Composition for improving fatigue, improving exercise performance, or improving endurance
By using a composition of gallate and isoquercetin during exercise, the accumulation of lactic acid in myocytes and the number of mitochondria is inhibited, and the fatigue caused by energy depletion during exercise is solved, which significantly improves exercise execution ability and endurance.
Patent Information
- Application Number
- CN202411416977.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-10-11
- Filing Date
- 2024-10-11
- Publication Date
- 2025-04-11
AI Technical Summary
The energy in the body is depleted sharply during exercise, resulting in insufficient ATP production and causing muscle fatigue and pain. The existing technology is difficult to effectively solve this problem.
A composition containing gallocatechin Gallate (GCG) and isoquercitrin (IQC) as active ingredients is provided, which increases intracellular mitochondria by inhibiting the accumulation of lactic acid in myocytes, thereby enhancing energy generation ability.
It significantly inhibits the accumulation of lactic acid in myocytes, increases the number of mitochondria, improves energy generation ability during exercise, reduces fatigue and pain, and improves exercise execution ability and endurance.
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Figure CN119792324A_ABST
Abstract
Description
Technical Field
[0001] This specification discloses a composition for improving fatigue, improving sports performance or improving endurance. Background Art
[0002] In order to produce a large amount of ATP, the oxidative phosphorylation reaction as the energy metabolism of aerobic respiration by mitochondria is necessary. However, such oxidative phosphorylation reaction has the disadvantage that the ATP generation rate is slow. In the case of rapid exhaustion of energy in the body due to exercise, if the ATP amount generated is insufficient compared with the ATP consumed, then a large amount of ATP supplied by oxidative phosphorylation is replaced, and ATP is quickly supplied through an anaerobic process. The representative anaerobic ATP supply process is lactic acid fermentation, and pyruvic acid is directly converted into lactic acid by lactate dehydrogenase, and a small amount of ATP generated in this process is used as an energy source, and is converted into acetyl-CoA and passes through a citric acid cycle and an electron transfer system after being generated as pyruvic acid by a sugar decomposition process to replace glucose. The lactic acid accumulated in this process induces muscle fatigue and pain, and lactic acid is considered to be a representative fatigue mark for this.
[0003] Patent document: (Patent document 1) Korean Patent KR2022-0145604A Summary of the invention
[0004] An object of the present invention is to provide a composition for improving fatigue, improving sports performance or improving endurance.
[0005] In order to achieve the above object, the present invention provides a composition for improving fatigue, improving exercise performance or improving endurance, comprising gallocatechin gallate (GCG) and isoquercetin (IQC) as active ingredients.
[0006] On one hand, the composition of the present invention comprises epigallocatechin gallate and isoquercetin composite components to effectively inhibit the accumulation of lactic acid in muscle cells and significantly increase the mitochondria in cells, thereby promoting the generation of energy in situations where energy is required, such as during exercise, or in daily life, thereby improving exercise ability or reducing fatigue. The composition can be used as a material for food or medicine as an agent for improving exercise performance, endurance, and fatigue prevention and improvement. BRIEF DESCRIPTION OF THE DRAWINGS
[0007] Figure 1The inhibitory effects of gallocatechin gallate (GCG) and isoquercetin (IQC) mixture (AdiPhenon) on the expression of genes related to lactic acid fermentation in muscle cells were compared according to the composition ratio.
[0008] Figure 2 The inhibitory effect of lactic acid accumulation in myocytes was compared according to the composition ratio of the mixture.
[0009] Figure 3 The inhibitory effect of lactic acid accumulation in myocytes according to the detailed composition ratio of the mixture was compared.
[0010] Figure 4 Involves mitochondrial-related gene expression in myocytes via a mixture.
[0011] Figure 5 Promotion of fat oxidation gene expression in myocytes involving a mixture.
[0012] Figure 6 Involves an increase in mitochondria within myocytes via the mixture.
[0013] exist Figures 1 to 6 The experimental groups with statistically significant differences (P<0.05) are represented by different marks. DETAILED DESCRIPTION
[0014] Hereinafter, the present invention will be described in detail.
[0015] The present invention relates to a composition for improving fatigue, improving exercise performance or improving endurance, comprising gallocatechin gallate (GCG) and isoquercetin (IQC) as active ingredients.
[0016] In an exemplary implementation example, the epigallocatechin gallate and isoquercetin may be included in a weight ratio of 9:1 or more, 8:2 or more, 7:3 or more, 6:4 or more, 5:5 or more, or 4:6 or more, and may be included in a weight ratio of 1:9 or less or 2:8 or less. For example, the epigallocatechin gallate and isoquercetin may be included in a weight ratio of 9:1 to 1:9, but is not limited thereto.
[0017] In an exemplary implementation example, the epigallocatechin gallate and isoquercetin can be included in a weight ratio of 1:1 or more, 1:1.1 or more, 1:1.2 or more, 1:1.3 or more, 1:1.4 or more, 1:1.5 or more, 1:1.6 or more, 1:1.7 or more, 1:1.8 or more, 1:1.9 or more, 1:2.0 or more, 1:2.1 or more, 1:2.2 or more, and can be included in a weight ratio of less than 1:9, less than 1:8, less than 1:7, less than 1:6, less than 1:5, less than 1:4, less than 1:3.5, less than 1:3.4, less than 1:3.3, less than 1:3.2, less than 1:3.1, less than 1:3, less than 1:2.9, less than 1:2.8, less than 1:2.7, less than 1:2.6 or less than 1:2.5. When the epigallocatechin gallate and isoquercetin are included in the weight ratio, fatigue can be improved, or exercise performance or endurance can be improved. For example, the epigallocatechin gallate and isoquercetin can be included in a weight ratio of 1:1 to 1:9 or 1:1.5 to 1:4, but is not limited thereto.
[0018] In this specification, the term "apply" means providing the composition to an applicable subject by any appropriate method, including administration, application, absorption and ingestion, etc. In this case, the applicable subject means all animals such as humans, monkeys, dogs, goats, pigs or mice to which the composition can be applied.
[0019] In an exemplary implementation, the composition may be characterized as being suitable for a subject in need of inhibiting lactic acid accumulation in muscle cells.
[0020] In an exemplary implementation, the composition may be characterized as being suitable for a subject in need of reducing the expression of the LDHA (Lactate dehydrogenase A) gene.
[0021] In an exemplary implementation, the composition can be characterized as being suitable for use in a subject in need of increased aerobic energy metabolism.
[0022] In an exemplary implementation, the composition may be characterized in that it is suitable for a subject that needs to increase the expression of mitochondrial or fat oxidation related genes, the mitochondrial related gene may be NDUFA9 (NADH: ubiquinoneoxidoreductase subunit A9) or COX4 (Cytochrome COxidase Subunit 4) gene, and the fat oxidation related gene may be ACO (Acyl-CoA Oxidase) or CPT-1 (Carnitine-Palmitoyl Transferase1) gene.
[0023] In an exemplary implementation, the composition can be characterized as being suitable for use in a subject in need of increasing mitochondria in muscle cells.
[0024] In an exemplary implementation example, the daily applicable amount of the active ingredient of the composition can be 5 mg / kg or more, 6 mg / kg or more, 7 mg / kg or more, 8 mg / kg or more, 9 mg / kg or more, 10 mg / kg or more, 20 mg / kg or more, 30 mg / kg or more, 40 mg / kg or more, 50 mg / kg or more, 60 mg / kg or more, 70 mg / kg or more, 80 mg / kg or more, 90 mg / kg or more, 100 mg / kg or more, 1 g / kg or more, 2 g / kg or more, 3 g / kg or more, 4 g / kg or more, 5 g / kg or more, or 6 g / kg or more, and can be less than 60 g / kg, less than 59 g / kg, less than 58 g / kg, less than 57 g / kg, less than 56 g / kg, less than 55 g / kg, less than 54 g / kg, less than 53 g / kg, less than 52 g / kg, or less than 51 g / kg. It can be that fatigue improvement, exercise execution ability improvement or endurance improvement effect are excellent under the applicable amount, fatigue improvement, exercise execution ability improvement or endurance improvement effect are small when it is lower than the applicable amount, and toxicity and other problems occur when it is higher than the applicable amount. The application can also be applied once a day to multiple times. For example, it can be applied 2 to 24 times a day, 1 to 2 times in 3 days, 1 to 6 times a week, 1 to 10 times in 2 weeks, 1 to 15 times in 3 weeks, 1 to 3 times in 4 weeks, or 1 to 12 times a year, but is not limited to this.
[0025] In an exemplary implementation, the composition may be a food composition.
[0026] In an exemplary implementation example, when the composition is used as an additive for health functional food, it can be added as it is or used together with other food or food ingredients, and can be used appropriately according to the usual method. The mixing amount of the active ingredient can be appropriately determined according to the purpose of use such as prevention, health or treatment. The dosage form of health functional food can be not only in the form of powder, granules, pills, tablets, capsules, but also in any form of ordinary food or beverage.
[0027] In an exemplary implementation example, there is no particular limitation on the types of health functional foods. Examples of foods to which the composition can be added include meat, cakes, noodles, chewing gum, dairy products including ice cream, various soups, beverages, teas, oral liquids, alcoholic beverages, and vitamin complexes, etc., which can include all foods in the usual sense.
[0028] In an exemplary implementation example, when preparing the health functional food or beverage, the composition can be added in an amount of 15 parts by weight or less, preferably 10 parts by weight or less, relative to 100 parts by weight of the raw material. However, in the case of long-term intake for the purpose of health and hygiene or for the purpose of health regulation, the amount can be below the range.
[0029] In an exemplary implementation example, the beverage in the health functional food may contain various flavorings or natural carbohydrates as additional ingredients like ordinary beverages. The above-mentioned natural carbohydrates may be monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, sugar alcohols such as xylitol, sorbitol, and erythritol. As sweeteners, natural sweeteners such as thaumatin and stevia extract, saccharin, and synthetic sweeteners such as aspartame may be used. The proportion of the natural carbohydrates may be about 0.01 to 0.04 g per 100 ml of beverage according to the present invention, preferably about 0.02 to 0.03 g, but is not limited thereto.
[0030] In an exemplary implementation example, in addition to the above, the health functional food according to the present invention may also contain various nutrients, vitamins, electrolytes, flavoring agents, colorants, pectin acid and its salts, alginic acid and its salts, organic acids, protective colloid thickeners, pH regulators, stabilizers, preservatives, glycerol, alcohol, and carbonating agents used in carbonated beverages. In addition, the health functional food according to the present invention may contain pulp for the preparation of natural fruit juices, fruit juice drinks, and vegetable drinks. These ingredients can be used independently or in combination. The proportion of these additives is not limited, but is generally selected within the range of 0.01 to 0.1 parts by weight compared to every 100 parts by weight of the health functional food according to the present invention.
[0031] In another aspect, the present invention is a method for improving fatigue, enhancing exercise performance or improving endurance, comprising administering a composition comprising an effective amount of gallocatechin gallate (GCG) and isoquercitrin (IQC) to a subject.
[0032] In yet another aspect, the present invention is a use of gallocatechin gallate (GCG) and isoquercitrin (IQC) for preparing a composition for improving fatigue, enhancing exercise performance or endurance.
[0033] In yet another aspect, the present invention provides gallocatechin gallate (GCG) and isoquercitrin (IQC) for improving fatigue, enhancing exercise performance or enhancing endurance.
[0034] In yet another aspect, the present invention is a non-therapeutic use of gallocatechin gallate (GCG) and isoquercitrin (IQC) for improving fatigue, enhancing exercise performance or enhancing endurance.
[0035] The following examples are given to more specifically describe the configuration and effects of the present invention. However, the following examples are provided for the purpose of illustration only to help understanding of the present invention, and the scope and range of the present invention are not limited thereto.
[0036] [Example]
[0037] [Example 1]
[0038] Comparison of the inhibitory effects of gallocatechin gallate (GCG) and isoquercitrin (IQC) mixture (AdiPhenon) on the accumulation of fatigue substances in muscle cells
[0039] In order to confirm whether the accumulation of lactic acid in muscle cells is suppressed, mouse myofibroblast C2C12 cells were purchased from ATCC and cultured in Dulbecco's Modified Eagle's Medium (DMEM; SigmaAldrich) containing 10% fetal bovine serum (Gibco) and 1% penicillin / streptomycin (P / S; Sigma Aldrich). When C2C12 cells were 100% full in the culture dish, they were differentiated into muscle cells using DMEM medium containing 2% horse serum (Gibco) and 1% P / S. Differentiation into muscle cells takes about 7 days, and the medium is changed every day during the differentiation of muscle cells.
[0040] If cells are treated with CoCl2, they will recognize hypoxia and start lactic acid fermentation even in the presence of oxygen. CoCl2 can be used to induce lactic acid accumulation in cells. In order to confirm whether a mixture of gallocatechin gallate (GCG) and isoquercetin (IQC) (AdiPhenon) can inhibit lactic acid accumulation in muscle cells, differentiated muscle cells were pre-treated with a mixture of various ratios (GCG:IQC = 10:0 to 0:10) and then treated with CoCl2 (100 μM; Sigma Aldrich) for 24 hours. The culture medium was then recovered and used to measure the amount of accumulated lactic acid, and the cells were washed with phosphate buffered saline (PBS) and used in RNA expression measurement experiments. The recovered cells were used to extract RNA using TaKaRa MiniBEST Universal RNA Extraction Kit (Takara Bio) and the same amount of RNA (1 mg) was used to extract RNA using RevertAid 1 stcDNA was synthesized using the RevertAid First-strand cDNA Synthesis Kit (Thermo Fisher Scientific). The expression of genes related to lactic acid fermentation (lactate dehydrogenase A) was observed using a CFX96 thermocycler (Bio-Rad), and the amount of accumulated lactic acid was quantified using a Lactate Assay Kit (Sigma-Aldrich).
[0041] The results, such as Figure 1 as well as Figure 2 As shown, the inhibitory effect of lactic acid fermentation in muscle cells by the mixtures of various composition ratios was confirmed, and the effect was most excellent when the ratio of GCG:IQC was between 4:6 and 2:8.
[0042] [Example 2]
[0043] Comparison of effects according to mixture ratio
[0044] In the results of Example 1, the mixture inhibited the accumulation of lactic acid by CoCl2 treatment, and the lactic acid accumulation inhibition effect was manifested differently depending on the composition ratio of the mixture. In order to confirm the optimal composition ratio of GCG and IQC constituting the mixture, the GCG:IQC ratio (4:6 to 2:8) that exhibited the most excellent lactic acid accumulation inhibition effect was slightly further subdivided to compare the lactic acid accumulation inhibition effect.
[0045] The results, such as Figure 3 As shown in the figure, it can be seen that the lactic acid accumulation inhibition effect is most excellent when the GCG:IQC ratio is 1:2.4. In the following examples, the mixture composition ratio is set to GCG:IQC=1:2.4 and the experiment is performed.
[0046] [Example 3]
[0047] Comparison of activation of energy metabolism in myocytes treated with the mixture
[0048] In order to confirm whether the lactate accumulation inhibitory effect of the mixture is due to the increase in aerobic energy metabolism, differentiated muscle cells were treated with the mixture at various concentrations (10, 50, and 100 μg / ml) for 24 hours, and the expression of mitochondrial and fat oxidation-related genes was confirmed.
[0049] The results, such as Figure 4 as well as Figure 5 As shown, the expression levels of mitochondrial constituents and fat oxidation-related genes increased in a concentration-dependent manner by the mixture treatment.
[0050] Next, in order to investigate whether the mitochondria in muscle cells were actually increased by the mixture treatment, the cells were treated with the mixture under the same conditions, washed with PBS, and subjected to Mitotracker for 30 minutes. TM Mitochondria were stained by treatment with Green FM (mitochondrial green fluorescent probe, 20 nM; Invitrogen), and the stained cells were washed twice with PBS to remove residual Mitotracker, and the fluorescence value (ex 490 nm, em 512 nm) was measured using TECAN Infinite M200 Microplate Reader.
[0051] The results, such as Figure 6 As shown in Figure 2, it was confirmed that the amount of mitochondria in muscle cells increased when the mixture was treated, which was consistent with the Figure 4 The results were consistent with the results that the expression of mitochondrial-related genes was increased by the mixture treatment.
Claims
1. A fatigue-relieving composition comprising gallocatechin gallate (GCG) and isoquercitrin (IQC) as active ingredients.
2. A composition for improving sports performance, comprising gallocatechin gallate (GCG) and isoquercitrin (IQC) as active ingredients.
3. A composition for improving endurance, comprising gallocatechin gallate (GCG) and isoquercitrin (IQC) as active ingredients.
4. The composition according to any one of claims 1 to 3, wherein The composition includes gallocatechin gallate (GCG) and isoquercitrin (IQC) in a weight ratio of 9:1 to 1:
9.
5. The composition according to any one of claims 1 to 3, wherein The composition is suitable for a subject in need of inhibiting lactic acid accumulation in muscle cells.
6. The composition according to any one of claims 1 to 3, wherein The composition is suitable for a subject in need of increasing aerobic energy metabolism.
7. The composition according to any one of claims 1 to 3, wherein The composition is suitable for a subject in need of increasing the expression of mitochondrial or fat oxidation related genes.
8. The composition according to any one of claims 1 to 3, wherein The composition is suitable for a subject in need of increasing mitochondria in muscle cells.
9. The composition according to any one of claims 1 to 3, wherein The composition is a food composition.