KR20160098568A - COMPOSITION COMPRISING EXTRACT OF Quamoclit angulata HAVING ANTI-INFLAMMATORY ACTIVITY - Google Patents
COMPOSITION COMPRISING EXTRACT OF Quamoclit angulata HAVING ANTI-INFLAMMATORY ACTIVITY Download PDFInfo
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- KR20160098568A KR20160098568A KR1020150019380A KR20150019380A KR20160098568A KR 20160098568 A KR20160098568 A KR 20160098568A KR 1020150019380 A KR1020150019380 A KR 1020150019380A KR 20150019380 A KR20150019380 A KR 20150019380A KR 20160098568 A KR20160098568 A KR 20160098568A
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- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/39—Convolvulaceae (Morning-glory family), e.g. bindweed
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/324—Foods, ingredients or supplements having a functional effect on health having an effect on the immune system
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Abstract
Description
The present invention relates to an antiinflammatory pharmaceutical composition and a food composition containing a Quamoclit angulata extract.
Inflammation is one of the defenses of the body against physical stimuli, chemical stimuli, bacterial infections, etc. It is one of the mechanisms to remove external substances and regenerate damaged areas. Once an inflammation-related stimulus is applied, vasoactive substances such as histamine, serotonine, bradykinin, prostaglandin, hydroxyeicosatetraenoic acid (HETE), leukotriene And the vascular permeability is increased to cause inflammation.
Monocytes are transformed into macrophages that are activated by bacterial infection and act as phagocytic cells. Macrophages induce inflammation by secretion of NO, prostaglandin E2, and proinflammatory cytokines, and regulatory cells important in both inflammation and immune response In order for macrophages to function in this way, they must undergo an activation process.
LPS (lipopolysaccharide), one of the cell wall components of Gram-negative bacteria and well known as endotoxin, is the most well-known external factor involved in macrophage activation. Particularly, in monocytes and macrophages such as RAW 264.7 cells, proinflammatory cytokines such as TNF-α, IL-6 (interleukin-6) and IL-1β (interleukin- -inflammatory cytokine secreted by LPS (lipopolysaccharide) in the inflamed area.
When LPS stimulates macrophages, nitric oxide (NO) is produced in the process of converting L-arginine into L-citrulline by an enzyme called iNOS (inducible nitric oxide synthase) Phagocytes produce NO.
In mammals, NO is synthesized by three kinds of NO synthase (NOS): nNOS (neuronal NOS), eNOS (endothelial NOS) and iNOS (inducible NOS). Among these, NO produced by nNOS and eNOS is produced for normal biological function, and the concentration in tissues is kept low to a certain level. However, the amount of NO produced by iNOS is excessively high, and it is harmful to living organisms such as pathological vasodilation, cytotoxicity and tissue damage. In addition, prostaglandin E2 (PGE2), an inflammatory factor, stimulates phospholipid, which is a constituent of cell membrane, stimulated by LPS, and arachidonic acid liberated by an enzyme called phospholipase A2 causes catalytic action of an enzyme called COXs (cyclooxygenase) And is induced to induce an inflammatory reaction.
COX is classified as COX-1 and COX-2. COX-1 acts on normal biological functions such as platelet formation, gastric wall protection and maintenance of renal function in the body. COX-2 synthesizes PHE2 as an inflammatory mediator. PHE2 is known to be deeply involved in the development of cancer, such as promoting inflammation (pain, fever, etc.), immune response, and angiogenesis. Inhibition of iNOS is mostly due to its mechanism of action being linked to inhibitors of COXs. Therefore, iNOS inhibition materials that are relatively easy to search are discovered and developed as anti-inflammatory materials.
On the other hand, non-steroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors, have anti-inflammatory, antipyretic and analgesic effects. However, the long-term use of these drugs can sometimes lead to serious side effects. For example, secondary anemia due to gastrointestinal peptic ulcer bleeding, platelet function suppression, inhibition of induction of labor, side effects to the kidney, liver damage, hypersensitivity.
In order to overcome the side effects of these drugs, natural products such as plants are more preferable as a safer material. In this regard, researches are being actively carried out to find and use the anti-inflammatory materials in natural products.
Quamoclit angulata , an annual plant of Convolvulaceae , is a native plant of tropical Americas and cultivated for ornamental purposes. No studies have been reported on the anti-inflammatory effect of this plant.
It is an object of the present invention to provide a composition containing a plant extract having excellent antiinflammatory activity, and it has been confirmed that a component extracted from Quamoclit angulata has an inhibitory effect on inflammatory factor expression, And to provide a food composition.
In order to achieve the above object, the pharmaceutical composition of anti-inflammatory activity according to one embodiment of the present invention contains Quamoclit angulata extract.
The above-mentioned Curly Leaf Root Extract may be one selected from the group consisting of alcohols having 1 to 5 carbon atoms, hexane, chloroform, alcohol, water, and mixtures thereof, and may be extracted by cold precipitation.
The above-mentioned Curly Leaf Root Extract is obtained by extracting 1 to 5 times by adding a solvent having a dry weight of 3 to 20 times by weight to a dry powder of Curly Leaf Leaf, and extracting it at an extraction temperature of 20 to 120 캜 for 30 minutes to 10 days An extract or a powder from which the solvent has been removed from the extract.
The food composition according to another embodiment of the present invention contains an extract of Quamoclit angulata and has an anti-inflammatory function. The food composition has antibacterial activity and can be used as a food composition in the form of a health functional food, a nutritional supplement, a health food, or a food additive.
Hereinafter, the present invention will be described in more detail.
The anti-inflammatory composition according to one embodiment of the present invention contains a Quamoclit angulata extract.
The above-mentioned Curly Leaf Root Extract may be obtained by extracting Curd Leaf Leaf, drying and crushing and pulverizing. The above-mentioned dried and pulverized curd leaves may be leaves, stems, roots, flowers, fruits, mixtures or outbreaks of the curd leaf, and the drying may be carried out in such a range that the useful components in the collected curd leaves are not destroyed It can be carried out by a known method, for example, by a method of natural drying in shade. In addition, it is preferable that the above-mentioned crushing is carried out after crushing to such an extent that the useful components of the curd leaf can be sufficiently extracted in the subsequent extraction process and pulverized. The drying and crushing steps may be carried out in reverse order or repeatedly as required.
The extraction may be carried out by, for example, hot water extraction, cold extraction, warming extraction, reflux cooling extraction, ultrasonic extraction, or the like, preferably by a cold extraction method.
The extraction is carried out using a solvent, which may be an alcohol of 1 to 5 carbon atoms, hexane, chloroform, alcohol, water and mixtures thereof, preferably water, methanol, ethanol, .
The extraction is carried out at a temperature of 20 to 100 ° C, preferably 20 to 70 ° C, for 30 to 10 minutes, preferably 3 to 20 times, preferably 3 to 10 times, Day, or 1 to 2 days of extraction time, and it is preferable to use a method of preparing a curd leaf foliage comprising 1 to 5 times, preferably 2 to 3 times, Followed by continuous extraction to obtain a liquid-phase extract.
The above-mentioned liquid-phase curly leaf extract can be subjected to a process such as concentration filtration or drying after separating it from the foliage of the curly leaf by a method such as reduced pressure filtration. For example, the above-mentioned liquid phase curly leaf extract can be concentrated in a vacuum rotary condenser at 20 to 100 ° C, preferably at 40 to 70 ° C, and the liquid phase curd leaf extract is dried to obtain powdered You can also obtain a Curly Leaf Root Extract. The thus-concentrated or powdered Curly Leaf Root Extract can be used as needed in water, alcohol or a mixed solvent thereof.
In addition, the above-mentioned liquid round-rooted hwangchongcho extract, its concentrate or its powder may be an extract obtained by fractionation with nucleic acid or ethyl acetate or fractionation of the fraction.
The above-mentioned Curly Leaf Root Leaf Extract inhibits the expression of iNOS, an inflammation mediator, and inhibits the expression of NO produced by this enzyme, thereby providing a pharmaceutical composition of anti-inflammatory activity containing components useful for prevention and treatment of inflammation-related diseases And can be used as a pharmaceutical composition for the prevention or treatment of inflammatory diseases, and provides a pharmaceutical composition for preventing or treating inflammation caused by infection from external bacteria.
The anti-inflammatory composition may further comprise additional components and may further comprise at least one of, for example, a carrier, excipient, and diluent, for example, lactose, dextrose, sucrose, sorbitol, But are not limited to, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate Tartrate, magnesium stearate, and mineral oil.
The antiinflammatory composition may have various formulations and may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, external preparations such as syrups and aerosols, have. In the case of formulation, it can be prepared using diluents or excipients such as fillers, extenders, binders, humectants, disintegrants, surfactants and the like which are usually used, and the preparations for non-oral administration include sterilized aqueous solutions, Emulsions, freeze-dried preparations, suppositories. Examples of the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. Examples of the suppository base include withexol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.
The preferred dosage of the anti-inflammatory composition may be appropriately selected depending on the condition and body weight of the patient, the degree of disease, the form of the drug, the route of administration and the period of time. However, for the desired anti-inflammatory effect, the extract or the compound of the present invention can be administered in an amount of 0.01 to 500 mg / kg per day, preferably 0.1 to 200 mg / kg per day, divided once to several times per day. The dose of the compound may also be increased or decreased depending on the route of administration, degree of disease, sex, weight, age, and the like.
The food composition according to another embodiment of the present invention contains an extract of Quamoclit angulata and has an anti-inflammatory function and is used as a food composition in the form of a health functional food, a nutritional supplement, a health food, or a food additive Can be utilized.
Food compositions of this type can be prepared in a variety of forms according to conventional methods. For example, the health food may be prepared by lyophilization, granulation, encapsulation and pulverization so as to be prepared in the form of tea, juice and drink, and then drinking the same. In addition, it can be prepared in the form of a composition by mixing together the above-mentioned Curly Leaf Root Extract and a known active ingredient known to have anti-inflammatory effect. Functional foods also include, but are not limited to, beverages (including alcoholic beverages), fruits and processed foods such as canned fruits, jars, jam, maare marlade, fish, meat and processed foods (Eg butter, cheeses, etc.), edible vegetable oils (eg, sourdoughs, etc.), breads and noodles (eg udon, buckwheat noodles, ramen noodles, spaghetti, macaroni, , Margarine, vegetable protein, retort food, frozen food, various kinds of seasoning (e.g., soybean paste, soy sauce, sauce, etc.). The preferred content of the Curly Leaf-Root Extract in the food composition is not particularly limited, but is preferably 0.01 to 50% by weight in the finally prepared food.
The anti-inflammatory composition and the food composition of the present invention contain Quamoclit angulata extract and have an inflammatory factor expression inhibiting activity and are useful as a pharmaceutical composition or a functional food composition.
FIG. 1 shows the results of evaluation of the amount of NO produced from the samples treated with the extract of Curcuma longa root, prepared in Example 1 of the present invention.
FIG. 2 shows the results of evaluating iNOS activity by samples obtained from the samples treated with the extract of Curly Leaf Root Prepared in Example 1 of the present invention, and evaluating the iNOS inhibitory effect of the extracts according to their concentrations.
Hereinafter, embodiments of the present invention will be described in detail with reference to the accompanying drawings so that those skilled in the art can easily carry out the present invention. The present invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein.
Example 1: Curly leaf foliage ( Quamoclit angulata ) Preparation of extract
The outposts of Quamoclit angulate, which is native to Korea, were collected, dried in a well-ventilated shade, and then dried to a size of 20 mesh or less.
1 g of ethanol was added to 100 g of the dry powder of the mouth, and the mixture was cooled at room temperature for 7 days at room temperature for 7 days. The mixture was extracted three times repeatedly and filtered through a filter paper (Wattsman, USA) to obtain a filtered extract. The filtrate was subjected to removal of ethanol at 40 ° C by using a vacuum rotary condenser to obtain 12 to 20 g of a round-mouth yuchongcho extract residue. 10 mg of the sample was used as a sample for the detection of the anti-inflammatory activity.
Example 2: Anti-inflammatory activity of the extract of Curcuma pseudo-acacia var.
The anti - inflammatory effect of the extract of Curcuma longa root was confirmed by measuring the amount of NO and using iNOS (inducible nitric oxide synthase) assay.
RAW 264.7 cells were inoculated into a 24-well plate at a density of 10 x 10 cells / well using DMEM medium and cultured for 12 hours. The RAW 264.7 cells were cultured in the same manner as in Example 1, / ml and LPS (1? / ml) at the same time, and cultured for 24 hours. From the cultured samples, the amount of NO 2 - present in the cell culture was measured using a Griess reagent, and the amount of NO produced and iNOS activity were measured. Specifically, 500 μl of the cell culture supernatant of the above cultured samples and 50 μl of a grease reagent (2.5% sulfanilamide, 0.25% naphthylethylenediamine dissolved in 10% phosphoric acid) were mixed and reacted on a 24-well plate for 10 minutes Absorbance was measured at 540 nm using an ELISA reader. The standard concentration curve was obtained by serial dilution of DMSO, and the amount of produced NO and the activity of iNOS were evaluated. The results are shown in FIGS. 1 and 2. As a positive control, aspirin was applied.
Referring to FIG. 1, it can be confirmed that the extract of Curcuma pseudo-acacia L. leaves effectively inhibited the production of NO in RAW 264.7 c cells induced by LPS. As a result, It is also confirmed that it is dependent.
NO is synthesized from L-arginine by nitric oxide synthase (NOS). Under pathologic conditions, increased NO promotes the development of inflammation, which is synthesized by iNOS, a synergistic agent with other inflammatory mediators. In addition, iNOS is strongly stimulated by exposure to inflammatory cytokines and bacterial endotoxins. Therefore, a substance capable of reducing NO production by iNOS can be utilized as an anti-inflammatory agent.
In addition, referring to FIG. 2, it was confirmed that the extract of R. leucocyte showed an inhibitory effect on iNOS in RAW 264.7 cells induced by LPS, and that it was dose-dependent overall, except for 20 ug / ml.
NO produced by activated iNOS in inflammatory conditions has deleterious effects on the organism such as pathological vasodilation, cytotoxicity, and tissue damage. The effect of LPS treatment on RAW 264.7 on the NO production of the leaf currant leaf showed a strong inhibitory effect. The positive control (Aspirin, 100 μg / ml) effectively inhibited the activity of iNOS.
The above-mentioned Curcuma longa root extract showed a concentration-dependent reduction of LPS-induced NOS production, and it was confirmed that the Curcuma longa root extract showed a strong inhibitory effect on iNOS protein expression in RAW 264.7 cells induced by LPS .
While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the invention is not limited to the disclosed exemplary embodiments, Of the right.
Claims (4)
Wherein the curd leaf is at least one selected from the group consisting of alcohols having 1 to 5 carbon atoms, hexane, chloroform, alcohol, water, and mixtures thereof, and is extracted by cold precipitation.
The above-mentioned Curly Leaf Root Extract is obtained by extracting 1 to 5 times by adding a solvent having a dry weight of 3 to 20 times by weight to a dry powder of Curly Leaf Leaf, and extracting it at an extraction temperature of 20 to 120 캜 for 30 minutes to 10 days An extract or a powder from which the solvent is removed from the extract.
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