WO2021080297A1 - Composition contenant un extrait de fleur d'onagre en tant que principe actif pour prévenir ou traiter l'obésité ou des syndromes métaboliques ainsi induits - Google Patents

Composition contenant un extrait de fleur d'onagre en tant que principe actif pour prévenir ou traiter l'obésité ou des syndromes métaboliques ainsi induits Download PDF

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WO2021080297A1
WO2021080297A1 PCT/KR2020/014363 KR2020014363W WO2021080297A1 WO 2021080297 A1 WO2021080297 A1 WO 2021080297A1 KR 2020014363 W KR2020014363 W KR 2020014363W WO 2021080297 A1 WO2021080297 A1 WO 2021080297A1
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obesity
evening primrose
metabolic syndrome
extract
induced
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PCT/KR2020/014363
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English (en)
Korean (ko)
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이진호
김선홍
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(주)닥터티제이
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    • 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)
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • 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
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q90/00—Cosmetics or similar toiletry preparations for specific uses not provided for in other groups of this subclass
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/3262—Foods, ingredients or supplements having a functional effect on health having an effect on blood cholesterol

Definitions

  • the present invention relates to a composition for the prevention or treatment of obesity or metabolic syndrome induced from obesity, comprising an evening primrose extract as an active ingredient, and more particularly, it has an adipogenesis inhibitory activity, and thus obesity occurs through adipogenesis in adipocytes.
  • a pharmaceutical composition for improving or treating obesity or metabolic syndrome induced from obesity, comprising an evening primrose extract which can be very usefully used in the prevention, improvement, and treatment of metabolic syndrome disease induced from obesity as an active ingredient.
  • Metabolic syndrome is a phenomenon in which abdominal obesity, impaired glucose tolerance, high blood pressure, and dyslipidemia form a cluster. Among them, obesity is considered as the most basic factor of the outbreak, and the obese population is increasing year by year. In modern society, overeating, stress, and insomnia have been known as causes of obesity. Gradually, interest in the cause of obesity and demand for treatment are also increasing.
  • the evening primrose is a biennial plant of the dicotyledonous zygomatic needles family. It is native to South America and is distributed as a naturalized plant in North America, Korea, Japan, and China. Evening primroses used for medicinal purposes use slightly different plants for each country. Commonly used medicinal evening primroses include Oenothera odorata , Oenothera biennis , and Oenothera brevipes . These have slightly different efficacy and medicinal properties, but are used interchangeably for medicinal purposes.
  • Korean Patent Registration No. 10-0829083 discloses an extract having physiological activity
  • Korean Patent Laid-Open No. 10-1994-0000050 discloses a method for preparing a beverage containing the seed oil and a composition thereof
  • Korean Patent Registration No. 10-1584431 discloses a pharmaceutical composition for preventing or treating muscle atrophy caused by microgravity or nerve damage containing an evening primrose extract as an active ingredient
  • Korean Patent No. 10-1499457 discloses an evening primrose extract.
  • Food and pharmaceutical compositions for preventing or improving muscle atrophy containing as an active ingredient are disclosed, but the use of preventing, improving or treating metabolic syndrome induced by obesity or obesity is based on preventing obesity through the inhibition of fat production using evening primrose extract. None has been revealed about the content used as.
  • the present inventors have tried to develop a material that can prevent, improve or treat obesity and the metabolic syndrome caused by it, and as a result of ensuring safety, confirmed that the evening primrose extract exhibits an effect of inhibiting adipogenesis of adipocytes.
  • the present invention was completed.
  • an object of the present invention is to provide a method for preventing or treating obesity or metabolic syndrome induced from obesity, comprising administering a pharmaceutically effective amount of evening primrose extract to an individual.
  • an object of the present invention is to provide a use of an evening primrose extract for use as a pharmaceutical composition for the prevention or treatment of obesity or metabolic syndrome induced from obesity.
  • An object of the present invention is a pharmaceutical composition for preventing or treating obesity or metabolic syndrome induced from obesity, comprising an evening primrose extract as an active ingredient;
  • the evening primrose extract is to be contained in a concentration of 5 to 600 ⁇ g / ml.
  • the obesity is to be induced by adipocyte differentiation and proliferation.
  • the metabolic syndrome induced from obesity is one or more selected from the group consisting of abdominal adipogenesis, impaired glucose tolerance, hypertension, and dyslipidemia.
  • the evening primrose extract is to be extracted with one or more solvents selected from the group consisting of water and organic solvents.
  • the organic solvent is composed of at least one selected from the group consisting of alcohols having 1 to 5 carbon atoms, ethyl acetate, acetone, ether, chloroform, benzene, hexane and dichloromethane.
  • the evening primrose extract is made of at least one extract selected from the group consisting of evening primrose flowers, leaves, branches, stems, roots, fruits, and seed shells.
  • the evening primrose extract is to be an extract of evening primrose roots.
  • the object of the present invention can also be achieved by providing a health functional food composition for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient.
  • the evening primrose extract is to contain 0.0001 to 100% by weight.
  • the obesity is to be induced by adipocyte differentiation and proliferation.
  • the metabolic syndrome induced from obesity is one or more selected from the group consisting of abdominal adipogenesis, impaired glucose tolerance, hypertension, and dyslipidemia.
  • the evening primrose extract is to be extracted with one or more solvents selected from the group consisting of water and organic solvents.
  • the organic solvent is composed of at least one selected from the group consisting of alcohols having 1 to 5 carbon atoms, ethyl acetate, acetone, ether, chloroform, benzene, hexane and dichloromethane.
  • the evening primrose extract is made of at least one extract selected from the group consisting of evening primrose flowers, leaves, branches, stems, roots, fruits, and seed shells.
  • the evening primrose extract is to be an extract of evening primrose roots.
  • an object of the present invention is a health functional food composition for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it can be achieved by providing the use of an evening primrose extract for use as a health functional food composition for improving metabolic syndrome induced from obesity or obesity.
  • an object of the present invention is an external preparation for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it may be achieved by providing the use of an evening primrose extract for use as an external application for improving metabolic syndrome induced from obesity or obesity.
  • an object of the present invention is a cosmetic product for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it may be achieved by providing the use of an evening primrose extract for use as a cosmetic for improving metabolic syndrome induced from obesity or obesity.
  • the pharmaceutical composition for the prevention or treatment of obesity or metabolic syndrome induced from obesity comprising the evening primrose extract according to the present invention as an active ingredient contains an evening primrose extract having an adipogenesis inhibitory activity as an active ingredient, through adipogenesis in adipocytes. It shows an excellent effect that can be very usefully used in the prevention, improvement and treatment of obesity or metabolic syndrome disease induced from obesity.
  • FIG. 1A and 1B show the results of measuring the cytotoxicity of the evening primrose (Oenothera biennis ) ethanol extract (FIG. 1A) or the hot water extract of evening primrose (FIG. 1B) prepared through Example 1 of the present invention.
  • FIG. 2A and 2B show the effect of inhibiting adipogenesis of adipocytes by concentration of the evening primrose ethanol extract (FIG. 2a) or the evening primrose hot water extract (FIG. 2b) prepared through Example 1 of the present invention.
  • Figures 3a and 3b is a visual check of the adipogenesis inhibitory effect of adipocytes according to concentrations of the evening primrose ethanol extract ( Figure 3a) or the evening primrose hot water extract ( Figure 3b) prepared through Example 1 of the present invention.
  • adipocytes refers to cells that produce fat in vivo from adipocytes differentiated from adipocytes.
  • the term “obesity” means providing the cause of a disease or disease caused by excessive adipogenesis.
  • the "metabolic syndrome" in the present invention includes, for example, a comprehensive symptom of symptoms that appear as a cluster of abdominal fat production, impaired glucose tolerance, high blood pressure, and dyslipidemia.
  • the obesity disease treated, improved or prevented by the present invention is abdominal fat production, impaired glucose tolerance, high blood pressure, and dyslipidemia belonging to the metabolic syndrome.
  • Metabolic syndrome includes comprehensive symptoms of symptoms such as abdominal adipogenesis, impaired glucose tolerance, hypertension, and dyslipidemia. Evening primrose extract, which very efficiently inhibits adipogenesis of adipocytes, is very effective in treating metabolic syndrome diseases. Valid.
  • prevention has not been diagnosed as possessing a disease or disease, but refers to suppressing the occurrence of a disease or disease in an animal prone to such a disease or disease.
  • treatment refers to (i) inhibition of the disease or development of the disease; (ii) alleviation of the disease or disease; And (iii) a disease or disease.
  • the present invention is a pharmaceutical composition for preventing or treating metabolic syndrome induced from obesity or obesity, comprising an evening primrose (Oenothera biennis) extract as an active ingredient; A method for preventing or treating obesity or metabolic syndrome induced from obesity, comprising administering a pharmaceutically effective amount of evening primrose extract to an individual; And it provides the use of an evening primrose extract for use as a pharmaceutical composition for the prevention or treatment of obesity or metabolic syndrome induced from obesity.
  • primrose extract which is an active ingredient of the present invention, is preferably prepared by a method comprising the following steps, but is not limited thereto:
  • the evening primrose of step 1) may be grown or commercially available without limitation.
  • the evening primrose it is preferable to use at least one portion selected from the group consisting of evening primrose flowers, leaves, branches, stems, roots, fruits, and seed shells, and more preferably, the roots are used.
  • the extraction solvent of step 1) is preferably extracted with at least one solvent selected from the group consisting of water and an organic solvent
  • the organic solvent is an alcohol having 1 to 5 carbon atoms, ethyl acetate, acetone, ether, chloroform, More preferably, it consists of at least one selected from the group consisting of benzene, hexane and dichloromethane.
  • the alcohol may be selected from the group consisting of methanol, ethanol, propanol, butanol, and isopropanol, preferably ethanol.
  • the extraction method is preferably ultrasonic extraction, shaking extraction, Soxhelt extraction, or reflux extraction, but is not limited thereto.
  • the extraction solvent It is preferable to extract by washing the extraction solvent and adding 1 to 15 times the amount of the well-dried evening primrose, and more preferably, extracting by adding 2 to 10 times, but is not limited thereto.
  • the extraction time is preferably 1 to 72 hours, more preferably 2 to 48 hours, but is not limited thereto.
  • the number of extractions is preferably 1 to 5, but is not limited thereto.
  • the evening primrose extract of the present invention includes a fraction obtained by fractionating the primary extract extracted using the extraction solvent again using an extraction solvent having a different polarity, for example, the evening primrose extract contains the active ingredient contained in the evening primrose. After extraction with an alcohol having 1 to 5 carbon atoms, the fraction may be fractionated again with a solvent having a different polarity such as ether, benzene, or hexane.
  • each solvent extract may be prepared by sequentially using or mixing according to the polarity of the solvent, but is not limited thereto.
  • the extract prepared through the above process or the fraction obtained by performing the fractionation process may be filtered, concentrated, or dried to remove the solvent, and filtration, concentration, and drying may be performed.
  • the filtration may be performed using a filter paper or a reduced pressure filter, and the concentration may be concentrated under reduced pressure using a reduced pressure concentrator, for example, a rotary evaporator, and the drying may be performed by, for example, a freeze drying method.
  • the evening primrose extract is 5 to 600 ⁇ g/ml, specifically 10 to 500 ⁇ g/ml, more specifically 15 to 400 ⁇ g/ml, more specifically 20 to 300 ⁇ g/ml, more specifically 25 It is preferably contained in a concentration of 200 ⁇ g/ml.
  • the obesity is induced by adipocyte differentiation and proliferation
  • the metabolic syndrome is induced by such obesity, and more specifically, the metabolic syndrome is in the group consisting of abdominal adipogenesis, impaired glucose tolerance, hypertension and dyslipidemia. Is more than one selected.
  • the present inventors confirmed that the evening primrose extract exhibits an effect of inhibiting adipogenesis of adipocytes, so the extract is a metabolic syndrome induced from obesity or obesity caused by adipogenesis in adipocytes. It can be very usefully used as an active ingredient of a pharmaceutical composition for prevention, improvement and treatment.
  • the pharmaceutical composition according to the present invention may include a pharmaceutically acceptable carrier in addition to active ingredients such as evening primrose extract.
  • the carrier is commonly used in the formulation of pharmaceutically acceptable ingredients, and lactose, dextrose, sucrose, sorbitol, mannitol, starch, gum acacia, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline Cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil, and the like, but are not limited thereto.
  • the pharmaceutical composition of the present invention may further include a lubricant, a wetting agent, a sweetening agent, a flavoring agent, an emulsifying agent, a suspending agent, a preservative, and the like in addition to the above components.
  • a lubricant e.g., a talc, a kaolin, a kaolin, a kaolin, a kaolin, a kaolin, kaolin, kaolin, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, a talct, a talct, a talct, a stea, stevia, glycerin, glycerin, glycerin, g
  • the appropriate dosage of the pharmaceutical composition according to the present invention is determined by factors such as formulation method, mode of administration, age, weight, sex, pathology of the patient, food, administration time, route of administration, excretion rate and response sensitivity. It can be prescribed in a variety of ways.
  • the pharmaceutical composition of the present invention can be administered orally or parenterally, and when administered parenterally, it can be administered by intravenous injection, subcutaneous injection, intramuscular injection, intraperitoneal injection, transdermal administration, etc. Depending on the type, it is preferable that the route of administration is determined.
  • the pharmaceutical composition according to the present invention is formulated using a pharmaceutically acceptable carrier and/or excipient according to a method that can be easily carried out by a person having ordinary knowledge in the technical field to which the present invention pertains. It may be manufactured in a form or may be prepared by placing it in a multi-dose container. In this case, the formulation may be in the form of a solution, suspension, or emulsion in an oil or aqueous medium, or may be in the form of an extract, powder, granule, tablet or capsule, and may additionally include a dispersant or a stabilizer.
  • the pharmaceutical composition according to the present invention may further include a carrier and vehicle commonly used in the pharmaceutical field.
  • a carrier and vehicle commonly used in the pharmaceutical field.
  • ion exchange resins e.g., Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite IR-120, Amberlite-120,
  • protamine sulfate disodium hydrogen phosphate, camium hydrogen phosphate, sodium chloride and zinc salts
  • colloidal silica magnesium trisilicate
  • polyvinylpyrrolidone polyvinylpyrrolidone
  • cellulose-based substrate polyethylene glycol, sodium carboxy It may include methylcellulose, polyarylate, wax or wool paper, but is not limited thereto.
  • the pharmaceutical composition according to the present invention may be in the form of granules, powders, coated tablets, tablets, capsules, suppositories, syrups, juices, suspensions, emulsions, drops, injections, or sustained-release formulations of the active compound.
  • It can be administered in various dosage forms, oral or parenteral, and when formulated, it can be prepared using diluents or excipients such as fillers, bulking agents, binders, wetting agents, disintegrants, surfactants, etc. that are commonly used in the pharmaceutical field.
  • the present invention is a health functional food composition for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it provides the use of an evening primrose extract for use as a health functional food composition for improving metabolic syndrome induced from obesity or obesity.
  • the evening primrose extract is preferably contained in an amount of 0.0001 to 100% by weight, but is not limited thereto.
  • the extraction method of the evening primrose extract and the type of metabolic syndrome induced from obesity or obesity with the extraction target are described in the pharmaceutical composition for improvement or treatment of obesity or metabolic syndrome induced from obesity comprising the evening primrose extract as an active ingredient. Since the contents are the same, the specific description uses the above contents, and hereinafter, only the unique configuration of the health functional food will be described.
  • the present inventors confirmed that the evening primrose extract exhibits an effect of inhibiting adipogenesis of adipocytes, so the extract is a health functional food for preventing or improving metabolic syndrome induced from obesity or obesity caused by adipogenesis in adipocytes. It can be very usefully used as an active ingredient of the composition.
  • the health functional food of the present invention may be added as it is or used with other foods or food ingredients, and may be appropriately used according to a conventional method.
  • Such foods include drinks, meat, sausage, bread, biscuits, rice cakes, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, alcoholic beverages and vitamins.
  • the mixing amount of the extract according to the present invention may be appropriately determined according to the purpose of use (for prevention or improvement).
  • the amount of the extract in the health food may be added in 0.01 to 15% by weight of the total food weight.
  • the amount may be less than the above range, and there is no problem in terms of safety, so the active ingredient may be used in an amount above the above range.
  • the health functional beverage composition of the present invention is not particularly limited in other ingredients other than those containing the above extract as an essential ingredient in the indicated ratio, and may contain various flavoring agents or natural carbohydrates, etc. as an additional ingredient like a normal beverage.
  • natural carbohydrates include monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sucrose, and the like; And polysaccharides, for example, common sugars such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol.
  • natural flavoring agents taumatin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.)
  • synthetic flavoring agents sacharin, aspartame, etc.
  • the food of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic flavoring agents and natural flavoring agents, coloring agents and thickeners (cheese, chocolate, etc.), pectic acid and salts thereof, alginic acid and its Salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonates used in carbonated beverages, and the like may be contained.
  • the extract of the present invention may contain natural fruit juice and flesh for the production of fruit juice beverages and vegetable beverages. These components may be used independently or in combination. The proportion of these additives is not so important, but is generally selected in the range of 0 to about 20 parts by weight per 100 parts by weight of the extract of the present invention.
  • the present invention is an external preparation for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it provides the use of an evening primrose extract for use as an external application for improving metabolic syndrome derived from obesity or obesity.
  • the present invention is a cosmetic for improving metabolic syndrome induced from obesity or obesity, comprising an evening primrose extract as an active ingredient; And it provides the use of an evening primrose extract for use as a cosmetic for improving metabolic syndrome induced from obesity or obesity.
  • the method of extracting the evening primrose extract and the type of metabolic syndrome induced from obesity or obesity are the pharmaceutical composition for improving or treating obesity or metabolic syndrome induced from obesity comprising the evening primrose extract as an active ingredient Since the contents are the same as those described in, the detailed description uses the above contents, and hereinafter, only the unique configurations of external preparations and cosmetics will be described.
  • the present inventors have confirmed that the evening primrose extract exhibits an effect of inhibiting adipogenesis of adipocytes, so the extract is effective as an external preparation or cosmetics for improving metabolic syndrome induced from obesity or obesity caused by adipogenesis in adipocytes. It can be very useful as an ingredient.
  • Ingredients included in the external preparation or cosmetic composition of the present invention may include ingredients commonly used in external preparations or cosmetic compositions in addition to the above active ingredients, such as antioxidants, stabilizers, solubilizers, vitamins, pigments, and fragrances. Phosphorus adjuvants, and carriers.
  • the active ingredient of the present invention In order to formulate the active ingredient of the present invention, it can be easily formulated if carried out according to conventional methods, and surfactants, excipients, coloring agents, spices, preservatives, stabilizers, buffers, suspensions, and other commercially available auxiliary agents can be appropriately used.
  • composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, It may be formulated as an oil, powder foundation, emulsion foundation, wax foundation, pack, massage cream and spray, but is not limited thereto. More specifically, it may be prepared in the form of a softening lotion, a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray, or a powder.
  • a softening lotion a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray, or a powder.
  • the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, or zinc oxide may be used as a carrier component.
  • animal oil vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, or zinc oxide
  • silicone e.g., bentonite, silica, talc, or zinc oxide
  • a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 ,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or fatty acid ester of sorbitan.
  • the formulation of the present invention is a suspension
  • a liquid diluent such as water, ethanol or propylene glycol, an ethoxylated isostearyl alcohol, a suspending agent such as polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, and crystallites Sex cellulose, aluminum metahydroxide, bentonite, agar, or tracant
  • a suspending agent such as polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester
  • lactose When the formulation of the present invention is a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder may be used as a carrier component.
  • additional chlorofluorohydrocarbon propane / May contain propellants such as butane or dimethyl ether.
  • Evening primrose ( Oenothera biennis ) roots were dried and then pulverized. 1.0 L of distilled water was added to 100 g of the pulverized evening primrose root sample, and then extracted by heating in a hot water of 100 ⁇ 5° C. for 2 to 3 hours, and a cooler was installed to maintain a constant temperature and prevent loss to steam. The evening primrose extract obtained as described above was filtered under reduced pressure and then freeze-dried to prepare a hot water extract of evening primrose.
  • 3T3-L1 mouse embryonic fibroblast cell line
  • adipocytes were purchased from ATCC (American type culture collection), 10% BCS (bovine calf serum, WelGene Biopharmaceuticals, Daegu, Korea) and antibiotics (penicillin/streptomycin 100 units/ml) , Bioshop, Burlington, Ontario, Canada) was added to DMEM medium (Dulbecco's modified Eagle's medium, WelGene Biopharmaceuticals, Daegu, Korea), and cultured in a cell incubator under conditions of 37°C and 5% CO 2.
  • BCS bovine calf serum
  • WelGene Biopharmaceuticals Daegu, Korea
  • antibiotics penicillin/streptomycin 100 units/ml
  • the cytotoxicity of the evening primrose extract prepared in ⁇ Example 1> was evaluated using the MTT assay method.
  • the medium solution was removed from the 100 cm 2 culture plate in which 3T3-L1 adipocytes were cultured by the method disclosed in ⁇ Experimental Example 1>, and washed with CMF-PBS (calcium magnesium free-phosphate buffered saline, pH 7.2). After that, the cells were removed by treatment with 0.25% trypsin/EDTA, neutralized with a cell culture solution, and centrifuged at 1500 rpm for 5 minutes. After adding the culture solution to the pellet of the remaining cells, repeat suction with a sterile pipette to make a single cell suspension, and then mix trypan blue with the cell suspension in a ratio of 9:1 to obtain a hemocytometer on an optical microscope.
  • CMF-PBS calcium magnesium free-phosphate buffered saline, pH 7.2
  • a differentiation inducing agent IBMX, dexamethasone, Insulin
  • Fig. 1a evening primrose ethanol extract
  • Fig. 1b evening primrose hot water extract
  • Figs. 1a and 1b when the case where no evening primrose extract is not added is determined as a survival rate of 100%, the addition group to which evening primrose ethanol extract (Fig. 1a) or hot water extract of evening primrose (Fig. 1b) is added It was also confirmed that the survival rate was similar to that of the group to which it was not added.
  • the evening primrose extract of the present invention did not show toxicity to adipocytes.
  • adipogenesis was confirmed by treating 3T3-L1 adipocytes and inducing adipocyte differentiation, and then adipogenesis using Oil Red O adipogenesis.
  • the ethanol extract of evening primrose prepared in Example ⁇ 1-1> or the hot water extract of evening primrose prepared in ⁇ 1-2> by the same method as described in ⁇ Experimental Example 2> was 0, 25, 50, 100 .
  • the 3T3-L1 adipocytes cultured in ⁇ Experimental Example 1> were treated at a concentration of 200 ⁇ g/ml to induce adipocyte differentiation.
  • the adipogenesis stimulation was maintained for 48 hours by replacing with a new 10% FBS serum medium containing 10 ⁇ g/ml of insulin, and a stable period was maintained again for 48 hours with a new medium containing serum.
  • 10% formalin (formalin, Junsei Chemical, Tokyo, Japan) was treated in each well and fixed at room temperature for 1 hour.
  • each well was treated with Oil Red O stain solution and stained for 10 minutes.
  • evening primrose ethanol extract Fig. 3a
  • evening primrose hot water extract Fig. 3b
  • the wavelength was measured with a 490 nm microplate reader.
  • FIGS. 2A and 2B it was confirmed that adipogenesis of adipocytes was significantly increased when only insulin was treated after adipocyte differentiation was achieved.
  • the adipogenesis of adipocytes was significantly reduced when the evening primrose ethanol extract (FIG. 2a) or the evening primrose hot water extract (FIG. 2b) was treated together.
  • adipogenesis of adipocytes decreased in a concentration-dependent manner as the concentration of the evening primrose extract was increased (FIGS. 2A and 2B ).
  • FIGS. 3A and 3B when only insulin was treated after adipocyte differentiation was performed, it was confirmed through microscopic observation that the size and number of droplets on which fat was formed significantly increased.
  • FIGS. 3A and 3B when the evening primrose ethanol extract (FIG. 3a) or the evening primrose hot water extract (FIG. 3b) was treated together, it was confirmed that the size and number of droplets formed with fat were significantly reduced.
  • the concentration of the evening primrose extract increased, it was confirmed that the size and number of droplets formed with fat decreased in a concentration-dependent manner (FIGS. 3A and 3B ).
  • the evening primrose extract of the present invention exhibits an effect of inhibiting adipogenesis of adipocytes in a concentration-dependent manner.
  • the evening primrose extract according to the present invention exhibits an effect of inhibiting adipogenesis of adipocytes
  • the extract prevents obesity and obesity by reducing the likelihood of obesity occurring through adipogenesis in adipocytes. It can be very useful for early prevention, improvement and treatment of induced metabolic syndrome diseases.
  • the above ingredients were mixed and filled in an airtight cloth to prepare a powder.
  • tablets were prepared by tableting according to a conventional tablet preparation method.
  • a gelatin capsule was filled according to a conventional capsule preparation method to prepare a capsule.
  • 0.1 to 5.0 parts by weight of the extract of the present invention were added to soups and juices to prepare health-promoting meat products, noodles soup, and broth.
  • Ground beef for health promotion was prepared by adding 10 parts by weight of the extract of the present invention to ground beef.
  • Brown rice, barley, glutinous rice, and adlay were gelatinized and dried by a known method, and then roasted, and then prepared into a powder having a particle size of 60 mesh with a grinder.
  • Black soybeans, black sesame seeds, and perilla seeds were also steamed and dried by a known method, and then roasted, and then prepared into a powder having a particle size of 60 mesh with a grinder.
  • the extract of the present invention was concentrated under reduced pressure in a vacuum concentrator, sprayed and dried with a hot air dryer, and the resulting dried product was pulverized with a grinder to a particle size of 60 mesh to obtain a dry powder.
  • Extract of the present invention (3 parts by weight),
  • Vegetable juice was prepared by adding 100 mL of the extract of the present invention to 1,000 mL of tomato or carrot juice.
  • Fruit juice was prepared by adding 100 mL of the extract of the present invention to 1,000 mL of apple or grape juice.
  • An ointment containing the extract of the present invention was prepared by a conventional method according to the composition shown in the following [Table 1].
  • Extract of the present invention 1.0 glycerin 8.0 Butylene glycol 4.0 Floating paraffin 15.0 Ketaglucan 7.0 Carbomer 0.1 Caprylic/Capric Triglyceride 3.0 Squalane 1.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 Beeswax 4.0 antiseptic a very small amount Spices a very small amount Purified water Balance Sum 100
  • Nutrient lotion containing the extract of the present invention was prepared by a conventional method in the composition ratio of the following [Table 2].
  • Extract of the present invention 2.0 Glyceryl stearate SE 1.5 Cetearyl alcohol 1.5 lanolin 1.5 Polysorbate 60 1.3 Sorbitastearate 0.5 Hydrogenated vegetable oil 4.0 Mineral oil 5.0 Trioctanoine 2.0 Dimethicone 0.8 Tocopherol acetate 0.5 Carboxyvinyl polymer 0.12 glycerin 5.0 1,3-butylene glycol 3.0 Sodium hyaluronate 5.0 Triethanolamine 0.12 Uniside-U 13 0.02 incense a very small amount Distilled water Balance Sum 100
  • a nutrient cream containing the extract of the present invention was prepared by a conventional method in the ratio of the ingredients in the following [Table 3].
  • Extract of the present invention 2.0 Glycerin monostearate 1.5 Cetearyl alcohol 1.5 Stearic acid 1.0 Polysorbate 60 1.5 Sorbitastearate 0.6 Isostearyl isosterate 5.0 Squalane 5.0 Mineral oil 35.0 Dimethicone 0.5 Hydroxyethyl cellulose 0.12 glycerin 6.0 Triethanolamine 0.7 Uniside-U 13 0.02 incense a very small amount Distilled water Balance Sum 100
  • the evening primrose extract since it was confirmed that the evening primrose extract has an adipogenesis inhibitory activity, the evening primrose extract can be very useful in the prevention, improvement and treatment of obesity or metabolic syndrome disease induced from obesity caused by adipogenesis in adipocytes. have.

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Abstract

La présente invention se rapporte à une composition pharmaceutique, contenant un extrait de fleur d'onagre en tant que principe actif, pour prévenir ou traiter l'obésité ou les syndromes métaboliques ainsi induits. En particulier, l'extrait de fleur d'onagre s'est avéré avoir une activité anti-adipogénétique et peut donc être utilisé efficacement dans la prévention, l'amélioration et le traitement de l'obésité ou des syndromes métaboliques induits par l'obésité et provoqués par l'adipogenèse.
PCT/KR2020/014363 2019-10-24 2020-10-21 Composition contenant un extrait de fleur d'onagre en tant que principe actif pour prévenir ou traiter l'obésité ou des syndromes métaboliques ainsi induits WO2021080297A1 (fr)

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KR1020190133233A KR20210048933A (ko) 2019-10-24 2019-10-24 달맞이꽃 추출물을 유효성분으로 포함하는 비만 또는 비만으로부터 유도된 대사증후군의 예방 또는 치료용 조성물

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CN116057764A (zh) 2021-04-15 2023-05-02 株式会社Lg新能源 卷型原材料供应装置

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KR101533191B1 (ko) * 2014-04-18 2015-07-02 주식회사김정문알로에 알로에 베라 겔을 농축한 고분자분획과 달맞이꽃 종자 추출물을 포함하는 제2형 당뇨병 예방 및 치료용 의약조성물
KR102087033B1 (ko) * 2019-01-28 2020-03-10 고려대학교 세종산학협력단 달맞이꽃 추출물 또는 이의 분획물을 유효성분으로 포함하는 체중감량용 조성물

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JP2004256522A (ja) * 2003-02-06 2004-09-16 Noevir Co Ltd 糖尿病予防・治療用組成物
KR100551718B1 (ko) * 2003-02-26 2006-11-17 박정현 지방산 합성효소의 활성을 억제할 수 있는 비만 억제용조성물
JP2005008572A (ja) * 2003-06-19 2005-01-13 Yakult Honsha Co Ltd リパーゼ阻害剤
KR101533191B1 (ko) * 2014-04-18 2015-07-02 주식회사김정문알로에 알로에 베라 겔을 농축한 고분자분획과 달맞이꽃 종자 추출물을 포함하는 제2형 당뇨병 예방 및 치료용 의약조성물
KR102087033B1 (ko) * 2019-01-28 2020-03-10 고려대학교 세종산학협력단 달맞이꽃 추출물 또는 이의 분획물을 유효성분으로 포함하는 체중감량용 조성물

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116407580A (zh) * 2023-03-28 2023-07-11 五邑大学 素馨花提取物在调节肠道菌群及改善代谢综合征中的应用

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