WO2018190501A1 - Composition anti-inflammatoire contenant un extrait de pédoncule de fleur de ginseng - Google Patents

Composition anti-inflammatoire contenant un extrait de pédoncule de fleur de ginseng Download PDF

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Publication number
WO2018190501A1
WO2018190501A1 PCT/KR2018/001449 KR2018001449W WO2018190501A1 WO 2018190501 A1 WO2018190501 A1 WO 2018190501A1 KR 2018001449 W KR2018001449 W KR 2018001449W WO 2018190501 A1 WO2018190501 A1 WO 2018190501A1
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Prior art keywords
composition
extract
ginseng
ginseng flower
alcohol
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PCT/KR2018/001449
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English (en)
Korean (ko)
Inventor
김수환
김주원
박찬웅
서대방
조동현
조재열
한상윤
Original Assignee
(주)아모레퍼시픽
성균관대학교산학협력단
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Publication of WO2018190501A1 publication Critical patent/WO2018190501A1/fr

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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)
    • A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258—Panax (ginseng)
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30—Extraction of the material
    • A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH

Definitions

  • the present specification relates to an anti-inflammatory composition
  • an anti-inflammatory composition comprising ginseng flower rapeseed extract as an active ingredient.
  • the inventors of the present invention have studied the ginseng flower stalk extract and found that the ginseng flower stalk extract has an anti-inflammatory effect, thus leading to the present invention.
  • One aspect of the present invention to provide an anti-inflammatory composition
  • a ginseng flower stem extract as an active ingredient.
  • One aspect of the present invention is to provide a health food, cosmetic or pharmaceutical composition as an anti-inflammatory composition.
  • One aspect of the present invention provides an anti-inflammatory composition
  • a ginseng flower extract as an active ingredient.
  • the composition provides a composition that inhibits the production of nitric oxide (NO).
  • NO nitric oxide
  • the composition provides a composition that inhibits the expression of any one or more of TNF- ⁇ , iNOS and COX-2.
  • the extract is an extract extracted using water, C 1 -C 5 alcohol or C 1 -C 5 alcohol aqueous solution, provides a composition.
  • the concentration of the C 1 -C 5 alcohol aqueous solution is 40% to 90% (v / v) to provide a composition.
  • the C 1 -C 5 alcohol using any one or more selected from the group consisting of methanol, ethanol, isopropyl alcohol, n-propyl alcohol, n-butanol and isobutanol provides a composition do.
  • the extract is an extract extracted using an aqueous ethanol solution of 60 to 80% (v / v) concentration, to provide a composition.
  • the ginseng flower stalk provides a composition that is removed ginseng fruit.
  • the composition provides a health food or cosmetic composition.
  • the composition provides a pharmaceutical composition.
  • the composition provides a composition formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, and external preparations.
  • composition according to one aspect of the present invention has an anti-inflammatory effect.
  • composition according to one aspect of the present invention has the effect of inhibiting the production of nitric oxide (NO).
  • composition according to one aspect of the present invention has the effect of inhibiting the expression of TNF- ⁇ .
  • composition according to one aspect of the present invention has the effect of inhibiting the expression of iNOS.
  • composition according to one aspect of the present invention has the effect of inhibiting the expression of COX-2.
  • One aspect of the present invention has the effect of providing a health food composition having an anti-inflammatory effect.
  • One aspect of the present invention has the effect of providing a cosmetic composition having an anti-inflammatory effect.
  • One aspect of the present invention has the effect of providing a pharmaceutical composition having an anti-inflammatory effect.
  • composition according to one aspect of the present invention is generally effective in finding the value of the part discarded by recycling the ginseng flower stem discarded during ginseng processing.
  • Figure 3 is an experimental result confirming the inflammation-related protein expression in Example 1 according to the present invention Experiment 3.
  • the ginseng refers to the ginseng root, which is the root of ginseng, which is used as a medicinal herb or has been ingested and cooked as food.
  • Ginseng Panax ginseng CA Meyer
  • anti-cancer activity immune function control action, anti-diabetic action, anti-diabetic liver effect, cardiovascular disorders improvement, blood pressure control action, menopausal disorders improvement, anti-stress and anti-fatigue effect, antioxidant activity and anti-aging effect.
  • Ginseng flower stalks are not usually used as a medicinal herb, it is difficult to find a history of ingestion in the form of food.
  • the ginseng flower stalk comes out in May-June, which is the fourth year of planting seeds, and is discarded along with the ginseng flower in June, before it blooms for the smooth growth of ginseng roots.
  • Ginsenoside a representative physiologically active ingredient of ginseng, is distributed evenly on the ground and underground parts of ginseng. Especially, ginsenoside content and composition are different depending on the parts such as ginseng root (root), ginseng leaf and ginseng fruit. It is known. These differences in composition make a difference in the presence or absence of various efficacy and cause different site-specific efficacy characteristics. For example, ginseng flower extract has been shown to have an excellent effect and about 23 times more effective in the prevention and treatment of diabetes compared to ginseng root extract.
  • One aspect of the present invention provides an anti-inflammatory composition
  • a ginseng flower extract as an active ingredient.
  • Ginseng flower stalk as used herein is the axial portion of the ginseng flower peduncle and flower stem.
  • extract includes any material obtained by extracting a component therefrom from a natural product, regardless of the method of extraction or the kind of the component.
  • it is a broad concept including the thing which extracted the component melt
  • the organic solvent is not particularly limited, C1 ⁇ C5 lower alcohol, glycerol, ethylene, such as methanol, ethanol, isopropyl alcohol, n-propyl alcohol, n-butanol and isobutanol
  • Polyhydric alcohols such as glycol, propylene glycol, 1,3-butylene glycol, hydrocarbon solvents such as methyl acetate, ethyl acetate, benzene, n-hexane, diethyl ether, dichloromethane, chloroform, petroleum ether, methyl acetate
  • Non-polar organic solvents such as benzene, hexane, chloroform, methylene chloride, dimethyl ether, ethyl acetate and the like.
  • the extract may be an extract extracted with water, in particular hot water.
  • the extract may be an extract extracted with C 1 -C 5 alcohol.
  • the extract may be an extract extracted with ethanol, but is not limited thereto.
  • the extract is an extract extracted using water, C 1 -C 5 alcohol or C 1 -C 5 alcohol aqueous solution, provides a composition.
  • the concentration of the C 1 -C 5 alcohol aqueous solution is 40% to 90% (v / v) to provide a composition.
  • the concentration of the C 1 -C 5 alcohol aqueous solution is at least 40%, at least 45%, at least 50%, at least 55%, at least 60%, at least 65%, at least 66%, at least 67%, 68% Or at least 69%, at least 70%, at least 71%, at least 72%, at least 73%, at least 74%, at least 75%, or at least 80%.
  • the concentration of the C 1 -C 5 alcohol aqueous solution is 90% or less, 85% or less, 80% or less, 75% or less, 74% or less, 73% or less, 72% or less, 71% or less, 70% or less, 69 Up to 68%, up to 67%, up to 65%, or up to 60%.
  • concentration of the C 1 -C 5 alcohol aqueous solution is in the above range, the cell regeneration efficacy or anti-inflammatory effect is excellent.
  • the C 1 -C 5 alcohol using any one or more selected from the group consisting of methanol, ethanol, isopropyl alcohol, n-propyl alcohol, n-butanol and isobutanol provides a composition do.
  • the extract is an extract extracted using an aqueous ethanol solution of 60 to 80% (v / v) concentration, to provide a composition.
  • the ginseng flower rapeseed extract may be included in 0.001 to 90% by weight based on the total weight of the composition.
  • the ginseng flower stalk extract is 0.001% by weight, 0.01% by weight, 0.1% by weight, 1% by weight, 1.1% by weight, 1.5% by weight, 2% by weight or more based on the total weight of the composition , At least 3 wt%, at least 5 wt%, at least 10 wt%, at least 20 wt% or at least 30 wt%.
  • the ginseng flower stalk extract is 90 wt% or less, 85 wt% or less, 80 wt% or less, 70 wt% or less, 50 wt% or less, 40 wt% or less, 30 wt% or less, 20 wt%, based on the total weight of the composition. It may be up to%, 10% by weight, 5% by weight, 4% by weight, 3% by weight, 2% by weight, 1% by weight, 0.1% by weight or 0.05% by weight or less.
  • the ginseng flower stalk provides a composition that is removed ginseng fruit.
  • the composition provides a composition that inhibits the production of nitric oxide (NO).
  • NO nitric oxide
  • the composition provides a composition that inhibits the expression of any one or more of TNF- ⁇ , iNOS and COX-2.
  • the composition provides a health food or cosmetic composition.
  • the composition provides a composition formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, and external preparations.
  • the composition may be a cosmetic composition.
  • Cosmetic compositions herein can be prepared in any formulation commonly prepared in the art, including, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing , Oils, powder foundations, emulsion foundations, wax foundations and sprays, and the like, but are not limited thereto.
  • the dosage determination is within the level of those skilled in the art, and the daily dosage of the composition depends on various factors such as the age, health condition, and complications of the subject to be administered, but is based on an adult
  • the ginseng flower stalk extract may be administered by dividing 1 to 500 mg / kg, preferably 30 to 200 mg / kg, once or twice a day, and the dosage may be any amount of the present invention. It is not intended to limit the scope of.
  • the composition may be a food composition, for example, various foods, beverages, gums, teas, vitamin complexes, dietary supplements, and the like, and may be used in the form of powders, granules, tablets, capsules, or beverages. Can be.
  • the food composition of each formulation may be suitably selected by a person skilled in the art according to the formulation or purpose of use in addition to the active ingredient, and may be synergistic when applied simultaneously with other raw materials.
  • the amount of the active ingredient included in the food or beverage may generally include 0.1 to 60% by weight of the total food, if the health food composition, the health beverage composition is 0.002 to 50g, 0.02 in one side based on 100ml To 10 g.
  • Dosage determination when using the ginseng flower rapeseed extract as a food composition is within the level of those skilled in the art, its daily dosage is, for example, 0.1 mg / kg / day to 5000 mg / kg / day, more specifically 50 mg / kg It may be / day to 500 mg / kg / day, but is not limited thereto, and may vary depending on various factors such as age, health condition, complications of the subject to be administered.
  • the composition may contain other ingredients and the like that can give a synergistic effect to the main effect within a range that does not impair the main effect of the present invention.
  • it may further include additives such as perfumes, pigments, fungicides, antioxidants, preservatives, moisturizers, thickeners, inorganic salts, emulsifiers and synthetic polymer materials to improve physical properties.
  • additives such as perfumes, pigments, fungicides, antioxidants, preservatives, moisturizers, thickeners, inorganic salts, emulsifiers and synthetic polymer materials to improve physical properties.
  • supplementary ingredients such as water soluble vitamins, oil soluble vitamins, polymer peptides, polymer polysaccharides and seaweed extract may be further included.
  • the components may be appropriately selected and blended by those skilled in the art according to the formulation or purpose of use, and the amount of the additives may be selected within a range that does not impair the object and effect of the present invention.
  • the amount of the components added may range from 0.01-5% by weight, more specifically 0.01-3% by weight, based on the total weight of the composition.
  • the composition may be a pharmaceutical composition.
  • the carrier in the preparation of pharmaceutical formulations, it is preferred to mix or dilute the active ingredient with the carrier or to enclose it in a carrier in the form of a container.
  • the carrier when used as a diluent, it may be a solid, semisolid or liquid substance which acts as a carrier, excipient or medium for the active ingredient.
  • the formulation may be in the form of tablets, pills, powders, sachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, soft or hard gelatin capsules, sterile injectables, sterile powders and the like.
  • Suitable carriers, excipients and diluents include lactose, dextrose, sucrose, sorbitol, mannitol, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propyl Hydroxybenzoate, talc, magnesium stearate and mineral oil.
  • the formulation may further comprise fillers, anti-coagulants, lubricants, wetting agents, fragrances, emulsifiers, preservatives and the like.
  • the pharmaceutical compositions of the invention can be formulated using methods well known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to a mammal.
  • compositions of the present invention may be administered via several routes including oral, transdermal, subcutaneous, intravenous, abdominal, muscle, topical application, patch and iontophoresis, of which topical application and oral administration are preferred. can do.
  • a typical daily dosage of the active compound may range from 0.1 to 100 mg / kg body weight, preferably 5 to 70 mg / kg body weight, and may be administered once or in several doses.
  • the actual dosage of the active ingredient should be determined in light of several relevant factors such as the disease to be treated, the route of administration, the age, sex and weight of the patient, and the severity of the disease, and therefore the dosage may be determined in any way. Nor does it limit the scope of the present invention.
  • compositions according to the invention may be in various forms, such as solutions, emulsions, viscous mixtures, tablets, powders, and the like, which may be administered by various methods such as simple drinking, injection, spray or squeeze.
  • the present invention may be directed to a method for alleviating, ameliorating or treating skin inflammation comprising administering to a subject in need thereof a composition comprising the ginseng flower stalk extract.
  • the administration of the method may be carried out according to the administration method and administration dose described herein.
  • the present invention may be directed to the use of ginseng flower stalk extract for preparing an anti-inflammatory cosmetic composition.
  • the present invention may be directed to the use of ginseng flower stalk extract for preparing an anti-inflammatory health food composition.
  • the present invention may relate to the use of ginseng flower stalk extract for the preparation of an anti-inflammatory pharmaceutical composition.
  • ginseng flower stalk extract In the case of ginseng flower stalk extract, the ginseng flower stalks were collected and the fruit parts were separated and then dried in daylight or hot air to prepare ginseng flower stalk as a raw material. Thereafter, 70% ethanol was added to 1 kg of dried ginseng flower stalk, reflux extracted, filtered, and concentrated under reduced pressure at 40 to 45.
  • the ginseng flower stalk extract obtained through the above process was used in the following experimental example.
  • Red ginseng prepared by steaming and drying the ginseng harvested in Geumsan as Comparative Example 1 was extracted and used in the same extraction method as in Example 1.
  • the ginseng flower stalk extract of Example 1 and the red ginseng extract of Comparative Example 1 were analyzed according to the guideline of Health Food Code.
  • the ginseng flower stalk extract of Example 1 of the present invention was confirmed that there is a difference in the red ginseng extract and ginsenoside components of Comparative Example 1. Therefore, it was confirmed that the red ginseng extract and the ginseng flower stalk extract of the present invention are different substances in the content of ginsenosides.
  • Example 1 In order to confirm the anti-inflammatory effect of the ginseng flower rapeseed extract of Example 1 (70% ethanol extract) was measured the amount of nitric oxide produced as an inflammatory factor.
  • Example 1 and Comparative Example 1 were used in this experiment. The experiment was carried out according to the following method.
  • RAW264.7 cells were incubated for 24 hours at 1 * 10 5 in 96 well plates. After incubating Example 1 and Comparative Example 1 with LPS (1 ug / ml) for 12 hours, NO levels were measured. The absorbance at 540 nm of the cultured cell supernatant was measured by the same amount of N-1-Naphthylethylenediamine and Sulfanilamide reaction.
  • FIGS. 1 and 2 are graph showing the NO production amount of Example 1
  • Figure 2 is a graph showing the NO production amount of Comparative Example 1.
  • TNF- ⁇ , iNOS and COX-2 of the ginseng flower stalk extract of Example 1 (70% ethanol extract) were measured. The experiment was carried out according to the following method.
  • RAW264.7 cells were incubated in 6 well plates for 24 hours at 2 * 10 6 .
  • Example 1 was pretreated for 30 minutes and then treated with LPS (1 ug / ml) for 6 hours. After extraction of the total RNA, each mRNA expression was measured by RT-PCR method with 1000 ng cDNA. GAPDH was used as a control.
  • Example 1 was mixed with 30% by weight, corn starch 30% by weight, glycerin 20% by weight and sorbitol powder 20% by weight, and the ring was prepared using a deconcentrator. The final weight of the contents was 3.5 g.
  • Injectables were prepared by conventional methods according to the compositions set forth in Table 4 below.
  • Example 1 20mg Vitamin A Acetate 70 ⁇ g Vitamin E 1.0mg Vitamin B1 0.13mg Vitamin B2 0.15mg Vitamin B6 0.5mg Vitamin B12 0.2 ⁇ g Vitamin c 10mg Biotin 10 ⁇ g Nicotinic acid amide 1.7mg Folic acid 50 ⁇ g Calcium Pantothenate 0.5mg Ferrous sulfate 1.75mg Zinc oxide 0.82 mg Magnesium carbonate 25.3 mg Potassium phosphate monobasic 15 mg Dicalcium Phosphate 55 mg Potassium citrate 90 mg Calcium carbonate 100mg Magnesium chloride 24.8 mg

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Abstract

La présente invention concerne une composition anti-inflammatoire contenant un extrait d'un pédoncule de fleur de ginseng en tant que principe actif, et la composition inhibe la production d'oxyde nitrique (NO) ou inhibe l'expression d'un ou plusieurs parmi TNF-α, iNOS et COX-2, l'extrait d'un pédoncule de fleur de ginseng est un extrait obtenu à l'aide d'eau, d'un alcool C1-C5, ou d'une solution aqueuse d'alcool C1-C5, et la composition peut être utilisée en tant qu'aliment santé ou produit cosmétique ou composition pharmaceutique et a d'excellents effets anti-inflammatoires.
PCT/KR2018/001449 2017-04-11 2018-02-02 Composition anti-inflammatoire contenant un extrait de pédoncule de fleur de ginseng WO2018190501A1 (fr)

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KR1020170046527A KR102371417B1 (ko) 2017-04-11 2017-04-11 인삼 꽃대 추출물을 포함하는 항염증용 조성물

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CN111134321A (zh) * 2020-01-16 2020-05-12 张盛南 一种人参的加工方法

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KR102131917B1 (ko) 2018-11-22 2020-07-08 동의대학교 산학협력단 2-노나데카논을 포함하는 항염증용 조성물
KR20240040441A (ko) 2022-09-21 2024-03-28 한국해양과학기술원 검은지느러미 빙어 추출물 또는 에메랄드 암치 추출물을 유효성분으로 포함하는 항염증용 조성물

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