KR20110051476A

KR20110051476A - Skin whitening agent

Info

Publication number: KR20110051476A
Application number: KR1020090108077A
Authority: KR
Inventors: 김청택
Original assignee: 주식회사 알엔에스
Priority date: 2009-11-10
Filing date: 2009-11-10
Publication date: 2011-05-18

Abstract

PURPOSE: A cosmetic composition containing a compound which suppresses melanogenesis is provided to suppress pigmentation and to ensure effective skin whitening. CONSTITUTION: A skin whitening agent contains a compound selected from chemical formula 1-3 as an active ingredient. The compounds of chemical formulas 1, 2, and 3 are mollugin, wogonin, and dihydromollugin, respectively. The compound is derived from animals and plants. A composition for skin whitening is manufactured in the form of skin lotion, cream, foundation, essence, gel, pack, foam cleansing, or ointment.

Description

Skin whitening agent

The present invention relates to a cosmetic for skin whitening, in more detail can be used safely without side effects on the skin and has a melanin production inhibitory activity (mollugin), wogonin (wogonin), dihydromollugin (dihydromollugin) compound And it relates to a composition for skin whitening containing the same, and more particularly to an external composition for skin excellent in whitening effect.

Skin melanogenesis is a defense mechanism against melanocyte melanocytes (melanocytes) stimulation of ultraviolet light and the like melanogenesis is increased and a large amount of melanin is transferred to the keratinocytes accumulated in the skin epidermal layer The result is. Although melanin protects the skin, hyperpigmentation of the skin causes blemishes, freckles, darkening of the skin after skin inflammation, and senile pigment spots. It may also result. The melanin production process is made through the non-enzymatic oxidation reaction of tyrosine, an amino acid, by the action of tyrosinase, which is transformed into dopa and dopaquinone. It is known that abnormal deposition occurs for spots, blotch, and the like. To alleviate, prevent, and treat pigmentation, blemishes, and spots, substances that inhibit melanin production, such as hydroquinone, arbutin, ascorbic acid, and kojic acid ) And glutathione have been developed and blended with cosmetics to achieve skin whitening or improve skin hyperpigmentation such as blemishes and freckles. However, although hydroquinone is once recognized for its effectiveness, its use is generally limited due to severe skin irritation. Ascorbic acid is easily oxidized, and the cosmetics containing the same cause problems such as discoloration and deodorization. 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.

In order to solve the above problems, the present invention has no side effects on the skin, and excellent in inhibiting melanin production to provide a composition for skin whitening excellent in inhibiting skin pigmentation.

In order to solve the above technical problem, the present invention provides a melanin production inhibitor selected from the group consisting of compounds represented by the following formulas 1 to 3 excellent in melanin inhibitory effect and whitening effect.

The present invention also provides a skin whitening agent selected from the group consisting of the compounds represented by Formulas 1 to 3 and a composition for skin whitening containing any one or more of these as an active ingredient.

As such, mollugin, molybgin, wogonin, and dihydromollugin of the present invention inhibit melanin production of melanocytes, and thus compositions such as cosmetics containing them as active ingredients improve blemishes and freckles. It can be used very effectively to improve skin hyperpigmentation and to achieve skin whitening.

Hereinafter, the present invention will be described in more detail.

The present invention relates to mollugin (mollugin, C17H16O4, CAS No. 55481-88-4, MW: 284.3) of Formula 1, wogonin (C16H12O5, CAS No. 632-85-9, MW: 284.3) and dihydromollugin (C ₁₇ H ₁₈ O 4, MW: 286.3) of Formula 3 to provide a melanogenesis inhibitor.

The present inventors conducted a new whitening agent study on native plants and animals using B16 mouse melanoma cells capable of screening even substances that inhibit melanin synthesis induction. The compounds of the compounds 1 to 3 have been found to have a very strong melanin production inhibitory effect and whitening effect to complete the present invention.

Compounds of the above-mentioned formulas (1) to (3) can be easily purchased on the market, either individually or by mixing two or more kinds, such as skins, lotions, creams, foundations, essences, gels, packs, foam cleansing, soaps, etc. An effective amount may be added to various compositions such as ointments to exhibit skin lightening effects. In consideration of the skin whitening effect and economical efficiency, the amount of the compound added is preferably 0.00001 to 10% by weight based on the total weight of the composition, more preferably 0.001 to 1.0% by weight.

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. The embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.

Experimental Example 1. Testing of melanogenesis inhibitory effect at the cellular level

Commercially available compounds of Formulas 1 to 3 were purchased and used. Each compound was added to the culture medium of B-16 mouse melanoma cells and the whitening effect at the cellular level was tested as follows (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980). Each compound was added to the culture medium at the final concentration of 5 μg / ml, 20 μg / m, and cultured for B-16 melanoma cells, incubated for 3 days, and treated with trypsin, and then from the culture vessel. After stripping off and centrifugation, melanin was extracted. To the extracted melanin, 1 ml of sodium hydroxide solution (1N concentration) was added, boiled for about 10 minutes to dissolve the melanin, and the absorbance was measured at 400 nanometers (nm) with a spectrophotometer. ^The experiment was carried out by a method showing the absorbance of ⁶ cells). The experiment was repeated three times and the average value was used to calculate the relative melanin production relative to the control group as inhibition rate (%), and the results are shown in Table 1 below.

sample Melanin production % Inhibition Control group (no addition) 0.044 ± 0.004 - arbutin (final concentration 300 ㎍ / ml) 0.028 ± 0.004 36 mollugin (final concentration 5 ㎍ / ml) 0.034 ± 0.001 23 mollugin (final concentration 20 ㎍ / ml) 0.020 ± 0.003 55 wogonin (final concentration 5 ㎍ / ml) 0.036 ± 0.002 18 wogonin (final concentration 20 ㎍ / ml) 0.028 ± 0.002 36 dihydromollugin (final concentration 5 ㎍ / ml) 0.030 ± 0.002 32 dihydromollugin (final concentration 20 ㎍ / ml) 0.014 ± 0.003 68

Iterations = 3

As shown in Table 1, the compounds of Formulas 1 to 3 showed excellent melanin production inhibitory activity even at low concentrations against melanoma cells of cultured mice, compared to arbutin, a whitening substance known in the art, and cytotoxicity Did not appear. This indicates that the present invention can be very useful for improving blemishes and freckles and skin whitening.

Manufacturing example 1 to 3 and Comparative example One

Each component shown in Table 2 below was mixed in the ratio shown in Table 2 to prepare an external skin ointment.

Composition weight% Preparation Example 1 Production Example 2 Production Example 3 Comparative Example 1 mollugin
wogonin
dihydromollugin
Diethyl sebacate
Prepayment
Polyoxyethylene Oleyl Ether Phosphate
Sodium benzoate
vaseline 0.1
-
-
8
5
6

Suitable amount
Remaining amount * -
0.1
-
8
5
6

Suitable amount
Remaining amount * -
-
0.1
8
5
6

Suitable amount
Remaining amount * -
-
-
8
5
6

Suitable amount
Remaining amount *

*: Amount to be 100% by weight in total

In order to verify the skin whitening effect on the external skin study prepared with the above-described composition, the pigmentation inhibition and blemish improvement experiment was conducted as follows.

Experimental Example 2. Pigmentation inhibition effect experiment

Twenty healthy men and women were selected as subjects, covered with aluminum foil with two rows of three holes with a diameter of 7 mm in the lower part of both arms, and 60 mJ with a ORIEL Solar Simulator 1000W at a distance of 10 cm from the arm. The amount of light of / cm 2 was investigated. The bases prepared according to Preparation Examples 1-3 and Comparative Example 1 were applied to the same row twice a day from 3 days before irradiation to 3 weeks after irradiation. 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 in two stages of the effect and no difference compared to the comparative example, and the results are shown in Table 3.

Experimental substance Effective (persons) No difference (persons) Preparation Example 1 17 3 Production Example 2 15 5 Production Example 3 19 One

As can be seen from the results of Table 3, the external application ointment of Preparation Examples 1 to 3 showed a whitening effect on at least 15 of 20 subjects, and did not show any side effects in the skin and was safe and improved freckles and freckles. It can be seen that the skin whitening agent has an excellent effect on.

Claims

Skin whitening agent selected from the group consisting of compounds represented by the formula (1 to 3).

A skin whitening composition comprising any one or more selected from the group consisting of compounds represented by Formulas 1 to 3 as an active ingredient.

The composition for skin whitening according to claim 2, wherein the content of the active ingredient is 0.00001 to 10 wt% based on the total weight of the composition.

According to claim 2, wherein the skin whitening composition is a skin whitening composition, characterized in that formed in any one formulation selected from the group consisting of skin, lotion, cream, foundation, essence, gel, pack, product cleansing and ointment.