KR20100036644A - Cosmetic composition comprising corilagin as active ingredients - Google Patents

Abstract

PURPOSE: A cosmetic composition containing corilagin or derivative thereof is provided to ensure effects of enhancing protein synthesis, epidermis collagen synthesis and to suppress MMP-1(matrix metalloprotease-1) generation and oxidation. CONSTITUTION: A cosmetic composition for anti-aging contains corilagin of chemical formula 1 or derivative thereof as an active ingredient. A cosmetic composition for anti-wrinkle contains corilagin of chemical formula 1 or derivative thereof as an active ingredient. The corilagin is isolated from Euphorbia helioscopia L., Terminalia chebula Retz., and Phyllanthus urinaria. The cosmetic composition is used in the form of solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing formulation, oil, powder foundation, emulsion foundation, wax foundation or spray.

Description

Cosmetic composition containing coryazine as an active ingredient {Cosmetic Composition Comprising Corilagin as Active Ingredients}

The present invention relates to a cosmetic composition containing coryazine or a derivative thereof as an active ingredient.

Human skin undergoes various physical and chemical changes during the aging process. The causes are largely divided into internal aging and photo-aging, and research on this has been actively conducted. Free radicals may be activated by UV rays, stress, disease conditions, environmental factors, wounds, and age. If this condition is exacerbated, it destroys antioxidant defenses in vivo and damages cells and tissues. And aging. More specifically, lipids, proteins, polysaccharides, and nucleic acids, which are major constituents of the skin, are oxidized to destroy skin cells and tissues, resulting in skin aging. In particular, the oxidation of proteins is caused by severe cuts in the connective tissues of collagen, hyaluronic acid, elastin, proteoglycan, fibronectin, and so on, resulting in severe over-inflammatory reaction and skin elasticity. If this worsens, mutations in the DNA can lead to mutations, cancer, and reduced immune function.

Therefore, it protects the cell membrane by eliminating free radicals caused by metabolic processes of the body, irradiation by ultraviolet rays, and inflammatory reactions.Also, damaged cells should be regenerated by active metabolism to proliferate the cells. You can recover quickly and maintain healthy skin. Aging involves not only free radicals, but also an enzyme called matrix metalloprotease (MMP) .In vivo, the synthesis and degradation of extracellular substrates such as collagen are properly regulated, but their synthesis decreases as aging progresses. Expression of matrix metalloproteinase (MMP), which is an enzyme that degrades, is promoted, thereby decreasing the elasticity of the skin and forming wrinkles. Ultraviolet irradiation also activates these degrading enzymes. Therefore, there is a need for the development of a substance capable of regulating MMP expression that inhibits activation or inhibiting its activity in cells. Until now, most of the raw materials used as materials for cosmetics simply inhibited enzyme activity. Therefore, we tried to regulate the expression and activity of MMP expression induced by intracellular natural aging and photoaging.

On the other hand, a variety of chemicals are used as a cosmetic composition, but recently, cosmetics using natural products have been developed to reduce skin irritation caused by such chemicals. Natural ingredients have less side effects on the skin, and as the consumer's response to cosmetics using natural materials has increased recently, the development value of cosmetics as a raw material for cosmetics is increasing.

Recently, many cosmetic companies have been making various research and development to overcome the above problems, it has been found that various natural products such as rhododendrons, stalks and potions are effective in preventing skin aging. However, most of these components have a problem such that the relative effect of the stability of the cosmetic, skin irritation and concentration is weakened when used in a high concentration as an extract mixed with various components.

The present inventors have diligently researched to improve the skin aging phenomenon by promoting the synthesis of skin proteins damaged by ultraviolet rays, etc., coryazine enhances the protein synthesis of fibroblasts, and the collagen synthesis enhancement effect of the dermal layer, MMP- The present invention was completed by finding that the production inhibitory effect and the antioxidant effect of 1 are excellent, as well as the skin wrinkle improving effect and the skin elasticity improving effect in the case of the composition containing the same.

Accordingly, it is an object of the present invention to provide a cosmetic composition for preventing skin aging comprising corylazine or a derivative thereof as an active ingredient.

Another object of the present invention to provide a cosmetic composition for improving skin wrinkles containing coryazine or a derivative thereof as an active ingredient.

Another object of the present invention to provide a cosmetic method using a cosmetic composition containing the corylazine or a derivative thereof.

Other objects and advantages of the invention will be apparent from the following examples and claims.

The present invention relates to a cosmetic composition containing coryazine or a derivative thereof as an active ingredient. More specifically, the present invention relates to a cosmetic composition for preventing skin aging and improving skin wrinkles containing coryazine or a derivative thereof as an active ingredient. In the present invention, corylazine is excellent in protein synthesis promoting effect, dermal layer collagen synthesizing effect, MMP-1 production inhibitory effect and antioxidant effect, and cosmetics containing coryazine is excellent in skin wrinkle improvement effect.

The present invention relates to a cosmetic composition for skin aging and skin wrinkle improvement comprising coryazine or a derivative thereof as an active ingredient.

Corilagin included as an active ingredient of the present invention has a molecular formula of C ₂₇ H ₂₂ O ₁₈ , 1-O-galloyl-3,6- (R) -hexahydroxydiphenoli-beta-glucopy It is a compound having a molecular weight of 634.45 having a structure of Formula 1 represented by Lanose.

Corylazine used in the present invention can be separated from natural sources such as reading aloud, talc, ripening, let's go, pearl pearl, pilantus urianna, and can be synthesized chemically. In addition, an anti-B-type infectious virus composition (patent application No. 2000-31970) containing corylazine has been found.

On the other hand, according to a preferred embodiment of the present invention, the corylazine or a derivative thereof is 0.000001-15.0 wt% with respect to the composition, preferably contained in an amount of 0.001-10.0 wt%. At this time, if the content of the corylazine contained in the cosmetic composition is less than the minimum content, the expected effect is less likely to appear, and if the content exceeds the maximum content, the effect does not increase any more and is likely to cause irritation to the skin, and also stabilizes the formulation. Great influence

According to the present invention, corylazine has a protein synthesis promoting effect (Experimental Example 1), dermal layer collagen synthesis enhancing effect (Experimental Example 2), MMP-1 production inhibitory effect (Experimental Example 3) and antioxidant effect (Experimental Example 4) Not only is it excellent, the cosmetic composition containing coryazine is excellent in the skin wrinkle improvement effect (Experimental example 5).

Therefore, the cosmetic composition containing corylazine having various functions as an active ingredient has an excellent effect on preventing skin aging such as promoting protein synthesis, enhancing dermal collagen synthesis, inhibiting MMP-1 production, antioxidant effect and improving skin wrinkles. Have

In addition, it is apparent to those skilled in the art in view of the technical level in the art that derivatives obtained by addition or substitution reaction of the substituents commonly practiced in the art with respect to the compound of Formula 1 are included in the scope of the present invention.

The composition of the present invention can achieve its effect by topical application or spraying on the skin. Therefore, according to a preferred embodiment of the present invention, the composition of the present invention may be prepared in the form of cosmetic compositions such as creams, lotions and softening water or pharmaceutical compositions such as sprays and ointments.

Ingredients included in the cosmetic composition of the present invention as an active ingredient includes components commonly used in cosmetic compositions in addition to the active ingredient, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavors, And carriers.

The cosmetic composition of the present invention may be prepared in any formulation commonly prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing , Oils, powder foundations, emulsion foundations, wax foundations and sprays, and the like, but are not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

When the formulation of the present invention is a paste, cream or gel, animal oils, vegetable oils, waxes, paraffins, starches, trachants, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide may be used as carrier components. Can be.

In the case where the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. Especially, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol esters and polyoxyethylene sorbitan esters, and microcrystals are used as carrier components. Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

In addition, the present invention provides a cosmetic method using a cosmetic composition containing the corylazine of the present invention or a derivative thereof.

The cosmetic method of the present invention refers to all cosmetic methods applied to the human skin using the cosmetic composition of the present invention. That is, all the methods known in the art for applying the cosmetic composition to the skin belong to the cosmetic method of the present invention.

The cosmetic composition of the present invention may be used alone or in duplicate, or may be used in combination with other cosmetic compositions other than the present invention. In addition, the cosmetic composition with excellent skin protection effect according to the present invention can be used according to a conventional method of use, the number of times of use can be varied according to the user's skin condition or taste.

If the cosmetic composition of the present invention is a soap, a surfactant-containing cleansing or a surfactant-free cleansing formulation, it may be wiped off, peeled off, or washed with water after application to the skin. As a specific example, the soap is liquid soap, powdered soap, solid soap and oil soap, the surfactant-containing cleansing formulation is a cleansing foam, cleansing water, cleansing towels and cleansing pack, the surfactant-free cleansing formulation is a cleansing cream , Cleansing lotion, cleansing water and cleansing gel, but are not limited thereto.

By carrying out a cosmetic method using a cosmetic composition comprising the corylazine or derivatives thereof of the present invention, it is possible to obtain excellent skin anti-aging and skin wrinkle improvement.

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 embodiments are only for describing the present invention in more detail and that the scope of the present invention is not limited by these embodiments in accordance with the gist of the present invention .

Experimental Example 1. Experiment of the protein synthesis promoting effect of corilagin

Human normal fibroblasts (Korea Cell Line Bank) were seeded to 1 x 10 ⁶ cells in each well of a 48-well microplate and incubated for 24 hours at 37 ° C. in DMEM medium. Corylazine-containing serum free DMEM medium (experimental group) was then prepared so that the final concentrations of coryazine from Sigma were 5, 10, 20, 50 and 100 ppm, respectively, and the cell culture was Replacement with rilagin-containing serum free medium was further incubated for 24 hours. After incubation, the supernatant of each well was collected and the amount of newly synthesized protein was measured using a protein assay kit (Protein assay kit, Biorad, USA), and the results are shown in Table 1 below. At this time, the control group was incubated with serum-free medium replaced with purified water instead of coryazine.

Protein synthesis promoting effect (protein production amount (㎍ / ㎖)) Concentration of corylazine (ppm) Protein production amount (µg / ml) Control 64.3 5 65.2 10 80.3 50 99.3 100 113.2

As can be seen from the results of Table 1, in the case of the experimental group cultured by replacing with the corylazine-containing serum-free medium of the present invention, the amount of protein produced is greater than the amount of protein produced in the control group (corylazine-free) The amount of protein produced was increased as the concentration of corylazine increased.

Experimental Example 2 Corylgin (corilagin) of the dermal layer collagen synthesis promoting effect

Human normal fibroblasts (Korea Cell Line Bank) were seeded to 1 x 10 ⁶ cells in each well of a 48-well microplate and incubated for 24 hours at 37 ° C in DMEM medium. Subsequently, it was replaced with coryazine-containing serum free DMEM medium (experimental group) prepared so that the final concentrations of coryazine were 5, 10, 20, 50 and 100 ppm, respectively, and further incubated for 24 hours. Then, after collecting the supernatant of each well, the amount of C-peptide (PICP) of newly synthesized procollagen type I was measured using a PICP kit (PICP collagen assay kit, Takara, Japan). PICP amount was converted to ng / ml, and the collagen production increase rate was calculated using Equation 1 below. The results are shown in Table 2 below. In this case, serum-free DMEM medium containing TGF-β (10 ng / ml, Roche, United States) was used as a positive control, and serum-free DMEM medium containing none of the above components was used as a negative control.

Corylazine Concentration (ppm) Collagen production increase rate (%) 0 (voice control) 130.4 5 285.1 10 380.1 50 420.7 100 473.4 TGF-β (positive control) 410.3

As shown in Table 2, in the experimental group cultured with the medium of the corylazine of the present invention, compared to the negative control group containing nothing, there was a significant difference in the amount of collagen production, TGF- used as a positive control group Better results were obtained when compared to β 100 μg / ml.

Experimental Example 3. Inhibitory Effect of Corylazine on MMP-1 Production

The effect of corylazine on the production of collagen degrading enzyme MMP-1 was examined.

Fibroblasts (Korean Cell Line Bank, South Korea), which are human normal skin cells, were seeded in 48-well microplates (Nunc, Denmark) at 1 x 10 ⁶ cells per well, and treated with DMEM medium (Sigma, USA) and 37 ° C. After 24 hours of incubation, Coryazine-containing serum-free DMEM medium with corylazine added at a final concentration of 5, 10, 50, 100 μg / ml and serum-free DMEM with no coryazine as negative control Further incubation for 48 hours in the medium. After incubation, the supernatant of each well was collected and the amount of ng / ml newly synthesized MMP-1 was measured using an MMP-1 assay kit (Amersham, USA), and MMP-1 production was performed according to Equation 3 below. Inhibition rate was calculated and the results are shown in Table 3. At this time, TGF-β (10 ng / ml, Roche, United States) was used as a positive control of MMP-1 production inhibition rate.

MMP-1 Production Inhibition Rate (%) Corylazine Concentration (µg / mL) % Inhibition of MMP-1 production 0 (voice control) 0.0 5 78.3 10 87.5 50 98.5 100 120.6 TGF-β (positive control) 79.5

As shown in Table 3, in the experimental group cultured in the corylazine-containing medium of the present invention, the inhibition rate of MMP-1 production was significantly superior to that of the negative control group without corylazine and nothing, and used as a positive control group. Better results were obtained when compared to 100 μg / ml TGF-β.

Experimental Example 4: TBA Antioxidant Experiment of Coryazine

In order to determine the antioxidant effect of corylazine, antioxidant activity was measured using the TBA method as follows.

The experiment was performed with Fenton's reagent (2% SDS, 0.79 mM Potassium chloride, 0.25 mM Trizma base (pH 7.4), 1 μM FeCl ₂ , 0.025 mM H ₂ O ₂ ) 4.8 mL, 100 μl linoleic acid and 5, 10 corylazines. , 50, 100 μg / μl was mixed to block the light and reacted at 55 ° C. for 16 hours, followed by adding 100 μl of 4% BHT. 2 ml of the reaction solution, 1 ml of trichloroacetic acid, and 2 ml of 0.75% TBA were mixed, and the mixture was immersed in a water bath for 10 minutes, and then cooled after blocking light. 500 µl of the reaction solution, 100 µl of acetic acid and 200 µl of chloroform were mixed and centrifuged at 12,000 rpm for 10 minutes. 200 μl of the supernatant, which was centrifuged, was measured and absorbed at 530 nm three times, and then averaged. The results are shown in Table 4. At this time, the vitamin C (vit-C; 100 ㎍ / ㎖) was used as a positive control.

Corylazine Concentration (µg / mL) Oxidation inhibition rate (%) 0 (voice control) - 5 58.37 10 75.98 50 79.59 100 87.20 vit-C 100 (Yangseong Control) 76.19

As shown in Table 4, in the experimental group to which the corylazine of the present invention was added, as the concentration was increased, the antioxidant inhibition rate, which is an antioxidant effect index, increased, and was not inferior to that of vitamin C used as a positive control group. Rather better results were obtained.

Hereinafter, the formulation examples exemplify the cosmetic formulation containing the corylazine of the present invention, but the formulation of the present invention is not necessarily limited thereto.

Formulation Example 1. Softening Longevity

Formulation examples of the flexible longevity was prepared as follows according to a conventional method.

ingredient Content (unit: weight%) Coryazine Glycerin 1.3-Butylene Glycol PEG 1500 Allantoin DL-Pantenol E.D.T.-2-2 Benzophenone-9 Sodium Hyaluronate Ethanol Octicdodeces-16 Polysorbate 20 Preservative, Flavor, Pigment Distilled Water 3.0 5.0 3.0 1.0 0.1 0.3 0.02 0.04 5.0 10.0 0.2 0.1 Sum 100

Formulation Example 2. Converging Cosmetic Water

Formulation examples of convergent longevity were prepared as follows according to a conventional method.

ingredient Content (unit: weight%) Corylazine Glycerin 1.3-Butylene Glycol Allantoin DL-Pantenol E.D.T.A-2NA Benzophenone-9 Sodium Hyaluronate Ethanol Polysorbate 20 Witch Hazel Extract Citric Acid Preservative, Flavor, Pigment Distilled Water        1.5 2.0 2.0 0.2 0.2 0.02 0.04 3.0 15.0 0.3 2.0 Sum 100

Formulation Example 3. Nutrients

Formulation examples of nutrient cosmetics was prepared as follows in a conventional manner.

ingredient Content (unit: weight%) Corylazine Stearyl Alcohol Lanolin Polysorbate 60 Sorbitastearate Cured Vegetable Oil Mineral Oil Squalane Trioctanoin Dimethicone Tocopherol Acetate Carboxyvinyl Polymer Glycerin 1.3-Butylene Glycol Sodium Hyaluronate Tri Ethanolamine Preservative, Flavor, Dye Water        1.5 1.5 1.5 1.3 0.5 1.0 5.0 3.0 2.0 0.8 0.5 0.12 5.0 3.0 5.0 0.12 Sum 100

Formulation Example 4. Nutrition Cream

Formulation of nutrition cream was prepared as follows according to a conventional method.

ingredient Content (unit: weight%) Corylazine lipophilic monostearate glycerine cetearyl alcohol stearic acid wax polysorbate 60 sorbitan stearate cured vegetable oil squalane mineral oil trioctanoin dimethicone sodium magnesium silicate glycerin betaine triethanolamine sodium hyaluronate preservative, flavoring, coloring Distilled water        3.0 2.0 2.2 1.5 1.0 1.5 0.6 1.0 3.0 5.0 5.0 1.0 0.1 5.0 3.0 1.0 4.0 Sum 100

Formulation Example 5. Massage Cream

Formulation example of a massage cream was prepared as follows in a conventional manner.

ingredient Content (unit: weight%) Corylazine lipophilic monostearic acid glycerin stearyl alcohol stearic acid polysorbate 60 sorbitan stearate isostearyl isosterate squalane mineral oil dimethicone hydroxyethyl cellulose glycerin triethanolamine preservative, fragrance, pigment distilled water        3.0 1.5 1.5 1.0 1.5 0.6 5.0 5.0 35.0 0.5 0.12 6.0 0.7 Micro balance Sum 100

Formulation Example 6. Essence

Formulation examples of the essence was prepared as follows in a conventional manner.

ingredient Content (unit: weight%) Corylazine Glycerine Betaine Fiji 1500 Allantoin DL-Pantenol E.D.T-2Na Benzophenone-9 hydroxyethyl cellulose Sodium Hyaluronate Carboxyvinylpolymer Triethanolamine Octyldodecanol Octyldodeces -16 Ethanol Preservative, fragrance, pigment distilled water        5.0 10.0 5.0 2.0 0.1 0.3 0.02 0.04 0.1 8.0 0.2 0.18 0.3 0.4 6.0 Sum 100

Formulation Example 7 Pack

Formulation examples of the pack were prepared as follows in a conventional manner.

ingredient Content (unit: weight%) Corylazine Polyvinyl Alcohol Cellulose Gum Glycerin Fig 1500 Cycloastrin DL-Panthenol Allantoin Glycyrisin Monomonium Nicotinamide Ethanol Fig 40 Hardened Castor Oil Flavor, Pigment, Preservative Distilled Water        3.0 15.0 0.15 3.0 2.0 0.15 0.4 0.1 0.3 0.5 6.0 0.3 Micro balance Sum 100

Experimental Example 5. Skin Wrinkle Improvement

A clinical trial was conducted on the skin wrinkle improvement effect of the cream cosmetic containing the corylazine of the present invention. Clinical trials were evaluated through the actual use test of each cosmetic.

The experiment was made to use together the nutrition cream of Formulation Example 4 containing coryazine and the cream substituted with the water of Coryazine in Formulation Example 4 as a control example on one cheek of each subject. Among 40 30-40 year old women, women who had a lot of external activity were randomly divided into two groups, and the creams of Formulation Example 4 and Control Example were washed two times each morning, and then the appropriate amount was corrected continuously for 2 months around the eyes. The wrinkle improvement effect of each subject was Arch Dermatol vol. 137 (8): 1043-1051, 2001 (see Table 12) by reference to the reference, the evaluation was made by visual observation by an experienced doctor. The results are shown in Table 13 below.

score The degree of light damage around the eyes between subjects 0 none One none / mild 2 mild 3 mild / moderate 4 moderate 5 moderate / severe 6 severe 7 Verysevere

Wrinkle improvement effect (visual evaluation) of the cosmetics of the present invention 0 weeks 4 weeks 8 Weeks Formulation Example 4 Control Formulation Example 4 Control Formulation Example 4 Control Average 3.8 5.8 3.6 5.85 3.5 5.84 Standard Deviation 0.5 0.45 0.6 0.5 0.5 0.54 p value - - 0.0427 0.0430 0.0025 0.0036

As can be seen from the results of Table 13, the cream of the formulation example 4 containing coryazine showed a high wrinkle improvement effect compared to the cream of the control example containing nothing. In other words, it was judged to be a product that helped to improve wrinkles before and after use at a statistically significant level (p <0.05) from the mean value of 4 weeks.

Having described the specific part of the present invention in detail, it is apparent to those skilled in the art that such a specific technology is only a preferred embodiment, and the scope of the present invention is not limited thereto. Therefore, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof.

Claims (5)

A cosmetic composition for preventing skin aging containing corylazine of Formula 1 or a derivative thereof as an active ingredient. [Formula 1]

A cosmetic composition for improving skin wrinkles comprising corylazine of Formula 1 or a derivative thereof as an active ingredient. The cosmetic composition according to claim 1 or 2, wherein the content of the corylazine or a derivative thereof is included in an amount of 0.000001-15.0% based on the total weight of the cosmetic composition. 3. The cosmetic composition according to claim 1 or 2, wherein the cosmetic composition is a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing formulation, oil, powder foundation, emulsion foundation, wax Cosmetic composition, characterized in that it has a formulation selected from the group consisting of foundation and spray. The cosmetic method using the cosmetic composition of Claim 1 or 2.