Composition for SGLT inhibition

Abstract

To provide a composition capable of inhibiting SGLT.SOLUTION: The present invention provides a composition that comprises Garcinia and / or garcinol.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a composition for SGLT inhibition, which is characterized by containing garcinia. The present invention also relates to a composition for SGLT inhibition, which is characterized by containing garcinol.

Background Art

[0002] In recent years in Japan, it is said that the number of diabetic patients and those in the pre-diabetes group is on the increase. For the treatment and prevention of diabetes, appropriate control of blood glucose levels is important. Sodium-dependent glucose transporters (SGLT) expressed on the luminal membranes of epithelial cells in the small intestine and kidneys are involved in the absorption and reabsorption of glucose. SGLT is known to be classified into SGLT1, SGLT2, SGLT3, SGLT4, SGLT5, SGLT6, etc. according to the affinity for substrates and differences in gene sequences. Research on pharmaceuticals and foods targeting this SGLT has been conducted (Patent Document 1, Patent Document 2, etc.). However, since the compositions developed so far are not necessarily sufficiently effective, the development of new compositions with excellent SGLT inhibitory effects is required.

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0004] An object of the present invention is to provide a composition capable of inhibiting SGLT.

[0005] As a result of intensive studies to solve the above problems, the inventors surprisingly found that Garcinia has an excellent SGLT inhibitory effect. Further, as a result of intensive studies to solve the above problems, the inventors surprisingly found that garcinol has an excellent SGLT inhibitory effect. The present invention has been completed based on such findings.

[0006] The outline of the present invention is as follows. [1] A composition for inhibiting SGLT, characterized by containing Garcinia. [2] A composition for inhibiting SGLT, characterized by containing garcinol. [3] The composition for inhibiting SGLT according to [1] or [2], which is used for reducing body fat, reducing neutral fat, lowering blood cholesterol, increasing HDL cholesterol, lowering blood glucose level, lowering blood pressure, lowering uric acid level, and / or improving liver function. [Effects of the Invention]

[0007] The composition of the present invention exhibits an excellent SGLT inhibitory effect. [Brief Description of the Drawings]

[0008]

Figure 1

[0009] Hereinafter, the present invention will be described in detail. Note that the present invention is not limited to the following embodiments.

[0010] [Garcinia] The composition of the present invention is characterized by containing Garcinia. Garcinia is a general term for plants of the genus Garcinia in the family Clusiaceae (also known as the Garcinia genus). For example, Garcinia cambogia, Garcinia indica, Garcinia atroviridis, Garcinia mangostana, Garcinia subelliptica can be mentioned. From the point of being able to obtain higher effects, it is preferable to use Garcinia cambogia or Garcinia indica, and it is particularly preferable to use Garcinia indica.

[0011] The part of Garcinia used is not particularly limited, and leaves, fruits, and other parts can be preferably used in combination. However, from the point of being able to more effectively exert the effects of the present invention, fruits are preferable, and pulp and pericarp are particularly preferable.

[0012] In the present invention, the harvested Garcinia may be used as it is, or processed Garcinia (Garcinia processed product) may be used. When using processed Garcinia, for example, pulverized products such as powders and granules, juice extracts, and extracts can be used. The juice extract and extract may be in a liquid or slurry state, but it is preferable to use a dry powder. Among these, from the point of being able to more effectively exert the effects of the present invention, pulverized products and extracts are preferable, and extracts are particularly preferable. In the present invention, the extract includes the concept of the dry powder of the extract (the extract dried and powdered). The Garcinia processed product may be manufactured by a method commonly known to those skilled in the art, or may be a product currently on the market.

[0013] In the present invention, the Garcinia extract can include an extract solution, its dilution or concentrate, or their dry powder, etc. The solvent used for extraction can be, for example, water; lower alcohols such as methanol, ethanol, isopropanol, butanol; lower esters such as ethyl acetate, methyl acetate; acetone; mixed solvents of these with water, etc. Among these, polar solvents are preferred from the viewpoint of obtaining higher effects, water or ethanol or a mixture of water and ethanol is more preferred, and ethanol is most preferred.

[0014] When extracting with a polar solvent, the extraction method is not particularly limited, and continuous extraction, immersion extraction, countercurrent extraction, etc. can be suitably selected, and any apparatus can be used under room temperature to reflux heating. The extract can be concentrated and dried into a powder as needed. When the extract is made into a dry powder, an excipient can be blended as needed. In this specification, when the Garcinia extract contains an excipient, the content is the amount excluding the excipient.

[0015] [Garcinol] The composition of the present invention is characterized by containing garcinol. Garcinol is a kind of polyisoprenylated benzophenone derivative and is contained in plants of the genus Garcinia (also called the genus Garcinia) of the family Hypericaceae.

[0016] The garciniaol contained in the composition of the present invention may be a purified one, or a plant containing garciniaol may be used. However, from the viewpoint of safety in oral ingestion, it is preferable to use a plant containing garciniaol. As the plant containing garciniaol, it is preferable to use a plant of the genus Garcinia (also referred to as the genus Garcinia) of the family Clusiaceae. Garcinia cambogia, Garcinia indica, Garcinia atroviridis, Garcinia mangostana, and Garcinia subelliptica are more preferable. From the viewpoint of obtaining higher effects, it is even more preferable to use Garcinia cambogia or Garcinia indica, and it is particularly preferable to use Garcinia indica.

[0017] The amount of garciniaol in the oral composition of the present invention can be analyzed by HPLC. For example, it can be measured by an HPLC analyzer equipped with an ultraviolet absorption detector. The analytical column used is Unison UK-C18 HT 3μm φ3×150mm manufactured by Imtakt. As the liquid medium of the mobile phase, 0.1% acetic acid (mobile phase A) and acetonitrile (mobile phase B) are used. The column temperature can be 40°C and the flow rate can be 1.0 mL / min. The gradient conditions can be as follows.

[0018]

Table A

[0019] In addition to garcinia and garcinol, other components can be blended into the composition of the present invention as needed. Examples of other components include excipients, lubricants, dietary fibers such as water-soluble dietary fibers and insoluble dietary fibers, proteins, various vitamins and minerals, microorganisms such as algae and yeast, and the like. Furthermore, as needed, sweeteners, acidulants, dietary supplements, stabilizers, binders, brighteners, thickeners, colorants, diluents, emulsifiers, food additives, seasonings, etc., which are commonly used in the food field, can be mentioned. The content of these other components can be appropriately selected according to the form of the composition of the present invention and the like.

[0020] As described in the examples described later, the composition of the present invention exhibits an SGLT inhibitory effect. Examples of SGLT include SGLT1, SGLT2, SGLT3, SGLT4, SGLT5, SGLT6, etc., and it is not particularly limited. However, the composition of the present invention exhibits excellent inhibitory activity against SGLT1 and / or SGLT2, and particularly excellent inhibitory activity against SGLT2.

[0021] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, it excretes glucose, which is an energy source, as urine sugar, resulting in a significant calorie loss. Thereby, the energy balance becomes negative, and the decomposition of fat is enhanced, so that a body fat reduction effect can be expected.

[0022] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, it reduces the blood insulin level with the promotion of urine sugar excretion. Thereby, the promotion of fat decomposition, the reduction of fat cell size, and the reduction of fat mass occur in fat cells, so that a neutral fat reduction effect can be expected.

[0023] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, it reduces lipid accumulation in visceral fat, regulates serum lipoprotein levels, beneficially changes the ratio of LDL particles, reduces lipid oxidation, shifts substrate utilization to more efficient utilization of ketone bodies in myocardial metabolism, reduces reactive oxygen species generated by its oxidation, and affects β-oxidation and the transport of intracellular lipid molecules. Thereby, an increase in LDL cholesterol is suppressed, and a blood cholesterol-lowering effect can be expected.

[0024] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, insulin sensitivity is improved by enhancing lipolysis and attenuating systemic glucotoxicity, and by reducing the triglyceride concentration in the serum, an HDL cholesterol-increasing effect can be expected.

[0025] Since the composition of the present invention exhibits an SGLT1 inhibitory effect, it inhibits the function of SGLT1 present in the small intestine and suppresses gastrointestinal absorption of sugar, so a blood glucose-lowering effect can be expected. In addition, since the composition of the present invention exhibits an SGLT2 inhibitory effect, by suppressing the reabsorption of urinary glucose into the blood in the proximal renal tubule, excessive sugar in the primary urine cannot be completely reabsorbed into the body, and by promoting the excretion of a large amount of sugar into the urine, a blood glucose-lowering effect can be expected.

[0026] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, the reabsorption of water and sodium in the proximal renal tubule of the kidney decreases, natriuresis and osmotic diuresis occur, and the plasma volume and extracellular volume decrease, so a blood pressure-lowering effect can be expected.

[0027] Since the composition of the present invention exhibits an SGLT2 inhibitory effect, it increases the glucose concentration in the proximal renal tubule, and glucose competes with urate and the transporter GLUT9b, reducing the reabsorption of urate, so a uric acid-lowering effect can be expected.

[0028] Since the composition of the present invention has an SGLT2 inhibitory effect, it improves insulin resistance through the function of reducing blood glucose, decreases neutral fat in the liver, reduces lipotoxicity, suppresses inflammation and apoptosis, and is expected to have an effect of improving liver function such as a decrease in blood ALT, AST, and γ-GTP values, which are indicators of liver health status.

[0029] Since the composition of the present invention has an SGLT inhibitory effect, an effect of reducing body fat, reducing neutral fat, decreasing blood cholesterol, increasing HDL cholesterol, decreasing blood glucose level, decreasing blood pressure, decreasing uric acid level, and / or improving liver function can be expected by the mechanism described above. Therefore, the composition of the present invention can be used as a composition for reducing body fat, reducing neutral fat, decreasing blood cholesterol, increasing HDL cholesterol, decreasing blood glucose level, decreasing blood pressure, decreasing uric acid level, and / or improving liver function.

[0030] The composition of the present invention can be used as an oral composition such as a so-called health food such as pharmaceuticals (including quasi-drugs), foods for specified health use, foods with nutrient functions, functional foods with functional claims approved by a specified agency, etc.

[0031] The composition of the present invention can be used as a composition for SGLT inhibition. As such a composition for SGLT inhibition, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of SGLT inhibition. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that display the function of improving SGLT inhibition is included in the scope of the present invention.

[0032] Specifically, health foods displaying statements such as "inhibiting SGLT", "inhibiting SGLT1", "inhibiting SGLT2", "helping to reduce body fat by inhibiting SGLT", "helping to reduce BMI (body weight) by inhibiting SGLT", "helping to reduce waist circumference by inhibiting SGLT", "helping to reduce triglycerides by inhibiting SGLT", "lowering total cholesterol by inhibiting SGLT", "increasing HDL cholesterol by inhibiting SGLT", "lowering blood pressure by inhibiting SGLT", "suppressing an increase in blood glucose level by inhibiting SGLT", "suppressing an increase in blood glucose level by inhibiting SGLT", "lowering blood pressure by inhibiting SGLT", "lowering uric acid level by inhibiting SGLT", etc., or health foods displaying statements to the effect that they exhibit functions (such as body fat reduction) listed due to the SGLT inhibitory action can be exemplified. In addition, among foods with functional claims, those having scientific grounds for the function of SGLT inhibition are included.

[0033] The composition for inhibiting SGLT of the present invention may be labeled with garcinia and / or garcinol as the active ingredient, but is not limited to products whose packaging, etc., labels garcinia or garcinol as the active ingredient. For example, it may be one that does not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials referring to SGLT inhibition as personal impressions of the consumers who have ingested them described on a homepage, etc., are also included in the scope of the present invention.

[0034] The composition of the present invention can be used as a composition for reducing body fat. As a composition for reducing body fat, it contains garcinia and / or garcinol and can be distinguished from other products as a product in that it exhibits the function of reducing body fat. There is no particular limitation as long as it can be distinguished from other products, for example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that displays the function of reducing body fat is included in the scope of the present invention. In the present invention, reducing body fat is a concept that includes the prevention, treatment, and / or improvement of symptoms related to reducing body fat. For example, reducing body fat, suppressing body fat accumulation, suppressing body fat increase, anti-obesity, preventing obesity, improving obesity, and promoting weight loss are also included in reducing body fat.

[0035] Specifically, health foods that display "reduce weight", "reduce body fat", "reduce visceral fat", "reduce abdominal fat", "support the reduction of the waist circumference", "improve a high BMI", etc., or health foods that display that the functions listed have been reported can be exemplified. Also, among foods with functional claims, those that have scientific evidence for the function of reducing body fat are included.

[0036] The composition for reducing body fat of the present invention may display garcinia and / or garcinol as an active ingredient, but is not limited to those in which garcinia or garcinol is displayed as an active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials on a homepage, etc., that mention reducing body fat as the personal impression of the person who consumed them are also included in the scope of the present invention.

[0037] The composition of the present invention can be used as a composition for reducing neutral fat. As a composition for reducing neutral fat, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of reducing neutral fat. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that displays the function of reducing neutral fat is included in the scope of the present invention. In the present invention, reducing neutral fat is a concept including the prevention, treatment, and / or improvement of symptoms related to reducing neutral fat. For example, reducing neutral fat, suppressing neutral fat accumulation, suppressing neutral fat increase, preventing neutral fat increase, improving neutral fat, etc. are also included in reducing neutral fat.

[0038] Specifically, health foods that display "(blood) neutral fat lowering", "suppressing the rise of (blood) neutral fat after meals", etc., or health foods that display that the functions listed have been reported can be exemplified. In addition, among the foods with functional claims, those that have scientific basis for the function of reducing neutral fat are included.

[0039] The composition for reducing neutral fat of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials about reducing neutral fat described on a homepage, etc., as personal impressions of the people who have consumed them, are also included in the scope of the present invention.

[0040] The composition of the present invention can be used as a composition for reducing blood cholesterol. As a composition for reducing blood cholesterol, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exhibiting the function of reducing blood cholesterol. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that display the function of reducing blood cholesterol is included in the scope of the present invention. In the present invention, reducing blood cholesterol is a concept including prevention, treatment, and / or improvement of symptoms related to reducing blood cholesterol. For example, cholesterol reduction, suppression of cholesterol increase, suppression of cholesterol elevation, prevention of high cholesterol, improvement of high cholesterol, etc. are also included in reducing blood cholesterol.

[0041] Specifically, health foods that display "reducing total cholesterol", "suppressing the oxidation of LDL cholesterol (bad cholesterol) in the blood to oxidized LDL cholesterol", "reducing the LDL cholesterol value", "lowering the ratio (L / H ratio) of the LDL (bad) cholesterol value to the HDL (good) cholesterol value", etc., or health foods that display that the functions listed have been reported can be exemplified. Also, among foods with functional claims, those with scientific grounds for the function of reducing blood cholesterol are included.

[0042] The composition for reducing blood cholesterol of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials on a homepage, etc., that mention a reduction in blood cholesterol as a personal impression of the person who consumed them are also included in the scope of the present invention.

[0043] The composition of the present invention can be used as a composition for increasing HDL cholesterol. As a composition for increasing HDL cholesterol, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exhibiting the function of reducing HDL cholesterol. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that display the function of increasing HDL cholesterol is included in the scope of the present invention. In the present invention, increasing HDL cholesterol is a concept including the prevention, treatment, and / or improvement of symptoms related to increasing HDL cholesterol. For example, increasing HDL cholesterol, suppressing the decrease of HDL cholesterol, suppressing the increase of HDL cholesterol, preventing low HDL cholesterol, and improving low HDL cholesterol are also included in increasing HDL cholesterol.

[0044] Specifically, health foods displaying "increasing HDL (good) cholesterol" or "lowering the ratio (L / H ratio) of LDL (bad) cholesterol value to HDL (good) cholesterol value" and health foods displaying that the functions listed have been reported can be exemplified. Also, among foods with functional claims, those having scientific grounds for the function of increasing HDL cholesterol are included.

[0045] The composition for increasing HDL cholesterol of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials referring to an increase in HDL cholesterol as personal impressions of the consumers who have ingested them described on a homepage, etc. are also included in the scope of the present invention.

[0046] The composition of the present invention can be used as a composition for lowering blood glucose levels. As a composition for lowering blood glucose levels, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of lowering blood glucose levels. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that display the function of lowering blood glucose levels are included in the scope of the present invention. In the present invention, lowering blood glucose levels is a concept that includes the prevention, treatment, and / or improvement of symptoms related to lowering blood glucose levels. For example, blood glucose reduction, suppression of blood glucose increase, prevention of high blood glucose levels, and improvement of high blood glucose levels are also included in lowering blood glucose levels.

[0047] Specifically, health foods that display "suppressing the rise of postprandial blood glucose levels" or "lowering blood glucose levels (for those with higher blood glucose levels)" and health foods that display that the functions listed have been reported can be exemplified. Also, among foods with functional claims, those that have scientific evidence for the function of lowering blood glucose levels are included.

[0048] The composition for lowering blood glucose levels of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials on a homepage, etc., that mention a personal experience of lowering blood glucose levels as the personal impressions of the person who consumed them are also included in the scope of the present invention.

[0049] The composition of the present invention can be used as a composition for lowering blood pressure. As a composition for lowering blood pressure, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of lowering blood pressure. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that displays the function of lowering blood pressure is included in the scope of the present invention. In the present invention, lowering blood pressure is a concept that includes the prevention, treatment, and / or improvement of symptoms related to blood pressure reduction. For example, blood pressure drop, suppression of blood pressure increase, antihypertensive, prevention of hypertension, improvement of hypertension, etc. are also included in lowering blood pressure.

[0050] Specifically, health foods that display "lowering blood pressure (for those with higher blood pressure)" or the like, or health foods that display that the listed functions have been reported, can be exemplified. In addition, functional display foods that are based on the scientific basis of blood pressure reduction are included.

[0051] The composition for lowering blood pressure of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with suggestions of their uses are included in the scope of the present invention. For example, foods sold with testimonials on a homepage or the like that mention blood pressure reduction as the personal feelings of the person who consumed them are also included in the scope of the present invention.

[0052] The composition of the present invention can be used as a composition for reducing uric acid levels. As a composition for reducing uric acid levels, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of reducing uric acid levels. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that displays the function of reducing uric acid levels is included in the scope of the present invention. In the present invention, reducing uric acid levels is a concept that includes the prevention, treatment, and / or improvement of symptoms related to reducing uric acid levels. For example, reducing uric acid levels, suppressing an increase in uric acid levels, preventing hyperuricemia, and improving hyperuricemia are also included in reducing uric acid levels.

[0053] Specifically, health foods that display "suppressing the increase in postprandial uric acid levels" or "lowering the uric acid level (for those with higher uric acid levels)" and health foods that display that the functions listed have been reported can be exemplified. Also, among foods with functional claims, those with scientific evidence for the function of reducing uric acid levels are included.

[0054] The composition for reducing uric acid levels of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials on a homepage, etc., that mention a reduction in uric acid levels as the personal impressions of the person who consumed them are also included in the scope of the present invention.

[0055] The composition of the present invention can be used as a composition for improving liver function. As a composition for improving liver function, it contains garcinia and / or garcinol, and is not particularly limited as long as it can be distinguished from other products as a product in terms of exerting the function of improving liver function. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that displays the function of improving liver function is included in the scope of the present invention. In the present invention, improving liver function is a concept that includes prevention, treatment, and / or improvement of symptoms related to improving liver function. For example, improvement of liver function, decrease in ALT value, decrease in AST value, decrease in γ-GTP value, etc. are also included in improving liver function.

[0056] Specifically, health foods that display "lowering blood ALT value", "lowering blood AST value", "helping to lower γ-GTP value", "helping to lower the values of enzymes related to liver function (ALT, AST, γ-GTP)", etc., or health foods that display that the functions listed have been reported can be exemplified. Also, in functional display foods, those based on scientific evidence of improving liver function are included.

[0057] The composition for improving liver function of the present invention may display garcinia and / or garcinol as the active ingredient, but is not limited to those in which garcinia or garcinol is displayed as the active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with a suggested use are included in the scope of the present invention. For example, foods sold with testimonials on a homepage, etc., that mention improvement of liver function as the personal impressions of the consumers who have ingested them are also included in the scope of the present invention.

[0058] The composition of the present invention is not particularly limited as long as it is in a form suitable for oral use. For example, tablets, capsules, powders, granules, liquids, granular agents, rod-shaped agents, plate-shaped agents, block-shaped agents, solid-shaped agents, round-shaped agents, paste-shaped agents, cream-shaped agents, caplet-shaped agents, gel-shaped agents, chewable agents, stick-shaped agents, etc. can be mentioned. Among these, from the viewpoint of ease of taking, the forms of tablets, capsules, powders, granules, and liquids are preferred, and tablets, capsules, and granules are more preferred. Examples of oral compositions used as tablets, capsules, powders, granules, and liquids include supplements, food additives, container-packed beverages filled in PET bottles, cans, bottles, etc., and powder beverages to be dissolved in water (hot water), milk, fruit juice, etc. and drunk.

[0059] The content of Garcinia in the composition of the present invention may be appropriately contained within the range where its effects are exhibited. From the viewpoint of obtaining higher effects, in the solid content, 0.01% by mass or more is preferred, more preferably 0.1% by mass or more, and particularly preferably 1.0% by mass or more. Also, from the viewpoint of being easily continuously orally ingested in daily life, the content of Garcinia is preferably 90% by mass or less, more preferably 80% by mass or less, and particularly preferably 70% by mass or less in the solid content.

[0060] The content of garcinol in the composition of the present invention may be appropriately contained within the range where its effects are exhibited. From the viewpoint of obtaining higher effects, in the solid content, 0.0005% by mass or more is preferred, more preferably 0.005% by mass or more, and particularly preferably 0.05% by mass or more. Also, from the viewpoint of being easily continuously orally ingested in daily life, the content of garcinol is preferably 60% by mass or less, more preferably 50% by mass or less, and particularly preferably 40% by mass or less in the solid content.

[0061] Although the intake amount of Garcinia in the present invention is not particularly limited, from the viewpoint of obtaining higher effects, the intake amount of Garcinia is preferably 5 mg or more per day, more preferably 25 mg or more per day, and particularly preferably 50 mg or more per day. Also, from the viewpoint of being easily continuously orally ingested in daily life, the intake amount of Garcinia is preferably 5000 mg or less per day, more preferably 1000 mg or less per day, and particularly preferably 500 mg or less per day.

[0062] Although the intake amount of garcinol in the present invention is not particularly limited, from the viewpoint of obtaining higher effects, the intake amount of garcinol is preferably 1 mg or more per day, more preferably 5 mg or more per day, and particularly preferably 10 mg or more per day. Also, from the viewpoint of being easily continuously orally ingested in daily life, the intake amount of Garcinia is preferably 1000 mg or less per day, more preferably 200 mg or less per day, and particularly preferably 100 mg or less per day.

[0063] The composition of the present invention is not particularly limited with respect to the daily intake amount of Garcinia and / or garcinol. For example, it may be appropriately designed to achieve the above intake amount, and it may be a mode of ingesting the above intake amount at one time, or a mode of ingesting the above intake amount in multiple divided times. That is, for example, it can be contained as one day's amount in one container or divided into two to four containers.

[0064] The packaging form of the composition of the present invention is not particularly limited and can be appropriately selected according to the dosage form, etc. For example, blister packs such as PTP; strip packaging; heat sealing; aluminum pouches; film packaging using plastics or synthetic resins, etc.; glass containers such as vials; plastic containers such as ampoules, etc.

Examples

[0065] Hereinafter, the present invention will be described in more detail with reference to examples. However, the present invention is not limited to these examples, and the present invention can take various forms as long as the problems of the present invention can be solved.

[0066] Test 1. Evaluation of SGLT inhibitory effect To evaluate the SGLT inhibitory effect of garcinia or garcinol, the amount of 2-deoxy-D-glucose (hereinafter also referred to as 2-DG) uptake via SGLT2 was evaluated using human proximal tubular cell line (HK-2) by the test described below. SGLT2 is a protein called "sodium-glucose cotransporter" present in the renal tubules and plays a role in the reabsorption of sodium and glucose in the urine. It is known that two types of glucose transporters, SGLT2 and GLUT2, function in the human proximal tubular cell line (HK-2). SGLT2 requires sodium for glucose uptake, while GLUT2 does not require sodium. Therefore, the amount of 2-DG uptake via SGLT2 can be measured by subtracting the amount of 2-DG uptake in the absence of sodium (the amount of uptake via GLUT2) from the amount of 2-DG uptake in the presence of sodium (the amount of uptake via SGLT2 and GLUT2). The amount of 2-DG uptake via SGLT2 serves as an indicator of SGLT2 inhibition.

[0067] <Preparation of Test Substances> The details of the test substances are as follows. Garcinia: The part (pulp and peel) obtained by removing seeds from the fruit of Garcinia indica was dried and then extracted with ethanol at 70°C or higher for 6 hours or more. The obtained extract was filtered to remove impurities and concentrated. The concentrated extract was processed into a powder to obtain a powdered extract of Garcinia indica. When the extract was analyzed by HPLC, it contained 20% by mass of garcinol. Phlorizin (positive control): Commercially available phlorizin (manufactured by Tokyo Chemical Industry) was used as a reagent.

[0068] <Test Method> The human proximal tubular cell line (HK-2) was cultured in a growth medium (0.05 mg / mL Bovine Pituitary Extract (BPE) - 5 ng / mL Human EGF Recombinant Protein - Keratinocyte SFM).

[0069] The above cells were seeded in a 96-well plate at 100 μL / well to a density of 10,000 cells / well and pre-cultured in a 37°C, 5% CO2 incubator for 48 hours.

[0070] After removing the medium, the cells were washed three times with a Na+-free buffer (140 mM N-Methyl-D-glucamine, 5 mM KCl, 2.5 mM CaCl2, 1 mM MgSO4, 1 mM KH2PO4, and 10 mM HEPES (pH 7.4)). A Na+-free buffer or a Na+ buffer (140 mM NaCl, 5 mM KCl, 2.5 mM CaCl2, 1 mM MgSO4, 1 mM KH2PO4, and 10 mM HEPES (pH 7.4)) containing 200 μM 2-DG (manufactured by WAKO) and the test substance was added at 100 μL / well, and the cells were cultured in a 37°C, 5% CO2 incubator for 3 hours.

[0071] For the group to which Garcinia indica extract was added as the test substance (Example 1), the final concentration of Garcinia indica extract was 10 μg / mL. For the group to which phlorizin was added as a positive control (Reference Example 1), 100 μM phlorizin was used. For the control, a buffer without the test substance was used.

[0072] After culturing, the medium was removed, and the cells were washed three times with ice-cold Na+-free buffer to stop the glucose uptake reaction. The amount of 2-DG taken up into the cells was measured using a Glucose Cellular Uptake Assay Kit (Wide Range, Fluorometric Method) (manufactured by Cosmo Bio Co., Ltd.). The amount of 2-DG uptake in the Na+-free buffer (the amount of uptake in the absence of Na+) was subtracted from the amount of 2-DG uptake in the Na+ buffer (the amount of uptake in the presence of Na+) to calculate the amount of 2-DG uptake via SGLT2. Based on the obtained amount of 2-DG uptake via SGLT2, % of control (relative value with control set as 100%) was calculated, and SGLT2 inhibition was evaluated for Example 1 (Garcinia indica extract) and Reference Example 1 (phlorizin). The results are shown in Fig. 1.

[0073] <Test Results> In Fig. 1, for Example 1 (Garcinia indica extract), the amount of 2-DG uptake via SGLT2 decreased compared to the control and Reference Example 1 (phlorizin). From this, it was found that Garcinia indica has an SGLT2 inhibitory effect. Also, since garcinol is contained in the Garcinia indica extract, garcinol is considered to be effective for SGLT2 inhibition.

[0074] Therefore, by ingesting a composition containing Garcinia, an excellent SGLT inhibitory effect can be obtained, and thus, it can be expected to have effects such as body fat reduction, triglyceride reduction, blood cholesterol reduction, HDL cholesterol increase, blood glucose level reduction, blood pressure reduction, uric acid level reduction, and liver function improvement. Also, by ingesting a composition containing garcinol, an excellent SGLT inhibitory effect can be obtained, and thus, it can be expected to have effects such as body fat reduction, triglyceride reduction, blood cholesterol reduction, HDL cholesterol increase, blood glucose level reduction, blood pressure reduction, uric acid level reduction, and liver function improvement.

[0075] <Production Example> Based on the results of the examples, the production examples of the present invention are shown below.

[0076] [Production Examples 1 - 4: Granules] As per the formulation in Table 1, after mixing Garcinia with other raw materials, fluidized bed granulation was carried out using a granulator to produce the granules described in Production Examples 1-4. The granules described in Production Examples 1-4 may be dissolved in 100 ml of water or the like at 3 g per day for ingestion, or may be ingested as they are without dissolution. Any of the granules in Production Examples 1-4 is effective for SGLT inhibition, and it can be expected to have effects such as body fat reduction, neutral fat reduction, blood cholesterol reduction, HDL cholesterol increase, blood glucose level reduction, blood pressure reduction, uric acid level reduction, and liver function improvement.

[0077] [Table 1]

[0078] [Production Examples 5-8: Tablets] As per the formulation in Table 2, after mixing Garcinia with other raw materials, tableting was carried out using a rotary tableting machine to produce the tablets (250 mg) of Production Examples 5-8. The tablets described in Production Examples 5-8 may be ingested 1 to 2 tablets per day together with water or the like. Any of the tablets in Production Examples 5-8 is effective for SGLT inhibition, and it can be expected to have effects such as body fat reduction, neutral fat reduction, blood cholesterol reduction, HDL cholesterol increase, blood glucose level reduction, blood pressure reduction, uric acid level reduction, and liver function improvement.

[0079] [Table 2]

[0080] [Production Examples 9-12: Hard Capsules] As per the formulation in Table 3, Garcinia was mixed with other raw materials and encapsulated with a coating containing gelatin or hydroxypropyl cellulose to produce hard capsules (content volume: 300 mg). 1 to 2 capsules per day may be ingested together with water or the like. Any of the hard capsules in Production Examples 9-12 is effective for SGLT inhibition, and it can be expected to have effects such as body fat reduction, neutral fat reduction, blood cholesterol reduction, HDL cholesterol increase, blood glucose level reduction, blood pressure reduction, uric acid level reduction, and liver function improvement.

[0081]

Table 3

Industrial Applicability

[0082] Since the composition of the present invention enables SGLT inhibition and can be used as a health food or the like, it is industrially useful.

Claims

1. A composition for SGLT inhibition, characterized by containing Garcinia.

2. A composition for SGLT inhibition, characterized by containing garcinol.

3. The composition for SGLT inhibition according to claim 1 or 2, which is used for reducing body fat, reducing neutral fat, lowering blood cholesterol, increasing HDL cholesterol, lowering blood glucose level, lowering blood pressure, lowering uric acid level, and / or improving liver function.

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