KR20190119736A - Composition for improving lipid metabolism compsing shepherd's purse extracts and extracts of flower bud of kobus magnolia as an active ingredient - Google Patents

Abstract

The present specification discloses a composition for improving lipid metabolism containing a Capsella bursa-pastoris extract and a Magnoliae flos extract as active components. The composition, which is an aspect of the present invention can inhibit the accumulation of lipids such as cholesterol in cells and can increase a high-density lipoprotein (HDL) value in the blood, thereby being able to effectively improve lipid metabolism in the body. In addition, the composition is non-toxic to the human body to ensure human stability, thereby being able to be widely used in various fields, for example the food field or the pharmaceutical field.

Description

COMPOSITION FOR IMPROVING LIPID METABOLISM COMPSING SHEPHERD'S PURSE EXTRACTS AND EXTRACTS OF FLOWER BUD OF KOBUS MAGNOLIA AS AN ACTIVE INGREDIENT}

Disclosed herein is a composition for improving lipid metabolism comprising a extract of horseradish and sinyi extract as an active ingredient.

Cholesterol is an essential component of cells and plays an important role in cell growth, differentiation and development. However, when blood cholesterol levels are higher than the standard, macrophages, foam cells, and the like are formed and deposited on the walls of blood vessels, and plaques are formed, thereby causing arteriosclerosis, which inhibits blood circulation. Continued accumulation of cholesterol eventually closes the arteries and leads to serious cardiovascular diseases such as various heart diseases and angina pectoris.

Therefore, as a therapeutic agent for atherosclerosis, statins, which are substances capable of inhibiting the activity of HMG-CoA reductase, an important enzyme involved in the synthesis of cholesterol, or lowering low density lipoprotein (LDL) Drugs have been developed and widely used. However, these drugs are at the limit because of the low cases of LDL lipoproteins and the reported onset of atherosclerosis, various complications and side effects.

On the other hand, high density lipoprotein (HDL) is known to play an important role in the back transport of cholesterol transported from each tissue to the liver, adrenal glands and hormone-producing organs, and can prevent atherosclerosis. Efforts are being made to develop lipid metabolism improvers.

KR 10-1462326 B1

In one aspect, an object of the present invention is to improve lipid metabolism in the body.

In one aspect, an object of the present invention is to improve lipid metabolism in the body by a different route than cholesterol synthesis inhibitors.

In one aspect, an object of the present invention is to promote reverse cholesterol transport (RCT).

In one aspect, it is an object of the present invention to provide a composition that can effectively improve lipid metabolism in the body when used in combination with a cholesterol synthesis inhibitor.

In one aspect, an object of the present invention is to maximize the physiological activity inherent in each of the extract and Sinyi extract.

In order to achieve the above object, the present invention provides a composition for improving lipid metabolism comprising, in one aspect, extracts and extract of Sinai as an active ingredient.

The composition containing the extract of the cold and the extract of the present invention as an active ingredient, which is an aspect of the present invention, can suppress the accumulation of lipids such as cholesterol in the cells, and through the back transport, it is possible to increase the high density lipoprotein (HDL) levels in the blood It can effectively improve lipid metabolism in the body. In addition, since the composition is non-toxic to the human body to ensure human stability, it can be widely used in various fields, for example, the food field or the pharmaceutical field.

1 is a result showing the cholesterol back-transportation effect when treated with the leaf extract (N-leaf (wa): water extract of horseradish leaf, N-leaf (Et): ethanol extract of horseradish leaf).
2 is a result showing the cholesterol back-transportation effect when treated with the extract of radish root (N-root (wa): radish root water extract, N-root (Et): radish root ethanol extract).
Figure 3 is a result showing the result of cholesterol reverse transport effect when treated with a mixture of Sinyi extract, Sinyi extract and wasabi extract (S: Sinyi water extract, N + S: Wasabi leaf water extract + Sinyi water extract).

Hereinafter, the present invention will be described in detail.

The present invention, in one aspect, is a composition for improving lipid metabolism, including the extract and Sinyi extract as an active ingredient.

The " capsella bursa-pastoris " is a biennial herb of cruciferous plants, a wasteland plant that grows well in rough lands, and flowers and seeds in May-June. The leaves from the roots round together. The leaves are 10 cm or more in length and are two idols (large-headed feathers) with dull toothed teeth on the leaves. Root leaves cluster together and leaf sequence of flower leaves is displaced. Foliage is lanceolate (small, long, needle-like), smaller as it goes up. The flower is white and the fruit is a flat triangular triangular shape with an angled fruit enclosed by hard picks. It is native to Eastern Europe and Asia Minor, but grows all over the world. Wasabi was used for food, all seeds, leaves, and roots.

In the present specification, the wasabi extract may include an extract of leaves, roots or outposts of wasabi.

"Shinyi" may mean a bud of magnolia and plants.

In the present specification, "extract" includes all materials obtained by extracting the components of natural products, regardless of the extraction method, extraction solvent, extracted components or the form of the extract, and after extracting the materials obtained by extracting the components of natural products It is a broad concept including all materials that can be obtained by processing or processing in other ways, specifically, the processing or treatment may be to further ferment or enzymatically extract. Therefore, in the present specification, the extract is a broad concept including fermentation, concentrate, and dry matter, and specifically, the extract herein may include an extract of fermentation.

In such aspects, the lipid metabolism improvement may include inhibiting intracellular lipid accumulation, or promoting extracellular release of intracellular lipids; Increase in high density lipoprotein (HDL) -cholesterol in the blood; And a decrease in low density lipoprotein (LDL) -cholesterol in the blood.

The HDL-cholesterol and HDL-cholesterol may mean a complex (conjugate) of cholesterol of HDL and LDL, respectively.

The lipid metabolism involves the delivery of lipids produced in the liver to each tissue, or vice versa.

Specifically, LDL is involved in the delivery of lipids produced by the liver to each tissue, and HDL is involved in the transfer of lipids from each tissue to the liver.

Promoting extracellular excretion of the intracellular lipids may mean, for example, cholesterol transport back. The cholesterol back transport may refer to a route for transporting cholesterol from peripheral tissues (cells) to the liver using HDL as a medium.

Specifically, reverse cholesterol transport may refer to a process of receiving phospholipids and cholesterol from peripheral cells and transporting them directly to the liver or indirectly by delivering them to very low density lipoprotein (VLDL) and LDL residues. Apolipoprotein A1 produced in the liver or intestine receives phospholipids through ABC-A1 (ATP-binding cassette transporter A1) to form nascent HDL in the form of a bilayer disc. It receives excess free cholesterol from peripheral tissues, and the free cholesterol is esterified by lecithin-cholesterol acyl transferase (LCAT) to be converted into cholesterol esters and moved to the center. HDL transfers cholesterol esters (CE) to the chylomicrons or VLDL residues through the cholesterol ester transfer protein (CETP) in the blood, and these are exchanged to obtain triglycerides. Eventually, in the liver or in tissues that require cholesterol, it binds to HDL receptors (cleaning receptor B1) to deliver cholesterol and apolipoprotein A1 is reused or metabolized in the kidneys.

In the aspect as described above, the extract of cold and extract extract of the composition may be included in a weight ratio of 50 ~ 150: 50 ~ 150. Preferably, the extract of horseradish and sinyi extract, in the order of weight ratio of 80 ~ 120: 80 ~ 120, more preferably, may be included in the weight ratio of 90 ~ 110: 90 ~ 110.

The wasabi extract and sinyi extract may be included in 0.1 to 90% by weight based on the total weight of the composition. Wasabi extract and Sinyi extract, within the content range, may be included in the content ratio.

In the above aspect, the extracting solvent of the extract may include water, an organic solvent or an organic solvent aqueous solution.

The organic solvent may be hexane, methylene chloride, alcohol, or the like as the organic solvent, but is not limited thereto. In the above, water includes distilled water or purified water, and the organic solvent is a group consisting of alcohol, acetone, ether, ethyl acetate, diethyl ether, methanol, ethyl methyl ketone, and chloroform, for example, a lower alcohol having ₁ to ₅ carbon atoms. Including but not limited to one or more selected from.

When the extraction solvent is water, heat extraction, cold extraction, reflux cooling extraction, or ultrasonic extraction may be used, and preferably may be warm extraction, preferably about 40 to 120 ℃, more preferably about Extraction may be performed at a temperature of 70 ° C., but is not limited thereto. Extraction time may preferably be performed for about 1 to 4 hours, more preferably about 2 to 3 hours, but is not limited thereto.

In one embodiment, the organic solvent may be an alcohol, the alcohol may be ethanol.

The radish extract and / or acid extract may yield a result with better activity than when ethanol is used when water is used as the extraction solvent.

In one aspect, the lipid may comprise cholesterol.

In one aspect, the composition may be a composition for preventing or improving various circulatory diseases. For example, it may be used as a composition for preventing or improving cardiovascular diseases, specifically, atherosclerosis, arteriosclerosis, senile sclerosis, hyperlipidemia, angina pectoris, myocardial infarction, arteriosclerosis, ischemic stroke, ischemic heart disease, and the like.

 In one aspect, the composition may be a pharmaceutical composition, a food composition or a cosmetic composition.

The compositions of the present invention can be prepared in pharmaceutical formulations according to conventional methods. In the preparation of the formulation, it is preferred that the active ingredient is mixed or diluted with the carrier or enclosed in a carrier in the form of a container. When the carrier is used as a diluent, it may be a solid, semisolid or liquid substance which acts as a carrier, excipient or medium for the active ingredient. Thus, the formulation may be in the form of tablets, pills, powders, sachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, soft or hard gelatin capsules, sterile injectables, sterile powders and the like.

Examples of suitable carriers, excipients and diluents include lactose, dextrose, sucrose, sorbitol, mannitol, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propyl Hydroxybenzoate, talc, magnesium stearate and mineral oil. The formulation may further comprise fillers, anti-coagulants, lubricants, wetting agents, fragrances, emulsifiers, preservatives and the like. Compositions of the present invention may be formulated using methods well known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to a mammal.

The pharmaceutical composition of the present invention may be administered through several routes including oral, transdermal, subcutaneous, intravenous, abdominal, muscle, topical application, patch and iontophoresis, of which topical application and oral administration are preferred. Do.

In humans, a typical daily dosage of the composition may range from 1 to 100 mg / kg body weight, preferably 5 to 70 mg / kg body weight, and may be administered once or in several doses. However, it is to be understood that the actual dosage of the composition should be determined in light of several relevant factors such as the disease to be treated, the route of administration, the age, sex and weight of the patient, and the severity of the disease, and therefore the dosage may be determined in some way. Nor does it limit the scope of the invention.

The food composition may include a health functional food. Health functional foods are manufactured by using nutrients or ingredients (functional ingredients) that are useful for the human body, which are easily deficient in daily meals, and maintain and improve health by maintaining normal functions of the human body or activating physiological functions. It may mean a food, but is not limited thereto. The health food may be manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, and the like, but is not limited thereto and may be manufactured and processed in any form according to the law.

The mixed amount of the active ingredient may be suitably determined depending on the purpose of use (prevention, health or therapeutic treatment). In general, each of the extracts of the present invention is added in an amount of 15% by weight or less, preferably 10% by weight or less, based on the raw materials, in the manufacture of food or beverage. However, in the case of long-term intake for health and hygiene or health control purposes, the amount may be below the above range, and the active ingredient may be used in an amount above the above range because there is no problem in terms of safety.

There is no particular limitation on the kind of food. Examples of the food to which the extract of the present invention may be added include dairy products including meat, sausage, bread, chocolate, candy, snacks, confectionary, pizza, ramen, other noodles, gum, ice cream, various soups, drinks, tea, Drink agents, alcoholic beverages and vitamin complexes, and the like, and include all healthy foods in the conventional sense.

In addition to the above, the extract of the present invention contains various nutrients, vitamins, electrolytes, flavoring agents, coloring agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonic acid. Carbonating agents and the like used in beverages.

Specifically, the cosmetic composition may include, for example, a hair cosmetic, a body cosmetic, a basic cosmetic, a makeup cosmetic, and the like, and its formulation is not particularly limited and may be appropriately selected as desired.

For example, the cosmetic composition is formulated into solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, sprays, and the like. It may be, but is not limited thereto. More specifically, hair cosmetics such as shampoo, conditioner, hair cleanser, hair tonic, gel or mousse, hair cosmetic composition such as wool or hair dye, softening lotion, nourishing lotion, lotion, body lotion, nourishing cream, Basic cosmetics such as massage cream, moisture cream, hand cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, gel, patch, oil-in-water (O / W), water-in-oil (O / W) It can be formulated as.

The cosmetic composition contains a cosmetically acceptable medium or base. These are all formulations suitable for topical application, for example emulsions, suspensions, microemulsions, microcapsules, microgranules or ionic (liposomes) obtained by dispersing an oil phase in a solution, gel, solid or pasty anhydrous product, aqueous phase, and / or It may be provided in the form of a nonionic vesicle dispersant or in the form of a cream, skin, lotion, powder, ointment, spray or cone stick. These compositions can be prepared according to conventional methods in the art.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a paste, cream or gel, animal oils, vegetable oils, waxes, paraffins, starches, trachants, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide may be used as carrier components. Can be.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, in particular in the case of a spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

In one embodiment of the present invention, the cosmetic composition may further contain a thickener. The thickener included in the cosmetic composition of the present invention is methyl cellulose, carboxy methyl cellulose, carboxy methyl hydroxy guanine, hydroxy methyl cellulose, hydroxyethyl cellulose, carboxy vinyl polymer, polyquaternium, cetearyl alcohol, stearic acid, Carrageenan and the like can be used, and preferably, at least one of carboxy methyl cellulose, carboxy vinyl polymer and polyquaternium can be used, and most preferably, carboxy vinyl polymer.

In one embodiment of the present invention, the cosmetic composition may contain a variety of suitable bases and additives as necessary, the type and amount of these components can be easily selected by the inventors. If necessary, it may contain an acceptable additive, for example, may further include components such as preservatives, pigments, additives and the like conventional in the art.

Hereinafter, the present invention will be described in more detail with reference to the following Examples and Experimental Examples. However, these Examples and Experimental Examples are provided only for the purpose of illustration to help the understanding of the present invention is not limited to the scope and scope of the present invention by the following examples.

[Production example]

Preparation Example 1 Preparation of Wasabi Leaf and Wasabi Root Hot Water Extract

After drying the dried leaves and roots of horseradish, 30 g of the powder obtained by grinding was put in 600 g of purified water and left at 70 ° C. for 2 hours, and then filtered to a nonwoven fabric having a hole of 6 μm. The filtered solution is concentrated at 65 ° C. at 140 rpm. The concentrate was prepared as a powder using a lyophilization method.

Preparation Example 2 Preparation of Wasabi Leaf and Wasabi Root Ethanol Extract

After drying the dried leaves or roots of corn, 30 g of the powder obtained by grinding was put in 600 g of 30% ethanol and left at 60 ° C. for 2 hours, and then filtered to a nonwoven fabric having a hole of 6 μm. The filtered solution is concentrated at 75 ° C. at 140 rpm. The concentrate was prepared as a powder using a lyophilization method.

Preparation Example 3 Preparation of Sinyi Hydrothermal Extract

After drying the thinner, 30 g of the powder obtained by grinding was put in 600 g of purified water and left at 70 ° C. for 2 hours, and then filtered to a nonwoven fabric having a hole of 6 μm. The filtered solution is concentrated at 65 ° C. at 140 rpm. The concentrate was prepared as a powder using a lyophilization method.

Experimental Example 1 Confirmation of Cholesterol Reverse Transport Effect of Radish Extract

In experiments, J774.1 cells, macrophage cell lines, were used to represent peripheral tissues. The cells were treated with horseradish extract to measure the lipid-improving effect through the ratio of how much cholesterol was released from the cells. That is, the cholesterol released from the macrophage cells were combined with HDL, so the ratio of HDL increased.

The experiment was carried out using Biohole Cholesterol Efflux Fluometirc Assay kit. This kit contains fluorescence-labeled cholesterol so that the fluorescent marker cholesterol can be added into the cells when culturing macrophage cells, and then the extracellular fluorescence cholesterol is extracted with HDL when treated with cold extract. It is supposed to measure.

1) The J774.1 cells were cultured in RPMI1640 medium, and the cells were divided into 96-well plates with about 100,000 cells per well.

2) The fluorescently labeled cholesterol was added to the cells and cultured for 16 hours.

3) After changing the medium of the cells, the extract was put in RPMI medium by the corresponding concentration and incubated for 4 hours.

4) Human serum was put into the cholesterol receptor discharged to the medium. It contains HDL protein, which allows cholesterol to be released from cells.

5) The amount of cholesterol released into the medium and the amount of cholesterol remaining in the cells was measured using a fluorophotometer. For reference, the fluorescent material is a material that emits fluorescent light of 515nm wavelength while being activated and stabilized at 482nm.

6) The amount of cholesterol efflux was measured by calculating the ratio of the amount of fluorescence emitted to the medium among the total amount of fluorescence.

<Wheat leaf extract>

When only 50% DMSO solvent in which the extract was dissolved was added, less than about 60% of cholesterol secretion occurred. In the case of a positive standard in the kit, cholesterol secretion was increased by about 5% to 7% compared to the DMSO-treated cells, and less than 20% when the human serum was not put into the receptor. Low cholesterol secretion was identified. In the case of treatment of the extract was observed that up to 80% cholesterol secretion occurred in the water extract. Wasabi extract extracted with ethanol was lower than water extract but showed higher cholesterol secretion promoting ability than the positive standard (FIG. 1).

<Wheat root extract>

Similar results were obtained in the case of wasabi root extract. When the water extract was treated to about 10μg / ml, it was confirmed that higher cholesterol secretion occurred than the group treated with the positive standard. Ethanol extract was lower than water extract, but promoted higher cholesterol secretion than positive standard (FIG. 2).

Experimental Example 2 Confirmation of Cholesterol Reverse Transport Effect of Sinyi Extract

In the same manner as in Experimental Example 1, it was confirmed that the cholesterol back-transporting effect also for the extract of Sinyi.

As a result, when treated to about 10μg / ml, it was confirmed that higher cholesterol secretion occurred than the group treated with a positive standard material (Fig. 3).

Experimental Example 3 Confirmation of Cholesterol Reverse Transport Effect of Wasabi Extract and Sinyi Extract Mixture

Wasabi leaf extract and Sinyi water extract was mixed in the same amount (5μg) to confirm the cholesterol transport back effect in the same manner as above.

As a result, it was confirmed that the cholesterol secretion effect was improved by about 120% or more compared with the case of treating the cold and shin each, and the synergistic effect on the cholesterol back-transport effect according to the combined use was confirmed.

Claims (7)

A composition for improving lipid metabolism comprising a extract of horseradish and sinyi as an active ingredient. The method of claim 1,
The lipid metabolism improvement,
Inhibit intracellular lipid accumulation, or promote extracellular excretion of intracellular lipids;
Increase in high density lipoprotein (HDL) -cholesterol in the blood; And
A composition for improving lipid metabolism comprising at least one selected from the group consisting of low density lipoprotein (LDL) -cholesterol in the blood. The method of claim 1,
The wasabi extract and god shin extract,
A composition for improving lipid metabolism, which is included in a weight ratio of 50 to 150: 50 to 150. The method of claim 1,
Extraction solvent of the extract,
A composition for improving lipid metabolism, comprising water, an organic solvent or an organic solvent aqueous solution. The method of claim 1,
The lipid comprises cholesterol, lipid metabolism improving composition. The method of claim 1,
The composition is for preventing or improving circulatory diseases, compositions for improving lipid metabolism. The method according to any one of claims 1 to 6,
The composition,
A pharmaceutical composition, a food composition or a cosmetic composition, a composition for improving lipid metabolism.

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