JP3431383B2 - Melanin inhibitor - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a melanin inhibitor which causes pigmentation such as spots and freckles, and more particularly to a duck with water, a hydrophilic organic solvent or this
The present invention relates to a melanin inhibitor containing, as an active ingredient, an extract of ducks obtained by performing an extraction treatment with these mixtures . [0002] Blots, freckles, liver spots and pigmentation after sunburn are less likely to occur, increase or disappear with age, and are one of the concerns for middle-aged and older people.
Although the mechanism of the onset of these pigmentation diseases has not been elucidated yet, it is considered that the melanocyte synthesizing function of melanocytes was enhanced by the action of ultraviolet rays, melanocyte stimulating hormone (MSH) and the like. In addition, the tendency of keratinocytes (keratinocytes) to delay keratinization with aging also delays the rate of excretion of melanin to the outside of the epidermis and increases the density of melanin granules in the epidermis together with the enhancement of melanin synthesis. Is believed to be something. Furthermore, since these pigmented areas are present locally and have a clear difference from the surrounding normal skin color, the pigmentation site is locally enhanced in melanin synthesizing function or the result of modulation of the mechanism controlling melanin synthesis. It is considered. Conventionally, studies have been conducted to restore these acquired pigments, that is, melanin deposits, to a normal skin color, and many proposals have been reported so far. [0003] For example, a hot water or ethanol extract of the stem, leaf or root of Ashitaba is mixed with a cosmetic base,
Fair-skin cosmetics having a melanin-suppressing action (JP-A-60-2
No. 09509), which contains an extract of oguruma and / or its congener, prevents and alleviates skin inflammation, and also has an effect of preventing and improving skin blackening due to sunburn, spots and freckles. External preparation for skin
JP-A-3-303919), and a cosmetic composition containing an extractive component from the fruiting body of Reishi, which has a melanin production inhibitory action and a melanin lightening action (Japanese Unexamined Patent Publication No.
124809) and the like have been proposed. [0004] However, the inhibitory effects of these melanin inhibitors are not always satisfactory, and there is a strong demand for the development of melanin inhibitors having even better effects. [0005] For Therefore SUMMARY OF THE INVENTION The present inventors to solve the above problems, safety, high stability, melanin inhibitors having a function having excellent melanin suppression effect, the function especially As a result of diligent research on extracts of various plants having sorghum , duck (MYRCIARIA DUBIA)
Extract with water, a hydrophilic organic solvent or a mixture of these.
Extract of Kamoka model obtained by Rukoto is to possess a function of inhibiting the formation of melanin, whitening effect, and more moisturizing effect, it found that it is also effective in anti-aging skin, leading to the present invention . Camo duck is an edible plant belonging to the family Myrtaceae and is a shrub that grows on the banks of the Amazon basin or the shores of flowing lakes in the eastern part of Peru to the northwestern part of Brazil. It is known that the amount of the active ingredient is increased, and that the mineral content is high and other active ingredients are included in a large amount. In the field, the fruit is used as it is for eating, or the fruit juice is squeezed for drinking as juice. The ducks are fruits of the family Myrtaceae as described above, and in the present invention, any of raw, semi-dried, and dried products can be used, and these raw materials are preferably ground and used. [0007] That is, the present invention provides a duck with water and hydrophilic water.
Extraction with a neutral organic solvent or a mixture of these
The gist of the present invention is a melanin inhibitor containing as an active ingredient the resulting extract of ducks. BEST MODE FOR CARRYING OUT THE INVENTION
It can be easily obtained by performing an extraction treatment with a hydrophilic organic solvent or a mixture thereof. Examples of the hydrophilic organic solvent used in the extraction treatment include solvents such as methanol, ethanol, n-propyl alcohol, acetone, propylene glycol, and glycerin. These solvents can be used, for example, in the form of a hydrated solvent mixed with water in an arbitrary ratio, but it is preferable to perform extraction with about 10 to about 99.9% of a hydrated solvent. The extraction operation and the extraction conditions can be variously changed according to the type of extraction solvent used. However, when the extraction is carried out using a hydrophilic organic solvent as described above or a mixed solution thereof with water as described above. For example, about 1.5 times to about 50 times the amount of a solvent is added to duck and the mixture is allowed to stand or stirred at room temperature to the boiling point of the solvent used for about 5 minutes to about 24 hours. After performing the extraction operation in this manner, a duck extract can be obtained by removing insoluble residues by, for example, centrifugation, filtration, squeezing, or other solid-liquid separation means. If necessary, an extraction solvent can be added to the insoluble extraction residue, and the same operation can be repeated to perform the extraction. Furthermore, at the time of the extraction operation, by adding an enzyme such as pectinase and performing the enzyme treatment, the extraction efficiency can be increased. In the present invention, the extract obtained from the duck by the above method may be used as it is as the extract of the present invention, or a concentrate obtained by removing the solvent from the extract, The dried product obtained by drying it under reduced pressure or freeze-drying can also be used as the extract of the present invention. Further, the extract obtained by the above method may be decolorized and deodorized with an adsorbent such as silica gel, activated carbon, activated alumina, bentonite, acid clay, and diatomaceous earth. The adsorption operation can be performed by adding an appropriate amount of an adsorbent to a solution of the extract as it is or a concentrate obtained by dissolving the extract in a suitable solvent such as water. As the adsorption treatment liquid, a concentrated liquid obtained as it is or by concentrating it under reduced pressure, and a dried product obtained by drying it under reduced pressure or freeze-drying can be used as an extract. Further, the extract before or after the above decolorization and deodorization treatment is dissolved in, for example, an appropriate amount of water, and is effectively treated with a synthetic adsorbent made of a resin such as styrene vinyl benzene or methacrylic acid ester. Absorb components
Then, for example, ethanol, methanol, acetone, purified by performing a desorption operation with a hydrophilic organic solvent such as ethyl acetate or a mixed solvent of these and water, and concentrating the active ingredient in the extract of duck, the present invention It can also be used as an extract. The adsorption and desorption operations can be performed in a batch mode or a continuous mode using a column, and a continuous mode using a column is preferably employed. The desorbed solution after this operation can be used as it is as the extract of the present invention, and it is also a concentrated solution obtained by concentrating under reduced pressure, and further, for example, a dried product obtained by drying under reduced pressure or freeze-drying Can also be used as the extract of the present invention. [0013] The extract of ducks prepared as described above has excellent melanin-suppressing ability. The melanin inhibitor of the present invention can be made into various forms by adding other optional components. In general, for example, lotion, emulsion, cream, ointment, stick, organic It is preferable to use a solvent-based solution, pack, gel, or the like. In addition, as other optional components that can be blended in addition to the duck extract, components commonly blended and used in cosmetics, for example, purified water, ethanol,
Oily substances, humectants, whitening agents, thickeners, preservatives, emulsifiers,
Examples include medicinal ingredients, powders, ultraviolet absorbers, dyes, fragrances, emulsion stabilizers, pH adjusters, and the like. Examples of the humectant include, for example, γ-linoleic acid, sphingolipid, xanthan gum, hyaluronic acid, bovine bone marrow extract, water-soluble collagen, chitin, chitosan, mucin, lactic acid bacteria culture solution, bifidobacterium metabolite, yeast fermentation metabolite , Yeast extract, pyrrolidonecarboxylic acid, pullulan, maltose, loofah extract; Examples of whitening agents include placenta extract, kojic acid, mulberry bark, toki extract, waremokou, ivukitorano, vitamin C and derivatives thereof. When the extract of the duck of the present invention is used in combination, the whitening effect, the moisturizing effect, and the effect of preventing skin aging can be enhanced. The melanin inhibitor of the present invention thus obtained is applied topically to affected areas such as skin spots, freckles, and pigmented areas after sunburn. In general, the amount of use is not particularly limited, but it is usually used in the range of about 0.5 to 10 mg per 1 cm ² of the skin surface in the case of a cream or ointment, and about 1 to 15 mg in the case of a liquid preparation. . The embodiments of the present invention will be described in more detail with reference to the following examples. Example (Preparation of duck duck extract sample) 50 g of duck duck
Then, 400 g of a 50% aqueous ethanol solution was added thereto, and an extraction treatment was carried out for 3 days with occasional stirring, followed by centrifugation and filtration to obtain 350 g of a filtrate. The filtrate was concentrated to dryness under reduced pressure to obtain 45 g of a dry extract. This extract is measured for its ability to suppress melanin production, that is, its ability to inhibit tyrosinase activity. (Measurement of tyrosinase activity inhibiting ability) An enzyme solution (25,000 units manufactured by Wako Pure Chemical Industries, Ltd.) was added to 0.4 mg of the above extract sample.
Tyrosinase was dissolved in 20 ml of 0.1 M phosphate buffer (pH 7.0)), 0.1 ml was added, and 0.1 M phosphate buffer (pH 7.0) was further added to make 4 ml. For 10 minutes. To this was added 1.0 ml of a substrate solution (198.0 mg of L-DOPA (manufactured by Tokyo Chemical Industry Co., Ltd.) dissolved in 100 ml of 0.1 M phosphate buffer (pH 7.0)) previously kept at 25 ° C. Allowed to react for minutes. Then, the absorbance at 475 nm was measured, and this was measured as OD _C , and further, the absorbance OD _D of the same reaction using the enzyme inactivated by heating, the absorbance when water was added instead of the sample as OD _A , Add the water in place of the sample and use the inactivated enzyme to measure the absorbance at OD.
These were measured as _B , and the tyrosinase activity inhibition rate was determined by the following equation. Tyrosinase activity inhibition rate (%) = [｛OD _A -OD _B- (OD _C -O
_{D D)} / (OD A} -OD B)] × 100 = 82. 6 (%) However, OD _A :( water + enzyme + substrate) absorbance OD _B :( water + inactivation enzyme + substrate) absorbance of the OD _C : absorbance of (sample + enzyme + substrate) OD _D : absorbance of (sample + inactivated enzyme + substrate) From this result, it can be seen that the extract of duckling has an excellent melanin production inhibitory function. According to the present invention, a melanin inhibitor having an excellent ability to inhibit tyrosinase activity, which effectively suppresses melanin production, can be provided.

──────────────────────────────────────────────────続 き Continuation of the front page (51) Int.Cl. ⁷ Identification symbol FI A61P 43/00 101 A61P 43/00 101 (56) References JP-A-2-200610 (JP, A) JP-A-51-142514 (JP, A) Sci, FOOd, Agric, 1993, Vol. 61, pp. 349-351 (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 35/78 A61K 7/00 BIOSIS (DIALOG) CA (STN) MEDLINE (STN)

Claims (1)

(57) [Claims] [Claim 1] A duck is added to water, a hydrophilic organic solvent or
A melanin inhibitor comprising, as an active ingredient, an extract of ducks obtained by performing an extraction treatment with these mixtures .