KR20030037992A - Composition for skin whitening containing Sitosterol - Google Patents

Abstract

PURPOSE: A skin whitening composition containing sitosterol as an effective ingredient is provided. The composition inhibits pigmentation by suppressing the formation of melamine and thus is effective in skin whitening or treating chloasma or freckles and can be safely applied to the skin without adverse effect. CONSTITUTION: The skin whitening composition contains 0.000001 to 10% by weight of sitosterol represented by the formula(1) and commonly known as an anticholesteremic agent or an anticarcinogenic agent, based on the total weight of the composition. The sitosterol is an organic compound(C29H50O) containing 29C and contained in plants such as Pisum sativum, Paeonia lactiflora, Panax ginseng, Patrinia scabiosaefolia Fisch., Paulownia coreana Uyeki, Perilla frutescens L., Phytolacca esculenta V. Houtt, Pinellia ternata(Thunb.) Breit., Piper nugrum, Ostericum koreanum(Maxim.) Kitagawa, Plantago asiatica L., Polygonum hydropiper, Pleuropterus multiflorus Turcz., Polygonum orientale, Polygonum tinctoria, Poncirus trifoliata, Portulaca oleracea L., Lycium chinense Mill., Daphne genkwa, etc.

Description

Composition for skin whitening containing Sitosterol}

The present invention relates to a composition for skin whitening, and more particularly, to a composition for skin whitening containing cytosterol, which has excellent product stability and can be safely used without side effects on the skin, and inhibits melanin production and has excellent pigmentation inhibitory effect. will be.

It is everyone's constant desire to have white, fair skin. Human skin color is determined by the concentration and distribution of melanin in the skin. In addition to genetic factors, it is also influenced by environmental or physiological conditions such as ultraviolet rays, fatigue and stress. Melanin is a type of amino acid tyrosine (tyrosinase) acts as an enzyme called tyrosinase (tyrosinase) is converted to dopa (DOPA), dopaquinone (dopaquinone) is produced through a non-enzymatic oxidation reaction. However, although the pathway by which melanin is made is known, it is still not clear what mechanisms induce melanin synthesis, the previous step in which tyrosinase works.

When such synthesis of melanin occurs excessively in the skin, it may darken the skin tone, and may cause spots and freckles. Therefore, by inhibiting the synthesis of melanin pigment in the skin, not only can brighten the skin tone to realize skin whitening, but also improve skin hyperpigmentation such as spots, freckles, etc. caused by ultraviolet rays, hormones and genetic causes. have.

Therefore, conventionally, substances having inhibitory activity against tyrosinase such as hydroquinone, ascorbic acid, kojic acid, glutathione, and the like are applied to cosmetics such as skin ointments and essences. By blending, skin whitening was realized or skin hyperpigmentation such as blemishes and freckles was improved. However, hydroquinone exhibits a predetermined whitening effect, but has a problem of limiting the blending amount to a very small amount due to severe skin irritation. Kojic acid has the disadvantage of being unstable in solution, which complicates the manufacturing process of the cosmetic. In addition, thiol-based compounds such as glutathione and cysteine not only have a characteristic unpleasant odor, but also have problems with transdermal absorption, and glycosides and derivatives thereof have high polarity, making it difficult to use as a cosmetic ingredient. Placenta extract, on the other hand, has no irritation to the skin, but lacks a whitening effect.

Therefore, the technical problem to be achieved by the present invention is to solve the above problems to provide a composition for skin whitening excellent in product stability and safe use without side effects on the skin, as well as inhibiting melanin production to inhibit pigmentation. have.

In order to achieve the above technical problem, the present invention provides a composition for skin whitening containing cytosterol as an active ingredient.

In the composition for skin whitening according to the present invention, the content of cytosterol is preferably 0.000001 to 10% by weight based on the total weight of the composition.

Hereinafter, the composition for skin whitening according to the present invention will be described in detail.

Sitosterol (Sitosterol; CAS 83-46-5; β-sitosterol, (3β) -stigmast-5-en-3-ol) contained in the cosmetic composition for skin whitening according to the present invention; C ₂₉ H ₅₀ O, Mw 414.72, hereinafter referred to as Sitosterol) is represented by the following general formula (1).

<Formula 1>

These cytosterols have the effect of inhibiting the absorption of cholesterol (anticholesteremic), and also inhibits cancer (J. Natl. Cancer Inst. 69, 1982; Clin. Ther., 2000, 22 (5), 573-582). Reported.

As described above, although cytosterol is known as an inhibitor of cholesterol absorption and cancer development, the present inventors have used mice to screen the mouse melanoma cells (B16 mouse melanoma cells) capable of screening to substances that inhibit melanin synthesis induction. Experiments with the subjects revealed that they exhibit very potent melanin inhibitory and whitening effects. Therefore, according to the present invention, the addition of cytostolol to a cosmetic composition such as skin, lotion, cream, foundation, essence, gel, pack, foam cleansing, soap or pharmaceutical composition such as external skin ointment has a strong skin whitening effect without any side effects. Can be represented.

Cytosterol, an active ingredient of the composition for skin whitening according to the present invention, is an organic compound consisting of 29 carbon atoms (C ₂₉ H ₅₀ O), pea ( Pisum sativum ), Paeonia lactiflora , ginseng ( panax ginseng ), Patrinia scabiosaefolia ), Foliage, Paulownia tomentosa , Perilla frutescens , Landing ( Phytolacca acinosa ), Pinellia ternata , Piper nugrum , Notopterygium incisum , Teapot ( Plantago asiatica ), Urinary tract Hundreds of plants , including Polygonum hydropiper , Polygonum multiflorum , Bridges ( Polygonum orientale ), Cheongdae ( Polygonum tinctoria ), Cheon ( Poncirus trifoliata ), Portulaca oleracea , Lycium chinense , Daphne genkwa It is reported to be contained in, and is sold by Sigma. For example, a method of extracting cytosterol from Daphne genkwa is as follows.

First, a commercialized herbal medicine is purchased and ground finely, and then extracted by heating in an extractor equipped with a reflux condenser with a solvent such as methanol. The resultant was filtered with a filter cloth, and the residue was further extracted one or more times in the same manner. The extracts were combined, concentrated under reduced pressure, and lyophilized or spray dried to obtain a dry extract. The dried extract was suspended in water, and then the same volume of methanol, followed by liquid-liquid extraction to obtain a methanol fraction, which was then purified by column chromatography and high-performance liquid chromatography (HPLC) filled with silica gel, activated alumina, and the like. High purity cytosterol can be obtained.

Cytosterol may be used in various skin whitening compositions such as cosmetics or cosmetics such as external skin ointment. The content of cytosterol contained in preparing the composition according to the present invention is preferably 0.000001 to 10% by weight, more preferably 0.0001 to 10.0% by weight, based on the total weight of the composition. If the content is less than 0.000001% by weight, it is difficult to expect a clear melanin production inhibitory effect and a whitening effect, and when the content is more than 10% by weight, a distinct effect is not expected.

Hereinafter, the present invention will be described in detail with reference to Examples. However, embodiments according to the present invention can be modified in many different forms, the scope of the present invention should not be construed as limited to the embodiments described below. Embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.

Experimental Examples 1-3

Cytosterol (β-sitosterol from soybeans; minimum purity 97%) and a hydroquinone aqueous solution purchased from Sigma were added to the culture medium of B-16 mouse melanomacell to test the whitening effect at the cellular level ( Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980). The final concentration of cytosterol was 1 µg / ml, 5 µg / ml and 20 µg / ml (Experimental Examples 1 to 3), and the final concentration of hydroquinone was 1 µg / ml, respectively, of B-16 melanoma cells. After culturing for 3 days by adding to the culture medium, cells were trypsinized, separated from the culture vessel, centrifuged, and melanin was extracted.

1 ml of sodium hydroxide solution (1N concentration) was added thereto to boil for 10 minutes to dissolve the melanin, and the absorbance was measured at 400 nm using a spectrophotometer to indicate the amount of melanin produced per unit cell count (10 ⁶ cell). In addition, the relative melanin production relative to the control was calculated as the inhibition rate (%) and the results are shown in Table 1 below.

sample Melanin production % Inhibition Control group (no addition) 0.054 ± 0.003 - Experimental Example 1 (final concentration 1 μg / ml) 0.036 ± 0.001 30% Experimental Example 2 (final concentration 5 µg / ml) 0.022 ± 0.003 56% Experimental Example 3 (final concentration 20 µg / ml) 0.009 ± 0.001 79% Hydroquinone (final concentration 1 µg / ml) 0.022 ± 0.002 47%

* Repeat count = 3

Referring to Table 1, it can be seen that the cytosterol has a very strong melanin production inhibitory ability against the melanoma cells of the cultured mice compared to the control group (Experimental Examples 1 to 3), and hydroqui, a known whitening substance. It can be seen that the effect does not drop even when compared to rice fields. In addition, hydroquinone has a strong melanin production inhibitory ability at low concentrations, it is not applicable to the cytotoxicity is more than 1 µg / ml or more. However, since cytosterol does not exhibit cytotoxicity even at high concentrations of 20 µg / ml or more, it may exhibit a higher melanin production inhibitory effect (Experimental Examples 2 and 3) than hydroquinone.

In the following, the preparation of the skin whitening composition by adding the cytosterol to the external skin ointment, cream, supple cosmetics, essences, packs and nutrient cosmetics, and examines the pigmentation inhibitory effect by prescribing them to the test subjects.

Example 1

Cytosterol was added as an active ingredient, and an external skin ointment was prepared using the ingredients and contents shown in Table 2 below.

Comparative Example 1

Skin ointment was prepared by using the ingredients and contents shown in Table 2 without adding cytosterol.

Composition Example 1 (% by weight) Comparative Example 1 (% by weight) Sitosterol 0.1 - Diethyl sebacate 8 8 Prepayment 5 5 Polyoxyethylene oleyl ether phosphate 6 6 Sodium benzoate Quantity Quantity vaseline to 100 to 100

Example 2

Sitosterol was added as an active ingredient, and a cream was prepared using the ingredients and contents shown in Table 3 below.

Comparative Example 2

Cream was prepared with the ingredients and contents shown in Table 3 below without the addition of cytosterol.

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

Example 3

Sitosterol was added as an active ingredient, and the softener was prepared in the ingredients and contents shown in Table 4 below.

Comparative Example 3

Without adding cytosterol, the softening water was prepared with the ingredients and contents shown in Table 4 below.

Composition Example 3 (% by weight) Comparative Example 3 (wt%) Sitosterol 0.1 - ethanol 10.0 10.0 Polylauric acid polyoxyethylene sorbitan 1.0 1.0 Methyl paraoxybenzoate 0.2 0.2 glycerin 5.0 5.0 1,3-butylene glycol 6.0 6.0 incense Quantity Quantity Pigment Quantity Quantity Purified water to 100 to 100

Example 4

Cytosterol was added as an active ingredient, and nutritional cosmetics were prepared using the ingredients and contents shown in Table 5 below.

Comparative Example 4

No nutrients were added to the ingredients and contents shown in Table 5 below without the addition of cytosterol.

Composition Example 4 (% by weight) Comparative Example 4 (wt%) Sitosterol 0.1 - Waselin 2.0 2.0 Sesquioleate sorbitan 0.8 0.8 Polyoxyethylene oleylethyl 1.2 1.2 Methyl paraoxybenzoate Quantity Quantity Propylene glycol 5.0 5.0 ethanol 3.2 3.2 Carboxy Vinyl Polymer 18.0 18.0 Potassium hydroxide 0.1 0.1 Pigment Quantity Quantity incense Quantity Quantity Purified water to 100 to 100

Example 5

Sitosterol was added as an active ingredient, and a pack was prepared with the ingredients and contents shown in Table 6 below.

Comparative Example 5

Packs were prepared with the ingredients and contents shown in Table 6 below without the addition of cytosterol.

Composition Example 5 (% by weight) Comparative Example 5 (wt%) Sitosterol 0.2 - glycerin 5.0 5.0 Propylene glycol 4.0 4.0 Polyvinyl alcohol 15.0 15.0 ethanol 8.0 8.0 Polyoxyethylene oleylethyl 1.0 1.0 Methyl paraoxybenzoate 0.2 0.2 incense Quantity Quantity Pigment Quantity Quantity Purified water to 100 to 100

Example 6

Sitosterol was added as an active ingredient, and an essence was prepared with the ingredients and contents shown in Table 7 below.

Comparative Example 6

Essence was prepared with the ingredients and contents shown in Table 7 below, without the addition of cytosterol.

Composition Example 6 (% by weight) Comparative Example 6 (wt%) Sitosterol 0.5 - Propylene glycol 10.0 10.0 glycerin 10.0 10.0 Sodium hyaluronate aqueous solution (1%) 5.0 5.0 ethanol 5.0 5.0 Polyoxyethylene Cured Castor Oil 1.0 1.0 Methyl paraoxybenzoate 0.1 0.1 incense Quantity Quantity Purified water to 100 to 100

The method used to verify the pigmentation inhibitory effect by the skin external ointment, cream, supple cosmetics, nutrient cosmetics, pack, essence prepared as described above is as follows.

First, select 20 healthy men and women and attach aluminum foil with two rows of 6 holes with a diameter of 7 mm in the lower part of both arms, and use 60mJ / ㎠ light with a ORIEL solar simulaltor 1000W at a distance of 10cm from the arm. Was investigated. The irradiation site was washed well with 70% ethanol aqueous solution before irradiation. Cytosterol-containing compositions prepared according to Examples 1 to 6 twice a day from 3 days before irradiation to 3 weeks after irradiation, and a base without cytososterol according to Comparative Examples 1 to 6 were applied to the same row in pairs. . Here, the pack agents of Example 5 and Comparative Example 5 were removed 15 minutes after the application.

After prescribing a composition according to each example and a comparative example according to the above method, the degree of pigmentation was visually determined, and the pigmentation inhibition degree of the composition according to each example and the composition according to the comparative example was effective. , And evaluated in two stages of no difference, and also examined the occurrence of skin side effects are shown in Table 8 below.

Experimental substance Effective (persons) No difference (persons) Side effects (persons) Example 1 14 6 0 Example 2 13 7 0 Example 3 10 10 0 Example 4 10 10 0 Example 5 9 11 0 Example 6 14 6 0

As shown in Table 8, the cytosterol-containing composition prepared according to Examples 1 to 6 showed a significant skin whitening effect on at least 9 or more of 20 subjects, and showed no side effects in the skin. there was.

As described above, the composition for skin whitening containing cytosterol according to the present invention inhibits melanin production and inhibits pigmentation, and thus is effective for improving skin whitening or blemishes and freckles. It can also be used safely because it does not show any side effects in the skin.

Claims (3)

Skin whitening composition characterized in that it contains a sitosterol (Sitosterol) represented by the general formula (1) as an active ingredient. <Formula 1> According to claim 1, wherein the content of the cytosterol is a skin whitening composition, characterized in that 0.000001 to 10% by weight based on the total weight of the composition. According to claim 1, wherein the skin whitening composition is a skin whitening, characterized in that consisting of any one selected from the group consisting of skin, lotion, cream, foundation, essence, gel, pack, foam cleansing, soap and skin ointment. Composition.