JP5230212B2 - Melanin production inhibitor and whitening agent containing the same - Google Patents

Description

  The present invention relates to a melanin production inhibitor. Furthermore, this invention relates to the whitening agent containing the said melanin production inhibitor.

  Since various pollen such as cedar and ragweed cause hay fever, pollen is now recognized as an allergen. Moreover, since pollen stimulates the immune system, the pharmacological action of pollen on the immune system has also been studied.

  Patent Document 1 describes that a culture in which pollen is fermented with lactic acid bacteria, bifidobacteria, or yeast has a skin regeneration action, an anti-wrinkle action, and the like, and is blended in pharmaceuticals and cosmetics.

  Patent Document 2 describes that an oil body can be obtained from pollen derived from rapeseed.

  Pollen has a high nutritional value and is known to be used as a nutritional food either directly or wrapped in sugar (Non-patent Document 1).

Patent Document 3 discloses a soft capsule of an extract made from pollen of thymus, corn, hazel, rye, pussy willow, box willow, French peony or pine, and the capsule is suitable for prostatitis and benign prostatic hyperplasia. It is described as having an inhibitory action.
JP-T-2001-504510 Japanese translation of PCT publication No. 2002-503268 Japanese Patent Laid-Open No. 9-278665 "Bees Science" 7 (1): 9-12 Honeybee Science (1986)

  An object of the present invention is to provide these new uses based on physiological activities newly found for pollen, pollen load or extracts thereof. Specifically, it aims at providing the use as a melanin production inhibitor and the use as a whitening agent about pollen, pollen load, or these extracts.

  As a result of studying the bioactive action of pollen, pollen load or these extracts, the present inventor has found pollen load extracts such as rapeseed, buckwheat, tea, watermelon, corn, cistus, Jara and Mali, particularly water and alcohol. It has been found that an extract of a polar solvent has an excellent inhibitory effect on melanin production.

  The present invention has been completed based on such findings, and provides the following melanin production inhibitor and whitening agent.

I. Melanin production inhibitor (I-1) A melanin production inhibitor comprising as an active ingredient at least one selected from the group consisting of pollen, pollen cargo and extracts thereof.
(I-2) The above-mentioned pollen or pollen load is derived from at least one plant selected from the group consisting of Brassicaceae, Tadaceae, Camellia, Hanicyceae, Gramineae and Eucalyptus, The melanin production inhibitor described in I-1).
(I-3) The melanin production inhibitor according to (I-2), wherein the plant is at least one selected from the group consisting of rapeseed, buckwheat, tea, watermelon, corn, cistus, jala, and Mali.
(I-4) Pollen or pollen-loaded water, ethanol or a mixture thereof of at least one plant selected from the group consisting of rapeseed, buckwheat, tea, watermelon, corn, cistus, jala, and Mali The melanin production inhibitor described in (I-1), which is an extract by a solvent.

II. Whitening agent (II-1) A whitening agent comprising the melanin production inhibitor described in any of (I-1) to (I-4) above.

In addition, the said whitening agent can also be paraphrased as follows.
(II-a) A whitening agent comprising as an active ingredient at least one selected from the group consisting of pollen, pollen cargo and extracts thereof.
(II-b) The above-mentioned pollen or pollen load is derived from at least one plant selected from the group consisting of Brassicaceae, Taceae, Camellia, Hanicyceae, Gramineae and Eucalyptus, The whitening agent described in II-a).
(II-c) The whitening agent according to (II-b), wherein the plant is at least one selected from the group consisting of rapeseed, buckwheat, tea, watermelon, corn, cistus, jala, and Mali.
(II-d) The extract is pollen or pollen water, ethanol or a mixture of at least one plant selected from the group consisting of rapeseed, buckwheat, tea, watermelon, corn, cistus, jala, and Mali. The whitening agent as described in (II-a) which is an extract by a solvent.

  Melanin pigments that cause skin coloring are produced by pigment cells (melanocytes) in the skin tissue. Pigmentation such as skin spots and freckles occurs due to abnormal deposition of melanin as a result of activation of pigment cells due to stimulation by ultraviolet exposure from sunlight, hormonal abnormalities, or genetic factors. It is thought to do. Normally, melanin is metabolized by metabolism (turnover) of skin tissue, but a decrease in metabolism of skin tissue with aging also causes pigmentation.

  As shown in the test examples described later, pollen, pollen load or these extracts have an action of suppressing melanin production, and thus have an effect of whitening (improvement of pigmentation and dullness), a melanin production inhibitor, In addition to being useful as an active ingredient of a whitening agent, it is useful as an active ingredient of an external skin preparation (especially a cosmetic) that has an effect of whitening. In particular, the water-containing ethanol extract of tea, corn, jallah or Mali pollen load strongly suppresses the production of melanin, and therefore, a melanin production inhibitor, a whitening agent, and a skin external agent that has an effect on whitening (especially cosmetics). It is excellent as an active ingredient.

  The cosmetic containing the whitening agent of the present invention has an excellent whitening action, has a skin-beautifying effect, such as pigmentation after sunburn, lightening of spots, freckles, erythema, etc. Since the skin can be maintained, it is useful as an external preparation for skin, particularly as a whitening cosmetic, a beautiful skin cosmetic, a skin care cosmetic and the like.

(I) Melanin production inhibitor The melanin production inhibitor of the present invention is characterized by containing pollen, pollen cargo or an extract thereof as an active ingredient.

  Here, the pollen load is made by bees hardened with nectar, and is also called pollen dumpling. The pollen load is stored in the nest with honey. This pollen load can be easily collected.

  In the present invention, either pollen or pollen cargo may be used, but pollen cargo is preferably used because it is easily available in the above points. In addition, although pollen and pollen load can each be used independently, both can also be mixed and used.

  As a source of pollen or / and pollen load (hereinafter simply referred to as “pollen / pollen load”) of the present invention, the following table shows the family name, genus / species name, and Japanese name (name) of a suitable plant. It is shown in 1.

  That is, preferred plants from which the pollen / pollen load used in the present invention is derived include plants belonging to the Brassicaceae, Tadeidae, Camelliaaceae, Hannibalidae, Gramineae, and Eucalyptus families. Specifically, examples of Brassicaceae plants include araseito, rapeseed, and Japanese radish. Rapeseed is more preferable. An example of a plantaceae is buckwheat. As the camellia plant, sasanqua, tea, nuts, and camellia are preferably exemplified. More preferred is cha. Preferred examples of the plant belonging to the family Canniaceae are cistus. Maize is preferably exemplified as the gramineous plant. Examples of Eucalyptus plants are preferably Mali and Jara.

  More preferably, the active ingredient of the melanin production inhibitor is Cha, which is a camellia plant, Maize, which is a Gramineae plant, Mali and Jara, which is a Eucalyptus plant.

  Pollen / pollen load can be used as it is, but can also be used in the form of an extract prepared with an appropriate solvent.

  Here, the pollen / pollen load can be extracted with a solvent such as water, a water-containing solvent, and an organic solvent. Specifically, water, lower alcohol (methanol, ethanol, n-propanol, isopropanol, etc.), ketones (acetone, methyl ethyl ketone, methyl butyl ketone, etc.), esters (methyl acetate, ethyl acetate, etc.), ethers (diethyl) Ether, diisopropyl ether, etc.), aromatic hydrocarbons (toluene, xylene, etc.), halogenated hydrocarbons (methylene chloride, chloroform, etc.), glycols (ethylene glycol, propylene glycol), glycol ethers (methyl cellosolve, 1, 2 -Dimethoxyethane), glycerin, tetrahydrofuran, acetonitrile, acetic acid, propionic acid, acetamide, dimethylformamide, dimethylsulfoxide. Moreover, even if these extraction solvents are used by 1 type, 2 or more types can also be combined arbitrarily and can also be used as a liquid mixture. Preferably, water, lower alcohol (preferably ethanol) or a mixture thereof (hydrous alcohol, preferably hydrous ethanol).

  Extraction is performed by adding pollen / pollen load to the solvent, extracting at 30 ° C. to 24 ° C. for about 30 minutes to 24 hours, and then removing the insoluble matter. This can be done easily.

  In the present invention, the above-mentioned pollen / pollen load extract can be used as it is as a melanin production inhibitor, but if necessary, a solution obtained by concentrating the extract (concentrated solution) or freezing of the extract Dry products such as dried products and spray-dried products can also be used.

  The extract thus obtained may be subjected to treatment such as decolorization, masking or deodorization as necessary in order to remove the color, taste or odor. Examples of such treatment include adsorption treatment with activated carbon and the like, purification by column chromatography, ion exchange chromatography, and the like.

  Among the pollen load extracts of various plants (Table 1), the extract of the tea pollen load (preferably a hydrous ethanol extract) which is a camellia plant, the extract of the corn pollen load (preferably a rice plant) Is a water-containing ethanol extract), and the Eucalyptus plant Mali and Jara pollen extract (preferably a water-containing ethanol extract) has an excellent inhibitory effect on melanin production, and is an active ingredient of a melanin production inhibitor. And as an active ingredient of a whitening agent.

  In the melanin production inhibitor of the present invention, the blending amount of pollen / pollen cargo or an extract thereof is not particularly limited as long as it has a melanin production inhibitory action, but is 0.0001 to 100% by weight, preferably 0, in terms of dryness. 0.001 to 50% by weight, more preferably 0.01 to 25% by weight.

  The melanin production inhibitor of this invention has the effect | action which suppresses the production of melanin, and can be conveniently used as an active ingredient of the cosmetics which have the effect of whitening as an active ingredient of a whitening agent.

(2) Whitening agent The whitening agent of the present invention is characterized by containing the melanin production inhibitor described above as an active ingredient. The ratio of the melanin production inhibitor to be blended with the whitening agent is not particularly limited as long as it has a whitening action based on the melanin production inhibitory action of the melanin production inhibitor. Usually, however, the amount of pollen / pollen load or their extract In terms of (converted to dry matter), 0.0005 to 20% by weight, preferably 0.001 to 10% by weight, more preferably 0.01 to 1% by weight.

  The whitening agent can be suitably used as an external preparation for skin that has an effect of whitening (including prevention and reduction of spots and dullness), preferably as an active ingredient of cosmetics.

  You may mix | blend conventionally well-known whitening agent with the whitening agent of this invention in combination with pollen / pollen load or these extracts. In addition, ingredients commonly used in cosmetics, such as humectants, antioxidants, oily ingredients, UV absorbers, surfactants, thickeners, alcohols, powder ingredients, color materials, aqueous ingredients, water, various A skin nutrient or the like can be appropriately blended as necessary.

  The dosage forms of the whitening agent of the present invention are aqueous solution system, solubilization system, emulsification system, powder system, oil liquid system, gel system, ointment system, aerosol system, water-oil two-layer system, and water-oil-powder 3 A wide range of dosage forms such as layer systems can be adopted. Examples of the form include lotion, milky lotion, cream, gel, essence, cosmetic liquid, pack, mask and the like.

  The whitening agent of the present invention can also be used as a skin external preparation having an effect of whitening, particularly as an active ingredient of cosmetics. In this case, the blending ratio of the whitening agent to the external preparation for skin (preferably cosmetics) is not particularly limited as long as the external preparation for skin exhibits a whitening effect, but it is converted into the amount of pollen / pollen cargo or their extract. (In terms of dry matter), 0.0005 to 20% by weight, preferably 0.001 to 10% by weight, and more preferably 0.01 to 1% by weight. The form of the external preparation for skin is not particularly limited. For example, when the external preparation for skin is a basic cosmetic, examples of the form include lotion, milky lotion, cream, gel, essence, cosmetic liquid, pack, and mask. In addition, if the external preparation for skin is a makeup cosmetic, examples of the form include foundation, lipstick, blusher, eye shadow, eyeliner, mascara and the like. Other forms include face wash, massage agent, cleansing agent, after shave lotion, pre-shave lotion, shaving cream, body soap, soap and the like.

  EXAMPLES Hereinafter, although an Example, a test example, and a formulation example demonstrate this invention in detail, this invention is not limited at all by these Examples.

Example 1 Preparation of water-containing ethanol extract of pollen cargo 70 g by volume of water-containing ethanol (ethanol: purified water = 7: 2 g) each of pollen cargo (rapeseed, buckwheat, tea, watermelon, corn, cistus, jala, mari) 3 (v / v)) was added, and the mixture was shaken and mixed at room temperature for 1 hour. Thereafter, the mixture was centrifuged at 2500 rpm for 20 minutes to obtain a supernatant and a precipitate. To the resulting precipitate, 10 ml of 70% by volume hydrous ethanol was added, and the same treatment (extraction and centrifugation) as above was performed. The supernatants obtained by a total of three treatments were combined and centrifuged at 8000 rpm for 40 minutes, and the supernatants were collected. The supernatant thus obtained was subjected to a rotary evaporator to remove ethanol to some extent and then freeze-dried. This was used as a water-containing ethanol extract (dried product) of pollen of each plant (rapeseed, buckwheat, tea, watermelon, corn, cistus, Jara, Mali).

Test Example 1 Melanin production inhibition test (1)
Using the hydrous ethanol extract of the pollen load (rapeseed, tea, corn, cistus, jallah, mari) prepared in Example 1, the melanin production inhibitory action was measured by the following method.

(1) Cell culture mouse-derived B-16 melanoma cells were used as test cells. Specifically, using a 6-well plate for cell culture, the cells are placed in 3 ml of 10% FBS (fetal bovine serum) -containing E-MEM medium per well so that the number of cells becomes 1 × 10 ^5. After seeding, the cells were cultured overnight at 37 ° C. in 5% CO ₂ -95% air. Thereafter, the medium was replaced with the medium containing the test sample, and cell culture was performed for 3 days under the same conditions as described above. The medium containing the test sample was prepared by adding the test sample dissolved in 70% by volume aqueous ethanol to 10% FBS-containing E-MEM medium and further adding theophylline to a final concentration of 2 mM. Table 2 shows the amount of the test sample added to the medium. After culturing for 3 days, the cells were collected, and the amount of melanin produced was measured according to the following method.

  In addition, as a control test, instead of the test sample, cell culture was performed in the same manner using 70 vol% aqueous ethanol equal to the test sample solution, and the melanin production amount of the cell was measured (control).

(2) Evaluation of inhibitory action on melanin production Cells collected by the above cell culture are dissolved in 1N NaOH (containing 10 wt% DMSO), the amount of protein is measured, and each solution is diluted to a uniform protein concentration. The absorbance at 405 nm was measured. From the obtained absorbance, the melanin production inhibition rate (%) was calculated according to the following formula. The results are shown in Table 2.

  From the above results, it was revealed that the pollen load extract of the present invention (rapeseed, tea, corn, cistus, Jara, Mali) has a melanin production inhibitory action. In particular, pollen-loaded extracts of tea, corn, Jara and Mali had an excellent melanin production inhibitory action. From this, these pollen load extracts are considered useful as a melanin production inhibitor based on the melanin production inhibitory action, and as a whitening agent and an active ingredient of cosmetics that have a whitening effect.

Test Example 2 Melanin Production Inhibition Test (Part 1)
The melanin production inhibitory effect was measured in the same manner as in Test Example 1 using the water-containing ethanol extract of pollen cargo (buckwheat and watermelon) prepared in Example 1 as a test sample.

  The results are shown in Table 3.

  From the above results, it was revealed that the pollen load extract (buckwheat, watermelon) of the present invention has a melanin production inhibitory action. From this, these pollen load extracts are considered useful as a melanin production inhibitor based on the melanin production inhibitory action, and as a whitening agent and an active ingredient of cosmetics that have a whitening effect.

Formulation Example 1-2 : Whitening agent which has a lotion form Using each component shown in the following Table 4, the whitening agent which has a lotion form was prepared according to the conventional method.

Formulation Examples 3-4 : Whitening agent having a cosmetic liquid form Using each component shown in Table 5 below, a whitening agent having a cosmetic liquid form was produced according to a conventional method.

Formulation Examples 5 to 7 : Whitening agent having emulsion form An emulsion was prepared according to a conventional method using each component shown in Table 6 below.

Claims (3)

The active ingredient is at least one selected from the group consisting of pollen, pollen load and extracts thereof, and the pollen or pollen load is selected from the group consisting of rapeseed, tea, watermelon, corn, cistus, jala and mari A melanin production inhibitor derived from at least one plant. The extract is an extract of pollen or pollen-loaded water, alcohol or a mixed solvent thereof of at least one plant selected from the group consisting of rapeseed, tea, watermelon, corn, cistus, jara and Mali. Item 2. A melanin production inhibitor according to Item 1. The whitening agent formed by mix | blending the melanin production inhibitor described in Claim 1 or 2 .