KR101762736B1 - Composition for Anti-obesity Using Clausena excavata - Google Patents
Composition for Anti-obesity Using Clausena excavata Download PDFInfo
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- KR101762736B1 KR101762736B1 KR1020150071563A KR20150071563A KR101762736B1 KR 101762736 B1 KR101762736 B1 KR 101762736B1 KR 1020150071563 A KR1020150071563 A KR 1020150071563A KR 20150071563 A KR20150071563 A KR 20150071563A KR 101762736 B1 KR101762736 B1 KR 101762736B1
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- extract
- obesity
- clausena
- extracts
- composition
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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Abstract
The present invention discloses an anti-obesity composition using a Clausena xcavata extract having the activity of inhibiting the differentiation of preadipocytes into adipocytes.
Description
The present invention relates to a process for the preparation of < RTI ID = 0.0 & The present invention relates to a composition for an anti-obesity treatment using an excavata extract.
Obesity is defined as a state of abnormal accumulation of energy in the body resulting from an imbalance of energy intake and consumption (Clinical Obstetrics 28: 675-689, 1998; Clinical Obesity (eds. MJ) 248-89 (Blackwell Science, Oxford 1998) and the World Health Organization (WHO) see obesity as the target of a disease to be treated.
The World Health Organization (WHO) defines an Asian standard body mass index (BMI) of 23 to 25 as overweight, 25 to 30 as obesity, and 30 as elevation obesity.
The causes of obesity include environmental dietary factors such as high fat and high calorie diet, lack of exercise due to busy social environment, and endocrine abnormalities, among which 50 to 70% of obesity is caused by environmental factors And the rest is known to be caused by genetic factors.
The energy in the body is stored in the form of triglyceride in the fat cells. When the energy source in the body is exhausted, the stored fat is decomposed into free fatty acid and glycerol and used as an energy source. However, And increases the amount of stored fat in the body, which is a direct cause of obesity.
There are three major pharmacological mechanisms for the development of obesity treatment drugs so far: the mechanism of interfering with the absorption of fat in the small intestine, the mechanism of suppressing the appetite, and the excess energy entering the body without being stored as fat, It is the mechanism that promotes energy metabolism and releases it into heat.
Xenical ™ (Roche Pharmaceuticals, Switzerland) is a representative treatment for obesity using a pharmacological mechanism to inhibit fat digestion and absorption, and Reductil ™ (Abbott Laboratories, Inc.) is a representative treatment for obesity using a pharmacological mechanism to suppress appetite. , USA). Exorise (Exorise ™, Acopama, France) is a representative treatment for obesity using a pharmacological mechanism for promoting energy metabolism in the body.
In the adipocyte differentiation, fat accumulation occurs and fat cell specific proteins (aP2, FAS, GLUT4, LPL, leptin) are induced to express PPARγ (peroxisome (C / EBBR), adipocyte determination differentiation factor 1 (ADR1 / SREBP1c) / (sterol regulatory element binding protein 1c), proliferator-activated receptor γ, C / EBP family (CCAAT / enhancer binding proteins C / EBRα, C / EBRβ and C / EBRδ) And adipokines are known to play a pivotal role ( Genes De 2000, 14 (11) 1293-1307) ( Physiol Rev 1998, 78 (3): 783-809; Annu Rev Biochem 2008, 77: 289-312; Genes Dev 1996, 10: 1096-1107).
Thus, attempts have been made to treat obesity through adipocyte regulation, which attempts to reduce the number of adipocytes by inhibiting adipocyte differentiation, suggesting that these transcription factors and adipokines are targets for the development of new therapeutic agents for obesity .
The present invention discloses an anti-obesity activity of the extract of Clausena xcavata, which is confirmed through the activity of inhibiting the differentiation of preadipocytes into adipocytes.
It is an object of the present invention to provide an anti-obesity composition using Clausena xcavata extract.
Specific objects of the present invention will be described below.
As shown in the following Examples and Experimental Examples, the present inventors have found that the extract of Clausena xcavata ethanol solution (70% (v / v)) extracts the differentiation of 3T3-L1 mouse preadipocytes into adipocytes , Respectively. Here, Clausena X Cabata is a plant belonging to the family Rutaceae, which is native to Bangladesh, Bhutan, Cambodia, Vietnam and India.
The composition for anti-obesity of the present invention is characterized by containing Clausena xcavata extract as an active ingredient.
In the present specification, the term "Clausena xcavata extract" refers to an extract of Clausena xcavata stem, leaf, fruit, flower, root or the like to be extracted with water, a lower alcohol having 1 to 4 carbon atoms such as methanol, ethanol or butanol, (DMF), dimethylsulfoxide (DMSO), 1,3-butylene glycol, propylene glycol, or a mixed solvent thereof, in the presence of an organic solvent such as methanol, ethanol, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, Extracts obtained by leaching using a supercritical extraction solvent such as carbon dioxide or pentane or fractions obtained by fractionating the extracts, and the extraction method refers to a fraction obtained by fractionating the extract , Reflux, warming, ultrasonic irradiation, supercritical extraction, and the like. In the case of the fractionated extract, the crude extract is suspended in a specific solvent, and the fractions obtained by mixing and leaving with a solvent having a different polarity are adsorbed on a column packed with silica gel or the like, and a hydrophobic solvent, a hydrophilic solvent or a mixture thereof Quot; means a fraction obtained by using a solvent as a mobile phase. Also, the meaning of the extract includes a concentrated liquid extract or a solid extract in which the extraction solvent is removed by a method such as freeze drying, vacuum drying, hot air drying, spray drying and the like. Preferably an extract obtained by using water, ethanol or a mixed solvent thereof as an extraction solvent, and more preferably an extract obtained by using a mixed solvent of water and ethanol as an extraction solvent.
In the present specification, the term " active ingredient "alone means an ingredient which exhibits the desired activity or which can exhibit activity together with a carrier which is not itself active.
In the present specification, "anti-obesity" means a decrease in body fat and / or a decrease in body weight. Thus, it includes the prevention of obesity and the treatment of obesity, and further includes the reduction of weight / body fat for beauty or health purposes (aka diet) although the weight is not classified as obesity or overweight.
In the present specification, the term "obesity" means an abnormally increased state of adipose tissue, whether it is obesity due to genetic factors or obesity due to environmental factors. When the body mass index (BMI) It is meant to include obesity (for BMI> 30.0), obesity (for BMI 25-30), and overweight (for BMI between 23 and 25).
The anti-obesity composition of the present invention may contain the active ingredient in any amount (effective amount) as long as it can exhibit anti-obesity activity, depending on the purpose of use, formulation, compounding purpose, etc. A typical effective amount is based on the total weight of the composition To < RTI ID = 0.0 > 99.999% < / RTI > by weight. Here, "effective amount" refers to the amount of active ingredient capable of inducing an anti-obesity effect. Such effective amounts can be determined experimentally within the ordinary skill of those skilled in the art.
The subject to which the composition of the present invention can be applied (prescription) is preferably a mammal and a person, particularly a human.
The anti-obesity composition of the present invention can be identified as a food composition in a specific embodiment.
The food composition of the present invention can be manufactured as a health functional food such as a functional beverage, a health supplement food, a food supplement for a special nutrition, and the form of the food is a beverage such as tea, juice, carbonated drink, ionic drink, milk, Food products such as processed oil, gum, rice cakes, Korean lamb, bread, confectionery, cotton, etc., powders for health functional foods such as powders, tablets and capsules.
The food composition of the present invention may contain sweetening agents, flavoring agents, physiologically active ingredients, minerals and the like in addition to the active ingredients thereof.
Sweetening agents may be used in an amount that sweetens the food in a suitable manner, and may be natural or synthetic. Preferably, natural sweeteners are used. Examples of natural sweeteners include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose and maltose.
Flavors may be used to enhance taste or flavor, both natural and synthetic. Preferably, a natural one is used. When using natural ones, the purpose of nutritional fortification can be performed in addition to the flavor. Examples of natural flavoring agents include those obtained from apples, lemons, citrus fruits, grapes, strawberries, peaches, and the like, or those obtained from green tea leaves, Asiatica, Daegu, Cinnamon, Chrysanthemum leaves and Jasmine. Also, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, banks and the like can be used. The natural flavoring agent may be a liquid concentrate or a solid form of extract. Synthetic flavors may be used depending on the case, and synthetic flavors such as esters, alcohols, aldehydes, terpenes and the like may be used.
Examples of the physiologically active substance include catechins such as catechin, epicatechin, gallocatechin and epigallocatechin, and vitamins such as retinol, ascorbic acid, tocopherol, calciferol, thiamine and riboflavin.
As the mineral, calcium, magnesium, chromium, cobalt, copper, fluoride, germanium, iodine, iron, lithium, magnesium, manganese, molybdenum, phosphorus, potassium, selenium, silicon, sodium, sulfur, vanadium and zinc can be used.
In addition, the food composition of the present invention may contain preservatives, emulsifiers, acidifiers, thickeners and the like as needed in addition to the above sweeteners.
Such preservatives, emulsifiers and the like are preferably added in a very small amount as long as they can attain an application to which they are added. The term " trace amount " means, when expressed numerically, in the range of 0.0005% by weight to about 0.5% by weight based on the total weight of the food composition.
Examples of the preservative which can be used include calcium sodium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate and EDTA (ethylenediaminetetraacetic acid).
Examples of the emulsifier which can be used include acacia gum, carboxymethyl cellulose, xanthan gum, pectin and the like.
Examples of the acidulant that can be used include acid, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, and phosphoric acid. Such an acidulant may be added so that the food composition has a proper acidity for the purpose of inhibiting the growth of microorganisms other than the purpose of enhancing the taste.
Agents that may be used include suspending agents, sedimentation agents, gel formers, bulking agents and the like.
In addition, the food composition of the present invention may contain a powder or extract derived from a natural product in order to improve flavor or palatability and to impart other functionalities, and may be a pregelatinized powder or extract, a soybean powder or extract, a shell powder or extract, Extracts, juice or extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng, extracts of ginseng juice or extracts, extracts of ginseng juice or extracts, extracts of ginseng juice or extracts, extracts of spinach juice or extracts, lotus juice or extracts, Powder or extract, licorice powder or extract, granular powder or extract, granular powder or extract, sine powder or extract, pistachio powder or extract, ginger powder or extract, jujube powder or extract, Water-based powder or extract, dried powder or extract, Or extract, dermis (crustacea bark) powder or extract, ginger powder or extract, green tea powder or extract, omija powder or extract, hinoki powder or extract, dirt powder or extract, egg yolk powder or extract, cinnamon powder or extract, Cyano and the like can be exemplified. Such an extract may be obtained by mixing the object to be extracted.
In another specific embodiment, the composition of the present invention can be identified as a pharmaceutical composition.
The pharmaceutical composition of the present invention may be in a form suitable for oral use (tablets, suspensions, granules, emulsions, capsules, syrups, etc.), parenteral formulations (sterile injectable aqueous or non- Ointments, ointments, solutions, creams, ointments, gels, lotions, patches, and the like).
The term "pharmaceutically acceptable" as used herein means that the application (subject) does not have an adaptive or higher toxicity (sufficiently low toxicity) without inhibiting the activity of the active ingredient.
Examples of pharmaceutically acceptable carriers include lactose, glucose, sucrose, starch (e.g. corn starch, potato starch, etc.), cellulose, derivatives thereof (e.g. sodium carboxymethylcellulose, ethylcellulose, etc.), malt, gelatin, talc, (E.g., peanut oil, cottonseed oil, sesame oil, olive oil, etc.), polyols (e.g., propylene glycol, glycerin, etc.), alginic acid, emulsifiers (e.g., TWEENS), wetting agents (For example, sodium lauryl sulfate), a coloring agent, a flavoring agent, a tableting agent, a stabilizer, an antioxidant, a preservative, water, a saline solution and a phosphate buffer solution. The carrier may be selected from one or more of suitable pharmaceutical formulations according to the formulation of the pharmaceutical composition of the present invention. Suitable pharmaceutically acceptable carriers and formulations are described in Remington's Pharmaceutical Sciences (19th ed., 1995). The pharmaceutical composition of the present invention may further comprise an emulsifier (e.g., TWEENS), a wetting agent (e.g., sodium lauryl sulfate), a coloring agent, a flavoring agent, a stabilizer, a preservative, water, saline, a phosphate buffer solution and the like.
The excipient may be selected according to the formulation of the pharmaceutical composition of the present invention. For example, when the pharmaceutical composition of the present invention is prepared by an aqueous suspension, suitable excipients include sodium carboxymethylcellulose, methylcellulose, hydropropylmethylcellulose , Sodium alginate, polyvinylpyrrolidone, and the like can be used. As a suitable excipient when prepared by injection, Ringer's solution, isotonic sodium chloride and the like can be used.
The pharmaceutical composition of the present invention can be administered orally or parenterally, and its daily dose is usually in the range of 0.001 to 150 mg / kg body weight, and can be administered once or several times. However, since the dosage of the pharmaceutical composition of the present invention is determined in view of various related factors such as route of administration, age, sex, weight, and patient's severity of the patient, the dose is limited in any aspect to the scope of the present invention Should not be understood to be.
As described above, according to the present invention, an anti-obesity composition using Clausena xcavata extract can be provided. The composition for anti-obesity of the present invention can be commercialized as a functional food, medicine, or the like.
Fig. 1 shows the activity of inhibiting the differentiation of precursor adipocytes of the extract of Clausena xcavata into adipocytes.
Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these examples and experimental examples.
< Example > Clausena X Cabata Preparation of extract
The dried < RTI ID = 0.0 > Clausena < minutum ) 100 g of leaf and stem crushed water was added with 1 L of 70% ethanol, repeatedly extracted once at room temperature for 24 hours, and then filtered with a filter paper. The obtained 70% ethanol filtrate was concentrated under reduced pressure and then lyophilized to obtain Clausena xcavata extract.
< Experimental Example > Clausena X Cabata Experiments to improve obesity of extracts
3T3-L1 (ATCC CL-173), a mouse precursor adipocyte, was cultured in a 10% BCS DMEM medium at 37 ° C and 5% CO 2 . 3T3-L1 progenitor adipocytes were plated in 24-well plates at 5 × 10 4 cells / well and maintained at 100% confluency for 2 days. The precursor adipocytes were cultured in 10% FBS DMEM medium containing 0.5 mM 3-isobutyl-1-methylxanthine (Calbiochem 410957), 1 uM dexamethasone (Calbiochem 265005) and 1 ug / ml insulin (Sigma I9278) Were induced for 2 days and cultured for 48 hours with 10% FBS DMEM containing 1 ug / ml insulin for two days. Subsequently, the cells were replaced with 10% FBS DMEM medium for 2 days every 4 days. During the induction of adipocyte differentiation, the extracts of Clausena xcavata were treated with 50, 100 and 200 ㎍ / ml of each culture medium, and the degree of adipocyte differentiation was observed on the 8th day when the differentiation was completed. The degree of adipocyte differentiation was firstly confirmed by microscopy through Oil Red O staining. The degree of adipocyte staining was measured at 510 nm absorbance using an ELISA reader (SPECTRAmax 340PC, Molecular Devices, USA) Respectively. The results were obtained by repeating the experiment three times by concentration.
The results of oil red O staining and quantitative analysis of fat mass are shown in FIG. 1, and it is seen from FIG. 1 that the extract of Clausena xcavata has an activity of inhibiting fat accumulation of adipocytes in a concentration-dependent manner have.
Claims (4)
Wherein the extract is obtained by using water, ethanol or a mixed solvent thereof as an extraction solvent.
Wherein the extract is obtained by using 70% ethanol as an extraction solvent.
Wherein the extract is obtained by using water, ethanol or a mixed solvent thereof as an extraction solvent.
Wherein said extract is obtained by using 70% ethanol as an extraction solvent.
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| KR1020150071563A KR101762736B1 (en) | 2015-05-22 | 2015-05-22 | Composition for Anti-obesity Using Clausena excavata |
| PCT/KR2016/005104 WO2016190580A1 (en) | 2015-05-22 | 2016-05-13 | Anti-obesity composition using clausena excavata extract |
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