KR20050037103A - Cosmetic composition for whitening of the skin - Google Patents

Abstract

The present invention relates to a cosmetic composition for skin whitening, and more particularly, for skin whitening comprising Jervine ((3β, 23β) -17,23-Epoxy-3-hydroxyveratraman-11-one) as an active ingredient. It relates to a cosmetic composition.

The cosmetic composition for skin whitening of the present invention suppresses melanin production of the skin, and is very excellent in improving blemishes and freckles and skin whitening effect.

Description

Cosmetic composition for skin whitening {Cosmetic Composition for Whitening of the Skin}

[Industrial use]

The present invention relates to a cosmetic composition for skin whitening, and more particularly, to a cosmetic composition for skin whitening which is very excellent in reducing skin and freckles and improving skin whitening effect by inhibiting melanin production.

[Private Technology]

It is everyone's constant desire to have white, fair skin. Human skin color is genetically determined by the concentration and distribution of melanin in the skin, but is also influenced by environmental or physiological conditions such as sun ultraviolet rays, fatigue and stress.

Melanin is produced through a non-enzymatic oxidation reaction after tyrosine, an amino acid, acts as an enzyme called tyrosinase, transforming it into dopa and dopaquinone. However, although the pathway by which melanin is made is known, it is not yet known in detail what mechanisms induce melanin synthesis, which is the previous step in the action of tyrosinase.

Therefore, conventionally, a substance having tyrosinase inhibitory activity, such as arbutin, hydroquinone, ascorbic acid, kojic acid, or glutathione, is blended into ointments or cosmetics, and the skin is whitened or blemished. It has been used for the purpose of improving freckles, but the use is limited because it causes skin irritation or poor product stability, and thus the effect is also weak.

Therefore, there is an urgent need for the development of new skin whitening agents having less irritation, better stability, and superior melanin production and skin whitening cosmetic compositions using such skin whitening cosmetic compositions.

The present invention is to solve the above-mentioned conventional problems, an object of the present invention is to provide a cosmetic composition for skin whitening excellent in suppressing the melanin production of skin, freckles and skin whitening effect is very excellent.

In order to achieve the above object, the present invention provides a melanin containing Jervine ((3β, 23β) -17,23-Epoxy-3-hydroxyveratraman-11-one) (hereinafter referred to as 'zerbin') An inhibitor composition is provided.

The present invention also provides a cosmetic composition for skin whitening comprising the gerbin as an active ingredient.

EMBODIMENT OF THE INVENTION Hereinafter, this invention is demonstrated in detail.

The inventors of the present invention have developed a substance having an excellent skin whitening effect as an active ingredient of a cosmetic composition for skin whitening, and have found that the gerbin is not toxic, has good stability, and has an excellent skin whitening effect and completes the present invention. It became. There has been no previous study on the skin whitening effect of gerbin, the active ingredient of the present invention.

The zerbin is represented by the following formula (1).

Zerbin in its natural state is an alkaloid compound mainly found in the roots of lilies. There are many ways to get a gerbin. For example, finely chopped roots of lilies can be obtained by adding water, anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms, ethyl acetate, acetone, chloroform or a mixture thereof, followed by warm extraction, solvent fractionation and recrystallization. have.

By preparing a cosmetic composition for skin whitening containing gerbin as an active ingredient and applying it to the human body, it is possible to obtain an excellent melanin production inhibitory effect and skin whitening effect. In this case, the cosmetic composition for skin whitening may include 1 × 10 ⁻⁶ wt% to 10 wt% of gerbin as a skin whitening agent, preferably 0.001 wt% to 10 wt%, and more preferably Preferably from 0.1% to 10% by weight. If the content of the zerbin is less than 1 × 10 ^-6 % by weight can not expect a distinct effect, if the content of more than 10% by weight does not increase the effect compared to the increase in the amount.

The cosmetic composition for skin whitening according to the present invention is an external ointment, cream, foam, lotion, pack, softening water, latex, foundation, makeup base, essence, soap, liquid cleanser, bathing agent, sunscreen cream, or sun oil It can be prepared by.

In addition, the cosmetic composition of the present invention can be appropriately blended with conventional ingredients, such as oil, water, surfactants, moisturizers, lower alcohols, thickeners, chelating agents, pigments, preservatives, fragrances and the like, which are blended in general skin cosmetics.

Hereinafter, preferred examples are provided to help understanding of the present invention, but the following examples are merely to illustrate the present invention, and the scope of the present invention is not limited to the following examples.

 Example 1 Extraction of Zerbin

1-1: Extraction of Zerbin Using Methanol

1 kg of dried root of Veratrum nigrum was placed in 10 liters of methanol, and extracted by heating at 80 ° C. for 3 hours in an extractor equipped with a reflux condenser to obtain 52 g of methanol extract. The hexane and chloroform fractions were removed from the methanol extract through a solvent fraction, and the obtained fractions were fractionated three times with saturated butanol to obtain 24 g butanol fraction. The obtained butanol fraction was subjected to silica column chromatography several times to obtain 0.3 g of a fraction containing zerbin, and the fraction was purified by preparative HPLC (Prep-HPLC) and recrystallization. Got it. Zerbin obtained by the above method was identified by nuclear magnetic resonance (NMR) and mass spectroscopy (Mass spectroscopy) to determine the composition and content (99.9% by weight or more). 1 and 2 show ¹ H-NMR spectra and ¹³ C-NMR spectra of the gerbins, respectively, and the numbers in each peak correspond to the numbers in the chemical formulas of FIGS. 1 and 2. 3 shows the mass spectrum of the zerbin.

1-2: Gerbin Extraction Using Chloroform

1 kg of dried dried roots were placed in 10 liters of chloroform, and extracted by heating at 100 ° C. for 3 hours in an extractor equipped with a reflux condenser to obtain 20 g of chloroform extract. To the chloroform extract was added 5% by weight aqueous solution of tartaric acid (tartaric acid) to obtain a soluble part, neutralized with NaOH, and 1 g of the chloroform fraction obtained by solvent fractionation with chloroform was purified using preparative HPLC (Prep-HPLC) and recrystallization. Got a bin. Zerbin obtained by the above method was identified by nuclear magnetic resonance (NMR) and mass spectroscopy (Mass spectroscopy) to determine the composition and content (99.9% by weight or more).

Example 2 Skin Whitening Effect of Zerbin

Gerbin was added to the culture medium of B-16 mouse melanoma cells to test the skin whitening effect at the cellular level. (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980) .

Gerbin was added to the culture medium of the melanoma cells at a final concentration of 1 μg / ml, 5 μg / ml, 10 μg / ml, and 20 μg / ml, respectively, and cultured for 3 days, and then the cells were trypsin After treatment and separation from the culture vessel and centrifugation, 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 calculated by absorbance per unit cell number (1 × 10 ⁻⁶ cells), and the amount and the inhibition rate of melanin are shown in Table 1 below. For comparison, melanin production and inhibition rate were measured in the same manner for the control group containing arbutin and the control group without gerbin, which are known as skin whitening agents. Inhibition rate in the following table is calculated relative to the control melanin production in%.

[Table 1] Melanin production inhibitory effect at the cellular level according to the concentration

Sample added Application concentration (µg / ml) Melanin Production (Abs) % Inhibition Control - 0.060 ± 0.003 - Zerbin One 0.041 ± 0.001 32 5 0.028 ± 0.001 54 10 0.016 ± 0.001 73 20 0.005 ± 0.001 91 Arbutin 200 0.032 ± 0.001 47

                                                 * Number of repeat tests = 3

As can be seen from the results of Table 1, it can be seen that gerbin has a much superior melanin production inhibitory effect on melanoma cells in cultured rats, compared to the known whitening agent arbutin.

Hereinafter, the production examples and comparative examples of the cosmetic composition for skin whitening containing zerbin are shown.

[Example 3 and Comparative Example 1] skin external ointment for skin whitening

Formulation of the skin whitening ointment for skin whitening comprising a zebin was prepared in Example 3, Comparative Example to prepare a skin external ointment in the same manner as in Example 3, except that it does not contain a gerbin It was set to 1. Detailed compositions are shown in Table 2 below.

TABLE 2

Composition water Example 3 (% by weight) Comparative Example 1 (% by weight) Zerbin 2 - Diethyl sebacate 8 8 Prepayment 5 5 Polyoxyethylene Oleyl Ether Phosphate 6 6 Sodium benzoate 0.1 0.1 Waselin to 100 to 100

[Example 4 and Comparative Example 2] cosmetic cream for skin whitening

Formulation of the skin whitening cosmetic cream containing zerbin was prepared in Example 4, except that it does not contain a gerbin of the above Example 4 to prepare a cosmetic cream as in Comparative Example 2 It was. Detailed compositions are shown in Table 3 below.

TABLE 3

Composition water Example 4 (% by weight) Comparative Example 2 (wt%) Zerbin 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 0.05 0.05 incense 0.05 0.05 Purified water to 100 to 100

[Example 5 and Comparative Example 3] supple cosmetics for skin whitening

Formulation of the skin whitening softener containing a zerbin was prepared in Example 5, except that it does not contain a gerbin of the above Example 5 to prepare a flexible cosmetics in the same manner as in Comparative Example 3 It was. The detailed composition is shown in Table 4 below.

TABLE 4

Composition water Example 5 (% by weight) Comparative Example 3 (wt%) Zerbin 0.2 - 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 0.05 0.05 Pigment 0.05 0.05 Purified water to 100 to 100

[Example 6 and Comparative Example 4] cosmetic nutrient cosmetics for skin whitening

Formulation of the skin whitening nutrient for the skin whitening containing zerbin was prepared in Example 6, except that the formulation was prepared in the same manner as in Example 6, except that it does not contain the gerbin of Comparative Example 4 It was. Detailed compositions are shown in Table 5 below.

TABLE 5

 Composition water Example 6 (% by weight) Comparative Example 4 (wt%) Zerbin 0.1 - Waselin 2.0 2.0 Sesquioleate sorbitan 0.8 0.8 Polyoxyethylene oleylethyl 1.2 1.2 Methyl paraoxybenzoate 0.1 0.1 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 0.05 0.05 incense 0.05 0.05 Purified water to 100 to 100

[Example 7 and Comparative Example 5] cosmetic pack for skin whitening

Formulation of the skin whitening cosmetic pack containing a zerbin was prepared in Example 7, except that the formulation does not include a zerbin in Example 7 to prepare a cosmetic pack in Comparative Example 5 It was. Detailed compositions are shown in Table 6 below.

TABLE 6

 Composition water Example 7 (% by weight) Comparative Example 5 (wt%) Zerbin 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 Pigment 0.05 0.05 incense 0.05 0.05 Purified water to 100 to 100

[Example 8 and Comparative Example 6] Cosmetic Essence for Skin Whitening

Formulation of the skin whitening cosmetic essence comprising a zerbin was prepared in Example 8, except that the formulation does not include a zerbin of the same as in Example 8 to prepare a cosmetic essence to Comparative Example 6 It was. The detailed composition is shown in Table 7 below.

TABLE 7

 Composition water Example 8 (% by weight) Comparative Example 6 (wt%) Zerbin One - 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 0.05 0.05 Purified water to 100 to 100

Example 9 Skin Whitening Effect Test Through Panel Test

The cosmetic composition of Examples 3 to 8 and Comparative Examples 1 to 6 was tested on the skin whitening effect of 20 healthy men and women as follows.

Twenty males and females, 35 to 50 years old, were placed in the lower arm of each arm with two holes of 6 mm diameter holes in two rows of aluminum foil, and ORIEL solar simulator 1000 W at a distance of 10 cm from the arm. The amount of light of 60 mJ / cm ² was irradiated. The irradiation site was washed well with 70% ethanol aqueous solution before irradiation. The cosmetic composition prepared according to Examples 3 to 8 and Comparative Examples 1 to 6 was applied to the same line twice a day from 3 days before irradiation to 3 weeks after irradiation. The cosmetic packs of Example 7 and Comparative Example 5 were removed 15 minutes after the application.

The degree of pigmentation of each Example and Comparative Example was visually determined, and the degree of suppression of pigmentation was evaluated by two steps of 'Effective' and 'No Effect' compared to Comparative Example, and the results are shown in the following table. 8 is shown.

[Table 8] Skin wrinkle improvement effect of the embodiment according to the present invention (person)

sample Effective no effect Example 3 13 7 Example 4 11 9 Example 5 11 9 Example 6 10 10 Example 7 12 8 Example 8 14 6

As can be seen in Table 8, the cosmetic composition comprising a gerbin prepared according to Examples 3 to 8 of the present invention showed a whitening effect on at least 10 or more of 20 subjects, and no side effects appear in the skin There is no toxicity to the skin, stability is good, it can be seen that the cosmetic composition for skin whitening has a very good skin whitening effect. In addition, in the test results of Example 9, no skin irritation or side effects by the gerbin of the present invention was found.

As described above, the cosmetic composition for skin whitening containing gerbin as an active ingredient has suppressed melanin production, and thus the effect of improving blemishes and freckles and skin whitening showed very excellent effects.

The cosmetic composition for skin whitening of the present invention contains gerbin as an active ingredient, inhibits melanin production of the skin, and is very excellent in improving the blemishes and freckles and skin whitening effect.

1 shows the ¹ H-NMR spectrum of Zerbin.

2 shows the ¹³ C-NMR spectrum of Zerbin.

3 shows the mass spectrum of the gerbin.

Claims (5)

Melanin inhibitor composition comprising Jervine (Jervine: (3β, 23β) -17,23-Epoxy-3-hydroxyveratraman-11-one) as an active ingredient. As a melanin production inhibitor, a cosmetic composition for skin whitening comprising gerbin as an active ingredient. The cosmetic composition for skin whitening according to claim 2, wherein the cosmetic composition for skin whitening comprises 1 × 10 ⁻⁶ wt% to 10 wt% of gerbin based on the total weight of the composition. The cosmetic composition for skin whitening according to claim 2, wherein the cosmetic composition for skin whitening comprises 0% by weight to 10% by weight with respect to the total weight of the composition. The cosmetic composition for skin whitening according to claim 2, wherein the cosmetic composition for skin whitening is an external ointment, a cream, a foam, a lotion, a pack, a soft water, an emulsion, a foundation, a makeup base, an essence, a soap, a liquid cleanser, a bath, a sunscreen cream, and a sun oil Cosmetic composition for skin whitening having a formulation selected from the group consisting of.