KR101229927B1 - Skin Whitening Composition Using a Litter Extract or a Silk Worm Extract - Google Patents

Abstract

The present invention discloses a skin lightening agent composition using silkworm extract or silkworm extract having tyrosinase inhibitory activity and melanin production inhibitory activity.

Silkworm, silkworm, extract, skin, whitening

Description

Skin Whitening Composition Using a Litter Extract or a Silk Worm Extract}

The present invention relates to a skin lightening composition using a silkworm extract or silkworm extract.

It is well known that skin whitening is directly related to melanin pigment.

Melanin protects sub-dermal skin organs by blocking UV rays, and protects the damage of proteins and genes in the skin caused by free radicals in the skin. It causes hyperpigmentation such as blemishes and freckles.

Melanin synthesis is mediated by the action of tyrosinase and tyrosinase related proteins in melanomas. Specifically, tyrosine is oxidized by tyrosinase and is converted into dopa (DOPA, 3,4-dihydroxyphenylalanine), followed by oxidization of dopa oxidase (dopaoxidase) to dopaquinone. In addition, melanin is produced by the action of tyrosinase-related proteins TRP-1 (5,6-dihydroxy indole-2-carboxylic acid oxidase) and TRP-2 (dopachrome tautomerase).

Therefore, when the activity of tyrosinase is inhibited or the production of melanin is inhibited, a whitening effect can be expected.

Korean Patent Publication No. 2008-0105808 (the active ingredient is a phenolic compound isolated from the root), and Korean Patent No. 090535 (the active ingredient is a phenolic compound isolated from the wood vinegar) as a whitening effect and tyrosinase inhibitory activity And melanin production inhibitory activity is disclosed.

The present invention also discloses a silkworm extract and silkworm extract having tyrosinase inhibitory activity and melanin production inhibitory activity.

An object of the present invention is to provide a skin whitening composition using silkworm extract and silkworm extract having tyrosinase inhibitory activity and melanin production inhibitory activity.

Other and specific objects of the present invention will be presented below.

As the present invention is confirmed in the following Examples and Experimental Examples, the silkworm hot water extract, silkworm 70% ethanol extract, silkworm water extract and silkworm 70% ethanol extract, when treated with B16F10 melanoma cells, these extracts Both were completed by confirming that they have tyrosinase inhibitory activity and melanin production inhibitory activity.

Therefore, the skin whitening agent composition of the present invention is characterized in that it comprises a silkworm extract and / or silkworm extract as an active ingredient.

In the present specification, "silk" refers to the feces of silkworms, also called Jambun, and has been used in the folk medicine such as joint pain, headache, neuralgia, lumbar cold pain, stroke, skin diseases and the like.

In addition, in the present specification, "extract" refers to an extract obtained by extracting an extraction object with ethanol, methanol, acetone, ethyl acetate, saturated normal butanol, chloroform, methylene chloride, water or a mixed solvent thereof regardless of the extraction method and the extract thereof. It is understood as meaning including extracts fractionated with the solvents listed above. Regardless of the extraction method, it is to be understood that the extraction method may be applied to any method such as cooling, refluxing, heating, and ultrasonic wave, as long as the extraction object is extracted through immersion in the extraction solvent. Nevertheless, the extract is preferably obtained by extracting the object to be extracted with water, ethanol or a mixed solvent thereof, and is meant to include a concentrated liquid extract or solid extract from which the extraction solvent is removed.

In addition, in the present specification, "skin whitening" is understood as a result of the inhibition of the production of melanin, specifically, means the prevention, delayed expression or treatment of symptoms caused by the production of melanin, such as blemishes, freckles, skin aging, etc. .

In addition, in the present specification, "active ingredient" means a component that can exhibit the desired activity alone or in combination with a carrier that is not active itself.

Terms not specifically defined herein follow the Korean dictionary meaning or meaning commonly used in the art.

The skin whitening agent composition of the present invention may contain any amount (effective amount) according to the use, formulation (cosmetic, soap, ointment, etc.), blending purpose, etc., as long as the active ingredient may include silkworm extract or silkworm extract. Conventional effective amounts will be determined within the range of 0.001% to 99.900% by weight based on the total weight of the composition. Here, the "effective amount" refers to the amount of the active ingredient that can induce a skin lightening effect. Such effective amounts can be determined experimentally within the ordinary skill of those skilled in the art.

The skin lightening composition of the present invention may include other known compounds or plant extracts that are known to have a skin whitening effect so as to enhance or enhance the skin whitening effect, in addition to the silk extract or silkworm extract, which is an active ingredient. It may include a compound or a plant extract having a skin lightening effect to be revealed.

Herein, the other compounds or plant extracts include mercaptosuccinic acid, mercaptodextran, tefrenone, dihydroxy-isoquinoline, indomethacin, 3-hydroxymanul, vitamin K, thiazolidone, kynurenine, and mulberry leaves. Extract, mulberry root extract, mulberry stem extract, lemon extract, cucumber extract, licorice extract, rosemary extract, acerola cherry extract, ginkgo extract, carob extract, geranium extract, herbal extract, etc. However, the present invention is not limited thereto.

Compounds or plant extracts as exemplified above may be included in the skin whitening agent composition of the present invention together with one or more of silkworm extract or silkworm extract as its active ingredient.

In another aspect, the present invention relates to an atopic dermatitis improving composition comprising a silkworm extract and / or silkworm extract as an active ingredient.

As used herein, the term "atopic dermatitis" is defined to include all diseases classified as atopic dermatitis in the art, regardless of the direct or indirect cause of its occurrence. Atopic dermatitis is generally classified into infantile atopic dermatitis, pediatric atopic dermatitis, adult atopic dermatitis and maternal atopic dermatitis, according to the time of its onset or subject of the invention, where atopic dermatitis includes all these types of atopic dermatitis. It should be understood as. In the following experimental example of the present invention, a clinical trial was conducted on 60 subjects with randomly selected atopic dermatitis symptoms, and it was found to be effective for about 84% of subjects. Since these results are obtained from randomly selected subjects, it can be seen that the atopic dermatitis improving agent composition of the present invention is effective in all types of atopic dermatitis regardless of the cause of atopic dermatitis.

The content of the silkworm extract or silkworm extract, which is an active ingredient included in the atopy improving agent composition of the present invention, is effective as described above with respect to the skin whitening agent composition of the present invention.

In another aspect, the present invention relates to a skin moisturizer composition comprising a silkworm extract and / or silkworm extract as an active ingredient.

Experimental Example The lotion containing the silkworm extract and / or silkworm extract of the present invention was used in 30 experimental participants according to a conventional method. As a result, 27 out of 30 experimental participants answered that the skin was moisturized. In addition, there was a markedly high skin moisturizing effect compared to the case of using a lotion that does not contain the extract.

The content of the silkworm extract or silkworm extract, which is an active ingredient included in the skin moisturizer composition of the present invention, is also effective as described above with respect to the skin whitening agent composition of the present invention.

The skin whitening agent composition, atopic dermatitis improving agent composition and skin moisturizing agent composition (hereinafter "composition of the present invention") of the present invention may be regarded as a cosmetic composition in a specific embodiment.

When the composition of the present invention is conceived as a cosmetic composition, the cosmetic composition can be prepared in various forms, for example, emulsions, lotions, creams (oil-in-water, water-in-oil, multiphase), solutions, suspensions (anhydrous and Aqueous), anhydrous products (oil and glycol based), gels, masks, packs or powders and the like.

The composition of the present invention may include an acceptable carrier in cosmetic preparations in addition to silkworm extracts or silkworm extracts.

As used herein, the term " acceptable carrier for cosmetic preparation "refers to a compound or composition which is already known and used in the cosmetic preparations, or which is a compound or composition to be developed in the future, and which has no toxicity, instability or irritability It says.

The carrier may be included in the composition of the present invention in an amount of from about 1% by weight to about 99.99% by weight, preferably from about 50% by weight to about 99% by weight of the composition, based on the total weight thereof.

However, since the ratio depends on the form of the above-described preparation of the cosmetic of the present invention and its specific application site (face or hand) or its preferred application amount, the ratio is in any aspect the scope of the present invention. It should not be understood as limiting.

Meanwhile, examples of the carrier include alcohols, oils, surfactants, fatty acids, silicone oils, wetting agents, moisturizers, viscosity modifiers, emulsions, stabilizers, sunscreens, colorants, fragrances, and the like.

The components of the alcohol, oil, surfactant, fatty acid, silicone oil, wetting agent, moisturizer, viscosifier, emulsion, stabilizer, sunscreen agent, coloring agent and fragrance which can be used as the carrier are already well known in the art, The substance / composition can be selected and used.

The composition of the present invention may be regarded as a soap composition in another specific embodiment.

When the composition of the present invention is understood as a soap composition, the soap composition of the present invention may be prepared by including a silkworm extract or silkworm extract on a soap base, and may be prepared by including a skin moisturizer, an emulsifier, a water softener, and the like as an additive. Can be.

Examples of the soap base material include vegetable oils such as palm oil, palm oil, soybean oil, perm free oil, olive oil and palm kernel oil or animal fats such as tallow, lard, sunshine and fish oil. Examples of the skin moisturizers include glycerin, erythritol, polyethylene glycol , Propylene glycol, butylene glycol, pentylene glycol, hexyl glycol, isopropyl myristate, silicone derivatives, aloe vera, sorbitol and the like. Examples of the emulsifier include natural oils, wax fatty alcohols, hydrocarbons, May be used. As the water softening agent, tetrasodium ethylenediate and the like may be used.

The soap composition of the present invention may further include an antimicrobial agent, a dispersant, a foam inhibitor, a solvent, a scale inhibitor, a corrosion inhibitor, a perfume, a pigment, a metal ion blocking agent, an antioxidant, a preservative, and the like as an additive.

In the soap composition of the present invention, the soap base or additives may be included in an amount generally used in the art, and the soap base is generally 99.9 to 50 wt% based on the total content of the soap composition. It may be added, the additive may be added in 1% to 20% by weight.

Meanwhile, the skin whitening agent composition and the atopic dermatitis improving agent composition of the present invention may be regarded as a pharmaceutical composition in another specific embodiment.

When the skin whitening agent composition of the present invention is identified as a pharmaceutical composition, its pharmacological effect can be grasped as a therapeutic or preventive effect on a disease resulting from an increase of melanin, and the skin whitening is a result of treatment or prevention ≪ / RTI > As a disease resulting from the increase of the melanin means blemishes, freckles, skin aging and the like.

The pharmaceutical composition of the present invention includes oral formulations (tablets, suspensions, granules, emulsions, capsules, syrups, etc.), parenteral formulations, including pharmaceutically acceptable carriers, excipients, etc., in addition to silk extracts and silkworm extracts, which are active ingredients. (Sterile injectable aqueous or oily suspensions), topical formulations (solutions, creams, ointments, gels, lotions, patches) and the like.

The term "pharmaceutically acceptable" as used herein means that the application (subject) does not have the above-mentioned toxicity that is adaptable without inhibiting the activity of the active ingredient.

Examples of pharmaceutically acceptable carriers include lactose, glucose, sucrose, starch (such as corn starch, potato starch, etc.), cellulose, derivatives thereof (such as sodium carboxymethyl cellulose, ethylcellulose, etc.), malt, gelatin, talc, solids Lubricants (such as stearic acid, magnesium stearate, etc.), calcium sulfate, vegetable oils (such as peanut oil, cottonseed oil, sesame oil, olive oil, etc.), polyols (such as propylene glycol, glycerin, etc.), alginic acid, emulsifiers (such as TWEENS), wetting agents ( Sodium lauryl sulfate), colorants, flavoring agents, tableting agents, stabilizers, antioxidants, preservatives, water, saline, phosphate buffer solutions and the like. The carrier may be selected from one or more of suitable pharmaceutical formulations according to the formulation of the pharmaceutical composition of the present invention.

Excipients may be selected and used according to the formulation of the pharmaceutical composition of the present invention, for example, when the pharmaceutical composition of the present invention is prepared with an aqueous suspending agent, suitable excipients are sodium carboxymethyl cellulose, methyl cellulose, hydropropylmethylcellulose And suspending agents and dispersing agents such as sodium alginate and polyvinylpyrrolidone. Suitable excipients when prepared from injection solutions include Ringer's solution, isotonic sodium chloride, and the like.

The pharmaceutical compositions of the present invention may be administered orally or parenterally, but will usually be administered topically to the skin, usually in a topical formulation.

The daily dose of the pharmaceutical composition of the present invention is usually 0.001 to 150 mg / kg body weight, and may be administered once or several times. However, since the dosage of the pharmaceutical composition of the present invention is determined in view of various related factors such as route of administration, age, sex, weight, and patient's severity of the patient, the dose is limited in any aspect to the scope of the present invention It should not be understood.

As described above, according to the present invention can provide a skin lightening composition using a silkworm extract or silkworm extract. In addition, according to the present invention can provide atopic dermatitis improving composition and skin moisturizer composition using a silkworm extract or silkworm extract. Such compositions of the present invention may be formulated into pharmaceuticals such as cosmetics, soaps or ointments.

Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these examples and experimental examples.

<Examples> Preparation of Silkworm and Silkworm Extract Extract

Example 1 Preparation of Silkworm Extract

1L of water was added to 50 g of lyophilized silkworms and extracted for 12 hours while warming to a temperature of about 65 ° C. After extraction, the resultant was filtered and the residue was extracted and concentrated in dark and dark to obtain a solid silkworm extract.

Example 2 Preparation of Silkworm Extract

1L of 70% ethanol was added to 50 g of lyophilized silkworms and extracted by standing for 24 hours. After extraction, the resultant was filtered and the residue was extracted and concentrated in dark and dark to obtain a solid silkworm extract.

Example 3 Preparation of Silkworm Extract

1 g of water was added to 50 g of lyophilized silkworms and extracted for 12 hours while warming to a temperature of about 65 ° C. After extraction, the resultant was filtered and the residue was extracted and concentrated in dark and dark to obtain solid silkworm extract.

Example 2 Preparation of Silkworm Extract

1 g of 70% ethanol was added to 50 g of lyophilized silkworms, and the extract was left for 24 hours. After extraction, the resultant was filtered and the residue was extracted and concentrated in dark and dark to obtain solid silkworm extract.

<Experimental Example> Whitening effect, atopic dermatitis improvement effect and moisturizing effect experiment

Experimental Example 1 Whitening Effect Cell Experiment

Experimental Example 1-1 B16F10 Melanoma Cell Culture

B16F10 melanoma cells were cultured in DMEM medium containing 10% fetal bovine serum (FBS), 100 units / ml penicillin, and 100 units / ml streptomycin at 37 ° C. and maintained at 5% CO ₂ . Subculture was performed once.

Experimental Example 1-2 Cytotoxicity Evaluation

Toxicity to the B16F10 cells of the Example extract was evaluated using the MTT assay. B16F10 cells (2.0 × 10 ⁴ cells / ml) were dispensed into 24 wells and cultured for 18 hours, followed by further incubation for 24 hours by treatment with the extract of the above example (10 μg / ml). 200 µl of the MTT solution prepared at a concentration of 5 mg / ml PBS was added thereto, followed by further 4 hours of incubation. The culture solution was removed, and 200 µl of DMSO was added to each well, and the absorbance of the formazan produced by MTT reduction was measured at 570 nm.

The results are shown in FIG. 1. Referring to Figure 1, it can be seen that the extract of the above example does not show any particular cytotoxicity (I to IV are the extract of Example 1 to the extract of Example 4, respectively).

Experimental Example 1-3 Tyrosinase Inhibitory Activity Experiment

After dispensing B16F10 cells (2.0 × 10 ⁴ cells / ml) into 24 wells, each extract (10 μg / ml) in the above example was treated and incubated for 48 hours. Next, the cells of each well were collected, suspended in 100 µl of 10 mM PBS, the suspension was vortexed, and the supernatant obtained by centrifugation was used as an enzyme solution. Tyrosinase inhibitory activity experiment was carried out in 24 wells of the supernatant 40μL and its substrate L-DOPA (2mg / ㎖) 100μL, reacted for 1 hour at 37 ℃ and absorbance at 405nm using an ELISA reader Was measured. The activity of tyrosinase is shown in FIG. 2 as a percentage of the absorbance of the untreated group control.

Referring to Figure 2, it can be seen that the extracts of the above examples all inhibit the activity of tyrosinase (I to IV are the extracts of Examples 1 to 4, respectively).

Experimental Example 1-4 Melanin Production Inhibition Activity Experiment

After dispensing B16F10 cells (2.0 × 10 ⁴ cells / ml) into 24 wells, each extract of the above example (10 μg / ml) was treated with α-MSH (50 nM), a melanogenesis-stimulating agent, for 72 hours. Incubated. Cells were harvested and 1N NaOH was added to lyse the cells, and then absorbance was measured by ELISA at 405 nm.

The results are shown in FIG. 3 as a percentage of the control group (α-MSH treated group). Referring to FIG. 3, it can be seen that the extract of Example suppresses the production of melanin while showing a similar tendency to the results of FIG. 2 (I to IV are extracts of Examples 1 to 4, respectively). being).

Experimental Example 2 Clinical Trial of Moisturizing Effect and Atopic Dermatitis Improvement Effect

Experimental Example 2-1 Moisturizing Effect Clinical Experiment

For the clinical experiment of the moisturizing effect was prepared a lotion with the ingredients and contents as shown in Table 1 below.

[Table 1]

Ingredients and content (% by weight) of lotions

Ingredients Production Example 1  Production Example 2 Purified water to 100 glycerin 5.0 Allantoin 2.5 Alcohol 7.0 Fiji-40 Hydrogenated Castor Oil 3.0 Phenoxyethanol 0.5 Methylparaben 0.2 Example extract 2.5 2.5 incense 1.0  * In <Production Example 1> includes the extract of <Example 1>, <Production Example 2> contains the extract of <Example 2>.

Here, as a lotion of the comparative example, a lotion containing purified water in its amount was used instead of the extract of the example.

The moisturizing effect test was conducted for 30 women in their 20s to 50s and was evaluated daily after 4 weeks of use. The evaluation method was very good (5 points), excellent (3 points), moderate (0 points), bad (-3 points), and very bad (-5 points) according to the 5-point scale method. In the case of skin irritation, which is an evaluation item, it was examined whether the phenomenon of itching, skin itching or erythema of the skin was alleviated.

The results are shown in [Table 2] below.

[Table 2]

Results for skin irritation and moisturizing effect

number Skin irritation Moisturizing effect Production Example 1 Production Example 2 Comparative example Production Example 1 Production Example 2 Comparative example One 5 3 5 3 5 3 2 3 5 5 5 3 3 3 5 3 0 5 5 5 4 5 3 3 5 5 5 5 3 5 5 5 3 5 6 5 5 5 5 5 3 7 5 5 3 5 5 5 8 3 5 3 5 5 5 9 5 3 3 3 5 3 10 3 5 5 5 5 3 11 5 5 0 5 5 5 12 5 3 5 5 3 5 13 3 5 5 5 5 5 14 5 5 3 3 5 5 15 5 3 5 5 3 3 16 5 5 3 3 5 3 17 3 3 5 5 5 3 18 5 5 5 5 3 5 19 5 3 3 5 5 5 20 3 5 5 5 3 5 21 5 5 5 5 5 3 22 5 3 5 5 5 3 23 3 5 5 5 3 5 24 5 5 3 3 5 3 25 3 3 5 5 5 3 26 5 5 5 5 5 5 27 5 5 5 3 3 0 28 3 3 5 5 3 5 29 5 3 5 5 5 3 30 5 5 5 5 5 3 Average 4.33 4.26 4.13 4.60 4.40 3.90

Referring to the <Table 2>, it can be seen that the extract of the embodiment does not cause skin irritation, as well as the effect of inhibiting skin irritation. In addition, it can be seen that the moisturizing effect is also superior to the comparative example. Although not shown in Table 2, most of the test participants responded that the whitening effect was also excellent.

Experimental Example 2-2 Atopic Dermatitis Improvement Effect Experiment

Atopic dermatitis improvement activity was performed in 60 men and women with atopic dermatitis symptoms over 3 years old.

After 12 weeks after using the lotion of [Table 1] 2 to 3 times a day, the SCORAD index (measured with higher atopic symptoms) was measured. ].

[Table 3]

SCORAD

division 0 parking 8 parking Production Example 1 35.6 ± 7.2 21.5 ± 4.7 ** Production Example 2 34.7 ± 8.2 23.4 ± 7.2 * Comparative example 32.4 ± 6.1 28.5 ± 5.5 ** p <0.01, * p <0.05

Significance test was performed at 5% and 1% level using paired T-test.

1 is a result showing that the silkworm extract and silkworm extract does not have cytotoxicity. Data is shown as mean ± standard deviation of three experiments.

Figure 2 is a result showing the silkworm extract and silkworm extract tyrosinase inhibitory activity. Data is shown as mean ± standard deviation of three experiments.

3 is a result showing the mesa production inhibitory activity of silkworm extract and silkworm extract. Data is shown as mean ± standard deviation of three experiments.

Claims (14)

It contains a silkworm extract as an active ingredient, The extract is a skin lightening composition, characterized in that obtained by extracting the silkworms to be extracted by dipping in water, ethanol or a mixed solvent thereof and removing the extraction residue after extraction. delete delete The method of claim 1, The composition is a skin whitening composition, characterized in that it further comprises a mulberry leaf extract and mulberry root extract. The method according to claim 1 or 4, The composition is a skin lightening composition, characterized in that the cosmetic composition. The method according to claim 1 or 4, The composition is a skin whitening composition, characterized in that the soap composition. delete delete delete delete delete delete A skin moisturizing cosmetic composition comprising extract obtained by dipping sap in water, ethanol or a mixed solvent thereof and removing the extraction residue after extraction. A skin moisturizing soap composition comprising an extract obtained by dipping sap in water, ethanol or a mixed solvent thereof and removing the extraction residue after extraction.

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