Composition for increasing vigor / vitality, composition for improving lethargy / lassitude

Abstract

The present invention addresses the problem of providing a composition for increasing vigor / vitality or a composition for improving lethargy / lassitude.　Provided is a composition for increasing vigor / vitality or a composition for improving lethargy / lassitude that contains an agrimol. Provided is a composition for increasing vigor / vitality or a composition for improving lethargy / lassitude that contains an agrimony extract as an agrimol. The present invention makes it possible to provide a composition for increasing vigor / vitality or a composition for improving lethargy / lassitude.

Description

Composition for improving vitality and energy, composition for improving lethargy and fatigue

[0001] The present invention relates to a composition for improving vitality and energy and a composition for improving lethargy and fatigue. More specifically, the present invention relates to a composition for improving vitality and energy and a composition for improving lethargy and fatigue, which are used in the fields of pharmaceuticals, health foods, etc.

[0002] The global population has been aging in recent years, with the proportion of people aged 65 and over estimated to reach 16% by 2050, up from approximately 10% in 2022. While average life expectancy is increasing, age-related physical, mental, and social problems are on the rise, and the risk of death and caregiving among the elderly is increasing. Aging begins around the age of 40, and multiple factors, including genetic and environmental factors, cause a decline in various physiological functions. Proposed causes of aging include genomic instability, telomere shortening, epigenetic changes, loss of proteostasis, impaired autophagy, dysregulated nutrient sensing, mitochondrial dysfunction, cellular senescence, stem cell depletion, altered intercellular communication, chronic inflammation, and changes in the gut microbiota. Among these factors, cellular senescence is a particularly important one. Senescent cells, whose proliferation has irreversibly ceased due to cellular senescence, are not only unable to maintain their function in tissues but also known to reduce the function of surrounding normal cells through the Senescence-Associated Secretory Phenotype (SASP) and induce chronic inflammation, thereby accelerating aging. The decline in physiological function due to aging leads to vulnerability to various stresses and a decline in quality of life (QOL). QOL is defined as an individual's perception of their own life situation in relation to their goals, expectations, standards, and interests within the context of their culture and values. It is the ultimate goal of all health interventions and is assessed by physical and mental function as well as perceived well-being. QOL is related to mortality risk and prognosis and is an important factor in healthy longevity. In recent years, the extension of average life expectancy has placed greater emphasis on maintaining health for as long as possible, and the assessment of QOL has become an important factor in major global healthcare research.

[0003] In Japan, where the aging population is particularly rapid, extending healthy lifespan is an important issue. The present inventors have therefore been developing agrimony extract as a food ingredient with anti-aging properties. Agrimony, also known as Longyao Grass or Xianhe Grass, is a plant of the Rosaceae family traditionally used in traditional Chinese medicine. It is known to contain physiologically active compounds such as phloroglucinol, flavonoids, tannins, phenols, triterpenoids, and organic acids, including agrimols. Regarding anti-aging measures, it has been suggested that senolysis, the removal of senescent cells from the body, may improve physiological function decline due to aging. For example, Patent Document 1 confirms that agrimony extract and the agrimols contained therein have the ability to remove senescent cells. Furthermore, agrimony extract has been reported to have medicinal properties such as antioxidant, anti-inflammatory, antibacterial, antitumor, and antidiabetic effects, and is therefore attracting attention as a food ingredient with anti-aging properties.

[0004] Japanese Patent Application Laid-Open No. 2023-044668

[0005] In terms of QOL, improving vitality and energy and alleviating lethargy and fatigue are important, and in order to improve QOL, there is a need for a composition that improves vitality and energy and a composition that alleviates lethargy and fatigue. Therefore, an object of the present invention is to provide a composition for improving vitality and energy and a composition for alleviating lethargy and fatigue.

[0006] As a result of intensive research into the above-mentioned problems, the inventors discovered that compositions containing agrimols have the effect of improving vitality and energy, and of improving lethargy and fatigue, and thus completed the present invention.

[0007] That is, the present invention provides the following [1] to [7]. [1] A composition for improving vitality and energy, containing Agrimols. [2] A composition for improving lethargy and fatigue, containing Agrimols. [3] The composition according to [1] or [2], characterized in that the Agrimols are contained as a plant extract. [4] The composition according to [3], characterized in that the plant extract is an agrimony extract. [5] The composition according to [1] or [2], characterized in that the daily intake of the Agrimols is 0.1 mg or more. [6] The composition according to [1] or [2], characterized in that the intake period is 12 weeks or more. [7] The composition according to [1] or [2], characterized in that the subject to be treated is a person who feels that vitality and energy are reduced or who has lethargy and fatigue.

[0008] According to the present invention, it is possible to provide a composition for improving vitality and energy, and a composition for improving lethargy and fatigue.

[0009] 1 is a graph showing the effect of the composition containing Agrimols of the present invention in improving vitality and energy, and in improving lethargy and fatigue.

[0010] The composition for improving vitality and energy and the composition for improving lethargy and fatigue of the present invention will be described below. Hereinafter, these will be collectively referred to as "compositions." Furthermore, in this specification, when a numerical range is expressed as "X to Y" (X and Y are numerical values), it means a numerical range that includes both ends. Note that the compositions described in the embodiments are merely examples used to explain the present invention, and are not intended to be limiting.

[0011] [Composition] The composition for improving vitality and energy and the composition for improving lethargy and fatigue of the present invention are characterized by containing Agrimols, and can be used for medicines, foods, veterinary medicines, feed, etc. As for foods, in addition to ordinary foods, the composition of the present invention can be added to nutritional supplements, functional foods, health foods, foods for specified health uses, etc. in order to achieve the above-mentioned effects.

[0012] The composition of the present invention is an oral composition, and continuous ingestion of the composition has the effect of improving vitality and energy and ameliorating lethargy and fatigue. The effects of improving vitality and energy and ameliorating lethargy and fatigue can be evaluated using the Profile of Mood States (POMS) or the Profile of Mood States 2nd Edition (POMS2).

[0013] <Agrimols> The agrimols of the present invention are compounds represented by the following chemical formula 1. The agrimols of the present invention are not particularly limited as long as they are acceptable for use in pharmaceuticals, foods, veterinary medicines, feed, etc., and can be used by chemical synthesis or by extraction, separation, and purification from natural products such as plants. The agrimols may also be contained as a plant extract of a plant containing the agrimols. Furthermore, commercially available products available on the market can also be purchased and used. (wherein R1, R2, and R3 are independently a hydrocarbon group having 1 to 6 carbon atoms.)

[0014] Specific examples of Agrimols include Agrimol A to Agrimol G, and the compounds shown in the following chemical formulas 3 and 4 (hereinafter referred to as "compounds 3 and 4"). Agrimol B, compound 3, and compound 4 are preferred, and a mixture of Agrimol B, compound 3, and compound 4 is more preferred.

[0015] Agrimol B is a compound shown in the following chemical formula 2 (MW: 682.75).

[0016]

[0017] Agrimols can be chemically synthesized using phloroglucinol or the like as a starting material, for example, by the method described in Acta Pharmaceutica Sinica 1989, 24(6): pp. 431-437, or the method disclosed in JP-A-11-335256.

[0018] In addition, there are two types of Agrimols that can be obtained by synthesis: (S)-(+)-Agrimols and its optical isomer, (R)-(-)-Agrimols. In this specification, "Agrimols" may refer to a single compound consisting of one of these types, or a mixture consisting of two types.

[0019] The content of agrimols in the composition of the present invention is not particularly limited and can be changed depending on the purity and origin of the agrimols, the subject and purpose of administration, etc., but is, for example, 0.001 to 2% by mass of the total composition. The lower limit is more preferably 0.01% by mass or more, and even more preferably 0.02% by mass or more. On the other hand, the upper limit is more preferably 1% by mass or less, even more preferably 0.6% by mass or less, and most preferably 0.3% by mass or less. By setting the content of agrimols within the above range, the effects of the present invention can be more reliably achieved.

[0020] <Plant Extract> As described above, the composition of the present invention may contain agrimols as a plant extract. Such plant extracts are not particularly limited as long as they contain agrimols, but agrimony extract derived from agrimony is preferably used. Agrimony (scientific name: Agrimony pilosa) is a perennial plant of the genus Agrimonia in the family Rosaceae, and grows wild on forest edges, in fields, and along roadsides in Honshu, Shikoku, Kyushu, and other areas. It is also known as dragon's tooth plant. In the present invention, wild or cultivated whole plants can be collected and naturally or heat-dried and used. Alternatively, dried agrimony commercially available as an ingredient in herbal medicines, folk remedies, and health foods (herbal teas) can also be used. Dried whole agrimony plants are commercially available under the herbal name Senkakuso.

[0021] Examples of plant extracts in the present invention include extracts with water or various organic solvents, distillates obtained by steam distillation, dried powders, grated material, and juice squeezed from grated material. From the viewpoint of yield and purity of agrimony extract, extracts with water or various organic solvents are preferred, and extracts with ethyl alcohol or hydrous ethyl alcohol containing water are more preferred. Extraction with water or various organic solvents can be carried out using known extraction methods using water, various organic solvents, and mixtures thereof as solvents. Prior to extraction, raw materials or coarsely shredded materials may be washed with a hydrophobic or hydrophilic solvent, either alone or in a mixture, to remove unwanted materials such as pigments. Examples of hydrophobic solvents include chloroform, ether, hexane, cyclohexane, toluene, dichloromethane, petroleum ether, and benzene. Examples of hydrophilic solvents include lower alcohols (e.g., alcohols with 4 or fewer carbon atoms, such as methyl, ethyl, n-propyl, isopropyl alcohol, isobutyl alcohol, and butyl alcohol), ethyl acetate, acetone, and acetonitrile. If desired, water may be added to the raw materials to moisten them.

[0022] To perform extraction with water, for example, 0.5 to 10 parts by mass of water is added to 1 part by mass of the raw material, and extraction is carried out at 40 to 120°C for 5 minutes to 2 hours, preferably 10 to 60 minutes, and more preferably 10 to 20 minutes. The extraction efficiency can be increased by stirring. Extraction can also be carried out by heating under reflux. After extraction, filtration or squeezing is carried out using a filter cloth, filter, or wire mesh. In this case, pressure may be applied to increase the working efficiency. Alternatively, an extract can be obtained by centrifugation (1,000 to 20,000 rpm). To increase the recovery rate, this extraction and filtration process can be repeated 1 to 5 times.

[0023] To perform extraction with an organic solvent, for example, 0.5 to 10 parts by weight of the solvent is added to 1 part by weight of the raw material, and an extract can be obtained in the same manner as with extraction with water. The solvent used can be the hydrophobic or hydrophilic solvents described above, either alone or in combination. Water-containing solvents can also be used. In particular, when washing the raw material with a hydrophobic solvent to remove unwanted substances such as pigments before extraction as described above, and when washing the crude extract after extraction with a hydrophobic solvent as described below, water, lower alcohols, and 50 to 80% (v / v) water-containing lower alcohols are preferred as the solvent used for extraction. Examples of these lower alcohols include those described above. Solvent removal can be performed using conventional methods such as filtration, centrifugation, and distillation.

[0024] A particularly preferred method for extracting a plant extract (particularly an agrimony extract) can be, for example, as follows. The whole plant, whether wild or cultivated, is harvested and dried naturally or by heating. The shredded plant is then immersed in approximately 10 times its volume of water or 0 to 99.5% (v / v) ethyl alcohol, preferably 1 to 50% ethyl alcohol, and particularly preferably 5 to 10% ethyl alcohol, for 3 to 5 days at room temperature for extraction, or extracted at 50 to 80°C for 5 to 24 hours using a reflux condenser, followed by filtration to recover the extract. The water and ethyl alcohol are removed from the extract using a reduced-pressure vacuum dryer such as a rotary evaporator or a freeze-drying device to obtain a plant extract (solid).

[0025] Next, the plant extract is concentrated. In this process, the plant extract is concentrated by washing with 0-40% ethyl alcohol to remove 0-40% ethyl alcohol-soluble components. Specifically, the plant extract (solid) is washed with 0-40% ethyl alcohol, particularly preferably 10-30% ethyl alcohol, and the 0-40% ethyl alcohol-soluble components, particularly preferably 10-30% ethyl alcohol, are removed by filtration or other means. The filtration residue is then subjected to a reduced-pressure vacuum drying apparatus such as a rotary evaporator or a freeze-drying apparatus to remove water and ethyl alcohol, thereby obtaining a more concentrated plant extract. The concentrated plant extract is then redissolved in 50-99.5% ethyl alcohol, particularly preferably 70-90% ethyl alcohol, and the excipients used in formulation are added and freeze-dried to obtain a plant extract of the desired concentration. Sieving may also be performed to facilitate mixing with other powders.

[0026] The content of agrimony extract in the composition of the present invention is not particularly limited and can be changed depending on its purity, degree of purification, the subject and purpose of administration, etc., but is, for example, 0.5 to 100% by mass of the total composition. By setting the content of agrimony extract within the above range, the effects of the present invention can be more reliably exhibited.

[0027] (Other Components) The composition of the present invention may contain active ingredients and additives as needed, in addition to the agrimols and the plant extract containing the agrimols. Specific examples of additives include excipients, binders, disintegrants, lubricants, stabilizers, preservatives, colorants, flavorings, sweeteners, etc. In addition, the components contained in the agrimony extract include:

[0028] The active ingredient is not particularly limited as long as it exhibits efficacy and effect and is acceptable for use in pharmaceuticals, foods, veterinary drugs, feed, etc. Examples include medicinal ingredients and functional ingredients used in pharmaceuticals, quasi-drugs, OTC drugs, herbal medicines, natural medicines, cosmetics, beauty products, health foods, supplements, veterinary drugs, feed, etc. Specific examples of medicinal ingredients and functional ingredients include vitamin A, vitamin D, vitamin E, vitamin B1, vitamin B2, vitamin B6, vitamin B12, folic acid, biotin, niacin, niacinamide, pantothenic acid, iron, copper, zinc, manganese, selenium, chromium, molybdenum, polyglutamic acid, wisteria tea polyphenols, lipid regulators, antidiabetic agents, antihypertensive agents, vasodilators, beta-adrenergic receptor blockers, cardiac ion channel agents, antiarrhythmic agents, anticoagulants, central nervous system function improvers, sympathomimetics, parasympathomimetics, antimuscarinic agonists, dopaminergic agents, tranquilizers, antidepressants, and anti-anxiety agents. Examples of the active ingredients include drugs, hypnotics, animal-derived substances, plant-derived substances, lapidin, nobiletin, sulforaphane, ampelopsin, curcumins, resveratrols, geraniol, osajin, isoliquiritigenin, hydroxytyrosol, 25-hydroxycholecalciferol, S-adenosylmethionine, anthocyanins, proteoglycans, N-acetylglucosamine, collagen, bilberry extract, carrot powder, malt extract, lotus germ extract powder, gokahi, licorice, peony, cinnamon bark, fennel, scutellaria, bifidobacteria, lactic acid bacteria, yeast, and dietary fibers such as polydextrose. Among these, it is preferable to use an active ingredient that exhibits a synergistic effect with the effects of improving vitality and energy and improving lethargy and fatigue, which are expected as the effects of the essential ingredients of the present invention. Furthermore, these medicinal ingredients and functional ingredients may be formulated alone or in combination of two or more.

[0029] (Form of Composition) The form of the composition of the present invention is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, veterinary medicines, feeds, etc. For example, in addition to powders or fine granules as powders, solid preparations such as plain tablets, sugar-coated tablets, buccal tablets, coated tablets, chewable tablets, etc., pills, soft capsules, hard capsules, granules, etc., liquid preparations such as suspensions, emulsions, syrups, elixirs, and lozenges can be mentioned. Among these, from the viewpoint of realizing low cost, a powder form is preferred, and a powder mixture in which powders of each component are mixed is more preferred. These formulations can be prepared by known means in formulation. Furthermore, these formulations can be used, depending on the purpose, in processed foods, health foods (nutritional supplements, nutritionally functional foods, foods for patients, foods for specified health uses, functional foods, etc.), supplements, foods for patients (hospital foods, sick foods, nursing care foods, etc.), confectioneries, oils and fats, dairy products, retort foods, microwave foods, frozen foods, seasonings, health supplements, beverages, nutritional drinks, etc.

[0030] [Composition dosage and administration] The daily intake of the composition of the present invention is not particularly limited, but is, for example, 0.01 mg or more in terms of the amount of Agrimoles. Preferably, it is 0.1 mg or more, more preferably 0.15 mg or more, and particularly preferably 0.2 mg or more. On the other hand, the upper limit of the daily intake of the composition of the present invention is not particularly limited, but is, for example, 1000 mg or less in terms of the amount of Agrimoles, preferably 500 mg or less, more preferably 100 mg or less, and even more preferably 10 mg or less. By keeping the intake of the composition of the present invention within the above range, the effects of the present invention can be more reliably achieved.

[0031] The number of times the composition of the present invention is taken per day is not particularly limited, but from the viewpoint of reducing the burden of ingestion, it is preferably taken once a day. Furthermore, the timing of ingestion is not particularly limited, and may be, for example, before or after meals, upon waking up, or before sleeping. From the viewpoint of excellent absorbability, it is preferably taken before or after meals, more preferably after meals.

[0032] The intake period of the composition of the present invention is not particularly limited, but is, for example, 4 weeks or more, preferably 8 weeks or more, and more preferably 12 weeks or more. The longer the intake period, the more the effects of the present invention are exerted.

[0033] The target subjects of the composition of the present invention are not particularly limited, and include, for example, healthy individuals. Preferably, the target subjects are those who feel that their vitality and energy have decreased, or those who feel lethargic and fatigued. A target subject who feels that their vitality and energy have decreased is, for example, a subject with a T-score of 50 or less for VA (vitality-energy) on the POMS-2 short form for adults. Furthermore, a target subject who feels lethargic and fatigued is, for example, a subject with a T-score of 50 or more for FI (fatigue-lethargy) on the POMS-2 short form for adults. Particularly preferred target subjects are those with a T-score of 50 or less for VA (vitality-energy) and a T-score of 50 or more for FI (fatigue-lethargy) on the POMS-2 short form for adults. Furthermore, the target subjects may be of any age or gender, and may be, for example, men or women aged 40 to 60 years.

[0034] Hereinafter, examples of the present invention will be described, but the present invention is not limited to these examples, and various modifications are possible within the technical concept of the present invention.

[0035] The effects of a composition containing Agrimols on improving vitality and energy, and on improving lethargy and fatigue were confirmed by the following procedure.

[0036] <Test Method> The subjects were divided into a test food group and a control food group, and the effects of agrimols derived from agrimony were evaluated in a randomized, double-blind, placebo-controlled, parallel-group comparative study. (Subjects) The subjects were Japanese men and women aged 40 to 60 years, with a T-score of 50 or less for VA (vigor-vitality) and 50 or more for FI (fatigue-lethargy) on the POMS-2 short adult version. These subjects were divided into a test food group (41 subjects) and a control food group (41 subjects). (Test Food and Control Food) Test Food: Hard capsules containing 0.2 mg of agrimony-derived agrimols (a mixture of agrimol B, compound 3, and compound 4) per capsule. Control Food (Placebo): Hard capsules containing no agrimony-derived agrimols, and matched in weight and color to be indistinguishable from the test food as a placebo. (Intake of Test Food) During the intake period, one tablet of the test food was taken once daily after a meal with about a glass of water or lukewarm water. The intake period was 12 weeks. (Evaluation Method) Before intake, and at 4, 8, and 12 weeks after the start of intake, the VA (vigor-vitality) T-score and FI (fatigue-lethargy) T-score of the POMS2 short version for adults were evaluated, and the changes in VA and FI before and after intake were calculated. The values ​​of each evaluation item were calculated as mean ± standard error, and compared between the test food intake group and the control food intake group. In addition, a significant difference test was performed using the Student's t-test to compare the test food intake group and the control food intake group.

[0037] Figure 1 shows the VA and FI after 12 weeks of intake and the change from before intake. The change in VA after 12 weeks of intake was 12.2 ± 1.7 points in the test food intake group and 5.6 ± 1.1 points in the control food intake group, which was significantly higher in the test food intake group than in the control food intake group (p = 0.003). Furthermore, the change in FI after 12 weeks of intake was -12.7 ± 1.6 points in the test food intake group and -5.7 ± 1.6 points in the control food intake group, which was significantly lower in the test food intake group than in the control food intake group (p = 0.001).

[0038] In this randomized, double-blind, placebo-controlled, parallel-group comparative study, taking a supplement containing 0.2 mg of agrimols derived from agrimony significantly improved fatigue-lethargy and vitality-vigor compared to the control food intake group. The QOL improvement effect of taking the test food confirmed in this study is thought to be the result of the agrimols derived from agrimony acting directly or indirectly on these fatigue factors, resulting in improvement in fatigue.

[0039] The composition of the present invention has the effect of improving vitality and energy and improving lethargy and fatigue, and therefore can be used as a composition for improving vitality and energy or a composition for improving lethargy and fatigue, in the form of pharmaceuticals, quasi-drugs, drinkable cosmetics, drinkable cosmetics, health foods (nutritional supplements, foods with nutrient functions, foods for the sick, foods for specified health uses, foods with functional claims, etc.), supplements, feeds, etc.

Claims

1. A composition containing agrimols for improving vitality and energy.

2. A composition containing Agrimols for improving lethargy and fatigue.

3. A composition according to claim 1 or 2, characterized in that it contains the agrimols as a plant extract.

4. The composition according to claim 3, characterized in that the plant extract is an agrimony extract.

5. A composition according to claim 1 or 2, characterized in that the daily intake of the Agrimoles is 0.1 mg or more.

6. The composition according to claim 1 or 2, characterized in that the intake period is 12 weeks or more.

7. The composition according to claim 1 or 2, characterized in that the subject to which it is applied is a person who feels a decrease in vitality and energy or a person who has a feeling of lethargy and fatigue.

Images