JPH11302149A - Melanin production inhibitor and external preparation for skin containing the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a melanogenesis inhibitor by including a specific essence. SOLUTION: This external preparation for skin such as a skin lightening cosmetic or the like contains preferably 0.01-10 wt.% of a melanogenesis inhibitor composed of an essence of Illicium verum Hook fil.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a melanin production inhibitor useful for a skin external preparation such as a whitening cosmetic.

[0002]

2. Description of the Related Art Beautiful fair skin has been desired by all people since ancient times, and various efforts have been made to obtain such skin. In this, it was revealed that the cause of the whiteness of the color, in other words, the blackness of the color, was melanin generated in melanocytes. It was also clarified that depending on the amount of the melanin, the skin color became black or white. It is already known that proteins called tyrosinase and tyrosinase-related proteins are involved in the biosynthesis of melanin. In addition, materials and cosmetics for realizing fair skin by inhibiting the action of such enzymes and the like have been developed, and it has become possible to make the color white to a considerable extent. However, there remain factors that cannot be explained from the relationship between dark-black and melanin biosynthesis.Also, it is not surprising that the factors involved in melanin biosynthesis differ depending on the type of dark-black. It has become known. However, it has already been well known that even if a melanin production inhibitor is considered to have a relatively high effect, some people do not exhibit the effect. The reason for this is thought to be that there are many factors involved in melanin production, and that these differences may cause the melanin production inhibitor to exert no effect. It cannot be said that such factors and the mechanism of melanin production have been elucidated. Therefore, it has to be said that there is a need to find various kinds of novel melanin production inhibitors.

[0003] On the other hand, the fennel is a plant belonging to the family Lyricaceae and has the scientific name I. verum Hook file. It is widely known, and is also known as Star Anise, Octagon Fenka or Octagon, and is used in spices such as Chinese cuisine.The essence of this essence is derived from alcohol, especially ethanol, which is derived from alcohol. It is already known that it has an action to relieve irritation, and that the hot water extract has a moisturizing action and is suitable as a component of bath agents, but it has a melanin production inhibitory action. It was not known at all that the effect contained in the components contained in the non-polar part of the polar solvent extract of the fruit part was remarkable.
Further, it has not been known at all that the whitening cosmetic contains such an essence.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made under such circumstances, and an object of the present invention is to provide a novel melanin production inhibitor.

[0005]

In view of such circumstances, the present inventors have conducted intensive studies in search of a novel melanin production inhibitor, and as a result, have found such characteristics in the essence of fennel, thereby completing the invention. Reached. Hereinafter, the present invention will be described in detail focusing on embodiments of the present invention.

(1) Melanin production inhibitor of the present invention The melanin production inhibitor of the present invention comprises the essence of Fennel. Here, the essence referred to in the present invention is:
Processed product obtained by drying, shredding, pulverizing, etc. of the whole or part of the plant, extract of the whole or part of the plant or the processed product extracted with a solvent, solvent-extracted extract, plant A generic term for distillates obtained by distilling all or part of the body or their processed products directly or in the presence of steam, and fractionated products obtained by fractionating distillates and extracts by liquid-liquid extraction, column chromatography, etc. I do. Among them, extracts are water, alcohols such as methanol, ethanol and 1,3-butanediol, ethers such as diethyl ether and tetrahydrofuran, halogenated hydrocarbons such as chloroform and methylene chloride, and ketones such as acetone and methyl ethyl ketone. And one or more selected from esters such as ethyl acetate and methyl formate.
Of these, alcohols are particularly preferred from the viewpoint of safety and solubility. Extraction is performed on the plant or its processed product by 1
The solvent may be immersed for several days at room temperature or several hours at a temperature near the boiling point. Among these essences, particularly preferred as the melanin production inhibitor of the present invention are extracts, and among them, alcohol extracts are preferred. It is particularly preferable that the polar portion is removed from the alcohol extract by liquid-liquid extraction or the like. Liquid-liquid extraction as a means for removing such a polar portion is performed, for example, by adding a hydrocarbon such as normal hexane to the extract extracted with methanol or the like without removing the solvent, shaking to remove the hydrocarbon layer, and removing the solvent. Preferable examples include distilling off, concentrating the alcohol extract once, dissolving by adding ethyl acetate and water, shaking to remove the ethyl acetate layer, and concentrating. Fruit is particularly preferred as a site for preparing such an extract. These are preferable because such an essence contains a component having an excellent action of suppressing melanin production. The preferred content of the melanin production inhibitor in the skin external preparation of the present invention is 0.01 to 10% by weight.
And more preferably 0.05 to 5% by weight.

(2) External preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing the above-mentioned melanin production inhibitor. As the external preparation for skin of the present invention, for example, a pharmaceutical composition for external use on skin and cosmetics can be preferably exemplified. Among them, internal cosmetics are preferable, and cosmetics for whitening are particularly preferable. This is because the effect of the melanin production inhibitor, which is an essential component of the present invention, can be realized better. The cosmetic of the present invention can contain optional components usually used in cosmetics and external preparations for the skin, in addition to the above-mentioned melanin production inhibitor as an essential component. Such optional components include, for example, hydrocarbons such as petrolatum and microcrystalline wax, esters such as jojoba oil and gay wax, tallow, triglycerides such as olive oil, cetanol, and higher alcohols such as oleyl alcohol.
Fatty acids such as stearic acid and oleic acid, polyhydric alcohols such as glycerin and 1,3-butanediol, nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants, ethanol, carbopol, etc. Preferred examples include thickeners, preservatives, ultraviolet absorbers, antioxidants, pigments, and powders. Above all, whitening components such as vitamin C and its derivatives, hydroquinone glycosides such as arbutin, and resorcinol and its derivatives can be contained. The external preparation for skin of the present invention can be produced by treating these components according to a conventional method. The external preparation for skin of the present invention can take any dosage form such as a liquid preparation, an emulsion cream preparation, an emulsion preparation, a mousse preparation, an ointment preparation and the like. Since the base plant of the melanin production inhibitor used in the present invention has been widely used in foods since ancient times, the melanin production inhibitor and the skin external preparation of the present invention have excellent safety. Needless to say.

[0008]

The present invention will be described in more detail with reference to the following examples, but it goes without saying that the present invention is not limited only to these examples.

<Example 1> Production Example Daikyo (I. verum Hook fi)
l. ) Was immersed in 5 l of methanol at room temperature for 7 days, filtered to remove insoluble portions, and concentrated to obtain essence 1 (melanin production inhibitor 1). One liter of methylene chloride and water were added thereto, and the mixture was shaken to remove the methylene chloride layer and concentrated to obtain essence 2 (melanin production inhibitor 2).

<Example 2> Preparation Example 500 g of the fruit portion of the Fennel is immersed in 5 l of methanol at room temperature for 7 days, and the insoluble portion is removed by filtration. The extract was concentrated and used as essence 3 (melanin production inhibitor 3).

<Example 3> Melanin production inhibitory action The above essences 1 to 3 were examined for melanin production inhibitory action using mouse melanoma B-16 F1 cells. That is, RPMI-1 with 10% FBS in a plastic culture flask (25 cm ² )
2 × 10 ⁵ mouse melanoma B-16 in 640 medium
F1 cells were inoculated and cultured at 37 ° C. in a stream of 5% carbon dioxide gas. 24 hours after sowing, the final concentration was 1 × ¹⁰⁻³ (W /
V) The above melanin production inhibitor is DMS
After dissolving in O, the cells were further cultured for 2 days. At this time, D
Care was taken that the MSO did not exceed 0.2% at the final concentration. After cultivation, remove the medium, wash with phosphate-buffered saline, and trypsinize to detach the cells.Collect the cells by centrifugation. Judged. The criterion is that the cytotoxicity is significantly less than ++: no sample added (control),
+: Apparently lower than control, ±: slightly lower than control, −: comparable to control, melanin production inhibitory effect ++: significantly whiter than control, +: higher than control It was apparently white, ±: slightly white compared to the control, −: black as much as the control. Table 1 shows the results. This indicates that the melanin production inhibitor of the present invention is excellent in melanin production inhibitory action despite low cytotoxicity.

[0012]

[Table 1]

Example 4 A cosmetic of the present invention was prepared according to the following formulation. That is, the ingredients were stirred and dissolved at room temperature to obtain a lotion as the cosmetic of the present invention. Melanin production inhibitor 1 1 part by weight Polyoxyethylene (60) hydrogenated castor oil 0.5 part by weight Ethanol 10 parts by weight Glycerin 5 parts by weight Water 83.5 parts by weight

Example 5 A cosmetic of the present invention was prepared according to the following formulation. That is, the ingredients were stirred and dissolved at room temperature to obtain a lotion as the cosmetic of the present invention. Melanin production inhibitor 2 0.1 parts by weight Polyoxyethylene (60) hydrogenated castor oil 0.5 parts by weight Ethanol 10 parts by weight Glycerin 5 parts by weight Water 84.4 parts by weight

Example 6 A cream according to the present invention was prepared according to the following formulation. That is, after well kneading the components of (a), the mixture is heated to 80 ° C., and (b) and (c) are preheated to 80 ° C., (b) is added and diluted, (c) is gradually added, emulsified, and stirred. Upon cooling, a cream was obtained. I Triglycerin diisostearate 5 parts by weight Maltitol 70% aqueous solution 5 parts by weight Glycerin 3 parts by weight 1,3-butanediol 5 parts by weight Melanin production inhibitor 2 0.7 parts by weight Methyl paraben 0.2 parts by weight Butyl paraben 0 Liquid paraffin 15 parts by weight Microcrystalline wax 3 parts by weight Neopentyl glycol diisooctaneate 5 parts by weight Carnauba wax 2 parts by weight C Water 56 parts by weight

Example 7 A cream according to the present invention was prepared according to the following formulation. That is, after well kneading the components of (a), the mixture is heated to 80 ° C., and (b) and (c) are preheated to 80 ° C., (b) is added and diluted, (c) is gradually added, emulsified, and stirred. Upon cooling, a cream was obtained. I Triglycerin diisostearate 5 parts by weight Maltitol 70% aqueous solution 5 parts by weight Glycerin 3 parts by weight 1,3-butanediol 5 parts by weight Melanin production inhibitor 3 0.7 parts by weight Methyl paraben 0.2 parts by weight Butyl paraben 0 Liquid paraffin 15 parts by weight Microcrystalline wax 3 parts by weight Neopentyl glycol diisooctaneate 5 parts by weight Carnauba wax 2 parts by weight C Water 56 parts by weight

Example 8 Using the lotion of Example 5, an actual use test was performed to confirm the whitening effect. That is, Comparative Example 1 in which the melanin production inhibitor 2 of Example 5 and the melanin production inhibitor 2 of Example 5 were replaced with vitamin C sodium salt using 10 panelists in a group suffering from black and white and 4 groups in total of 40 persons. The four groups of Comparative Example 2 in which the melanin production inhibitor 2 of Example 5 was replaced with arbutin, and the control example in which the melanin production inhibitor 2 of Example 5 was replaced with water were used in the morning and evening 2 days a day. Times, 2
Having been used for months in a row, the impression of improvement in color and black was ++: excellent improvement, +: obvious improvement, ±: slightly improvement,-:
We asked them to answer the questionnaire according to their rank without improvement. The results are shown in Table 2 as the number of occurrences. This indicates that the cosmetic of the present invention has an excellent whitening effect.

[0018]

[Table 2]

[0019]

According to the present invention, a novel melanin production inhibitor can be provided.

Claims (7)

[Claims] 1. A melanin production inhibitor comprising the essence of Daikyo (Daen Feng). 2. The melanin production inhibitor according to claim 1, wherein the essence is a polar solvent extract of a fruit portion. 3. The method according to claim 1, wherein the essence is a non-polar part of a polar solvent extract of the fruit part.
5. The melanin production inhibitor according to the above. 4. An external preparation for skin, comprising the melanin production inhibitor according to any one of claims 1 to 3. 5. The external preparation for skin according to claim 4, which is a whitening cosmetic. 6. A cosmetic composition comprising a non-polar portion of a polar solvent extract of a fruit portion of a fennel. 7. The cosmetic according to claim 6, which has a whitening effect.