KR101268460B1 - Anti-allergic composition - Google Patents

Abstract

The present invention provides a pharmaceutical composition, health functional food and cosmetic composition containing a extract of Siegesbeckiae glabrescens as an active ingredient for the treatment of allergic diseases derived from natural plants with low side effects and effective.

Description

Anti-allergic composition {Anti-allergic composition}

The present invention relates to an anti-allergic composition, and more particularly, to an anti-allergic composition containing a natural plant extract as an active ingredient.

 Allergy or allergy is a biochemical phenomenon that shows a specific and modified reaction to a foreign substance (antigen, Allergen), and when the released substance causes symptoms, it is called allergen. It is called. It is a pathological process of living organisms resulting from antigen-antibody reactions that are the source of allergy, and is generally classified into type 1 to type 4 from the time required for causing the reaction and the absence of complement involvement.

Type 1 is anaphylatctic (immediate type). The target organs are mainly digestive organs, skin and lungs. Common symptoms include gastrointestinal allergy, gall bladder, atrophic dermatitis, allergic rhinitis and bronchial asthma. There is this. Pathology of type 1 activates target cells by contacting antigens with IgE antibodies attached to the surface of mast cells and basophils to secrete chemical media such as histamine, serotonin, leukotrienes, and PAF, resulting in blood vessels and smooth muscle. It is known to shrink, which is often combined with type 4 (delayed type). In other words, this anaphylaxis and allergic reaction are due to various changes occurring in mast cells and the like.

In recent years, research has been actively conducted due to an increase in allergic diseases such as atopic dermatitis, and the development of radical immunology has made a lot of progress in the lifesaving and treatment of allergic diseases. There is no drug that can cure the disease, and the patient is expected to improve symptoms through the drug, but the side effects are large.

The present invention has been made to solve the above problems, an object of the present invention to provide a pharmaceutical composition for preventing and treating allergic diseases derived from safe and effective natural plants.

The present invention aims to provide a health functional food for preventing and improving allergic diseases derived from safe and effective natural plants.

An object of the present invention is to provide a functional cosmetic composition for alleviating and improving allergic skin symptoms derived from safe and effective natural plants.

However, these problems are exemplary and do not limit the scope of the present invention.

According to an aspect of the present invention, there is provided a pharmaceutical composition for preventing and treating allergic diseases containing Siegesbeckiae glabrescens extract as an active ingredient.

At this time, the rare extract may be prepared by extracting the rare water with water, C ₁ ~ C ₄ lower alcohol or a mixture thereof, or may be a fraction obtained by fractionating these extracts again with an organic solvent. The fraction may be a single fraction of a specific organic solvent, may be any one or more of the sequential fractions sequentially divided according to the polarity of the organic solvent. For example, the rare extract is dissolved in 70% ethanol, and then sequentially fractionated in the order of N-hexane, chloroform, ethyl acetate, butanol and water, and the organic solvent is evaporated to use one or more fractions of the remaining residues. Can be.

The allergic disease may be, but is not limited to, bronchial asthma, contact allergy, urticaria, pruritus, atopic dermatitis, allergic rhinitis, angioedema, food allergy, drug allergy or anaphylaxis.

The present inventors confirmed that the treatment of the composition of the present invention on RBL-2H3 cells, a kind of mast cells, inhibited the extracellular release of β-hexosaminidase, an allergic indicator (see FIG. 1). Mast cells (mast cell, RBL-2H3, ATCC No. CRL-2256, USA) secrete histamine, which is activated by an immune response and acts as a major cause of allergies. When degranulation occurs in activated mast cells, β-hexosaminidase is released together, and the released β-hexosaminidase can be used as an indicator of degranulation (Ho, C. et al ., Planta Med . 64: 577-578, 1998).

In addition, the inventors of the present invention did not stop the effect of the rare extract in vitro conditions, animal experiments in animal models in which allergic diseases such as itching or atopic dermatitis caused the skin extracts effectively treat allergic diseases Proved possible (see FIGS. 2 and 3). Therefore, the rare extract of the present invention can be used as a composition for treating various allergic diseases.

The pharmaceutical composition according to one embodiment of the present invention preferably comprises 0.1 to 50% by weight of the rare extract based on the total weight of the composition.

In general, the pharmaceutical composition according to an embodiment of the present invention can be used for oral and parenteral administration during clinical administration, and can also be used in the form of a general pharmaceutical formulation, since it is possible to apply skin during parenteral administration.

Oral compositions according to one embodiment of the present invention may further comprise inert ingredients including pharmaceutically acceptable carriers, diluents, fillers, solubilizers or emulsifiers and salts well known in the art. For example, the pharmaceutical compositions of the present invention may be formulated in tablet form according to conventional methods using solid carriers well known in the art, and alternatively any pharmaceutically acceptable substance such as gelatin or cellulose derivatives It can also be prepared in the form of capsules.

In practical use, the pharmaceutical compositions according to one embodiment of the present invention may be combined with pharmaceutical carriers according to conventional pharmaceutical preparation techniques. The carrier may take a wide variety of forms depending upon the preparation desired, for example, for oral or parenteral administration (including intravenous administration).

Pharmaceutical compositions according to one embodiment of the invention are useful for the treatment of allergic diseases and, for these purposes, in the form of dosage unit dosage forms comprising conventional non-toxic pharmaceutically acceptable carriers, adjuvants and vehicles. It can be administered orally or parenterally (subcutaneous, intravenous, intramuscular, intrasternal or infusion, transdermal, intranasal, etc.) or rectally.

Each oral composition according to one embodiment of the present invention further comprises an inert ingredient, including a pharmaceutically acceptable carrier. As used herein, a "pharmaceutically acceptable carrier" is a term that refers to a composition, specifically an ingredient other than the active substance of the pharmaceutical composition. Examples of pharmaceutically acceptable carriers include binders, disintegrants, diluents, fillers, lubricants, solubilizers or emulsifiers and salts.

According to another aspect of the present invention, there is provided a health functional food for alleviating and improving allergic diseases containing a rare extract as an active ingredient.

According to one embodiment of the present invention, by adding a rare extract to food, it is possible to prepare a functional food for the prevention of symptoms and improvement of symptoms. In this case, the health functional food is manufactured in the form of tablets, capsules, powders, granules, liquids, pills, etc., using raw materials or ingredients having functional properties useful for the human body, as defined in Article 3 of the Health Functional Food Act. It refers to a possible food, and examples of the food which may include the rare extract of the present invention include various capsules, tablets, granules, drinks, tea, beverages, vitamin complexes, and the like, and the amount of the active ingredient is used for its purpose (prevention, symptom relief, Or adjuvant treatment).

The health functional food of the present invention may include 0.01 to 95% by weight, preferably 1 to 80% by weight of the rare extract based on the total weight of the food for the purpose of preventing and improving symptoms of allergic diseases such as atopic dermatitis. There is no restriction | limiting in particular in manufacture of the functional food of this invention, Any of normal food manufacturing methods, etc. can be applied as it is or modified suitably.

In addition, according to another aspect of the present invention, there is provided a functional cosmetic composition for alleviating and improving allergic skin symptoms comprising a rare extract as an active ingredient.

The cosmetic composition of the present invention may be added various additives, additives, and carriers that are acceptable in the manufacture of cosmetics, in addition to the rare extract as the active ingredient, such components include fats and oils, moisturizers, emollients, surfactants, organic and inorganic Pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, blood circulation accelerators, coolants, limiting agents, purified water, and the like. Any of those described in the above may be used.

The blending ratio of the rare extract contained in the cosmetic composition according to an embodiment of the present invention is not particularly limited, but may be blended within the range not impairing the object and effect of the present invention, and preferably 0.01-to the total weight. 5% by weight, more preferably 0.01-3% by weight.

The cosmetic of the present invention may take the form of a solution, an emulsion, a viscous mixture or the like.

The cosmetic composition of the present invention may be prepared in any formulation commonly prepared in the art, and includes, for example, emulsion, cream, lotion, pack, foundation, lotion, essence, and the like.

Specifically, the cosmetic composition of the present invention can be used as a skin lotion, a skin softener, a skin toner, an astringent, a lotion, a milk lotion, a moisturizing lotion, a nutrition lotion, a massage cream, a nutrition cream, a moisturizing cream, a hand cream, Packs, soaps, cleansing foams, cleansing lotions, cleansing creams, body lotions and body cleansers.

When the formulation of the present invention is a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

In the case where 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. Especially, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solvating agent or emulsifying agent 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, microcrystalline Cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is an interfacial active agent-containing cleansing, the carrier component may include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolenic derivatives or ethoxylated glycerol fatty acid esters.

According to one embodiment of the present invention made as described above, the present invention has fewer side effects by using a natural plant extract as an active ingredient, the symptoms of allergic diseases such as atopic dermatitis and skin itching when administered to a model animal remarkably Because of the improvement, the composition of the present invention can be used not only as a therapeutic agent for allergic diseases, but also as a dietary supplement for alleviation and improvement of these diseases and cosmetics for alleviation and improvement of allergic skin symptoms. Of course, the scope of the present invention is not limited by these effects.

1 is a graph showing the anti-allergic effect through the β-hexosaminidase release inhibition of the composition according to an embodiment of the present invention.
Figure 2 is a graph showing the itch improvement effect of the itch-induced model animal of the composition according to an embodiment of the present invention.
Figure 3 is a photograph showing the anti-atopic effect of the composition according to an embodiment of the present invention.

Hereinafter, the present invention will be described in more detail with reference to Examples and Experimental Examples. It should be understood, however, that the invention is not limited to the disclosed embodiments and examples, but may be embodied in many different forms and should not be construed as being limited to the embodiments set forth herein. Rather, these embodiments are provided so that this disclosure will be thorough and complete, It is provided to fully inform the owner of the scope of the invention.

Example 1: Preparation of Rare Extract

300 g of starch (Siegesbeckie Herba.) Excluding the roots of Siegesbeckiae glabrescens were placed in a 5 L flask and refluxed for 3 hours by adding 3 L of 75% ethanol. The liquid phase obtained by removing solids was filtered, concentrated and lyophilized to obtain 20 g of extract.

Experimental Example 1 β-hexosaminidase Release Experiment

RBL-2H3 cells used in the experiment were distributed by the Korea Cell Line Bank (KCLB) and DMEM containing 10% heat-inactivated FBS (Gibco BRL, USA) and 1% penicillin and streptomycin (Gibco BRL, USA) for culturing the cells. (Gibco BRL, USA) culture was incubated. Cells were cultured under 37 ° C., 5% CO ₂ , and the cells were suspended and passaged after treatment with 0.05% trypsin-EDTA solution (Gibco BRL, USA) in order to eliminate the over-density of cells.

β-hexosaminidase release experiment was performed by Dastych's method (Dastych et al ., J. Allergy Clin. Immunol ., 103 (6): 1108-1114, 1999). Specifically, the RBL-2H3 cells were suspended in DMEM containing 10% FBS, followed by 2 × 10 ⁵ cells per well in a 24-well culture dish, and then cultured overnight in a 37 ° C. 5% CO ₂ incubator. Cells in each well were washed twice with extracellular buffer (5 mM KCl, 12.5 mM NaCl, 20 mM HEPES, 1.5 mM MgCl, 1.5 mM CaCl ₂ , 1 mM dextros, pH 7.4), followed by extracellular buffer and sample per well. After treatment with (0, 10, 100, 200 mg / L) it was reacted for 1 hour. After using PMA (50 nM) and A23187 (1 mM) the cells were reacted for 1 hour in a 37 ℃ 5% CO ₂ incubator and incubated for 10 minutes in an ice bath to terminate the reaction. 20 μl of supernatant was transferred to a 96 well plate, and pellets were dissolved in 1 ml of Triton X-100 (0.1%) in a 24 well plate, and 20 μl was added to the 96 well plate. 100 μl of substrate buffer (4-p-Nitrophenyl-N-acetyl-β-D-glucosaminide 1 mM, sodium citrate 0.05 M, pH 4.5) was added to a 96 well plate containing supernatant and pellets. The reaction was terminated by adding 200 μl of stop solution per well. Then the absorbance was measured at 405 nm using a Microplate reader (Molecular Devices, USA). The total emission rate (%) was calculated by the following equation as the absorbance values of the sample and the control.

Total release rate (%) = [S / (S + P) -S _control / (S _control + P _control )] × 100

Where S is the absorbance of the supernatant, P is the absorbance of the pellets, and S _control / (S _control + P _control ) (%) is the spontaneous release in the absence of stimulation.

The experimental results showed that the amount of β-hexosaminidase released from RBL-2H3 cells was 9.20 ± 0.60% in untreated cells and 39.45 ± 1.12% in cells stimulated with PMA and A23187, compared with untreated cells. One (p <0.05) increase was shown. On the other hand, in cells treated with 10, 100 and 200 mg / L samples 30 minutes before PMA and A23187 stimulation, the total release rate was 35.33 ± 1.31%, 27.24 ± 1.22 and 10.42 ± 1.33%, respectively. Compared to the cells stimulated with PMA and A23187 without, it showed a significant (p <0.05) decrease at all concentrations (FIG. 1).

Experimental Example 2: Animal Experiment

<2-1> Itching Induction Experiment

Animal experiments were performed using a rat of SD series. Specifically, after exposing and exposing the back of the mouse's neck, Krebs-Ringer buffer (Rothschild, Br. J ) containing 0.5% of Compound 48/80 (Sigma Chemical Co., USA), a material that causes itching Pharmac . , 38: 253-262, 1970) was applied to the exposed skin and the number of back scratches with the hind legs for 1 hour was recorded. After 24 hours, the same amount of Compound 48/80 and the sample were mixed with 0, 10, 100 and 200 mg / L samples, respectively, and applied to the same place, and the number of scratches was recorded for 1 hour. In this case, the degree of scratching was expressed in terms of the number of scratches after applying the mixed solution of the sample and Compound 48/40 when the number of scratches of the mouse coated with only Compound 48/80 without the sample was 100.

 As a result, it can be seen that in the experimental group treated with the rare extract of the present invention, the number of times of scratching the back was significantly reduced (FIG. 2).

<2-2> degree of improvement of skin condition

Induced atopic dermatitis by irradiating UV to the back of nude mice (Central test animal, Korea) for 30 minutes, applying 1 ml of 200 mg / L rare extract to the affected area and observing the healing effect over time. Photographed (Figure 3).

As a result, it was found that the skin condition was remarkably improved from the third day after the treatment.

Although the present invention has been described with reference to the above examples and experimental examples, these are merely exemplary, and it will be understood by those skilled in the art that various modifications and equivalent other embodiments are possible. Therefore, the true technical protection scope of the present invention will be defined by the technical spirit of the appended claims.

Claims (6)

A skin coating for treating atopic dermatitis, containing extract of Siegesbeckiae Herb, ethanol aqueous solution except for root. delete delete delete Functional cosmetic composition for alleviating and improving atopic dermatitis symptom comprising the extract of Siegesbeckiae Herb ethanol aqueous solution excluding the root as an active ingredient. delete

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