WO2022119230A1 - Anti-allergic composition using extract from persicaria longiseta - Google Patents

Anti-allergic composition using extract from persicaria longiseta Download PDF

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WO2022119230A1
WO2022119230A1 PCT/KR2021/017458 KR2021017458W WO2022119230A1 WO 2022119230 A1 WO2022119230 A1 WO 2022119230A1 KR 2021017458 W KR2021017458 W KR 2021017458W WO 2022119230 A1 WO2022119230 A1 WO 2022119230A1
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allergic
composition
extract
food
present
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PCT/KR2021/017458
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French (fr)
Korean (ko)
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안은경
홍성수
조영락
박기태
이지은
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재단법인 경기도경제과학진흥원
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Publication of WO2022119230A1 publication Critical patent/WO2022119230A1/en

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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)
    • A61K36/70—Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A23V2200/304—Foods, ingredients or supplements having a functional effect on health having a modulation effect on allergy and risk of allergy

Definitions

  • the present invention relates to a composition for anti-allergy using an extract of Gaeyeogwi ( Persicaria longiseta ).
  • Allergy is a compound word created by combining the Greek words 'allos' meaning 'change' and 'ergo' meaning 'action'.
  • an allergy refers to a hypersensitivity reaction such as urticaria, itchiness, runny nose, and cough in a specific person due to an abnormality in innate or acquired immune function to an allergen, a substance that does not show any reaction to ordinary people.
  • Typical allergens include pollen, drugs, vegetable fibers, bacteria, mold, house dust mites, food (eg, egg albumin, milk protein, peanuts), hair dye, and chemicals. Due to an increase in substances, environmental pollution, a decrease in immune function due to stress, and changes in diet, these allergic diseases are increasing worldwide.
  • Allergic reactions are classified into five types: type I anaphylaxis type, type II cytolytic type, type III immune complex type, type IV cell mediated type, and type V stimulatory hypersensitivity type, most of which belong to type I, and generally Allergic reaction is used in the same sense as type I (Roitt I, Brostoff J, Male D. Immunology 6th eds. U.S.A. Mosby. 2001:323-383).
  • Suitable allergic diseases include atopic dermatitis, bronchial asthma, allergic rhinitis, allergic keratitis, and skin urticaria.
  • mast cells are known as important effector cells (Wills-Karp M., et al., Science, 282:2258-61, 1998; Grunig G., et al., Science, 282:2261-2263, 1998).
  • Mast cells are cells that are widely distributed in organs throughout the body, such as the skin, respiratory system, lymphatic vessels, mucous membranes of the gastrointestinal tract, blood vessels, and brain (Ishizaka t., et al. J. Immunol. 119:1589, 1997).
  • Allergic reactions are induced through activation of intracellular signaling pathways when an allergen binds to IgE, which is bound to the IgE high affinity receptor (Fc ⁇ RI) on the surface of mast cells.
  • IgE IgE high affinity receptor
  • T-helper cells and B cells are sequentially activated to generate IgE.
  • Allergens that invade the living body are recognized by antigen-presenting cells, which differentiate Th0 (T helper cell type 0) into Th2 cells by presenting the allergen.
  • the differentiated Th2 cells secrete cytokines such as IL-4, IL-5, and IL-13, which promote the development of acid leukocytes in the bone marrow and induce acid leukocytes to the inflamed tissue, as well as B cells. It induces the production of IgE and IgG1.
  • the generated IgE binds to the high-affinity IgE receptor (FcRI ⁇ ) of the mast cell membrane, and when allergens such as mites and pollen bind to it and cross-link it, the receptor (FcRI ⁇ ) aggregates.
  • FcRI ⁇ high-affinity IgE receptor
  • the increase in calcium ion concentration acts on several types of intracellular regulators such as cholesterol in the cell membrane and the cytoskeleton system, and moves the granules to the cell membrane, and at the same time degranulation through vacuolization of granules, fusion of granules with each other, and fusion of granules with cell membranes. causes When degranulation occurs, preformed mediators stored in mast cells, such as histamine, are released and, at the same time, newly synthesized prostaglandin and leukotriene are secreted together.
  • intracellular regulators such as cholesterol in the cell membrane and the cytoskeleton system
  • Chemical transmitters liberated by degranulation include histamine, serotonin, and leukotriene, which have actions such as vasodilation, enhancement of vascular permeability, contraction or hypersecretion of bronchial smooth muscle, and NCF acting as a chemotactic factor of inflammatory cells such as eosinophils and neutrophils. , ECF, PAF, etc.
  • Cyclooxygenase (COX) and lipoxygenase (LO) are known to catalyze a part of the process of producing prostaglandins and leukotrienes, which are allergy symptom-causing substances, from arachidonic acid (Sekiya K , et al., Biochem Biophys Acta 713:68-72, 1982)
  • substances that inhibit the activation of mast cells, inhibit the release of histamine, or inhibit the synthesis of prostaglandins and leukotrienes can be effective therapeutic drugs for allergies.
  • anti-allergic drugs include antihistamines (alkylamines, desloratadine, etc.), mast cell stabilizers (cromoglycate, etc.), leukotriene blockers (montelukast, etc.), and anti-IgE antibody (Omalizumab).
  • antihistamines alkylamines, desloratadine, etc.
  • mast cell stabilizers cromoglycate, etc.
  • leukotriene blockers montelukast, etc.
  • anti-IgE antibody Optab
  • the present invention discloses anti-allergic activity of the extract
  • the present invention inhibits degranulation when treated with the mast cell line RBL-2H3 (rat basophilic leukemia) activated with IgE and antigen (DNP-BSA). It is completed by doing
  • the present invention can be identified as an anti-allergy composition or antihistamine composition comprising the extract of Gaejaekyi as an active ingredient.
  • the term "gaeyeogwi extract” refers to the stem, leaf, fruit, flower, root, outpost, above-ground part, underground part, or a mixture thereof, which is an extraction target, water, a lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, butanol, etc.) ), methylene chloride, ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol or It refers to an extract obtained by leaching using a mixed solvent, an extract obtained by using a supercritical extraction solvent such as carbon dioxide or pentane, or a fraction obtained by fractionating the extract, and the extraction method is the polarity of the active material, extraction degree, and preservation degree In consideration of this, any method such as chilling, reflux, warming, ultrasonic radiation,
  • the meaning of the extract includes a concentrated liquid extract or solid extract from which the extraction solvent is removed by methods such as freeze drying, vacuum drying, hot air drying, spray drying, and the like.
  • it refers to an extract obtained by using water, ethanol, or a mixed solvent thereof as an extraction solvent, and more preferably an extract obtained by using a mixed solvent of water and ethanol as an extraction solvent.
  • active ingredient refers to a component that alone exhibits the desired activity or can exhibit activity together with a carrier that has no activity by itself.
  • anti-allergy is meant to include improvement (relief of symptoms), treatment, and prevention (suppression or delay of onset) of allergic diseases as defined below.
  • allergic disease means a pathological symptom caused by an allergic reaction mediated by the activation of mast cells, such as degranulation of mast cells, and such allergic diseases include atopic dermatitis, asthma. , allergic rhinitis, allergic conjunctivitis, allergic dermatitis, allergic contact dermatitis, allergic keratitis, and the like.
  • the anti-allergic composition of the present invention may contain the active ingredient in any amount (effective amount) as long as it can exhibit the amelioration activity of the intended treatment according to the use, formulation, purpose of formulation, etc. It will be determined within the range of 0.001% to 15% by weight based on the total weight of the composition.
  • the term "effective amount” refers to the intended medical and pharmacological effects, such as the improvement of allergic diseases, when the composition of the present invention is administered to a mammal, preferably a human subject to the application, during the administration period as suggested by a medical professional. It refers to the amount of the active ingredient included in the composition of the present invention. Such an effective amount can be determined empirically within the ordinary ability of one of ordinary skill in the art.
  • the anti-allergic composition of the present invention may further include any compound or natural extract known to have anti-allergic activity and safety has already been verified to increase/reinforce anti-allergic activity.
  • Enterococcus faecalis heat-treated dry powder which has been individually recognized for its 'alleviation of hypersensitivity immune response' function according to the ⁇ Health Functional Food Act ⁇ in Korea
  • a complex such as guava leaf extract, Actinidia extract, leaf extract, Composite such as picaopreto powder, PLAG (1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol), L. sakei Probio 65, which has been individually recognized for its 'improving sensitive skin condition' function, oil containing gamma-linolenic acid , fruit and vegetable-derived lactic acid bacteria ( L. plantarum CJLP133 ), probiotics ATP, and the like.
  • One or more of these compounds or natural extracts may be included in the anti-allergic composition of the present invention together with its active ingredient.
  • the anti-allergic composition of the present invention can be grasped as a food composition.
  • the composition of the present invention is identified as a food composition, its use may be understood to inhibit allergic skin hypersensitivity reaction.
  • the food composition of the present invention can be prepared in any form, for example, beverages such as tea, juice, carbonated drinks, and ion drinks, processed oils such as milk and yogurt, gums, rice cakes, Korean sweets, bread, confectionery, noodles, etc. Foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jellies, and health functional food preparations such as bars can be manufactured.
  • beverages such as tea, juice, carbonated drinks, and ion drinks
  • processed oils such as milk and yogurt, gums, rice cakes, Korean sweets, bread, confectionery, noodles, etc.
  • Foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jellies, and health functional food preparations such as bars can be manufactured.
  • the food composition of the present invention may have any product classification in terms of legal and functional classification as long as it conforms to the enforcement laws at the time of manufacture and distribution.
  • it is a health functional food according to Korea's "Health Functional Food Act”, or confectionery, beans, tea, and beverages according to each food type in the Food Ordinance of Korea “Food Sanitation Act” (Ministry of Food and Drug Safety Notification “Food Standards and Specifications”) , special purpose food, and the like.
  • the food composition of the present invention may contain food additives in addition to the active ingredients thereof.
  • Food additives can be generally understood as substances that are mixed or infiltrated with food in manufacturing, processing, or preserving food. Food additives with guaranteed safety are limited in terms of ingredients or functions in the Food Additives Ordinance in accordance with the laws of each country that regulates the manufacture and distribution of food (“Food Sanitation Act” in Korea). In the Korean Food Additives Code (“Food Additive Standards and Specifications” notified by the Ministry of Food and Drug Safety), food additives are classified into chemically synthetic products, natural additives, and mixed preparations in terms of ingredients. It is classified into an agent, a preservative, an emulsifier, an acidulant, and a thickener.
  • the sweetener is used to impart appropriate sweetness to food, and both natural and synthetic ones may be used in the composition of the present invention.
  • a natural sweetener is used.
  • sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.
  • Flavoring agents may be used to improve taste or aroma, and both natural and synthetic ones may be used. Preferably, it is a case where a natural thing is used. In the case of using a natural product, the purpose of nutritional enhancement in addition to flavor may be concurrently used.
  • the natural flavoring agent may be obtained from apples, lemons, tangerines, grapes, strawberries, peaches, or the like, or obtained from green tea leaves, honeysuckle, bamboo leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. In addition, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, and ginkgo can be used.
  • the natural flavoring agent may be a liquid concentrate or a solid extract.
  • a synthetic flavoring agent may be used, and the synthetic flavoring agent may be an ester, an alcohol, an aldehyde, a terpene, or the like.
  • sodium calcium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate, EDTA (ethylenediaminetetraacetic acid), etc. can be used, and as an emulsifier, acacia gum, carboxymethylcellulose, xanthan gum, Pectin, etc. are mentioned, and acidulant, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid, etc. can be used as an acidulant.
  • the acidulant may be added so that the food composition has an appropriate acidity for the purpose of inhibiting the growth of microorganisms in addition to the purpose of enhancing the taste.
  • a thickening agent As a thickening agent, a suspending agent, a settling agent, a gel former, a bulking agent, etc. can be used.
  • the food composition of the present invention may contain, in addition to the food additives described above, physiologically active substances or minerals known in the art for the purpose of supplementing and reinforcing functionality and nutrition and guaranteed stability as food additives.
  • physiologically active substances include catechins contained in green tea and the like, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoylthiamine, and the like.
  • Minerals include calcium preparations such as calcium citrate, magnesium stearate
  • Magnesium preparations, such as iron preparations, such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, zinc, etc. are mentioned.
  • the food additives as described above may be included in an appropriate amount to achieve the purpose of the addition according to the product type.
  • composition of the present invention may be regarded as a pharmaceutical composition in another specific embodiment.
  • the pharmaceutical composition of the present invention may be prepared as an oral dosage form or a parenteral dosage form according to the route of administration by a conventional method known in the art, including a pharmaceutically acceptable carrier in addition to the active ingredient.
  • the route of administration may be any suitable route including topical route, oral route, intravenous route, intramuscular route, and direct absorption through mucosal tissue, and two or more routes may be used in combination.
  • An example of the combination of two or more routes is a case in which two or more formulations of drugs according to the route of administration are combined. For example, one drug is first administered by an intravenous route and the other drug is secondarily administered by a local route.
  • Pharmaceutically acceptable carriers are well known in the art depending on the route of administration or formulation, and specifically, reference may be made to the pharmacopoeia of each country including the "Korea Pharmacopoeia”.
  • suitable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, Cellulose such as hydroxypropylmethylcellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable oil, ethanol, glycerol and the like.
  • suitable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, Cellulose such as hydroxypropylmethylcellulose, polyvinylpyr
  • an appropriate binder, lubricant, disintegrant, colorant, diluent, etc. may be included as needed.
  • Suitable binders include starch, magnesium aluminum silicate, starch paste, gelatin, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, glucose, corn sweetener, sodium alginate, polyethylene glycol, wax, and the like, and lubricants include sodium oleate.
  • the disintegrant includes starch, methyl cellulose, agar, bentonite, xanthan gum, starch, alginic acid or its sodium salt and the like.
  • the diluent include lactose, dextrose, sucrose, mannitol, sorbitol, cellulose, and glycine.
  • the pharmaceutical composition of the present invention When the pharmaceutical composition of the present invention is prepared for parenteral use, it may be formulated in the form of injections, transdermal administrations, nasal inhalants and suppositories together with suitable carriers according to methods known in the art.
  • suitable carriers for aqueous isotonic solution or suspension
  • PBS phosphate buffered saline
  • isotonic solution such as 5% dextrose
  • formulated for transdermal administration When formulated for transdermal administration, it can be formulated in the form of an ointment, a cream, a lotion, a gel, an external solution, a pasta agent, a liniment agent, an air roll, and the like.
  • a suitable propellant such as dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, and the like.
  • tween 61 polyethylene glycols, cacao fat, laurin fat, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearate, sorbitan fatty acid esters, and the like can be used.
  • a preferred dosage of the pharmaceutical composition of the present invention is in the range of 0.001 mg/kg to 10 g/kg per day, preferably 0.001 mg/kg to 1 g, depending on the patient's condition, weight, sex, age, severity of the patient, and the route of administration. It can be in the range /kg. Administration may be performed once or divided into several times a day. These dosages should not be construed as limiting the scope of the invention in any respect.
  • the composition of the present invention can be identified as a cosmetic composition.
  • a cosmetic composition its use may be understood as a use for suppressing allergic skin troubles, alleviating allergic skin irritation, and the like.
  • the cosmetic composition can be classified into any product in terms of its use or by law, and specifically functional cosmetics, non-functional products having uses such as improvement of skin troubles and improvement of atopic dermatitis It may be general cosmetics and the like.
  • product form it may take any product form, and specifically, solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax It can take the form of products such as foundation and spray.
  • it may be in the form of a flexible lotion, a nourishing lotion, a nourishing 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 cosmetic composition of the present invention may include components commonly used in cosmetic compositions in addition to the active ingredient, for example, conventional adjuvants such as stabilizers, solubilizers, surfactants, vitamins, pigments and fragrances, and carriers.
  • conventional adjuvants such as stabilizers, solubilizers, surfactants, vitamins, pigments and fragrances, and carriers.
  • 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.
  • lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component.
  • a solvent, solubilizer or emulsifier is used as a carrier component, specifically water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol, fatty acid ester of sorbitan, etc. may be used.
  • the formulation of the present invention is a suspension
  • a liquid diluent such as water, ethanol or propylene glycol
  • a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, polyoxyethylene sorbitan ester, microcrystals
  • cellulose aluminum metahydroxide, bentonite, agar, etc.
  • the formulation of the present invention is a surfactant-containing cleansing agent
  • Ether sulfate, alkylamidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester and the like may be used.
  • the cosmetic composition of the present invention can be prepared according to the method for preparing a cosmetic composition conventionally performed in the art, except that it contains the active ingredient exhibiting anti-allergic activity.
  • composition for anti-allergy of the present invention may be commercialized as food, cosmetics, drugs, etc. for the purpose of improving allergic diseases.
  • FIG. 1 is a result showing the degranulation inhibitory activity in the mast cell line RBL-2H3 (rat basophilic leukemia) activated with IgE and antigen (DNP-BSA) of Gaeyeogwi extract.
  • Rat basophilic leukemia cell line RBL-2H3 cell line, in MEM medium containing 15% FBS, 100 unit/ml penicillin and streptomycin and 2 ⁇ 10 5 /well in a 24 well plate at 37°C and 5% CO 2 condition. After dispensing, culture was performed for 24 hours.
  • MEM medium containing 25 ng/ml anti-DNP IgE was added and cultured for 4 hours. After incubation, the cells were washed twice with PIPES buffer (25mM PIPES, 119mM NaCl, 5mM KCl, 1mM CaCl 2 , 0.4mM MgCl 2 , 40mM NaOH, 5.6mM glucose, 0.1% BSA) and pre-incubated for 10 minutes. After pre-incubation, the samples of Example were treated for 20 minutes by concentration and then reacted with DNP-BSA for 20 minutes.
  • PIPES buffer 25mM PIPES, 119mM NaCl, 5mM KCl, 1mM CaCl 2 , 0.4mM MgCl 2 , 40mM NaOH, 5.6mM glucose, 0.1% BSA
  • Ketotifen used as a positive control, is an antihistamine, which is used for allergic skin diseases such as allergic rhinitis, atopic dermatitis, and allergic asthma.

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Abstract

Disclosed is an anti-allergic composition using an extract from Persicaria longiseta, the extract having degranulation-suppressing activity when used on rat basophilic leukemia (RBL-2H3), which is an obesity cell line activated by IgE and antigen (DNP-BSA).

Description

개여뀌 추출물을 이용한 항알러지용 조성물Composition for anti-allergy using extract
본 발명은 개여뀌(Persicaria longiseta) 추출물을 이용한 항알러지용 조성물에 관한 것이다.The present invention relates to a composition for anti-allergy using an extract of Gaeyeogwi ( Persicaria longiseta ).
알러지(Allergy)는 그리스어의 '변한다'는 의미의 'allos'와 '작용'의 의미인 'ergo'가 결합되어 생성된 합성어로 생체 이상 반응의 뜻을 가지고 있다. 어원이 이러하듯, 알러지는 보통 사람에게는 아무런 반응도 나타내지 않은 물질인 알러지원(allergen)이 선천적 또는 후천적 면역기능의 이상으로 특정 사람에는 두드러기, 가려움, 콧물, 기침 등의 과민반응을 일으키는 것을 말한다. 전형적인 알러지원은 꽃가루, 약물, 식물성 섬유, 세균, 곰팡이, 집먼지진드기, 음식물(난알부민, 우유단백질, 땅콩), 염색약, 화학 물질 등이 있으며, 최근 실내 생활의 증가, 신소재 화학물질 등과 같은 알러지 유발 물질의 증가, 환경오염, 스트레스로 인한 면역기능 저하, 그리고 식생활의 변화 등으로 이러한 알러지 질환은 전세계적으로 증가하고 있는 추세이다. Allergy is a compound word created by combining the Greek words 'allos' meaning 'change' and 'ergo' meaning 'action'. As the etymology is like this, an allergy refers to a hypersensitivity reaction such as urticaria, itchiness, runny nose, and cough in a specific person due to an abnormality in innate or acquired immune function to an allergen, a substance that does not show any reaction to ordinary people. Typical allergens include pollen, drugs, vegetable fibers, bacteria, mold, house dust mites, food (eg, egg albumin, milk protein, peanuts), hair dye, and chemicals. Due to an increase in substances, environmental pollution, a decrease in immune function due to stress, and changes in diet, these allergic diseases are increasing worldwide.
알러지 반응은 Ⅰ형 anaphylaxis형, Ⅱ형 세포용해형, Ⅲ형 면역복합체형, Ⅳ형 세포중개형, Ⅴ형 자극성 과민반응형의 5가지 유형으로 분류되는데, 대부분은 제Ⅰ형에 속하며, 일반적으로 알러지 반응이라 하면 제Ⅰ형과 동일한 의미로 사용된다(Roitt I, Brostoff J, Male D. Immunology 6th eds. U.S.A.. Mosby. 2001:323-383). Allergic reactions are classified into five types: type I anaphylaxis type, type II cytolytic type, type III immune complex type, type IV cell mediated type, and type V stimulatory hypersensitivity type, most of which belong to type I, and generally Allergic reaction is used in the same sense as type I (Roitt I, Brostoff J, Male D. Immunology 6th eds. U.S.A. Mosby. 2001:323-383).
대표적인 알러지 질환으로는 아토피성 피부염, 기관지 천식, 알러지성 비염, 알러지성 각막염, 피부 두드러기 등이 있으며, 이들 알러지 질환에는 비만세포(mast cell)가 중요한 작동세포로 알려져 있다(Wills-Karp M., et al., Science, 282:2258-61, 1998; Grunig G., et al., Science, 282:2261-2263, 1998). 비만세포는 피부, 호흡기, 림프관 주위, 위장관의 점막, 혈관 주위, 뇌 등 전신의 장기에 널리 분포하고 있는 세포이다(Ishizaka t., et al. J. Immunol. 119:1589, 1997).Representative allergic diseases include atopic dermatitis, bronchial asthma, allergic rhinitis, allergic keratitis, and skin urticaria. In these allergic diseases, mast cells are known as important effector cells (Wills-Karp M., et al., Science, 282:2258-61, 1998; Grunig G., et al., Science, 282:2261-2263, 1998). Mast cells are cells that are widely distributed in organs throughout the body, such as the skin, respiratory system, lymphatic vessels, mucous membranes of the gastrointestinal tract, blood vessels, and brain (Ishizaka t., et al. J. Immunol. 119:1589, 1997).
알러지 반응은 이러한 비만세포 표면의 IgE 고친화성 수용체 (FcεRI)에 결합되어 있는 IgE에 알러지원이 결합할 때 세포내 신호전달경로의 활성화를 통해 유도된다. 구체적으로 알러지원이 생체에 침입하면 T-조력세포(T-helper cell)와 B 세포가 순차적으로 활성화되어 IgE가 생성된다. 생체에 침입한 알러지원은 항원제시세포에 의해 인지되며, 이 항원제시세포는 알러지원 제시를 통해 Th0(T helper cell type 0)를 Th2 세포로 분화시킨다. 이렇게 분화된 Th2 세포는 IL-4, IL-5 및 IL-13과 같은 사이토카인을 분비하며, 이들은 골수에서의 산성백혈구 발달을 촉진시켜 염증이 발생한 조직으로 산성백혈구를 유도할 뿐만 아니라, B세포에 작용하여 IgE 및 IgG1의 생성을 유도한다.Allergic reactions are induced through activation of intracellular signaling pathways when an allergen binds to IgE, which is bound to the IgE high affinity receptor (FcεRI) on the surface of mast cells. Specifically, when an allergen invades a living body, T-helper cells and B cells are sequentially activated to generate IgE. Allergens that invade the living body are recognized by antigen-presenting cells, which differentiate Th0 (T helper cell type 0) into Th2 cells by presenting the allergen. The differentiated Th2 cells secrete cytokines such as IL-4, IL-5, and IL-13, which promote the development of acid leukocytes in the bone marrow and induce acid leukocytes to the inflamed tissue, as well as B cells. It induces the production of IgE and IgG1.
이렇게 생성된 IgE는 비만세포막의 고친화성 IgE 수용체(FcRIα)에 결합하고 여기에 진드기, 꽃가루 등의 알러지원이 결합하여 가교를 이루면 수용체 (FcRIα)가 응집한다. 수용체(FcRIα)의 가교 및 응집에 의하여 비만세포는 활성화되어 세포질 내의 칼슘이온(Ca++) 농도 등이 상승한다. 칼슘이온 농도의 상승은 세포막의 콜레스테롤이나 세포골격계 등 여러 종류의 세포 내 조절인자에 작용하여 과립을 세포막에 이동시킴과 동시에 과립의 공포화, 과립 상호의 융합 및 과립과 세포막의 융합 등을 거쳐 탈과립을 일으킨다. 탈과립이 되면 히스타민(histamine)과 같이 비만세포 내에 미리 저장되어 있는 화학전달물질(preformed mediator)이 유리됨과 동시에 새로 합성된 프로스타글란딘(prostaglandin), 류코트리엔(leukotriene) 등이 함께 분비된다. 탈과립으로 유리되는 화학전달물질에는 혈관확장, 혈관투과성 항진, 기관지 평활근의 수축이나 분비항진 등의 작용을 갖는 히스타민, 세로토닌(serotonin) 및 류코트리엔 이외에 호산구나 호중구등 염증 세포의 주화성 인자로 작용하는 NCF, ECF, PAF등이 있어서 알러지 반응이 일어나게 된다(Ennis M, et al., Br J Pharmacol 70:329-334, 1980; Metcalfe DD, et al., Crit Rev Immunol 3:23-74, 1981; Miyajima I, et al., J Clin Invest 99:901-914, 1997; Church MK, et al., J Allergy Clin Immunol 99:155-160, 1997; Jones DA, et al., J Biol Chem 268:9049-9054, 1993).The generated IgE binds to the high-affinity IgE receptor (FcRIα) of the mast cell membrane, and when allergens such as mites and pollen bind to it and cross-link it, the receptor (FcRIα) aggregates. By crosslinking and aggregation of the receptor (FcRIα), mast cells are activated and the concentration of calcium ions (Ca ++ ) in the cytoplasm, etc. rises. The increase in calcium ion concentration acts on several types of intracellular regulators such as cholesterol in the cell membrane and the cytoskeleton system, and moves the granules to the cell membrane, and at the same time degranulation through vacuolization of granules, fusion of granules with each other, and fusion of granules with cell membranes. causes When degranulation occurs, preformed mediators stored in mast cells, such as histamine, are released and, at the same time, newly synthesized prostaglandin and leukotriene are secreted together. Chemical transmitters liberated by degranulation include histamine, serotonin, and leukotriene, which have actions such as vasodilation, enhancement of vascular permeability, contraction or hypersecretion of bronchial smooth muscle, and NCF acting as a chemotactic factor of inflammatory cells such as eosinophils and neutrophils. , ECF, PAF, etc. cause an allergic reaction (Ennis M, et al., Br J Pharmacol 70:329-334, 1980; Metcalfe DD, et al., Crit Rev Immunol 3:23-74, 1981; Miyajima I, et al., J Clin Invest 99:901-914, 1997; Church MK, et al., J Allergy Clin Immunol 99:155-160, 1997; Jones DA, et al., J Biol Chem 268:9049- 9054, 1993).
사이클로옥시게나제(cyclooxygenase, COX)와 리폭시게나제(lipoxygenase, LO)는 아라키돈산(arachidonic acid)으로부터 알러지 증상 유발 물질인 프로스타글란딘류와 류코트리엔류를 만들어내는 과정의 일부를 촉매한다고 알려져 있다(Sekiya K, et al., Biochem Biophys Acta 713:68-72, 1982)Cyclooxygenase (COX) and lipoxygenase (LO) are known to catalyze a part of the process of producing prostaglandins and leukotrienes, which are allergy symptom-causing substances, from arachidonic acid (Sekiya K , et al., Biochem Biophys Acta 713:68-72, 1982)
따라서 비만세포의 활성화를 억제하거나, 히스타민 방출을 억제하거나 프로스타글란딘류와 류코트리엔류의 합성을 억제하는 물질 등은 알러지의 유효한 치료약이 될 수 있다.Therefore, substances that inhibit the activation of mast cells, inhibit the release of histamine, or inhibit the synthesis of prostaglandins and leukotrienes can be effective therapeutic drugs for allergies.
현재 항알러지 약물로서는 항히스타민제(alkylamines, desloratadine 등), 비만세포 안정화제(cromoglycate 등), 류코트리엔 차단제(montelukast 등), 항-IgE 항체(Omalizumab) 등이 사용되고 있다. 그러나 이러한 약물은 그 효과가 일시적인 경우가 대부분이고 부작용이 심한 경우도 많다. 따라서 알러지 질환의 예방 및 개선효과를 가지면서 부작용이 적고 효과가 지속적인 새로운 물질의 개발이 여전히 필요하다고 할 수 있으며, 특히 천연물은 상대적으로 독성이 적은 장점을 가진다.Currently, anti-allergic drugs include antihistamines (alkylamines, desloratadine, etc.), mast cell stabilizers (cromoglycate, etc.), leukotriene blockers (montelukast, etc.), and anti-IgE antibody (Omalizumab). However, in most cases, the effect of these drugs is temporary and the side effects are severe in many cases. Therefore, it can be said that there is still a need to develop a new substance that has a preventive and ameliorating effect on allergic diseases, few side effects and a continuous effect, and in particular, natural products have the advantage of relatively low toxicity.
본 발명은 개여뀌 추출물의 항알러지 활성을 개시한다.The present invention discloses anti-allergic activity of the extract
본 발명의 목적은 개여뀌 추출물을 이용한 항알러지용 조성물을 제공하는 데 있다.It is an object of the present invention to provide a composition for anti-allergy using the extract
본 발명의 다른 목적이나 구체적인 목적은 이하에서 제시될 것이다.Other objects or specific objects of the present invention will be set forth below.
본 발명은 아래의 실시예 및 실험예에서 확인되는 바와 같이, 개여뀌 추출물이 IgE 및 항원(DNP-BSA)으로 활성화된 비만세포주 RBL-2H3(rat basophilic leukemia)에 처리될 때 탈과립을 억제함을 확인함으로써 완성된 것이다.As confirmed in the Examples and Experimental Examples below, it was confirmed that the present invention inhibits degranulation when treated with the mast cell line RBL-2H3 (rat basophilic leukemia) activated with IgE and antigen (DNP-BSA). It is completed by doing
전술한 바를 고려할 때, 본 발명은 개여뀌 추출물을 유효성분으로 포함하는 항알러지용 조성물 또는 항히스타민 조성물로 파악할 수 있다.In consideration of the above, the present invention can be identified as an anti-allergy composition or antihistamine composition comprising the extract of Gaejaekyi as an active ingredient.
본 명세서에서, "개여뀌 추출물"이란 추출 대상인 개여뀌의 줄기, 잎, 열매, 꽃, 뿌리, 전초, 지상부, 지하부, 또는 이들의 혼합물을 물, 탄소수 1 내지 4의 저급 알콜(메탄올, 에탄올, 부탄올 등), 메틸렌클로라이드, 에틸렌, 아세톤, 헥산, 에테르, 클로로포름, 에틸아세테이트, 부틸아세테이트, N,N-디메틸포름아미드(DMF), 디메틸설폭사이드(DMSO), 1,3-부틸렌글리콜, 프로필렌글리콜 또는 이들의 혼합 용매를 사용하여 침출하여 얻어진 추출물, 이산화탄소, 펜탄 등 초임계 추출 용매를 사용하여 얻어진 추출물 또는 그 추출물을 분획하여 얻어진 분획물을 의미하며, 추출 방법은 활성물질의 극성, 추출 정도, 보존 정도를 고려하여 냉침, 환류, 가온, 초음파 방사, 초임계 추출 등 임의의 방법을 적용할 수 있다. 분획된 추출물의 경우 추출물을 특정 용매에 현탁시킨 후 극성이 다른 용매와 혼합·정치시켜 얻은 분획물, 상기 조추출물을 실리카겔 등이 충진된 칼럼에 흡착시킨 후 소수성 용매, 친수성 용매 또는 이들의 혼합 용매를 이동상으로 하여 얻은 분획물을 포함하는 의미이다. 또한 상기 추출물의 의미에는 동결건조, 진공건조, 열풍건조, 분무건조 등의 방식으로 추출 용매가 제거된 농축된 액상의 추출물 또는 고형상의 추출물이 포함된다. 바람직하게는 추출용매로서 물, 에탄올 또는 이들의 혼합 용매를 사용하여 얻어진 추출물, 더 바람직하게는 추출용매로서 물과 에탄올의 혼합 용매를 사용하여 얻어진 추출물을 의미한다.In the present specification, the term "gaeyeogwi extract" refers to the stem, leaf, fruit, flower, root, outpost, above-ground part, underground part, or a mixture thereof, which is an extraction target, water, a lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, butanol, etc.) ), methylene chloride, ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol or It refers to an extract obtained by leaching using a mixed solvent, an extract obtained by using a supercritical extraction solvent such as carbon dioxide or pentane, or a fraction obtained by fractionating the extract, and the extraction method is the polarity of the active material, extraction degree, and preservation degree In consideration of this, any method such as chilling, reflux, warming, ultrasonic radiation, and supercritical extraction can be applied. In the case of the fractionated extract, a fraction obtained by suspending the extract in a specific solvent and mixing and standing still with a solvent having a different polarity, and adsorbing the crude extract to a column filled with silica gel, etc. It is meant to include the fraction obtained as a mobile phase. In addition, the meaning of the extract includes a concentrated liquid extract or solid extract from which the extraction solvent is removed by methods such as freeze drying, vacuum drying, hot air drying, spray drying, and the like. Preferably, it refers to an extract obtained by using water, ethanol, or a mixed solvent thereof as an extraction solvent, and more preferably an extract obtained by using a mixed solvent of water and ethanol as an extraction solvent.
또 본 명세서에서 "유효성분"이란 단독으로 목적하는 활성을 나타내거나 또는 그 자체는 활성이 없는 담체와 함께 활성을 나타낼 수 있는 성분을 의미한다.In addition, as used herein, the term "active ingredient" refers to a component that alone exhibits the desired activity or can exhibit activity together with a carrier that has no activity by itself.
또 본 명세서에서, "항알러지"는 아래에서 정의되는 알러지 질환의 개선(증상의 경감), 치료, 그러한 질환의 예방(발병 억제 또는 지연)을 포함하는 의미이다.In addition, in the present specification, "anti-allergy" is meant to include improvement (relief of symptoms), treatment, and prevention (suppression or delay of onset) of allergic diseases as defined below.
또 본 명세서에서, "알러지 질환"은 비만세포의 탈과립 등 비만세포의 활성화가 매개된 알러지 반응으로 인하여 초래되는 병리적 증상을 의미하며, 이러한 알러지 질환에는 아토피 피부염(atopic dermatitis), 천식(asthma), 알러지성 비염(allergic rhinitis), 알러지성 결막염(allergic conjunctivitis), 알러지성 피부염(allergic dermatitis), 알러지성 접촉성 피부염(allergic contact dermatitis), 알러지성 각막염 등이 포함된다. In addition, in the present specification, "allergic disease" means a pathological symptom caused by an allergic reaction mediated by the activation of mast cells, such as degranulation of mast cells, and such allergic diseases include atopic dermatitis, asthma. , allergic rhinitis, allergic conjunctivitis, allergic dermatitis, allergic contact dermatitis, allergic keratitis, and the like.
본 발명의 항알러지 조성물은 그 유효성분을 용도, 제형, 배합 목적 등에 따라 치료를 의도하는 알러지 질환의 개선 활성 등을 나타낼 수 있는 한 임의의 양(유효량)으로 포함할 수 있는데, 통상적인 유효량은 조성물 전체 중량을 기준으로 할 때 0.001 중량 % 내지 15 중량 % 범위 내에서 결정될 것이다. 여기서 "유효량"이란 그 적용 대상인 포유동물 바람직하게는 사람에게 의료 전문가 등의 제언에 의한 투여 기간 동안 본 발명의 조성물이 투여될 때, 알러지 질환의 개선 효과 등 의도한 의료적·약리학적 효과를 나타낼 수 있는, 본 발명의 조성물에 포함되는 유효성분의 양을 말한다. 이러한 유효량은 당업자의 통상의 능력 범위 내에서 실험적으로 결정될 수 있다.The anti-allergic composition of the present invention may contain the active ingredient in any amount (effective amount) as long as it can exhibit the amelioration activity of the intended treatment according to the use, formulation, purpose of formulation, etc. It will be determined within the range of 0.001% to 15% by weight based on the total weight of the composition. Herein, the term "effective amount" refers to the intended medical and pharmacological effects, such as the improvement of allergic diseases, when the composition of the present invention is administered to a mammal, preferably a human subject to the application, during the administration period as suggested by a medical professional. It refers to the amount of the active ingredient included in the composition of the present invention. Such an effective amount can be determined empirically within the ordinary ability of one of ordinary skill in the art.
본 발명의 항알러지 조성물은 유효성분 이외에, 항알러지 활성의 상승·보강을 위하여 이미 안전성이 검증되고 항알러지 활성을 갖는 것으로 공지된 임의의 화합물이나 천연 추출물을 추가로 포함할 수 있다. In addition to the active ingredient, the anti-allergic composition of the present invention may further include any compound or natural extract known to have anti-allergic activity and safety has already been verified to increase/reinforce anti-allergic activity.
구체적으로 그러한 화합물 또는 추출물로서는 한국 「건강기능식품에관한법률」에 따라 '과민 면역반응 완화' 기능성으로 개별인정을 받은 Enterococcus faecalis 가열 처리 건조 분말, 구아바 잎 추출물 등의 복합물, 다래 추출물, 소엽 추출물, 피카오프레토 분말 등의 복합물, PLAG(1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol)와, '과민 피부상태 개선' 기능성으로 개별인정을 받은 L. sakei Probio 65, 감마리놀렌산 함유 유지, 과채 유래 유산균(L.plantarum CJLP133), 프로바이오틱스 ATP 등을 들 수 있다.Specifically, as such a compound or extract, Enterococcus faecalis heat-treated dry powder, which has been individually recognized for its 'alleviation of hypersensitivity immune response' function according to the 「Health Functional Food Act」 in Korea, a complex such as guava leaf extract, Actinidia extract, leaf extract, Composite such as picaopreto powder, PLAG (1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol), L. sakei Probio 65, which has been individually recognized for its 'improving sensitive skin condition' function, oil containing gamma-linolenic acid , fruit and vegetable-derived lactic acid bacteria ( L. plantarum CJLP133 ), probiotics ATP, and the like.
이러한 화합물 또는 천연 추출물은 본 발명의 항알러지 조성물에 그 유효성분과 함께 하나 이상 포함될 수 있다.One or more of these compounds or natural extracts may be included in the anti-allergic composition of the present invention together with its active ingredient.
본 발명의 항알러지 조성물은 구체적인 양태에 있어서, 식품 조성물로서 파악할 수 있다. 본 발명의 조성물이 식품 조성물로 파악될 경우 그 용도는 알러지성 피부 과민 반응 억제로 이해될 수 있다.In a specific embodiment, the anti-allergic composition of the present invention can be grasped as a food composition. When the composition of the present invention is identified as a food composition, its use may be understood to inhibit allergic skin hypersensitivity reaction.
본 발명의 식품 조성물은 어떠한 형태로도 제조될 수 있으며, 예컨대 차, 쥬스, 탄산음료, 이온음료 등의 음료류, 우유, 요구르트 등의 가공 유류, 껌류, 떡, 한과, 빵, 과자, 면 등의 식품류, 정제, 캡슐, 환, 과립, 액상, 분말, 편상, 페이스트상, 시럽, 겔, 젤리, 바 등의 건강기능식품 제제류 등으로 제조될 수 있다. The food composition of the present invention can be prepared in any form, for example, beverages such as tea, juice, carbonated drinks, and ion drinks, processed oils such as milk and yogurt, gums, rice cakes, Korean sweets, bread, confectionery, noodles, etc. Foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jellies, and health functional food preparations such as bars can be manufactured.
또 본 발명의 식품 조성물은 법률상·기능상의 구분에 있어서 제조·유통 시점의 시행 법규에 부합하는 한 임의의 제품 구분을 띨 수 있다. 예컨대 한국 「건강기능식품에관한법률」에 따른 건강기능식품이거나, 한국 「식품위생법」의 식품공전(식약처 고시 「식품의 기준 및 규격」)상 각 식품유형에 따른 과자류, 두류, 다류, 음료류, 특수용도식품 등일 수 있다.In addition, the food composition of the present invention may have any product classification in terms of legal and functional classification as long as it conforms to the enforcement laws at the time of manufacture and distribution. For example, it is a health functional food according to Korea's "Health Functional Food Act", or confectionery, beans, tea, and beverages according to each food type in the Food Ordinance of Korea "Food Sanitation Act" (Ministry of Food and Drug Safety Notification "Food Standards and Specifications") , special purpose food, and the like.
본 발명의 식품 조성물에는 그 유효성분 이외에 식품첨가물이 포함될 수 있다. 식품첨가물은 일반적으로 식품을 제조, 가공 또는 보존함에 있어 식품에 첨가되어 혼합되거나 침윤되는 물질로서 이해될 수 있는데, 식품과 함께 매일 그리고 장기간 섭취되므로 그 안전성이 보장되어야 한다. 식품의 제조·유통을 규율하는 각국 법률(한국에서는 「식품위생법」임)에 따른 식품첨가물공전에는 안전성이 보장된 식품첨가물이 성분 면에서 또는 기능 면에서 한정적으로 규정되어 있다. 한국 식품첨가물공전(식약처 고시 「식품첨가물 기준 및 규격」)에서는 식품첨가물이 성분 면에서 화학적 합성품, 천연 첨가물 및 혼합 제제류로 구분되어 규정되어 있는데, 이러한 식품첨가물은 기능 면에 있어서는 감미제, 풍미제, 보존제, 유화제, 산미료, 점증제 등으로 구분된다. The food composition of the present invention may contain food additives in addition to the active ingredients thereof. Food additives can be generally understood as substances that are mixed or infiltrated with food in manufacturing, processing, or preserving food. Food additives with guaranteed safety are limited in terms of ingredients or functions in the Food Additives Ordinance in accordance with the laws of each country that regulates the manufacture and distribution of food (“Food Sanitation Act” in Korea). In the Korean Food Additives Code (“Food Additive Standards and Specifications” notified by the Ministry of Food and Drug Safety), food additives are classified into chemically synthetic products, natural additives, and mixed preparations in terms of ingredients. It is classified into an agent, a preservative, an emulsifier, an acidulant, and a thickener.
감미제는 식품에 적당한 단맛을 부여하기 위하여 사용되는 것으로, 천연의 것이거나 합성된 것 모두 본 발명의 조성물에 사용할 수 있다. 바람직하게는 천연 감미제를 사용하는 경우인데, 천연 감미제로서는 옥수수 시럽 고형물, 꿀, 수크로오스, 프룩토오스, 락토오스, 말토오스 등의 당 감미제를 들 수 있다. The sweetener is used to impart appropriate sweetness to food, and both natural and synthetic ones may be used in the composition of the present invention. Preferably, a natural sweetener is used. Examples of the natural sweetener include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.
풍미제는 맛이나 향을 좋게 하기 위하여 사용될 수 있는데, 천연의 것과 합성된 것 모두 사용될 수 있다. 바람직하게는 천연의 것을 사용하는 경우이다. 천연의 것을 사용할 경우에 풍미 이외에 영양 강화의 목적도 병행할 수 있다. 천연 풍미제로서는 사과, 레몬, 감귤, 포도, 딸기, 복숭아 등에서 얻어진 것이거나 녹차잎, 둥굴레, 댓잎, 계피, 국화 잎, 자스민 등에서 얻어진 것일 수 있다. 또 인삼(홍삼), 죽순, 알로에 베라, 은행 등에서 얻어진 것을 사용할 수 있다. 천연 풍미제는 액상의 농축액이나 고형상의 추출물일 수 있다. 경우에 따라서 합성 풍미제가 사용될 수 있는데, 합성 풍미제는 에스테르, 알콜, 알데하이드, 테르펜 등이 이용될 수 있다. Flavoring agents may be used to improve taste or aroma, and both natural and synthetic ones may be used. Preferably, it is a case where a natural thing is used. In the case of using a natural product, the purpose of nutritional enhancement in addition to flavor may be concurrently used. The natural flavoring agent may be obtained from apples, lemons, tangerines, grapes, strawberries, peaches, or the like, or obtained from green tea leaves, honeysuckle, bamboo leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. In addition, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, and ginkgo can be used. The natural flavoring agent may be a liquid concentrate or a solid extract. Optionally, a synthetic flavoring agent may be used, and the synthetic flavoring agent may be an ester, an alcohol, an aldehyde, a terpene, or the like.
보존제로서는 소듐 소르브산칼슘, 소르브산나트륨, 소르브산칼륨, 벤조산칼슘, 벤조산나트륨, 벤조산칼륨, EDTA(에틸렌디아민테트라아세트산) 등이 사용될 수 있고, 또 유화제로서는 아카시아검, 카르복시메틸셀룰로스, 잔탄검, 펙틴 등을 들 수 있으며, 산미료로서는 연산, 말산, 푸마르산, 아디프산, 인산, 글루콘산, 타르타르산, 아스코르브산, 아세트산, 인산 등이 사용될 수 있다. 산미료는 맛을 증진시키는 목적 이외에 미생물의 증식을 억제할 목적으로 식품 조성물이 적정 산도로 되도록 첨가될 수 있다.As a preservative, sodium calcium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate, EDTA (ethylenediaminetetraacetic acid), etc. can be used, and as an emulsifier, acacia gum, carboxymethylcellulose, xanthan gum, Pectin, etc. are mentioned, and acidulant, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid, etc. can be used as an acidulant. The acidulant may be added so that the food composition has an appropriate acidity for the purpose of inhibiting the growth of microorganisms in addition to the purpose of enhancing the taste.
점증제로서는 현탁화 구현제, 침강제, 겔 형성제, 팽화제 등이 사용될 수 있다.As a thickening agent, a suspending agent, a settling agent, a gel former, a bulking agent, etc. can be used.
본 발명의 식품 조성물은 전술한 바의 식품첨가물 이외에, 기능성과 영양성을 보충, 보강할 목적으로 당업계에 공지되고 식품첨가물로서 안정성이 보장된 생리활성 물질이나 미네랄류를 포함할 수 있다.The food composition of the present invention may contain, in addition to the food additives described above, physiologically active substances or minerals known in the art for the purpose of supplementing and reinforcing functionality and nutrition and guaranteed stability as food additives.
그러한 생리활성 물질로서는 녹차 등에 포함된 카테킨류, 비타민 B1, 비타민 C, 비타민 E, 비타민 B12 등의 비타민류, 토코페롤, 디벤조일티아민 등을 들 수 있으며, 미네랄류로서는 구연산 칼슘 등의 칼슘 제제, 스테아린산마그네슘 등의 마그네슘 제제, 구연산철 등의 철 제제, 염화 크롬, 요오드칼륨, 셀레늄, 게르마늄, 바나듐, 아연 등을 들 수 있다. Examples of such physiologically active substances include catechins contained in green tea and the like, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoylthiamine, and the like. Minerals include calcium preparations such as calcium citrate, magnesium stearate Magnesium preparations, such as iron preparations, such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, zinc, etc. are mentioned.
본 발명의 식품 조성물에는 전술한 바의 식품첨가물이 제품 유형에 따라 그 첨가 목적을 달성할 수 있는 적량으로 포함될 수 있다.In the food composition of the present invention, the food additives as described above may be included in an appropriate amount to achieve the purpose of the addition according to the product type.
본 발명의 식품 조성물에 포함될 수 있는 기타의 식품첨가물과 관련하여서는 각국 식품공전이나 식품첨가물 공전을 참조할 수 있다.In relation to other food additives that may be included in the food composition of the present invention, reference may be made to the Food Ordinance of each country or the Food Additives Code.
본 발명의 조성물은 다른 구체적인 양태에 있어서는 약제학적 조성물로 파악될 수 있다.The composition of the present invention may be regarded as a pharmaceutical composition in another specific embodiment.
본 발명의 약제학적 조성물은 유효성분 이외에 약제학적으로 허용되는 담체를 포함하여 당업계에 공지된 통상의 방법으로 투여 경로에 따라 경구용 제형 또는 비경구용 제형으로 제조될 수 있다. 여기서 투여 경로는 국소 경로, 경구 경로, 정맥 내 경로, 근육 내 경로, 및 점막 조직을 통한 직접 흡수를 포함하는 임의의 적절한 경로일 수 있으며, 두 가지 이상의 경로를 조합하여 사용할 수도 있다. 두 가지 이상 경로의 조합의 예는 투여 경로에 따른 두 가지 이상의 제형의 약물이 조합된 경우로서 예컨대 1차로 어느 한 약물은 정맥 내 경로로 투여하고 2차로 다른 약물은 국소 경로로 투여하는 경우이다. The pharmaceutical composition of the present invention may be prepared as an oral dosage form or a parenteral dosage form according to the route of administration by a conventional method known in the art, including a pharmaceutically acceptable carrier in addition to the active ingredient. Here, the route of administration may be any suitable route including topical route, oral route, intravenous route, intramuscular route, and direct absorption through mucosal tissue, and two or more routes may be used in combination. An example of the combination of two or more routes is a case in which two or more formulations of drugs according to the route of administration are combined. For example, one drug is first administered by an intravenous route and the other drug is secondarily administered by a local route.
약학적으로 허용되는 담체는 투여 경로나 제형에 따라 당업계에 주지되어 있으며, 구체적으로는 "대한민국약전"을 포함한 각국의 약전을 참조할 수 있다. Pharmaceutically acceptable carriers are well known in the art depending on the route of administration or formulation, and specifically, reference may be made to the pharmacopoeia of each country including the "Korea Pharmacopoeia".
본 발명의 약제학적 조성물이 경구용 제형으로 제조될 경우, 적합한 담체와 함께 당업계에 공지된 방법에 따라 분말, 과립, 정제, 환제, 당의정제, 캡슐제, 액제, 겔제, 시럽제, 현탁액, 웨이퍼 등의 제형으로 제조될 수 있다. 이때 적합한 담체의 예로서는 락토스, 글루코스, 슈크로스, 덱스트로스, 솔비톨, 만니톨, 자일리톨 등의 당류, 옥수수 전분, 감자 전분, 밀 전분 등의 전분류, 셀룰로오스, 메틸셀룰로오스, 에틸셀룰로오스, 나트륨 카르복시메틸셀룰로오스, 하이드록시프로필메틸셀룰로오스 등의 셀룰로오스류, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 마그네슘 스테아레이트, 광물유, 맥아, 젤라틴, 탈크, 폴리올, 식물성유, 에탄올, 글리세롤 등을 들 수 있다. 제제화할 경우 필요에 따라적절한 결합제, 윤활제, 붕해제, 착색제, 희석제 등을 포함시킬 수 있다. 적절한 결합제로서는 전분, 마그네슘 알루미늄 실리케이트, 전분 페이스트, 젤라틴, 메틸셀룰로스, 소듐 카복시메틸셀룰로스, 폴리비닐피롤리돈, 글루코스, 옥수수 감미제, 소듐 알지네이트, 폴리에틸렌 글리콜, 왁스 등을 들 수 있고, 윤활제로서는 올레산나트륨, 스테아르산나트륨, 스테아르산마그네슘, 벤조산나트륨, 초산나트륨, 염화나트륨, 실리카, 탈쿰, 스테아르산, 그것의 마그네슘염과 칼슘염, 폴리데틸렌글리콜 등을 들 수 있으며, 붕해제로서는 전분, 메틸 셀룰로스, 아가(agar), 벤토나이트, 잔탄검, 전분, 알긴산 또는 그것의 소듐 염 등을 들 수 있다. 또 희석제로서는 락토즈, 덱스트로즈, 수크로즈, 만니톨, 소비톨, 셀룰로스, 글라이신 등을 들 수 있다. When the pharmaceutical composition of the present invention is prepared as an oral dosage form, powder, granules, tablets, pills, dragees, capsules, liquids, gels, syrups, suspensions, wafers according to methods known in the art together with a suitable carrier It can be prepared in a formulation such as Examples of suitable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, Cellulose such as hydroxypropylmethylcellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable oil, ethanol, glycerol and the like. In the case of formulation, an appropriate binder, lubricant, disintegrant, colorant, diluent, etc. may be included as needed. Suitable binders include starch, magnesium aluminum silicate, starch paste, gelatin, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, glucose, corn sweetener, sodium alginate, polyethylene glycol, wax, and the like, and lubricants include sodium oleate. , sodium stearate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride, silica, talcum, stearic acid, its magnesium salt and calcium salt, polyethylene glycol, etc., and the disintegrant includes starch, methyl cellulose, agar, bentonite, xanthan gum, starch, alginic acid or its sodium salt and the like. Examples of the diluent include lactose, dextrose, sucrose, mannitol, sorbitol, cellulose, and glycine.
본 발명의 약제학적 조성물이 비경구용 제형으로 제조될 경우, 적합한 담체와 함께 당업계에 공지된 방법에 따라 주사제, 경피 투여제, 비강 흡입제 및 좌제의 형태로 제제화될 수 있다. 주사제로 제제화할 경우 적합한 담체로서는 수성 등장 용액 또는 현탁액을 사용할 수 있으며, 구체적으로는 트리에탄올 아민이 함유된 PBS(phosphate buffered saline)나 주사용 멸균수, 5% 덱스트로스 같은 등장 용액 등을 사용할 수 있다. 경피 투여제로 제제화할 경우 연고제, 크림제, 로션제, 겔제, 외용액제, 파스타제, 리니멘트제, 에어롤제 등의 형태로 제제화할 수 있다. 비강 흡입제의 경우 디클로로플루오로메탄, 트리클로로플루오로메탄, 디클로로테트라플루오로에탄, 이산화탄소 등의 적합한 추진제를 사용하여 에어로졸 스프레이 형태로 제제화할 수 있으며, 좌제로 제제화할 경우 그 담체로는 위텝솔(witepsol), 트윈(tween) 61, 폴리에틸렌글리콜류, 카카오지, 라우린지, 폴리옥시에틸렌 소르비탄 지방산 에스테르류, 폴리옥시에틸렌 스테아레이트류, 소르비탄 지방산 에스테르류 등을 사용할 수 있다.When the pharmaceutical composition of the present invention is prepared for parenteral use, it may be formulated in the form of injections, transdermal administrations, nasal inhalants and suppositories together with suitable carriers according to methods known in the art. When formulated as an injection, an aqueous isotonic solution or suspension may be used as a suitable carrier, and specifically, PBS (phosphate buffered saline) containing triethanolamine, sterile water for injection, or isotonic solution such as 5% dextrose may be used. . When formulated for transdermal administration, it can be formulated in the form of an ointment, a cream, a lotion, a gel, an external solution, a pasta agent, a liniment agent, an air roll, and the like. In the case of nasal inhalants, it can be formulated in the form of an aerosol spray using a suitable propellant such as dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, and the like. witepsol), tween 61, polyethylene glycols, cacao fat, laurin fat, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearate, sorbitan fatty acid esters, and the like can be used.
약제학적 조성물의 구체적인 제제화와 관련하여서는 당업계에 공지되어 있으며, 예컨대 문헌[Remington's Pharmaceutical Sciences(19th ed., 1995)] 등을 참조할 수 있다. 상기 문헌은 본 명세서의 일부로서 간주 된다.Specific formulations of pharmaceutical compositions are known in the art, and reference may be made to, for example, Remington's Pharmaceutical Sciences (19th ed., 1995). This document is considered a part of this specification.
본 발명의 약제학적 조성물의 바람직한 투여량은 환자의 상태, 체중, 성별, 연령, 환자의 중증도, 투여 경로에 따라 1일 0.001mg/kg ~ 10g/kg 범위, 바람직하게는 0.001mg/kg ~ 1g/kg 범위일 수 있다. 투여는 1일 1회 또는 수회로 나누어 이루어질 수 있다. 이러한 투여량은 어떠한 측면으로든 본 발명의 범위를 제한하는 것으로 해석되어서는 아니 된다. A preferred dosage of the pharmaceutical composition of the present invention is in the range of 0.001 mg/kg to 10 g/kg per day, preferably 0.001 mg/kg to 1 g, depending on the patient's condition, weight, sex, age, severity of the patient, and the route of administration. It can be in the range /kg. Administration may be performed once or divided into several times a day. These dosages should not be construed as limiting the scope of the invention in any respect.
본 발명의 조성물은 또 다른 구체적인 양태에 있어서, 화장료 조성물로 파악할 수 있다. 본 발명의 조성물이 화장품 조성물로 파악될 경우 그 용도는 알러지성 피부 트러블 억제, 알러지성 피부 자극 완화 등의 용도로 이해될 수 있다.In another specific embodiment, the composition of the present invention can be identified as a cosmetic composition. When the composition of the present invention is identified as a cosmetic composition, its use may be understood as a use for suppressing allergic skin troubles, alleviating allergic skin irritation, and the like.
본 발명의 조성물이 화장료 조성물로 파악될 경우에도 그 화장료 조성물은 그 용도상, 법률상 임의의 제품 구분을 띨 수 있으며, 구체적으로 피부 트러블 개선, 아토피 피부염 개선 등의 용도를 가진 기능성 화장품, 비기능성 일반 화장품 등일 수 있다. 제품 형태에 있어서도 임의의 제품 형태를 띨 수 있는데, 구체적으로 용액, 현탁액, 유탁액, 페이스트, 젤, 크림, 로션, 파우더, 비누, 계면활성제-함유 클렌징, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션, 스프레이 등의 제품 형태를 띨 수 있다. 구체적인 제품 형태에 있어서는 유연 화장수, 영양 화장수, 영양 크림, 마사지 크림, 에센스, 아이 크림, 클렌징 크림, 클렌징 폼, 클렌징 워터, 팩, 스프레이 또는 파우더의 제형 등일 수 있다.Even when the composition of the present invention is identified as a cosmetic composition, the cosmetic composition can be classified into any product in terms of its use or by law, and specifically functional cosmetics, non-functional products having uses such as improvement of skin troubles and improvement of atopic dermatitis It may be general cosmetics and the like. In terms of product form, it may take any product form, and specifically, solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax It can take the form of products such as foundation and spray. In the specific product form, it may be in the form of a flexible lotion, a nourishing lotion, a nourishing 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.
본 발명의 화장료 조성물은 그 유효성분 이외에 화장료 조성물에 통상적으로 이용되는 성분들, 예컨대, 안정화제, 용해화제, 계면활성제, 비타민, 색소 및 향료와 같은 통상적인 보조제, 및 담체를 포함할 수 있다. The cosmetic composition of the present invention may include components commonly used in cosmetic compositions in addition to the active ingredient, for example, conventional adjuvants such as stabilizers, solubilizers, surfactants, vitamins, pigments and fragrances, and carriers.
본 발명의 제형이 페이스트, 크림 또는 젤인 경우에는 담체 성분으로서 동물성유, 식물성유, 왁스, 파라핀, 전분, 트라칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크 또는 산화아연 등이 이용될 수 있다.When 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. can
본 발명의 제형이 파우더 또는 스프레이인 경우에는 담체 성분으로서 락토스, 탈크, 실리카, 알루미늄 히드록시드, 칼슘 실리케이트 또는 폴리아미드 파우더가 이용될 수 있고, 특히 스프레이인 경우에는 추가적으로 클로로플루오로히드로카본, 프로판/부탄 또는 디메틸 에테르와 같은 추진체를 포함할 수 있다.When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. In particular, in the case of a spray, additional chlorofluorohydrocarbon, propane /may contain propellants such as butane or dimethyl ether.
본 발명의 제형이 용액 또는 유탁액인 경우에는 담체 성분으로서 용매, 용해화제 또는 유탁화제가 이용되는데, 구체적으로 물, 에탄올, 이소프로판올, 에틸 카보네이트, 에틸 아세테이트, 벤질 알코올, 벤질 벤조에이트, 프로필렌 글리콜, 1,3-부틸글리콜 오일, 글리세롤 지방족 에스테르, 폴리에틸렌 글리콜, 소르비탄의 지방산 에스테르 등이 이용될 수 있다.When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as a carrier component, specifically water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol, fatty acid ester of sorbitan, etc. may be used.
본 발명의 제형이 현탁액인 경우에는 담체 성분으로서 물, 에탄올 또는 프로필렌 글리콜과 같은 액상의 희석제, 에톡실화 이소스테아릴 알코올, 폴리옥시에틸렌 소르비톨 에스테르, 폴리옥시에틸렌 소르비탄 에스테르와 같은 현탁제, 미소결정성 셀룰로오스, 알루미늄 메타히드록시드, 벤토나이트, 아가 등이 이용될 수 있다.When the formulation of the present invention is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, polyoxyethylene sorbitan ester, microcrystals Adult cellulose, aluminum metahydroxide, bentonite, agar, etc. can be used.
본 발명의 제형이 계면-활성제 함유 클렌징인 경우에는 담체 성분으로서 지방족 알코올 설페이트, 지방족 알코올 에테르 설페이트, 설포숙신산 모노에스테르, 이세티오네이트, 이미다졸리늄 유도체, 메틸타우레이트, 사르코시네이트, 지방산 아미드 에테르 설페이트, 알킬아미도베타인, 지방족 알코올, 지방산 글리세리드, 지방산 디에탄올아미드, 식물성 유, 라놀린 유도체 또는 에톡실화 글리세롤 지방산 에스테르 등이 이용될 수 있다.When the formulation of the present invention is a surfactant-containing cleansing agent, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide as carrier components Ether sulfate, alkylamidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester and the like may be used.
본 발명의 화장료 조성물은 항알러지 활성을 나타내는 그 유효성분을 포함하는 것을 제외하고는 당업계에 통상적으로 행하여지는 화장료 조성물의 제조방법에 따라 제조할 수 있다.The cosmetic composition of the present invention can be prepared according to the method for preparing a cosmetic composition conventionally performed in the art, except that it contains the active ingredient exhibiting anti-allergic activity.
전술한 바와 같이, 본 발명에 따르면 개여뀌 추출물을 이용한 항알러지용 조성물을 제공할 수 있다. As described above, according to the present invention, it is possible to provide a composition for anti-allergy using an extract of the sagebrush.
본 발명의 항알러지용 조성물은 알러지 질환의 개선 등의 용도로 식품, 화장품, 약품 등으로 제품화될 수 있다.The composition for anti-allergy of the present invention may be commercialized as food, cosmetics, drugs, etc. for the purpose of improving allergic diseases.
도 1은 개여뀌 추출물의 IgE 및 항원(DNP-BSA)으로 활성화된 비만세포주 RBL-2H3(rat basophilic leukemia)에서의 탈과립 억제 활성을 보여주는 결과이다.1 is a result showing the degranulation inhibitory activity in the mast cell line RBL-2H3 (rat basophilic leukemia) activated with IgE and antigen (DNP-BSA) of Gaeyeogwi extract.
이하 본 발명을 실시예 및 실험예를 참조하여 설명한다. 그러나 본 발명의 범위가 이러한 실시예 및 실험예에 한정되는 것은 아니다.Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these Examples and Experimental Examples.
<< 실시예Example > 개여뀌 추출물의 제조> Manufacture of extract
건조된 개여뀌(Persicaria longiseta) 지상부 분말 100 g에 50% 에탄올 1 L를 가하여 상온에서 24 시간 1회 침지추출 후 여과지로 여과하였다. 얻어진 50% 에탄올 여액을 감압 농축 후 동결 건조하여 개여뀌 추출물을 얻었다. 1 L of 50% ethanol was added to 100 g of dried persicaria longiseta above ground powder, followed by immersion extraction once for 24 hours at room temperature, followed by filtration with filter paper. The obtained 50% ethanol filtrate was concentrated under reduced pressure, and then freeze-dried to obtain an extract of the succulents.
<< 실험예Experimental example > > 항알러지anti-allergy 활성 실험 - β-hexosaminidase assay Activity test - β-hexosaminidase assay
Rat basophilic leukemia 셀 라인인 RBL-2H3 세포주를 15% FBS, 100 unit/ml의 페니실린과 스트렙토마이신을 포함하는 MEM 배지와 37℃, 5% CO2 조건에서 24 well plate에 2×105/well로 분주한 후 24시간 배양하였다. Rat basophilic leukemia cell line, RBL-2H3 cell line, in MEM medium containing 15% FBS, 100 unit/ml penicillin and streptomycin and 2×10 5 /well in a 24 well plate at 37°C and 5% CO 2 condition. After dispensing, culture was performed for 24 hours.
상등액을 제거 후 25 ng/ml anti-DNP IgE가 포함된 MEM 배지를 넣고 4시간 배양하였다. 배양 후 PIPES buffer (25mM PIPES, 119mM NaCl, 5mM KCl, 1mM CaCl2, 0.4mM MgCl2, 40mM NaOH, 5.6mM glucose, 0.1% BSA)로 두 번 세척하고 10분 동안 전 배양하였다. 전 배양 후 실시예의 시료를 농도별로 20분간 처리 후 DNP-BSA 20분간 반응시켰다. Ice에 10분간 방치하여 반응을 종결시킨 후 상등액을 96 well plate에 넣고, 1mM P-니트로페닐-아세틸-β-D-글루코사미니드를 넣은 후 37℃에서 1시간 반응시켰다. stop solution(0.1M NaHCO3, O.1M Na2CO3)를 넣고 반응을 종결시킨 후 405nm 파장대에서 ELISA 리더로 흡광도를 측정하였다. 양성 대조군으로는 ketotifen(100 ㎍/ml)을 사용하였다.After removing the supernatant, MEM medium containing 25 ng/ml anti-DNP IgE was added and cultured for 4 hours. After incubation, the cells were washed twice with PIPES buffer (25mM PIPES, 119mM NaCl, 5mM KCl, 1mM CaCl 2 , 0.4mM MgCl 2 , 40mM NaOH, 5.6mM glucose, 0.1% BSA) and pre-incubated for 10 minutes. After pre-incubation, the samples of Example were treated for 20 minutes by concentration and then reacted with DNP-BSA for 20 minutes. After terminating the reaction by standing on ice for 10 minutes, the supernatant was placed in a 96 well plate, 1 mM P-nitrophenyl-acetyl-β-D-glucosaminide was added, and the reaction was carried out at 37° C. for 1 hour. Stop solution (0.1M NaHCO 3 , 0.1M Na 2 CO 3 ) was added and the reaction was terminated, and absorbance was measured with an ELISA reader at a wavelength of 405 nm. As a positive control, ketotifen (100 μg/ml) was used.
결과를 도 1에 나타내었는데, 실시예의 시료는 농도 의존적으로 탈과립을 억제함을 알 수 있으며, IC50은 40.75 ㎍/mL로 나타났다. 양성 대조군인 케토티펜(ketotifen)의 경우는 IC50이 38.13 ㎍/mL를 보였다. 양성 대조군으로 사용한 케토티펜은 항히스타민제로서 알러지성 비염, 아토피 등 알러지성 피부 질환, 알러지성 천식 등에 쓰이는 약물이다.The results are shown in FIG. 1, and it can be seen that the sample of Example inhibits degranulation in a concentration-dependent manner, and the IC 50 is 40.75 μg/mL. The positive control, ketotifen, showed an IC 50 of 38.13 μg/mL. Ketotifen, used as a positive control, is an antihistamine, which is used for allergic skin diseases such as allergic rhinitis, atopic dermatitis, and allergic asthma.

Claims (6)

  1. 개여뀌 추출물을 유효성분으로 포함하는 항알러지용 조성물.A composition for anti-allergy comprising an extract of sagebrush as an active ingredient.
  2. 제1항에 있어서,According to claim 1,
    상기 개여뀌 추출물은 물, 에탄올 또는 이들의 혼합 용매로 추출하여 얻은 추출물인 것을 특징으로 하는 항알러지용 조성물.The anti-allergic composition, characterized in that the extract is an extract obtained by extraction with water, ethanol, or a mixed solvent thereof.
  3. 제1항에 있어서,According to claim 1,
    상기 항알러지는 알러지성 질환의 개선, 치료, 그러한 질환의 발병 억제 또는 지연을 의미하고,The anti-allergic means the improvement, treatment of allergic diseases, inhibition or delay of the onset of such diseases,
    상기 알러지성 질환은 아토피 피부염(atopic dermatitis), 천식(asthma), 알러지성 비염(allergic rhinitis), 알러지성 결막염(allergic conjunctivitis), 알러지성 피부염(allergic dermatitis), 알러지성 접촉성 피부염(allergic contact dermatitis), 및 알러지성 각막염로 구성된 군에서 선택된 하나인 것을 특징으로 하는 항알러지용 조성물.The allergic disease is atopic dermatitis, asthma, allergic rhinitis, allergic conjunctivitis, allergic dermatitis, allergic contact dermatitis (allergic contact dermatitis) ), and an anti-allergic composition, characterized in that it is one selected from the group consisting of allergic keratitis.
  4. 제1항 내지 제3항 중 어느 한 항에 있어서,4. The method according to any one of claims 1 to 3,
    상기 조성물은 약제학적 조성물인 것을 특징으로 하는 항알러지용 조성물.The composition is an anti-allergic composition, characterized in that it is a pharmaceutical composition.
  5. 제1항 내지 제3항 중 어느 한 항에 있어서,4. The method according to any one of claims 1 to 3,
    상기 조성물은 식품 조성물인 것을 특징으로 하는 항알러지용 조성물.The composition is an anti-allergic composition, characterized in that it is a food composition.
  6. 제1항 내지 제3항 중 어느 한 항에 있어서,4. The method according to any one of claims 1 to 3,
    상기 조성물은 화장품 조성물인 것을 특징으로 하는 항알러지용 조성물.The composition is an anti-allergy composition, characterized in that it is a cosmetic composition.
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