JP2014019695A - Tyrosinase inhibitor with burdock fine powder as active ingredient - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a tyrosinase active inhibitor or composition with burdock fine powder giving a safe dietary habit as an active ingredient.SOLUTION: The present invention provides a tyrosinase active inhibitor and composition with burdock fine powder as an active ingredient. Further, whitening agent such as cosmetics, browning inhibitor of foods, a food and drink composition, a pharmaceutical composition and pet foods that comprise the tyrosinase active inhibitor or composition are provided.

Description

The present invention relates to a tyrosinase inhibitor characterized by containing fine burdock powder. The present invention relates to a tyrosinase inhibitor useful as a whitening agent, and further, as a new skin external preparation having a whitening action or the like, a pharmaceutical agent (animal therapeutic agent for animals) given to humans or non-human animals. Including foods), foods and drinks, and feed or pet food compositions, as well as food browning inhibitors and the like.

Typical skin troubles are wrinkles caused by aging and loss of elasticity, but there are also dark skin, spots, freckles, etc., which are particularly serious problems for women. Skin darkening, spots, freckles, etc. are caused by the deposition of melanin pigment. Tyrosine, a kind of amino acid, is converted into dopa in the presence of tyrosinase in skin tissue called melanocytes. It is caused by a metabolic pathway that further becomes dopaquinone and then forms melanin by autooxidation. This metabolic pathway is mainly a redox reaction involving tyrosinase, and many activated oxygens (free radicals) are generated during the oxidation, which may cause cell damage.

For the above-mentioned skin darkening, stains, buckwheat, etc., various whitening agents have been proposed to eliminate this, and many of them are already on the market. In particular, tyrosinase inhibitors that inhibit the activity of tyrosinase and suppress the production of melanin. As for, no effective one has been found yet. Moreover, even if it has a certain effect, it still has some problems such as insufficient skin permeability and skin irritation.

The root part of the burdock, which is a root vegetable, is edible, and the present invention uses this part as a raw material to prepare a fine powder. The total polyphenol content contained in the burdock fine powder was 13.5 mg gallic acid equivalent / gram, and the antioxidant activity was 10.8 mg BHA equivalent / gram. These values are characterized by being very high compared to other root vegetables. However, the effect of burdock on tyrosinase activity has not been clarified at all.

Problems to be solved by the invention

The present invention has been proposed in view of such a conventional situation. That is, an object of the present invention is to provide a tyrosinase inhibitor that inhibits the activity of tyrosinase, suppresses the production of melanin, has few side effects, and is useful as a whitening component. Furthermore, an object of the present invention is to provide a novel external preparation for skin having a tyrosinase inhibitory function and useful as a cosmetic.

Means for solving the problem

In order to achieve the above-mentioned object, the present inventor has intensively studied for a long time. As a result, it came to find out that the component which has a tyrosinase inhibitory function was contained in the fine powder of a burdock prepared by grind | pulverizing the root part of the burdock | edible used as an edible.

The present invention has been completed based on such findings. That is, the tyrosinase inhibitor and the external preparation for skin of the present invention are characterized by containing burdock fine powder as an active ingredient.

The details of the tyrosinase inhibitor contained in the burdock fine powder are still unknown, but the water-soluble components eluted from the burdock fine powder by water extraction are effective in inhibiting tyrosinase. Has been confirmed experimentally. Therefore, the white powder of burdock exhibits whitening effect as it is as a constituent of the tyrosinase inhibitor and external preparation for skin of the present invention.

That is, the present invention provides the following.

[1] A tyrosinase inhibitor containing burdock fine powder as an active ingredient.

[2] A tyrosinase inhibitor comprising a composition containing burdock fine powder as an active ingredient.

[3] A whitening agent such as a cosmetic comprising the tyrosinase inhibitor according to [1] or [2].

[4] A food browning inhibitor comprising the tyrosinase inhibitor according to [1] or [2].

[5] A food and drink composition containing the tyrosinase inhibitor according to [1] to [4].

[6] A pharmaceutical composition containing the tyrosinase inhibitor according to [1] to [4].

[7] The agent or composition according to [1] to [6] for the purpose of whitening or preventing browning.

Effect of the invention

Since the tyrosinase inhibitor of the present invention or a composition containing the same suppresses the activity of tyrosinase responsible for melanin production in the body, it can be expected to have a whitening effect and a browning prevention effect. Therefore, it is useful for the elimination and prevention of skin darkening, spots, freckles and the like in the beauty field. It is also useful for use as an additive to prevent food discoloration. Furthermore, since it is possible to produce the agent or composition of the present invention from ingredients with food experience, it is safe to take.

The tyrosinase inhibitor of the present specification is an agent and a composition having a tyrosinase inhibitory action containing burdock fine powder as an active ingredient. Although content of said compound is not limited, it should just be contained in the range which can exhibit a tyrosinase inhibitory effect.

The composition for eating and drinking of the present invention is a composition containing the tyrosinase inhibitor described above, and these are mixed with general foods. Further, capsules, tablets, granules and the like that are easy to take may be used by using appropriate carriers and auxiliaries as known foods. The food and drink here refers to, for example, general foods, health functional foods (special health foods, nutritional functional foods), health foods, nutritional supplements, pet foods, and the like. General food as used herein includes, but is not limited to, beverages, dairy products, fermented milk, lactic acid bacteria beverages, processed milk, coffee beverages, juices, ice creams, strawberries, biscuits, wafers, jellies, soups, and noodles. is not. Preferably, beverages, dairy products, processed milk, fermented milk, lactic acid bacteria beverages, wafers, and jelly are included.

The pharmaceutical composition of the present invention is a composition containing the above-mentioned tyrosinase inhibitor, which may be the above-mentioned agent itself, or a composition containing a pharmaceutically acceptable carrier as desired. Good. The use is not limited, and examples thereof include readily available drugs such as over-the-counter drugs (OTC) or quasi drugs. The form of the pharmaceutical composition is not limited, and examples thereof include pills, solutions, powders, granules, tablets, capsule tablets, troches, syrups, and dry syrups. Preferably, capsules, liquids, elixirs, tablets, cachets, suppositories and the like are used. A pharmaceutically acceptable carrier is any material suitable for oral, enteral, transdermal, and subcutaneous administration, such as water, gelatin, gum arabic, lactose, microcrystalline cellulose, starch. Sodium starch glycolate, calcium hydrogen phosphate, magnesium stearate, talc, colloidal silicon dioxide, and the like.

Burdock fine powder and the composition are blended as an active ingredient of a tyrosinase inhibitor, but when formulated as a tyrosinase inhibitor, the dosage form may be any dosage form such as powder, granule, tablet, etc. Can be adopted. At that time, in order to facilitate storage and handling, carriers such as dextrin and cyclodextrin, preservatives and other optional auxiliaries can be blended as necessary. Moreover, the form is not limited, The composition for food and drink and the composition for pharmaceuticals are included. Although content of these is not limited, it should just be contained in the range which can exhibit an effect with respect to tyrosinase activity.

The tyrosinase inhibitor is absorbed transcutaneously to reach melanocytes (chromophore cells) and inhibits the activity of tyrosinase so that melanin is not generated.

The most effective method of utilizing the action of the tyrosinase inhibitor is to blend it into cosmetics or any other external preparation for skin. Examples of skin external preparations that are suitable for blending include ointments, creams, emulsions, lotions, packs, bathing agents, and the like. Here, the preferred blending ratio of the burdock fine powder and the composition is 0.01 to 10% by weight. If the blending ratio is less than 0.01% by weight, a sufficient effect cannot be expected. On the other hand, when it exceeds 10 parts by weight, the color of the burdock fine powder and the composition itself becomes a problem.

Even if the tyrosinase inhibitor of the present invention is blended in order to impart a whitening action to a skin external preparation such as a cosmetic, the original composition of the skin external preparation is not limited thereby. Therefore, various main agents and auxiliaries usually used in the production of general cosmetics and the like can be blended into the external preparation for skin according to the present invention by conventional methods. In addition, any auxiliary agent effective for improving the action of the tyrosinase inhibitor to be incorporated can be contained.

Typical constituents include astringents, bactericides / antibacterial agents, whitening agents, UV absorbers, humectants, cell activators, anti-inflammatory / anti-allergic agents, antioxidant / active oxygen scavengers, and the like.

Here, as astringents, citric acid or salts thereof, tartaric acid or salts thereof, lactic acid or salts thereof, aluminum chloride, aluminum sulfate / potassium sulfate, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum, zinc paraphenolsulfonate, zinc sulfate, Illustrate jellyfish extract, ages extract, hamamelis extract, genus pepper extract, tea catechins, diatomaceous earth extract, nettle extract, hypericum extract, diaper extract, cornflower extract, horsetail extract, kizuta extract, cucumber extract, maronier extract, salvia extract, melissa extract, etc. Can do.

As the bactericidal / antibacterial agent, benzoic acid, sodium benzoate, paraoxybenzoic acid ester, distearylmethylammonium chloride, benzethonium chloride, alkyldiaminoethylglycine chloride solution, chlorhexidine hydrochloride, orthophenylphenol, photosensitizer 101, photosensitizer 201 No., salicylic acid, sodium salicylate, sorbic acid, halocarban, resorcin, parachlorophenol, phenoxyethanol, bisabolol, hinokitiol, menthol, chitosan, chitosan degradation product, jellyfish extract, kujin extract, enmiso extract, loquat extract, walrus extract, hop extract, yucca An extract, an aloe extract, a cinnamon extract, a gadget extract, etc. can be mentioned.

Whitening agents include ascorbic acid and derivatives thereof, sulfur, placental extract, kojic acid and derivatives thereof, glucosamine and derivatives thereof, azelain and derivatives thereof, arbutin and derivatives thereof, hydroxycinnamic acid and derivatives thereof, glutathione, arnica extract, Ougon extract, Senkyu extract, Sakuhakuhi extract, Psycho extract, Bowfu extract, Hamaboufu extract, Mannen mycelium culture or its extract, Gymnema extract, Linden extract, Peach leaf extract, Ages extract, Kuzin extract, Jiuyu extract, Toki extract, Yakuinin extract , Oyster leaf extract, Daio extract, Buttonpi extract, Hamamelis extract, Maronnier extract, Hypericum extract, Oyster extract, Oil-soluble Licorice extract (Liquorice hydrophobic flavone, Green Burijin, glabrene, can be exemplified licochalcone A) or the like.

UV absorbers include β-isopropylfuranone derivatives, urocanic acid, ethyl urocanate, oxybenzone, oxybenzonesulfonic acid, tetrahydroxybenzophenone, dihydroxydimethoxybenzophenone, dihydroxybenzophenone, cinoxalate, methyl diisopropylcinnamate, octyl methoxycinnamate, paraaminobenzoic acid Glyceryl acid, amyl paradimethylaminobenzoate, octyl paradimethylbenzoate, paraaminobenzoic acid, ethyl paraaminobenzoate, butylmethoxydibenzoylmethane, titanium oxide, β-carotene, γ-oryzanol, rice bran extract, aloe extract, birch extract, White birch extract, chamomile extract, white-eye extract, hawthorn extract, henna extract, butterfly Vinegar, horse chestnut extract, ginkgo leaf extract, chamomile extract, hawthorn extract, mention may be made of oil-soluble licorice extract, and the like.

Moisturizers include serine, glycine, threonine, alanine, collagen, hydrolyzed collagen, vitronectin, fibronectin, keratin, elastin, royal jelly, chondroitin, heparin, glycerophospholipid, glyceroglycolipid, sphingophospholipid, sphingoglycolipid, linoleic acid Or its esters, eicosapentaenoic acid or its esters, pectin, algae colloid, bifidobacteria fermentation product, lactic acid fermentation product, yeast extract, litchi mycelium culture or extract thereof, wheat germ oil, avocado oil, rice germ Oil, jojoba oil, soybean phospholipid, γ-oryzanol, bellows oyster extract, yokuinin extract, siamese extract, typhoid extract, diatomaceous earth extract, kidachi aloe extract, burdock extract, malonie extract, mannenloue Vinegar, mention may be made of arnica extract, wheat bran, and rice bran extract and the like.

Cell activators include riboflavin or derivatives thereof, pyridoxine or derivatives thereof, nicotinic acid or derivatives thereof, pantothenic acid or derivatives thereof, α-tocopherol or derivatives thereof, arnica extract, carrot extract, rapeseed extract, sorghum extract, loofah extract (Saponin), sicon extract, white birch extract, peonies extract, button pea extract, peonies extract, mugwort extract, safflower extract, ashitaba extract, loquat leaf extract, hikikoshi extract, cypress extract, yellow cocoon extract, salvia extract, garlic extract, mannen wax extract, etc. Can be mentioned.

Anti-inflammatory and anti-allergic agents include azulene, allantoin, aminocaproic acid, indomethacin, lysozyme chloride, epsilon aminocaproic acid, oxybenzone, glycyrrhizic acid or its derivatives, glycyrrhetinic acid or its derivatives, photosensitizer 301, photosensitizer 401, diphenhydramine hydrochloride , Tranexamic acid or its derivatives, adenosine phosphate, estradiol, eslon, ethinyl estradiol, cortisone, hydrocortisone, prednisone, progesterone, corticosterone, arnica extract, inchinko extract, sanshi extract, jujube extract, horse chestnut extract, licorice extract, Toki extract, mugwort extract, bitumen extract, gentian extract, psycho extract, senkyu extract, bowfish Kiss, yarrow extract, Coptis extract, is the mint extract and the like.

Antioxidant and active oxygen scavengers include dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate, baicalin, baicalein, superoxide dismutase, catalase, rosemary extract, melissa extract, oxon extract, agetsu extract, loquat leaf extract, hops Extract, Hamamelis extract, Peonies extract, Sage extract, Kina extract, Chamomile extract, Perilla extract, Ginkgo biloba extract, Eucalyptus extract, Thyme extract, Cardamom extract, Callaway extract, Nutmeg extract, Mace extract, Laurel extract, Clove extract, Turmeric extract, Yanagitade An extract etc. can be illustrated.

Examples are given below to describe the present invention in more detail, but the present invention is not limited by these.

Examination of burdock tyrosinase inhibition The effect of burdock on tyrosinase activity was examined using an enzyme reaction system in a test tube.

The sample was added to 10 ml of water and mixed with 500 mg of burdock powder pulverized to about 10 μm, mixed with 40 ml of methanol, and shaken at room temperature for 3 hours as a suspension. The sample was further diluted with 80% methanol solution to prepare a dilution series. 150 μl of sample solution of each concentration was added to make a total volume of 3300 μl / reaction tube.

The solutions (A to D solutions) used for the reaction in this test were prepared as follows. In solution A, 3.22 grams of potassium dihydrogen phosphate and 3.74 grams of disodium hydrogen phosphate were dissolved in water to make the total volume 500 ml (pH 6.8). Liquid B was 1.29 grams of citric acid and 6.23 grams of disodium hydrogen phosphate dissolved in water to a total volume of 500 ml (pH 6.8). For solution C, tyrosinase (Sigma, 4200 units / mg) was dissolved in solution A to 400 units / ml. In solution D, 6 mg of tyrosine was dissolved in 30 ml of solution A.

The tyrosinase reaction in a test tube was performed by mixing 1.5 ml of solution B, 0.15 ml of solution C and 0.15 ml of diluted sample at each concentration, preincubating at 37 ° C. for 10 minutes, and then adding 1.5 ml of solution D. In addition, the incubation was performed at the same temperature for 20 minutes. Thereafter, tyrosinase activity was evaluated by measuring absorbance at 490 nm. As a control, 80% methanol was added instead of the sample. In each test group, a blank in which solution A was added instead of solution C was set.
The inhibition rate was calculated from the following calculation formula. Inhibition rate = 1- (absorbance of sample-absorbance of sample blank) / (absorbance of control-absorbance of control blank). Table 1 shows the relative tyrosinase inhibition rate in relation to the solvent and concentration, with 100 as the control.

As is clear from Table 1, strong tyrosinase activity inhibition was observed in burdock fine powder. The inhibition of tyrosinase activity did not change even when heated at 120 ° C. for 20 minutes. Because of such high heat resistance, burdock powder seems to be usable for various materials. The IC _{50 for} inhibition was 78 μg / ml. Therefore, it was demonstrated that burdock fine powder is effective in inhibiting tyrosinase activity.

Claims (7)

A tyrosinase inhibitor containing burdock fine powder as an active ingredient. A tyrosinase inhibitor containing a composition containing burdock fine powder as an active ingredient. A whitening agent such as a cosmetic comprising the tyrosinase inhibitor according to [1] or [2]. A food browning inhibitor comprising the tyrosinase inhibitor according to [1] or [2]. A dietary composition containing the tyrosinase inhibitor according to [1] to [4]. [1] A pharmaceutical composition comprising the tyrosinase inhibitor according to [4]. The agent or composition according to [1] to [6] for the purpose of whitening or preventing browning.