WO2010035675A1 - Agent immunopotentialisateur ou antiallergique - Google Patents

Agent immunopotentialisateur ou antiallergique Download PDF

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Publication number
WO2010035675A1
WO2010035675A1 PCT/JP2009/066203 JP2009066203W WO2010035675A1 WO 2010035675 A1 WO2010035675 A1 WO 2010035675A1 JP 2009066203 W JP2009066203 W JP 2009066203W WO 2010035675 A1 WO2010035675 A1 WO 2010035675A1
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Prior art keywords
salacia
immunopotentiator
antiallergic agent
extract
mass
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PCT/JP2009/066203
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English (en)
Inventor
Fumitaka Ueda
Chihaya Kakinuma
Yuriko Serizawa
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Fujifilm Corporation
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Publication of WO2010035675A1 publication Critical patent/WO2010035675A1/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)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716—Glucans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • This invention relates to an immunopotentiator or antiallergic agent, which comprises a pulverized product or extract of a plant belonging to the genus Salacla.
  • an allergen-specific IgE antibody excessively produced from the B cell, histamine and leukotriene released from the mast cell and basophilic leukocyte and inclination of the Thl/Th2 balance to Th2 side are directly concerned in pollinosis.
  • the allergen advanced into the living body is incorporated into natural immunity system cells and thereby decomposed, and a part of the information is presented to the T cell via MHC class II.
  • the T cell which received antigen presentation is differentiated and activated into Th2 cell and thereby allows IL-4 or the like cytokine to act upon the B cell.
  • the IgE antibody is produced from the B cell that received stimulation by the Th2 cell and binds to an Fc receptor which is present on the surface of the mast cell and basophilic leukocyte.
  • the allergen again breaks into the living body and binds to the IgE antibody on the surface of mast cell and basophilic leukocyte, the cells undergo degranulation and thereby release a large amount of histamine and the like chemical mediators and, at the same time, leukotriene and the like are synthesized on the surface of cells.
  • These various substances cause nasal congestion by accelerating vascular permeability and generate airway contraction by contracting smooth muscle.
  • it has been revealed by degrees that inclination of the Thl/Th2 balance to the Th2 side due to changes in the life style and dietary life, and the like, in the recent years is one of the causes of the increasing tendency of allergic diseases.
  • a method for lessening chances of contacting with pollen by using a mask, a goggle or an air cleaner, a method for ingesting an antihistaminic or a food having degranulation inhibiting ability or leukotriene synthesis inhibiting ability, such as sweet tea, beefsteak plant leaf and the like, a desensitization therapy which induces tolerance by periodically injecting an allergen itself, and the like are known as the methods for improving symptoms of pollinosis, and their improving effect can be expected to a certain degree (cf., "Supplement Health Bible (written in Japanese) " edited by Japan Supplement Association, p. 74 (2004) and "Pollinosis (written in Japanese)” edited by H. Otsuka, published by Hoken Dojin Sha (1999), and JP-A-2000-041639 and JP-A-2004-217604) .
  • the problem that the invention is to solve is to provide a food or pharmaceutical preparation which is safe even when internally used for a prolonged period of time, because it is derive from a natural material and therefore shows fewer side effects, and can prevent pollinosis, atopy and the like allergic symptoms and carcinogenesis based on its immune balance adjusting and immunopotentiation actions.
  • the present inventors have conducted intensive examinations on the influences of ingestion of Salacia on blood, and as a result, have found for the first time that Salacia has an immunopotentiation action and also has the effect to alleviate allergy by adjusting immune balance.
  • the invention consists illustratively of the following constitutions.
  • An immunopotentiator which comprises: a pulverized product or extract of a plant belonging to the genus Salacia.
  • ⁇ 2> The immunopotentiator as described in ⁇ 1> above, wherein the plant belonging to the genus Salacia is at least one species of plant selected from the group consisting of Salacia reticulata, Salacia oblonga and Salacia chinensis.
  • ⁇ 3> The immunopotentiator as described in ⁇ 1> or ⁇ 2> above, wherein the pulverized product or extract of a plant belonging to the genus Salacia shows a sucrase 50% inhibition concentration (IC 50 value) of from 10 ⁇ g/ml to 1,000 ⁇ g/ml.
  • ⁇ 5> The immunopotentiator as described in any one of ⁇ 1> to ⁇ 4> above, wherein the substance capable of binding with a Toll-like receptor is at least one species selected from the group consisting of a glucopolysaccharide, a lipopolysaccharide and hyaluronic acid, or a degradation product thereof.
  • a food or pharmaceutical preparation which comprises : the immunopotentiator as described in any one of ⁇ 1> to ⁇ 5> above.
  • An antiallergic agent which comprises: a pulverized product or extract of a plant belonging to the genus Salacia.
  • ⁇ 9> The antiallergic agent as described in ⁇ 7> or ⁇ 8> above, wherein the pulverized product or extract of a plant belonging to the genus Salacia shows a sucrase 50% inhibition concentration (IC 50 value) of from 10 ⁇ g/ml to 1,000 ⁇ g/ml.
  • ⁇ 11> The antiallergic agent as described in any one of ⁇ 7> to ⁇ 10> above, wherein the substance capable of binding with a Toll-like receptor is at least one species selected from the group consisting of a glucopolysaccharide, a lipopolysaccharide and hyaluronic acid, or a degradation product thereof.
  • a food or pharmaceutical preparation which comprises : the antiallergic agent as described in any one of ⁇ 7> to ⁇ 11> above.
  • the immunopotentiator or antiallergic agent of the invention includes a pulverized product or extract of a plant belonging to the genus Salacia.
  • the plant belonging to the genus Salacia is a plant of the family Celastraceae growing naturally mainly in Sri Lanka, India and Southeast Asia regions, and more illustratively, one species or more of plants selected from Salacia reticulata, Salacia oblonga, Salacia prinoides, Salacia chinensis, Salacia latifolia, Salacia burunoniana, Salacia grandiflora and Salacia macrosperma are used, of which at least one species of plant selected from Salacia reticulata, Salacia oblonga and Salacia chinensis is desirable.
  • the pulverized product or extract of a plant belonging to the genus Salacia means a pulverized product, dried product, extract or dried powder (extract powder) or the like of a root, trunk, leaf, flower, fruit or the like edible part.
  • extract powder dried powder
  • One or more kinds of parts may be used by mixing them. More desirably, an extract powder extracted from a root or trunk is used.
  • Said extract powder is a product prepared by drying an extract obtained by a solvent extraction from the aforementioned edible part or the like.
  • the extraction solvent it may be selected from water, or alcohols including methanol and ethanol, or mixed solvents of water with alcohols or acetone and the like ketones.
  • water, an alcohol or an aqueous alcohol is used. More preferably, hot water or ethanol or an aqueous alcohol is used.
  • the alcohol concentration of the aforementioned aqueous alcohol those having a concentration of from 30 to 90% by mass, preferably from 40 to 70% by mass, may be used. (In this specification, mass ratio is equal to weight ratio.)
  • drying method spray drying, freeze drying and the like can be exemplified, though not limited thereto.
  • the pulverized product or extract of a plant belonging to the genus Salacia has a sucrase 50% inhibition concentration (IC 50 value) of from 10 ⁇ g/ml to 1,000 ⁇ g/ml.
  • IC 50 value sucrase 50% inhibition concentration
  • the sucrase 50% inhibition concentration of the extract of a plant belonging to the genus Salacia is more preferably from 10 ⁇ g/ml to 600 ⁇ g/ml, further preferably from 100 ⁇ g/ml to 450 ⁇ g/ml.
  • sucrase 50% inhibition concentration (IC 5O value) is measured by the following method. [Test method 1] Measurement of sucrase IC 5O value
  • sample solution A 2 mg portion of a sample (a pulverized product or extract of a plant belonging to the genus Salacia) is weighed and put into a tube and thoroughly suspended in 2 ml of water added thereto, thereby preparing a sample solution having a concentration of 1 mg/ml. This is diluted with water to respective concentrations of 0, 50, 100, 250 and 500 ⁇ g/ml .
  • sucrose is dissolved in 0.2 M maleate buffer (pH 6.0) to a sucrose concentration of 100 mM, and this is used as the substrate liquid.
  • a 400 ⁇ l portion of the substrate liquid is added to 500 ⁇ l of each of the aforementioned sample solution having respective concentrations and preliminarily heated at 37°C for 5 minutes in a water bath.
  • a 100 ⁇ l portion of the crude enzyme liquid is added to each of them and allowed to undergo the reaction at 37°C for 60 minutes. After completion of the reaction, the reaction is terminated by deactivating the enzyme through heating at 95°C for 2 minutes. Determination of concentration of the thus formed glucose is carried out using a commercially available kit for mutarotase glucose oxidase method (Glucose CII Test Wako, mfd. by Wako Pure Chemical Industries) .
  • Preparation of blank A 200 ⁇ l portion of the substrate liquid and 50 ⁇ l of the crude enzyme liquid are added to 250 ⁇ l of each of the aforementioned sample solution having respective concentrations and immediately heated at 95°C for 2 minutes to effect thermal deactivation of the enzyme, to be used as blank data.
  • the amount of a pulverized product or extract of a plant belonging to the genus Salacia in the daily dose of the immunopotentiator or antiallergic agent is, in the case of using an extract of a plant belonging to the genus
  • Salacia having an IC 50 value of 50 ⁇ g/ml for example, preferably from 10 to 600 mg, more preferably from 40 to 450 mg, particularly preferably from 50 to 350 mg.
  • Desirable amount of a plant belonging to the genus Salacia in the immunopotentiator or antiallergic agent can be optionally calculated from the above-mentioned desirable daily dose.
  • a tablet having a daily dose of 3 tablets it is desirable that it contains 1/3 of the daily dose per tablet. That is, it contains preferably from 3 to 200 mg, more preferably from 13 to 150 mg, particularly preferably from 17 to 117 mg of a pulverized product or extract of a plant belonging to the genus Salacia.
  • the value calculated by the following formula 1 is 0.5 or more, more preferably 0.8 or more, particularly preferably 1.7 or more .
  • the IC 50 value the pulverized product or extract as a whole is preferably from 0.1 to 7.5, more preferably from 0.15 to 4.50, particularly preferably from 0.3 to 3.75, as the value calculated by a formula 2.
  • the aforementioned pulverized product or extract of a plant belonging to the genus Salacia contains 0.8% by mass or more, more preferably from 1 to 30% by mass or more, particularly from 3.0 to 11% by mass or more of mangiferin based on the total amount of the extract.
  • the mangiferin content of the immunopotentiator or antiallergic agent of the invention is preferably 1 mg or more, more preferably from 1.8 to 54 mg, particularly preferably from 5.5 to 19 mg, based on the daily dose.
  • Mangiferin can be measured by a test method 2.
  • the mangiferin content is measured by the following method using HPLC.
  • Solvent A 1.0% acetic acid
  • Solvent B methanol
  • a sample is prepared by dissolving it in 50% methanol and then removing the insoluble matter using a syringe filter.
  • the content is calculated from the detected peak area of mangiferin using a calibration curve of an authentic sample.
  • the i ⁇ ununopotentiator or antiallergic agent of the invention further contains a substance which can bind and react with a Toll-like receptor (TLR) presenting on the surface of macrophage in the living body.
  • TLR Toll-like receptor
  • a substance capable of binding and reacting with TLR 2 and a substance capable of binding and reacting with TLR 4 are desirable, and containment of both of them is further desirable.
  • ⁇ glucan and the like glucopolysaccharide or yeasts lactic acid bacteria, lipopeptides, lipoteichoic acid, riboarabinomannan and the like can be cited, of which ⁇ glucan ( ⁇ l, 3-glucan) is more desirable.
  • Origins of the ⁇ glucan such as plant-derived, fungi-derived, bacteria-derived and the like ones, are not particularly limited, but those which are derived from fungi such as mushrooms (e.g., Agaricus blazei, reishi mushroom and Fomes yucatensis) , yeasts (e.g., baker's yeast and beer yeast) and the like are more desirable.
  • hyaluronic acid or a degradation product thereof As the substance capable of binding and reacting with TLR 4, hyaluronic acid or a degradation product thereof, a hyaluronic acid oligomer, a lipopolysaccharide or a Gram-negative bacterium containing the same, mannans and the like can be cited.
  • macrophage is activated when a substance capable of binding with a Toll-like receptor binds to a TLR, such as production of cytokine (interferon or TNF- ⁇ ) , surface expression increase of CD 40, CD 80, CD 86, MHC class II, and the like.
  • TLR cytokine
  • the substance capable of binding with a Toll-like receptor is at least one species selected from a glucopolysaccharide, a lipopolysaccharide and hyaluronic acid, or a degradation product thereof.
  • the substance capable of binding with a Toll-like receptor is dispersed to a nano scale order.
  • an emulsion or suspension having an average particle diameter of from 1 nm to 1,000 nm is desirable, and the average particle diameter is more preferably from 5 nm to 200 nm.
  • the "high concentration emulsion" according to the invention means an emulsion having 0.1% by mass or more of the content of the substance capable of binding with a Toll-like receptor. It is desirable that the high concentration emulsion of the invention has an average particle diameter of 200 nm or more, more desirably from 300 to 10,000 nm or more.
  • Particle diameter of the emulsion can be measured by a particle size distribution analyzer or the like.
  • the emulsion can be prepared by a conventionally known emulsion preparation method which is described for example in "Techniques for Emulsification and Solubilization (written in Japanese)" (edited by Tsuji, published by Kogyo Tosho) , pp. 65 - 66 and pp. 92 - 105, and both of the flocculation method and dispersion method can be suitably used.
  • Emulsifiers for Food Use written in Japanese
  • Hidaka published by Saiwai Shobo
  • any on of the methods classified into (1) self emulsification method, (2) soap forming method, (3) simple emulsification method, (4) transfer emulsification method and (5) surfactant method emulsification method is preferable, but when a high concentration emulsion is prepared, the simple emulsification method or surfactant method emulsification method is desirable, and the surfactant method emulsification method is particularly desirable. It is desirable that the emulsion of a substance capable of binding with a Toll-like receptor is prepared via the high concentration emulsion of the invention.
  • the suspension it is desirable to prepare it by a crushing method such as shearing, high pressure pulverization and the like, or a method which is effected through the mediation of an enzymatic degradation, thermal degradation, hydrolysis, emulsion polymerization or the like reaction.
  • a crushing method such as shearing, high pressure pulverization and the like, or a method which is effected through the mediation of an enzymatic degradation, thermal degradation, hydrolysis, emulsion polymerization or the like reaction.
  • the surfactant method emulsification method When it is prepared via the high concentration emulsion of the invention by the surfactant method emulsification method, it can be prepared by adding the high concentration emulsion, while stirring, to a solution to be used as the emulsion composition.
  • the dilution ratio of this case is preferably from 5 to 1,000 times, more preferably from 10 to 200 times.
  • Molecular weight of the substance capable of binding with a Toll-like receptor is preferably from 100 to 8,000,000.
  • the molecular weight is more preferably from 1,000 to 1,000,000, further preferably from 3,000 to 300,000.
  • the substance capable of binding with a Toll-like receptor is contained in the immunopotentiator or antiallergic agent in an amount of from 0.1% by mass to 95% by mass, more preferably from 0.5% by mass to 70% by mass, further preferably from 1% by mass to 50% by mass.
  • the immunopotentiator or antiallergic agent of the invention may further contain other components, for example, it may contain a lactic acid bacterium, a mineral yeast, a flavonoid, a polyphenol and the like.
  • the lactic acid bacteria can be orally administered to mammals including human and are bacteria which exert useful actions in the digestive tracts of the living body.
  • lactic acid bacteria for example, an acidophilus lactobacillus ⁇ Lactobacillus acidophilus) , a bifidobacterium (Bifidobacterium longum or the like) , a faecalis bacterium (Streptococcus faecalis) a reuteri lactobacillus (Lactobacillus reuteri) , a casei lactobacillus (Lactobacillus casei) , a plantarum lactobacillus (Lactobacillus plantarum) , a fermentum lactobacillus (Lactobacillus fermentum) , a rhamnosus lactobacillus (Lactobacobacillus (Lactobacillus ⁇ ) , a rhamnosus lactobacillus (Lactobac
  • Obtained origins of these lactic acid bacteria are not particularly limited so far as they are intact strains, and for the sake of convenience, commercially available counterparts can be broadly used.
  • the amount of the lactic acid bacteria to be used in the invention is preferably from ten million to one hundred billion, more preferably from fifty million to fifty billion, particularly preferably from one hundred million to ten billion, as the number of viable cells of lactic acid bacteria in daily dose of the immunopotentiator or antiallergic agent.
  • the mineral yeast means a yeast containing minerals.
  • As the minerals 16 metallic elements of sodium (Na) , potassium (K) , chlorine (Cl) , calcium (Ca) , magnesium (Mg) , phosphorus (P) , sulfur (S) and so-called trace elements iron (Fe) , zinc (Zn) , cupper (Cu) , manganese (Mn), cobalt (Co), chromium (Cr), iodine (I), molybdenum (Mo) and selenium (Se) can be cited.
  • chromium yeast which contains chromium is desirable. Though kinds of the yeast are not particularly limited, baker' s yeast or beer yeast is desirable.
  • the chromium content of chromium yeast is preferably from 0.01 to 5 parts by mass, more preferably from 0.05 to 1 part by mass, particularly preferably from 0.1 to 0.3 part by mass, based on 100 parts by mass of the chromium yeast.
  • the chromium yeast content in an immunopotentiator or antiallergic agent is preferably from 0.5 to 50 parts by mass, more preferably from 1 to 10 parts by mass, particularly preferably from 3 to 5 parts by mass, based on 100 parts by mass of the immunopotentiator or antiallergic agent.
  • the amount of the chromium yeast in the daily dose of the immunopotentiator or antiallergic agent is preferably from 5 to 500 mg, more preferably from 10 to 100 mg, particularly preferably from 30 to 50 rag.
  • the amount of chromium in the daily dose of the immunopotentiator or antiallergic agent is preferably from 20 to 200 ⁇ g, more preferably from 40 to 150 ⁇ g, particularly preferably from 60 to 100 ⁇ g.
  • Flavonoid is a general term for the pigment components distributing in all organs of plants, which is contained mainly in fruits and vegetables and is present particularly in the form of glycosides in green and white vegetables and skins of citrus fruits.
  • the flavonoid is a general term for the pigment components broadly distributing in plants, and particularly, it means flavan derivatives frequently contained in vegetables and fruits .
  • flavonols As the flavonoid, flavonols, isoflavones and catechins are preferable. Flavonols are known as polyphenols .
  • Flavonoid is a substance ingested into the body, but is generally hard to be absorbed. However, since flavonoid is effective even at a small amount and is a strong antioxidant, it is known that it suppresses the activity of carcinogens and has blood circulation accelerating action and anti-thrombus action.
  • flavonoid can be obtained from tea, grape, onion and the like respective origins.
  • the origins mean those which are extracted from at least a part of an organism.
  • the above-mentioned method for preparing an extract of a plant of the genus Salacia can be employed for the extraction, and the form of the extract can also be the same as described in the above; for example, it may be any one of the filtrate after extraction as such, or its concentrated or diluted state or in the form of its dried powder, or a mixture thereof.
  • the tea extract containing catechins is prepared from a tea plant which is an evergreen tree belonging to the family Theaceae.
  • tea plant both of the assamica cultivated in India, Sri Lanka and Southeast Asia and Camellia sinensis cultivated in China and Japan can be used.
  • water an alcohol or a hydrous alcohol is preferably used in the extraction. More preferably, hot water or ethanol or hydrous ethanol is used as the extraction solvent.
  • alcohol concentration of the aforementioned hydrous alcohol those which having a concentration of from 30 to 90% by mass, preferably from 40 to 70% by mass, may be used.
  • drying method spray drying, freeze drying and the like can be exemplified, though not limited thereto.
  • Polyphenol, catechins and the like antioxidants are contained in the tea extract. It is desirable that catechin, epicatechin, gallocatechin, epigallocatechin, catechin gallate, epicatechin gallate, gallocatechin gallate or epigallocatechin gallate is contained therein, and it is particularly desirable that epigallocatechin gallate is contained therein.
  • the immunopotentiator or antiallergic agent of the invention contains said tea extract in an amount of from 0.1 to 40% by mass, more preferably from 0.5 to 35% by mass, particularly preferably from 1.0 to 30% by mass.
  • the flavonols as one of the flavonoid eliminate active oxygen and thereby show anti-oxidation actions such as suppression of arteriosclerosis and improvement of blood circulation.
  • resveratrol as one of the polyphenol has been drawing attention as an antioxidant.
  • Resveratrol is constituted from the stilbene backbone and contained in a large amount in the rind of grapes so that it is also contained in red wine produced from grapes .
  • the invention comprises a grape extract or grape wine concentrate which contains said flavonols as a component.
  • the immunopotentiator or antiallergic agent of the invention contains the grape extract in an amount of from 0.1 to 30% by mass, more preferably from 0.1 to 10% by mass.
  • resveratrol has the actions to burn fat, to prevent a blood vessel system disease, arteriosclerosis, to exert anti-cancer action and to prevent shortening of DNA caused by cell division, and has the effect to prolong life of cells similar to the case of carrying out calorie control, so that it has the excellent effect as a material for preventing life style-related diseases.
  • the resveratrol content in the immunopotentiator or antiallergic agent of the invention is preferably from 0.0001 to 5.00% by mass, more preferably from 0.001 to 2.00% by mass.
  • quercetin as a polyphenol has been drawing attention as an antioxidant. Quercetin has the flavan structure and is contained in a large amount in onion skins.
  • Vitamin C absorption support, anti-oxidation action, immune action and the like physiological actions of quercetin have been reported, and it has been revealed that it is effective in suppressing fat absorption and it has been revealed also that it has the excellent effect as a material for preventing life style-related diseases.
  • the quercetin content in the immunopotentiator or antiallergic agent of the invention is preferably from 0.001 to 15% by mass, more preferably from 0.05 to 10% by mass, further preferably from 0.1 to 5.0% by mass.
  • the immunopotentiator or antiallergic agent of the invention contains catechin in an amount of particularly from 1 to 50% by mass.
  • catechin a green tea-derived one or the like is particularly desirable.
  • the immunopotentiator or antiallergic agent of the invention contains a polyphenol having lipase activity inhibitory effect in an amount of from 2 to 80% by mass.
  • a polyphenol having lipase activity inhibitory effect those which are derived from Oolong tea, derived from grape, derived from apple, derived from Lychee, derived from pine bark, derived from kanka and the like are particularly desirable.
  • the immunopotentiator or antiallergic agent of the invention is intended for mammals including human and orally administered to said mammals.
  • the immunopotentiator or antiallergic agent of the invention may be food (including drinks) , food materials, quasi drugs, pharmaceutical preparations, medicinal materials or quasi drug materials.
  • various types of carriers pharmaceutically or food sanitarily acceptable as oral preparations such as fillers, lubricants, stabilizers, dispersing agents, binders, diluents, spices, sweeteners, flavors, colorants and the like, can be exemplified.
  • the shape of the immunopotentiator or antiallergic agent of the invention is not particularly limited with the proviso that it exerts the effect of the invention, and its examples include tablets, pills, granules, fine subtilaes, chewable preparations, capsules (those which are filled in hard capsules or soft capsules), solutions, chewable tablets, drinks and the like. It may be shapes of other food.
  • pills and granules in the case of tablets, pills and granules, they can be made into certain dosage forms to which commonly use coatings are applied as occasion demands, such as sugar coated tablets, gelatin coated preparations, enteric coated preparations, film coated preparations and the like, and the tablets can also be made into double layer tablets and the like multiple layer tablets.
  • vitamins, vitamin-like substances, proteins, amino acids, oils and fats, organic acids, carbohydrate, plant-derived materials, animal- derived materials, microorganisms, food additives, pharmaceutical additives and the like orally ingestible components can be optionally contained in the immunopotentiator or antiallergic agent of the invention.
  • IFN- ⁇ in the serum is increased and the immune balance therefore is improved.
  • mass of the blind gut having an intestinal tract immune organ is increased and the number of lymphocytes in the blind gut epithelial cells is increased so that the immune system is activated. Accordingly, alleviation of pollinosis, atopy and the like allergic symptoms, prevention of a cold and prevention of cancer development are expected.
  • the immunopotentiator or antiallergic agent of the invention is derived from an edible natural source, a plant belonging to the genus Salacia, it is safe even when ingested for a prolonged period of time and shows fewer side effects.
  • Wistar male rats (6 weeks of age, about 200 g in body weight) were preliminarily reared for 7 days and then reared by dividing them into the administration groups shown in Table 1, in 5 animals per group.
  • the administration of each aqueous solution (100 mg/ml liquid) was carried out using a stomach tube, and the same volume of water was administered to the control.
  • results of IFN- ⁇ , blind gut mass and the number of lymphocytes in blind gut epithelial cells, which showed large differences are shown in Table 1.
  • the values were shown as relative values of average values of 5 animals for each group when the control group was regarded as 100.
  • the IFN- ⁇ in serum was significantly increased in the inventive examples of the invention in comparison with the comparative examples, thus showing that immune balance was improved.
  • mass of the blind gut having an intestinal tract immune organ was increased and the number of lymphocytes in the blind gut epithelial cells was significantly increased in comparison with the control group, it was found that there is an immunopotentiator effect.
  • Powders having the formulations of the samples 1 to 8 of Table 1 were prepared using this Salacia extraction powder, and sucrase IC 50 value per 1 sample tablet was measured by the method described in "Test method 1". Using these, the formulation components shown in the following Table 2 were made into tablets to prepare the samples 7 to 12.
  • the dose for the persons to be tested was set to 3 tablets/day for each sample of Table 2.
  • "Pure White” manufactured by ALPRON CO., LTD. was used as the ⁇ glucan, and an article manufactured by NAKAHARA CO., LTD. as a low molecular weight hyaluronic acid (molecular weight 100,000 or less), and "CEOLUS FD-IOl” manufactured by ASAHI KASEI CHEMICALS as crystalline cellulose.
  • one tablet of each of the samples 7 to 12 was orally ingested within 30 minutes after each meal every day by each group of 5 members, and this was repeated for 30 days. After completion of the ingesting period, effects were evaluated by them regarding the rhinitis symptoms, and average value of the results was calculated for each group .
  • a supplement was prepared by preparing tablets and applying shellac coating thereto.
  • the material prepared in Test Example 1 was used as the Salacia extract powder 1, and the following substances as the other respective components .
  • Green tea extract Sunphenon 100s (contains 55% by mass of catechin) manufactured by Taiyo Kagaku Co., Ltd.
  • Hematococcus algal pigment ASTOTS-S (the content of astaxanthins; 20% by mass) , manufactured by TAKEDA SHIKI CO., LTD.
  • Chromium yeast LALLEMAND BIO-INGREDIENTS (contains 0.2% by mass or more of chromium), manufactured by LALLEMAND Inc.
  • Sucrose lauric acid ester Ryoto® Sugar Ester L- 1695, manufactured by Mitsubishi-kagaku Foods Corporation ⁇ Carnitine: manufactured by ILS Inc.
  • a drinking liquid was prepared by mixing and dissolving the components of Table 4. This was filled in 50 cc portions in bottles, sterilized by heating at 85°C for 10 minutes and then cooled to room temperature to be used as a drink.
  • An immunopotentiator, an antiallergic agent and a food or pharmaceutical preparation which are safe even when internally used for a prolonged period of time, because they are derive from a natural material and therefore show fewer side effects, are provided by the invention.
  • pollinosis and the like allergic symptoms are alleviated and immune index is improved so that preventive effects for cancers and the like can be expected.

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Abstract

La présente invention concerne un agent immunopotentialisateur ou antiallergique comprenant : un produit ou extrait pulvérisé d’une plante appartenant au genre Salacia.
PCT/JP2009/066203 2008-09-24 2009-09-10 Agent immunopotentialisateur ou antiallergique WO2010035675A1 (fr)

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JP2010235544A (ja) * 2009-03-31 2010-10-21 Kobayashi Pharmaceutical Co Ltd 免疫活性化剤および飲食品
JP2012102026A (ja) * 2010-11-08 2012-05-31 Fujifilm Corp 抗ウイルス剤
JP2012167049A (ja) * 2011-02-14 2012-09-06 Fujifilm Corp がん関連遺伝子発現抑制剤
JP2014080448A (ja) * 2014-02-14 2014-05-08 Fujifilm Corp 腸内バクテロイデス増殖促進剤
JP2016098184A (ja) * 2014-11-19 2016-05-30 富士フイルム株式会社 サラシア属植物の抽出物を含む錠剤及びその製造方法
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