Oral composition, muscle-strengthening composition, and anti-obesity composition

Abstract

To provide compositions excellent in muscle-enhancing and antiobestic effects.SOLUTION: An oral composition contains corosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an oral composition, a muscle-strengthening composition, and an anti-obesity composition containing colchicinic acid and at least one selected from myricetin and 5-hydroxymethylfurfural.

Background Art

[0002] In recent years, due to the increasing interest in health, there has been a growing demand for further improvement in effects from the viewpoints of health and beauty. For example, regarding the anti-obesity effect, there is an increasing need not only to reduce body fat but also to enhance muscle mass and muscle strength while reducing body fat.

[0003] As components having a muscle-strengthening effect, for example, a muscle mass-increasing agent containing a hydrophobic extract of licorice as an active ingredient (Patent Document 1), panaxatriol, and panaxadiol are known (Patent Document 2). However, none of these muscle mass-increasing agents were sufficiently satisfactory in terms of the muscle mass-increasing effect.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide an oral composition having an excellent muscle-strengthening action and anti-obesity action.

Means for Solving the Problems

[0006] In order to solve the above problems, the present applicant has intensively studied various substances. Surprisingly, by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural, an oral composition excellent in muscle strengthening effect and anti-obesity effect can be obtained. The present invention has been completed based on such findings.

[0007] The outline of the present invention is as follows. <1> An oral composition characterized by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural. <2> A composition for enhancing muscle strength characterized by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural. <3> An anti-obesity composition characterized by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural. <4> An oral composition characterized by containing colosolic acid, myricetin and 5-hydroxymethylfurfural. <5> A composition for enhancing muscle strength characterized by containing colosolic acid, myricetin and 5-hydroxymethylfurfural. <6> An anti-obesity composition characterized by containing colosolic acid, myricetin and 5-hydroxymethylfurfural.

Effects of the Invention

[0008] According to the present invention, by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural, an oral composition can be provided that exhibits a synergistically excellent muscle strengthening effect as compared with the case of using each alone. Further, according to the present invention, by containing colosolic acid and at least one selected from myricetin and 5-hydroxymethylfurfural, an oral composition can be provided that exhibits a synergistically excellent anti-obesity effect as compared with the case of using each alone.

Brief Description of the Drawings

[0009]

Figure 1

Figure 2

Modes for Carrying Out the Invention

[0010] Hereinafter, the present invention will be described in detail.

[0011] [1. Corosolic acid] Corosolic acid is a kind of triterpene and is represented by the following structural formula (1).

[0012]

Chemical

[0013] Corosolic acid is known to be contained in plants such as kalin, almond, banaba leaf, cranberry, loquat leaf, and perilla leaf. In the present invention, those extracted from these plants or those obtained by chemical synthesis can be used, but from the viewpoints of muscle strengthening effect, anti-obesity effect, and safety, those extracted from plants are preferred.

[0014] When obtaining corosolic acid by extracting from a plant, the extraction solvent is not particularly limited, and examples thereof include solvents such as water, alcohol (for example, methanol, ethanol, n-propanol, n-butanol, etc.), and acetone. Preferably, water and / or ethanol can be used. The temperature of the solvent when obtaining the extract is not particularly limited, and it can be appropriately selected, for example, from room temperature to below the boiling point of the solvent. Also, when obtaining the extract powder, it can be obtained by removing the solvent of the extract by a method commonly used by those skilled in the art, such as drying under reduced pressure or spray drying.

[0015] [2. Millicetin] The oral composition of the present invention contains millicetin in addition to colosolic acid. Millicetin is a kind of flavonol and is represented by the following structural formula (2).

[0016] [Chemical formula]

[0017] Millicetin is known to be contained in fruits such as grapes and berries, vegetables such as onions, and plants such as herbs. In the present invention, those extracted from these plants or those obtained by chemical synthesis can be used, but from the viewpoints of muscle strengthening effect, anti-obesity effect, and safety, those extracted from plants are preferred.

[0018] When obtaining millicetin by extracting from plants, the extraction solvent is not particularly limited. For example, solvents such as water, alcohol (e.g., methanol, ethanol, n-propanol, n-butanol, etc.), and acetone can be mentioned. Preferably, water and / or ethanol, etc. can be used. The temperature of the solvent when obtaining the extract is not particularly limited, and can be appropriately selected from room temperature (about normal temperature) to below the boiling point of the solvent. Also, when obtaining the extract powder, it can be obtained by removing the solvent of the extract by methods commonly used by those skilled in the art, such as drying under reduced pressure or spray drying.

[0019] [3. 5-Hydroxymethylfurfural] The oral composition of the present invention contains 5-hydroxymethylfurfural (hereinafter, also referred to as "HMF") in addition to colosolic acid. HMF is a kind of organic compound having a furan skeleton and is represented by the following structural formula (3).

[0020] [Chemical formula]

[0021] HMF is known to be contained in foods such as milk, fruit juice, distilled liquor, and honey, fruits including citrus fruits, and various plants such as rose hips. In the present invention, those obtained by heating these foods, those extracted from plants, or those obtained by chemical synthesis can be used, but from the viewpoints of muscle strengthening effect, anti-obesity effect, and safety, those extracted from plants are preferred.

[0022] When obtaining HMF by extraction from plants, the extraction solvent is not particularly limited, and examples thereof include solvents such as water, alcohol (e.g., methanol, ethanol, n-propanol, n-butanol, etc.), and acetone. Preferably, water and / or ethanol can be used. The temperature of the solvent when obtaining the extract is not particularly limited, and it can be appropriately selected, for example, from room temperature to below the boiling point of the solvent. Also, when obtaining an extract powder, it can be obtained by removing the solvent of the extract by a method commonly used by those skilled in the art, such as drying under reduced pressure or spray drying.

[0023] [4. Oral composition] The oral composition of the present invention contains colosolic acid and at least one selected from millesetin and HMF. By configuring the present invention, excellent muscle strengthening effects and anti-obesity effects are exhibited as compared with the case of using each alone.

[0024] The form of the oral composition of the present invention is not particularly limited and can be any form. For example, forms suitable for oral use, specifically, powder, granule, granule, tablet, liquid, beverage, gel, paste, capsule-like such as hard capsule and soft capsule, caplet-like, chewable-like, etc. can be mentioned. Depending on the form to be used, various excipients, binders, lubricants, stabilizers, diluents, bulking agents, thickeners, gelling agents, emulsifiers, colorants, flavors, sweeteners, additives, etc. can be blended. From the viewpoints of stability and ease of ingestion, the oral composition of the present invention is preferably in the form of powder, granule, granule, tablet, chewable, or capsule, and more preferably in the form of tablet or powder.

[0025] The packaging form of the oral composition of the present invention is not particularly limited and can be appropriately selected according to the dosage form and the like. For example, blister packs such as PTP; strip packaging; heat sealing; aluminum pouches; film packaging using plastics, synthetic resins, etc.; glass containers such as vials; plastic containers such as ampoules, etc.

[0026] The content of choline phosphate is not particularly limited as long as the muscle strengthening effect and / or anti-obesity effect can be recognized. For example, when the above oral composition is a beverage, it is 0.000025 to 0.08% by mass, preferably 0.00005 to 0.04% by mass, more preferably 0.0001 to 0.02% by mass, based on the total amount of the composition. In the case of food forms other than beverages, and when the solid content of the beverage is converted into the composition, it is 0.00063 to 20% by mass, preferably 0.00125 to 10% by mass, more preferably 0.0025 to 5% by mass, based on the total amount of the composition.

[0027] The content of myricetin is not particularly limited as long as the muscle strengthening effect and / or anti-obesity effect can be recognized. For example, when the above oral composition is a beverage, it is 0.00000025 to 0.0016% by mass, preferably 0.0000005 to 0.0008% by mass, more preferably 0.000001 to 0.0004% by mass, based on the total amount of the composition. In the case of food forms other than beverages, and when the solid content of the beverage is converted into the composition, it is 0.00001 to 0.4% by mass, preferably 0.00002 to 0.2% by mass, more preferably 0.00004 to 0.1% by mass, based on the total amount of the composition.

[0028] The content of HMF is not particularly limited as long as it is an amount that exhibits a muscle-strengthening effect and / or an anti-obesity effect. For example, when the oral composition is a beverage, it is 0.00000025 to 0.0016% by mass, preferably 0.0000005 to 0.0008% by mass, more preferably 0.000001 to 0.0004% by mass, based on the total amount of the composition. In the case of food forms other than beverages, and when the solid content of the beverage is converted as the composition, it is 0.00001 to 0.4% by mass, preferably 0.00002 to 0.2% by mass, more preferably 0.00004 to 0.1% by mass, based on the total amount of the composition.

[0029] When the oral composition of the present invention contains chololic acid and myricetin, the blending ratio of chololic acid and myricetin is not particularly limited, but chololic acid:myricetin = 0.1:1 to 9500:1 is preferable, 0.5:1 to 5000:1 is more preferable, and 1:1 to 1000:1 is particularly preferable from the viewpoints of excellent muscle-strengthening action and anti-obesity action.

[0030] Also, when the oral composition of the present invention contains chololic acid and HMF, the blending ratio of chololic acid and HMF is not particularly limited, but chololic acid:HMF = 0.1:1 to 9500:1 is preferable, 0.5:1 to 5000:1 is more preferable, and 1:1 to 1000:1 is particularly preferable from the viewpoints of excellent muscle-strengthening action and anti-obesity action.

[0031] In addition, when the oral composition of the present invention contains both myricetin and HMF in addition to chololic acid, the blending ratio of myricetin and HMF is not particularly limited, but myricetin:HMF = 50:1 to 1:50 is preferable, 25:1 to 1:25 is more preferable, and 10:1 to 1:10 is particularly preferable from the viewpoints of excellent muscle-strengthening action and anti-obesity action.

[0032] The daily usage amount of the oral composition of the present invention is not particularly limited and can be appropriately set according to the usage mode, the content of use by the user, etc. For example, when the above oral composition is a beverage, based on the weight of the user, it is 6.25 to 4000 ml / 60 kg, preferably 12.5 to 2000 ml / 60 kg, and from the viewpoints of muscle strengthening effect and anti-obesity effect, more preferably 25 to 1000 ml / 60 kg. In the case of food forms other than beverages, and when the solid content of the beverage is converted as a composition, based on the weight of the user, it is 0.025 to 160 g / 60 kg, preferably 0.05 to 80 g / 60 kg, and from the viewpoints of muscle strengthening effect and anti-obesity effect, more preferably 0.1 to 40 g / 60 kg. Similarly, the single usage amount of the oral composition of the present invention is not particularly limited. For example, when the above oral composition is a beverage, and when the solid content of the beverage is converted as a composition, based on the weight of the user, it is 2 to 4000 ml / 60 kg, preferably 4 to 2000 ml, and from the viewpoints of muscle strengthening effect and anti-obesity effect, more preferably 8 to 1000 ml / 60 kg. In the case of food forms other than beverages, based on the weight of the user, it is 0.005 to 160 g / 60 kg, preferably 0.01 to 80 g / 60 kg, and from the viewpoints of muscle strengthening effect and anti-obesity effect, more preferably 0.02 to 40 g / 60 kg.

[0033] The oral composition of the present invention may contain only choline phosphate and at least one selected from myricetin and HMF, or may contain other components in addition to these two components. The other components are not limited as long as they are those usually used as foods. For example, nutritional components such as vitamins and minerals, plant-derived components, animal-derived components, functional saccharides, polypeptides, vitamins, lactic acid bacteria, bifidobacteria, and fungi such as butyric acid bacteria can be mentioned. From the viewpoints of muscle strengthening and anti-obesity effects, water-soluble vitamins (vitamin B1, B2, B3, B5, B6, B12, B13, B15, B17, biotin, choline, folic acid, inositol, PABA, vitamin C, vitamin P), fat-soluble vitamins (vitamins A, D, E, K), etc.; minerals such as magnesium, phosphorus, zinc, and iron; sulfur-containing compounds contained in taurine, garlic, etc.; flavonoids or flavonoid-like substances such as hesperidin and quercetin; proteins such as collagen; peptides; amino acids; animal fats and oils; vegetable fats and oils; pulverized products or extracts of animals and plants, etc. can be mentioned. Components necessary for muscle synthesis are particularly preferred, and examples include amino acids containing branched-chain amino acids and high-protein raw materials such as whey protein. The content of the other components can be appropriately selected according to the usage form of the oral composition of the present invention, etc.

[0034] The oral composition of the present invention can be used, for example, as so-called health foods such as pharmaceuticals (including quasi-drugs), functional foods whose efficacy display is recognized by a predetermined agency such as foods for specified health use, foods with nutritional functions, and foods with functional claims, general foods, food additives, feeds, etc.

[0035] The oral composition of the present invention can be used as a muscle-strengthening composition used for muscle strengthening. Such muscle-strengthening compositions include colosolic acid and at least one selected from millesetin and HMF, and are not particularly limited as long as they can be distinguished from other products as products in terms of being used for muscle strengthening and muscle fatigue recovery. For example, any of the main body, packaging, instruction manual, and promotional materials of the product according to the present invention can display muscle strengthening, enhancement of muscle synthesis, suppression of muscle breakdown, suppression, maintenance, or increase of muscle mass (muscle weight, muscle cross-sectional area, muscle density), suppression, maintenance, or improvement of the deterioration of muscle quality, suppression, maintenance, or increase of muscle strength (power, endurance), suppression, maintenance, or improvement of the decline in motor ability, suppression, maintenance, or improvement of metabolism (basal metabolism, metabolism at rest and during exercise), suppression, maintenance, or increase of fat-free body weight, prevention or improvement of muscle fatigue, metabolic improvement effect due to muscle strengthening, prevention or improvement effect of locomotive syndrome, and prevention or improvement effect of sarcopenia. In addition, the muscle-strengthening composition of the present invention is not limited to those in which the components of the combination in the present invention (colosolic acid and at least one selected from millesetin and HMF) are displayed as active ingredients for muscle strengthening on the packaging of the product or the like. For example, it may not specify the active ingredient, or it may display only colosolic acid as the active ingredient, or it may display only millesetin or HMF as the active ingredient.

[0036] Specifically, the muscle-strengthening composition of the present invention includes pharmaceuticals (including quasi-drugs) and so-called health foods. Among so-called health foods, those that display "support the power to build muscles", "suppress muscle breakdown", "enhance muscle strength", "suppress, maintain, improve, and enhance the decline of walking ability", "improve metabolism by enhancing muscles", "suppress the decline of metabolism", "prevent and recover from muscle fatigue", "suppress and maintain the decline of balance ability", "shape up", "macho", "slim macho", "beautiful body", "prevent bedridden state", "prevent falls", "improve metabolism by enhancing muscles", "maintain muscle mass and muscle strength", etc. can be exemplified. The subject for ingesting the oral composition of the present invention is not particularly limited as long as it is a person who needs muscle enhancement, but those aiming for shaping up, athletes, elderly people with weak lower limbs and waists, etc. can be preferably exemplified.

[0037] In addition, the oral composition of the present invention can be used as an anti-obesity composition used for anti-obesity. Such anti-obesity compositions are not particularly limited as long as they contain cholosolic acid and at least one selected from myricetin and HMF and can be distinguished from other products as a product in terms of being used for anti-obesity (obesity suppression). For example, those that display the function of anti-obesity (including diet, body fat reduction, suppression of body fat accumulation, improvement of metabolic syndrome, weight loss, etc.) in any of the main body, packaging, instruction manual, and promotional materials of the product according to the present invention are included in the scope of the present invention. Note that the anti-obesity composition of the present invention is not limited to those in which the components of the combination in the present invention (cholosolic acid and at least one selected from myricetin and HMF) are displayed as active ingredients for anti-obesity on the packaging of the product, etc. For example, it may not specify the active ingredient, may display only cholosolic acid as the active ingredient, or may display only myricetin or HMF as the active ingredient.

[0038] Specifically, the anti-obesity composition of the present invention includes pharmaceuticals (including quasi-drugs) and so-called health foods. Among the so-called health foods, those labeled with "For those concerned about body fat", "For those who are overweight", "For those concerned about weight (BMI)", "Reduce weight and abdominal fat (visceral fat and subcutaneous fat)", "Reduce waist circumference", etc. can be exemplified.

[0039] The muscle strengthening effect and anti-obesity effect of the oral composition of the present invention can be obtained by ingesting the composition of the present invention in daily life. However, by combining with exercise, more excellent effects can be obtained. The exercise mentioned here is any one or more of aerobic exercise or resistance exercise (muscle strength training, weight training). In particular, when obtaining the muscle strengthening effect by the oral composition of the present invention, the type of exercise combined with the oral composition of the present invention is not particularly limited, but it is preferable to perform any one or more of aerobic exercise and resistance exercise, and it is particularly preferable to perform resistance exercise. Also, as the amount of exercise when performing exercise, it is 10 minutes or more per day, preferably 20 minutes or more, more preferably 30 minutes or more.

Examples

[0040] Hereinafter, the present invention will be described in more detail with reference to examples. However, the present invention is not limited to these examples, and the present invention can take various forms as long as the problems of the present invention can be solved.

[0041] 1. Evaluation of muscle strengthening effect by measuring the expression level of IGF-1 / Rps28 gene [Test substance] The following substances were used as test substances. · Colosolic acid: A reagent manufactured by Nagara Science Co., Ltd. was used. · Millicetin: A reagent manufactured by Fujifilm Wako Pure Chemical Corporation was used. · HMF: A reagent manufactured by Fujifilm Wako Pure Chemical Corporation was used.

[0042] [Preparation of test substance] Each test substance was prepared as follows. Each test substance was dissolved in DMSO and diluted to a test substance concentration of 2000 μg / mL using a differentiation induction medium prepared by adding 1% penicillin / streptomycin to DMEM and adjusting to 2% HS (horse serum). It was prepared so that the final concentration of DMSO was 0.5%, and each test substance was mixed at the following ratios. The contents of the test substances used in the following tests are as shown in Tables 1 and 2.

[0043]

Table 1

[0044]

Table 2

[0045] [Measurement of IGF-1 / Rps28 gene expression level] (1) Mouse myoblast C2C12 cells were seeded at 3.0×10 4 cells / well in a collagen-coated 24-well plate and cultured in an incubator at 37°C and 5% CO 2 for 24 hours. (2) After removing the medium, 1 mL / well of differentiation induction medium (2% HS-DMEM) was added and cultured in an incubator at 37°C and 5% CO 2 for 6 days (to induce differentiation into myotubes). (3) After removing the medium, 500 μL / well of differentiation induction medium containing the test substance was added and cultured in an incubator at 37°C and 5% CO 2 for 24 hours. (4) After removing the medium, the cells were washed twice with PBS, RNA was recovered using the RNeasy Mini Kit (QIAGEN), and cDNA was synthesized using ReverTra Ace(R) qPCR RT Master Mix (TOYOBO). (5) Using the obtained cDNA as a template, quantitative real-time PCR was performed with the Rotor-Gene SYBR Green PCR Kit (manufactured by QIAGEN) using primers for IGF1 (manufactured by QIAGEN) to measure the gene expression level of IGF-1. As an endogenous control, primers for Rps28 (manufactured by QIAGEN) were used to measure the gene expression level of Rps28. Relative values were calculated based on Comparative Examples 1 and 3 (colophonic acid). The results are shown in FIGS. 1 and 2.

[0046] Since IGF-1 has an action of promoting protein synthesis in skeletal muscle, it is known to be involved in muscle strengthening. From FIG. 1, the relative values of the mRNA expression levels of Rps28 in Comparative Examples 1 and 2 were 1.00 and 0.52, respectively. On the other hand, the mRNA expression levels of Rps28 in Examples 1 and 2 containing colophonic acid and myricetin were 1.5 times or more compared to Comparative Example 1 and 2.9 times or more compared to Comparative Example 2. Also, the mRNA expression levels of Rps28 in Comparative Examples 3 and 4 were 1.00 and 0.68, respectively. On the other hand, the mRNA expression levels of Rps28 in Examples 3 and 4 containing colophonic acid and HMF were 1.25 times or more compared to Comparative Example 1 and 2.4 times or more compared to Comparative Example 2. From the above, it can be seen that the oral composition of the present invention contains colophonic acid and at least one selected from myricetin and HMF, and thus shows an excellent muscle strengthening effect because the mRNA expression level of Rps28 increases.

[0047] 2. Evaluation of muscle strengthening effect and anti-obesity effect Male C57BL / 6J mice were acclimated for 9 days and grouped based on body weight values. From the start of the test, the mice were allowed to freely consume the feed described in Table 3 below for 56 days. The feed was based on AIN-76, and for choline phosphate, myricetin, and HMF, a mixture containing choline phosphate:myricetin:HMF = 253:1:1.5 was used. On the 56th day of the test, after measuring the body weight, dissection was performed under 1 hour of fasting. The dissection was carried out by laparotomy under isoflurane anesthesia, and visceral fat, subcutaneous fat, and skeletal muscles (gastrocnemius muscle, quadriceps femoris muscle) were excised and weighed. Note that the visceral fat was the total amount of fat excised from the mesentery, around the testis, around the kidney, and retroperitoneum. The results are shown in Table 4.

[0048]

Table 3

[0049]

Table 4

[0050] From Table 4, it can be seen that Example 5 containing choline phosphate, myricetin, and HMF has less weight gain compared to Comparative Example 5. Also, since the fat weight per body weight is less and the muscle weight per body weight is more, it can be understood that it is possible to enhance muscle and reduce body fat.

[0051] From the above, the oral composition of the present invention contains choline phosphate, myricetin, and HMF, thereby suppressing weight gain and fat increase, increasing muscle, and enhancing the expression of the IGF-1 gene, so it can be seen that it exhibits excellent anti-obesity and muscle-enhancing effects.

[0052] Example 6 Tablets (250 mg per tablet) composed of the following components were manufactured. By ingesting the obtained tablets twice a day, two tablets each time, excellent muscle-enhancing and anti-obesity effects can be obtained.

[0053]

Table 5

[0054] Example 7 A drink agent (200 mL) consisting of the following components was produced. By ingesting the obtained drink agent twice a day, excellent muscle strengthening and anti-obesity effects can be obtained.

[0055] [Table 6]

[0056] Example 8 A granule consisting of the following components was produced. By dissolving 3 g of the obtained granule in 100 mL of water and ingesting it three times a day, excellent muscle strengthening and anti-obesity effects can be obtained.

[0057] [Table 7]

[0058] Example 9 A granule consisting of the following components was produced. By dissolving 15 g of the obtained granule in 150 mL of water and ingesting it twice a day, excellent muscle strengthening and anti-obesity effects can be obtained.

[0059] [Table 8]

[0060] Example 10 Granules consisting of the following components were produced, and 300 mg was encapsulated in a capsule shell. By ingesting the obtained capsule agent twice a day, two capsules each time, excellent muscle strengthening and anti-obesity effects can be obtained.

[0061] [Table 9] [Industrial Applicability]

[0062] Since the oral composition of the present invention has excellent muscle strengthening and anti-obesity effects, its industrial utility is high.

Claims

1. An anti-obesity composition characterized by containing corosolic acid, 5-hydroxymethylfurfural, and myricetin.

2. The anti-obesity composition according to Claim 1, wherein the mass ratio of corosolic acid to myricetin is 0.1:1 to 9500:

1.

3. The anti-obesity composition according to Claim 1 or 2, wherein the mass ratio of myricetin to 5-hydroxymethylfurfural is 50:1 to 1:50.

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