TWI566772B - Whitening agent and malanin production inhibitor - Google Patents

Description

Whitening agent and melanin production inhibitor (related application)

The present invention claims the priority of Japanese Patent Application No. 2011-88317 filed on Apr. 12, 2011, the disclosure of which is incorporated herein.

The present invention relates to whitening agents and melanin production inhibitors, in particular to their active ingredients.

Pigmentation such as dull skin/freckles is thought to be caused by excessive formation of melanin due to abnormalities of hormones or ultraviolet rays, local inflammation of the skin, and the melanin is deposited in the skin. The melanin, which is the cause of pigmentation of the skin, is produced by a cell called a melanosome in a pigment cell (melanocyte) found in the basal layer of the epidermis, and the produced melanin enters. Peripheral keratinocytes.

As a method for preventing/improving the above-described pigmentation, a substance having a whitening effect is used, that is, a substance which suppresses melanin production is mainly used. As a method for preventing/improving pigmentation, for example, a method of administering vitamin C in a large amount orally, a method of injecting glutathione, or the like; or a method of injecting citric acid, vitamin C and a derivative thereof, and cysteine A method of locally applying to the skin in the form of an ointment, a cream, a lotion or the like.

On the other hand, chafuroside is a compound which can be isolated by extraction from tea such as oolong tea. The tea amphoteric acid is effective for an allergic disease, and it is known that a tea containing the tea amphoteric acid is obtained in a high proportion. Method (Patent Document 1). However, it is not a report on the whitening effect of the chafuroside B and the inhibitory effect on melanin production.

[Previous Technical Literature] [Patent Literature]

[Patent Document 1] Japanese Patent Laid-Open Publication No. 2009-131161

The present invention has been made in view of the above-described prior art, and an object of the present invention is to provide a compound which has an excellent whitening action and a melanin production suppressing action, and is useful as a whitening agent and a melanin production inhibitor.

In order to solve the above problems, the inventors of the present invention have conducted intensive studies, and as a result, it has been found that the tea buckwheat acid B system has an excellent whitening action and melanin production suppressing action, and the present invention has been completed.

That is, the whitening agent of the present invention contains tea belly acid B.

The melanin production inhibitor of the present invention contains Chabian An acid B.

The method for inhibiting melanin production according to the present invention is to orally administer a composition comprising an effective amount of catechin B.

Further, the melanin production inhibiting method of the present invention is a method comprising applying an effective amount of a composition of Cha Vinic Acid B to the skin.

In the above method for inhibiting melanin production, the function of the tea amphoteric acid B is preferred as a whitening agent.

The use of a tea belly acid B as an active ingredient in the manufacture of a whitening agent containing tea belly acid B of the present invention.

In the above-mentioned use, the aforementioned tea amphoteric acid B is preferred to inhibit melanin production.

The whitening agent and the melanin production inhibitor of the present invention contain a tea succinic acid B, and can provide a preparation excellent in whitening action and melanin production inhibitory action.

The whitening agent and the melanin production inhibitor of the present invention contain the tea belly acid B. The tea amphoteric acid B is a flavone C glycoside represented by the following formula (I).

The method for producing the tea belly acid B is not particularly limited, and a synthetic product synthesized by a known method can be used, and can be separated from tea leaves such as green tea, roasted tea, black tea, and oolong tea by a known purification method.

When the composition of the tea succinic acid B containing the active ingredient of the whitening agent and the melanin production inhibitor is administered orally, it is preferred to administer an effective amount of the tea succinic acid B. Tea abalone B is administered 0.001 mg/kg body weight per day (b.w.) The above is appropriate. Further, it is particularly preferable to administer 1 mg/kg body weight (b.w.) or more per day.

The whitening agent and the melanin production inhibitor of the present invention can also be formulated into a whitening beverage or a whitening food. In the whitening beverage or whitening food, the additive may be arbitrarily selected and formulated as needed in addition to the active ingredient of the tea. Examples of the additive include an excipient, a flavoring agent, a coloring agent, a preservative, a tackifier, a stabilizer, a gelling agent, an antioxidant, and a functional raw material.

Examples of functional raw materials include various vitamins, pantothenic acid, folic acid, biotin, zinc, calcium, magnesium, amino acids, oligosaccharides, propolis, royal jelly, EPA, DHA, and coenzyme. Q10 (coenzyme Q-10), chondroitin, lactic acid bacteria, lactoferrin, isoflavones, prune, chitin, chitosan, glucosamine, etc. .

The excipient is generally not limited as long as it is a desired dosage form, and examples thereof include powders such as microparticles of cerium oxide; sucrose fatty acid esters, crystalline cellulose/carboxymethylcellulose sodium, and phosphoric acid. Hydrogen calcium; wheat starch, rice starch, corn starch, potato starch, dextrin, cyclodextrin and other starches; crystalline cellulose; lactose, glucose, sugar, reduced maltose, starch syrup, fructo-oligosaccharide And saccharides such as emulsified oligosaccharides; sugar alcohols such as sorbitol, erythritol, xylitol, lactitol, and mannitol.

Examples of the flavoring agent include a mandarin extract of a fruit juice extract, a lychee extract, an apple juice, a citrus juice, a grapefruit extract, a peach flavor, a plum flavor, and a sweetener potassium acesulfame K (acesulfame K). ); Alcohol, oligosaccharides, mannose, xylitol, heterosexual sugar, tea green tea, oolong tea, Lagerstroemia speciosa tea, Eucommia tea, Tieguanyin tea, 薏苡 tea, espresso tea, Tea, kumbu tea, yogurt and other flavors.

A coloring agent, a preservative, a tackifier, a stabilizer, a gelling agent, and an antioxidant can be suitably selected from those well-known for use in foods and drinks.

The form of the whitening agent and the melanin production inhibitor of the present invention may be in the form of an ampoule, a capsule, a pill, a tablet, a powder, a granule, a solid, a liquid, a gel, or a bubble or a cream.

Specifically, for example, a beauty/health drink or a food, a pharmaceutical, a western-style snack, a dim sum, a chewing gum, a candy, a milk candy, or the like; a general refreshing drink such as a fruit juice; a fish plate; Bamboo products and other processed aquatic products; sausages, ham and other livestock products; noodles, cooked noodles, soba noodles, etc.; sauce, sauce, sauce, tare, sugar, honey, starch powder, starch Seasonings such as syrup; spices such as curry powder, mustard powder, and pepper; jam, marmalade, chocolate sauce; cheese, cream, yogurt, etc. Preferably, a beauty/health drink or a beauty/health food or the like which is orally administered for good ingestion can be cited.

Further, these systems can be produced by a conventionally known method.

Further, the whitening agent and the melanin production inhibitor of the present invention can be formulated into a composition such as an external preparation for skin by the effect of percutaneous absorption. Examples of the form of the external preparation for skin include a cosmetic, a patch, a pharmaceutical, and the like.

For external use on the skin, in addition to the active ingredient tea abalone B, visible It is suitable for blending with ingredients suitable for external preparations for skin such as cosmetics or pharmaceuticals, for example, moisturizers, antioxidants, oily ingredients, ultraviolet absorbers, surfactants, tackifiers, alcohols, powder ingredients, Colorants, aqueous ingredients, water, various skin nutrients, and the like.

In the external preparation for skin containing the whitening agent of the present invention, it is suitable to formulate an effective amount of the tea belly acid B. In the total amount of the external preparation for skin, the blending amount of the tea and the acid B is particularly preferably 0.001 to 5.0% by mass. If the amount of blending is too small, the whitening effect cannot be fully exerted, and even if the blending amount is too large, the corresponding significant lifting effect cannot be achieved, which is not preferable.

(Example)

The following examples are given in further detail to the invention, but the invention is not limited thereto.

For the animals used in the following experiments, DBA/2 mouse males (CHARLES RIVER LABORATORIES JAPAN Co., Ltd.) were used. Mice that were 5 weeks old were used and domesticated for 1 week.

In addition, the mice were allowed to freely ingest sterile distilled water and feed AIN-93G (Nippon Agritec Co., Ltd.).

Vitexin and isovitexin are commercially available (SIGMA-ALDRICH Co., Ltd.), and the tea abalone B is a well-known method (J. Agric. Food Chem. 2009, 57, 6779-6786) Separated from tea. Then, using the above animals, the melanocyte activation inhibition test was carried out by the following test method.

Further, vitexin and isovite are flavonoids contained in tea, respectively, in the same manner as the tea buckwheat acid B.

‧ Melanocyte activation inhibition test method

On the 9th day, the mice were orally administered with vitexin or isovite or tea abalone B (1 mg/kg body weight (bw)) into the stomach, and irradiated after administration. The amount of ultraviolet light (UVB) is 120mJ. Similarly, the vehicle was administered to the control group (non-UV group irradiated) and the control group (UV irradiation group). Further, each group was tested with 8 mice.

In this test, the medium and its dosage were carried out in a 0.5 w/v% methylcellulose 400 solution, 5 mL/kg body weight (b.w.).

The skin was taken on the 10th day for DOPA reaction. The number of DOPA-positive melanocytes per unit area was calculated under microscope observation.

The results are shown in Figure 1. In addition, the * in the figure is statistically processed by the Student t test (significant level *p<0.05, **p<0.01), indicating that it can be confirmed relative to the control group (UV irradiation group) ) is significantly worse.

According to Fig. 1, vitexin, which has a flavonoid structure similar to that of catechu B, has a tendency to suppress an increase in the number of melanocytes, but is not significantly inhibited. Further, isovite having a flavonoid similar in structure to agaric acid A significantly inhibited the increase in the number of melanocytes.

Surprisingly, it was surprising that the tea amphoteric acid B significantly inhibited the increase in the number of melanocytes.

Next, the present inventors conducted a melanocyte activation inhibition test in the same manner as the above test method using tea amphoteric acid A and tea belly acid B as samples. The results are shown in Figure 2.

According to Figure 2, it was confirmed that by irradiating UV, DOPA-positive melanin The number of cells was significantly increased (UV irradiation group). The tea amphoteric acid A and the tea amphoteric acid B system significantly inhibited the increase in the number of melanocytes. However, it is clear that the tea Brine An acid B system significantly inhibited the increase in the number of melanocytes compared to the tea albino A.

Therefore, the whitening agent and the melanin production inhibitor of the present invention are characterized by containing a tea succinic acid B.

Hereinafter, examples of the formulation of the tea succinic acid B of the whitening agent of the present invention and the melanin production inhibitor are listed. However, the present invention is not limited to this.

Figure 1 is a graph showing the effect of vitexin, isovite, and catechin B on the activation of UVB epidermal melanocytes.

Fig. 2 is a graph showing the effect of tea amphoteric acid A and tea belly acid B on the activation of UVB epidermal melanocytes.

The drawings in this case are all experimental data charts, which are not enough to represent the technical characteristics of this case.

Claims (4)

A use of a tea belly acid B for the manufacture of a melanin production inhibitor which is orally administered and which comprises an effective amount of tea belly acid B. A use of a tea belly acid B for producing a melanin production inhibitor which is applied to the skin and which comprises an effective amount of tea belly acid B. The use of the tea amphoteric acid B as a whitening agent, as claimed in claim 1 or 2. The use according to the first aspect of the invention, wherein the tea amphoteric acid B is administered at a dose of 0.001 mg/kg body weight (b.w.) or more per day.