KR20180036024A - A composition comprising Sauropus spatulifolius Beille extracts having anti-inflammation activity - Google Patents

Abstract

The present invention relates to a composition comprising a Sauropus spatulifolius beille extract having anti-inflammation activity, and more specifically, to an anti-inflammatory cosmetic composition, an anti-inflammatory pharmaceutical composition, and an anti-inflammatory food composition, which comprise the Sauropus spatulifolius beille extract. The Sauropus spatulifolius beille extract of the present invention inhibits the production and secretion of inflammatory mediators such as NO and TNF-α, which are involved in an inflammatory reaction, and thus the composition comprising the extract as a raw material can effectively inhibit inflammation. Accordingly, the anti-inflammatory composition comprising the extract as an active ingredient can be applied as an anti-inflammatory agent for inhibiting inflammation in inflammation-related diseases and a pharmaceutical composition, a cosmetic composition, a health food composition and the like having an anti-inflammatory effect.

Description

A composition comprising Sauropus spatulifolius Beille extracts having anti-inflammation activity,

The present invention relates to a composition comprising an extract of Saulopus sp. Lipolius having an anti-inflammatory activity, and more particularly to a composition comprising an extract of Saulopus sp. To Lipolarius, an anti-inflammatory cosmetic composition, Inflammatory health food composition.

Skin is an organs covering the entire surface of the body. It protects the human body from the external environment and stimulation, and suppresses evaporation of water in the body. Therefore, the skin is exposed directly to the external environment.

The activity of the cells constituting the skin and the skin protecting ability against the external infectious diseases are reduced as the ozone layer breaks up, the ultraviolet rays reaching the surface, the weakening of the immunity due to the stress, and the exposure to pollution sources such as toxic chemicals are increased.

As a result, the skin is sensitive to external stimuli, and skin troubles such as erythema, edema, itching, and inflammatory reaction are induced. In addition, the substances produced during the inflammatory reaction cause skin pigmentation, skin elastic fibers and collagen fibers to collapse, thus affecting the increase of skin wrinkles.

Inflammation is one of physiological defense reactions of biological tissues to external stimuli. Clinically, symptoms such as fever, fever, swelling, pain, and dysfunction are observed. This is caused by intrusion of external foreign substances such as bacteria and mechanical damage To protect the skin from the physiological mechanism. Various inflammatory mediators activate oxidant production and reduce tissue antioxidant capacity, thus impairing the basic metabolic structural factors of the tissue and causing toxicity. Oxidation in these various cells and tissues produces a unique oxidant, A secondary tissue reaction of reactive oxygen species begins.

Specifically, when an inflammatory reaction occurs, various inflammatory factors are produced. Macrophages play an important role in various inflammatory responses, and activated macrophages have been reported to secrete inflammatory cytokines, NO, proteases, and the like. Lipopolysaccharide (LPS) is a lipopolysaccharide that constitutes the outer membrane of Gram-negative bacteria and induces a variety of inflammatory cytokines and causes an inflammatory reaction. When inflammatory stimulation is initiated by LPS, TLR4 undergoes LPS signaling and NF-kB in the cytoplasm undergoes phosphorylation of ubiquitin-mediated protein degradation upon binding of I-kB to the inhibitory subunit I-kB. NF-kB, which is free from I-kB, migrates into the nucleus and induces the inducible nitric oxide synthase (iNOS), cyclooxygenase (COX-2), tumor necrosis And activates genes such as tumor necrosis factor-α, TNF-α and the like. NO is synthesized by three types of NOS: neuronal NOS (nNOS), endothelial NOS (eNOS), and iNOS. Although nNOS and eNOS are always present in cells, iNOS is expressed only when exposed to interferon-γ (IFN-γ), LPS and various inflammatory cytokines. Excessive NO production causes inflammation leading to tissue damage, gene mutations, and nerve damage. TNF-α is produced by activated macrophages, fibroblasts and various other cells. It is a cell active substance that mediates the pathophysiological responses of various diseases. It is essential for biological defense, and is known as an inflammatory mediator that causes various inflammatory diseases when secreted in large amounts have. In the presence of a large amount of LPS, TNF-α is excessively produced, leading to damage to the tissue, systemic vascular clotting, endotoxic shock, and the like. Excessive production of inflammatory mediators such as NO and TNF-alpha causes excessive immune responses, thereby causing various inflammatory diseases to deteriorate. Accordingly, it is important to inhibit the excessive production of inflammatory mediators such as NO, COX-2, and TNF-a for the treatment of inflammatory diseases.

For example, Korean Patent Laid-Open No. 10-2015-0105903, as a natural herbicide for treating inflammation, has found that an extract of Gossypia ganicum reduces the expression of inflammatory cytokines IL-6, TNF-α and IL-1β and inhibits ERK phosphorylation And suppresses the expression of NF-κB and effectively suppresses the inflammatory reaction of the skin, thereby decreasing the epithelial spasm or epidermal edema of the skin. Thus, it has been disclosed that there is an excellent effect for preventing, improving or treating inflammatory skin diseases .

Korean Patent Publication No. 10-2015-0105903

The present inventors have made intensive studies on natural ingredients that have anti-inflammatory activity and are less likely to cause side effects, and as a result, the extract of Saulopus sp. Lipolius exhibits an anti-inflammatory activity, and a composition containing it as an effective ingredient The present invention can be applied to a pharmaceutical composition, a cosmetic composition, a health food composition, and the like that have anti-inflammatory and anti-inflammatory effects for suppressing inflammation in diseases.

The object of the present invention is to provide a plant extract capable of inhibiting the production and secretion of inflammatory mediators such as NO and TNF-alpha which are not only safe from side effects such as natural plants, As an active ingredient, an anti-inflammatory composition.

In order to achieve the above object, the present invention provides a pharmaceutical composition for antiinflammation, which comprises an extract of Sauropus spatulifolius Beille as an active ingredient.

The present invention also relates to the use of the Sauropus sp. spatulifolius Beille) extract as an active ingredient.

The present invention also relates to the use of the Sauropus sp. spatulifolius Beille) extract as an active ingredient.

The Sauropus sp. Spatulifolius Beille) extract inhibits the production and secretion of inflammatory mediators such as NO and TNF-α which are involved in the inflammatory reaction, and thus the composition can effectively inhibit inflammation as a raw material. Therefore, the anti-inflammatory composition Can be applied as an anti-inflammatory agent for suppressing inflammation in diseases related to inflammation and a pharmaceutical composition having anti-inflammatory effect, a cosmetic composition, a food composition and the like.

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

Sauropus Spaulipolius ( Sauropus) spatulifolius beille) is a 10 ~ 40 ㎝ high shrub with a foxtail neck. The leaf is gathered on the upper part of a cylindrical stem of 2 ~ 5 mm diameter. The leaf is ovate of 4.5 ~ 16.5 ㎝ length and 2.5 ~ 6.5 ㎝ width. There is a red or purple flower in the middle or lower part of the branch in July to September. It grows naturally in Guangdong province of China.

In the present invention, the SD in crispus SPA-to-lipoic Julius (Sauropus spatulifolius Beille) extract is that obtained by extraction from various organs or in part, by Southern crispus SPA-to-lipoic Julius (Sauropus spatulifolius beille), leaves, flowers, stems, branches, roots, outposts and fruits. Preferably leaves or stems are used.

The extract of Sauropus spatulifolius Beille used as a raw material in the present invention can be obtained by extracting the leach solution obtained by leaching from the Sauropus spatulifolius Beille or transferring the leach solution partially or totally , Or an extract obtained by drying the concentrate again and a chemical substance itself exhibiting the main effect contained in the extract.

The extract of the present invention can be produced by a conventional method known in the art, that is, by using a conventional solvent, such as a commonly used method such as cold-water treatment, reflux cooling, hot water extraction, room temperature extraction, warm- Extraction, and the like.

Specific examples thereof include purified water, alcohols having 1 to 6 carbon atoms, glycerin, alkylene glycols having 2 to 6 carbon atoms, alkanes having 1 to 6 carbon atoms, halogenated hydrocarbons having 1 to 6 carbon atoms, alkylalkanoates having 2 to 6 carbon atoms, and mixtures thereof Can be used. More specifically, extraction solvents selected from purified water, methanol, ethanol, 1,2-propanediol, glycerin, ethylene glycol, butylene glycol, propylene glycol, dichloromethane, dichloroethane, hexane, ethyl acetate and mixtures thereof .

In this case, the amount of the extraction solvent used is 5 to 30 times the volume of the raw material, more preferably 5 to 20 times.

The extraction temperature can be varied by a person skilled in the art in a variety of temperature ranges suitable for the extraction method, for example, but not limited to, from 20 캜 to 100 캜. In addition, the extraction time differs depending on the extraction method, and a person skilled in the art can adopt an appropriate extraction time, and can be performed in a single or multiple cycles within a range of about 1 hour to several days, though not limited thereto. The extract obtained by performing the extraction with the primary extraction solvent may be obtained in the form of a liquid in which impurities are removed by filtration according to a conventional method, or the obtained liquid form extract may be concentrated under reduced pressure and / Can be obtained.

In the present invention, anti-inflammatory function of Sauropus spatulifolius Beille as a material for healthy skin was examined, and anti-inflammatory function was measured for the change of inflammatory mediator. The changes of nitric oxide (NO) and tumor necrosis factor (TNF-α) were measured at the cellular level as the inflammatory mediator through Experimental Example 1 and Experimental Example 2, ( Sauropus spatulifolius Beille) extracts inhibited the production of nitric oxide and tumor necrosis factor.

From these results, it can be seen that Sauropus spatulifolius Beille is applied to a pharmaceutical composition, a cosmetic composition or a health food composition so as to alleviate inflammation, improve the healing effect, and treat a disease related to inflammation such as skin inflammation.

The content of the extract according to the present invention is preferably in the range of 0.001 to 30.0% by weight based on the whole composition. The content of the extract is preferably at least the above-mentioned minimum value so as to attain the minimum anti-inflammatory effect by inhibiting the production and secretion of inflammatory mediators such as NO and TNF-α involved in the inflammatory reaction, And the applicability to various formulations, the content of the extract is preferably not more than the maximum value. At this time, it is preferable that the content of the extract is appropriately controlled within the above range according to the content of the components contained in the formulation.

In addition, when the extract according to the present invention is used as a constituent component, it can be used not only in the form of a lyophilized powder, but also in the form of a liquid dispersed or dissolved in water or a common organic solvent.

In addition, the composition according to the present invention may contain, in addition to the above-mentioned extract components, other components which can give a synergistic effect to the main effect, within a range not impairing the intended main effect of the present invention.

The pharmaceutical composition of the present invention is not particularly limited in its formulation, and the composition of the present invention may be a solid preparation, a semi-solid preparation or a liquid preparation. At this time, in the composition of each formulation, components other than the above-mentioned Sauropus spatulifolius Beille extract may be selected by a person skilled in the art according to the formulation or use purpose of the other pharmaceutical composition.

The cosmetic composition of the present invention is not particularly limited in its formulation and may be in the form of a solution, suspension, emulsion, gel, lotion, essence, cream, powder, soap, pack mask, cleansing oil, foundation, . ≪ / RTI >

In addition, the compositions of each formulation may contain various bases and additives necessary for formulation of the formulation, and may contain non-ionic surfactants, silicone polymers, extender pigments, flavorings, preservatives, But are not limited to, disinfectants, oxidative stabilizers, organic solvents, ionic or nonionic thickeners, plasticizers, antioxidants, free radical scavengers, opacifiers, stabilizers, emollients, silicones, A preservative, a surfactant, an anti-inflammatory agent, a substance P antagonist, a filler, a polymer, a propellant, a basicizing or acidifying agent, or a coloring agent.

Health food composition of the present invention is added to SPA-to-lipoic crispus Julius (Sauropus spatulifolius Beille) extracts as SD or be used in combination with other foods or food ingredients, can be used suitably in a conventional manner.

There is no particular limitation on the kind of the food. Examples of foods to which the Sauropus spatulifolius Beille extract can be added include caramel, meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, ice cream , Various soups, beverages, tea, drinks, alcoholic beverages, and vitamin complexes, all of which include health foods in a conventional sense.

Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided to further understand the present invention, and the present invention is not limited by the examples.

Example  1: Preparation of extract

Sauropus Spaulipolius ( Sauropus) Spatulifolius Beille) leaves and stems were lyophilized, pulverized and pulverized. Functional ethanol was added 10 times the weight of the natural product powder and reacted at room temperature for 5 days. The solution was filtered and concentrated under reduced pressure to obtain an extract.

Experimental Example  1: Confirming NO inhibitory activity

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.

The extract obtained in Example 1 was dissolved in a concentration of 1 wt% using 50 wt% of 1,3-butylene glycol and diluted to a proper concentration using a culture medium to prepare a sample solution of the extract of Sapropus sp. Lipolius NO production inhibitory effect was confirmed.

RAW 264.7 cells were inoculated in a 96 well plate at 5 X 10 ⁴ cells / well using DMEM medium and cultured for 6 hours. The culture medium containing the extracts 5, 10, 20 and 40 ug / ml was cultured for 1 hour, and treated with LPS (0.1 μg / ml) for 16 hours. From the thus cultured samples, the amount of NO present in the cell culture solution was measured using a Griess reagent.

Specifically, 150 μl of the cell culture supernatant of the above cultured samples and 150 μl of a grease reagent (2.5% sulfanilamide, 0.25% naphthylethylenediamine dissolved in 10% phosphoric acid) were mixed and reacted on a 96-well plate for 15 minutes, The absorbance at 540 nm was measured using a reader. The standard concentration curve was obtained by continuously diluting sodium nitrite as a medium. The amount of NO produced was measured and evaluated. The results are shown in Table 1. In addition, the test results were validated using indomethacin as a positive control.

NO production inhibition (%)
Positive control group 5
ug / ml 10
ug / ml 20
ug / ml 40
ug / ml 46.0 31.6 40.8 48.9 49.0

Referring to Table 1, it was confirmed that the extract of Saulopus sp. To Lipolius effectively reduced the production of NO in RAW 264.7 cells induced by LPS, and it was also confirmed that the degree of reduction was concentration-dependent.

Experimental Example  2: TNF -α secretion suppression efficacy

TNF-α secreted by macrophages, monocytes and natural killer cells is an inflammation-mediated cytokine that acts in vivo alone or with cytokines such as IL-1 and IFN-γ to induce tumor necrosis Or infection by microorganisms induces host resistance, and abrupt overproduction has a deleterious effect on the organism. Therefore, a substance capable of reducing TNF-a production can be used as an anti-inflammatory agent.

The extract obtained in Example 1 was dissolved in a concentration of 1 wt% using 50 wt% of 1,3-butylene glycol and diluted to a proper concentration using a culture medium to prepare a sample solution of the extract of Sapropus sp. Lipolius TNF-α production inhibitory effect was confirmed.

RAW 264.7 cells were inoculated into 24 well plates at 2 × 10 ⁵ cells / well using DMEM medium and cultured for 6 hours. The culture medium containing the extracts 5, 10, 20, and 40 ug / ml was cultured for 1 hour, treated with LPS (0.1 ng / ml), and cultured for 24 hours. The amount of TNF-α present in the cell culture solution was measured using the TNF-α immunoassay (R & D system) from the thus cultured samples, and the results are shown in Table 2. In addition, the test results were validated using dexamethasone as a positive control.

TNF-α secretion inhibition (%)
positivity
Control group 5
ug / ml 10
ug / ml 20
ug / ml 40
ug / ml 47.8 45.7 22.3 29.0 37.5

Referring to Table 2 above, it was confirmed that the extract of Saulopus sp. To Liporrius effectively reduced the production of TNF-? In RAW 264.7 cells induced by LPS, and it was also confirmed that the degree of reduction was concentration-dependent .

Hereinafter, the composition of the composition containing the extract of Sauropus spatulifolius Beille prepared in Example 1 of the present invention will be described in more detail. However, the composition of the present invention is not limited to these formulation examples.

(Formulation Example 1) Flexible longevity (skin lotion)

As shown in Table 3 below, Sauropus sp. Spatulifolius Beille) extract was prepared according to a conventional method.

Compounding ingredient weight% Sauropus spatulifolius Beille extract 1.0 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 Phage-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water to 100

(Formulation Example 2) Nutritional lotion (milk lotion)

As shown in Table 4 below, Sauropus sp. Spatulifolius Beille) extract was prepared by a conventional method.

Compounding ingredient weight% Sauropus spatulifolius Beille extract 1.0 Squalane 4.0 Wax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 1.5 Liquid paraffin 0.5 Caprylic / capric triglyceride 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water to 100

(Formulation Example 3) Nourishing cream

As shown in Table 5 below, Sauropus sp. Spatulifolius Beille) extract was prepared by a conventional method.

Compounding ingredient weight% Sauropus spatulifolius Beille extract 1.0 Wax 10.0 Polysorbate 60 1.5 Piggy 60 hardened castor oil 2.0 Sorbitan sesquioleate 0.5 Liquid paraffin 10.0 Squalane 5.0 Caprylic / capric triglyceride 4.0 glycerin 5.0 Butylene glycol 3.0 Propylene glycol 3.0 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water to 100

(Formulation Example 4) Pack

As shown in Table 6 below, Sauropus sp.Sauropus spatulifolius Beille) extract was prepared according to a conventional method.

Compounding ingredient weight% Sauropus spatulifolius Beille extract 1.0 Polyvinyl alcohol 12.0 Sodium carboxymethylcellulose 0.2 glycerin 5.0 Allantoin 0.1 ethanol 6.0 Fingi-12 nonylphenyl ether 0.3 Polysorbate 60 0.3 Preservative, coloring, fragrance Suitable amount Purified water to 100

(Formulation Example 5)

As shown in Table 7 below, Sauropus sp. Spatulifolius Beille) extract was prepared by a conventional method.

Compounding ingredient weight% Sauropus spatulifolius Beille extract 1.0 Ethylenediamine sodium acetate 0.05 glycerin 5.0 Carboxyvinyl polymer 0.3 ethanol 5.0 Piggy-60 hardened castor oil 0.5 Triethanolamine 0.3 Preservative, coloring, fragrance Suitable amount Purified water to 100

(Formulation Example 6) Powder

As shown in Table 8 below, Sauropus sp. spatulifolius Beille) extract was prepared by a conventional method.

Compounding ingredient weight Sauropus spatulifolius Beille extract 0.001 g Lactose ` 1g

(Formulation Example 7) Fruit juice

Sauropus Spaulipolius ( Sauropus) Spatulifolius Beille) extract was added to 1,000 mL of apple or grape juice to prepare fruit juice for health promotion.

Claims (13)

Sauropus Spaulipolius ( Sauropus) Spatulifolius Beille) extract as an active ingredient. The method of claim 1, wherein the extract
A pharmaceutical composition for antiinflammatory, which comprises 0.001 to 30.0% by weight, based on the total weight of the pharmaceutical composition. The method of claim 1, wherein the extract
A pharmaceutical composition for antiinflammatory, characterized by having a liquid phase, a concentrated solid phase and a lyophilized powder phase. The method of claim 1, wherein the extract
Characterized in that it is extracted with an extraction solvent selected from purified water, methanol, ethanol, 1,2-propanediol, glycerin, ethylene glycol, propylene glycol, butylene glycol, hexane, dichloromethane, dichloroethane, ethyl acetate and mixtures thereof A pharmaceutical composition for antiinflammation. A cosmetic composition for antiinflammation comprising an extract of Sauropus spatulifolius Beille as an active ingredient. 6. The method of claim 5, wherein the extract
The cosmetic composition for anti-inflammation according to any one of claims 1 to 3, wherein the composition contains 0.001 to 30.0% by weight based on the total weight of the cosmetic composition. 6. The method of claim 5, wherein the extract
Characterized in that it has a liquid phase, a concentrated solid phase and a lyophilized powder form. 6. The method of claim 5, wherein the extract
Characterized in that it is extracted with an extraction solvent selected from purified water, methanol, ethanol, 1,2-propanediol, glycerin, ethylene glycol, propylene glycol, butylene glycol, hexane, dichloromethane, dichloroethane, ethyl acetate and mixtures thereof A cosmetic composition for antiinflammation. The cosmetic composition according to claim 5, wherein the cosmetic composition comprises
A cosmetic composition for antiinflammation characterized by having one type of formulation selected from the group consisting of a solution, a suspension, an emulsion, a gel, a lotion, an essence, a cream, a powder, a soap, a pack mask, a cleansing oil, a foundation, . An anti-inflammatory health food composition containing an extract of Sauropus spatulifolius Beille as an active ingredient. 11. The composition of claim 10, wherein the extract
Wherein the composition contains 0.001 to 30.0% by weight based on the total weight of the composition. 11. The composition of claim 10, wherein the extract
Wherein the composition has a liquid, concentrated, and lyophilized powder form. 11. The composition of claim 10, wherein the extract
Characterized in that it is extracted with an extraction solvent selected from purified water, methanol, ethanol, 1,2-propanediol, glycerin, ethylene glycol, propylene glycol, butylene glycol, hexane, dichloromethane, dichloroethane, ethyl acetate and mixtures thereof Anti-inflammatory health food composition.