WO2010095808A2 - Procédé de production d'extrait d'astragalus membranaceus par enzymolyse, et composition pour prévenir ou soulager le diabète ou l'obésité, contenant un principe actif comprenant un extrait d'astragalus membranaceus produit à l'aide dudit procédé de production - Google Patents

Procédé de production d'extrait d'astragalus membranaceus par enzymolyse, et composition pour prévenir ou soulager le diabète ou l'obésité, contenant un principe actif comprenant un extrait d'astragalus membranaceus produit à l'aide dudit procédé de production Download PDF

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WO2010095808A2
WO2010095808A2 PCT/KR2009/007591 KR2009007591W WO2010095808A2 WO 2010095808 A2 WO2010095808 A2 WO 2010095808A2 KR 2009007591 W KR2009007591 W KR 2009007591W WO 2010095808 A2 WO2010095808 A2 WO 2010095808A2
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Prior art keywords
extract
astragalus
diabetes
composition
active ingredient
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PCT/KR2009/007591
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English (en)
Korean (ko)
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WO2010095808A3 (fr
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이현우
김성규
윤승원
박종철
Original Assignee
주식회사 의림바이오텍
재단법인충북테크노파크
제천시
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Priority claimed from KR1020090013579A external-priority patent/KR101066434B1/ko
Priority claimed from KR1020090126025A external-priority patent/KR101088711B1/ko
Application filed by 주식회사 의림바이오텍, 재단법인충북테크노파크, 제천시 filed Critical 주식회사 의림바이오텍
Publication of WO2010095808A2 publication Critical patent/WO2010095808A2/fr
Publication of WO2010095808A3 publication Critical patent/WO2010095808A3/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)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/481—Astragalus (milkvetch)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Definitions

  • the present invention relates to a method for preparing an extract of Astragalus by using an enzymatic digestion method and a composition for preventing or alleviating diabetes or obesity containing the Astragalus extract prepared by the method as an active ingredient, more specifically, astragalus amylase and / Or hydrolysis using cellulase to increase the extraction recovery rate of the insoluble substance, and to prevent diabetic or obesity, including as an active ingredient, astragalus extraction method using the enzymatic decomposition method and the astragalus extract prepared using the above method. It relates to a composition for relaxation.
  • Diabetes mellitus and its complications are various diseases such as circulatory disease, eye disease, foot ulcer and other diseases such as heart disease, kidney disease, and vascular disease.
  • Symptoms of diabetes may include the following: polyuria, polyps.
  • Urine is the excretion of glucose and water, frequent urination, drinking a lot of water from severe thirst, and eat a lot of food to feel fasting. Diabetes is classified into insulin dependent diabetes mellitus (type 1 diabetes: childhood diabetes) and insulin independent diabetes mellitus (type 2; adult diabetes). Section 1 diabetes is a symptom caused by severe insulin deficiency. In Gumi, it is estimated that about 5 to 10% of all diabetics, but about 1 to 2% in Korea.
  • diabetes Most of the diabetic patients in Korea are type 2 diabetic patients, mainly after the age of 40, because the onset of close family, genetic factors are recognized as important factors, high calorie intake, lack of exercise, obesity, stress And environmental factors such as drug abuse are known to cause diabetes.
  • type 2 diabetes both insulin secretion in pancreatic beta cells and insulin resistance in target cells are observed.
  • fatty acidization in mitochondria causes a change in the mitochondrial gene, causing metabolic syndrome such as type 2 diabetes.
  • the concentration of triglycerides in the blood is high, it is presumed to be various pathological causes such as circulatory diseases by clouding blood. In particular, it is known as a major cause of various heart diseases, such as hyperlipidemia, arteriosclerosis, diabetes.
  • Oral hypoglycemic agents include sulfonylureas, biguanides, and acarbose.
  • Sulfonylurea preparations are used in non-obese adult diabetic patients, and biguanides and acarbose are mainly used in obese diabetic patients. Biguanide and acarbose have the advantage of low incidence of hypoglycemia.
  • Insulin is excellent in hypoglycemic effect, but it is formulated as an injection, which is inconvenient to use and can cause hypoglycemia.
  • Herbal materials are traditionally known to be low toxicity and have various therapeutic effects.
  • the causes of obesity are genetic factors, environmental factors, metabolic factors, etc.
  • the types can be divided into simple (primary) obesity and symptomatic (secondary) obesity.
  • Primary obesity is caused by excessive nutrition and calorie intake and lack of exercise.
  • Secondary obesity is caused by hypothyroidism, corticosteroids, oral contraceptives, neurostabilizers, steroid hormones, and drugs containing antihistamines. It is known to cause.
  • Obesity is known to cause adult diseases and various metabolic disorders such as diabetes, hypertension, arteriosclerosis, hyperlipidemia, cardiovascular disease, fatty liver, etc.
  • obesity caused by obesity caused by fat tissue caused by constipation
  • WHO World Health Organization
  • Obesity treatments include exercise therapy to increase the use of calories, diet to reduce calorie absorption and drug therapy. However, for busy modern people, exercise therapy and diet alone cannot expect proper effects, so it is appropriate to combine safe drug therapy.
  • sibutramine which reduces appetite by inhibiting reuptake of the neurotransmitters serotonin and noradrenaline, stimulates the sympathetic nerve to increase blood pressure or cardiac output. It can not be prescribed, and can cause serious side effects such as constipation, nausea, indigestion, vomiting, diarrhea, shortness of breath, amblyopia, convulsions, urinary tract infection, and uterine bleeding.
  • orlistat preparations have the effect of inhibiting the lipase activity necessary for fat absorption, thereby reducing the absorption of fat from food, thereby reducing body weight. There is a disadvantage of being inadequate, and there are side effects of increasing the amount of fatty stool or diarrhea or gas.
  • Astragalus membranaceus is a perennial plant of the dicotyledonous rosaceae, distributed in Korea, Japan, Manchuria, northeastern China and eastern Siberia, and is harvested in autumn to remove outcrops and fine roots. It is used as a herbal medicine to dry in, and is commonly referred to as an herbal medicine prepared by drying this way. Herbal medicine has been widely used as a medicine for the treatment of various diseases, and is commonly used as a food ingredient such as Astragalus, and has been recognized as a safe food. Although Astragalus has been used as a raw material for various medicines and foods, it is only used as an auxiliary ingredient of liver drink in general processed foods, and few examples are used as main ingredients of health foods.
  • Astragalus is known to be effective in preventing or treating diabetes or obesity when extracted with other medicinal plants.
  • the Republic of Korea Patent No. 0468653 discloses that the extract extracted from the organic solvent of bellflower, licorice, Astragalus and jujube has an anti-obesity effect, and the Republic of Korea Patent No. 0528565, ginseng, tangerine peel, plum extract, honey, Astragalus and It is disclosed that the extract obtained by hydrothermal extraction of dietary fiber has an anti-obesity effect.
  • the active ingredient of the Astragalus is not sufficiently extracted due to low yield when extracting Astragalus by the hot water extraction method or the organic solvent extraction method, and when only Astragalus is extracted alone, It is not reported that the organic solvent extract itself is effective in obesity.
  • the present inventors also saw that the sulfur can be used as a composition for inhibiting or improving obesity as a part of the component, the organic acid was extracted using a conventional hot water (pressurized) extraction or ethanol alone, but the rat experiment was conducted alone. However, effective effects related to obesity, such as strong cholesterol, triglycerides and weight loss, were not obtained.
  • an object of the present invention is to provide a composition capable of preventing or alleviating diabetes or obesity, while containing as an active ingredient the extract of Astragalus prepared according to the above-mentioned manufacturing method. It is another object of the present invention to provide a composition for lowering blood cholesterol or triglycerides containing the Astragalus extract as an active ingredient, and to provide a composition for preventing or alleviating heart diseases such as fatty liver, hyperlipidemia, and atherosclerosis. .
  • the inventors of the present invention prepare an Astragalus extract using an enzymatic method of hydrolyzing Astragalus using amylase and / or cellulase, thereby increasing the extraction efficiency and increasing the content of an insoluble active ingredient having pharmacological activity in the final product.
  • Astragalus extract prepared using this enzymatic decomposition method was found to be effective in diabetes, obesity and the like unlike conventional extracts, and completed the present invention.
  • the present invention provides the following means.
  • the present invention provides a method for producing an extract of Astragalus, comprising the steps of swelling Astragalus and hydrolyzing with amylase and / or cellulase followed by filtration or precipitation to obtain Astragalus extract.
  • the present invention may further comprise the step of making the powder finely pulverized with a crusher in order to increase the extraction recovery rate of the sulfur when swelling the sulfur and to prevent the formation of precipitates.
  • the present invention comprises the steps of, for example, mixing with sulfur water and heating to swell; Hydrolyzing by adding one or more enzymes of amylase and cellulase to the swelled Astragalus; And it provides a method for producing an extract of the yellowberry using the enzymatic decomposition method comprising the step of filtering or precipitation the hydrolyzed mixed solution to obtain a sulfur extract.
  • the present invention comprises the steps of powdering the sulfur; Mixing the powdered sulfur groups with water and heating to swell; Hydrolyzing by adding one or more enzymes of amylase and cellulase to the swelled Astragalus; And filtering or precipitating the hydrolyzed mixed solution to obtain a sulfur extract.
  • the present invention also provides a composition for the prevention or alleviation of obesity or diabetes, containing the Astragalus extract prepared according to the preparation method as an active ingredient.
  • the present invention further provides a blood sugar, cholesterol or triglyceride-lowering composition containing the Astragalus extract prepared according to the preparation method as an active ingredient, and furthermore, for the prevention or alleviation of heart diseases such as fatty liver, hyperlipidemia, arteriosclerosis, etc.
  • a blood sugar, cholesterol or triglyceride-lowering composition containing the Astragalus extract prepared according to the preparation method as an active ingredient, and furthermore, for the prevention or alleviation of heart diseases such as fatty liver, hyperlipidemia, arteriosclerosis, etc.
  • a method of preparing an extract based on an enzymatic decomposition method hydrolyzes starch and a part of cellulose in an anhydrous polysaccharide with amylase and / or a cellulase so that these polymers and other poorly soluble components are well extracted, thereby improving recovery.
  • the extraction recovery rate of Astragalus component which is hard to be extracted by conventional extraction method is hindered by insoluble polysaccharide and insoluble polysaccharide. It is characterized by six times higher.
  • the Astragalus extract prepared by the manufacturing method according to the present invention is useful as a material for medicines, foods, cosmetics, etc. having new efficacy and functionality by extracting the components that are not well extracted by the existing conventional extraction method.
  • Astragalus extract according to the present invention in a high-fat diet-induced diabetic C57 mouse increases hepatic PPAR-gamma expression and increases insulin and adiponectin in the blood.
  • the blood glucose lowering effect was excellent due to the decrease of triglyceride in the blood, increase of insulin sensitivity and insulin action. Therefore, Astragalus extract produced by the method of the present invention is useful as a hypoglycemic agent of blood sugar and blood triglycerides, and has a superior effect on diabetes, especially insulin-independent diabetes mellitus (type 2 diabetes), which is useful as a composition for preventing and alleviating diabetes.
  • Type 2 diabetes insulin-independent diabetes mellitus
  • the hypoglycemic, blood triglyceride and cholesterol-lowering effects of the Astragalus extract according to the present invention were found to be very excellent compared to the effects of the Astragalus extract produced by the general extraction method.
  • FIG. 1 is a flow diagram schematically showing a method for producing an enzyme conversion sulfur extract according to an embodiment of the present invention.
  • Figure 2 is a high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA), Astragalus extract administration group (HF-0.5HW) extracted by the general extraction method, 70% A graph showing changes in blood sugar levels of C57 mice in the Astragalus extract-administered group (HF-0.5% Et-OH) extracted with ethanol.
  • HF high fat diet
  • Figure 3 is a high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA), Astragalus extract administration group extracted by the general extraction method (HF-0.5% HW), 70 A graph showing changes in triglyceride (TG) and free fatty acids (FFA) in blood of C57 mice in the Astragalus extract administration group (HF-0.5% Et-OH) extracted with% ethanol.
  • HF high fat diet
  • HF-0.5% EA Astragalus extract administration group extracted by the general extraction method
  • HF-0.5% HW Astragalus extract administration group extracted by the general extraction method
  • 70 A graph showing changes in triglyceride (TG) and free fatty acids (FFA) in blood of C57 mice in the Astragalus extract administration group (HF-0.5% Et-OH) extracted with% ethanol.
  • Figure 4 is a graph showing the change of insulin in the blood of C57 mice in the high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA) and the like.
  • HF 5 is a graph showing the change of adiponectin in the blood of C57 mice in the high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA) and the like.
  • Figure 6 is a graph showing changes in hepatic PPAR-gamma of C57 mice in the high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA) and the like.
  • Figure 7 is a graph showing the blood glucose load test (OGTT) results of C57 mice in the high fat diet (HF) and enzyme conversion Astragalus extract administration group (HF-0.25% EA, HF-0.5% EA, HF-1.0% EA) and the like.
  • OGTT blood glucose load test
  • Figure 8 is a graph showing the results of the hourly weight measurement of rats in each group shown in the rat experiment to confirm the effects associated with the obese extract of the Astragalus extract according to the present invention in units of two days.
  • Figure 9 is a graph showing the time-weighted results of the rats in each group in the rat experiment to confirm the effects related to the obesity of the Astragalus extract according to the present invention in units of two weeks.
  • Figure 10 is a graph showing the total feed intake and total weight gain during the experimental period of the rats of each group shown in the rat experiment to confirm the effect of the Astragalus extract according to the present invention.
  • Astragalus is a perennial herb belonging to the legumes, but the use site is not particularly limited, but as a herbal medicine commonly sold on the market, Astragalus means washing and washing the root area. In the present invention, it is preferable to use a yellow-based washing and drying of the root and fine roots (sulfur).
  • step by step the preparation method of the Astragalus extract
  • the swelling step is to loosen the tissue of the yellow sugar polysaccharide so that the action effect of the enzyme is well exhibited, and may be performed by immersing the yellow sugar in water and heating.
  • the expansion conditions are not particularly limited, but in order to loosen the tissue sufficiently to facilitate the enzyme action, the amount of water used is 2 to 10 times based on the weight of the yellow base. It can be carried out by heating for 80 ⁇ 120 °C, preferably 80 ⁇ 100 °C, 0.5 ⁇ 5 hours, but is not necessarily limited to this, and those skilled in the art to properly select the expansion conditions so that the structure of the Astragalus can be sufficiently expanded Can be set. In some cases, it may be expanded by adding 10% or less of ethanol. The expanded sulfuric acid is cooled appropriately. This is because the enzyme added to the next hydrolysis step is a protein, so in order to maintain the activity of the enzyme, the hydrolysis step must be carried out below the temperature at which the denaturation of the protein occurs.
  • the expansion step may further include a powdering step of powdering the sulfur group in order to reduce the expansion time, increase the extraction efficiency while reducing the generation of precipitates in the extract.
  • the powdering step is to improve the extraction efficiency and prevent the precipitation phenomenon in the final product is made by immersion and enzyme action in the Astragalus, may be by mechanical grinding.
  • the particle size of the powdered sulfur group powder is preferably an average particle diameter of 50 ⁇ 300 mesh, but is not limited thereto. The smaller the particle size, the more favorable the expansion and extraction. However, if too finely powdered, the solids having no pharmacological activity may not be filtered out by filtration or precipitation after hydrolysis.
  • the hydrolysis step is to facilitate the extraction of poorly soluble components including insoluble polysaccharides by destroying the polymer surrounding the yellow tissue, and is carried out using amylase and / or cellulase.
  • the hydrolysis conditions are not particularly limited.
  • the weight, temperature and time of the enzyme with respect to the weight of the sulfur may be adjusted.
  • the amount of the enzyme may be used in an amount of 0.1 to 5 parts by weight, preferably 0.1 to 2 parts by weight, and more preferably 0.1 to 1 part by weight, based on 100 parts by weight of sulfur. If the amount is less than 0.1 part by weight, the amount of enzyme is insufficient, so that hydrolysis does not occur sufficiently.
  • the hydrolysis time is not particularly shortened, so it is not necessary to economically use more than 5 parts by weight.
  • Amylase and / or cellulase are added to hydrolyze at 20-110 ° C, preferably 20-70 ° C.
  • the reaction time is preferably 0.5 to 5 hours, but is not limited thereto.
  • For hydrolysis it is necessary to maintain the activity of protein amylase or cellulase. Above 70 ° C, enzyme activity may not appear due to protein denaturation. Although not limited, the activity of the enzyme is less than 20 °C, hydrolysis time may be too long.
  • Amylase or cellulase enzymes used for hydrolysis, can be used in any of them. Commercially available products can be used. Amylase is an enzyme that breaks down starch. It is divided into alpha-, beta- and gamma-amylase. Specific names include 1,4-alpha-D-glucan glucano-hydrolase, glucoamylase, glucosidase and alpha-1,6-glucosidase. All enzymes classified as amylase are available as enzymes that degrade starch.
  • Cellulase is an enzyme that catalyzes the hydrolysis reaction of cellulose, which hydrolyzes the ⁇ -1,4 glycosidic bonds of cellulose, resulting in cellobiose.
  • Cellulase is classified into Endo-celluase, Exo-cellulase, Cellobiase, Oxidative celluase, and Cellose phosphorylase. Any cellulase that participates in the process of breaking down cellulose can be used.
  • the hydrolyzed mixed solution can be filtered or precipitated to obtain an Astragalus extract by the enzymatic decomposition method. That is, the obtained hydrolyzed mixture can be filtered to obtain an extract.
  • the solid content in the process of obtaining the extract may be further compressed by pressing the extract.
  • the press may use a conventional handle herbal extractor or may be manually compressed. This can further increase the extraction efficiency.
  • the pore size and the press pressure of the filter net used for filtration are not limited, but may be suitable for smooth working speed.
  • the hydrolyzate mixed solution may be precipitated and then only the supernatant is taken to obtain an organic extract. However, the method through filtration may be more useful for obtaining the maximum extract while removing the maximum solids.
  • the extract contains amylase and / or cellulase as an enzyme, and may be further subjected to a process of deactivating (deactivating) the amylase and / or cellulase to prevent further hydrolysis of the extract.
  • deactivating it is preferable to heat the extract to 70 ⁇ 130 °C, preferably 70 ⁇ 100 °C. 5 minutes-1 hour of heating time is enough.
  • the precipitate may be mainly a solid component having no pharmacological activity, so that the precipitate may be filtered or precipitated to increase the content of the active ingredient in the extract.
  • the primary extract obtained may be further subjected to precipitation to remove the large solids once more. This process can be accomplished by allowing the primary extract to settle to precipitate solids and take the supernatant. In order to maximize the content of the active ingredient in the final product and to obtain the desired precipitate formation inhibiting effect, the settling time can be appropriately adjusted and about 1 to 20 hours is sufficient.
  • the Astragalus component content of the obtained Astragalus extract is about 4-10%, and can be used as health functional foods and pharmaceutical compositions in which the Astragalus component content needs to be high.
  • the sulfur extract obtained by filtration or precipitation according to the present invention may further comprise the step of concentrating the content of the sulfur component is about 20w / v% ⁇ 99.9w / v%.
  • the production method according to the invention may be further subjected to the step of drying and powdering the extract of the liquid or concentrated liquid.
  • the composition in powder form thus obtained can be stored in a dehumidified packaging. Through this step, by obtaining the Astragalus extract in powder form, there is an advantage that can be formulated or applied in various forms.
  • the Astragalus component contained in the Astragalus extract prepared according to the specific manufacturing method according to the present invention is 30 to 45% by weight based on the initial Astragalus weight. This is a result of improvement of 3 to 6 times or more compared with the recovery rate of the sulfur in the existing Astragalus extract was about 5 to 12% by weight.
  • the present invention provides a composition called Astragalus extract prepared by the above method.
  • the present invention also provides a pharmaceutical use of the Astragalus extract prepared by the above method. That is, the Astragalus extract prepared by the manufacturing method according to the present invention may produce an effect of lowering blood sugar, lowering blood cholesterol or triglyceride in animals including humans. Therefore, by applying these effects, it can be expected to be effective in the prevention or alleviation of heart disease, including diabetes (including type 2 diabetes), fatty liver, hyperlipidemia, arteriosclerosis and the like.
  • the Astragalus extract prepared by the production method according to the present invention can not only suppress the appetite in the animal, including human, but also can reduce the weight to exert the effect of preventing or alleviating obesity.
  • the present invention provides a blood glucose lowering agent, blood cholesterol and triglyceride lowering agent comprising the Astragalus extract prepared according to the method for producing the Astragalus extract using the enzymatic decomposition method according to the present invention as an active ingredient.
  • Another embodiment of the present invention provides a composition for the prevention or alleviation of heart disease, obesity, including diabetes, in particular, type 2 diabetes, fatty liver, hyperlipidemia, arteriosclerosis, and the like including the extract as an active ingredient.
  • the content of Astragalus extract and the like in the pharmaceutical composition can be appropriately adjusted according to the symptoms of the disease, the progress of the symptoms, the condition of the patient, and the like, for example, 0.01 to 99.9% by weight based on the total weight of the composition can be used.
  • compositions may further comprise suitable carriers, excipients and diluents commonly used in the manufacture of pharmaceutical compositions, and oral preparations such as powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like according to conventional methods It may be used in the form of a dosage form, an external preparation, a suppository, or a sterile injectable solution.
  • Carriers, excipients and diluents which may be included here include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl Cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, and the like, but are not limited thereto.
  • Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and these solid preparations include at least one excipient such as starch and calcium carbonate, in addition to the enzyme conversion extract of Astragalus. ), Sucrose (sucrose) or lactose (lactose), gelatin and the like can be prepared by mixing. In addition to simple excipients, lubricants such as magnesium styrate talc may also be used.
  • Liquid preparations for oral administration include suspensions, liquid solutions, emulsions, and syrups.
  • Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories.
  • non-aqueous solvent and suspending agent propylene glycol, polyethylene glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate, and the like may be used, but are not limited thereto.
  • base of the suppository witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like may be used, but are not limited thereto.
  • the preferred dosage of the composition depends on the condition and weight of the patient, the severity of the disease, the form of the drug, the route of administration and the duration, and may be appropriately selected by those skilled in the art.
  • the dosage of the composition of the present invention is preferably 1mg ⁇ 1g / kg per day based on the content of the Astragalus extract as an active ingredient. Administration may be administered once a day or may be divided several times. All modes of administration can be expected, for example by oral, intravenous, intramuscular, subcutaneous injection.
  • the pharmaceutical dosage form of the composition of the present invention may be used in the form of a pharmaceutically acceptable salt of the active ingredient, and may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable collection.
  • the health functional food of the present invention is a combination of various foods, beverages, gums, teas, vitamins for the purpose of lowering blood sugar, lowering blood cholesterol or triglyceride or for preventing, alleviating or improving diabetes (including type 2 diabetes), obesity , Health functional supplements, food additives, and the like, and may be provided in the form of powders, granules, tablets, capsules, or beverages.
  • the dietary supplement of the present invention may be added to foods or beverages for the purpose of suppressing and improving obesity.
  • the content of the composition in the food or beverage may be generally 0.001 to 100% by weight of the total food weight based on the enzyme conversion extract of Astragalus.
  • the health functional food of the present invention is not particularly limited to other ingredients other than containing the Astragalus extract according to the present invention, and may contain various flavors or natural carbohydrates as additional ingredients, such as ordinary food or drink.
  • natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose, for example polysaccharides such as maltose and sucrose, and conventional sugars such as dextrin and cyclodextrin.
  • sugar alcohols such as xylitol, sorbitol, and erythritol, but are not limited thereto.
  • natural flavoring agents such as, tauumatin, stevia extract (e.g., Rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used.
  • synthetic flavoring agents sacharin, aspartame, etc.
  • the ratio of the natural carbohydrate is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention, but is not limited thereto.
  • the health functional food of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, coloring and neutralizing agents (such as cheese and chocolate), pectic acid and salts thereof, alginic acid And salts thereof, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and the like.
  • the compositions of the present invention may also contain pulp for the production of natural fruit juices and fruit juice beverages and vegetable beverages. These components can be used independently or in combination. The proportion of such additives is not particularly limited.
  • Astragalus root material was used by powdering.
  • the powder was pulverized for 5 to 10 minutes by a pulverizer to obtain a powder having an average particle diameter of 50 to 300 mesh.
  • Amylase (amylase DS, Amano) and cellulase (cellulase A, Amano) were hydrolyzed for 3 hours using an amount of 1% by weight of the initial use of Astragalus while maintaining the temperature at 47 ° C. Filtration was performed using a nonwoven fabric (nonwoven fabric for general Chinese medicine manufacture), and the solids were compressed using a press (handle-type herbal extractor, Korea Techno-Pack) to recover the residue, combined with the extract, and the remaining solids were removed.
  • a nonwoven fabric nonwoven fabric for general Chinese medicine manufacture
  • a press handle-type herbal extractor, Korea Techno-Pack
  • the extract was heated at 100 ° C. for 20 minutes to sterilize the enzyme while inactivating it, and then allowed to stand for about 1 hour in a precipitation tank to precipitate solids and to recover the supernatant except the precipitate. Solids in this example were not noticeably high. About 40L of Astragalus enzyme conversion extract was obtained, and the content of Astragalus from Astragalus was about 7%.
  • the obtained extract was concentrated under reduced pressure to 5.6 L (solid content 50 w / v%) to obtain a concentrated concentrate.
  • 125 g (5% of solids) of lactose was added to the concentrated concentrate obtained above, followed by lyophilization to obtain 2925 g (2800 g of pure sulfur component, 10% of water).
  • the yield of pure sulfur component in the powder of the extract was about 40%.
  • a total of 49 C57 mice were divided into seven groups of seven dogs.
  • the first group was a normal control group fed with feed (feed wrap)
  • the second group was a high-fat diet (HF, 45% high fat feed, feed wrap) control group
  • the sixth group (HF-0.5% HW) was supplied with 0.5% of a sample (7% solids recovery compared to sulfur raw material) prepared by freeze-drying the extract obtained by pressurized hot water extraction at 100 ° C. for 3 hours.
  • the seventh group (HF-0.5% Et-OH) is a sample prepared by freeze-drying the extract extracted with pressurized hot water at 100 ° C. for 3 hours using water-ethanol (3: 7v / v) mixture of sulfuric acid (solid recovery rate compared to sulfur raw material 12 %) was mixed with 0.5%.
  • Each feed was limited to 9% by weight of body weight daily and water was fed free.
  • Each dose was well mixed in the powdered feed and fed in powder form, and was bred at 22 ⁇ 1 °C with day and night control for 12 hours.
  • mice fasted for 16 hours after 10 weeks of breeding were stunned with carbon dioxide to collect blood, and the centrifuged serum was analyzed by an automatic blood analyzer (Fujifilm, DRI). -CHEM 35001).
  • the obtained result is shown in FIG.
  • Figure 3 when the intake of the Astragalus extract of Example 1, showed a significant decrease in triglycerides and free fatty acids effect compared to the high fat diet control. The decrease was found to be concentration dependent.
  • the amount of insulin and adiponectin in serum obtained in the same manner as in Example 2.2 was measured by ELISA (BD kit) method. The obtained results are shown in FIGS. 4 and 5.
  • Adiponectin is a type of adipocaine produced from adiposite, which increases insulin sensitivity in liver and muscle cells, and is known to have an anti-arteriosclerosis effect.
  • the macrophage is known as an antidiabetic factor known as a factor that inhibits the production of TNF-alpha, interlukine-6 (IL-6), which is considered as a diabetes-causing factor.
  • IL-6 interlukine-6
  • adiponectin in the blood by the intake of Astragalus extract is considered to be an important mechanism of the hypoglycemic effect of Astragalus and the effect of lowering cholesterol and triglycerides, and is evidence of the antidiabetic effect of Astragalus extract.
  • adiponectin is known as a factor that promotes fatty acidization in muscle cells, etc., which may explain the mechanism of hypotriglyceridemia and cholesterol lowering effect in blood. This is evidence showing the triglyceride and cholesterol lowering effect of the Astragalus extract.
  • PPAR-gamma peroxisome proliferator activated receptor gamma
  • PPAR-gamma sense 5'-GAG ATG CCA TTC TGG CCC ACC AAC TTC GGA-3 '; antisense 5'-TAT CAT AAA TAA GCA TCA ATC GGA TGG TTC-3') and beta-actin (sense 5'-TGG AAT CCT GTG GCA TCC ATG AAA C-3 '; antisense 5'-TAA AAC GCA GCT CAG TAA CAG TCC G-3') for 1 cycle at 97 ° C for 5 minutes, followed by 95 ° C (30 seconds), After repeating 30 cycles at 55 ° C. (30 seconds) and 72 ° C. (1 minute), the reaction was carried out at 72 ° C.
  • the Astragalus extract of Example 1 increases the expression of PPAR-gamma in a concentration-dependent manner.
  • PPAR-gamma is well known for promoting fatty acid metabolism in liver and muscle cells, and lowering blood sugar by increasing glucose uptake.
  • the PPAR-gamma agonist is a hypoglycemic agent that is widely used in the treatment of diabetes.
  • Oral administration of Astragalus extract increases PPAR-gamma expression in the liver and is considered to be a major mechanism of action that contributes to lowering blood glucose and lowering cholesterol and triglycerides.
  • the high-fat diet and 0.5% Astragalus extract (EA-0.5%) were fasted for 16 hours for 8 weeks.
  • C57 mice of 0.5% Astragalus extract (EA-0.5%) were forced orally administered 15 mg / ml of Astragalus extract dissolved in PBS, and after 1 hour, 0.1 ml / 10g of 2 g / kg D-(+)-glucose Intraperitoneally.
  • the high-fat diet group (HF) was forced orally administered the same amount of PBS, and after 1 hour, 2 g / kg of D-(+)-glucose was intraperitoneally administered at 0.1 ml / 10 g body weight.
  • mice fed a normal diet and rats fed a high cholesterol diet as a control group can compare the effect of weight change on the intake of Astragalus extract in SD rat (male) induced by high cholesterol diet. It was designed to be. The change in body weight was measured for 6 weeks while inducing obesity with a high cholesterol diet.
  • the increase in body weight appeared compared to the control group (control) intake of the conventional feed, intake of the Astragalus extract according to the present invention, such as the third group and fourth group
  • the increase in body weight was noticeably reduced as compared to the second group (HCD) fed a high cholesterol diet and the first group (control) fed a normal diet.
  • Figure 10 shows the feed intake and weight gain for each experimental group, as can be seen in Figure 10, the third group (HCD + low) and the fourth group (HCD + high) ingested the Astragalus extract of Example 1 ) Has decreased feed intake compared to the second group (HCD). It is understood that the Astragalus extract according to the present invention inhibits appetite in part.
  • the third and fourth groups were found to have increased feed intake while reducing weight gain compared to the first group, which indicates that Astragalus extract according to the present invention inhibits appetite and promotes fat metabolism in the body. It is assumed to have the same effect.
  • the Astragalus extraction method using the enzymatic decomposition method according to the present invention is not only higher extraction efficiency than the conventional extraction method, but also to extract the components not extracted by the conventional extraction method. Therefore, the Astragalus extract prepared using the enzymatic decomposition method of the present invention can be usefully used in medicine, cosmetics, food, health functional food. More specifically, the Astragalus extract prepared using the enzymatic decomposition method of the present invention may be usefully used as a composition for preventing or alleviating diabetes or a pharmaceutical composition for preventing or alleviating obesity.

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Abstract

L'invention concerne un procédé de production d'extrait d'Astragalus membranaceus par enzymolyse, et une composition pour prévenir ou soulager le diabète ou l'obésité, contenant un principe actif comprenant un extrait d'Astragalus membranaceus produit à l'aide dudit procédé de production. En particulier, l'invention concerne un procédé d'extraction d'Astragalus membranaceus utilisant l'enzymolyse, caractérisé en ce que le taux d'extraction et de récupération de substances insolubles augmente lors de la soumission d'Astragalus membranaceus à une hydrolyse à l'aide d'une amylase et/ou d'une cellulase; et une composition pour prévenir ou soulager le diabète ou l'obésité contenant un principe actif comprenant un extrait d'Astragalus membranaceus produit à l'aide dudit procédé. L'extrait d'Astragalus membranaceus produit par enzymolyse est avantageux pour réduire la glycémie et pour réduire le cholestérol et les triglycérides. Il présente également des effets avantageux pour prévenir ou soulager le diabète (y compris le diabète de type 2), la stéatose hépatique, l'hyperlipidémie, l'artériosclérose et l'obésité.
PCT/KR2009/007591 2009-02-18 2009-12-18 Procédé de production d'extrait d'astragalus membranaceus par enzymolyse, et composition pour prévenir ou soulager le diabète ou l'obésité, contenant un principe actif comprenant un extrait d'astragalus membranaceus produit à l'aide dudit procédé de production WO2010095808A2 (fr)

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KR10-2009-0013579 2009-02-18
KR1020090013579A KR101066434B1 (ko) 2009-02-18 2009-02-18 효소전환 황기 추출물 및 이의 제조 방법
KR1020090126025A KR101088711B1 (ko) 2009-12-17 2009-12-17 효소분해 방법을 이용하여 제조된 황기 추출물을 유효성분으로 함유하는 비만 예방 또는 완화용 약학적 조성물
KR10-2009-0126025 2009-12-17

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CN102631415A (zh) * 2011-03-01 2012-08-15 四川升和药业股份有限公司 中药组合物及其制成品和用途
CN104152491A (zh) * 2014-08-18 2014-11-19 中国农业科学院兰州畜牧与兽药研究所 一种发酵黄芪的制备方法及其总皂苷的提取方法
CN112094741A (zh) * 2020-08-13 2020-12-18 赣州禾绿康健生物技术有限公司 一种接骨木莓提取液的免有机溶剂提纯设备
CN112451678A (zh) * 2020-12-04 2021-03-09 首都医科大学附属北京朝阳医院 HMG-CoA还原酶抑制剂-维D的药物组合物及用途

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CN104152491B (zh) * 2014-08-18 2017-02-15 中国农业科学院兰州畜牧与兽药研究所 一种发酵黄芪的制备方法及其总皂苷的提取方法
CN112094741A (zh) * 2020-08-13 2020-12-18 赣州禾绿康健生物技术有限公司 一种接骨木莓提取液的免有机溶剂提纯设备
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CN112451678A (zh) * 2020-12-04 2021-03-09 首都医科大学附属北京朝阳医院 HMG-CoA还原酶抑制剂-维D的药物组合物及用途
CN112451678B (zh) * 2020-12-04 2022-08-02 首都医科大学附属北京朝阳医院 HMG-CoA还原酶抑制剂-维D的药物组合物及用途

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