JP2002154920A - Elongation inhibitor of dendrite of melanocyte and cosmetic comprising the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To solve problems in providing an effective prophylactic or an ameliorating means for dyschromia accompanied by inflammations or dyschromia such as ephelides. SOLUTION: This cosmetic is obtained by including an essence of a ripe dried seed, preferably a fruit of Prunus armeniaca L. var. ansu axim. of the family Rosaceae having excellent inhibitory actions on elongation of dendrites of melanocytes in a skin care preparation such as the cosmetic.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a melanocyte dendrite elongation inhibitor and an external preparation for skin such as cosmetics, and more particularly to a melanocyte dendrite elongation inhibitor which is suitable as a whitening cosmetic. Suitable for suppressing the interaction of
The present invention relates to a skin external preparation for treating skin phenomena involving melanocytes and macrophages.

[0002]

2. Description of the Related Art It is already known that melanocytes play a major role in the vital phenomena related to pigments in animals. However, melanin, which is a pigment, is produced in melanocytes, and how It is not yet known in detail whether the cells move to cells, and it is only known that such movement of melanin granules often involves macrophages. It has been pointed out that the involvement of such macrophages is achieved by producing a dendritic elongation factor (DEF) of melanocytes. Suppressing dendrite elongation of melanocytes,
No attempt has been made to suppress the movement of melanin granules and to prevent the skin from being darkened by suppressing the elongation of the dendrite. In addition, Rosaceae (Kyonin)
unus armeniaca L. var.ansu axim.
It is not known at all that the essence of E. has an action to suppress the elongation of melanocytes.

[0003] On the other hand, the solution of the pigment abnormality caused by the abnormality of melanin granules produced by melanocytes is a long-standing problem for human beings to realize beautiful white skin. Have been obtained, and various mechanisms have been obtained.However, none of them focused on the suppression of dendritic elongation of melanocytes. Therefore, it is not known at all that it is useful for prevention or improvement of pigment inflammation accompanied by inflammation. In addition, the effects of conventionally well-known melanin production inhibitors such as ascorbic acid on pigment abnormalities such as inflammation-related pigment abnormalities and freckles are not yet effective, and the prevention or amelioration of such pigment abnormalities is not sufficient. Development was desired.

[0004] Furthermore, the essence of the dried mature seeds of Rosaceae gyonin (Prunus armeniaca L. var. Ansuaxim.) Has a pneumoconiosis effect and an intestinal bowel effect. Is already known, but it is not known at all that it has an action to suppress the dendritic elongation of melanocytes, and therefore, external preparations for skin such as cosmetics containing this Inhibits the dendritic elongation of melanocytes, and is therefore not known to be useful for the prevention and improvement of pigment abnormalities associated with pigment abnormalities, particularly, light and associated with inflammation.

[0005]

DISCLOSURE OF THE INVENTION The present invention has been made under such circumstances, and is particularly suitable for skin whitening, which is particularly effective against pigment abnormalities accompanied by inflammation and pigment abnormalities such as freckles. It is an object of the present invention to provide a skin external preparation suitable as a preventive or ameliorating means.

[0006]

In view of such circumstances, the present inventors have conducted intensive studies in search of effective preventive or ameliorating means for pigment abnormalities accompanied by inflammation and pigment abnormalities such as freckles. As a result, Rosaceae (Kyonin)
us armeniaca L. var.ansu axim.), which has an excellent essence of melanosite dendrite elongation inhibitory action, and contains a substance having such an action in an external preparation for skin. The agent was found to be useful for the prevention and improvement of pigment abnormalities such as inflammation and freckles such as freckles, and completed the invention. That is, the present invention relates to the following technology. (1) Rose family (Rosaceae) Kyounin (Prunus arm)
eniaca L. var. ansu axim., a melanocyte elongation inhibitor, comprising the essence of mature seed dried product). (2) The melanocyte dendrite elongation inhibitor according to (1), wherein the essence is an extract of the fruit with a polar solvent. (3) The melanocyte elongation inhibitor according to (1) or (2), wherein suppression of dendrite elongation is caused by an inhibitory action of a dendritic elongation promoting factor derived from macrophages. (4) A skin external preparation for treating skin phenomena involving melanocytes and macrophages, comprising the melanocyte elongation inhibitor according to any one of (1) to (3). (5) A skin preparation for treating skin phenomena involving melanocytes and macrophages according to (4), which is a cosmetic. (6) Skin phenomena involving melanocytes and macrophages cause inflammation due to light. A skin external preparation for skin phenomena involving melanocytes and macrophages according to (4) or (5), which is associated with skin blackening or freckles (7) Rosaceae : Prunus arm
An essence of eniaca L. var. ansu axim. (dried mature seed), a whitening cosmetic. (8) Rose family (Rosaceae) Kyounin (Prunus arm)
eniaca L. var.ansu axim.) is characterized in that the extract is a polar solvent extract of fruit.
The cosmetic for whitening according to (7). (9) whitening action is characterized by a mechanism of dendrite elongation suppression action in melanocytes as a mechanism,
The cosmetic for whitening according to (7) or (8). Hereinafter, the present invention will be described in detail focusing on embodiments.

[0007]

DETAILED DESCRIPTION OF THE INVENTION (1) The melanocyte dendrite elongation inhibitor of the present invention The melanocyte dendrite elongation inhibitor of the present invention is:
Rose family (Rosaceae) Kyounin (Prunus armeniaca)
An essence of L. var. Ansu axim. Yamakyo is the base plant of Chinese medicine. The substance that suppresses dendrite elongation of the present invention is also included in both of them. Therefore, any of these plants can be used as the essence of the present invention. Here, the essence refers to the plant itself of such a plant, a processed product obtained by drying, shredding, or pulverizing the plant, an extract obtained by extracting the plant or the processed product with a solvent, and a solvent of the extract. Removed,
It is a general term for a solvent-removed product, an extract or a purified fraction obtained by purifying the solvent-removed product by column chromatography or liquid-liquid extraction. Among them, as the melanocyte dendrite elongation inhibitor of the present invention, a rhizome solvent extract or a solvent removal product thereof can be preferably exemplified, and as such a solvent, a polar solvent can be particularly preferably exemplified. Examples of such a polar solvent include water, alcohols such as ethanol, methanol, 1,3-butanediol and propylene glycol, esters such as ethyl acetate and methyl formate, ketones such as acetone and methyl ethyl ketone, chloroform and the like. One or more selected from halogenated hydrocarbons such as methylene chloride, nitriles such as acetonitrile, and ethers such as diethyl ether and tetrahydrofuran can be preferably exemplified. Of these, water and / or alcohols are particularly preferred. In order to prepare such an extract, a 1 to 10-fold amount of a solvent is added to a plant or a processed product thereof, and immersed for several days at room temperature or several hours at a temperature near the boiling point. Thereafter, insolubles are removed by filtration or the like, and if necessary, the solvent can be removed by concentration under reduced pressure or freeze-drying. Rose family (Rosaceae) Kyounin (Prunus armeniaca)
L. var. Ansu axim. (Mature seed dried product) is thoroughly dried, extracted with methanol, and then filtered, concentrated under reduced pressure, and optionally freeze-dried. This is because the fruit portion contains a large amount of a melanocyte dendrite elongation inhibitory component, which is particularly preferable. The thus obtained melanocyte dendrite elongation inhibitor of the present invention, Rosaceae (Rosaceae)
Kyounin (Yamazu: Prunus armeniaca L. var. Ansu ax
The essence of dried mature seeds of im.) is excellent in the effect of suppressing the elongation of melanocytes to dendrites, and thus suppresses the transfer of melanin granules from melanocytes to skin tissues. It has the effect of preventing or improving pigmentation abnormalities such as inflammation-induced blackening and freckles caused by light irradiation, which is caused by movement as a mechanism. It is considered that such an action has a mechanism of inhibiting the action of a dendritic elongation factor of melanocytes released by macrophages on melanocytes. Of course, since the pigment abnormality takes such a route in the production of melanin granules, the melanocyte dendritic elongation inhibitor of the present invention also suppresses pigmentation abnormalities other than blackening and freckles accompanied by inflammation by light irradiation. Since such pigment abnormalities can be prevented or improved by other means, the feature of the effect of the present invention is to prevent or improve the pigment abnormalities such as inflammation-induced blackening and freckles that occur upon irradiation with light. It can be said that it works. Further, since such an essence contains a substance having an inhibitory effect on tyrosinase activity and melanin production, it can be contained in a whitening cosmetic for the purpose of such an effect. Since such an action works synergistically or additively with the dendrite elongation inhibitory action of the present invention, it is also possible to incorporate these essences into a cosmetic to produce a whitening cosmetic. Belongs to.

(2) A skin external preparation for treating skin phenomena involving melanocytes and macrophages of the present invention The melanocyte dendrite elongation inhibitor of the present invention acts on a melanocyte dendrite elongation factor acting on melanocytes released by macrophages. Since the mechanism is to inhibit, it is possible to suppress the life phenomenon in which melanocytes and macrophages work cooperatively, and by including such a melanocyte dendritic elongation inhibitor in a skin external preparation, melanocytes and It can respond to skin phenomena involving macrophages. That is, the external preparation for skin of the present invention is for treating skin phenomena involving melanocytes and macrophages, and contains the melanocyte dendrite elongation inhibitor of the present invention. Here, the external preparation for skin referred to in the present invention is a generic name of a composition applied externally to the skin, and a skin external medicine including a patch and a cosmetic including a cleansing agent can be preferably exemplified. Then, it is particularly preferred that the composition is a cosmetic. This is because the melanocyte dendrite elongation inhibitor of the present invention has high safety and moderate action. As skin phenomena involving melanocytes and macrophages, particularly preferably, pigmentation abnormalities such as blackening and freckles accompanied by inflammation by light irradiation are mentioned as the most important issues, but other inflammatory reactions are also included. . The preferred content of the melanocyte dendrite elongation inhibitor in the skin external preparation for treating skin phenomena involving melanocytes and macrophages of the present invention is 0.001% by weight to 10% by weight based on the total amount of the skin external preparation. And more preferably 0.01 to 5% by weight.
This is because if the amount is too small, the effect of suppressing dendrite elongation may not be exhibited, and if the amount is too large, the effect may reach a plateau and the degree of freedom of other formulation components may be impaired.

The topical skin preparation of the present invention for treating skin phenomena involving melanocytes and macrophages can be combined with prednisolone, hydrocortisone, indomethacin, diclofenac sodium, etc., which are known as anti-inflammatory agents, to reduce inflammation due to sunlight due to a synergistic effect. Significant for accompanying melanosis. Further, in addition to the above essential components, any components commonly used in cosmetics or external medicine for skin can be contained. Such optional components include, for example, squalane,
Hydrocarbons such as petrolatum and microcrystalline wax, jojoba oil, carnauba wax, esters such as octyldodecyl oleate, triglycerides such as olive oil, tallow, coconut oil, stearic acid, oleic acid,
Fatty acids such as ritinoleic acid, higher alcohols such as oleyl alcohol, stearyl alcohol, and octyl dodecanol; anionic surfactants such as sulfosuccinates and sodium polyoxyethylene alkyl sulfate; amphoteric surfactants such as alkyl betaine salts; dialkyl Cationic surfactants such as ammonium salts, sorbitan fatty acid esters, fatty acid monoglycerides, their polyoxyethylene adducts, polyoxyethylene alkyl ethers, nonionic surfactants such as polyoxyethylene fatty acid esters, polyethylene glycol, glycerin, It can contain polyhydric alcohols such as 1,3-butanediol, thickening / gelling agents, antioxidants, ultraviolet absorbers, coloring agents, preservatives, powders, and the like. Of course, the addition of hydroquinones such as ascorbic acids and arbutin, which are conventional melanin production inhibitors, may also exert a synergistic effect, which is advantageous.

[0010]

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 to these examples.

<Example 1> 5 l of methanol was added to 500 g of Rosaceae ginseng (dried mature seed of Prunus armeniaca L. var. Ansu axim.) And stirred at 90 ° C. for 2 hours while stirring. After heating at room temperature, the mixture was cooled to room temperature, filtered to remove insolubles, and further concentrated under reduced pressure.
Then, it was freeze-dried. And, the melanocyte dendrite elongation inhibitor of the present invention, Rosaceae (Kyonin) (Prunus armeniaca L. var. Ansu axim.
(Matured seed dried product) was obtained.

Example 2 The dendrite elongation inhibitory effect of the melanocyte dendrite elongation inhibitor of Example 1 was examined. That is, macrophages were recovered from the peritoneal cavity of the mouse according to a conventional method, diluted with the minimum medium of Eagle supplemented with 10% FBS, and a macrophage solution having a concentration of 2 × 10 6 cells / ml was prepared. 90μ
Dispense into 35 mm Petri dishes at a rate of 0.05 mW
/ Cm 2 for 20 minutes. Rosaceae (Ros
aceae) Kyonin (Prunus armeniaca L. var. a)
nsu axim. mature seed dried product) essence of dry weight%
Dissolve in DMSO to 0.005% and add 37
C. overnight. On the other hand, the tail of the mouse was cut off, the epidermis of the tail was finely chopped, put in a petri dish, treated with 0.5% trypsin at 37 ° C. overnight, separated into epidermis and dermis using forceps, and only the epidermis was collected. And 0.5% trypsin at 37 ° C. for 20 minutes, and only melanocytes were collected as a filtrate by filtration. The filtrate containing the melanocytes was added to a medium obtained by adding 10% FBS, 10 @ -4 M IBMX and 10 ng / ml TPA to Eagle's minimal medium.
The cells were cultured at 37 ° C. for 48 hours. This is suspended in the same medium,
Dispense 1000 cells / well into 96 wells, 37
Cultured overnight at ℃. Discard the melanocyte culture medium and add PBS
After washing three times with, the medium was replaced with 35 μl of a minimum medium of Eagle supplemented with 10% FBS. To this, 35 μl of the culture supernatant of the macrophage containing the specimen was added, and the mixture was cultured at 37 ° C. for two nights, a photograph was taken under an optical microscope, and the length of the dendrite was measured from this photograph. Table 1 shows the results. Thus, the melanocyte dendrite elongation inhibitor of the present invention, Rosaceae gyonin (Prunus armen)
It can be seen that the essence of iaca L. var. ansu axim. (Specimen) 1) Rosaceae, a melanocyte dendrite elongation inhibitor, kyonin (Prunus armeniaca L.)
var. ansu axim. mature seed dried product) essence DM
SO solution (0.005%) 2) DMSO (positive control) 3) No macrophage supernatant is added (negative control)

[0013]

[Table 1]

Example 3 A lotion was prepared according to the following formulation. That is, the ingredients were stirred and solubilized at room temperature to obtain a lotion. Using this lotion, three panelists in one group suffering from spots and freckles were used twice a day for 1 month in the morning and evening to evaluate the preventive and ameliorating effects of the spots and freckles. The evaluation criteria were as follows: score 2: marked improvement, score 1:
Obvious improvement, rating 0.5: slight improvement, rating 0: no improvement. The average score was 0.89. The rose family (Rosaceae) of the melanocyte of the present invention, which has the effect of suppressing dendrite elongation, is known as "Prunus armeniaca".
The lotion containing the essence of L. var. Ansu axim. (Dried mature seed) was found to be effective in improving spots and freckles. Almond essence of Example 1 1 part by weight 1,3 butanediol 5 parts by weight Glycerin 3 parts by weight Sodium citrate 0.1 part by weight Methylparaben 0.2 parts by weight Ethanol 8 parts by weight Water 82.7 parts by weight

Example 4 A pharmaceutical composition for external use on the skin was prepared according to the following formulation. That is, the prescription components were stirred and dispersed to obtain a skin external preparation. This was remarkably effective against light-induced skin blackening or freckles accompanied by light-induced inflammation. Almond essence of Example 1 0.5 parts by weight Prednisolone 1 part by weight Vaseline 85 parts by weight

Example 5 A cream was prepared according to the following recipe. That is, (a), (b) and (c) were each heated and dissolved at 80 ° C., (b) was gradually added to (a), and (c) was further added and emulsified. The homogenized particles were homogenized by a homomixer and cooled to obtain a cream. This cream had an excellent effect on preventing and improving freckles with inflammation. B) Squalane 10 parts by weight Cetanol 3 parts by weight Sorbitan sesquistearate 2 parts by weight Polyoxyethylene (20) behenyl ether 2 parts by weight Vitamin A acid 1 part by weight b) 1,3-butanediol 5 parts by weight Essence of 1 part by weight Carboxyvinyl polymer 0.3 part by weight Water 40 parts by weight c) Water 37.3 parts by weight Potassium hydroxide 0.2 parts by weight

Example 6 A pharmaceutical composition for external use on the skin was prepared according to the following formulation. That is, the prescription components were stirred and dispersed to obtain a skin external preparation. This was remarkably effective against light-induced skin blackening or freckles accompanied by light-induced inflammation. Example 2 apricot kernel essence 0.5 parts by weight Prednisolone 1 part by weight Vaseline 85 parts by weight

[0018]

According to the present invention, it is possible to provide an effective preventive or ameliorating means for pigment abnormality accompanied by inflammation and pigment abnormality such as freckles.

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Claims (9)

[Claims] (1) Rosaceae (Kyonin)
unus armeniaca L.var.ansu axim.
A melanocyte elongation inhibitor consisting of the essence of 2. The melanocyte dendrite elongation inhibitor according to claim 1, wherein the essence is an extract of a dried mature seed with a polar solvent. 3. The melanocyte elongation inhibitor according to claim 1, wherein the dendrite elongation inhibition is caused by an inhibitory effect of a dendritic elongation promoting factor derived from macrophages. 4. A skin external preparation for treating skin phenomena involving melanocytes and macrophages, comprising the melanocyte elongation inhibitor according to any one of claims 1 to 3. 5. The external preparation for skin according to claim 4, which is a cosmetic, for treating skin phenomena involving melanocytes and macrophages. 6. The skin phenomenon involving melanocytes and macrophages according to claim 4 or 5, wherein the skin phenomenon involving melanocytes and macrophages is a skin blackening phenomenon or freckles accompanied by inflammation due to light. External preparation for skin. 7. Rosaceae Kyounin (Yamazu: Pr
unus armeniaca L.var.ansu axim.
A whitening cosmetic containing the essence of 8. Rosaceae Kyonin (Yama-Kyo: Pr
The whitening cosmetic according to claim 7, wherein the essence of unus armeniaca L.var. ansu axim). is a polar solvent extract of dried mature seeds. 9. The whitening cosmetic according to claim 7, wherein the whitening effect is based on a dendrite elongation inhibiting effect in melanocytes.