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

Abstract

An object of the present invention is to provide a composition having excellent muscle-building and anti-obesity effects. [Solution] 1. An oral composition comprising corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is corosolic acid:maslinic acid=3.3:1 to 7:1.

Description

Technical Field

[0001] The present invention relates to an oral composition containing chololic acid and maslinic acid, a composition for muscle enhancement, and an anti-obesity composition.

Background Art

[0002] In recent years, due to the increasing health consciousness, there has been a strong 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-enhancing 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 fully satisfactory in terms of the muscle mass increasing effect.

Prior Art Documents

Non-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-enhancing action and anti-obesity action.

Means for Solving the Problems

[0006] In order to solve the above problems, the applicant of the present application has intensively studied various substances. Surprisingly, it has been found that by containing corosolic acid and maslinic acid in a specific content ratio, an oral composition excellent in muscle strengthening action and anti-obesity action 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 corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is corosolic acid:maslinic acid = 3.3:1 to 7:1 by mass ratio. <2> A composition for enhancing muscle strength characterized by containing corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is corosolic acid:maslinic acid = 3.3:1 to 7:1 by mass ratio. <3> An anti-obesity composition characterized by containing corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is corosolic acid:maslinic acid = 3.3:1 to 7:1 by mass ratio.

Effects of the Invention

[0008] According to the present invention, by containing corosolic acid and maslinic acid in a specific content ratio, an oral composition can be provided that exhibits a synergistically excellent muscle strengthening effect compared to when used alone. Further, according to the present invention, by containing corosolic acid and maslinic acid in a specific content ratio, an oral composition can be provided that exhibits a synergistically excellent anti-obesity effect compared to when used alone.

Brief Description of the Drawings

[0009]

Figure 1

Modes for Carrying Out the Invention

[0010] The present invention will be described in detail below.

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

[0012] [Chemical formula]

[0013] Corosolic acid is known to be contained in plants such as kali, almond, banaba leaf, cranberry, loquat leaf, perilla leaf, etc. 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 plants, the extraction solvent is not particularly limited. For example, solvents such as water, alcohol (for example, methanol, ethanol, n-propanol, n-butanol, etc.), acetone, etc. 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, 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 methods commonly used by those skilled in the art, such as vacuum drying or spray drying.

[0015] [2. Maslinic acid] Maslinic acid is a kind of triterpene and is represented by the following structural formula (2).

[0016] [Chemical formula]

[0017] Maslinic acid is known to be contained in plants such as olives, jujubes, almonds, banaba leaves, sage, almonds, apples, cranberries, and Chinese quince. 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 maslinic acid by extraction from a plant, 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 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 methods commonly used by those skilled in the art, such as vacuum drying or spray drying.

[0019] [3. Oral Composition] The oral composition of the present invention contains corosolic acid and maslinic acid in a specific content ratio. By setting the content ratio of the present invention, excellent muscle strengthening effects and anti-obesity effects are exhibited as compared with the case where each is used alone or when the content ratio is different. The content ratio of corosolic acid and maslinic acid in the present invention is preferably corosolic acid:maslinic acid = 3.3:1 to 7:1, more preferably 3.3:1 to 6:1, and particularly preferably 3.3:1 to 5:1 by mass ratio.

[0020] The form of the oral composition of the present invention is not particularly limited and can be in any form. For example, forms suitable for oral use, specifically, powder form, granular form, granule form, tablet form, liquid form, beverage, gel form, paste form, capsule form such as hard capsules and soft capsules, caplet form, chewable form, etc. can be mentioned. Depending on the form to be used, various excipients, binders, lubricants, stabilizers, diluents, extenders, 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 powder form, granular form, granule form, tablet form, chewable form, or capsule form, and more preferably in tablet form or powder form.

[0021] 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, etc. 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. can be mentioned.

[0022] 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 as 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.

[0023] The content of malic acid is not particularly limited as long as it exhibits muscle-strengthening effects and / or anti-obesity effects. For example, when the above oral composition is a beverage, it is 0.000006 to 0.02% by mass, preferably 0.000013 to 0.01% by mass, more preferably 0.000025 to 0.005% 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 0.00013 to 4% by mass, preferably 0.00025 to 2% by mass, more preferably 0.0005 to 1% by mass, based on the total amount of the composition.

[0024] 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 and the usage content of the user. For example, when the above oral composition is a beverage, it is 6.25 to 4000 ml / 60 kg, preferably 12.5 to 2000 ml / 60 kg, more preferably 25 to 1000 ml / 60 kg, based on the weight of the user. In the case of food forms other than beverages, and when the solid content of the beverage is converted as the composition, it is 0.025 to 160 g / 60 kg, preferably 0.05 to 80 g / 60 kg, more preferably 0.1 to 40 g / 60 kg, based on the weight of the user. The single usage amount of the oral composition of the present invention is also not particularly limited. For example, when the above oral composition is a beverage, it is 2 to 4000 ml / 60 kg, preferably 4 to 2000 ml, more preferably 8 to 1000 ml / 60 kg, based on the weight of the user. In the case of food forms other than beverages, and when the solid content of the beverage is converted as the composition, it is 0.005 to 160 g / 60 kg, preferably 0.01 to 80 g / 60 kg, more preferably 0.02 to 40 g / 60 kg, based on the weight of the user.

[0025] The oral composition of the present invention may contain only choline phosphate and maslinic acid, or may contain other components in addition to these two components. The other components are not limited as long as they are those commonly 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 (vitamin 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.

[0026] 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 approved by a predetermined agency such as foods for specified health use, nutritional functional foods, and foods with functional claims, general foods, food additives, feeds, etc.

[0027] The oral composition of the present invention can be used as a muscle strengthening composition for muscle strengthening. Such muscle strengthening compositions are not particularly limited as long as they contain cholosine phosphate and maslinic acid in a specific content ratio and can be distinguished from other products as a product 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 indicates muscle strengthening, enhanced muscle synthesis, suppressed muscle breakdown, suppression / maintenance / increase of muscle mass (muscle weight, muscle cross-sectional area, muscle density), suppression / maintenance / improvement of the decline in muscle quality, suppression / maintenance / increase of muscle strength (power, endurance), suppression / maintenance / improvement of the decline in motor ability, suppression / maintenance / improvement of metabolism (basal metabolism, metabolism at rest and during exercise), suppression / maintenance / increase of fat-free body weight, prevention / improvement of muscle fatigue, metabolic improvement effect by muscle strengthening, prevention / improvement effect of locomotive syndrome, and prevention / 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 (choline phosphate and maslinic acid) are indicated 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 indicate only cholosine phosphate as the active ingredient, or it may indicate only maslinic acid as the active ingredient.

[0028] Specifically, examples of the muscle-strengthening composition of the present invention include pharmaceuticals (including quasi-drugs) and so-called health foods. Among so-called health foods, those labeled with statements such as "supporting the power to build muscles", "suppressing muscle breakdown", "enhancing muscle strength", "suppressing, maintaining, improving, and enhancing the decline of walking ability", "aiming to improve metabolism through muscle strengthening", "suppressing the decline of metabolism", "preventing and recovering from muscle fatigue", "suppressing and maintaining the decline of balance ability", "shaping up", "masculine", "slim and masculine", "beautiful body", "preventing bedridden state", "preventing falls", "aiming to improve metabolism through muscle strengthening", "maintaining muscle mass and muscle strength", etc. can be exemplified. The subjects for ingesting the oral composition of the present invention are not particularly limited as long as they are people who need muscle strengthening, but people aiming for shaping up, sports players, elderly people with weak legs and waists, etc. can be preferably exemplified.

[0029] 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 corosolic acid and maslinic acid in a specific content ratio and can be distinguished from other products as a product in terms of being used for anti-obesity (obesity suppression). For example, any of the main body, packaging, instruction manual, and promotional materials of the product according to the present invention that display the function of anti-obesity (including diet, body fat reduction, suppression of body fat accumulation, improvement of metabolic syndrome, weight loss, etc.) is 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 (corosolic acid and maslinic acid) are displayed as active ingredients for anti-obesity on the packaging of the product, etc. For example, it may not specify the active ingredient, or it may display only corosolic acid as the active ingredient, or it may display only maslinic acid as the active ingredient.

[0030] Specifically, examples of the anti-obesity composition of the present invention include pharmaceuticals (including quasi-drugs) and so-called health foods. Among so-called health foods, those labeled with "For those concerned about body fat", "For those who seem overweight", "For those concerned about weight (BMI)", "Reduce weight and abdominal fat (visceral fat and subcutaneous fat)", "Reduce waist circumference", etc. can be exemplified.

[0031] 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 it 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, the amount of exercise when performing exercise is 10 minutes or more per day, preferably 20 minutes or more, more preferably 30 minutes or more.

Examples

[0032] 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.

[0033] 1. Evaluation of muscle strengthening effect by measuring IGF-1 / Gapdh gene expression level [Test substance] The following substances were used as test substances. · Colosolic acid: A reagent manufactured by Nagara Science Co., Ltd. was used. · Maslinic acid: A reagent manufactured by Nagara Science Co., Ltd. was used.

[0034] [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 3 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 content of the test substances used in the following tests is as shown in Table 1.

[0035]

Table 1

[0036] [Measurement of IGF-1 / Gapdh gene expression levels] (1) Mouse myoblast C2C12 cells were seeded at 5.0×10 4 cells / well in a collagen-coated 24-well plate and cultured in a 37°C, 5% CO2 incubator for 24 hours. (2) After removing the medium, the cells were washed twice with DMEM and then 1 mL / well of differentiation induction medium (2% HS-DMEM) was added, and the cells were cultured in a 37°C, 5% CO2 incubator 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 the cells were cultured in a 37°C, 5% CO2 incubator for 24 hours. (4) After removing the medium, the cells were washed twice with PBS, and RNA was recovered using the RNeasy Mini Kit (QIAGEN). (5) Using the obtained RNA and primers for IGF-1 (QIAGEN), one-step real-time PCR was performed using the One Step TB Green (registered trademark) PrimeScript RT-PCR Kit II (Perfect Real Time) (Takara Bio) to measure the gene expression level of IGF-1. Using primers for Gapdh (QIAGEN) as an endogenous control, the gene expression level of Gapdh was measured, and the relative value to the control was calculated. The results are shown in Figure 1.

[0037] Since IGF-1 has the effect of promoting protein synthesis in skeletal muscle, it is known to be involved in muscle strengthening. As shown in Figure 1, the gene expression levels of IGF-1 in Comparative Examples 1 to 5 were 1.06 to 1.23, respectively. On the other hand, the gene expression levels of IGF-1 in Examples 1 to 4 containing specific amounts of cholosolic acid and maslinic acid were 1.50 or more, showing an excellent gene expression promoting effect compared to Comparative Examples 1 to 3. In particular, when the content ratio of cholosolic acid:maslinic acid was 3.3:1 to 6:1 by mass, the gene expression level of IGF-1 was 1.58 or more, showing a particularly excellent gene expression promoting effect. From the above, it can be seen that the oral composition of the present invention contains cholosolic acid and maslinic acid at a specific content ratio, and the gene expression level of IGF-1 increases, so it exhibits an excellent muscle strengthening effect.

[0038] 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 2 below for 56 days. The feed was based on AIN-76, and a mixture containing cholosolic acid and maslinic acid at a cholosolic acid:maslinic acid = 4:1 ratio was used. After measuring the body weight on the 56th day of the test, dissection was performed under 1 hour of fasting. The dissection was performed by laparotomy under isoflurane anesthesia, and visceral fat, subcutaneous fat, and skeletal muscle (gastrocnemius muscle, quadriceps femoris muscle) were excised and weighed. 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 3.

[0039]

Table 2

[0040]

Table 3

[0041] From Table 3, it can be seen that Example 5 containing colosolic acid: maslinic acid at a ratio of 4:1 has less weight gain compared to Comparative Example 6. 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 capable of enhancing muscles and reducing body fat.

[0042] From the above, the oral composition of the present invention contains colosolic acid and maslinic acid at a specific content ratio, thereby suppressing weight gain and fat increase, increasing muscle, and enhancing the gene expression of IGF-1. Thus, it can be seen that it exhibits excellent anti-obesity and muscle-enhancing effects.

[0043] Example 6 Tablets (250 mg per tablet) consisting of the following components were produced. By ingesting 2 tablets twice a day, excellent muscle-enhancing and anti-obesity effects can be obtained.

[0044]

Table 4

[0045] Example 7 A drink (200 mL) consisting of the following components was produced. By ingesting the obtained drink twice a day, excellent muscle-enhancing and anti-obesity effects can be obtained.

[0046]

Table 5

[0047] Example 8 Granules consisting of the following components were produced. By dissolving 3 g of the obtained granules in 100 mL of water and ingesting it three times a day, excellent muscle-enhancing and anti-obesity effects can be obtained.

[0048]

Table 6

[0049] Example 9 A granule comprising 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.

[0050] [Table 7]

[0051] Example 10 Granules comprising the following components were produced, and 300 mg thereof was encapsulated in a capsule shell. By ingesting the obtained capsule twice a day, two capsules each time, excellent muscle strengthening and anti-obesity effects can be obtained.

[0052] [Table 8] [Industrial Applicability]

[0053] Since the oral composition of the present invention has excellent muscle strengthening and anti-obesity effects, its industrial utility is high.

Claims

**Claim 1** An oral composition for anti-obesity, characterized by containing cholosolinic acid and maslinic acid, wherein the content ratio of cholosolinic acid to maslinic acid is cholosolinic acid:maslinic acid = 3.3:1 to 7:1 by mass ratio.

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