WO2022071117A1 - Composition anti-fatigue et composition pour améliorer, supprimer la réduction de, et maintenir la performance de production d'énergie - Google Patents

Composition anti-fatigue et composition pour améliorer, supprimer la réduction de, et maintenir la performance de production d'énergie Download PDF

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Publication number
WO2022071117A1
WO2022071117A1 PCT/JP2021/035097 JP2021035097W WO2022071117A1 WO 2022071117 A1 WO2022071117 A1 WO 2022071117A1 JP 2021035097 W JP2021035097 W JP 2021035097W WO 2022071117 A1 WO2022071117 A1 WO 2022071117A1
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Prior art keywords
sesamin
lutein
fatigue
composition
fatty acid
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PCT/JP2021/035097
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English (en)
Japanese (ja)
Inventor
千絵 阿部
友紀 八木田
いづみ 川▲崎▼
佳子 小野
高生 田中
大輔 竹本
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サントリーホールディングス株式会社
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Priority to JP2022553898A priority Critical patent/JPWO2022071117A1/ja
Priority to KR1020237012019A priority patent/KR20230079092A/ko
Priority to CN202180067608.4A priority patent/CN116322370A/zh
Priority to AU2021354418A priority patent/AU2021354418A1/en
Publication of WO2022071117A1 publication Critical patent/WO2022071117A1/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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals

Definitions

  • the present invention relates to an anti-fatigue composition.
  • the present invention also relates to a composition for improving, suppressing or maintaining energy producing ability.
  • the present invention also relates to the use of one or more of sesamin and lutein and / or fatty acid esters thereof for suppressing, reducing or ameliorating fatigue.
  • the present invention further relates to the use of one or more sesamin and lutein and / or fatty acid esters thereof for improving, suppressing or maintaining energy production capacity.
  • Energy production refers to the production of energy necessary for humans and non-human animals to maintain their activity. Most of the energy production takes place in mitochondria, one of the organelles. Nutrient sources such as sugars, lipids, and amino acids taken from the diet are metabolized by glycolysis, the pentose phosphate pathway, and the citric acid cycle, and converted to NADH (nicotinamide adenine dinucleotide). The NADH electrons are then transferred to the mitochondrial respiratory chain protein (electron transport chain) to produce energy in the form of ATP (adenosine triphosphate). It is known that when ATP production decreases, for example, in humans, various problems such as obesity due to decreased metabolic capacity, increased risk of developing diabetes, decreased muscle strength, increased fatigue, decreased lethargy / concentration, and depression are caused. There is.
  • Maintaining ATP production is important for reducing fatigue, maintaining concentration, exercising with muscles, and maintaining physical and mental vitality.
  • Patent Document 1 describes a composition for improving energy production and metabolism from an intracellular fatty acid containing xanthophyll as an active ingredient.
  • Non-Patent Documents 1 and 3 the substrate required for ATP production is converted to ATP via the mitochondrial electron transport chain, but if the substrate increases but the mitochondrial function declines, it produces ATP. It is not possible. It is known that the decrease in mitochondrial function is caused by aging and oxidative stress, and the amount of ATP produced decreases (Non-Patent Documents 1 and 3).
  • Sesamin is a lignan compound contained in sesame and has been reported to have an antioxidant effect. It has been reported that sesamin has an inhibitory effect on mitochondrial function decline due to an antioxidant effect in a diabetic model mouse (Non-Patent Document 4). Further, it is known that sesamin exerts an action of suppressing the production of active oxygen in mitochondria and an action of suppressing a decrease in the membrane potential of mitochondria due to its antioxidant action (Non-Patent Document 2). In addition, it has been reported that sesamin activates PGC1 ⁇ involved in mitochondrial biosynthesis (Patent Document 2).
  • Non-Patent Document 5 lutein has been reported to have an action of activating mitochondrial function in nerve cell lines. It has been reported that ingestion of a mixture containing lutein improves psychological stress (Non-Patent Document 6) and eye strain (Non-Patent Documents 7 and 8).
  • the present invention provides a composition capable of improving, suppressing or maintaining mitochondrial function, effective for improving, suppressing or maintaining energy production ability, and anti-fatigue, and having high safety and continuous ingestion.
  • the purpose is to provide.
  • the present inventors have diligently studied to solve the above problems, and have investigated components that can be used to improve, suppress or maintain mitochondrial function. Then, by combining sesamines which are components for maintaining or activating mitochondrial function with lutein and / or fatty acid esters thereof which are components for activating mitochondrial function, sesamines alone or lutein and / or fatty acid esters thereof can be obtained. It has been found that mitochondrial function and energy production capacity can be improved, suppressed or maintained more effectively (synergistically) than when used alone.
  • the present invention includes, but is not limited to, the following anti-fatigue compositions, compositions for improving, suppressing or maintaining energy production ability, and the like.
  • An anti-fatigue composition containing one or more of sesamin and lutein and / or a fatty acid ester thereof.
  • the composition according to the above [1] which suppresses, reduces or improves fatigue by improving, suppressing or maintaining energy production ability.
  • a composition for improving, suppressing or maintaining an energy-producing ability containing one or more of sesamin and lutein and / or a fatty acid ester thereof.
  • composition Selected from the group consisting of "reduction of fatigue”, “reduction of fatigue”, “reduction of discomfort”, “suppression of decrease in activity motivation”, “helping energy production” and “maintenance and improvement of vitality”.
  • the composition according to any one of the above [1] to [9], which is labeled with one or more.
  • [11] Use of one or more of sesamin and lutein and / or its fatty acid ester for suppressing, reducing or ameliorating fatigue.
  • Use of one or more of sesamin and lutein and / or its fatty acid ester for improving, suppressing or maintaining energy production ability.
  • a composition capable of improving, suppressing or maintaining mitochondrial function, effective for improving, suppressing or maintaining energy production ability, and anti-fatigue, highly safe, and continuously ingestible. can be provided.
  • FIG. 1 is a graph showing the effects of sesamin / episesamin mixture (SE) and lutein on ATP production.
  • the anti-fatigue composition of the present invention contains one or more of sesamin and lutein and / or a fatty acid ester thereof.
  • the anti-fatigue composition of the present invention contains one or more of sesamin and lutein and / or a fatty acid ester thereof as active ingredients.
  • the composition for improving, suppressing or maintaining the energy producing ability of the present invention contains one or more of sesamin and lutein and / or a fatty acid ester thereof.
  • the composition for improving, suppressing or maintaining the energy producing ability of the present invention contains one or more of sesamin and lutein and / or a fatty acid ester thereof as active ingredients.
  • Energy production refers to the production of energy necessary for humans or non-human animals to maintain their activity.
  • the composition for anti-fatigue of the present invention and the composition for improving, suppressing or maintaining the energy producing ability are collectively referred to as the composition of the present invention below.
  • sesamin is a general term for compounds containing sesamin and its analogs. Sesamin is one of the major lignan compounds contained in sesame seeds. Examples of sesamin analogs include episesamin and dioxabicyclo [3.3.0] octane derivatives described in JP-A-4-9331. As one or more kinds of sesamin, one kind of these compounds may be used alone, or two or more kinds may be used. Specific examples of sesamin include sesamin, episesamin, sesaminol, episesaminol, sesamol, sesamolin and the like, and these stereoisomers or racemates can be used alone or in combination.
  • sesamin and / or episesamin can be preferably used as one or more of the sesamin, and sesamin and episesamin can be more preferably used.
  • sesamin and episesamin their ratios are not particularly limited, but for example, sesamin: episesamin (weight ratio) is preferably 1: 0.1 to 1: 9, and more preferably 1: 0.3 to 1: 3. , 1: 0.5 to 1: 2 are more preferable.
  • sesamin used in the present invention is not limited by its form, production method, or the like.
  • Sesamin is one of the main lignan compounds of sesame, and is contained in sesame in an amount of about 0.5 to 1.0% by weight.
  • sesamin referred to as sesamin extract or purified product
  • a known method for example, the method described in JP-A-4-9331
  • commercially available sesame oil liquid can be used as it is.
  • sesame oil liquid
  • the flavor peculiar to sesame oil may be evaluated to be sensually unfavorable.
  • a tasteless and odorless sesamin extract (or refined sesamin) extracted from sesame oil is used. Is preferable.
  • sesame oil the sesamin content is low, and if a preferred amount of sesamin is to be added, the volume of the prescribed composition per unit dose becomes too large, which may cause inconvenience in intake. ..
  • the product tablettes, etc.
  • sesamin and episesamin can be synthesized by the method of Beroza et al. (J. Am. Chem. Soc., 78, 1242 (1956)).
  • the metabolites of sesamin and episesamin can be synthesized by the method of Urata et al. (Chem. Pharma. Bull. (Tokyo), 56 (11) 1611-2 (2008)).
  • the composition of the present invention comprises lutein and / or a fatty acid ester thereof.
  • Lutein is a type of carotenoid.
  • Lutein and / or its fatty acid ester is contained in plants and the like, and can be prepared by extracting from plants, for example.
  • Fatty acid esters of lutein are used in, for example, green-yellow vegetables such as spinach, kale, broccoli, pumpkin, carrots and paprika; fruits such as oranges, peaches, papayas, prunes, mangoes, avocados, raspberries and rose hips; and petals of marigolds. include.
  • a plant-derived raw material or the like rich in lutein and / or a fatty acid ester thereof may be contained in the composition of the present invention as long as the effects of the present invention are exhibited.
  • Commercially available products can also be used for lutein and / or its fatty acid ester.
  • the fatty acid ester of lutein is a fatty acid ester in which a fatty acid is bound to one or two hydroxyl groups of lutein.
  • Examples of the fatty acid in the fatty acid ester of lutein include fatty acids having 4 to 20 carbon atoms, and preferably fatty acids having 8 to 18 carbon atoms.
  • the fatty acid ester of lutein may be one kind or two or more kinds. Hydrolysis of fatty acid esters of lutein produces lutein.
  • Sesamin and lutein and / or its fatty acid ester are compounds contained in natural products and foods and drinks, have abundant eating experience, and are recognized for their high safety. Therefore, sesamin and lutein and / or its fatty acid esters are suitable for continuous and long-term ingestion.
  • the composition of the present invention contains one or more of the above sesamin and lutein and / or a fatty acid ester thereof as active ingredients.
  • the combination of sesamin and lutein and / or its fatty acid ester yields remarkably excellent effects in improving, suppressing or maintaining mitochondrial function.
  • By improving, suppressing or maintaining mitochondrial function it is possible to obtain an effect of improving, suppressing or maintaining energy production ability.
  • the improvement, suppression or maintenance effect of mitochondrial function obtained by the combination of sesamines and lutein and / or its fatty acid ester, and the improvement, reduction suppression or maintenance effect of energy production ability are the sesamines or lutein and /.
  • the composition of the present invention lutein and lutein with respect to the total content of sesamines from the viewpoint of synergistically enhancing the effect of improving the mitochondrial function, the effect of suppressing or maintaining the decrease, the effect of improving the energy production ability, the effect of suppressing the decrease or the effect of maintaining the effect.
  • the weight ratio of the total content of the fatty acid ester in terms of lutein ((the value of lutein in terms of the total content of lutein and / its fatty acid ester) / the total content of sesamines) is 0.005 to 200. Is preferable, 0.01 to 40 is more preferable, and 0.4 to 16 is even more preferable.
  • the molar ratio of lutein and / or its fatty acid ester to sesamin is preferably 0.003 to 125, more preferably 0.006 to 25, and 0.25 to 10. Is more preferable, and 0.3 to 10 is particularly preferable.
  • the above-mentioned molar ratio is the ratio of the total number of moles of lutein and / or its fatty acid ester to the total number of moles of sesamine ((total number of moles of lutein and / or its fatty acid ester) / total number of moles of sesamine). ..
  • the ratio of sesamin to lutein and / or its fatty acid ester is in the above range from the viewpoint of anti-fatigue action.
  • the composition for improving, suppressing or maintaining energy production ability of the present invention is used, for example, to improve, suppress or maintain energy production ability through improvement, suppression or maintenance of mitochondrial function. Can be done.
  • the composition of the present invention can be used as a composition for improving, suppressing or maintaining energy production ability through improvement, suppression or maintenance of mitochondrial function.
  • the anti-fatigue composition of the present invention can suppress, reduce or improve fatigue by improving, suppressing or maintaining energy production ability, and can be used for such a purpose.
  • the anti-fatigue composition of the present invention can be used to suppress, reduce or improve fatigue by improving, suppressing or maintaining energy production ability through improvement, suppression or maintenance of mitochondrial function.
  • sesamin and lutein and / or its fatty acid ester By using one or more of sesamin and lutein and / or its fatty acid ester, these mitochondrial function improving action, lowering inhibitory action or maintenance action, and energy production ability improving action, lowering inhibitory action or maintenance action can be obtained. Can be increased synergistically. As a result, when sesamines and lutein and / or its fatty acid ester are used as an active ingredient for improving, suppressing or maintaining energy production ability, or as an active ingredient for anti-fatigue, the active ingredient is produced at a low dose. Even if it is present, the above-mentioned action can be exerted, so that the intake amount of the active ingredient can be reduced. Reducing the amount of intake leads to ease of intake, and it is possible to obtain an anti-fatigue composition that is easier to continuously ingest, a composition for improving, suppressing or maintaining energy production ability, and the like.
  • fatigue refers to diminished physical or mental activity and / or diminished mental vitality. Fatigue is usually accompanied by a feeling of fatigue (eg, discomfort, decreased activity motivation, etc.). Anti-fatigue means suppressing, reducing or improving fatigue. Fatigue control includes increasing tolerance to fatigue, preventing fatigue (including reducing risk in subjects at risk of fatigue), and the like. Reducing fatigue includes reducing symptoms of fatigue (eg, feeling tired) and the like. Improvement of fatigue includes recovery from fatigue, improvement of fatigue symptoms, and the like.
  • the anti-fatigue composition of the present invention shall be used for suppressing, reducing or ameliorating physical fatigue and / or mental fatigue, and for suppressing, reducing or ameliorating physical fatigue and / or mental fatigue.
  • the anti-fatigue composition of the present invention can be used, for example, for the prevention or amelioration of fatigue-related conditions or diseases.
  • Fatigue-related conditions or illnesses include chronic fatigue syndrome.
  • Prevention of a condition or disease includes preventing the onset, delaying the onset, reducing the incidence, reducing the risk of onset, and the like. Improvement of a condition or disease is to recover the subject from the condition or disease, alleviate the symptoms of the condition or disease, improve the symptoms of the condition or disease, delay the progression of the condition or disease, or prevent it. Etc. are included.
  • the compositions of the present invention can be applied to either therapeutic or non-therapeutic use.
  • Non-therapeutic is a concept that does not include medical practice, ie human surgery, treatment or diagnosis.
  • the mitochondrial function may be evaluated based on ordinary knowledge in the technical field to which the present invention belongs, and the method thereof is not particularly limited.
  • OCR oxygen consumption rate
  • Mitochondrial function can be assessed by continuous measurement with the addition of a conjugate (eg, carbonyl cyanide-p-trifluoromethoxyphenylhydrazone (FCCP)).
  • FCCP carbonyl cyanide-p-trifluoromethoxyphenylhydrazone
  • the evaluation item can evaluate mitochondrial function by analyzing, for example, basal respiratory volume, ATP-producing ability or maximum respiratory volume, which are the main indicators in the evaluation of mitochondrial function.
  • the composition of the present invention can be in the form of foods and drinks, pharmaceuticals, quasi-drugs, feeds and the like.
  • the composition of the present invention may be a food or drink, a pharmaceutical product, a quasi-drug, a feed or the like for anti-fatigue itself or for improving, suppressing or maintaining energy production ability, and these may be used. It may be a material or a preparation used in combination with.
  • the composition of the present invention can be provided, as an example, in the form of an agent, but is not limited to this form.
  • the agent can be provided as it is as a composition or as a composition containing the agent.
  • the anti-fatigue composition of the present invention can also be referred to as an anti-fatigue agent.
  • the composition of the present invention may be either an oral composition or a parenteral composition, but is preferably an oral composition.
  • oral composition include foods and drinks, oral medicines, quasi-drugs, and feeds, preferably foods and drinks or oral medicines, and more preferably foods and drinks.
  • the composition of the present invention may contain any additive and any component in addition to one or more of sesamin and lutein and / or a fatty acid ester thereof, as long as the effects of the present invention are not impaired.
  • additives and components can be selected according to the form of the composition and the like, and generally, those that can be used for foods and drinks, pharmaceuticals, quasi-drugs, feeds and the like can be used.
  • the composition of the present invention is a food or drink, a pharmaceutical product, a quasi-drug, a feed or the like, the production method thereof is not particularly limited and can be produced by a general method.
  • composition of the present invention when used as a food or drink, one or more of sesamin and lutein and / or a fatty acid ester thereof are mixed with components that can be used in the food or drink (for example, food materials, foods used as necessary). Additives, etc.) can be blended to make various foods and drinks.
  • the food and drink is not particularly limited, and examples thereof include general food and drink, health food, health drink, food with functional claims, food for specified health use, food and drink for the sick, and the like.
  • the above-mentioned health foods, foods with functional claims, foods for specified health use, etc. include, for example, various types of fine granules, tablets, granules, powders, capsules, chewables, dry syrups, syrups, liquids, beverages, liquid foods, etc. It can be used as a pharmaceutical form.
  • composition of the present invention is a pharmaceutical product or a quasi-drug, for example, it is added to one or more of sesamines and lutein and / or a fatty acid ester thereof with a pharmacologically acceptable carrier and, if necessary.
  • Additives and the like can be added to make various dosage forms of drugs or quasi-drugs.
  • Such carriers, additives and the like may be pharmacologically acceptable as long as they can be used in pharmaceutical products or quasi-drugs, for example, excipients, binders, disintegrants, lubricants, etc. 1 or 2 or more of antioxidants, colorants and the like can be mentioned.
  • Examples of the administration (ingestion) form of the drug or quasi-drug include oral or parenteral (transdermal, transmucosal, enteral, injection, etc.) administration.
  • oral or parenteral (transdermal, transmucosal, enteral, injection, etc.) administration When the composition of the present invention is a drug or a quasi-drug, it is preferably an oral drug or a quasi-drug.
  • Dosage forms for oral administration include liquids, tablets, powders, fine granules, granules, sugar-coated tablets, capsules, suspensions, emulsions, chewables and the like.
  • the drug may be a non-human animal drug.
  • composition of the present invention When the composition of the present invention is used as a feed, one or more of sesamin and lutein and / or a fatty acid ester thereof may be added to the feed.
  • the feed also contains feed additives. Examples of the feed include livestock feed used for cattle, pigs, chickens, sheep, horses and the like; small animal feed used for rabbits, rats, mice and the like; pet food used for dogs, cats, small birds and the like.
  • the content of sesamin contained in the composition of the present invention is not particularly limited and can be set according to the form and the like.
  • the total content of sesamin in the composition of the present invention is, for example, preferably 0.001% by weight or more, more preferably 0.01% by weight or more, still more preferably 0.05% by weight or more in the composition. Further, 10% by weight or less is preferable, and 5% by weight or less is more preferable.
  • the total content of sesamin is preferably 0.001 to 10% by weight, more preferably 0.01 to 10% by weight, still more preferably 0.05 to 5% by weight in the composition.
  • the total content of lutein and / or its fatty acid ester contained in the composition of the present invention is not particularly limited and can be set according to its form and the like.
  • the total content of lutein and / or its fatty acid ester in the composition of the present invention is preferably 0.001% by weight or more, more preferably 0.01% by weight or more in the composition in terms of lutein, for example. It is more preferably 0.05% by weight or more, more preferably 10% by weight or less, and even more preferably 5% by weight or less.
  • the total content of lutein and / or its fatty acid ester is preferably 0.001 to 10% by weight, more preferably 0.01 to 10% by weight, and 0.05 to 0.05% by weight in the composition in terms of lutein. 5% by weight is more preferable.
  • the composition of the present invention is preferably taken orally (orally administered).
  • the dose (which can also be referred to as ingestion) of the composition of the present invention is not particularly limited.
  • the dose of the composition of the present invention is such that an effect of improving, suppressing or maintaining mitochondrial function, an effect of improving, suppressing or maintaining energy production ability, and / or an anti-fatigue effect can be obtained. It may be appropriately set according to the administration form, administration method, body weight of the subject, and the like.
  • the total dose of sesamin is 60 kg / day of body weight, preferably 0.5 mg or more, more preferably. It is 1 mg or more, more preferably 3 mg or more, preferably 200 mg or less, more preferably 100 mg or less, still more preferably 80 mg or less.
  • the total dose of lutein and / or its fatty acid ester is preferably 0.5 mg or more, more preferably 1 mg or more, still more preferably 3 mg or more, and preferably 200 mg or less per 60 kg of body weight per day in terms of lutein. , More preferably 100 mg or less, still more preferably 80 mg or less.
  • the total dose of sesamin is preferably 0.5 to 200 mg, more preferably 1 to 100 mg, still more preferably 3 to 80 mg per 60 kg body weight per day for humans (adults).
  • the total dose of lutein and / or its fatty acid ester is preferably 0.5 to 200 mg, more preferably 1 to 100 mg, more preferably 1 to 100 mg per 60 kg of body weight per day for humans (adults) in terms of lutein. Is 3-80 mg. It is preferable to ingest or administer the above amount once or more a day, for example, once a day or several times (for example, 2 to 3 times).
  • the above amounts of sesamin and lutein and / or a fatty acid ester thereof are orally ingested or administered to humans.
  • the composition of the present invention can be used to ingest or administer the above amounts of sesamin and lutein and / or its fatty acid ester per 60 kg body weight per day to humans.
  • the total dose of sesamin is the total dose when two or more sesamin compounds are used.
  • the total dose of lutein and / or its fatty acid ester is the total amount of lutein and its fatty acid ester.
  • sesamin and / or episesamin is used as the total dose of sesamin and / or episesamin at a body weight of 60 kg per day, preferably 0.5 to 200 mg, more preferably 1 to 100 mg, still more preferably 3 to 80 mg. It is preferable to ingest or administer it orally to humans (adults).
  • composition of the present invention is preferably continuously ingested or administered. It is expected that a higher effect can be obtained by continuously ingesting or administering sesamin and lutein and / or its fatty acid ester.
  • the composition of the present invention is preferably ingested or administered continuously for 1 week or longer, more preferably 4 weeks or longer, still more preferably 8 weeks or longer, and particularly preferably 12 weeks or longer. preferable.
  • the subject to ingest or administer the composition of the present invention is not particularly limited, and examples thereof include humans and animals other than humans.
  • animals other than humans include industrial animals, pets, experimental animals and the like.
  • industrial animals include livestock such as cattle, horses, pigs, goats and sheep, poultry such as chickens, ducks, quail, turkeys and ostriches, as well as yellowtail, hamachi, madai, maji, koi, nigga and eel. It refers to animals that are industrially required to be bred, such as fish such as yellowtail.
  • Pets are so-called companion animals such as dogs, cats, marmosets, birds and hamsters, and companion animals, and experimental animals are mice, rats, guinea pigs, beagle dogs, miniature pigs, lizard monkeys and crab monkeys, etc., medicine, biology, agriculture. And represents animals used for research in fields such as pharmaceuticals.
  • the administration target of the composition of the present invention is preferably a human or a non-human mammal, and more preferably a human.
  • the subject to be administered is a subject who needs or desires improvement, suppression or maintenance of mitochondrial function, a subject who needs or desires improvement, suppression or maintenance of energy production ability, and suppression of fatigue. , Targets that need or desire mitochondria or improvements.
  • mitochondrial function decreases with aging and energy production ability decreases.
  • middle-aged and elderly people are preferable as the target of the composition of the present invention.
  • the composition of the present invention may be an anti-fatigue composition for middle-aged and elderly people (preferably for elderly people), and a composition for improving, suppressing or maintaining energy production ability.
  • the middle-aged person may be, for example, a human being 40 years or older. Middle-aged and elderly people include the elderly. Further, the composition of the present invention is intended for a healthy person for the purpose of obtaining, for example, an effect of improving, suppressing or maintaining mitochondrial function, an effect of improving, suppressing or maintaining energy production ability, and an anti-fatigue effect. Can also be used.
  • the composition of the present invention includes, for example, "reduction of fatigue”, “reduction of fatigue”, “reduction of discomfort”, “suppression of decrease in motivation for activity”, “helping energy production”, and “maintenance and improvement of vitality”.
  • “It is hard to feel fatigue”, “Maintaining vitality”, “Full of energy”, etc. may be attached with one or more indications.
  • the composition of the present invention “reduces fatigue”, “reduces fatigue”, “reduces discomfort”, “suppresses a decrease in motivation for activity”, “helps energy production” and “maintains vitality”. It may have one or more indications selected from the group consisting of "improvement”.
  • the feeling of fatigue may be easily felt with aging.
  • Energy production may be that produced by cells or mitochondria.
  • the composition of the present invention is preferably a food or drink with the above indication. Further, the above display may be a display to the effect that it is used to obtain the above function.
  • the present invention also includes the use of one or more sesamin for producing anti-fatigue compositions, as well as the use of lutein and / or fatty acid esters thereof.
  • the present invention also includes the use of one or more sesamin for producing compositions for improving, suppressing or maintaining energy production, as well as the use of lutein or its fatty acid esters.
  • the present invention also includes the following methods.
  • the present invention also includes the following uses. Use of one or more sesamin and lutein and / or fatty acid esters thereof for the control, reduction or amelioration of fatigue. Use of one or more of sesamin and lutein and / or fatty acid esters thereof for improving, suppressing or maintaining energy production ability.
  • the method or use may be a therapeutic method or use, or may be a non-therapeutic method or use.
  • By administering one or more of sesamin and lutein and / or its fatty acid ester to a subject it becomes possible to improve, suppress or maintain mitochondrial function, thereby improving, suppressing or maintaining energy production ability. , Anti-fatigue effect can be obtained. Fatigue is preferably physical fatigue.
  • One or more of the sesamin, and lutein and / or its fatty acid ester may be administered simultaneously or separately, but preferably at the same time.
  • the lutein-equivalent weight ratio of the total dose of lutein and / or its fatty acid ester to the total dose of sesamine ((lutein-equivalent value of the total dose of lutein and / or its fatty acid ester) / sesamine).
  • the total dose) is preferably 0.005 to 200, more preferably 0.01 to 40, still more preferably 0.4 to 16.
  • sesamin one kind of compound of sesamin may be used, and two or more kinds may be used.
  • Lutein and its fatty acid esters may be used.
  • the subject is administered at least once a day, for example, once to several times a day (for example, 2 to 3 times), one or more of sesamin, and lutein and / or its fatty acid ester. (Ingestion) is preferable.
  • the above use is preferably in humans or non-human mammals, more preferably in humans.
  • one or more kinds of sesamin in an amount (which can be said to be an effective amount) capable of obtaining a desired action, and lutein and / or a fatty acid ester thereof may be used.
  • the preferred doses of sesamin and lutein and / or its fatty acid ester, the subject of administration, and the like are the same as those of the above-mentioned composition of the present invention.
  • Sesamin and lutein and / or its fatty acid ester may be administered as they are, or may be administered as a composition containing them.
  • the composition of the present invention described above may be used.
  • one or more kinds of sesamines (or a composition containing the same) and lutein and / or a fatty acid ester thereof (or a composition containing the same) are individually prepared and prepared at almost the same time. Or, if one is ingested or administered and then the other is ingested or administered while the effect is sustained, it contains one or more of the sesamines intended by the present invention, and lutein and / or a fatty acid ester thereof.
  • An effect of enhancing the effect of the composition improvement of mitochondrial function, suppression or maintenance effect of reduction, improvement of energy production ability, suppression or maintenance effect of reduction, and / or anti-fatigue effect
  • kits or the like containing one or more kinds of sesamin (or a composition containing the same) and lutein and / or a fatty acid ester thereof (or a composition containing the same) is also included in the scope of the present invention.
  • sesamin / episesamin mixture a mixture of sesamin and episesamin having a weight ratio of sesamin: episesamin of 1: 1 was used as the sesamin / episesamin mixture.
  • the sesamin / episesamin mixture may be referred to as SE.
  • Examples 1 to 3 Evaluation test of mitochondrial function of cells treated with sesamin / episesamin mixture (SE) and lutein>
  • SE sesamin / episesamin mixture
  • lutein a substance that influences mitochondrial function.
  • TIG-3 cells fetal lung-derived cells
  • the sesamin / episesamin mixture and lutein were added to the medium in the wells at the concentrations shown in Table 1 below, respectively, and cultured for 24 hours.
  • the molar ratio of lutein to sesamin in the medium was 0.3 in Example 1, 3 in Example 2, and 10 in Example 3.
  • the medium supplemented with the sesamin / episesamin mixture and lutein was removed, and the cells in the wells were treated with the medium supplemented with H2O 2 (800 ⁇ M) for 2 hours. Then, the medium was replaced with an analytical medium, and the oxygen consumption rate (pmol / min) was analyzed with an analytical instrument (XF analyzer, Agilent, Inc.). After the analysis was completed, the nuclei were stained with Hoechst He, the cells were photographed with a fluorescence microscope BZ-x (Keyence Co., Ltd.), and the number of cells was counted by image analysis. By measuring the amount of decrease in oxygen consumption of living cells with an XF analyzer, the amount of ATP produced indicating mitochondrial function can be evaluated.
  • ATP synthase inhibition (oligomycin) was added to the well, and the amount of decrease in oxygen consumption rate due to the addition of oligomycin (pmol / min / 10 3 ). cells) were measured and used as the amount of ATP produced.
  • Basal respiration exhibits cellular energy demand under baseline conditions, and a portion of basal respiration is used for ATP production.
  • the amount of decrease in oxygen consumption rate due to the addition of oligomycin indicates the amount of ATP produced. The results obtained are shown in Table 1.
  • ⁇ Reference example 1 Evaluation test of mitochondrial function in the untreated group> To examine mitochondrial function, 5.5 ⁇ 10 3 cells / well TIG-3 cells were seeded on a dedicated plate and cultured at 37 ° C. and CO 2 (5%) for 24 hours. After 24 hours of culturing, the cells were further cultured for 26 hours without adding the sesamine / episesamine mixture and lutein to the medium and treating the cells in the wells with H2O2 ( 800 ⁇ M) -added medium for 2 hours. Except for the above, the oxygen consumption rate in Reference Example 1 was analyzed and the number of cells was counted in the same manner as in Example 1. In addition, the amount of ATP produced was measured. The results obtained are shown in Table 1.
  • ⁇ Comparative Example 1 Evaluation test of mitochondrial function in H 2 O 2 treatment group> To examine mitochondrial function, 5.5 ⁇ 10 3 cells / well TIG-3 cells were seeded on a dedicated plate and cultured at 37 ° C. and CO 2 (5%) for 24 hours. After 24 hours of culturing, the oxygen consumption rate in Comparative Example 1 was analyzed in the same manner as in Example 1 except that the sesamin / episesamin mixture and lutein were further cultured for 24 hours without addition to the medium, and the number of cells was analyzed. Was counted. In addition, the amount of ATP produced was measured. The results obtained are shown in Table 1.
  • ⁇ Comparative Examples 2 to 5 Evaluation test of mitochondrial function of cells treated with sesamin / episesamin mixture or lutein> To examine mitochondrial function, 5.5 ⁇ 10 3 cells / well TIG-3 cells were seeded on a dedicated plate and cultured at 37 ° C. and CO 2 (5%) for 24 hours. After 24 hours of culturing, a sesamin / episesamin mixture (Comparative Example 2) or lutein (Comparative Examples 3 to 5) was added to the medium in the wells at the concentrations shown in Table 1 below, and the cells were cultured for 24 hours. Other than this, the oxygen consumption rate in Comparative Examples 2 to 5 was analyzed in the same manner as in Example 1 above, and the number of cells was counted. In addition, the amount of ATP produced was measured. The results obtained are shown in Table 1.
  • the "measured value” (pmol / min / 10 3 cells) shows the amount of ATP produced (the amount of decrease in oxygen consumption rate due to ATP synthase inhibition) obtained above.
  • the “measured value” of Examples 1 to 3 and Comparative Examples 1 to 5 shown in Table 1 is divided by the “measured value” of Comparative Example 1 and multiplied by 100 (100 ⁇ (Example or Comparative Example). (Actually measured value) / (actually measured value of Comparative Example 1)) is shown in Table 1 as "relative value (%)" (relative value with respect to Comparative Example 1).
  • FIG. 1 shows the recovery rate (%) (recovery rate with respect to Comparative Example 1) obtained for Examples and Comparative Examples.
  • SE represents a sesamin / episesamin mixture.
  • “Comparative Example 4 + Comparative Example 2” is the sum of the recovery rate of Comparative Example 2 and the recovery rate of Comparative Example 4, and "Comparative Example 5 + Comparative Example 2” is compared with the recovery rate of Comparative Example 2.
  • Example 5 It is the sum of the recovery rates of Example 5.
  • “Comparative Example 4 + Comparative Example 2” and “Comparative Example 5 + Comparative Example 2” are sesamin predicted from the recovery rate in the case of sesamin alone (Comparative Example 2) and lutein alone (Comparative Example 4 or 5). The recovery rate when the class and lutein are combined (Examples 2 and 3) is shown.
  • the amount of ATP produced decreased by 47.5% with respect to the control group (Reference Example 1 ) by the 800 ⁇ M H2O2 treatment according to Comparative Example 1 .
  • the ATP production amounts were 5.4% and 1.3% higher than those of the H 2 O 2 treatment group according to Comparative Example 1, respectively.
  • the sesamin / episesamin mixture (100 nM) treatment according to Comparative Example 2 the amount of ATP produced was 2.8 % higher than that in the H2O2 treatment group according to Comparative Example 1.
  • Example 4 Human test> (Evaluation sample) A food product in which 10 mg of a sesamine / episesamine mixture and 10 mg of lutein were dispersed in edible vegetable oil with a glycerin fatty acid ester per 3 grains was encapsulated with a film containing gelatin and glycerin, and used as a test food. A food product prepared using the same raw materials as the test food except that the sesamin / episesamin mixture and lutein were not used was used as the control food. The test food and the control food had the same calorific value, protein amount, fat, and carbohydrate amount per three grains, and the two foods were indistinguishable from each other in terms of appearance and the like.
  • a Visual Analogue Scale was used to evaluate the feeling of fatigue. Specifically, regarding the degree of fatigue of the subject, the left end (0 cm) was defined as “the best feeling of not feeling tired at all", and the right end (10 cm) was defined as “the worst feeling of being exhausted so much that nothing could be done”. The subject himself was asked to mark which part of the straight line it would hit. Regarding the mark position, the distance (cm) from the left end of the 10 cm straight line was measured and used as the measured value of fatigue. From the measured values of fatigue feelings (1) to (5), the amount of change in fatigue feeling at each time point in the 8th week was calculated using the following formulas (i) to (iv).
  • Amount of change in fatigue at the time of visit (Fatigue at the time of visit in the 8th week (1))-(Fatigue at the time of visit in the 0th week (1)) Equation (i)
  • Amount of change in fatigue due to physical load ⁇ (Fatigue immediately after exercise load at week 8 (3))-(Fatigue after creperin test at week 8 (2)) ⁇ - ⁇ (Fatigue immediately after exercise load at week 0 (3))- (Fatigue after Kleperin test at week 0 (2)) ⁇ Equation (ii)
  • Amount of change in fatigue after a break (Fatigue after 60 minutes of exercise load in the 8th week (4))-(Fatigue after 60 minutes of exercise load in the 0th week (4)) Equation (iii)
  • Table 2 shows the results of changes in fatigue at the time of visit, which were analyzed by excluding subjects who violated the exclusion criteria (6 subjects in the test food group and 4 subjects in the control food group).
  • the significant difference test was performed by a paired t-test (before and after difference (for fatigue feeling at week 0) #: p ⁇ 0.10). Only in the test food group, the feeling of fatigue at the time of visit tended to improve. From this, it was confirmed that the composition containing sesamin and lutein improves the feeling of fatigue in daily life.
  • Table 3 shows the results (change amount of fatigue feeling) analyzed by the formulas (ii) to (iv) using the persons (8 persons per group) who were judged to have appropriately applied the load to the whole body.
  • the significant difference test was performed by the paired t-test for comparison before and after the test, and by the unpaired t-test for comparison between groups (before and after difference (for fatigue feeling at week 0) #: p ⁇ 0. 10, ⁇ : p ⁇ 0.05, difference between groups ⁇ : p ⁇ 0.10).
  • the improvement in fatigue due to physical load was greater in the test food group. From this, it was found that the composition containing the combination of sesamin and lutein improves the feeling of fatigue when a body fatigue is applied. Ingestion of the test food significantly improved the feeling of fatigue after a break and the next morning. From this, it is considered that the composition containing sesamin and lutein acts on the recovery of fatigue after physical fatigue load and / or mental fatigue load.

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Abstract

Le but de la présente invention est de fournir une composition qui peut améliorer, supprimer la réduction de, ou maintenir une fonction mitochondriale, qui est efficace dans l'amélioration, la suppression de la réduction de ou le maintien de la production d'énergie et qui est efficace contre la fatigue, et qui est très sûre et peut être ingérée en continu. La présente invention se rapporte à une composition anti-fatigue contenant un ou plusieurs types de sésamine, et de la lutéine et/ou un ester d'acide gras de cette dernière.
PCT/JP2021/035097 2020-10-02 2021-09-24 Composition anti-fatigue et composition pour améliorer, supprimer la réduction de, et maintenir la performance de production d'énergie WO2022071117A1 (fr)

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CN202180067608.4A CN116322370A (zh) 2020-10-02 2021-09-24 抗疲劳用组合物及用于能量产生能的提高、降低抑制或维持的组合物
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WO2008126587A1 (fr) * 2007-03-15 2008-10-23 Suntory Holdings Limited Agent anti-fatigue
CN103446197A (zh) * 2013-09-11 2013-12-18 白心亮 一种新型保肝制品
JP2016135765A (ja) * 2009-09-18 2016-07-28 株式会社明治 筋拘縮予防剤

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JP2009215170A (ja) 2008-03-06 2009-09-24 Fuji Chem Ind Co Ltd エネルギー産生代謝向上組成物
JP6882622B2 (ja) 2016-11-14 2021-06-02 株式会社ケーヒン 車両用空調装置

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WO2008126587A1 (fr) * 2007-03-15 2008-10-23 Suntory Holdings Limited Agent anti-fatigue
JP2016135765A (ja) * 2009-09-18 2016-07-28 株式会社明治 筋拘縮予防剤
CN103446197A (zh) * 2013-09-11 2013-12-18 白心亮 一种新型保肝制品

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RIARUMEITO [REAL MATE]: "[Meclear Lutein 20mg (Naturally Derived Free) Cassis Anthocyanin Sesamin Seeing Power Supplement / Supplement for about 1 month]", 16 May 2019 (2019-05-16), JP, pages 1 - 12, XP009536052, Retrieved from the Internet <URL:https://www.amazon.co.jp/%E8%96%AC%E5%89%A4%E5%B8%AB%E3%81%8C%E7%9B%A3%E4%BF%AE%E3%81%97%E3%81%9F%E7%9B%AE%E3%81%AE%E3%82%B5%E3%83%97%E3%83%AA-%E3%82%A2%E3%83%B3%E3%83%88%E3%82%B7%E3%82%A2%E3%83%8B%E3%83%B3-%E7%9B%AE%E3%81%AE%E7%96%B2%E3%82%8C%EF%BC%88%E3%82%BB%E3%82%B5%E3%83%9F%E3%83%B3-%E3%82%A2%E3%83%B3%E3%83%88%E3%82%B7%E3%82%A2%E3%83%8B%E3%83%B3%EF%BC%89-%E3%83%AA%E3%82%A2%E3%83%AB%E3%83%A1%E3%82%A4%E3%83%88/dp/B08YYF2VCK> *

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