KR101968299B1 - Anti-allergic Composition Comprising Lappaol A as an Active Ingredient - Google Patents

Abstract

The present invention relates to a composition for preventing or treating allergic diseases containing lappaol A as an active component. More specifically, the present invention: to the composition for preventing or treating atopic dermatitis, asthma, allergic rhinitis, or allergic conjunctivitis containing lappaol A as the active component; and a method for preventing or treating allergic diseases comprising a step of administering the composition to an individual. The composition containing lappaol A as the active component of the present invention can inhibit inflammatory mediators and degranulation, and also can effectively inhibit allergic reactions at the level of a signal transduction pathway, thereby being usefully used as the composition for preventing or treating allergic diseases.

Description

[0001] Anti-allergic composition comprising Lappaol A as an active ingredient [

The present invention relates to a composition for the prevention or treatment of allergic diseases comprising Lappaol A as an active ingredient, and more particularly to a composition for preventing or treating allergic conjunctivitis, atopic dermatitis, asthma, allergic rhinitis or allergic conjunctivitis comprising Lappaol A as an active ingredient And a method for preventing or treating an allergic disease comprising administering the composition to a subject.

Recently, allergic diseases are on the rise, and research and development of therapeutic agents are under way. Allergic disease means a disease caused by immune hypersensitivity reaction. Allergic reaction is a complicated reaction involving various cells and mediators, and acts as a cause of various diseases. Therefore, it is expected that various diseases can be treated through the control of allergic reactions. Allergic diseases include atopic dermatitis, asthma, allergic rhinitis, allergic conjunctivitis, allergic dermatitis and the like.

Atopic dermatitis is a common worldwide disease that can occur in any age group, with 70% to 95% occurring at infancy under 5 years of age. In Korea, the problem of atopic dermatitis has already reached serious social and medical problems. According to various reports, about 15% of the total population in Korea are atopic dermatitis patients, of which 18-22 per 100 children aged 1 to 4 years are known to be atopic. In recent years, the increase of atopic dermatitis in adults as well as adults has become serious, and severe cases of social problems such as employment and marriage are causing severe social problems. In such cases, severe psychological stress can cause severe depression and avoidance of interpersonal abuse. Despite the fact that atopic dermatitis is a serious social and medical problem, there is no effective treatment until now.

Allergic rhinitis is the most common allergic disease, and its incidence is gradually increasing, affecting the quality of life, decreasing the production capacity and increasing the burden of the treatment cost, which is a socioeconomic problem. However, It is true. Although currently used pharmacotherapy is the basic treatment for allergic rhinitis, recurrence is common and serious side effects may occur during drug withdrawal, and immunotherapy may be the primary treatment to restore the originally modified immune system, but it is costly .

Allergic conjunctivitis is an allergic disease that refers to an acute inflammatory disease caused by conjunctiva (whitish) caused by specific allergen causing substances such as pollen of spring, air dust, animal dandruff, When an allergic reaction occurs through immune cells such as mast cells, eosinophils or basophils, various inflammatory substances such as histamine are secreted to cause an inflammatory reaction to the conjunctiva. These allergic conjunctivitis can be treated with glucocorticoid based steroid eye drops. However, these antiinflammatory drugs can cause sudden adrenal insufficiency, fever, fever, elevated intraocular pressure, (Warner Carr, et al., Allergy Rhinol (Providence), 2016 Summer; 7 (2): e107-e114.), Antiallergic agents without such problems are required.

Under these circumstances, the inventors of the present invention have made extensive efforts to develop drugs capable of effectively treating allergic diseases. As a result, Lappaol A has excellent antiallergic effect with little cytotoxicity, and thus has an effect of preventing or treating allergic diseases And confirmed the present invention.

It is an object of the present invention to provide a pharmaceutical composition for the prevention or treatment of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

It is another object of the present invention to provide a health functional food for the prevention or amelioration of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

It is another object of the present invention to provide a quasi-drug composition for the prevention or amelioration of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

It is another object of the present invention to provide a cosmetic composition for preventing or improving an allergic disease comprising Lappaol A and a cosmetically acceptable salt thereof.

It is another object of the present invention to provide a method of preventing or treating an allergic disease comprising administering a composition comprising Lappaol A and a pharmaceutically acceptable salt thereof to a subject other than a human.

As one aspect for solving the above problems, the present invention provides a pharmaceutical composition for the prevention or treatment of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

Hereinafter, the antiallergic composition comprising Lappaol A as an active ingredient in the present invention will be described in detail.

The term " Lappaol A " of the present invention is a kind of lignan having a structure of the following formula (1) and has a molecular weight of 536.577 g / mol. The function of Lappaol A is not well known.

[Chemical Formula 1]

The Lappaol A can be obtained through extraction and purification from natural products, or commercially available, but is not limited thereto.

The Lappaol A may be one that inhibits degranulation, inhibits the production of inflammatory mediators, inhibits arachidonic acid chain reaction or inhibits the FcεRI signaling mechanism.

In one embodiment of the present invention, it was confirmed that Lappaol A was effectively inhibited the degranulation reaction, which is an index of the allergic reaction, as a result of treating the mast cell with allergic reaction (FIG. 1).

In one embodiment of the present invention, the supernatant of mast cells treated with the compound was analyzed to confirm that the effect of inhibiting the production of inflammatory mediators relative to the control group was excellent (FIG. 3).

In one embodiment of the present invention, after inducing an allergic reaction, the mast cells treated with the compound were dissolved to extract the total protein, and the protein related to the allergic reaction mechanism was quantitatively determined to inhibit the expression of a large number of related proteins And 5).

The term " allergic disease " of the present invention means a disease caused by an immunological hypersensitivity reaction. The allergic reaction is a complex reaction involving various cells and mediators, and serves as a cause of various diseases. Specifically, the allergic disease may be any disease selected from the group consisting of allergic rhinitis, asthma, atopic dermatitis, and allergic conjunctivitis, but is not limited thereto.

The term " prevention " of the present invention may mean all actions that inhibit or delay the onset of an allergic disease by administering Lappaol A according to the present invention to a subject.

The term " treatment " of the present invention may mean all actions which cause the symptom of an allergic disease to be improved or benefited by administering the composition of the present invention to a suspected individual having an allergic disease.

The pharmaceutical composition of the present invention may be used as a single preparation or may be manufactured into a combination preparation containing a drug known to have an effect of treating an approved allergic disease and may be formulated using a pharmaceutically acceptable carrier or excipient May be prepared in unit dosage form or may be manufactured by intrusion into a multi-dose container.

The term " pharmaceutically acceptable carrier " of the present invention may mean a carrier or diluent that does not disturb the biological activity and properties of the compound being injected, without irritating the organism. The type of the carrier that can be used in the present invention is not particularly limited, and any carrier conventionally used in the art and pharmaceutically acceptable may be used. Non-limiting examples of the carrier include saline, sterilized water, Ringer's solution, buffered saline, albumin injection solution, dextrose solution, maltodextrin solution, glycerol, ethanol and the like. These may be used alone or in combination of two or more. The carrier may comprise a non-naturally occuring carrier.

In addition, if necessary, other conventional additives such as an antioxidant, a buffer and / or a bacteriostatic agent can be added and used. A diluent, a dispersant, a surfactant, a binder, a lubricant, Pills, capsules, granules or tablets, and the like.

In addition, the pharmaceutical composition of the present invention may contain a pharmaceutically effective amount of Lappaol A. The term " pharmaceutically effective amount " as used herein means an amount sufficient to treat a disease at a reasonable benefit / risk ratio applicable to medical treatment and is generally in the range of 0.001 to 1000 mg / kg, preferably 0.05 To 200 mg / kg, more preferably 0.1 to 100 mg / kg, may be administered once a day to several times per day. For purposes of the present invention, however, the specific therapeutically effective amount for a particular patient will depend upon the nature and extent of the reaction to be achieved, the particular composition, including whether or not other agents are used, the age, weight, Sex and diet of the patient, the time of administration, the route of administration and the rate of administration of the composition, the duration of the treatment, the drugs used or concurrently used with the specific composition, and similar factors well known in the medical arts.

The pharmaceutical composition of the present invention may be administered as an individual therapeutic agent or in combination with another therapeutic agent, and may be administered sequentially or simultaneously with conventional therapeutic agents. And can be administered singly or multiply. It is important to take into account all of the above factors and to administer an amount that can achieve the maximum effect in a minimal amount without causing side effects, and can be readily determined by those skilled in the art.

The term " administering " of the present invention means introducing the pharmaceutical composition of the present invention to a patient by any suitable method, and the administration route of the composition of the present invention may be administered orally or parenterally in various routes ≪ / RTI >

The mode of administration of the pharmaceutical composition according to the present invention is not particularly limited and may be conventionally used in the art. As a non-limiting example of such a mode of administration, the compositions may be administered orally or parenterally. The pharmaceutical composition according to the present invention can be manufactured into various formulations according to the intended administration mode.

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

The term " pharmaceutically acceptable salt " of the present invention means a formulation that does not impair the biological activity and properties of Lappaol A administered. The pharmaceutically acceptable salts include those acids which form a non-toxic acid addition salt containing a pharmaceutically acceptable anion such as inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, hydrobromic acid, hydroiodic acid and the like, Organic carboxylic acids such as formic acid, citric acid, acetic acid, trichloroacetic acid, trifluoroacetic acid, gluconic acid, benzoic acid, lactic acid, fumaric acid, maleic acid and salicinic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p- Sulfonic acid such as sulfonic acid, sulfonic acid, sulfonic acid, and the like. For example, pharmaceutically acceptable carboxylic acid salts include metal salts or alkaline earth metal salts formed with lithium, sodium, potassium, calcium, magnesium and the like, amino acid salts such as lysine, arginine and guanidine, dicyclohexylamine, N Organic salts such as methyl-D-glucamine, tris (hydroxymethyl) methylamine, diethanolamine, choline and triethylamine, and the like.

In another aspect, the present invention provides a health functional food for the prevention or amelioration of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

Functional food is the same term as Food for special health use (FoSHU). It refers to foods that have been processed so that the biocontrol function can be efficiently displayed in addition to the nutritional supply. , The food may be prepared in various forms such as tablets, capsules, powders, granules, liquids, rings and the like in order to obtain a useful effect for prevention or improvement of disease.

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

There is no particular limitation on the type of food to which the composition containing Lappaol A of the present invention can be added, and examples thereof include various drinks, gums, tea, vitamin complex, and health supplement foods. The food composition may be supplemented with other ingredients that do not interfere with the preventive or ameliorative effect of an allergic disease, and the kind thereof is not particularly limited. For example, various herbal medicine extracts, food-acceptable food-aid additives or natural carbohydrates, such as ordinary foods, may be added as an additional ingredient.

The food-aid additive is added to produce a health functional food of each formulation and can be appropriately selected and used by those skilled in the art. For example, various kinds of nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, colorants and fillers, pectic acid and its salts, alginic acid and its salts, organic acids, protective colloid thickeners, , A stabilizer, a preservative, a glycerin, an alcohol, a carbonating agent used in a carbonated drink, and the like, but the kind is not limited by the above examples.

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

When the food is a beverage, it may be contained in a proportion of 1 to 30 g, preferably 3 to 20 g based on 100 ml. In addition, the composition may contain additional ingredients which are commonly used in food compositions and which can improve odor, taste, vision and the like. For example, vitamins A, C, D, E, B1, B2, B6, B12, niacin, biotin, folate, panthotenic acid and the like. In addition, it may include minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn) and copper (Cu) It may also include amino acids such as lysine, tryptophan, cysteine, valine, and the like. In addition, it is also possible to use antiseptics (such as potassium sorbate, sodium benzoate, salicylic acid, and sodium dehydroacetate), disinfectants (such as bleaching powder and highly bleached white powder, sodium hypochlorite), antioxidants (butylhydroxyanilide (BHA), butylhydroxytoluene BHT, etc.), coloring agents (tar pigments, etc.), coloring agents (such as sodium nitrite and sodium acetates), bleaching agents (sodium sulfite), seasonings (sodium glutamate, etc.), sweeteners (such as hypocotyls, cyclamates, saccharin, sodium Etc.), flavorings (vanillin, lactones, etc.), swelling agents (alum, potassium hydrogen D-tartrate etc.), enhancers, emulsifiers, thickeners (foams), encapsulating agents, gum bases, foam inhibitors, Food additives may be added. The additives are selected according to the type of food and used in an appropriate amount.

The health functional food of the present invention can be manufactured by a method commonly used in the art and can be prepared by adding raw materials and ingredients which are conventionally added in the art. Also, unlike general medicine, there is an advantage that there is no side effect that can occur when a medicine is used for a long time by using food as a raw material, and it is excellent in portability.

In yet another aspect, the present invention provides a quasi-drug composition for the prevention or amelioration of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.

The term " quasi-drug product " in the present invention means products which are used for diagnosing, treating, improving, alleviating, treating or preventing a disease of a human or an animal. For example, quasi-drugs according to the Pharmaceutical Affairs Law include products used for the treatment and prevention of diseases of humans and animals, products which are mild to the human body or which do not act directly on the human body.

Specifically, the quasi-drug may include external preparation for skin and personal hygiene products. More specifically, it may be sterilization cleaner, shower foam, gagrin, wet tissue, detergent soap, hand wash, or ointment, but is not limited thereto.

When the composition according to the present invention is used as a quasi-drug additive, the composition may be added as it is or may be used together with other quasi-drugs or quasi-drugs, and may be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be appropriately determined depending on the purpose of use.

In another aspect, the present invention provides a cosmetic composition for preventing or improving allergies comprising Lappaol A and a cosmetically acceptable salt thereof.

In the present invention, the cosmetic composition may further comprise at least one cosmetically acceptable carrier mixed with a cosmetic composition for general skin. Examples of the cosmetic composition include oil, water, a surfactant, a humectant, a lower alcohol , A thickening agent, a chelating agent, a coloring agent, a preservative, a flavoring agent, and the like, but is not limited thereto.

The cosmetically acceptable carrier contained in the cosmetic composition of the present invention varies depending on the formulation of the cosmetic composition.

When the formulations of the present invention are ointments, pastes, creams or gels, the carrier component may be an animal oil, a vegetable oil, a wax, a paraffin, a starch, a tracer, a cellulose derivative, polyethylene glycol, silicon, bentonite, silica, talc, zinc oxide May be used, but is not limited thereto. These may be used alone or in combination of two or more.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder and the like may be used as a carrier component. In particular, But are not limited to, propellants such as rocaborn, propane / butane or dimethyl ether. These may be used alone or in combination of two or more.

When the formulation of the present invention is a solution or an emulsion, a solvent, a dissolving agent or an emulsifying agent may be used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, Propylene glycol, 1,3-butyl glycol oil and the like can be used, and particularly fatty acid esters of cottonseed oil, peanut oil, corn oil, olive oil, castor oil and sesame oil, glycerol aliphatic ester, polyethylene glycol or sorbitan May be used, but is not limited thereto. These may be used alone or in combination of two or more.

When the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspension such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Crystalline cellulose, aluminum metahydroxide, bentonite, agar or tracant, but are not limited thereto. These may be used alone or in combination of two or more.

When the formulation of the present invention is a soap, an alkali metal salt of a fatty acid, a fatty acid hemiester salt, a fatty acid protein hydrolizate, isethionate, a lanolin derivative, an aliphatic alcohol, a vegetable oil, glycerol, But is not limited thereto. These may be used alone or in combination of two or more.

In yet another aspect, the invention provides a method of preventing or treating an allergic disease comprising administering to a subject other than a human, a composition comprising Lappaol A and a pharmaceutically acceptable salt thereof.

The term " individual " of the present invention may mean any animal, including a human, who is or may be at risk of developing an allergic disease. The animal may be, but is not limited to, a mammal such as a cow, a horse, a sheep, a pig, a goat, a camel, a nutrient, a dog, a cat,

The preventive or therapeutic method of the present invention may specifically include the step of administering the composition in a pharmaceutically effective amount to a subject suffering from or at risk of developing an allergic disease.

The term " administering " of the present invention means introducing the pharmaceutical composition of the present invention to a patient by any suitable method, and the administration route of the composition of the present invention may be administered orally or parenterally in various routes ≪ / RTI >

The composition comprising Lappaol A as an active ingredient of the present invention can be effectively used as a composition for preventing or treating an allergic disease since the inflammatory mediator and degranulation can be inhibited and the allergic reaction can be effectively inhibited at the level of signal transduction .

FIG. 1 is a graph illustrating the inhibitory effect of Lappaol A on mast cell degranulation. ** P <0.01 compared to IgE / DNP-HSA group. In this case, DNP-IgE (Dinitrophenyl-immunoglobulin E) and DNP-HSA (Dinitrophenyl-human serum albumin) means that the substance does not sensitize (+) or sensitize (+) mast cells.
FIG. 2 is a diagram showing cytotoxicity according to the concentration of Lappaol A. FIG. At this time, DNP-IgE and DNP-HSA mean (+) and (+) not sensitized (-) mast cells.
Figure 3 is a schematic illustration of the inhibitory effect of Lappaol A on the production of inflammatory mediators. * P <0.05, ** P <0.01 compared to IgE / DNP-HSA group. A is TNF-α, B is IL-4, C is LTC _4, and D is the expression level of PGD ₂ . At this time, DNP-IgE and DNP-HSA mean (+) and (+) not sensitized (-) mast cells.
FIG. 4 is a graph showing the inhibitory effect of Lappaol A on the arachidonic acid chain reaction.
Figure 5 is a schematic illustration of the efficacy of Lappaol A in the FcεRI signaling pathway. A is p-Syk, p-Lyn and p-Fyn, B is p-PLCγ1, p-PLCγ2 and p-PKCδ, C is the expression amount of p-ERK and p-Akt. At this time, β-Actin was used as a loading control.

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

Example  One. Lappaol  Of A Degranulation  Check inhibitory efficacy

In order to confirm the detergent inhibition effect of Lappaol A, allergic reactions of mast cells were induced. The allergic reaction induced mast cell-induced degranulation and led to the activation of β-hexosaminidase secreted by Lappaol A The efficacy was tested. Specifically, RBL-2H3 cells were plated in a 24-well plate at a concentration of 1 × 10 ⁵ cells / well, and the cells were treated with 100 units / mL penicillin, 100 μg / mL streptomycin and 5% The cells were cultured in MEM-α medium containing fetal serum overnight at 37 ° C, 5% CO2 and humidified conditions. After completion of the incubation, the cells were washed with 1 × PBS buffer and incubated with 0.1 μg / mL of DNP-IgE (Sigma, Co., Ltd) for 24 hours to sensitize the cells.

Lappaol A was added to each concentration and incubated for 1 hour. Then, 0.1 μg / mL of DNP-HSA (Dinitrophenyl-human serum albumin) (Sigma, Co., Ltd.) was added to induce hypersensitive reaction and incubated again for 4 hours . The supernatant was centrifuged at 17,000 g for 10 minutes at 4 ° C and the supernatant was stored at -80 ° C and thawed for analysis.

In order to measure the activity of? -Hexosaminidase secreted from the cells into the medium by the above method, 25 μl of the supernatant and 10 μl of 10 mM p-NAG (pH 4.5) prepared with 0.1 M sodium citrate buffer 4-Nitropheyl N-acetyl -? - D-glucosaminide) was added to a 96-well plate and cultured at 37 ° C. After 1 hour of incubation, the reaction was terminated with 0.1 M Na ₂ CO ₃ buffer (pH 10.0), and the amount of p-nitrophenol was measured by absorbance at 405 nm to determine the activity of β-hexosaminidase Respectively. Each result was expressed as the average value of three experiments.

As a result, as shown in FIG. 1, Lappaol A of the present invention was able to inhibit the secretion of? -Hexosaminidase from mast cells in a concentration-dependent manner, and the IC ₅₀ value was 131.3 μM. Especially, the extract of Lappaol A inhibited the secretion of β-hexosaminidase by 90% or more compared to the negative control at a concentration of 400 μM, indicating that Lappaol A inhibits allergic reaction by inhibiting degranulation of mast cells.

Example  2. Lappaol  A cytotoxicity

To confirm the cytotoxicity of Lappaol A, RBL-2H3 cells were divided into 96-well plates at a concentration of 1 × 10 ⁴ cells / well, and then MEM-α containing 5% (v / v) fetal bovine serum Lt; RTI ID = 0.0 &gt; 37 C &lt; / RTI &gt; for 12 hours. Cells cultured the following day were washed with 1 x PBS buffer and incubated with 50 ng / mL of DNP-IgE (Dinitrophenyl-immunoglobulin E; Sigma, Co., Ltd.) for 24 hours to sensitize the cells.

Lappaol A was added to the sensitized cells for an additional 1 hour, and then 10 μl of WST-1 reagent (Daeil Lab Service Co., Ltd.) and 10 μl of DNP-HSA (Sigma, Co.) were added. , Ltd.) was added at the same time and incubated again for 4 hours. The cell viability of mast cells was determined by measuring the absorbance at 450 nm using a micro-plate reader (Emax, Molecular Devices Inc., Sunnyvale, Calif., USA) to confirm cell viability.

As a result, as shown in Fig. 2, it was confirmed that Lappaol A did not show cytotoxicity.

Example  3. Lappaol  Inflammation of A Parameter  Check inhibitory efficacy

IL-4 (Interleukin 4), PGD ₂ (Prostaglandin D ₂ ), and LTC in the supernatant of allergic reaction-induced mast cells in the method of Example 1 to confirm the inhibitory effect of Lappaol A on inflammatory mediators ₄ (Leukotriene C ₄ ) was measured using an ELISA kit (e-Bioscience, Inc.) and an EIA kit (Cayman Chemical, Inc.).

As a result, as shown in Fig. 3, Lappaol A showed IC ₅₀ values of 59.50 μM, 11.58 μM, 10.99 μM and 17.85 μM for TNF-α, IL-4, PGD ₂ and LTC ₄ , The inhibitory effect of Lappaol A on the induction of allergic diseases by inflammatory reaction was confirmed by confirming that the generation of the mediator was inhibited in a concentration - dependent manner.

Example  4. Lappaol  A allergy-related mechanism inhibition efficacy

Example  4-1. Lappaol  Confirming the effect of A on the chain reaction of arachidonic acid

The arachidonic acid chain reaction is a reaction in which a physiologically active substance such as prostaglandin or leukotriene is produced from arachidonic acid, eicosapentaenoic acid or the like through an enzyme reaction mechanism, and the physiologically active substance is generated and closely related to allergic diseases.

Therefore, in order to confirm the arachidonic acid chain reaction inhibitory effect, the allergic reaction-induced mast cells of Example 1 were dissolved to extract total proteins, and the arachidonic acid chain reaction related proteins (p-cPLA ₂ , COX-2, p -5-LO, L-PGDS and LTC ₄ S) were quantitated by Western blotting. The antibody used for Western blotting was Cell signaling Technology, Inc. .

After a forward amount, as shown in Fig. 4, Lappaol A is arachidonic acid chain reaction-related protein, _{p-cPLA 2, COX-2} , p-5-LO, the concentration of L-PGDS and Expression of LTC ₄ S dependent , Respectively.

Example  4-2. Lappaol  Of A FcεRI  Confirmation of signal transduction inhibition efficacy

FcεRI is a high affinity IgE receptor and is known to mediate IgE-dependent allergen expression and induce allergic diseases.

Thus, in order to confirm the inhibitory effect of the FcεRI signal transduction mechanism, FcεRI signal transduction related proteins (p-Syk, p-Lyn, p-Fyn, p-PLCγ1, p- -PKC?, P-ERK, and p-Akt).

As a result, it was confirmed that Lappaol A inhibited the expression of p-Syk, p-Lyn, p-PLCγ1, p-PLCγ2, p-PKCδ p-ERK and p-Akt in a concentration- .

Through Example 4, we confirmed that Lappaol A inhibits allergic responses at cell signaling level by confirming allergic-related inhibition of Lappaol A.

Taken together, it can be seen from the above examples that Lappaol A inhibits the degranulation of mast cells as an index of allergic diseases, inhibits the production of inflammatory mediators, and inhibits the mechanism associated with allergic reactions , It was confirmed that it can be used as an antiallergic composition.

From the above description, it will be understood by those skilled in the art that the present invention may be embodied in other specific forms without departing from the spirit or essential characteristics thereof. In this regard, it should be understood that the embodiments described above are illustrative in all aspects and not restrictive. The scope of the present invention should be construed as being included in the scope of the present invention without departing from the scope of the present invention as defined by the appended claims.

Claims (7)

A pharmaceutical composition for the prevention or treatment of an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.
The pharmaceutical composition according to claim 1, wherein the allergic disease is any disease selected from the group consisting of allergic rhinitis, asthma, atopic dermatitis, and allergic conjunctivitis.
The pharmaceutical composition according to claim 1, wherein said Lappaol A inhibits degranulation inhibition, inhibition of inflammatory mediator production, inhibition of arachidonic acid chain reaction, or FcεRI signal transduction.
A health functional food for the prevention or amelioration of allergic diseases, including Lappaol A and its pharmaceutically acceptable salts.
A quasi-drug composition for preventing or ameliorating an allergic disease comprising Lappaol A and a pharmaceutically acceptable salt thereof.
A cosmetic composition for preventing or improving allergies comprising Lappaol A and a cosmetically acceptable salt thereof.
A method of preventing or treating an allergic disease comprising administering to a subject other than a human a composition comprising Lappaol A and a pharmaceutically acceptable salt thereof.

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