KR20130017159A - Composition for skin lightening comprising extract of ecklonia cava treated by enzyme - Google Patents

Abstract

PURPOSE: A composition containing an Ecklonia cava extract treated with an enzyme and a method for manufacturing the same are provided to suppress tyrosinase and melanogenesis. CONSTITUTION: A composition for skin whitening contains 0.001-20 wt% of an Ecklonia cava extract treated with an enzyme as an active ingredient. The enzyme is a cell wall degrading enzyme including celluclast or protease including pectinase. The composition is a cosmetic composition or a pharmaceutical composition. A method for preparing the composition comprises: a step of treating Ecklonia cava with an enzyme; and a step of extracting the enzyme-treated Ecklonia cava with water, an organic solvent, or a mixture thereof.

Description

Composition for skin lightening comprising extract of Ecklonia cava treated by enzyme}

The present invention relates to a skin whitening composition comprising an enzyme-treated Ecklonia cava extract.

Human skin color is determined by several factors, including the activity of melanocytes that produce melanin, the distribution of blood vessels, the thickness of the skin, or the presence of pigments such as carotenoids and bilirubin. Among them, the formation of melanin, a black pigment produced by melanocytes, is one of the most important factors for determining skin color by the action of various enzymes such as tyrosinase.

Melanin, which is present in the skin, plays an important role in protecting the body from UV rays.However, when excessive, melanin causes pigmentation of skin such as blemishes, freckles, and moles, and also promotes skin aging and causes skin cancer. It is known to work.

In order to treat or alleviate skin pigmentation due to melanin overproduction, several substances have been used that exhibit skin whitening effects, such as ascorbic acid, kojic acid, arbutin, hydroquinone, glutathione or derivatives thereof, but they are perfect skin It does not show the whitening effect, can not guarantee the safety of the body, if it is included in cosmetics, etc. difficult to formulate and even if formulated, there is a limit to its use is not secured.

Accordingly, studies on bio-friendly and stable natural substances showing skin whitening effects have been continued, and it has been reported that Ecklonia cava extract has a skin whitening effect. Endeavors to further improve the skin whitening effect of the Ecklonia cava extract have been completed the present invention.

Korean Patent Publication No. 10-2002-0015816 (published Mar. 02, 2002) Korean Patent Publication No. 10-2010-0097293 (published Sep. 03, 2010)

One aspect of the present invention is to provide a composition having an excellent skin lightening effect.

Another aspect of the present invention is to provide a method for producing a composition having an excellent skin whitening effect.

One aspect of the invention is an enzyme treatment Ecklonia cava ) Provides a composition for skin whitening comprising the extract as an active ingredient.

Another aspect of the invention the step of treating the enzyme in the Ecklonia; And it provides a method for producing a skin whitening composition comprising an enzyme-treated Ecklonia cava extract comprising the step of extracting the enzyme-treated Ecklonia cava in water, an organic solvent and a mixture of water and an organic solvent.

The composition according to the present invention includes an enzyme-treated Ecklonia cava extract as an active ingredient, thereby inhibiting the activity of tyrosinase and inhibiting melanin production, thereby effectively improving and treating blemishes, freckles, spots or skin pigmentation, and thus, excellent skin whitening effect. Can have

As used herein, the term "extract" refers to a substance obtained by extracting a component contained therein from a natural product, regardless of the method of extraction or the kind of the component. For example, it is a broad concept including both extracts of components dissolved in a solvent from natural products by using water or an organic solvent, and extracts of specific components of natural products, such as oils, and extracts of specific components.

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.

Hereinafter, the present invention will be described in detail.

One aspect of the present invention provides a composition for skin whitening comprising an enzyme-treated Ecklonia cava extract as an active ingredient. Enzymatically treated Ecklonia cava extract has a superior effect of inhibiting the activity of tyrosinase and inhibiting melanogenesis, compared to the general Ecklonia cava extract known to have a skin whitening effect, the composition comprising the same can have a very excellent skin whitening effect.

Another aspect of the invention the step of treating the enzyme in the Ecklonia; And it provides a method for producing a skin whitening composition comprising an enzyme-treated Ecklonia cava extract comprising the step of extracting the enzyme-treated Ecklonia cava in water, an organic solvent and a mixture of water and an organic solvent.

Ecklonia cava of the present invention is a perennial brown algae belonging to the Kelpaceae family, is widely used on the coast of Jeju Island and is also used for food.

In one aspect of the invention, the enzyme comprises one or more of cell wall degrading enzymes and proteolytic enzymes. Cell wall degrading enzymes widely include enzymes involved in the decomposition of plant cell walls, and specifically include cell degrading enzymes of cellulose, hemicellulose, pectin substances or lignin, which are the main components of the cell wall, and more specifically, celluclast. do. Proteolytic enzymes widely include enzymes that hydrolyze peptide bonds of proteins and peptides, and specifically include endopeptidase and exopeptidase, and more specifically, pectinase.

In one aspect of the invention, the Ecklonia cava is at a temperature of 25 ° C. to 70 ° C., specifically 30 ° C. to 60 ° C. and at a pH of 5 to 9, specifically at a pH of 6 to 8 for 10 minutes to 5 hours, specifically 30 minutes to 2 hours. Enzyme treatment.

In one aspect of the present invention, the enzyme-treated Ecklonia cava may be extracted with at least one selected from the group consisting of water, an organic solvent, and a mixture of water and an organic solvent to form an enzyme-treated Ecklonia cava extract. The organic solvent includes one or more selected from the group consisting of alcohol, acetone, ether, ethyl acetate, diethyl ether, ethyl methyl ketone and chloroform, but is not limited thereto. The alcohol includes a C ₁ ~ C ₅ lower alcohol, C ₁ ~ C ₅ lower alcohol is one selected from the group consisting of methanol, ethanol, isopropyl alcohol, n-propyl alcohol, n-butanol and isobutanol Including but not limited to the above.

The composition according to one aspect of the invention comprises from 0.001% to 20% by weight, in particular from 0.01% to 10% by weight, more specifically from 0.1% to 5% by weight, based on the total weight of the composition can do. When used in the above range is not only suitable for showing the intended effect of the present invention, it can satisfy both the stability and safety of the composition, it may be appropriate to use in the above range in terms of cost-effectiveness. Specifically, when the enzyme treated Ecklonia cava extract is less than 0.01% by weight, sufficient skin whitening effect may not be obtained, and when it exceeds 20% by weight, safety and formulation stability may be lowered.

One aspect of the present invention provides a composition for external application for skin containing an enzyme-treated Ecklonia cava extract as an active ingredient. Another aspect of the present invention provides a cosmetic composition comprising the enzyme-treated Ecklonia cava extract as an active ingredient.

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 include other ingredients in addition to the above-mentioned substances within the range not impairing the main effect, preferably giving a synergistic effect to the main effect. Specifically, it may further include kojic acid, arbutin or ascorbic acid derivatives which may increase the skin whitening effect of the cosmetic composition according to the present invention. In addition, the cosmetic composition according to the present invention may further include a moisturizer, an emulsifier, a surfactant, a ultraviolet absorber, a preservative, a bactericide, an antioxidant, a pH adjuster, organic and inorganic pigments, flavors, coolants, or limiting agents. have. The blending amount of the above components can be easily selected by those skilled in the art within the range that does not impair the object and effect of the present invention, the blending amount may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight based on the total weight of the composition. have.

One aspect of the present invention provides a pharmaceutical composition comprising the enzyme-treated Ecklonia cava extract as an active ingredient. The pharmaceutical composition may exhibit a skin lightening effect, and in particular, may improve or treat blemishes, freckles, moles, and skin pigmentation.

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 tablets, pills, soft and hard capsules, granules, powders, granules, solutions, emulsions or pellets, but are not limited thereto. It is not. Formulations for parenteral administration may be, but are not limited to, solutions, suspensions, emulsions, gels, injections, drops, suppositories, patches or spray formers. The formulations may be readily prepared according to conventional methods in the art and may be prepared by conventional means including, but not limited to, surfactants, excipients, wetting agents, emulsifying accelerators, suspending agents, salts or buffers for controlling osmotic pressure, colorants, spices, stabilizers, preservatives, Other commonly used adjuvants may be used.

The active ingredient of the pharmaceutical composition according to one aspect of the present invention will vary depending on the age, sex, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Dosage determination based on these factors is within the level of one skilled in the art and its daily dosage may be, for example, from 0.1 mg / kg / day to 100 mg / kg / day, more specifically from 5 mg / kg / day to 50 mg / kg. May be, but is not limited to.

Hereinafter, the structure and effects of the present invention will be described in more detail with reference to Preparation Examples, Comparative Examples, Examples and Test Examples. However, these preparation examples, comparative examples, examples and test examples are provided only for the purpose of illustration in order to facilitate understanding of the present invention, and the scope and scope of the present invention is not limited thereto.

Preparation Example Eckloniasis Powder Preparation

The Ecklonia cava is washed with purified water, dried and pulverized to obtain Ecklonia cava powder.

Comparative Example Preparation of Ecklonia cava Extract

2 g of Ecklonia cava powder obtained in Preparation Example was extracted with 100 mL of ethanol and then filtered. After filtration, the supernatant was dried under reduced pressure to obtain an Ecklonia cava extract having a dry weight of 0.30 g.

Example 1 Preparation of Enzymatic Treated Ecklonia cava Extract

20 mL of distilled water was added to 2 g of the Ecklonia cava powder obtained in Preparation Example, and then adjusted to pH 5-8 using 1M HCl and 1M NaOH. To this, celluclast and pectinase are added 2% (w / w), respectively. This is placed in a constant temperature water bath and stirred at 50 ° C. for 1 hour to react with the enzyme. The Ecklonia cava composition reacted with the enzyme is extracted with 100 mL of ethanol and filtered. After filtration, the supernatant was dried under reduced pressure to obtain an enzyme treated Ecklonia cava extract with a dry weight of 0.32 g.

Example 2 Preparation of Enzymatic Treated Ecklonia cava Extract

2 g of Ecklonia cava powder obtained in Preparation Example was extracted with 100 mL of ethanol and then filtered. The Ecklonia cava extract is then adjusted to a pH of 5-8 with 1M HCl and 1M NaOH. Subsequently, 2% (w / w) of celluclast and pectinase are added to the extract. This is placed in a constant temperature water bath and stirred at 50 ° C. for 1 hour to react with the enzyme. After filtering the Ecklonia cava extract reacted with the enzyme, the supernatant was dried under reduced pressure to obtain an enzyme-treated Ecklonia cava extract having a dry weight of 0.18 g.

Test Example 1 Evaluation of Inhibitory Effect of Tyrosinase Activity

To evaluate the effect of inhibiting tyrosinase activity of the comparative example and the example, the following test was conducted. Mushroom tyrosinase and tyrosine were obtained from Sigma Chemical. Comparative Ecklonia cava extract and Example Enzyme Treatment with 150 μl of 0.1 M phosphate buffer (pH 6.5), 8 μl of mushroom tyrosinase (2,100 units / ml, 0.05 M phosphate buffer, pH 6.5) and 36 μl of 1.5 mM L-tyrosine Ecklonia cava extracts were treated respectively. After enzymatic reaction of the test material for 20 minutes at 37 ℃ was measured for the tyrosinase activity by measuring the absorbance at 490 nm with a microplate reader (Bio-Rad 3550, Richmond, California, USA). The concentration of each test substance (IC ₅₀ ) required to reduce tyrosinase activity by half was calculated and the results are shown in the table below.

Test substance IC ₅₀ Kojic acid 200 ppm Arbutin 420 ppm Comparative example 240 ppm Example 1 174 ppm Example 2 160 ppm

As can be seen from the results, the effect of inhibiting tyrosinase activity of the enzyme-treated Ecklonia cava extract of Examples 1 and 2 compared to the Ecklonia cava extract of Comparative Example. Therefore, the Ecklonia cava extract treated with enzyme has an excellent inhibitory effect on tyrosinase activity, and further it can be seen that it has an excellent skin whitening effect.

[Test Example 2] melanin production inhibitory effect

The degree of melanin production in melanocytes was produced by Dooley's method. The cell line used Mel-Ab cell line derived from skin pigment cells of C57BL / 6. Incubation was performed at 37 ° C., 5% CO _It carried out under the conditions of ₂ . The cultured Mel-Ab cells were detached with 0.25% Trypsin-EDTA, inoculated in the same number (1 × 10 ⁵ cells / well) again in a 24-well vessel and then compared for 2 consecutive days. The test material was treated by replacing the medium with each of the examples. After 5 days, the melanin was dissolved by treating with 1N NaOH, and the absorbance was measured at 400 nm to determine the amount of melanin. The concentration of test substance (IC ₅₀ ) required to reduce melanin production in melanocytes by half is calculated and the results are shown in the table below.

Test substance IC ₅₀ Kojic acid 1500 ppm Arbutin 180 ppm Comparative example 112 ppm Example 1 89 ppm Example 2 71 ppm

As can be seen from the above results, melanin production inhibitory effect of Examples 1 and 2 is superior to kojic acid and arbutin, which are known to have a skin whitening effect. In addition, compared to the Ecklonia cava extract of Comparative Example, the enzyme-treated Ecklonia cava extract of Examples 1 and 2 is superior to the melanin production inhibitory effect. Therefore, the Ecklonia cava extract treated with enzyme has an excellent melanin production inhibitory effect, and further has an excellent skin whitening effect.

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 described in the table below.

Content (% by weight) Enzyme Treatment Ecklonia Extract 2.0 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 PEG 12 nonyl phenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water Balance

Formulation Example 2 @ Nutritional Cream

Nutritive creams are prepared according to the usual methods with the composition shown in the table below.

Content (% by weight) Enzyme Treatment Ecklonia Extract 2.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.5 PEG 60 hardened castor oil 2.0 Liquid paraffin 10.0 Squalane 5.0 Caprylic / caproic triglyceride 5.0 glycerin 5.0 Butylene glycol 3.0 Propylene glycol 3.0 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 3] Massage cream

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

Content (% by weight) Enzyme Treatment Ecklonia Extract 1.0 Wax 10.0 Polysorbate 60 1.5 PEG 60 hardened castor oil 2.0 Sorbitan sesquioleate 0.8 Liquid paraffin 40.0 Squalane 5.0 Caprylic / capric triglyceride 4.0 glycerin 5.0 Butylene glycol 3.0 Propylene glycol 3.0 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 4] Pack

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

Content (% by weight) Enzyme Treatment Ecklonia Extract 1.0 Polyvinyl alcohol 13.0 Sodium carboxymethylcellulose 0.2 glycerin 5.0 Allantoin 0.1 ethanol 6.0 PEG 12 nonyl phenyl ether 0.3 Polysorbate 60 0.3 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 5]

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

Content (% by weight) Enzyme Treatment Ecklonia Extract 0.5 Ethylenediamine sodium acetate 0.05 glycerin 5.0 Carboxyvinyl polymer 0.3 ethanol 5.0 PEG 60 hardened castor oil 0.5 Triethanolamine 0.3 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 6] ointment

Ointment was prepared by the conventional method with the composition shown in the following table.

Content (% by weight) Enzyme Treatment Ecklonia Extract 0.1 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / Capric Triglycerides 3.0 Squalane 1.0 Cetearyl Glucoside 1.5 Sorbitan stearate 0.4 Cetearyl Alcohol 1.0 Wax 4.0 Preservative, coloring, fragrance Suitable amount Purified water Balance

Claims (9)

Enzyme-treated Eckloniasis ( Ecklonia) cava ) Skin whitening composition comprising the extract as an active ingredient.
The method of claim 1,
The enzyme comprises at least one of cell wall degrading enzymes and proteolytic enzymes.
The method of claim 2,
The cell wall degrading enzyme comprises celluclast, and the proteolytic enzyme comprises pectinase.
The method of claim 1,
The composition comprises from 0.001% to 20% by weight of an enzyme treated Ecklonia cava extract based on the total weight of the composition.
The method of claim 1,
The composition is a composition that inhibits the activity of tyrosinase.
The method of claim 1,
The composition is a composition that inhibits melanin production.
7. The method according to any one of claims 1 to 6,
Wherein the composition is a cosmetic composition.
7. The method according to any one of claims 1 to 6,
The composition is a pharmaceutical composition.
A method for preparing a composition according to any one of claims 1 to 6,
Treating the enzyme with Ecklonia cava ; And
Method for producing a composition for skin whitening comprising an enzyme-treated Ecklonia cava extract comprising the step of extracting the enzyme-treated Ecklonia cava at least one selected from the group consisting of water, an organic solvent and a mixture of water and an organic solvent.