WO2012128461A2 - Composition contenant des extraits d'ail noir et de garcinia cambogia et destinée à traiter ou prévenir l'obésité ou l'hyperlipidémie - Google Patents

Composition contenant des extraits d'ail noir et de garcinia cambogia et destinée à traiter ou prévenir l'obésité ou l'hyperlipidémie Download PDF

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WO2012128461A2
WO2012128461A2 PCT/KR2012/000471 KR2012000471W WO2012128461A2 WO 2012128461 A2 WO2012128461 A2 WO 2012128461A2 KR 2012000471 W KR2012000471 W KR 2012000471W WO 2012128461 A2 WO2012128461 A2 WO 2012128461A2
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Prior art keywords
extract
obesity
composition
black garlic
hyperlipidemia
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PCT/KR2012/000471
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English (en)
Korean (ko)
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WO2012128461A3 (fr
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정남호
정영미
유명진
이동섭
이선하
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의성농산영농조합법인
경운대학교 산학협력단
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Publication of WO2012128461A2 publication Critical patent/WO2012128461A2/fr
Publication of WO2012128461A3 publication Critical patent/WO2012128461A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/38—Clusiaceae, Hypericaceae or Guttiferae (Hypericum or Mangosteen family), e.g. common St. Johnswort
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/896—Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • A61K36/8962—Allium, e.g. garden onion, leek, garlic or chives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics

Definitions

  • composition for the treatment or prophylaxis of obesity or hyperlipidemia comprising pulverized garlic and garcinia cambogia extract
  • the present invention is in the field of natural extracts, and specifically relates to black garlic extract and garcinia cambogia combination extract.
  • Obesity can be judged as being overweight, and specifically, it can be judged as an increase in body fat (eg, abdominal obesity) at a specific site. Obesity has a higher prevalence and mortality than other diseases, and a four-fold mortality from diabetes, twice the mortality from hepatic cirrhosis, and cerebrovascular disease. The mortality rate is 1.6 times higher and the mortality rate from coronary artery disease is 1.8 times higher.
  • treatment for obesity includes diet, exercise therapy, appetite suppressants, diuretics, drug therapy using diarrhea or satiety fiber, behavioral modifications that correct wrong eating habits and lifestyles, and surgical intestines.
  • liposuction surgery such as a method of reducing the volume of the stomach, a method of decomposing and removing fat cells using ultrasound in plastic surgery and the like.
  • fat absorbing agents such as jenga (Roche) and appetite suppressant Reductil (Abbott) occupy 80% of the world market, respectively, but in the domestic market each has a negative growth (-10 each in 2007) %),
  • jenga Fucosa
  • Abbott appetite suppressant Reductil
  • a problem that prohibits taking of organs due to serious side effects including depression, insomnia or digestive disorders.
  • Generic and improved new drug products of Korean pharmaceutical companies are leading the market growth, but only 5% of patients who visit obese medical centers are treated with obesity, and only 103 ⁇ 4 of them are obese patients. Is about 80 billion won, less than 10% of the total obesity market.
  • the present invention is to provide an extract, a composition and a health functional food that can be effectively used for the treatment or prevention of anti-obesity using natural substances.
  • the present application provides a composition for treating or preventing obesity or hyperlipidemia comprising a combination of black garlic extract and garcinia cambogia extract.
  • the present invention also provides a composition comprising a combination of the black garlic extract and garcinia cambogia extract in an amount of 8 to 16 parts by weight based on 1 part by weight of black garlic extract All.
  • the present application also provides a composition wherein the black garlic extract is prepared by the far-infrared irradiation warm aging method.
  • the present invention also provides a composition for the treatment or prevention of obesity or hyperlipidemia wherein the obesity causes metabolic syndrome.
  • the present application also provides a composition for the treatment or prevention of obesity or hyperlipidemia, wherein the metabolic syndrome has symptoms including at least one of glucose tolerance, hypertension, hyperlipidemia, liver disease and nephropathy.
  • the present application also provides a composition for improving obesity or hyperlipidemia provided by the composition as a dietary supplement, a functional food, a food additive.
  • composition comprising a black garlic extract and Garcinia cambogia extract of the present application in combination with a health food comprising the same as compared to the case of obesity treatment, prevention of obesity and hypoglycemia, nephropathy, liver disease, hyperlipidemia Has an elevated effect on prevention, treatment and alleviation.
  • FIG. 1 is a photograph of a combination powder of Garlic extract and Garcinia cambogia extract of Uji Hanji garlic extract powder and garlic extract according to processing form and extraction method.
  • FIG. 2 shows the results of analysis of AMPK activity in the cells of the garlic extract, garlic extract, and garcinia cambogia combination extract of FIG.
  • A garlic hydrothermal extract (FIG. 1 a);
  • B black garlic hot water extract prepared by far-infrared irradiation aging (FIG. 1 b);
  • C Black garlic hot water extract (FIG. 1 b) and Garcinia cambogia extract (FIG. 1 c).
  • C in the picture represents the control group and Met represents the comparative group metformin (Metformin) 2 mM.
  • ⁇ represents p phosphorylated form in pACC, and t represents phosphorylated and non-phosphorylated form total in tAMPKa and tACC.
  • FIG. 3 is a result of measuring the effect of garlic hot water extract (A) of FIG. 1 on adipocyte differentiation (A) and the amount of fat accumulated in cells (B).
  • FIG. 4 is a result of measuring the effect of black garlic hot water extract prepared by the far-infrared irradiation warming method of FIG. 1 on adipocyte differentiation (A) and the amount of fat accumulated in the cell (C) (left panel) , The effect of the same black garlic extract and Garcinia cambogia extract composition on adipocyte differentiation (B) and the amount of intracellular stored fat (D) Right panel).
  • FIG. 5 is a real-time PCR method for the effects of the same composition of the umami garlic extract and the garcinia cambogia extract, which are the same as the sorghum hot water extract prepared by the far-infrared irradiation warming aging method, on the expression level of the adipocyte differentiation control gene. Observed.
  • the present application provides a composition for the treatment or prevention of obesity and / or hyperlipidemia comprising a combination of black garlic extract and Garcinia cambogia extract as an active ingredient.
  • AMPK AMP act ivated protein kinase
  • AMPK is signaling pathway for synthesis of ATP
  • a protein that is activated by detecting intracellular AMP (Adenosine Mono-Phosphate) 3 ⁇ 4 ⁇ to inhibit the signal transduction pathways that consume ATP activates and serves to protect cells from external stress .
  • Substances that increase the activity of AMPK have the effects of promoting ATP (Adenosine Tri-Phosphate) synthesis, increasing glucose uptake, promoting ⁇ -oxidation of fat, inhibiting cholesterol synthesis, and alleviating inflammation. It has been reported to be used as a drug target for the development of therapeutic drugs for metabolic diseases such as diabetes, insulin resistance, hyperlipidemia and inflammation, including obesity.
  • AMPK is a phosphatase that detects intracellular ATP concentrations and is a very important enzyme for maintaining the balance of energy in cells. Usually, AMPK is increased by intracellular biosynthesis (ATP consumption) or rapid ATP due to exercise. It is known to be activated by the increased AMP: ATP ratio by consumption, leading to the ATP production process. Activated AMPK is known to phosphorylate substrates in several substeps, blocking ATP-consuming pathways such as fat synthesis or cholesterol synthesis and activating ATP-producing pathways such as fatty acid oxidation or glycolysis. (DG Hardie et al., FEBS Lett., 546, ppll3-120, 2003; D. Carling, Trends Biochem.
  • Acetyl-CoA carboxylase inhibits enzyme activity through small protein phosphorylation.
  • ACC is an important enzyme that regulates lipid metabolism in various tissues such as liver and muscle. It acts to carbonate acetyl-CoA to malonyl-CoA (BE Kemp, Biochem. Soc. Trans., 31, pp 162-168).
  • malonyl-CoA is present in the outer membrane of the mitochondria It acts as an inhibitor of CPT1 (carnitine palmitoyl transferase 1), and its activity plays an important role in ⁇ -oxidation of fat in mitochondria (Leh inger, Principles of Biochemistry, Worth Publishers, NY, 3rd Ed., Pp 599 -605, 2000; Cohen P., Miyazaki, M., Socci, ND, Hagge-Greenberg, A., Liedtke, W., Soukas, AA, Sharma, R., Hudgins, LC, Ntambi, JM & Friedman, JM , Science 297, 240-243, 2002).
  • AMPK Activation of AMPK enhances the phosphorylation of ACC and the inhibition of enzyme activity leads to a decrease in the production of malonyl-CoA, leading to the activation of AMPK (Va as D et al., J. Biol. Chem., 272, pp 13255-13261, 1997) ATP production is increased by the oxidation of fatty acids.
  • phosphorylation of AC by AMPK activation is important for the reduction of body fat due to fatty acid oxidation mechanism. Therefore, if ACC enzyme activity is controlled by AMPK at the beginning of fatty acid synthesis, it is possible to suppress fat accumulation in the body more than necessary, and consequently, weight gain can be suppressed.
  • HMG-CoA reductase a target molecule of statin, a hyperlipidemia drug
  • statin a target molecule of statin, a hyperlipidemia drug
  • the synthesis of cholesterone can also be regulated in liver tissue by AMPK activation.
  • the effect of lowering the concentration of triglycerides and cholesterol in the blood can be obtained. Therefore, when AMPK is activated, the synthesis of fat decreases and ⁇ -oxidation is increased, thereby increasing the oxidation of ovaries, thereby reducing the weight of the body due to the decrease of body fat and reducing the concentrations of neutral fat and cholesterol in the blood.
  • composition of the present invention contains a combination of black garlic and garcinia cambogia extract, and activates AMPK to reduce body fat, thereby exhibiting anti-obesity effect and alleviation and / or therapeutic effect of hyperlipidemia.
  • the term "obesity” refers to a condition or disease in which fat accumulated in the body due to energy imbalance has excessive body fat higher than normal.
  • WHO World Health Organization
  • the Asia-Pacific region used to diagnose obesity is the weight of its own weight divided by the square of its height (meters), and if it is 25.0 or more, it is defined as obesity. Less than 25 is defined as overweight (dangerous).
  • Obesity is classified according to classification into endocrine obesity (due to endocrine abnormalities or from brain diseases), simple obesity (due to excessive nutrition); Proliferative obesity (obesity due to an increase in the number of fat cells), hypertrophy ' type obesity (obesity due to an increase in the size of fat cells); Upper body obesity, lower body obesity; And visceral obesity, subcutaneous fat, and the like, all of which are included in the scope of the present invention.
  • said obesity is obesity associated with metabolic syndrome.
  • metabolic syndrome means that diseases such as diabetes mellitus type 2, hyperlipidemia, obesity, nephropathy and hepatic disease occur simultaneously (Pershadsingh HA, Dual Peroxisome Prolifer at or ⁇ Activated Recept or-a 1 pha / gamma Agonists: In the Treatment of Type 2 Diabetes Mellitus and the Metabolic Syndrome.Treat 'Endocrinol. 2006; 5 (2): 89—99).
  • hyperlipidemia refers to hyperlipidemia when the concentration of fat components, especially cholesterol and triglyceride, is high in the blood and generally exceeds 240 mg / dC or when triglyceride is 200 mg / de or more. do. Hyperlipidemia can be caused by genetic predisposition, obesity, dietary habits, diabetes, nephrotic syndrome, hypothyroidism.
  • Hyperlipidemia to which the extract of the present application is effective includes, but is not limited to, hyperlipidemia due to obesity, metabolic syndrome, diabetes, dietary habits, hypothyroidism, nephrotic syndrome.
  • the hyperlipidemia herein is due to obesity.
  • the hyperlipidemia herein is due to diabetes.
  • the hyperlipidemia herein is due to metabolic syndrome.
  • treatment refers to any action that ameliorates or beneficially alters obesity or hyperlipidemia or other diseases and conditions resulting from administration of an extract or a composition comprising the same.
  • Those of ordinary skill in the art will be able to know the exact criteria of obesity or hyperlipidemia or the disease for which the composition of the present invention is effective, and can determine the degree of improvement, improvement and treatment, with reference to data presented by the Korean Medical Association. .
  • prevention refers to any action that inhibits or delays the development of obesity or hyperlipidemia or other diseases resulting from administration of an extract or a composition comprising the same. It will be apparent to those skilled in the art that the extract herein, which has a therapeutic effect on obesity or hyperlipidemia, can prevent these diseases if taken before the initial symptoms of, or before appearing, obesity hyperlipidemia.
  • extract refers to an active ingredient isolated from natural products, ie, a substance that exhibits the desired activity.
  • the extract may be obtained by an extraction process using water, an organic solvent or a mixed solvent thereof, and the extract may include a dry powder thereof or any form formulated using the same.
  • the extract also includes a fraction obtained by the extraction process.
  • the raw material of the extract used herein is a food Used in perennial bulbous plants belonging to the allium of the family Liliaceae, along with leeks, onions, leeks and soothe.
  • the garlic is Uiji Hanji Garlic.
  • the garlic is processed garlic, in particular black garlic.
  • the black garlic is black garlic prepared from pseudo-Korean garlic. Lumps of garlic are prepared by ripening fresh garlic for a certain period of time at appropriate temperature and humidity conditions.
  • black garlic extract refers to an active ingredient separated from natural products, that is, a material showing a desired activity, and is typically prepared by an extraction process using water, an organic solvent, or a mixed solvent thereof. Extracts of mixed solvents, dry powders thereof or any form formulated using them. In addition, the extract also includes a fraction obtained by the extraction process.
  • the garlic extract of the present application is used in combination with a garcinia cambogia extract.
  • Garcinia cambogia is a tropical fruit tree of the family Gutti ferae, which originates mainly in Southeast Asia including India.
  • Garcinia cambogia extract is powdered by extracting Garcinia cambogia fruit, especially skin.
  • Garcinia cambogia extract contains HCA (hydroxy citric acid) based on about 10 ⁇ 30 trillion weight) and is very similar to citric acid in citrus fruits such as orange and lemon, but has hydroxyl group. It is a rare substance in nature.
  • HCA inhibits the conversion of citrate to acetyl-CoA in vivo, inhibits the synthesis of fatty acids, promotes oxidation, and converts into glucogen synthesis, which increases energy production. When used in combination with, it has a synergistic effect on anti-obesity.
  • the composition of the present invention is derived from natural foods and is not toxic or resistant and does not have side effects such as insomnia, neuroanxiety, and depression that are present in other appetite suppressants.
  • the composition comprising the gum garlic extract and garcinia cambogia of the present disclosure contains about 5 to 20 parts by weight of garcinia cambogia with respect to 1 part by weight of gum garlic extract. In another embodiment, about 7 to 17 parts by weight of garcinia cambogia per 1 part by weight of black garlic extract. In another embodiment, about 8 parts by weight or about 16 parts by weight of garcinia cambogia against 1 part by weight of black garlic extract. These black garlic and garcinia cambogia extracts can be prepared according to known methods.
  • the Garcinia cambogia extract and lump garlic extract or powder thereof may be prepared according to a known method using hot water extraction or a suitable organic solvent such as methanol, ethanol, or the like as an extraction solvent (Nomura T. Phenolic compounds of the mulberry tree and related plants.In: Progress in the Chemistry of Organic Natural Products (Herz W, Gr i sebach H, Kirby GW, Tamm Ch, eds.), vol. 53. Springe- ' Vienna, 1988; 87 -201.)
  • the solvent may be water, an organic solvent or a mixed solvent thereof.
  • water, methane, a low-carbon alcohol having 1 to 5 carbon atoms, including ethanol, butanol, propanol and isopropanol, a polar solvent such as ethyl acetate, and a nonpolar solvent of nucleic acid or dichloromethane may be an organic solvent such as or a mixed solvent thereof, in particular may be water, an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof, and more particularly water, 50 to 100% methanol, ethane to 1 to 4 may be an alcohol.
  • Extracts herein can be prepared using known general methods for preparing conventional plant extracts, and are not particularly limited. For example, ultrasonic extraction, reflux . It may be an extraction method, a hot water extraction method or a method prepared by a known method using the solvent as an extraction solvent (see, for example, Nomura T, 1988, etc.).
  • the extract after the extraction process can be further subjected to the fractionation process with a solvent selected from the group consisting of nucleic acid, methylene chloride, acetone, ethyl acetate, chloroform and their mixtures.
  • two or more solvents may be used individually or in combination, and may be sequentially used according to the polarity of the solvent to prepare an extract of each solvent.
  • Extract preparation may be from 4 to 120 ° C, but is not limited thereto.
  • the extraction time is not particularly limited, but may be 10 minutes to 30 days, and a conventional extraction device, an ultrasonic grinding extractor, or a fractionator may be used.
  • the prepared extract can then be filtered under reduced pressure or / and lyophilized to remove the solvent.
  • the solvent is added to the black garlic in a heating circulating extraction tank in a weight ratio of 1: 1 to 1: 20, and purified water or edible alcohol is extracted for 6 to 24 hours at 80 to 100 ° C, followed by filtration to obtain a filtrate.
  • the same process can be repeated several times by adding purified water or edible alcohol to the residue.
  • the filtrates can be combined, used as is, or concentrated under reduced pressure with a vacuum concentrator, and then dried by hot air or lyophilization.
  • the garcinia cambogia extract or lump garlic extract of the present invention is a material
  • the extraction is carried out by adding 0.1 to 1 (per 100 g of water, followed by extraction.
  • the extraction temperature may be about 80 to 150 ° C, but is not limited thereto.
  • the extraction time is not limited but may be 30 minutes to several days. It is possible to use a conventional extraction device or an ultrasonic grinding extractor
  • the prepared extract can be used after filtration under reduced pressure and lyophilization.
  • the garcinia cambogia extract or black garlic extract may be suspended by adding about 0.5 to 5 ethanol per 100 g of ash to about 10 to 15 g of the concentrate obtained by concentrating the extract in about 100 to 1000 water.
  • Nucleic acid fractions are extracted after adding 100 to 1000 mC of nucleic acid. After removing the nucleic acid fraction extract, methylene chloride is added to the remaining water layer again 100 to 1000, and then extracted
  • methylene chloride, ethyl acetate, butanol extraction temperature may be 20 to 40 ° C, but is not limited to this, extraction time is not limited, but may be 30 minutes to 20 hours, conventional An extraction device or an ultrasonic grinding extractor can be used.
  • the prepared extract is then filtered under reduced pressure and lyophilized to remove the solvent.
  • the black garlic or garcinia cambogia extract is extracted by adding 0.1 to 5 methanol per 100 g of material to prepare a methanol extract.
  • the methanol extract is added to the nucleic acid or methylene chloride later to obtain a fraction for each solvent to prepare a nucleic acid extract or methylene chloride.
  • ethyl acetate and butanol are sequentially added to the residue to fractionate to prepare ethyl acetate extract and butanol extract, respectively.
  • the water fraction not extracted from the solvent is prepared as a water extract.
  • the solvent is added to the extraction object in a ratio of 1: 0.1 to 10 by volume.
  • the filtration is a process for removing suspended solid particles from the extract, it may be used to filter the particles using cotton, nylon or the like, or ultrafiltration, filtration, centrifugal separation, etc., but is not limited thereto. In addition, it may further include a separation process by a variety of chromatography (chromatography according to the size, charge, hydrophobicity or hydrophilicity).
  • the drying process is freeze drying, vacuum drying, hot air drying, spray drying, reduced pressure drying, foam drying, high frequency drying or infrared It may be carried out by a method including drying, but is not limited thereto.
  • fatty acid intake leads to the accumulation of triglycerides in various tissues of the body, especially adipose tissue, thereby increasing lipolysis in adipose tissue.
  • This increase in fatty acids in the bloodstream leads to insulin resistance and increases in fatty acids to non-fat tissues such as muscle, pancreas and liver.
  • the concentration of fatty acid-binding transport proteins (FABP and CD36) in fat and non-fat tissues is increased to promote uptake of fatty acids. Accumulation of such excess free fatty acids and fatty acids in muscle leads to a vicious cycle in insulin signaling and sugar use.
  • FABP and CD36 fatty acid-binding transport proteins
  • Prolonged exposure of the pancreas to free fatty acids is known to impair insulin secretion through lipotoxic mechanisms (Lebovitz HE. Insulin resistance: definition and consequences.Exp Clin Endocrinol Diabetes. 2001; 109: S135-48).
  • the liver is also known to enhance glucose release and interfere with insulin's action (Goldstein BJ. Insulin resistance as the core defect in type 2 diabetes mel 1 itus. Am J Cardiol. 2002; 90: 3G-10G).
  • Accumulation of triglycerides in the liver leads to non-alcoholic fatty liver, which leads to liver damage such as fattyosis, hepatitis, hepatocellular necrosis and fibrosis and prevents glucose metabolism, a major function of the liver (Angulo P.
  • Nonalcoholic fatty liver disease N Engl J Med. 2002; 346: 1221-31). These symptoms are also important for metabolic syndrome (Kadowaki T, Yamauchi T. Adionectin and adiponectin receptors. Endocr Rev. 2005; 26: 439-51).
  • the black garlic and garcinia cambogia extracts of the present application have an excellent anti-obesity effect and an improvement in the symptoms of metabolic syndrome and hyperlipidemia due to obesity than when used individually.
  • the pharmaceutical composition comprising the garlic garlic extract Garcinia cambogia extract of the present application may be administered simultaneously or sequentially, and the combination may be used alone or in other pharmaceuticals for the treatment of symptoms of obesity and / or metabolic syndrome such as hyperlipidemia. It may be administered in parallel with the active ingredient.
  • Compositions comprising the black garlic extract and Garcinia cambogia extract of the present application may be any suitable carriers, diluents, preservatives, stabilizers, wetting agents, emulsifiers, solubilizers, sweeteners, colorants, osmotic agents, antioxidants commonly used in the manufacture of pharmaceutical compositions. Department of the back May contain more brothers.
  • lactose lactose, dextrose, sucrose, sorbet, manny, xili, erysri, malty, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, celrose, methylcellrose, Microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium, stearate, mineral oil and the like.
  • a method of administering a pharmaceutical composition for preventing or treating obesity or hyperlipidemia including the garlic seed extract and garcinia cambogia extract of the present application may be easily selected according to the dosage form, and may be used in various routes in mammals such as livestock and humans. May be administered. For example, it may be formulated in the form of powders, tablets, pills, granules, dragees, hard or soft capsules, liquids, emulsions, suspensions, syrups, elixirs, external preparations, suppositories, sterile injectable solutions, systemically or topically. Oral or parenteral administration, with oral administration being preferred.
  • Solid dosage forms for oral administration include tablets, pills, powders, granules, capsules, and the like.
  • Such solid formulations are prepared by mixing black garlic extract and garcinia cambogia extract with at least one excipient such as starch, carbonate, sucrose or lactose, gelatin and the like.
  • excipients such as starch, carbonate, sucrose or lactose, gelatin and the like.
  • lubricants such as magnesium styrate talc are also used.
  • Liquid dosage forms for oral administration include suspensions, solutions, emulsions, and syrups. Water, liquid paraffin, which is a commonly used simple diluent, and various excipients such as wetting agents, sweeteners, fragrances, and preservatives Can be.
  • Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions ⁇ emulsions, copper lyophilizers, suppositories.
  • non-aqueous solvent and the suspension solvent propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate can be used.
  • injectable esters such as ethyl oleate
  • Group zero of suppositories above tepsol (witepsol), Macrogol, Tween (tween) 61, cacao butter, laurin butter, glycerol, gelatin and the like may be used.
  • compositions comprising black garlic extract and Garcinia cambogia extracts of the present disclosure may be prepared using the appropriate methods known in the art,
  • the dosage of the pharmaceutical composition comprising the black garlic extract and the garcinia cambogia extract of the present application may vary depending on the weight, age, sex, health condition, diet, time of administration, method of administration, excretion and severity of the patient. May vary, but black garlic extract and
  • the effective dose of the Garcinia cambogia extract is typically about 1 to 100 g / day, in particular about 10 to 50 g / day, more preferably about 30 g / day for adults (60 kg). Since the dosage may vary depending on various conditions, it will be apparent to those skilled in the art that the dosage may be added or subtracted, and thus the dosage does not limit the scope of the present invention in any aspect.
  • the frequency of administration may be administered once a day or divided into several times within a desired range, and the administration period is not particularly limited.
  • the composition comprising the extract of the present application may be added to any food and drink, in addition to oral administration as it is, ingested daily.
  • the pharmaceutical composition comprising the black garlic extract and Garcinia cambogia extract of the present application not only provides excellent therapeutic effects on obesity and metabolic syndrome and hyperlipidemia, but also does not have toxicity and side effects caused by drugs, even when taken for a long time. Can be used with confidence. Accordingly, the black garlic extract and garcinia cambogia extract of the present application can be used as the main, subsidiary and food additive of food.
  • the present invention is a composition comprising the black garlic extract of the present invention as described above
  • Lecinia cambogia extract may be provided as a cut, for example, dietary supplements, functional foods, food additives and the like.
  • the term "food” means a natural product or processed product containing one or more nutrients, and preferably means that it can be directly eaten through a certain processing process. , In a general sense, it is intended to include all foods, food additives, functional foods and beverages.
  • the term "functional food” refers to a food group or food composition that has added value to the food by using physical, biochemical, or biotechnological techniques to act and express the function of the food for a specific purpose. Means foods that have been designed and processed to fully express the function of the gymnastic nodes on the control of biological defense, disease prevention and recovery, and especially includes "health functional foods”.
  • the term "health supplement” is a food prepared and processed using raw materials or ingredients having useful functions for the human body, and controls nutrients or physiological effects on the structure and function of the human body. It refers to foods that are manufactured and processed by extracting, concentrating, refining, and mixing certain ingredients as raw materials or ingredients contained in food raw materials for the purpose of health supplement to obtain useful effects for health use.
  • the functional food or health supplement food in the present invention before ingesting the food Means foods that are effective in improving, reducing or eliminating the symptoms of obesity, hyperlipidemia and diseases caused by the same, and those skilled in the art to which the present invention belongs. If so, the information provided by the Korean Medical Association will be able to know the exact criteria of the disease and determine the degree of improvement.
  • the functional foods and health supplements may further include food acceptable food additives, and may further include appropriate carriers, excipients and diluents commonly used in the manufacture of functional foods.
  • Foods to which the black garlic extract and garcinia cambogia extract of the present application can be added include, for example, various foods, beverages, gums, teas, vitamin complexes, and functional foods.
  • the food includes special nutritional products (e.g., prepared oils, infants, infant foods, etc.), processed meat products, fish products, tofu, jelly, noodles (e.g. ramen, noodles, etc.), health supplements, seasoned foods ( Soy sauce, miso, red pepper paste, mixed soy sauce), sauces, confectionery (eg snacks)
  • Dairy products e.g. fermented milk, cheese dung
  • other processed foods e.g. kimchi, pickles (various kimchi, pickles)
  • beverages e.g. fruits, vegetable drinks, soy milk, fermented beverages, etc.
  • natural seasonings e.g., Ramen soup, etc.
  • the food, beverage or food additives may be prepared by conventional manufacturing methods.
  • Beverage herein refers to a generic term for drinking to quench thirst or to enjoy a taste and is intended to include functional drinks.
  • the beverage is not essential in addition to the black garlic extract and Garcinia cambogia extract of the present application as an essential ingredient in the indicated ratios as an active ingredient, and does not have any particular limitations, such as ordinary drinks, various flavors or natural carbohydrates May be contained as an additional component.
  • natural carbohydrates include monosaccharides such as glucose, fructose and other disaccharides such as maltose, sucrose and the like and polysaccharides such as conventional sugars such as dextrin and cyclodextrin, And sugar alcohols such as xylitol, sorbitol, and eritry.
  • natural flavoring agents such as tauumatin, stevia extract (e.g. rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame dong) can be advantageously used.
  • the ratio of the natural carbohydrate is generally about 1 to X 20g, preferably 5 to 12g per 100m of the composition of the present invention, in addition to the composition of the present invention for the production of natural fruit juices, fruit juice drinks, vegetable drinks It may further contain pulp.
  • a functional beverage is used in the beverage as physical, biochemical, or biotechnological methods.
  • Beverages that are designed to express the function of the beverage to the specific purpose and to express the gymnastics functions related to the biological defense rhythm control, disease prevention and recovery, etc. It means, preferably means a beverage for improving metabolic syndrome symptoms, for example hyperlipidemia.
  • the functional beverage is not particularly limited to other ingredients except the black garlic extract and garcinia cambogia extract of the present application as essential ingredients in the indicated ratios, and various flavors or natural carbohydrates may be used as additional ingredients as in general beverages. It may contain.
  • natural carbohydrates include monosaccharides such as glucose, fructose and other disaccharides such as maltose, sucrose and the like and polysaccharides such as conventional sugars such as dextrin, cyclodextrin, and xyl Sugar alcohols such as sorbitol and erythritol.
  • natural flavoring agents tautin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used.
  • the proportion of said natural carbohydrates is generally about 1 to 20 g, preferably 5 to 12 g per composition of the present invention.
  • composition of the present application includes various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, coloring and neutralizing agents (such as cheese, chocolate), pectic acid and salts thereof, and alginic acid. And salts thereof, organic acids, protective colloid thickeners, pH adjusters, stabilizers and preservatives, glycerin, alcohols, carbonation agents used in carbonated drinks, and the like. These components can be used independently or in combination. The proportion of such additives is not so critical, but may be selected in the range of 0.001 to 20 parts by weight per 100 parts by weight of the extract of the present invention.
  • the combination of the black garlic extract Garcinia cambogia extract of the present application is about 0.01 to 90% by weight of about 0.1 to 80% by weight, about 1% to 70%, about 1% to 50%, about 1% to 40%, about 1% to 30%, may include a range of about 20%, but does not exclude the above range.
  • the beverage composition may comprise a ratio of 0.02 to 10 g, preferably 0.3 to lg, based on 100.
  • Uiseong Hanji Garlic was purchased from Uiseong Agricultural Cooperative Corporation (Korea). Dried whole garlic lOOg was put in 1 £ distilled water and thoroughly decocted at 80 ° C. for 2 hours under reflux, and the resultant was filtered by suction filtration to prepare an extract. The same extraction procedure was repeated once more for the residue remaining after filtration.
  • Uiseong Hanji Garlic was purchased from Uiseong Agricultural Cooperative (Korea). Purified fresh garlic was first aged at 24 ° C for 24 hours after maintaining the humidity above 8OT in a thermo-hygrostat equipped with far infrared rays. Dark brown garlic (Black garl ic, BG) was prepared by subjecting the light brown garlic obtained after the first aging to secondary aging for 15 days in a thermo-hygrostat maintained at 60 ° C. and a humidity of 85%. The whole black garlic lOOg dried at 100 ° C for 24 hours was put in 1 distilled water, thoroughly decocted at 80 ° C for 2 hours under reflux, and then filtered by suction filtration to prepare an extract.
  • Black garl ic, BG Black garl ic, BG
  • the whole black garlic lOOg dried at 100 ° C for 24 hours was put in 1 distilled water, thoroughly decocted at 80 ° C for 2 hours under reflux, and then filtered by suction filtration to prepare an extract
  • Garcinia cambogia extract used herein was used powder purchased from Rexgene Biotech Co., Ltd.
  • the extract prepared above is named as Uiji Hanji garlic hot water extract (a), black garlic hot water extract (b) prepared by far-infrared irradiation warming ripening method, black garlic hot water extract and garcinia cambogia mixed extract (c). It was used for the following experiment.
  • AMPK AMPK
  • ACC Alcohol-CoA carboxylase
  • ⁇ -oxidation is increased to increase oxidation of body fat.
  • HMG-CoA reductase enzyme another important target molecule of ⁇ , is regulated, thus inhibiting the synthesis of cholesterol in hepatic tissues, which is effective in hyperlipidemia.
  • L6 myocytes are American Type Culture Collection (ATCC; Manassas, VA,
  • Example 2-2 activation effect according to the processing form of garlic
  • each of the extracts a, b, and c prepared in Example 1 was final concentration of 2 mg / ml, 5 mg / ml,
  • L6 cells were treated with 2 mM concentration of metformin, which inhibits obesity induced by high fat, at a concentration of 10 mg / ml and as a reference group. Subsequently, after 24 hours, cells were harvested to extract total protein, and the degree of phosphorylation of AMPK and ACC was measured to investigate AMPK and ACC activity.
  • 3T3-L1 preadipocyte was purchased from American Type Culture-Collection (ATCC; Manassas, VA, USA), and Dulbecco's modified Eagle's medium (DMEM; high glucose 4.5 g / L).
  • ATCC American Type Culture-Collection
  • DMEM Dulbecco's modified Eagle's medium
  • FBS fetal bovine serum
  • FCS Fetal Calf Serum
  • 3T3-L1 cells were incubated in DMEM medium containing 25 mM glucose (high glucose), 10% FCS, 1% penicillin / streptomycin under 37 ° C., 5% C02 at 100% humidity. To maintain cell function, cells were recovered and passaged at about 60% saturation. Cells were washed once with PBS (Phosphate Buffered Saline, pH 8.0) for subculture and then treated with trypsin-EDTA (Sigma) according to the manufacturer's instructions to separate cells from the bottom.
  • PBS Phosphate Buffered Saline, pH 8.0
  • Differentiation into adipocytes was carried out for 4 days when the 3T3-L1 cells were 100% saturated in the culture dish and replaced with a differentiation medium, followed by DMEM containing 25 mM glucose, 10% FBS and 1 mg / ml insulin. Exchange with medium and incubate for 4 more days. After the insulin treatment, the cells were replaced with DMEM medium containing 25 mM glucose and 10% FBS until use, and the medium was replaced with the same medium every 2 days. Each extract used in the experiment was treated to the final concentrations described in Figures 3 to 4, and the extracts were also added during the medium exchange period of 10 days. At the end of differentiation, the culture medium was removed and the cells were fixed by treatment with a fixed solution (10% formalin) for 5 minutes.
  • the differentiation of fat was increased by concentration of medicinal Hanji garlic extract (FIG. 3A), and the fat accumulation in adipocytes was slightly increased depending on the concentration (FIG. 3B).
  • Example 3-3 Combined Treatment of Gum-Garlic Extract Alone and Gum-Garlic Extract and Garcinia Cambogia Extract
  • Extracts of Ujihanji black garlic extract increased fat differentiation consistently (FIG. 4A), and fat accumulation in adipocytes was slightly increased (FIG. 4C).
  • admixture of black garlic extract and garcinia cambogia extract at the ratio of Preparation Example 2 was treated as in Example 3-1 to measure adipocyte differentiation.
  • adipocyte differentiation was inhibited (FIG. 4B). It was confirmed that the decrease (Fig. 4D).
  • garlic and Garcinia cambogia extracts were used in combination, the degree of differentiation of adipocytes was significantly reduced compared to the use of each extract alone, and the accumulation of intracellular fat was also reduced compared to the use of each extract alone. there was.
  • RNA isolation and cDNA synthesis used for real time PCR for gene expression analysis were performed as follows. Trizol (Invitrogen) solution was used to isolate total RNA from cells according to the instructions of the company. The total RNA concentration was quantified using a nanodrop spectrophotometer, and 5 mg of total RNA was used for cDNA synthesis. Synthesis of cDNA was performed by manufacturer of reverse transcriptase (Takara, Japan) kit.
  • the gene expression level was read by real-time PCR (ABI 7500, ABI, USA) using Syber Green kit using the manufacturer's instructions.
  • the primer sequences used for the detection of each gene are as follows:
  • the primers used for the aP2 gene detection are Forward Primer CCA TCC GGT CAG AGA GTA CTT TTA A and Reverse Primer CGA ATT CCA CGC CCA GTT T.
  • Primers for C / gBPa gene detection are Forward Primer TGC GAG CAC GAG ACG TCT ATA G and Reverse Primer GCC AGG AAC TCG TCG TTG A.
  • Primers for PPARY gene detection include Forward Primer CAC AAG AGC TGA CCC AAT GGT and Reverse Primer GAT CGC
  • Primers used to detect adiponectin gene are Forward Primer AAC CCC TGG CAG GAA AGG and Reverse Primer CAC TGA ACG CTG AGC GAT ACA.
  • Primers used to detect the SREBPlc (ADD1) gene are Forward Primer AGA GGG TGA GCC TGA CM and Reverse Primer CCT CTG C TTT CCA GAT.
  • Forward Primer ACC TCC TTC TTC CGG CTT and Reverse Primer CTC CAG TCT TTA TCA GCT were used for 36B4 (GLUT4) gene detection.
  • black garlic extract and Garcinia cambogia extract were treated with the expression of C / EBPa and PPARg, the master transcriptional regulators that regulate the differentiation of adipocytes, and absorption of glucose synthesis in adipocytes.
  • the glucose transporter 4 (GLUT4) gene and fatty acid synthease (FAS), which regulates the expression of GAS, also decreased the expression level by the combination treatment with Garlic extract.
  • the expression of adiponectin showed little change compared to the control group.
  • adipocyte differentiation was carried out using a combination of Garcia cambogia extract alone, black garlic extract, and garcinia cambogia extract (included in each component of Preparation Example 2) in the amounts shown in FIG. 6 as in Example 3-1. Measured. The results are shown in FIG. 6, and as shown, when the garcinia cambogia extract was treated with the extract of black garlic powder in combination, the concentration-dependent fat cell differentiation was suppressed with 15-20% better effect. I could.
  • the composite composition contained 35% less than the Garcinia cambogia extract alone, and it can be seen that synergistic effects were induced even with the use of a smaller amount by the combined use with black garlic extract. .
  • the tablets were prepared by directly using the above powders for experiments or by mixing and tableting the above components according to conventional tablet production methods.
  • the above powder was used for direct experiments, or the tablets were prepared by mixing and tableting the above components according to a conventional tablet production method.
  • Purified water was added to adjust the total volume to 1000 ml. According to the conventional method for preparing a liquid solution, the above components were mixed and then layered and sterilized in a brown bottle to prepare a liquid solution.
  • composition ratio of the above-mentioned vitamin and mineral mixture is a common composition of relatively suitable ingredients for health foods as a preferred manufacturing example, but the formulation ratio may be arbitrarily modified, and according to the conventional health food manufacturing method, The ingredients were combined and then health foods were prepared in granule formulations.

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Abstract

La présente invention concerne une composition anti-obésité contenant un mélange d'extraits d'ail noir et d'extraits de Garcinia cambogia. La composition mixte de la présente invention exerce une action anti-obésité en inhibant la synthèse des graisses et la différentiation des cellules graisseuses grâce à l'activation de l'AMPK et à l'inhibition de l'ACC, qui constitue une cible de l'AMPK, et son action se révèle plus efficace que lorsque l'on utilise une seule de ces deux espèces, ladite composition pouvant donc être efficacement utilisée en vue du traitement ou de la prévention de l'obésité.
PCT/KR2012/000471 2011-03-22 2012-01-19 Composition contenant des extraits d'ail noir et de garcinia cambogia et destinée à traiter ou prévenir l'obésité ou l'hyperlipidémie WO2012128461A2 (fr)

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KR101849932B1 (ko) * 2016-11-29 2018-04-18 무안군 양파와 가르시니아 캄보지아를 포함하는 쓴맛이 제거된 혼합 건강기능성 음료 및 이의 제조방법

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KR20050045666A (ko) * 2003-11-12 2005-05-17 (주)새롬바이오 비만억제 조성물
KR100840991B1 (ko) * 2007-02-27 2008-06-24 류병호 냄새 없는 흑마늘의 제조 방법
JP2010202634A (ja) * 2008-06-05 2010-09-16 Green Kanpo Seiyaku Kk 生薬含有組成物及びその利用
KR100990260B1 (ko) * 2010-05-03 2010-10-26 의성농산영농조합법인 발효 흑마늘 추출물을 유효성분으로 포함하는 비만 또는 고지혈증의 예방 또는 치료용 조성물

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20050045666A (ko) * 2003-11-12 2005-05-17 (주)새롬바이오 비만억제 조성물
KR100840991B1 (ko) * 2007-02-27 2008-06-24 류병호 냄새 없는 흑마늘의 제조 방법
JP2010202634A (ja) * 2008-06-05 2010-09-16 Green Kanpo Seiyaku Kk 生薬含有組成物及びその利用
KR100990260B1 (ko) * 2010-05-03 2010-10-26 의성농산영농조합법인 발효 흑마늘 추출물을 유효성분으로 포함하는 비만 또는 고지혈증의 예방 또는 치료용 조성물

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