KR101902244B1 - Composition for improving skin defensive power - Google Patents

Abstract

The present invention discloses a composition for enhancing skin protection comprising at least one of a protopanaxadiol compound and a visa extract as an active ingredient.

Description

{Composition for improving skin defensive power}

The present invention relates to a composition for promoting skin defense.

So far, if you want to prevent and improve skin acne and trouble, tea tree oil, salicylic acid, triclosan, and fruit acids that have self-antibacterial power have been used. However, since these substances exhibit antibacterial activity, they may be irritating to the skin. Therefore, it is difficult to use them at a concentration that can exhibit the actual efficacy, and it is not easy to obtain a practical effect because the use concentration thereof is limited. Therefore, it is necessary to develop a material exhibiting excellent skin antimicrobial and anti-inflammatory effects without irritating the skin.

Korean Registered Patent No. 10-0884616 (registered on Feb. 12, 2009) Korean Patent Publication No. 10-2006-0043067 (published May 15, 2006)

The present invention is intended to provide a composition capable of enhancing skin defense.

One aspect of the present invention is the use of protopanaxadiol-based compounds and visas ( Torreya < RTI ID = 0.0 > nucifera extract of the present invention as an active ingredient.

Another aspect of the invention is a pharmaceutical composition comprising at least one of a protopanaxadiol compound and a visa extract; And epigallocatechin gallate as an active ingredient.

The composition according to the present invention comprises at least one of a protopanaxadiol compound and a visa extract; And optionally epigallocatechin gallate, thereby promoting the activity of the antibacterial peptide of the skin, thereby enhancing the skin's own defense power without stimulating the skin, and exhibiting excellent skin antibacterial and anti-inflammatory activity.

FIG. 1 is a graph comparing the effects of Compound K, Visa seed oil, epigallocatechin gallate, a mixture thereof, and tea tree oil on skin antimicrobial peptide expression.

As used herein, the term "skin" refers to a tissue covering the body surface of an animal, and is a concept of the broadest notion including a scalp and hair as well as a tissue covering a body surface such as a face or a body. As used herein, the term "extract" refers to an oil component extracted from a natural product, which is a broad concept including all the substances obtained by extracting components of natural products, regardless of the extraction method, extraction solvent, . In the present specification, the term "skin defense force" is an ability to protect the skin from external stimuli or toxins, and the stimulus is a broad concept including allergens that are harmful to the skin such as bacteria, viruses, ultraviolet rays,

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

Skin breaks bacteria against itself by releasing the antimicrobial peptide itself when bacteria enter. Therefore, a substance that promotes the activity of the antimicrobial peptide of the skin may enhance the antimicrobial and anti-inflammatory activity of the skin by enhancing the skin's own defense without stimulating the skin.

One aspect of the present invention provides a composition for promoting skin protection comprising at least one of a protopanaxadiol compound and a visa extract as an active ingredient. Protopanaxadiol-based compounds or visa extracts can promote skin antimicrobial peptide expression and enhance skin protection. Thus, a composition comprising at least one of a protopanaxadiol compound and a visa extract can enhance skin defense, particularly skin antimicrobial and anti-inflammatory activity, and further improve skin troubles including acne. In one aspect of the present invention, an antimicrobial peptide is a peptide that is induced to express when an external stimulus is received,  hBD1, hBD2, LL37 or Rnase7, but the present invention is not limited thereto.

In one aspect of the invention, the protopanaxadiol-based compound is a ginsenoside, a ginseng saponin. In another aspect of the present invention, the protopanaxadiol compound can be obtained by enzymatic treatment of ginseng, specifically red ginseng. In another aspect of the present invention, the protopanaxadiol compound comprises compound K. Compound K is 20-O- (beta-D-glucopyranosyl) -20 (S) -protonanaxadiol 20-O- protopanaxadiol) and can be represented by the following chemical formula.

[Chemical Formula 1]

The composition according to one aspect of the present invention comprises from 0.001% to 10% by weight, in particular from 0.01% to 5% by weight, more specifically from 0.1% to 3% by weight, based on the total weight of the composition, of protopanaxadiol compound . ≪ / RTI > When it is included in the above range, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy both the stability and safety of the composition, and may be suitably included in the above range in terms of cost effectiveness. Specifically, when the composition contains protopanaxadiol compound in an amount of less than 0.001% by weight, the skin protective effect may be insignificant. When the composition contains more than 10% by weight, the solubility of protopanaxadiol compound in a solvent is lowered The stability of the composition may deteriorate.

In one aspect of the invention, the visa extract is a visa tree ( Torreya nucifera ), specifically extracts of visa seeds. In another aspect of the present invention, the visa extract includes viscous oil, specifically viscose oil, which is a preservative ingredient obtained by squeezing viscose or extracting with an organic solvent. The organic solvent includes, but is not limited to, at least one selected from the group consisting of alcohol, hexane, acetone, ethyl acetate, diethyl ether, ethyl methyl ketone and chloroform.

In one aspect of the invention, the composition may comprise from 0.001 wt% to 99 wt%, specifically from 0.1 wt% to 80 wt%, more specifically from 10 to 50 wt%, of a visa extract, based on the total weight of the composition. When it is included in the above range, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy both the stability and safety of the composition, and may be suitably included in the above range in terms of cost effectiveness. Specifically, when the composition contains less than 0.001% by weight of the visa extract, the effect of enhancing skin protection may be insignificant.

The composition for enhancing skin protection according to one aspect of the present invention may further comprise Epigallocatechin Gallate. The composition for enhancing skin protecting power according to the present invention may further have skin antibacterial and antiinflammatory activity effects by further including epigallocatechin gallate, thereby having a better skin protecting ability.

In the present specification, Epigallocatechin Gallate is a type of polyphenol, which is a catechin contained mainly in green tea, and can be represented by the formula of (-) - epigallocatechin-3-gallate. In one aspect of the present invention, epigallocatechin gallate can be obtained by extracting green tea.

The composition according to one aspect of the present invention comprises from 0.00001 wt.% To 10 wt.%, Specifically 0.0001 wt.% To 5 wt.%, More specifically 0.001 wt.% To 1 wt.% Of epigallocatechin gallate . ≪ / RTI > When it is included in the above range, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy both the stability and safety of the composition, and may be suitably included in the above range in terms of cost effectiveness. Specifically, when the composition contains less than 0.00001% by weight of epigallocatechin gallate, the effect of enhancing the skin protective ability may be insignificant. If it exceeds 10% by weight, oxidation tends to occur, have.

One aspect of the invention is a pharmaceutical composition comprising at least one of a protopanaxadiol compound and a visa extract; And, optionally, epigallocatechin gallate as an active ingredient. The cosmetic composition of the present invention can exhibit an effect of enhancing skin-protecting ability, specifically exhibiting excellent antibacterial and anti-inflammatory activity, and further improving or preventing skin troubles including skin acne.

The cosmetic composition according to the present invention may be provided in all formulations suitable for topical application. For example, it may be provided as a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an oil phase in water, a suspension, a solid, a gel, a powder, a paste, a foam or an aerosol composition. Compositions of such formulations may be prepared according to conventional methods in the art.

The cosmetic composition according to the present invention may further comprise a moisturizing agent, an emollient agent, a surfactant, an ultraviolet absorber, an antiseptic, a bactericide, an antioxidant, a pH adjusting agent, organic and inorganic pigments, a fragrance, . The compounding amount of the above components can be easily selected by those skilled in the art within a range not to impair the objects and effects of the present invention. The amount thereof may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, have.

One aspect of the invention is a pharmaceutical composition comprising at least one of a protopanaxadiol compound and a visa extract; And optionally epigallocatechin gallate as an active ingredient. The pharmaceutical composition can exhibit an effect of enhancing the skin defense force, specifically exhibiting an excellent antibacterial and anti-inflammatory activity, and further treating or improving skin troubles including skin acne.

The pharmaceutical composition according to one aspect of the present invention may be administered orally, parenterally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, and the like.

Formulations for oral administration may be in the form of tablets, pills, soft and hard capsules, granules, powders, granules, solutions, emulsions or pellets, It is not. These formulations may contain, in addition to the active ingredient, a diluent such as lactose, dextrose, sucrose, mannitol, sorbitol, cellulose or glycine, a lubricant such as silica, talc, stearic acid or polyethylene glycol, or a binder such as magnesium aluminum Silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose or polyvinylpyrrolidone). And may optionally contain pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, or sweeteners. The tablets may be prepared by conventional mixing, granulating or coating methods.

Formulations for parenteral administration may be, but are not limited to, injections, drops, lozenges, ointments, gels, creams, suspensions, emulsions, suppositories, patches or spraying agents.

The effective ingredients of the pharmaceutical composition according to one aspect of the present invention will vary depending on the age, sex, weight, pathological condition and severity of the subject to be administered, route of administration, or judgment of the prescriber. Determination of the amount of application based on these factors is within the level of ordinary skill in the art and its daily dose is, for example, from 0.1 mg / kg / day to 100 mg / kg / day, more specifically from 5 mg / kg / day to 50 mg / / Day, but is not limited thereto.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to Examples and Experimental Examples. However, the following examples and experimental examples are provided for illustrative purposes only in order to facilitate understanding of the present invention, and the scope and scope of the present invention are not limited thereto.

[Example]

Compound K was obtained by hydrolyzing red ginseng with an enzyme. Visa seed oil was obtained by squeezing the seeds of visas or extracting them with an organic solvent.

Epigallocatechin gallate (EGCG) was obtained in the following manner. First, green tea leaf (dry water content of 3% or less) was subjected to hot water reflux extraction with 10 times of purified water at 30 to 70 ° C for 1 hour to 24 hours, followed by primary filtration to remove the residue, The water-soluble components were separated. Only the epigallocatechin gallate among the separated water soluble components was selectively precipitated and concentrated through crystallization, and the undissolved filtrate was removed by filtration. The precipitate was redissolved and purified by chromatography and the solvent was evaporated to finally obtain high purity epigallocatechin gallate.

[Experimental Example] Assessment of promoting effect of skin antimicrobial peptide expression

Compound K, visa seed oil, epigallocatechin gallate (EGCG), compound K and visa seed oil, compound K, visa seed oil and EGCG, and tea tree oil were used as the keratinocytic cell line (HaCaT) (Dr. NE Fusenig , Deutsches Krebsforschungszentrum (Germany), Heidelberg, Germany) and the change of hBD1, hBD2, LL37 and Rnase7 gene expression, representative skin antimicrobial peptides, was measured by real time PCR after 24 hours. The gene expression changes of each treatment group on the basis of the untreated group are shown in FIG. 1 (average) and Table 1 (mean + standard deviation).

hBD1 hBD2 LL37 Rnase7 Untreated group One One One One Compound K 1.200431 ± 0.117122 1.2501451 ± 0.060240 1.4266929 ± 0.478567 1.2435783 ± 0.065722 Visa seed oil 1.136352 ± 0.067012 1.119184 ± 0.074302 1.209884 ± 0.175301 1.133979 ± 0.090271 EGCG 1.124634 ± 0.365302 1.120488 ± 0.032836 1.91 ± 1.000007883 1.158407 ± 0.164803 Compound K + visa seed oil 1.209359 ±
0.0915457 1.320578 ±
0.165871 1.491648 ±
0.365904 1.310674 ±
0.164829 Compound K + visa seed oil + EGCG 1.277801 ±
0.200185 1.351209 ±
0.095638 1.59781 ±
0.360825 1.899171 ±
0.095602 Tea tree oil 0.762495 ± 0.153398 0.993401 ± 0.022563 0.847556 ± 0.073745 0.919438 ± 0.127590

As can be seen from the above results, the compound K, visa seed oil, epigallocatechin gallate (EGCG), the compound K and visa seed oil, the compound K, visa seed oil and EGCG were the skin antimicrobial peptides hBD1, hBD2, LL37, Rnase7 Gene, while tea tree oil, a frequently used raw material in antimicrobial cosmetics, suppressed the expression of all four genes. In other words, tea tree oil can not enhance the skin's own defense, whereas compound K, visa seed oil, epigallocatechin gallate (EGCG) and mixtures thereof activate the skin antimicrobial peptides, It can be seen that

Formulation examples of compositions according to one aspect of the present invention are described below, but may be applied to various other formulations, which are not intended to be limiting but merely illustrative of the invention.

[Formulation Example 1] Lotion

The lotion is prepared according to a conventional method with the composition shown in the following table.

ingredient Content (% by weight) Compound K 1.0 Visa seed oil 5.0 L-ascorbic acid-2-phosphate magnesium salt 1.0 Water soluble collagen (1% aqueous solution) 1.0 Sodium citrate 0.1 Citric acid 0.05 1,3-butylene glycol 3.0 Purified water Balance

[Formulation Example 2] Cream

Creams are prepared according to a conventional method with the composition shown in the following table.

ingredient Content (% by weight) Protopanaxadiol compound 2.0 Polyethylene glycol monostearate 2.0 Glycerin monostearate 5.0 Cetyl alcohol 4.0 Squalene 3.0 Tri-2-ethylhexane glyceryl 6.0 Sphingoglycolipids 1.0 1,3-butylene glycol 7.0 Purified water Balance

[Formulation Example 3] Pack

A pack is prepared according to a conventional method with the composition shown in the following table.

ingredient Content (% by weight) Visa Extract 20.0 Polyvinyl alcohol 13.0 L-ascorbic acid-2-phosphate magnesium salt 1.0 Lauroylhydroxyproline 1.0 Water soluble collagen (1% aqueous solution) 2.0 1,3-butylene glycol 3.0 ethanol 5.0 Purified water Balance

[Formulation Example 4] Soft capsule

A mixture of protopanaxadiol compound 50 mg, visa extract 200 mg, epigallocatechin gallate 10 mg, soybean extract 50 mg, soybean oil 180 mg, palm oil 2 mg, palm kernel oil 8 mg, yellow bean 4 mg and lecithin 6 mg , And a soft capsule is prepared according to a conventional method.

[Formulation Example 5] Tablets

A mixture of 10 mg of compound K, 200 mg of visa seed oil, 10 mg of epigallocatechin gallate, 50 mg of soybean extract, 100 mg of glucose, 96 mg of starch and 4 mg of magnesium stearate and 40 mg of 30% Dried, and tableted using a tablet machine.

Claims (10)

(Protopanaxadiol) compound as an active ingredient,
Wherein the protopanaxadiol compound is 20-O- (beta-D-glucopyranosyl) -20 (S) -protopanaxadiol.
The method according to claim 1,
Wherein the composition further comprises a Torreya nucifera extract.
3. The method of claim 2,
Wherein the visa extract comprises visa seed oil.
The method according to claim 1,
Wherein the composition comprises from 0.001% to 10% by weight of the protopanaxadiol compound based on the total weight of the composition.
3. The method of claim 2,
Wherein the composition comprises from 0.001% to 99% by weight of the visa extract, based on the total weight of the composition.
The method according to claim 1,
Wherein the composition further comprises Epigallocatechin Gallate. ≪ RTI ID = 0.0 > 11. < / RTI >
The method according to claim 6,
Wherein the composition comprises 0.00001 wt% to 10 wt% of epigallocatechin gallate based on the total weight of the composition.
The method according to claim 1,
Wherein the composition enhances the antibacterial and anti-inflammatory activity of the skin.
The method according to claim 1,
Wherein the composition promotes antimicrobial peptide expression in the skin.
10. The method according to any one of claims 1 to 9,
Wherein the composition is a cosmetic composition.

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