KR100588469B1 - Composition for prevention and treatment of obesity comprising shogaol from zingiber officinale - Google Patents

Abstract

A composition for prevention and treatment of obesity comprising shogaol isolated from Zingiber officinale is provided to inhibit formation of adipocytes by inhibiting adipogenesis through which pre-adipocytes are differentiated into adipocytes, and promote release of neutral fats in adipocytes by decomposing triglyceride into free fatty acids and glycerol without side effects. The composition for prevention and treatment of obesity comprises shogaol represented by the formula(1) as an effective ingredient, wherein the shogaol is isolated from Zingiber officinale; the amount of shogaol is 0.01-100 wt.% based on the total weight of the composition; the dosage of shogaol is 0.1-100 mg/kg; and the composition is formulated as food.

Description

Composition for prevention and treatment of obesity comprising shogaol from Zingiber officinale}

1 is a view of a method for extracting ginger using an organic solvent.

Figure 2 is a graph showing the degree of fat cell formation inhibition according to the concentration of shogaol.

3 is a graph showing the results of promoting fat release according to the concentration of shogaol.

The present invention relates to a composition for preventing and treating obesity, including shogaol isolated from ginger. By confirming that the shogaol isolated from ginger inhibits the formation of adipocytes and promotes fat excretion in adipocytes, it is possible to treat and prevent obesity without side effects through a food or pharmaceutical composition comprising the same.

Ginger (Ginger, Zingiber officinale ) contains 40-60% of starch and contains aromatic ingredients, resinous protein, fiber, pentosan, and minerals, and ginger's pungent taste is ginger. ), Gingerol, shogaol, dihydrogingerol, fragrance components are known about 40 species such as citral, camphene and the like.

Ginger is widely used as a seasoning. Ginger processed products include ginger, ginger ale, ginger wine, gingerbread, ginger powder and ginger essence. Root stems are dried and used as spices for breads, sweets, curry, sauces, and pickles. Peel and cut, then marinated in syrup. Ginger tea and ginger are also made. In oriental medicine, the root stem is used as a medicine called health (이는), which is effective for indigestion, vomiting and diarrhea, promotes blood circulation, and inhibits inflammation and analgesia.

More than 20 billion fat cells exist in the human body and are responsible for accumulating or releasing energy in mammals. Within these fat cells, there are complex regulatory mechanisms for the accumulation and release of energy. If the supply is much greater than the demand for energy, it is stored as triglycerides in the fat cells. It is broken down into glycerol and used as an energy source. Obesity is reported to be due to the increase in the size of fat cells due to the accumulation of excessive energy due to the imbalance of the process.

Various efforts have been made in various fields to treat body fat gain and obesity. However, most of the conventional lipolytic accelerators are methylxanthine-based substances such as caffeine and theophylline, and adenylate cyclase, which is an enzyme closely related to the breakdown of fat in adipocytes. Lipolytic activity was shown through the promotion of cyclase or the inhibition of phosphodiesterase. However, these are known to have various side effects such as inducing bronchial expansion or worsening premenstrual syndrome as an addictive substance, which has a problem in stability.

On the other hand, Japanese Patent No. 2002-138045 has a composition using fat extract cell (pre-) as a composition using one or more plant extracts selected from the group consisting of citron, squash, golgol, kaaba, red pepper, caraway, wolfberry and magnolia Techniques for inhibiting the differentiation of adipocytes into adipocytes are known. Through this technique, it is possible to suppress the induction of differentiation of fat precursor cells and to prevent and treat obesity, diabetes, and skin wrinkles.

The Japanese patent was a technology that has fewer side effects in that it uses natural products such as citron, but the above-mentioned mixture of plant extracts suppresses obesity and diabetes by inhibiting adipogenesis of adipocyte cells to mature adipocytes. Only the results that can be prevented are described and there is no mention of the action and effect of decomposing and releasing and eliminating triglycerides that are already excessively accumulated in mature adipocytes, as in the case of the present invention.

Therefore, there is a need to develop a new material using natural products that are safe for the human body, have no side effects, and have the same or better efficacy than the conventional obesity inhibitors.

Therefore, the present inventors have extensively researched and examined to confirm the safe lipolytic active ingredient while promoting the decomposition and excretion of fat in adipocytes. The present invention was completed by confirming that adipocytes can inhibit adipocyte differentiation into mature adipocytes and have an activity of releasing triglycerides in adipocytes.

Therefore, an object of the present invention is to provide a composition for the prevention and treatment of obesity, including shogaol separated from ginger.

The present invention is characterized by a pharmaceutical or food composition for the prevention and treatment of obesity using the shogaol represented by the following formula (1) as an active ingredient.

The present invention will be described in more detail as follows.

The present invention relates to a composition for the prevention and treatment of obesity, including shogaol isolated from ginger. By confirming that the shogaol isolated from ginger inhibits the formation of adipocytes and promotes fat excretion in adipocytes, it is possible to treat and prevent obesity without side effects through a food or pharmaceutical composition comprising the same.

Shogaol according to the present invention not only inhibits the process of differentiating progenitor cells into mature adipocytes, but also has an excellent effect of releasing triglycerides in adipocytes. That is, it inhibits the differentiation of 3T3-L1 cells, which are adipocyte progenitors into mature adipocytes, and also breaks down triglycerides into free fatty acids and glycerol in mature adipocytes. It has the effect of promoting lipolysis.

Therefore, when ingesting the shogaol of ginger according to the present invention, not only suppresses the accumulation of fat in adipocytes, but also promotes the decomposition of triglycerides in the adipocytes, thereby effectively removing body fat.

The shogaol of the present invention may be used by itself or in the form of a pharmaceutically acceptable salt and is included in the scope of the present invention for all salts, hydrates, and solvates prepared by conventional methods. Shogaol may also be isolated from ginger or synthesized according to conventional organic synthesis methods.

Extracting, separating, and purifying shogaol from ginger is not limited to a specific method, but suggests a preferred method as follows.

Grind ginger, dipping with ethanol, filtration and concentration to obtain an ethanol leaching solution, which is then fractionated with hexane and water to obtain a hexane layer. The hexane layer was concentrated under reduced pressure, separated by silica gel column chromatography using hexane as an eluent, and a high-performance liquid chromatography using 70% acetonitrile was selected by selecting a section having antioxidant activity using a DPI solution. You can get it. Ethyl acetate may be used instead of hexane.

The pharmaceutical composition of the present invention may include a shogaol separated from ginger as an active ingredient, and may further include one or more pharmaceutically acceptable carriers. Pharmaceutically acceptable carriers include saline solution, sterile water, Ringer's solution, buffered saline solution, dextrose solution, maltodextrin solution, glycerol, ethanol and one or more of these components. Other conventional additives such as buffers and bacteriostatic agents can be added.

Diluents, dispersants, surfactants, binders and lubricants may also be added in addition to formulate into injectable formulations, pills, capsules, granules or tablets such as aqueous solutions, suspensions, emulsions and the like. Formulation methods are not limited to specific methods and the preferred method may be selected depending on autologous diseases or components having ordinary skill in the art.

The pharmaceutical composition of the present invention may be administered parenterally (eg, intravenously, subcutaneously, intraperitoneally or topically) or orally according to the desired method, and the dosage may be based on the weight, age, sex, health status, It may vary depending on the diet, the time of administration, the method of administration, the rate of excretion and the severity of the disease.

The daily dose of shogaol is preferably 0.1 to 100 mg / kg, preferably 0.4 to 50 mg / kg, and more preferably administered once to several times a day.

The food composition of the present invention includes shogaol separated from ginger as an active ingredient, and may be used together with other food or food additives. The blending amount of the active ingredient with other additives may be appropriately determined within a conventional range depending on the purpose of use (prevention or treatment).

Shogaol may be included from 0.01 to 100% by weight of the total food composition. However, the content of long-term intake for the purpose of weight control and prevention of obesity may be below the above range, and the active ingredient may be used in an amount above the above range because there is no problem in terms of safety and side effects.

There is no particular limitation on the kind of food to which the composition of the present invention is applied. Examples of the food to which the substance can be added include dairy products including meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, drinks, Alcoholic beverages and vitamin complexes, etc., includes all of the health food in the conventional sense.

The health beverage composition of the present invention may contain various flavors or natural carbohydrates, etc. as additional components, as in the general beverage. The natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin and sugar alcohols such as xylitol, sorbitol and erythritol. As a sweetener, natural sweeteners, such as tautin and a stevia extract, or synthetic sweeteners, such as saccharin and aspartame, can be used. The ratio of said natural carbohydrate is generally 0.01 to 0.04 g, preferably 0.02 to 0.03 g per 100 ml of the composition of the present invention.

The composition of the present invention, in addition to the above components, various nutrients, vitamins, electrolytes, flavors, coloring agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols And carbonation agents used in carbonated beverages. In addition, the composition of the present invention may contain a pulp for the production of natural fruit juices, fruit juice drinks and vegetable drinks. These components can be used independently or in combination. The proportion of such additives is not critical, but is generally selected in the range of 0.01 to 0.1 parts by weight based on 100 parts by weight of the composition of the present invention.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to Examples.

Example 1 Separation of Shogaol from Ginger

1 kg of ginger was ground, immersed in 5 liters of ethanol, filtered, and concentrated. 16.65 g of hexane and ethyl acetate were further fractionated to obtain 2.5838 g of hexane layer and 2.5696 g of ethyl acetate layer, respectively.

The hexane layer and the ethyl acetate layer were subjected to silica gel column chromatography using hexane and ethyl acetate solvent and identified several sections having antioxidant activity using DPI solution, and particularly selected sections having strong activity to 70% acetonitrile ( 1.5 ml / min) was used for high performance liquid chromatography to obtain 14 mg of shogaol.

The method using the hexane layer is shown in FIG. 1.

Example 2 securing experimental animals

Progenitor cell lines of mice (3T3-L1) were purchased from Korea Cell Line Bank and DMEM culture, Trypsin and Fetal Bovine Serum (FBS) were purchased from Gibco (Invitrogen corporation).

Example 3 Confirmation of Fat Formation Inhibitory Activity of Shogaol

5 × 10 ⁴ / ml of 3T3-L1 fibroblasts were precultured for 2 days in a carbon dioxide incubator with DEME medium containing 10% serum and antibiotics. Thereafter, 2 mmol of insulin, 250 mmol of isobutylmethylxanthine and 10 mmol of dexamethasone were treated to differentiate into adipocytes. At this time, the medium was changed every two days, and the degree of differentiation into adipocytes was confirmed by treating and culturing the reagents for differentiation and shogaol of Example 1 for each concentration.

Differentiate into adipocytes for at least 5 days, discard the medium, dry, fix in 10% formaldehyde solution for 1 hour, wash with phosphate buffered saline (PBS) and dry. Well, it was stained for 3-4 hours with a reagent for fat staining (oil red O). The stained cells were washed and observed under a microscope. The absorbed values were measured at 510 nm by dissolving the red stained portion using isoprophyl alcohol.

The absorbance results thus measured are shown in the graph of FIG. 2.

Example 4 Intracellular Fat Discharge Enhancement Activity of Shogaol

5 × 10 ⁴ / ml of 3T3-L1 fibroblasts were precultured for 2 days in a carbon dioxide incubator with DEME medium containing 10% serum and antibiotics. Thereafter, 2 mmol of insulin, 250 mmol of isobutylmethylxanthine and 10 mmol of dexamethasone were treated to differentiate into adipocytes. At this time, the medium was changed every two days, and the degree of differentiation into adipocytes was confirmed by treating a reagent for inducing differentiation.

After differentiation into adipocytes for 5 days or more, the cells were changed to a medium containing 10% serum and antibiotics, and then treated with different concentrations of shogaol. After 16 to 18 hours, the medium was discarded and dried, fixed in 10% formaldehyde solution for 1 hour, washed with phosphate buffered saline (PBS), dried, and then stained with a fat red dye (oil red O). Staining for 3 to 4 hours. The stained cells were washed and observed under a microscope. The red stained portions were dissolved using isoprophyl alcohol to measure absorbance at 510 nm.

The absorbance results thus measured are shown in the graph of FIG. 3.

Formulation Example 1 Preparation of Syrup

A syrup containing 2% (weight / volume) of shogaol or a pharmaceutically acceptable salt thereof according to the present invention was prepared by the following method.

Shogaol, saccharin and sugars were dissolved in 80 g of warm water. After the solution was cooled, a solution consisting of glycerin, saccharin, spices, ethanol, sorbic acid and distilled water was prepared and mixed thereto. Water was added to this mixture to 100 ml.

The components of the syrup are as follows.

Shogaol ········ 2 g

Saccharin 0.8 g

25.4 g of sugar

Glycerin 8.0 g

Spices ·········· 0.04 g

Ethanol 4.0 g

0.4 g of sorbic acid

Distilled water ········

Formulation Example 2 Preparation of Tablet

Tablets containing 15 mg of Shogaol were prepared by the following method.

250 g Shogaol was mixed with 175.9 g lactose, 180 g potato starch and 32 g colloidal silicic acid. 10% gelatin solution was added to the mixture, which was then ground and passed through a 14 mesh sieve. It was dried and the mixture obtained by adding 160 g of potato starch, 50 g of talc and 5 g of magnesium stearate was made into a tablet.

Formulation Example 3 Preparation of Injection Solution

Injection solution containing 10 mg of the active ingredient was prepared by the following method.

1 g of shogaol, 0.6 g of sodium chloride and 0.1 g of ascorbic acid were dissolved in distilled water to make 100 ml. The solution was bottled and sterilized by heating at 20 ° C. for 30 minutes.

The components of the injection solution are as follows.

Shogaol ········· 1 g

Sodium chloride 0.6 g

Ascorbic acid0.1 g

Distilled water ········

Formulation Example 4 Preparation of Beverage

After dissolving 500 mg of shogaol according to the present invention in an appropriate amount of water, vitamin C as an auxiliary component, citric acid, sodium citrate, and oligosaccharides as an auxiliary agent are added, and an appropriate amount of sodium benzoate is added as a preservative, and then water is added thereto. The total amount was made to 100 ml to prepare a beverage composition. At this time, taurine, myo-inositol, folic acid, pantothenic acid, etc. may be added alone or together.

As described above, the composition comprising shogaol isolated from ginger of the present invention is prepared as a medicine or food, thereby preventing and forming fat cells and promoting fat release in adipocytes, thereby treating and preventing obesity without side effects. .

In addition, it is possible to prevent various diseases such as coronary artery disease, diabetes mellitus, hypertriglyceridemia and hypertension that may be caused by obesity.

Claims (4)

Pharmaceutical composition for the prevention and treatment of obesity using shogaol as an active ingredient. The pharmaceutical composition of claim 1, wherein the shogaol is isolated from ginger. Food composition for the prevention and treatment of obesity using shogaol as an active ingredient. The food composition of claim 3, wherein the shogaol is isolated from ginger.

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