WO2011122872A2 - 쿠메스트롤 또는 쿠메스트롤을 포함하는 콩 추출물 포함 조성물 - Google Patents
쿠메스트롤 또는 쿠메스트롤을 포함하는 콩 추출물 포함 조성물 Download PDFInfo
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Definitions
- the present invention relates to a composition for activating mitochondria.
- Mitochondria are intracellular organelles that are present in most eukaryotic cells and have their own mitochondrial DNA (mtDNA), which is separated from nuclear DNA.
- mtDNA mitochondrial DNA
- the main function of mitochondria is to produce ATP, an intracellular energy source. ATP is produced in the electron transport system using NADH, FADH 2 , which is produced via the TCA circuit in the mitochondrial substrate. The ATP thus produced is used for many biosynthetic and metabolic processes that require energy.
- mitochondria store calcium ions in the substrate, which play an important role in intracellular signal transduction, and supply the cytoplasm when needed. In addition, it is known to play a role in regulating cell death, proliferation, metabolism, and the like.
- Mitochondrial DNA unlike nuclear DNA in cells, does not have its own repair mechanism, and is relatively prone to damage because it lacks histone proteins that protect DNA. Damage to mitochondrial DNA decreases the function of mitochondria, reducing the synthesis of ATP, an energy source necessary for cellular activity, and causing the development of various mitochondrial related diseases.
- One aspect of the present invention is to provide a composition for activating mitochondria.
- One aspect of the present invention provides a composition for activating mitochondria, including Kumestrol or soybean extract including Kumestrol as an active ingredient.
- the composition according to one aspect of the present invention may include Kumestrol or soybean extract including Kumestrol as an active ingredient, thereby activating SIRT1 and increasing the amount of mitochondria in the cell. Therefore, the composition promotes energy metabolism to exhibit fatigue recovery, endurance improvement, muscle strength improvement, or exercise function improvement effect, and may reduce or reduce body fat to prevent or improve obesity, hyperlipidemia or hypertension. The composition may also prevent or ameliorate mitochondrial related diseases.
- 1 is a graph showing the degree of increase in SIRT1 activity by cumestrol.
- FIG. 1 shows mitochondrial related genes with increased expression by cumestrol.
- 3 is a graph showing the degree of increase in mitochondria in muscle cells by cumestrol.
- extract includes any material obtained by extracting a component therefrom from a natural product, regardless of the method of extraction or the kind of the component.
- extract includes all the components which are dissolved in a solvent from a natural product using water or an organic solvent, and those obtained by extracting only a specific component such as an oil such as oil.
- One aspect of the present invention is cumestrol; Or it provides a composition for activating mitochondria comprising a natural product or an extract thereof including the cumestrol as an active ingredient.
- Cumestrol 3,9-dihydroxy-6H-benzofuro (3,2-c) (1) benzopyran-6-one
- CMS 3,9-dihydroxy-6H-benzofuro (3,2-c)
- benzopyran-6-one has a structure as shown in Formula 1 below.
- Coumestrol is one of the phytoestrogens found primarily in the seeds, roots or leaves of legumes, comositae plants. It is a kind of isoflavonoid that can be classified as a coumestan-based compound and is known to have an estrogen effect.
- compositions according to one aspect of the present invention include cumestrol, or natural products or extracts thereof including cumestrol.
- natural products including cumestrol include at least one legume selected from soybeans, peas, green beans and germinated soybeans, red shamrock, purple forsythia (alfalfa) or sprout cabbage.
- the natural product comprising cumestrol may be soybean.
- the soybean can be used without particular limitation so long as the legumes containing cumestrol.
- the kind of beans that can be used in the present invention may be varieties for tofu and tofu, for herbs, for rice or for soybeans.
- tofu and tofu Daepoong, Hojang, Jangwon, Rhubarb, Sodam, Songhak, Daewon, Genuine, and protein ), Soy milk, Shinpaldal, Taekwang, Great Wall, Longevity, Wuhan, Baiyun, New Egg, Golden and Long Leaf. .
- Varieties for herbs include mythology, wishes, Anpyeong, southwest, colorful, sorok, soho, vocation, tea garden, and fengshan Herbs, Iksan Herbs, Sobaek Herbs, Gwang'an, Single Leaf, and Galaxy.
- rice varieties include celadon, black blue, black sea flakes, black and white, black soybeans and one black soybeans.
- varieties for green soybeans include Daol, fresh green, birds, black, sorghum green beans, Hwaeum green soybeans, and large greens.
- the soybean is preferably a variety capable of germinating and resistant to pests.
- Such beans include, for example, myths, wishes, Anpyeong, southwest, colorful, sorok, soho, vocation, and tea gardens. ), Pungsan greens, Iksan greens, Sobaek greens, Gwangan, single leaves and galaxies.
- the natural product or extract thereof may comprise a large amount of cumetrol, specifically 0.01 to 50% by weight, more specifically 0.1 to 30% by weight, based on the total weight of the natural product or extract thereof. Can be.
- the extract of the natural product containing cumestrol is completely concentrated after extracting the natural product containing cumestrol in water or ethanol at room temperature or immersed in water and then dispersed again in water, the same amount of hexane , Dichloromethane, chloroform, ethyl acetate, butanol, ethanol, methanol, and water.
- the extraction method is not limited thereto, and any extraction method may be used such that the final extract contains cumestrol.
- mitochondria break down glucose through cellular respiration to synthesize ATP, which is the basic energy of physical life. Therefore, if mitochondria do not work normally, the cells will die, and further affect tissues and organs.
- the abnormal action of mitochondria causes disorders and metabolic disorders, particularly of nerve and muscle tissue, and is also a cause of aging.
- composition according to an aspect of the present invention as an active ingredient may increase the activity of SIRT1 (sirtuin 1) to promote the activity of mitochondria.
- SIRT1 is a NAD-dependent deacetylase, involved in the production of mitochondria.
- composition according to one aspect of the present invention includes cumestrol as an active ingredient, promotes energy metabolism by promoting the activity of SIRT1 and mitochondria, thereby promoting fatigue recovery, endurance improvement, muscle strength improvement or exercise function improvement. Can be.
- cumestrol as an active ingredient, promotes energy metabolism by promoting the activity of SIRT1 and mitochondria, thereby promoting fatigue recovery, endurance improvement, muscle strength improvement or exercise function improvement. Can be.
- by increasing the amount of energy used in the body to reduce body fat can prevent or improve obesity, hyperlipidemia or hypertension.
- composition according to one aspect of the present invention may include cumestrol as an active ingredient to prevent or ameliorate mitochondrial related diseases.
- mitochondrial related diseases include one or more of neuropsychiatric, cardiovascular, visceral, endocrine, sensory, joint and muscle diseases caused by decreased mitochondrial activity.
- the neuropsychiatric disorders include, but are not limited to, one or more of dementia, Parkinson's disease, stroke, neuropsychiatric disorders, autism, mental retardation, seizure, stroke-like seizures, migraine and nerve pain It doesn't happen.
- the above diseases can be caused by free radical accumulation and neural tissue disorders caused by reduced mitochondrial activity.
- cardiovascular diseases include heart dysfunction, heart attack, cardiomyopathy, tachycadia, sideroblastic anemia, Pearson syndrome, refractory anemia And hypotension, but is not limited thereto. These diseases can be caused by overloading of calcium ions or excessive oxidative stress, which can cause heart function problems due to reduced mitochondrial activity.
- the visceral diseases include liver failure, intestinal pseudo-obstruction, irritable bowel syndrome, gastroesophageal reflux disease, constipation, diarrhea, renal tubular acidosis and fanconi syndrome. syndromes), including but not limited to.
- the above diseases may be caused by a decrease in mitochondrial activity, damage to the mitochondrial respiratory system, and increased oxidative stress.
- the endocrine disease is at least one of extra pancreatic dysfunction, hypothyroidism, hypothyroidism, hypogonadism, delayed development, type 2 diabetes and hypoglycemia It includes, but is not limited to.
- Stomach diseases can be caused by endocrine disorders due to mitochondrial abnormalities.
- sensory diseases include, but are not limited to, optic nerve atrophy, strabismus, retinitis pigmentosa, blindness and hearing loss.
- Stomach diseases can be caused by sensory abnormalities due to reduced mitochondrial function.
- the joint disease includes, but is not limited to, one or more of degenerative arthritis, rheumatoid arthritis and osteoarthritis. These diseases may be caused by increased expression of inflammation-related factors such as COX-2 (Cyclooxygenase 2) in chondrocytes due to reduced mitochondrial activity.
- COX-2 Cyclooxygenase 2
- the muscle disease is ataxia, dysarthria, dysphagia, spasticity, encephalopathy, myalgia, muscular dystrophy, muscle cramps, ptosis, eye muscle paralysis, It includes, but is not limited to, progressive extraocular palsy, Leber's hereditary optic neuropathy, respiratory disorders, reflex decline, and autonomic ataxia.
- the above diseases are mainly caused by a decrease in the activity of mitochondria, inhibiting the production of ATP, which is an energy source in the body, resulting in muscle weakness caused by poor metabolism of muscles, exercise intolerance due to muscle wasting, and fatigue caused by this.
- Kumetrol or a composition comprising a soybean extract comprising the cumestrol according to an aspect of the present invention can activate or promote the production of mitochondria to prevent or ameliorate the diseases caused by mitochondrial degradation.
- the composition according to one aspect of the present invention comprises a soybean extract comprising 0.001 to 30% by weight, specifically 0.01 to 10% by weight, more specifically 0.1 to 5% by weight of cumestrol or cumestrol relative to the total weight of the composition. can do.
- weight percent not only is it appropriate to exhibit the intended effect of the present invention, but also satisfies both the stability and safety of the composition, it may be appropriate to be included in the above range in terms of cost-effectiveness.
- a composition comprising an extract of soybean including cumestrol or cumestrol may be a food composition.
- the food composition may be a health food composition.
- the food composition may be formulated in various forms, including, but not limited to, powders, granules, tablets, capsules and drinks.
- the food composition may include one or two or more of the following additives as necessary.
- the additives include concentrated juices or powder juices such as grapes, apples, oranges, lemons, pineapples, bananas, pears; Palmitic acid retinol, riboflavin, pyridoxine, cyanocobalamine, ascorbic acid, nicotinic acid amide, calcium pantothenate, folic acid, biotin, cholecalciferol, cholinergic tartaric acid, tocopherol, ⁇ -carotene, etc.
- Water-soluble or fat-soluble vitamins Flavoring agents such as lemon flavor, orange flavor, strawberry flavor, grape flavor and vanilla essence; Amino acids, nucleic acids or salts thereof such as glutamic acid, sodium glutamate, glycine, alanine, aspartic acid, sodium aspartic acid or inosinic acid; Plant fibers such as polydextrose, pectin, xanthan gum, glucomannan and alginic acid; Or sodium chloride, magnesium sulfate, potassium chloride, magnesium chloride, magnesium carbonate, calcium chloride, dipotassium phosphate, monosodium phosphate, calcium glycerophosphate, sodium ferrous citrate, ammonium ferric citrate, iron citrate, manganese sulfate, copper sulfate, Minerals such as sodium iodide, potassium sorbate, zinc, manganese, copper, iodine or cobalt and the like are exemplified.
- a composition including a cumetrol or a soybean extract including the cumestrol may be a pharmaceutical composition.
- the pharmaceutical composition may further include pharmaceutical adjuvants such as preservatives, stabilizers, hydrating or emulsifying accelerators, salts and / or buffers for controlling osmotic pressure, and other therapeutically useful substances, and various oral methods according to conventional methods. Or in parenteral dosage forms.
- pharmaceutical adjuvants such as preservatives, stabilizers, hydrating or emulsifying accelerators, salts and / or buffers for controlling osmotic pressure, and other therapeutically useful substances, and various oral methods according to conventional methods. Or in parenteral dosage forms.
- Formulations for oral administration include tablets, pills, hard and soft capsules, solutions, suspensions, emulsifiers, syrups, granules, etc. These formulations may contain, in addition to the active ingredient, diluents (e.g., lactose, dextrose, water, Cros, mannitol, sorbitol, cellulose and glycine), glidants such as silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols.
- diluents e.g., lactose, dextrose, water, Cros, mannitol, sorbitol, cellulose and glycine
- glidants such as silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols.
- parenteral formulations are injectable formulations, preferably aqueous isotonic solutions or suspensions.
- Determination of dosage of the active ingredient is within the level of those skilled in the art, and the daily dosage of the drug according to the present invention depends on various factors such as disease progression, time of onset, age, health condition, complications, etc. of the subject to be administered. However, based on an adult, generally 1 to 500 mg / kg, preferably 30 to 200 mg / kg of the composition according to the present invention may be administered in divided doses once or twice a day. The method does not limit the scope of the present invention.
- test examples are provided for the purpose of illustration only to help the understanding of the present invention, and the scope and scope of the present invention are not limited thereto.
- the SIRT1 Activity Assay Kit (Biomol) was treated with 10 ⁇ M of cumestrol to assess whether cumestrol can activate SIRT1.
- As a positive control 50 M of resveratrol (Res; resveratrol), which is known as a SIRT1 activator, and 1 mM of nicotinamide (NAM), an inhibitor of SIRT1, were used as a negative control. It was shown in Figure 1 by calculating the degree of SIRT1 activity of each group compared to the untreated group.
- CMS cumestrol
- this effect was comparable to resveratrol treated at very high concentrations compared to cumestrol.
- Kumestrol is therefore thought to be far more effective than resveratrol, known as the SIRT1 activator.
- the composition containing cumestrol may activate SIRT1 to inhibit aging, promote energy metabolism, and further improve fatigue recovery, endurance, strength and motor function.
- Mouse-derived C2C12 muscle cells (mouse fibroblast, ATCC) were differentiated for a week and then treated with 10 M of cumestrol for 24 hours. Since the expression of protein levels of mitochondrial related genes were confirmed by Western blotting, it is shown in Figure 2.
- the genes used in the test were PGC1, which induces mitochondrial biosynthesis, and NDUFA9 and ATP5a, proteins that make up the mitochondrial electron transport system. As can be seen in Figure 2, the treatment of cumestrol significantly increases the expression of the genes compared to the untreated group.
- the graph showing the degree of mitochondria increase compared to the untreated group when treated with cumestrol in FIG. .
- the amount of mitochondria in cells is greatly increased when the cumestrol is treated.
- cumestrol increases mitochondrial biosynthesis in muscle cells. Therefore, the composition containing cumestrol may increase the amount of mitochondria in the muscle to improve exercise ability, and further prevent or improve mitochondrial myopathy. In addition, by increasing the energy metabolism in the muscle can increase the amount of energy in the body can reduce body fat.
- a soft capsule fill solution 80 mg of cumestrol, 9 mg of vitamin E, 9 mg of vitamin C, 2 mg of palm oil, 8 mg of vegetable hardened oil, 4 mg of succinate and 9 mg of lecithin are mixed and mixed according to a conventional method to prepare a soft capsule fill solution. 400 mg per capsule is filled to prepare a soft capsule.
- a soft capsule sheet is prepared at a ratio of 66 parts by weight of gelatin, 24 parts by weight of glycerine, and 10 parts by weight of sorbitol solution and filled with the filler to prepare a soft capsule containing 400 mg of the composition according to the present invention.
- Injections are prepared in the above amounts per ampoule (2 ml) according to the conventional method for preparing injections.
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Abstract
Description
Claims (15)
- 쿠메스트롤; 또는 쿠메스트롤을 포함하는 콩 추출물을 유효 성분으로 포함하는 미토콘드리아 활성화용 조성물.
- 제 1 항에 있어서,조성물은 에너지 대사를 촉진하는 조성물.
- 제 2 항에 있어서,조성물은 피로 회복, 지구력 향상, 근력 향상 또는 운동 기능 향상을 위한 조성물.
- 제 2 항에 있어서,조성물은 체지방 감소를 통해 비만, 고지혈증 또는 고혈압을 예방 또는 개선하는 조성물.
- 제 1 항에 있어서,조성물은 미토콘드리아 관련 질환을 예방 또는 개선하는 조성물.
- 제 5 항에 있어서,미토콘드리아 관련 질환은 미토콘드리아 활성 저하로 야기되는 신경 정신 질환, 심혈관계 질환, 내장 질환, 내분비계 질환, 감각계 질환, 관절 질환 및 근육 질환 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,신경 정신 질환은 치매, 파킨슨병, 뇌졸중, 신경정신장애, 자폐증, 정신 지체, 발작(seizure), 뇌졸중 유사 발작, 편두통 및 신경 통증 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,심혈관계 질환은 심장 기능 장애, 심장마비, 심장근육병증, 빈맥(tachycadia), 철적아구성 빈혈(sideroblastic anemia), 피어슨 증후군(Pearson syndrome), 불응성 빈혈(refractory anemia) 및 저혈압 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,내장 질환은 간부전, 장 가폐색증(intestinal pseudo-obstruction), 과민성 장 증후군, 위식도역류질환, 변비, 설사, 신세뇨관성산증(renal tubular acidosis) 및 판코니 증후군(fanconi syndrome) 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,내분비계 질환은 췌장외 분비 기능 부족증, 갑상선 기능 저하증(hypothyroidism), 부갑상선 기능 저하증(hypoparathyroidism), 생식 기능 저하증(hypogonadism), 발달 지연, 제2형 당뇨 및 저혈당 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,감각계 질환은 신경위축, 사시, 망막색소변성증, 실명 및 청력 손실 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,관절 질환은 퇴행성 관절염, 류마티스성 관절염 및 골성관절염 중 하나 이상을 포함하는 조성물.
- 제 6 항에 있어서,근육 질환은 운동실조(ataxia), 구음장애(dysarthria), 연하곤란(dysphagia), 경직(spasticity), 뇌근병증, 근육통, 근이영양증, 근육 경련, 안검하수, 눈근육마비, 진행성 외안근 마비, 레버 시신경 위축증(Leber's hereditary optic neuropathy), 호흡 장애, 반사 작용 저하 및 자율신경실조증 중 하나 이상을 포함하는 조성물.
- 제 1 항 내지 제 13 항 중 어느 한 항에 있어서,조성물은 식품 조성물인 조성물.
- 제 1 항 내지 제 13 항 중 어느 한 항에 있어서,조성물은 약학 조성물인 조성물.
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CN2011800265882A CN102905714A (zh) | 2010-03-31 | 2011-03-31 | 含有香豆雌酚或包含香豆雌酚的豆提取物的组合物 |
US13/637,962 US20130090377A1 (en) | 2010-03-31 | 2011-03-31 | Composition comprising coumestrol or a bean extract containing coumestrol |
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US (1) | US20130090377A1 (ko) |
KR (2) | KR20110110053A (ko) |
CN (2) | CN104906177A (ko) |
WO (1) | WO2011122872A2 (ko) |
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KR101866924B1 (ko) | 2011-10-24 | 2018-06-15 | (주)아모레퍼시픽 | 시링가레시놀을 포함하는 대사 이상증 개선용 조성물 |
CN105796546B (zh) | 2011-10-18 | 2020-03-03 | 株式会社爱茉莉太平洋 | 包含丁香脂素的sirt1活化剂 |
KR102200014B1 (ko) | 2013-05-06 | 2021-01-08 | (주)아모레퍼시픽 | 쿠메스트롤을 포함하는 콩 추출물을 유효성분으로 포함하는 갱년기 증상의 예방 및 치료용 조성물 |
KR20160090662A (ko) * | 2015-01-22 | 2016-08-01 | 한국과학기술연구원 | 쥐눈이콩 추출물을 포함하는 망막질환의 예방 또는 치료용 조성물 |
KR20170002846A (ko) | 2015-06-30 | 2017-01-09 | (주)아모레퍼시픽 | 콩잎 추출물을 유효성분으로 함유하는 근질환 억제 및 예방용 조성물 |
CN114848702A (zh) * | 2015-10-30 | 2022-08-05 | 株式会社Hubio | 含有香豆雌酚的发芽发酵豆提取物及包含其的组合物 |
KR102249710B1 (ko) * | 2017-10-20 | 2021-05-10 | (주)아모레퍼시픽 | 콩 배양조직 추출물을 포함하는 탈모방지 또는 육모촉진용 조성물 및 이의 제조방법 |
KR102226151B1 (ko) * | 2017-11-20 | 2021-03-11 | (주)아모레퍼시픽 | 콩과식물 배양근을 이용한 쿠메스트롤 생산 방법 |
KR20200040583A (ko) * | 2018-10-10 | 2020-04-20 | (주)아모레퍼시픽 | 코티존 환원효소 저해용 조성물 |
WO2023140407A1 (ko) * | 2022-01-21 | 2023-07-27 | 경상국립대학교병원 | 쿠메스트롤을 포함하는 근감소증 예방 또는 치료용 약학 조성물 |
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KR100701269B1 (ko) * | 2006-12-19 | 2007-03-29 | (주)아모레퍼시픽 | 쿠메스트롤을 함유한 비만 개선 및 예방용 조성물 |
KR100706279B1 (ko) * | 2005-11-11 | 2007-04-12 | (주)아모레퍼시픽 | 쿠메스트롤을 함유한 비만 개선 및 예방용 조성물 |
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US5424331A (en) * | 1994-06-10 | 1995-06-13 | Bio-Virus Research Incorporated | Pharmaceutical compositions and dietary soybean food products for the prevention of osteoporosis |
KR100338654B1 (ko) * | 2000-06-23 | 2002-05-30 | 임병철 | 페룰산에스테르 유도체, 3,9-디페룰릴쿠메스트롤 및 이를함유한 화장료 |
CN1289080C (zh) * | 2004-11-11 | 2006-12-13 | 蒋谷人 | 替代雌激素的太太天雌素及其应用 |
CN101411437B (zh) * | 2007-10-18 | 2012-05-30 | 北京小西保健食品有限公司 | 纳豆制备工艺及含纳豆提取物的保健食品 |
-
2011
- 2011-03-31 US US13/637,962 patent/US20130090377A1/en not_active Abandoned
- 2011-03-31 WO PCT/KR2011/002222 patent/WO2011122872A2/ko active Application Filing
- 2011-03-31 KR KR1020110029585A patent/KR20110110053A/ko active Application Filing
- 2011-03-31 CN CN201510322898.9A patent/CN104906177A/zh active Pending
- 2011-03-31 CN CN2011800265882A patent/CN102905714A/zh active Pending
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KR100701269B1 (ko) * | 2006-12-19 | 2007-03-29 | (주)아모레퍼시픽 | 쿠메스트롤을 함유한 비만 개선 및 예방용 조성물 |
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Also Published As
Publication number | Publication date |
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WO2011122872A3 (ko) | 2012-03-08 |
CN104906177A (zh) | 2015-09-16 |
KR20130132712A (ko) | 2013-12-05 |
US20130090377A1 (en) | 2013-04-11 |
KR101433539B1 (ko) | 2014-08-27 |
KR20110110053A (ko) | 2011-10-06 |
CN102905714A (zh) | 2013-01-30 |
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