KR20170116597A - COMPOSITION COMPRISING WATER EXTRACTS FROM pleurotus cornucopiae(paulet) Rolland FOR TREATING OR PREVENTING HYPERLIPIDEMIA - Google Patents

Abstract

More particularly, the present invention relates to a water extract which is effective for the treatment and prevention of hyperlipidemia and which can be used for the treatment and prevention of obesity, as an active ingredient.
The composition comprising the water extract of white mushroom of the present invention as an active ingredient inhibits the activity of pancreatic cholesterol esterase and pancreatic lipase, and can be usefully used for the treatment or prevention of hyperlipemia.

Description

Technical Field [0001] The present invention relates to a composition for treating or preventing hyperlipidemia, which comprises a water-extract of white oyster mushroom, a composition for treating or preventing hyperlipidemia,

The present invention relates to a method for the production of pleurotus cornucopiae (paulet) Rolland) extract, and more particularly, to a composition for treating or preventing hyperlipidemia, which comprises water extract of white mushroom effective for the treatment and prevention of hyperlipidemia.

Hyperlipidemia refers to a disease of high blood fat content. Generally, when total cholesterol is over 240 ㎎ / dl or triglycerides are over 200 ㎎ / dl, it is called hyperlipidemia. Hyperlipidemia is known to be a major cause of hypertension, myocardial infarction, and stroke due to cholesterol blocks the blood vessels and inhibits blood circulation.

BACKGROUND ART In order to prevent or treat hyperlipidemia due to cholesterol, studies have been made on substances that inhibit the absorption of cholesterol. Currently, statin drugs are widely used for the treatment of hyperlipidemia due to inhibition of cholesterol absorption. The drug in this series is an inhibitor of Hmg-CoA reductase and has the effect of inhibiting cholesterol synthesis and lowering blood LDL-cholesterol. In addition, ezetimibe, niacin and fibrate preparations are mainly used. However, there is a possibility that side effects such as myalgia, constipation or digestive disorder and hepatic dysfunction are rarely observed when the drug is administered.

In PCT / KR2012 / 10604, it has been disclosed that the alcohol extract of Pseudomonas aeruginosa can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipidemia.

In PCT / KR2012 / 10612, it has been disclosed that the water extract of red mulberry can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipemia.

In PCT / KR2012 / 10550, it has been disclosed that the alcohol extract of the flower shield mushroom can inhibit the activity of pancreatic cholesterol ester raise and lower the absorption of cholesterol, thereby being used as a composition for treating and preventing hyperlipidemia.

On the other hand, in order to treat and prevent hyperlipidemia due to triglyceride, studies have been made on drugs having a mechanism of action that acts on digestive enzymes and inhibits the absorption of fat.

Xenical ^TM (orlistat) is well known as a typical drug. It inhibits the activity of TGL by covalent bonding with serine, which is the active site of triglyceride lipase (TGL), and prevents fat from being degraded and absorbed .

Development of a specific egg yolk antibody against the pancreatic lipase domain for inhibition of obesity Kor . J. Microbiol . Biotechnol . Vol. 36, No. 4, 299 ~ 306 (2008) proposes a method of inhibiting the absorption of fat by inhibiting the activity of pancreatic lipase using a specific egg yolk antibody.

In PCT / KR2012 / 10558, it has been disclosed that the alcohol extract of yellow vanda mushroom can be used as a composition for treating and preventing obesity by inhibiting the activity of pancreatic lipase.

In PCT / KR2012 / 10602, it has been disclosed that water extract of Chrysanthemum morbus Mushroom can be used as a composition for treating and preventing obesity by inhibiting the activity of pancreatic lipase.

On the other hand, in PCT / KR2012 / 10621, water extract of acacia mushroom suppresses the activity of pancreatic lipase and the activity of raising pancreatic cholesterol ester, and it is known that it can inhibit fat absorption.

However, there is a continuing need for a new mushroom water extract that can effectively prevent the hyperlipemia and obesity by inhibiting the absorption of fat and cholesterol.

A problem to be solved by the present invention is to provide a new water extract of mushroom which shows little side-effects in vivo and can inhibit absorption of fat and cholesterol.

Another object of the present invention is to provide a new water extract of mushroom which can inhibit the activity of raising pancreatic cholesterol ester and the activity of pancreatic lipase.

A problem to be solved by the present invention is to provide a composition capable of inhibiting the absorption of fat and cholesterol and treating or preventing hyperlipidemia.

In order to accomplish the above object, the present invention provides a composition for treating or preventing hyperlipidemia comprising water extract of white mushroom as an active ingredient.

The present invention provides a medicament for the treatment or prevention of hyperlipidemia, which comprises water extract of white mushroom as an active ingredient.

The present invention provides a method for treating or preventing hyperlipidemia, comprising the step of administering an aqueous extract of white mushroom to an animal.

The present invention provides a health functional food for improving or preventing a hyperlipidemia comprising an aqueous extract of white mushroom as an active ingredient.

In addition, the present invention provides a composition for inhibiting the activity of raising pancreatic cholesterol ester comprising water extract of white oyster mushroom as an active ingredient.

The present invention provides a medicament for inhibiting the activity of raising pancreatic cholesterol ester comprising a water extract of white mushroom as an active ingredient.

The present invention provides a method for inhibiting the activity of a pancreatic cholesterol esterase, comprising the step of administering an aqueous extract of white mushroom to an animal.

The present invention provides a health functional food for inhibiting the activity of raising pancreatic cholesterol ester comprising water extract of white mushroom as an active ingredient.

In addition, the present invention provides a composition for inhibiting the activity of pancreatic lipase comprising water extract of white mushroom as an active ingredient.

The present invention provides a medicament for inhibiting the activity of pancreatic lipase comprising water extract of white mushroom as an active ingredient.

The present invention provides a method for inhibiting the activity of pancreatic lipase comprising the step of administering an aqueous extract of white mushroom to an animal.

The present invention provides a health functional food for inhibiting the activity of pancreatic lipase comprising water extract of white mushroom as an active ingredient.

In addition, the present invention can be used as a composition for prevention and treatment of obesity by inhibiting the absorption of fat by inhibiting the activity of pancreatic lipase in white oyster mushroom.

In the present invention, the extract of white mushroom, especially water of white mushroom, lowers the activity of pancreatic cholesterol ester raise and effectively inhibits the activity of pancreatic lipase, which is triglyceride lipase (TGL) Can replace drugs that treat or prevent hyperlipemia.

In the present invention, the weight or weight of the mushroom is understood to refer to the weight or weight of the dried mushroom unless otherwise noted.

On the other hand, the water extract of white mushroom as described above may be prepared according to a conventional method for producing a plant extract. Preferably, the white rot fungus is dried and ground, and then the residue is removed. Then, 0.1 to 20 g of the pulverized product per 100 ml of water is added, and most preferably, 1 to 5 g of pulverized product per 100 ml of water is added, will be. When the content of ground white mushroom ground water is too small as compared with that of water, the effect of the active ingredient of white mushroom is not sufficient, and when the amount of water is excessively large relative to the amount of water, The cost is increased, which is not preferable from the viewpoint of productivity.

At this time, the extraction conditions are preferably a mixture of white mushroom with water as an extraction solvent, and then cooled at a temperature of 20 to 60 DEG C for 12 to 36 hours, most preferably at a temperature of 30 to 40 DEG C for 20 to 24 hours .

When extracting at a temperature lower than the above temperature, it takes a long time to extract the active ingredient, and when extracting at a temperature higher than the above temperature, the activity of the active ingredient is deteriorated.

When the extraction time is shorter than the above range, the concentration of the active ingredient to be extracted is low, and when the extraction is performed for a longer time than the above, not.

The water extract of white mushroom extracted by the above method is filtered through a filter cloth, etc., and the filtrate is centrifuged to remove the precipitate. The filtrate can be concentrated or concentrated under reduced pressure, followed by lyophilization.

On the other hand, the content of the water extract of white mushroom as an active ingredient in the composition for treating or preventing obesity and hyperlipidemia in the above-mentioned embodiment is not limited, but may be preferably 0.001 to 50% by weight. When the content of the water extract of white mushroom as an active ingredient is less than 0.001% by weight, digestion and absorption of the fat in the body are insignificant. When the content is more than 50% by weight, the effect of increasing the inhibitory activity is insignificant, It is not economical. More preferably, the content of the water extract of white mushroom in the composition may be 0.01 to 50% by weight, and most preferably 0.1 to 30% by weight.

The present invention provides a medicament for the treatment or prevention of hyperlipidemia or obesity comprising the water extract of white mushroom contained in the composition as an active ingredient according to an embodiment. Such a medicament containing the water extract of white mushroom as an active ingredient may further contain suitable carriers, excipients and diluents conventionally used in the production thereof.

Examples of carriers, excipients and diluents that can be contained in pharmaceuticals containing the water extract of white mushroom of the present invention as an active ingredient include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, Alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil .

Each of the medicines containing the water extract of white mushroom of the present invention as an active ingredient may be used as oral formulations such as powders, granules, tablets, suspensions, emulsions and syrups according to a conventional method.

The oral formulations are meant to include solid and liquid formulations for oral administration and solid formulations for oral administration may include tablets, pills, powders, granules, capsules and the like, For example, starch, calcium carbonate, sucrose or lactose, gelatin and the like in combination with at least one excipient. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral use include suspensions, solutions, emulsions, and syrups. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, have.

The preferred dosage of the composition containing the water extract of white fungus mushroom of the present invention varies depending on the condition and body weight, the degree of disease, the type of drug, the route of administration and the period of time, but can be appropriately selected by those skilled in the art. Preferably, the medicinal product containing the water extract of white mushroom of the present invention as an active ingredient is 0.0001 to 100 mg / kg per day based on the amount of water extract of white mushroom, preferably 0.01 to 10 mg / kg. < / RTI > The administration may be carried out once a day or divided into several doses. The dose and the number of administrations do not limit the scope of the present invention in any aspect.

According to another embodiment of the present invention, there is provided a health functional food for improving or preventing hyperlipidemia or obesity comprising water extract of white mushroom as an active ingredient. Herein, the term "health functional food" means a natural product or a processed product containing one or more nutrients, preferably a state of being able to be directly eaten through a certain processing step.

Examples of the health functional food to which the water extract of white fungus mushroom of the present invention can be added include various foods, beverages, gum, tea, and vitamin complex. In addition, in the present invention, the food may contain special nutritional foods (eg, crude oil, infant formula, etc.), meat products, fish products, tofu, mackerel, noodles (eg, (Such as soy sauce, soybean paste, hot pepper paste, mixed sauce), sauces, confectionery (eg snacks), dairy products (eg fermented milk, cheese), other processed foods, kimchi, pickled foods (For example, fruits and vegetables, beverages, fermented beverages, etc.), natural seasonings (eg, ramen soup, etc.). The food, beverage or food additive may be prepared by a conventional production method.

In the present specification, the functional food refers to a food group which is imparted with added value to function and express the function of the food by using physical, biochemical, biotechnological techniques, etc., Means a food which is processed and designed so that the body control function related to restoration and the like is sufficiently expressed to the living body. The functional food may include a food-acceptable food-aid additive, and may further comprise suitable carriers, excipients and diluents conventionally used in the production of functional foods.

In the present specification, beverage means a generic term for drinking or enjoying a taste and is intended to include a functional beverage. The above-mentioned beverage has no particular limitation on the ingredients other than the above-mentioned water extract of white mushroom as an active ingredient as an essential ingredient at the indicated ratio, and may contain various flavors or natural carbohydrates as an additional ingredient can do. Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and Xylitol, sorbitol, and erythritol. Natural flavors (tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate may be generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the composition of the present invention. In addition, the composition of the present invention may be used for natural fruit juice, fruit juice drink, And may further contain flesh for manufacture.

In addition to the above, the health functional food of the present invention may contain various kinds of nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, colorants and heavies (cheese, chocolate etc.), pectic acid and its salts, And salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like. These components can be used independently or in combination. The ratio of such additives is not so critical, but may be selected in the range of 0 to 20 parts by weight per 100 parts by weight of the water extract of white mushroom of the present invention.

In the present specification, functional beverages are used to control the bio-defense rhythm of the beverage group or beverage composition to which the added value is imparted so that the function of the beverage functions for a specific purpose by using physical, biochemical, biotechnological techniques, Means a beverage which has been designed so that the body control function related to restoration and the like is sufficiently expressed in the living body.

The functional beverage is not particularly limited to the other components other than the water extract of white mushroom of the present invention as an essential ingredient in the indicated ratios and may contain various flavors or natural carbohydrates as an additional ingredient . Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and xylitol , Sorbitol, and erythritol. Natural flavors (tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate is generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the composition of the present invention.

In addition, in a health functional food for the purpose of improving or preventing hyperlipidemia or obesity, the amount of the extract may be 0.01 to 15% by weight of the total food, and the beverage composition may contain 0.02 to 5 g , Preferably 0.3 to 1 g.

According to another embodiment of the present invention, there is provided a method for preparing a water extract of white mushroom as described above.

According to an embodiment of the present invention, there is provided a method for preparing a water extract of white mushroom, comprising the steps of preparing white mushroom, mixing the white mushroom with an alcohol or water having 1 to 10 carbon atoms, And extracting for 12 to 36 hours at a temperature of 20 to 60 DEG C, and each extract is evaluated.

Meanwhile, in the case of producing the alcohol or water extract of white mushroom according to the above-described embodiment, when the extract is extracted with such an extraction solvent, the extracted extract has an effect of inhibiting digestion and absorption of cholesterol and inhibiting digestion and absorption of fat And the effect of decreasing the cholesterol and fat absorption from the digestive tract to blood was significantly different. The specific extraction time, extraction temperature, mixing ratio of white mushroom and extraction solvent and the like are different from those described above.

The composition comprising the water extract of white oyster mushroom according to the present invention as an active ingredient at a low temperature of 30 to 40 DEG C remarkably inhibits the activity of pancreatic cholesterol esterase and pancreatic lipase and is useful for the digestion and absorption of cholesterol, And thus can be usefully used for the treatment or prevention of hyperlipemia and for the treatment or prophylaxis of obesity.

BRIEF DESCRIPTION OF THE DRAWINGS Fig. 1 is a graph showing the inhibitory activity of pancreatic cholesterol ester-raising of water extract of Pleurotus ostreatus according to the present invention in comparison with a control.
FIG. 2 is a graph showing the inhibitory activity of pancreatic lipase activity of the water extract of white fungus mushroom of the present invention compared with a control.
FIG. 3 is a graph showing neutral lipid absorption inhibition measured by the water extract of white mushroom of the present invention. FIG.
Fig. 4 is a graph showing the distribution cornucopiae (paulet) Rolland).

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, the structure and effects of the present invention will be described in detail with reference to specific embodiments of the present invention. It should be understood, however, that the following examples are provided for a better understanding of the invention and are not to be construed as limiting the scope of the invention.

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

Example : Invention White mushroom  Water extract preparation

50 ml of water as an extraction solvent was mixed with 2 g of pleurotus cornucopiae (paulet) Rolland powder shown in FIG. 4, which was provided by the Forest Environment Research Institute of Gyeongsangbuk-do, and the mixture was placed in a shaking incubator at 37 ° C for 24 hours to extract Respectively. The supernatant of the shaking incubator was centrifuged at 2500 rpm for 10 minutes, and the water extract of white mushroom was collected and stored at -20 ° C.

Experimental Example:

1. Measurement of Pancreatic Cholesterol Ester Raise Activity of White Oyster Water Extract of the Present Invention

Pancreatic cholesterol esterase plays a role in recognizing acyl chain-bearing substrates as non-specific and isolating acyl chains. To measure the pancreatic cholesterol ester raising activity by the white oyster mushroom water extract of the Example, a poison flinic acid cholesterol ester raise made by Sigma chemical was used as an enzyme. The pancreatic cholesterol esterase cleaved the chromogenic substrate (p-nirophenylbutyrate), and the activity of the enzyme was confirmed by the color reaction. The inhibitory effect of the enzyme was measured by the change of absorbance at 405 nm using a microplate reader and calculated as% based on the absorbance at 405 nm of the untreated group of white mushroom water extract.

As a result, it was confirmed that the water extract of White oyster mushroom reduced pancreatic cholesterol ester raising activity in a concentration-dependent manner. The results are briefly shown in Fig.

2. Measurement and Results of Pancreatic Lipase Activity by Water Extract of White Oyster Mushroom of the Invention

Pancreatic lipase plays a role in recognizing acyl chain-bearing substrates nonspecifically and isolating acyl chains. Porcine pancreatic lipase type 2 (Sigma chemical, Type II, manufactured by Sigma Chemical Co., Ltd.) was used as an enzyme to measure the pancreatic lipase activity by the white oyster mushroom water extract. Using pancreatic lipase's ability to decompose chromo-genic substrate (p-nirophenylbutyrate), the activity of the enzyme was confirmed through color development. The inhibitory effect of the enzyme was measured by the change of absorbance at 405 nm using a microplate reader and calculated as% based on the absorbance at 405 nm of the untreated group of white mushroom water extract.

The activity of the enzyme was determined by the water extract of white oyster mushroom. As a result, the pancreatic lipase activity of the white mushroom water extract of the Example was decreased in a concentration-dependent manner. The results are briefly shown in Fig.

3. Measurement of neutral fat absorption inhibition by white oyster mushroom water extract of the present invention

Plasma triglyceride was measured to determine whether the water extract of white mushroom extract of the Example showing inhibitory effect on pancreatic lipase activity was also effective at the individual level. A 0.5 ml oral fat suspension was orally administered to 8-week-old Balb / c mice (male, body weight ~ 25 g) fasted for 16 hours. The fat suspension consisted of 30% olive oil, 0.5% (w / v) carboxymethylcellulose sodium (CMC-Na) and 1% (v / v) Tween 80, 100 mg (4 g / kg) was added. After 2 hours, mouse blood was collected and centrifuged at 3000 rpm for 15 minutes at 4 ° C. The amount of triacylglycerol in the serum was measured using a serum triglyceride determination kit (Sigma). As a result, it was confirmed that the white oyster mushroom water extract of the Example lowered the neutral fat absorption. The results are briefly shown in Fig.

Preparation: The present invention white oyster mushroom (pleurotus cornucopiae (paulet) Rolland) Water extract formulation

Production Example 1. Preparation of powder

White oyster mushroom water extract powder 20 ㎎, lactose 100 ㎎, talc 10 ㎎.

The above ingredients were mixed and filled in an airtight container to prepare powders.

Production Example 2. Preparation of tablets

White oyster mushroom water extract 10 mg, corn starch 100 mg, lactose 100 mg, magnesium stearate 2 mg.

After mixing the above components, tablets were prepared by tableting according to the usual preparation method of tablets.

Production Example 3. Preparation of capsules

10 mg of white mushroom water extract powder, 3 mg of crystalline cellulose, 14.8 mg of lactose and 0.2 mg of magnesium stearate.

The above components were mixed according to a conventional capsule preparation method and filled in gelatin capsules to prepare capsules.

Production Example 4. Production of liquid agent

20 ㎎ of water extract powder of white mushroom, 10 g of isomerized sugar, 5 g of mannitol, and purified water.

Each component was added to purified water in accordance with the usual liquid preparation method and dissolved, and the lemon flavor was added in an appropriate amount. Then, the above components were mixed, and purified water was added thereto. The whole was adjusted to 100 ml with purified water, And sterilized to prepare a liquid preparation.

Production Example 5. Production of Health Food

Vitamin B acetate, Vitamin B, Vitamin B, Vitamin B, Vitamin B, Vitamin A, Vitamin B, Vitamin B, Vitamin B, Vitamin B, 10 mg of nicotinic acid amide, 1.7 mg of nicotinic acid amide, 50 mg of folic acid, 0.5 mg of calcium pantothenate, 1.75 mg of ferrous sulfate, 0.82 mg of zinc oxide, 25.3 mg of magnesium carbonate, 15 mg of potassium phosphate monobasic Mg of potassium citrate, 90 mg of potassium citrate, 100 mg of calcium carbonate, and 24.8 mg of magnesium chloride.

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

Claims (9)

White mushroom ( pleurotus cornucopiae (paulet) Rolland) is extracted at a temperature of 20 to 60 ° C for 12 to 36 hours to obtain a water extract of White Pleurotus ostreatus. The method according to claim 1, wherein the water extract is prepared by mixing 0.1 to 20 g of white mushroom per 100 mL of water. A water extract of white oyster mushroom prepared according to the method of claim 1. The composition according to claim 3, wherein the composition comprises 0.001 to 50% by weight of the water extract of white mushroom. 5. The composition of claim 4, wherein the composition is a formulation of any one of an acid, a granule, a tablet, a suspension, an emulsion or a syrup. A health functional food composition for improving or preventing hyperlipidemia, which comprises the water extract of white mushroom of claim 3. The food composition according to claim 6, wherein the food composition is at least one selected from the group consisting of gum, tea, vitamin complex, preparation oil, infant formula, processed food, processed fish meat, tofu, mushrooms, ramen noodles, soy sauce, miso, , Kimchi, pickles, beverages, and natural seasonings. A pharmaceutical composition for treating or preventing hyperlipidemia, which comprises the water extract of white mushroom of claim 3 as an active ingredient. A method for treating or preventing hyperlipidemia, comprising administering the water extract of white mushroom of claim 3 to an animal other than human.

Images