KR100879900B1 - The cosmetics composition for beautification skin containing the Rubus parvifolius extracts as effective components - Google Patents

Abstract

The present invention relates to a cosmetic composition for skin whitening containing Rubus parvifolius extract as an active ingredient, the Rhus berry extract not only has a strong antioxidant activity but also inhibits melanin production and inhibits tyrosinase activity, in particular. Since there is little cytotoxicity, it may be usefully used as a cosmetic composition for skin whitening.

Moonberry Extract, Whitening, Cosmetics, Composition

Description

The cosmetics composition for beautification skin containing the Rubus parvifolius extracts as effective components}

The present invention relates to a composition for whitening containing Rubus parvifolius extract and Rubus parvifolius extract for antioxidant.

Skin protects the human body from the external environment and consists of the epidermis, dermis and subcutaneous fat layer. Determining the color of a person has many factors such as platelets, melanin and keratin, but melanin pigments have the greatest effect on skin brightness. These melanin pigments are produced in endoplasmic reticulum in the form of melanosomes, and melanosomes are made in cells called melanocytes. Melanocyte endoplasmic reticulum produced by melanocytes is transferred to keratinocytes, keratinocytes, is transferred from the basal epidermal layer to the stratum corneum through keratinization process, and separated from the skin with keratinocytes lost every 28 days.

Melanin absorbs ultraviolet rays and protects cells in the skin. If melanin is not produced smoothly, pigmented diseases such as vitiligo may occur. On the contrary, if melanin is excessively produced, blemishes, freckles, and the like are generated, and such lesions may cause skin cancer.

The blackening of the skin caused by melanin causes a problem in terms of beauty, and mainly Asian women are required to suppress the production of melanin as white skin is regarded as a standard of beauty.

A major factor in melanogenesis is an enzyme called tyrosinase, which produces melanin by tyrosine being oxidized by tyrosinase to dopa and then converted to dopachrome. The reaction after dopachrome can occur only by spontaneous oxidation, so the first and second steps of oxidizing tyrosine are the key part of melanogenesis. Therefore, studies on tyrosinase inhibition, which is a major factor of melanogenesis, are actively conducted to prevent skin blackening.

In the conventional cosmetic field, as a whitening component, substances that inhibit tyrosinase enzyme activity such as kojic acid, arbutin, hydroquinone, vitamin-C (L-Ascorbic acid), and derivatives thereof Various plant extracts have been used.

However, the whitening ingredients are poor in stability in the prescription system, and are degraded or colored, or their use is limited due to the occurrence of off-flavor, efficacy at the biological level, unclear effect and safety problems. For example, kojic acid inhibits enzymatic activity by adsorbing copper ions present in the active site of tyrosinase, but when used in cosmetics, instability, problems of skin side effects, and recent animal experiments have revealed liver cancer. Stopped. Vitamin-C and its derivatives are difficult to use as raw materials for cosmetics due to their oxidative instability. Hydroquinone has excellent whitening effect on the skin but causes allergy, toxicity to melanocytes, and permanent depigmentation to the skin. It is highly irritating to skin, and is recently prescribed as a carcinogenic substance, so its use is banned and only a limited concentration is allowed in each country. In addition, arbutin is a derivative in which glucopyranoside is combined with hydroquinone, and has little side effects when using hydroquinone and inhibits the synthesis of melanin pigments without toxicity to humans, thereby increasing melanin pigmentation. Although it has been suggested that it can be used as a therapeutic agent for skin diseases, it is disadvantageous to be partially degraded by skin enzymes.

In addition to these whitening substances, research has been conducted to find whitening active ingredients in natural products, especially plants. Among them, white skin (Japanese Patent Publication No. 55-44375, Small 64-26507, Small 64-83009, Pyeong 1-25687 No. 5-139950, Korean Patent Publication Nos. 92-002109, 97-021273, Licorice (Japanese Patent Laid-Open No. 60-214721, No. 60-214728, No. 63-23809, No. 64- 63506, Hei 1-149706, and Korean Patent Nos. 92-002109, 97-025601), Peony (Japanese Patent Laid-Open No. 61-246109 and Korean Laid-Open Patent No. 92-002111), Cinnamon Patent Nos. 63-30403, Hep. 5-139954), Gosam (Japanese Patent Laid-Open No. 64-26507 and Korean Patent Laid-Open No. 92-002110), Brown root (Japanese Laid-Open Patent Nos. 60-214727, Small 64-16709 ), Angelica (Japanese Patent Laid-Open No. 56-92211, Hei 4-26610), Mokdanpi (Japanese Laid-Open Patent No. 60-214721, No. 61-50915, No. 61-246109), Banha (Japanese Laid-Open Patent Publication) Pyeong 2-207028, for A number of plant extracts and herbal extracts such as Korean Patent Publication No. 96-033442) and Aloe (Japanese Patent Laid-Open No. 52-44375, Hei 2-207030, Hei 5-139950) act on tyrosinase to act as melanin. Although it has been found that the production is suppressed, they also have a lot of problems in the use of more than the effective concentration in cosmetics or pharmaceuticals in terms of safety, discoloration, etc., and still does not show an excellent effect.

The present inventors have been known in Korea, Japan, Taiwan, China, etc., but the effect is related to anti-cancer, anti-inflammatory, but have not been reported whitening effect, but the fruit extract reduces melanin production, tyrosinase activity It is to suppress and have an antioxidant effect, it was to reveal that it can be usefully used as a composition for skin whitening.

Accordingly, it is an object of the present invention to provide a cosmetic composition for skin whitening comprising a strawberry extract.

In addition, another object of the present invention is to provide an extract of dabberry for antioxidant.

In order to achieve the above objects as well as yet another object that can be easily expressed in the present invention by preparing the gumsberry extract, by adding it to 0.001 ~ 30.0% by weight to the known cosmetic composition can obtain a cosmetic excellent in skin whitening effect It was confirmed that the bilberry extract can be used for antioxidant.

The cosmetic composition for skin whitening according to the present invention is a cosmetic composition for skin whitening not only has a powerful antioxidant activity but also inhibits melanin production and inhibits tyrosinase activity, and in particular, shows little cytotoxicity. It can be usefully used.

In addition, the berry extract has a strong antioxidant activity can be useful for the antioxidant of various products.

The present invention provides a cosmetic composition for skin whitening and an extract of strawberry berry for extract including the strawberry berry extract.

The whitening effect of the cosmetic composition is characterized by inhibition of melanin production, inhibition of tyrosinase activity.

Rubus parvifolius is a deciduous shrub of the family Rosaceae, with short thorns, leaves alternate, 3 small leaves, but 5 in number. Small leaves are broad-shaped, egg-shaped, round. The small leaf at the end is often divided into three, fine hairs on the surface, dense white hairs on the back, and serrated at the edges. Flowers bloom in red in May and up. Fruits are round, round, ripen in July-August and taste good. Hairless leaves on the back of the chungseom strawberry, the length of the leaves are about 2cm and the thorns on the stem is also known as Sasson strawberry. It grows in the lower part of the foothills of Korea, Japan and Taiwan. Fruits are reproduced and outposts are effective for wild fish, pain, detoxification, insecticide, and hemorrhage, bruises, postpartum body pain, dysentery, intestinal tract, inflorescence and nausea. Roots have the effect of clearing, detoxification, swelling, diarrhea, blood loss, small bowel, and other treatments for high fever, sore throat, hepatitis and rheumatic pain caused by cold.

Dabberberry extract according to the present invention can be prepared as follows.

In order to obtain the berry extract used as an active ingredient of the cosmetic composition of the present invention, the berry is dried in a cool place and then physically pulverized, and then extracted by adding an extraction solvent to the pulverized product. Examples of the extraction solvent include distilled water, anhydrous alcohols having 1 to 4 carbon atoms (methanol, ethanol, propanol, butanol), acetone, ethyl acetate, chloroform, glycerin, butylene glycol, propylene glycol, dichloromethane, hexane and benzene. At least one selected may be used alone, or two or more solvents may be mixed and used. The ratio of the pulverized product and the solvent is 1:10 to 1:30, preferably 1:20. It is extracted in the extractor and freeze dried.

On the other hand, the berry strawberry extract is effective to contain 0.001 to 30.0% by weight, preferably 0.1 to 10.0% by weight relative to the total weight of the cosmetic composition. If the content of the berry strawberry extract is less than 0.001% by weight, it is difficult to expect the effect, when it exceeds 30.0% by weight does not appear to increase the apparent effect of the increase in content.

The strawberry fruit extract according to the present invention has a whitening effect of reducing melanin production by melanogenesis cells (Table 1) and inhibiting tyrosinase activity (Table 2). In addition, it has an antioxidant effect (Table 3) that eliminates free radicals and is less cytotoxic (Table 4).

Therefore, the berry strawberry extract of the present invention can be effectively used as a whitening composition for inhibiting excessive melanin production. In addition, it can be usefully used for antioxidants in various products.

The composition of the present invention may further contain one or more active ingredients exhibiting the same or similar function in addition to the berry extract.

Cosmetics made of a cosmetic composition containing the berry extract of the present invention as an active ingredient can be prepared in the form of a general emulsion formulation and solubilized formulation. Cosmetics of the emulsified formulations include nutrient cosmetics, creams, essences, etc., and cosmetics of the solubilized formulations are flexible cosmetics. In addition to the cosmetic containing the wormwood extract of the present invention, by containing a dermatologically acceptable medium or base may be prepared in the form of a topical or systemic application commonly used in the field of dermatology.

Suitable cosmetic formulations include, for example, emulsions, suspensions, microemulsions, microcapsules, microgranules or ionics (liposomes), nonionics obtained by dispersing an oil phase in a solution, gel, solid or pasty anhydrous product, aqueous phase. It may be provided in the form of a vesicle dispersant, in the form of a cream, skin, lotion, powder, ointment, spray or conceal stick. It may also be prepared in the form of a foam or in the form of an aerosol composition further containing a compressed propellant.

In addition, the cosmetic composition of the present invention, in addition to the bilberry extract, fatty substances, organic solvents, solubilizers, thickening and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, Commonly used in water, ionic or nonionic emulsifiers, fillers, metal ion sequestrants and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or cosmetics And any other ingredients that may be used, such as adjuvants commonly used in the cosmetic or dermatological arts. In addition, the above components may be introduced in an amount generally used in the field of dermatology.

Examples of products to which the cosmetic composition of the present invention may be added include, for example, cosmetics such as astringent cosmetics, soft cosmetics, nourishing cosmetics, various creams, essences, packs, foundations, and the like, cleansing agents, soaps, treatments, and essences. Etc.

Specific formulations of the cosmetic composition of the present invention include skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, essence, nutrition essence, pack, Formulations such as soaps, shampoos, cleansing foams, cleansing lotions, cleansing creams, body lotions, body cleansers, emulsions, press powders, loose powders, eye shadows and the like.

Hereinafter, preferred examples and experimental examples are presented to help understand the present invention. However, the following Examples and Experimental Examples are provided only to more easily understand the present invention, and the contents of the present invention are not limited by the Examples.

Preparation Example 1 Preparation of Dabber Extract for Skin Whitening

The stupid strawberry of this example was used in Korea.

Dry the leaves and fruits of the berry in a cool shade. Thereafter, finely crushed the dried dried strawberry by using a grinder, 200g of the pulverized product is put in a reflux extractor, and 20% of 70% ethanol of the weight of the ground crushed strawberry is put there and extracted by heating at 75 ° C. for 10 hours. The extract was filtered with a 400 mesh filter cloth, and the filtrate was collected and lyophilized.

Test Example  One : Intracellular  Melanin inhibitory effect

B16F1 melanoma cells were provided by the Korea Cell Line Bank and cultured. B16F1 melanoma cells are cell lines producing melanin and are generally used for screening whitening substances.

The medium for culturing the cells was sterile by adding DMEM, 10% FBS, 1% penicillin / streptomycin. Cell cultures were incubated in an incubator at 37 ° C., 5% CO ₂ . Melanoma cells were cultured and passaged when the 100 mm Petri dishes were about 90% full.

In order to measure the whitening effect of the fruit extract, the amount of melanin produced by treating B16F1 melanoma cells was measured. Cells were seeded on the 6 well plate and treated with the Rhozollum extract prepared in Preparation Example 1 at a concentration of 200 µg / ml, and then cultured for 2 days to recover the cells. The recovered cells were added with 1N NaOH containing 10% DMSO, reacted at 90 ° C for 1 hour to be sufficiently dissolved in melanin, and the absorbance was measured at a wavelength of 405 nm using an ELISA reader.

Experimental results were calculated using the following equation, the inhibition is shown in Table 1. Arbutin, which is known as a general whitening substance, has a melanin production inhibitory effect similar to that of arbutin, while Arbutin has a melanin content of 70.6% at a concentration of 200 ㎍ / ml, compared to the untreated group. Could.

Melanin Formation (%) = Treatment Absorbance / Untreated Absorbance × 100

Sample Name Untreated Arbutin  Dabberberry Extract Melanin Production (%) 100 70.6 69.1

Test Example  2: measurement of tyrosinase activity inhibition

It was determined whether the locust fruit extract affected tyrosinase enzyme activity, which plays an important role in producing melanin.

20 μl of 0.1 M phosphate buffer (pH 6.8) is added to the 96 well plate, 200 μg / ml of berry extract or 50 μl of distilled water is added, followed by 10 μl of mushroom-derived tyrosinase. After adding 20ul of 5mM L-DOPA as a substrate and reacting for 2 minutes at 37 ℃, the absorbance was measured at a wavelength of 475nm using an ELISA reader.

Tyrosinase activity was calculated using the following formula, and the melanin inhibitory effect of koji acid and the extract, which was widely used as a whitening agent, is shown in Table 2. When Koji acid was treated, only 2.5% of the total activity was active, whereas when treated with locust berries extract showed about 50.4% activity. Compared with koji acid, the inhibitory effect was weak, but the barkberry extract was found to inhibit the tyrosinase enzyme activity more than 49.6% compared to the untreated.

Tyrosinase Activity (%) = Treated Absorbance / Untreated Treated Absorbance × 100

Sample Name Untreated Kojisan Dabberberry Extract Tyrosinase Activity (%) 100 2.5 50.4

Test Example  3: toxicity test

In order to use the bilberry extract as a whitening cosmetic, an experiment was carried out to check for cytotoxicity. Cells were inoculated into 96 well plates and treated with 200 ug / ml of the berry extract, and after 2 days, the medium was removed. After lysis, the absorbance was measured at a wavelength of 540 nm using an ELISA reader.

Cell viability was calculated using the following formula, and the results are shown in Table 3. Compared to the cells that did not receive the berry extract, despite the high concentration of 200 ㎍ / ㎖, the viable cell rate is 99.8%, it can be seen that there is little cytotoxicity.

Cell viability (%) = (1-treated absorbance / untreated absorbance) × 100

Sample Name Untreated Arbutin Dabberberry Extract Cell survival rate (%) 100 98.3 99.8

Test Example 4: Antioxidant Activity Experiment I

In order to confirm the antioxidant activity of the wormwood extract, it was generally measured using a DPPH solution, which is a method of measuring antioxidant activity.

After mixing 25 μg / ml of the Rhodiola raspberry extract and 100 μl of DPPH solution, which is an antioxidant measurement solution, and reacting at 37 ° C. for 30 minutes, the absorbance was measured at 570 nm using an ELISA reader.

Experiments with vitamin C, known as antioxidants, compared the relative activity of extracts. As can be seen from Table 4, it was found that the antioxidant activity of the berry fruit extract was 80.7%, indicating that it had a strong antioxidant power. Of particular note is that the fruit berry extract showed 4.5 times better antioxidant activity than vitamin C.

% Antioxidant activity = (1-treated absorbance / untreated absorbance) × 100

Sample Name Vitamin c Dabberberry Extract Antioxidant activity (%) 17.9% 80.7%

Test Example 5: Antioxidant Activity Experiment II

As another method of measuring the antioxidant activity of the locust strawberry, Superoxide dimutase like activity (Superoxide scavenging activity) was measured by NBT assay.

Add 10ul of NBT solution to a 96-well plate and 40ul of Xanthine as a substrate. Add 25 ㎍ / ㎖ of berry strawberry extract and phosphate buffer, and add 20ul of enzyme xanthine oxidase. After reacting at 25 ° C. for 20 minutes, the absorbance was measured at a wavelength of 560 nm using a LISA reader.

As can be seen from Table 5, the NBT activity of the berry extract was very high at 41.5%.

Superoxide scavenging effect (%) = (1-treatment absorbance / untreated absorbance) × 100

Sample Name Dabberberry Extract Superoxide Scavenging Effect (%) 41.5%

Examples of preparations for the compositions of the present invention are illustrated below.

Production Example  2 : Example  And Comparative example

To prepare a cosmetic composition containing the extract of Ruffberry of Preparation Example 1, and to compare with the cosmetic composition lacking Ruffberry extract was prepared in the composition ratio of Table 6.

division Content (% by weight) ingredient Example Comparative example Dabberberry Extract 4.0 - Cetearyl Octanoate 5.0 5.0 Isopropyl Palmitate 5.0 5.0 Polyacrylamide / C13-14 Isoparaffin / Laureth-7 2.0 2.0 Polysorbate 60 1.7 1.7 Solbitan Sesquioleate 1.3 1.3 Spices, preservatives dose dose Purified water Remaining amount Remaining amount Sum 100 100

Test Example  5

In order to test the clinical whitening efficacy of the cosmetics of the present invention, 40 healthy adult men and women with blemishes, freckles and pigmentation were randomly divided into two groups (A and B) of 20 people, and then performed on the A group. For example, after applying the comparative example twice a day for 12 weeks for group B, the change in skin color was measured using chromatameter (Minolta CR300), and the change in color brightness (ΔL) was measured. Objective visual observation by and subjective visual observation by subject were performed to measure the whitening effect. The results are shown in Table 7 below. At this time, the degree of whitening efficacy was classified into the following seven ratings.

* Evaluation criteria for whitening efficacy:

-3: very bad -2: worse -1: slightly worse 0: no change

 1: slightly improved 2: improved 3: highly improved

Subject Change in brightness of skin color (△ L) Objective evaluation of the skilled person Subjective Evaluation of Subject A group B group A group B group A group B group One 5.7 2.5 2 0 One One 2 4.7 2.7 2 0 3 0 3 4.6 2.2 3 One 3 One 4 4.4 1.8 One 0 2 One 5 4.9 2.1 3 0 One 0 6 5.2 2.4 3 One 3 One 7 4.7 0.7 One 0 2 One 8 4.0 0.1 2 One One 2 9 4.8 2.5 One One One One 10 4.8 2.9 2 0 2 0 11 4.2 3.4 One 0 0 -One 12 3.9 3.9 3 0 0 0 13 4.1 2.4 2 0 2 One 14 4.9 2.7 One 0 2 0 15 4.3 2.2 3 One 3 One 16 5.5 3.5 2 One 0 0 17 5.6 2.9 2 0 One 0 18 5.2 2.2 One 0 2 One 19 5.2 3.0 0 0 0 0 20 5.1 2.7 2 2 One 0 Average 4.8 2.4 1.9 0.4 1.5 0.5

In the results shown in Table 7, the change in skin brightness was twice as effective when applying the Example compared to the Comparative Example, the objective evaluation of the skilled person and subjective evaluation of the subject was also applied when the Comparative Example was applied to the Example In comparison, the improvement was 4.75 and 3 times higher.

As a result, the fact that can be confirmed through the results shown in Table 7 can be seen that the cosmetics containing the rosemary extract prepared by the preparation example according to the present invention exhibits an excellent effect as to enhance the skin whitening effect.

Formulation Example 1: Flexible Lotion

Based on the results of the preliminary experimental example, to present a cosmetic composition containing the berry strawberry extract of the present invention. However, the composition of the present invention is not intended to be limited to the following formulation examples. Formulation example of the flexible lotion containing the fruit berry extract was prepared as shown in Table 8.

Raw material Content (% by weight) Dabberberry Extract 2.00 1,3-butylene glycol 1.00 Disodium ID 0.05 Allantoin 0.10 Dipotassium glycylizate 0.05 Citrix Acid 0.01 Sodium citrate 0.02 Glyceres-26 1.00 Arbutin 2.00 Hydrogenated Castor Oil 1.00 ethanol 30.00 Preservative a very small amount coloring agent a very small amount Flavor a very small amount Purified water Remaining amount

Formulation Example 2: Nutrition Cream

An example of the preparation of the nourishing cream containing the berry strawberry extract was prepared as shown in Table 9.

Raw material Content (% by weight) Dabberberry Extract 10.0 1,3-butylene glycol 7.0 glycerin 1.0 D-panthenol 0.1 Plant extracts 3.2 Magnesium Aluminum Silicate 0.3 PEG-40 Stearate 1.2 Stearic acid 2.0 Polysorbate 60 1.5 Lipophilic glyceryl stearate 2.0 Sorbitan sesquioleate 1.5 Cetearyl Alcohol 3.0 Mineral oil 4.0 Squalane 3.8 Carlylic / Capric Triglycerides 2.8 vegetable oil 1.8 Dimethicone 0.4 Dipotassium glycylizate a very small amount Allantoin a very small amount Sodium hyaluronate a very small amount Tocopheryl Acetate Quantity Triethanolamine Quantity Preservative Quantity Flavor Quantity Purified water Remaining amount

Claims (7)

Cosmetic composition for skin whitening containing Rubus parvifolius extract as an active ingredient The cosmetic composition for skin whitening according to claim 1, wherein the dapberry extract is extracted by adding at least one polar solvent selected from the group consisting of water, a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof. The cosmetic composition for skin whitening according to claim 1, wherein the berry extract is contained in an amount of 0.001 to 30.0 wt% based on the total weight of the cosmetic composition. The cosmetic composition for skin whitening according to claim 1, wherein the skin whitening effect of the composition is due to inhibition of melanin production. The cosmetic composition for skin whitening according to claim 1, wherein the skin whitening effect of the composition is due to inhibition of tyrosinase activity. The skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisture lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, essence, nutrition essence according to any one of claims 1 to 5 Cosmetics for skin whitening, comprising any of the following formulas: packs, soaps, shampoos, cleansing foams, cleansing lotions, cleansing creams, body lotions, body cleansers, emulsions, press powders, loose powders and eye shadows Composition. delete