Oral composition
An oral composition with garcinol and hydroxycitric acid in specific ratios addresses taste issues and enhances fat reduction and energy consumption, achieving effective anti-obesity effects.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- TOYO SHINYAKU KK
- Filing Date
- 2025-07-08
- Publication Date
- 2026-05-29
AI Technical Summary
Existing anti-obesity compositions often have unpleasant tastes and fail to meet the diverse preferences of consumers, and there is a need for effective oral compositions that can reduce body fat, visceral fat, and improve energy consumption.
An oral composition containing garcinol and hydroxycitric acid in specific mass ratios, optionally with isogarcinol, to enhance anti-obesity effects, body fat reduction, and improve energy consumption.
The composition effectively reduces body fat, visceral fat, suppresses fat accumulation, and enhances energy consumption by promoting lipolysis and fat burning, with improved efficacy when garcinol:hydroxycitric acid ratio is 1:0.01 to 10 and optionally with isogarcinol.
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Abstract
Description
Technical Field
[0001] The present invention relates to oral compositions and food and drink products.
Background Art
[0002] In recent years, in the lives of Japanese people, although the overall amount of physical activity has been showing a downward trend, the energy intake from food is relatively excessive, so there is concern about becoming obese. In the past, many people became obese due to aging, but in recent years, obese young people are also becoming prominent. Since obesity can lead to more serious diseases such as arteriosclerosis and cancer, it is required to prevent or improve obesity in daily diet.
[0003] Based on such needs, various anti-obesity compositions that can be easily ingested in daily life have been developed. For example, Patent Document 1 describes an anti-obesity composition containing lime algae and globin proteolysate as active ingredients. However, since globin proteolysate has a peculiar taste, there are consumers who dislike the taste. Also, because people's preferences vary widely, there are consumers who are not satisfied with existing anti-obesity compositions from viewpoints other than taste. Therefore, the development of new oral compositions showing an anti-obesity effect has been demanded.
Prior Art Documents
Patent Documents
[0004]
Patent Document 1
Summary of the Invention
Problems to be Solved by the Invention
[0005] The present invention aims to provide a novel oral composition that exhibits anti-obesity effects, body fat reduction effects, abdominal fat or visceral fat reduction effects, BMI reduction effects, blood triglyceride reduction or suppression of increase effects, blood cholesterol reduction effects, fat burning promotion effects, lipolysis promotion effects, energy consumption improvement effects, or fat accumulation suppression effects. [Means for solving the problem]
[0006] The inventors have discovered that by setting the mass ratio of garcinol to hydroxycitric acid within a specific range in a composition containing garcinol and hydroxycitric acid, an oral composition can be obtained that has excellent anti-obesity effects, effects for reducing body fat, reducing abdominal or visceral fat, reducing BMI, reducing or suppressing the rise of blood triglycerides, reducing blood cholesterol, promoting fat burning, promoting lipolysis, improving energy consumption, or suppressing fat accumulation.
[0007] In other words, the outline of the present invention is as follows: [1] An oral composition containing garcinol and hydroxycitric acid, An oral composition wherein the mass ratio of garcinol to hydroxycitric acid in the composition is garcinol:hydroxycitric acid = 1:0.01 to 10. [2] An oral composition according to claim 1, used for one or more purposes selected from among anti-obesity, reduction of body fat, reduction of abdominal fat or visceral fat, reduction of BMI, reduction or suppression of increase in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation. [3] The oral composition according to [1] or [2], further containing isogarcinol. [4] The oral composition according to [3], wherein the mass ratio of garcinol and isogarcinol is garcinol:isogarcinol = 1:0.01 to 10. [5] Food and beverages containing garcinol as an active ingredient, Furthermore, it contains hydroxycitric acid, The mass ratio of garcinol to hydroxycitric acid in the aforementioned food and beverage is garcinol:hydroxycitric acid = 1:0.01~10. Food and beverages that are labeled as having one or more functions selected from the following: anti-obesity, reduction of body fat, reduction of abdominal or visceral fat, reduction of BMI, reduction or suppression of increase in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation. [6] Food and beverages containing garcinol as an active ingredient, Furthermore, it contains hydroxycitric acid and isogarcinol, The mass ratio of garcinol to hydroxycitric acid in the aforementioned food and beverage is garcinol:hydroxycitric acid = 1:0.01~10. Food and beverages that are labeled as having one or more functions selected from the following: anti-obesity, reduction of body fat, reduction of abdominal or visceral fat, reduction of BMI, reduction or suppression of increase in blood triglycerides, reduction or suppression of increase in blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation. [7] The food and beverage described in [6], wherein the mass ratio of garcinol and isogarcinol is garcinol:isogarcinol = 1:0.01 to 10. [8] Foods and beverages described in any one of items [5] to [7] that are foods with functional claims or foods for specified health uses. [Effects of the Invention]
[0008] According to the present invention, it is possible to provide oral compositions containing garcinol and hydroxycitric acid, and in particular, oral compositions such as foods and beverages that are effective for anti-obesity, body fat reduction, abdominal fat or visceral fat reduction, BMI reduction, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, or suppression of fat cell maturation. [Modes for carrying out the invention]
[0009] The following describes preferred embodiments of the oral composition of the present invention. The oral composition of the present invention contains garcinol as an active ingredient and has functions related to anti-obesity, reduction of body fat, reduction of abdominal fat or visceral fat, reduction of BMI, reduction or suppression of increase in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation.
[0010] 1. Garcinol The garcinol used in this invention is a compound of polyisoprenylated benzophenone derivatives. Garcinol is known to have anti-obesity, body fat reduction, and abdominal fat or visceral fat reduction effects, and functions as an active ingredient in the composition of this invention. The garcinol used in this invention is not particularly limited as long as it can be used as a food or beverage, and plant-derived garcinol or synthetically obtained garcinol can be used. When plant-derived garcinol is used in the composition of this invention, plant extracts or pulverized powders may be used as the garcinol source, or purified products thereof may be used. As for plant extracts, extracts in which garcinol has been concentrated to increase its concentration may be used. In this application, plant extracts include both extracts obtained by extracting plants with a solvent and extracts obtained by juicing plants, and the concept includes extracts that have been dried and powdered. Also, in this application, pulverized plant powder refers to powder obtained by drying and pulverizing plants.
[0011] The content of gallocatechin in the oral composition of the present invention is not particularly limited. However, from the perspective of further enhancing the functions related to anti-obesity, body fat reduction, abdominal fat or visceral fat reduction, BMI reduction, reduction or increase suppression of blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of adipocyte maturation, it is preferably 0.0005 to 60 parts by mass, more preferably 0.005 to 50 parts by mass, still more preferably 0.05 to 40 parts by mass, particularly preferably 0.1 to 30 parts by mass, and most preferably 0.3 to 20 parts by mass in the solid content of the oral composition. In this specification, when the composition is in a solid state, the solid content refers to the content in the composition, and when the composition is in a liquid or fluid state, the solid content refers to the total amount of all components excluding water in the composition.
[0012] The content of gallocatechin in the composition of the present invention can be measured by the HPLC method. For example, it can be measured as follows using an HPLC analyzer (equipped with an ultraviolet absorption detector), an analytical column manufactured by Imtakt Corporation (Imtakt Unison UK-C18 HT 3μm φ3×150mm), and a membrane filter (0.45μm). Note that any device with equivalent functions can be substituted.
[0013] [Standard] Gallocatechin
[0014] [Reagents Used] Acetic acid (special grade), acetonitrile (for HPLC, special grade). Any reagent with equivalent purity can be substituted.
[0015] [Preparation of Standard Solution] Precisely weigh about 10 mg of the standard, dissolve it in acetonitrile, and prepare solutions with concentrations of 0.02, 0.04, and 0.2 mg / mL. The solutions filtered through a membrane filter are used as standard solutions. Note that appropriate treatment may be performed as necessary, such as removing impurities in the sample to conform to the separation ability of the device.
[0016] [Preparation of sample solution] If the sample to be measured is solid, the sample should be made homogenized by grinding it in a mortar and pestle, then approximately 50 mg should be accurately weighed out, acetonitrile should be added to make exactly 50 mL, and the solution should be filtered through a membrane filter to obtain the sample solution. If the sample is liquid, the amount should be adjusted appropriately according to the garcinol concentration in the sample, acetonitrile should be added to make exactly 50 mL, and the solution should be filtered through a membrane filter to obtain the sample solution.
[0017] [HPLC operating conditions] Analytical column: Imtakt Unison UK-C18 HT3μm φ3×150mm Column temperature: 40℃ Injection volume: 5μL Flow rate: 1.0mL / min Measurement wavelength: 350nm Mobile phase A: 0.1% aqueous acetic acid solution Mobile phase B: Acetonitrile
[0018] The gradient conditions are shown in Table 1.
[0019] [Table 1]
[0020] By analyzing under the above conditions, chromatograms of the standard solution and the sample solution are obtained. A calibration curve is created from the garcinol peak area and concentration of the standard solution, and the garcinol concentration (mg / mL) in the sample solution is determined from the calibration curve, thereby measuring the garcinol content in the composition.
[0021] 2. Hydroxycitric acid The composition of the present invention contains hydroxycitric acid. Hydroxycitric acid is a derivative of citric acid and is a compound having a hydroxylated structure at position 1. The hydroxycitric acid used in the present invention is not particularly limited as long as it can be used as a food or beverage, and plant-derived hydroxycitric acid or synthetically obtained hydroxycitric acid can be used. When plant-derived hydroxycitric acid is used in the composition of the present invention, plant extracts or powders may be used as the source of hydroxycitric acid, or purified products thereof may be used. Furthermore, the hydroxycitric acid used in the present invention may be in the form of a salt. When a salt of hydroxycitric acid is used in the present invention, for example, calcium hydroxycitrate can be mentioned. Note that when a salt is used as hydroxycitric acid in the present invention, the amount of hydroxycitric acid is the amount in terms of hydroxycitric acid equivalent.
[0022] In this invention, the inventors consider hydroxycitric acid to be an auxiliary component that enhances the effects of garcinol. In order for the effects of both components to be exerted, the mass ratio of garcinol to hydroxycitric acid in the composition of this invention must be garcinol:hydroxycitric acid = 1:0.01 to 10. As shown in the examples described later, in this invention, by including garcinol and hydroxycitric acid in an oral composition in a specific mass ratio, the functions of anti-obesity, reduction of body fat, reduction of abdominal fat or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation can be effectively enhanced.
[0023] In the composition of the present invention, the mass ratio of garcinol to hydroxycitric acid is not particularly limited as long as garcinol:hydroxycitric acid = 1:0.01 to 10. However, from the viewpoint of further enhancing the effects of the present invention, the lower limit of the mass of hydroxycitric acid per 1 part by mass of garcinol is preferably 0.02 parts by mass or more, more preferably 0.03 parts by mass or more, even more preferably 0.05 parts by mass or more, particularly preferably 0.08 parts by mass or more, and most preferably 0.1 parts by mass or more. Furthermore, from the viewpoint of further enhancing the effects of the present invention, the upper limit of the mass of hydroxycitric acid per 1 part by mass of garcinol is preferably 9 parts by mass or less, more preferably 5 parts by mass or less, even more preferably 3 parts by mass or less, particularly preferably 1 part by mass or less, and most preferably 0.5 parts by mass or less.
[0024] The content of hydroxycitric acid in the oral composition of the present invention is not particularly limited, but from the viewpoint of further enhancing the functions related to anti-obesity, reduction of body fat, reduction of abdominal fat or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation, the content of hydroxycitric acid in the solid content of the oral composition is preferably 0.0005 to 30 parts by mass, more preferably 0.001 to 25 parts by mass, even more preferably 0.005 to 20 parts by mass, particularly preferably 0.01 to 15 parts by mass, and most preferably 0.05 to 10 parts by mass.
[0025] The hydroxycitric acid content in the composition of the present invention can be measured by HPLC. For example, it can be measured as follows using an HPLC analyzer (with ultraviolet absorption detector), an analytical column manufactured by Showa Denko K.K. (Shorex RSpak KC-811 x 2, φ8.0 mm x 300 mm), and a membrane filter (0.45 μm). Note that any instrument with equivalent functionality can be substituted.
[0026] [Standard product] (―)―Calcium hydroxycitric acid salt standard
[0027] [Preparation of standard solutions] After weighing a fixed amount of the standard, dissolve it in 5% perchloric acid to prepare solutions with concentrations of 0.5, 0.2, and 0.01 mg / mL. These solutions are filtered through a membrane filter and used as standard solutions. If necessary, the samples may be treated to remove impurities or otherwise adjust them to suit the separation capabilities of the instrument.
[0028] [Preparation of sample solution] The sample is ground in a mill, approximately 200 mg is precisely weighed out, 10 mL of 1 mol / L sodium hydroxide solution is added and mixed, and the mixture is heated. After cooling, 10 mL of 1 mol / L hydrochloric acid and 20 mL of 5% perchloric acid are added and mixed, then the mixture is diluted to exactly 200 mL with water, filtered through a membrane filter, and this is the sample solution.
[0029] [HPLC operating conditions] Analytical column: Shorex RSpak KC-811 x 2, φ8.0mm x 300mm Column temperature: 40℃ Injection volume: 20μL Flow rate: 1.0mL / min Measurement wavelength: 220nm Mobile phase: 3mmol·L perchloric acid
[0030] By analyzing under the above conditions, chromatograms of the standard solution and the sample solution are obtained. A calibration curve is created from the peak height and concentration of the standard solution, and the hydroxycitric acid concentration (mg / mL) in the sample solution is determined from the calibration curve, thereby measuring the hydroxycitric acid content in the composition.
[0031] 3. Isogarcinol The oral composition of the present invention is more preferably further containing isogarcinol, from the viewpoint of further enhancing its functions related to anti-obesity, reduction of body fat, reduction of abdominal or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of adipocyte maturation. Isogarcinol is a compound of polyisoprenylated benzophenone. The isogarcinol used in the present invention is not particularly limited as long as it can be used as a food or beverage, and plant-derived isogarcinol or isogarcinol obtained by synthesis can be used. When plant-derived isogarcinol is used in the composition of the present invention, plant extracts or pulverized powders may be used as the isogarcinol source, or purified products thereof may be used.
[0032] When the oral composition of the present invention contains isogarcinol, there is no particular lower limit to the amount of isogarcinol per 1 part by mass of garcinol. However, from the viewpoint of further enhancing the effects of the present invention, it is preferable that the amount be 0.01 parts by mass or more (garcinol:isogarcinol = 1:0.01 or more), more preferably 0.02 parts by mass or more, even more preferably 0.03 parts by mass or more, particularly preferably 0.04 parts by mass or more, and most preferably 0.05 parts by mass or more. Similarly, there is no particular upper limit to the amount of isogarcinol per 1 part by mass of garcinol. However, from the viewpoint of further enhancing the effects of the present invention, it is preferable that the amount be 10 parts by mass or less (garcinol:isogarcinol = 1:10 or less), more preferably 5 parts by mass or less, even more preferably 3 parts by mass or less, particularly preferably 1 part by mass or less, and most preferably 0.5 parts by mass or less.
[0033] When the oral composition of the present invention contains isogarcinol, the amount of isogarcinol in the oral composition is not particularly limited. However, from the viewpoint of further enhancing the functions related to anti-obesity, reduction of body fat, reduction of abdominal fat or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation, the amount of isogarcinol in the solid content of the oral composition is preferably 0.0005 to 25 parts by mass, more preferably 0.001 to 20 parts by mass, even more preferably 0.005 to 15 parts by mass, particularly preferably 0.01 to 10 parts by mass, and most preferably 0.03 to 7 parts by mass.
[0034] The isogarcinol content in the composition of the present invention can be measured by HPLC. For example, it can be measured as follows using an HPLC analyzer (with ultraviolet absorption detector), an analytical column manufactured by Imtakt Corporation (Imtakt Unison UK-C18 HT3μm φ3×150mm), and a membrane filter (0.45μm). Note that any instrument with equivalent functionality can be substituted.
[0035] [Standard product] Isogarcinol
[0036] [Reagents used] Acetic acid (special grade), acetonitrile (HPLC grade). For reagents, any equivalent purity product can be used as a substitute.
[0037] [Preparation of standard solutions] After accurately weighing approximately 1 mg of the standard, dissolve it in acetonitrile to prepare solutions with concentrations of 0.02, 0.04 mg / mL, and 0.04 mg / mL. These solutions are then filtered through a membrane filter to obtain the standard solutions. If necessary, the samples may be treated to remove impurities or otherwise adjust them to suit the separation capabilities of the instrument.
[0038] [Preparation of sample solution] If the sample to be measured is solid, the sample should be made homogenized by grinding it in a mortar and pestle, then approximately 30 mg should be accurately weighed out, acetonitrile should be added to make exactly 50 mL, and the solution should be filtered through a membrane filter to obtain the sample solution. If the sample is liquid, the amount should be adjusted appropriately according to the isogarcinol concentration in the sample, acetonitrile should be added to make exactly 50 mL, and the solution should be filtered through a membrane filter to obtain the sample solution.
[0039] [HPLC operating conditions] Analytical column: Imtakt Unison UK-C18 HT3μm φ3×150mm Column temperature: 40℃ Injection volume: 5μL Flow rate: 1.0mL / min Measurement wavelength: 278nm Mobile phase A: 0.1% aqueous acetic acid solution Mobile phase B: Acetonitrile
[0040] The gradient conditions are shown in Table 2.
[0041] [Table 2]
[0042] By analyzing under the above conditions, chromatograms of the standard solution and the sample solution are obtained. A calibration curve is created from the isogarcinol peak area and concentration of the standard solution, and the isogarcinol concentration (mg / mL) in the sample solution is determined from the calibration curve, thereby measuring the isogarcinol content in the composition.
[0043] 4. Oral Composition The oral composition of the present invention may contain other components besides garcinol, hydroxycitric acid, and isogarcinol. Examples of such other components include sugars, vitamins, minerals, proteins, dietary fiber such as insoluble dietary fiber, plants or plant products, and yeast. Furthermore, it may contain, if necessary, sweeteners, acidulants, colorants, thickeners, glazing agents, lubricants, excipients, anticaking agents, nutritional supplements, binders, lubricants, stabilizers, diluents, bulking agents, emulsifiers, food additives, seasonings, and the like, which are commonly used in the food industry.
[0044] Examples of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, granular preparations, rod-shaped preparations, plate-shaped preparations, block-shaped preparations, solid preparations, round preparations, paste-like preparations, cream-like preparations, caplet-like preparations, gel-like preparations, chewable preparations, stick-shaped preparations, and the like. Among these forms, tablets, capsules, powders, granules, and liquid preparations are preferred from the viewpoint of ease of administration.
[0045] The oral composition of the present invention can take the form of a pharmaceutical product (including quasi-drugs) or a food or beverage. Among these, a food or beverage is particularly preferred because it can be easily consumed in daily life.
[0046] Examples of foods and beverages of the present invention include general foods, nutritional functional foods, functional foods whose efficacy has been approved by a designated institution, and so-called health foods such as foods for specified health uses. Foods that display efficacy are sometimes collectively referred to as "health functional foods" or "functional foods." When the oral composition of the present invention is a food or beverage, it is particularly preferable that it be a functional food or a food for specified health uses, from the viewpoint of being able to communicate the effects of the present invention to consumers.
[0047] The present invention does not particularly limit the food and beverages, but examples include: milk and dairy products; beverages such as soft drinks, fruit juices, milk beverages, alcoholic beverages, sports drinks, and nutritional drinks; seasonings; alcoholic beverages; processed agricultural and forestry products; confectionery and bread; flour and noodles; processed marine products; processed livestock products; oils and fats; frozen prepared foods; retort foods; instant foods; food ingredients; and supplements. Examples of supplement forms include tablets, capsules, powders, granules, and liquids.
[0048] 5. Oral compositions used for anti-obesity and other purposes. As shown in the examples described below, the oral composition of the present invention suppresses fat accumulation in adipocytes. Therefore, the oral composition of the present invention is suitably used for one or more of the following purposes: (1) anti-obesity, (2) reduction of body fat, (3) reduction of visceral fat or internal abdominal fat, (4) reduction of BMI (Body Mass Index), (5) reduction or suppression of increase in blood triglycerides, (6) reduction of blood cholesterol, (7) promotion of lipolysis, (8) promotion of fat burning, (9) improvement of energy consumption, (10) suppression of fat accumulation, and (11) suppression of adipocyte maturation. Therefore, the compositions of the present invention can be used as (1) an anti-obesity composition, (2) a body fat reduction composition, (3) a abdominal fat or visceral fat reduction composition, (4) a BMI (Body Mass Index) reduction composition, (5) a blood triglyceride reduction or suppression of increase composition, (6) a blood cholesterol reduction composition, (7) a lipolysis promotion composition, (8) a fat burning promotion composition, (9) an energy consumption improvement composition, (10) a fat accumulation suppression composition, and (11) an adipocyte maturation suppression composition.
[0049] In the present invention, (1) "anti-obesity" encompasses the effect of suppressing (maintaining) the increase in body weight or body fat and the effect of reducing body weight or body fat, and is a concept that encompasses not only the effect on patients with obesity as a disease, but also the effect of suppressing or reducing the increase in body weight and body fat in overweight individuals, as well as diet and slimming effects for cosmetic purposes.
[0050] In this application, "body fat" refers to fat in the body and is a general term for visceral fat and subcutaneous fat. In other words, in this invention, (2) "body fat reduction" means the action of reducing the amount of body fat (visceral fat or subcutaneous fat; abdominal fat and total abdominal fat are also included in body fat).
[0051] In the present invention, (3) "reduction of abdominal fat or visceral fat" means the effect of reducing the amount of abdominal fat or visceral fat.
[0052] In the present invention, (4) "reduction of BMI" means reducing the value of BMI.
[0053] In the present invention, (5) "reduction or suppression of the rise in blood triglycerides" means reducing the concentration of triglycerides in the blood when fasting or after a meal, or suppressing the rise in triglycerides.
[0054] In the present invention, (6) "reduction of blood cholesterol" means reducing the concentration of cholesterol in the blood.
[0055] In the present invention, (7) "fat breakdown promotion" means promoting the breakdown of fat (triglycerides) in the body.
[0056] In the present invention, (8) "fat burning promotion" means promoting metabolism that breaks down fat (triglycerides) in the body and converts it into energy for consumption.
[0057] In the present invention, (9) "improvement of energy consumption" means improving the amount of energy consumed in the body by burning fat or sugar in the body.
[0058] In the present invention, (10) "inhibition of fat accumulation" means the suppression of fat accumulation in the body.
[0059] In the present invention, (11) "inhibition of fat cell maturation" means inhibiting the maturation of fat cells in the body.
[0060] The mechanism by which functions (1) to (11) are performed is as follows: As described later, the composition of the present invention has the effect of (10) suppressing the accumulation of fat in adipocytes. Therefore, it exhibits the effects of (1) anti-obesity, (2) reduction of body fat, (3) reduction of abdominal fat or visceral fat, and (4) reduction of BMI. Furthermore, tests described later have confirmed that the composition of the present invention suppresses the accumulation of lipid droplets (an indicator of fat content). Since lipid droplets are composed of neutral fats (triglycerides) and cholesterol esters, the composition of the present invention also exhibits effects such as (5) reduction or suppression of the rise of blood neutral fats and (6) reduction of blood cholesterol.
[0061] Furthermore, the mechanism of fat accumulation suppression is thought to be due to fatty acids produced by the breakdown of fat in adipocytes being transported to other tissues via blood vessels and consumed as an energy source (Takashi Ohsumi, Fat Metabolism and its Regulation - Energy Balance of the Body -, Research Introduction Materials, University of Hyogo, 2008 University Open Lecture; URL: https: / / www.sci.u-hyogo.ac.jp / life / molbio / KOKAI.pdf). For this reason, the fat accumulation suppression effect is considered an indicator of the promotion of fat breakdown, and for example, in Japanese Patent Publication No. 7428430 (Iwase Cosfa Co., Ltd.), the fat breakdown promoting effect is evaluated by a confirmation test of fat accumulation suppression. Accordingly, the composition of the present invention suppresses fat accumulation in adipocytes, thereby exhibiting effects such as (7) promotion of fat breakdown, (8) promotion of fat burning, and (9) improvement of energy consumption. Furthermore, after differentiation from stem cells and progenitor cells, adipocytes accumulate fat within the cell to become mature adipocytes (Teruo Kawada, Obesity and Lifestyle-Related Diseases: The Merits and Demerits of Adipocytes; Micronutrient Research 22, 2005: pp. 1-5, URL: https: / / www.jstage.jst.go.jp / article / jtnrs / 22 / 0 / 22_1 / _pdf). Therefore, if fat accumulation is inhibited, they cannot mature. Accordingly, the composition of the present invention also exhibits the effect of (11) inhibiting the maturation of adipocytes.
[0062] From the viewpoint of enhancing functions related to anti-obesity, reduction of body fat, reduction of abdominal or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of fat cell maturation, the oral composition of the present invention preferably contains 1 to 1000 mg of garcinol per adult per day, more preferably 5 to 200 mg, and most preferably 10 to 100 mg.
[0063] If the oral composition of the present invention is an oral composition used for any of the functions (1) to (11) described above, it is not particularly limited as long as it contains garcinol and hydroxycitric acid in a specific mass ratio and is distinguishable from other products in that it is used for any of the functions (1) to (11). For example, if any of the functions (1) to (11) are displayed on the product itself, packaging, instructions, or promotional materials (advertising media), it is included within the scope of the present invention. The oral composition used for any of the functions (1) to (11) of the present invention may display garcinol as the active ingredient, but is not limited to products in which garcinol is displayed as the active ingredient on the product packaging, etc. For example, it may not specify an active ingredient. Furthermore, even general foods are included within the scope of the present invention if they are manufactured and sold with the use of (1) to (11) in mind. For example, foods sold with testimonials on a website, etc., that mention the maintenance and / or improvement of any of the functions (1) to (11) as personal impressions of people who have consumed them are also included within the scope of the present invention. Furthermore, the scope of this invention also includes functional foods in which garcinol is the functionally active ingredient, and which use papers or other documents demonstrating the maintenance and / or improvement of any of the functions (1) to (11) as the scientific basis for functionality, and which have a function related to any of (1) to (11) as the notified function. As stated above, in this invention, ingredients other than garcinol are auxiliary ingredients to enhance the effect of garcinol, and therefore are not usually listed as active ingredients in functional foods or foods for specified health uses that display any of the functions (1) to (11). However, the oral composition used for any of the functions (1) to (11) in this invention does not exclude those in which auxiliary ingredients such as hydroxycitric acid or isogarcinol are listed as active ingredients, and functional foods that display hydroxycitric acid, etc. as active ingredients are also included in this oral composition.
[0064] As described above, oral compositions used for any of the functions (1) to (11) include foods and beverages that display a claim that they have one or more functions selected from among anti-obesity, body fat reduction, abdominal fat and visceral fat reduction, BMI reduction, blood triglyceride reduction and suppression of increase, blood cholesterol reduction, fat burning promotion, energy consumption improvement, and fat accumulation suppression. It is particularly preferable that such foods and beverages be foods with functional claims or foods for specified health uses.
[0065] Foods and beverages that display a claim to have one or more functions selected from (1) to (11) include, for example, foods and beverages that make claims that appeal to people who are concerned about obesity or body fat, such as "for those who are overweight," "for those who are concerned about obesity," "for those who are concerned about their waistline," "for those who are concerned about their weight," "for those who are concerned about abdominal fat (visceral fat and subcutaneous fat, etc.)," "for those who are concerned about their BMI," etc., as well as foods and beverages that make claims that help to reduce weight, help to reduce body fat, help to reduce abdominal fat (visceral fat, subcutaneous fat, total abdominal fat, etc.), help to reduce waist circumference, help to lower BMI, help to resolve obesity, make it easier to reduce fat, help to diet, make it easier to lose weight This includes foods and beverages that display claims to have specific functions, such as supporting weight loss, supporting the reduction of body fat, supporting the reduction of abdominal fat (visceral fat, subcutaneous fat, total abdominal fat, etc.), supporting the reduction of waist circumference, supporting a decrease in BMI, supporting weight loss, supporting fat reduction, supporting dieting, helping to reduce blood triglycerides, suppressing the rise in blood triglycerides, helping to reduce blood cholesterol, making it easier to burn fat, promoting fat burning, making it easier to consume energy, promoting energy consumption, making it harder to accumulate fat, and suppressing fat accumulation. [Examples]
[0066] 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 refers to "parts by mass" and "%" refers to "percentage by mass".
[0067] 1. Evaluation of fat accumulation suppression The suppression of fat accumulation in adipocytes was evaluated using the method described below.
[0068] 1-(1) Obtaining the test substance The following substances were used as test materials, as listed in Tables 3 and 4. • Garcinol: Commercially available reagent-grade garcinol (purity 95% or higher) was used. • Hydroxycitric acid: Commercially available reagent-grade hydroxycitric acid (purity 98% or higher) was used. • Isogarcinol: Commercially available reagent-grade isogarcinol (purity 95% or higher) was used.
[0069] 1-(2). Evaluation test for the suppression of fat accumulation Using the above-mentioned test substance, a cell test was conducted to evaluate the suppression of fat accumulation according to the following procedures (a) to (g). (a) 75 cm³ in a 37°C, 5V %CO2 incubator 2 Mouse fibroblasts 3T3-L1 were cultured in a flask in DMEM medium containing 10% (v / v) FBS. (b) 3T3-L1 was suspended by trypsin treatment and 75 cm 2 2 x 10⁶ wells of a collagen-coated 96-well plate are transferred from the flask to each well. 4 Cells were seeded at a cell density of cells / well and cultured in DMEM medium containing 10% (v / v) FBS in a 37°C, 5V %CO2 incubator until confluence. (c) Next, the culture medium was replaced with differentiation induction medium containing the test sample of the example or comparative example (control was cultured in differentiation induction medium only), and the samples were cultured for 2 days to induce differentiation. As the differentiation induction medium, 10% (v / v) FBS-containing DMEM medium containing 0.5 mM isobutylmethylxanthine, 0.5 μM dexamethasone, and 10 μg / mL insulin was used. For each test sample, the total amount of the test substance was prepared in the differentiation induction medium to reach the predetermined concentration (1 μg / mL). Tables 3 and 4 show the mass percentage of the test substance in each test sample. (d) The culture medium was replaced from the differentiation induction medium to the differentiation maintenance medium containing the test sample (the control was cultured in differentiation maintenance medium only), and the samples were incubated for 5 days. As the differentiation maintenance medium, 10% (v / v) FBS-containing DMEM medium containing 10 μg / mL insulin was used. For each test sample, the total amount of the test substance was prepared in the differentiation maintenance medium to reach the predetermined concentration (1 μg / mL). Tables 3 and 4 show the mass percentage of the test substance in each test sample. After culturing in (e)(d), the supernatant was removed and 10% (v / v) formalin solution was added to fix the cells. (f) Lipid droplets generated by oil red staining were stained, and the absorbance of the extract was measured (520 nm and 650 nm). As a blank, wells without cells were similarly stained with oil red. The protein content of each well was calculated using the Pierce™ BCA Protein Assay kit (Thermo Fisher Scientific). (g) The amount of fat accumulation per unit of protein was calculated using the formula below, and the relative values to the control are shown in Tables 3 and 4. A smaller relative value indicates that fat accumulation in adipocytes is suppressed. <Expression 1> Relative value of fat accumulation (%) = [[(Abs520 sample - Abs520 blank) - (Abs650 sample - Abs650 blank) ] / (Protein sample)] / [(Abs520 control - Abs520 blank) - (Abs650 control - Abs650 blank) ] / (Protein control)]] × 100 (%) Abs520 sample, Abs650 sample: Absorbance of each example or comparative example at 520nm and 650nm. Abs520 control, Abs650 control: Absorbance of the control at 520nm and 650nm. Abs520 blank, Abs650 blank: Absorbance of the blank at 520nm and 650nm. Protein sample: Protein content in cells in each example or comparative example. Protein control: Protein levels in cells under control.
[0070] Furthermore, the rate of fat accumulation suppression was calculated using the following formula. The results are shown in Tables 3 and 4. <Expression 2> Fat accumulation suppression rate (%) = 100 - Relative value of fat accumulation
[0071] [Table 3]
[0072] [Table 4]
[0073] 1-(3).Results The results are shown in Tables 3 and 4. Although garcinol alone (Comparative Example 1) showed a fat accumulation inhibitory effect, the effect was not very high. Furthermore, no fat accumulation inhibitory effect was observed with hydroxycitric acid alone (Comparative Example 2) or isogarcinol alone (Comparative Example 3). Therefore, it was expected that the effect of combining garcinol and hydroxycitric acid would be lower than that of garcinol alone. Surprisingly, however, compositions with a mass ratio of garcinol to hydroxycitric acid of garcinol:hydroxycitric acid = 1:0.01 to 10 (Examples 1 to 7) showed a significant improvement in fat accumulation inhibitory effect compared to garcinol alone (Comparative Example 1). In particular, compositions with a mass ratio of garcinol:hydroxycitric acid = 1:0.05 to 1 (Examples 2 to 5) showed particularly excellent effects. From this, it was found that the effect of garcinol can be enhanced by setting the mass ratio of garcinol to hydroxycitric acid in the composition to the range of garcinol:hydroxycitric acid = 1:0.01 to 10. Furthermore, when the mass ratio of hydroxycitric acid to garcinol exceeded 1:10, the effect was not significantly improved compared to garcinol alone (Comparative Example 1) (Comparative Examples 4 and 5). Furthermore, compositions containing garcinol and hydroxycitric acid in a predetermined mass ratio, and also containing isogarcinol (Examples 8-13), showed a further improvement in the effect of suppressing fat accumulation compared to compositions containing garcinol and hydroxycitric acid in a predetermined mass ratio but without isogarcinol (Examples 1-7).
[0074] 2. Tablets of the present invention Each raw material was mixed according to the proportions shown in Tables 5 and 6, and tablets (swallowing tablets) of Examples 14-43, each containing 250 mg and having a tablet diameter of 8 mm, were manufactured using a single-shot tablet press. The compression pressure was set to 3 kN. The resulting tablets, when taken at a rate of 2 tablets per day, exhibited the following effects: anti-obesity, reduction of body fat, reduction of abdominal or visceral fat, reduction of BMI, reduction or suppression of rise in blood triglycerides, reduction of blood cholesterol, promotion of lipolysis, promotion of fat burning, improvement of energy consumption, suppression of fat accumulation, and suppression of adipocyte maturation.
[0075] [Table 5]
[0076] [Table 6]
Claims
[Claim 1] The invention described in the specification.