KR20190136728A - A composition for prevention and treatment of obesity comprising extracts of oat hull - Google Patents

Abstract

The present invention relates to: a composition for preventing or treating obesity, containing an oat hull extract; functional food for preventing or alleviating obesity; and a method for preventing or treating obesity comprising a step of administering the extract to an individual except a human. A pharmaceutical composition for preventing or treating obesity containing the oat hull extract according to the present invention has low cytotoxicity and exhibits excellent anti-differentiation activity of preadipocyte cells to have an excellent effect of treating obesity, thereby being able to be provided as an active component of the pharmaceutical composition, health functional food, and a therapeutic method for preventing or treating obesity.

Description

A composition for prevention and treatment of obesity comprising extracts of oat hull}

The present invention relates to a pharmaceutical composition for preventing or treating obesity, including an oat shell extract, a dietary supplement for preventing or improving obesity, and a method for preventing or treating obesity comprising administering the extract to an individual except a human.

Oat is a two-year-old herbaceous family of rice plants. Its scientific name is Avena sativa, and it is also known as ointment. It is clustered at the bottom and reaches 1m in height. Stems stand straight and have almost no hairs, but nodes have hairs facing down. Leaves are 15-30cm long, 6-12mm wide, wider than wheat, and dark green. The leaflet is long, the leaf tongue is short, and finely divided. Flowers bloom in May-June and cone-shaped inflorescences are 20-30cm long. The spikelets are green, with stems, with two small flowers, and hang down.

Oats, like other grains, are carbohydrates, but have 13-14% protein, more than rice, barley and wheat, and 5-6% lipids. However, oats have the same amino acid composition as lysine, tryptophan, threonine and methionine. Oats are used primarily for livestock food and feed, but peeled and pressed flat to make oatmeal or cookies. Oats are rich in fiber, which lowers blood cholesterol, prevents constipation, and is rich in unsaturated fatty acids that lower blood pressure. However, little research has been conducted on oat shells.

On the other hand, obesity refers to a condition in which there is an excessive amount of fat in the body. Specifically, when the body obesity index (body mass index: weight (kg) divided by height (m) squared) is defined as obesity do. Obesity can be caused by very complex causes, such as genetic and environmental factors, but as a result, fat is accumulated due to energy imbalances when nutrients are consumed in excess of energy consumption over a long period of time. Obesity increases the likelihood of developing diabetes and hyperlipidemia, and increases the risk of developing sexual dysfunction, arthritis, and cardiovascular disease. Gallstones can develop and in some cases are also linked to the development of cancer ( Cancer Research 67.6, 2007: 2391-2393.).

This obesity has become a very important national issue because of the increase in obesity in each country. The US obesity population is 33 percent, and overweight population is 67 percent, and the federal government continues to provide a range of policies and assistance to reduce obesity rates. Korea's obesity population is 30% as of 2015, which is lower than the United States, but it is steadily increasing. Therefore, measures against obesity are urgently needed.

Currently, two anti-obesity drugs in Korea are serotonin-based appetite suppressants, lorcaserin and lipase inhibitor orlistat, which can be used for a long time. Obesity treatments using natural materials have not been met.

Thus, the present inventors have made intensive studies to develop a natural-derived material having a therapeutic effect on obesity. As a result, the present inventors have completed the present invention by confirming the progenitor cell differentiation inhibitory activity of oat shell extract.

It is a main object of the present invention to provide a pharmaceutical composition for preventing or treating obesity comprising oat shell extract.

Another object of the present invention to provide a dietary supplement for the prevention or improvement of obesity, including oat shell extract.

Still another object of the present invention is to provide a method for preventing or treating obesity, comprising the step of administering an oat shell extract to an individual except a human.

As one aspect for achieving the above object, the present invention provides a pharmaceutical composition for the prevention or treatment of obesity, including oat shell extract.

Hereinafter, a pharmaceutical composition for preventing or treating obesity including oat shell extract in the present invention will be described in detail.

As used herein, the term "oats" is a biennial herbaceous family of rice plants and the scientific name is Avena sativa . Oat shell of the present invention may mean by-products other than the grains that come out after the processing of the oats, due to technical limitations may also include oat shells with some grains attached.

Oat shell of the present invention may be to include an oat grain chamber.

As used herein, the term "extract" refers to a substance obtained by extracting a substance, and specifically, an extract obtained by the extraction process of the oat shell of the present invention, a dilution of the extract, a concentrated solution, and the extract Extracts of all formulations that can be formed using the extract itself and the extract, such as dried products obtained by drying, crudes or purified products of the extract or mixtures thereof.

The method of extracting the oat shell is not particularly limited, and may be extracted according to a method commonly used in the art. Non-limiting examples of the extraction method may include solvent extraction, ultrasonic extraction, filtration, reflux extraction, and the like, which may be performed alone or in combination of two or more methods.

In the present invention, the type of the extraction solvent used for the extraction of the oat shell is not particularly limited, and any solvent known in the art may be used. Non-limiting examples of the extraction solvent may be water, an alcohol having 1 to 4 carbon atoms, hexane (Hexane) or a mixed solvent thereof, but is not limited thereto and may be used alone or in combination of one or more.

 Specifically, the solvent may be water, alcohol, hexane, and more specifically, alcohol, but is not limited thereto.

In one embodiment of the present invention, water, hexane and spirits were added to the oat shell, respectively, and oat shell water and hexane spirit extract were prepared through stirring, extraction, filtration and concentration.

As used herein, the term "obesity" refers to an excessive state of fat in the body, and specifically, the body obesity index (body mass index: body mass index: weight (kg) divided by height (m) squared) is 25 If above, it is defined as obesity. Obesity can be caused by very complex causes, such as genetic and environmental factors, but as a result, fat is accumulated due to energy imbalances when nutrients are consumed in excess of energy consumption over a long period of time. Obesity increases the likelihood of developing diabetes and hyperlipidemia, and increases the risk of developing sexual dysfunction, arthritis, and cardiovascular disease.

As used herein, the term "prevention" may mean any action of inhibiting or delaying obesity by administering an oat shell extract according to the present invention to an individual.

As used herein, the term "treatment" may refer to all the actions of administering the composition of the present invention to a suspicious subject to obesity to improve or benefit from obesity.

Oat shell extract provided by the present invention may be low in cytotoxicity and have an effect of inhibiting the accumulation of fat to have a therapeutic effect on obesity.

In one embodiment of the present invention, when the oat bark extract was treated by concentration and solvent in the fat precursor cells and the survival rate was confirmed, water and nucleic acid showed little cytotoxicity and alcohol showed low cytotoxicity (FIG. 3). .

The composition of the present invention may be characterized by inhibiting fat precursor cells.

In one embodiment of the present invention, as a result of treating the oat bark extract to the fat precursor cells, it showed an excellent differentiation inhibitory activity compared to the untreated control group to confirm the obesity treatment effect of the oat bark extract (Fig. 4).

The pharmaceutical composition of the present invention may also be used as a single agent, and may be prepared and used in a combination formulation, further including a drug known to have a recognized therapeutic effect on obesity, and formulated using a pharmaceutically acceptable carrier or excipient, in a unit dose. It may be prepared in the form or prepared by incorporating into a multi-dose container.

As used herein, the term "pharmaceutically acceptable carrier" may refer to a carrier or diluent that does not interfere with the biological activity and properties of the compound to be injected without stimulating the organism. The kind of the carrier usable in the present invention is not particularly limited, and any carrier can be used as long as it is a conventionally used and pharmaceutically acceptable carrier in the art. Non-limiting examples of the carrier include saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, dextrose solution, maltodextrin solution, glycerol, ethanol and the like. These may be used alone or in combination of two or more thereof. The carrier may include a non-naturally occuring carrier.

In addition, if necessary, other conventional additives such as antioxidants, buffers and / or bacteriostatic agents may be added and used, and diluents, dispersants, surfactants, binders, lubricants, and the like may be additionally added to provide a solution such as an aqueous solution, a suspension, an emulsion, or the like. It may be formulated into a use formulation, pills, capsules, granules or tablets.

In addition, the pharmaceutical composition of the present invention may include a pharmaceutically effective amount of oat shell extract.

As used herein, the term “pharmaceutically effective amount” means an amount sufficient to treat a disease at a reasonable benefit / risk ratio applicable to medical treatment, generally in an amount of 0.001 to 1000 mg / kg, preferably The amount of 0.05 to 200 mg / kg, more preferably 0.1 to 100 mg / kg may be administered once to several times daily. However, for the purposes of the present invention, the specific therapeutically effective amount for a particular patient is determined by the specific composition, including the type and extent of the reaction to be achieved, whether or not other agents are used in some cases, the age, body weight, general state of health of the patient, It is desirable to apply differently depending on various factors and similar factors well known in the medical field, including sex and diet, time of administration, route of administration and rate of composition, duration of treatment, drugs used with or co-specific with the specific composition.

The pharmaceutical compositions of the present invention may be administered as individual therapeutic agents or in combination with other therapeutic agents and may be administered sequentially or simultaneously with conventional therapeutic agents. And single or multiple administrations. In consideration of all the above factors, it is important to administer an amount that can achieve the maximum effect in a minimum amount without causing side effects, and can be easily determined by those skilled in the art.

The term "administration" in the present invention means introducing the pharmaceutical composition of the present invention to the patient in any suitable way, and the route of administration of the composition of the present invention is various oral or parenteral routes as long as the target tissue can be reached. It can be administered through.

The mode of administration of the pharmaceutical composition according to the present invention is not particularly limited, and may be in accordance with methods commonly used in the art. As a non-limiting example of the mode of administration, the composition may be administered orally or parenterally. The pharmaceutical compositions according to the invention may be prepared in various formulations depending on the desired mode of administration.

The frequency of administration of the composition of the present invention is not particularly limited, but may be administered once a day or several times in divided doses.

The administration concentration of the composition of the present invention is not particularly limited, but may be 1 μg / ml or more but less than 150 μg / ml, specifically 2 μg / ml or more and less than 120 μg / ml, and more specifically 3 μg / ml or more and less than 100 μg / ml.

As another aspect, the present invention provides a dietary supplement for preventing or improving obesity comprising oat shell extract.

The oat bark extract has been used as a natural material for a long time has been proved stability, can be prepared in the form of a food that can prevent or improve obesity, but can also be eaten.

Functional food is the same term as food for special health use (FOSHU), and means foods that have high medical effects and medical effects that are processed so that their bioregulatory functions are efficiently displayed in addition to nutrition. In addition, the food may be prepared in various forms such as tablets, capsules, powders, granules, liquids, pills, etc. in order to obtain a useful effect in the prevention or improvement of obesity.

The food composition of the present invention may further comprise a food acceptable carrier.

There is no restriction | limiting in particular in the kind of food which can add the composition containing oat shell extract of this invention, For example, there are various drinks, gum, tea, a vitamin complex, a health supplement food, etc. The food composition may be added to other ingredients that do not interfere with the prevention or improvement effect of obesity, the kind is not particularly limited. For example, various herbal extracts, food acceptable additives, natural carbohydrates, and the like may be contained as additional ingredients, such as conventional foods.

The food supplement additive is added to prepare the health functional food of each formulation can be used by those skilled in the art as appropriate. For example, various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic and natural flavors, colorants and fillers, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusters , Stabilizers, preservatives, glycerin, alcohols, carbonation agents used in the carbonated beverage, and the like, but the type is not limited by the above examples.

At this time, the content of the extract included in the food is not particularly limited, but may be included in 0.01 to 100% by weight, more preferably 1 to 80% by weight relative to the total weight of the food composition.

When the food is a beverage, it may be included in a ratio of 1 to 30 g, preferably 3 to 20 g based on 100 ml. In addition, the composition may include additional ingredients that are commonly used in food compositions to improve the smell, taste, time and the like. For example, it may include vitamins A, C, D, E, B1, B2, B6, B12, niacin, biotin, folate, panthotenic acid, and the like. In addition, it may include minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn), copper (Cu). It may also contain amino acids such as lysine, tryptophan, cysteine, valine and the like. In addition, preservatives (potassium sorbate, sodium benzoate, salicylic acid, sodium dehydroacetate, etc.), fungicides (bleaching powder and highly bleaching powder, sodium hypochlorite, etc.), antioxidants (butylhydroxyanisol (BHA), butylhydroxytoluene ( BHT), etc.), colorants (such as tar pigments), colorants (such as sodium nitrite, sodium nitrite), bleach (sodium sulfite), seasonings (such as MSG glutamate), sweeteners (ducin, cyclate, saccharin, sodium, etc.) , Food additives such as flavorings (vanillin, lactones, etc.), swelling agents (alum, potassium D-tartrate, etc.), reinforcing agents, emulsifiers, thickeners (pigments), coatings, gum herbicides, foam inhibitors, solvents, improvers, etc. ) Can be added. The additive is selected according to the type of food and used in an appropriate amount.

The health functional food of the present invention can be prepared by a method commonly used in the art, and the preparation can be prepared by adding raw materials and ingredients commonly added in the art. In addition, unlike the general medicine has the advantage that there is no side effect that can occur when taking a long-term use of the drug with food as a raw material, can be excellent in portability.

As another aspect, the present invention provides a method for preventing or treating obesity, comprising administering oat shell extract to a subject other than humans.

As used herein, the term "individual" may mean any animal, including a human who has or is likely to become obese. The animal may be a mammal such as, but not limited to, a human, a cow, a horse, a sheep, a pig, a goat, a camel, a antelope, a dog, a cat, and the like, which require treatment of similar symptoms.

In particular, the prophylactic or therapeutic method of the present invention may include administering the composition in a pharmaceutically effective amount to a subject who has or is likely to become obese.

As used herein, the term "administration" refers to introducing the pharmaceutical composition of the present invention to a patient in any suitable manner, the route of administration of the composition of the present invention being oral or parenteral as long as it can reach the target tissue. Administration can be via a variety of routes.

Preventive or therapeutic pharmaceutical composition comprising oat bark extract according to the present invention has a low cytotoxicity and shows excellent differentiation inhibitory activity of fat progenitor cells, and has an excellent anti-obesity effect, pharmaceutical composition for preventing or treating obesity, health It can be provided as an active ingredient of nutraceuticals and methods of treatment.

1 is a graph showing the cytotoxicity analysis of oat grains and oat shell extract.
Figure 2 is a graph showing the proliferation inhibiting activity of oocyte proliferation and oat bark extract of fat precursor cells; + differentiation media: differentiation medium added, vesicle: control
Figure 3 is a graph showing the cytotoxicity analysis of oat shell extract by solvent.
Figure 4 is a graph showing the activity of differentiating progenitor cell differentiation of oat shell extract by solvent.
Figure 5 is a graph showing the beta glucan content of ganggang and oat shell extract.
Figure 6 is a graph confirming the activity of differentiating progenitor cells different from the concentration of oat shell extract by the image.
Figure 7 is a graph confirming the activity of differentiating progenitor cells different from the concentration of gangan extract by the image.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, these examples are for illustrating the present invention, and the scope of the present invention is not limited to these examples.

Example 1: Preparation of Oat Shell Extract

2L of spirits are added to 1kg of oat shell (Jeongeup-Gwiri Specialization Project), extracted by stirring for 24 hours at room temperature, filtered with filter paper, and this process is repeated three times, and all the filtrates are collected and concentrated by using a vacuum concentrator. Prepared.

In addition, 2L of hexane was added to 1 kg of oat shell, and extracted by stirring for 24 hours at room temperature, followed by filtration with a filter paper. This process was repeated three times, and all the filtrates were collected and concentrated using a reduced pressure concentrator to prepare hexane extract.

Comparative Example 1: Preparation of Oat Grain Extract

The oat grain extract was prepared in the same manner as in Example 1 by adding a spirit to the oat grains from which the oat shells were removed.

Experimental Example 1. Evaluation of Cytotoxicity of Oat and Oat Shell Extracts

To confirm the safety of the oat extract, the cytotoxicity of the extract against the cells was evaluated.

Specifically, the progenitor cell line 373-L1 (Korean Cell Line Bank, Korea) was counted at 2 × 10 ² cells / well in 96-well plates, and the oats and oat shells at 3, 10, 30, and 100 μg / mL concentrations were divided. After the extracts were treated with the cells and incubated for 24 hours or 72 hours, values were obtained at 500 nm absorbance using a cell counting kit-8 (CCK-8) reagent from Dojindo, and expressed as relative cell viability (%).

As a result, as shown in Figure 1, it was confirmed that the oat grain extract and the oat shell extract did not exhibit cytotoxicity or low cytotoxicity of about 10%.

In addition, in order to confirm the safety of the oat shell extract for each extraction solvent, the cytotoxicity for each extract was confirmed by the same method as Experimental Example 1.

As a result, as shown in FIG. 2, the nucleic acid extract showed low cytotoxicity at 30 μg / mL, and the alcohol extract showed low cytotoxicity at all concentrations.

Experimental Example 2. Analysis of fat formation inhibitory activity of oat and oat shell extract

In order to confirm the therapeutic effect of the obesity, the effects of oat and oat bark extract on the degree of adipocyte differentiation were analyzed.

Specifically, 37% using DMEM (Dulbecco's modified eagle medium) medium containing 10% FBS (Fetal Bobine Serum) and 1% antibiotic (penicillin 100U / mL and streptomycin 0.1mg / mL) was added to the fat precursor cell line 373-L1. Incubated at C ° under CO ₂ (95% air) conditions. Thereafter, 3T3-L1 was differentiated, the medium was removed, washed with PBS (phosphate buffered saline), and the cells were fixed with 10% formaldehyde solution. After washing with PBS again, oil-red-O solution was added and stained at room temperature for 30 minutes, the oil-red-O solution was removed, washed with distilled water, dried and observed under a phase contrast microscope. The cells stained with 100% isopropyl alcohol were lysed and the absorbance was measured at 500 nm.

As a result, as shown in FIG. 3, the oat grain extract had little effect on fat formation, whereas the oat shell extract showed a significant fat formation inhibitory activity from 10 μg / mL.

In addition, as a result of measuring the effect on the degree of adipocyte differentiation of each extract by extraction solvent in the same manner, as shown in Figure 4, the oat shell nucleic acid extract showed a significant inhibitory activity at a concentration of 30 ㎍ / mL or more , Oat bark alcohol extract was found to exhibit a significant level of inhibitory activity at a concentration of 10 ㎍ / mL or more.

Experimental Example 3. Confirmation of the activity of inhibiting fat formation of beta glucan

3-1. Confirmation of Beta Glucan Content in Oat Shell and Magnesium Extract

In order to confirm whether the fat formation inhibitory activity of the oat shell extract was due to beta glucan, the beta glucan content of the oat shell was measured. Beta glucan content was analyzed using the Megazyme β-glucan assay kit using the McCley method. Absorbance was analyzed at 510 nm. As a control group, three types of ganggang were compared and their contents were compared.

As a result, as shown in Figure 5, while the beta glucan content of the gangue is 3 to 4% level, the oat shell was confirmed to be present at 0.09% to confirm that the beta glucan content of the oat shell is very small.

3-2. Confirmation of Fat Formation Inhibitory Activity of Oat Shell and Magnesium Extract

The stained cells were confirmed under a microscope using the same method as in Experimental Example 2.

As a result, as shown in Figs. 6 and 7, oat shell alcohol extract can visually confirm the fat formation inhibitory activity from 10 μg / mL, whereas the gangan extract is 30 μg / mL for the white arachnid ganglia, 100 for the Saegang ganggang. Formation inhibition was shown from μg / mL, and no formation inhibitory activity was found in the saccharic bran.

Taken together, oat shells have very low levels of beta glucan but have excellent fat-forming inhibitory activity. Meggang has high beta glucan content in all three varieties, but does not have good inhibitory activity, and there are differences between varieties. It was confirmed that the beta glucan does not affect the fat formation inhibitory activity.

The experiment of the present invention was confirmed that oat bark alcohol extract has a low cytotoxicity and shows a very good fat formation inhibitory activity. It was also confirmed that the lipid formation inhibitory activity of oat shell alcohol extract was not due to beta glucan.

From the above description, those skilled in the art will appreciate that the present invention can be implemented in other specific forms without changing the technical spirit or essential features. In this regard, the embodiments described above are to be understood in all respects as illustrative and not restrictive. The scope of the present invention should be construed that all changes or modifications derived from the meaning and scope of the following claims and equivalent concepts rather than the detailed description are included in the scope of the present invention.

Claims (7)

A pharmaceutical composition for preventing or treating obesity comprising oat shell extract or a fraction thereof.
The pharmaceutical composition of claim 1, wherein the oat shell comprises an oat grain chamber.
The pharmaceutical composition of claim 1, wherein the oat shell extract is an extract by any one solvent selected from the group consisting of water, C ₁ to C ₁₀ alcohols, hexane, Hexane, and mixtures thereof.
The pharmaceutical composition of claim 3, wherein the solvent is alcohol.
The pharmaceutical composition of claim 1, wherein the composition exhibits an inhibitory effect on adipocyte differentiation.
Obesity prevention or improvement health functional food composition comprising oat shell extract.
A method for preventing or treating obesity, comprising administering oat shell extract to an individual except a human.

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