KR20150144160A - Composition for reducing body fat comprising xanthorrhizol or Java tumeric extract - Google Patents

Abstract

The present invention relates to a composition for reducing body fat of xanthorrhizol or a Java turmeric extract comprising the same. The xanthorrhizol or the Java turmeric extract comprising the same of the present invention shows an excellent body fat reducing effect by reducing weight of visceral adipose tissues and adipocyte size in an obesity animal model. Therefore, the composition shows an outstanding effect in decreasing the body fat and can be safely without side effects since the composition is based on natural substances.

Description

Technical Field [0001] The present invention relates to a composition for reducing body fat comprising, as an active ingredient,

The present invention relates to a new use of Janssorzol or a Java tumeric extract containing it. More particularly, the present invention relates to a composition for reducing body fat comprising, as an active ingredient, jazzor sol or a Java tumeric extract containing the same.

Obesity is a disease caused by an ideal increase in adipose tissue due to an imbalance of energy accumulation and consumption. Adipose tissue is an energy-storing organ. Excess energy intake promotes the differentiation of adipocytes and increases the amount of stored fat in the body, which is a direct cause of obesity. Obesity is recognized as a serious health problem in many countries around the world. In Korea, too, the prevalence of obesity is rapidly increasing due to various reasons such as high industrial growth, westernization of diet patterns and lack of physical activity. Obesity is a cause of many diseases such as hyperinsulinemia, arteriosclerosis, circulatory system diseases, cancer, diabetes and the like, as well as the problem itself, and the severity of the disease is further increasing (Nature 404: 635-643 , 2000, Obes., Rev. 12: 1-13, 2011).

Among the representative anti-obesity drugs developed so far, Reductil ^™ (Abbott Corporation, USA), which lowers appetite, and Xenical ^™ (Roche Pharmaceuticals, Switzerland), which inhibits fat absorption, are used clinically. However, heart diseases, respiratory diseases , Elevated blood pressure and insomnia (Phytochem. 71: 1625-1641, 2010).

Java tumeric is Curcuma xanthorrhiza Roxb., A kind of Zingiberaceae. It is used as a spice in tropical regions of Southeast Asia and has been widely used as a traditional medicine because of its strong antioxidant and anti-inflammatory action. Java turmeric has antimicrobial activity (J. Microbiol., 46, 228-232, 2008; Asian Pac. J. Trop. Biomed., 2, S637-S640, 2012), antioxidant activity (Evid. Based Complement Alternat. , Article ID 438356, 2012), antitumor activity (Phytother. Res., 22, 695-698, 2008), gastrointestinal protective activity (Biomed Res. Int., Article ID 416409, 2014) Plants Res. 4, 2512-2517, 2010).

Xanthorrhizol isolated from Java turmeric has antifungal activity (Fitoterapia, 71, 321-323, 2000; Planta Med., 66, 196-197, 2000), antifungal activity (Phytother. Res., 21, 434-438 , 2007), antiinflammatory activity (J. Environ. Pathol. Toxicol. Oncol. 21, 141-148, 2002), anticancer activity (Biochem. Biophys. Res. Commun., 326, 210-217, 2005) (Phytother. Res., 23, 1299-1302, 2009), neuroprotective activity (J. Neurosci. Res. 82, 831-838, 2005). However, prior to the present invention, there has been no detailed report on the effect of reducing the body fat of Janssorzol or the Java turmeric extract containing it.

Accordingly, the present inventors conducted a research to search for a natural substance which can be safely applied with excellent fat-reducing activity and found that xanthorrhizol or a Java tumeric extract containing the same is effective in the weight of visceral fat tissue And fat cells by decreasing the size of adipose cells. Thus, the present invention has been completed.

Accordingly, an object of the present invention is to provide a pharmaceutical composition for reducing body fat comprising, as an active ingredient, a jazzariz represented by the following formula 1 or a Java turmeric extract containing the same.

[Chemical Formula 1]

Another object of the present invention is to provide a food composition for reducing body fat comprising the active ingredient of the present invention.

To achieve the above object, the present invention provides a pharmaceutical composition for reducing body fat comprising xanthorrhizol represented by the following formula (1) or a Java tumeric extract containing the same as an active ingredient.

[Chemical Formula 1]

In order to accomplish the above object, the present invention provides a food composition for reducing body fat comprising, as an active ingredient, Jansseliz represented by Chemical Formula 1 or a Java turmeric extract containing the same.

Hereinafter, the contents of the present invention will be described in more detail.

The present invention can be used for the purpose of reducing body fat, which comprises the active ingredient of the jazzariz represented by the above formula (1) or the Java turmeric extract containing the same.

[Chemical Formula 1]

The Java turmeric extract of the present invention refers to an extract containing the jazzarizole represented by the above formula (1).

There is no limitation on the preparation method of the Java turmeric extract as long as it can contain the Nazorizol represented by the above-mentioned formula (1), but preferably from the Java turmeric plant or part of the plant (rhizome or root), water, an organic solvent having 1 to 6 carbon atoms, And may be extracted with one or more solvents selected from the group consisting of subcritical or supercritical fluids. It can also be prepared, if necessary, in addition to filtration and concentration steps according to methods known to those skilled in the art. In addition, specific fractions enriched in active material can be prepared using techniques such as solvent fractionation, silica gel chromatography, and prep-HPLC.

The organic solvent having a carbon number of 1 to 6 is not limited thereto, but preferably an alcohol having 1 to 6 carbon atoms, acetone, ether, benzene, chloroform, ethyl (ethyl) acetate, methylene chloride, hexane, cyclohexane, and petroleum ether.

Preferably, the Java turmeric extract of the present invention can be obtained by extracting and purifying rhizome of dried Java turmeric using purified water, ethanol and supercritical carbon dioxide suitable for food processing, or supercritical carbon dioxide, And directly separating and purifying the obtained oil.

In the pharmaceutical and food composition for reducing body fat of the present invention, the jazorsol represented by the above formula (1) can be extracted from Java turmeric plants or other plants and isolated or synthesized by a chemical synthesis method.

The separation and purification of the jazzyrazol represented by the above formula (1) of the present invention can be carried out by using column chromatography and high performance liquid chromatography (HPLC) packed with various synthetic resins such as silica gel and activated alumina, However, the method of extraction and separation and purification of Java turpentine is not necessarily limited to the above method.

In one embodiment of the present invention, a Java turmeric extract such as an ethanol extract, a hot water extract, a hexane extract, and an ethyl acetate extract was prepared using dried Java rhizome rhizome (see Example 1).

In another embodiment of the present invention, the Nansorizol represented by the above formula (1) was isolated from the extract of Java turmeric ethanol (see Example 2).

In another embodiment of the present invention, it has been confirmed that Janssorzol effectively reduces visceral fat weight and fat cell size in an obesity animal model (see Example 3).

In another embodiment of the present invention, it has been confirmed that the extract of Java turmeric ethanol effectively reduces visceral fat weight and fat cell size in an obesity animal model (see Example 4).

In another embodiment of the present invention, it was confirmed that the hot water extract of Java turmeric effectively reduces the weight of visceral fat in an obesity animal model (see Example 5).

In another embodiment of the present invention, it was confirmed that the extract of Java turmeric hexane effectively reduced the visceral fat weight in the obese animal model (see Example 6).

In another embodiment of the present invention, it has been confirmed that the extract of Java turmeric ethyl acetate effectively reduces the weight of visceral fat in an obesity animal model (see Example 7).

Therefore, the present invention can be used as a necessary ingredient of a pharmaceutical composition or a food composition because of its excellent effect of reducing body fat.

The jazzarizole of the present invention or the Java turmeric extract containing it can be used in its own or in a pharmaceutically acceptable form. The term " pharmaceutically acceptable " as used herein means physiologically acceptable and does not generally cause an allergic reaction or a similar reaction when administered to humans, and the salt includes a pharmaceutically acceptable free acid, Lt; / RTI > is preferred. As the free acid, an organic acid and an inorganic acid can be used. The organic acids include, but are not limited to, citric, acetic, lactic, tartaric, maleic, fumaric, formic, propionic, oxalic, trifluroacetic, benzoic, gluconic, methosulfonic, glycolic, succinic, Glutamic acid and aspartic acid. The inorganic acid includes, but is not limited to, hydrochloric acid, bromic acid, sulfuric acid, and phosphoric acid.

The pharmaceutical composition of the present invention may contain a pharmaceutically effective amount of jazzarizol or a Java turmeric extract containing it, or may comprise one or more pharmaceutically acceptable carriers. The term "pharmaceutically effective amount" as used herein refers to an amount exhibiting a reaction higher than that of the negative control, and preferably refers to an amount sufficient to reduce the body fat. The pharmaceutical composition of the present invention may contain 0.01 to 99.99% of Janssor sol or a Java turmeric extract containing the same, and the remaining amount may be occupied by a pharmaceutically acceptable carrier.

The pharmacologically effective amount of the zanthoxylated extract of the present invention is 0.001 to 100 mg / day / kg body weight, preferably 0.01 to 10 mg / day / kg body weight. However, the pharmaceutically effective amount may be appropriately changed depending on various factors such as the disease and its severity, the patient's age, weight, health, sex, administration route, and treatment period.

The term "pharmaceutically acceptable" as used herein means a non-toxic composition which is physiologically acceptable and which, when administered to humans, does not inhibit the action of the active ingredient and does not normally cause an allergic reaction such as gastrointestinal disorder, dizziness, . Such carriers include all kinds of solvents, dispersion media, oil-in-water or water-in-oil emulsions, aqueous compositions, liposomes, microbeads and microsomes.

Meanwhile, the pharmaceutical composition according to the present invention may be formulated together with a suitable carrier according to the route of administration. The administration route of the pharmaceutical composition according to the present invention is not limited thereto, but it can be administered orally or parenterally. Parenteral routes of administration include, for example, various routes such as transdermal, nasal, peritoneal, muscular, subcutaneous or intravenous.

In addition, when administered parenterally, the pharmaceutical composition of the present invention can be formulated together with a suitable parenteral carrier according to methods known in the art in the form of injection, transdermal drug delivery, and nasal inhalation. In the case of such injections, they must be sterilized and protected against contamination of microorganisms such as bacteria and fungi. Examples of suitable carriers for injectables include, but are not limited to, solvents or dispersion media containing water, ethanol, polyols (e.g., glycerol, propylene glycol and liquid polyethylene glycol, etc.), mixtures thereof and / or vegetable oils . More preferably, suitable carriers include isotonic solutions such as Hanks' solution, Ringer's solution, phosphate buffered saline (PBS) containing triethanolamine, or sterile water for injection, 10% ethanol, 40% propylene glycol and 5% dextrose Etc. may be used. In order to protect the injection from microbial contamination, various antibacterial and antifungal agents such as parabens, chlorobutanol, phenol, sorbic acid, thimerosal and the like may be further included. In addition, the injections may in most cases additionally include isotonic agents, such as sugars or sodium chloride.

Examples of transdermal dosage forms include ointments, creams, lotions, gels, solutions for external use, pastes, liniments, and air lozenges. By "transdermal administration" as used herein, it is meant that the pharmaceutical composition is locally administered to the skin so that an effective amount of the active ingredient contained in the pharmaceutical composition is delivered into the skin. These formulations are described in Remington's Pharmaceutical Science, 15th Edition, 1975, Mack Publishing Company, Easton, Pennsylvania, which is a commonly known formulary in pharmaceutical chemistry.

In the case of inhalation dosage forms, the compounds used according to the present invention may be formulated into a pressurized pack or a pressurized pack using a suitable propellant, for example dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide or other suitable gases. It can be conveniently delivered in the form of an aerosol spray from a nebulizer. In the case of a pressurized aerosol, the dosage unit may be determined by providing a valve that delivers a metered amount. For example, gelatin capsules and cartridges for use in an inhaler or insufflator may be formulated to contain a compound, and a powder mixture of a suitable powder base such as lactose or starch.

Other pharmaceutically acceptable carriers can be found in Remington's Pharmaceutical Sciences, 19th ed., Mack Publishing Company, Easton, Pa., 1995).

The pharmaceutical composition according to the present invention may also contain one or more buffers (e.g., saline or PBS), a carbohydrate (e.g., glucose, mannose, sucrose or dextran), an antioxidant, a bacteriostat, (E. G., EDTA or glutathione), an adjuvant (e. G., Aluminum hydroxide), a suspending agent, a thickening agent and / or a preservative.

In addition, the pharmaceutical compositions of the present invention can be formulated using methods known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to the mammal.

In addition, the pharmaceutical composition of the present invention can be administered in combination with a known compound having a body fat reducing effect.

Furthermore, the present invention can provide a nasal sol or a Java turmeric extract containing the same in the form of a food composition for the purpose of reducing body fat. The food composition of the present invention includes all forms of functional foods, nutritional supplements, health foods, food additives and feeds, It is targeted for eating. Food compositions of this type may be prepared in a variety of forms according to conventional methods known in the art.

For example, as a health food, it is possible to ingest the jazzarizol of the present invention or the Java turmeric extract itself containing the same in the form of tea, juice and drink for drinking, granulating, encapsulating and pulverizing. Also, the present invention can be prepared in the form of a composition by mixing the active ingredient of the present invention with a known active ingredient known to have a body fat reducing effect.

Functional foods also include beverages (including alcoholic beverages), fruits and their processed foods (e.g., canned fruits, bottled, jam, maalmalade, etc.), fish, meat and processed foods such as ham, Etc.), breads and noodles (eg udon, buckwheat noodles, ramen noodles, spaghetti, macaroni, etc.), fruit juice, various drinks, cookies, The present invention can be prepared by adding the jazzarizol of the present invention or the Java turmeric extract containing the same to the protein, the retort food, the frozen food, various kinds of seasonings (e.g., miso, soy sauce,

In addition, in order to use the Janssor sol of the present invention or the Java turmeric extract containing the same in the form of a food additive, it may be used in the form of powder or concentrate.

The preferred content of the janssor sol of the present invention or the Java turmeric extract containing the same in the food composition of the present invention may include about 0.01 to 100% by weight based on the total weight of the food.

INDUSTRIAL APPLICABILITY As described above, the present invention provides a composition for reducing body fat comprising jazzor sol or a Java turmeric extract containing the same as an active ingredient. The present invention relates to a method for reducing body fat by reducing the weight of visceral fat and the size of adipocytes. Accordingly, the present invention provides a composition for reducing body fat which can be safely used as a natural product without side effects, and exhibits an excellent effect for reducing body fat.

Fig. 1 shows the result of measuring the effect of reducing the visceral fat weight by the treatment with nasal spray in an obesity animal model.
FIG. 2 shows the results of measuring the effect of reducing the fat cell size by the treatment with Nasolizol in an obesity animal model.
FIG. 3 shows the results of measuring the effect of reducing the visceral fat weight by treatment with the extract of Javanese Calcium Ethanol containing Jansorizol in an obesity animal model.
FIG. 4 shows the results of measuring the effect of reducing the fat cell size by treatment with the extract of Javanese Calcium Ethanol containing Janssorol in an obesity animal model.

Hereinafter, the present invention will be described in more detail with reference to examples.

However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples. The experimental results of the following examples were expressed as mean ± standard deviation, and statistical analysis was evaluated using Duncan's test to be significant when the p value was 0.05 or 0.01 or less

Manufacture of Java turmeric extract

<1-1> Preparation of Ethanol Extract of Rhizobia root of Java

The dried rhizome of Java was pulverized with a mixer, and 100 g of the ground rhizosphere sample was added to 1 L of ethanol and extracted at room temperature for 48 hours. The extracted sample was filtered with filter paper of Whatman No. 2, and the filtered extract was concentrated with a vacuum rotary condenser to remove the solvent component, thereby obtaining an ethanol extract of Java Persimmon root.

<1-2> Preparation of hot water extract

The dried rhizome of Java was pulverized with a mixer, and 100 g of the ground rhizosphere sample was extracted with 1 L of water and stirred at 100 캜 for 4 hours. The extracted sample was filtered with filter paper No. 2 of Wattman, and the filtered extract was concentrated with a vacuum rotary condenser to remove the solvent component to obtain a hot water extract of Java Persimmon root.

<1-3> Preparation of hexane extract of rhizome root of Java

The dried rhizome was pulverized with a mixer, and then 100 g of the ground rhizosphere sample was added to 1 L of nucleic acid and extracted with stirring at 50 ° C for 60 minutes. The extracted sample was filtered with Wattman No. 2 filter paper, and the filtered extract was concentrated with a vacuum rotary condenser to remove the solvent component to obtain a hexane extract of Macaca fascicularis.

<1-4> Preparation of ethyl acetate extract

The dried rhizome was pulverized with a mixer, and 100 g of the ground rhizosphere sample was extracted with 1 L of ethyl acetate at 50 캜 with stirring for 60 minutes. The extracted sample was filtered with filter paper No. 2 of Wattman, and the filtered extract was concentrated with a vacuum rotary condenser to remove the solvent component to obtain an extract of ethyl acetate as a solvent.

Separation of Zazorizole

(11.1 g) obtained in the above-described Example 1-1 was placed in a column packed with silica gel, and a solvent system in which hexane and ethyl acetate were mixed at a ratio of 10: 1 (v / v) was used Lt; / RTI &gt; The fractions were divided into 6 fractions according to the sorting procedure, and the fractions were concentrated and dried. Five fractions (fraction 5) out of the six fractions were fractionated using developing solvent 80% methanol using Rp-18 reverse phase column chromatography (Lichroprep Rp-18 25-40 um, Merck & Co., USA). The fractions were divided into three fractions according to the above sorting order and concentrated and dried. The third fraction (fraction 3-3) of the three fractions was concentrated to dryness to isolate the pure single active substance zanthoxylate (0.52 g).

Determination of body fat reduction by obesity sol treatment in obese animal model

Obesity was induced by feeding a high fat diet (Product # D12492, Research Diet Inc., New Brunswick, NJ, USA) for 8 weeks to induce obesity and adaptation for 4 weeks to C57BL / 6 male mice for 1 week. 7 were randomly divided into two groups and used in the experiment. The test group was orally administered to the test group at a constant dose of 16 mg / day / kg of body weight per day for 16 weeks by suspending the test compound in 0.25% carboxymethylcellulose prepared in Example 2 . At this time, only the same amount of 0.25% carboxymethylcellulose was orally administered to the control group. Dietary and individual weights of the mice were measured every week.

As shown in FIG. 1, the visceral adipose tissue (epididymal fat, kidney fat, subcutaneous fat) was weighed and measured, The weight of visceral adipose tissue in the test group was 6.38% (p <0.05) lower than that of the control group. As shown in Fig. 2, the fat cells of the visceral adipose tissues were orally administrated with orally administered jazzyrazol, and the size of the adipose tissues was 20.1% ( p <0.05). These results indicate that the nansol sol of the present invention provides a body fat reducing effect.

Reduction of body fat reduction by treatment with ethanol extract of Java turmeric in obese animal model

The animal model of obesity induced by the same method as in Example 3 was orally administered at a dose of 100 mg / day / kg body weight of the extract of Java corn oil of the Example 1-1 for 16 weeks once a day for a predetermined time . As a result, as shown in Fig. 3, the weight of visceral adipose tissue of the test group administered with the extract of Java turmeric was decreased by 4.80% (p <0.05) compared to the control group. As shown in FIG. 4, the fat cells of the visceral adipose tissues of the extracted visceral adipose tissues were 22.6 times larger than those of the control group, % (p &lt; 0.01). These results indicate that the Java corn ethanol extract of the present invention provides a body fat reducing effect.

Decrease of body fat by treatment of hot water extract of Java turmeric in obese animal model

The animal model of obesity induced by the same method as in Example 3 was orally administered at a dose of 500 mg / day / kg body weight of the aqueous extract of Java turmeric in Example 1-2 for 16 weeks once a day for a predetermined time . As a result, the weight of visceral adipose tissue in the test group of oral administration of Java hydrothermal extract was 7.74% (p <0.05) lower than that of the control group.

Obesity Animal Model Reduces Fat Loss by Treatment of Java Turmeric Hexane Extract

The animal model of obesity induced by the same method as that of Example 3 was orally administered at a dose of 200 mg / day / kg body weight of the extract of Java turmeric hexane of Example 1-3 for 16 weeks once a day for a predetermined time . As a result, the weight of visceral adipose tissues in the oral group administered with the extract of Java vulcanized with hexane decreased by 8.20% (p <0.05) compared to the control group.

Determination of body fat reduction effect by treatment with Java citrus ethyl acetate in an obesity animal model

The animal model in which obesity was induced in the same manner as in Example 3 was administered at an administration concentration of 500 mg / day / kg body weight of Java Persimmon's ethyl acetate extract of Example 1-4, once per day for 16 weeks, Respectively. As a result, the weight of the visceral adipose tissue of the test group treated with the extract of Java potassium ethylacetate was 6.09% (p <0.05) lower than that of the control group.

As described above, the present invention provides a composition for reducing body fat comprising xanthorrhizol or a Java tumeric extract containing the same as an active ingredient. The present invention provides a method of reducing body fat by reducing the weight of visceral adipose tissue and the size of adipocytes in an obesity animal model. Therefore, the present invention can be used safely without side effects because it is a natural product, and it is possible to provide a composition showing an excellent effect on reduction of body fat, so that it is highly likely to be used industrially.

Claims (5)

A pharmaceutical or food composition for reducing body fat comprising xanthorrhizol represented by the following formula (1) as an active ingredient:

[Chemical Formula 1]

2. The pharmaceutical or food composition for reducing body fat according to claim 1, wherein the jazorsol represented by the formula (1) is isolated from Java tumeric extract.
A pharmaceutical or food composition for reducing body fat comprising an extract from Java as an active ingredient.
[4] The composition of claim 3, wherein the Java turmeric extract is an extract of at least one solvent selected from the group consisting of water, an organic solvent having 1 to 6 carbon atoms, and a subcritical or supercritical fluid.
The method of claim 4, wherein the organic solvent having 1 to 6 carbon atoms is selected from the group consisting of alcohol having 1 to 6 carbon atoms, acetone, ether, benzene, chloroform, ethyl acetate ), Methylene chloride, hexane, cyclohexane, and petroleum ether (petroleum
ether). &lt; / RTI &gt;

Images