KR20150085543A - Composition for Improving, Preventing or Treating Obesity Comprising Allium sativum L. Extracts and Momordica charanti Extract - Google Patents

Abstract

The present invention relates to a composition for improving, preventing or treating extracts of Allium sativumL. and Momordica charantia or a mixture thereof as an active ingredient wherein the composition inhibits the expression of PPAR-γ which controls differentiation of fatty cell and fat metabolism and glycometabolism.

Description

(Composition for Improving, Preventing or Treating Obesity Comprising Allium sativum L. Extracts and Momordica charanti Extract containing Garlic Extract and Latex Extract)

The present invention relates to a composition for improving, preventing or treating obesity, which comprises garlic extract and yeast extract.

Garlic ( Allium sativum L.) is a bulbous plant belonging to the genus Lilliaceae ( Allium ). Recently, many researchers have reported that there are various pharmacological physiological activities such as cancer prevention effect, blood circulation disorder prevention effect and antioxidant activity . The major component of the pharmacological activity of garlic is the s-allyl-cysteine sulfoxide (S-alkenyl-l-cysteine sulfoxides) L-cysteine sulfoxide (S-allyl-L-cysteine sulfoxide) is produced by the action of allinase, an enzyme in garlic, and the azoenes produced by polymerization and decomposition of allicin and allicin ajoene) and the vinyl who (vinyl dithiins), etc. are known, which are various types of sulfur compounds (Lawson et al Planta Med 57: ... 363-370 (1991)).

Momordica charantia ) is called pak and real, bitter melon in the United States, bitter grourd, wild cucumber in Africa, karela in India, ampalaya in South East Asia and so on. Yeoju's typical effects include anti-cancer, anti-necrotic action, anti-hyperglycemic action, and prevention of diabetic complications. Other effects include skin diseases (eczema, psoriasis), night blindness, parasites, rheumatism, gout, digestive ulcers, pneumonia, malaria have. There are many kinds of minerals such as beta-carotene, potassium and iron which are changed into vitamin C and vitamin A in body, and there are glucoside, saponin, alkaloid, oil, tryptene, protein and steroid system.

Obesity is defined as the unbalanced state of energy metabolism in which the body's excess fat tissue accumulates because of the energy consumption exceeding the energy consumed. If the body mass index (BMI) defined by WHO is above 25, it is classified as overweight. do. Obesity is a serious socioeconomic problem, as well as personal health problems such as diabetes, cardiovascular disease, metabolic diseases such as hyperlipidemia, fatty liver and musculoskeletal disorders. Currently, there are surgical treatments such as dietary modification, exercise therapy, medication, medicinal therapy, liposuction, and gastrectomy. However, currently available drug therapies are the treatment of obesity with fluoxetine, There are only a few drugs, such as orlistat, sibutramine, rimonabant, and side effects of long-term use.

Numerous papers and patent documents are referenced and cited throughout this specification. The disclosures of the cited papers and patent documents are incorporated herein by reference in their entirety to better understand the state of the art to which the present invention pertains and the content of the present invention.

The present inventors have sought to find a natural material having an anti-obesity effect. As a result, garlic ( Allium sativum L.) Extract, Yeoju ( Momordica charantia ) extract and a mixture thereof inhibit the expression of PPAR-y which regulates differentiation and lipid metabolism and glucose metabolism of adipocytes.

Accordingly, an object of the present invention is to provide a composition for improving, preventing or treating obesity.

Other objects and advantages of the present invention will become more apparent from the following detailed description of the invention, claims and drawings.

According to one aspect of the present invention, there is provided a composition for improving, preventing or treating obesity comprising garlic ( Allium sativum L.) extract, Momordica charantia extract or a mixture thereof as an active ingredient.

The present inventors have sought to find a natural material having an anti-obesity effect. As a result, it was confirmed that the garlic extract, Lactobacillus japonica extract and a mixture thereof inhibit the expression of PPAR-γ which regulates adipocyte differentiation, lipid metabolism and glucose metabolism.

The extract of Garlic and Lyciumcholapon extract used in the composition of the present invention can be used in various extracting solvents when they are obtained by treating extractive solvent in garlic or yeast. Preferably, a polar solvent or a non-polar solvent can be used. Suitable polar solvents are (i) water, (ii) alcohols (preferably methanol, ethanol, propanol, butanol, n-propanol, iso-propanol, n-butanol, 1-pentanol, Or ethylene glycol), (iii) acetic acid, (iv) dimethyl-formamide (DMFO) and (v) dimethyl sulfoxide (DMSO). Suitable nonpolar solvents are acetone, acetonitrile, ethyl acetate, methyl acetate, fluoroalkane, pentane, hexane, 2,2,4-trimethylpentane, decane, cyclohexane, cyclopentane, diisobutylene, 1- But are not limited to, pentane, 1-chlorobutane, 1-chloropentane, o -xylene, diisopropyl ether, 2- chloropropane, toluene, 1- chloropropane, chlorobenzene, benzene, diethyl ether, diethylsulfide, Methane, 1,2-dichloroethane, aniline, diethylamine, ether, carbon tetrachloride, and THF.

More preferably, the extraction solvent used in the present invention is (a) water, (b) anhydrous or hydrated lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, propanol, butanol, etc.) (E) ethyl acetate, (f) chloroform, (g) butyl acetate, (h) 1,3-butylene glycol, (i) hexane and (j) diethyl ether. . Most preferably, the garlic extract of the present invention is extracted with water, and the aristoculite extract is obtained by treatment of ethanol with yeast.

The extract of the present invention can be extracted by a known natural substance extraction method. For example, the extract may be extracted by a cold extraction, a hot water extraction, an ultrasonic extraction, a reflux cooling extraction, or a heating extraction. According to one embodiment of the present invention, the extract of the present invention can be extracted through hot water extraction or reflux cooling extraction, 1 to 10 times, 1 to 8 times, or 1 to 6 times.

As used herein, the term " extract " means that it is used in the art as a crude extract as described above, but broadly includes fractions obtained by further fractionating the extract. That is, the garlic extract or the lemon extract has not only been obtained by using the above-mentioned extraction solvent, but also obtained by further applying a purification process thereto. For example, a fraction obtained by passing the above extract through an ultrafiltration membrane having a constant molecular weight cut-off value, and a separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity) The fraction obtained by the purification method is also included in the garlic extract or the lily extract of the present invention.

The garlic extract or Lycium chinense extract used in the present invention may be prepared in powder form by an additional process such as vacuum distillation and freeze drying or spray drying.

As used herein, the term " comprising as an active ingredient " is meant to include an amount sufficient to achieve the potency or activity of the following garlic extract, fennel extract or a mixture thereof. Since the present invention is a composition extracted from natural plant material such as garlic and / or fennel, there is no adverse effect on the human body even when it is administered in an excessive amount. Therefore, the quantitative upper limit of the amount of garlic extract and / or fennel extract contained in the composition of the present invention is .

The invention garlic (Allium sativum L.) extract, Momordica charantia extract or a mixture thereof as an active ingredient.

According to one embodiment of the present invention, the mixture is composed of garlic extract and lemon juice extract at a weight ratio of 1: 1 to 2: 1. According to another embodiment of the present invention, the mixture is constituted at a weight ratio of 1: 1 to 1.5: 1.

The composition of the present invention can improve, prevent or treat obesity.

According to one embodiment of the present invention, the composition for improving, preventing or treating obesity comprising the garlic extract inhibits 5-20%, 7-17% or 10-15% of differentiation of adipocytes. According to another embodiment of the present invention, the composition for improving, preventing or treating obesity, which comprises said extract, inhibits the differentiation of adipocytes by 15-35%, 18-30% or 20-28%. According to a particular embodiment of the present invention, the composition for improving, preventing or treating obesity comprising a mixture of garlic extract and yeast extract comprises 20-40%, 15-35% or 27-33% inhibition of differentiation of adipocytes do.

The composition of the present invention inhibits the expression of PPAR-y which regulates lipid metabolism and glucose metabolism.

According to one embodiment of the present invention, the composition for improving, preventing or treating obesity comprising the garlic extract inhibits the expression of PPAR-y by 1-20%, 1-15%, or 5-10%. According to another embodiment of the present invention, the composition for improving, preventing or treating obesity, which comprises the extract of Liliaceae, inhibits the expression of PPAR-y by 15-35%, 20-30% or 22-28%. According to a specific embodiment of the present invention, the composition for improving, preventing or treating obesity, which comprises a mixture of garlic extract and yeast extract, contains 30-60%, 35-55% or 40-50% .

The composition for improving, preventing or treating obesity, which comprises a mixture of garlic extract and yucca extract of the present invention, has a synergistic effect in comparison with a composition comprising garlic extract and yuzu extract alone.

The composition of the present invention can be provided as a food composition. When the composition for improving obesity containing the active ingredient of the garlic extract, lily extract or mixture thereof according to the present invention is prepared from a food composition, not only the garlic extract and / or the lily extract as the active ingredient, but also the garlic extract and / And includes, for example, proteins, carbohydrates, fats, nutrients, flavoring agents, and flavoring agents. Examples of the above-mentioned carbohydrates are monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sucrose, oligosaccharides and the like; And polysaccharides such as dextrin, cyclodextrin and the like, and sugar alcohols such as xylitol, sorbitol and erythritol. Natural flavorings such as tau martin and stevia extract (e.g., rebaudioside A and glycyrrhizin) and synthetic flavorings (saccharine, aspartame, etc.) can be used as flavorings. For example, when the food composition of the present invention is prepared as a drink, it may contain citric acid, liquid fructose, sugar, glucose, acetic acid, malic acid, juice, mulberry extract, jujube extract, licorice extract, etc., in addition to the garlic extract and / Can be added.

The composition for improving obesity comprising the garlic extract of the present invention, Yeast extract or a mixture thereof as an active ingredient may be manufactured from a functional food composition. When the composition of the present invention is prepared with a functional food composition, it includes components that are conventionally added in food production, and includes, for example, proteins, carbohydrates, fats, nutrients, and seasonings. For example, in the case of being made with a drink, as an active ingredient, a flavoring agent or a natural carbohydrate may be added as an additional ingredient in addition to the garlic extract and / or the rumen extract. For example, natural carbohydrates include monosaccharides (e.g., glucose, fructose, etc.); Disaccharides (e.g., maltose, sucrose, etc.); oligosaccharide; Polysaccharides (e.g., dextrin, cyclodextrin and the like); And sugar alcohols (e.g., xylitol, sorbitol, erythritol, etc.). Natural flavoring agents (e.g., tau marin, stevia extract, etc.) and synthetic flavoring agents (e.g., saccharin, aspartame, etc.) may be used as flavorings.

The compositions of the present invention may be prepared with pharmaceutical compositions.

According to a preferred embodiment of the present invention, the composition of the present invention comprises (a) a pharmaceutically effective amount of the above-described garlic extract, lily extract or mixture thereof of the present invention; And (b) a pharmaceutically acceptable carrier. As used herein, the term " pharmaceutically effective amount " means an amount sufficient to achieve efficacy or activity of the above-described garlic extract, fennel extract or a mixture thereof.

When the composition of the present invention is manufactured from a pharmaceutical composition, the pharmaceutical composition of the present invention includes a pharmaceutically acceptable carrier. The pharmaceutically acceptable carriers to be contained in the pharmaceutical composition of the present invention are those conventionally used in the present invention and include lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, calcium phosphate, alginate, gelatin, But are not limited to, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrups, methylcellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. It is not. The pharmaceutical composition of the present invention may further contain a lubricant, a wetting agent, a sweetening agent, a flavoring agent, an emulsifying agent, a suspending agent, a preservative, etc. in addition to the above components. Suitable pharmaceutically acceptable carriers and formulations include, but are not limited to, Remington's Pharmaceutical Sciences (19th ed., 1995).

The pharmaceutical composition of the present invention may be administered orally or parenterally, preferably by oral non-administration.

The appropriate dosage of the pharmaceutical composition of the present invention may vary depending on factors such as the formulation method, administration method, age, body weight, sex, pathological condition, food, administration time, administration route, excretion rate, . Typical dosages of the pharmaceutical compositions of this invention are in the range of 0.001-100 mg / kg on an adult basis.

The pharmaceutical composition of the present invention may be formulated into a unit dose form by formulating it using a pharmaceutically acceptable carrier and / or excipient according to a method which can be easily carried out by a person having ordinary skill in the art to which the present invention belongs. Or by intrusion into a multi-dose container. The formulations may be in the form of solutions, suspensions, syrups or emulsions in oils or aqueous media, or in the form of excipients, powders, powders, granules, tablets or capsules, and may additionally contain dispersing or stabilizing agents.

The features and advantages of the present invention are summarized as follows:

(a) The present invention relates to a method for producing sativum L.) Extract, Yeoju ( Momordica charantia ) extract or a mixture thereof as an active ingredient.

(b) The composition of the present invention effectively inhibits the expression of PPAR-y which regulates adipocyte differentiation and fat metabolism and glucose metabolism.

(c) The present invention can improve side effects caused by the use of conventional long-term drug treatment of obesity by using natural material.

FIGS. 1A to 1B show the effect of garlic extract, Liliaceae extract and a mixture thereof on mast cell differentiation. FIG. 1A shows the treatment of hormone mixtures under the treatment or non-treatment of garlic extract, Liliaceae extract and mixtures thereof to induce differentiation of 3T3-L1 precursor adipocytes. On day 8, cytoplasmic triglycerol was stained with oil red O. [ 1B shows lipid accumulation by measuring the absorbance at 490 nm. Figure 1c shows cell viability by MTT assay. Results were expressed as mean ± standard deviation (n = 3; * P <0.05).
Fig. 2 shows the results of suppressing the degree of lipid peroxidation transcription factor of a mixture of garlic extract and mung bean extract. The expression of PPAR-y was measured by ELISA. Results were expressed as mean ± standard deviation (n = 3; * P <0.05, ** P <0.01).

Hereinafter, the present invention will be described in more detail with reference to Examples. It is to be understood by those skilled in the art that these embodiments are only for describing the present invention in more detail and that the scope of the present invention is not limited by these embodiments in accordance with the gist of the present invention .

Example

Materials and Experiments

The garlic samples used in the experiment were purchased from the year 2000, and the sample was used as the experimental material in the year of 2012. The purchased garlic was boiled for 5 minutes to 7 minutes in boiling water, and then pulverized by a crusher. Then, 400 g of water was added to 200 g of garlic, and the mixture was extracted with water three times and then lyophilized and used as a sample. The purchased product was pulverized with a crusher, and 1800 ml of 80% ethanol was added to 600 g of the crushed sample, followed by repeated extraction three times. The ethanol extract was concentrated by using a vacuum concentrator and then lyophilized to be used as a sample. Garlic and herring mixture were prepared at a ratio of 1: 1 by weight.

Cell culture and differentiation

3T3-L1 cells were cultured in DMEM (Dulbecco's Modified Eagle's Medium) medium containing 10% calf serum at 37 ° C and 5% CO _2. 3T3-L1 cells were seeded in 48 well plates After the incubation, the hormone mixture [10 μg / ml insulin, 0.5 μM dexamethasone, 0.5 mM IBMX (3-isobutyl-1-methylxanthine)] was treated for 48 hours and replaced with DMEM medium containing insulin and FBS. After the differentiation, the cells were washed twice with PBS, fixed with 3.7% formaldehyde, and stained for 1 hour with an oil red dye (Oil Red O) O dye) and then the reaction was added to isopropanol and by measuring the absorbance at 490 ㎚ measure the amount of triglyceride (triglyceride). cell images were analyzed using a solution i- total imaging solutions program was used to Olympus CKX41 .

Cell viability assay

Cell proliferation assay was performed to prove that 3T3-L1 cell differentiation inhibitory effect of each extract was not due to the toxicity of the extract. Cells were cultured in 96-well plates, and 24 hours later, each extract was treated and MTT analysis was performed after 24 hours.

PPAR-γ ELISA analysis

Peroxisome proliferator-activated receptor-gamma (PPAR-γ) is a transcription factor belonging to the nuclear receptor that regulates lipid metabolism and glucose metabolism and regulates cell proliferation and differentiation.

Especially in early stages of adipocyte differentiation process. In this study, the amount of protein expression was confirmed by ELISA analysis (Cayman chemical company, MI USA) to confirm the effect of each extract and mixed extract on the expression of PPAR-γ.

result

Effect of Yeoju and Garlic Mixture Extracts on the Fatty Differentiation.

In order to confirm the efficacy of the mixed extract of Yeoju extract and garlic extract to inhibit the differentiation of 3T3-L1 adipocytes, the oil red O staining of adipocytes showed that the inhibition of differentiation was 13.6% in the group treated only with garlic extract , And 24.1% reduction was observed in the group treated with Yeoju extract only. In the group treated at the ratio of 1: 1, the inhibition rate of differentiation was 30.9%. The extracts containing Garlic extract and Yeoju extract showed higher inhibition rate of differentiation (Fig. 1). This is thought to be a synergistic effect of garlic and mung bean extract. In addition, after the cultivation of adipocytes, each of the extracts was treated, and it was confirmed that neither garlic extract, lily extract, nor mixed extract were cytotoxic.

PPAR -γ inhibitory efficacy

Peroxisome proliferator-activated receptor-gamma (PPAR-γ) is a transcription factor belonging to the nuclear receptor that regulates lipid metabolism and glucose metabolism and regulates cell proliferation and differentiation. The expression level of PPAR-γ, which was increased more than 3-fold in the differentiation-induced group, decreased to 2.8-fold when treated with garlic extract and decreased to 2.32-fold with only the extract of yeast extract. In the treated group, the protein expression level of PPAR-γ was reduced by 1.72 times by 40%.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the same is by way of illustration and example only and is not to be construed as limiting the scope of the present invention. It is therefore intended that the scope of the invention be defined by the claims appended hereto and their equivalents.

Claims (5)

Garlic ( Allium sativum L.) extract, Momordica charantia extract or a mixture thereof as an active ingredient.
2. The composition of claim 1, wherein the mixture comprises a garlic extract and a raspberry extract at a weight ratio of 1: 1 to 2: 1.
2. The composition of claim 1, wherein the composition inhibits the differentiation of adipocytes.
2. The composition of claim 1, wherein the composition inhibits the expression of PPAR-gamma (Peroxisome proliferator-activated receptor gamma).
The composition of claim 1, wherein the composition is a food composition, a functional food composition, or a pharmaceutical composition.

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