E. Composition according to claim 8, characterized in that it contains by weight: 100 mg of soybean extract with 20% by weight of isoflavones, 20 mg of Chasteberry extract with 0.6% of casticine, 50 mg of sage extract standardized to 15% carnosic acid, 290 mg of magnesium oxide, 3.18 mg of vitamin B6 at 82% of active product, 87.00 mg of vitamin C at 90% of active product, mg of sodium selenite 12 mg retinol acetate 10% vitamin A, 32.00 mg vitamin E preparation containing 37.00% active product. Phytohormonal composition according to any one of claims 1 to 8, used as a hormonal substitute in the treatment of premenopausal disorders, menopause and andropause.
FR0553611A 2005-11-28 2005-11-28 PHYTOHORMONAL COMPOSITION AND ITS USE AS A HORMONAL SUBSTITUTE Expired - Fee Related FR2893848B1 (en)

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WO2002074321A1 (en) * 2001-03-21 2002-09-26 N.V. Nutricia Composition comprising cocoa and a dopamine d2 receptor agonist
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FR2940123A1 (en) * 2008-12-22 2010-06-25 Granions Lab Des Combination product, useful e.g. to treat hot flushes and sweats caused by menopause, comprises compound having direct estrogenic activity at the level of estrogen receptors and compound able to be converted into enterolactone in body

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