JPH08104646A - Tyrosinase biosynthesis inhibitor and skin-beautifying agent mixed with the same - Google Patents

Abstract

PURPOSE: To obtain a tyrosinase biosynthesis inhibitor effective with a small amount and a skin-beautifying agent having excellently beautifying effect, safety and stability, containing the tyrosinase biosynthesis inhibitor. CONSTITUTION: This tyrosinase biosynthesis inhibitor contains one or more extracts of Polygonum cuspidatum, Reynoutria Japonica Houtt, Artemiseaca pillaris, Achillea millefolium, Eupatorim fortunei, Tilia platyphyllos, Tilia cordata and Tilia europaea. This skin-beautifying agent contains the tyrosinase biosynthesis inhibitor. The tyrosinase biosynthesis inhibitor effectively suppresses biosynthesis of tyrosinase in skin and effectively controls melanism from tyrosine.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a tyrosinase biosynthesis inhibitor which is highly effective and highly safe, and which contains a specific plant extract, and a whitening agent which contains the same. .

[0002]

2. Description of the Related Art Whitening cosmetics have been of great interest in improving the darkness of skin, spots, freckles, etc., and ascorbic acid, glutathione, colloidal sulfur, etc. are effective in them. It has been compounded as an ingredient.

There are also examples in which various medicinal plant extracts, plant-derived gallic acid, geraniin and the like are used. further,
Whitening ingredients such as kojic acid and arbutin, a glucopyranoside derivative, have also been used recently. It has become clear that among such whitening ingredients, there is one that inhibits tyrosinase activity and inhibits the production of dopa-dopaquinone-dopachrome from tyrosine, thereby suppressing the production of melanin pigment and exerting a whitening effect. Came.

[0004]

However, ascorbic acid is liable to be oxidized and is unstable, and glutathione and colloidal sulfur have a drawback that they have a peculiar offensive odor and precipitation.

In addition, the conventional medicinal plant extracts have problems that the effect is insufficient and the quality is not constant. Furthermore, it was necessary to consider maintaining the stability of kojic acid and the like. Besides,
In some cases, side effects occurred due to continuous use. Furthermore, even when a substance having a tyrosinase activity inhibitory effect is used as a whitening agent, the inhibitory activity was not sufficient, and in many cases, a considerable amount had to be added to expect an effect.

In order to solve the above problems, the present invention inhibits the biosynthesis of tyrosinase in the skin tissue and reduces the amount of tyrosinase itself.
The purpose of the present invention is to provide a tyrosinase biosynthesis inhibitor exhibiting an excellent whitening effect, and to apply it as a whitening agent having excellent effects and high stability and safety.

[0007]

As a tyrosinase biosynthesis inhibitor, it is desirable to use a tyrosinase biosynthesis inhibitor capable of exhibiting excellent effects even in a small amount. In addition, it has no adverse side effects on safety, and when incorporated into a whitening agent formulation,
It should not deactivate and should not affect the stability of the system. As a result of screening the substance having the tyrosinase biosynthesis inhibitory activity, we found an extremely excellent tyrosinase biosynthesis inhibitory activity in the extract of a specific plant.

That is, in the present invention, the knotweed ( Po
lygonum cuspidatum , Reynoutria japonica Houtt.),
Artemisea capillaris , Achillea millefolium , Fujibacama, Eupa
torium fortunei ), Natsubodaiju ( Tilia platyphyl)
los ), Fuyudaidai ( Tilia cordata ), and one or more kinds of extracts of Tilia europaea are used as tyrosinase biosynthesis inhibitors. These extracts had no adverse effects on the skin such as skin irritation and contact sensitization, and when incorporated into a whitening agent, the tyrosinase biosynthesis inhibitory activity was not inactivated and the quality was stable. . Furthermore, it did not affect the stability of the whitening agent itself.

The above-mentioned plant extracts used in the present invention are generally dried or shredded fresh plants.
To 30 parts of an organic solvent such as ethanol, ethyl acetate, acetone, hexane or a mixture of these organic solvents, or a mixture of water and the above organic solvent or 100 parts of water is added, and the mixture is stirred at room temperature for about 1 week. After performing the extraction
It is obtained by filtering and collecting the filtrate. When a volatile solvent such as acetone or hexane is used, the solvent can be distilled off and the residue can be dried. Knotweed ( Polygonum
cuspidatum , Reynoutria japonica Houtt.) with hexane, ethyl acetate or water extract, and with Artemisea capillaris , ethyl acetate or acetone extract showed particularly high activity.

In the present invention, the amount of the tyrosinase biosynthesis inhibitor comprising the above plant extract added to the whitening agent is 0.0.
01 to 20% by weight is suitable. If the blending amount is 0.001% by weight or less, a sufficient whitening effect cannot be obtained, but since the whitening effect is quite strong, it is not necessary to blend a too large amount, and if it exceeds 20% by weight, the stability of the whitening agent, etc. Can also affect.

In the present invention, the above-mentioned tyrosinase biosynthesis inhibitor may be blended to provide a whitening agent. The whitening agent may be in the form of lotion, emulsion, cream, ointment or the like. Furthermore, softening lotion, astringent lotion, lotion such as cleaning lotion, emollient cream, moisturizing cream, massage cream, cleansing cream, cream such as makeup cream, emollient emulsion, moisturizing emulsion, nourishing It can also be provided as a whitening cosmetic in various formulation forms such as milky lotion, milky lotion such as cleansing milky lotion, packs such as jelly pack, peel-off pack, powdery pack, and face wash.

[0012]

The action of the tyrosinase biosynthesis inhibitor according to the present invention was evaluated. The evaluation was performed as follows.

First, 10 g of each dried plant strip was placed in 100 ml of 50% by weight ethanol and extracted at room temperature for 1 week. This plant extract was diluted 100-fold with purified water to prepare a sample solution. Next, this sample solution
The tyrosinase activity in the cells was measured after the cells were added to a mouse-derived melanoma cell line at a concentration of 00 μg / ml and cultured for 3 days. Culturing was performed from about 50,000 cells.

The tyrosinase activity in cells is 1/15 M
2 ml of phosphate buffer (pH 6.8) was mixed with 0.5 ml of 1.0 wt% dopa aqueous solution and 0.5 ml of culture cell solution, incubated at 37 ° C. for 1 hour to carry out an enzymatic reaction, and then 405 nm It was measured by the absorbance (As) at. As a control, 0.5% by weight instead of the sample solution
Similarly, an enzyme reaction was carried out in a system using a cell solution obtained by culturing by adding ethanol in the same manner, and the absorbance (Ab) in that case was measured. The tyrosinase biosynthesis inhibition rate was calculated by the equation 1.

[Equation 1]

Also, the Japanese knotweed ( Polygonum cuspidatum ,
Reynoutria japonica Houtt.) Was extracted with hexane, ethyl acetate or purified water, and the hexane extract was distilled to remove hexane, and the residue was dissolved in ethanol. The sagebrush ( Artemisea capillaris ) was also extracted with ethyl acetate or acetone, and the acetone extract was distilled off, and the residue was dissolved in ethanol. 100 with purified water
The sample solution was double-diluted, and the tyrosinase biosynthesis inhibition rate was measured by the above method. At this time, 1.0 wt% ethanol was used as a control for the hexane extract, 1.0 wt% ethyl acetate was used for the ethyl acetate extract, and purified water was used as a control for the purified water extract.

The measurement results are shown in Table 1. As is clear from Table 1, all the plant extracts used in the present invention showed a significantly high tyrosinase biosynthesis inhibition rate. Among them, Japanese knotweed ( Polygonum cuspidatum , Reynoutria jap
onica Houtt.) in extracts with hexane, ethyl acetate, purified water, and wormwood ( Artemise).
a capillaris ), the inhibition rate was particularly high in the extracts with ethyl acetate and acetone. Therefore, these plant extracts can suppress the production of melanin from tyrosine and exhibit an effective whitening effect.

[Table 1]

[0017]

EXAMPLES Next, the present invention will be described in more detail by way of examples.

Examples 1 to 4 are whitening creams according to the present invention. The prescription is shown in Table 2. In Table 2, (1) to (7)
Was melted by heating to 75 ° C, and this was heated and melted at 75 ° C (1
Add (0) to (13) to emulsify, cool and (8), (9) at 50 ° C.
Is added and the mixture is further cooled to obtain a whitening cream. At that time, of the plant extract of (9), the hexane extract and the ethyl acetate extract were used after the solvent was distilled off and the residue was dissolved or dispersed in ethanol. Further, Comparative Example 1 was prepared by substituting the plant extract with ascorbic acid, dissolving it in a part of (13) and adding it after emulsification.

[Table 2]

Examples 5 to 7 are whitening emulsion type ointments according to the present invention. The prescription is shown in Table 3. In Table 3, (1)
~ Mix the oil phase components of (4), dissolve and homogenize, heat to 75 ℃, add (5) to (7) and heat to 75 ℃, add to emulsify, and after cooling Add (6) at 50 ℃,
Mix. In this case as well, of the plant extract of (6), the ethyl acetate and acetone extracts were used by distilling off the solvent and dissolving or dispersing in ethanol. In addition, as a comparative example 2, a plant extract was replaced with ascorbic acid and dissolved in a part of (7) and added after emulsification.

[Table 3]

Examples 8 and 9 are whitening emulsions according to the present invention. The prescription is shown in Table 4. In Table 4, (1) to (6) were heated and dissolved at 75 ° C, and then heated and dissolved at 75 ° C (9).
~ (13) is added to emulsify, cool and at 50 ℃ (7), (8)
Is added and further cooled to obtain a whitening emulsion. in this case,
As the plant extract in (8), an ethanol extract was used.
Further, this was replaced with ascorbic acid, dissolved in a part of (13), and added after emulsification, to make Comparative Example 3.

[Table 4]

Example 10 is a whitening lotion according to the present invention. The prescription is shown in Table 5. In Table 5, the components (1) to (12) are mixed and dissolved to homogenize. Also in this case, (6) ~
As the plant extract in (8), an ethanol extract was used.
Further, Comparative Example 4 was prepared by substituting (6) to (8) with 3.0% by weight of ascorbic acid.

[Table 5]

A use test was conducted on the above-mentioned Examples and Comparative Examples to evaluate the whitening effect. The use test was carried out by using 20 female panelists aged 30 to 40 years old who are concerned about stains and freckles as one group, and using each sample of Examples and Comparative Examples in a blind for each group. Every morning and night 2
After washing and washing the face, an appropriate amount of the sample was applied to the face and continued to be used for 2 months. The whitening effect was evaluated by observing the condition of facial spots and freckles after the use test. The results are shown in Table 6.

[Table 6]

In Table 6, in the group using the examples,
In 50% or more of the panelists, clear improvement of spots and freckles was observed, and the remaining panelists also showed an improvement tendency. The effective rate for improving spots and freckles was 100% in all Examples. In particular,
In the use groups of Examples 2 to 4, Example 6, and Example 7 in which the extract having a high tyrosinase biosynthesis inhibition rate was blended, the proportion of panelists in which spots and freckles were obviously improved was high, and in Example 4, Acknowledged a clear improvement for all. On the other hand, in each of the groups used in Comparative Examples, the poor stability of ascorbic acid also had an effect, and an improvement tendency was observed only in 50% of the panelists at best.

Further, no panelists complained of skin irritation such as pain and itch or skin disorder such as allergic reaction in any of the groups used in the above-mentioned use test period. In addition, the quality of the whitening agent such as sedimentation and deterioration of the blended components was not observed.

[0025]

Industrial Applicability As described above, according to the present invention, a tyrosinase biosynthesis inhibitor capable of effectively inhibiting the biosynthesis of tyrosinase can be obtained by adding a small amount thereof, and by adding this, an excellent whitening effect can be obtained. And a whitening agent having good stability and safety.

Claims (5)

[Claims] 1. A knotweed ( Polygonum cuspidatum , Reyn
outria japonica Houtt., Artemisea
capillaris ), Achillea mille
folium ), Fuji Bacama ( Eupatorium fortunei ), Natsubodaiju ( Tilia platyphyllos ), Fuyubodaiju ( Tilia cordata ), Tilia europae
A tyrosinase biosynthesis inhibitor, comprising one or more kinds of the extract of a ). 2. A knotweed ( Polygonum cuspidatum , Reyn
outria japonica Houtt., Artemisea
capillaris ), Achillea mille
folium ), Fuji Bacama ( Eupatorium fortunei ), Natsubodaiju ( Tilia platyphyllos ), Fuyubodaiju ( Tilia cordata ), Tilia europae
A whitening agent comprising one or more kinds of the extract of a ) as a tyrosinase biosynthesis inhibitor. 3. A knotweed ( Polygonum cuspidatum , Reyn
extract of outria japonica Houtt.) with hexane, ethyl acetate, or water, and / or wormwood ( Artemise)
a capillaris ) and an ethyl acetate or acetone extract thereof. 4. A knotweed ( Polygonum cuspidatum , Reyn
extract of outria japonica Houtt.) with hexane, ethyl acetate, or water, and / or wormwood ( Artemise)
a whitening agent, characterized by comprising an ethyl acetate or acetone extract of a capillaris ) as a tyrosinase biosynthesis inhibitor. 5. The whitening agent according to claim 2, wherein the whitening agent is a whitening cosmetic composition.