WO2006035897A1 - 性ホルモン結合グロブリン阻害組成物 - Google Patents
性ホルモン結合グロブリン阻害組成物 Download PDFInfo
- Publication number
- WO2006035897A1 WO2006035897A1 PCT/JP2005/018012 JP2005018012W WO2006035897A1 WO 2006035897 A1 WO2006035897 A1 WO 2006035897A1 JP 2005018012 W JP2005018012 W JP 2005018012W WO 2006035897 A1 WO2006035897 A1 WO 2006035897A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition
- isoflavones
- composition according
- derived
- isoflavone
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic 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
- A61K31/352—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
- C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
- C07D311/34—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 3 only
- C07D311/36—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 3 only not hydrogenated in the hetero ring, e.g. isoflavones
Definitions
- Sex hormone binding globulin inhibitor composition
- the present invention relates to a sex hormone binding globulin inhibitor composition, and relates to a composition that can reduce or improve various symptoms based on the sex hormone binding globulin inhibitory effect.
- isoflavones have the effect of increasing the blood concentration of SHBG by stimulating the inhibition of competition with endogenous estrogens and the production of sex hormone-binding globulin (hereinafter referred to as "SHBG"). Is considered to have. And it has been confirmed in cell tests that genistein stimulates the production of SHBG (Non-patent Document 2). That is, by isoflavones promoting the production of SHBG, it was thought that increased SHBG binds to and controls endogenous estrogens and improves the above symptoms. However, no evidence has been obtained for the above-mentioned mechanism of action, which has never been demonstrated in clinical trials.
- Non-Patent Document 1 New Food Ind., Vol.40, No.8, 9-14, 1998.
- Non-Patent Document 2 Steroids, vol.58, July, 301-304, 1993.
- the problem of the present invention is that it is derived from natural products and has high safety even when added to foods. It is an object of the present invention to provide a composition that finds a common use and uses this to improve various symptoms.
- the present inventors have conducted intensive research on the effect of human intake of isoflavones, which are abundant in leguminous plants such as soybeans and clover, on blood hormones and the like. It was found that it inhibits SHBG, which was previously thought to increase in blood levels by isoflavone intake, and promotes the secretion of estradiol, one of the endogenous hormones, through this action. As a result of further research, it was found that among the isoflavones, the active ingredient that exhibits a particularly remarkable effect is a daidzein group that contains a large amount of hypocotyl of soybean.
- the present invention relates to
- a sex hormone-binding globulin inhibitor composition containing isoflavones as active ingredients containing isoflavones as active ingredients.
- composition according to 1 above, wherein the source of the active ingredient is a plant-derived isoflavone-containing material.
- composition according to 4 above, wherein the plant-derived isoflavone-containing material is derived from soybean hypocotyls.
- composition according to 5 above, wherein the plant-derived isoflavone-containing material is an extract derived from soybean hypocotyl or a purified product thereof.
- composition according to 1 above wherein the composition is a food or agent.
- composition according to 1 above which is a food or pharmaceutical product with a health label based on a sex hormone binding globulin inhibitory action.
- composition of the present invention makes it possible to inhibit blood SHBG, thereby suppressing an increase in blood SHBG concentration associated with aging, estradiol into blood, etc. Can promote the secretion of endogenous hormones. It is possible to provide a composition that can be expected to have various effects based on such effects, such as reduction of climacteric symptoms, prevention of osteoporosis, improvement of lipid metabolism, improvement of brain function, etc. Can contribute.
- the sex hormone binding globulin inhibitor composition of the present invention is characterized by containing isoflavones as active ingredients.
- the isoflavones of the present invention are abundant in plants such as soybeans, red clovers, and duckweeds, and are classified according to their structures.
- daidzein groups with daidzein as the aglycone skeleton (daidzein as the aglycone body, daidzin with glucose ⁇ -bonded to the aglycone skeleton, malonyldidine with a functional group bonded to the glucose part of daidzin, 'acetylidin' and succinyl daidin)
- Genicing noreps with glycine skeletons (genistin, genistin, maloninoregenistin, acechinoregenistin, succinylgenistine, etc.) Chin, succininoreglicitin, etc.), biocanin lees, formononetin and the like. It also includes etaol, a metabolite of the daidzin group,
- a purified pure product may be used, and a plant-derived isoflavone-containing material prepared as a raw material for plants such as soybeans, black soybeans, duckweeds, and clovers may be used as a supply source. You can also.
- a plant-derived isoflavone-containing substance an ingredient having a Daisying Nolepe / Genistin group weight ratio of 2 or more is more preferable in order to exert the effect of the active ingredient more. Specifically, the content derived from soybean hypocotyl in soybean is mentioned.
- the preparation method from the legume plant is not particularly limited, but for example, using a method of pulverizing the legume plant, an organic solvent such as water or ethanol, acetone, or a mixture thereof.
- An extraction method, a method of purifying the extract with an adsorption resin, an ion exchange resin, or the like, or a method of purification by liquid-liquid distribution with an organic solvent can be used.
- processing for imparting various characteristics to the active ingredient of the present invention is free.
- an active ingredient may be included by cyclodextrin, or a soluble saccharide such as glucose may be bound to the active ingredient.
- j3-Dalcosidase may be allowed to act to fully aglyconize the active ingredient, and fermentation using straw, yeast, lactic acid bacteria, Bacillus natto, etc. may be performed for such enzymatic reaction.
- the content of the active ingredient in the composition of the present invention varies depending on the form and amount of the composition and can be appropriately set. In general, a person skilled in the art may set the content of the composition in consideration of the intake of the composition per day so that the intake of the active ingredient per day can be taken. For example, if the daily intake of the active ingredient is set to lOmg, and the daily intake of the composition is lOOg, the content of the active ingredient in the composition is 0.01% by weight. Just do it.
- the composition of the present invention includes proteins, lipids, carbohydrates, dietary fibers, oligosaccharides, amino acids, peptides, minerals, vitamins, catechins, yew leaves, anthocyanins, gerberas, depending on the purpose.
- Useful components derived from animals and plants such as L-carnitine, ⁇ -lipoic acid, soybean saponin and other saponins, useful components derived from microorganisms such as yeast extract, polyglutamic acid, natto and lactic acid bacteria, or Coenzyme Q10 It is possible to use raw materials rich in coenzymes and enzymes.
- the composition of the present invention refers to a food or agent, and in the case of an agent, it can be prepared in various dosage forms. That is, in the case of oral administration, it can be administered in the form of solid preparations such as tablets, hard capsules, soft capsules, granules or pills, or liquids such as solutions, emulsions or suspensions. In the case of parenteral administration, it is administered in the form of injection solution or suppository.
- additives that are acceptable for formulation such as excipients, stabilizers, preservatives, wetting agents, emulsifiers, lubricants, sweeteners, coloring agents, fragrances, tonicity adjustments. It can be made into a preparation by using a preparation, buffer, antioxidant, pH adjuster and the like together.
- composition of the present invention is a food, soft drinks, dairy products, soy milk, fermented soy milk, soy protein drinks, tofu, natto, fried chicken, fried chicken, cancer return, which are general food forms Hamba It can be added to various foods such as candy, meatballs, fried chicken, nuggets, various prepared dishes, baked goods, cereals, rice cakes, gums and other confectionery, tablets, breads and cooked rice. Furthermore, since the content of active ingredients (isoflavones) in foods can be easily measured, it is used as an active ingredient (involved ingredient) in food packaging, pamphlets, etc. for various effects resulting from sex hormone binding globulin inhibition. It can also be used for health foods (special health foods, etc.) that describe their effects.
- Sex hormone-binding globulin inhibitor obtained ⁇ Effective intake of food is intended for use 'Use target ⁇ Depending on form, humans can usually ingest about 10 to 500mg of active ingredient per day Adjust it once or several times. From the viewpoint of safety, the intake of more than the proper amount of many pharmaceuticals may cause safety problems, whereas the effective component of the present invention can use natural plant-derived contents. The upper limit of intake is almost never a problem.
- isoflavone-containing material was prepared from soybean hypocotyl as follows. That is, the soybean hypocotyl was heated to dry heat, unnecessary polysaccharides were removed by water immersion, and a soybean hypocotyl extract was obtained by hot water extraction. This was powdered with a spray dryer to obtain an isoflavone-containing material. The resulting isoflavone-containing material had a daizing loop / genistin group ratio of 3.8. The total content of daidzein group and genistein group was 5.3% per dry weight of the contents. The total isoflavone content for the Daricity group was 8.3%.
- Test tablets were prepared using the isoflavone-containing material.
- An isoflavone-containing material per lg of total raw material was mixed with lactose so that the total amount of isoflavone aglycone was 7 mg, and then tableted to give 0-285 g per tablet to prepare a test tablet.
- This tablet is Assuming an intake of 20 tablets on day Z, the amount of isoflavone aglycone per day was 40 mg, and the total amount of isoflavone was 68 mg.
- a placebo tablet used as a control was prepared by replacing the isoflavone-containing material of Example 1 with lactose.
- the subjects were 45 menopausal women and 13 menopausal women.
- the tablet of the present invention (IF tablet) obtained in Example 1 (40 mg as the amount of isoflavone aglycone per day)
- An intervention study was conducted using an isoflavone aglycone amount of 27 mg) and a placebo tablet obtained in Comparative Example 1.
- the test was conducted in a double blind crossover test in which IF tablets and placebo tablets were taken for 4 weeks each. Before intervention (baseline), 4 weeks, and 8 weeks later, menopausal symptoms were measured, urinalysis and blood samples were taken. They also recorded the intake of pills. Blood collected during the baseline, IF and placebo tablets was used to measure hormone levels.
- Hormones were measured by Flouoroimmunometric Assay using DELIFIA for estradiol, progesterone, luteinizing hormone, follicle stimulating hormone, prolatatin, and SHBG. Use 7 simplified menopausal index (ivll) as an index of climacteric symptoms.
- isoflavones are active ingredients for blood SHBG inhibition and promotion of estradiol secretion. This also indicates that among the isoflavones, the isoflavone of the daidzein group is an active ingredient.
- FIG. 1 is a graph showing the effect of improving menopausal symptoms by taking IF tablets.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Botany (AREA)
- Mycology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Nutrition Science (AREA)
- Polymers & Plastics (AREA)
- Obesity (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Neurology (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Food Science & Technology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/664,387 US20080161385A1 (en) | 2004-09-30 | 2005-09-29 | Composition Inhibiting Sex Hormone-Binding Globulin |
| JP2006537819A JPWO2006035897A1 (ja) | 2004-09-30 | 2005-09-29 | 性ホルモン結合グロブリン阻害組成物 |
| US12/845,008 US20110046214A1 (en) | 2004-09-30 | 2010-07-28 | Composition inhibiting sex hormone-binding globulin |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2004286784 | 2004-09-30 | ||
| JP2004-286784 | 2004-09-30 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US12/845,008 Division US20110046214A1 (en) | 2004-09-30 | 2010-07-28 | Composition inhibiting sex hormone-binding globulin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2006035897A1 true WO2006035897A1 (ja) | 2006-04-06 |
Family
ID=36119043
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/JP2005/018012 Ceased WO2006035897A1 (ja) | 2004-09-30 | 2005-09-29 | 性ホルモン結合グロブリン阻害組成物 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20080161385A1 (ja) |
| JP (1) | JPWO2006035897A1 (ja) |
| CN (1) | CN101031292A (ja) |
| WO (1) | WO2006035897A1 (ja) |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07506822A (ja) * | 1992-05-19 | 1995-07-27 | ノボゲン リサーチ ピーティーワイ リミッテッド | フィト−エストロゲン,類似体またはその代謝産物を含有する健康補助剤 |
| JPH11332512A (ja) * | 1998-05-29 | 1999-12-07 | Fuji Oil Co Ltd | 大豆胚軸加工品を含有する食品 |
| JP2000014348A (ja) * | 1998-04-28 | 2000-01-18 | Fuji Oil Co Ltd | 大豆胚軸加工品及びその製造法 |
| JP2001523258A (ja) * | 1997-05-01 | 2001-11-20 | ノボゲン インコーポレイテッド | 更年期症状および骨粗鬆症の治療または予防 |
| WO2003077904A1 (en) * | 2002-03-15 | 2003-09-25 | Nichimo Co., Ltd. | Biological activity-promoting compositions containing soybean germ-origin isoflavone aglycon |
| JP2005041803A (ja) * | 2003-07-25 | 2005-02-17 | Nichimo Co Ltd | 閉経症候群緩和素材 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1309716C (zh) * | 2001-06-21 | 2007-04-11 | 不二制油株式会社 | 含有可溶性异黄酮组成物的制造方法 |
| JP4442422B2 (ja) * | 2002-12-24 | 2010-03-31 | 不二製油株式会社 | 高濃度かつ高溶解性のイソフラボン含有組成物及びその製造法 |
| JP4826740B2 (ja) * | 2003-07-02 | 2011-11-30 | 不二製油株式会社 | フラボノイドの可溶化剤及び可溶化方法 |
-
2005
- 2005-09-29 WO PCT/JP2005/018012 patent/WO2006035897A1/ja not_active Ceased
- 2005-09-29 JP JP2006537819A patent/JPWO2006035897A1/ja active Pending
- 2005-09-29 US US11/664,387 patent/US20080161385A1/en not_active Abandoned
- 2005-09-29 CN CNA2005800331361A patent/CN101031292A/zh active Pending
-
2010
- 2010-07-28 US US12/845,008 patent/US20110046214A1/en not_active Abandoned
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07506822A (ja) * | 1992-05-19 | 1995-07-27 | ノボゲン リサーチ ピーティーワイ リミッテッド | フィト−エストロゲン,類似体またはその代謝産物を含有する健康補助剤 |
| JP2001523258A (ja) * | 1997-05-01 | 2001-11-20 | ノボゲン インコーポレイテッド | 更年期症状および骨粗鬆症の治療または予防 |
| JP2000014348A (ja) * | 1998-04-28 | 2000-01-18 | Fuji Oil Co Ltd | 大豆胚軸加工品及びその製造法 |
| JPH11332512A (ja) * | 1998-05-29 | 1999-12-07 | Fuji Oil Co Ltd | 大豆胚軸加工品を含有する食品 |
| WO2003077904A1 (en) * | 2002-03-15 | 2003-09-25 | Nichimo Co., Ltd. | Biological activity-promoting compositions containing soybean germ-origin isoflavone aglycon |
| JP2005041803A (ja) * | 2003-07-25 | 2005-02-17 | Nichimo Co Ltd | 閉経症候群緩和素材 |
Non-Patent Citations (3)
| Title |
|---|
| ADLERCREUTZ H. ET AL.: "Dietary phytoestrogens and cancer: in vitro and in vivo studies", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 41, no. 3-8, 1992, pages 331 - 337, XP009028783 * |
| NAGATA C. ET AL.: "Soy product intake and serum isoflavonoid and estradiol concentrations in relation to bone mineral density in postmenopausal Japanese women", OSTEOPOROSIS INTERNATIONAL, vol. 13, no. 3, 2002, pages 200 - 204, XP003000494 * |
| TAKAMATSU S.: "Daizu no Kodo Riyo toshiteno Daizu Isoflavon no Kino to Shokuhin eno Riyo", NEW FOOD INDUSTRY, vol. 140, no. 8, 1998, pages 9 - 14, XP003000493 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20080161385A1 (en) | 2008-07-03 |
| JPWO2006035897A1 (ja) | 2008-05-15 |
| US20110046214A1 (en) | 2011-02-24 |
| CN101031292A (zh) | 2007-09-05 |
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