KR102099627B1 - 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

Disclosed herein is a composition for improving lipid metabolism, including horseradish extract and kidney extract as an active ingredient. The composition, which is an aspect of the present invention, can inhibit lipids such as cholesterol from accumulating in cells, and can increase the level of high-density lipoprotein (HDL) in the blood through reverse transport, thereby effectively improving lipid metabolism in the body. In addition, since the composition is non-toxic to the human body and ensures human body stability, it can be widely used in various fields, such as the food field or the pharmaceutical field.

Description

Composition for improving lipid metabolism, including horseradish extract and soybean extract as an active ingredient.

Disclosed herein is a composition for improving lipid metabolism, including horseradish extract and kidney extract as an active ingredient.

Cholesterol is an essential component of cells and plays an important role in cell growth, differentiation and development. However, it is known that when the level of cholesterol in the blood is higher than the standard, arteriosclerosis that inhibits blood circulation is likely to occur because macrophages and foam cells are formed and deposited on the blood vessel walls and form plaques. The continuous accumulation of cholesterol eventually closes the arteries, leading to serious cardiovascular diseases such as various heart diseases and angina.

Thus, as a therapeutic agent for arteriosclerosis, it is a statin-based substance that can inhibit the activity of HMG-CoA reductase, an important enzyme involved in the synthesis of cholesterol, or lower low density lipoprotein (LDL). Drugs have been developed and widely used. However, these drugs are still at the limit, as arteriosclerosis cases and various complications and side effects have been reported even when the LDL lipoprotein is low.

Meanwhile, high density lipoprotein (HDL) is known to play an important role in reverse transport of cholesterol from each tissue to the liver, adrenal glands, and organs that produce hormones, and is known to prevent arteriosclerosis. Efforts are underway to develop a lipid metabolism improving agent.

KR 10-1462326 B1

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

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

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

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

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

In order to achieve the above object, the present invention, in one aspect, provides a composition for improving lipid metabolism, including wasabi extract and soybean extract as an active ingredient.

A composition containing an extract of horseradish and soybean extract as an active ingredient, which is an aspect of the present invention, can inhibit lipids such as cholesterol from accumulating in cells, and can increase high-density lipoprotein (HDL) levels in the blood through reverse transport. , Can effectively improve the lipid metabolism in the body. In addition, since the composition is non-toxic to the human body and ensures human body stability, it can be widely used in various fields, such as the food field or the pharmaceutical field.

1 is a result showing the result of reverse cholesterol transport when the horseradish leaf extract is treated (N-leaf (wa): horseradish leaf water extract, N-leaf (Et): horseradish leaf ethanol extract).
2 is a result showing the effect of reverse cholesterol transport when treated with horseradish root extract (N-root (wa): horseradish root water extract, N-root (Et): horseradish root ethanol extract).
Figure 3 is a result of the treatment of a mixture of Shini extract and Shini extract and horseradish extract, results showing the effect of reverse cholesterol transport (S: Shini water extract, N + S: Horseradish leaf water extract + Sini water extract).

Hereinafter, the present invention will be described in detail.

The present invention is, in one aspect, a composition for improving lipid metabolism, comprising an extract of horseradish and an extract of kidney as an active ingredient.

The " Crazella ( Capsella bursa-pastoris )" is a biennial plant of the cruciferous family. It is a wasteland plant that grows well on rough ground. It blooms in May to June and bears seeds. The leaves coming out of the root are rounded together. The leaves are more than 10 cm long and have two teeth (우 大羽 頭, feathers with large heads) with dull teeth on the edge of the leaves. The root leaves are aggregated and the leaves of the foliage that come up as flowers are out of order. Foliage is lanceolate (spin-shaped, elongated like needles) and becomes smaller as it goes up. The flowers are white, and the fruit is an oblong fruit surrounded by a hard pod, and is a flat, triangular (inverted triangular shape). Horseradish is native to Eastern Europe and Asia Minor, but grows all over the world. Horseradish uses seeds, leaves, and roots for edible purposes, and was used as a hemostatic agent in oriental medicine.

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

The "shinyi" may mean a bud of a magnolia family.

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 extracts, and also extracts the substances obtained by extracting components of natural products It is a broad concept that includes all materials that can be obtained by processing or processing in other ways, and specifically, the processing or processing may be additionally fermenting or enzymatically treating the extract. Therefore, the extract in the present specification is a broad concept including a fermented product, a concentrate, and a dried product. Specifically, the extract in the present specification may include an extract of a fermented product.

In the above aspect, the lipid metabolism is improved by inhibiting intracellular lipid accumulation, or promoting extracellular release of intracellular lipids; An increase in high density lipoprotein (HDL) -cholesterol in the blood; And reduction of low density lipoprotein (LDL) -cholesterol in the blood.

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

The lipid metabolism includes the process of delivering lipids produced by the liver to each tissue, or vice versa.

Specifically, LDL is involved in the process of delivering lipids produced by the liver to each tissue, and HDL is involved when delivering lipids from each tissue to the liver.

The promotion of extracellular release of the intracellular lipid may mean, for example, reverse transport of cholesterol. The reverse cholesterol transport may refer to a path of transporting cholesterol from peripheral tissues (cells) to the liver using HDL as a medium.

Specifically, reverse cholesterol transport may refer to a process in which phospholipids and cholesterol are received from peripheral cells and transported directly to the liver, or indirectly delivered to the liver through delivery to a very low density lipoprotein (VLDL) and LDL residue. Apolipoprotein A1 (apolipoprotein A1) produced in the liver or intestine receives phospholipids and the like 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 the peripheral tissues, and free cholesterol is esterified by lecithin-cholesterol acyl transferase (LCAT), converted into cholesterol ester, and moved to the center, where it is changed into a spherical shape. HDL delivers cholesterol ester (CE) to chylomicron or VLDL residues through cholesterol ester transfer protein (CETP) in the blood, and exchanges them to obtain triglycerides. Eventually, in the liver or in tissues requiring cholesterol, it binds to the HDL receptor (clean receptor B1) to deliver cholesterol and the apolipoprotein A1 is used again or metabolized in the kidneys.

In the same aspect, the extract of horseradish and soybean extract of the composition may be included in a weight ratio of 50 to 150: 50 to 150. Preferably, the horseradish extract and Shini extract may be included in a weight ratio of 80 to 120: 80 to 120 in order, more preferably 90 to 110: 90 to 110.

The horseradish extract and Shini extract may be included in 0.1 to 90% by weight based on the total weight of the composition. Wasabi extract and soybean extract, within the above content range, may be included in the content ratio.

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

The organic solvent, hexane, methylene chloride, alcohol, etc. may be used as the organic solvent, but is not limited thereto. In the above, the water contains distilled water or purified water, and the organic solvent is a group consisting of alcohols, acetone, ether, ethyl acetate, diethyl ether, methanol, ethyl methyl ketone and chloroform, for example, lower alcohols of C ₁ to C ₅ . One or more selected from, but is not limited to.

When the extraction solvent is water, heat extraction, cold immersion extraction, reflux cooling extraction, or ultrasonic extraction may be used, preferably warm extraction, preferably about 40 to 120 ° C, more preferably about It can be extracted at a temperature of 70 ℃, but is not limited thereto. The extraction time may 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 alcohol, and the alcohol may be ethanol.

Wasabi extract and / or acid extract, when using water as an extraction solvent, it is possible to obtain a result having a better activity than when using ethanol.

In one aspect, the lipid may include cholesterol.

In one aspect, the composition may be a composition for preventing or improving various circulatory system diseases. For example, it can be used as a composition for the prevention or improvement of cardiovascular diseases, specifically, atherosclerosis, atherosclerosis, 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, food composition or cosmetic composition.

The composition of the present invention can be prepared in a pharmaceutical formulation according to a conventional method. In the preparation of the formulation, it is preferred to mix or dilute the active ingredient with the carrier or enclose it in a carrier in the form of a container. When the carrier is used as a diluent, it may be a solid, semi-solid or liquid substance that acts as a carrier, excipient or medium for the active ingredient. Accordingly, the formulation may be in the form of tablets, pills, powders, sachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, soft or hard gelatin capsules, sterile injections, sterile powders, and the like.

Examples of suitable carriers, excipients and diluents are 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 include fillers, anticoagulants, lubricants, wetting agents, flavoring agents, emulsifying agents, preservatives, and the like. Compositions of the present invention can 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 can be administered through various routes including oral, transdermal, subcutaneous, intravenous, intraperitoneal, intramuscular, topical application, patch and iontophoresis, among which topical application and oral administration are preferred. Do.

In the case of humans, the typical daily dosage of the composition may range from 1 to 100 mg / kg body weight, preferably from 5 to 70 mg / kg body weight, and may be administered in single or multiple doses. However, it should be understood that the actual dosage of the composition should be determined in light of a number of related 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, so that the dosage can be determined in any way. Nor is it intended to limit the scope of the invention.

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

The mixing amount of the active ingredient may be appropriately determined according to the purpose of use (prevention, health or therapeutic treatment). Generally, 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, with respect to the raw materials, in the preparation of a food or beverage. However, in the case of long-term intake for health and hygiene purposes or for health control, the amount may be below the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount above the above range.

There are no particular restrictions on the type of food. Examples of foods to which the extract of the present invention can be added are meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other dairy products including noodle, gum, ice cream, various soups, beverages, tea, Drinks, alcoholic beverages, and vitamin complexes are included, and include all healthy foods in the ordinary sense.

In addition to the above, the extracts of the present invention are 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, alcohol, carbonic acid And carbonated agents used in beverages.

Specifically, the cosmetic composition may include, for example, a cosmetic for hair, a cosmetic for a body, a basic cosmetic, and a makeup cosmetic, and the formulation is not particularly limited and may be appropriately selected according to the purpose.

For example, the cosmetic composition is formulated as a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleaning, oil, powder foundation, emulsion foundation, wax foundation and spray, etc. It may be, but is not limited to this. More specifically, shampoo, rinse, body cleanser and other cleaning agents, hair tonics, hair or cosmetic agents for hair, such as gels or mousse, hair or cosmetic composition for hair, softening, longevity, nutrient makeup, lotion, body lotion, nutrition 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) type Can be formulated as

The cosmetic composition contains a cosmetically acceptable medium or base. These are all formulations suitable for topical application, for example solutions, gels, solid or dough anhydrous products, emulsions, suspensions, microemulsions, microcapsules, microgranules or ionic (liposomes) obtained by dispersing an oil phase in an aqueous phase and / or It may be provided in the form of a non-ionic vesicle dispersant, or in the form of a cream, skin, lotion, powder, ointment, spray or conceal 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 a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or fatty acid ester of sorbitan.

When the formulation of the present invention is a suspension, liquid diluents such as water, ethanol or propylene glycol as carrier components, ethoxylated isostearyl alcohol, suspensions such as polyoxyethylene sorbitol esters and polyoxyethylene sorbitan esters, microcrystals Sex cellulose, aluminum metahydroxide, bentonite, agar or trakant, etc. can be used.

When the formulation of the present invention is a paste, cream, or gel, animal oil, vegetable oil, wax, paraffin, starch, trakant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide, etc. may be used as a carrier component. You can.

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 as a carrier component, and 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 additionally 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 or the like can be used, preferably, one or more 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 various bases and additives as necessary, and the types and amounts of these components can be easily selected by the inventor. If necessary, it may contain an acceptable additive, for example, it may further include components such as preservatives, pigments, additives, etc., which are customary 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 for the purpose of illustration only to aid understanding of the present invention, and the scope and scope of the present invention are not limited by the following examples.

[Production example]

[Production Example 1] Wasabi leaf, wasabi root hot water extract preparation

After drying the horseradish leaves and roots, 30 g of the powder obtained by crushing was placed in 600 g of purified water, left for 2 hours at 70 ° C., and then filtered on 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.

[Production Example 2] Preparation of ethanol extract of horseradish leaves and horseradish root

After drying the horseradish leaves or roots, 30 g of the powder obtained by crushing was placed in 600 g of 30% ethanol, left for 2 hours at 60 ° C., and then filtered on 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.

[Production Example 3] Preparation of hot water extract

After drying Shin-Yi, 30 g of the powder obtained by crushing was placed in 600 g of purified water, left at 70 ° C. for 2 hours, and then filtered on a non-woven 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 reverse cholesterol transport effect of horseradish extract

In the experiment, J774.1 cells, which are cell lines of macrophage cells, were used to represent peripheral tissues. Lipid improvement effect was measured through the ratio of how much cholesterol was discharged out of the cells by treating the cells with horseradish extract. In other words, the cholesterol released from macrophage cells was combined with HDL, so the ratio of HDL was increased.

The experiment was conducted using Biohole's Cholesterol Efflux Fluometirc Assay kit. This kit contains fluorescently labeled cholesterol. When culturing giant phagocytic cells, fluorescently labeled cholesterol is put into the cells, and then fluorescent cholesterol released from the cells is collected with HDL when processed with horseradish extract. It is supposed to measure.

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

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

3) After changing the medium of the cells, the wasabi extract was added to the RPMI medium at the appropriate concentration and incubated for 4 hours.

4) Human serum was added to the cholesterol receptors discharged into the medium. It contains HDL protein so that cholesterol can be released from the cells.

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

6) The ratio of the amount of fluorescence emitted to the medium out of the total amount of fluorescence was calculated, and the amount of cholesterol efflux was measured.

<Ice leaf extract>

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

<Rice root extract>

In the case of the extract of horseradish root, the result was similar to that of the leaf extract. When the water extract was treated to about 10 μg / ml, it was confirmed that higher cholesterol secretion occurred than the group treated with the positive standard. The ethanol extract was found to promote cholesterol secretion lower than that of the water extract but higher than the positive standard (FIG. 2).

[Experimental Example 2] Confirming the effect of sini extract on the reverse transport of cholesterol

In the same manner as in Experimental Example 1, the effect of reverse cholesterol transport was also confirmed for the Sini extract.

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

[Experimental Example 3] The effect of reverse transport of cholesterol in the mixture of horseradish extract and kidney extract was confirmed

Wasabi leaf extract, and the same amount of water extract (5μg) was mixed to check the cholesterol reverse transport effect in the same manner as above.

As a result, it was confirmed that the cholesterol secretion effect improved by about 120% or more compared to the case where the horseradish and shin were treated respectively, and the synergistic effect on the reverse cholesterol transport effect according to the bilateral combination was confirmed.

Claims (7)

As a composition for improving lipid metabolism,
The composition,
Contains Wasabi Extract and Sini Extract as active ingredients,
The lipid metabolism improvement,
Inhibiting intracellular lipid accumulation, or promoting extracellular release of intracellular lipids;
An increase in high density lipoprotein (HDL) -cholesterol in the blood; And
Containing one or more selected from the group consisting of a reduction in blood low density lipoprotein (LDL) -cholesterol,
The composition is a food composition, a composition for improving lipid metabolism. delete According to claim 1,
The wasabi extract and soybean extract,
A composition for improving lipid metabolism, which is included in a weight ratio of 50 to 150: 50 to 150. According to claim 1,
The extraction solvent of the extract,
A composition for improving lipid metabolism, comprising water, an organic solvent, or an aqueous organic solvent solution. According to claim 1,
The lipid, cholesterol, lipid metabolism improving composition. According to claim 1,
The composition is for preventing or improving circulatory system disease, a composition for improving lipid metabolism. delete

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