JPS6410488B2 - - Google Patents

Description

[Detailed description of the invention]

<Industrial Application Field> This invention is a novel skin whitening cosmetic, especially one that contains as an active ingredient a substance that has the effect of suppressing tyrosinase activity, which is extracted from a type of mushroom "Keroji", and has extremely low irritation. Regarding cosmetics. <Prior Art and Background of the Invention> It is believed that the pigment melanin is deeply involved in the darkening of the skin. That is, it is thought that melanin proliferates in the skin tissue of the skin in response to external stimuli such as ultraviolet rays, which promotes the darkening of the skin and causes symptoms such as age spots, freckles, and dark skin. There are several mechanisms of action for skin whitening, and one proposed mechanism is to inhibit the activation of tyrosinase (enzyme) involved in melanin production. Conventionally, glutathione has been considered to be effective as a known substance capable of suppressing the activity of tyrosinase. However, when the cosmetics containing this glutathione are moist, the glutathione is easily oxidized and easily causes discoloration and odor, which poses a fatal problem especially for the cosmetics. Also,
Mulberry bark, peony, dangki, yellow spirit, river kiyu, large sow,
It is known that there are substances that have a tyrosinase activity inhibiting effect in various herbal medicines (natural products) such as raw Kyoto and Yellow Gon. In addition, it has been reported that there are substances in herbal medicines (natural products), especially in fungi such as Poria cocos and Auricularia auricula, that have the effect of suppressing tyrosinase activity (Fragrance Journal Vol. 13, p. 26- 29
<1975>). In addition to the above-mentioned herbal medicines, there are also certain types of mushrooms, namely Agaricus mushrooms.
bisporus) extract (Special Publication No. 59-48804),
Extract of shiitake mushroom (Lentinus edodes) [Shufu no Tomo Seikatsu Series “Health Foods and Health Laws” p29,
It has been reported that each of these products contains substances that have a skin-whitening effect. All of the known tyrosinase activity inhibitors present in these natural products have the advantage of being less irritating;
On the other hand, there is a problem that the inhibition rate of tyrosinase activity is low. Therefore, it is desired to discover and develop a substance that exists in natural products, has a high inhibition rate of tyrosinase activity, and has chemical stability and preservability suitable for cosmetics. <Problems to be Solved by the Invention> In order to solve the above-mentioned problems and meet the above-mentioned demands, the present invention aims to search for and develop substances that are less irritating and have the effect of inhibiting tyrosinase activity. When we searched for substances that inhibit tyrosinase activity in foods and measured the inhibition rate, we found that the fungus belongs to a ``genus'' that is taxonomically completely different from the various fungi found in the above-mentioned literature and reports. Sarcodon scabrosus (Fr.), a type of fungus belonging to the family Sarcodonaceae.
It was completed based on the discovery of a new substance that has an excellent inhibitory effect on tyrosinase activity in an extract extracted from Karst. with an organic solvent, glycol, and/or water alone or in combination. An object of the present invention is to provide a whitening cosmetic that is highly stable, less irritating, and has an excellent tyrosinase activity inhibiting effect. <Means for solving the problems> In order to achieve the above object, the present invention has the following features:
Sarcodon scabrosus (Fr.) Karst.
One or more extracts selected from extracts extracted from fruiting bodies (mushrooms) using organic solvents, glycol, and/or water are used as active ingredients. To explain in more detail how to prepare the active ingredient from Sarcodon scabrosus, the raw material is Sarcodon scabrosus (Fr.
Use the living fruiting body (mushroom) of Karst.) or the dried fruiting body (mushroom). The above-mentioned Keroji is a type of basidiomycete that belongs to the family Ibotake of the order Hydanasitake, and is also known as Inushitake, Inustake, Inutake, Karajishi, and Mustard mushroom,
Forms non-toxic fruiting bodies (mushrooms) containing bitter substances. Kerouji is not considered edible because it contains the bitter components mentioned above. It is also considered to be a formidable enemy of Matsutake because it shares the same habitat with Matsutake and once established, it does not disappear easily. Therefore, this invention also opens up a way to effectively utilize Keroji, which has hitherto been underutilized. As the solvent for extracting the novel active ingredient having the effect of inhibiting tyrosinase activity from Quercus chinensis, various organic solvents, glycols, and water can be used as single solutions or/and mixtures thereof. Examples of the organic solvents used for extracting a new substance having the effect of suppressing tyrosinase activity from Keroji include methanol, ethanol, propanol, isopropyl alcohol, n-butanol,
In addition to lower and/or higher straight chain and/or side chain monohydric alcohols having 1 to 22 carbon atoms such as lauryl alcohol, cetanol, stearyl alcohol, oleyl alcohol, and behenyl alcohol, acetone, ethyl methyl ketone,
Various ketones such as isopropyl methyl ketone,
Various esters such as ethyl acetate and ethyl esters of fatty acids, halogenated alkanes (mainly chlorides) such as dichloromethane, chloroform, and dichloroethane, various ethers such as diethyl ether and ethyl cellosolve, and aromatic hydrocarbons such as benzene and toluene. etc., various polar organic solvents and/or various non-polar organic solvents can be used. Further, the above organic solvents can be used alone, or a mixture of them in an appropriate blending ratio can be used. Moreover, it is of course possible to appropriately utilize a material obtained by heating and melting or a material obtained by mixing and melting two or more kinds of solvents, etc., as necessary. Among the organic solvents mentioned above, the alcohols include methanol, ethanol, isopropanol, n-
Lower alcohols with 1 to 5 carbon atoms such as butanol; ethers such as diethyl ether; ketones such as acetone, ethyl methyl ketone, and isopropyl methyl ketone; esters such as ethyl acetate; halogenated alkanes such as dichloromethane, chloroform, For aromatic hydrocarbons such as dichloroethane, highly polar to moderately polar organic solvents such as benzene are particularly preferred. In addition, examples of the glycols used in the extraction of new substances having the effect of inhibiting tyrosinase activity from Keroji include various glycols such as polyethylene glycol, propylene glycol, and 1,3-butylene glycol (1,3-BG). Available. In addition, glycerin, diglycerin,
Polyhydric alcohols such as triglycerin can be used. Among the glycols, 1,3-
Butylene glycol is particularly preferred. Furthermore, the new substance contained in Keroji that has the effect of inhibiting tyrosinase activity can be extracted with water. In addition, substances having the effect of suppressing tyrosinase activity can be extracted from Keroji using the various organic solvents, glycols, and water alone.
2 of each of these various organic solvents and glycols
It is also possible to use a mixture of more than one type of organic solvent (for example, benzene/ethyl acetate (4:1 mixture), etc.), or one or more of the above organic solvents and one or more of the above organic solvents. Of course, extraction can be carried out using a mixture with glycol (for example, a 30% 1,3-butylene glycol/water mixture) or a mixture of these organic solvents/glycol/water. For example, add an organic solvent such as dichloromethane (CH ₂ Cl ₂ ) (1 to 20 parts by weight or 1 to 20 parts by volume) to dried (including air-dried) Keroji or fresh Keroji (1 part by weight or 1 volume). After extraction is performed once or twice at room temperature for about 5 to 20 days, solid-liquid separation is performed to obtain an extracted portion (dichloromethane extract in the above example). This extract (part) is stored by distilling off the solvent, if necessary, and diluted to an appropriate concentration if necessary, and then used as a sample for the measurement of the inhibition rate of tyrosinase activity below. In addition, each Keroji extract is obtained in the same manner using a desired organic solvent, glycol, water, etc. Each of the extracts of Amberjack chinensis obtained in this way is used as a sample for measuring the inhibition rate of tyrosinase activity. Each of the above-mentioned extracts (for example, methanol extract, n-butanol extract, dichloromethane extract, ethyl acetate extract, 30% 1,3-butylene glycol (1,3
-BG) aqueous solution extraction section, distilled water extraction section, etc.) are each used to measure the tyrosinase activity inhibition rate. As a result, it was observed that all of the above extracts had a remarkable tyrosinase activity inhibiting effect. The inhibition rate of the tyrosinase activity of each of the extracted sections of Kerouji is measured by the following method. For example, each extracted part of the above Keroji is 30%1,3
- Prepare a test solution by diluting it with an appropriate solvent such as a butylene glycol aqueous solution to an appropriate concentration (e.g., a concentration of approximately 1 to 5%, and within a range where the absorbance at 475 nm shows an appropriate value). . Add L-tyrosine solution (0.3mg/
ml) and 1 ml of McIlvain buffer (McIlvain´s
Add 1ml of Buffer Solution (PH6.8) and
Add 0.9 ml of the diluted Kerouji extract and 30% 1,3-butylene glycol aqueous solution for blank test to each of these test tubes.
Incubate for 10 minutes in a constant temperature water bath at 37°C. Add 0.1 ml of tyrosinase solution (1 mg/ml, pine kilvain buffer) to the above-incubated material.
In addition, after stirring well, each reaction solution was immediately set in a spectrophotometer and the absorbance at 475 nm was measured over time. (The absorbance value at each time is indicated with the subscript o for the value immediately after the addition of the tyrosinase solution, and the subscript x for the value after x minutes of incubation after the addition.) Substitute each absorbance value into the following equation. Calculate the tyrosinase activity inhibition rate. In addition, in calculating the tyrosinase activity inhibition rate of this invention, after adding the reaction solution,
Use the absorbance value after 15 minutes. Tyrosinase activity inhibition rate = (Bx − Bo) − (Ax − Ao
)/(Bx-Bo)×100...Formula Bo: Absorbance value of blank solution after 0 minutes Bx: Absorbance value of blank solution after x minutes Ao: Absorbance value of test solution after 0 minutes Ax: Test solution Absorbance value after x minutes of the above-mentioned absorbance value is measured based on the amount of dobachrome (precursor of melanin) produced. As is clear from the extraction process, each of the above-mentioned extracts extracted from Keroji has excellent compatibility with various organic solvents (polar solvents, non-polar solvents), glycols, water, and the like. In particular, it has excellent solubility, miscibility, and compatibility with various bases and various organic solvents used in cosmetics. In other words, organic solvents commonly used in cosmetics include ethanol, isopropyl alcohol, lauryl alcohol, cetanol, stearyl alcohol, oleyl alcohol, behenyl alcohol, propylene glycol, 1,3-butylene glycol, dipropylene glycol, isopropyl myristate, palmitin. It has excellent solubility in isopropyl acid, various other animal oils, vegetable oils, etc. The above-mentioned extracts extracted from Keroji using various organic solvents, glycols, water, etc. can be mixed with various known cosmetic bases, etc. to make various creams, emulsions, lotions, packs, facial cleansers, etc. It can be widely applied to basic cosmetics, foundations, various makeup materials such as blushers, lipsticks, and white powders, soaps, shampoos, conditioners, perfumes, colognes, and other cosmetics. The various cosmetics may be in the form of solutions, emulsions, ointments, oils, waxes, gels, sol, etc.
It can be applied in various forms such as powder and spray (aerosol). The above-mentioned extracts made using various organic solvents, glycols, and/or water are all non-toxic and irritating to the skin (according to cumulative irritation test, patch test, etc.), are highly stable against heat and light, and are highly stable against heat and light. Stability against various cosmetic bases and various cosmetic additives (e.g., various surfactants, solvents, pigments, fragrances, preservatives, antioxidants, humectants, vitamins, animal and plant extracts, and other various additives) It has the outstanding property of having a high viscosity and can be used in combination with these various cosmetic bases and cosmetic additives. The amounts of each organic solvent extract, glycol extract, and water extract of Kerouji in various cosmetics are not particularly limited, as they can be changed depending on the form of use; in principle, they are effective. Generally, it is 0.01 to 20% by weight, preferably 0.5 to 10% by weight based on the total weight of the cosmetic composition.
It is better to mix them. <Function> The whitening cosmetic composition according to the present invention exhibits an excellent whitening effect due to the tyrosinase activity inhibiting effect of the extract extracted from Kerouji with an organic solvent, glycol, and/or water. <Example> (1) Preparation of Kerouji extract. A living body of Keroji (1 kg) is air-dried at room temperature for about 24 hours to obtain dried Keroji (about 90 to 100 g). Approximately 500 ml of dichloromethane (CH ₂ Cl ₂ ) was added to the dried Keroji (50 g), and the mixture was extracted with occasional stirring at room temperature for 7 days. Extract this dichloromethane by 2
Repeat this several times to separate solid and liquid, collect the liquid layer, obtain a dichloromethane extract (approximately 950 ml), and then evaporate the solvent and store. Similarly, the organic solvents include methanol, n
-butanol, ethyl acetate, glycol
Each extract is obtained from Kerouji using a 30% 1,3-butylene glycol/water mixture and distilled water in addition. The following extracts were obtained from air-dried Keroji.
(It is recognized that 50 to 55% of Keroji is extracted in the distilled water extract (crude extract), and a particularly large amount is extracted compared to other extraction parts.) (a) Methanol extraction part ( b) Dichloromethane extraction part (c) Ethyl acetate extraction part (d) 30% 1,3-butylene glycol/water extraction part (e) Distilled water extraction part (2) Experiment to measure the inhibition rate of tyrosinase activity of each extract of Keroji The tyrosinase activity inhibiting effect of each of the above-obtained extracts (extracts) of Kerouji is measured by the method described above. Each extract contains 30
% 1,3-butylene glycol/water at a specified concentration (for measuring the tyrosinase activity inhibitory effect).
(concentration that shows an appropriate absorbance value at 475 nm)
Dilute to 100% and use for measurement. In order to measure the tyrosinase activity inhibition rate of each extract of Keroji, the absorbance of each was measured after 15 minutes, and the tyrosinase activity inhibition rate (%) of each extract was calculated using the formula described below based on the above formula. Table 1 shows the results of the tyrosinase activity inhibition rate of each extract (product). Incidentally, the tyrosinase activity inhibiting effect of the extracts of the Tsukuritake, Shiitake, Botsuri and Mokum, which have been reported to have a skin-whitening effect among the conventionally known fruiting bodies (mushrooms), has been compared with the Keroji according to the present invention. Table 2 shows a comparison of the measured values when measured under the same conditions. Tyrosinase activity inhibition rate = (B ₁₅ −Bo) − (A ₁₅ −
Ao) / (B ₁₅ - Bo) x 100...Formula Bo: Absorbance value _B of the blank solution after 0 minutes Ao: Absorbance value A of the test solution after 15 minutes ₁₅ : Absorbance value of test solution after 15 minutes

【table】

【table】

[Table] (3) Cumulative irritation test of Kerouji extract. A cumulative irritation test will be conducted on guinea pigs to determine the safety (irritancy) of the Keroji extract. This cumulative irritation test was conducted using one of each of the above extracts of C.
% ethanol solution is repeatedly applied to the skin of 5 male Hartley white guinea pigs weighing approximately 250 to 300 g twice a day, and the condition of the skin of each guinea pig is observed 6 days later. Table 3 shows the cumulative irritation test results for each extract of Kerouji.

[Table] (4) Cosmetic cream <composition> (wt%) ● Kerouji extract ………5.0 ● Beeswax ………2.0 ● Stearyl alcohol ………5.0 ● Stearic acid ………8.0 ● Squalane ………10.0 ●Self-emulsifying glyceryl monostearate
………3.0 ●Polyoxyethylene cetyl ether (20E.
O) ………1.0 ●Propylene glycol ………5.0 ●Potassium hydroxide ………0.3 ●Fragrance ………appropriate amount ●Preservatives/antioxidants ………appropriate amount ●Purified water ………Remaining amount (5) Emulsion <Composition> (Weight %) ● Kerouji extract ………5.0 ● Squalane ………8.0 ● Vaseline ………2.0 ● Beeswax ………0.5 ● Sorbitan sesquioleate ………0.8 ● Polyoxyethylene oleyl ether (20E .
O) ………1.2 ● Carboxyvinyl polymer ………0.2 ● Propylene glycol ………5.0 ● Potassium hydroxide ………0.1 ● Ethanol ………7.0 ● Fragrance ………appropriate amount ● Preservative/antioxidant … ...Appropriate amount ●Purified water ...Remaining portion (6) Lotion <Composition> (Weight%) ● Kerouji extract ......5.0 ● Glycerin ......5.0 ● Polyoxyethylene sorbitan monolaurate (20E.O) ... ……1.5 ● Ethanol ………10.0 ● Fragrance ………appropriate amount ● Preservatives/antioxidants ………appropriate amount ● Statutory pigments ………appropriate amount ● Purified water ……… Remainder (7) Packaging agent <Composition> ( (weight%) ●Keroji extract......5.0 ●Vinyl acetate resin emulsion......15.0 ●Polyvinyl alcohol......10.0 ●Olive oil...3.0 ●Glycerin...5.0 ●Titanium oxide......8.0 ●Kaolin... …7.0 ● Ethanol ………5.0 ● Fragrance ………appropriate amount ● Preservatives/antioxidants ………appropriate amount ● Purified water ……… Remainder <Effect of the invention>Keroji's organic solvent, glycols, or/
The excellent tyrosinase activity inhibiting effect of the water-based extract makes it possible to create an excellent whitening cosmetic with high stability and safety.

Claims (1)

[Claims] 1 Sarcodon scabrosus (Fr.)
It is characterized by containing as an active ingredient one or more extracts selected from the extracts extracted from the fruiting bodies (mushrooms) of Karst. with an organic solvent, glycol, and/or water. Whitening cosmetics.