KR100829718B1 - Cosmetic Composition for Whitening the Skin Comprising the Extract of Ilex rotunda as Active Ingredient - Google Patents

Abstract

The present invention provides a cosmetic composition for skin whitening comprising distant extract as an active ingredient. The far-tree extract of the present invention has an excellent effect of inhibiting tyrosinase activity and inhibits melanin production in melanocytes, and is useful as an active ingredient of a cosmetic composition for skin whitening having excellent stability because it hardly irritates the skin. Can be.

Farwood extract, tyrosinase, melanin, whitening, cosmetic composition

Description

Cosmetic composition for skin whitening comprising distant extract as an active ingredient {Cosmetic Composition for Whitening the Skin Comprising the Extract of Ilex rotunda as Active Ingredient}

The present invention relates to a cosmetic composition for skin whitening comprising distant extract as an active ingredient.

It is everyone's constant desire to have white, fair skin. In general, the color of human skin, hair and eyes is determined by melanin, carotene and hemoglobin and the like. In particular, melanin is the most important factor for determining the skin color, the skin color is determined according to the amount, nature and distribution of melanin. Human skin and hair pigments protect skin and hair from the harmful effects of sunlight, especially ultraviolet light. For example, people who lack these pigments are very sensitive to sunlight and are prone to burns and have a high probability of developing skin cancer even at a young age. Short wavelength ultraviolet (290-320 nm) and carcinogens form harmful radicals in the skin, such as oxygen radicals, which are known to attack skin cells and age the skin.

The main function of melanin is to remove these harmful radicals and protect the skin from the damage thereby. Therefore, high levels of melanin means that it has an effective response system that can protect the skin from physical or chemical toxic substances.

On the other hand, melanin is tyrosine (tyrosine) is converted to dopa (DOPA), dopaquinone (Dopaquinone) by an enzyme called tyrosinase (tyrosinase) is produced through a non-enzymatic oxidation reaction. The produced melanin is delivered to the skin cells and has a cyclic process in which melanin is lost and disappeared along with epidermal detachment.

The melanin production process is a naturally occurring phenomenon. In human skin in a normal state, melanin is not excessively produced, but melanin is excessively produced when the skin reacts with external stimuli such as ultraviolet rays, environmental pollution or stress. When the excessively produced melanin is not discharged out of the skin and remains in the skin, pigmentation occurs, resulting in blemishes and freckles.

Therefore, skin whitening can be achieved by inhibiting melanin production. Representative methods of inhibiting melanin production include blocking external stimuli such as ultraviolet light, inhibiting the activity of tyrosinase related to melanin formation, and producing melanin. There is a method for preventing the division of melanocytes that control the use, a method using a vitamin C derivative.

Japanese Patent Application Laid-Open No. 4-9320 discloses ascorbic acid as a whitening substance. Ascorbic acid has a whitening effect but has poor stability in the formulation, and as a result, the activity of the active ingredient decreases as time passes. Ascorbic acid is used as a capsule or liposome. Various methods such as stabilization have been proposed, but no clear stabilization method has yet been proposed.

In Japanese Patent Laid-Open No. 6-192062, hydroquinone is disclosed as a whitening substance. Hydroquinone is excellent in whitening effect but is limited to its use as a cosmetic since it is a carcinogenic substance.

As another whitening substance, kojic acid (Japanese Patent Laid-Open No. 56-7710) has an excellent inhibitory ability of tyrosinase and shows an excellent whitening effect, but it is not suitable for use in cosmetics and foods due to the toxicity and carcinogenicity of kojic acid. There is a problem.

As another whitening substance, arbutin (Japanese Patent Application Laid-Open No. 4-9315), which can be extracted from alpine bilberry or synthesized, has been proven to inhibit tyrosinase, but arbutin has a sugar attached to hydroquinone. As it is, it is pointed out that the sugar is separated by skin enzymes when applied to cosmetics, causing skin irritation.

Until now, various cosmetic companies have been conducting various research and development related to skin whitening, but nothing is known about the skin whitening effect of distant trees or its use as a skin whitening agent.

The present inventors have made diligent efforts to overcome the problems of the conventional skin whitening cosmetic composition, such as weakening the stability, side effects and whitening effect of the cosmetics, it was confirmed that the far-tree extract exhibits excellent whitening effect and skin stability.

Therefore, it is an object of the present invention to provide a cosmetic composition for skin whitening comprising as an active ingredient extract of distant tree with excellent skin whitening effect.

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

The present invention provides a cosmetic composition for skin whitening comprising distant extract as an active ingredient.

" Ilex rotunda " used as an active ingredient in the cosmetic composition of the present invention is a dicotyledonous plant belonging to the Awuifoliaceae family, reaching a height of 10 m, an evergreen broad-leaved arborescent, with dark brown and hairless. Leaves are alternate, oval, wedge-shaped or rounded at the bottom, sharp at the ends, without sawtooth. The petiole is long and glossy, and the leaf vein is faint.

The bark and root bark of distant trees are commonly called "gu pil nyeong" and are characterized by clear heat, detoxification, pain, diarrhea and hemostasis. It also exhibits antipyretic and anti-inflammatory effects on fever, tonsillitis, and sore throat caused by colds, and is also used as a therapeutic agent for acute hepatitis, acute gastritis, bruises and burns.

 Gufilung contains flavonoids, tannins and triterphenes, which are separated from beta-amyrin, beta-sitosterol and oleanolic acid. acid), rotundic acid.

The pharmacological effect of gufilungeum is to shorten the blood coagulation time in the test tube, exhibit the contractile action of vascular smooth muscle, and inhibit the development of Staphylococcus aureus, hemolytic streptococci, dysentery, typhoid bacteria, and Pseudomonas aeruginosa.

In clinical trials, the herbal medicine of Gu Pil-eung showed the prevention of purulent disease (changongbong cellulitis and deep adenoma), respiratory infection, acute tonsillitis, acute gastroenteritis, dysentery, burns and postoperative infection. Abdominal pain, stomach pain, cardiac pain, etc. showed painful effects and did not show systemic side effects during treatment.

In the present invention, distant extract means that obtained by extracting from various organs or parts (such as leaves, flowers, fruits, stems, branches, roots, etc.) of distant trees, preferably roots, stems or branches, most preferably Means an extract obtained from eggplant.

The mulberry extract of the present invention may be prepared according to conventional methods known in the art, that is, using conventional solvents, under conditions of conventional temperature and pressure.

The mulberry extract in the present invention is a variety of extraction solvents, for example, water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, propanol and butanol), acetone, ethyl acetate, chloroform, 1,3-butylene glycol And an extraction solvent selected from the group consisting of butyl acetate, preferably one obtained by using a suitable mixture of water and ethanol, and more preferably one using 70% ethanol. On the other hand, it will be apparent to those skilled in the art that the far-tree extract of the present invention can obtain an extract having substantially the same effect using not only the aforementioned extraction solvent but also other extraction solvents.

In addition, the extract of the present invention includes not only the extract by the above-described extraction solvent, but also the extract that has undergone a conventional purification process. Obtained by various additional purification methods, such as, for example, separation using an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity). The active fraction is also included in the extract of the present invention.

The far tree extract of the present invention is characterized by being used as a skin whitening ingredient. The mulberry extract inhibits the activity of tyrosinase and inhibits the production of melanin from tyrosine, and inhibits melanin production in melanocytes.

The mulberry extract in the composition of the present invention comprises an effective amount of mulberry extract capable of inhibiting tyrosinase activity or inhibiting melanogenesis of melanocytes. The content of the mulberry extract in the composition of the present invention is 0.0001-20.0% by weight, preferably 0.001-10.0% by weight based on the total weight of the composition. If the content of distant tree extract is less than 0.0001% by weight, the improvement of the whitening effect through inhibition of tyrosinase activity and inhibition of melanin production in melanocytes is somewhat insufficient. There is a problem that the skin sensitivity is increased without increasing the whitening effect.

The components included in the cosmetic composition of the present invention include components commonly used in cosmetic compositions in addition to the extract of mulberry as an active ingredient, and include, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavorings, and Carrier.

The skin lightening composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing It may be formulated as such, but is not limited thereto. More specifically, in the formulation of flexible lotion, nutrition lotion, milk lotion, nutrition cream, massage cream, essence, eye cream, cleansing lotion, cleansing cream, cleansing foam, cleansing water, powder wash, cleansing oil, mask, pack Can be prepared.

When the formulation of the present invention is a paste, cream or gel, the carrier component is animal oil, vegetable oil, ester oil, wax, paraffin, starch, tracant, cellulose derivative, carbomer, polyacrylamide, polyethylene glycol, silicone, Bentonite, silica, talc or zinc oxide and the like can be used.

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 , Fatty acid esters of 1,3-butylene glycol, oils, glycerol aliphatic esters, polyethylene glycols or sorbitan.

When the dosage form of the present invention is a suspension, a carrier diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Microcrystalline 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 an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, an isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a 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.

The cosmetic composition comprising the extract of the far-tree of the present invention exhibits excellent skin whitening effect through the inhibition of tyrosinase activity and the inhibition of melanin production of melanocytes, and has excellent skin safety because of low irritation to the skin. This fact is specified in detail in the Examples below.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are intended to illustrate the present invention in more detail, and the scope of the present invention is not limited by these examples. In addition, the part,%, and ratio used in this Example correspond to a mass reference | standard unless there is particular notice.

Preparation Example 1 Preparation of Mulberry Extract

First, the dried distant branches were dried well and then crushed to prepare a powder form. 100 g of distant eggplant powder was added to 600 ml of 70% ethyl alcohol, extracted at room temperature for 5 days, and filtered using Whatman filter paper (No. 5). It was placed in an extractor equipped with a cooling condenser and concentrated and dried at 70 ° C. under a reduced pressure concentrator to obtain a dry weight of 7.75 g. The dried mulberry extract powder was dissolved in 50% 1,3-butylene glycol and used to dissolve to a final concentration of 1% (w / v).

Experimental Example 1: Inhibition of tyrosinase activity of distant extract

Tyrosinase activity inhibition experiment was conducted to see the degree of inhibition of tyrosinase activity of the extracts of distant tree. As tyrosinase activity inhibiting substrate, 1.5 mmol / L tyrosine (Sigma, USA) dissolved in sodium phosphate buffer (pH 6.8) was used. Mulberry extract was diluted by concentration with 0.05 M sodium phosphate buffer (pH 6.8) to prepare a sample solution, and 40 μl of tyrosine was added to 240 μl of the sample solution for each concentration, and tyrosinase (Sigma, 1500 U / Ml) 20 μl was added and then reacted at 37 ° C. for 15 minutes, and then the absorbance was measured at 490 nm. Inhibition of activity on tyrosinah was calculated according to Equation 1 below, and the results are shown in Table 1 below.

티로시나아제 활성 저해도(%)=1-ㅧ 100

Inhibition of Tyrosinase Activity (%) = 1- ㅧ 100

Concentration of Far-Tree Extract (%) % Inhibition of tyrosinase activity 0.00 0.00 0.01 15.6 0.02 26.3 0.05 45.6 0.10 78.8 0.20 89.8

As can be seen from the results of Table 1, the far-tree extract of the present invention showed an excellent effect on the inhibition of tyrosinase activity, and also the activity inhibition was found to increase depending on the concentration of far-tree extract.

Experimental Example  2: A distant tree  Experiment to Inhibit Melanin Production by Extracts

Mice-derived melanoma cells B-16 (murine melanoma cells, Korea Cell Line Bank) were seeded in 12-well plates (Falcon, USA) to 1 ㅧ 10 ⁴ cell / well and cultured for one day to stabilize the cells. Next, each tree was treated with distant extracts at a concentration of 0 to 0.2% and incubated for 3-4 days. The cultured plate was centrifuged, the culture solution was removed, cells were lysed with 500 μl of 1N NaOH solution dissolved in dimethyl sulfoxide (DMSO), and then heated in a 90 ° C. water bath for 10 minutes. After centrifugation again, the supernatant was measured for absorbance at a wavelength of 570 nm. The melanin production inhibition was calculated according to Equation 2 using the measured values, and the results are shown in Table 2.

멜라닌 생성 저해도(%)= 1-ㅧ 100

Melanin production inhibition rate (%) = 1- ㅧ 100

Concentration of Far-Tree Extract (%) % Melanin production inhibition 0.00 0.0 0.01 3.5 0.02 10.2 0.05 23.5 0.10 45.7 0.20 77.6

As can be seen from the results of Table 2, it can be seen that far tree extract of the present invention significantly inhibits melanogenesis in melanocytes. In addition, the inhibition of melanogenesis was increased depending on the concentration of distant tree extract. Therefore, it can be seen that the composition comprising the far-tree extract of the present invention has an excellent effect on inhibiting melanin production.

Experimental Example 3: Cytotoxicity Test of Mulberry Extract

To determine the cytotoxicity of distant extracts, the toxicity was confirmed by MTT analysis. Human fibroblasts (fibroblasts) were seeded in 96-well plates at 8 ㅧ 10 ³ cells / well per well in a 96-well plate and incubated for 24 hours in 200 μl DMEM (Dulbecco Minimum Essential Medium) medium, followed by 0 for each well. The mulberry extract was treated by the concentration of -0.2% and incubated for another 24 hours. The cultured plate was added with a 0.5 mg / ml MTT solution (Sigma, USA) 4 hours later, the medium was removed, and the cells were lysed with 200 μl of DMSO solution. The reaction solution was then used for ELISA Reader (Molecular Device, USA). Absorbance at 570 nm was measured. At this time, as a control group was treated with no distant extract was calculated as a control according to the following equation (4), the results are shown in Table 3 below.

% Cell proliferation = (absorbance of experimental group / absorbance of control group) ㅧ 100

Concentration of Far-Tree Extract (%) Cell proliferation rate (%) 0.00 100.0 0.01 101.2 0.02 101.5 0.05 102.8 0.10 103.1 0.20 101.6

As can be seen from the results of Table 3, the extract of the present invention does not show cytotoxicity to fibroblasts even at relatively high concentrations, it was confirmed that the composition containing far-tree extract is quite safe against cytotoxicity.

Hereinafter, based on the results of the experimental examples described above to present a cosmetic composition for skin whitening comprising distant extract as an active ingredient. However, the composition of the present invention is not limited to the following formulation examples.

Formulation Example 1 Flexible Lotion

Formulation example of the flexible longevity containing the far-wood extract obtained by the method of Preparation Example 1 was prepared in the composition of Table 4 in accordance with a conventional method (Example 1), as the comparative group also has a softened longevity not added to the far-wood extract It was prepared together (Comparative Example 1).

Soft Cosmetics (Content-Weight%) ingredient Example 1 Comparative Example 1 Distula Extract Acetic Acid Tocopherol Ole Alcohol Ethanol Benzophenone-9 Carboxylvinyl Polymer Cellulose Gum Flavor Preservative Purified Water 2.0 5.2 1.5 3.2 2.0 1.0 3.5 Minor balance -5.2 1.5 3.2 2.0 1.0 3.5 Minor balance system 100 100

Formulation Example 2: Nutrients

Formulation example of nutrient lotion comprising a distant tree extract obtained by the method of Preparation Example 1 was prepared in the composition of Table 5 according to a conventional method (Example 2), nutrient lotion not added distant extract as a comparison group It was prepared together (Comparative Example 2).

ingredient Example 2 Comparative Example 2 Distula Extract Glycerine Propylene Glycol Tocopheryl Acetate Liquid Paraffin Triethanolamine Squalane Macadamia Nut Oil Polysorbate 60 Sorbanthesquirrolate Propylparaben Carboxyvinyl Polymer Fragrance Preservative Purified Water 2.0 5.1 4.2 3.0 4.6 1.0 3.1 2.5 1.6 1.6 0.6 1.5 Minor balance -5.1 4.2 3.0 4.6 1.0 3.1 2.5 1.6 1.6 0.6 1.5 Trace Amount system 100 100

Formulation example  3: nutrition cream

Formulation example of the nourishing cream containing a distant tree extract obtained by the method of Preparation Example 1 was prepared in the composition of Table 6 according to a conventional method (Example 3), nutrient cream without distant extract added as a comparative group ( Comparative Example 3) was also prepared.

ingredient Example 3 Comparative Example 3 Distant Extract Glycerin Vaseline Triethanolamine Liquid Paraffin Squalane Beeswax Tocopheryl Acetate Polysorbate 60 Carboxylvinyl Polymer Sorbanthesquioleate Flavor Preservative 2.0 4.0 3.5 2.1 5.3 3.0 2.6 5.4 3.2 1.0 3.1 Minor balance -4.0 3.5 2.1 5.3 3.0 2.6 5.4 3.2 1.0 3.1 Trace Amount system 100 100

Experimental Example 4: Whitening Effect Experiment of Cosmetic Composition

The whitening effect of the cosmetic composition of the present invention was measured in 30 Korean women aged 19-40 years, especially those with dark skin. 9 parts of the arms were measured by 1 cm in width and length, and the cosmetics of Examples 2 and 3 and Comparative Examples 2 and 3 prepared in Formulation Examples 2 and 3 were applied to each of the two parts, and the other one was compared. It was used as a control for. Each cosmetic was applied steadily for 8 weeks at 2 weeks interval, after 8 weeks to measure the skin color (L value) using Minolta CR 300 and calculated the degree of change of skin color (ΔL) using the following equation 4, The results are shown in Table 7 below.

Skin color change (ΔL) = L value before cosmetic application-L value after cosmetic application

Skin color gradient (ΔL) division Example 2 Example 3 Comparative Example 2 Comparative Example 3 Control ΔL value 1.72 1.50 0.20 0.50 0.00

As can be seen from the results of Table 7, 8 weeks after the ΔL value, the cosmetics of the present invention (Examples 2 and 3) containing the extract of distant trees did not contain distant trees (Comparative Examples 2 and 3) and the control group It was much higher than that. Therefore, it can be seen that the cosmetic composition of the present invention has a very good whitening effect.

Experimental Example 5: Skin irritation test of the cosmetic composition

50 healthy adult male and female subjects were tested for skin irritation of the products prepared according to the Examples and Comparative Examples. After a certain amount (approximately 0.1 g) of each sample (Examples 1 to 3 and Comparative Examples 1 to 3) was patched for 24 hours at 5 ㅧ 20 cm 2 in the lower arm of each subject, after 1 hour and 24 hours had elapsed. The skin condition change was visually checked and the degree of skin reaction was determined according to the skin response evaluation criteria of Table 8. In addition, the skin irritation rate was calculated using Equation 5 based on the result of the determination, and the results are shown in Table 9.

피부 자극율(%) = ㅧ 100

Skin irritation rate (%) = ㅧ 100

Skin Response Evaluation Criteria division Skin response No erythema or unusual symptoms - Slightly redder than the surroundings -+ Significantly redder than the surroundings + Severe redness and swelling than around ++

Skin response (persons) and skin irritation rate (%) division Example 1 Example 2 Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 - 47 48 48 46 48 47 -+ 3 2 2 4 2 3 + - - - - - - ++ - - - - - - Stimulation rate (%) 2.00 1.33 1.33 2.66 1.33 2.00

As can be seen from the results of Table 8, the cosmetic composition of Examples 1 to 3 of the present invention containing the far-tree extract has a nearly similar skin irritation rate compared to the cosmetic composition of Comparative Examples 1 to 3 not containing the far-tree extract It can be seen that the far tree extract of the present invention shows little irritation to the skin. Therefore, the cosmetic composition of the present invention was found to have less skin irritation and excellent skin safety.

As described in detail above, the present invention provides a cosmetic composition for skin whitening comprising a distant extract as an active ingredient. The mulberry extract of the present invention has an improved inhibitory effect on tyrosinase activity and an excellent melanin production inhibitory effect on melanocytes compared to the conventional whitening ingredients, and the cosmetic composition comprising the mulberry extract of the present invention exhibits an excellent skin whitening effect. In addition, the far-tree extract of the present invention can be effectively used as an active ingredient of the cosmetic composition because it hardly irritates the skin.

Claims (4)

Cosmetic composition for skin whitening, including distant ( Ilex rotunda ) extract as an active ingredient. The method of claim 1, wherein the far-tree extract is water, anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, propanol and butanol), acetone, ethyl acetate, chloroform, 1,3-butylene glycol and butyl acetate Cosmetic composition, characterized in that extracted using an extraction solvent selected from the group consisting of. The cosmetic composition according to claim 1, wherein the mulberry extract is contained in an amount of 0.0001-20.0 wt% based on the total weight of the cosmetic. The composition of claim 1 wherein the cosmetic composition consists of a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray Cosmetic composition, characterized in that it has a formulation selected from the group.