JP2008127374A - Estrogen-like composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an extract substance derived from a plant having an estrogen-similar effect. <P>SOLUTION: The estrogen-like composition comprises the extract substance extracted from a flower of the genus Rhodiola of the family Crassulaceae that effectively prevents and ameliorates diseases caused by estrogen deficiency and a fugitive complaint. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

  The present invention relates to an estrogen-like composition comprising an extract extracted from the genus Pleuroaceae. The present invention also relates to a pharmaceutical composition containing an estrogen-like composition that prevents and ameliorates diseases and unstable complaints associated with a decline (deficiency) in estrogen secretion.

  In today's rapidly aging society, people have a common desire to live their daily lives even after aging. In order to meet this desire, planning and development of anti-aging products in various fields, especially in the fields of pharmaceuticals, foods and cosmetics, have been performed remarkably. However, there are many health food products based only on tradition, and there are concerns about their safety in use. In addition, side effects of chemical synthetic drugs are a concern and it is essential to pay attention to their use. Accordingly, there is a demand for the development of a composition that can be used effectively and safely on animals.

  Estrogens are a kind of female hormone and a general term for substances that have estrus and similar effects. Although estrogen is secreted on a daily basis in both men and women, its secretion gradually decreases with age due to apoptosis of hormone-secreting cells and a decrease in blood flow, aging of hormone-secreting organs, and oxidative stress. In particular, it is known that the amount of estrogen secretion decreases rapidly after menopause. The effects of estrogens include vasodilatory action, blood pressure control action, lipid metabolism control, production of antioxidant enzyme SOD (antioxidant action), and regulation of autonomic nerves. It is a feature. As the secretion amount of estrogen having such actions decreases, it affects the body in the form of various diseases, unstable complaints and skin aging. Thus, supplementing with estrogen-like substances can be said to be very effective in enhancing various functions of the mind and body that decline with age.

  In recent years, soy isoflavone is known as a female hormone-like substance, and health foods and cosmetics containing high isoflavone content alone have been developed. However, taking a large amount of only a specific component as an excellent substance may cause side effects similar to those of chemically synthesized drugs. In addition to this, there are some plant-derived estrogen-like substances, but there are concerns about the safety of their use.

  Rhodiola is a member of the family Crassulaceae and grows naturally in the alpine rocks of Tibet, China. In China, there is a description of a herb medicine called “Keiten” in the oldest book of the book, “Shinnohonkaku”. ing. The medicinal effects of "Keiten" include burn treatment, fever and gynecological diseases, lightness with long-term use, improved visual acuity, and nutritional tonic. On the other hand, “Hongjing Tian” is positioned as a traditional drug in China and other countries, but there are still many points that have yet to be elucidated regarding the evaluation of the efficacy of modern medicine.

In recent years, in Japan, various researches have been conducted on red scenic heaven, and products that exhibit pharmacological effects in the fields of health foods and cosmetics have been developed (Patent Documents 1 to 5). However, in these proposals, no report has been made that the red ginseng extract has an estrogen-like action (an effect similar to estrogen action).
JP 2002-20308 A JP 2002-316938 A JP2003-12529 JP 2001-316221 A JP 2003-26532 A

Summary of the Invention

  At the time of the present invention, the inventors of the present invention focused on the extract of Rhodiola, and found that it has the same pharmacological action (effect) as estrogen. The present invention has been made based on such knowledge. Accordingly, the present invention provides an estrogen-like composition comprising an extract material extracted from the genus Pleuroaceae.

  The estrogen-like composition according to the present invention is not a chemically synthesized product, but uses an extract of a naturally-derived Benjasaceae red scenic genus plant, and this extract has an estrogenic effect, resulting in an estrogen deficiency. Prevent and improve diseases and unstable complaints such as diabetes, hypertension, hyperlipidemia, lifestyle-related diseases such as arteriosclerosis, autonomic dysfunction, menopause, skin troubles, wrinkles, sagging etc. It has a medicinal effect.

The definition “estrogen-like composition” refers to a substance that performs the same or similar action, effect, role, and the like as estrogen when administered to a mammal (including a human in the present specification). Thus, “estrogen-like composition” also means an estrogen replacement composition.
“Extract” includes an extract obtained by an extraction process, a diluted or concentrated solution of the extract, a dried product obtained by drying the extract, or a crude product or a preparation thereof. It is a concept to do.

1. Estrogen-like composition The estrogen-like composition according to the present invention may be an extract of the genus Pleuroaceae, or may contain other components.
Extract / Extraction method
The raw material is a plant belonging to Rhodiola, and its type and production area are not particularly limited. Specifically, R.rosea, Shiki Kokei Heaven (R.quadrifida (Pall.)), Sekiji Kagetenten (all Ben) (R. sacra), Ohana Kagekeiten (R.crenulate), Kiyo Kurekageten (R.algida), Karako Kageki Tengu (R.algida var.Tangutica), Nishikawa Benkeiten (R.alsia), Koza Benkeiten (R.dumulosa), Long Whip gilid), red bean landscape (R. henryi), R.heterodonta, R. kirillowii, rough red landscape (R.scabrida), coarse red landscape (R. wallichiana), R. wallichiana var. Cholaensis, R. yunnanensis, R. sachalinensis, etc. (R.rosea), Shiki Kageten (R.quadrifida (Pall.)), Sekiji Kageten (Ren sacra), Ohana Kageten ( R.crenulate) is preferred. Moreover, as a raw material, you may use the whole plant of a diatomaceae red-viewing genus plant, or the leaf, stem, petal, seed, rhizome or root, or 2 or more types of these mixed. The raw material may be dried or non-dried, but a dried product is preferable from the viewpoint of handling and storage stability.

Extraction Solvent In the present invention, as an extraction solvent, water, a linear or branched lower alcohol having 1 to 5 carbon atoms, a linear or branched lower alcohol having 1 to 5 carbon atoms, a linear or A branched C1-C5 lower acetone and a mixture of two or more of these are used. Specific examples of the straight or branched lower alcohol having 1 to 5 carbon atoms include methanol, ethanol, propanol, butanol and the like, more preferably methanol and ethanol (preferred). Specific examples of the lower ester having 1 to 5 carbon atoms having a straight chain or a branched chain preferably include methyl acetate and ethyl acetate, and more preferably ethyl acetate. As the C1-C5 lower acetone having a straight chain or a branched chain, acetone is preferably mentioned. In the present invention, when a solvent extract extracted with a solvent is used as it is as an estrogen-like composition, it is preferable to select and use one of these solvents used as a food, more preferably water, ethanol. And mixtures thereof.

  The addition amount of the extraction solvent can be appropriately determined according to the amount of raw material, extraction temperature, and the like. Further, the solvent extraction may be performed at normal temperature and normal pressure, and the extraction temperature can be appropriately determined in consideration of the boiling point of each solvent.

  In the present invention, in the case of solvent extraction, the weight ratio of the diatomaceae red ginseng plant (dried) and the solvent is 1:20 to 1: 1, preferably 1:15, more preferably. 1:10. Moreover, the temperature when heating at the time of extraction is 30 degreeC or more and about 100 degrees C or less, Preferably, a lower limit is 45 degreeC or more and an upper limit is 90 degrees C or less. In addition, when performing extraction at room temperature, although it depends on the amount of raw material, the quality, composition and amount of the extraction solvent, it is about 2 days to 6 days per kg of raw material, and the lower limit is 3 days or more. And the upper limit is 5 or less.

Concentration According to another aspect of the present invention, an extract obtained by removing the solvent from the solvent extract can be obtained. As a method for removing the solvent, generally, vacuum concentration, heat concentration, ventilation concentration, freeze concentration, spray concentration, and other concentration methods, or a mixing method thereof can be used. The pressure, temperature, wind force, spraying, and the like at the time of concentration can be appropriately set according to the amount of the extract obtained and the intended use. In the present invention, vacuum concentration is preferably used. In the case of concentration under reduced pressure, the pressure and temperature can be appropriately set according to the amount of the obtained concentrate and the intended use.

Dry / Dry Product According to another aspect of the present invention, the extract or the extract from which the solvent has been removed can be dried to obtain a dry product. In the present invention, the drying method includes sun drying, (hot) air drying, vacuum drying, aeration drying, fluidized drying, spray drying, freeze drying, vacuum drying, infrared drying, high frequency drying, and other drying methods, or these The following mixing method is used. Drying may be performed simultaneously with the concentration described above.

Preferred Extraction Embodiment According to a preferred aspect of the present invention, for example, 3 to 5 liters of a solvent is added to 1 kg of herbal medicine powder of the genus Papaveraceae, and the extract is extracted by heating or cooling. Obtainable. When heating, it is preferable to immerse at room temperature (around 25 degree | times) for 3 days when cooling at the temperature of 80-90 degreeC for several hours. After performing the heating or cooling treatment, it can be filtered to obtain an extract extracted from the genus Papaveraceae. According to a more preferred embodiment of the present invention, the extract can be concentrated under reduced pressure, for example, at 45 ° C. or lower, and the solvent can be distilled off to obtain a dry extract.

Manufacturing Method Thus, according to another aspect of the present invention, a method of manufacturing an estrogen-like composition can be proposed, which method comprises:
Prepare a red celestial plant
While adjusting the temperature as necessary, the diatomaceous earth red plant genus plant is immersed in a solvent,
Obtaining a soaked extract from the Benxisaceae Red Scenery genus plant.
The production method according to the present invention may comprise, if necessary, concentrating and / or drying the extract material and adding a third component to the extract material.

2. Application
Estrogen-like composition According to the present invention, an estrogen-like composition comprising an extract material extracted from the genus Pleuroaceae can be used for various purposes, and specifically has the following uses. .

Food additive / functional food (health food)
The estrogen-like composition according to the present invention may be used as a food additive. According to another aspect of the present invention, a food (functional food, health food) comprising the estrogen-like composition according to the present invention is proposed. The food product according to the present invention can supply an estrogen-like composition to an estrogen-deficient animal and exert its function as an estrogen-like agent. The food product according to the present invention is obtained by adding the extract of the red genus Papaveraceae plant according to the present invention to the food product in a form capable of realizing its pharmacological effect.

  As specific examples of the food according to the present invention, processed cereal products such as noodles, bread, cooked rice, rice cake, and the like, which contain the extract of the genus Pleuroaceae plant according to the present invention; processed fats and oils such as margarine and mayonnaise; Processed meat products such as ham and sausage; processed fishery products such as kamaboko and chikuwa; dairy products such as yogurt, butter, cheese and ice cream; processed fruit products such as jam; processed vegetable products such as pickles; chocolate, cookies and cakes Candy such as candy, chewing gum and jelly; various beverages such as juice, coffee, tea, green tea, oolong tea, carbonated beverages and milk; seasonings such as soy sauce, sauce and mirin;

  The functional food (health food) according to the present invention has a daily intake amount of 1.0 mg to 1,000 mg in terms of the mass of the extract of the genus Pleuroceae family, preferably lower limit. It is preferable that the upper limit value is set to 10 mg or more and 600 mg or less.

Pharmaceutical Composition According to another aspect of the present invention, a pharmaceutical composition comprising an estrogen-like composition according to the present invention can be proposed. This pharmaceutical composition supplements estrogen deficiency and exerts an effect on anti-estrogen deficiency. Specifically, the pharmaceutical composition according to the present invention is used for diseases associated with estrogen deficiency or extractive unstable complaints such as lifestyle diseases such as diabetes, hypertension, hyperlipidemia, arteriosclerosis, autonomic dysfunction, climacteric disorder. Prevents, improves, and cures skin troubles, wrinkles, sagging, etc. The anti-menopausal agent according to the present invention is used for the purpose of preventing, suppressing, improving, or treating climacteric disorder (juvenile climacteric disorder), and its efficacy Is recognized.

  The pharmaceutical composition according to the present invention can be administered to an animal by any route of oral and parenteral (eg, rectal administration, transdermal administration). The pharmaceutical composition according to the present invention is preferably provided as an appropriate dosage form according to the administration route. For example, various preparations such as liquid preparations, capsules, tablets, granules, powders, pills, fine granules, oral preparations such as troche tablets, rectal administration preparations and the like can be used.

  In order to ensure the effect as a pharmaceutical composition, for example, excipients, extenders, binders, wetting agents, disintegrants, surfactants, lubricants, dispersants, buffers, storage Pharmaceutically acceptable carriers or additives such as agents, solubilizers, flavoring agents, soothing agents, stabilizers, and the like may be appropriately selected and added to the pharmaceutical composition according to the present invention. Non-toxic additives that can be used are, for example, lactose, fructose, glucose, starch, gelatin, magnesium carbonate, synthetic magnesium silicate, talc, magnesium stearate, methylcellulose, carboxymethylcellulose or salts thereof, gum arabic, polyethylene glycol, Examples include syrup petrolatum, glycerin, ethanol, propylene glycol, citric acid, sodium chloride, sodium sulfite, and sodium phosphate.

  The pharmaceutical composition according to the present invention has a daily intake of 1.0 mg or more and 1,000 mg or less, preferably a lower limit of 10 mg or more, in terms of the mass per day of the extract of the genus Pleuroaceae. It is preferable to set the upper limit value to be 600 mg or less.

Skin Composition / Cosmetic The estrogenic composition according to the invention can also be used as a skin (pharmaceutical) composition or cosmetic. The dermatological composition or cosmetic according to the present invention is excellent in the feeling of use and safety when applied to the skin. The dermatological composition or cosmetic according to the present invention includes, for example, ointments, creams, milky lotions, lotions, packs, bathing agents, etc. in consideration of the intended use. The addition amount of the extract of the genus Benxiaceae is about 0.0001% or more and 20% or less with respect to the total weight of the dermatological composition (cosmetics), and preferably has a lower limit value. It is 0.0001% by weight or more and the upper limit is 10% by weight or less.

  The dermatological composition or cosmetic according to the present invention may comprise an optional component. Specific examples of optional components include humectants, ultraviolet absorbers, complex lipids, substances having an action of eliminating active oxygen, anti-inflammatory agents, vitamins and derivatives thereof, oily components, surfactants, preservatives, antioxidants, cholesterol , Plant sterols, lipoproteins, microorganism-derived components, algal extracts, blood circulation promoters, antiseborrheic agents, thickeners, colorants and the like.

  The contents of the present invention will be described in detail with reference to the following examples, but the present invention should not be construed as being limited to these examples. In the examples, unless otherwise specified, the blending amount (addition amount) indicates parts by weight.

Sample preparation
Preparation of extract (powder) of Astragalusaceae red splendid genus plant A mixture of 150 mL of purified water and 150 mL of ethanol was added to 10 g of Astragalus vermicelliae plant and allowed to stand for 24 hours, followed by filtration to remove the solvent. Then, it was set as the powder of the genus Papaveraceae red ginseng plant extract powder (hereinafter referred to as “implemented sample”).
Preparation of soy extract (powder) A mixture of 150 mL of purified water and 150 mL of ethanol was added to 10 g of soybean, left to stand for 24 hours, filtered, the solvent was removed, and soybean extract powder (hereinafter referred to as “Comparative Sample”). Said).

Evaluation test
Evaluation 1: Estrogen-like action test Each of the working sample and the comparative sample prepared above was added to a medium in which MCF-7 cells were seeded and cultured for a certain period of time, and then the number of proliferating cells was measured to calculate the action rate. The calculation was performed by setting the action rate of the cultured cells when the sample solvent was added to 100%. This result is as shown in Table 1 below, and it is understood that each added amount (25, 50, 100, 200 ppm) of the working sample according to the present invention has an estrogen-like action like the comparative sample (25 ppm). It was. In particular, when compared at a working concentration of 25 ppm, it is understood that the working sample of the present invention has a higher working rate than the comparative sample (soybean). "MCF-7" used in this evaluation 1 has abundant receptors for estrogen, a female hormone, among human breast cancer-derived cells, and has the property of proliferating in an estrogen-dependent manner.

Evaluation 2: Effect test of skin composition A skin beautification effect test was performed using a skin composition (cosmetic specification) prepared according to the composition shown in Table 2 below. The test method was a panel of 30 women aged 35 to 60 years. After washing the face twice a day for 12 weeks, Example 1 and Comparative Example 1 and a control skin composition were applied in an appropriate amount to the face. The items of each skin effect after application were evaluated according to the following criteria, and the results are shown in Table 3.
Evaluation standard evaluation A: A remarkable effect was recognized (over 60% of all panelists).
Evaluation (circle): The clear effect was recognized (over 40% and 60% or less of all the panelists).
Evaluation Δ: Some effect was observed (over 20% over 40% of all panelists).
Evaluation x: No effect was observed at all (0% to 20% of all panelists).

Evaluation 3: Menopausal disorder prevention / improvement test After mixing the ingredients shown in Table 4 below, a climacteric disorder prevention / improvement test was conducted using a 0.3 g oval tablet-shaped food preparation prepared as a tablet. In the test method, five women with subjective symptoms of climacteric disorder aged 45 to 65 years were allowed to take Example 2, Comparative Example 2, and control food preparations 5 tablets a day for 10 days. The interview was conducted to examine the mental state and skin state before and after ingestion in each case, and the improvement effect after ingestion was evaluated according to the following criteria. The results are shown in Table 5. From the results in Table 5, it can be seen that it reduces the unstable complaints specific to menopause. In addition, there were no complaints such as side effects due to oral intake in each case.
Evaluation standard evaluation A: A remarkable effect was recognized (over 60% of all panelists).
Evaluation (circle): The clear effect was recognized (over 40% and 60% or less of all the panelists).
Evaluation Δ: Some effect was observed (over 20% over 40% of all panelists).
Evaluation x: No effect was observed at all (0% to 20% of all panelists).

Claims (5)

  An estrogen-like composition comprising an extract material extracted from a genus Benxisaceae red splendid genus plant.   The estrogen-like composition according to claim 1, which is a food additive.   A food comprising the estrogen-like composition according to claim 1.   A pharmaceutical composition for an anti-estrogen deficiency comprising the estrogen-like composition according to claim 1.   A dermatological composition or cosmetic comprising the estrogen-like composition according to claim 1.