KR20020046615A - Skin whitening composition containing arctium lappa extracts - Google Patents

Abstract

PURPOSE: A whitening agent containing an Arctii Fructus extract as a main material is provided. By directly acting on a melanin metabolic pathway induced by α-MSH, it exhibits excellent whitening action. CONSTITUTION: This whitening agent contains 0.0001 to 50.0% by weight of an Arctii Fructus extract, based on the total dried weight of the whitening agent. The fructus of Arctium lappa is ground and soaked in a solvent at room temperature for 1 to 15 days and concentrated under reduced pressure, wherein the solvent is selected from water, lower alcohol, a mixture of water and lower alcohol, acetone, ethylacetate, 1,3-butylene glycol, hexane, diethylether, n-propanol, iso-propanol, n-butanol.

Description

Skin whitening composition containing arctium lappa extracts}

The present invention relates to a whitening agent containing milkybean extract, purified from the fruit of Burdock ( Arcium lappa ).

One of the main themes of cosmetics is whitening cosmetics that whiten the skin by eliminating blemishes, freckles, etc., or suppressing their production. Recently, studies on the effects of various plant resources on skin physiology have been actively conducted. From this, materials having excellent stability and excellent skin whitening effect have been developed.

Human skin color varies according to ethnicity, individual, and body parts, but the pigment that determines skin and hair color is melanin. Melanin pigment is made by oxidizing and polymerizing by melanin synthase (Tyrosinase) action based on one of the amino acids Tyrosine in melanocytes (Melanocyte) scattered on the basement layer of the epidermis. Melanin not only determines the color of human skin, but also absorbs ultraviolet rays and protects the skin from harmful UV rays.However, melanin can cause pigmentation and freckles when excessively generated in the skin by UV exposure or inflammation.

Melanin production in melanocytes is influenced by several factors, including external conditions, hormones, and cytokines. Α-Melanocyte stimulating hormone (α-MSH) is an important hormone involved in skin pigmentation and is produced by protein hydrolysis of POMC (Proopiomelanocortin) protein. It is secreted from cells (Keratinocyte) and acts on melanocytes, causing pigmentation. Therefore, in order to prevent the pigmentation phenomenon, it can be suppressed by controlling some of the melanin production process.

Conventional whitening agents such as kojic acid (arbutin), arbutin, lettuce extract and licorice extract play a role in inhibiting the activity of tyrosinase. Substances having such a mechanism of action have an effect by directly interacting with tyrosinase, and it is difficult to show an effect when absorption into skin cells and penetration into melanosomes are not easy.

Therefore, the present inventors have tried to develop a whitening cosmetic composition that can exhibit a whitening effect more effectively than a substance that inhibits only the activity of the existing melanin synthase. As a result, allium extract can directly control and inhibit melanin production by directly acting on melanin metabolic pathways induced by α-MSH, showing much better effects than conventional whitening agents and broadening its application to whitening products. It was found and completed the present invention.

Accordingly, it is an object of the present invention to provide a whitening agent containing an allergy extract capable of suppressing the activity of α-MSH induced by ultraviolet rays and exhibiting an excellent whitening effect.

1 is a diagram showing the inhibitory effect of the allergy extract on the expression of melanin synthase in melanocytes.

The present invention relates to a whitening agent containing allium extract.

Allium extract of the present invention is contained in an amount of 0.0001 to 50.0% by weight, preferably 0.005 to 5.0% by weight based on the total dry weight of the whitening agent.

Allies are the fruit of burdock, an Asteraceae plant. Burdock is a biennial herb of Asteraceae, with 40 cm long petiole on its root. The leaf is heart shaped with white hairs on the back. In the spring of 2nd or 3rd year, a flower stem 1.5cm in height and several purple flowers like thistle bloom. Wild species grow in Europe, Siberia, and Manchuria. In Europe, young leaves and roots are sometimes eaten, and fruit is used as a diuretic in China. Originally grown as a food and medicinal plant in farmhouses, it grows around roads and on hillsides. Collect it in late autumn, remove the debris and dry it in the sun.

In the present invention, allies suitable for the above properties were used.

The manufacturing method of the allergy extract of the present invention is as follows.

The dried parts of the burdock are washed with clean water, dried and powdered. The dry weight of the powdered milkybean is extracted with water, lower alcohol (methanol and ethanol), a mixture of water and lower alcohol, acetone and ethyl as extraction solvents. Acetate, 1,3-butylene glycol, hexane, diethyl ether, normal propanol, iso-propanol and normal-butanol are added in an amount of 1 to 15 times, and the active ingredient is extracted by immersion at room temperature for 1 to 15 days. The extraction solution thus extracted is concentrated under reduced pressure using a distillation apparatus equipped with a cooling condenser to obtain the desired mate extract of the present invention.

The whitening agent containing the allergy extract of the present invention is not particularly limited in the formulation, for example, cosmetics for basic products such as lotion, cream, essence, cleansing foam, cleansing water, pack and body oil; Color cosmetics such as foundation, lipstick, mascara, makeup base, etc .; And hair cosmetics such as shampoos, rinses, hair conditioners, hair gels, and the like.

The following Examples, Experimental Examples, and Formulation Examples illustrate the content of the present invention, but the content of the present invention is not limited thereto.

Example 1

After washing with purified water and drying, 1Kg of powdered milk powder was added to 5L of water, extracted for 5 days at 15-40 ° C., filtered through 300 mesh filter cloth, left at 4-15 ° C. for 7-10 days, and then aged at low temperature. It was filtered twice by filter paper. The extract was concentrated under reduced pressure at 60 ° C. in a distillation apparatus equipped with a cooling condenser and dried to obtain 60.4 g (dry weight).

Example 2

After washing with purified water and drying, 1Kg of powdered milk powder was added to 5L of 10% ethanol, extracted for 3 days in an extractor equipped with a cooling condenser, filtered through a 300 mesh filter cloth, and left at 4 to 15 ° C for 7 to 10 days to mature at low temperature. After filtration was performed using Whatman No. 2 filter paper. The extract was concentrated under reduced pressure at 60 ° C. in a distillation apparatus equipped with a cooling condenser and dried to obtain 78.6 g (dry weight).

Examples 3 to 21

Using the solvent described in Table 1 below to extract the method of Example 2 to obtain a dry weight as described in Table 1 below.

division menstruum Dry weight in g Example 3 20% ethanol 80.5 Example 4 30% ethanol 83.1 Example 5 40% ethanol 88.4 Example 6 50% ethanol 92.7 Example 7 60% ethanol 98.6 Example 8 70% ethanol 108.1 Example 9 80% ethanol 107.4 Example 10 90% ethanol 107.8 Example 11 100% ethanol 107.3 Example 12 80% methanol 98.7 Example 13 100% methanol 99.2 Example 14 Acetone 36.8 Example 15 Ethyl acetate 66.8 Example 16 50% 1,3-butylene glycol aqueous solution 10.4 Example 17 Hexane 24.5 Example 18 Diethyl ether 20.2 Example 19 Normal-propanol 21.7 Example 20 Iso-propanol 27.9 Example 21 Normal-butanol 19.7

Experimental Example 1

The melanin production inhibitory effect of the already prepared allergy extract was measured.

1) Experiment Method

Allium extract was used to make an allium powder in high concentration in 1,3-butylene glycol, diluted in buffer solution, and then adjusted to an appropriate concentration to make an extract sample solution. Melanosite was used by purchasing a mouse-derived B-16 melanoma (ATCC CRL 6323) cell line. α-MSH was dissolved in 10% DMSO (dimethyl sulfoxide) and used as a 1 mM solution. Melanoma cell lines were inoculated in DMEM medium containing 4.5 g / L glucose, 10% serum and 1% antibiotics and incubated at 37 ° C. in a 75 cm 2 T-flask. After 24 hours of incubation under 5% CO ₂ conditions, cells were treated with 0.05% Trypsin containing 0.02% EDTA, inoculated in a 75 cm 2 T-flask and incubated for 6 hours. Wherein the cell number is 1 × 10 ⁷ cells / flask. Allium extract and α-MSH of appropriate concentration were diluted in MEM medium and treated with cultured melanoma cells and cultured at 37 ° C. for 5 days. After incubation, the medium was obtained and the absorbance was measured at 475 nm to compare the melanin production.

2) Experiment result

Table 2 shows the melanin production inhibitory effect of allium extract.

extract Melanin inhibitory effect (%) Experimental concentration (㎍ / ㎖) 60 100 140 180 Example 1 9.4 24.2 30.3 51.9 Example 2 10.5 27.4 33.2 55.4 Example 3 12.1 30.9 36.7 56.3 Example 4 14.7 33.8 39.4 58.1 Example 5 16.2 36.2 41.5 61.7 Example 6 17.4 37.5 42.1 62.5 Example 7 18.8 38.1 44.6 63.8 Example 8 19.2 38.2 45.0 64.1 Example 9 18.4 37.5 44.7 63.5 Example 10 18.2 36.3 43.9 62.8 Example 11 18.1 33.4 41.5 60.8 Example 12 17.5 32.6 40.3 58.5 Example 13 18.3 35.7 43.2 61.9 Example 14 7.3 15.1 17.8 30.8 Example 15 9.3 20.4 24.5 35.4 Example 16 9.5 21.4 26.3 36.7 Example 17 8.6 19.5 22.6 35.2 Example 18 5.9 17.8 22.3 34.1 Example 19 6.1 19.4 21.0 33.7 Example 20 9.4 22.4 24.8 31.7 Example 21 10.1 22.6 26.1 35.9

* The above value is the average of 3 runs

Allium extracts showed the highest inhibitory effect, and especially the 70% ethanol extract of Example 8 had the highest inhibitory effect. In Examples 1 to 13 using ethanol and methanol as extraction solvents, the elution of substances having a melanin inhibitory effect was higher than those using other solvents. Indicated.

Experimental Example 2

The inhibitory effect of melanin synthase on melanocytes was measured.

1) Experiment Method

Melanosite was used by purchasing a mouse-derived B-16 melanoma (ATCC CRL 6323) cell line. α-MSH was dissolved in 10% DMSO (dimethyl sulfoxide) and used as a 1 mM solution. Melanoma cell lines were inoculated in DMEM medium containing 4.5 g / L glucose, 10% serum and 1% antibiotics and incubated at 37 ° C. in a 75 cm 2 T-flask. After 24 hours of incubation under 5% CO ₂ conditions, cells were treated with 0.05% Trypsin containing 0.02% EDTA, inoculated in a 75 cm 2 T-flask and incubated for 6 hours. Wherein the cell number is 1 × 10 ⁷ cells / flask. Here, the appropriate concentration of allium extract and α-MSH were diluted in MEM medium, and treated with melanoma cells incubated under the conditions shown in Table 3, followed by incubation at 37 ° C. for 5 days. After incubation, the cells were treated with 0.05% trypsin containing 0.02% EDTA to separate the cells, followed by centrifugation for 5 minutes to collect only the cells. The collected cells were triturated with 0.1% Triton-X 100, then electrophoresed on 10% Tris-Glycine gel and stained with 0.2% DOPA solution for melanin synthase. The degree of formation of was compared.

Allium extract added (㎍ / ㎖) α-MSH addition amount (nM) Cell 1 0 0 Cells 2 0 100 Cell 3 100 0 Cell 4 100 100

2) Experiment result

The experimental result is as shown in FIG.

Each lane in Figure 1 represents Cell 1, Cell 2, Cell 3 and Cell 4 in that order.

As a result, compared with the cell (1), the amount of tyrosianase protein of the cell (2) treated with α-MSH was increased, and only the α-MSH was used for the cell (4) treated with both α-MSH and allergy extract. The amount of tyrosinase protein was significantly reduced compared to the treated cells (2). Therefore, it can be seen that the sperm extract inhibits the increase of tyrosinase protein by α-MSH treatment.

Experimental Example 3

Toxicity of fibroblast cells of the prepared ovarian extract was measured.

1) Experiment Method

Fibroblast cells were purchased from a mouse-derived NIH / 3T3 (ATCC CRL 1658) cell line. Fibroblast cell lines are inoculated in DMEM medium containing 4.5 g / L glucose, 10% serum and 1% antibiotic and incubated at 37 ° C. in a 75 cm 2 T-flask. After incubation for 24 hours under 5% CO ₂ condition, cells were isolated by treatment with 0.05% Trypsin containing 0.02% EDTA, and then inoculated in a 96-well-flask and incubated for 6 hours. Wherein the cell number is 1 × 10 ⁴ cells / well. An allium extract of an appropriate concentration was added thereto and incubated for 12 hours. After incubation, 10 μl of MTT (3- (4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazolin bromide) solution (5 mg / ml) was added to the wells and incubated for 4 hours, followed by DMSO (dimethyl sulfoxide). ) 100 μl of the solution was added, and then the absorbance was measured at 570 nm to compare the viability of the cells.

2) Experiment result

The experimental results are shown in Table 4.

Concentrate of Allium Extracts (㎍ / ㎖) Survival rate (%) 20 81.9 60 75.5 100 86.1 140 88.3 180 82.8

-Determination of toxicity to cells

Survival below 70%-addictive,

Greater than 70% and less than 80%-mild toxicity,

Greater than 80% and less than 90%-non-toxic,

Over 90%-non-toxic

As a result of the above experiment, it was found that the cell stimulation was almost non-toxic in the culture of the addition of the allergy extract.

Hereinafter, based on the results of the above experimental examples, to present a cosmetic composition containing the allergy extract in Example 8. However, it is not intended to limit the composition of the present invention to the following formulation examples.

Formulation Example 1 Softening Cosmetic (Skin Lotion)

As shown in the following table, the softening lotion containing the alligator extract was prepared according to a conventional method.

ingredient Content (unit: weight%) Ally extract 1.0 glycerin 5.0 1,3-butylene glycol 3.0 Fiji 1500 1.0 Allantoin 0.1 DL-panthenol 0.3 E.T.A.-2Na 0.02 Benzophenone-9 0.04 Sodium hyaluronate 5.0 ethanol 10.0 Octicdodeceth-16 0.2 Polysorbate 20 0.2 incense 0.02 Uniside-Y13 0.01 Green # 3 0.001 Distilled water Remaining amount Sum 100

Formulation Example 2. Converging Cosmetic Water

As shown in the following table, astringent cosmetics containing allium extract were prepared according to a conventional method.

ingredient Content (unit: weight%) Ally extract 1.0 glycerin 2.0 1,3-butylene glycol 2.0 Allantoin 0.2 DL-panthenol 0.2 E.T.A.-2NA 0.02 Benzophenone-9 0.04 Sodium hyaluronate 3.0 ethanol 15.0 Polysorbate 0.3 Witch Hagel Extract 2.0 Citric acid a very small amount incense 0.02 Uniside-Y13 0.01 Green # 3 0.001 Distilled water Remaining amount Sum 100

Formulation Example 3. Nutrients

As shown in the following table, nutritious longevity containing allium extract was prepared according to a conventional method.

ingredient Content (unit: weight%) Allies Extract 3.0 Glyceryl Stearate SE 1.5 Stearyl alcohol 1.5 lanolin 1.5 Polysorbate 60 1.3 Sorbitan stearate 0.5 Cured Vegetable Oil 1.0 Mineral oil 5.0 Squalane 3.0 Trioctanoine 2.0 Dimethicone 0.8 Tocopherol Acetate 0.5 Carboxy Vinyl Polymer 0.12 glycerin 5.0 1,3-butylene glycol 3.0 Sodium hyaluronate 5.0 Triethanolamine 0.12 incense 0.01 Uniside-Y13 0.02 Green # 3 0.003 Distilled water Remaining amount Sum 100

Formulation Example 4. Nutrition Cream

Nutritious cream containing allergy extract as shown in the following table was prepared according to a conventional method.

ingredient Content (unit: weight%) Allies Extract 3.0 Lipophilic monostearate 2.0 Cetearyl Alcohol 2.2 Stearic acid 1.5 Beeswax 1.0 Polysorbate 60 1.5 Sorbitan stearate 0.6 Cured Plants 1.0 Squalane 3.0 Mineral oil 5.0 Trioctanoine 5.0 Dimethicone 1.0 Sodium magnesium silicate 0.1 glycerin 5.0 Betaine 3.0 Triethanolamine 1.0 Sodium hyaluronate 4.0 incense 0.01 Uniside-Y13 0.02 Green # 3 0.003 Distilled water Remaining amount Sum 100

Formulation Example 5. Massage Cream

Massage creams containing the allergy extract as shown in the following table were prepared according to a conventional method.

ingredient Content (unit: weight%) Ally extract 3.0 Lipophilic monostearic acid glycerin 1.5 Stearyl alcohol 1.5 Stearic acid 1.0 Polysorbate 60 1.5 Sorbitan stearate 0.6 Isostearyl Isosterate 5.0 Squalane 5.0 Mineral oil 35.0 Dimethicone 0.5 Hydroxyethyl cellulose 0.12 glycerin 6.0 Triethanolamine 0.7 incense 0.01 Uniside-Y13 0.02 Green # 3 0.003 Distilled water Remaining amount Sum 100

Formulation Example 6. Essence

Essences containing allium extract as shown in the following table were prepared according to a conventional method.

ingredient Content (unit: weight%) Allies Extract 3.0 glycerin 10.0 Betaine 5.0 Fiji 1500 2.0 Allantoin 0.1 DL-panthenol 0.3 E.T.A.-2Na 0.02 Benzophenone-9 0.04 Hydroxyethyl cellulose 0.1 Sodium hyaluronate 8.0 Carboxy Vinyl Polymer 0.2 Triethanolamine 0.18 Octyldodecanol 0.3 Octyldodeceth-16 0.4 ethanol 6.0 incense 0.02 Uniside-Y13 0.01 Green # 3 0.001 Distilled shoe Remaining amount Sum 100

Formulation Example 7 Pack

As shown in the following table, a pack containing the alligator extract was prepared according to a conventional method.

ingredient Content (unit: weight%) Allies Extract 1.0 Polyvinyl alcohol 15.0 Cellulose gum 0.15 glycerin 3.0 Fiji 1500 2.0 Cyclodextrin 0.15 DL-panthenol 0.4 Allantoin 0.1 Monomethylammonium Glycyric Acid 0.3 Nicotinamide 0.5 ethanol 6.0 Fiji 40 Cured Castor Oil 0.3 incense 0.01 Uniside-Y13 0.02 Green # 3 0.003 Distilled water Remaining amount Sum 100

The whitening agent containing the alligator extract of the present invention acts directly on the melanin metabolic pathway induced by α-MSH, thereby controlling and inhibiting melanin production, thereby exhibiting excellent whitening effect, and a wide range of application to whitening products.

Claims (4)

Whitening agent containing allergy extract. The whitening agent according to claim 1, wherein the allium extract is contained in an amount of 0.0001 to 50.0% by weight based on the dry weight of the cosmetic. The method according to claim 1, wherein the allium extract powdered allium extract is water, lower alcohol (methanol, ethanol), a mixture of water and lower alcohol, acetone, ethyl acetate, 1,3-butylene glycol, hexane, diethyl ether, It is added to an extraction solvent selected from normal propanol, iso-propanol, and normal-butanol, and the active ingredient is extracted by immersion at room temperature for 1 to 15 days, and then the extraction solution is concentrated under reduced pressure using a distillation apparatus equipped with a cooling condenser. Whitening agent characterized by being obtained. The whitening agent according to claim 1, wherein the formulation is a basic cosmetic, a color cosmetic and a hair cosmetic.