PGC-1α activating composition
A composition of natural compounds activates PGC-1α, addressing the need for safe and effective activation to improve endurance, muscle hypertrophy, obesity suppression, and glucose metabolism.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2024-08-13
- Publication Date
- 2026-03-27
AI Technical Summary
There is a lack of readily available and safe natural compounds that effectively activate PGC-1α, which is crucial for improving endurance, muscle hypertrophy, obesity suppression, stress reduction, and glucose metabolism, necessitating the development of a composition that can safely activate PGC-1α.
A composition comprising various natural compounds such as chalcones, alkaloids, anthraquinones, isoflavones, and other phytochemicals is developed to activate PGC-1α, enhancing its activity and promoting mitochondrial biosynthesis and oxidative phosphorylation.
The composition achieves improved endurance, muscle hypertrophy, obesity suppression, stress reduction, and enhanced glucose metabolism by safely activating PGC-1α, contributing to better quality of life for patients and the elderly.
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Abstract
Description
Technical Field
[0001] The present invention relates to a composition useful for activating PGC-1α containing a predetermined compound.
Background Art
[0002] PGC-1α (Peroxisome proliferator-activated receptor gamma coactivator 1-alpha) is known as a factor that controls energy metabolism in vivo. PGC-1α was initially identified as a transcriptional cofactor that activates transcription by the nuclear receptor PPARγ in brown adipose tissue. Subsequently, it has been clarified that PGC-1α interacts not only with PPARγ but also with numerous nuclear receptors and various transcription factors, and controls the expression of target genes as a transcriptional coactivator.
[0003] The expression of PGC-1α increases in skeletal muscle by exercise and is involved in the biosynthesis of mitochondria and the increased expression of genes related to energy metabolism. In addition, it is known that PGC-1α also plays a role in controlling cellular energy production by participating in the biosynthesis of mitochondria and the promotion of oxidative phosphorylation in organs such as fat, the brain, and blood vessels. Based on such a regulatory action of energy production, the functions of PGC-1α are known to be involved in improving endurance (Non-Patent Document 1), muscle hypertrophy (Non-Patent Document 2), obesity suppression (Non-Patent Document 3), stress reduction (Non-Patent Document 4), improvement of glucose metabolism function (Non-Patent Document 5), and suppression of muscle atrophy (Non-Patent Document 6), etc.
[0004] When the energy in the living body becomes deficient, the intracellular AMP concentration increases and AMPK (AMP kinase) is activated. This AMPK promotes the phosphorylation of PGC-1α and also promotes the deacetylation of PGC-1α. As a result, PGC-1α localized in the cytoplasm translocates into the cell nucleus and promotes the expression of target genes as a transcriptional coactivator (Non-Patent Document 7).
[0005] While it has been reported that resveratrol, found in wine, activates AMPK through phosphodiesterase inhibition, thereby activating PGC-1α (Non-Patent Literature 8), there are no reports regarding the PGC-1α activating ability of other natural product components. [Prior art documents] [Non-patent literature]
[0006] [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 Document 6] Proc Natl Acad Sci USA 2009; 106: 20405-20410 [Non-Patent Document 7] Diabetes, 2007 Jan 19;56(3): 836-48. [Non-Patent Document 8] Cell. 2012 Feb 3;148(3): 421-33. [Overview of the project] [Problems that the invention aims to solve]
[0007] Compounds that activate PGC-1α are expected to exhibit the above-mentioned effects such as improved endurance and muscle hypertrophy. However, to date, compounds with such effects that are readily available and safe enough to be widely used in the food and beverage industry are not readily available natural products. No other substance has been found besides resveratrol, and its rapid development is urgently needed.
[0008] Therefore, the present invention aims to provide a composition that is highly biosafe and contributes to the activation of PGC-1α. Furthermore, the present invention aims to provide a composition for activating PGC-1α and a method for activating PGC-1α. [Means for solving the problem]
[0009] As a result of diligent research to achieve the above objective, the inventors discovered that a specific compound derived from natural products has the ability to activate PGC-1α. Based on this finding, the inventors completed the present invention.
[0010] In other words, the present invention relates to, but is not limited to, the following. (1) A PGC-1α activating composition comprising at least one compound selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallylheptanoids, diterpenoids, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanonols, flavanones, flavonols, flavones, and lignans. (2) The chalcones are 2-hydroxy chalcone, trans-chalcone, isoliquiritigenin, 4'-hydroxy chalcone, 2',4'-dihydroxy-4,6'-dimethoxy chalcone, 4-hydroxy Chalcone, 4'-methoxychalcone, butein, 2,3-dimethoxy-2'-hydroxychalcone, 2',6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2',6'-dihydroxy-4,4'-dimethyl Toxichalcone, 4-methoxychalcone, and 3,4,2',4',6'-pentahydroxychalcone The composition according to (1), which is at least one compound selected from the group. (3) The composition according to (1) or (2), wherein the alkaloids are piperlongmine and / or mahanine. (4) The composition according to any one of (1) to (3), wherein the anthraquinone is emodin and / or anthraflavinic acid. (5) The isoflavone is (±)-equol as described in any of (1) to (4) composition. (6) Isoflavones include 4',6,7-trihydroxyisoflavones, 5-methyl-7-methoxy- The composition according to any one of (1) to (5), wherein the composition is at least one compound selected from the group consisting of isoflavones and ipriflavones. (7) The composition according to any one of (1) to (6), wherein ellagic acid is urolithin and / or ellagic acid. (8) The composition according to any one of (1) to (7), wherein the coumarin is esculetin. (9) The composition according to any one of (1) to (8), wherein the diallyl heptanoid is at least one compound selected from the group consisting of curcumin 1, curcumin 2, and curcumin 3. (10) The composition according to any one of (1) to (9), wherein the diterpenoid is isosteviol. (11) The sesquiterpenes are (-)-trans caryophyllene and / or nookatones , the composition described in any of (1) to (10). (12) The composition according to any one of (1) to (11), wherein the triterpenes are hederagenin and / or corosolic acid. (13) The composition according to any one of (1) to (12), wherein the neoflavones are dalbergine. (14) The composition according to any one of (1) to (13), wherein the phytochemical is at least one compound selected from the group consisting of apocynin, 3-anisaldehyde, (+)-cuparene, and hydroxytyrosol. (15) The composition according to any one of (1) to (14), wherein the flavanonol is (+)-taxifolin. (16) Flavanones include 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone The composition according to any one of (1) to (15), wherein the composition is at least one compound selected from the group consisting of roxyflavanone, flavanone, and 6-methoxyflavanone. (17) Flavonols include galangin, 3-methoxyflavone, kaempferol, 3',5,7- Trihydroxy-3,4'-dimethoxyflavone, 3',4',5,5',6,7,8-heptamethoxyflavone The composition according to any one of (1) to (16), wherein the composition is at least one compound selected from the group consisting of fisetin, 6-methoxyflavonol, 7-hydroxyflavonol, and isorhamnetin. (18) A small number of flavonoids selected from the group consisting of violanthin, 3',4'-dihydroxyflavone, tangeretin, 2'-methoxyflavone, 7,4'-dihydroxyflavone, chrysoeriol, 3',4'-dimethoxyflavone, flavone, α-naphthoflavone, diosmetin, 4'-methoxyflavone, ougonin, 6-hydroxyflavone, and 5-methoxyflavone. A composition according to any one of (1) to (17), which is at least one compound. (19) The composition according to any one of (1) to (18), wherein the lignan is at least one compound selected from the group consisting of eudesmin, (-)-sesamin, honokiol, sesamolin, sesamin, nordihydroguaiaretic acid, sesaminol, sesamol, episesamin, and matairesinol. (20) The composition according to any one of (1) to (19), which is for enhancing endurance, promoting muscle hypertrophy, suppressing obesity, reducing stress, improving sugar metabolism function, or suppressing muscle atrophy. (21) The composition according to any one of (1) to (20), which is labeled with the indication of the function exerted by the activation of PGC-1α. (22) The indication of the function is selected from the group consisting of "enhancing endurance", "supporting endurance", "maintaining endurance", "gaining endurance", "helping to increase stamina", "making the body less prone to fatigue", "reducing fatigue", "suppressing fatigue", "accelerating fatigue recovery", "building muscle", "increasing muscle", "creating muscle", "reducing fat", "burning fat", "suppressing obesity", "preventing obesity", "enhancing lipid metabolism", "reducing stress", "enhancing stress tolerance", "suppressing depression", "preventing depression", "promoting sugar metabolism", "enhancing sugar metabolism", "promoting sugar combustion", "supporting sugar metabolism", "consuming sugar", "maintaining muscle", "suppressing muscle atrophy", "preventing muscle loss", "suppressing muscle loss", "preventing muscle decline", and "suppressing muscle decline". The composition according to (21). (23) Use of at least one compound selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallyl heptanoids, diterpenoids, sesquiterpenoids, triterpenoids, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones, and lignans for activating PGC-1α. (24) A method for activating PGC-1α by using at least one compound selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallyl heptanoids, diterpenoids, sesquiterpenoids, triterpenoids, neoflavones, phytochemicals, flavanols, flavanones, flavonols, flavones, and lignans.
Advantages of the Invention
[0011] The present invention provides a composition having excellent PGC-1α activating activity. By using the composition of the present invention, effects such as improved endurance, muscle hypertrophy, obesity suppression, stress reduction, improved glucose metabolism function, and suppression of muscle atrophy can be obtained through the activation of PGC-1α. Achieving these effects according to the present invention will lead to providing a new means that contributes to improving the quality of life of patients with illnesses and the elderly.
[0012] Furthermore, since all the compounds used in this invention are derived from natural products, they are considered to be highly safe. Therefore, this invention can provide a composition that has excellent PGC-1α activating activity and is safe and can be taken continuously. [Modes for carrying out the invention]
[0013] (compound) One aspect of the present invention is a composition containing a predetermined compound. The composition of the present invention has the predetermined compound as an active ingredient.
[0014] The compositions of the present invention include chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallylheptanoids, diterpenoids, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanonols, flavanones, flavonols, flavones, and It contains at least one compound selected from the group consisting of lignans. In the composition of the present invention, the compound may contain two or more, or three or more.
[0015] The compounds used in this invention are trans-chalcone, 2',4'-dihydroxy-4,6'-dimethoxychalcone, 2',6'-dihydroxy-4,4'-dimethoxychalcone, 2-hydroxychalcone, 3,4,2',4',6'-pentahydroxychalcone, acacetin, acteoside, andrographolide, apigenin, and apigeninidin chloride. Chloride, baicalein, baicalin, butein, chrysin, cyanin, diamine Daidzein, Delphin, Delphinidin Chloride, δ-(3,4-Dihydroxyphenyl)-γ-valerolactone, Diosmetin, Diosmin, Ella Ellagic acid, Eriodictyol, Fisetin, Flavone, Galangin, Gallic acid, Sanguisorbic acid, Hesperetin, Isoliquiritigenin, Kaempferol, Lipoic acid, Luteoli Luteolin, Mahanine, Myricetin, Protocatechuic acid, Procyanidin B2, Quercetin dihydrate, Sesamin, Episesamin, Tellimagrandin 1, Tellimagrandin 2, Theobromine, Theophylline, Wogonin, Silibinin, Rottlerin, 6-Hydroxyflavone, 7-Hydroxyflavone, Isorhamnetin, Morin, Biochanin A A) Chrysoeriol, Formononetin, Peonidin Chloride, Ame Amentoflavone, Cupressuflavone, 3',4'-Dihydroxyflavone, 7,4'-Dihydroxyflavone, 7,8-Dihydroxyflavone, 6,7-Dihydroxyflavone, 3',4'-Dimethoxyflavone, 3-Hydroxyflavone, Ipriflavone, 2 '-Methoxyflavone (2'-Methoxyflavone), 3-Methoxyflavone (3-Methoxyflavone) 5-Methoxyflavone, 4'-Methoxyflavone, 5-Methyl-7-methoxy-isoflavone, 3',4',5',5,7-Pentamethoxyflavone, 3',4',7,8-Tetrahydroxyflavone hydroxyflavone), 3',5,7-trihydroxy-3,4'-dimethoxyflavone, 4',6,7-trihydroxyisoflavone, 7-Hydroxyflavonol, 7-Methoxyflavonol, 6-Methoxyflavonol 6-Methoxyflavonol, Flavanone, Flavanone hydrazone, 2'-Hydroxyflavanone, 4'-Hydroxyflavanone, 3'-Hydroxyflavanone α-Naphthoflavone, 4'-Methoxyflavanone, 5-Methoxyflavanone, 6-Methoxyflavanone, 2',6'-Dihydroxy-4,4'-Dimethoxydihydrochalcone, 2',6'-Dihydroxy-4'-Methoxychalcone (1) hydroxy-4'-methoxychalcone, 2,3-dimethoxy-2'-hydroxychalcone, sesaminol, 4-methoxychalcone, 4'-methoxychalcone, quercetin-3,7,3',4'-tetramethylether, fisetinidine Chloride (Fisetinidin chloride), Luteolinidin chloride ), 8-Acetyl-6-hydroxy-7-methoxycoumarin, 8-Acetyl-7-methoxycoumarin, 3-aminoc Marine (3-Aminocoumarin), Bergamotin, Bergapten, Bergaptol, Citropten, Coumarin, Coumaric acid, Coumestrol, Dalbergin, Daphnetin, 5,7-Dihydroxy-4-methylcoumarin, Esculetin dibenzyl ether, 4- Ethoxycoumarin (4-Ethoxycoumarin), 7-Ethoxycoumarin (7-Ethoxycoumarin), Fraxetin, Herniarin, 3-Hydroxycoumarin (3-Hydroxycoumarin), 4-Hydroxycoumarin (4-Hydroxycoumarin), Imperatorin, Isobergapten, Isopimpinellin, Isoscopoletin, 6-Methylcoumarin, Umbell Umbelliferone, 3-Acetyl-β-boswellic acid, α-Amyrin, β-Amyrin, Artemisinin, Betulin, Betulinic acid, Methyl betulinate Betulinic acid methyl ester, bilobalide, cafestol, (-)-carveol, (+)-carvone, (-)-car Carvone, Caulophyllogenin, Deoxyacting 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, Physcion, Rhein, Lyoniresinol, Urolithin, 5,7,4'-Trimethoxyflavone, Amarogentin, 6-Methylflavone, 4-Hydroxychalcone, 4'-Hydroxychalcone, Coumalic acid, Kojic acid, Pa Lutenolide, Icariin, Ginsenoside Rb1 Rb 1), Gingerol, 10-hydroxy-2-decenoic acid, Epipinoresinol-Glc, Phillyrin, Pinoresinol, Epipinoresinol, Phillygenin, Curcumin 1, Curcumin 2 Curcumin 3, Diasesamin, Honokiol, 5,7-Dimethoxyflavone, Sennidine A Esculetin, Sesamol, Scopoletin, Nordihydroguaiaretic acid, Vanillic acid, trans-Cinnamic acid, Allantoin, α- Salon (α-Asarone), (±)-Synephrine, Itaconic acid, Asiatic acid, Boldine, Shikimic acid, Tyrosol, Corosolic acid, Picein, Rosmarinic acid, Isosteviol, Artepillin C, Apiole, Azulene, Marrubiin, (-)-Perillic acid, Madecassic acid acid), Mangiferin, Linalool, 2-Anisaldehyde, 3-Anisaldehyde, 4-Anisic acid, Urokani Urocanic acid, α-(-)-Bisabolol, (-)-trans carboxylate Caryophyllene (-)-trans-Caryophyllene), Caryophyllene oxide, Hamamelitannin, Perillaldehyde, Bavachinin A, Betonicine, (+)-Cuparene Nootkatone, (-)-Perillyl alcohol, pi Piperlongumine, Chamazulen, (-)-Asarinin, (-)-Sesamin, 2',4,4',6'-Tetrahydroxychalcone, Hinokitiol, Fucoxanthine, Enterodiol, Matairesinol Podophyllotoxin, Trigonelline monohydrate, Trachelogenin, 7-Hydroxy-4'-methoxyflavone, Glycyrrhizic acid, 6-Hydroxy-4'-methoxyflavone, Dihydromyricetin, 2'-Hydroxychalcone, Zerumbone ), apocynin, oleacein, crocetin, isosorbide diinitrate, hydroxytyrosol, homoprotocatechuic acid, glutathione, kahweol, corilagin, sesamolin, ole Oleuropein, (±)-Equol, Rutin trihydrate, Vitexin, Orientin, Isovitexin, Violanthin, (+)-Taxifolin, Nari Naringin, Eudesmine, Saponarin, Limonin, Chafuroside B, Chafuroside A, Ta Tangeretin, Sinensetin, and 3',4',5,5',6,7,8-hept It may also be tamethoxyflavone (3',4',5,5',6,7,8-Heptamethoxyflavone). The composition of the present invention contains one or more of the above compounds.
[0016] The specific compounds mentioned above are represented by the chemical formulas shown in the table below.
[0017] [Table 1-1] [Table 1-2] [Table 1-3] [Table 1-4] [Table 1-5] [Table 1-6] [Table 1-7] [Table 1-8] [Table 1-9] [Table 1-10] [Table 1-11] Table 1-12 Table 1-13 Table 1-14 Table 1-15 Table 1-16 Table 1-17 Table 1-18 Table 1-19 Table 1-20 Table 1-21 Table 1-22 Table 1-23 Table 1-24 Table 1-25 Table 1-26 Table 1-27 Table 1-28 Table 1-29 Table 1-30 Table 1-31 Table 1-32 Table 1-33 Table 1-34 Table 1-35 Table 1-36 Table 1-37 Table 1-38 Table 1-39 Table 1-40 Table 1-41 Table 1-42 Table 1-43 Table 1-44 Table 1-45 [Table 1-46] [Table 1-47] [Table 1-48] [Table 1-49] [Table 1-50] [Table 1-51]
[0018] The above compounds may be commercially available or prepared using methods known to those skilled in the art. These compounds can be prepared, for example, by isolating or purifying them from plants containing various compounds using solvents such as water or oil. The above compounds may be in any form, such as crystallized, recrystallized, or concentrated, and are not particularly limited in form.
[0019] Furthermore, the above compounds may be derivatized, such as glycosides. In this specification, "glycoside" refers to a compound formed when the hydroxyl group of a sugar is bonded to a non-carbohydrate compound. The sugar in the glycoside may be a monosaccharide, a disaccharide, or more than one sugar, and is not particularly limited. The type of sugar is also not particularly limited, and examples include glucose, mannose, galactose, fucose, rhamnose, arabinose, xylose and other aldoses, fructose and other ketoses, glucuronic acid, galacturonic acid, mannuronic acid and other uronic acids, apiose, rutinose, etc. In addition, the sugar used in the glycoside may be a D-isomer, an L-isomer, or a mixture of D-isomers and L-isomers (DL-isomer), and is not particularly limited.
[0020] The composition of the present invention may contain any two or more of the above compounds. Furthermore, the composition of the present invention may contain any three or more, four or more, five or more, six or more, seven or more, eight or more, nine or more, or ten or more of the above compounds.
[0021] When multiple types of compounds are used, for example, biochanin A, 5-methyl-7-methoxyiso Flavones, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, ipriflavone, buty N, formononetin, 4'-methoxyflavone, 5,7,4'-trimethoxyflavone, 5,7-dimethoxyflavone, chrysin, 3',4'-dihydroxyflavone, 6-methoxyflavonol, diosmetine, diasesamin, luteolin, 5-methoxyflavone, apigenin, baicalein, anthraflavic acid, 6-hydroxyflavone, flavone, honokiol, ginsenoside Rb1, urocanic acid, daidzein, 4'-methoxychalcone, apiol, 4'-methoxyf Lavanone, filigenin, matairesinol, babakinin A, (-)-trans caryophyllene, (±)-synephrine, mangiferin, 4-methoxychalcone, 2'-methoxyflavone, 2',4,4',6'-tetrahydroxychalcone, madecassic acid, 2,3-dimethoxy-2'-hydroxychalcone N, (-)-Periryl alcohol, Caryophyllene oxide, α-(-)-Bisabolol, Hamamelis Litannin, Urolitin, Lein, Malvin, 6-Methoxyflavanone, Noctaktone, Esculetin, Pinoresinol, Nordihydroguaiaretic acid, Gingerol, 10-H Droxy-2-decenoic acid, fucoxanthin, filirin, α-asalon, 4'-hydroxycal Cone, Curcumin 1, (-)-Asarinin, Azulene, Hinokitiol, 3-Anisaldehyde, Dalbergin, Curcumin 2, 7-Hydroxyflavone, Borzin, Betonicin, (-)- Sesamin, picein, 6,7-dihydroxyflavone, 4-anisic acid, vanillic acid, rosmarinic acid, artemisinin, epipinoresinol glucoside, emodin, icariin, rottrelin, chrysoeriol, ellagic acid, senidin A, linalool, 4-hydroxychalcone, 4',6,7-trihydroxyisoflavones, 3',4'-dimethoxyflavone, piperlongine Fisetinidine chloride, hederagenin, (+)-cuparene, coumaric acid, epipinolesiol, 2-anisaldehyde, trans-cinnamic acid, artepillin C, 3-hydroxyflavone, 2',6'-dihydroxy-4,4'-dimethoxydihydrochalcone, allantoin, perillaldehyde These are used in combination with kojic acid or 4'-hydroxyflavanone, but especially this The above compounds are not limited to these. Furthermore, although not particularly limited, preferred compounds among them are biochanin A, 5-methyl-7-methoxy-isoflavon, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, ipriflavone, butein, formononetin, and 4'-methoxyflavone. , 5,7,4'-trimethoxyflavone, 5,7-dimethoxyflavone, chrysin, 3',4'-dihydro Xyflavone, 6-methoxyflavonol, diosmetine, diasesamin, luteolin, 5-methoxyflavone, apigenin, baicalein, anthraflavic acid, 6-hydroxyf Lavons, Flavones, Honokiol, Ginsenoside Rb1, Urocanic Acid, Daidzein, 4'-Methoxychalcone, Apiol, 4'-Methoxyflavanone, Phyligenin, Matairesinol Lu, Babakinin A, (-)-trans-caryophyllene, (±)-synephrine, Mangiferin, 4-Me Toxychalcone, 2'-Methoxyflavone, 2',4,4',6'-Tetrahydroxychalcone, Madecassic acid, 2,3-Dimethoxy-2'-Hydroxychalcone, (-)-Periryl alcohol, Caryophyllene oxide, α-(-)-Bisabolol, Hamamelitannin, Uroritin, Rain, Malvi In, 6-methoxyflavanone, noctaktone, esculetin, pinoresinol, nordihydroguaiaretic acid, gingerol, 10-hydroxy-2-decenoic acid, fucoxanthin, filirin, α-asalone, 4'-hydroxychalcone, curcumin 1, (-)-asalinine, azulene, hinokitiol, 3-anisaldehyde, dalbergin, or curcumin 2 may be used in combination.
[0022] In the compositions of the present invention, compounds that are preferably used as chalcones are 2-hydroxychalcone, trans-chalcone, isoliquiritigenin, 4'-hydroxychalcone, and 2',4'- Dihydroxy-4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone These include butein, 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.
[0023] In the composition of the present invention, the compound preferably used as an alkaloid is piper These are Longmin and Mahanin.
[0024] In the compositions of the present invention, the compounds preferably used as anthraquinones are emodin and anthraflavinic acid.
[0025] In the composition of the present invention, the compound preferably used as an isoflavane is (±)- It is equol.
[0026] In the compositions of the present invention, the compounds preferably used as isoflavones are 4',6,7-trihydroxyisoflavones, 5-methyl-7-methoxyisoflavones, and ipriflavones. It is.
[0027] In the compositions of the present invention, the compounds preferably used as ellagic acid are urolithin and ellagic acid.
[0028] In the compositions of the present invention, the compound preferably used as a coumarin is esculetin.
[0029] In the compositions of the present invention, the compounds preferably used as diallylheptanoids are curcumin 1, curcumin 2, and curcumin 3.
[0030] In the compositions of the present invention, the compound preferably used as a diterpenoid is isosteviol.
[0031] In the compositions of the present invention, the compounds preferably used as sesquiterpenes are (-)-trans-caryophyllene and nootkatone.
[0032] In the compositions of the present invention, the compounds preferably used as triterpenes are hederagenin and corosolic acid.
[0033] In the compositions of the present invention, the compound preferably used as a neoflavonoid is dalbergin.
[0034] In the compositions of the present invention, the compounds preferably used as phytochemicals are apocynin, 3-anisaldehyde, (+)-cuparene, and hydroxytyrosol.
[0035] In the compositions of the present invention, the compound preferably used as a flavanonol is (+)-taxifolin.
[0036] In the composition of the present invention, the compound preferably used as a flavanone is 4'-meth These are xyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone, and 6-methoxyflavanone.
[0037] In the compositions of the present invention, compounds preferably used as flavonols include galangin, 3-methoxyflavone, kaempferol, and 3',5,7-trihydroxy-3,4'-dimethoxyflavone. Lavons, 3',4',5,5',6,7,8-heptamethoxyflavones, fisetin, 6-methoxyflavones These are 7-hydroxyflavonol and isorhamnetin.
[0038] In the compositions of the present invention, compounds that are preferably used as flavonoids are violanthin, 3',4'-dihydroxyflavone, tangeretin, 2'-methoxyflavone, and 7,4'-dihydroxy Xyflavone, chrysoeriol, 3',4'-dimethoxyflavone, flavone, α-naphthof These are lavons, diosmetine, 4'-methoxyflavone, ougonin, 6-hydroxyflavone, and 5-methoxyflavone.
[0039] In the compositions of the present invention, compounds that are preferably used as lignans are eudesmin, (-)-sesamin, honokiol, sesamolin, sesamin, nordihydroguaiaretic acid, sesaminol, sesamol, episesamin, and matairesinol.
[0040] The compounds used in the composition of the present invention include 3',4'-dihydroxyflavone, 4'-methoxyflavanone, anthraflavic acid, 4'-methoxychalcone, and 2'-methoxyflavones. n, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7- Trihydroxy-3,4'-dimethoxyflavone, flavone, diosmetine, 5-methyl-7-meth Xy-isoflavones, 4'-methoxyflavones, 6-methoxyflavonols, 6-hydroxyf Labon, ipriflavone, 5-methoxyflavone, and matairesinol are more preferred. Using these compounds, the effects of the present invention can be achieved at low concentrations (low content).
[0041] Furthermore, more preferred compounds used in the composition of the present invention are 3',4'-dihydroxyflavone, 4'-methoxyflavanone, anthraflavic acid, 4'-methoxychalcone, and 2'-methoxy These compounds include cyflavones, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, flavone, diosmetine, 5-methyl-7-methoxy-isoflavonone, 4'-methoxyflavone, and 6-methoxyflavonol. Using these compounds, the effects of the present invention can be achieved at low concentrations (low content) and over a wide concentration range.
[0042] (PGC-1α) 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 PGC-1α activating composition. PGC-1α is a transcriptional coactivator represented by the name Peroxisome proliferator-activated receptor gamma coactivator 1-alpha. Its functions include promoting mitochondrial biosynthesis by interacting with various transcription factors and increasing the expression level of the glucose transporter GLUT4.
[0043] PGC-1α is involved in energy metabolism in the body and is highly expressed in skeletal muscle, brown adipose tissue, and the liver, among other organs. High expression of PGC-1α is particularly observed in the soleus muscle within skeletal muscle. The mRNA for PGC-1α in humans is listed in the GenBank accession number... It is registered under the code NM_013261, and for mice, the GenBank accession number is NM_008904. It is registered as such.
[0044] In this specification, PGC-1α activation means that the function of PGC-1α is enhanced. PGC-1α activation in this specification includes inducing or promoting PGC-1α activation, and also includes phosphorylation or deacetylation of PGC-1α, translocation of cytoplasmic PGC-1α to the cell nucleus, interaction between nuclear-localized PGC-1α and other nuclear receptors or transcription factors, inhibition of PGC-1α protein degradation, and promotion of PGC-1α expression at any stage in the translation of the PGC-1α gene into the PGC-1α protein.
[0045] The activity of PGC-1α is not particularly limited, but as shown in the examples below, a plasmid incorporating cDNA conjugated with PGC-1α and GAL4DBD, and a plasmid containing the UAS base sequence and luciferase cDNA are introduced into a predetermined cell, and This can be measured by examining the luciferase activity after expression. In this process, a comparison condition is set up, and if a higher measurement is obtained than the measurement under that condition, it can be concluded that PGC-1α is more activated than under the comparison condition.
[0046] (composition) The content of the above-mentioned compounds in the composition of the present invention is not particularly limited, and should be such that the desired effect of the present invention is obtained, taking into consideration the form and method of administration. For example, the content of the above-mentioned compounds is 0.1% by weight or more, preferably 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.5, 2, 5, or 10% by weight or more, and 90% by weight or less, preferably 80, 70, 60, 50, 40, 30, 20, or 15% by weight or less, based on the total weight of the composition of the present invention. As described above, the composition of the present invention may contain only one of the above-mentioned compounds, or it may contain two or more. If two or more compounds are included, the above-mentioned content is defined by the total value of the content of each compound. In this specification, "weight %" means weight / weight (w / w) unless otherwise specified.
[0047] The composition of the present invention is characterized by containing the above-mentioned compound as an active ingredient, and PGC-1α is activated by the action of this compound. Activation of PGC-1α in the body can effectively achieve effects related to PGC-1α function, such as improved endurance, muscle hypertrophy, obesity suppression, stress reduction, improved glucose metabolism, and suppression of muscle atrophy. Therefore, the composition of the present invention can be used as a composition for improving endurance, muscle hypertrophy, obesity suppression, stress reduction, improved glucose metabolism, or suppression of muscle atrophy. The concept of endurance includes both muscular endurance and overall endurance. While not particularly limited, in the present invention, endurance preferably refers to muscular endurance.
[0048] Depending on its form, the composition of the present invention may contain, in addition to the above-mentioned compounds, any additives and any commonly used components. Examples of these additives and components include, but are not limited to, vitamins such as vitamin E and vitamin C, minerals, nutritional components, and physiologically active components such as fragrances, as well as excipients, binders, emulsifiers, tensioning agents (isotonic agents), buffers, solubilizers, preservatives, stabilizers, antioxidants, colorants, coagulants, or coating agents that are incorporated in formulation.
[0049] The compositions of the present invention can be formulated according to known methods into solid preparations such as tablets (including coated tablets), granules, powders, or capsules, or into liquid preparations such as liquids, suspensions, or emulsions. These compositions can be taken directly with water or other liquids. Alternatively, they can be prepared into easily compoundable forms (for example, powder or granules) and used, for example, as raw materials for pharmaceuticals.
[0050] Examples of compositions of the present invention include, but are not limited to, pharmaceutical compositions, food and beverage compositions, food compositions, beverage compositions, cosmetic compositions, etc. Examples of non-limited food compositions include functional foods, health supplements, nutritional functional foods, foods for special dietary uses, foods for specified health uses, nutritional supplements, dietary therapy foods, health foods, supplements, food additives, etc.
[0051] The compositions of the present invention can be applied to either therapeutic (medical) or non-therapeutic (non-medical) uses. Specifically, examples include use as pharmaceuticals, quasi-drugs, and cosmetics, and also use as compositions that explicitly or implicitly promote improved endurance, muscle hypertrophy, obesity suppression, stress reduction, improved glucose metabolism, and suppression of muscle atrophy, although these do not fall under the Pharmaceutical Affairs Law.
[0052] In another aspect, this invention includes a label indicating the function exhibited by the activation of PGC-1α. This relates to compositions. Such claims or functional claims are not particularly limited, but examples include: "increases endurance," "supports endurance," "maintains endurance," "builds endurance," "helps increase stamina," "makes the body less prone to fatigue," "reduces fatigue," "suppresses fatigue," "speeds up recovery from fatigue," "builds muscle," "increases muscle mass," "creates muscle," "reduces fat," "burns fat," "suppresses obesity," "prevents obesity," "enhances lipid metabolism," "reduces stress," "increases stress tolerance," "suppresses depressive states," "prevents depression," "promotes glucose metabolism," "enhances glucose metabolism," "promotes glucose burning," "supports glucose metabolism," "causes glucose consumption," "maintains muscle," "suppresses muscle atrophy," "prevents muscle loss," "suppresses muscle loss," "prevents muscle deterioration," "suppresses muscle deterioration," etc., or claims or functional claims that can be considered equivalent thereto. In this specification, such claims and functional claims may be affixed to the composition itself or to the container or packaging of the composition.
[0053] The compositions of the present invention can be ingested by an appropriate method depending on their form. The compositions of the present invention can be in the form of, for example, oral solid preparations, oral liquid preparations such as oral solutions or syrups, or parenteral preparations such as injections, topical preparations, suppositories or transdermal absorption preparations, but are not limited to these forms. In this specification, "ingestion" is used to include all forms such as ingestion, administration, or drinking.
[0054] The dosage of the composition of the present invention is determined as needed depending on its form, method of administration, intended use, and the age, weight, and symptoms of the patient or animal to which it is administered, and is not fixed. The effective human intake of the composition of the present invention is not fixed, but for example, the weight of the above-mentioned compound, which is the active ingredient, is preferably 100 mg or more, more preferably 500 mg or more, even more preferably 1000 mg or more per day for a human weighing 50 kg, preferably 10 g or less, more preferably 5 g or less, and even more preferably 3 g or less. Furthermore, administration may be carried out as a single dose or in several divided doses within a day, within the desired dosage range. The duration of administration is also arbitrary. The effective human intake of the composition of the present invention refers to the amount of the composition of the present invention that shows an effective effect in humans, and the type of compound contained in the composition is not particularly limited.
[0055] The composition of the present invention is preferably applied to humans, but may also be applied to livestock animals such as cattle, horses, and goats, pet animals such as dogs, cats, and rabbits, or laboratory animals such as mice, rats, guinea pigs, and monkeys. When administered to animals other than humans, the daily dose per rat (approximately 20 g) will vary depending on the amount of active ingredients in the composition, the condition of the subject, weight, sex, and age, etc. For example, the total amount of the above compound is preferably 10 mg / kg or more, more preferably 50 mg / kg or more, even more preferably 100 mg / kg or more, and preferably 1 g / kg or less, more preferably 500 mg / kg or less, and even more preferably 300 mg / kg or less.
[0056] (Use to activate PGC-1α) One aspect of the present invention involves the use of at least one compound selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallylheptanoids, diterpenoids, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanonols, flavanones, flavonols, flavones, and lignans to activate PGC-1α.
[0057] In the present invention, the specific compounds described above can be used. In the use of the present invention, the chalcones include 2-hydroxychalcone, trans-chalcone, isoliquiritigenin, 4'-hydroxychalcone, 2',4'-dihydroxy-4,6'-dimethoxychalcone, and 4-hydroxychalcone. Droxychalcone, 4'-methoxychalcone, butein, 2,3-dimethoxy-2'-hydroxyca Lucone, 2',6'-dihydroxy-4,4'-dimethoxydihydrochalcone, 2',6'-dihydroxy-4 ,4'-dimethoxychalcone, 4-methoxychalcone, and 3,4,2',4',6'-pentahydroxychalcone Lucon is preferred.
[0058] In the use of the present invention, piperlongmine and mahanine are preferred as alkaloids.
[0059] In the use of the present invention, emodin and anthraflavinic acid are preferred as anthraquinones.
[0060] In the use of the present invention, (±)-equol is preferred as the isoflavan.
[0061] In the use of the present invention, isoflavones include 4',6,7-trihydroxyisoflavonoids. 5-methyl-7-methoxy-isoflavones and ipriflavones are preferred.
[0062] In the use of the present invention, urolithin and ellagic acid are preferred as ellagic acid.
[0063] In the use of the present invention, esculetin is preferred as the coumarin.
[0064] In the use of the present invention, curcumin 1, curcumin 2, and curcumin 3 are preferred as diallylheptanoids.
[0065] In the use of the present invention, isosteviol is preferred as the diterpenoid.
[0066] In the use of the present invention, the sesquiterpenes include (-)-trans-caryophyllene and no Tokaton is preferred.
[0067] In the use of the present invention, hederagenin and corosolic acid are preferred as triterpenes.
[0068] In the use of the present invention, dalbergin is preferred as the neoflavonoid.
[0069] In the use of the present invention, apocynin, 3-anisaldehyde, (+)-cuparene, and hydroxytyrosol are preferred as phytochemicals.
[0070] In the use of the present invention, (+)-taxifolin is preferred as the flavanonol.
[0071] In the use of the present invention, preferred flavanones include 4'-methoxyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone, and 6-methoxyflavanone. It seems so.
[0072] In the use of the present invention, preferred flavonols are galangin, 3-methoxyflavone, kaempferol, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, 3',4',5,5',6,7,8-heptamethoxyflavone, fisetin, 6-methoxyflavonol, 7-hydroxyflavonol, and isorhamnetin.
[0073] In the use of the present invention, preferred flavonoids include violanthin, 3',4'-dihydroxyflavone, tangeretin, 2'-methoxyflavone, 7,4'-dihydroxyflavone, chrysoeriol, 3',4'-dimethoxyflavone, flavone, α-naphthoflavone, diosmetin, 4'-methoxyflavone, ougonin, 6-hydroxyflavone, and 5-methoxyflavone. It's nice.
[0074] In the use of the present invention, preferred lignans are eudesmin, (-)-sesamin, honokiol, sesamolin, sesamin, nordihydroguaiaretic acid, sesaminol, sesamol, episesamin, and matairesinol.
[0075] The compounds used in this invention include 3',4'-dihydroxyflavone and 4'-methoxy Cyflavanone, anthraflavic acid, 4'-methoxychalcone, 2'-methoxyflavone, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7-trihydride Roxy-3,4'-dimethoxyflavone, flavone, diosmetine, 5-methyl-7-methoxy-isoflavonone, 4'-methoxyflavone, 6-methoxyflavonol, 6-hydroxyflavone, ipriflavone, 5-methoxyflavone, and matailesinol are more preferred. Using these compounds, the effects of the present invention can be achieved at low concentrations (low content).
[0076] Furthermore, more preferred compounds used in the present invention include 3',4'-dihydroxyflavone, 4'-methoxyflavanone, anthraflavic acid, 4'-methoxychalcone, and 2'-methicone. Toxiflavone, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, flavone, diosmetine, 5- With thyl-7-methoxy-isoflavones, 4'-methoxyflavones, and 6'-methoxyflavonols Yes, these compounds can be used to achieve the effects of the present invention at low concentrations (low content) and over a wide concentration range.
[0077] The use of the present invention includes, but is not limited to, the use of the above-mentioned compounds for purposes such as improving endurance, muscle hypertrophy, obesity suppression, stress reduction, improvement of glucose metabolism function, or suppression of muscle atrophy. Furthermore, such use may be in humans or non-human animals, and may be therapeutic or non-therapeutic. Here, "non-therapeutic" is a concept that does not include medical procedures, i.e., treatment of the human body.
[0078] (Methods for activating PGC-1α) One aspect of the present invention is a method for activating PGC-1α using at least one compound selected from the group consisting of chalcones, alkaloids, anthraquinones, isoflavans, isoflavones, ellagic acid, coumarins, diallylheptanoids, diterpenoids, sesquiterpenes, triterpenes, neoflavones, phytochemicals, flavanonols, flavanones, flavonols, flavones, and lignans. Another aspect of the method is a method for activating PGC-1α, comprising administering a therapeutically effective amount of the above compound as an active ingredient to a subject requiring PGC-1α activation.
[0079] In the method of the present invention, the specific compounds described above can be used. Compounds that are preferably used as chalcones in the method of the present invention are 2-hydroxychalcone, trans-chalcone, isoliquiritigenin, 4'-hydroxychalcone, 2',4'-dihydroxy-4,6'-dimethoxychalcone, 4-hydroxychalcone, 4'-methoxychalcone, butein, 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.
[0080] In the method of the present invention, the compounds preferably used as alkaloids are piperlongmine and mahanine.
[0081] In the method of the present invention, the compounds preferably used as anthraquinones are emodin and anthraflavinic acid.
[0082] In the method of the present invention, the compounds preferably used as isoflavanes are (±)-E It is a quall.
[0083] In the method of the present invention, the compounds preferably used as isoflavones are 4',6,7- These are trihydroxyisoflavones, 5-methyl-7-methoxyisoflavones, and ipriflavones.
[0084] In the method of the present invention, the compounds preferably used as ellagic acid are urolithin and ellagic acid.
[0085] In the method of the present invention, the compound preferably used as a coumarin is esculetin.
[0086] In the method of the present invention, the compounds preferably used as diallylheptanoids are curcumin 1, curcumin 2, and curcumin 3.
[0087] In the method of the present invention, the compound preferably used as a diterpenoid is isosteviol.
[0088] In the method of the present invention, the compounds preferably used as sesquiterpenes are (-)-trans caryophyllene and nookatone.
[0089] In the method of the present invention, the compounds preferably used as triterpenes are hederagenin and corosolic acid.
[0090] In the method of the present invention, the compound preferably used as a neoflavonoid is dalbergine.
[0091] In the method of the present invention, compounds that are preferably used as phytochemicals are apocynin, 3-anisaldehyde, (+)-cuparene, and hydroxytyrosol.
[0092] In the method of the present invention, the compound preferably used as a flavanonol is (+)-taxifolin.
[0093] In the method of the present invention, the compound preferably used as a flavanone is 4'-methyl These are cyflavanone, 2'-hydroxyflavanone, 3'-hydroxyflavanone, flavanone, and 6-methoxyflavanone.
[0094] In the method of the present invention, compounds preferably used as flavonols are galangin, 3-methoxyflavone, kaempferol, and 3',5,7-trihydroxy-3,4'-dimethoxyflavone. Bon, 3',4',5,5',6,7,8-heptamethoxyflavone, fisetin, 6-methoxyflavonol These are 7-hydroxyflavonol and isorhamnetin.
[0095] In the method of the present invention, compounds that are preferably used as flavonoids are violanthin, 3',4'-dihydroxyflavone, tangeretin, 2'-methoxyflavone, 7,4'-dihydroxyflavone, chrysoeriol, 3',4'-dimethoxyflavone, flavone, and α-naphthoflavone. These are von, diosmetine, 4'-methoxyflavone, ougonin, 6-hydroxyflavone, and 5-methoxyflavone.
[0096] In the method of the present invention, compounds that are preferably used as lignans are eudesmin, (-)-sesamin, honokiol, sesamolin, sesamin, nordihydroguaiaretic acid, sesaminol, sesamol, episesamin, and matairesinol.
[0097] The compounds used in the method of the present invention include 3',4'-dihydroxyflavone, 4'- Methoxyflavanone, anthraflavic acid, 4'-methoxychalcone, 2'-methoxyflavone, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7- Dihydroxy-3,4'-dimethoxyflavone, flavone, diosmetine, 5-methyl-7-methoxy C-Isoflavone, 4'-Methoxyflavone, 6-Methoxyflavonol, 6-Hydroxyflavonol Bon, ipriflavone, 5-methoxyflavone, and matairesinol are more preferred. Using these compounds, the effects of the present invention can be achieved at low concentrations (low content).
[0098] Furthermore, more preferred compounds used in the method of the present invention include 3',4'-dihydroxyflavone, 4'-methoxyflavanone, anthraflavic acid, 4'-methoxychalcone, and 2'-methoxy These compounds include flavones, butein, 2,3-dimethoxy-2'-hydroxychalcone, 4-methoxychalcone, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, flavones, diosmetine, 5-methyl-7-methoxy-isoflavonone, 4'-methoxyflavone, and 6-methoxyflavonol. Using these compounds, the effects of the present invention can be achieved at low concentrations (low content) and over a wide concentration range.
[0099] In the above method, the target subject requiring PGC-1α activation is the same as the target subject to which the composition of the present invention is applied. Furthermore, in this specification, the therapeutically effective dose is the amount by which PGC-1α is activated when the composition of the present invention is administered to the above subject compared to a subject that does not receive the composition. The specific effective dose is not fixed and is determined on a case-by-case basis depending on the form of administration, method of administration, purpose of use, and the age, weight, symptoms, etc. of the subject.
[0100] In the method of the present invention, the above-mentioned compound may be administered as is or as a composition containing the above-mentioned compound in order to reach the therapeutically effective amount.
[0101] According to the method of the present invention, it is possible to activate PGC-1α without causing side effects. [Examples]
[0102] The present invention will be described in more detail below with reference to examples, but this will not limit the scope of the invention. Those skilled in the art can use the method of the present invention in various modified and adapted ways, and these are also included within the scope of the invention. All of the following examples were carried out at Shizuoka Prefectural University.
[0103] Commercially available human fetal kidney-derived HEK293T cells were placed in D-MEM (10% FBS + antibiotic medium containing penicillin, streptomycin, and amphotericin B) in a 60mm petri dish and subcultured in a CO2 incubator at 37°C, 5% CO2 + 95% air, and 100% humidity. After confirming that the cell density reached 70-90% confluence, the HEK293T cells were washed with PBS, then treated with trypsin solution (0.05% (w / v) trypsin, 0.53 mM EDTA·4Na), and the detached cells were collected by centrifugation at 1,200 rpm. The collected cells were resuspended in D-MEM (containing 10% FBS), the cell count was measured, and the cells were used for subculturing and testing.
[0104] A cDNA conjugated between yeast-derived GAL4DBD (GAL4-DNA Binding Domain) and mouse-derived PGC-1α was inserted into an expression plasmid to create a PGC-1α plasmid. This PGC-1α plasmid and a UAS sequence-containing plasmid were used. Furthermore, an internal standard plasmid containing the luciferase gene was introduced into HEK293T cells.
[0105] HEK293T cells, after gene transfer, were cultured in a CO2 incubator at 37°C, 5% CO2 + 95% air, and 100% humidity for 24 hours. Subsequently, the test substance, dissolved in water or DMSO, was added to a final concentration of 1 μg / mL or 10 μg / mL.
[0106] Luciferase (Luc) activity was measured 24 hours after adding the test substance, and this value was divided by the internal standard Luc activity to determine the PGC-1α activity. Furthermore, to evaluate the PGC-1α activity of the test substances, the PGC-1α activity of water or DMSO was set as 100%, and the PGC-1α activity of all test substances was expressed as a relative percentage. The results are shown in the table below.
[0107] [Table 2]
[0108] [Table 3-1] [Table 3-2]
[0109] As described above, compounds whose measured values (relative percentage) exceeded 200% when the final concentration was 1 μg / mL or 10 μg / mL were all shown to have the ability to activate PGC-1α. In addition, 3',4'-dihydroxyflavone, 4'-methoxyflavanone, anthraflavic acid, and 4'-dihydroxyflavone were all shown to have the ability to activate PGC-1α. '-Methoxychalcone, 2'-Methoxyflavone, Butein, 2,3-Dimethoxy-2'-Hydroxy Chalcone, 4-methoxychalcone, 3',5,7-trihydroxy-3,4'-dimethoxyflavone, f Lavons, diosmetine, 5-methyl-7-methoxy-isoflavones, 4'-methoxyflavones, and For 6-methoxyflavonol, the measured values exceeded 200% at both final concentrations of 1 μg / mL and 10 μg / mL. In addition, 31 other compounds were tested, and it was confirmed that these compounds did not exhibit PGC-1α activating ability. [Industrial applicability]
[0110] This invention provides a composition useful for activating PGC-1α, which contains a predetermined compound as an active ingredient. Because this invention provides a novel means for improving endurance, muscle hypertrophy, obesity suppression, stress reduction, improved glucose metabolism, and suppression of muscle atrophy, it has high industrial applicability.
Claims
1. A PGC-1α activating composition comprising at least one compound selected from the group consisting of sesamin, episesamin, (-)-sesamin, and sesamolin, wherein the composition is for inhibiting muscle atrophy, and the content of the compound is 0.5% by weight or more.
2. The composition according to claim 1, wherein the function exhibited by the activation of PGC-1α is indicated.
3. The composition according to claim 2, wherein the function indication is selected from the group consisting of "maintain muscle," "suppress muscle atrophy," "prevent muscle loss," "suppress muscle loss," "prevent muscle deterioration," and "suppress muscle deterioration."
Citation Information
Patent Citations
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