JP2009203164A - Skin-whitening agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a skin-whitening agent recognized to have a sufficient skin-whitening effect. <P>SOLUTION: This skin-whitening agent contains an extract of huamansamana (Jacaranda copaia). <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to a whitening agent and a melanin production inhibitor.

  A skin external preparation containing jacaranda copaia (Patent Document 1, Japanese Patent Application Laid-Open No. 2002-121111) is known, and an anti-aging effect based on an antioxidant action has been found. Also known are antibacterial agents and anti-inflammatory agents (Patent Document 2, Japanese Patent Application Laid-Open No. 2002-316936) containing jacaranda copaia. However, the whitening effect of Jacaranda copaia extract is not known.

  The amount of ultraviolet rays reaching the epidermis tends to increase year by year due to air pollution and ozone layer destruction, and along with this, skin troubles such as skin spots, freckles, and darkness due to ultraviolet rays are becoming more serious. Ultraviolet rays oxidize tyrosine present in the skin by the action of the tyrosinase enzyme to produce a melanin pigment. If excessively produced, it causes skin problems such as spots, buckwheat, and darkness. As a method for suppressing the production of this melanin pigment and preventing spots, freckles, and darkness, skin cosmetics containing L-ascorbic acid and a glucose glycoside of L-ascorbic acid, which is a derivative thereof (Patent Document 3) JP-A-4-82412), and a topical skin preparation (Patent Document 4, JP-A-4-82413) in which a glucose glycoside of L-ascorbic acid and an amino acid or a derivative thereof are combined is proposed. .

JP 2002-121111 JP JP 2002-316936 JP Japanese Patent Laid-Open No. 4-182412 Japanese Laid-Open Patent Publication No.4-182413

  However, these whitening agents may not have a sufficient whitening effect, and if a component showing a whitening effect is blended in a concentration at which the whitening effect is recognized, there may be problems in safety and stability. An object of this invention is to provide the plant extract useful as a whitening agent and a melanin production inhibitor.

  Therefore, as a result of researches and efforts made on the above-mentioned problems, the present inventors have found that an extract of Jacaranda copaia has a whitening effect and completed the present invention.

The main configuration of the present invention is as follows.
(1) A whitening agent containing an extract of Jacaranda copaia.
(2) A melanin production inhibitor containing an extract of Jacaranda copaia.

Hereinafter, embodiments of the present invention will be described in more detail.
Jacaranda copaia used in the present invention (Huamansamana, scientific name Jacaranda copaia
) Is a Takagi native to South America.

  Jacaranda copaia extracts include jacaranda copaia leaves, stems, buds, flowers, wood, bark, seeds, roots, fruits or pressed juices thereof, or dried products, hydrolysates of dried products, or ground products thereof. Crude extraction with organic solvents such as water or alcohol such as ethanol, hydrous alcohol, methanol, propanol, ethyl acetate, cyclohexane, dichloromethane, chloroform, ether, acetone, 1,3-butylene glycol, 1,2-pentanediol, propylene glycol And the extract fraction obtained by stepwise purification by various chromatographies such as column chromatography, etc., and the crude extract, hydrolyzate of the extract fraction, etc. Including. These may be used alone or in combination of two or more. The extraction solvent is preferably ethanol or hydrous ethanol. In addition, the extraction site of Jacaranda copaia is preferably leaves.

  Extraction can be performed by immersing in an extraction solvent. In order to increase the extraction efficiency, stirring, homogenization or pressure can be applied in the extraction solvent. The extraction temperature is suitably about 5 to 100 ° C., and the extraction time is about 5 minutes to 1 year. These conditions can be appropriately set according to the purpose. When hydrolysis is performed, degradation with enzymes such as esterase, degradation with microorganisms such as lactic acid bacteria and yeast, acids such as hydrochloric acid, sulfuric acid, acetic acid, phosphoric acid, citric acid, lactic acid, tartaric acid, fumaric acid, malic acid, etc. And decomposition with alkali such as sodium hydroxide and potassium hydroxide. Hydrolysis conditions are not particularly limited. When enzymes or microorganisms are used, however, the hydrolysis is usually performed at 10 to 55 ° C., pH 3 to 8, or 5 to 24 hours according to the optimum temperature or pH of the enzymes or microorganisms to be used. I do. When the hydrolysis is performed using an acid or an alkali, the hydrolysis is usually carried out at a concentration of 2 to 15% by weight at room temperature to 60 ° C. for about 0.5 to 24 hours.

  The whitening agent of the present invention can be used in various forms and applications, for example, whitening emulsion cosmetics, whitening creams, whitening lotions, whitening oily cosmetics, whitening packs, whitening foundations, and the like. The whitening agent of the present invention includes a whitening skin external medicine, a whitening quasi-drug, and a whitening cosmetic. The whitening agent of the present invention may be used as an oral whitening agent, an injection, an oral medicine, or a food for whitening. As a food, in addition to a normal food, it may be used as a nutritional supplement, a functional food, a health food, a food for specified health use, etc., and can be blended in a beverage such as a juice, for example.

  The melanin production inhibitor of the present invention can be blended with various whitening agents in order to develop a whitening effect.

The whitening agent containing the extract of Jacaranda copaia of the present invention can be produced according to a commonly used formulation method.
The whitening agent of the present invention includes fats and oils such as vegetable oils, higher fatty acids, higher alcohols, silicones, anionic surfactants, cationic surfactants, amphoteric surfactants, nonionic surfactants, preservatives, sugars, metals A sequestering agent, a polymer such as a water-soluble polymer, a thickener, a powder component, a UV absorber, a UV blocker, a moisturizer such as hyaluronic acid, a fragrance, a pH adjuster, etc. . Vitamins, skin activators, blood circulation promoters, resident bacteria control agents, active oxygen scavengers, anti-inflammatory agents, whitening agents, bactericides, and other medicinal and physiologically active components can also be included.

  Examples of the fats and oils include camellia oil, evening primrose oil, macadamia nut oil, olive oil, rapeseed oil, corn oil, sesame oil, jojoba oil, germ oil, wheat germ oil, toglycerin, glyceryl trioctanoate, etc. , Palm oil, hydrogenated coconut oil, palm oil, palm kernel oil, owl, owl kernel oil, hydrogenated oil, hardened castor oil and other solid fats, beeswax, candelilla wax, cotton wax, nuka wax, lanolin, lanolin acetate, liquid lanolin And waxes such as sugarcane wax, liquid paraffin, squalene, squalane, and microcrystalline wax.

  Examples of higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), and the like.

  Examples of the higher alcohol include linear alcohols such as lauryl alcohol, stearyl alcohol, cetyl alcohol, and cetostearyl alcohol, and branched chain alcohols such as monostearyl glycerin ether, lanolin alcohol, cholesterol, phytosterol, and octyldodecanol.

  Examples of the silicone include linear polysiloxanes such as dimethylpolysiloxane and methylphenylpolysiloxane, and cyclic polysiloxanes such as decamethylpolysiloxane.

  Examples of the anionic surfactant include fatty acid salts such as sodium laurate, higher alkyl sulfates such as sodium lauryl sulfate, alkyl ether sulfates such as POE lauryl sulfate triethanolamine, N-acyl sarcosine acid, sulfosuccinate , N-acylamino acid salts and the like.

  Examples of the cationic surfactant include alkyltrimethylammonium salts such as stearyltrimethylammonium chloride, benzalkonium chloride, and benzethonium chloride.

  Examples of amphoteric surfactants include betaine surfactants such as alkyl betaines and amide betaines.

  Examples of nonionic surfactants include sorbitan fatty acid esters such as sorbitan monooleate and hydrogenated castor oil derivatives.

  Examples of preservatives include methyl paraben and ethyl paraben.

  Examples of the sequestering agent include edetates such as disodium ethylenediaminetetraacetate, edetic acid, and sodium edetate.

  Examples of polymers include gum arabic, gum tragacanth, galactan, guar gum, carrageenan, pectin, agar, quince seed, dextran, pullulan, carboxymethyl starch, collagen, casein, gelatin, methylcellulose, methylhydroxypropylcellulose, hydroxyethylcellulose, carboxymethylcellulose Examples thereof include vinyl polymers such as sodium (CMC), sodium alginate, carboxyvinyl polymer (such as CARBOPOL), and bentonite.

  Examples of the thickener include carrageenan, gum tragacanth, quince seed, casein, dextrin, gelatin, CMC, hydroxyethyl cellulose, hydroxypropyl cellulose, carboxyvinyl polymer, guar gum, xanthan gum and the like.

  Examples of the powder component include talc, kaolin, mica, silica, zeolite, polyethylene powder, polystyrene powder, cellulose powder, inorganic white pigment, inorganic red pigment, titanium oxide coated mica, titanium oxide coated talc, and colored titanium oxide coated mica. And organic pigments such as Red No. 201 and Red No. 202.

  Examples of the ultraviolet absorber include paraaminobenzoic acid, phenyl salicylate, isopropyl paramethoxycinnamate, octyl paramethoxycinnamate, and 2,4-dihydroxybenzophenone.

  Examples of the ultraviolet blocking agent include titanium oxide, talc, carmine, bentonite, kaolin, and zinc oxide.

  Examples of humectants include polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, glycerin, diglycerin, polyglycerin, xylitol, maltitol, maltose, sorbitol, glucose, fructose, sucrose, lactose, and chondroitin. Examples thereof include sodium sulfate, sodium hyaluronate, sodium lactate, pyrrolidone carboxylic acid, cyclodextrin and the like.

  Examples of medicinal ingredients include vitamin A oil, vitamin A such as retinol, vitamin B2 such as riboflavin, B6 such as pyridoxine hydrochloride, L-ascorbic acid, L-ascorbic acid phosphate, L-ascorbic acid Vitamin C such as monopalmitic acid ester, L-ascorbic acid dipalmitic acid ester, L-ascorbic acid-2-glucoside, pantothenic acid such as calcium pantothenate, vitamin D such as vitamin D2, cholecalciferol; α- Vitamins such as vitamin E such as tocopherol, tocopherol acetate and DL-α-tocopherol nicotinate can be mentioned.

  Whitening agents such as glutathione and yukinoshita extracts, skin activators such as royal jelly and beech tree extract, blood circulation promoters such as capsaicin, gingeron, cantalis tincture, ictamol, caffeine, tannic acid and γ-oryzanol, glycyrrhizic acid derivatives , Glycyrrhetinic acid derivatives, anti-inflammatory agents such as azulene, amino acids such as arginine, serine, leucine and tryptophan, maltose sucrose condensates of resident bacteria control agents, lysozyme chloride and the like.

  In addition, chamomile extract, parsley extract, wine yeast extract, grapefruit extract, honeysuckle extract, rice extract, grape extract, hop extract, rice bran extract, loquat extract, buckwheat extract, yakuinin extract, assembly extract, merirot extract, birch extract, elephant extract, peony extract, Soap extract, loofah extract, capsicum extract, lemon extract, gentian extract, perilla extract, aloe extract, rosemary extract, sage extract, thyme extract, tea extract, seaweed extract, cucumber extract, carrot extract, carrot extract, maronier extract, hamamelis Examples include various extracts such as extracts and mulberry extracts.

As an oral whitening agent, the extract of Jacaranda Copaia as it is, or with various nutritional components added or contained in foods and drinks, dietary supplements, functional foods, health foods, foods for specified health use, or normal foods Can be used as a material. For example, suitable auxiliaries such as starch, lactose, maltose, vegetable oil powder, cocoa butter powder, stearic acid and the like can be added.
The effective dose of the extract of Jacaranda Copaia as an oral whitening agent is appropriately selected and determined according to the subject's age, weight, symptoms, administration route, administration schedule, formulation form, strength of activity of the material, etc. For example, 1 to 50000 mg per day is preferable, and 10 to 1000 mg is particularly preferable. This may be divided into several times a day.

  The blending amount of the Jacaranda copaia extract to the whitening agent is preferably 0.00001 to 30% by mass as a dry weight, but is not necessarily limited thereto.

  Since the extract of Jacaranda copaia of the present invention is a natural product, its toxicity is low and no harmful side effects have been reported.

Hereinafter, the present invention will be specifically described with reference to examples, but the present invention is not limited thereto.
[Production Example 1]
The dried leaves of Jacaranda Copaia (produced in Brazil) were pulverized by a pulverizer (Wander Blender, Osaka Chemical Co., Ltd.). 6 g of the pulverized leaves were extracted using ASE 200 Accelerated Solvent Extractor (manufactured by Nippon Dionex) under conditions of 40 ml of 99.5% ethanol, room temperature, and pressure of 1500 psi. The extract solvent was distilled off under reduced pressure to obtain an extract of Jacaranda Copaia. The resulting extract of Jacaranda Copaia is 289 mg, which is 4.8% of the dried leaves of the original Jacaranda Copaia.

[Production Example 2]
The dried leaves of Jacaranda Copaia (produced in Brazil) were pulverized by a pulverizer (Wander Blender, Osaka Chemical Co., Ltd.). 6 g of pulverized leaves were extracted using ASE 200 Accelerated Solvent Extractor (manufactured by Nippon Dionex) under the conditions of 40 ml of 70% ethanol, room temperature, and pressure of 1500 psi. The extract solvent was distilled off under reduced pressure to obtain an extract of Jacaranda Copaia. The extract of jacaranda copaia obtained is 1022 mg, which is 17.4% of the dried leaves of the original jacaranda copaia.

[Melanin production inhibition test]
The melanin production inhibitory activity was measured by the following test using the extract obtained by using the methods of Production Examples 1 and 2.

As positive controls, arbutin and the extracts of Production Examples 1 and 2 were each adjusted to 10 mg / ml using dimethyl sulfoxide and used as test substances.
Melanin production inhibitory activity was obtained by seeding mouse-derived B16 melanoma F10 in 1 well of 10 × ⁵ cells / well on 6 well plate, and 24 hours later, 100 nM [NLE4, D-PHE7] α-MSH (manufactured by SIGMA-ALDRICH), and Arbutin at each concentration, the extract of Production Example 1 and the extract of Production Example 2 were added. After culturing for 72 hours, the cells were collected with trypsin, 250 μl of 1% triton X was added, and melanin was dispersed by sonication. Samples were transferred to 96-well plates in 100 μl increments, and melanin was measured at an absorbance of 405 nm. IC _{50 of} each test substance is calculated with the amount of melanin when only [NLE4, D-PHE7] α-MSH is treated without adding the extract of Production Example 1 and the extract of Production Example 2 as 100%. did. The melanin production inhibition rate (%) was determined by the following equation, where A is the 405 nm absorbance when only [NLE4, D-PHE7] α-MSH is treated, and As is the 405 nm absorbance when the sample is added at each concentration.

Melanin production inhibition rate (%) = (1−As / A) × 100

As shown in Table 1 and FIG. 1, it can be seen that the addition of Jacaranda copaia extract suppresses melanin production, and the Jacaranda copaia extract exhibits a whitening effect. The Jacaranda copaia extract of Production Example 1 has an IC ₅₀ that is 1/10 that of arbutin, which has an excellent melanin production inhibitory effect, and showed an extremely high melanin production inhibitory effect. Further, the Jacaranda copaia extract of Production Example 2 showed an IC ₅₀ equivalent to that of arbutin.

  Below, the formulation example of this invention is shown. Each was produced according to a conventional method. The Jacaranda copaia extract in the formulation examples is dry mass.

Formulation Example 1 Whitening Lotion Ingredients Amount (% by mass)
1. Glycerin 10
2. 1,3-butylene glycol 5
3. Glucose 2
4). Ethanol 5
5. Carboxyvinyl polymer 0.02
6). Dipotassium glycyrrhizinate 0.1
7). Sodium hyaluronate 0.001
8). Jacaranda copaia extract of Production Example 1 0.1
9. Citric acid 0.05
Ten. Sodium citrate 0.1
11． Potassium hydroxide 0.01
12． Purified water residue

Formulation Example 2 Whitening Cream Ingredients Amount (% by mass)
1. Stearyl alcohol 6
2. Stearic acid 2
3. Squalane 10
4). Octild decanol 5
5. Olive oil 5
6. 1,3-Butylene glycol 8
7). Polyethylene glycol 1500 4
8). POE (25) cetyl alcohol ether 3
9. Glyceryl monostearate 2
Ten. Jacaranda Copaia Extract 2 from Production Example 1
11． Purified water residue

Formulation Example 3 Whitening Pack Ingredients Amount (% by mass)
1. Polyvinyl alcohol 15
2. Carboxymethylcellulose 5
3. 1,3-butylene glycol 5
4). Ethanol 12
5. Jacaranda Copaia Extract from Production Example 1 3
6). POE oleyl alcohol ether 0.5
7). Citric acid 0.02
8). Sodium citrate 0.04
9. Purified water residue

Formulation Example 4 Whitening Tablet Ingredients Amount (% by mass)
1. Jacaranda copaia extract of Production Example 1 63
2. Lactose 24
3. Cornstarch 12
4). Guar gum 1

Formulation Example 5 Whitening beverage Ingredients Amount (mass%)
1. Jacaranda copaia extract of Production Example 1 10
2. Fructose butter sugar liquid sugar 15
3. Citric acid 10
4). Vitamin C 5
5. Fragrance 1
6). Dye 1
7). Purified water residue

Graph showing melanin production inhibition test results

Claims (2)

  Jacaranda Whitening agent containing copaia extract.   A melanin production inhibitor containing an extract of jacaranda copaia.

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