KR20130074124A - Cosmetic composition for skin whitening comprising columbianetin - Google Patents

Abstract

PURPOSE: A cosmetic composition containing columbianetin isolated from an Aralia cordata var. continentalis extract is provided to suppress melanogenesis with safety, to ensure whitening effect with solubility and stability. CONSTITUTION: A cosmetic composition for skin whitening contains columbiatin or an Aralia cordata var. continentalis extract as an active ingredient. The Aralia cordata var. continentalis extract is a methanol extract of Aralia cordata var. continentalis. The cosmetic composition is manufactured in the form selected from the group consisting of an external use skin ointment, a cream, a skin softener, a lotion, a pack, an essence, a hair tonic, a shampoo, a rinse, a hair conditioner, a hair treatment, a gel, a skin toner, an astringent, a milk lotion, a moisture lotion, a nutrition lotion, a massage cream, a nutrition cream, a hand cream, a foundation, a nutrition essence, a sun screen, a soap, a cleansing foam, a cleansing lotion, a body lotion, and a body cleanser.

Description

Cosmetic composition for skin whitening containing Colombianine {{Cosmetic composition for skin whitening comprising columbianetin}

The present invention relates to a cosmetic composition for skin whitening, and more particularly, includes Colombianetine (Columbianetin, CAS no. 3804-70-4, Molecular Formula C ₁₄ H ₁₄ O ₄ , Molecular Weight 246.26) or more excellent in melanin production inhibitory effect It relates to a cosmetic composition for skin whitening containing a poison active extract as an active ingredient.

The skin color of a person is determined by various factors such as the activity of the melanocyte which forms the melanin pigment, the distribution of blood vessels, the thickness of the skin, and the presence or absence of pigment in and out of the body such as carotenoid and bilirubin. Among them, melanin, which is formed in melanocyte, is considered to be the most important factor for skin color formation. Melanin is converted to tyrosine by tyrosinase through 3,4-dihydroxyphenylalanine, dopaquinone, leucodopachrome, dopachrome, 5,6-dihydroxyindole and indole-5,6-quinone and finally to melanin It is the end product of the oxidation process being converted. However, melanin biosynthesis is a very complex process, and the exact mechanism by which melanin synthesis is induced is still unknown. Melanin provides a natural defense against harmful ultraviolet rays, but when melanin is overproduced, it causes overpigmentation such as blemishes and freckles.

Active ingredients such as arbutin, deoxyalbutin, octadecenedioic acid, conjugated linoleic acid, niacinamide, hydroquinone, kojic acid, glutathione, azelaic acid and the like that inhibit skin pigmentation and have a whitening effect are known. Such materials are known to have tyrosinase inhibitory activity and have in fact been used in whitening products. However, the above-mentioned active ingredients are limited in their use due to insufficient whitening effect, safety to skin, difficulty in formulation and stability, and the like.

Meanwhile, Korean Patent No. 0829045 discloses a composition for preventing or treating periodontal disease, including a poisonous extract or a compound separated therefrom, and Japanese Patent Application No. 2002-275085 discloses a 'skin external preparation'. It is. However, as described in the present invention, there is no disclosure about the whitening effect of Colombianetine isolated from the venom extract.

The present invention is derived from the above demands, and is safe for the skin even after long-term use, and it is stable without heat, light, time, and the like during the manufacture and storage of the product, and is stable, and makes various formulations. It is effective to apply Colombianine (columbianetin) isolated from the extract of Aralia cordata var. Continentalis, which has physicochemical properties such as solubility, and which, among other things, can provide excellent whitening effect. By providing the composition for skin whitening containing as a component, the present invention has been completed.

In order to solve the above problems, the present invention provides a cosmetic composition for skin whitening containing Colombianine (columbianetin) or a poison active extract comprising the same as an active ingredient.

According to the present invention, Colombianetine isolated from the venom extract of the present invention not only has an excellent effect of inhibiting melanin production, but is also safe for the skin, has solubility suitable for producing various formulations, and has excellent stability during cosmetic preparation and storage, Cosmetic compositions containing Colombianine as an active ingredient may be used as an effective skin whitening cosmetic composition.

The present invention provides a cosmetic composition for skin whitening containing Colombiantine of the formula (1) or a poison active extract comprising the same as an active ingredient.

When the whitening component is applied to the actual skin, in order to exert an excellent whitening effect, it shows high activity of the skin whitening activity at low concentration, excellent ability to penetrate and absorb the skin, and volatile to stay for a sufficient time to show the whitening effect. It is preferable that this is low, the active ingredient is stably maintained on the composition or the skin, and is easily formulated into medicines and cosmetics and is safe for the skin. However, among the known whitening components, the whitening component that satisfies all of the above properties is rare. For example, some whitening ingredients have excellent whitening activity even at low concentrations in in vitro experiments, but are difficult to apply to actual skin due to their poor ability to penetrate and absorb the skin. Other whitening ingredients are less hydrophilic and difficult to formulate into cosmetics or medicines. In addition, some of the whitening ingredients may be broken down or transformed into other compounds when exposed to heat, light, or oxygen, and the whitening effect may already disappear before application to the skin. However, when compared to the known whitening component arbutin, the Colombianetine of the present invention exhibits excellent melanin production inhibitory activity at low concentrations and is very safe for the skin.

In the present invention, the term "whitening" refers to inhibiting, inhibiting or alleviating hyperpigmentation of skin. Hyperpigmentation of the skin includes freckles, blemishes, hyperpigmentation after UV exposure, hyperpigmentation after inflammation, senile black spots, brown spots or blotch.

In the cosmetic composition according to an embodiment of the present invention, the poisonous extract may be preferably a poisonous methanol extract, but is not limited thereto.

In the cosmetic composition according to the embodiment of the present invention, the cosmetic composition for skin whitening may include Colombianinetin 0.0001% by weight to 10% by weight relative to the total weight. When it contains less than 0.0001% by weight of Colombianetine of the skin whitening composition of the present invention, sufficient whitening effect cannot be expected, and when it contains more than 10% by weight, the whitening effect no longer increases. The composition for skin whitening of the present invention can provide a desirable whitening effect when it contains an effective amount of Colombianetine.

In the present invention, the term 'effective amount' means an amount of a compound capable of inhibiting, inhibiting or alleviating hyperpigmentation of the skin. The effective amount of the compound included in the skin whitening composition of the present invention will vary depending on the form in which the skin whitening composition is commercialized, the method in which the compound is applied to the skin, and the time to stay in the skin. For example, when the composition for skin whitening is commercialized as a medicament for dermatological treatment due to hyperpigmentation of the skin, Colombianinetin may be contained at a higher concentration than when cosmetically applied to the skin. will be. Even in the case of cosmetics, the wash-off type of cosmetics such as makeup remover, detergent, etc., in which the active ingredient stays on the skin within a short period of time, may include a relatively high concentration of the compound of Colombianetine. On the other hand, in the case of a leave-on type cosmetic such as a lotion, an emulsion, a cream or an essence in which the active ingredient stays on the skin for a long time, it may contain a lower concentration of Colombianetine than a wash-off type cosmetic. will be.

In the cosmetic composition according to an embodiment of the present invention, the cosmetic composition for skin whitening is an external skin ointment, cream, supple cosmetics, nourishing cosmetics, pack, essence, hair tonic, shampoo, conditioner, hair conditioner, hair treatment, gel , Skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisture lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, foundation, nutrition essence, sunscreen, soap, cleansing foam, cleansing lotion It may have a formulation selected from the group consisting of cleansing cream, body lotion and body cleanser, but is not limited thereto. The composition of each of these formulations may contain various kinds of bases and additives necessary for formulation of the formulation, and the kinds and amounts of these ingredients can be easily selected by those skilled in the art.

When the formulation of the present invention is a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

In the case where the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. Especially, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

In the case of the solution or emulsion of the present invention, a solvent, a solvent or an emulsifier is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

When the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may 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, isethionate, an imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

Formulations of the present invention may further contain excipients, including fluorescent substances, fungicides, hydrogenic agents, moisturizers, fragrances, fragrance carriers, proteins, solubilizers, sugar derivatives, sunscreens, vitamins, plant extracts, and the like. .

When the cosmetic composition for skin whitening is formulated as a medicine or cosmetic as described above, it may include a known excipient applicable to the skin to act as a carrier for the active ingredient. When formulating into pharmaceuticals, reference may be made to what is disclosed in Remington's Pharmaceutical Science, Mack Publishing Company, Easton PA, and when formulating into cosmetics, the International cosmetic ingredient dictionary, 6th ed., The cosmetic, Toiletry and Fragrance Association , Inc., Washington, 1995. Such documents are incorporated as part of this specification.

Hereinafter, the present invention will be described in detail by way of examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.

Example  One

Toxic acid (Aralia Continentalis) was purchased and 100 g of the pulverized product was placed in 500 ml of 100% methanol, boiled for 3 hours in a reflux extractor equipped with a cooling capacitor, filtered through a 300 mesh filter cloth, and the residue was extracted once more in the same manner. Each extract was combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, concentrated under reduced pressure at 60 ° C. in a distillation apparatus equipped with a cooling condenser, suspended in 300 ml of purified water, and 300 ml of normal butanol was added to normal butanol. A lysate was obtained. This normal butanol lysate was chromatographed on a silica gel column to obtain 530 mg of a fraction containing the active ingredient. This was purified again by high performance liquid chromatography to separate 320 mg of Colombianine.

Experimental Example  1: Confirmation of the Melanin-inhibiting Effect of Colombian Netine

Colombiantine was added to the culture medium of B-16 mouse melanoma cells to test the whitening effect at the cellular level (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980 ). The final concentration of Colombian netine was 2μg / ml, 10μg / ml, 50μg / ml, 100μg / ml was added to the B-16 rat melanoma cell culture medium with an arbutin aqueous solution and incubated for 3 days. Cells were trypsin-treated and removed from the culture vessel, centrifuged, and melanin was extracted. 1 ml of sodium hydroxide solution (1N concentration) was added thereto, and the mixture was boiled for 10 minutes to dissolve melanin, and the absorbance was measured at 400 nm using a spectrophotometer. The amount of melanin produced was expressed as absorbance per unit cell count (10 ⁶ cells). The relative melanin production of the group treated with the Colombianetine compound compared to the control group without the Colombianetine compound was calculated as the inhibition rate (%) and the results are summarized in Table 1.

sample Melanin production Inhibition rate (%) Control group (no addition) 0.072 ± 0.004 - Colombian netine (final concentration 2µg / ml) 0.063 ± 0.002 12% Colombian netine (final concentration 10㎍ / ml) 0.033 ± 0.001 54% Colombian netine (final concentration 50㎍ / ml) 0.009 ± 0.002 88% Colombian netine (final concentration 100㎍ / ml) 0.005 ± 0.003 95% Arbutin (final concentration 300 µg / ml) 0.035 ± 0.002 52%

* Number of iterations = 3

As can be seen from the results of Table 1, Colombianetine showed an excellent melanin production inhibitory ability against cultured B-16 rat melanoma cells, compared with Arbutin, a known whitening substance.

Manufacturing example  1 and Comparative example  One

The external skin ointment containing Colombiantine was prepared according to a conventional method as shown in the table below. In addition, the external skin ointment prepared with the remaining ingredients except Colombianine was prepared in Comparative Example 1.

Composition Preparation Example 1 (% by weight) Comparative Example 1 (% by weight) Colombianetine
-Diethyl sebacate
-Payment
Polyoxyethylene oleyl ether phosphate
Sodium benzoate
-vaseline 5
8
5
6
Suitable amount
to 100 -
8
5
6
Suitable amount
to 100

Manufacturing example  2 and Comparative example  2

A cream containing Colombianinetin was prepared according to a conventional method as shown in the table below. In addition, a cream prepared with the remaining ingredients except for Colombianetine was prepared in Comparative Example 2.

Composition Preparation Example 2 (% by weight) Comparative Example 2 (wt%) Colombianetine
Stearic acid
Cetanol
Potassium hydroxide
-glycerin
Propylene glycol
-antiseptic
-incense
-Purified water 0.5
15.0
1.0
0.7
5.0
3.0
Suitable amount
Suitable amount
to 100 -
15.0
1.0
0.7
5.0
3.0
Suitable amount
Suitable amount
to 100

Manufacturing example  3 and Comparative example  3

A flexible lotion containing Colombian netine as in the composition of the following table was prepared according to a conventional method. In addition, a flexible lotion prepared with the remaining ingredients except Colombianine was prepared in Comparative Example 3.

Composition Preparation Example 3 (wt%) Comparative Example 3 (wt%) Colombianetine
-ethanol
Polylauric acid polyoxyethylene sorbitan
Paraoxybenzoic acid methyl
-glycerin
-1,3-butylene glycol
-incense
Pigment
-Purified water 0.05
10.0
1.0
0.2
5.0
6.0
Suitable amount
Suitable amount
to 100 -
10.0
1.0
0.2
5.0
6.0
Suitable amount
Suitable amount
to 100

Manufacturing example  4 and Comparative example  4

A nutritional lotion containing Colombian netine as in the composition of the following table was prepared according to a conventional method. In addition, the nutritional lotion prepared with the remaining ingredients except for the compound of Colombianetine was prepared in Comparative Example 4.

Composition Preparation Example 4 (wt%) Comparative Example 4 (wt%) Colombianetine
Waselin
Sesquioleate sorbitan
Polyoxyethylene oleylethyl
Paraoxybenzoic acid methyl
Propylene glycol
-ethanol
Carboxy vinyl polymer
Potassium hydroxide
Pigment
-incense
-Purified water 1.0
2.0
0.8
1.2
Suitable amount
5.0
3.2
18.0
0.1
Suitable amount
Suitable amount
to 100 -
2.0
0.8
1.2
Suitable amount
5.0
3.2
18.0
0.1
Suitable amount
Suitable amount
to 100

Manufacturing example  5 and Comparative example  5

A pack containing Colombianetine was prepared according to the conventional method as shown in the table below. In addition, a pack prepared with the remaining components except for the compound of Colombianine was prepared in Comparative Example 5.

Composition Preparation Example 5 (% by weight) Comparative Example 5 (wt%) Colombianetine
-glycerin
Propylene glycol
Polyvinyl alcohol
-ethanol
-Polyoxyethylene oleyl ethyl
Paraoxybenzoic acid methyl
Pigment
-incense
-Purified water 0.01
5.0
4.0
15.0
8.0
1.0
0.2
Suitable amount
Suitable amount
to 100 -
5.0
4.0
15.0
8.0
1.0
0.2
Suitable amount
Suitable amount
to 100

Manufacturing example  6 and Comparative example  6

Essences containing Colombianinetin as in the composition of the following table was prepared according to a conventional method. In addition, an essence prepared with the remaining components except for the compound of Colombianine was prepared in Comparative Example 6.

Composition Preparation Example 6 (wt%) Comparative Example 6 (wt%) Colombianetine
Propylene glycol
-glycerin
Sodium hyaluronate (1%)
-ethanol
Polyoxyethylene Cured Castor Oil
Paraoxybenzoic acid methyl
-incense
-Purified water 0.3
10.0
10.0
5.0
5.0
1.0
0.1
Suitable amount
to 100 -
10.0
10.0
5.0
5.0
1.0
0.1
Suitable amount
to 100

Experimental Example  2 Colombian  Confirmation of pigmentation inhibitory effect

Twenty healthy men and women were selected to attach aluminum foil in two rows of 6 holes with a diameter of 7 mm in the lower part of both arms, and 60mJ / cm ² light was irradiated using ORIEL solar simulator 1000W at a distance of 10 cm from the arm. . The irradiation site was washed well with 70% ethanol aqueous solution before irradiation. The bases prepared according to Preparation Examples 1-3 and Comparative Examples 1-3 were applied twice a day until three weeks after the irradiation, from three days before the irradiation, to the same row in pairs.

For each, the degree of pigmentation of the preparation example and the comparative example was visually determined, and the degree of suppression of pigmentation was evaluated by two steps of effective and no effect compared to the comparative example, and the results are shown in Table 8.

Experimental material Effective (persons) No effect (persons) Production Example 1 15 5 Production Example 2 13 7 Production Example 3 12 8

As can be seen from the results in Table 8, the skin ointment, cream, and flexible lotion containing Colombianinetin prepared according to Preparation Example 1-3 as an active ingredient has a whitening effect on at least 12 or more of 20 subjects. Indicated. It also shows no side effects in the skin of the subject, suggesting that Colombianetine is a safe and effective whitening ingredient.

Claims (4)

Colombian tintin (columbiatin) or a cosmetic composition for skin whitening containing a poison active extract comprising the same as an active ingredient. The cosmetic composition according to claim 1, wherein the poison extract is a poison methanol extract. The cosmetic composition according to claim 1, wherein the content of Colombianetine is contained in an amount of 0.0001% to 10% based on the total weight of the composition. The cosmetic composition according to any one of claims 1 to 3, wherein the cosmetic composition is an external skin ointment, cream, softening lotion, nourishing lotion, pack, essence, hair tonic, shampoo, rinse, hair conditioner, hair treatment, gel, Skin Lotion, Skin Softener, Skin Toner, Astringent, Lotion, Milk Lotion, Moisture Lotion, Nutrition Lotion, Massage Cream, Nutrition Cream, Moisture Cream, Hand Cream, Foundation, Nutrition Essence, Sunscreen, Soap, Cleansing Foam, Cleansing Lotion, Cosmetic composition, characterized in that it has a formulation selected from the group consisting of cleansing cream, body lotion and body cleanser.