JP6906830B1 - Oral compositions, muscle-building compositions and anti-obesity compositions - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition having an excellent muscle-building action and anti-obesity action. 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. An oral composition. [Selection diagram] None

Description

The present invention relates to oral compositions containing corosolic acid and maslinic acid, muscle building compositions and anti-obesity compositions.

In recent years, with increasing health consciousness, there is an increasing demand for further improvement of effects from the viewpoint 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 increase muscle mass and strength while reducing body fat.

As a component having a muscle-building effect, for example, a muscle-building agent containing a licorice hydrophobic extract as an active ingredient (Patent Document 1), panaxatriol, and panaxadiol are known (Patent Document 2). However, none of these muscle-building agents was sufficiently satisfactory in terms of muscle-building effect.

Japanese Unexamined Patent Publication No. 2012-193157 Japanese Unexamined Patent Publication No. 2015-059102

An object of the present invention is to provide an oral composition having an excellent muscle-building effect and an anti-obesity effect.

The applicant has made extensive studies on various substances in order to solve the above-mentioned problems, and surprisingly, by containing corosolic acid and maslinic acid in a specific content ratio, a muscle-building effect and an anti-muscular effect are achieved. It has been found that an oral composition having an excellent obesity effect can be obtained.
The present invention is a completed invention based on such findings.

The outline of the present invention is as follows.
<1> An oral composition comprising corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is a mass ratio of corosolic acid: maslinic acid = 3.3: 1-7. An oral composition of 1: 1.
<2> A composition for strengthening muscle strength characterized by containing corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is a mass ratio of corosolic acid: maslinic acid = 3.3: 1. A composition for strengthening muscle strength of ~ 7: 1.
<3> An anti-obesity composition containing corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is mass ratio of corosolic acid: maslinic acid = 3.3: 1. ~ 7: 1 anti-obesity composition.

According to the present invention, it is possible to provide an oral composition in which corosolic acid and maslinic acid are contained in a specific content ratio, thereby exhibiting a synergistically superior muscle strengthening effect as compared with the case where each is used alone. can. Further, according to the present invention, by containing corosolic acid and maslinic acid in a specific content ratio, an oral composition exhibiting a synergistically superior anti-obesity effect as compared with the case where each is used alone is provided. be able to.

It is a relative value of the gene expression level of IGF-1 in Examples and Comparative Examples.

Hereinafter, the present invention will be described in detail.

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

Corosolic acid is known to be contained in plants such as carin, almond, banaba leaf, cranberry, loquat leaf, and perilla leaf. In the present invention, those extracted from these plants and those obtained by chemical synthesis can be used, but those extracted from plants are preferable from the viewpoints of muscle-building action, anti-obesity action and safety. ..

When corosolic acid is obtained by extracting it 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 and the like can be used. The temperature of the solvent for obtaining the extract is not particularly limited, and can be appropriately selected from, for example, about room temperature to below the boiling point of the solvent. Further, when the extract powder is obtained, it can be obtained by removing the solvent of the extract by a method usually used by those skilled in the art, such as vacuum drying or spray drying.

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

Maslinic acid is known to be contained in plants such as olives, jujubes, almonds, banaba leaves, sage, almonds, apples, cranberries and carins. In the present invention, those extracted from these plants and those obtained by chemical synthesis can be used, but those extracted from plants are preferable from the viewpoints of muscle-building action, anti-obesity action and safety. ..

When masphosphate is obtained by extracting it 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 and the like can be used. The temperature of the solvent for obtaining the extract is not particularly limited, and can be appropriately selected from, for example, about room temperature to below the boiling point of the solvent. Further, when the extract powder is obtained, it can be obtained by removing the solvent of the extract by a method usually used by those skilled in the art, such as vacuum drying or spray drying.

[3. Oral composition]
The oral composition of the present invention contains corosolic acid and maslinic acid in a specific content ratio. By using the content ratio of the present invention, excellent muscle-building action and anti-obesity action are exhibited as compared with the case where each is used alone or 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 in terms of mass ratio. 1 to 5: 1 is particularly preferable.

The form of the oral composition of the present invention is not particularly limited and may be any form. For example, forms suitable for oral use, specifically powder, granules, granules, tablets, liquids, beverages, gels, pastes, capsules such as hard capsules and soft capsules, caplets, chewables. Various forms such as shapes are listed, and various excipients, binders, lubricants, stabilizers, diluents, bulking agents, thickeners, gelling agents, emulsifiers, and colorants are used according to the form to be used. , Fragrances, sweeteners, additives and the like can be blended. From the viewpoint of stability and ease of ingestion, the oral composition of the present invention is preferably in the form of powder, granules, granules, tablets, chewables, or capsules, and more preferably in the form of tablets or powders.

The packaging form of the oral composition of the present invention is not particularly limited and may be appropriately selected depending on the dosage form and the like. For example, a blister pack such as PTP; strip packaging; heat seal; aluminum pouch; plastic or synthetic resin is used. Film packaging; glass containers such as vials; plastic containers such as ampoules.

The content of corosolic acid is not particularly limited as long as it has a muscle-building effect and / or an anti-obesity effect. For example, when the oral composition is a beverage, it is 0.000025 to 0 to the total amount of the composition. It is .08% by mass, preferably 0.00005 to 0.04% by mass, and more preferably 0.0001 to 0.02% by mass. In the case of a food form other than a beverage, and when the solid content of the beverage is converted as a composition, it is 0.00063 to 20% by mass, preferably 0.00125 to 10% by mass, more preferably 0.00125 to 10% by mass, based on the total amount of the composition. Is 0.0025 to 5% by mass.

The content of maslinic acid is not particularly limited as long as it has a muscle-building effect and / or an anti-obesity effect. For example, when the oral composition is a beverage, it is 0.000006 to 0 with respect to the total amount of the composition. It is 0.02% by mass, preferably 0.000013 to 0.01% by mass, and more preferably 0.000025 to 0.005% by mass. In the case of food forms other than beverages, and when the solid content of beverages is converted as a composition, it is 0.00013 to 4% by mass, preferably 0.00025 to 2% by mass, more preferably to the total amount of the composition. Is 0.0005 to 1% by mass.

The daily amount of the oral composition of the present invention to be used is not particularly limited and may be appropriately set according to the mode of use, the content of use by the user, and the like. Based on the body weight, it is 6.25 to 4000 ml / 60 kg, preferably 12.5 to 2000 ml / 60 kg, and more preferably 25 to 1000 ml / 60 kg from the viewpoint of muscle-building action and anti-obesity action. In the case of food forms other than beverages, and when the solid content of beverages is converted as a composition, it is 0.025 to 160 g / 60 kg, preferably 0.05 to 80 g / 60 kg, based on the weight of the user. From the viewpoint of muscle-building action and anti-obesity action, it is more preferably 0.1 to 40 g / 60 kg. Similarly, the amount of the oral composition of the present invention used at one time is not particularly limited. For example, when the oral composition is a beverage, it is 2 to 4000 ml / 60 kg, preferably 2 to 4000 ml / 60 kg, based on the body weight of the user. It is 4 to 2000 ml, and more preferably 8 to 1000 ml / 60 kg from the viewpoint of muscle-building action and anti-obesity action. In the case of food forms other than beverages, and when the solid content of beverages is converted as a composition, it is 0.005 to 160 g / 60 kg, preferably 0.01 to 80 g / 60 kg, based on the weight of the user. From the viewpoint of muscle-building action and anti-obesity action, it is more preferably 0.02 to 40 g / 60 kg.

The oral composition of the present invention may contain only corosolic acid and maslinic acid, or may contain other components in addition to these two components. Other ingredients are not limited as long as they are usually used as foods, and for example, nutritional ingredients such as vitamins and minerals, plant-derived ingredients, animal-derived ingredients, functional sugars, polypeptides, vitamins, lactic acid bacteria, and bifidus. Bacteria such as butyric acid bacteria can be mentioned, and water-soluble vitamins (vitamins B1, B2, B3, B5, B6, B12, B13, B15, B17, biotin, choline) can be mentioned from the viewpoint of muscle-building action and anti-obesity action. , Vitamins such as folic acid, inositol, PABA, vitamin C, vitamin P), oil-soluble vitamins (vitamins A, D, E, K); Minerals such as magnesium, phosphorus, zinc, iron; contained in taurine, garlic, etc. Sulfur-containing compounds; flavanoids or flavonoids such as hesperidin and quercetin; proteins such as collagen; peptides; amino acids; animal fats and oils; vegetable fats and oils; crushed products or extracts of animals and plants. In particular, components necessary for muscle synthesis are preferable, and examples thereof include amino acids containing branched-chain amino acids and high-protein raw materials such as whey protein. The content of other components can be appropriately selected depending on the usage mode of the oral composition of the present invention and the like.

The oral composition of the present invention includes, for example, pharmaceuticals (including non-pharmaceutical products), functional foods whose efficacy has been approved by a predetermined organization such as foods for specified health use, foods with nutritional function, foods with functional claims, etc. It can be used as a so-called health food, general food, food additive, feed and the like.

The oral composition of the present invention can be used as a muscle-building composition used for muscle-building. As such a composition for muscle building, if it contains corosolic acid and mass phosphoric acid in a specific content ratio and can be distinguished from other products as a product in that it is used for muscle building and recovery from muscle fatigue. It is not particularly limited, and for example, muscle strengthening, enhancement of muscle synthesis, suppression of muscle decomposition, muscle mass (muscle weight, muscle breakage) in any of the main body, packaging, instruction manual, and advertisement of the product according to the present invention. Suppression / maintenance / increase of area, muscle density), suppression / maintenance / improvement of muscle quality, suppression / maintenance / increase of muscle strength (power, endurance), suppression / maintenance / improvement of athletic ability, metabolism Suppression / maintenance / improvement of (basal metabolism, resting and exercise metabolism), suppression / maintenance / increase of lean body mass, prevention / improvement of muscle fatigue, metabolism improvement effect by muscle strengthening, prevention / improvement of locomotive syndrome The scope of the present invention includes those indicating that they have an effect and a function of preventing / improving sarcopenia. The muscle-building composition of the present invention is not limited to the one in which the combinational components (corosolic acid and maslinic acid) of the present invention are displayed as active ingredients for muscle-building on the packaging of the product or the like. For example, the active ingredient may not be specified, only corosolic acid may be labeled as the active ingredient, or only maslinic acid may be labeled as the active ingredient.

Specifically, examples of the muscle-building composition of the present invention include pharmaceuticals (including non-pharmaceutical products) and so-called health foods. In so-called health foods, "supporting the ability to build muscle" and "muscle" "Suppress the decomposition of", "Strengthen muscle strength", "Suppress / maintain / improve / improve walking ability", "Improve metabolism by strengthening muscles", "Suppress the decline of metabolism", "Prevent muscle fatigue"・ Recovery, "suppression and maintenance of balance ability", "shape up", "macho", "fine macho", "beautiful body", "prevention of falling asleep", "prevention of falls", "improvement of metabolism by muscle building" It is possible to exemplify those displaying "to plan", "maintain muscle mass and strength", and the like. The target for ingesting the oral composition of the present invention is not particularly limited as long as it is a person who needs muscle strengthening, but a person for the purpose of shape-up, an athlete, an elderly person with weak legs, etc. It can be preferably exemplified.

In addition, the oral composition of the present invention can be used as an anti-obesity composition used for anti-obesity. As such an anti-obesity composition, if it contains corosolic acid and mass phosphoric acid in a specific content ratio and can be distinguished from other products as a product in that it is used for anti-obesity (obesity suppression). It is not particularly limited, and for example, anti-obesity (diet, reduction of body fat, suppression of body fat accumulation, improvement of metabolic syndrome, slimming, etc. Is included in the scope of the present invention. The anti-obesity composition of the present invention is not limited to the one in which the combinational ingredients (corosolic acid and maslinic acid) of the present invention are displayed as active ingredients of anti-obesity on the packaging of the product. For example, the active ingredient may not be specified, only corosolic acid may be labeled as the active ingredient, or only maslinic acid may be labeled as the active ingredient.

Specifically, examples of the anti-obesity composition of the present invention include pharmaceuticals (including non-medicinal products) and so-called health foods. In so-called health foods, "for those who are concerned about body weight" and " "For those who are overweight", "For those who are concerned about body weight (BMI)", "Reduce weight and abdominal fat (visceral fat and subcutaneous fat)", "Reduce waist circumference", etc. It can be exemplified.

The muscle-building 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, but when used in combination with exercise, a more excellent effect can be obtained. Obtainable. The exercise referred to here is any one or more of aerobic exercise and resistance exercise (strength training, weight training). In particular, when the muscle-building effect of the oral composition of the present invention is obtained, the type of exercise used in combination with the oral composition of the present invention is not particularly limited, but one or more of aerobic exercise and resistance exercise is carried out. It is preferable, and it is particularly preferable to carry out a resistance exercise. The amount of exercise when exercising is 10 minutes or more, preferably 20 minutes or more, and more preferably 30 minutes or more per day.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to these Examples, and the present invention can take various aspects as long as the problems of the present invention can be solved. ..

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

[Preparation of test substance]
Each test substance was prepared as follows.
Each test substance was dissolved in DMSO, and DMEM supplemented with 1% penicillin / streptomycin was prepared to have a differentiation-inducing medium of 2% HS (horse serum) so that the test substance concentration was 3 μg / mL. Diluted. The final concentration of DMSO was adjusted to 0.5%, and each test substance was mixed in the following ratio. Table 1 shows the contents of the test substances used in the following tests.

[Measurement of IGF-1 / Gapdh gene expression level]
(1) Mouse myoblasts C2C12 were seeded on a collagen-coated 24-well plate at 5.0 × 10 ⁴ cells / well, and cultured at 37 ° C. in a 5% CO ₂ incubator for 24 hours.
(2) After removing the medium, the medium was washed twice with DMEM, 1 mL / well of differentiation-inducing medium (2% HS-DMEM) was added, and the _{cells were cultured in a 5% CO 2} incubator at 37 ° C for 6 days (muscle tube). Induced differentiation into).
(3) After removing the medium, a differentiation-inducing medium containing the test substance was added at 500 μL / well, and the _{cells were cultured at 37 ° C. in a 5% CO 2} 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 (manufactured by QIAGEN).
(5) One-step real-time PCR using the obtained RNA and IGF-1 primers (manufactured by QIAGEN) using One Step TB Green (registered trademark) PrimeScript RT-PCR Kit II (Perfect Real Time) (manufactured by Takara Bio). , And the gene expression level of IGF-1 was measured. As an endogenous control, the gene expression level of Gapdh was measured using a Gapdh primer (manufactured by QIAGEN), and the relative value with respect to the control was calculated. The results are shown in FIG.

Since IGF-1 has a protein synthesis promoting action on skeletal muscle, it is known to be involved in a muscle strengthening action. From FIG. 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 level of IGF-1 in Examples 1 to 4 containing a specific amount of corosolic acid and maslinic acid was 1.50 or more, showing an excellent gene expression promoting action as compared with Comparative Examples 1 to 3. .. In particular, when the content ratio of corosolic acid: maslinic acid is 3.3: 1 to 6: 1 by mass ratio, the gene expression level of IGF-1 is 1.58 or more, and a particularly excellent gene expression promoting action is exhibited. Indicated. From the above, it can be seen that the oral composition of the present invention exhibits an excellent muscle-building effect because the gene expression level of IGF-1 is increased by containing corosolic acid and maslinic acid in a specific content ratio. ..

2. Evaluation of muscle-building and anti-obesity effects Male C57BL / 6J mice were acclimatized for 9 days and grouped based on body weight. From the start of the test, the feeds listed in Table 2 below were allowed to be freely ingested for 56 days. The feed was based on AIN-76, and as corosolic acid and maslinic acid, a mixture containing corosolic acid: maslinic acid = 4: 1 was used. After weighing on the 56th day of the test, autopsy was performed under a 1-hour fast. The abdomen was opened under isoflurane anesthesia, and visceral fat, subcutaneous fat, and skeletal muscle (gastrocnemius muscle, quadriceps femoris muscle) were removed and weighed. The visceral fat was the total amount of fat removed from the mesentery, peri-testis, perirenal and retroperitoneum. The results are shown in Table 3.

From Table 3, it can be seen that Example 5 containing corosolic acid: maslinic acid at a ratio of 4: 1 gained less body weight than Comparative Example 6. Further, since the fat weight per body weight is small and the muscle weight per body weight is large, it can be seen that the muscle can be strengthened and the body fat can be reduced.

Based on the above, the oral composition of the present invention contains corosolic acid and maslinic acid in a specific content ratio to suppress weight gain and fat gain, increase muscle, and express the gene of IGF-1. It can be seen that it exhibits an excellent anti-obesity effect and a muscle-building effect.

Example 6
A tablet (250 mg per tablet) consisting of the following components was produced. By ingesting the obtained tablets twice a day, 2 tablets at a time, excellent muscle-building action and anti-obesity action can be obtained.

Example 7
A drink (200 mL) consisting of the following ingredients was produced. By ingesting the obtained drink twice a day, an excellent muscle-building effect and an anti-obesity effect can be obtained.

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 them three times a day, excellent muscle-building and anti-obesity effects can be obtained.

Example 9
Granules consisting of the following components were produced. By dissolving 15 g of the obtained granules in 150 mL of water and ingesting them twice a day, excellent muscle-building and anti-obesity effects can be obtained.

Example 10
Granules consisting of the following components were produced, and 300 mg was encapsulated in a capsule film. By ingesting the obtained capsules twice a day, 2 capsules at a time, excellent muscle-building action and anti-obesity action can be obtained.

Since the oral composition of the present invention has an excellent muscle-building effect and an anti-obesity effect, it is highly industrially useful.

Claims (1)

A composition for strengthening muscle strength, which comprises corosolic acid and maslinic acid, wherein the content ratio of corosolic acid to maslinic acid is mass ratio of corosolic acid: maslinic acid = 3.3: 1 to 7 :. The composition for strengthening muscle strength, which is 1.

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