Composition for promoting glucagon-like peptide-1 secretion

Abstract

To provide an oral composition having excellent glucagon-like peptide-1 secretion promoting action and appetite suppressing action.SOLUTION: The glucagon-like peptide-1 secretion-promoting composition contains Terminalia beryllia. The appetite suppressing composition contains Terminalia beryllia.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a composition for promoting glucagon-like peptide-1 secretion containing Terminalia bellirica, and a composition for suppressing appetite containing Terminalia bellirica. [Background technology]

[0002] In recent years, due to various environmental changes, an increasing number of people are concerned about metabolic syndrome. Because metabolic syndrome increases the risk of various diseases, its improvement is a social issue.

[0003] Glucagon-like peptide-1 (GLP-1), a hormone secreted by L cells scattered throughout the gastrointestinal tract, has been shown to stimulate the satiety center and inhibit gastrointestinal peristalsis in response to food. GLP-1 has also attracted attention for its anti-obesity properties, and is expected to be effective in treating metabolic syndrome. However, because GLP-1 has very low stability in the body, optimization of the administration method and route, as well as the search for functional analogs with high stability in the body, are necessary.

[0004] Therefore, instead of directly administering glucagon-like peptide-1, research has been conducted on substances that promote the secretion of glucagon-like peptide-1 in the digestive tract. For example, Patent Document 1 discloses that hydroxybutyl-β-cyclodextrin has the effect of promoting the secretion of glucagon-like peptide-1. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Japanese Patent Application Laid-Open No. 2016-098173 Summary of the Invention [Problem to be solved by the invention]

[0006] An object of the present invention is to provide a novel composition having an excellent glucagon-like peptide-1 secretion-stimulating effect. [Means for solving the problem]

[0007] In order to solve the above problems, the present applicant has conducted extensive research into various substances and has surprisingly found that Terminalia bellirica has excellent glucagon-like peptide-1 secretion promoting and appetite suppressing effects. The present invention has been completed based on this finding.

[0008] The outline of the present invention is as follows. <1> A composition for promoting glucagon-like peptide-1 secretion, characterized by containing Terminalia bellirica. <2> The glucagon-like peptide-1 is an active glucagon-like peptide-1. <1> 2. A composition for promoting glucagon-like peptide-1 secretion according to claim 1. <3> A composition for suppressing appetite, characterized by containing Terminalia bellirica. <4> A food characterized by containing gallic acid or a salt thereof derived from Terminalia bellirica. <1> ~ <3> The composition according to any one of the preceding claims. [Effects of the Invention]

[0009] According to the present invention, by containing Terminalia bellirica, a composition having an excellent glucagon-like peptide-1 secretion promoting effect can be provided. Furthermore, according to the present invention, by containing Terminalia bellirica, a composition having an excellent appetite suppressing effect can be provided because it has the ability to promote glucagon-like peptide-1 secretion.

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

[0011] Terminalia belliricca is a broad-leaved tree of the genus Terminalia in the family Combretaceae. In the present invention, any of the leaves, stems, and fruit can be used, but the fruit is preferably used. From the viewpoint of the glucagon-like peptide-1 secretion-promoting effect and appetite suppressing effect, parts of the fruit excluding the seeds (the peel and flesh) are more preferably used.

[0012] The Terminalia bellirica of the present invention can be used in processed forms such as pulverized material, juice, and extract. Examples of pulverized material include powder and granules. The juice and extract may be in liquid form, but they can also be used as a paste or dry powder. When preparing a paste or dry powder, the juice or extract obtained from Terminalia bellirica may be produced alone, or processed with an excipient. The extract can be obtained by extraction using an appropriate solvent. Examples of solvents that can be used include water, methanol, ethanol, isopropanol, acetone, 1,3-butylene glycol, ethylene glycol, propylene glycol, glycerin, acetic acid, ethyl acetate, diethyl ether, hexane, or a mixture thereof. In the present invention, water, methanol, ethanol, or a mixture thereof is preferably used to effectively exert the glucagon-like peptide-1 secretion-promoting effect. The extraction temperature can be adjusted appropriately from room temperature to a temperature below the boiling point of the extraction solvent. Commercially available products can be used in the present invention.

[0013] The content of Terminalia bellirica in the oral composition of the present invention is not particularly limited as long as it is an amount that is observed to have the effect of promoting glucagon-like peptide-1 secretion and suppressing appetite, but for example, it is preferably 0.005% by mass or more and 80% by mass or less in the composition, more preferably 0.01% by mass or more and 50% by mass or less, and particularly preferably 0.05% by mass or more and 30% by mass or less.

[0014] In the present invention, it is preferable to contain gallic acid or a salt thereof derived from Terminalia bellirica. The content of gallic acid or a salt thereof in the oral composition of the present invention is preferably 0.0001% by mass or more in the composition, more preferably 0.0005% by mass or more, and particularly preferably 0.001% by mass or more. There is no particular upper limit to the content of gallic acid or a salt thereof, but it is preferably 30% by mass or less in the composition, more preferably 20% by mass or less, and particularly preferably 10% by mass or less.

[0015] The content of gallic acid or a salt thereof in the oral composition of the present invention can be measured by a commonly known analytical method for gallic acid or a salt thereof that is suitable for the conditions of the sample to be measured. For example, analysis can be performed by liquid chromatography. Note that, during measurement, appropriate treatment may be performed as needed, such as removing impurities from the sample, to adapt the sample to the separation capacity of the apparatus.

[0016] [2. Oral Composition] The oral composition of the present invention is characterized by containing Terminalia bellirica.

[0017] 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, granules, granules, tablets, liquid, beverage, gel, paste, capsules such as hard capsules and soft capsules, caplets, chewable forms, etc., can be mentioned. Depending on the form used, various excipients, binders, lubricants, stabilizers, diluents, bulking agents, thickeners, gelling agents, emulsifiers, colorants, flavorings, sweeteners, additives, etc. can be blended.From the viewpoint of stability and ease of intake at the same time as meals, the oral composition of the present invention is preferably in the form of powder, granules, granules, tablets, chewable forms, or capsules, and more preferably in the form of tablets or powder.

[0018] The oral composition of the present invention may contain only Terminalia bellirica or may contain other ingredients. The other ingredients are not limited to those commonly used in foods, and include, for example, nutritional components such as vitamins and minerals, plant-derived components, animal-derived components, functional sugars, polypeptides, vitamins, and fungi such as lactic acid bacteria, bifidobacteria, and butyric acid bacteria. From the viewpoint of glucagon-like peptide-1 secretion-promoting activity and appetite suppressing activity, examples of the other ingredients include water-soluble vitamins (vitamins B1, B2, B3, B5, B6, B12, B13, B15, B17, biotin, choline, folic acid, inositol, PABA, vitamin C, and vitamin P) and oil-soluble vitamins (vitamins A, D, E, and K), minerals such as magnesium, phosphorus, zinc, and iron, sulfur-containing compounds found in foods such as taurine and garlic, flavanoids or flavonoids such as hesperidin and quercetin, proteins such as collagen, peptides, amino acids, animal fats and oils, vegetable fats and oils, and ground products or extracts of animals and plants.

[0019] The daily intake amount of the oral composition of the present invention is not particularly limited and can be set appropriately depending on the mode of use and the content of use by the user. For example, it is 0.01 to 160 g / 60 kg, preferably 0.05 to 80 g / 60 kg, based on the user's body weight. From the viewpoint of promoting glucagon-like peptide-1 secretion and suppressing appetite, it is more preferably 0.1 to 40 g / 60 kg. The amount of the oral composition of the present invention used per dose is also not particularly limited. For example, it is 0.005 to 160 g / 60 kg, preferably 0.01 to 80 g / 60 kg, based on the user's body weight. From the viewpoint of promoting glucagon-like peptide-1 secretion and suppressing appetite, it is more preferably 0.02 to 40 g / 60 kg. When the oral composition is taken as a beverage, the amount is the solid content of the beverage (excluding water).

[0020] The oral composition of the present invention can be used as, for example, a pharmaceutical product (including quasi-drugs), a so-called health food such as a functional food whose efficacy has been approved by a designated organization, such as a food for specified health uses, a food with nutrient function claims, or a food with functional claims, or as a general food, a food additive, a feed, etc. The oral composition of the present invention may be taken before meals, between meals, after meals, or simultaneously with meals; however, from the viewpoint of the glucagon-like peptide-1 secretion-promoting effect and the appetite suppressing effect, it is preferably taken before meals, after meals, or simultaneously with meals, and more preferably simultaneously with meals.

[0021] The oral composition of the present invention can be used as a composition for promoting glucagon-like peptide-1 secretion. Glucagon-like peptide-1, also known as GLP-1, is a hormone found in the body and is known to be secreted from the small intestine. As described in detail in the Examples, the oral composition of the present invention is particularly effective in promoting the secretion of active glucagon-like peptide-1. The glucagon-like peptide-1 secretion-promoting composition of the present invention is not particularly limited as long as it contains Terminalia bellirica and can be distinguished from other products in that it is used to promote glucagon-like peptide-1 secretion. For example, the scope of the present invention includes a product that displays on the product itself, packaging, instructions, or promotional materials that it has the function of promoting glucagon-like peptide-1 secretion. Note that the glucagon-like peptide-1 secretion-promoting composition of the present invention is not limited to products that display Terminalia bellirica as the active ingredient for promoting glucagon-like peptide-1 secretion on the product packaging, etc., and may also be a product in which the active ingredient is not specified.

[0022] Specifically, examples of the compositions of the present invention for promoting glucagon-like peptide-1 secretion include so-called health foods such as pharmaceuticals (including quasi-drugs) and functional foods whose efficacy has been approved by designated organizations, such as foods for specified health uses, foods with nutrient functions, and foods with functional claims.Examples of so-called health foods include those that are labeled as "promoting the secretion of glucagon-like peptide-1."

[0023] The oral composition of the present invention can also be used as an appetite suppressant. Glucagon-like peptide-1 suppresses gastric motility, making it easier to feel full during meals and reducing hunger between meals. It is known that the appetite suppressant composition of the present invention has the effect of suppressing appetite, such as making it difficult to suppress appetite. There are no particular limitations on the appetite suppressant composition, as long as it contains Terminalia bellirica and can be distinguished from other products in that it is used to suppress appetite. For example, the scope of the present invention includes products that display the appetite suppressant function on the product itself, packaging, instructions, or promotional materials of the present invention. Note that the appetite suppressant composition of the present invention is not limited to products that display Terminalia bellirica as the appetite suppressant active ingredient on the product packaging, etc., and may also be a product in which the active ingredient is not specified.

[0024] Specifically, the appetite suppressant composition of the present invention includes so-called health foods such as pharmaceuticals (including quasi-drugs) and functional foods such as foods for specified health uses, foods with nutrient functions, and foods with functional claims whose efficacy has been approved by designated organizations.Examples of so-called health foods include those that claim to "suppress appetite," "prevent overeating," "for those concerned about overeating," "reduce excessive food intake," "for those who want to feel full," "reduce hunger," "for those who want to reduce snacking," and "suppress stomach motility."

[0025] The packaging form of the oral composition of the present invention is not particularly limited and can be appropriately selected depending on the dosage form, etc., and examples include blister packs such as PTPs; strip packaging; heat seals; aluminum pouches; film packaging using plastics, synthetic resins, etc.; glass containers such as vials; and plastic containers such as ampoules. [Example]

[0026] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples, and the present invention can take various forms as long as the object of the present invention can be achieved.

[0027] The effect of ingestion of a composition containing Terminalia bellirica on the secretion of glucagon-like peptide-1 (1) Test Substance Example 1: Terminalia bellirica extract (manufactured by Toyo Shinyaku Co., Ltd.) was mixed with reduced palatinose, powdered cellulose, calcium stearate, and fine silicon dioxide, and the mixture was compressed into tablets. Each tablet weighed 250 mg, and 4 tablets contained 20.8 mg of gallic acid (derived from Terminalia bellirica). Comparative Example 1: The Terminalia bellirica extract of Example 1 was replaced with caramel color, and a product colored in the same way as Example 1 was used.

[0028] (2) Glucagon-like peptide-1 (GLP-1) secretion promotion test: A placebo-controlled, randomized, double-blind, crossover study was conducted in healthy adult men and women using the test substance of Example 1 or Comparative Example 1. Seven subjects (aged 20 to 65 years, 4 men and 3 women) were divided into two groups, and two studies were conducted in which each subject ingested either Example 1 or Comparative Example 1 once with a meal. That is, in the first study, four tablets of the test substance of Example 1 or Comparative Example 1 were ingested with water or lukewarm water, and 300 g of cooked rice was ingested within 10 minutes as a loading meal. In the second study, four tablets of the test substance were ingested with water or lukewarm water, in the reverse order of the first study (e.g., if Example 1 was ingested the first time, Comparative Example 1 was ingested the second time), and 300 g of cooked rice was ingested within 10 minutes as a loading meal. Note that the second study was conducted with a rest period of at least two weeks to avoid any influence from the first study.

[0029] Blood samples were taken before, 30, 60, 90, 120, and 180 minutes after ingestion of the test food and the challenge meal, and active GLP-1 was measured. A Glucagon-Like Peptide-1 (Active) ELISA KIT (Millipore) was used to measure active GLP-1. The difference in GLP-1 levels between before ingestion and 30, 60, 90, 120, and 180 minutes after ingestion was calculated. The area under the blood concentration curve (iAUC) was calculated using the trapezoidal method based on the results.

[0030] The iAUC of active GLP-1 when Comparative Example 1 was taken was 288 pmol·min / L, and the iAUC of active GLP-1 when Example 1 was taken was 369 pmol·min / L, which were significantly higher than when Comparative Example 1 was taken.

[0031] From the above, it can be seen that taking an oral composition containing Terminalia bellirica with a meal shows an excellent effect of promoting the secretion of glucagon-like peptide-1. From this, it can be seen that an oral composition containing Terminalia bellirica has an excellent appetite suppressing effect.

[0032] Example 2 Tablets (250 mg) containing the following ingredients were manufactured. Taking two tablets three times a day provides excellent glucagon-like peptide-1 secretion promoting and appetite suppressing effects.

[0033] [Table 1]

[0034] Example 3 A liquid beverage containing the following ingredients was produced. By consuming the resulting liquid beverage at a dose of 100 ml three times a day, it is possible to obtain excellent glucagon-like peptide-1 secretion promoting effects and appetite suppression effects.

[0035] [Table 2]

[0036] Example 4 Granules containing the following ingredients were prepared. By dissolving 3 g of the resulting granules in 100 ml of water and taking them three times a day, excellent glucagon-like peptide-1 secretion promoting and appetite suppressing effects can be obtained.

[0037] [Table 3]

[0038] Example 5 Granules containing the following ingredients were prepared and 200 mg of each was placed in a capsule. Taking two capsules three times a day provides excellent glucagon-like peptide-1 secretion promoting and appetite suppressing effects.

[0039] [Table 4] [Industrial Applicability]

[0040] The oral composition of the present invention has excellent glucagon-like peptide-1 secretion-stimulating and appetite-suppressing effects, and is therefore highly useful industrially.

Claims

1. A composition for promoting glucagon-like peptide-1 secretion, characterized by containing 2.08% by mass or more of gallic acid or a salt thereof derived from Terminalia bellirica.

2. A composition for suppressing appetite, characterized by containing 2.08% by mass or more of gallic acid or its salt derived from Terminalia bellirica.

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