WO2021086017A1 - Composition pour l'amélioration de la fonction musculaire comprenant du ginsénoside rf, composition de ginsénoside comprenant du ginsénoside rf, ou mélange de l'un quelconque ou plusieurs de ceux-ci en tant que principe actif - Google Patents

Composition pour l'amélioration de la fonction musculaire comprenant du ginsénoside rf, composition de ginsénoside comprenant du ginsénoside rf, ou mélange de l'un quelconque ou plusieurs de ceux-ci en tant que principe actif Download PDF

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WO2021086017A1
WO2021086017A1 PCT/KR2020/014832 KR2020014832W WO2021086017A1 WO 2021086017 A1 WO2021086017 A1 WO 2021086017A1 KR 2020014832 W KR2020014832 W KR 2020014832W WO 2021086017 A1 WO2021086017 A1 WO 2021086017A1
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ginsenoside
composition
weight
mixture
muscle
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PCT/KR2020/014832
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English (en)
Korean (ko)
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이영경
김경탁
신은주
이영철
임원철
임태규
조장원
최재웅
홍희도
송노을
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한국식품연구원
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Priority claimed from KR1020200140963A external-priority patent/KR102483300B1/ko
Publication of WO2021086017A1 publication Critical patent/WO2021086017A1/fr

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    • 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
    • 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
    • A23L5/00—Preparation or treatment of foods or foodstuffs, in general; Food or foodstuffs obtained thereby; Materials therefor
    • 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
    • A23L5/00—Preparation or treatment of foods or foodstuffs, in general; Food or foodstuffs obtained thereby; Materials therefor
    • A23L5/51—Concentration
    • 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
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q90/00—Cosmetics or similar toiletry preparations for specific uses not provided for in other groups of this subclass
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/316—Foods, ingredients or supplements having a functional effect on health having an effect on regeneration or building of ligaments or muscles
    • 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
    • A23V2250/00—Food ingredients
    • A23V2250/20—Natural extracts
    • A23V2250/21—Plant extracts
    • A23V2250/2124—Ginseng

Definitions

  • the present invention is a ginsenoside Rf, ginsenoside composition comprising a ginsenoside Rf, or a food composition for improving muscle function, such as increasing exercise capacity, increasing muscle strength or increasing muscle mass, comprising a mixture of one or more of them as an active ingredient, It relates to a cosmetic composition for improving muscle function, a food composition for improving or preventing sarcopenia, or a pharmaceutical composition for treating or preventing sarcopenia.
  • Skeletal muscle is an organ that occupies the largest part of the human body and accounts for 40-50% of the total body weight, and plays an important role in various metabolic functions in the body, including energy homeostasis and heat generation.
  • Human muscles decrease by more than 1% every year from the age of 40, and by the age of 80, the level of maximum muscle mass decreases by 50%, and the loss of muscles in old age is recognized as the most important factor that degrades overall physical function.
  • the body shape changes such as the content of muscle and fat, and skeletal distortion, and the prevalence of obesity due to muscle loss in old age is showing a continuous increasing trend at a level of 30% or more worldwide.
  • sarcopenia is also closely related to senile chronic diseases such as osteoporosis, insulin resistance and arthritis, and it is possible to suppress a decrease in physical activity due to aging through the prevention or improvement of sarcopenia.
  • the global advanced ataxia and muscle weakness treatment market reached about $14 billion in 2011, and is expected to grow at a compound annual growth rate of 9.4% since then, reaching about $23.5 billion in 2017.
  • a food composition for improving muscle function such as increasing exercise capacity, muscle strength, or muscle mass increase, using natural substances that are safe to consume for sarcopenia patients or the elderly and can be taken for a long time
  • cosmetic composition for improving muscle function, improvement or prevention of sarcopenia There is a demand for a food composition or a pharmaceutical composition for the treatment or prevention of sarcopenia.
  • ginsenoside Rg1 or Rb1 among the active ingredients of ginseng is related to muscle differentiation, but ginsenoside Rf, which is not contained in Hwagisam and is characteristic of Korean ginseng, It has not been revealed whether it is relevant.
  • Ginsenoside Rg1 from Panax ginseng enhances myoblast differentiation and myotube growth, 2017, Journal of Ginseng Research
  • Ginsenoside Rb1 and Rb2 upregulate Akt/mTOR signaling emediated muscular hypertrophy and myoblast differentiation, 2019, Journal of Ginseng Research
  • An object of the present invention is to provide a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • Another object of the present invention is to provide a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a cosmetic composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • Another object of the present invention is to provide a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving or preventing sarcopenia comprising a mixture of one or more of them as an active ingredient It is to do.
  • Another object of the present invention is to provide a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a pharmaceutical composition for the treatment or prevention of sarcopenia comprising a mixture of one or more of them as an active ingredient It is to do.
  • the present invention for achieving the above object provides a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving muscle function comprising a mixture of one or more of them as an active ingredient.
  • the present invention provides a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a cosmetic composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • the present invention provides a ginsenoside Rf, a ginsenoside composition comprising a ginsenoside Rf, or a food composition for improving or preventing sarcopenia comprising a mixture of one or more of them as an active ingredient.
  • the present invention provides a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a pharmaceutical composition for the treatment or prevention of sarcopenia comprising a mixture of at least one of them as an active ingredient.
  • a ginsenoside composition comprising ginsenoside Rf, or a mixture of any one or more of them promotes the expression of Myosin Heavy Chain, a muscle differentiation marker, regulates energy homeostasis in the body, and develops and grows skeletal muscle It promotes phosphorylation of AMPK, which plays an important role in regulation, and can increase exercise capacity, increase muscle strength, increase muscle mass, and alleviate muscle atrophy by increasing swimming duration in the forced swimming test in animal experiments.
  • FIG. 1 is a photograph confirming the expression of MHC (Myosin Heavy Chain) when ginsenosides Rf, Rb2 and Rg1 were treated with 10, 20 and 40 ⁇ M, respectively, through Western blot.
  • MHC Myosin Heavy Chain
  • FIG. 2 is a graph comparing the size of the western blot band representing the expression of MHC (Myosin Heavy Chain) of FIG. 1 with respect to actin.
  • FIG. 3 is a photograph confirming phosphorylation of 5′-adenosine monophosphate-activated protein kinase (AMPK) when ginsenosides Rf, Rb2 and Rg1 were treated with 10, 20 and 40 ⁇ M, respectively, through Western blot.
  • AMPK 5′-adenosine monophosphate-activated protein kinase
  • Figure 4 is a relative expression level of the western blot band size of phosphorylated p-AMPK (phosphorylated 5'-adenosine monophosphate-activated protein kinase) of Figure 3 for non-phosphorylated AMPK (phosphorylated 5'-adenosine monophosphate-activated protein kinase) It is a graph comparing.
  • FIG. 5 shows MHC, PGC-1 ⁇ , phosphorylated p-AMPK, phosphorylated p38 when 10 ⁇ M of ginsenoside Rf and 0.2, 1, and 5 ⁇ M of ginsenosides Rh1 and Rg2, respectively, were confirmed through Western blot. It's a picture.
  • FIG. 6 is a graph comparing the relative expression levels of MHC, PGC-1 ⁇ , phosphorylated p-AMPK, and phosphorylated p38 to actin of FIG. 5.
  • FIG. 8 is a graph comparing the relative expression levels of MHC, PGC-1 ⁇ , phosphorylated p-AMPK, and phosphorylated p38 to actin of FIG. 7.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a cosmetic composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • the present invention also relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving or preventing sarcopenia comprising a mixture of at least one of them as an active ingredient.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a pharmaceutical composition for the treatment or prevention of sarcopenia comprising a mixture of one or more of them as an active ingredient.
  • the composition may further include a ginsenoside composition including ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of them.
  • the composition comprises 1 to 100 parts by weight, 2 parts by weight or more, 5 parts by weight or more, 10 parts by weight or more, 20 parts by weight or more, 30 parts by weight or more, 40 parts by weight, based on 100 parts by weight of the ginsenoside Rf component. It may be at least 90 parts by weight, 80 parts by weight or less, 70 parts by weight or less, and 60 parts by weight or less.
  • the ginsenoside composition comprising the ginsenoside Rf may be a ginsenoside Rf concentrate obtained by treating a plant of the genus Panax or an extract thereof by any one or more processes selected from heating, enzyme treatment, and fermentation.
  • the ginsenoside composition comprising the ginsenoside Rh1 may be a ginsenoside Rf concentrate obtained by treating a plant of the genus Panax or an extract thereof by any one or more processes selected from heating, enzyme treatment, and fermentation.
  • the plant extract of the genus Panax may be an extract using water, an alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof.
  • the water is suitable for food production, there is no need to specifically limit it, but for example, ground water, purified water, distilled water, deionized water, and the like may be used.
  • the alcohol having 1 to 4 carbon atoms is not particularly limited, but for example, methanol, ethanol, propanol, butanol, normal-propanol, iso-propanol or normal-butanol may be used, preferably ethanol.
  • the mixed solvent is not particularly limited, but for example, in the case of a mixed solvent of water and ethanol, 5 to 95% by weight aqueous ethanol solution, 10 to 90% by weight aqueous ethanol solution, 20 to 80% by weight aqueous ethanol solution, 30 to 70% by weight An aqueous ethanol solution can be used.
  • the preparation of the water extract is not particularly limited, but can be prepared by extracting the plant of the genus Panax with water at 10 to 100° C. for 2 to 60 hours.
  • the preparation of the alcohol extract or the extract of a mixed solvent of water and alcohol is not particularly limited, but, for example, the plant of the genus Panax is prepared by extracting the genus Panax with an aqueous ethanol solution of 30 to 70% by weight at 20 to 60°C for 2 to 48 hours. do.
  • Plants of the genus Panax are Korean ginseng (Panax ginseng), Hwagi ginseng (Panax quinquefolia), Panax notoginseng, bamboo japonica, Panax trifolia, Himalayan ginseng (Panax pseudoginseng), Vietnamese ginseng (Panax vietnamensis). ) And may be any one or more selected from cultured roots thereof.
  • the plant of the genus Panax may be any one or more selected from roots, seeds, fruits, and leaves of the plant.
  • the ginsenoside composition comprising the ginsenoside Rf or the ginsenoside composition comprising ginsenoside Rh1 is an extract of the genus Panax plant, a fraction fractionated from them, a concentrate obtained by additionally concentrating these extracts or fractions, Purified or separated purified product is also included, and the extract, fraction, concentrate, or purified product is dried or pulverized.
  • various additionally performed such as passing through an ultrafiltration membrane having a molecular weight cut-off value, or separation by various chromatography (made for separation according to size, charge, hydrophobicity, or affinity) Purification methods can be added.
  • composition that is, 1) a ginsenoside composition comprising ginsenoside Rf, or 2) a mixture of a ginsenoside composition comprising ginsenoside Rf and ginsenoside Rf, or 3) ginsenoside Rf, ginseno A ginsenoside composition comprising a side Rf, or a mixture of any one or more of them; and a ginsenoside composition comprising ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of these; a mixture of ginsenosides Ginsenoside Rf 30% by weight or more, 35% by weight or more, 40% by weight or more, 45% by weight or more, 50% by weight or more, 60% by weight of the total ginsenoside weight consisting of the sum of Rf, Rh1, Rg1 and Rb2 It may contain more than, or 70% by weight or more, and may contain 80% by weight or less, 90% by weight or less, 95% by weight or less, 99% by weight
  • composition that is, 1) a ginsenoside composition comprising ginsenoside Rf, or 2) a mixture of a ginsenoside composition comprising ginsenoside Rf and ginsenoside Rf, or 3) ginsenoside Rf, ginseno A ginsenoside composition comprising a side Rf, or a mixture of any one or more of them; and a ginsenoside composition comprising ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of these; Ginsenoside Rf of 20% by weight or more, 22% by weight or more, 25% by weight or more, 30% by weight or more, 35% by weight or more, 40% by weight or more, 45% by weight or more, 50% by weight of the total weight of all ginsenosides It may contain more than, 60% by weight or more, or 70% by weight or more, and also include 80% by weight or less, 90% by weight or less, 95% by weight or less, 99% by weight or less, or 100%
  • composition that is, 1) a ginsenoside composition comprising ginsenoside Rf, or 2) a mixture of a ginsenoside composition comprising ginsenoside Rf and ginsenoside Rf, or 3) ginsenoside Rf, ginseno A ginsenoside composition comprising a side Rf, or a mixture of any one or more of them; and a ginsenoside composition comprising ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of these; a mixture of ginsenosides Ginsenoside Rf in the total weight of 10% by weight or more, 12% by weight or more, 15% by weight or more, 20% by weight or more, 25% by weight or more, 30% by weight or more, 35% by weight or more, 40% by weight or more, 45% by weight % Or more, 50% by weight or more, 60% by weight or more, or 70% by weight or more, and also 80% by weight or less, 90% by weight or less, 95% by weight
  • the term'contained as an active ingredient' means 1) ginsenoside Rf, 2) ginsenoside composition comprising ginsenoside Rf, or 3) any one or more mixtures of these, or 4) ginsenoside Rf, ginseno A ginsenoside composition comprising a side Rf, or a mixture of any one or more of them; and a ginsenoside composition comprising ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of these; Achieving the efficacy of a mixture of It means to contain enough amount to do.
  • muscle function improvement refers to tendons, muscles, and tendons generically, and'muscle function' refers to the ability to exert power by contraction of muscles.
  • Muscle strength capable of exerting contractility
  • Muscle endurance the ability to describe how long or how many times a muscle can contract and relax for a given weight
  • instantaneous power which is an ability to exert a strong power within a short time.
  • the improvement of muscle function may be any one selected from an increase in exercise capacity, an increase in muscle strength, and an increase in muscle mass.
  • the sarcopenia refers to a disease in which muscle volume and muscle strength gradually decline due to muscle function decline, muscle wasting or muscle degeneration, and muscle atrophy, myasthenia, muscle dystrophy, muscle stiffness, muscle tone reduction, muscle weakness, muscle regression, muscle atrophy. It may be any one selected from lateral sclerosis and myasthenia gravis.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a food composition for improving muscle function or improving or preventing sarcopenia, comprising a mixture of one or more of them as an active ingredient.
  • the food composition may further include a ginsenoside composition including ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of them.
  • the'food composition' is a standard and standard of food commonly used in food production ('food Food ingredients and food additives that can be used as foods described in the code') include food additives described in the code.
  • the carbohydrates include monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sugar, lactose, and the like; Oligosaccharides or polysaccharides such as dextrin, starch syrup, cyclodextrin, and the like; Sugar alcohols such as xylitol, sorbitol, erythritol, and the like can be used.
  • the flavoring agent may be a natural flavoring agent [taumatin, stevia extract (eg, rebaudioside A, glycyrrhizin, etc.]) and a synthetic flavoring agent (saccharin, aspartame, etc.).
  • Ginsenoside comprising ginsenoside Rf, ginsenoside Rf when preparing a food composition using the ginsenoside Rf, ginsenoside Rf, or a mixture of any one or more of them as an active ingredient
  • the composition, or a mixture of any one or more thereof does not need to be particularly limited as long as it is an amount exhibiting an effect of improving muscle function or sarcopenia, but, for example, 0.1 to 99% by weight, 0.5 to 95% by weight, 1 to 90% by weight, It may be included in 2 to 80% by weight, 3 to 70% by weight, 4 to 60% by weight, and 5 to 50% by weight.
  • the ginsenoside composition comprising ginsenoside Rf and ginsenoside Rf, which are active ingredients in the food composition, or a mixture of any one or more of them varies depending on the condition of the ingestor, weight, the presence or absence of disease, and the duration, but usually It can be appropriately selected by the technician of For example, it may be 1 to 5,000 mg, preferably 5 to 2,000 mg, more preferably 10 to 1,000 mg, even more preferably 20 to 800 mg, most preferably 50 to 500 mg, based on the daily dosage.
  • the number of administrations does not need to be particularly limited, but can be adjusted by a person skilled in the art within the range of 3 times a day to once a week. In the case of long-term intake for the purpose of health and hygiene or for the purpose of health control, it may be less than the above range.
  • the food composition is not particularly limited, but may be, for example, a powder, a granule, a tablet, a capsule, a pill, an extract, a jelly formulation, a tea bag formulation, or a beverage formulation.
  • a ginsenoside composition including the ginsenoside Rf and ginsenoside Rf, or a mixture of any one or more of these may be added in order to impart the function of improving muscle function or sarcopenia to general foods due to ultraviolet rays.
  • Foods that can be allowed are not particularly limited, but for example, confectionery, bread or rice cakes, processed cocoa products or chocolates, meat or eggs exemplified in the food standards and standards ('Food Code') according to Article 7 of the Food Sanitation Act.
  • Processed products processed fish products, tofu or jelly, noodles, tea, coffee, beverages, special purpose foods, pastes, seasoned foods, dressings, kimchi, salted fish, pickles, stewed foods, alcoholic beverages, raisins, and other foods.
  • dairy products processed meat products and packaged meats, and egg products as exemplified in the processing standards and ingredient specifications of livestock products pursuant to Article 4 of the Livestock Hygiene Management Act ('Livestock Products Code').
  • the ginsenoside composition comprising the ginsenoside Rf, ginsenoside Rf, or a food composition comprising any one or more of these as an active ingredient may be used as a "health functional food that helps improve muscle function” It can be used as "health functional food that helps to enhance muscle strength", “health functional food that helps to increase exercise capacity”, or "health functional food that helps to improve sarcopenia”.
  • The'health functional food' refers to a food (including processing) manufactured (including processing) according to legal standards using raw materials or ingredients having useful functions for the human body (Article 3, No. 1 of the Health Functional Food Act).
  • The'health functional food' may differ in terms or ranges from country to country, but'Dietary Supplement' in the United States,'Food Supplemnet' in Europe, and'Health Functional Food' in Japan or ' It may correspond to'Food for Special Health Use (FoSHU)' and'Health Food' in China.
  • the food composition or health functional food may additionally contain food additives, and the suitability as a food additive is determined according to the standards and standards for the relevant item in accordance with the general rules and general test methods of the'Food Additive Code' unless otherwise specified.
  • the health functional food may be used in combination with a ginsenoside composition including the ginsenoside Rf and ginsenoside Rf, or a health functional food material related to improvement of muscle function or sarcopenia with a mixture of one or more of them. have.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a cosmetic composition for improving muscle function comprising a mixture of at least one of them as an active ingredient.
  • the cosmetic composition may further include a ginsenoside composition including ginsenoside Rh1, ginsenoside Rh1, or a mixture of one or more of them.
  • the cosmetic composition for improving muscle function When used as the cosmetic composition for improving muscle function, additionally fatty substances, organic solvents, solubilizers, thickeners and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water , Ionic emulsifiers, nonionic emulsifiers, fillers, sequestering agents, chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic activators, lipophilic activators or lipid vesicles, etc. It may contain adjuvants commonly used in the field of dermatology, such as any other ingredients used as. In addition, the above ingredients may be introduced in an amount generally used in the field of dermatology.
  • the cosmetic composition is not particularly limited, but may be a formulation such as an ointment, patch, gel, cream or spray.
  • the present invention relates to a ginsenoside composition
  • a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a pharmaceutical composition for treating or preventing sarcopenia comprising a mixture of at least one of them as an active ingredient.
  • the pharmaceutical composition may further include a ginsenoside composition including ginsenoside Rh1, ginsenoside Rh1, or a mixture of any one or more of them.
  • the present invention provides a method for treating sarcopenia by administering the composition to humans or animals other than humans.
  • the present invention provides a novel use of a ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or a mixture of any one or more of them for the manufacture of a medicine for the treatment of sarcopenia.
  • The'pharmaceutical composition' or'medicine' is a ginsenoside composition including ginsenoside Rf and ginsenoside Rf as an active ingredient, or a mixture of any one or more of them, as well as suitable for conventional use in the manufacture of pharmaceutical compositions, etc. It may further include a carrier, excipient and diluent.
  • The'carrier' is a compound that facilitates the addition of the compound into cells or tissues.
  • The'diluent' is a compound that is diluted in water to dissolve the compound as well as stabilize the biologically active form of the target compound.
  • the carrier, excipient and diluent do not need to be particularly limited, but for example, lactose, glucose, sugar, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate, cellulose , Methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil.
  • the amount of use of the pharmaceutical composition or drug may vary depending on the age, sex, and weight of the patient or the animal to be treated, and above all, the condition of the subject to be treated, the specific category or type of the disease to be treated, the route of administration, and the therapeutic agent used. It will be attribute dependent.
  • the pharmaceutical composition or medicament is appropriately selected according to the degree of absorption of the active ingredient in the body, the excretion rate, the age and weight, sex and condition of the patient or the animal to be treated, the severity of the disease to be treated, etc.
  • the unit dosage form formulation thus formulated can be administered several times at regular time intervals as needed.
  • the pharmaceutical composition or medicament may be individually administered as a prophylactic or therapeutic agent, or may be administered in combination with other therapeutic agents, and may be administered sequentially or simultaneously with a conventional therapeutic agent.
  • compositions or drugs may be formulated and used in oral dosage forms such as powders, granules, tablets, capsules, troches, suspensions, emulsions, syrups, aerosols, etc., according to conventional methods.
  • oral dosage forms such as powders, granules, tablets, capsules, troches, suspensions, emulsions, syrups, aerosols, etc.
  • diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants.
  • Solid preparations for oral administration include tablets, pills, powders, granules, capsules, troches, and the like, and these solid preparations include at least one excipient for the compound, such as starch, calcium carbonate, sugar or lactose, gelatin. It can be prepared by mixing and the like. In addition, in addition to simple excipients, lubricants such as magnesium stearate and talc may also be used.
  • Liquid preparations for oral use include suspensions, liquid solutions, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, fragrances, and preservatives may be included. .
  • the method for treating sarcopenia is a ginsenoside composition comprising 1) ginsenoside Rf, 2) ginsenoside Rf, or 3) a mixture of any one or more of these in humans or non-human animals, particularly mammals. , Or 4) ginsenoside composition comprising ginsenoside Rf, ginsenoside Rf, or any one or more mixtures thereof; and ginsenoside composition comprising ginsenoside Rh1, ginsenoside Rh1, or among these
  • a mixture of any one or more mixtures for example, a ginsenoside composition comprising the ginsenoside Rf, ginsenoside Rf, or a mixture of any one or more thereof to an individual to be treated with sarcopenia It is administered orally.
  • Whether or not the subject to be treated with sarcopenia may be the case where the amount of skin moisture loss is increased, the skin moisture content is decreased, the roughness of the skin is increased, and the elasticity of the skin is decreased.
  • the dosage, administration method, and number of administrations for the treatment may refer to the dosage, administration method, and number of administrations of the pharmaceutical composition or drug.
  • MHC myosin heavy chain
  • C2C12 muscle cells were purchased and used from the American Type Culture Collection (ATCC). C2C12 muscle cells were cultured in a DMEM medium containing 10% FBS and 1% antibiotic in an incubator at 37°C and 5% CO2. When replacing with 2% horse serum DMEM medium, muscle differentiation is induced, and ginsenosides Rf, Rg1 and Rb2 are treated 2 days after treatment with differentiation inducing conditions (DM, 2% horse serum DMEM medium) in muscle cells (C2C12). Did
  • the cell pellet prepared by the above method was prepared using a cell lysis buffer (cell signaling) to which a protease inhibitor and a phosphatase inhibitor were added.
  • cell signaling cell signaling
  • the same amount of the protein is mixed with the SDS sample buffer and heated at 95° C. for 10 minutes to denature the protein to be used in the experiment.
  • Samples were electrophoresed on gradient SDS-polyacrylamide gel. After transferring the protein of the gel to a nitrocellulose (NC) membrane, blocking is performed for 1 hour at room temperature with a 5% skim milk solution. Thereafter, the primary antibody was incubated overnight at 4° C., and then the appropriate secondary antibody with HRP was added, and the expression of each protein was confirmed by chemiluminescent method using an ECL solution, as shown in FIG. 1.
  • ginsenoside Rg1 The muscle differentiation efficacy of ginsenoside Rg1 is described in "Ginsenoside Rg1 from Panax ginseng enhances myoblast differentiation and myotube growth, 2017, Journal of Ginseng Research". As described in myoblast differentiation and myotube growth, 2017, Journal of Ginseng Research", these ginsenosides were used as positive controls.
  • ginsenoside Rf compared to ginsenosides Rg1 and Rh2, which are known for their muscle differentiation efficacy (see FIGS. 1 and 2).
  • ginsenoside Rf increased muscle differentiation efficacy by 4.1 times compared to ginsenoside Rg1
  • ginsenoside Rf increased muscle differentiation efficacy by 5.3 times compared to ginsenoside Rb2.
  • AMPK (5'-adenosine monophosphate-activated protein kinase) is a major enzyme that regulates energy homeostasis in the body and is known to play an important role in skeletal muscle development and growth regulation. Changes in AMPK phosphorylation, a signal protein related to energy metabolism by treatment with ginsenosides Rf, Rb2 and Rg1, were confirmed using the Western blot method of Experimental Example 1, and the results are shown in FIGS. 3 and 4.
  • Ginsenosides Rf, Rb2 and Rg1 treatment all increased phosphorylation of AMPK, a well-known marker related to energy metabolism.
  • ginsenoside Rf significantly increased phosphorylation of AMPK compared to ginsenosides Rb2 and Rg1. Therefore, it can be seen that ginsenoside Rf had an effect on inducing muscle differentiation through AMPK phosphorylation.
  • Ginsenoside Rf is a ginsenoside that is specifically present in Korean ginseng (Panax ginseng) and red ginseng produced therefrom. Ginsenoside Rf works with other ginsenosides to increase muscle differentiation and energy metabolism. It was confirmed whether it showed an effect.
  • Ginsenosides Rh1, Rg2, Rk3, Rh4, Rk1, (S)-Rg3 and Rg5 are 7 types of ginsenosides, which are known to increase their content in red ginseng extract compared to white ginseng. Sides were targeted.
  • C2C12 muscle cells prepared in the same manner as in Experimental Example 1 were treated with differentiation inducing conditions (DM, 2% horse serum DMEM medium) 2 days after treatment with ginsenoside Rf 5, 10 and 20 ⁇ M, respectively, and ginsenoside Rh1 with Rf 10 ⁇ M , Rg2, Rk3, Rh4, Rk1, (S)-Rg3 and Rg5 A total of 7 ginsenosides were treated in combination with 0.2, 1 and 5 ⁇ M, respectively.
  • differentiation inducing conditions DM, 2% horse serum DMEM medium
  • Ginsenosides Rh1, Rg2, Rk3, Rh4, Rk1, (S)-Rg3 and Rg5 administered in combination with ginsenoside Rf compared to the case of Rf alone treatment only in combination with Rh1 among a total of 7 ginsenosides.
  • the expression of the muscle differentiation biomarker MHC myosin heavy chain was increased, and in particular, when treated with 10 to 50 parts by weight of Rh1 with respect to 100 parts by weight of Rf, it exhibited a synergistic effect (see FIGS. 5 and 6).
  • Hot water extraction was performed 3 times for 2 hours each using a reflux cooling extractor at 80°C with 50 times the amount of distilled water to 1 g of Hwagisam.
  • the supernatant was filtered using Whatman No2 filter paper, concentrated under reduced pressure, diluted again in distilled water, and freeze-dried to prepare a hot water extract of Hwagisam.
  • the Hwagisam hot water extract did not contain ginsenoside Rf, ginsenoside Rg1, 0.32 mg/g, and ginsenoside Rb2, 0.33 mg/g.
  • Ginsenoside composition containing ginsenoside Rf by mixing 10 ⁇ M and 20 ⁇ M of ginsenoside Rf in the Hwagisam hot water extract (100 ⁇ g/mL), ginsenoside in the Hwagi ginseng hot water extract (100 ⁇ g/mL) Ginsenoside composition containing ginsenoside Rg1 by mixing 10 ⁇ M and 20 ⁇ M of Rg1, ginsenoside Rb2 in the Hwagisam hot water extract (100 ⁇ M/mL), respectively, by mixing 10 ⁇ M and 20 ⁇ M of ginsenoside Rb2 Each ginsenoside composition comprising a was prepared.
  • muscle differentiation biomarker MHC myosin heavy chain
  • the ginsenoside composition comprising ginsenoside Rg1, which is a mixture of 10 ⁇ M and 20 ⁇ M of ginsenoside Rg1, respectively, 10 ⁇ M and 20 ⁇ M of ginsenoside Rb2, respectively, and the ginsenoside composition containing ginsenoside Rb2
  • the increase in MHC expression could not be confirmed, the expression of MHC was 1.77 in the ginsenoside composition containing ginsenoside Rf by mixing 10 ⁇ M and 20 ⁇ M of ginsenoside Rf in Hwagisam hot water extract (100 ⁇ g/mL), respectively. It was confirmed that the increase was doubled and 1.6-fold.
  • the above ingredients are mixed and filled in an airtight cloth to prepare a powder.
  • tablets are prepared by tableting according to a conventional tablet manufacturing method.
  • the above ingredients are mixed and filled into gelatin capsules to prepare a capsule.
  • Vitamin A acetate 70 ⁇ g
  • Vitamin B12 0.2 ⁇ g
  • composition ratio of the vitamin and mineral mixture is relatively suitable for granules, but it is also possible to arbitrarily modify the mixing ratio. After mixing the above ingredients according to a conventional granule preparation method, granules And can be used to prepare a health functional food composition according to a conventional method.
  • the resulting solution is filtered and obtained in a sterilized 2 L container, sealed and sterilized, and then stored in a refrigerator. It is used to prepare the functional beverage composition of the present invention.
  • composition ratio is a mixture of ingredients suitable for a relatively preferred beverage in a preferred embodiment, but the mixing ratio may be arbitrarily modified according to regional and ethnic preferences such as the demand class, the country of demand, and the purpose of use.

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Abstract

La présente invention concerne du ginsénoside Rf, une composition de ginsénoside comprenant du ginsénoside Rf, ou un mélange de l'un quelconque ou de plusieurs parmi ceux-ci, qui promeut l'expression d'une chaîne lourde de myosine, qui est un marqueur de différenciation musculaire, régule l'homéostasie énergétique dans le corps, promeut la phosphorylation de l'AMPK, qui joue un rôle important dans la régulation du développement et de la croissance des muscles squelettiques, et dans le test de nage forcée dans des expérimentations sur des animaux, augmente la durée de la nage, ce qui permet d'augmenter la capacité d'exercice, la force musculaire, et la masse musculaire et d'atténuer l'atrophie musculaire, et peut ainsi servir de composition alimentaire pour l'amélioration de la fonction musculaire, de composition cosmétique pour l'amélioration de la fonction musculaire, de composition alimentaire pour l'atténuation ou la prévention de la sarcopénie, ou de composition pharmaceutique pour le traitement ou la prévention de la sarcopénie.
PCT/KR2020/014832 2019-10-28 2020-10-28 Composition pour l'amélioration de la fonction musculaire comprenant du ginsénoside rf, composition de ginsénoside comprenant du ginsénoside rf, ou mélange de l'un quelconque ou plusieurs de ceux-ci en tant que principe actif WO2021086017A1 (fr)

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