KR20140034267A - Composition for anti-obesity using an extract of sargassum muticum - Google Patents

Abstract

Disclosed is a composition for an anti-obesity agent using an extract of Sargassum muticum, which inhibits the differentiation of preadipocytes differentiation-promoted by insulin or the like into adipocytes, reduces weight in a high-fat diet induced mouse model, lowers the blood lipid level, and suppresses the fat accumulation in the liver.

Description

Technical Field [0001] The present invention relates to an anti-obesity composition using an extract of dumpling bean moth,

The present invention relates to a saddle- The present invention relates to an anti-obesity agent composition using a muticum extract.

Recently, as the national income has improved and the food has been westernized along with the economic growth, the intake of various animal foods is increasing. In 2008, the average daily food intake per capita was 80.5% for whole plant food and 19.5% for animal food. The proportion of animal food intake was 6 times higher than the 3% surveyed in 1969 Of the total.

The proportion of obesity (BMI> 25) in Korea has increased from 11.7% in 1995 to 30.7% in 2008 and the proportion of obesity (BMI> 30) has risen from 2.3% in 1998 to 4.1% (Ministry of Health and Welfare, 2009).

Obesity is a condition in which energy is excessively accumulated in the body due to unbalanced energy intake and consumption, resulting in abnormally increased adipose tissue (Clinical Obstetrics 28: 675-689, 1998; Clinical Obesity (eds. ) 248-89 (Blackwell Science, Oxford 1998).

The World Health Organization (WHO) estimates that the BMI (body mass index) of the Asian standard is 23 to 25 overweight, 25 to 30 for obesity, and 30 for high obesity.

The causes of obesity include genetic factors, high fat and high calorie diet, lack of exercise due to busy social environment, and environmental factors such as endocrine abnormality. Among them, about 50 to 70% of obesity is caused by environmental factors And the rest are known to be caused by genetic factors.

Obesity treatments include Xenical ™ (Roche Pharmaceuticals, Switzerland), Reductil ™ (Abbott, USA), Acomplia ™ (Sanofi-Aventis, France), Exorise ™ , And these treatments for obesity generally fall into three categories: an appetite suppressant, a body energy metabolism promoter, and a digestive absorption inhibitor. Xenical is a lipase inhibitor that inhibits the digestion and absorption of fat. Reductil and acomplia inhibit appetite by acting as an antagonist of the CB1 receptor that suppresses the reuptake of noradrenaline and serotonin, the appetite regulating hormone, or appetite in the brain. It is medicine. In the case of exorizers, it has a heat-generating effect, which increases the basic metabolism of the body and inhibits digestion and absorption of fat by inhibiting gastrointestinal lipase.

However, these treatments have side effects such as hypertension, depression, anxiety, and suicidal tendency, and the value of natural medicine is newly emerging.

The present invention has been completed based on the anti-obesity activity of the dandelion extract.

Korean Patent No. 10-1302739 Title of the invention: An agent for improving allergic diseases using an extract of dumpling bean mushroom or an active substance isolated therefrom

It is an object of the present invention to provide an anti-obesity composition using dumpling bean moth extract.

Other and further objects of the present invention will be described below.

The inventors of the present invention found that 3T3-L1 precursor adipocytes induced by insulin or the like inhibit the differentiation of adipocyte and water extract of dumpling beads into adipocytes as shown in Examples and Experimental Examples, In the mouse model in which obesity was induced, the weight of the experimental animals was decreased and the weight of the adipose tissues was decreased.

The present invention is provided based on the results of these experiments, and the anti-obesity composition of the present invention is characterized in that it contains a mulberry myrtle extract as an active ingredient.

As used herein, the term "extract" means water, lower alcohol having 1 to 4 carbon atoms such as methanol, ethanol and butanol, ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, dichloromethane, N, A crude extract obtained by using amide (DMF), dimethylsulfoxide (DMSO), 1,3-butylene glycol, propylene glycol or a mixed solvent thereof and a fraction obtained by fractionating the extract with one or more of the above-listed solvents It says. The extraction method can be applied by any method such as cold-rolling, refluxing, heating, ultrasonic irradiation or the like in consideration of the degree of extraction and the degree of preservation of the active ingredient. In the case of the fractionated extract, a fraction obtained by suspending the crude extract in a specific solvent and mixing and leaving with a solvent having a different polarity, a step of adsorbing the crude extract on a column packed with silica gel or the like, and then adding a hydrophobic solvent, Means a fraction obtained by using a mixed 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, more preferably an extraction solvent such as water, ethanol or a mixed solvent thereof, as in the following examples, Means the obtained extract.

In the present specification, "obesity" refers to a state in which abnormally increased adipose tissue, whether obesity due to genetic factors or obesity due to environmental factors, is associated with obesity (BMI of 30.0 or more ) And overweight (when BMI is between 25 and 30).

* Also, 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 itself inactive.

Also, in this specification, "anti-obesity" is meant to include reduction of body fat and / or reduction of body weight, including prevention of obesity and treatment of obesity.

The anti-obesity composition of the present invention may contain the active ingredient in any amount (effective amount) as long as it exhibits the obesity-improving activity, depending on the purpose of use, formulation, compounding purpose and the like. And will be determined within the range of 0.001 wt% to 99.990 wt%. Here, "effective amount" refers to the amount of effective ingredient capable of inducing an obesity-improving 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.

In another aspect, the present invention relates to a composition for diet comprising as an active ingredient a dung beet moth extract.

As used herein, a "diet " is defined as a condition in which the weight is not obese or overweight, but is desirable or necessary for weight or body fat reduction for cosmetic or health purposes. In general, the composition for diet of the present invention will be manufactured and used for the purpose of beauty or health of a normal person.

In the composition for diet of the present invention, regarding the meaning of the bean mallow mung bean extract, the effective amount thereof and the like, the above-mentioned facts regarding the anti-obesity composition of the present invention are valid as they are.

In another aspect, the present invention relates to a composition for improving hyperlipemia and a composition for improving fatty liver comprising a dung bean moth extract as an active ingredient.

The following Examples and Experimental Examples show that the extract of dung bean moth is lowered in blood cholesterol concentration, triglyceride concentration and LDH cholesterol concentration and elevated blood cholesterol level It is shown that the concentration of HDL cholesterol does not lower the known concentration of HDL cholesterol and that when the dung bean moth extract is administered to experimental animals together with the high fat diet, .

As used herein, the term "fatty liver" refers to a disease that causes angina, myocardial infarction, stroke, arteriosclerosis, etc., and refers to a disease in which fat is accumulated in hepatocytes excessively due to liver fat metabolism disorder.

In the present specification, the term "hyperlipidemia" refers to a condition in which the amount of fat in the blood is increased because fat metabolism such as triglycerides and cholesterol is not properly performed. More specifically, it refers to a state in which lipid components such as triglyceride, LDL cholesterol, phospholipid and free fatty acid are increased in the blood.

Since hyperlipemia itself is not a symptom, it is a cause of cardiovascular diseases such as atherosclerosis and hypertension. Therefore, the composition for improving hyperlipemia of the present invention may be useful as a preventive agent for the above-mentioned diseases caused by hyperlipemia have.

In the hyperlipemia improving composition of the present invention and the fatty liver improver composition, the above-mentioned effect of the above-mentioned anti-obesity composition of the present invention is valid as it relates to the meaning of the dung beetle moth extract and the effective amount thereof.

The anti-obesity composition, diet composition, fat remedy composition or hyperlipidemia improving composition (hereinafter referred to as "composition of the present invention ") of the present invention can be used as an active ingredient, And a fatty acid ameliorating activity, and the like, so as to enhance or enhance the activity of improving the activity of the fatty liver.

Such natural products or compounds include, but are not limited to, hwanggi powder or extract, ginseng powder or extract, gyeongryeol powder or extract, licorice powder or extract, hwangjeol powder or extract, omija powder or extract, gugija powder or extract, (Leaves, stems, flowers, etc.), powder, or extract, hinoki powder or extract, pine powder or extract, pine powder or extract, (Leaves, stems, flowers, roots, husks, fruits) powder or extract, orchard powder or extract, and the like.

The meanings of the extracts as described above are as described above in connection with the dung bean mallow extract. Such an extract may be obtained by mixing the object to be extracted.

In a specific embodiment, the composition of the present invention can be identified as a food composition, particularly a functional beverage.

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. The natural flavor may be obtained from apples, lemons, citrus fruits, grapes, strawberries, peaches, and the like, or may be obtained from green tea leaves, round leaves, jujube leaves, cinnamon, chrysanthemum leaves, jasmine and the like. 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.

The composition of the present invention can be used as a pharmaceutical composition in a specific embodiment.

The pharmaceutical composition of the present invention may be in the form of oral formulations (tablets, suspensions, granules, emulsions, capsules, syrups, etc.), parenteral formulations (including sterile injectable aqueous (Oil, cream, ointment, gel, lotion, patch), and the like.

The term "pharmaceutically acceptable" as used herein means that the application (prescribing) subject does not have toxicity more than the adaptable 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 (such as sodium carboxymethylcellulose, ethylcellulose), malt, gelatin, talc, (E.g., peanut oil, cottonseed oil, sesame oil, olive oil, etc.), polyol (e.g., propylene glycol, glycerin and the like), alginic acid, emulsifiers (e.g., TWEENS), humectants Such as 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.

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. Suitable excipients when prepared from injection solutions include Ringer's solution, isotonic sodium chloride, and the like.

The pharmaceutical composition of the present invention can be administered orally or parenterally, and in some cases, can be administered topically.

The daily dose of the pharmaceutical composition of the present invention is usually 0.001 to 150 mg / kg body weight, and may 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, it is possible to provide an anti-obesity composition using a dung beet moth extract. According to the present invention, there can also be provided a composition for improving hyperlipemia and a composition for improving fatty liver using dumpling bean gum extract. The composition of the present invention can be commercialized as food or medicine.

FIG. 1 is a photograph showing that dendriticum bean mabbai extract inhibits the differentiation of adipose precursor cells induced by insulin into adipocytes in a concentration-dependent manner.
Fig. 2 is a photograph of a fat tissue taken from an experimental animal.
FIG. 3 shows the results of showing that the concentration of blood triglyceride, total cholesterol, and LDL cholesterol lowered by the high-fat diet was lowered by the high fat diet.
FIG. 4 shows the result of showing that the extract of dumpling bean moth extract lowered the liver fat follicle which was increased by high fat diet.

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 > Dumpling beads  Preparation of extract

The dumpling was collected from Udo, Jeju - si, Jeju Special Self - Governing Province. EtOH was added to the dry weight of 10 g of the dewatered mildew of the saline solution (DW, 20%, 40%, 60%, 80%, 100%) and stirred (where% is v / v). After stirring for 48 hours, a filter paper (125 mm) was applied using a vacuum filter. After the first filtration, the residues separated by concentration (DW, 20%, 40%, 60%, 80% %), And the mixture was stirred for 24 hours. After 1 hour of sonication, secondary filtration was performed. The filtrate from the primary and secondary filtration was taken and concentrated using a concentrator. The concentrated sample was dissolved in distilled water, transferred into a vial, and placed in a deep freezer, lyophilized (about 3 days), and finally a total of six extracts were prepared Respectively.

The 60% ethanol extract, which showed the best yield among the six extracts and showed the best inhibitory effect on the differentiation of adipocyte precursors into adipocytes when preliminary experiments were conducted according to the method of <Experimental Example 1> below, was used as a sample.

< Experimental Example > Obesity improving activity, hyperlipidemia improving activity, and fatty liver improving activity of the mulberry mulberry extract

<Experimental Example 1> Experiment on the inhibition of differentiation of fat-derived cells

3T3-L1 (CL-173) cells were purchased from ATCC (American Type Culture Collection, Manassas, Va., USA) and 3T3-L1 mouse preadipocytes were inoculated in DMEM medium supplemented with 10% CO ₂ . 3T3-L1 precursor adipocytes were plated at a density of 5 × 10 ⁴ cells / well in a 24-well plate and maintained at 100% confluency for 2 days. The adipocytes were induced for 2 days with 10% FBS DMEM medium containing MDI (0.5 mM 3-isobutyl-1-methylxanthine (IBMX), 1 μM dexamethasone and 1 μg / ml insulin) After a period of time, the cells were cultured for 2 days with 10% FBS DMEM containing 1 / / ml insulin. Subsequently, the cells were replaced with 10% FBS DMEM medium for 2 days every 4 days. During the induction of adipocyte differentiation, the ethanol extracts of dendritic cells were treated at 25, 50 and 100 ㎍ / ml for each culture, and the degree of adipocyte differentiation was observed at 8 days after the completion of differentiation. The degree of adipocyte differentiation was firstly confirmed by microscopy through Oil Red O staining and the degree of adipocyte differentiation was measured at 510 nm absorbance.

The results are shown in Fig. Referring to FIG. 1, it can be seen that the extract of dung bean moth mungbean reduces lipid droplets in a concentration-dependent manner.

<Experiment 2> DIO (diet - induced obesity ) mouse model experiment

A 5-week-old C57B / 6 male mouse (Koatech, Korea) was purchased and the animals were refined for one week before the start of the experiment to adjust to the changed ambient temperature, humidity, Lt; / RTI &gt;

The experimental animal room was adjusted to temperature of 222, relative humidity of 4510%, ventilation frequency of 10-15 times / hr, illumination interval of 12 hours, illuminance of 150-250 Lux and noise of 60dB or less. Polycarbonate was kept in three rabbits per week and the box was changed twice a week to keep the ammonia concentration below 20ppm. The feeds were fed autonomously, and the drinking water allowed free drinking of purified water.

5-week-old C57BL / 6 mice were arranged and sorted in order of weight. The groups were grouped as shown in Table 1 below so that the mean and standard deviation of the groups were equalized. In the normal group, 12% calories from fat (60% calories from fat) were fed to the negative control group (obesity induction group), and the high calorie diet was fed to the sample group and the sample (Xenical, Conjugated linoleic acid (CLA) Extract) was orally administered once a day for 6 weeks using sonde.

The weight of the adipose tissue (subcutaneous fat, peritoneal fat, and epididymal fat) was measured at the end of the experiment.

The results are shown in the following [Table 2] (weight change) and [Table 3] (weight change of fat tissue).

Referring to [Table 2] and [Table 3], it can be seen that the dung bean mallow extract decreases the body weight in proportion to the dose and decreases the fat tissue weight. FIG. 2 is a photograph showing the fat tissue extracted from an experimental animal, and the food efficiency (FER) and calorie efficiency (EER) are shown in Table 4 below. Referring to FIG. 2 and Table 4, it can be confirmed that the results are similar to those in [Table 2] and [Table 3].

<Experimental Example 3> Blood biochemical test

After 6 weeks of oral administration, the blood collected from the abdominal vein was placed in a blood collection bottle containing EDTA, an anticoagulant, and plasma was collected using a centrifuge. Total blood cholesterol, Triglyceride , HDL cholesterol and LDL cholesterol were analyzed.

The results are shown in Fig. The results of [Fig. 3] show that total cholesterol concentration, triglyceride concentration, and LDL cholesterol concentration were decreased in comparison with the negative control group (obesity induction group), but the concentration of HDL cholesterol It does not lower it.

<Experimental Example 2-2> Liver tissue test

After 6 weeks of oral administration, the animals were sacrificed and the liver was extracted and fixed in 10% formalin for 5 days, and paraffin blocks were made to make tissue slides with a thickness of 4 μm. The tissue slide was deparaffinized and functionalized with xylene, 100%, 95%, 90%, 80%, and 70% ethanol, stained with hematoxylin and eosin, sealed with permount, Respectively.

The results are shown in Fig. Referring to the results of FIG. 4, it can be seen that fat follicles were significantly reduced in the dendritic bead moth group (100 mg / kg group) compared to the obesity induction group.

Claims (4)

Composition for improving fatty liver comprising a dumpling bead cap extract as an active ingredient.
The method of claim 1,
The rice ball bead cap extract is a composition for improving fatty liver, characterized in that obtained by using water, ethanol or a mixed solvent thereof.
3. The method according to claim 1 or 2,
The composition is a composition for improving fatty liver, characterized in that the food composition.
3. The method according to claim 1 or 2,
The composition is a composition for improving fatty liver, characterized in that the pharmaceutical composition.

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