JP2011016727A - Melanogenesis inhibitor - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a melanogenesis inhibitor comprising a new component as an active ingredient.SOLUTION: The melanogenesis inhibitor comprises Euterpe oleracea and/or its extract, cherry flower and/or its extract and a rice-derived protein and/or peptide as active ingredients.

Description

  The present invention relates to a melanin production inhibitor.

  The cause of spots and freckles is caused by the deposition of melanin pigment in the skin. Causes of stains include changes in hormone balance, rough skin, ultraviolet rays, aging, etc., but all involve ultraviolet rays. When exposed to ultraviolet rays, keratinocytes, which occupy most of the epidermis from the epidermal cells that have been exposed to ultraviolet rays, are sent to melanocytes by signaling substances (endolysene and phospholipase), and tyrosine acts as a tyrosinase. So it becomes dopa and then dopaquinone. Oxidation reaction proceeds from dopaquinone, and melanin is formed through dopachrome, 5 • 6-dihydroxyindole or 5 • 6-dihydroxyindole-2-carboxylic acid and indole5 • 6-quinone. This series of actions is due to the body's natural action to protect the skin by blackening the skin with melanin so that harmful UV rays do not enter the skin, but the skin tissue usually has a 28-day cycle. Therefore, if this metabolism is carried out smoothly, this melanin pigment is also discharged out together with the old cells in a few months. However, as the age increases, the metabolism of the skin decreases, so that the melanin pigment is easily deposited on the skin without being discharged outside. In order to prevent this, various whitening cosmetics and health foods are used.

  Conventionally, drugs such as placenta extract, vitamin C and its derivatives, ellagic acid, and arbutin have been used for prevention and improvement of stains, freckles, etc., but sufficient effects are not always obtained. In Europe and the United States, hydroquinone is used for the purpose of depigmenting pigment spots, but its use is restricted due to safety problems.

  In addition, for example, Wenzhou mandarin orange extract and β-cryptoxanthin contained therein are known to have an inhibitory effect on tyrosinase activity (Patent Document 1).

JP 2006-089452 A

  Under such background, the present inventor found that B16 melanoma cells have an inhibitory action on melanin production in acai and its extract, cherry blossom and its extract, and rice-derived protein or rice-derived peptide. Completed the invention.

That is, an object of the present invention is to provide melanin production suppression using a novel component as an active ingredient.

The features of the present invention for solving the above-described problems are as follows.
1. A melanin production inhibitor containing acai and / or an extract thereof as an active ingredient.
2. Melanin production inhibitor as an active ingredient of cherry blossoms and / or extracts thereof.
3. A melanin production inhibitor containing rice-derived protein and / or peptide as an active ingredient.

Hereinafter, the present invention will be described in detail.
The present invention is characterized by containing acai and / or an extract thereof as an active ingredient.

Acai (Acai, Japanese name: Wakaba cabbage palm, scientific name: Euterpe oleracea) is a palm family plant native to the Brazilian Amazon. The fruit looks like blueberries and is edible.
In the present invention, the site of acai is not particularly limited. For example, fruits, seeds, leaves and the like can be used, but fruits (including seeds) are preferably used. Furthermore, it is preferable to use fruit puree.

Although the method of obtaining the extract from the said acai is not specifically limited, For example, polar solvent extraction, supercritical extraction, etc. are mentioned. Only one of these may be performed, or both of them may be performed. Moreover, this extraction may be performed only once each method, or may be performed twice or more.

Here, when extracting by polar solvent extraction, the polar solvent to be used is not particularly limited. For example, water, methanol, ethanol, isopropanol, acetone, 1,3-butylene glycol, ethylene glycol, propylene glycol, glycerin, acetic acid, Examples include ethyl acetate, ether, hexane and the like. Of these, water, methanol, and ethanol are preferred. It is because an active ingredient can be extracted efficiently. These may be used alone or in combination of two or more.

When water is used as the extraction solvent, the extraction temperature is 20 to 100 ° C, preferably about 40 to 70 ° C. This is because if the extraction temperature is too low, it is difficult to extract active ingredients. The kind of water for extraction is not particularly limited, and tap water, distilled water, mineral water, alkaline ionized water and the like can be used.

When hydrous alcohol is used as the extraction solvent, the alcohol concentration is preferably 30 wt% or more, and preferably 50 wt% or more. It is because it is difficult to obtain a high extraction amount of an active ingredient when it is less than 30 wt%. The extraction temperature is 0 to 95 ° C, preferably about 20 to 80 ° C. In addition, the water-containing ethanol extraction may be repeated at various concentrations in order to improve the content of the active ingredient.

  In addition, when extracting with a polar solvent, the extraction method is not particularly limited, and for example, any method such as continuous extraction, immersion extraction, countercurrent extraction, etc. can be adopted, and any apparatus at room temperature or under reflux heating. Can be used. In addition, when extracting by the method mentioned above, only one of these may be performed and these methods may be combined. These extractions may be performed only once or may be performed twice or more.

As a specific method, an extraction raw material (a puree excluding acai fruits or seeds) is put into a treatment tank filled with an extraction solvent, and an active ingredient is eluted while stirring. For example, when water or a hydrous alcohol is used as the extraction solvent, the extraction is performed for about 1 minute to 150 hours using a polar solvent of about 5 to 100 times (weight ratio) of the extraction raw material. The active ingredient is eluted in the solvent, and then filtered to remove the extraction residue to obtain an extract. Thereafter, the extract is subjected to treatments such as dilution, concentration, drying and purification according to a conventional method to obtain an extract containing high concentrations of anthocyanins and polyphenols.
Examples of the purification method include activated carbon treatment, resin adsorption treatment, ion exchange resin, liquid-liquid countercurrent distribution, and membrane separation.

  Furthermore, when performing extraction by supercritical extraction, the supercritical fluid used at this time is not particularly limited, and examples thereof include carbon dioxide and nitrogen. In addition, these may use only 1 type and may use 2 or more types together. Of these, carbon dioxide is particularly preferred. It is because an active ingredient can be extracted more easily. The extraction method at this time may be performed by a known method. Thereafter, the extract is subjected to treatments such as dilution, concentration, drying and purification according to a conventional method to obtain an extract containing a high concentration of polyphenol or anthocyanin.

In addition, the melanin production inhibitor of the present invention is characterized by containing a cherry blossom and / or an extract thereof as an active ingredient.
Sakura (cherry blossoms, buds) is a generic name of plants belonging to the family Rosaceae, excluding plums, peaches, apricots, etc., and generally refers to those belonging to the subgenus Subgen. Cerasus.

Cherry seeds used in the present invention are not particularly limited, and for example, cherry trees belonging to groups such as Yamazakura group, Edhigan group, Bean cherry group, Chojizakura group, Miyazakura group, Shinamizakura group can be used, and further limited to these groups Not.
The method for producing the cherry extract can be performed in the same manner as the method for producing the acai extract.

Furthermore, the melanin production inhibitor of the present invention comprises rice-derived protein and / or peptide as an active ingredient. This rice-derived protein can be extracted by a known method.
This rice-derived peptide can be obtained by extracting rice-derived protein by a known method and treating the rice-derived protein with a proteolytic enzyme.

  The present invention provides a food containing the melanin production inhibitor. This food may contain the extract as an active ingredient in an amount of 100 to 1,000 mg, preferably 250 to 500 mg, for example, per adult dose. In the melanin production inhibitor of the present invention, the content of the active ingredient may vary depending on age and the like.

  The melanin production inhibitor of this invention can be used as a raw material of various food-drinks. Examples of the food and drink include edible oil (salad oil), confectionery (gum, candy, caramel, chocolate, cookie, snack, jelly, gummy, tablet confection etc.), noodles (soba, udon, ramen etc.), and dairy products ( Milk, ice cream, yogurt, etc.), boiled simmered (boiled kelp, boiled sea bream, small fish simmered, etc.), seasonings (miso, soy sauce, etc.), soups, beverages (juice, coffee, tea, tea, carbonated drinks, sports General foods such as beverages), health foods (tablets, capsules, etc.), and nutritional supplements (nutrient drinks, etc.). The melanin production inhibitor of the present invention may be appropriately blended with these foods and drinks.

  These foods and drinks can be blended with various ingredients depending on the type, for example, glucose, fructose, sucrose, maltose, sorbitol, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, succinic acid. Acid, lactic acid, L-ascorbic acid, dl-α-tocopherol, sodium erythorbate, glycerin, propylene glycol, glycerin fatty acid ester, polyglycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, propylene glycol fatty acid ester, gum arabic, Food materials such as carrageenan, casein, gelatin, pectin, agar, vitamin Bs, nicotinic acid amide, calcium pantothenate, amino acids, calcium salts, pigments, fragrances and preservatives can be used. In addition, this melanin production inhibitor with health maintenance functions includes other antioxidants and health food ingredients such as antioxidants, reduced ascorbic acid (vitamin C), vitamin E, and reduced forms. Glutatin, tocotrienol, vitamin A derivative, lycopene, β-cryptoxanthin, astaxanthin, zeaxanthin, fucoxanthin, uric acid, ubiquinone, coenzyme Q10, folic acid, garlic extract, allicin, sezamin, lignans, catechins, isoflavones, chalcones, tannins, Flavonoids, coumarins, isocoumarins, blueberry extract, arbutin, tannin, anthocyanin, apple polyphenol, grape seed extract, ellagic acid, kojic acid, surge extract health food material, V. (vitamin) A, V.B1, V. B2, V.B6, V.B12, VC, VD, VE , VP, choline, niacin, pantothenic acid, calcium folate, EPA, oligosaccharide, dietary fiber, squalene, soy lecithin, taurine, donariella, protein, octacosanol, DHA, egg yolk lecithin, linoleic acid, lactoferrin, magnesium, zinc, chromium, Selenium, potassium, heme iron, oyster meat extract, chitosan, chitin oligosaccharide, collagen, chondroitin, turmeric, licorice, kukoshi, keihi, hawthorn, ginger, ganoderma, swordfish extract, suppon, plantain, chamomile, chamomile, dandelion, hibiscus , Honey, Boren, Royal Jelly, Lime, Lavender, Rosehip, Rosemary, Sage, Bifidobacterium, Facaris, Lacris, Wheat Germ Oil, Sesame Oil, Perilla Oil, Soybean Oil, Medium Chain Fatty Acid, Agaricus, Ichi Wu leaf extract, turmeric, chondroitin, brown rice germ extract, litchi, onion, DHA, EPA, DPA, green tea, cordyceps, garlic, bee, papaya, puer, propolis, megsuri tree, yabushitake, royal jelly, saw palmetto, hyaluron Acid, Collagen, Gabba, Harpseal Oil, Shark Cartilage, Glucosamine, Lecithin, Phosphatidylserine, Tabuchi Carrot, Mulberry Leaf, Soybean Extract, Echinacea, Ezoukogi, Barley Extract, Olive Leaf, Olive Seed, Gymnema, Banaba, Salacia , Garcinia, Chitosan, St. John's wort, jujube, carrot, passion flower, broccoli, placenta, pearl barley, grape seed, peanut seed coat, bilberry, black cohosh, maria thistle, laurel, sage, rosemary, rafma Black vinegar, bitter gourd, maca, safflower, flax, oolong tea, flower spine, caffeine, capsaicin, xylo-oligosaccharide, glucosamine, buckwheat, citrus, dietary fiber, protein, prunes, spirulina, barley young leaves, nucleic acid, yeast, shiitake mushroom, plum meat , Amino acids, deep sea bream extract, noni, oyster meat, suppon, champignon, plantain, acerola, pineapple, banana, peach, apricot, melon, strawberry, raspberry, orange, fucoidan, mesimacob, cranberry, chondroitin sulfate, zinc, iron, Ceramide, Silk Peptide, Glycine, Niacin, Chest Tree, Ceramide, L-Cysteine, L-Carnitine, Red Wine Leaf, Millet, Horsetail, Biotin, Centella Asiatica, Lotus Cup, Pycnogenol, Fuqui, Rhubarb, Clove, Rosemary Catechin, Puaru, Citric acid, Beer yeast, Merirot, Black zinger, Ginger, Gadju, Nattokinase, Benikouji, Tocotrienol, Lactoferrin, Cinnamon, Buckwheat, Cocoa, Yuzu seed extract, Perilla seed extract, Lychee seed extract, Evening primrose extract, Black rice extract, α-lipoic acid, GABA, fresh coffee bean extract, Japanese bursa extract, kiwi seed extract, Unshu mandarin orange extract, red ginger extract, astaxanthin, walnut extract, kanka extract, white jellyfish polysaccharide, lingonberry extract, fucoxanthin, resveratrol , Strawberry seed extract) and the like can also be blended.

As a specific production method, the melanin production inhibitor of the present invention is used as it is, and in the case of an extract, it is spray-dried or freeze-dried together with powdered dextrin, and this is easily converted into a powder, granule, tablet or solution. Instant foods). If necessary, it can also be mixed with a binder such as gum arabic to form a powder or granules, and added to a solid food. In the case of an extract, it can also be added to a beverage as it is or after being dispersed and dissolved in water, ethanol, glycerin or a mixture thereof.

The melanin production inhibitor of the present invention may be used as a raw material for medicines (including pharmaceuticals and quasi drugs). It can be produced by appropriately blending the melanin production inhibitor of the present invention with a raw material for a pharmaceutical preparation. In addition, the said chemical | medical agent may be used for a human and may be used for mammals other than a human. Examples of the raw material for preparation that can be blended in the melanin production inhibitor of the present invention include excipients (glucose, lactose, sucrose, sodium chloride, starch, calcium carbonate, kaolin, crystalline cellulose, cocoa butter, hydrogenated vegetable oil, kaolin, talc. Etc.), binder (distilled water, physiological saline, ethanol water, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.), disintegrant (sodium alginate, agar, hydrogen carbonate) Sodium, calcium carbonate, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, gum arabic powder, gelatin, ethanol, etc.), disintegration inhibitors (sucrose, stearin, cocoa butter, hydrogenated oil, etc.), absorption enhancers (fourth) Quaternary ammonium base, sodium lauryl sulfate Etc.), adsorbents (glycerin, starch, lactose, kaolin, bentonite, silicic acid, etc.), lubricants (purified talc, stearates, polyethylene glycol, and the like) and the like.

The administration method of the melanin production inhibitor according to the present invention can be generally administered orally in the form of tablets, pills, soft / hard capsules, fine granules, powders, granules and the like. The water-soluble preparation can be administered orally as a liquid. Furthermore, parenteral administration may be used. When administered as a parenteral agent, the melanin production inhibitor of the present invention is dispersed in an appropriate solubilizing agent such as ethanol or water, and then a dosage form such as a poultice, lotion, ointment, tincture or cream. Can be applied. In addition, the water-soluble preparation of the present melanin production inhibitor can be used as it is or in the form of a poultice, lotion, ointment, tincture, cream, etc. with a dispersant, suspension, stabilizer, etc. added. Can be applied.

The dose may vary depending on the administration method, medical condition, age of the patient, etc., but for adults, it can be generally administered in an amount of about 5 to 200 mg as an active ingredient per day and usually about 0.5 to 100 mg for children.

The compounding ratio when the melanin production inhibitor of the present invention is used as a drug can be appropriately changed depending on the dosage form, but is usually about 0.0001 to 30 wt% when administered orally or by mucosal absorption. In the case of parenteral administration, it may be about 0.0001-30 wt%. In addition, since the dose varies depending on various conditions, a dose smaller than the above dose may be sufficient, or it may be necessary to administer beyond the range. In addition to the melanogenesis inhibitor, the pharmaceutical composition may include other known compounds commonly used in the pharmaceutical field and compounds necessary for molding into a form suitable for oral administration. Examples of such compounds include lactose, starch, hydroxypropyl cellulose, kaolin, talc, calcium carbonate and the like.

Even when the melanin production inhibitor of the present invention is used as a skin external preparation (including cosmetics, pharmaceuticals and quasi drugs), it can be expected to have a melanin production inhibitory action.
Examples of the form of the external preparation for skin to which the melanin production inhibitor of the present invention can be formulated include, for example, emulsion, soap, facial cleanser, bath preparation, cream, emulsion, lotion, eau de cologne, shaving cream, shaving lotion, Cosmetic oil, suntan / sunscreen lotion, powder, foundation, perfume, pack, nail cream, enamel, enamel remover, eyebrow, blusher, eye cream, eye shadow, mascara, eyeliner, lipstick, lip balm, shampoo, rinse , Hair dyes, dispersions, cleaning agents and the like. Examples of the form of a pharmaceutical or quasi-drug that can contain the melanin production inhibitor of the present invention include ointments, creams, and liquids for external use.

In addition to the melanin production inhibitor according to the present invention, the external preparation for skin of the above form includes ingredients, oils, and high-grade ingredients blended in skin external preparations such as cosmetics and quasi-drugs as long as the melanin production inhibitory action is not impaired. Alcohols, fatty acids, ultraviolet absorbers, powders, pigments, surfactants, polyhydric alcohols / sugars, polymers, physiologically active ingredients, solvents, antioxidants, fragrances, preservatives, and the like can be blended.
Examples are listed below, but the present invention is not limited to these examples.

(1) Examples of oil components Ester-based oil phase components: glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate, butyl myristate, isopropyl palmitate, ethyl stearate, octyl palmitate, isostearic acid Isocetyl, butyl stearate, butyl myristate, ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl myristate, isostearyl myristate, isostearyl palmitate, octyldodecyl myristate, isocetyl isostearate, diethyl sebacate, adipine Diisopropyl acid, isoaralkyl neopentanoate, glyceryl tri (capryl / caprate), trimethylolpropane tri-2-ethylhexanoate, trimethylol triisostearate Propane, pentaerythritol tetra-2-ethylhexanoate, cetyl caprylate, decyl laurate, hexyl laurate, decyl myristate, myristyl myristate, cetyl myristate, stearyl stearate, decyl oleate, cetyl ricinoleate, isolaurate Stearyl, isotridecyl myristate, isocetyl myristate, isostearyl myristate, isocetyl palmitate, isostearyl palmitate, octyl stearate, isocetyl stearate, isodecyl oleate, octyldodecyl linoleate, octyldodecyl isoleate, isopropyl isostearate Cetostearyl 2-ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate, ethyleneglycol dioctanoate , Ethylene glycol dioleate, propylene glycol dicaprate, propylene glycol di (capryl / capric acid), propylene glycol dicaprylate, neopentyl glycol dicaprate, neopentyl glycol dioctanoate, glyceryl tricaprylate, glyceryl triundecylate, triisopalmitine Glyceryl acid, glyceryl triisostearate, octyldodecyl neopentanoate, isostearyl octanoate, octyl isononanoate, hexyl decyl neodecanoate, octyldodecyl neodecanoate, isocetyl isostearate, isostearyl isostearate, octyldecyl isostearate, polyglycerin oleic acid Ester, polyglycerol isostearate, dipropyl carbonate, charcoal Dialkyl (C12-18), triisocetyl citrate, triisoaralkyl citrate, triisooctyl citrate, lauryl lactate, myristyl lactate, cetyl lactate, octyl decyl lactate, triethyl citrate, acetyl triethyl citrate, acetyl tributyl citrate, Trioctyl citrate, diisostearyl malate, 2-ethylhexyl hydroxystearate, di-2-ethylhexyl succinate, diisobutyl adipate, diisopropyl sebacate, dioctyl sebacate, cholesteryl stearate, cholesteryl isostearate, cholesteryl hydroxystearate, olein Cholesteryl acid, dihydrocholesteryl oleate, phytosteryl isostearate, phytosteryl oleate, 12-stearoyl hydroxystearate Cetyl, 12-stearoyl-hydroxystearic acid stearyl 12-stearoyl-hydroxystearic acid isostearate, and the like.
Hydrocarbon oil phase components: squalane, liquid paraffin, α-olefin oligomer, isoparaffin, ceresin, paraffin, liquid isoparaffin, polybutene, microcrystalline wax, petrolatum and the like.
Animal and vegetable oils and their hydrogenated oils, and naturally occurring waxes: beef tallow, hydrogenated beef tallow, lard, hydrogenated tallow, horse oil, hydrogenated horse oil, mink oil, orange luffy oil, fish oil, hydrogenated fish oil, egg yolk oil and other animal oils and Its hardened oil, avocado oil, almond oil, olive oil, cacao butter, kiwi seed oil, apricot oil, kukui nut oil, sesame oil, wheat germ oil, rice germ oil, rice bran oil, safflower oil, shea butter, soybean oil, evening primrose oil , Perilla oil, tea seed oil, camellia oil, corn oil, rapeseed oil, hydrogenated rapeseed oil, palm kernel oil, hydrogenated palm kernel oil, palm oil, hydrogenated palm oil, peanut oil, hydrogenated peanut oil, castor oil, hydrogenated castor oil , Vegetable oils such as sunflower oil, grape seed oil, jojoba oil, hardened jojoba oil, macadamia nut oil, medhome oil, cottonseed oil, hardened cottonseed oil, coconut oil, hardened coconut oil and its hardened , Beeswax, high acid value beeswax, lanolin, reduced lanolin, hydrogenated lanolin, liquid lanolin, carnauba wax and montan wax.
Silicone oil phase components: dimethylpolysiloxane, methylphenylpolysiloxane, methylcyclopolysiloxane, octamethylpolysiloxane, decamethylpolysiloxane, dodecamethylcyclosiloxane, methylhydrogenpolysiloxane, polyether-modified organopolysiloxane, dimethyl Siloxane / methylcetyloxysiloxane copolymer, dimethylsiloxane / methylstearoxysiloxane copolymer, alkyl-modified organopolysiloxane, terminal-modified organopolysiloxane, amino-modified silicone oil, amino-modified organopolysiloxane, dimethiconol, silicone gel, acrylic Examples include silicone, trimethylsiloxysilicic acid, and silicone RTV rubber.
Fluorine oil phase components: perfluoropolyether, fluorine-modified organopolysiloxane, fluorinated pitch, fluorocarbon, fluoroalcohol, fluoroalkyl / polyoxyalkylene co-modified organopolysiloxane, and the like.

(2) Examples of higher alcohols include lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, oleyl alcohol, behenyl alcohol, 2-ethylhexanol, hexadecyl alcohol, octyldodecanol and the like.

(3) Examples of fatty acids Caprylic acid, capric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, arachidonic acid, behenic acid , Erucic acid, 2-ethylhexanoic acid and the like.

(4) Examples of UV absorbers Paraaminobenzoic acid, amyl paraaminobenzoate, ethyldihydroxypropyl paraaminobenzoate, glyceryl paraaminobenzoate, ethyl paraaminobenzoate, octyl paraaminobenzoate, octyldimethyl paraaminobenzoate, ethylene glycol salicylate, salicylic acid Octyl, triethanolamine salicylate, phenyl salicylate, butylphenyl salicylate, benzyl salicylate, homomenthyl salicylate, benzyl cinnamate, octyl paramethoxycinnamate, 2-ethylhexyl paramethoxycinnamate, mono-2-diparamethoxycinnamate Glyceryl ethylhexanoate, isopropyl paramethoxycinnamate, diethanolamine salt of paramethoxyhydrocinnamic acid, diisopropyl diisopropylcinnamic acid Stealth mixture, urocanic acid, ethyl urocanate, hydroxymethoxybenzophenone, hydroxymethoxybenzophenone sulfonic acid and its salts, dihydroxymethoxybenzophenone, dihydroxymethoxybenzophenone sodium disulfonate, dihydroxybenzophenone, dihydroxydimethoxybenzophenone, hydroxyoctoxybenzophenone, tetrahydroxybenzophenone, Butylmethoxydibenzoylmethane, 2,4,6-trianilino-p- (carbo-2-ethylhexyl-1-oxy) -1,3,5-triazine, 2- (2-hydroxy-5-methylphenyl) benzotriazole , Methyl-O-aminobenzoate, 2-ethylhexyl-2-cyano-3, 3-diphenyl acrylate, phenylbenzimidazole sulfate, 3- (4-methylbenzylidene) can Le, isopropyl dibenzoylmethane, 4- (3,4-dimethoxyphenyl methylene) 2-ethylhexyl-2,5-dioxo-1-imidazolidin propionate,, and polymer derivatives and silane derivatives thereof.

(5) Examples of powders and pigments Red 104, Red 201, Yellow 4, Blue 1, Black 401 and other dyes, Yellow 4 AL lake, Yellow 203 BA lake and other lake dyes, nylon powder , Silk powder, urethane powder, Teflon (registered trademark) powder, silicone powder, polymethyl methacrylate powder, cellulose powder, starch, silicone elastomer spherical powder, polyethylene powder, yellow iron oxide, red iron oxide, black Colored pigments such as iron oxide, chromium oxide, carbon black, ultramarine and bitumen, white pigments such as zinc oxide, titanium oxide and cerium oxide, extender pigments such as talc, mica, sericite, kaolin and barium sulfate plate, titanium mica Pearl pigments such as barium sulfate, calcium carbonate, magnesium carbonate, aluminum silicate, metal salts such as magnesium silicate, Inorganic powders such as Rica and alumina, metal soaps such as aluminum stearate, magnesium stearate, zinc palmitate, zinc myristate, magnesium myristate, zinc laurate, zinc undecylenate, bentonite, smectite, boron nitride, etc. It is done. There are no particular restrictions on the shape of these powders (spherical, rod-like, needle-like, plate-like, irregular shape, flake-like, spindle-like, etc.) and particle diameter. These powders are conventionally known surface treatments such as fluorine compound treatment, silicone treatment, silicone resin treatment, pendant treatment, silane coupling agent treatment, titanium coupling agent treatment, oil agent treatment, N-acylated lysine treatment, The surface treatment may or may not be performed in advance by polyacrylic acid treatment, metal soap treatment, amino acid treatment, lecithin treatment, inorganic compound treatment, plasma treatment, mechanochemical treatment or the like.

(6) Examples of surfactants Anionic surfactants: fatty acid soap, α-acyl sulfonate, alkyl sulfonate, alkyl allyl sulfonate, alkyl naphthalene sulfonate, alkyl sulfate, POE alkyl ether sulfate , Alkylamide sulfate, alkyl phosphate, POE alkyl phosphate, alkylamide phosphate, alkyloylalkyl taurine salt, N-acyl amino acid salt, POE alkyl ether carboxylate, alkyl sulfosuccinate, alkyl sulfoacetic acid Sodium, acylated hydrolyzed collagen peptide salt, perfluoroalkyl phosphate, etc. are mentioned.
Cationic surfactant: alkyltrimethylammonium chloride, stearyltrimethylammonium chloride, stearyltrimethylammonium bromide, cetostearyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, behenyltrimethylammonium bromide, benzalkonium chloride , Behenic acid amidopropyldimethylhydroxypropylammonium chloride, stearic acid diethylaminoethylamide, stearic acid dimethylaminopropylamide, lanolin derivative quaternary ammonium salts, and the like.
Amphoteric surfactants: carboxybetaine type, amide betaine type, sulfobetaine type, hydroxysulfobetaine type, amide sulfobetaine type, phosphobetaine type, aminocarboxylate type, imidazoline derivative type, amidoamine type and the like.
Nonionic surfactant: propylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, sorbitan fatty acid ester, POE sorbitan fatty acid ester, POE sorbitol fatty acid ester, POE glycerin fatty acid ester, POE alkyl ether, POE fatty acid ester, POE cured castor Oil, POE castor oil, POE / POP copolymer, POE / POP alkyl ether, polyether-modified silicone lauric acid alkanolamide, alkylamine oxide, hydrogenated soybean phospholipid, and the like.
Natural surfactant: lecithin, saponin, sugar surfactant and the like.

(7) Examples of polyhydric alcohols and sugars Ethylene glycol, diethylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, glycerin, diglycerin, polyglycerin, 3-methyl-1,3-butanediol, 1, 3 -Butylene glycol, sorbitol, mannitol, raffinose, erythritol, glucose, sucrose, fructose, xylitol, lactose, maltose, maltitol, trehalose, alkylated trehalose, mixed isomerized sugar, sulfated trehalose, pullulan and the like. These chemically modified compounds can also be used.

(8) Examples of polymers Acrylic ester / methacrylic acid ester copolymer (plus size, manufactured by Kyoyo Chemical), vinyl acetate / crotonic acid copolymer (resin 28-1310, manufactured by NSC), vinyl acetate / croton Acid / vinyl neodecanate copolymer (28-2930, manufactured by NSC), methyl vinyl ether maleic acid half ester (Gantrez ES, manufactured by ISP), T-butyl acrylate / ethyl acrylate / methacrylic acid copolymer (rubymer) , BASF), vinyl pyrrolidone / vinyl acetate / vinyl propionate copolymer (Rubicol VAP, BASF), vinyl acetate / crotonic acid copolymer (Rubiset CA, BASF), vinyl acetate / croton Acid / vinyl pyrrolidone copolymer (Rubiset CAP, manufactured by BASF), vinyl pyrrolidone / acrylate copolymer (Rubiflex, BAS) F), acrylate / acrylamide copolymer (Ultrahold, BASF), vinyl acetate / butyl maleate / isobornyl acrylate copolymer (Advantage, ISP), carboxyvinyl polymer (Carbopol, BF Goodrich), anionic polymer compounds such as acrylic acid / alkyl methacrylate copolymer (Pemulene, BF Goodrich), and acetic acid amphoteric products of dialkylaminoethyl methacrylate polymers (Yukaformer, Mitsubishi Chemical) Amphoteric polymer compounds such as octyl acrylate acrylate / hydroxypropyl acrylate / butylaminoethyl methacrylate copolymer (AMPHOMER, NSC), quaternized vinylpyrrolidone / dimethylaminoethyl methacrylate (GAFQUAT, ISP) , Methyl vinyl imidazolium chloride / Cationic polymer compounds such as vinylpyrrolidone copolymer (rubicoat, manufactured by BASF), polyvinylpyrrolidone (rubiscol K, manufactured by BASF), vinylpyrrolidone / vinyl acetate copolymer (rubiscol VA, manufactured by BASF) Nonionic polymer compounds such as vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer 937, manufactured by ISP), vinylcaprolactam / vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer VC713, manufactured by ISP), etc. is there. Cellulose or derivatives thereof, keratin and collagen or derivatives thereof, calcium alginate, pullulan, agar, gelatin, tamarind seed polysaccharide, xanthan gum, carrageenan, high methoxyl pectin, low methoxyl pectin, guar gum, gum arabic, crystalline cellulose, arabino Naturally derived polymer compounds such as galactan, gum karaya, gum tragacanth, alginic acid, albumin, casein, curdlan, gellan gum and dextran can also be suitably used.

(9) Examples of physiologically active ingredients Examples of physiologically active ingredients include substances that impart some physiological activity to the skin when applied to the skin. For example, whitening ingredients, immunostimulants, anti-aging agents, UV protection agents, slimming agents, tanning agents, antioxidants, hair growth agents, hair restorers, moisturizers, blood circulation promoters, antibacterial agents, bactericides, desiccants, A cooling sensation agent, a warming sensation agent, vitamins, an amino acid, a wound healing promoter, an irritation relaxation agent, an analgesic agent, a cell activator, an enzyme component, etc. are mentioned. Examples of these suitable ingredients include, for example, ashitaba extract, avocado extract, amateur extract, altea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract, fennel extract, turmeric extract, oolong tea extract, age Extract, Echinacea leaf extract, Ogon extract, Oat extract, Oen extract, Barley extract, Hypericum extract, Oyster extract, Dutch mustard extract, Orange extract, Seawater dried product, Seaweed extract, Hydrolyzed elastin, Hydrolyzed wheat powder, Hydrolyzed silk , Chamomile extract, Carrot extract, Kawara mugwort extract, Licorice extract, Calcade extract, Oyster extract, Kina extract, Cucumber extract, Guanosine, Gardenia extract, Kumazasa extract, Clarae Kiss, walnut extract, grapefruit extract, clematis extract, chlorella extract, mulberry extract, gentian extract, tea extract, yeast extract, burdock extract, fermented rice bran extract, rice germ oil, comfrey extract, collagen, bilberry extract, saicin extract, psycho extract Extract Kizuta extract, hawthorn extract, elderberry extract, yarrow extract, mint extract, sage extract, mallow extract, senki Sue extract, assembly extract, soybean extract, tiso extract, thyme extract, tea extract, clove extract, chigaya extract, chimpi extract, touki extract, toshinsen extract, tonin extract, spruce extract, dokudami extract, tomato extract, natto extract, carrot extract, garlic extract, Novara extract, hibiscus extract, bacmond extract, parsley extract, honey, hamamelis extract, parietalia extract, toad extract, bisabolol, loquat extract, dandelion extract, burdock extract, bukuro extract, butcher bloom extract, grape extract, propolis, loofah extract, Safflower extract, peppermint extract, bodaige extract, button extract, hop extract, pine extract, marronnier extract, mizubasho Kiss, Mukuroji extract, Melissa extract, Peach extract, Cornflower extract, Eucalyptus extract, Yukinoshita extract, Yokuinin extract, Artemisia extract, Lavender extract, Apple extract, Lettuce extract, Lemon extract, Lotus root extract, Rose extract, Rosemary extract, Roman chamomile extract And royal jelly extract.
Biopolymers such as deoxyribonucleic acid, mucopolysaccharide, sodium hyaluronate, sodium chondroitin sulfate, collagen, elastin, chitin, chitosan, hydrolyzed eggshell membranes, amino acids, hydrolyzed peptides, sodium lactate, urea, sodium pyrrolidonecarboxylate , Moisturizing ingredients such as betaine, whey, trimethylglycine, oily ingredients such as sphingolipid, ceramide, phytosphingosine, cholesterol, cholesterol derivatives, phospholipids, ε-aminocaproic acid, glycyrrhizic acid, β-glycyrrhetinic acid, lysozyme chloride, guaiazulene, Immunostimulants such as hydrocortisone, vitamin A, vitamin B2, vitamin B6, vitamin C, vitamin D, vitamin E, calcium pantothenate, biotin, nicotinamide, vitamin C ester Vitamins, active ingredients such as allantoin, diisopropylamine dichloroacetate, 4-aminomethylcyclohexanecarboxylic acid, antioxidants such as tocopherols, carotenoids, flavonoids, tannins, lignans, saponins, α-hydroxy acids, β-hydroxy acids, etc. Cell activators, blood circulation promoters such as γ-oryzanol and vitamin E derivatives, wound healing agents such as retinol and retinol derivatives, arbutin, kojic acid, placenta extract, sulfur, ellagic acid, linoleic acid, tranexamic acid, glutathione, etc. Whitening agent, cephalanthin, licorice extract, red pepper tincture, hinokitiol, garlic iodide extract, pyridoxine hydrochloride, DL-α-tocopherol, DL-α-tocopherol acetate, nicotinic acid, nicotinic acid derivative, calcium pantothenate, D-pan Tothenyl alcohol, acetyl pantothenyl ethyl ether, biotin, allantoin, isopropylmethylphenol, estradiol, ethinyl estradiol, capronium chloride, benzalkonium chloride, diphenhydramine hydrochloride, takanal, camphor, salicylic acid, nonyl acid vanillylamide, nonanoic acid vanillylamide, pyroctone Olamine, glyceryl pentadecanoate, L-menthol, mononitroguaiacol, resorcin, γ-aminobutyric acid, benzethonium chloride, mexiletine hydrochloride, auxin, female hormone, cantalis tincture, cyclosporine, zinc pyrithione, hydrocortisone, minoxidil, monostearic acid Examples include hair growth agents such as polyoxyethylene sorbitan, mint oil, and Sasanishiki extract.

(10) Examples of antioxidants: sodium bisulfite, sodium sulfite, erythorbic acid, sodium erythorbate, dilauryl thiodipropionate, tocopherol, tolylbiguanide, nordihydroguaiaretic acid, parahydroxyanisole, butylhydroxyanisole, dibutylhydroxy Examples include plant extracts having an antioxidant effect such as toluene, ascorbyl stearate, ascorbyl palmitate, octyl gallate, propyl gallate, carotenoid, flavonoid, tannin, lignan, saponin, apple extract and clove extract.

(11) Examples of solvents Examples include purified water, ethanol, lower alcohol, ethers, LPG, fluorocarbon, N-methylpyrrolidone, fluoroalcohol, volatile linear silicone, and next-generation fluorocarbon.

〔Example〕
Example 1 Production of Acai Extract The seeds were removed from the acai fruit and pureed, and extracted with 5 times the amount of 50% (W / W) water-containing ethanol for 2 hours. Then, it vacuum-dried and the acai extract of Example 1 was obtained.

Example 2: Production of cherry blossom extract A cherry blossom was extracted with 30% (W / W) water-containing ethanol for 1 hour (60 ° C). Thereafter, filtration and concentration were performed to obtain a cherry blossom extract.
Example 3 Production of Peptide Derived from Rice A protein powder (protein content 70%) extracted from rice was suspended in water and adjusted with hydrochloric acid so as to have a pH of 3.0. Thereafter, a proteolytic enzyme was added and the pH was adjusted to be substantially constant at 55 ° C. Then, the proteolytic enzyme was inactivated and centrifuged to remove the residue, followed by drying to obtain a rice-derived peptide. The peptide concentration at this time was 70%.

[Test example]
B16 melanoma cells were suspended (1 × 10 ⁵ cells / mL) in 2 mM theophylline-containing α-MEM medium (containing 10% FCS and penicillin / streptomycin), and seeded at 200 μL in a 48-well plate. The sample solutions (20 μL) of Examples 1 to 3 were added and cultured for 3 days, and then the cells were sonicated (1N NaOH). 200 μl of the disrupted solution was dispensed into a 96-well plate, and the absorbance at 415 nm was measured. As a comparative example (positive control), the same test was performed for arbutin, ascorbic acid glucoside, and kojic acid.

Results and Effects of Examples According to Table 1 above, it was found that the production of melanin was suppressed in a concentration-dependent manner for all acai extracts, rice-derived peptides, and cherry blossom extracts. In particular, the acai extract and rice-derived peptide suppressed the production of melanin to the same extent as the positive control.
Thereby, it was confirmed that the acai extract, cherry blossom extract, and rice-derived peptide are excellent as melanin production inhibitors.

[Example of formulation]
Although the compounding example of the melanin production inhibitor of this invention is given to the following, the following compounding example does not limit this invention.
Formulation Example 1: Chewing gum sugar 53.0 wt%
Gum base 20.0
Glucose 10.0
Minamata 16.0
Fragrance 0.5
Melanin production inhibitor 0.5
100.0wt%

Formulation Example 2: Gummy reduced starch syrup 40.0 wt%
Granulated sugar 20.0
Glucose 20.0
Gelatin 4.7
Water 9.68
Grape juice 4.0
Grape flavor 0.6
Dye 0.02
Melanin production inhibitor 1.0
100.0wt%

Formulation Example 3: Candy sugar 50.0 wt%
Minamata 33.0
Water 14.4
Organic acid 2.0
Fragrance 0.2
Melanin production inhibitor 0.4
100.0wt%

Formulation Example 4: Yogurt (hard / soft)
Milk 41.5wt%
Nonfat dry milk 5.8
Sugar 8.0
Agar 0.15
Gelatin 0.1
Lactic acid bacteria 0.005
Melanin production inhibitor 0.4
Perfume
Water residue
100.0wt%

Formulation Example 5: Soft Drink Fructose Glucose Liquid Sugar 30.0wt%
Emulsifier 0.5
Melanin production inhibitor 0.05
Perfume
Purified water residue
100.0wt%

Formulation Example 6: Soft capsule grape seed oil 87.0 wt%
Emulsifier 12.0
Melanin production inhibitor 1.0
100.0wt%

Formulation Example 7: Tablet Lactose 54.0 wt%
Crystalline cellulose 30.0
Starch degradation product 10.0
Glycerin fatty acid ester 5.0
Melanin production inhibitor 1.0
100.0wt%

Formulation Example 8: Oral granules (pharmaceuticals)
Melanin production inhibitor 1.0wt%
Lactose 30.0
Cornstarch 60.0
Crystalline cellulose 8.0
Polyvinylpyrrolidone 1.0
100.0wt%

Formulation Example 9: Tablet confectionery sugar 76.4 wt%
Glucose 19.0
Sucrose fatty acid ester 0.2
Melanin production inhibitor 0.5
Purified water 3.9
100.0wt%

Formulation Example 10: Cosmetic cream squalane 20.0 wt%
Beeswax 5.0
Refined jojoba oil 5.0
Glycerin 5.0
Glycerol monostearate 2.0
Polyoxyethylene (20) sorbitan-
Monostearate 2.0
Melanin production inhibitor 2.0
Antiseptic agent
Purified water residue
100.0wt%

Formulation Example 11: Lotion ethanol 5.0 wt%
Glycerin 2.0
1,3-butylene glycol 2.0
Polyethylene oleyl ether 0.5
Sodium citrate 0.1
Citric acid 0.1
Melanin production inhibitor 0.1
Purified water residue
100.0wt%

Formulation Example 12: Body gel macadamia nut oil 2.0 wt%
Octyldodecyl myristate 10.0
Methylphenylpolysiloxane 5.0
Behenyl alcohol 3.0
Stearic acid 3.0
Batyl alcohol 1.0
Glyceryl monostearate 1.0
Tetraoleic acid polyoxyethylene sorbit 2.0
Hydrogenated soybean phospholipid 1.0
Ceramide 0.1
Retinol palmitate 0.1
Preservative Appropriate amount Clover extract 1.0
Melanin production inhibitor 1.0
1,3-butylene glycol 5.0
Purified water residue
100.0wt%

Formulation Example 13: Latex Squalane 4.0 wt%
Vaseline 2.5
Cetanol 2.0
Glycerin 2.0
Lipophilic glyceryl monostearate 1.0
Stearic acid 1.0
L-Arginine 1.0
Melanin production inhibitor 0.5
Potassium hydroxide 0.1
Perfume
Purified water residue
100.0wt%

Formulation Example 14: Bath agent (liquid)
Propylene glycol 50.0wt%
Ethanol 20.0
Sodium sulfate 5.0
Melanin production inhibitor 0.5
Lanolin 0.5
Avocado oil 0.5
Dye 1.5
Fragrance 22.0
100.0wt%

  As described above, the present invention provides a safe melanin production inhibitor having a novel ingredient as an active ingredient.

Claims (3)

A melanin production inhibitor containing acai and / or an extract thereof as an active ingredient. A melanin production inhibitor comprising a cherry blossom and / or an extract thereof as an active ingredient. A melanin production inhibitor containing rice-derived protein and / or peptide as an active ingredient.