Female sex hormone-like activity enhancer
Combining equol with bird's nest extract enhances estrogen activity, addressing the inadequacy of existing agents and offering a more effective treatment for hormone-related symptoms.
Patent Information
- Application Number
- JP2025197746
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-11-18
- Publication Date
- 2026-02-03
AI Technical Summary
Existing agents do not fully enhance the female hormone-like effects of equol, which is known to have estrogenic activity.
A combination of equol with bird's nest and/or its extract is used to enhance female hormone-like effects, with specific ratios and forms of bird's nest extract being preferred for optimal efficacy.
The combination significantly enhances estrogen activity, providing a more effective treatment for symptoms associated with decreased female hormones such as menopausal disorders and osteoporosis.
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Abstract
Description
[Technical Field]
[0001] The present invention relates to an agent that enhances female hormone-like activity. [Background technology]
[0002] Women's health is greatly influenced by two female hormones, estrogen (the follicle hormone) and progesterone (the luteinizing hormone), which are secreted by the ovaries. A deficiency of female hormones can cause symptoms such as menopausal disorders and osteoporosis. Hormone replacement therapy (HRT) is widely used as a treatment to alleviate these symptoms. However, because HRT artificially supplements large amounts of female hormones, while highly effective, it also places a heavy burden on the body and is extremely difficult to adjust dosage.
[0003] Therefore, in recent years, plant-derived isoflavones have been attracting attention as components that exert female hormone-like effects. Such female hormone-like effects are thought to be due to the similarity of the chemical structure of isoflavones to that of estrogen. In particular, equol, derived from isoflavones contained in soybeans, is known to have estrogenic activity (Non-Patent Documents 1 and 2). [Prior art documents] [Non-patent literature]
[0004] [Non-Patent Document 1] Sathyamoorthy, N. and Wang, TT, Eur. J. Cancer, 33, 2384-2389 (1997) [Non-patent document 2] Schmitt, E. et al., Toxicol. In Vitro, 15, 433-439 (2001) Summary of the Invention [Problem to be solved by the invention]
[0005] Although equol is known to have female hormone-like effects, agents that can enhance this effect have not been fully investigated. Therefore, an object of the present invention is to provide an agent that can enhance the female hormone-like effects of equol. [Means for solving the problem]
[0006] As a result of extensive research, the present inventors have discovered that combining bird's nest and / or an extract thereof, which is not known to be related to female hormone-like effects, with equol enhances the female hormone-like effects.The present invention was completed based on this finding and through further research.
[0007] That is, the present invention provides the following aspects. Item 1. A female hormone-like activity enhancer containing equol and bird's nest and / or its extract. Item 2. The female hormone-like activity enhancer according to Item 1, wherein the content of the bird's nest extract is 0.1 to 10 parts by weight per part by weight of the equol. Item 3. The female hormone-like activity enhancer according to Item 1 or 2, wherein the bird's nest extract is a water extract of a bird's nest hydrolysate. Item 4. The female hormone-like agent according to any one of Items 1 to 3, which enhances estrogen activity. [Effects of the Invention]
[0008] According to the present invention, an agent capable of enhancing the female hormone-like action of equol is provided. DETAILED DESCRIPTION OF THE INVENTION
[0009] The female hormone-like activity enhancer of the present invention is characterized by containing equol and bird's nest and / or an extract thereof. The female hormone-like activity enhancer of the present invention will be described in detail below.
[0010] Equol Equol is a substance produced by the metabolism of daidzein, a type of isoflavone, by intestinal bacteria and digestive enzymes in the body, specifically 7-hydroxy-3-(4'-hydroxyphenyl)-chroman. Equol is known to have female hormone-like activity.
[0011] Equol may be synthetic equol obtained by chemical reduction of daidzeins (daidzein glycoside, daidzein and / or dihydrodaidzein), or it may be a metabolite of equol-producing bacteria from raw materials containing daidzeins (daidzein glycoside, daidzein and / or dihydrodaidzein).
[0012] Raw materials containing daidzeins are not particularly limited and include, for example, plants (specifically, soybeans, kudzu, kudzu root, red globe, alfalfa, etc.), processed products thereof (specifically, soybean flour, boiled soybeans, tofu, fried tofu, soy milk, soybean hypocotyls, soybean hypocotyl extracts, etc.), and fermented preparations thereof (specifically, natto, soy sauce, miso, tempeh, fermented soybean drinks, etc.). Furthermore, equol-producing bacteria may be any microorganism that can assimilate daidzeins to produce equol, including, for example, microorganisms belonging to the genus Lactococcus, Streptococcus, and Bacteroides.
[0013] In the present invention, the equol to be blended may be a product obtained by fermenting and culturing a raw material containing daidzeins with an equol-producing bacterium, or the metabolite equol may be isolated and purified from the fermentation culture.
[0014] The content of equol in the female hormone-like activity enhancer of the present invention may be set depending on the content of other ingredients to be added, the form of the female hormone-like activity enhancer, the amount to be taken per serving, etc., but may be, for example, 0.01 to 70% by weight, preferably 0.05 to 60% by weight, more preferably 0.1 to 55% by weight, and even more preferably 0.1 to 50% by weight. When a fermentation culture is used to add equol in the present invention, the fermentation culture is used so that the equol content in the fermentation culture satisfies the above-mentioned equol content.
[0015] Bird's nest and / or its extract Bird's nest is known as the nest (bird's nest) of the Collocaliini genus, and can be used in the present invention in the form of bird's nest powder. Bird's nest extract is an extract of bird's nest, and contains N-acetylneuraminic acid, EGF (epidermal growth factor), etc., and is a known component known to have antiviral, antibacterial, antiallergic, hair growth promoting, etc. Among these bird's nests and their extracts, bird's nest extract is preferred from the viewpoint of enhancing the female hormone enhancing effect.
[0016] Examples of bird's nest extracts include bird's nest extracts, bird's nest hydrolyzate extracts, and bird's nest extract hydrolyzates. The solvent used for extraction is preferably water. Among these bird's nest extracts, from the viewpoint of enhancing the female hormone enhancing effect, the bird's nest hydrolyzate extract is preferably used, and the water extract of the bird's nest hydrolyzate is more preferably used.
[0017] The bird's nest extract may be a liquid extract obtained by concentrating the extract as necessary, or may be a dried extract powder obtained by drying the liquid extract. The method for drying the liquid extract is not particularly limited, and includes known methods such as spray drying, and a method in which a suitable adsorbent (e.g., silicic anhydride, starch, etc.) is added to a soft extract obtained by increasing the concentration of the liquid extract to obtain an adsorbed powder.
[0018] The bird's nest and its extract used in the present invention may be those obtained by the above-mentioned method, or commercially available products may be used. Commercially available bird's nest extracts include Bird's Nest Extract-P, Bird's Nest Extract-PC, and Bird's Nest Extract-LC (Oryza Oil & Fat Chemical Co., Ltd.), Horus Swiftlet Nest Extract (F) (Horus Co., Ltd.), and Bird's Nest Extract (DSP Gokyo Food & Chemical Co., Ltd.).
[0019] In the female hormone-like activity enhancer of the present invention, the ratio of the equol content to the total amount of bird's nest and its extract is not particularly limited, but the total amount of bird's nest and its extract per 1 part by weight of equol can be, for example, 0.1 to 30 parts by weight. Furthermore, the ratio of the equol content to the bird's nest extract content can be 0.1 to 10 parts by weight per 1 part by weight of equol. To further enhance the effect of enhancing female hormone-like activity, the content of the bird's nest extract per 1 part by weight of equol is preferably 0.5 to 8.5 parts by weight, more preferably 3 to 7 parts by weight, even more preferably 5 to 7 parts by weight, and even more preferably 6 to 7 parts by weight.
[0020] The total amount of bird's nest and its extract in the female hormone-like activity enhancer of the present invention may be set so that the ratio to the equol content falls within the above range, for example, 0.01 to 30% by weight.
[0021] In the present invention, when a liquid extract such as a liquid extract or soft extract is used in blending bird's nest extract, it is used so that the remaining amount after excluding the solvent contained in the liquid extract is the ratio and content of the bird's nest extract described above, and when a dry extract powder containing additives such as excipients or adsorbents is used in blending bird's nest extract, it is used so that the remaining amount after excluding the additives contained in the dry extract powder is the ratio and content of the bird's nest extract described above.
[0022] Other ingredients The female hormone-like activity enhancer of the present invention may contain, if necessary, other pharmacological ingredients in addition to the above-mentioned ingredients. The types of such pharmacological ingredients are not particularly limited, but examples include antacids, stomachics, digestives, intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedatives, hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal powders, herbal extracts, vitamins, and menthols. These pharmacological ingredients may be used alone or in combination of two or more. The content of these pharmacological ingredients may be appropriately determined from known ones depending on the type of pharmacological ingredient used.
[0023] The female hormone-like activity enhancer of the present invention may contain pharmaceutically acceptable bases and additives, as necessary, to prepare the desired dosage form. Examples of such bases and additives include excipients, binders, disintegrants, lubricants, isotonicity agents, plasticizers, dispersants, emulsifiers, solubilizers, wetting agents, stabilizers, suspending agents, adhesives, coating agents, glossing agents, water, oils and fats, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, UV protection agents, preservatives, flavoring agents, fragrances, powders, thickeners, pigments, and chelating agents. These bases and additives may be used alone or in combination of two or more. The content of these bases and additives may be appropriately determined from known bases and additives depending on the type of additive used, dosage form, and the like.
[0024] Dosage form The dosage form of the female hormone-like activity enhancer of the present invention is not particularly limited, and may be any of tablets, granules, powders, pills, capsules, films, liquids (drinks), etc. Among these dosage forms, tablets, granules, and films are preferred from the viewpoint of ease of administration, etc. These dosage forms can be prepared using pharmaceutically acceptable bases and additives, and the types and amounts of the bases and additives are well known in the field of formulation technology.
[0025] Purpose The female hormone-like activity enhancer of the present invention is used for the purpose of enhancing female hormone-like activity, more specifically, for the purpose of enhancing physiological and pathophysiological actions expressed via female hormone receptors.
[0026] The female hormone-like activity enhancer of the present invention enhances the binding activity to estrogen receptors, and is therefore preferably used for the purpose of enhancing physiological and pathophysiological actions expressed via estrogen receptors.
[0027] More specifically, the female hormone-like activity enhancer of the present invention is used to prevent or improve symptoms caused by a decrease in female hormones, such as menopausal symptoms, menopausal disorders, osteoporosis, fluctuations in physical condition, menstrual pain, and a decrease in skin or hair quality (ability to retain collagen and / or elastin).
[0028] Therefore, the female hormone-like activity enhancer of the present invention is applicable to women with decreased female hormones, particularly women who are aware of symptoms caused by decreased female hormones. Specific examples of applicable subjects include women aged 40 or older, menopausal women, women with premature ovarian failure after oophorectomy or chemotherapy, women after hysterectomy, and elderly women.
[0029] Dosage / Usage The female hormone-like activity enhancer of the present invention is administered orally. The dosage of the female hormone-like activity enhancer of the present invention is appropriately determined depending on the degree of female hormone reduction, age, etc., but may be, for example, 0.1 to 100 mg, preferably 0.5 to 40 mg, more preferably 1.0 to 10 mg, even more preferably 1.5 to 5 mg, and particularly preferably 1.8 to 3 mg, in terms of daily equol intake.
[0030] Furthermore, there are no particular limitations on the timing of administration of the female hormone-like activity enhancer of the present invention, and it may be administered before meals, after meals, or between meals, but it is preferably administered before meals or between meals. [Example]
[0031] The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.
[0032] Test Example (S)-Equol (Fujifilm Wako Pure Chemical Industries, Ltd.) was prepared as equol, and Bird's Nest Extract-P (Oryza Oil & Fat Chemical Co., Ltd., a water extract of bird's nest hydrolysate, containing 80% by weight of dextrin and 20% by weight of bird's nest extract) was prepared as bird's nest extract.
[0033] Equol or bird's nest extract was dissolved in dimethyl sulfoxide to prepare a test sample solution.
[0034] The medium was prepared by adding 3% by weight of fetal bovine serum (FBS), 50 U / mL penicillin, and 50 mg / mL streptomycin to phenol red-free Dulbecco's modified Eagle's medium (liquid), and adding L-glutamine to a concentration of 0.5 mM. Ta.
[0035] MCF-7 cells (KAC Co., Ltd.) derived from human breast cancer were prepared. MCF-7 cells are cancer cells whose proliferation ability increases in an estrogen-dependent manner. It is used as a detection system for estrogenic activity.
[0036] 4 x 10 in medium 4 A suspension of MCF-7 cells adjusted to 50 cells / ml was seeded into each well of a 96-well plate at 50 μl / well. Next, dimethyl sulfoxide was added to each well at 0.1 μl / well, and the test sample solution was added so that the equol and / or bird's nest extract had the final concentrations shown in Table 1. The cells were then incubated at 37°C in the presence of CO2 for 72 hours. Cultivated.
[0037] After culturing, the absorbance at 450 nm (corresponding to the cell number) was measured using a cell proliferation / cytotoxicity assay kit (product name "Cell Counting kit-8", Dojindo Research Institute, Inc.). The measured absorbance at 450 nm was used to calculate the cell proliferation promotion rate according to the following calculation formula. The test was performed with n=4, and the average of the obtained cell proliferation promotion rates was used as the evaluation value for the female hormone-like effect. A cell proliferation promotion rate of more than 100% is considered to have a female hormone-like effect. In addition, a female hormone activity enhancement score was calculated according to the following calculation formula. A female hormone activity enhancement score of more than 1 is considered to exceed the additive effect of the female hormone-like effect when each component is used alone, that is, it is considered to have a significantly enhanced female hormone-like effect. The results are shown in Table 1.
[0038]
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[0039]
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[0040] [Table 1]
[0041] As shown in Comparative Examples 2 to 5, swallow's nest extract alone showed almost no female hormone-like effects, although some were observed to have female hormone-like effects depending on the concentration. In contrast, as shown in Examples 1 to 4, when equol was combined with swallow's nest extract, a significant female hormone-enhancing effect was observed.
Claims
1. A female hormone-like activity enhancer containing equol and swallow's nest and / or its extract.
2. 2. The female hormone-like activity enhancer according to claim 1, wherein the content of said bird's nest extract is 0.1 to 10 parts by weight per 1 part by weight of said equol.
3. 3. The female hormone-like activity enhancer according to claim 1, wherein the bird's nest extract is a water extract of a bird's nest hydrolysate.
4. The female hormone-like agent according to any one of claims 1 to 3, which enhances estrogen activity.