JPH06166609A - Whitening and beautifying agent - Google Patents

Abstract

PURPOSE:To obtain a beautifying and whitening agent or an improver for pigmentation having excellent effects. CONSTITUTION:This beautifying and whitening agent or improver for pigmentation comprises a bearberry leaf capable of suppressing melanogenesis causing the pigmentation such as dermal stains, ephelides or dark skin.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a whitening agent or an agent for improving pigmentation, which contains a Japanese lacquer tree or its extract as an active ingredient.

[0002]

2. Description of the Related Art Pigmentation diseases such as spots, freckles, and dark skin are diseases in which melanin pigment is excessively deposited on the skin.

This disease is not cosmetically preferable for women, and it has been desired to improve spots, freckles, and effectively whiten the skin.

The melanin is widely distributed in the animal and plant kingdoms. Regarding its biosynthesis in vertebrates, it is a cytoplasmic granular melanosome in melanocytes, in which tyrosine is oxidized by tyrosinase and dopa, dopaquinone,
A route known to be biosynthesized through indole quinone is known,
In addition, it is known that in this route, melanin production is promoted by autoxidation by ultraviolet rays.

On the other hand, the Japanese algae is a crude drug used as a urinary tract antiseptic, and has been used for folk allergic dermatitis since ancient times.

[0006] Arbutin, which is a component of Japanese lacquer, is known to have a whitening effect, but the whitening effect is far from sufficient.

[0007] However, regarding the Japanese lacquer itself, the whitening effect and the effect of improving pigmentation such as spots and freckles are not known.

[0008]

SUMMARY OF THE INVENTION It is an object of the present invention to provide a whitening agent or a pigmentation ameliorating agent which has superior efficacy as compared with conventionally known whitening agents.

[0009]

Means for Solving the Problems As a result of intensive studies to achieve the above-mentioned objects, the present inventors have found that the Japanese lacquer tree or its extract has a superior whitening effect and an improvement in pigmentation disease as compared with arbutin. The present invention has been completed by finding out that it has an effect.

As described above, the pigmentation disease according to the present invention is a disease in which melanin pigment is excessively deposited on the skin. Specific examples thereof include skin spots caused by spots, freckles, dark skin and steroids. Examples include melanosis.

[0011] In the present invention, as regards the extract of Stelleria vulgaris, the extract obtained by using a solvent usually used for extraction of herbal extracts such as water, warm water, ethanol and hydrous ethanol, and the above-mentioned solvent from the extract. Lyophilize,
The powder obtained by removing by a method such as spray drying or distillation under reduced pressure can also be mentioned.

Various methods such as oral administration and topical administration can be mentioned as the administration method of the porcupine or its extract of the present invention, but it is generally convenient to apply it to the skin as an external preparation.

Examples of the external preparation include ointments, creams, emulsions, liniments, lotions and the like.

These preparations may be produced by mixing known additives such as a crushed product of the Japanese porcupine or an extract or powder of the extract of Japanese porcupine with appropriate additives and excipients. it can.

The dose of the Japanese algae or its extract according to the present invention varies depending on the administration method, but when administered as an external preparation, an appropriate amount of the external preparation as described above may be applied to the skin disease area.

[0016]

EFFECTS OF THE INVENTION The Japanese lacquer tree or its extract according to the present invention showed an excellent inhibitory effect on the production of melanin pigment, which is a cause of pigmentation diseases such as spots, freckles, and dark skin.

Therefore, the present invention is excellent as a whitening agent and an agent for improving pigmentation disorders such as spots, freckles, and dark skin.

Hereinafter, the present invention will be described in more detail with reference to Reference Examples and Examples, but the present invention is not limited thereto.

[0019]

[Reference example] Roughly cut 100 kg of Japanese urchin "Urushi" to normal water 1000
Add l, raise the temperature to 90 ° C in about 30 minutes, and
After extracting at 1 ° C for 1 hour, the mixture was filtered at a liquid temperature of 65 ° C using a stainless steel wire mesh (120 mesh) to obtain a first extract.
1000 l of ordinary water was added to the residue, and the mixture was extracted for 1 hour in the same manner, and then filtered at a liquid temperature of 65 ° C using a stainless steel wire net (120 mesh) to obtain a second extract. The first extract and the second extract were combined and concentrated under reduced pressure (pressure reduction 120 mmHg) at 60 ° C. or lower to obtain about 24.0 kg of the Japanese lacquer extract. 120 l of absolute ethanol was added to this lacquer extract, and after thoroughly stirring, the mixture was allowed to stand overnight at room temperature and filtered using a stainless steel wire mesh (120 mesh). Concentrate the filtrate under reduced pressure at 60 ° C or lower (degree of vacuum 12
(0 mmHg), then suspended in about 100 l of normal water and spray-dried to obtain a dried extract (yield about 12.4 kg).

[0020]

【Example】

1) Subject ・ Dried extract of Steller's sea urchin extract (hereinafter abbreviated as U-ext) ・ Reference arbutin 2) Sample ・ Mushroom-derived tyrosinase (3870 Units / mg Si
gma) (5 mg of the above tyrosinase was added to 10 ml of 1/15 M
It was dissolved in a phosphate buffer before use.・ 1/15 M Phosphate buffer: monopotassium phosphate dipotassium phosphate (0.4999 g of the above-mentioned monopotassium phosphate and 0.5214 g of dipotassium phosphate were dissolved in 100 ml of purified water to obtain pH.
The one set to 6.8 was used.・ Dopa: manufactured by Nacalai Tesque, Inc.
It was dissolved in 100 ml of 15 M phosphate buffer before use. ) -Subjects were dissolved in a buffer and used.

Experimental Example 1: Inhibition of tyrosinase enzyme activity 1-1 Experimental method and results HS Mason (Biochem. Biophys. Acta., 111, 134 (1965)), T.
According to the method of Nagatu (Experientia, 28,634 (1972)), the enzyme tyrosinase solution (5 mg / 10 ml) was added to 1 ml of the test solution.
Add 1 ml and 0.9 ml of 1/15 M phosphate buffer (pH 6.8),
Incubated at 25 ° C for 10 minutes. Next, add 1 ml of the substrate dopa solution (0.03% pH 6.8 phosphate buffer) at 25 ° C,
Incubated for 5 minutes. After the reaction, the absorbance at 475 nm was measured (D ₁ ). Separately, the same operation was performed using a heat-inactivating enzyme, and the absorbance (D ₂ ) and the amount of dopachrome produced (D ₃ ) in the absence of the sample were measured. Inhibition rate (%) = [D ₃ − (D ₁ −D ₂ )] / D ₃ × 100 The results are shown in the table below.

[0022]

[Table 1] As is clear from the above results, U-ext suppressed the tyrosinase enzyme activity in a very small amount. On the other hand, arbutin isolated from U-ext also significantly suppressed tyrosinase enzyme activity. However, the tyrosinase enzyme inhibitory activity of U-ext was about 1000 times stronger than that of arbutin.

Experimental Example 2: Effect on melanin production by inhibition of tyrosinase enzyme activity 2-1 Experimental method and results HS Mason (Biochem.Biophys.Acta., 111,134 (1965)), T.
According to the method of Nagatu (Experientia, 28, 634 (1972)), the enzyme tyrosinase solution (5 mg / 10 ml) was added to 1 ml of the test solution.
Add 1 ml and 0.9 ml of 1/15 M phosphate buffer (pH 6.8),
Incubated at 25 ° C for 10 minutes. Next, add 1 ml of the substrate dopa solution (0.03% pH 6.8 phosphate buffer) at 25 ° C,
Incubated for 30 minutes or 60 minutes. 1N hydrochloric acid 0.2
The reaction was stopped with ml, and the precipitate was obtained by centrifugation at 3000 rpm for 15 minutes. This sediment is further added with 6N hydrochloric acid 1 ml × 1 time,
After washing with 2 ml of distilled water and centrifugation twice, it was dissolved in 2 ml of Solen 350 (manufactured by Packard). When it was difficult to dissolve, it was forcibly dissolved with a sonicator. The absorbance of the solution was measured at 400 nm, and the amount of melanin was calculated from the absorbance curve of standard melanin. The results are shown in the table below.

[0024]

[Table 2] As shown in the above results, U-ext significantly suppressed melanin production in a trace amount, but arbutin had no inhibitory effect.

Experimental Example 3: Effect on melanin production by inhibition of autoxidation from dopachrome 3-1 Experimental method and results HS Mason (Biochem.Biophys.Acta., 111,134 (1965)), T.M.
According to the method of Nagatu (Experientia, 28,634 (1972)) et al., 0.1 ml of enzyme tyrosinase solution (5 mg / 10 ml) and 1/15 M
0.9 ml of phosphate buffer (pH 6.8) was added, and the mixture was incubated at 25 ° C for 10 minutes. Next, the substrate dopa solution (0.03% p
H 6.8 phosphate buffer) (1 ml) was added, the mixture was incubated at 25 ° C. for 5 minutes, 1 ml of the test solution was further added, and the mixture was incubated for 30 minutes or 45 minutes. The reaction was stopped with 0.2 ml of 1N hydrochloric acid, and the precipitate was obtained by centrifugation at 3000 rpm for 15 minutes. This sediment was further added with 6N hydrochloric acid 1 ml × 1 time, distilled water 2 m
l x 2 times of centrifugation and then 2 ml of Solen 350
(Made by Packard). If it is difficult to dissolve,
It was forcibly dissolved with a sonicator. The absorbance of the solution is 40
The measurement was performed at 0 nm, and the melanin amount was calculated from the absorbance curve of the standard melanin. The results are shown in the table below.

[0026]

[Table 3] As shown in the above results, U-ext significantly suppressed melanin production even when dopachrome was produced, that is, when oxidization by tyrosinase, but not by autooxidation involved in melanin production, significantly suppressed melanin production. Did not show its inhibitory effect.

<Conclusion> As is clear from the above results, the Japanese lacquer extract showed superior tyrosinase enzyme activity inhibitory activity and melanin production inhibitory activity as compared with arbutin. Therefore, it was confirmed that the Japanese lacquer tree or its extract has an excellent whitening effect and an effect of improving pigmentation diseases such as spots, freckles, and black skin, as compared with arbutin.

Claims (3)

[Claims] 1. A whitening agent containing a Japanese lacquer tree or its extract as an active ingredient. 2. A pigmentation amelioration agent comprising a Japanese lacquer tree or its extract as an active ingredient. 3. The improving agent according to claim 2, wherein the pigmentation is a spot or freckles.