KR20180109156A - Composition for antiinflammatory and inflammatory neurodegenerative diseases comprising chaenomeles sinesis koehne extract - Google Patents

Abstract

The present invention relates to a composition for antiinflammatory and inflammatory neurodegenerative diseases comprising a Pseudocydonia sinensis extract.

Description

FIELD OF THE INVENTION The present invention relates to a composition for preventing or treating inflammatory and inflammatory neurodegenerative diseases, which comprises a mucilaginous extract and a composition for preventing or treating inflammatory and inflammatory neurodegenerative diseases,

The present invention relates to a composition for the prevention or treatment of anti-inflammatory and inflammatory neurodegenerative diseases,

 Chaenomelis Fructus is a mature fruit of Chaenomeles sinensis Koehne, a circular or elliptical fruit belonging to the rosacea that originated in China and is cultivated before the Goryeo Dynasty. It is ripe in yellow and smells yellow in September. The efficacy of the quince is well known as a coughing agent for colds and bronchitis, as an emollient for phlegm, and is known to be particularly good for rheumatism and pneumonia. In addition, quinceons are also used as fragrances because they are fragrant. However, in spite of these pharmacological functions, it has difficulty to be edible because its moisture content is low and its taste is strong compared with general fruit and stone cells and woody quality are developed and the meat quality is rough. There are many researches on processing of quince, but the experiment on functional efficacy is very few.

On the other hand, there are antioxidant enzymes that protect against reactive oxygen species in the body such as superoxide dismutase (SOD), glutathione peroxidase (GPX), catalase (CAT), glutathione reductase and glutathione-S- transferase. However, The role of antioxidants in the human body due to substances, smoking, stress, etc., exceeds the defense system, leading to protein degradation and DNA damage

Therefore, synthetic materials such as butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT) have been developed as antioxidants. However, studies on finding dietary antioxidants that are safe from nature have been actively carried out Become

Inflammation, on the other hand, is a defense mechanism to prevent damage to human tissues caused by infection, which involves symptoms such as development, fever and pain. If the inflammatory reaction is repeated for a long period of time, it can cause various chronic diseases such as neurodegenerative diseases and cancer.

Macrophages are involved in and regulate the production of inflammatory mediators such as nitric oxide (NO), prostaglandin (PG) and pro-inflammatory cytokines in the human immune response. These inflammatory mediators induce an inflammatory response and, if the host immune response does not respond appropriately, induce inflammatory diseases.

Korean Patent Laid-Open No. 10-2012-0011981 relates to a dermal extract having anti-inflammatory effect and a composition for external application for skin comprising the same, wherein the dermal extract is characterized in that the expression of hemeoxygenase-1 and sirtuin-1 And has an anti-inflammatory effect.

Korean Patent Publication No. 10-2012-0011981

The present invention aims to provide a composition for treating or preventing an inflammatory neurodegenerative disease.

The present invention also aims to provide an anti-inflammatory composition.

In order to achieve the above object,

The present invention provides a pharmaceutical composition for the prevention or treatment of inflammatory neurodegenerative diseases comprising an extract of a quinceae as an active ingredient.

In addition, the present invention provides a food composition for relieving inflammatory neurodegenerative diseases comprising an extract of Quinces herbicus as an active ingredient.

The present invention also provides a pharmaceutical composition for antiinflammation comprising a mucilaginous extract as an active ingredient.

The present invention also provides a functional food composition for anti-inflammation comprising an extract of Quinces herbicus as an active ingredient.

The present invention also provides a composition for antioxidation comprising an extract of Quinces herbicus as an active ingredient.

The present invention also provides a method for inhibiting the concentration of nitrogen monoxide produced in glial cells in vitro by treating an alcohol extract of a moss-extract with lipopolysaccharide-stimulated glial cells.

The composition comprising the extract of the present invention as a active ingredient can completely weaken LPS-induced NO production in BV-2 cells.

Therefore, the composition comprising the extract of the present invention as an active ingredient can be used as an anti-inflammatory agent and a therapeutic agent for neurodegenerative diseases.

Fig. 1 is a graph showing the DPPH inhibitory activity of the moss-containing extract.
2 is a graph showing the cell survival rate of the mucilage extract.
Fig. 3 is a graph showing inhibition of nitrogen monoxide (NO) production of the extract of the quinine extract.

Hereinafter, the present invention will be described in more detail.

The present invention relates to a pharmaceutical composition for the prophylaxis or treatment of inflammatory neurodegenerative diseases, which comprises an extract of a quinceaceptin as an active ingredient.

In one embodiment of the present invention, the composition is preferably but not limited to weaken nitrogen monoxide (NO) production.

In another embodiment of the present invention, the extraction solvent of the extract is preferably an alcohol, and most preferably, ethanol is not limited thereto.

In another embodiment of the present invention, the composition preferably inhibits microglial cell activity in microglial cells, but is not limited thereto.

The present invention also relates to a pharmaceutical composition for antiinflammation comprising an extract of Quinces herbaceousum as an active ingredient.

In one embodiment of the present invention, the composition is preferably but not limited to weaken inductive nitrogen monoxide (NO) production.

In another embodiment of the present invention, the extraction solvent of the extract is preferably an alcohol, and most preferably, ethanol is not limited thereto.

In another embodiment of the present invention, the composition preferably inhibits microglial cell activity in microglial cells, but is not limited thereto.

The pharmaceutical composition for the prevention or treatment of inflammatory neurodegenerative diseases and the pharmaceutical composition for anti-inflammation may be prepared by using pharmaceutically acceptable and physiologically acceptable adjuvants in addition to the above-mentioned active ingredients. Examples of the adjuvants include excipients, A sweetener, a binder, a coating agent, a swelling agent, a lubricant, a lubricant or a flavoring agent.

The pharmaceutical composition may be formulated into a pharmaceutical composition containing at least one pharmaceutically acceptable carrier in addition to the above-described active ingredients for administration.

The pharmaceutical composition may be in the form of granules, powders, tablets, coated tablets, capsules, suppositories, liquids, syrups, juices, suspensions, emulsions, drops or injectable solutions. For example, for formulation into tablets or capsules, the active ingredient may be combined with an oral, non-toxic pharmaceutically acceptable inert carrier such as ethanol, glycerol, water, and the like. Also, if desired or necessary, suitable binders, lubricants, disintegrants and coloring agents may also be included as a mixture. Suitable binders include, but are not limited to, natural sugars such as starch, gelatin, glucose or beta-lactose, natural and synthetic gums such as corn sweeteners, acacia, tracker candles or sodium oleate, sodium stearate, magnesium stearate, sodium Benzoate, sodium acetate, sodium chloride, and the like. Disintegrants include, but are not limited to, starch, methyl cellulose, agar, bentonite, xanthan gum and the like. Acceptable pharmaceutical carriers for compositions that are formulated into a liquid solution include sterile solutions suitable for the living body such as saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, dextrose solution, maltodextrin solution, glycerol, One or more of these components may be mixed and used. If necessary, other conventional additives such as an antioxidant, a buffer, and a bacteriostatic agent may be added. In addition, diluents, dispersants, surfactants, binders, and lubricants may be additionally added to formulate into injectable solutions, pills, capsules, granules or tablets such as aqueous solutions, suspensions, emulsions and the like. Further, it can be suitably formulated according to each disease or ingredient, using the method disclosed in Remington's Pharmaceutical Science, Mack Publishing Company, Easton PA as an appropriate method in the field.

The present invention also provides a method of preventing or treating an inflammatory neurodegenerative or anti-inflammatory disease comprising administering a therapeutically effective amount of a quince extract to an experimental subject, excluding a human.

It is preferable that the subject to be tested is a mammal to be treated or observed.

As used herein, the term "therapeutically effective amount " refers to the amount of active ingredient or pharmaceutical composition that induces a biological or medical response in a tissue system, animal or human, as contemplated by a researcher, veterinarian, This includes an amount that induces relief of the symptoms of the disease or disorder being treated. It will be apparent to those skilled in the art that the therapeutically effective dose and the number of administrations of the active ingredient of the present invention will vary depending on the desired effect. Thus, the optimal dosage to be administered can be readily determined by those skilled in the art and will vary with the nature of the disease, the severity of the disease, the amount of active and other ingredients contained in the composition, the type of formulation, and the age, The age, body weight, sex, diet, time of administration, route of administration and fraction of the composition, duration of treatment, concurrent medication, and the like.

The dose of the mosquito extract as an active ingredient in the pharmaceutical composition of the present invention may be 6 to 30 mL per kg of body weight once or three times a day depending on the patient's age, sex, symptom, method of administration, or prevention purpose . Dosage levels for patients exhibiting the specific symptoms may vary depending on the patient's body weight, age, sex, health condition, diet, time of administration, administration method, excretion rate, severity of disease, and the like.

In the therapeutic method of the present invention, the composition comprising the extract of the present invention as an active ingredient may be administered orally, rectally, intravenously, intraarterally, intraperitoneally, intramuscularly, intrasternally, transdermally, topically, Lt; / RTI >

In addition, the present invention relates to a food composition for relieving inflammatory neurodegenerative diseases comprising an extract of Quinces herbicus as an active ingredient.

In addition, the present invention relates to a functional food composition for anti-inflammation comprising an extract of mucilagia as an active ingredient.

The food composition of the present invention can be formulated and used as a functional food functionalized with a food composition for relieving inflammatory neurodegenerative diseases or as a functional food composition for antiinflammation, or can be added to various foods.

The form of the preparation may be formulated in the same manner as the pharmaceutical composition and used as a functional food or may be added to various foods.

Examples of foods to which the food composition for relieving inflammatory neurodegenerative diseases or the functional food composition for anti-inflammation of the present invention can be added include foods, beverages, meat, chocolates, foods, confections, pizza, ramen, Ice cream, alcoholic beverages, vitamin complexes, and health supplement foods.

The present invention also relates to a composition for antioxidation comprising an extract of Quinces herbicus as an active ingredient.

The present invention also relates to a method for inhibiting the concentration of nitric oxide produced in glial cells in vitro by treating an alcohol extract of a moth extract with lipopolysaccharide-stimulated gliocyte.

The alcohol is preferably ethanol, and the effective amount of the extract is preferably 10 to 100 μg / mL.

Hereinafter, the present invention will be described in more detail with reference to Examples. It is to be understood by those skilled in the art that these examples are for illustrative purposes only and that the scope of the present invention is not construed as being limited by these examples.

Example  1. Production of quince extract

The extract was extracted with ethanol (100 g) and ethanol (1 L) at room temperature for 72 hours.

Experimental Example 1. The extract of quince extract  Antioxidant capacity measurement

The DPPH radical scavenging activity of the herbal extract prepared in Example 1 was measured.

30 μL of the above-described extracts of corn extract and 30 μL of a 60 μM DPPH solution dissolved in ethanol were added to each well and allowed to react at room temperature for 2 minutes, and then transferred to a capillary tube and measured by electron spin resonance (ESR) spectrometer (JES-PX 2300, JEOL, Japan). At this time, the measurement conditions of the ESR spectrophotometer were 336.5 ± 5 mT for the magnetic field, 5 mW for the microwave power, and 9.41 GHz for the modulation frequency.

The DPPH free radical scavenging activity (%) for the antioxidant sample was calculated by the following equation (1), and the DPPH free radical scavenging activity according to the concentration of the seed extract was shown in FIG.

[Equation 1]

ESR signal intensity for the control medium)

The extracts of mosses showed the antioxidative effect because they reduce the concentration - dependent signal.

Experimental Example  2. Measurement of cell survival rate

To investigate the effect of LPS (lipopolysaccharide) and extracts of LPS on cell survival in BV-2 cells stimulated with LPS, cell biability was measured using 3- [4,5-Dimethylthiazol-2-yl] -2,5-diphenyl-tetrazolium bromide (MTT) assay.

Cells (1 × 10 ⁵ cells / ml) were seeded on a 96-well plate in a volume of 180 μL and cultured in a CO ₂ incubator for 12 hours or longer. After culturing, the culture medium was removed and 200 μL of medium containing 0.5 mg / mL MTT was added, followed by incubation for 4 hours to allow MTT reduction. After removing the culture medium, 100 μL of dimethylsulfoxide (DMSO) was added and the resulting formazone crystals were dissolved. The absorbance was measured at 540 nm using an ELISA reader, and the cell viability was expressed as a percentage (%) as compared with the control .

The cell survival rate can be determined by examining the number of cells having an activity and measuring the intracellular toxicity of the extract.

As a result, it was confirmed that the cell survival rate did not change in all experimental groups treated with LPS and moss-extract alone or in the same manner (FIG. 2). This means that inflammation inducers, LPS and mosses extract, do not affect cell survival.

Experimental Example  4. By LPS  Concentration-dependent inhibition of NO production of moth extracts in activated glial cells

In order to analyze the anti - inflammatory effects of the extracts, we examined the effect of LPS, an inflammation - inducing factor, on the concentration of nitric oxide (NO) produced in stimulated gliomas.

The NO concentration was determined by seeding 5 × 10 ⁵ cells / well in a 24-well plate, adding LPS and extracts at different concentrations, reacting in an incubator for 24 hours, and then adding 50 μL each of Griess reagent (1% sulfanilamide / 0.1% N- (1-naphthyl) -ethylenediamine dihydrochloride / 2.5% H ₃ PO ₄ ) and the value was measured using a Sunrise basic 96-well microplate spectrophotometer (TECAN AUSTRIA) with a wavelength of 540 nm.

The amount of NO induced by LPS (100 ng / mL) in the glial cells was about 20 μM, which was about 10 times higher than that of the control group 2 μM. The experimental group treated with the extracts of 10, 25, 50 and 100 μg / As a result, it was confirmed that the production of NO decreased in a concentration-dependent manner in the extract of corn (Fig. 3).

Claims (12)

A pharmaceutical composition for the prevention or treatment of inflammatory neurodegenerative diseases, comprising an extract of mosses as an active ingredient. The pharmaceutical composition according to claim 1, wherein the composition weakens nitrogen monoxide (NO) production. [Claim 2] The pharmaceutical composition according to claim 1, wherein the extracting solvent of the extract is an alcohol. The pharmaceutical composition for preventing or treating inflammatory neurodegenerative diseases according to claim 1, wherein the composition inhibits microglial cell activity in microglial cells. A food composition for relieving inflammatory neurodegenerative diseases, comprising a mucilaginous extract as an active ingredient. The food composition according to claim 5, wherein the food is beverage, jelly, candy, gum or dairy product. A pharmaceutical composition for antiinflammatory activity, comprising a mucilaginous extract as an active ingredient. 8. The pharmaceutical composition according to claim 7, wherein the composition weakens nitrogen monoxide (NO) production. A functional food composition for antiinflammatory activity, comprising an extract of mosses as an active ingredient. A composition for antioxidation comprising an extract of mosses as an active ingredient. A method of inhibiting the concentration of nitric oxide produced in glial cells in vitro by treating alcohol extracts of mosquito extract with lipopolysaccharide-stimulated glial cells. The method according to claim 11, wherein the effective amount of the extract of the quince extract is 10 to 100 μg / mL.

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