KR101895874B1 - Agent for inhibiting obesity comprising hot water extract of piper longum - Google Patents

Abstract

The present invention discloses an agent for inhibiting obesity comprising an extract of hot water as an active ingredient.

Description

[0001] The present invention relates to an agent for inhibiting obesity,

The present invention relates to a preparation for preventing or inhibiting obesity containing a water-based hot-water extract.

Surplus energy due to the imbalance of energy input and consumption is stored in adipose tissue in the form of triglycerides. Obesity is a cause of metabolic diseases such as type 2 diabetes, hyperlipidemia, hypercholesterolemia, hypertension, arteriosclerosis or various cancers, as well as changes in the external appearance It can also cause mental disorders such as loss of self-confidence, depression, and gangrene. One way of preventing or treating such obesity is to control fat metabolism in adipose tissue.

By controlling fat metabolism and decomposing fat in the body, it is possible to prevent excessive accumulation of body fat and prevent or treat obesity. Since the volume of 1 kg of fat is 4 times larger than that of the muscle of the same weight, when the decomposition of fat in the fat cells is accelerated, not only the body weight is reduced but also the volume of the body is reduced, so that a smooth body line and a resilient body have.

Korean Patent Publication No. 10-2002-0065120 (published on Aug. 13, 2002) Specification

The present invention provides an agent for suppressing obesity, specifically, an agent for suppressing obesity induced by lipid intake by promoting subcutaneous fat decomposition.

One aspect of the present invention provides an agent for suppressing obesity comprising a Piper longum hot water extract as an active ingredient.

The preparation according to the present invention can prevent or inhibit obesity by promoting lipolysis of subcutaneous adipocytes and inhibiting fat accumulation in subcutaneous adipocytes, by including a volatile hot-water extract as an active ingredient. Specifically, the preparation according to the present invention is excellent in preventing or inhibiting obesity induced by lipid intake.

FIG. 1 is a graph comparing the contents of the components of the water-in-oil-extracted hot-water extract and the water-containing alcoholic extract.
FIG. 2 is a graph showing the degree of lipolysis in human subcutaneous adipose cells treated with a water-extract of hot-water or a extract of a water-containing alcohol.
FIG. 3 is a photograph showing fat in human subcutaneous fat cells treated with a water-extract of hot-water or extract of a water-containing alcohol.
FIG. 4 is a graph showing the amount of fat remaining in human subcutaneous adipose cells treated with the extract of water-in-oil or water-in-oil extract.
FIG. 5 is a graph showing a change in body weight of a high-fat diet treated with water-extract of hot pepper powder or extract of powdered spirit extract.
FIG. 6 is a graph showing the epididolipids weight of high-fat diet-treated mice treated with a water-extract of hot pepper or a water-extracted ethanol extract.
FIG. 7 is a graph showing the weight of subcutaneous fat of a high-fat diet treated with a water-extract of hot pepper or a water-extract of alcohol.

Body fat can be divided into visceral fat and subcutaneous fat. Visceral fats in the abdominal cavity of the body secrete a large amount of hormones that are involved in energy metabolism and inflammation reaction, inducing obesity which causes various diseases, and it is present in the lower layer of the skin dermis to provide elasticity to the skin And subcutaneous fat, which protects the body, mainly causes obesity, which has a negative effect on cosmetics. Therefore, it is more important to reduce subcutaneous fat in order to have a beautiful body line and body shape. However, because subcutaneous adipocytes do not degrade more easily than visceral adipocytes, it is not easy to find a way to easily break them down.

Hereinafter, the present invention will be described in detail.

One aspect of the present invention provides an agent for suppressing obesity comprising a Piper longum hot water extract as an active ingredient. Lipid-hydrothermal extracts can prevent or inhibit obesity by promoting the breakdown of subcutaneous fat and inhibiting fat accumulation in subcutaneous adipocytes. In addition, it is more effective in preventing or inhibiting obesity induced by lipid intake than in sugar because it promotes direct degradation of subcutaneous fat rather than inhibiting fatty acid synthetase. It is considered that the effect of the hot water extract of the present invention can not be expected in the case of the extract of the present invention, but the content of the extract of the present invention is different from that of the extract of the present invention.

Another aspect of the present invention provides a formulation for body slimming comprising an extract of hot water as an active ingredient. In the present specification, the term "body slimming" means to have a thin and resilient body through a process of promoting the decomposition of subcutaneous fat.

In the present specification, it is known that the petal is an immature fruit of Piper longum belonging to the pepper family, which warms the stomach and intestines and induces heat, thereby eliminating the cold air of the body.

As used herein, the term "extract" can be obtained by a general extraction method in the art as a broad concept including a substance obtained by extracting a component of a natural product, regardless of the type of extraction method, extraction solvent or extract. In one aspect of the present invention, the water-based hot-water extract can be obtained by adding hot water at 80 to 120 ° C, specifically 85 to 110 ° C, to the petal and extracting it for 1 to 10 hours, specifically 2 to 8 hours. In another aspect of the present invention, the hot water comprises distilled water, purified water or deionized water at 80 to 120 ° C, specifically 85 to 110 ° C. In another aspect of the present invention, the extract of the present invention can be obtained by adding alcohol, specifically ethanol, to reflux and refluxing and concentration under reduced pressure.

The formulation according to one aspect of the present invention may comprise from 1 to 80% by weight, specifically from 5 to 60% by weight, more specifically from 10 to 30% by weight, of a volumetric hot water extract, based on the total weight of the formulation. When it is included in the above range, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy all the stability and safety of the preparation, and it may be appropriate to include the above range in terms of cost effectiveness. Concretely, when the amount of the hot water extract of the present invention is less than 1% by weight, a sufficient effect of preventing or inhibiting obesity can not be obtained. When it exceeds 80% by weight, safety and stability may be lowered.

One aspect of the present invention provides a food composition comprising a preparation comprising an extract of hot water as an active ingredient. The food composition may prevent or inhibit obesity, and may specifically have weight loss and body slimming effects. In another aspect of the invention, the food composition comprises a preference food or a health food composition.

The formulation of the food composition is not particularly limited, but may be formulated into, for example, tablets, granules, powders, pills, liquids such as drinks, gels, solid bars and the like. The food composition of each formulation can be blended with the ingredients commonly used in the field in addition to the active ingredient without difficulty by those skilled in the art depending on the purpose of formulation or use, and synergistic effect can be obtained when the composition is applied simultaneously with other ingredients.

Determination of the dosage of the active ingredient is within the level of ordinary skill in the art and its daily dose is, for example, from 0.1 mg / kg / day to 5000 mg / kg / day, more specifically from 50 mg / kg / day to 500 mg / kg / day, but it is not limited thereto, and may be varied depending on various factors such as the age, health condition, and complication of the subject to be administered.

One aspect of the present invention provides a pharmaceutical composition comprising a preparation comprising an extract of hot water as an active ingredient. The pharmaceutical composition may prevent or inhibit obesity, and may specifically have weight loss and body slimming effect.

The pharmaceutical composition according to one aspect of the present invention may be administered orally, parenterally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, and the like.

Formulations for oral administration may be in the form of tablets, pills, soft and hard capsules, granules, powders, granules, solutions, emulsions or pellets, It is not. These formulations may contain, in addition to the active ingredient, a diluent such as lactose, dextrose, sucrose, mannitol, sorbitol, cellulose or glycine, a lubricant such as silica, talc, stearic acid or polyethylene glycol, or a binder such as magnesium aluminum Silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose or polyvinylpyrrolidone). And may optionally contain pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, or sweeteners. The tablets may be prepared by conventional mixing, granulating or coating methods.

Formulations for parenteral administration may be, but are not limited to, injections, drops, lozenges, ointments, gels, creams, suspensions, emulsions, suppositories, patches or spraying agents.

The effective ingredients of the pharmaceutical composition according to one aspect of the present invention will vary depending on the age, sex, weight, pathological condition and severity of the subject to be administered, route of administration, or judgment of the prescriber. Determination of the amount of application based on these factors is within the level of ordinary skill in the art and its daily dose is, for example, from 0.1 mg / kg / day to 100 mg / kg / day, more specifically from 5 mg / kg / day. < / RTI >

One aspect of the present invention provides a cosmetic composition comprising a preparation containing an extract of hot water as an active ingredient. The cosmetic composition may prevent or inhibit obesity, and may have a weight loss and a body slimming effect.

The cosmetic composition according to the present invention may be provided in all formulations suitable for topical application. For example, it may be provided as a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an oil phase in water, a suspension, a solid, a gel, a powder, a paste, a foam or an aerosol composition. Compositions of such formulations may be prepared according to conventional methods in the art.

The cosmetic composition according to the present invention may further comprise a moisturizing agent, an emollient agent, a surfactant, an ultraviolet absorber, an antiseptic, a bactericide, an antioxidant, a pH adjusting agent, organic and inorganic pigments, a fragrance, . The compounding amount of the above components can be easily selected by those skilled in the art within a range not to impair the objects and effects of the present invention. The amount thereof may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, have.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to Examples, Comparative Examples and Experimental Examples. However, these examples, comparative examples, and experimental examples are provided for illustrative purposes only in order to facilitate understanding of the present invention, and the scope and scope of the present invention are not limited thereto.

[Example] Preparation of a hot water extract

Piper longum fruit was dried, and purified water corresponding to 10 times of dry petal fruit was added and extracted at 90 ° C for 4 hours. Thereafter, a concentrated hot water extract was obtained by using a concentrator.

[Comparative Example] Preparation of an extract of a petroleum spirit extract

Ethanol was added to the dry petal fruits, followed by reflux extraction and concentration under reduced pressure to prepare a pale orange extract.

[Experimental Example 1] Comparison between the extract of hot water and the ethanol extract

(Waters Alliance e2695 HPLC system / PDS 250 nm, Mightysil C18 (250 x 4.6 mm, 5 m), DIW acetonitrile gradient) to compare the contents of the water-in- Respectively. The results are shown in Fig.

As can be seen from Fig. 1, a specific peak not detected in the extract of Liliaceae was detected in the hot water extract of Liliaceae during 50 to 60 minutes. As a result, it can be seen that the contents of the water-containing hot-water extract and the water-containing ethanol extract are different from each other, and the effect thereof may be different.

[Experimental Example 2] Evaluation of lipolysis effect in human subcutaneous fat cells

The following experiment was conducted to evaluate the lipid degradation effect of the hydrolyzate of the extract from human subcutaneous fat cells.

Human subcutaneous adipocytes were purchased from Zen-Bio and cultured in a 5% CO ₂ incubator at 37 ° C in a medium for human subcutaneous fat cells (Zenbaio). The cultured human subcutaneous adipocytes were treated with water-extracted hot-water extracts and water-extracted ethanol extracts at 10, 50 and 100 g / ml for 24 hours. Negative controls were treated with water at a volume of 1/1000 and positive controls treated with IBMX, known to promote lipolysis by inhibiting the activity of phosphodiesterase (PDE) 4. Cells treated with each sample were further cultured for 72 hours, and the amount of degraded triglycerides was measured using a TG reagent reagent (Sigma). The results are shown in Fig.

As can be seen from Fig. 2, the extract from the petroleum hydrothermal solution promoted lipolysis in subcutaneous fat cells in a concentration-dependent manner. On the other hand, the extract of Peppercorn extract showed little decomposition of fat in subcutaneous fat cells. It can be seen that the extract of Phellodendri shower can hardly decompose human subcutaneous fat, whereas the extract of Phellodendron radical has excellent effect on the decomposition of subcutaneous fat.

[Experimental Example 3] Evaluation of lipid-lowering effect on human subcutaneous fat cells

Subcutaneous adipose fat cells were treated with 10, 50 and 100 g / ml of the extruded hot-water extract and the extract of liquor extract for 72 hours in substantially the same manner as in Experimental Example 2, washed with PBS and treated with formaldehyde (Sigma) Respectively. Fixed cells were washed once with PBS and treated with Oil-red O solution for 15 minutes to stain fat stored in the cells. The results are shown in FIG. The stained fat was dissolved in isopropanol (Sigma) and quantitated to be shown in FIG.

As can be seen in FIGS. 3 and 4, the amount of the remaining fat in the cells treated with the hot-water extract of petroleum waters was about 30% smaller than that of the negative control cells. On the other hand, there was no significant difference in the amount of fat remaining in the cells treated with the extract of P. vivax from the negative control. Based on these results, it can be seen that the extract of L. falciparum has an excellent effect of reducing the amount of fat accumulated in human subcutaneous adipocytes, whereas the extract of L. falciparum shows little effect of reducing the subcutaneous fat.

[Experimental Example 4] Weight and subcutaneous fat changes in mice fed with hot water extract

We measured the changes in body weight and epididymal fat weight before and after administration of 200 mg / kg of penicillin hydrothermal extract and water extract of pale yellow algae, respectively, to a 7 week old male C57BL / 6J mouse (n = 10) Respectively. The results are shown in Fig. 5 and Fig. The weight of subcutaneous fat of each mouse was measured and shown in FIG. In addition, mice fed only high fat diets and normal diets were evaluated together as controls.

As can be seen from FIGS. 5 to 7, the mice treated with the hot-water extract of P. vivax significantly slowed the weight gain (Fig. 5) and significantly decreased the epididymal fat weight (Fig. 6) Subcutaneous fat weight was also significantly lower (Fig. 7). On the other hand, in the mice treated with the extract of Phellodendron sunflower extract, there was almost no effect of slowing of weight gain, reduction of epididymal fat weight, and reduction of subcutaneous fat. Based on these results, it can be seen that the extract of petroleum jelly can be used to prevent or inhibit obesity by promoting the degradation of subcutaneous fat at an animal level, and is more effective in preventing or treating obesity caused by high fat diet, that is, lipid intake. Also, it can be confirmed that the effect of the water extract of Liliaceae can not be expected in the case of the Lilac extract.

Formulation examples of compositions according to one aspect of the present invention are described below, but may be applied to various other formulations, which are not intended to be limiting but merely illustrative of the invention.

[Formulation Example 1] Health food

Lilac hydrothermal extract ................... 1000 ㎎

Vitamin mixture

Vitamin A acetate ............ 70 ㎍

Vitamin E ........................ 1.0 mg

Vitamin B1 ....................... 0.13 mg

Vitamin B2 ...................... 0.15 mg

Vitamin B6 ........................ 0.5 mg

Vitamin B12 ....................... 0.2 g

Vitamin C .......................... 10 mg

Biotin ............................. 10 μg

Nicotinic acid amide ... 1.7 mg

Folic acid ............................... 50 ㎍

Calcium pantothenate ..................... 0.5 mg

Mineral mixture

Ferrous sulfate ........................ 1.75 mg

Zinc oxide .......................... 0.82 mg

Magnesium carbonate ...................... 25.3 mg

Potassium Phosphate ......................... 15 mg

Secondary Calcium Phosphate ..................... 55 mg

Potassium citrate .......................... 90 mg

Calcium carbonate ........................... 100 mg

Magnesium chloride ...................... 24.8 mg

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with the ingredient suitable for health food as a preferred embodiment, the compounding ratio thereof may be arbitrarily modified.

[Formulation Example 2] Health drinks

Lilium hydrothermal extract ........................ 1000 mg

Citric acid ................................ 1000 mg

Oligosaccharides ................................ 100 g

Taurine .................................... 1 g

Purified water .................................. Remaining amount

The above components are mixed according to a conventional health drink manufacturing method, and the mixture is stirred and heated at 85 DEG C for about 1 hour, and then the solution is sterilized by filtration.

[Formulation Example 3] Tablets

100 mg of soybean extract, 50 mg of glucose, 100 mg of red ginseng extract, 50 mg of red ginseng extract, 96 mg of starch and 4 mg of magnesium stearate were mixed and 40 mg of 30% ethanol was added thereto to form granules. And tableted using a tablet machine.

[Formulation Example 4]

The granules are formed by mixing 100 mg of the extract from the hot-water extract, 50 mg of the soybean extract, 100 mg of the glucose and 600 mg of the starch, and adding 100 mg of the 30% ethanol to the granules, followed by drying at 60 ° C. to form granules.

[Formulation Example 5] Ointment

Ointments were prepared in a conventional manner according to the compositions shown in Table 1 below.

ingredient Content (% by weight) Plum water extract 3.0 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Squalane 1.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 Wax 4.0 Preservative, coloring, fragrance Suitable amount Purified water Balance

Claims (8)

Piper longum Contains hot water extract as an active ingredient and inhibits subcutaneous fat accumulation.
The method according to claim 1,
Lipid extract is an anti - obesity agent that promotes the breakdown of subcutaneous fat.
The method according to claim 1,
Obesity is an obesity-suppressing agent including obesity induced by lipid intake.
The method according to claim 1,
Wherein the hot water contains water at 80 to 120 占 폚.
The method according to claim 1,
Wherein the preparation comprises 1 to 80% by weight of a volumetric hot water extract based on the total weight of the formulation.
A food composition for obesity control comprising the agent according to any one of claims 1 to 5.
A pharmaceutical composition for the inhibition of obesity comprising the agent according to any one of claims 1 to 5.
A cosmetic composition for obesity suppression comprising the preparation according to any one of claims 1 to 5.

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