Oral Composition
An oral composition with a specific ratio of gallic acid to ellagic acid, optionally with chebulic acid and catechins, addresses the need for effective fat and sugar absorption inhibition, reducing triglycerides and blood glucose levels, and decreasing body fat.
Patent Information
- Application Number
- JP2025080326
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2025-05-13
- Publication Date
- 2025-12-12
- Estimated Expiration
- 2044-11-08
AI Technical Summary
There is a demand for an oral composition that effectively inhibits fat and sugar absorption, reduces triglyceride and blood glucose levels, and decreases body fat or BMI without the unpleasant taste associated with existing anti-obesity ingredients like the pericarp of the Akebia family.
An oral composition containing gallic acid and ellagic acid in a specific mass ratio of 1:0.01 to 0.7, optionally with chebulic acid and catechins, to inhibit isomaltase and lipase activity, thereby suppressing fat and sugar absorption and reducing body fat.
The composition effectively inhibits fat and sugar absorption, reduces triglyceride and blood glucose levels, and decreases body fat, providing anti-obesity benefits.
Smart Images

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Abstract
Description
[Technical Field]
[0001] The present invention relates to an oral composition and a food or drink. [Background technology]
[0002] In recent years, the overall trend in Japanese people has been toward a decline in physical activity, while dietary energy intake has tended to be relatively excessive, raising concerns about the impact on health. It is believed that lifestyle habits such as these are deeply involved in the onset of diabetes and obesity. While diabetes and obesity were once thought to be caused by aging, in recent years their incidence has become more prevalent among young people, and subsequent research has revealed that lifestyle habits are deeply involved. Because diabetes and obesity can lead to more serious diseases such as arteriosclerosis and cancer, it is necessary to prevent or improve diabetes and obesity through daily eating habits.
[0003] One way to prevent diabetes and obesity is to suppress elevated blood glucose and triglyceride levels. To suppress elevated blood glucose levels, it is effective to inhibit the activity of disaccharidases present in the gastrointestinal mucosa and suppress glucose production. Inhibition of disaccharidases suppresses elevated blood glucose levels and inhibits intestinal sugar absorption, leading to reduced body fat, anti-obesity, and lower BMI. Another way to suppress blood triglycerides is to inhibit pancreatic lipase, which suppresses the production of free fatty acids. This suppresses the absorption of triglycerides in the intestine and, ultimately, the body, thereby suppressing blood triglyceride levels, leading to reduced triglyceride levels, reduced body fat, anti-obesity, and lower BMI. For example, Patent Document 1 describes that the pericarp of plants of the Akebia family exhibits anti-obesity effects and neutral fat elevation suppression effects due to its lipase inhibitory activity. However, some consumers dislike the taste of the pericarp of plants of the Akebia family. Therefore, there has been a demand for the development of a new oral composition that exhibits effects such as anti-obesity effects and neutral fat elevation suppression. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2010-265182 Summary of the Invention [Problem to be solved by the invention]
[0005] The present invention aims to provide a new oral composition that exhibits anti-obesity effects, inhibits fat absorption, inhibits increases in triglyceride levels, inhibits sugar absorption, inhibits increases in blood glucose levels, and reduces body fat or BMI. [Means for solving the problem]
[0006] The present inventors have surprisingly discovered that, by setting the mass ratio of gallic acid to ellagic acid in a composition containing gallic acid and ellagic acid within a specific range, an oral composition can be obtained that has excellent functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or reduction of BMI.
[0007] That is, the present invention provides an oral composition containing gallic acid and ellagic acid, wherein the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 1:0.01 to 0.7. [Effects of the Invention]
[0008] According to the present invention, an oral composition containing gallic acid and ellagic acid can be provided, and in particular, an oral composition such as a food or beverage that has isomaltase inhibitory activity and lipase inhibitory activity and is effective for anti-obesity, suppressing fat absorption, suppressing increases in triglyceride levels, suppressing sugar absorption, suppressing increases in blood sugar levels, reducing body fat, or reducing BMI can be provided. DETAILED DESCRIPTION OF THE INVENTION
[0009] Preferred embodiments of the oral composition of the present invention will be described below. The oral composition of the present invention contains gallic acid as an active ingredient for its functions of anti-obesity, inhibiting fat absorption, inhibiting increases in triglyceride levels, inhibiting sugar absorption, inhibiting increases in blood glucose levels, reducing body fat, or reducing BMI.
[0010] 1. Gallic Acid The gallic acid used in the present invention is a compound represented by the formula C7H6O5 and is also known as 3,4,5-trihydroxybenzoic acid. Gallic acid is known to have anti-obesity properties, inhibit fat absorption, inhibit increases in triglyceride levels, inhibit increases in sugar absorption, inhibit increases in blood glucose levels, reduce body fat, and reduce BMI, and it also functions as an active ingredient in the composition of the present invention. The gallic acid used in the present invention is not particularly limited as long as it is suitable for use as a food product, and plant-derived gallic acid or synthetically obtained gallic acid can be used. When plant-derived gallic acid is used in the composition of the present invention, plant extracts or ground powders may be used as the gallic acid source, or purified products thereof may also be used. Ground powder refers to powder obtained by drying and grinding plants. When plant-derived gallic acid is used, examples of the plant from which it is derived include green tea, dates, and persimmons. Furthermore, the gallic acid used in the present invention may be anhydrous or a hydrate, such as a monohydrate. Gallic acid may also be in the form of a salt. When a salt of gallic acid is used in the present invention, examples of the salt of gallic acid include alkali metal salts. When gallic acid is a hydrate in the present invention, the amount of gallic acid referred to in this specification is calculated as an anhydrous form. When a salt of gallic acid is used in the present invention, the amount of gallic acid refers to the amount calculated as gallic acid.
[0011] The proportion of gallic acid in the oral composition of the present invention is preferably from 0.001 to 96% by mass, more preferably from 0.001 to 90% by mass, even more preferably from 0.005 to 87% by mass, and particularly preferably from 0.01 to 84% by mass, based on the solid content of the composition, from the viewpoint of further enhancing the functions of gallic acid in anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of increase in blood glucose levels, and reduction of body fat or BMI, and from the viewpoint of taste when orally ingested. In this specification, the solid content refers to the content in the composition when the composition is in a solid form, and refers to the total amount of all components in the composition excluding water when the composition is in a liquid or fluid form.
[0012] The amount of gallic acid in the composition of the present invention can be measured by HPLC. For example, a Unison UK-C18 (HT 3 μm φ3 × 100 mm) manufactured by Imtakt Corporation can be used, with a 1% formic acid aqueous solution as mobile phase A and a 1% formic acid acetonitrile solution as mobile phase B, with a column temperature of 45°C and a flow rate of 0.7 ml / min. The gradient conditions can be as follows. During measurement, samples may be treated as needed, such as by removing impurities, to match the resolution of the instrument.
[0013] [Table A]
[0014] Column: Imtakt Unison UK-C18 HT 3 μm φ3 × 100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Measurement wavelength: 276 nm Mobile phase A solution: 1% formic acid aqueous solution Mobile phase B: 1% formic acid in acetonitrile
[0015] 2. Ellagic acid The composition of the present invention contains ellagic acid. Ellagic acid is a natural phenolic compound. 14 It is expressed as H6O8. The ellagic acid used in the present invention is not particularly limited as long as it is suitable for use as a food product, and plant-derived ellagic acid or synthetic ellagic acid can be used. When plant-derived ellagic acid is used in the composition of the present invention, the ellagic acid source may be a plant extract or pulverized powder, or a purified product thereof. When plant-derived ellagic acid is used, examples of the plant from which it is derived include strawberry, raspberry, and pomegranate. Furthermore, the ellagic acid used in the present invention may be an anhydride or a hydrate such as a monohydrate. Furthermore, ellagic acid may be in the form of a salt. When a salt of ellagic acid is used in the present invention, examples include alkali metal ellagic acid salts. Note that, in the present invention, when ellagic acid is a hydrate, the amount of ellagic acid referred to in this specification is calculated as an anhydride. In the present invention, when a salt is used as ellagic acid, the amount of ellagic acid referred to in this specification is calculated as an ellagic acid equivalent.
[0016] In the present invention, the inventors believe that ellagic acid is an auxiliary ingredient that enhances the effects of gallic acid. To ensure the effects of both ingredients, the mass ratio of gallic acid to ellagic acid in the composition of the present invention must be 1:0.01-0.7 (gallic acid:ellagic acid). As shown in the examples described below, the use of ellagic acid in the present invention can more effectively enhance the functions of gallic acid than when gallic acid is combined with a component other than ellagic acid (e.g., ascorbic acid or erythorbic acid) without ellagic acid. Furthermore, in the present invention, by maintaining the mass ratio of gallic acid to ellagic acid within the range of 1:0.01-0.7 (gallic acid:ellagic acid), the functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or BMI can be more effectively enhanced than when the ratio is outside this range.
[0017] In the present invention, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood glucose levels, reduction in body fat, or reduction in BMI, the mass ratio of gallic acid to ellagic acid in the composition is preferably gallic acid:ellagic acid = 1:0.03-0.5, more preferably 1:0.06-0.4, even more preferably gallic acid:ellagic acid = 1:0.07-0.3, particularly preferably gallic acid:ellagic acid = 1:0.08-0.25, and especially preferably gallic acid:ellagic acid = 1:0.1-0.2.
[0018] From the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood glucose levels, and reduction of body fat or BMI, the proportion of ellagic acid in the oral composition of the present invention is preferably from 0.00001% by mass to 40% by mass, more preferably from 0.00005% by mass to 30% by mass, and even more preferably from 0.0001% by mass to 25% by mass, of the solid content of the oral composition, provided that the mass ratio of gallic acid to ellagic acid is within the above-mentioned range.
[0019] The amounts of gallic acid and ellagic acid in the composition of the present invention can be measured by HPLC. For example, a Unison UK-C18 (HT 3 μm φ3 × 100 mm) manufactured by Imtakt Corporation can be used, with a 1% formic acid aqueous solution as mobile phase A and a 1% formic acid acetonitrile solution as mobile phase B, with a column temperature of 45°C and a flow rate of 0.7 mL / min. The gradient conditions can be as follows. During measurement, samples may be treated as needed, such as by removing impurities, to match the resolution of the instrument.
[0020] [Table B]
[0021] Column: Imtakt Unison UK-C18 HT 3 μm φ3 × 100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Measurement wavelength: 276 nm Mobile phase A solution: 1% formic acid aqueous solution Mobile phase B: 1% formic acid in acetonitrile
[0022] 3. Chebulic acid The oral composition of the present invention preferably further contains chebulic acid from the viewpoint of further enhancing the functions of anti-obesity, suppressing fat absorption, suppressing an increase in neutral fat, suppressing sugar absorption, suppressing an increase in blood glucose level, and reducing body fat or BMI. Chebulic acid has the molecular formula: C 14 H 12 O 11 Chebulic acid is a compound represented by the formula: Chebulic acid is known to have the following chemical structure (1). The chebulic acid used in the present invention is not particularly limited as long as it is suitable for use as a food product, and plant-derived chebulic acid or synthetically obtained chebulic acid can be used. When plant-derived chebulic acid is used in the composition of the present invention, the source of chebulic acid may be a plant extract or crushed powder, or a purified product thereof. When the composition of the present invention contains chebulic acid, the inventors believe that chebulic acid serves as an auxiliary ingredient that enhances the effects of gallic acid. Chebulic acid may be an anhydride or a hydrate. Chebulic acid may also be in the form of a salt. When a salt of chebulic acid is used in the present invention, examples include alkali metal salts of chebulic acid. When chebulic acid is a hydrate, the amount of chebulic acid referred to herein is calculated as an anhydride. When a salt of chebulic acid is used in the present invention, the amount of chebulic acid referred to herein is calculated as a chebulic acid equivalent.
[0023] [ka]
[0024] When the oral composition of the present invention contains chebulic acid, the amount of chebulic acid is not limited, but from the viewpoint of further enhancing the functions of anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, and reduction of body fat or BMI, it is preferable that the oral composition of the present invention contain 0.01 parts by mass or more of chebulic acid per 1 part by mass of gallic acid, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of chebulic acid per 1 part by mass of gallic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.
[0025] When the oral composition of the present invention contains chebulic acid, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, and reduction of body fat or BMI, it preferably contains 0.01 part by mass or more of chebulic acid per 1 part by mass of the total of gallic acid and ellagic acid, more preferably 0.02 part by mass or more, even more preferably 0.05 part by mass or more, and particularly preferably 0.1 part by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of chebulic acid per 1 part by mass of the total of gallic acid and ellagic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.
[0026] When chebulic acid is contained in the oral composition of the present invention, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood glucose levels, reduction of body fat or reduction of BMI, the content of chebulic acid in the solid content of the oral composition is preferably 0.00001% by mass or more and 40% by mass or less, more preferably 0.00005% by mass or more and 30% by mass or less, and even more preferably 0.0001% by mass or more and 25% by mass or less.
[0027] The amount of chebulic acid in the composition of the present invention can be measured by LCMS. For example, a Unison UK-C18 (HT 3 μm φ3 × 100 mm) manufactured by Imtakt Corporation can be used, with 0.1% formic acid aqueous solution as mobile phase A and acetonitrile as mobile phase B, at a column temperature of 45°C and a flow rate of 0.7 mL / min. The ionization method can be electrospray, and the ionization mode can be negative. The gradient conditions can be as follows. During measurement, samples can be treated as needed, such as by removing impurities, to match the resolution of the instrument.
[0028] [Table C]
[0029] Column: Imtakt Unison UK-C18 HT 3 μm φ3 × 100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Ionization method: Electrospray Ionization mode: negative Setting mass number (m / z): 355 Mobile phase A solution: 0.1% formic acid aqueous solution Mobile phase B: acetonitrile
[0030] 4. Catechins The composition of the present invention preferably further contains catechins from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of increase in sugar absorption, suppression of increase in blood glucose levels, and reduction of body fat or BMI. As used herein, "catechins" collectively refers to non-gallate catechins selected from the group consisting of catechin, gallocatechin, epicatechin, and epigallocatechin, as well as gallate catechins selected from the group consisting of catechin gallate, gallocatechin gallate, epicatechin gallate, and epigallocatechin gallate. The content of catechins in this specification refers to the total amount of the above-mentioned eight compounds. In the present invention, when catechins are hydrates, the amount of catechins referred to in this specification is calculated on an anhydrous basis.
[0031] From the viewpoint of functionality as an auxiliary component of gallic acid, the catechins used in the present invention preferably have a ratio C1:C2 of the non-gallate catechin content C1 to the gallate catechin content C2 of 1:0.01 to 13, more preferably 0.05 to 7, although this is not a limitation. Furthermore, among the catechins, epigallocatechin gallate (EGCG) preferably accounts for 0.1 to 70% by mass, more preferably 0.5 to 60% by mass. The combined proportion of epigallocatechin (EGC) and epicatechin (EC) among the catechins is preferably 20% by mass or more, more preferably 30% by mass or more. The catechins preferably have a catechin (C) content of 0.01 to 40% by mass, more preferably 0.1 to 20% by mass.
[0032] The catechins used in the present invention are not particularly limited as long as they are suitable for use as food, and plant-derived catechins or synthetic catechins can be used. When plant-derived catechins are used in the compositions of the present invention, plant extracts or crushed powders, or purified products thereof, can be used as the catechin source. Examples of plants from which catechins can be derived include acacia catechu, green tea, cocoa beans, and apples. The inventors believe that when the compositions of the present invention contain catechins, they serve as auxiliary ingredients that enhance the effects of gallic acid.
[0033] When the oral composition of the present invention contains catechins, there are no particular restrictions on the amount of catechins contained, but from the viewpoint of further enhancing the functions of anti-obesity, suppressing fat absorption, suppressing increases in triglyceride levels, suppressing sugar absorption, suppressing increases in blood glucose levels, and reducing body fat or BMI, the oral composition of the present invention preferably contains 0.01 parts by mass or more of catechins per part by mass of gallic acid, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of catechins per part by mass of gallic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.
[0034] When the oral composition of the present invention contains catechins, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, and reduction of body fat or BMI, it preferably contains 0.01 parts by mass or more of catechins per part by mass of gallic acid and ellagic acid in total, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of catechins per part by mass of gallic acid and ellagic acid in total, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.
[0035] When the oral composition of the present invention contains catechins, the oral composition preferably contains 0.001% by mass or more, more preferably 0.005% by mass or more, and even more preferably 0.01% by mass or more of catechins based on the solid content of the oral composition, from the viewpoint of further enhancing the functions of anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, body fat reduction, or BMI reduction. Furthermore, the oral composition preferably contains 50% by mass or less of catechins, more preferably 40% by mass or less, even more preferably 30% by mass or less, and particularly preferably 25% by mass or less of catechins based on the solid content of the oral composition, from the viewpoint of further enhancing the functions of anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, body fat reduction, or BMI reduction.
[0036] In order to further enhance the functions related to anti-obesity, inhibition of fat absorption, inhibition of increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, reduction of body fat or reduction of BMI, the oral composition of the present invention preferably contains at least chebulic acid in addition to gallic acid and ellagic acid, and more preferably contains chebulic acid and catechins.
[0037] The amount of catechins in the composition of the present invention can be measured by HPLC. For example, an L-Column ODS (3 μm diameter, 4.6 × 250 mm) manufactured by Chemicals Evaluation and Research Institute, Japan can be used, with a 0.1 M aqueous acetic acid solution as mobile phase A and a 0.1 M acetonitrile solution as mobile phase B, at a column temperature of 40°C and a flow rate of 1.0 ml / min. The gradient conditions can be as follows: During measurement, samples may be treated as needed, such as by removing impurities, to match the resolution of the instrument.
[0038] [Table D]
[0039] Column: L-Column ODS 3 μm, 4.6 × 250 mm (Chemicals Evaluation and Research Institute, Japan) Column temperature: 40℃ Injection volume: 10μL Flow rate: 1.0 mL / min Measurement wavelength: 280 nm Mobile phase A: 0.1 M acetic acid aqueous solution Mobile phase B: 0.1 M acetic acid in acetonitrile
[0040] 5. Oral Compositions The oral composition of the present invention may contain components other than gallic acid, ellagic acid, chebulic acid, and catechins, to the extent that the components do not inhibit the expression of functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or BMI. Examples of such components include sugars, vitamins, minerals, proteins, dietary fiber such as insoluble dietary fiber, plants or processed plant products, and yeast. If necessary, the composition may further contain sweeteners, acidulants, colorants, thickeners, glazing agents, lubricants, excipients, anti-caking agents, nutritional supplements, binders, lubricants, stabilizers, diluents, bulking agents, emulsifiers, food additives, seasonings, and the like, which are commonly used in the food industry.
[0041] Examples of the form of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, granules, rods, plates, blocks, solids, pills, pastes, creams, caplets, gels, chewable tablets, sticks, etc. Among these forms, tablets, capsules, powders, granules, and liquids are preferred from the viewpoint of ease of administration.
[0042] Specific examples of the oral composition of the present invention include pharmaceuticals (including quasi-drugs) and food and beverage products. Among these, food and beverage products are particularly preferred from the viewpoint of easy intake in daily life.
[0043] The food and drink of the present invention may include so-called health foods such as general foods, foods with nutrient function claims, foods for specified health uses that have been approved by a designated organization for efficacy claims, and foods with functional claims. Foods that claim efficacy claims are sometimes collectively referred to as "health claim foods" or "functional foods."
[0044] The food and drink of the present invention is not particularly limited, but examples thereof include milk and dairy products; beverages such as soft drinks, fruit juice drinks, dairy drinks, alcoholic drinks, sports drinks, and energy drinks; seasonings; alcoholic beverages; processed agricultural and forestry products; confectioneries and breads; grain flour and noodles; processed seafood products; processed livestock products; oils and fats; cooked frozen foods; retort foods; instant foods; food ingredients; supplements, etc. Examples of the form of the supplements include tablets, capsules, powders, granules, and liquids.
[0045] 6. Oral compositions used for inhibiting fat absorption, etc. As will be apparent from the examples described below, the oral composition of the present invention can effectively inhibit intestinal isomaltase activity and lipase activity. As will be described later, isomaltase is an enzyme involved in sugar absorption, and lipase is an enzyme involved in fat absorption. Therefore, the oral composition of the present invention is suitable for use in one or more applications selected from (1) inhibition of fat absorption, (2) inhibition of an increase in triglyceride levels, (3) inhibition of sugar absorption, (4) inhibition of an increase in blood glucose levels, (5) anti-obesity, (6) reduction of body fat, and (7) reduction of BMI (Body Mass Index). Body fat refers to body fat and is a general term for visceral fat and subcutaneous fat. That is, the oral composition of the present invention can be used as (1) a composition for inhibiting fat absorption, (2) a composition for inhibiting an increase in triglyceride levels, (3) a composition for inhibiting sugar absorption, (4) a composition for inhibiting an increase in blood glucose levels, (5) an anti-obesity composition, (6) a composition for reducing body fat, or (7) a composition for reducing BMI (Body Mass Index).
[0046] (1) “Inhibition of fat absorption” refers to the reduction of the amount of triglycerides ingested through food that are absorbed into the body. (2) "Inhibition of an increase in neutral fat" means inhibition of an increase in the concentration of neutral fat in the blood after a meal or when fasting. (3) "Inhibition of sugar absorption" means suppressing the amount of sugar absorbed in the small intestine. (4) "Suppression of increase in blood glucose level" means suppression of increase in blood glucose level after a meal or when fasting. (5) “Anti-obesity” means reducing or suppressing weight gain, and preventing or improving the accumulation of fat in the body, and is a concept that includes dieting for beauty purposes. (6) "Reducing body fat" means reducing the amount of body fat (visceral fat and subcutaneous fat), specifically abdominal body fat (visceral fat and subcutaneous fat). (7) "Reduction of BMI" means reducing the BMI value. The mechanism by which the functions (1) to (7) of the present invention are achieved is as follows.
[0047] By ingesting the oral composition of the present invention, lipase activity in the body is inhibited. Lipase (pancreatic lipase) is a digestive enzyme synthesized in the pancreas and secreted into pancreatic juice to hydrolyze neutral fats. Dietary neutral fats are broken down by lipase into fatty acids and glycerol, which are easily absorbed by the body. The fatty acids and glycerol are then absorbed by the small intestinal villus epithelial cells. The absorbed fatty acids and glycerol are then resynthesized into neutral fats, which are then transported into the bloodstream via the lymphatic system. As will be seen from the examples described below, ingestion of the oral composition of the present invention inhibits lipase activity. Therefore, the breakdown of dietary triglycerides into fatty acids and glycerol is suppressed, resulting in a decrease in the amounts of fatty acids and glycerol absorbed by small intestinal villus epithelial cells. In other words, (1) fat absorption is suppressed. Furthermore, the amount of fatty acids and glycerol resynthesized into triglycerides is reduced, resulting in (2) an increase in triglyceride levels. As a result, (5) fat accumulation in the body is prevented (anti-obesity), and (6) body fat is reduced. As body fat is reduced, weight loss occurs, and (7) BMI is also reduced.
[0048] Furthermore, by taking the oral composition of the present invention, isomaltase activity in the body is inhibited. Isomaltase is a type of α-glucosidase, a disaccharidase present in the small intestinal mucosa that breaks down disaccharides into monosaccharides. When sugars contained in food reach the small intestine, they are broken down by the action of enzymes into easily absorbed monosaccharides (such as glucose), which are then absorbed through the small intestinal mucosa and transported to the liver, from which they are transported into the bloodstream. When the concentration of glucose in the blood rises, insulin converts glucose into triglycerides, which are then stored in fat cells. When isomaltase activity is inhibited, the breakdown of disaccharides into monosaccharides is suppressed, reducing the amount of easily absorbed monosaccharides, (3) suppressing the amount of sugar absorbed in the small intestine. Furthermore, the amount of glucose absorbed in the small intestine after a meal is reduced, (4) suppressing the rise in blood glucose levels. Suppressing the rise in glucose concentration inhibits the conversion of glucose to neutral fats by the action of insulin, (5) preventing or suppressing the accumulation of fat in the body (anti-obesity), and (6) reducing body fat. As body fat decreases, weight loss occurs, and (7) BMI also decreases.
[0049] Furthermore, the oral composition of the present invention can be suitably used for inhibiting lipase, α-glucosidase, or isomaltase, i.e., the oral composition of the present invention can be used as a lipase inhibitory composition, an α-glucosidase inhibitory composition, or an isomaltase inhibitory composition.
[0050] To ensure the anti-obesity effects, the fat absorption suppression effect, the neutral fat increase suppression effect, the sugar absorption suppression effect, the blood glucose increase suppression effect, the body fat reduction effect, and the BMI reduction effect, the oral composition of the present invention preferably contains 10 to 100 mg, more preferably 20 to 80 mg, of gallic acid per adult per day, and preferably contains 10 to 120 mg, more preferably 20 to 100 mg, of gallic acid and ellagic acid in total per adult per day.
[0051] When the oral composition of the present invention is an oral composition used for any of the functions (1) to (7) described above, it is not particularly limited as long as it contains gallic acid and ellagic acid, the mass ratio of gallic acid to ellagic acid is set within a specific range, and the product can be distinguished from other products in that it is used for any of the functions (1) to (7). For example, the scope of the present invention includes a product in which any of the functions (1) to (7) is indicated on the product itself, packaging, instructions, or promotional materials (advertising media). The oral composition used for any of the functions (1) to (7) of the present invention may indicate gallic acid as an active ingredient, but is not limited to products in which gallic acid is indicated as an active ingredient on the product packaging, etc. For example, the active ingredient may not be specified. Furthermore, even general foods that are manufactured and sold with a suggested use are also included within the scope of the present invention. For example, foods sold with personal testimonials from users mentioning the maintenance and / or improvement of any of the functions (1) to (7) listed on a website, etc., are also included within the scope of the present invention. The scope of the present invention also includes functional foods that use papers or the like showing the maintenance and / or improvement of any of the functions (1) to (7) as scientific evidence of their functionality, contain gallic acid as a functional component, and notify the functional claim related to any of the functions (1) to (7). As mentioned above, in the present invention, components other than gallic acid are supplementary components for enhancing the effects of gallic acid, and therefore are not generally listed as components involved in functional foods or foods for specified health uses that claim any of the functions (1) to (7). However, the oral compositions used for any of the functions (1) to (7) of the present invention do not exclude those that list supplementary components such as ellagic acid or chebulic acid as components involved, and functional foods, etc. that list ellagic acid, etc. as components involved are also included in the oral compositions.
[0052] As described above, oral compositions used for any of the functions (1) to (7) include foods and beverages labeled as having one or more functions selected from the group consisting of anti-obesity function, fat absorption suppression function, neutral fat increase suppression function, sugar absorption suppression function, blood glucose level increase suppression function, body fat reduction function, and BMI reduction function. The method of such labeling is preferably the following embodiment (1) or (2).
[0053] (1) A label indicating that a food or beverage is a functional food that has been notified to the Consumer Affairs Agency and that the business operator is responsible for displaying on the product packaging, based on scientific evidence, that the food or beverage has anti-obesity properties, fat absorption inhibitory properties, neutral fat increase inhibitory properties, sugar absorption inhibitory properties, blood sugar increase inhibitory properties, and body fat reduction properties and / or BMI reduction properties. (2) A statement that the food or beverage is a food for specified health uses that has been approved by the Consumer Affairs Agency to be labeled on the product package as having, based on scientific evidence, anti-obesity functions, fat absorption suppression functions, neutral fat increase suppression functions, sugar absorption suppression functions, blood sugar level increase suppression functions, and body fat reduction functions and / or BMI reduction functions.
[0054] For example, examples of the above (1) and (2) displays include displays that appeal to subjects who are concerned about body fat, such as those concerned about obesity, those concerned about their stomach area, those concerned about their weight, and those concerned about abdominal fat (visceral fat, subcutaneous fat, etc.); displays that indicate that the product will help lose weight, help reduce abdominal fat (visceral fat, subcutaneous fat, etc.), help reduce waist circumference, support obesity reduction, support dieting, make fat reduction easier, reduce fat absorption, and help reduce or inhibit the increase of body fat; and displays that indicate that the product will suppress the rise in blood glucose levels, suppress sugar absorption, moderate the rise in blood glucose levels, suppress the rise in postprandial blood glucose levels, moderate the rise in postprandial blood glucose levels, suppress triglyceride absorption, suppress the rise in triglycerides, moderate the rise in triglycerides, suppress the rise in postprandial triglycerides, suppress the absorption of sugars and fats contained in food, etc.
[0055] The present invention provides the following: <1> An oral composition comprising gallic acid and ellagic acid, An oral composition, wherein the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid=0.01 to 0.7. <2> The composition of the present invention is used for one or more purposes selected from the group consisting of anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of increase in blood sugar level, reduction of body fat, and reduction of BMI. <1> The oral composition according to claim 1. <3> The above-mentioned compound further containing chebulic acid. <1> or <2> The oral composition according to claim 1. <4> The above-mentioned compound further containing catechins. <1> ~ <3> 1. The oral composition according to claim 1 , wherein the oral composition is selected from the group consisting of: <5> The composition is used for one or more purposes selected from the group consisting of anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of increase in blood sugar level, reduction of body fat, and reduction of BMI. <1> ~ <4> 1. The oral composition according to claim 1 , wherein the oral composition is selected from the group consisting of: <6> The above-mentioned composition is for suppressing an increase in postprandial neutral fat or an increase in postprandial blood glucose level. <1> ~ <5> 1. The oral composition according to claim 1 , wherein the oral composition is selected from the group consisting of: <7> The above-mentioned agent is for inhibiting lipase or α-glucosidase. <1> ~ <5> 1. The oral composition according to claim 1 , wherein the oral composition is selected from the group consisting of: <8> An oral composition containing gallic acid as an active ingredient, It also contains ellagic acid, the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid=0.01 to 0.7; An oral composition used for one or more purposes selected from anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood sugar levels, reduction of body fat, and reduction of BMI. <9> A food or drink containing gallic acid as an active ingredient, It also contains ellagic acid, the mass ratio of gallic acid to ellagic acid in the food or drink is gallic acid:ellagic acid=1:0.01 to 0.7; Food and beverage products that are labeled as having one or more functions selected from the group consisting of anti-obesity function, fat absorption suppression function, neutral fat increase suppression function, sugar absorption suppression function, blood sugar level increase suppression function, body fat reduction function, and BMI reduction function. <10> The above is a functional food or a food for specified health uses. <9> The food and drink described in [Example]
[0056] The present invention will be described below based on examples. However, the present invention is not limited to the following examples. Unless otherwise specified, "parts" below represent "parts by mass" and "%" represents "% by mass".
[0057] In the examples and comparative examples, a gallic acid reagent (anhydrous, powdery, purity of about 100% by mass) was used as the gallic acid. An ellagic acid reagent (anhydrous, powdery, purity of about 98% by mass or more) was used as the ellagic acid. An anhydrous, powdery, purity of 98% by mass or more was used as the chebulic acid. A purified tea-derived catechin was used as the catechin. As the ascorbic acid, L(+)-sodium ascorbate was used, and as the erythorbic acid, sodium erythorbate (monohydrate) was used.
[0058] [Examples 1 to 9 and Comparative Examples 1 to 10] The test substances of Examples 1 to 9 and Comparative Examples 1 to 10 were prepared using the raw materials listed in Tables 1 and 2. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The amounts of the raw materials used are as shown in Tables 1 and 2.
[0059] The test substances of Examples 1 to 9 and Comparative Examples 1 to 10 were subjected to the following isomaltase inhibition test.
[0060] <Isomaltase inhibition test> (1) 100 mg of rat intestinal acetone powder (SIGMA) was mixed with 900 μL of 56 mM maleic acid buffer (pH 6.0) and homogenized to prepare a mixture. The mixture was centrifuged (3000 rpm, 10 minutes, 4°C) and the supernatant was collected. The collected supernatant was diluted 2-fold with 56 mM maleic acid buffer (pH 6.0) to prepare an enzyme solution. (2) A substrate solution was prepared by dissolving isomaltose in 56 mM maleic acid buffer (pH 6.0) to a concentration of 5 mM. (3) A test substance solution was prepared by dissolving the test substance in a 10% DMSO solution so that the total amount of the test substance was 0.32 mg / mL. (4) 15 μL of the enzyme solution was added to 15 μL of the test substance solution and pre-incubated at 37° C. for 5 minutes, after which 90 μL of the substrate solution was added and incubated at 37° C. for 30 minutes to allow the reaction to proceed. (5) After the reaction, the enzyme reaction was stopped by treating at 98°C for 2 minutes. (6) After the reaction was stopped, the absorbance at 505 nm was measured using Glucose Test Wako (manufactured by Wako Pure Chemical Industries, Ltd.) to determine the isomaltase inhibitory activity of the test substance. The measured value was designated as Measured Value A. (7) Except for using a 10% DMSO solution instead of the test substance solution, the procedure was the same as that for measuring the isomaltase inhibitory activity described above, and the absorbance of the test solution was measured to obtain a measurement value B. (8) The procedure for measuring the isomaltase inhibitory activity described above was repeated, except that an enzyme solution heat-inactivated by treatment at 98°C for 2 minutes was used instead of the enzyme solution, and the absorbance of the test solution was measured to obtain the measurement value C. (9) The procedure was the same as that for measuring activity described above, except that a 10% DMSO solution was used instead of the test substance solution and an enzyme solution heat-inactivated by treatment at 98°C for 2 minutes was used instead of the enzyme solution. The absorbance of the test solution was measured and the measurement value D was obtained. (10) The isomaltase inhibition rate (% of control) was calculated using the following formula (1) from the measured values A, B, C, and D. The results are shown in Tables 1 and 2. Isomaltase inhibition rate (% of control) = (measured value A - measured value C) / (measured value B - measured value D) × 100 (1)
[0061] [Table 1]
[0062] [Table 2]
[0063] As is clear from Tables 1 and 2, Examples 1 to 9, in which the ratio of gallic acid to ellagic acid was in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, had significantly higher isomaltase inhibition rates than Comparative Examples 1 to 6, in which each was used alone. As a result of this improved effect, the decomposition of disaccharides to monosaccharides is inhibited in the present invention, and it is expected that the effects of inhibiting sugar absorption, suppressing increases in blood glucose levels, preventing obesity, reducing body fat, and reducing BMI will be effectively achieved. Such excellent effects were not achieved in Comparative Examples 7 to 9, in which gallic acid was used in combination with an antioxidant component other than ellagic acid, or in Comparative Example 10, in which the gallic acid and ellagic acid contents were outside the ranges of the present invention. In particular, it can be seen that the isomaltase inhibition rate differs depending on the ratio of gallic acid to ellagic acid among Examples 1 to 6, and that there is a preferred range of gallic acid to ellagic acid for increasing the isomaltase inhibition rate.
[0064] Furthermore, in Examples 7 and 8, in which gallic acid, ellagic acid, and chebulic acid were used in combination, the mass ratio of ellagic acid to 1 part by mass of gallic acid was the same as in Examples 3 and 4, but the isomaltase inhibition rate was higher than that of Examples 3 and 4, which did not contain chebulic acid. Therefore, in Examples 7 and 8, it was found that the combination of gallic acid, ellagic acid, and chebulic acid significantly and effectively inhibits intestinal isomaltase activity. Therefore, it was suggested that this combination further suppresses the breakdown of disaccharides into monosaccharides in the intestinal tract, thereby even more significantly suppressing sugar absorption, suppressing increases in blood glucose levels, and providing anti-obesity, body fat reduction, and BMI reduction effects.
[0065] Furthermore, in Example 9, which used a combination of gallic acid and ellagic acid with chebulic acid and catechins, the mass ratio of ellagic acid and the mass ratio of chebulic acid to 1 part by mass of gallic acid were the same as in Example 7, but the isomaltase inhibition rate was even higher than in Example 7, which did not contain catechins. Therefore, it was suggested that this combination further suppresses the breakdown of disaccharides into monosaccharides in the intestinal tract, thereby even more significantly suppressing sugar absorption, suppressing increases in blood sugar levels, anti-obesity, reducing body fat, and reducing BMI.
[0066] [Examples 10 to 16 and Comparative Examples 11 to 20] Test substances in Examples 10 to 16 and Comparative Examples 11 to 20 were prepared using the raw materials listed in Tables 3 and 4. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The amounts of the raw materials used are as shown in Tables 3 and 4.
[0067] The test substances of Examples 10 to 16 and Comparative Examples 11 to 20 were subjected to the following lipase inhibition test.
[0068] <Lipase inhibitory activity test> Lipase inhibitory activity was measured according to the method of Lipase Kit S (Sumitomo Bakelite Co., Ltd.). Specifically, the lipase inhibitory activity of the test substance was measured according to the following procedure. The substrate of Lipase Kit S is known to be highly reactive with pancreatic lipase. (1) Porcine pancreatic lipase (Sigma) was dissolved in 0.01 M phosphate buffer (pH 7.0) to prepare a 0.3 mg / mL lipase solution. For the inhibition test, this 0.3 mg / mL lipase solution was diluted 5-fold with 0.01 M phosphate buffer (pH 7.0) to obtain a 0.06 mg / mL lipase solution. (2) A test substance solution was prepared by dissolving the test substance in Tris-HCl buffer (pH 8.55) containing 2.5% DMSO to a total test substance concentration of 0.264 mg / mL. (3) 6 μL of the test substance solution, 80 μL of the color-developing solution included in the kit, 10 μL of the lipase solution, and 1.6 μL of the esterase inhibitor solution were mixed and pre-incubated at 37°C for 5 minutes. After that, 8 μL of the substrate solution included in the kit was added and the mixture was further incubated at 37°C for 30 minutes. (4) Then, 160 μL of the reaction stop solution included in the kit was added to the mixture and mixed. After that, the absorbance at 412 nm was measured to determine the lipase inhibitory activity, and a measurement value A was obtained. (5) The procedure was the same as that of the above-mentioned lipase inhibitory activity measurement test, except that 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) was used instead of the test substance solution, and the absorbance of the test solution was measured to obtain measurement value B. (6) After the addition of the reaction stopping solution, the procedure was the same as that of the above-mentioned lipase inhibitory activity measurement test, except that the substrate solution was added, and the absorbance of the test solution was measured to obtain the measured value C. (7) The procedure was the same as that for the lipase inhibitory activity measurement test described above, except that 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) was used instead of the test substance solution, and the substrate solution was added after the addition of the reaction stop solution. The absorbance of the test solution was measured, and the measurement value D was obtained. (8) The lipase inhibition rate (% of control) was calculated using the following formula (2) from the measured values A, B, C, and D. The results are shown in Tables 3 and 4. Lipase inhibition rate (% of control) = (measured value A - measured value C) / (measured value B - measured value D) × 100 (2)
[0069] [Table 3]
[0070] [Table 4]
[0071] As is clear from Tables 3 and 4, Examples 10 to 16, in which the ratio of gallic acid to ellagic acid was in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, exhibited significantly improved lipase inhibition rates compared to Comparative Examples 11 to 16, in which the raw materials were used alone. As a result of this improved effect, the present invention inhibits the breakdown of triglycerides into fatty acids and glycerol, thereby suppressing fat absorption into the body, and is expected to improve the effects of inhibiting fat absorption, suppressing increases in triglyceride levels, anti-obesity, reducing body fat, and reducing BMI. Such excellent effects were not achieved in Comparative Examples 17 to 19, in which gallic acid was used in combination with an antioxidant component other than ellagic acid, or in Comparative Example 20, in which the gallic acid:ellagic acid content ratio was outside the range of the present invention. In particular, among Examples 10 to 15, the lipase inhibition rate differs depending on the ratio of gallic acid:ellagic acid, and it is clear that there is a preferred range of gallic acid:ellagic acid in order to increase the lipase inhibition rate.
[0072] In particular, Example 16, which used a combination of gallic acid, ellagic acid, and chebulic acid, had a mass ratio of ellagic acid to 1 part by mass of gallic acid equivalent to that of Example 12, but had a higher lipase inhibition rate than Example 12, which did not contain ellagic acid. This suggests that this combination exerts the above-mentioned effects more significantly.
[0073] [Examples 17 to 24] The raw materials were mixed according to the proportions shown in Table 5, and tablets (tablets to be swallowed) each weighing 250 mg and having a diameter of 8 mm were produced using a single punch tablet press. The compression force was 3 kN. Taking two tablets per day provided anti-obesity effects, inhibited fat absorption, inhibited the rise in neutral fat levels, inhibited sugar absorption, inhibited the rise in blood glucose levels, reduced body fat, and reduced BMI.
[0074] [Table 5]
Claims
1. An oral composition containing gallic acid and ellagic acid, the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid=1:0.1 to 0.2; Further, an oral composition containing chebulic acid.
2. The oral composition according to claim 1, which is used for one or more purposes selected from anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood glucose levels, reduction of body fat, and reduction of BMI.
Citation Information
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