WO2017213437A1 - Composition comprenant un extrait de sicyos angulatus ou une fraction de ce dernier en tant qu'ingrédient efficace dans la prévention ou le traitement d'une maladie métabolique - Google Patents

Composition comprenant un extrait de sicyos angulatus ou une fraction de ce dernier en tant qu'ingrédient efficace dans la prévention ou le traitement d'une maladie métabolique Download PDF

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WO2017213437A1
WO2017213437A1 PCT/KR2017/005962 KR2017005962W WO2017213437A1 WO 2017213437 A1 WO2017213437 A1 WO 2017213437A1 KR 2017005962 W KR2017005962 W KR 2017005962W WO 2017213437 A1 WO2017213437 A1 WO 2017213437A1
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Prior art keywords
extract
dyslipidemia
fraction
composition
thorn
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PCT/KR2017/005962
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English (en)
Korean (ko)
Inventor
이철호
노정란
오원근
안진표
김경심
김용훈
이바울
최동희
황정환
서윤정
이인복
최영근
최정현
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한국생명공학연구원
서울대학교 산학협력단
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Publication of WO2017213437A1 publication Critical patent/WO2017213437A1/fr

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    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23K—FODDER
    • A23K10/00—Animal feeding-stuffs
    • A23K10/30—Animal feeding-stuffs from material of plant origin, e.g. roots, seeds or hay; from material of fungal origin, e.g. mushrooms
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • 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)
    • A61K36/42—Cucurbitaceae (Cucumber family)
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/332—Promoters of weight control and weight loss

Definitions

  • the present invention comprises a composition for the prevention, improvement or treatment of metabolic diseases, including the extract of Sicyos angulatus or fractions thereof as an active ingredient, and administering the composition to a subject suspected of metabolic diseases, the prevention of metabolic diseases Or to a method of treatment.
  • Obesity is widely known to cause chronic diseases such as fatty liver, high blood pressure, high blood sugar, diabetes, and cardiovascular diseases. According to the 2007 National Health and Nutrition Survey of the Ministry of Health, Welfare and Family Affairs, 31.7% of Korean adults are obese. Appeared. In addition, 1.7 billion people, or 25% of the world's population, are currently overweight (BMI> 25), and more than 300 million people in the Western region, including 120 million in major countries such as the United States, Europe and Japan, are obese patients (BMI>). 30). In China, 70 million people are known to be obese. In the world, 1 in 5 children are obese and are rapidly increasing, so childhood obesity is a serious social problem.
  • Zenical The domestic and overseas anti-obesity drugs are called Zenical, which is based on orlistat, which is approved by the US FDA.
  • Zenical which inhibits lipase action, gastrointestinal system such as fatty stool, gas production, and fat-soluble vitamin absorption absorption There are side effects.
  • Dyslipidemia is a condition in which high levels of total cholesterol, triglycerides, LDL-cholesterol or low HDL-cholesterol levels are found in the blood.
  • LDL-cholesterol is known to be bad cholesterol because it has a property to be deposited on the blood vessel wall, on the contrary, HDL-cholesterol is a good cholesterol because it functions to inhibit the deposition of fat components on the blood vessel wall. Therefore, if the lipid components such as LDL-cholesterol or triglyceride in the blood increases, blood flow is not smooth and lipid components adhere to the arterial wall, causing chronic inflammatory reactions and narrowing of the arterial wall. (arteriosclerosis) is caused.
  • clots generated from these clots may cause coronary or cerebral blood vessels, causing myocardial infarction, stroke or cerebral infarction (E. Falk et al., Circulation 92, 657-671, 1995).
  • drugs for treating hypercholesterolemia are used in the statin class of drugs that have an inhibitory activity of HMG-CoA reductase, which plays an important role in the synthesis of cholesterol in the liver. It is known to have side effects such as toxicity.
  • fibric acid derivatives fibric acid derivatives
  • digestive disorders may cause side effects such as myopathy.
  • the present inventors have made diligent efforts to discover natural substances for preventing or treating metabolic diseases such as obesity, dyslipidemia and dyslipidemia-related diseases without side effects.
  • the present invention was completed by confirming that there is an increase inhibitory effect, triglyceride reduction and increase inhibitory effect, HDL-cholesterol increase, hypoglycemia lowering blood glucose and improving glucose tolerance, and inhibiting the formation of arterial wall adhesion.
  • One object of the present invention is to provide a pharmaceutical composition for the prevention or treatment of metabolic diseases comprising Sicyos angulatus extract or fractions thereof as an active ingredient.
  • Still another object of the present invention is to provide a food composition for preventing or improving metabolic diseases, including Sicyos angulatus extract or a fraction thereof as an active ingredient.
  • Another object of the present invention to provide a feed composition for the prevention or improvement of metabolic diseases, including Sicyos angulatus extract or a fraction thereof as an active ingredient.
  • Another object of the present invention is to provide a method for preventing or treating metabolic disease, comprising administering the composition to a subject suspected of metabolic disease.
  • the present invention not only reduces the body weight and body fat, but also lowers the triglyceride in the blood, increases HDL-cholesterol, improves blood sugar lowering and glucose tolerance of hyperglycemia, and inhibits the formation of the adhesion of artery walls. It was confirmed that there is an excellent effect in the prevention and treatment of metabolic diseases such as obesity, dyslipidemia or dyslipidemia-related diseases.
  • the thorn gourd extract or a fraction thereof may be applied to drugs, food compositions and feed compositions for the prevention or improvement of metabolic diseases such as obesity, dyslipidemia or dyslipidemia-related diseases.
  • 1 is a graph showing that the weight gain rate of animals treated with ethyl acetate fraction of spiny gourd extract was significantly decreased in the mouse model induced obesity and dyslipidemia due to high fat diet (Student's t-test, * p ⁇ 0.05 vs control).
  • Figure 2 is a graph showing that the body weight of the animals administered the ethyl acetate fraction of spiny gourd extract significantly decreased in the mouse model induced obesity and dyslipidemia due to high fat diet (Student's t-test, * p ⁇ 0.05 vs control).
  • 3 is a graph showing that the body fat of the animals administered the ethyl acetate fraction of spiny gourd extract was significantly reduced in the mouse model inducing obesity and dyslipidemia due to high fat diet (Student's t-test, * p ⁇ 0.05 vs control).
  • FIG. 4 is a graph showing that the triglyceride levels in the animals administered with the ethyl acetate fraction of spiny gourd extract were significantly decreased in the mouse model induced obesity and dyslipidemia due to high fat diet (Student's t-test, * p ⁇ 0.05 vs control).
  • FIG. 5 is a graph showing a significant increase in blood HDL-cholesterol in animals administered with ethyl acetate fraction of spiny gourd extract in a mouse model induced obesity and dyslipidemia due to high fat diet (Student's t-test, * * p ⁇ 0.01 vs control).
  • FIG. 6 is a graph showing a significant decrease in blood glucose of animals treated with ethyl acetate fraction of spiny gourd extract in a mouse model inducing hyperglycemia due to high fat diet (Student's t-test, * p ⁇ 0.01 vs control).
  • FIG. 7 is a graph showing the improvement of glucose tolerance in animals administered with ethyl acetate fraction of spiny gourd extract in a high fat diet-induced hyperglycemia mouse model (A: blood glucose change by measurement time, B: area under curve (AUA, area under curve)) (Student's t-test, * p ⁇ 0.01 vs control).
  • FIG. 8 is a photograph and a graph showing that significantly reduced the formation of arterial wall adhesion in the arteries treated with ethyl acetate fraction of spiny gourd extract in a mouse model deficient in apolipoprotein E (ApoE) to induce atherosclerosis.
  • ApoE apolipoprotein E
  • One embodiment of the present invention provides a composition for the prevention or treatment of metabolic diseases comprising Sicyos angulatus extract or a fraction thereof as an active ingredient.
  • the thorn extract or fractions thereof, the weight loss and increase inhibitory effect, body fat decrease and increase inhibitory effect, triglyceride reduction and increase inhibitory effect, and HDL-cholesterol increase, hyperglycemia lowering blood sugar and improving glucose tolerance effect and arterial wall It has been confirmed that it can be used for the prevention or treatment of metabolic diseases such as obesity, dyslipidemia, or dyslipidemia-related diseases, as it has an inhibitory effect on the formation of liposomes.
  • the term "Sicyos angulatus” is a perennial vine plant belonging to the fruit family, herbicidal activity and antimicrobial activity is known, such as thorn gourd extract is related to obesity, dyslipidemia or dyslipidemia It has not been disclosed that there is a prophylactic or therapeutic effect of metabolic diseases such as diseases, and was first identified by the present inventors.
  • the spiny gourd may be purchased commercially, or may be used collected or grown in nature.
  • extract refers to an extract, such as an extract obtained by an extraction process of spiny gourd, a diluent or concentrate of the extract, a dried product obtained by drying the extract, a modifier or purified product of the extract, or a mixture thereof. And extracts of all formulations that can be formed using extracts.
  • the thorn gourd extract is pulverized after washing and drying the thorn gourd; And extracting the pulverized spiny gourd with a solvent selected from the group consisting of water, C1 to C6 alcohols, and mixed solvents thereof.
  • the thorn extract may be specifically extracted with methanol, ethanol, propanol, butanol, pentanol or hexanol, more specifically may be extracted with ethanol, but is not limited thereto.
  • the extraction method is not particularly limited and may be extracted at room temperature or warmed under conditions where the active ingredient is not destroyed or minimized. More specifically, the method for obtaining a thorn gourd extract in the present invention is as follows.
  • the dried spiny foil is a polar solvent of C1 to C6 alcohols such as water, methanol, ethanol, propanol, butanol, pentanol and hexanol in volumes of about 2 to 20 times, specifically about 3 to 5 times the weight, or A mixed solvent having a mixing ratio of about 1: 0.1 to 1:10 can be used as the elution solvent, but is not limited thereto.
  • the extraction temperature may be 1 to 100, specifically 25, the extraction period may be about 1 hour to 10 days, specifically 2 to 50 hours, the extraction method is shaking extraction, hot water extraction, cold extraction, reflux cooling Extraction, ultrasonic extraction, or a combination thereof, but is not limited thereto.
  • the process of soaking with 70% ethanol for 2 hours and then standing at room temperature for 1 hour was repeated three times a day, followed by extraction, filtration and concentration, and freeze-dried to obtain the spinach extract.
  • the prickly pear extract can be extracted from natural, hybrid, mutant plants, and can be extracted from plant tissue culture.
  • fraction in the present invention means the result obtained by performing the fractionation to separate a specific component or a specific component group from a mixture comprising various various components.
  • the fractionation method for obtaining the fraction is not particularly limited, and may be performed according to a method commonly used in the art.
  • an extract obtained by extracting spiny gourd may be treated with a predetermined solvent to obtain a fraction from the extract.
  • the kind of the fractionation solvent used to obtain the fraction in the present invention is not particularly limited, and any solvent known in the art may be used.
  • Non-limiting examples of the fractionation solvents include polar solvents such as water and alcohols; And nonpolar solvents such as hexane, ethylacetate, acetone, and chloroform. These may be used alone or in combination of two or more thereof.
  • the barley extract was extracted with 70% ethanol and concentrated to obtain a fraction obtained by solvent fractionation with ethyl acetate.
  • prevention means any action that inhibits or delays the development of metabolic diseases such as obesity, dyslipidemia or dyslipidemia related diseases by administration of the thorn gourd extract, fractions thereof, or the composition according to the present invention.
  • treatment in the present invention refers to any action in which the symptoms of the disease are improved or beneficially altered by administration of the thorn extract, fractions thereof or the composition according to the present invention.
  • metabolic disease refers to a disease caused by metabolic disorders in vivo, and may specifically include obesity, dyslipidemia or dyslipidemia related diseases, but is not limited thereto. Does not. In the present invention it was confirmed that the thorn gourd extract is effective in the prevention or treatment of metabolic diseases.
  • the term "obesity” refers to a state in which body fat is excessively accumulated. Criteria for obesity may be described as obesity if the body fat is 25% or more of body weight, women more than 30-35%, body mass general measurement methods as is shown by the weight (kg) / height (m) 2 index (BMI; Body Mass Index) is widely used.
  • Western body mass index of over 30kg / m 2 is defined as obesity, 25 ⁇ 30kg / m 2 is defined as overweight, in the case of Asians more than 28kg / m 2 , obesity, 23 ⁇ 28kg / m 2 Is overweight.
  • obesity may be defined on the basis of a waist to hip ratio (WHR) or abdominal fat mass, and the present invention includes all cases of obesity defined by a general standard other than the above-mentioned criteria. do.
  • WHR waist to hip ratio
  • the present invention using the thorn gourd extract confirmed the weight and body fat reduction and increase inhibitory effect.
  • the administration of the thorn gourd extract is more effective than the thorn gourd extract, so that the ethyl acetate fraction of the thorn gourd extract was administered in the remaining experiments.
  • the weight change according to the administration of ethyl acetate fraction of the thorn gourd extract was measured in the mice fed the high-fat diet for 8 weeks, and as a result, the weight gain rate was decreased in the group administered the ethyl acetate fraction of the thorn gourd extract compared to the control group.
  • the mouse was subjected to autopsy to measure the weight of the subcutaneous fat, the body fat was significantly reduced in the group administered the ethyl acetate fraction of thorn gourd extract compared to the control group It was confirmed that there was (Fig. 3).
  • the term “dyslipidemia” refers to a state in which lipid components such as triglycerides, LDL cholesterol, phospholipids and free fatty acids are increased or HDL-cholesterol is decreased in blood.
  • the dyslipidemias include hyperlipidemia, high LDL-cholesterolemia, low HDL-cholesterolemia and hypertriglyceridemia.
  • the ethyl acetate fraction of the spiny gourd extract was used to confirm the effect of inhibiting triglyceride in blood and increasing the blood HDL-cholesterol.
  • dyslipidemia related disease refers to various diseases caused by dyslipidemia, and the diseases that can be treated or prevented by the pharmaceutical composition of the present invention include, but are not limited to, arteriosclerosis, myocardial infarction. , Stroke, cerebral infarction, hypertension, hyperglycemia, diabetes, tangier disease, ischemic heart disease and ischemic brain disease.
  • blood triglyceride and HDL-cholesterol levels were measured in accordance with the administration of ethyl acetate fraction of spiny gourd extract in a mouse model inducing obesity and dyslipidemia due to high fat diet.
  • the triglyceride fraction was significantly decreased in blood triglyceride (FIG. 4), and significantly increased in HDL-cholesterol (FIG. 5).
  • blood glucose was measured according to the administration of ethyl acetate fraction of the thorn gourd extract.
  • composition comprising the thorn gourd extract of the present invention or a fraction thereof has an excellent effect for the prevention or treatment of metabolic diseases such as obesity, dyslipidemia or dyslipidemia-related diseases.
  • the pharmaceutical composition of the present invention may further include a pharmaceutically acceptable carrier.
  • compositions of the invention may be prepared in pharmaceutical formulations using methods well known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to a mammal.
  • the active ingredient is mixed or diluted with the carrier or enclosed in a carrier in the form of a container.
  • compositions of the present invention can be used in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like, oral formulations, external preparations, suppositories, and sterile injectable solutions according to conventional methods. And may further comprise suitable carriers, excipients and diluents conventionally used in the preparation of the composition.
  • carriers that may be included in the pharmaceutical compositions of the present invention 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.
  • diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used.
  • Solid form preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, which include at least one excipient such as starch, calcium carbonate, sucrose in the compound. Or lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used.
  • Oral liquid preparations include suspensions, solutions, emulsions, and syrups, and may include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin. have.
  • Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized formulations, 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 can be used.
  • base of the suppository witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.
  • the term "administration" means introducing the pharmaceutical composition of the present invention to a patient in any suitable manner.
  • the mode of administration of the pharmaceutical composition according to the present invention is not particularly limited, and may be in accordance with methods commonly used in the art.
  • the mode of administration is not limited as long as it can reach the target tissue, but may be intraperitoneal administration, intravenous administration, intramuscular administration, subcutaneous administration, intradermal administration, oral administration, topical administration, intranasal administration.
  • the pharmaceutical compositions according to the invention may be prepared in various formulations depending on the desired mode of administration.
  • the pharmaceutical composition of the present invention may be administered in a pharmaceutically effective amount.
  • the "pharmaceutically effective amount” means an amount sufficient to treat the disease at a reasonable benefit / risk ratio applicable to medical treatment, and the effective dose level is the type of subject and its severity, age, sex, type of virus infected, drug Activity, sensitivity to drug, time of administration, route of administration and rate of release, duration of treatment, factors including concurrent use of drugs, and other factors well known in the medical arts.
  • a typical daily dosage of a pharmaceutical composition according to the invention may be administered such that the spiny gourd extract or fractions thereof is administered at 10 to 1,000 mg / kg, specifically 10 to 600 mg / kg, divided once or in several portions. May be administered.
  • the ethyl acetate fraction of spiny gourd extract is administered orally once a day at a concentration of 300 mg / kg, thereby effectively treating a mouse model of obesity and dyslipidemia induced by high fat diet. It was confirmed.
  • composition of the present invention may be administered daily or intermittently, and the number of administrations per day may be administered once or divided into two or three times.
  • composition of the present invention can be used alone or in combination with other drug treatment for the prevention or treatment of obesity, dyslipidemia or dyslipidemia related diseases. Taking all of the above factors into consideration, it is important to administer an amount that can obtain the maximum effect in a minimum amount without side effects, and can be easily determined by those skilled in the art.
  • Another aspect of the present invention provides a method for preventing or treating a metabolic disease, comprising administering the pharmaceutical composition to a subject suspected of metabolic disease.
  • the metabolic disease may include obesity, dyslipidemia or dyslipidemia related diseases, but is not limited thereto.
  • the method provides a method for preventing or treating a metabolic disease, comprising administering the composition to a subject suspected of metabolic disease.
  • Prickly pear extracts, fractions, metabolic diseases are as described above.
  • the term "individual” means all animals, including humans, who have or are likely to develop metabolic diseases.
  • the animal may be a mammal such as, but not limited to, a human, a cow, a horse, a sheep, a pig, a goat, a camel, a antelope, a dog, a cat, and the like, which require treatment of similar symptoms.
  • the method of preventing or treating the present invention specifically includes administering the composition in a pharmaceutically effective amount to a subject having or at risk of developing a metabolic disease such as obesity, dyslipidemia or dyslipidemia related diseases. It may include.
  • Yet another aspect of the present invention provides a food composition for preventing or improving metabolic diseases, including thorn gourd extract or a fraction thereof as an active ingredient.
  • the metabolic disease may include obesity, dyslipidemia or dyslipidemia related diseases, but is not limited thereto.
  • Prickly pear extracts, fractions, metabolic diseases are as described above.
  • the food composition of the present invention can be consumed on a daily basis, it is very useful because it can be expected to prevent or improve metabolic diseases such as obesity, dyslipidemia or dyslipidemia-related diseases.
  • the term "improvement” means any action that at least reduces the parameters associated with a condition, e.g., the degree of symptoms, that are treated by administration of a composition comprising a spiny gourd extract or fractions thereof.
  • the food composition for preventing or improving metabolic diseases of the present invention includes the form of pills, powders, granules, acupuncture, tablets, capsules or liquids, and the like to which the composition of the present invention can be added, for example, Various foods, for example, drinks, chewing gum, tea, vitamin complexes, dietary supplements and the like.
  • ingredients except for containing the thorn gourd extract or a fraction thereof as an essential ingredient that may be included in the food composition of the present invention, and various herbal extracts, food supplement additives or natural carbohydrates, and the like, as in general foods, are additional ingredients. It may contain as.
  • the food supplement additives include food supplement additives conventional in the art, such as flavoring agents, flavoring agents, coloring agents, fillers, stabilizers and the like.
  • natural carbohydrates examples include monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sucrose and the like; And conventional sugars such as polysaccharides such as dextrin, cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol.
  • natural flavoring agents for example, rebaudioside A, glycyrrhizin, etc.
  • synthetic flavoring agents sacharin, aspartame, etc.
  • the food composition of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, colorants and fillers (such as cheese and chocolate), pectic acid and salts thereof, alginic acid and its Salts, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and the like.
  • Others may contain pulp for the production of natural fruit juices and fruit juice drinks and vegetable drinks. These components can be used independently or in combination.
  • the health supplement food in the present invention includes a health functional food and health food.
  • the functional food is the same term as a food for special health use (Food for special health use, FoSHU), in addition to the nutritional supply, the processed food, so that the bioregulatory function appears efficiently, high medical effect Means food.
  • the term "functionality” means obtaining useful effects for health purposes such as nutrient control or physiological action on the structure and function of the human body.
  • the food of the present invention may be prepared by a method commonly used in the art, and the preparation may be performed by adding raw materials and ingredients commonly added in the art.
  • the formulation of the food may also be prepared without limitation as long as the formulation is recognized as a food.
  • Food composition of the present invention can be prepared in various forms of formulation, unlike the general medicine has the advantage that there is no side effect that can occur when taking a long-term use of the drug as a food raw material, excellent portability, Food can be taken as an adjuvant for enhancing the effect of preventing or improving metabolic diseases such as obesity, dyslipidemia or dyslipidemia related diseases.
  • the present invention provides a feed composition for the prevention or improvement of metabolic diseases comprising a thorn gourd extract or a fraction thereof as an active ingredient.
  • the metabolic disease may include obesity, dyslipidemia or dyslipidemia related diseases, but is not limited thereto.
  • the feed composition may include a feed additive.
  • the feed additive of the present invention corresponds to a feed supplement in the Feed Control Act.
  • feed may refer to any natural or artificial diet, one meal, or the like, or a component of the one meal, for the animal to eat, ingest, and digest.
  • the kind of the feed is not particularly limited, and may be used a feed commonly used in the art.
  • Non-limiting examples of the feed include, but are not limited to, vegetable feeds such as cereals, fruits, food processing by-products, algae, fibres, pharmaceutical by-products, oils, starches, gourds or grain by-products; And animal feeds such as proteins, minerals, fats and oils, minerals, fats and oils, single cell proteins, zooplankton or foods. These may be used alone or in combination of two or more thereof.
  • Example 2 acute with corn fat intake Triglyceridemia In induced mouse model Barbed Extracts and Its Fraction Changes in Triglyceride Levels in Blood with Administration
  • Example 2 After fasting for 14 hours in 9-week-old male C57BL / 6 mice, the thorn gourd extract prepared in Example 1 and its ethyl acetate fraction were administered once daily at a concentration of 300 mg / kg, 30 minutes later, Corn oil (Corn oil, Sigma, USA), which is mostly triglycerides, was orally administered to each group of mice at a concentration of 9 g / kg.
  • Corn oil Corn oil, Sigma, USA
  • blood was collected from a heparin-treated capillary tube from the retro-orbital sinus of each animal, and centrifuged at 10,000 rpm for 10 minutes. The upper plasma was obtained and analyzed directly using an automatic blood analyzer (Hitachi 7150, Japan).
  • the triglyceride and the level of blood in the control group were 223 ⁇ 6mg / dl, whereas the group treated with spinach extract (SA extract) and its ethyl acetate fraction (SA fraction) were 197 ⁇ 13mg / dl and 190 ⁇ , respectively.
  • 2 mg / dl was found to be significantly reduced (Student's t-test, * p ⁇ 0.05) (Table 1). From these results, it was confirmed that the thorn gourd extract and fractions thereof have an effect of preventing hypertriglyceridemia or obesity by inhibiting the absorption of lipid components such as triglycerides from the outside through the diet.
  • Example 3-1 high fat diet ingested mice and Prickly Oral administration condition
  • Example 3-2 high fat Diet In ingested mouse model Barbed Weight change with administration
  • mice Eighty-week-old male C57BL / 6 mice were fed with ethyl acetate fraction of the spiny gourd extract prepared in Example 1 at a concentration of 300 mg / kg once a day while eating a high fat diet. Measured weekly. As a result, the weight of the mice administered the ethyl acetate fraction of the thorn extract was 27 ⁇ 0.6 g at 2 weeks of administration, compared to 30 ⁇ 0.8 g in the control group, and the weight gain was significantly inhibited. Lasting to 8 weeks, the weight of the control group was 41 ⁇ 0.5g, compared to 35 ⁇ 0.4g in the bakbak group.
  • the group administered with the ethyl acetate fraction of the spiny gourd extract was found to have a 20% lower weight gain than the control group (FIGS. 1 and 2). That is, it was found that the thorn gourd extract and its fractions are very excellent in weight loss and weight increase inhibitory effect.
  • Example 3-3 high fat Diet In ingested mouse model Barbed Body fat change with administration
  • Example 3-4 high fat Diet In ingested mouse model Barbed Changes in Triglyceride and HDL-Cholesterol Levels in Blood Following Administration
  • mice Eighty-week-old male C57BL / 6 mice were fed an ethyl acetate fraction of thorn gourd extract prepared in Example 1 for 8 weeks in a mouse model ingesting a high fat diet and inducing obesity and dyslipidemia.
  • Blood was collected using a capillary tube treated with heparin from a retro-orbital sinus. The collected blood was centrifuged at 10,000 rpm for 10 minutes to obtain plasma in the upper layer, and analyzed directly using an automatic blood analyzer (Hitachi 7150, Japan).
  • the blood triglycerides and levels in the control group were 271 ⁇ 63mg / dl, while the ethyl acetate fraction of thorn extract was significantly reduced to 129 ⁇ 11mg / dl (Fig. 4).
  • the control group was 85 ⁇ 8 mg / dl, whereas the group treated with ethyl acetate fraction of thorn extract was significantly increased to 132 ⁇ 10 mg / dl (FIG. 5). From these results, it was confirmed that the thorn gourd extract and its fractions lower the triglyceride in the blood and increase the HDL-cholesterol to effectively inhibit and improve dyslipidemia.
  • Example 3-5 high fat Diet In ingested mouse model Barbed Changes in blood sugar levels with administration
  • mice Eighty-week-old male C57BL / 6 mice were fed a high fat diet to induce hyperglycemia in a mouse model for 8 weeks, the ethyl acetate fraction of the thorny bark extract prepared in Example 1 at a concentration of 300 mg / kg 1 day 1 Oral administration was performed and blood glucose changes were measured at two week intervals.
  • the blood glucose level was significantly decreased in the group administered with ethyl acetate fraction of thorn bark extract from 2 weeks after administration, and at 8 weeks of administration, the control group showed 227 ⁇ 6 mg / dL at the start of administration.
  • the blood sugar level was increased by 16% compared to 196 ⁇ 6 mg / dL, whereas the group treated with ethyl acetate fraction of thorn extract showed 163 ⁇ mg / dL, 21% higher than 206 ⁇ 4 mg / dL at the start of administration. It was confirmed that the degree was significantly reduced (Fig. 6).
  • Example 3-6 high fat Diet In ingested mouse model Barbed According to administration Glucose tolerance change
  • mice in the control and experimental groups were tested for glucose tolerance test.
  • all the mice were fasted for 16 hours, intraperitoneally injected with glucose adjusted to a concentration of 2 g / kg, and blood was collected at 0, 30, 60, 90 and 120 minutes to measure blood glucose.
  • the measured blood glucose was shown in a line graph, and the area under the curve of the control group and the experimental group shown in the graph of the blood glucose change line and the X-axis of the graph was calculated and compared.
  • Example 4 Apolipoprotein E ( ApoE Deficiency induced by atherosclerosis in mouse model Artery wall Policy change
  • mice 8 week old male ApoE deficient mice were ingested atherosclerosis diet (Dyets # 102571, USA) containing 1.25% cholesterol for 8 weeks. Mice were divided into two groups, and both groups were fed orally with an atherosclerosis diet, and the oral solution was treated with 0.5% CMC solution in the control group and 0.5% CMC suspension in ethyl acetate fraction of 500mg / kg once daily. Administered directly. During the experiment, feed intake and water were freely available to all animals, and the breeding conditions of the animal room were maintained in a SPF environment controlled by a temperature of 22 ⁇ 2 ° C, 55 ⁇ 10% humidity, and a 12 hour light cycle. The experiment was performed.
  • the group of barbed gourd fractions administered at a concentration of 500 mg / kg showed that the degree of red coloration in the arterial wall was reduced visually.
  • the control group showed 32.3 ⁇ 2.7%, 18.5 ⁇ 4.0%.
  • the spinach fraction administered group was found to be very low as 57 ⁇ 4% of the adherence ratio of the control group (100 ⁇ 3%) of the lichen planar (atherosclerosis) rate of the inner artery wall. (Student's t-test, * p ⁇ 0.01) (FIG. 8).
  • the thorn extract or fractions thereof have weight loss and increase inhibition effect, body fat reduction and increase inhibition effect, triglyceride reduction and increase inhibition effect, HDL-cholesterol increase, hyperglycemia lowering blood sugar and improving glucose tolerance and artery It was found that there is an inhibitory effect on the formation of the paper fibers in the inner wall. This suggests that the thorn gourd extract of the present invention or a fraction thereof has a very good effect on the prevention, improvement and treatment of metabolic diseases such as obesity, dyslipidemia or dyslipidemia related diseases.

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Abstract

La présente invention concerne une composition comprenant un extrait de Sicyos angulatus ou une fraction de ce dernier en tant qu'ingrédient efficace pour prévenir, soulager ou traiter une maladie métabolique, et un procédé de prévention ou de traitement d'une maladie métabolique, comprenant une étape d'administration de la composition à un sujet susceptible de présenter une maladie métabolique.
PCT/KR2017/005962 2016-06-09 2017-06-08 Composition comprenant un extrait de sicyos angulatus ou une fraction de ce dernier en tant qu'ingrédient efficace dans la prévention ou le traitement d'une maladie métabolique WO2017213437A1 (fr)

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WO2019156498A1 (fr) * 2018-02-09 2019-08-15 한국 한의학 연구원 Composition comprenant un extrait de sicyos angulatus en tant que principe actif servant à prévenir, améliorer ou traiter une maladie attribuée à un effet secondaire d'un agent anticancéreux

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KR20150018365A (ko) * 2013-08-09 2015-02-23 고려대학교 산학협력단 가시박으로부터 시킴산을 수득하는 방법
KR20170069170A (ko) * 2015-12-10 2017-06-20 한국생명공학연구원 가시박 추출물을 유효성분으로 포함하는 간 질환의 치료 또는 예방용 조성물

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