CN115052591A - Anti-obesity composition and oral composition - Google Patents

Anti-obesity composition and oral composition Download PDF

Info

Publication number
CN115052591A
CN115052591A CN202180012480.1A CN202180012480A CN115052591A CN 115052591 A CN115052591 A CN 115052591A CN 202180012480 A CN202180012480 A CN 202180012480A CN 115052591 A CN115052591 A CN 115052591A
Authority
CN
China
Prior art keywords
composition
promoting
tectorigenin
pinitol
fat
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202180012480.1A
Other languages
Chinese (zh)
Inventor
中岛千绘
森川琢海
神谷智康
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Toyo Shinyaku Co Ltd
Original Assignee
Toyo Shinyaku Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Toyo Shinyaku Co Ltd filed Critical Toyo Shinyaku Co Ltd
Priority claimed from PCT/JP2021/003384 external-priority patent/WO2021255979A1/en
Publication of CN115052591A publication Critical patent/CN115052591A/en
Pending legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/075Ethers or acetals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Polymers & Plastics (AREA)
  • Mycology (AREA)
  • Nutrition Science (AREA)
  • Botany (AREA)
  • Food Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention addresses the problem of providing an anti-obesity composition and an oral composition that can promote the gene expression of proteins such as PGC1 alpha and UCP1 that are involved in brown adipocytes or their energy-wasting effects, and that have an effect of promoting the energy-wasting effect in brown adipocytes. The composition of the present invention contains tectorigenin and pinitol. The tectorigenin is preferably tectorigenin. The composition of the present invention is preferably used as an anti-obesity composition and an oral composition.

Description

Anti-obesity composition and oral composition
Technical Field
The present invention relates to compositions for anti-obesity, body fat reduction, fat metabolism promotion, fat burning promotion, thermogenesis promotion, energy consumption promotion, and oral administration. In addition, the present invention relates to the use of tectorigenins and pinitol for the manufacture of a functional food product for the improvement of obesity, the reduction of body fat, the promotion of fat metabolism, the promotion of fat burning, the promotion of thermogenesis or the promotion of energy expenditure. In addition, the present invention relates to a method for ameliorating obesity, reducing body fat, promoting fat metabolism, promoting fat burning, promoting thermogenesis, or promoting energy expenditure using a composition comprising tectorigenins and pinitol.
Background
Obesity is largely related to the consumption of fat in the body, which is specifically formed by the following mechanism.
When a fat-mobilizing hormone such as norepinephrine is secreted, hormone-sensitive lipase, which is a lipolytic enzyme, is activated in white adipocytes distributed subcutaneously or in internal organs, and triglycerides (neutral fats) accumulated in the white adipocytes are decomposed to become glycerol and free fatty acids and are released into the blood. Free fatty acids released into the blood are taken up into mitochondria of brown adipocytes distributed around the clavicle, around the chest, the shoulder, and the like, in addition to the liver and muscle, and are consumed as heat. In this way, white adipocytes play a role in accumulating extra energy in the body in the form of fat, while brown adipocytes play a role in burning fat and generating heat.
As one of candidate molecules involved in autonomous regulation of energy expenditure, UCP1 and PGC1 α are known.
UCP has the function of decoupling oxidative phosphorylation reactions in the inner mitochondrial membrane and dissipating energy in the form of heat. As UCP1, which is the most representative of brown cell fat, the following facts are known: 1. the function of UCP1 was decreased in obese animals, 2. UCP1 was not increased in animals that were obese even if eaten more, 3. mice with decreased UCP1 gene expression were artificially made fat, and mice with high expression were made thin. Further, PGC1 α is known to have an action of activating UCP1 and promoting mitochondrial proliferation by β adrenergic receptor stimulation of brown adipocytes (non-patent document 1).
Therefore, if UCP1 or PGC1 α is activated, an anti-obesity effect can be expected, and thus, a drug or food excellent in activation of UCP1 or PGC1 α has been searched for.
On the other hand, conventionally, various anti-obesity agents are known as a technique for reducing white adipose tissue such as subcutaneous fat, including patent document 1.
Documents of the prior art
Patent document
Patent document 1: japanese patent laid-open publication No. 2017-171654
Patent document 2: japanese patent laid-open publication No. 2009-196931
Non-patent document
Non-patent document 1: japanese society of Japanese medical science シンポジウム J.The Japan society of Japan "Yeast" Japan society of Japan "Japan society of Japan, 2003, p 62-70
Disclosure of Invention
An action of consuming energy such as fatty acids in brown adipocytes to generate heat (hereinafter also referred to as "energy-consuming action") is important for lipid metabolism, but if this action can be activated, it is expected that more fat in the body is converted into heat and an anti-obesity action is obtained more effectively.
However, in each of the above-mentioned prior arts, the effect of promoting energy expenditure in brown adipocytes has not been studied yet.
Further, the present inventors have conducted studies and found that conventional anti-obesity agents which are considered to be capable of reducing white adipose tissues individually are not sufficient in terms of promoting the energy expenditure effect in brown adipocytes.
The present inventors have intensively studied the constitution of a composition capable of promoting the energy expenditure effect in brown adipocytes by studying the gene expression of proteins such as PGC1 α and UCP1, which are involved in the energy expenditure effect in brown adipocytes. As a result, it has been found that by combining specific components, expression of these genes can be surprisingly promoted, and the above-mentioned excellent effect of promoting energy consumption can be obtained.
The present invention has been made in view of the above-mentioned findings, and provides an anti-obesity composition containing tectorigenin and pinitol.
Disclosed is a composition for reducing body fat or promoting fat metabolism, which contains tectorigenins and pinitol.
Disclosed is a composition for promoting fat burning, promoting thermogenesis or promoting energy consumption, which contains tectorigenins and pinitol.
The present invention also provides an oral composition containing tectorigenin and pinitol.
Further, the present invention provides the use of tectorigenin and pinitol for the manufacture of a functional food product for the improvement of obesity, the reduction of body fat, the promotion of fat metabolism, the promotion of fat burning, the promotion of thermogenesis or the promotion of energy expenditure.
Further, the present invention provides a method for ameliorating obesity, reducing body fat, promoting fat metabolism, promoting fat burning, promoting thermogenesis, or promoting energy expenditure, using a composition containing tectorigenins and pinitol.
Effects of the invention
The present invention can provide a useful oral composition containing a composition containing tectorigenins and pinitol, and in particular, can provide an anti-obesity composition, a body fat reducing composition, a fat metabolism promoting composition, a fat burning promoting composition, a thermogenesis promoting composition, and an energy consumption promoting composition that are effective in promoting gene expression of proteins such as PGC1 α and UCP1 that are involved in the energy consumption action in brown adipocytes and promoting the energy consumption action in brown adipocytes. Further, it is also possible to provide an oral composition which has an effect of promoting energy consumption in brown adipocytes through the aforementioned effect of promoting expression of the genes of PGC1 α and UCP1, and is effective in resisting various effects of obesity, body fat reduction, promotion of fat metabolism, promotion of fat burning, promotion of thermogenesis, and promotion of energy consumption. The present invention also provides a use of a composition containing tectorigenins and pinitol, which can promote the expression of PGC1 α and UCP1 genes, can promote energy consumption in brown adipocytes, and is effective for ameliorating obesity, and a method for ameliorating obesity using tectorigenins and pinitol as active ingredients.
Drawings
FIG. 1 is a graph showing the expression level of PGC1 alpha gene in examples and comparative examples.
FIG. 2 is a graph showing the expression level of UCP1 gene in examples and comparative examples.
Detailed Description
The present invention will be described in more detail below with reference to embodiments of the present invention, but the present invention is not limited to these embodiments. Hereinafter, the anti-obesity composition, the body fat reducing composition, the fat metabolism promoting composition, the fat burning promoting composition, the thermogenesis promoting composition, the energy consumption promoting composition, and the oral composition of the present invention are collectively referred to as "the composition of the present invention".
(tectorigenins)
Tectorigenin is tectorigenin, tectorigenin glycoside and their derivatives.
Tectorigenin is one of flavonoids existing in plants of Iridaceae, and is represented by formula C 16 H 12 O 6 This is also referred to as 5, 7-dihydroxy-3- (4-hydroxyphenyl) -6-methoxy-4H-1-benzofuran-4-one or 6-methoxy-5, 7-dihydroxy-3- (4-hydroxyphenyl) -4H-1-benzofuran-4-one. In the present specification, the term "tectorigenin" refers to a compound in such an aglycone form. Tectorigenin has the following chemical formula.
[ chemical formula 1 ]
Figure BDA0003779245630000041
Tectorigenin glycoside in the present invention refers to a compound obtained by binding 1 or 2 or more kinds of sugars and/or sugar acids selected from monosaccharides to tectorigenin. The monosaccharide is preferably a pentose or hexose, more preferably 1 or 2 or more selected from glucose, xylose, mannose, fructose, sorbose, galactose, apiose and rhamnose, and particularly preferably 1 or 2 selected from glucose and xylose. The sugar acid is preferably an uronic acid, and particularly preferably glucuronic acid or galacturonic acid. In glycosides, these sugars and/or sugar acids are generally bonded to the hydroxyl group at the 4' and/or 7 position of tectorigenin. In the present invention, a glycoside bonded to the hydroxyl group at the 7-position is preferable. The number of sugars and/or sugar acids (also referred to as the number of sugar and/or sugar acid bonds) in tectorigenin glycoside is, for example, 1 or more and 5 or less, preferably 1 or more and 4 or less, and particularly preferably 1 or more and 3 or less. The amount of sugar and/or sugar acid refers to the total number of sugar and/or sugar acid. Here, when n sugars are bonded to tectorigenin, the structure may be a linked body in which n sugars are bonded, or the total number of sugars bonded to different sites of tectorigenin may be n. The same applies to the case where the glycoside comprises a sugar acid.
Examples of the tectorigenin or glycoside derivative thereof include compounds obtained by substituting 1 or 2 or more hydrogen atoms in tectorigenin or glycoside thereof with a substituent. Examples of such a substituent include an amino group, a sulfonic acid group, an alkyl group having 1 to 6 carbon atoms, and an alkoxy group having 1 to 4 carbon atoms. The number of the substituents in tectorigenin is preferably 8 or less, more preferably 4 or less, most preferably 0.
In the composition of the present invention, as the tectorigenins, only 1 kind of the tectorigenins, glycosides thereof, and derivatives thereof may be used, or a mixture of 2 or more kinds of them may be used. In particular, in the composition of the present invention, it is preferable that the tectorigenin is tectorigenin and/or a glycoside thereof from the viewpoint of an anti-obesity effect. In particular, it is preferable that the composition of the present invention contains tectorigenin as the tectorigenins from the viewpoint of excellent effect of promoting energy consumption in brown adipocytes and easy availability. In the composition of the present invention, tectorigenin may be an organic synthetic product or may be extracted from plants or the like.
(pinitol)
Pinitol is also known as 3-O-methyl-D-chiro-inositol, a species of inositol. Pinitol is contained in plants such as carob bean and clover. In the composition of the present invention, pinitol may be an organic synthetic product or may be extracted from plants or the like.
In the present invention, when the content ratio of tectorigenin to pinitol is within a specific range, the gene expression of PGC1 α and UCP1 is excellent, and the energy-consuming effect in brown adipocytes is higher, and therefore, this is preferable. In order to enhance the energy expenditure effect in brown adipocytes, the content ratio of tectorigenins to pinitol is preferably, in terms of mass ratio, tectorigenins: pinitol is 1: 0.01 or more and 50 or less, more preferably 1: 0.05 or more and 30 or less, and particularly preferably 1: 0.1 to 26 inclusive. For the same reason, when tectorigenin is contained as tectorigenin, the content ratio of tectorigenin to pinitol is preferably tectorigenin: pinitol is 1: 0.01 to 50 inclusive, and particularly 1: more than 0.5 and 30 or less, more preferably 1: 0.7 or more and 30 or less, and most preferably 1: 1 to 26 inclusive.
The determination of the amount of tectorigenins in the composition of the invention may be performed by high performance liquid chromatography (HPLC method).
For example, the following may be set: as a liquid medium for the mobile phase, an acetonitrile/water/acetic acid mixture (mobile phase A volume ratio of 15: 85: 0.1 and mobile phase B volume ratio of 35: 65: 0.1), a column temperature of 35 ℃ and a flow rate of 1.0 ml/min were used, and YMC-Pack ODS AM12S05-2546WT (φ 4.6X 250mm) manufactured by YMC.
The gradient conditions can be as shown in table a below.
TABLE A
Time (minutes) Solution A (%) B liquid (%)
0 100 0
50 0 100
55 0 100
57 100 0
70 100 0
The amount of pinitol in the composition of the present invention can be determined by HPLC method.
For example, the following may be set: as a column, InertSustain NH2(3 μm,. phi.3X 250mM) manufactured by GL Sciences corporation was used, and as a liquid medium of a mobile phase, 1mM hydrochloric acid/acetonitrile for chromatography (volume ratio: 30/70) was used, the column temperature was 40 ℃ and the flow rate was 0.5 ml/min.
The composition of the present invention may contain other components that are generally used, in addition to the tectorigenins and pinitol, within a range that does not impair the effects of the present invention. Examples of such components include various excipients, binders, gloss agents, lubricants, stabilizers, diluents, extenders, thickeners, emulsifiers, antioxidants, pH adjusters, colorants, flavors, additives, and the like. The content of the other components may be appropriately selected depending on the form of the composition of the present invention.
The composition of the present invention can be used for any oral or parenteral use. Examples of the non-oral preparation include a preparation to be administered by a method of directly administering to the stomach using a catheter or the like. However, the composition of the present invention is preferably orally administered from the viewpoint of easily obtaining the effect of the present invention for promoting energy consumption.
When the oral preparation is used, examples of the form include tablets, capsules, powders, granules, liquids, granules, rods, tablets, blocks, solid preparations, pellets, pastes, creams, capsules, gels, chews, and rods. Among them, the form of tablets, capsules, powders, granules and liquids is particularly preferable. Examples of the oral composition used in the form of tablets, capsules, powders, granules, or liquids include nutritional supplements; food additive: packaged beverage filled in plastic bottles, cans, bottles, and the like: it can be dissolved in water (hot water), milk, fruit juice, etc. for drinking. They are preferable in that they can be easily eaten and the like and can improve the palatability.
In addition, specific examples of the oral composition of the present invention may include food as a dietary composition. The food may be various foods such as tea bags, bread-snacks, and noodles, and cooked foods. Examples of bread-snacks include bread such as staple bread, sweet bread, French bread, English bread, muffin, steamed bread, doughnut, and waffle; cake products such as cream cake, sponge cake, chiffon cake, and thin pancake; frozen dessert such as chocolate, ice cream, and ice sucker, jelly, cookie, etc. The noodles include udon noodles, plain noodles, and the like. The cooked food may be curry, stew, miso soup, vegetable soup, or their materials, seasonings, etc.
The composition of the present invention contains 0.001 mass% to 40 mass% of pinitol and tectorigenin in total in the solid content, and is preferably contained in an amount of 0.005 mass% to 35 mass%, more preferably 0.01 mass% to 30 mass%, from the viewpoint of an effect of promoting energy consumption in brown adipocytes and from the viewpoint of easy and continuous oral intake in daily life. The solid content means the amount of water removed from the composition.
In the case of oral ingestion of the composition of the present invention, the total amount of pinitol and tectorigenin administered orally is preferably about 0.1mg to 500mg, more preferably 0.5mg to 300mg per 1 day for an adult, from the viewpoint of promoting energy consumption in brown adipocytes and from the viewpoint of easy and sustained oral ingestion in daily life. The amount of the composition of the present invention taken 1 time is preferably about 1mg to 300mg per 1 day for an adult based on the total amount of the pinitol and the tectorigenins.
Specific examples of the mode of use of the composition of the present invention include so-called health foods such as pharmaceuticals (including therapeutic cosmetics), general foods, nutritional functional foods, specific health foods for which the therapeutic effect is confirmed by a predetermined institution, and functional display foods. Foods that exhibit therapeutic effects are sometimes collectively referred to as "functional foods".
As shown in examples described later, the composition of the present invention can promote energy expenditure in brown adipocytes and brown adipose tissue containing the same by promoting gene expression of a plurality of proteins involved in energy expenditure in brown adipocytes. Examples of such a gene include the PGC1 α gene and the UCP1 gene.
The protein PGC1 α (PPAR γ coactivator 1 α) encoded by the PGC1 α gene is a protein identified as a transcription cofactor that activates transcription based on the nuclear receptor PPAR γ. PGC1 α activates the transcription factor NRF (nuclear respiratory factor) 1/NRF2, which promotes transcription of TFAM (mitochondrial transcription factor), thereby activating mitochondrial biosynthesis. It is known that mitochondria are increased by promoting the gene expression of PGC1 α. In addition, PGC1 α is a factor that binds to nuclear receptors of brown adipocytes, and is involved in promoting the expression of UCP1 gene. Therefore, by promoting the gene expression of PGC1 α, an energy consumption promoting effect and the like can be expected through a mitochondrial increasing effect in brown adipocytes and a UCP1 gene expression promoting effect. The gene for PGC1 α was also designated Pgc1 α in some cases.
The UCP1 gene is a gene encoding molecular uncoupling protein 1 (UCP 1), and may be referred to as Ucp 1. In brown adipocytes, the UCP1 gene is specifically expressed in mitochondria of the cells. The UCP1 gene has an activity of uncoupling oxidative phosphorylation in mitochondria, and when it is activated, energy generated by oxidative decomposition of fatty acid or glucose is directly converted into heat without being diverted to ATP synthesis and dissipated. By promoting the expression of UCP1 gene, the consumption of fatty acid in brown fat cells can be promoted, and obesity can be inhibited or eliminated.
The effect of the present invention may be an effect of promoting the expression of only one of the PGC1 α gene and UCP1 gene, or an effect of promoting the expression of both of the PGC1 α gene and UCP1 gene. The composition of the present invention can be used for various purposes such as promotion of fat burning, promotion of thermogenesis, promotion of fat metabolism, reduction of body fat, and promotion of energy consumption, in addition to the use of the expression of the PGC1 α gene and UCP1 gene. The fat burning promoter is an action of promoting brown fat cells to convert fatty acids into heat. The thermogenesis promotion means, for example, promoting generation of heat from neutral fat by brown adipocytes. The fat metabolism promoting action is, for example, an action of qualitatively transforming fat cells or adipose tissues which are in an obese state into small normal fat cells, or a fatty acid metabolism action by brown fat cells. The body fat reducing effect is an effect of reducing body fat by, for example, turning fatty acid into heat. In addition, the anti-obesity use refers to an action of reducing body fat or inhibiting an increase in body fat, for example, by promoting the metabolism of fatty acids in brown adipocytes, brown adipose tissue. The energy consumption-promoting action is, for example, an action of promoting brown adipocytes to consume chemical energy such as fatty acids. These effects are mediated by activation of PGC1 α and UCP1 in brown adipocytes.
In the present invention, the position of the brown adipocytes includes, in addition to liver and muscle, the vicinity of the clavicle, the chest (around the chest), the shoulder (the scapula and its periphery), and the like.
The composition of the present invention may be used for purposes such as promotion of lipolysis, anti-obesity, and diet as long as it can be distinguished from other products, and for example, the term "having a lipolysis promoting function" means the following: examples of the expression of the present invention include an expression called for a subject of body fat, such as a subject with obesity, a subject with abdominal attention, a subject with body weight, and a subject with abdominal fat (visceral fat, subcutaneous fat, and the like), and an expression of the present invention is helpful for reducing body fat, such as helping to reduce body weight, helping to reduce abdominal fat (visceral fat, subcutaneous fat, and the like), helping to reduce waist diameter, supporting obesity elimination, supporting dieting, making fat easily consumed, making fat easily burned, helping fat consumption, helping fat burning, promoting lipolysis, making fat easily decomposed, and helping lipolysis.
Examples
The present invention will be described in more detail below with reference to examples. However, the scope of the present invention is not limited to these examples. In the following description, unless otherwise specified, "%" and "parts" represent% by mass and parts by mass, respectively.
Measurement of PGC1 alpha Gene expression level
Example 1 and comparative examples 1 and 2
(1) Tectorigenin (manufactured by tokyo chemical industries) was used as a test substance. D-pinitol (manufactured by Tokyo chemical industry) was used as pinitol.
(2) As the growth medium, a growth medium was used; as the differentiation induction medium, a differentiation induction medium was used; as the differentiation maintenance medium, an adipocyte maintenance medium was used. The medium of brown adipocyte culture kit F-8 (rat) (manufactured by Cosmo Bio, and derived from interscapular brown adipose tissue) was used for all of the 3 media. Among them, brown adipocytes derived from interscapular brown adipose tissue are frequently used in the study of brown adipocyte function associated with fat burning.
(3) The differentiation induction medium containing the test substance was prepared as follows. Specifically, each test substance was dissolved in DMSO, diluted with a differentiation induction medium, prepared so that the final DMSO concentration became 0.5 vol%, and filter-sterilized. After sterilization, tectorigenin and pinitol were diluted to the concentrations shown in table 1 below using differentiation induction medium containing 0.5 vol% DMSO.
(4) The differentiation-maintaining medium containing the test substance was prepared as follows. Specifically, each test substance was dissolved in DMSO, diluted with a differentiation-maintaining medium, prepared so that the final DMSO concentration became 0.5 vol%, and filter-sterilized. After sterilization, tectorigenin and pinitol were diluted to the concentrations shown in table 1 below using differentiation maintenance medium containing 0.5 vol% DMSO.
(5) Rat brown adipose precursor cells (manufactured by Cosmo Bio) were grown to 3.0X 10 using a growth medium 4 cells/well, 500. mu.l/well into collagen-coated 24-well plates at 37 ℃, 5 (vol/vol)% CO 2 Culturing in an incubator until the cell density reaches about 90 percent.
(6) After removing the medium, 500. mu.L/well of a differentiation-inducing medium containing the test substance was added thereto at 37 ℃ and 5 (vol/vol)% CO 2 The cells were cultured in an incubator for 48 hours to induce differentiation into brown adipocytes.
(7) After removing the medium, 500. mu.L/well of a differentiation maintenance medium containing the test substance was added thereto at 37 ℃ and 5 (vol/vol)% CO 2 Culturing in an incubator for 72 hours.
(8) After removing the medium, 500. mu.L/well of a differentiation maintenance medium containing the test substance was added thereto at 37 ℃ and 5 (vol/vol)% CO 2 The culture was further carried out in the incubator for 72 hours.
(9) After removing the medium, the medium was washed 2 times with PBS, RNA was recovered using RNeasy Mini Kit (QIAGEN), and cDNA was synthesized using Revert raAce (R) qPCR RT Master Mix (TOYOBO).
(10) The obtained cDNA was used as a template, and quantitative real-time PCR was carried out using a PGC 1. alpha. gene primer (QIAGEN) using QuantiNova SYBR Green PCR Kit (QIAGEN), to measure the mRNA gene expression level of PGC 1. alpha. The relative values of the expression levels of the mRNA gene of PGC1 α in example 1 and comparative examples 1 and 2 are shown in fig. 1, where the value of comparative example 1 is 1.
TABLE 1
Figure BDA0003779245630000101
Measurement of the expression level of UCP1 Gene
Examples 2 to 4 and comparative examples 3 and 4
A primer of UCP1 gene (QIAGEN) was used in place of Pgc1 α. In addition, as the test substance, a test substance having a composition described in table 2 below was used. The concentration of the test substance in the differentiation-inducing medium and the differentiation-maintaining medium was 50. mu.M. Except for this point, the amount of UCP1 mRNA gene expression was measured in the same manner as in [ example 1 and comparative examples 1 and 2 ]. The relative values of the expression levels of the mRNA genes of UCP1 in examples 2 to 4 and comparative examples 3 and 4 are shown in FIG. 2, where the value of comparative example 3 is 1.
TABLE 2
Figure BDA0003779245630000111
As shown in fig. 1 and 2, when the brown adipocytes were induced and maintained for differentiation in the presence of the composition of the present invention containing tectorigenin and pinitol in combination, the expression levels of PGC1 α gene and UCP1 gene were much higher than when tectorigenin and pinitol were used alone. In particular, a synergistic expression promoting effect was exhibited by using tectorigenin and pinitol in combination with the UCP1 gene, which plays an important role in energy consumption.
Therefore, it is found that the composition of the present invention exhibits an excellent effect of promoting energy consumption in brown adipocytes, and is excellent as an anti-obesity agent.
Granules (3000 mg per 1 pack) were prepared from the following ingredients. The obtained granules were suspended in water and ingested 2 times per day, 1 pack per 1 time, to obtain an excellent anti-obesity effect.
TABLE 3
Figure BDA0003779245630000121
Granules (2000 mg per 1 pack) were prepared from the following ingredients. The obtained granules were suspended in hot water for ingestion 3 times per day, 1 pack per 1 time, and excellent anti-obesity effects were obtained.
TABLE 4
Figure BDA0003779245630000122
Tablets (200 mg per 1 tablet) were prepared from the following ingredients. The obtained tablet can be ingested 2 times per 1 day, 4 tablets per 1 time, and excellent anti-obesity effect can be obtained.
TABLE 5
Figure BDA0003779245630000131
Tablets (300 mg per 1 tablet) were prepared from the following ingredients. The obtained tablet can be ingested 1 time per 1 day and 5 tablets per 1 time to obtain an excellent anti-obesity effect.
TABLE 6
Figure BDA0003779245630000132
Capsules (300 mg per 1 capsule) were prepared from the following ingredients. The obtained capsule can be taken 2 times per 1 day, 2 capsules 1 time per 1 time, and has excellent anti-obesity effect.
TABLE 7
Figure BDA0003779245630000141
Industrial applicability
The composition of the present invention is expected to have a high anti-obesity effect, and therefore, is highly useful industrially.

Claims (10)

1. An anti-obesity composition contains tectorigenin and pinitol.
2. The anti-obesity composition according to claim 1, wherein the content ratio of tectorigenin to pinitol is such that, in terms of mass ratio, tectorigenin: pinitol is 1: 0.1 to 26 inclusive.
3. The anti-obesity composition according to claim 1 or 2, wherein the tectorigenin is tectorigenin.
4. A composition for reducing body fat or promoting fat metabolism contains tectorigenin and pinitol.
5. The composition for reducing body fat or promoting fat metabolism according to claim 4, which acts by promoting fatty acid depletion in brown adipocytes.
6. A composition for promoting fat burning, promoting thermogenesis or promoting energy consumption comprises tectorigenin and pinitol.
7. The composition for promoting fat burning, promoting thermogenesis, or promoting energy expenditure according to claim 6, which acts by promoting fatty acid expenditure in brown adipocytes.
8. An oral composition comprises tectorigenin and pinitol.
9. Use of tectorigenin and pinitol in the manufacture of a functional food for the amelioration of obesity.
10. A method for reducing body fat, promoting fat metabolism or promoting fat burning comprises using a composition containing tectorigenin and pinitol.
CN202180012480.1A 2020-06-18 2021-01-29 Anti-obesity composition and oral composition Pending CN115052591A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2020105308 2020-06-18
JP2020-105308 2020-06-18
PCT/JP2021/003384 WO2021255979A1 (en) 2020-06-18 2021-01-29 Anti-obesity composition and composition for oral administration

Publications (1)

Publication Number Publication Date
CN115052591A true CN115052591A (en) 2022-09-13

Family

ID=76753174

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180012480.1A Pending CN115052591A (en) 2020-06-18 2021-01-29 Anti-obesity composition and oral composition

Country Status (4)

Country Link
US (1) US20230123101A1 (en)
JP (1) JP6903367B1 (en)
KR (1) KR20230023604A (en)
CN (1) CN115052591A (en)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009196931A (en) 2008-02-21 2009-09-03 Kobe Univ Antiobestic agent and food and drink using the same
JP6873467B2 (en) 2016-03-16 2021-05-19 株式会社東洋新薬 Composition for promoting tissue differentiation, composition for improving liver function

Also Published As

Publication number Publication date
KR20230023604A (en) 2023-02-17
US20230123101A1 (en) 2023-04-20
JP6903367B1 (en) 2021-07-14
JPWO2021255979A1 (en) 2021-12-23

Similar Documents

Publication Publication Date Title
EP2754444B1 (en) Composition for improving in vivo metabolism parameter
JP5985138B2 (en) Energy consumption promoter
KR102303570B1 (en) Agent or method for treatment and/or prevention of accelerated energy expenditure and/or diminished energy expenditure functionality
KR101692033B1 (en) Composition comprising D-psicose for preventing or treating lipid-related metabolic disease
EP2535053B1 (en) Mitochondrial function improver
EP2532351B1 (en) Agent for improving motility function
WO2012043808A1 (en) Heat shock protein expression inducer
JP2017171654A (en) Composition for promoting tissue differentiation, and composition for improving liver function
JP2009286703A (en) Body fat accumulation-improving agent and metabolic syndrome-improving agent containing d-tagatose as active ingredient
JP2004043373A (en) Lipase inhibitor
EP2351559B1 (en) Novel use of panduratin derivative or boesenbergia pandurata extract
CN115052591A (en) Anti-obesity composition and oral composition
WO2021255979A1 (en) Anti-obesity composition and composition for oral administration
AU2004206156B2 (en) Blood pressure-lowering agent, vascular flexibility-improving agent and foods having these functions imparted thereto
JP6391959B2 (en) Non-alcoholic steatohepatitis ameliorating agent and ameliorating nutrition composition
KR100886466B1 (en) New stigmasterol derivatives or pharmaceutically acceptable salts thereof, process for the preparation thereof and composition comprising the same for inhibiting obesity or for preventing and treating hyperlipidemia
US9801404B2 (en) IGF-1 production-promoting agent
KR20170027272A (en) Composition comprising D-psicose for preventing or treating lipid-related metabolic disease
JP7239135B2 (en) α-Glucosidase activity inhibitor and blood sugar elevation inhibitor
JP2023038107A (en) Lipid synthesis inhibitor, and food and drink, processed food for inhibited lipid synthesis and expression inhibitor comprising the same
EP1627632A1 (en) Therapeutic agent
JP5326349B2 (en) Phthalide derivatives and basal metabolic regulators
JP5326351B2 (en) Basal metabolism regulator

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40075501

Country of ref document: HK