TW201828987A - Composition for activating PGC-1[alpha] - Google Patents

Abstract

The purpose of the invention is to provide a composition that has high biological safety and contributes to the activation of PGC-1[alpha]. Also, the purpose of the invention is to provide a use for said composition for activating PGC-1[alpha] and a method for activating PGC-1[alpha]. It was found that a specific compound, among naturally occurring compounds, has a PGC-1[alpha] activating action. The invention provides a novel and effective means contributing to improving endurance, increasing muscle size, suppressing obesity, reducing stress, improving sugar metabolic functions, and suppressing muscular atrophy.

Description

Composition for activating PGC-1α

The present invention relates to a composition useful for activating PGC-1α containing a predetermined compound.

As a factor that controls energy metabolism in vivo, a peroxisome proliferator-activated receptor γ co-activator 1-α (PGC-1α; Peroxisome proliferator-activated receptor gamma coactivator 1-alpha) is known. PGC-1α was originally identified as a transfer conjugation factor in brown adipose tissue that can activate the transfer via the nuclear receptor PPARγ. Later, it was learned that PGC-1α not only interacts with most of nuclear receptors of PPARγ or various transfer factors, but also controls the expression of the target gene as a transfer co-activator.

PGC-1α increases in skeletal muscle through exercise, which is related to increased expression of genes related to mitochondrial biosynthesis or energy metabolism. In addition, it is known that PGC-1α plays a role in controlling the energy production of cells in organs such as fat, brain, and blood vessels, and is related to the promotion of mitochondrial biosynthesis or the promotion of acidified phosphorylation. Based on the control effect of such energy production, as the functions of PGC-1α, it is known to improve endurance (non-patent document 1), muscle hypertrophy (non-patent document 2), obesity suppression (non-patent document 3), and light pressure reduction ( Non-patent document 4), glucose metabolism improvement (non-patent document 5), and muscle atrophy suppression (non-patent document 6) are related.

When the body is in a state of energy deficiency, the AMP concentration in the cell will rise, and AMPK (AMP kinase) will be activated. This AMPK promotes the phosphorylation of PGC-1α, and also promotes the deacetylation of PGC-1α. As a result, cytoplasmic PGC-1α migrates into the nucleus and promotes the expression of the target gene as a transfer coactivator (Non-Patent Document 7).

Among compounds derived from natural products, resveratrol contained in wine activates AMPK by the inhibition of phosphodiesterase. As a result, a report on activating PGC-1α has been disclosed (Non-Patent Document 8), but there is no Related reports on PGC-1α activation energy of other natural ingredients. [Prior Art Literature] [Non-Patent Literature]

[Non-Patent Document 1] Nature. 2008 Jul 24; 454 (7203): 463-9. [Non-Patent Document 2] Cell. 2012 Dec 7; 151 (6): 1319-31. [Non-Patent Document 3] Nature. 2012 Jan 11; 481 (7382): 463-8. [Non-Patent Document 4] Cell. 2014 Sep 25; 159 (1): 33-45. [Non-Patent Document 5] J Biol Chem. 2003 Aug 15; 278 ( 33): 31385-90. [Non-Patent Literature 6] Proc Natl Acad Sci USA 2009; 106: 20405-20410 [Non-Patent Literature 7] Diabetes, 2007 Jan 19; 56 (3): 836-48. [Non-Patent Literature 8] Cell. 2012 Feb 3; 148 (3): 421-33.

[Problems Solved by the Invention]

It is expected that a compound that activates PGC-1α can exhibit the above-mentioned effects such as improvement of staying power and muscle hypertrophy. However, with regard to compounds having such effects, other than resveratrol, no natural system with high safety in the food and beverage field has been found that can be easily obtained and widely used. look forward to.

Among them, the present invention aims to provide a composition having high biological safety and capable of imparting activation to PGC-1α. It is another object of the present invention to provide a composition for activating PGC-1α and a method for activating PGC-1α. [Means for solving problems]

The present inventors conducted a detailed review in order to achieve the above object, and found that a specific compound among natural compounds has an activation effect of PGC-1α. Based on this knowledge, the present inventors have completed the present invention.

That is, this invention relates to the following, but it is not limited to these. (1) Contains a substance selected from the group consisting of Chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, Ellagic acid, coumarins, diallyl heptane Compounds, diterpenes, sesquiterpenes, triterpenes, neoflvons, phytochemicals, flavanones, flavanones, flavonols, flavones and lignans A composition for activating PGC-1α of at least one compound in a group. (2) Chalcones are selected from 2-hydroxychalcone, trans-chalcone, isoliquiritigenin, 4'-hydroxychalcone, 2 ', 4'-dihydroxy-4,6 '-Dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, Butin, 2,3-dimethoxy-2'-hydroxychalcone , 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4,4'-dimethoxychalcone, 4-methyl The composition described in (1) of at least one compound grouped by oxychalcone and 3,4,2 ', 4', 6'-pentahydroxychalcone. (3) Alkaloids are the compositions described in (1) or (2) of Piperlongumine and / or Mahane. (4) Anthraquinones are the composition according to any one of (1) to (3) of emodin and / or anthraflavinic acid. (5) Isoflavans are the composition according to any one of (1) to (4) of (±) -equol (Equol). (6) Isoflavones are at least one compound selected from the group consisting of 4 ', 6,7-trihydroxy isoflavones, 5-methyl-7-methoxy-isoflavones, and Ipriflavone ( The composition according to any one of 1) to (5). (7) Ellagic acid is the composition described in any one of (1) to (6) of urolithin and / or ellagic acid. (8) Coumarins are the composition according to any one of (1) to (7) of aescin. (9) The diallyl heptane is a composition according to any one of (1) to (8) selected from the group consisting of at least one compound consisting of curcumin 1, curcumin 2, and curcumin 3. (10) The diterpenes are the composition according to any one of (1) to (9) of isosteviol. (11) sesquiterpene is the composition according to any one of (1) to (10) of (-)-trans caryophyllene and / or nootkatone. (12) Triterpenes are the composition described in any one of (1) to (11) of ivy saponin (Hederagenin) and / or corosolic acid. (13) Neoflavones are the composition described in any one of (1) to (12) of Dalbergin. (14) Phytochemicals are at least one compound selected from the group consisting of Apocynin, 3-Anisaldehyde, (+)-Purellene, and Tyrosol (1) to (13) The composition described in any one of the above. (15) Flavone alcohols are the composition according to any one of (1) to (14) of (+)-taxifolin. (16) Flavanones are selected from the group consisting of 4'-methoxyflavone, 2'-hydroxyflavone, 3'-hydroxyflavone, flavone and 6-methoxyflavone The composition according to any one of (1) to (15) of at least one compound of the group. (17) Flavonols are selected from the group consisting of Galangin, 3-methoxyflavones, Kaempferol, 3 ', 5,7-trihydroxy-3,4'-dimethoxyflavones, 3 ', 4', 5,5 ', 6,7,8-Heptamethoxyflavones, Fisetin, 6-methoxyflavonols, 7-Hydroxyflavonols, and Isorhamnetin The composition according to any one of (1) to (16) in the group of at least one compound. (18) Flavonoids are selected from the group consisting of Violanthin, 3 ', 4'-dihydroxyflavones, Tangeretin, 2'-methoxyflavones, 7,4'-dihydroxyflavones , Chrysoeriol, 3 ', 4'-dimethoxyflavones, flavones, α-naphthoflavones, Diosmetin, 4'-methoxyflavones, Wogonin The composition according to any one of (1) to (17), which is at least one group of 6-hydroxyflavones and 5-methoxyflavones. (19) Lignans are selected from the group consisting of Eudesmin, (-)-sesamin, Honokiol, sesamolin, sesamin, and nordihydroguaiaretic acid ( Nordihydroguaiaretic acid), Sesaminol, Sesamol, Episesamin, and Matairesinol. The described composition. (20) It is used for the composition as described in any one of (1)-(19) which improves endurance, muscle hypertrophy, suppression of obesity, reduction of stress, improvement of a glucose metabolism function, or suppression of muscle atrophy. (21) The composition according to any one of (1) to (20), which is represented by a function exhibited by the activity of PGC-1α. (22) Function is selected from the group consisting of "improving endurance", "supporting endurance", "maintaining endurance", "improving endurance", "effective for improving endurance", "becoming a body that is less prone to fatigue", "reducing "Fatigue", "Suppress fatigue", "Promote recovery from fatigue", "Make muscle", "Grow muscle", "Make muscle", "Fat reduction", "Easily burn fat", "Suppress obesity", "Prevent obesity" "Improve lipid metabolism", "Relieve stress", "Improve stress tolerance", "Suppress depression", "Prevent depression", "Promote glucose metabolism", "Improve glucose metabolism", "Promote sugar combustion", "Support sugar metabolism" "(21)", "Consumption of Sugar", "Maintain Muscle", "Suppress Muscle Atrophy", "Prevent Muscle Loss", "Suppress Muscle Loss", "Prevent Muscle Decline" and "Suppress Muscle Decline" Documented composition. (23) Used for activating PGC-1α selected from chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, Ellagic acid, coumarins, diene Propylheptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones and lignans The use of at least one compound in a group of vegetals. (24) Use a compound selected from chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, Ellagic acid, coumarins, diallylheptanes, Terpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones and lignans A method for activating PGC-1α of a compound. [Effect of the invention]

According to the present invention, a composition having excellent PGC-1α activation effect can be provided. If the composition of the present invention is used, the effects of increasing endurance, muscle hypertrophy, suppressing obesity, reducing stress, improving glucose metabolism and inhibiting muscle atrophy can be obtained by activating PGC-1α. The achievement of these effects by the present invention is related to providing a novel method that contributes to the improvement of QOL in a patient or an elderly person.

In addition, since the predetermined compounds used in the present invention are all derived from natural products, they are considered to be highly safe. Therefore, the present invention provides a composition which not only has excellent PGC-1α activation effect but is safe and can be continuously ingested.

[Mode for Carrying Out the Invention]

(Compound) One aspect of the present invention is a composition containing a predetermined compound. The composition of the present invention is one in which the specified compound is used as an active ingredient.

The composition of the present invention contains a substance selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavones, isoflavones, and ellagic acid. (ellagic acid), Coumarins, Diarylheptanoids, Diterpenoids, Sesquiterpenes, Triterpenes, Neoflavones Neoflavones, phytochemicals, flavanonols, Flavanones, Flavonols, Flavones, and Lignans Groups of at least one compound. The aforementioned compound in the composition of the present invention may contain two or more kinds or may contain three or more kinds.

The compound used in the present invention is trans-chalcone, 2 ', 4'-dihydroxy-4,6'-dimethoxychalcone (2', 4-Dihydroxy-4 ' , 6'-dimethoxychalcone), 2 ', 6'-dihydroxychalcone (2', 6'-Dihydroxy-4,4'-dimethoxychalcone), 2-hydroxychalcone Ketone (2-Hydroxychalcone), 3,4,2 ', 4', 6'-pentahydroxychalcone (3,4,2 ', 4', 6'-Pentahydroxychalcon), Acacia (Acacetin), Wheat Acteoside, Andrographolide, Apigenin, Apigeninidin chloride, Baicalein, Baicalin, Butein, Paclitaxel (Chrysin), Cyanin, Daidzein, Delphin, Delphinidin Chloride, δ- (3,4-dihydroxyphenyl) -γ-valerolactone (δ- (3,4-Dihydroxyphenyl) -γ-valerolactone), Diosmetin, Diosmin, Ellagic acid, Eriodictyol, Fisetin , Flavones, Galangin, Gallic acid, Sanguisorbic acid, Orange peel (Hesperetin), Isoliquiritigenin, Kaempferol, Lipoic acid, Luteolin, Mahanine, Myricetin, Protocatechuic acid ), Procyanidin B2, Quercetin dihydrate, Sesamin, Episesamin, Tellimagrandin 1, Tinamagrandin 1 (Tellimagrandin 2), Theobromine, Theophylline, Wogonin, Silibinin, Rottlerin, 6-Hydroxyflavone, 7 -7-Hydroxyflavone, Isorhamnetin, Morin, Biochanin A, Chrysoeriol, Formononetin, Paeonia lactiflora Peonidin Chloride, Amentoflavone, Cupressuflavone, 3 ', 4'-Dihydroxyflavone, 7,4'-Dihydroxyflavone (7,4'-Dihydroxyflavone), 7,8-Dihydroxyflavone, 6,7-Dihydroxyflavone (6,7-Dihydroxyflavone), 3 ', 4'-Dimethoxyflavone, 3-Hydroxyflavone, Ipriflavone, 2'-A 2'-Methoxyflavone, 3-Methoxyflavone, 5-Methoxyflavone, 4'-Methoxyflavone, 5- 5-Methyl-7-methoxy-isoflavone, 3 ', 4', 5 ', 5,7-pentamethoxyflavone (3', 4 ', 5' , 5,7-Pentamethoxyflavone), 3 ', 4', 7,8-Tetrahydroxyflavone (3 ', 4', 7,8-Tetrahydroxyflavone), 3 ', 5,7-Trihydroxy-3,4'- Dimethoxyflavone (3 ', 5,7-Trihydroxy-3,4'-dimethoxyflavone), 4', 6,7-trihydroxyisoflavone (4 ', 6,7-Trihydroxyisoflavone), 7-hydroxyflavonol (7-Hydroxyflavonol), 7-Methoxyflavonol, 6-Methoxyflavonol, Flavanone, Flavanone hydrazone, 2 ' -2'-Hydroxyflavanone, 4'-Hydroxyflavanone, 3'-Hydroxyflavanone, α-Naphthoflavone, 4'-methoxyflavanone (4'-Metho xyflavanone), 5-Methoxyflavanone, 6-Methoxyflavanone, 2 ', 6'-dihydroxy-4,4'-dimethoxydi 2 ', 6'-Dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4'-methoxychalcone (2 ', 6'-Dihydroxy-4' -methoxychalcone), 2,3-Dimethoxy-2'-hydroxychalcone, 2,3-Dimethoxy-2'-hydroxychalcone, Sesaminol, 4-methoxychalcone (4 -Methoxychalcone), 4'-Methoxychalcone, Quercetin-3,7,3 ', 4'-tetramethyl ether (Quercetin-3,7,3', 4 ' -tetramethylether), Fisetinidin chloride, Luteolinidin chloride, 8-Acetyl-6-hydroxy- 7-methoxycoumarin), 8-Acetyl-7-methoxycoumarin, 3-Aminocoumarin, Bergamotin, Bergamot Lactone (Bergapten), Bergaptol, Citropten, Coumarin, Coumaric acid, Coumestrol, Dalbergin Daphnetin, 5,7-Dihydroxy-4-methylcoumarin, Esculetin dibenzylether, 4-ethoxylate 4-Ethoxycoumarin, 7-Ethoxycoumarin, Fraxetin, 7-Herniarin, 3-hydroxycoumarin (3 -Hydroxycoumarin), 4-Hydroxycoumarin, Imperatorin, Isobergapten, Isopimpinellin, Isoscopoletin, 6 -6-Methylcoumarin, Umbelliferone, 3-Acetyl-β-boswellic acid, α-Amyrin ), Β-Amyrin, Artemisinin, Betulin, Betulinic acid, Betulinic acid methyl ester, Bilobalide, Cafestol, (-)-carvol ((-)-Carveol), (+)-carvone ((+)-Carvone), (-)-carvone ((-)-Carvone), Caulophyllogenin, deoxysarcosine ( Deoxyactein, Erythrodiol, Ganoderic acid A, Hederagenin, d-Isomenthol, (±) Isomenthone, Oleanolic acid, Alizarin, Alkannin, Anthraflavic acid, Anthraquinone, 1,4-Benzoquinone, 2-tert-butyl-p-quinone (2-Tert-butyl-p-quinone), 1,4-Dimethylanthraquinone (Emodin), emodin methyl ether ( Physcion), Rhein, Lyoniresinol, Urolithin, 5,7,4'-trimethoxyflavone (5,7,4'-Trimethoxyflavone), Amygdalin ( Amarogentin), 6-Methylflavone, 4-Hydroxychalcone, 4'-Hydroxychalcone, Coumalic acid, Koji Acid (Kojic acid), parthenolide, icariin (Icariin), ginsenoside Rb1 (Ginsenoside Rb 1), gingerol (Gingerol), 10-hydroxy-2-decenoic acid (10-hydroxy -2-decenoic acid), Epipinoresinol- Glc), forsythiaside (Phillyrin), pinoresinol, epipinoresinol, forsythiagenin (Phillygenin), curcumin 1 (curcumin 2), curcumin 3 (Curcumin 3), Diasesamin, Honokiol, 5,7-Dimethoxyflavone, Sennidine A, Esculetin, Sesaminol ( Sesamol, Scopoletin, Nordihydroguaiaretic acid, Vanillic acid, trans-Cinnamic acid, Allantoin, α- Α-Asarone, (±) -Synephrine, (Itaconic acid), Asiatic acid, Boldine, Shikimic acid ( Shikimic acid, Tyrosol, Corosolic acid, Picein, Rosmarinic acid, Isosteviol, Artepillin C ), Apiole, Azulene, Marsoliin, (-)-Perillic acid, Madacsic acid, Mangiferin ) , Linalool, 2-Anisaldehyde, 3-Anisaldehyde, 4-Anisic acid, Urocanic acid, α- ( -)-Bisabolol, α-(-)-Bisabolol, (-)-trans-Caryophyllene, Caryophyllene oxide, Hamamelitannin ), Perillaldehyde, Bavachinin A, Betonicine, (+)-Cuparene, Nootkatone , (-)-Perylylalcohol, Piperlongumine, Chamazulen, (-)-Asarinin, (-)- Sesamin ((-)-Sesamin), 2 ', 4,4', 6'-Tetrahydroxychalcone, Hinokitiol, Fucoxanthin Fucoxanthine, Enterodiol, Matairesinol, Podophyllotoxin, Trigonelline monohydrate, Trachelogenin, 7-hydroxy-4 '-Methoxyflavone (7-Hydroxy-4'-methoxyflavone), Glycyrrhizic acid, 6-hydroxy-4'- 6-Hydroxy-4'-methoxyflavone, Dihydromyricetin, 2'-Hydroxychalcone, Zerumbone, Apocynin, Olive Bitter Oleacein, Crocetin, Isosorbide Dinitrate, Hydroxytyrosol, Homoprotocatechuic acid, Glutathione, Kahweol , Corilagin, sesamolin, Oleuropein, (±) -equol ((±) -Equol), Rutin trihydrate, Vitexin (Vitexin), Orientin, Isovitexin, Violanthin, (+)-Douglas Fir ((+)-Taxifolin), Naringin, Eucalyptus (Eudesmine), Saponarin, Limonin, Chafuroside B, Chafuroside A, Tangeretin, Sinensetin, and 3 ', 4', 5,5 ', 6, 7,8-heptamethoxyflavone (3 ', 4', 5,5 ', 6,7,8-Heptamethoxyflavone). The composition of the present invention contains one or more of the aforementioned compounds.

The above specific compounds are each represented by the chemical formula shown in the following table.

The above-mentioned compounds may be used by sellers or those prepared by methods known to industry experts. The compound can be prepared by, for example, separating or purifying a plant or the like containing various compounds using a solvent such as water or oil. The compound may be in any form such as a crystallized form, a recrystallized form, or a concentrate, and the form is not particularly limited.

The above compounds can be derivatized into, for example, a glycoside. The "glycoside" in this specification means a compound in which a hydroxyl group of a sugar is bonded to a non-glycan compound. The sugar in the glycoside may be a monosaccharide, or may be a disaccharide or a plurality of sugars, and is not particularly limited. The type of sugar is not particularly limited, and examples thereof include glucose, mannose, galactose, fucose, aldose such as rhamnose, arabinose, and xylose, ketose such as fructose, glucuronic acid, and galacturonic acid. , Uronic acid such as mannuronic acid, celery sugar, rue, etc. The sugar used for the glycoside may be D-form, L-form, or a mixture of D-form and L-form (DL form), and is not particularly limited.

The composition of the present invention may contain any one of the above compounds and any two or more of them. In addition, the composition of the present invention may contain 3 or more, 4 or more, 5 or more, 6 or more, 7 or more, 8 or more, 9 or more or 10 or more of any of the compounds described above.

When plural compounds are used, for example, hummus A, 5-methyl-7-methoxy-isoflavone, 3 ', 5,7-trihydroxy-3,4'-dimethoxyflavone can be used. , Ipriflavone, purine, formononetin, 4'-methoxyflavonoids, 5,7,4'-trimethoxyflavonoids, 5,7-dimethoxyflavonoids, Astaxanthin, 3 ', 4'-dihydroxyflavone, 6-methoxyflavonol, Diosmetin, Diasesamin, Luteolin, 5-methoxyflavonoids, Apigenin ), Baicalein, anthraxanthinic acid, 6-hydroxyflavonoids, flavones, honokiol, ginsenoside Rb1, urocanic acid, Daidzein, 4'-methoxychalcone Ketones, Apiole, 4'-methoxyflavanone, forsythiagenin (Phillygenin), grosvenol (Matairesinol), strobilin methyl ether A, (-)-trans caryophyllene, ( ±) -Symphorin, Mangiferin, 4-methoxychalcone, 2'-methoxyflavonoid, 2 ', 4,4', 6'-tetrahydroxychalcone, Markas Acid (Madecassic acid), 2,3-dimethoxy-2'-hydroxychalcone, (-)-fluorenyl alcohol, caryophyllene oxide, α -(-)-Bisabolol, Hamamelitannin, Urolithin, Rheinland, Marrubiin, 6-methoxyflavanone, Nootkatone ), Aescin, Pinoresinol, Nordihydroguaiaretic acid, Gingerol, 10-hydroxy-2-decenoic acid, Fucoxanthine, Forsythiaside (Phillyrin), α-Asarone, 4'-Hydroxychalcone, Curcumin 1, (-)-Asaridin, Amidine, Hinokitiol, 3-Anisaldehyde, Dalstonide , Curcumin 2, 7-hydroxyflavonoids, Boldine, Betonicine, (-)-sesamin, Picin, 6,7-dihydroxy Flavonoids, 4-Anisic acid, Vanillic acid, Rosmarinic acid, Artemisinin, Dex-episorol glucoside, Emodin, icariin ( Icariin, Rottlerin, Chrysoeriol, Ellagic acid, SennidineA, Linalool, 4-hydroxychalcone, 4 ', 6,7- Trihydroxy isoflavones, 3 ', 4'-dimethoxyflavones, stilbene Piperlongumine, Fisetinidin chloride, Hederagenin, (+)-Thujallene, Coumarinic acid, Epipinoresinol, 2-Anisaldehyde , Trans-cinnamic acid, aspirin C, 3-hydroxyflavone, 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, allantoin, perillaldehyde (Perillaldehyde), Kojic acid, 4'-hydroxyflavanones, and the like are not particularly limited. Although not particularly limited, among the aforementioned compounds, hummus A, 5-methyl-7-methoxy-isoflavone, and 3 ', 5,7-trihydroxy-3,4'-dimethylformaldehyde are preferred. Oxyflavones, Ipriflavone, Purine, Formononetin, 4'-methoxyflavones, 5,7,4'-trimethoxyflavones, 5,7-dimethoxy Flavonoids, chrysin, 3 ', 4'-dihydroxyflavone, 6-methoxyflavonol, Diosmetin, Diasesamin, luteolin, 5-methoxyflavonoids, celery Apigenin, baicalein, anthraxanthinic acid, 6-hydroxyflavonoids, flavones, honokiol, ginsenoside Rb1, Urocanic acid, Daidzein, 4'-methoxy Gichalcone, Apiole, 4'-methoxyflavanone, forsythiagenin (Phillygenin), Luotaisinol (Matairesinol), broken paper paper methyl ether A, (-)-trans Dianthus Ene, (±) -Simferin, Mangiferin, 4-methoxychalcone, 2'-methoxyflavonoid, 2 ', 4,4', 6'-tetrahydroxychalcone, Macadesic acid, 2,3-dimethoxy-2'-hydroxychalcone, (-)-fluorenyl alcohol, caryophyllene oxidation , Α-(-)-bisabolol, Hamamelitannin, Urolithin, Rheinland, Marsoliin, 6-methoxyflavanone, nocardione (Nootkatone), Aescin, Pinoresinol, Nordihydroguaiaretic acid, Gingerol, 10-Hydroxy-2-decenoic acid, Fucoxanthine ), Forsythiaside (Phillyrin), alpha-aspartin, 4'-hydroxychalcone, curcumin 1, (-)-octinolipin, hydrazone, hinokitiol, 3-anisaldehyde, Dalbergia A combination of lactone or curcumin 2.

For the composition of the present invention, as the chalcone compounds, 2-hydroxychalcone, trans-chalcone, Isoliquiritigenin, 4'-hydroxychalcone, 2 ', 4' are used. -Dihydroxy-4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, purine, 2,3-dimethoxy-2'- Hydroxychalcone, 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4,4'-dimethoxychalcone , 4-methoxychalcone and 3,4,2 ', 4', 6'-pentahydroxychalcone are preferred.

For the composition of the present invention, as the alkaloid compound, Piperlongumine and Mahanine are preferably used.

For the composition of the present invention, as the anthraquinone compound, it is preferable to use emodin and anthraxanthin.

As for the composition of the present invention, it is preferable to use (±) -equol as the isoflavane compounds.

For the composition of the present invention, as the isoflavone compounds, 4 ', 6,7-trihydroxy isoflavone, 5-methyl-7-methoxy-isoflavone and Ipriflavone are preferably used. .

For the composition of the present invention, it is preferable to use urolithin and ellagic acid as a compound of ellagic acid.

For the composition of the present invention, as the coumarin compounds, it is preferable to use aescin.

For the composition of the present invention, as the diallyl heptane compound, curcumin 1, curcumin 2, and curcumin 3 are preferably used.

For the composition of the present invention, it is preferable to use isosteviol as the diterpenoid compound.

For the composition of the present invention, as the sesquiterpene compounds, (-)-trans caryophyllene and Nootkatone are preferably used.

As for the composition of the present invention, as the terpene compound, it is preferable to use ivy saponin (Hederagenin) and corosolic acid.

For the composition of the present invention, as the flavonoid compound, it is preferable to use Dalstonolide.

For the composition of the present invention, as the phytochemicals, it is preferable to use oleander, 3-anisaldehyde, (+)-curcumene, and hydroxytyrosol.

For the composition of the present invention, it is preferable to use (+)-Douglas fir as the flavanone alcohol compound.

For the composition of the present invention, as the flavanone compounds, 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone, and 6-methyl are used. Oxyflavanones are preferred.

For the composition of the present invention, as the flavonol compounds, the ginger, 3-methoxyflavone, kaempferol, 3 ', 5,7-trihydroxy-3,4'-dimethoxyl are used. Flavonoids, 3 ', 4', 5,5 ', 6,7,8-heptamethoxyflavones, Fisetin, 6-methoxyflavonols, 7-hydroxyflavonols, and isorhamnetin Isorhamnetin is preferred.

For the composition of the present invention, as flavonoid compounds, Violanthin, 3 ', 4'-dihydroxyflavone, hesperetin, 2'-methoxyflavonoids, 7,4' are used. -Dihydroxyflavones, Chrysoeriol, 3 ', 4'-dimethoxyflavones, flavones, α-naphthoflavones, Diosmetin, 4'-methoxyflavones, Chinese scutellaria Wogonin, 6-hydroxyflavones and 5-methoxyflavones are preferred.

For the composition of the present invention, as the lignan compounds, eucalyptol, (-)-sesamin, honokiol, sesamolin, sesamin, and nordihydrogen are used. Nordihydroguaiaretic acid, Sesaminol, Sesamol, Episesamin and Matairesinol are preferred.

As the compound used in the composition of the present invention, 3 ', 4'-dihydroxyflavone, 4'-methoxyflavone, anthraxanthic acid, 4'-methoxychalcone, 2' -Methoxyflavone, purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4' -Dimethoxyflavones, flavones, Diosmetin, 5-methyl-7-methoxy-isoflavones, 4'-methoxyflavones, 6-methoxyflavonols, 6-hydroxyflavones , Ipriflavone, 5-methoxyflavone and Matairesinol are preferred. When these compounds are used, the effect of the present invention can be exhibited at a low concentration (low content).

In addition, more preferred compounds for use in the composition of the present invention are 3 ', 4'-dihydroxyflavone, 4'-methoxyflavone, anthraxanthic acid, 4'-methoxychalcone, 2' -Methoxyflavone, purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4' -Dimethoxyflavones, flavones, Diosmetin, 5-methyl-7-methoxy- isoflavones, 4'-methoxyflavones and 6-methoxyflavonols. When these compounds are used, the effects of the present invention can be exhibited in a low concentration (low content) and in a wide concentration range.

(PGC-1α) 之 The composition of the present invention can activate PGC-1α by using the above-mentioned compound as an active ingredient. Therefore, the composition of the present invention can be used as a composition for activating PGC-1α. PGC-1α is a transfer coactivator shown by the name Peroxisome proliferator-activated receptor gamma coactivator 1-alpha. As this function, it is known to have an effect equivalent to the interaction with various transfer factors, to promote mitochondrial biosynthesis, or to increase the expression of the glucose transporter GLUT4.

PGC-1α is related to energy metabolism in vivo, and it is manifested in skeletal muscle, brown fat cells and liver. Among the skeletal muscles, high performance of PGC-1α was seen particularly in soleus muscles. The mRNA of PGC-1α is registered as a GenBank accession number NM_013261 for humans, and as a mouse as a GenBank accession number NM_008904.

The activation of PGC-1α in the present specification means improving the function of PGC-1α. The activation of PGC-1α in this specification includes inducing or promoting the activation of PGC-1α, and it also contains PGC-1α that is phosphorylated or deacetylated, and that PGC-1α is present in the cytoplasm to the nucleus. Migrants, PGC-1α biased in the nucleus, interactions with other nuclear receptors or transfer factors, hinders the degradation of PGC-1α protein, and promotes the translation of PGC-1α gene into PGC-1α protein at any stage PGC-1α expressor.

The activity of PGC-1α is not particularly limited. For example, as shown in the examples described below, a plastid that incorporates PGC-1α and GAL4DBD is inserted, and a plastid containing a UAS base sequence and luciferase cDNA is introduced into a given cell It can be measured by investigating the luciferase activity after co-expression. In this case, a condition to be compared is set, and if a measurement value higher than the measurement value under this condition is obtained, it can be determined that PGC-1α can be activated under this condition.

(Composition) 的 The content of the compound in the composition of the present invention is not particularly limited as long as it takes into consideration the form of administration, the method of administration, and the like to obtain the desired effect of the present invention. For example, the content of the above compound is 0.1% by weight or more with respect to the total weight of the composition of the present invention, preferably 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.5, 2, 5, or Above 10% by weight and below 90% by weight, preferably 80, 70, 60, 50, 40, 30, 20 or 15% by weight. As described above, in the composition of the present invention, the compound may contain only one kind or may contain two or more kinds. When two or more compounds are contained, the aforementioned content can be determined by the total value of the contents of various compounds. In addition, "weight%" used in the present specification means weight / weight (w / w) unless otherwise specified.

The composition of the present invention is characterized by containing the above-mentioned compound as an active ingredient, and PGC-1α can be activated by the action of the compound. By activating PGC-1α in the body, as an effect related to the function of PGC-1α, for example, it can effectively improve endurance, muscle hypertrophy, suppress obesity, reduce stress, improve glucose metabolism and inhibit muscle atrophy. . Therefore, the composition of the present invention can be used as a composition for improving endurance, muscle hypertrophy, suppressing obesity, reducing stress, improving glucose metabolism, or inhibiting muscle atrophy. And, the concept of endurance includes both muscle endurance and whole body endurance. There is no particular limitation, but the so-called staying power in the present invention means better muscle endurance.

The composition of the present invention may be incorporated in this form, and may contain, in addition to the above-mentioned compounds, optional additives and optional components generally used. Examples of these additives and ingredients include vitamins such as vitamin E, vitamin C, and other physiologically active ingredients such as vitamins, minerals, nutritional ingredients, and fragrances, as well as excipients added during formulation, Binders, emulsifiers, tonicity agents (isotonizing agents), buffering agents, dissolution aids, preservatives, stabilizers, antioxidants, colorants, coagulants, or coating agents, but are not limited thereto .

The composition of the present invention can be formulated into a solid preparation such as a lozenge (containing a coated lozenge), a granule, a powder, a powder, or a capsule, or a liquid such as a general liquid, a suspension, or an emulsion according to a known method. These compositions can be taken simultaneously with water and the like. In addition, after preparing a form that can be easily added (for example, a powder form or a granular form), it can be used as a raw material for pharmaceuticals, for example.

Examples of the composition of the present invention include, but are not limited to, a pharmaceutical composition, a food and beverage composition, a food composition, a beverage composition, and a cosmetic composition. Examples which are not limited to food compositions include functional foods, health supplements, nutritional functional foods, special purpose foods, specific health foods, nutritional supplements, food therapy foods, health foods, supplements, and foods. Additives, etc.

The composition of the present invention can be applied to either a therapeutic use (medical use) or a non-therapeutic use (non-medical use). Specific examples include those that can be used as pharmaceuticals, quasi-drugs, cosmetics, etc. and are not covered by the Pharmaceutical Affairs Law. Examples include explicit or implied endurance improvement, muscle hypertrophy, obesity suppression, and stress reduction. , The use of components to improve glucose metabolism and inhibit muscle atrophy.

Another aspect of the present invention relates to a composition for imparting a functional expression by activation of PGC-1α. Although the expression or the functional expression is not particularly limited, examples include "improving endurance", "supporting endurance", "maintaining endurance", "improving endurance", "effectively improving endurance", and "not easy "Fatigued Body", "Reducing Fatigue", "Suppressing Fatigue", "Promoting Fatigue Recovery", "Making Muscles", "Growing Muscles", "Making Muscles", "Fat Reduction", "Easily Burns Fat", "Suppresses Obesity "," Preventing obesity "," improving lipid metabolism "," reducing stress "," improving stress tolerance "," inhibiting depression "," preventing depression "," promoting glucose metabolism "," improving glucose metabolism "," promoting sugar "Burning", "supporting glucose metabolism", "consuming sugar", "maintaining muscle", "inhibiting muscle atrophy", "preventing muscle loss", "inhibiting muscle loss", "preventing muscle decline", "inhibiting muscle decline", etc. or And may be equivalent to these or functional representations. For the purposes of this specification, such representations and functional representations may be given to the composition itself or to a container or package of the composition.

The composition of the present invention can be ingested by an appropriate method in accordance with this form. The composition of the present invention may be in the form of an oral liquid preparation such as an oral solid preparation, an oral solution or a syrup, or a parenteral preparation such as an injection, an external preparation, a suppository, or a percutaneous absorbent. , But not limited to these. The term "ingestion" as used in this specification means that it is contained in all forms such as ingestion, consumption, or drinking.

The applicable amount of the composition of the present invention can be set in a timely manner according to the form, the method of administration, the purpose of use, and the age, weight, and symptoms of the patient or sick animal to be administered, but it is not a certain amount. Although the effective human intake of the composition of the present invention is not a certain amount, for example, the weight of the above-mentioned compound as the active ingredient is preferably 100 mg or more, more preferably 500 mg or more, in a human who weighs 50 kg per day. It is preferably 1,000 mg or more, preferably 10 g or less, more preferably 5 g or less, and even more preferably 3 g or less. In addition, the administration may be performed in a single or divided manner within one day within a range of a desired administration amount. The period of investment is also arbitrary. The effective human intake of the composition of the present invention means the intake of the composition of the present invention which exhibits an effect effective for humans, and the type of the compound contained in the composition is not particularly limited.

The applicable object of the composition of the present invention is preferably human, but it can also be livestock animals such as cattle, horses, sheep, pets such as dogs, cats, rabbits, or experimental animals such as mice, rats, guinea pigs, and monkeys. When animals other than humans are administered, the daily dosage of approximately 20 g for one rat will depend on the content of the active ingredients in the composition, the status of the subject, weight, sex, and age. It is different, for example, as the total compounding amount of the above compound, 10 mg / kg or more is preferable, 50 mg / kg or more is preferable, 100 mg / kg or more is more preferable, 1 g / kg or less is preferable, and 500 mg / kg is more preferable. The ingestible amount is preferably less than kg, more preferably less than 300 mg / kg.

(Method for activating PGC-1α) One aspect of the present invention is to select from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, Ellagic acid, coumarins, diallyl heptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols Use of at least one compound of flavone, flavonols, flavones and lignans.

For the present invention, the above-mentioned specific compounds can be used. For use in the present invention, as the chalcones, 2-hydroxychalcone, trans-chalcone, Isoliquiritigenin, 4'-hydroxychalcone, 2 ', 4'-dihydroxy- 4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, purine, 2,3-dimethoxy-2'-hydroxychalcone , 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4,4'-dimethoxychalcone, 4-methyl Oxychalcone and 3,4,2 ', 4', 6'-pentahydroxychalcone are preferred.

For the use of the present invention, Piperlongumine and Mahane are preferred as alkaloids.

For the use of the present invention, as the anthraquinones, emodin and anthraxanthin are preferred.

For the use of the present invention, as the isoflavans, (±) -equol is preferred.

For the use of the present invention, as the isoflavones, 4 ', 6,7-trihydroxy isoflavone, 5-methyl-7-methoxy-isoflavone and Ipriflavone are preferred.

For the use of the present invention, Urolithin and Ellagic acid are preferred as Ellagic acid.

For the use of the present invention, as the coumarins, aescinol is preferred.

For the use of the present invention, as diallyl heptanes, curcumin 1, curcumin 2 and curcumin 3 are preferred.

For the use of the present invention, as the diterpenes, Isosteviol is preferred.

For the use of the present invention, as the sesquiterpene, (-)-trans caryophyllene and Nootkatone are preferred.

For the use of the present invention, as the triterpenes, it is preferred to use ivy saponin (Hederagenin) and corosolic acid.

For the use of the present invention, as the new flavones, Dalstonolide is preferred.

For the use of the present invention, as phytochemicals, oleander, 3-anisaldehyde, (+)-curcumene, and hydroxytyrosol (Tyrosol) are preferred.

For the use of the present invention, as the flavone alcohols, (+)-Douglas fir is preferred.

For the use of the present invention, as the flavanones, 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone and 6-methoxyflavan Ketones are preferred.

For the use of the present invention, as flavonols, there are ginger, 3-methoxyflavones, kaempferol, 3 ', 5,7-trihydroxy-3,4'-dimethoxyflavones, 3 ', 4', 5,5 ', 6,7,8-Heptamethoxyflavones, Fisetin, 6-methoxyflavonols, 7-Hydroxyflavonols, and Isorhamnetin Better.

For the use of the present invention, as the flavones, Violanthin, 3 ', 4'-dihydroxyflavones, hesperetin, 2'-methoxyflavones, 7,4'-dihydroxyflavones , Chrysoeriol, 3 ', 4'-dimethoxyflavones, flavones, α-naphthoflavones, Diosmetin, 4'-methoxyflavones, Wogonin 6-hydroxyflavones and 5-methoxyflavones are preferred.

For the use of the present invention, as the lignans, eucalyptol, (-)-sesamin, Honokiol, sesamolin, sesamin, nordihydroguaiaretic acid ( Nordihydroguaiaretic acid), Sesaminol, Sesamol, Episesamin, and Matairesinol are preferred.

As the compound used in the present invention, 3 ', 4'-dihydroxyflavone, 4'-methoxyflavanone, anthraxanthinic acid, 4'-methoxychalcone, 2'-methoxyflavonone , Purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4'-dimethoxy Flavonoids, flavones, Diosmetin, 5-methyl-7-methoxy-isoflavones, 4'-methoxyflavones, 6-methoxyflavonols, 6-hydroxyflavonoids, ipriflavone ( Ipriflavone), 5-methoxyflavone and Matairesinol are preferred. When these compounds are used, the effects of the present invention can be exhibited at a low concentration (low content).

Moreover, as a more preferable compound used in the present invention, 3 ', 4'-dihydroxyflavone, 4'-methoxyflavone, anthraxanthic acid, 4'-methoxychalcone, 2 '-Methoxyflavones, purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3', 5,7-trihydroxy-3,4 '-Dimethoxyflavones, flavones, Diosmetin, 5-methyl-7-methoxy- isoflavones, 4'-methoxyflavones and 6-methoxyflavonols. When these compounds are used, the effects of the present invention can be exhibited in a low concentration (low content) and in a wide concentration range.

The use of the present invention includes, but is not limited to, the aforementioned compounds used for improving endurance, muscle hypertrophy, suppressing obesity, reducing stress, improving glucose metabolism, or inhibiting muscle atrophy. In addition, the use is for use on humans or non-human animals, and may be for therapeutic use or for non-therapeutic use. Among them, "non-therapeutic" means medical behavior, that is, it does not include the concept of treatment behavior to the human body by treatment.

(Method for activating PGC-1α) One aspect of the present invention is to use a member selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, Coumarins, diallyl heptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols A method for activating PGC-1α by at least one compound grouped by flavonoids, flavones and lignans. Another aspect of this method is a method comprising activating a PGC-1α by administering a therapeutically effective amount of the compound as an active ingredient to a subject that must be activated by PGC-1α.

For the method of the present invention, the above-mentioned specific compounds can be used. For the method of the present invention, as the chalcone compound, 2-hydroxychalcone, trans-chalcone, Isoliquiritigenin, 4'-hydroxychalcone, 2 ', 4'- Dihydroxy-4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, purine, 2,3-dimethoxy-2'-hydroxy Chalcone, 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4,4'-dimethoxychalcone, 4-methoxychalcone and 3,4,2 ', 4', 6'-pentahydroxychalcone are preferred.

For the method of the present invention, as the alkaloids, Piperlongumine and Mahanine are preferably used.

For the method of the present invention, it is preferable to use emodin and anthraxanthin as the anthraquinone compounds.

For the method of the present invention, it is preferable to use (±) -equol as the isoflavane compound.

For the method of the present invention, as the isoflavone compounds, 4 ', 6,7-trihydroxy isoflavone, 5-methyl-7-methoxy-isoflavone and Ipriflavone are preferably used.

For the method of the present invention, it is preferable to use urolithin and ellagic acid as a compound of ellagic acid.

For the method of the present invention, as the coumarin compound, it is preferable to use aescin.

In the method of the present invention, as the diallyl heptane compound, curcumin 1, curcumin 2, and curcumin 3 are preferably used.

For the method of the present invention, it is preferable to use isosteviol as the diterpenoid compound.

For the method of the present invention, as the sesquiterpene compounds, (-)-trans caryophyllene and Nootkatone are preferably used.

For the method of the present invention, as the triterpene compounds, it is preferable to use ivy saponin (Hederagenin) and corosolic acid.

For the method of the present invention, as the flavonoid compound, it is preferred to use Dalstonolide.

For the method of the present invention, as the phytochemicals, it is preferable to use oleander, 3-anisaldehyde, (+)-purellene, and hydroxytyrosol (Tyrosol).

For the method of the present invention, it is preferable to use (+)-Douglas fir as the flavanone alcohol compound.

For the method of the present invention, as the flavanone compounds, 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone, and 6-methoxy are used. Methylflavanone is preferred.

In the method of the present invention, as the flavonol compounds, ginger, 3-methoxyflavone, kaempferol, 3 ', 5,7-trihydroxy-3,4'-dimethoxy are used. Flavonoids, 3 ', 4', 5,5 ', 6,7,8-heptamethoxyflavones, Fisetin, 6-methoxyflavonols, 7-hydroxyflavonols, and isorhamnetin (Isorhamnetin) is better.

In the method of the present invention, as the flavonoid compound, Violanthin, 3 ', 4'-dihydroxyflavone, hesperetin, 2'-methoxyflavonoid, 7,4'- Dihydroxyflavones, Chrysoeriol, 3 ', 4'-dimethoxyflavones, flavones, α-naphthoflavones, Diosmetin, 4'-methoxyflavones, and baicalein (Wogonin), 6-hydroxyflavones and 5-methoxyflavones are preferred.

In the method of the present invention, as the lignan compounds, eucalyptol, (-)-sesamin, honokiol, sesamolin, sesamin, and nordihydroguaiac are used. Nordihydroguaiaretic acid, Sesaminol, Sesamol, Episesamin and Matairesinol are preferred.

As the compound used in the method of the present invention, 3 ', 4'-dihydroxyflavone, 4'-methoxyflavone, anthraxanthic acid, 4'-methoxychalcone, 2'-methyl Flavonoids, purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4'-di Methoxyflavones, flavones, Diosmetin, 5-methyl-7-methoxy-isoflavones, 4'-methoxyflavones, 6-methoxyflavonols, 6-hydroxyflavones, Ipriflavone, 5-methoxyflavone, and Matairesinol are preferred. When these compounds are used, the effect of the present invention can be exhibited at a low concentration (low content).

Further, more preferred compounds used in the method of the present invention are 3 ', 4'-dihydroxyflavones, 4'-methoxyflavone, anthraxanthic acid, 4'-methoxychalcone, 2'- Methoxyflavone, purine, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4'- Dimethoxyflavones, flavones, Diosmetin, 5-methyl-7-methoxy- isoflavones, 4'-methoxyflavones, and 6-methoxyflavonols. When these compounds are used, the effects of the present invention can be exhibited in a low concentration (low content) and in a wide concentration range.

Regarding the above-mentioned method, the object of so-called activation of PGC-1α is the same as the object of application of the composition of the present invention. The therapeutically effective amount in the present specification is the amount of PGC-1α that is activated when the composition of the present invention is administered to the subject, compared with a subject not administered. As a specific effective amount, it can be set in a timely manner by the administration form, administration method, purpose of use, target age, weight, symptoms, etc., and is not a certain amount.

For the method of the present invention, if it is to be a therapeutically effective amount, the compound or a composition containing the compound may be directly administered.

According to the method of the present invention, PGC-1α can be activated without causing side effects. [Example]

Hereinafter, the present invention will be described in more detail through examples, but the scope of the present invention is not limited thereto. A person skilled in the art can use the method of the present invention after various changes and modifications, and these are all included in the scope of the present invention. In addition, the following examples are all implemented in Shizuoka Prefecture University.

The HEK293T cells from human embryo kidneys were placed in a D-MEM (10% FBS + antibiotic (containing penicillin, streptomycin, and amphotericin B)) medium in a 60 mm dish in a CO ₂ incubator. Subculture was performed at 37 ° C, 5% CO ₂ + 95% air, and 100% humidity. After confirming that the cell density became 70 to 90% confluence, HEK293T cells were washed with PBS, and then trypsinized The cells were treated with a solution (0.05% (w / v) trypsin, 0.53 mM EDTA ･ 4Na), and the detached cells were centrifuged at 1,200 rpm and recovered. The recovered cells were resuspended in D-MEM (containing 10% FBS) ), Calculate the number of cells and use it in subculture.

A GAL4-DBD (GAL4-DNA Binding Domain) derived from yeast and a mouse-derived PGC-1α cDNA were inserted into the expression plastid to prepare a PGC-1α plastid. This PGC-1α plastid, a plastid containing a UAS base sequence, and an internal standard plastid containing a luciferase gene were introduced into HEK293T cells.

After gene introduction, HEK293T cells are cultured in a CO ₂ thermostat incubator at 37 ° C, 5% CO ₂ + 95% air, and 100% humidity for 24 hours, and then dissolved in water or DMSO to the final concentration of the test substance. It was 1 μg / mL or 10 μg / mL.

24 hours after the test substance was added, the luciferase (Luc) activity was measured, and the value obtained by dividing the measured value by the internal standard Luc activity measurement value was defined as the PGC-1α activity. In addition, to evaluate the PGC-1α activity of the test substance, let the PGC-1α activity when water or DMSO be used as the test substance be 100%, and the PGC-1α activity of all test substances be expressed in relative proportions. The results are shown in the following table.

As described above, when the final concentration is set to 1 μg / mL or 10 μg / mL, when the measured value (relative ratio) is larger than 200% of the compounds, all have the activation energy of PGC-1α. Also, for 3 ', 4'-dihydroxyflavone, 4'-methoxyflavone, anthraxanthinic acid, 4'-methoxychalcone, 2'-methoxyflavone, purine, 2 , 3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3 ', 5,7-trihydroxy-3,4'-dimethoxyflavone, flavonoids, geranium Diosmetin, 5-methyl-7-methoxy-isoflavones, 4'-methoxyflavones, and 6-methoxyflavonols were measured at both final concentrations of 1 μg / mL and 10 μg / mL The value rose to 200%. In addition, 31 types of compounds other than the above were tested, and it was confirmed that no activation activity of PGC-1α was seen in the compounds. [Industrial availability]

The present invention is to provide a useful composition having an activated PGC-1α containing a predetermined compound as an active ingredient. The present invention provides a novel method that contributes to improvement of endurance, muscle hypertrophy, suppression of obesity, reduction of stress, improvement of glucose metabolism function, and suppression of muscle atrophy, and thus has high industrial applicability.

Claims (24)

A composition for activating PGC-1α, characterized in that it contains a substance selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, and coumarins. , Diallyl heptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones And at least one compound grouped by lignans. The composition according to claim 1, wherein the chalcones are selected from the group consisting of 2-hydroxychalcone, trans-chalcone, Isoliquiritigenin, 4'-hydroxychalcone, 2 ', 4'- Dihydroxy-4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, purine, 2,3-dimethoxy-2'-hydroxy Chalcone, 2 ', 6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2', 6'-dihydroxy-4,4'-dimethoxychalcone, At least one compound grouped by 4-methoxychalcone and 3,4,2 ', 4', 6'-pentahydroxychalcone. The composition of claim 1 or 2, wherein the alkaloids are Piperlongumine and / or Mahane. The composition according to any one of claims 1 to 3, wherein the anthraquinones are emodin and / or anthraxanthin. The composition according to any one of claims 1 to 4, wherein the isoflavans are (±) -equol. The composition according to any one of claims 1 to 5, wherein the isoflavones are selected from the group consisting of 4 ', 6,7-trihydroxy isoflavones, 5-methyl-7-methoxy-isoflavones, and ipriflavones. (Ipriflavone) a group of at least one compound. The composition according to any one of claims 1 to 6, wherein Ellagic acid is urolithin and / or ellagic acid. The composition according to any one of claims 1 to 7, wherein the coumarins are aescin. The composition according to any one of claims 1 to 8, wherein the diallyl heptane is at least one compound selected from the group consisting of curcumin 1, curcumin 2, and curcumin 3. The composition according to any one of claims 1 to 9, wherein the diterpenoid is Isosteviol. The composition according to any one of claims 1 to 10, wherein the sesquiterpene is (-)-trans caryophyllene and / or nootkatone. The composition according to any one of claims 1 to 11, wherein the triterpene is Hederagenin and / or corosolic acid. The composition according to any one of claims 1 to 12, wherein the new flavonoids are xantholactone. The composition according to any one of claims 1 to 13, wherein the phytochemical substance is at least one member selected from the group consisting of oleander, 3-anisaldehyde, (+)-purellene, and hydroxytyrosol (Tyrosol) Compound. The composition according to any one of claims 1 to 14, wherein the flavanols are (+)-Douglas fir. The composition according to any one of claims 1 to 15, wherein the flavanones are selected from the group consisting of 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, and flavan A ketone and 6-methoxyflavone group of at least one compound. The composition according to any one of claims 1 to 16, wherein the flavonols are selected from the group consisting of ginger, 3-methoxyflavone, kaempferol, 3 ', 5,7-trihydroxy-3,4 '-Dimethoxyflavones, 3', 4 ', 5,5', 6,7,8-Heptamethoxyflavones, Fisetin, 6-methoxyflavonols, 7-hydroxyflavones At least one compound grouped by alcohol and isorhamnetin. The composition according to any one of claims 1 to 17, wherein the flavonoid is selected from the group consisting of Violanthin, 3 ', 4'-dihydroxyflavone, hesperetin, and 2'-methoxyflavonoids. , 7,4'-dihydroxyflavones, Chrysoeriol, 3 ', 4'-dimethoxyflavones, flavones, α-naphthoflavones, Diosmetin, 4'-methoxy At least one compound in the group of flavonoids, wogonin, 6-hydroxyflavones, and 5-methoxyflavones. The composition according to any one of claims 1 to 18, wherein the lignans are selected from the group consisting of eucalyptol, (-)-sesamin (Sesamin), honokiol, sesamolin, At least one compound grouped by sesamin, nordihydroguaiaretic acid, Sesaminol, Sesamol, Episesamin, and Matairesinol . The composition according to any one of claims 1 to 19, which is used for improving endurance, muscle hypertrophy, suppressing obesity, reducing stress, improving glucose metabolism, or suppressing muscle atrophy. The composition according to any one of claims 1 to 20, further including a function expression exerted by activation of PGC-1α. For example, the composition of claim 21, wherein the function is selected from the group consisting of "improving endurance", "supporting endurance", "maintaining endurance", "improving endurance", "effectively improving endurance", "becoming less prone to fatigue" "Body", "Reducing Fatigue", "Suppressing Fatigue", "Promoting Fatigue Recovery", "Making Muscles", "Growing Muscles", "Making Muscles", "Reducing Fat", "Easily Burns Fat", "Suppresses Obesity" , "Preventing obesity", "improving lipid metabolism", "reducing stress", "improving stress tolerance", "inhibiting depression", "preventing depression", "promoting sugar metabolism", "improving sugar metabolism", "promoting sugar burning ”,“ Supports glucose metabolism ”,“ Consumes sugar ”,“ Maintains muscle ”,“ Suppresses muscle atrophy ”,“ Prevents muscle loss ”,“ Suppresses muscle loss ”,“ Prevents muscle decline ”and“ Suppresses muscle decline ” By. A kind of activated PGC-1α selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, Ellagic acid, coumarins, diallyl Heptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones and lignans Use of at least one compound in groups. A method for activating PGC-1α, characterized by using a compound selected from chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallyl Heptanes, diterpenes, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones and lignans Groups of at least one compound.