JP2003267873A - Demelanizing agent and bleaching ingredient composed of ergosterol derivative and composition containing ergosterol derivative - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a substance effective for bleaching of the suntan skin after ultraviolet irradiation and for preventing, ameliorating and treating pigmentation of the skin such as stains, freckles, liver spots, etc., and a composition containing the same. <P>SOLUTION: The demelanizing agent and the bleaching ingredient comprise an ergosterol derivative represented by formula (1). The demelanizing agent and the bleaching ingredient contain an ergosterol derivative represented by formula (1). The composition for demelanization and the composition for bleaching comprise the ergosterol derivative represented by formula (1). The cosmetic, the medicine and the skin care preparation comprise the ergosterol derivative represented by formula (1). The demelanizing food and the bleaching food comprise the ergosterol derivative represented by formula (1). <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a melanin production inhibitor and a whitening agent consisting of an ergosterol derivative, and a composition containing the ergosterol derivative, especially a cosmetic,
Pharmaceuticals, external preparations for skin, and foods. More specifically, melanin that suppresses melanin production in melanocytes, can whiten sunburned skin after UV irradiation, and can prevent, improve and treat skin pigmentation such as spots, freckles, and liver plaques due to sunburn. The present invention relates to a production inhibitor, a whitening agent, and a composition, particularly cosmetics, medicines, external preparations for skin, and foods.

[0002]

2. Description of the Related Art Pigmentation of skin such as spots, freckles, and liver plaques due to sunburn etc. occurs with age, and increases or hardly disappears with age, which is a problem for middle-aged and older people. ing. Although the onset mechanism of these pigmentation has not been clarified yet, melanin pigments are produced in melanin-producing granules called melanosomes in melanocytes present in epidermal cells by sunburn due to sun rays (especially ultraviolet rays), etc. It is believed that this is caused by the diffusion of the formed melanin pigment into adjacent cells.

There is a strong demand for development of a substance capable of recovering such pigmentation to a normal skin color, and many substances have been commercialized so far. For example,
L-ascorbic acid, kojic acid, hydroquinone and the like are known.

However, L-ascorbic acid has a difficulty in stability, and kojic acid has been confirmed to have an effect, but
Its effect is weak. On the other hand, although hydroquinone has been confirmed to have an effect for the time being, it has irritation and allergenicity, has a problem in safety, and has a problem in being incorporated as a drug. Therefore, at present, no substance having sufficient pigmentation preventing and improving effects is known.

[0005]

SUMMARY OF THE INVENTION The present invention has been made in view of the above circumstances, and its object is to whiten sunburned skin after irradiation with ultraviolet rays, and for pigments on skin such as spots, freckles and melasma due to sunburning. It is an object of the present invention to provide a substance effective for prevention, improvement and treatment of deposits and a composition containing the substance.

[0006]

As a result of intensive studies to solve the above problems, the present inventors have found that the extract of Kazuno Reishi has an inhibitory effect on melanin production,
Further, it was found that the ergosterol derivative having a specific structure obtained by fractionating the extract using a separation and purification means has a strong melanin production inhibitory action and a whitening action, and the above problems can be solved, Has been completed.

That is, the present invention provides the following formula (1):

[Chemical 2] A melanin production inhibitor and a whitening agent consisting of an ergosterol derivative represented by

Further, the present invention is a melanin production inhibitor and a whitening agent containing the ergosterol derivative represented by the above chemical formula 2.

Further, the present invention is a melanin production inhibiting composition and a whitening composition containing the ergosterol derivative represented by the above chemical formula 2.

The present invention is also a cosmetic containing the ergosterol derivative represented by the above chemical formula 2, and the cosmetic can be used for suppressing melanin production and whitening.

Further, the present invention is a medicine containing the ergosterol derivative represented by the above chemical formula 2, and the medicine can be for suppressing melanin production and for whitening.

Further, the present invention is a skin external preparation containing the ergosterol derivative represented by the above chemical formula 2, and the skin external preparation can be used for suppressing melanin production and whitening.

The present invention also provides a melanin production suppressing food and a whitening food containing the ergosterol derivative represented by the above chemical formula 2.

[0014]

BEST MODE FOR CARRYING OUT THE INVENTION Embodiments of the present invention will be described in detail below.

The following equation (1) used in the present invention:

[Chemical 3] It is known that the ergosterol derivative represented by can be conventionally extracted from mushrooms (Maitake) [Takaaki I
shizuka, et.al.Chemi.Pharm.Bull.45 (11) 1756-1760 (199
7)], a known substance. However, the ergosterol derivative represented by Chemical formula 3 (hereinafter simply referred to as Chemical formula 3)
Has an effect of suppressing melanin production and is not known to have a skin whitening effect.

Chemical formula 3 can be isolated from fungi,
Although any fungus including the chemical formula 3 can be used for the production of the above, it is convenient to use ganoderma such as Kazuno ganoderma. It can also be prepared by chemical synthesis. Isolation of chemical formula 3 from fungi containing chemical formula 3 can be performed as follows. That is, the fruiting bodies of fungi or hyphae, partial parts such as spores are preferably crushed, and then immersed in an extraction solvent or heated under reflux in the extraction solvent, and then insoluble matter is removed by filtration, centrifugation or the like. The obtained extraction solution may be optionally concentrated and then isolated by a known separation and purification means.

The solvent used for extraction may be a solvent usually used for extraction of fungi, plants and the like. For example, alcohols such as methanol and ethanol, organic solvents such as acetone and ethyl acetate, and water may be used alone or in combination. You can The extraction method may be an ordinary method, generally, the extraction temperature is in the range of 0 to 100 ° C., preferably 40 to 70 ° C., and the extraction time is 1 to 168 hours, preferably 2
4 to 72 hours. Isolation from the extraction solution can be performed, for example, by
It can be performed by chromatography such as reverse phase chromatography, gel filtration column chromatography, liquid chromatography and the like.

Specific examples of the extraction of fungi and the isolation of chemical formula 3 will be given below. [Purification Example] The cultivated Kazuno Reishi fruiting bodies were crushed, then immersed in ethanol and extracted at 40 ° C for 72 hours. Then, the insoluble material was removed by filtration, the obtained extraction solution was concentrated, and then purified by reverse phase chromatography.
The structure of the purified product was obtained by mass spectrometry gas chromatography,
Determined by NMR. The compound is 5α, 8α-epidioxy- (22E, 24R) -ergosta-6,22-dien represented by the formula (1).
It was -3β-ol.

The chemical formula 3 of the present invention has a melanin production suppressing action and a whitening action as described later. Therefore,
It can be used as a melanin production inhibitor and a whitening agent. Further, as a melanin production inhibitor and a whitening agent containing Chemical formula 3, as a composition, a melanin production inhibiting composition and a whitening composition, that is, for the prevention and treatment of symptoms related to melanin production inhibition and whitening. The composition can be applied to various cosmetics, pharmaceuticals, foods, etc. in the fields of cosmetics, pharmaceuticals and foods.

The composition of the present invention can take both oral (internal) and parenteral (external) forms. For oral use, the composition of the present invention is prepared in the form of, for example, a drug or food. In the case of parenteral use, it can be prepared in the form of cosmetics, quasi drugs, pharmaceuticals, external preparations for skin and the like.

In the case of incorporating the chemical formula 3 into the composition of the present invention, it is most preferable to use the pure chemical formula 3, and in principle, the method is as follows. It may be mixed in the form of extract.

Hereinafter, the specific composition of the present invention containing the chemical formula 3 will be described in more detail by use. The cosmetics, which is the first use of the present invention, includes, for example, ointments, solutions, creams, emulsions, lotions, lotions, gels, essences (foundations), foundations, packs / masks, lipsticks, sticks, bath agents, etc. It is widely applicable as a cosmetic containing a quasi drug such as an external preparation for skin.

The dosage form of the cosmetics is also solution type, solubilizing type, emulsion type, powder type, powder dispersion type, oil liquid type, gel type, ointment type, aerosol type, water-oil two-layer type, water. A wide range of dosage forms can be adopted, such as an oil-powder three-layer system.

The compounding amount of Chemical Formula 3 in the cosmetic of the present invention is preferably 0.001 to 20% by weight, more preferably 0.01 to 16% by weight, and further preferably 0.1 to 10% by weight based on the total amount of the cosmetic.
It is 12% by weight. Most preferred is 1 to 10% by weight. Since the cosmetic of the present invention has a melanin production suppressing action and a whitening action, it is used as a melanin production inhibiting cosmetic and a whitening cosmetic. In addition, the cosmetic of the present invention can be preferably applied to the use as a skin external preparation, and is therefore used as a skin external preparation for suppressing melanin production and a skin external preparation for whitening.

The pharmaceutical agent of the second use of the present invention may be administered orally or parenterally, and may be in the form of a pharmaceutical preparation suitable for each method. Examples of pharmaceutical preparations include liquids, syrups, injections, inhalants, liquids such as emulsions, tablets, powders, granules,
Solid agents such as capsules and inhalants, external preparations for skin such as ointments,
Examples thereof include external preparations such as suppositories.

The compounding amount of Chemical Formula 3 in the pharmaceutical preparation is 0.0 in the total amount.
It can be contained in an amount of 01 to 30% by weight. Preferably 0.01 to 20% by weight, most preferably 0.1 to 1
It is 0% by weight. The dose may be appropriately changed based on the age and weight of the patient, the route of application, the degree of progress of the disease and the treatment being performed in parallel, and although it is not specified, it is generally per day. About 4 to 10 ml can be administered once a day or in 2 to 3 divided doses,
It is not limited to this. The medicament of the present invention has a melanin production inhibitory action and a whitening action, and thus is used as a melanin production inhibitory drug and a whitening drug. Also,
Since the pharmaceutical agent of the present invention can be preferably applied to the use as a skin external preparation, it is used as a skin external preparation for suppressing melanin production and a skin external preparation for whitening.

The food which is the third use of the present invention is useful as a so-called health food, for example, confectionery,
It is widely applicable as beverages such as soft drinks, processed vegetables or fruits, meat products, seasonings and the like. As its form,
Powders, solid products, solutions, etc. The compounding amount of Chemical Formula 3 in the food can be appropriately changed depending on the purpose, the product form and the like. Generally, in the case of solutions such as drinks, for example, 30
In ml, 0.001 to 10 mg, preferably 0.01 to
5 mg, more preferably 0.15-1 mg. Also,
In the case of powdered solid products such as tablets, for example, 300 mg
Among them, the amount is 0.001 to 10 mg, preferably 0.01 to 5
mg, more preferably 0.1 to 1 mg. Since the food of the present invention has a melanin production suppressing action and a whitening action, it is used as a melanin production inhibiting food and a whitening food.

The composition of cosmetics, medicines, foods, etc. of the present invention may contain other components usually used in cosmetics, medicines, foods, etc. in addition to the above-mentioned Chemical Formula 3 within the range that does not impair the effects of the present invention. It can be blended.

For example, cosmetics include oil, powder, surfactant, moisturizer, thickener, lower alcohol, film-forming agent,
UV absorbers, sequestering agents, organic amines, pH
Examples include regulators, medicinal ingredients, sugars, preservatives, vitamins, other whitening agents, antioxidants, fragrances, and water.

Examples of the oil component include natural oils and fats such as jojoba oil, olive oil, avocado oil, castor oil, coconut oil, beef tallow, hydrogenated oil and their derivatives, waxes such as carnauba wax, beeswax and lanolin, liquid paraffin, microcrystalline wax. Hydrocarbons such as squalane, higher fatty acids such as stearic acid, cetyl alcohol, higher alcohols such as stearyl alcohol, triglyceride octanoate, isopropyl myristate, diisostearyl malate, glycerin di-2-heptylundecanoate,
Trimethylolpropane tri-2-ethylhexylate,
Examples thereof include esters such as di-2-ethylhexyl sebacate, mint oil, essential oils such as rose oil and citronellal, and silicone oils such as dimethylpolysiloxane and decamethylcyclopentasiloxane. The content of these oily components in the cosmetic is appropriately selected according to the form, dosage form, etc. of the cosmetic, but it can usually be 0.1 to 95% by weight in the total amount of the cosmetic.

Examples of powders include talc, mica, kaolin, silica, zinc white, mica titanium, titanium oxide, iron oxide, nylon powder and the like.

Examples of the surfactant include polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester,
Nonionic surfactants such as glycerin fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitol fatty acid ester, polyoxyalkylene modified polysiloxane, anionic surfactant such as sodium palmitate, cationic interface such as stearyltrimethylammonium chloride Examples include active agents, amphoteric surfactants such as betaine, amidobetaine, sulfobetaine, and imidazolinium.

Examples of moisturizers include glycerin, 1,3
-Butylene glycol, polyethylene glycol, dipropylene glycol, sorbitol and the like.

Examples of the thickener include water-soluble polymers such as carboxyvinyl polymer, carboxymethyl cellulose and polyvinyl alcohol, and clay minerals such as bentonite.

Examples of ultraviolet absorbers include para-aminobenzoic acid (hereinafter abbreviated as PABA), glyceryl PABA,
Ethyldihydroxypropyl PABA, octyl methoxycinnamate, 2-ethoxyethyl-p-methoxycinnamate, 2,4-dihydroxybenzophenone, 2
-Hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4-methylbenzophenone, 2
-Hydroxy-4-methoxy-4-methylbenzophenone sulfonate, urocanic acid ethyl ester, 2-phenyl-5-methylbenzoxazole, 4-methoxy-
4-t-butyldibenzoylmethane, ethylhexyl paramethoxycinnamate and the like can be mentioned.

Examples of the sequestering agent include tetrasodium edetate and citric acid. Examples of the lower alcohol include ethanol and the like. Examples of organic amines include monoethanolamine and triethanolamine. Examples of pH adjusters include:
Buffering agents such as lactic acid-sodium lactate and citric acid-sodium citrate can be mentioned.

Examples of the medicinal component include pantotenyl ethyl ether, glycyrrhizinate, and the like. Examples of vitamins include vitamin C or its derivative, vitamin E or its derivative, and the like. Examples of antioxidants include tocopherols, dibutylhydroxytoluene, propyl gallate, and the like.

Examples of saccharides include erythritol, sucrose, hyaluronic acid and the like. Examples of preservatives include ethylparaben, butylparaben, sodium benzoate and the like. Examples of the whitening agent include ascorbic acid or its derivative, kojic acid or its derivative, licorice extract, hydroquinone derivative, glutathione and the like.

Next, as pharmaceuticals, excipients, stabilizers, wetting agents, emulsifiers, absorption promoters, pH adjusters, surfactants,
Various additives such as a diluent and a carrier can be blended. Specific examples of these additive components include, for example, starch, sugars such as lactose, magnesium sulfate, talc, gelatin, cellulose derivatives such as hydroxypropyl cellulose, soybean oil, vegetable oil such as sesame oil, animal oil or synthetic oil, Examples thereof include water such as rubber and physiological saline, alcohols such as ethanol, 1,3-butylene glycol and polyalkylene glycol. In addition, it is also possible to select and blend from the components that can be blended in the cosmetic.

Next, as foods, sweeteners, acidulants, preservatives, flavors, colorants, excipients, stabilizers, wetting agents, emulsifiers, absorption promoters, pH adjusters, surfactants, and diluents. , Various carriers such as carriers can be added. Specific examples of these additional components include, for example, mushroom extract,
Carrot extract, ginger extract, extract solution of various foods such as honey, liquid food, and saccharides include cyclic oligosaccharide, reduced maltose, trehalose, lactose, sucrose fatty acid ester and the like. In addition, the above cosmetics,
It is also possible to select and blend from the components that can be blended in the medicine.

The composition of the present invention can be prepared in an arbitrary form and dosage form by a conventional method by mixing the essential components of the present invention with one or more of the above optional ingredients.

[0042]

EXAMPLES The present invention will be specifically described with reference to the following examples. In the compounded amount of the composition, the weight% is used unless otherwise specified.

[Example 1] Melanin production inhibitory effect [Melanin production inhibitory effect in B16 melanoma cells] Melanin production inhibitory effect was obtained by using mouse derived melanocyte B16 10F7 melanoma cells (obtained from Akita Prefectural Food Research Institute). (From the above), a solution obtained by diluting the compound of formula 3 purified in the above-mentioned purification example with a culture medium was allowed to act on cells to observe and evaluate the production of melanin. For B-16 cells, 70% confluent cells were washed with PBS, trypsin was added and detached, and a medium containing the same amount of serum as trypsin (E
-MEM + 10% FBS) was added and the cells were collected and centrifuged (800 rpm, 5 min.). Count the number of cells, about 10 ⁴
The cells / ml (E-MEM + 10% FBS) was adjusted.
Dilute the diluted solution to 2 in the cell culture plate (for adherent cells).
0 μL of sterilized PBS was dispensed, and 20 μL of the compound 3 solution was diluted twice (final concentration in the culture solution was 100 μg / mL to 0.0012).
μg / mL). As controls, arbutin (final concentration in culture medium 140 μg / mL to 0.22 μg / mL) and methanol were also diluted in the same manner.

80 μL of the cell suspension was dispensed to the plate containing the diluted solution. Further, the cells were cultured at 37 ° C. in a CO ₂ incubator for 72 hours, and the melanin production in the cells was observed with a microscope. Furthermore, if melanin is produced, remove the medium and add 300 μL of 1N NaOH.
Then, the amount of melanin produced was evaluated by dissolving melanin and measuring the absorption of ultraviolet light at 470 nm. The value obtained by reacting methanol as a solvent was set to 100%, the dose of Chemical formula 3 and arbutin was changed, and the concentration showing melanin synthesis inhibition at the lowest concentration was determined. The results are shown in Table 1. In addition,
The micrograph of B-1 also showed that B-1 was higher than that of arbutin.
It was also found that the black color of 6 cells was suppressed, and that it had an excellent melanin production inhibitory effect and a whitening effect.

[0045]

[Table 1]

As is apparent from Table 1, it was revealed that the chemical formula 3 showed a higher melanin production suppression effect on melanoma B16 cells than the melanin production inhibitor arbutin.

[0047] [Examples 2-3, Comparative Examples 1-2] Measurement of whitening effect       Ingredient amount (% by weight) (Alcohol phase) Ethyl alcohol 25.0 Polyoxyethylene (25 mol) hydrogenated castor oil 2.0 Antioxidant Appropriate amount Preservative Suitable amount Fragrance suitable amount Test compound (listed in Table 2) Amount listed in Table 2 (Water phase) Glycerin 5.0 Sodium hexametaphosphate Suitable amount Deionized water residual (Production method) After preparing an aqueous phase and an alcohol phase, they are solubilized.

(Test Method) Twenty panelists were exposed to sunlight for a total of 4 hours for two days from 11:00 am to 1:00 pm in summer. The above-mentioned composition (lotion) was applied to the exposed inner skin of the upper arm of the paneler 5 times a day from morning to evening 5 days after the day of exposure to sunlight.

(Evaluation method) The test results after use were evaluated according to the following criteria.

(Judgment criteria) Remarkable effect: Pigmentation was almost inconspicuous. Effective: Pigmentation is very light. Slightly effective: Pigmentation became light. Invalid: No change.

(Judgment) ⊚: 16 or more of the panelists showed more than effective effect. ◯: 11 to 15 of the panelists showed an effect of not less than effective. Δ: 6 to 10 of the panelists showed an effect of not less than effective. X: Five or less of the panelists showed an effect of not less than effective.

The evaluation results are shown in Table 2.

[0053]

[Table 2]

As is clear from Table 2, the composition containing the chemical formula 3 (lotion) prevented deposition of the melanin pigment and showed a whitening effect. On the other hand, no effect was observed when the test compound was not added (Comparative Example 1) or when hydroquinone was blended (Comparative Example 2).

Hereinafter, examples of the present invention in which various formulations are prepared by a conventional method will be shown. In each of the examples, excellent melanin production inhibitory effect and whitening effect were observed.

[0056] [Example 4] Cream       Ingredient amount (% by weight) Stearic acid 6.0 Glycerin monostearate 2.0 polyoxyethylene (20 mol) Solventane monostearate 2.0 1,3-butylene glycol 10.0 Chemical 3 5.0 Isopropyl myristate 12.0 Squalane 5.0 Liquid paraffin 3.0 Vitamin E 0.05 Sodium bisulfite suitable amount Preservative Suitable amount Fragrance suitable amount Deionized water residual

[0057] [Example 5] Emulsion       Ingredient amount (% by weight) Stearyl alcohol 2.0 Squalane 5.0 Liquid lanolin 3.0 Trimethylolpropane trioctanoate 2.0 Glyceryl trioctanoate 5.0 Glycerin monooleate 2.0 Polyoxyethylene (20 mol) Solvent monooleate 1.0 Vitamin C 0.1 Preservative Suitable amount Chemical 3 8.0 Para-aminobenzoic acid 0.1 Fragrance suitable amount Sodium bisulfite suitable amount Glycerin 5.0 Carboxy vinyl polymer 0.2 Triethanolamine 1.0 Purified water residue

[0058] [Example 6] Gel       Ingredient amount (% by weight) Dipropylene glycol 10.0 PEG 1500 5.0 Carboxy vinyl polymer 1.0 Ethyl alcohol 2.0 Polyoxyethylene (50 mol) oleyl alcohol ether 2.0 Potassium hydroxide 0.15 Chemical 3 1.0 2-Hydroxy-4-methoxybenzophenone sodium sulfonate 0.05 Preservative Suitable amount EDTA / 3Na suitable amount Fragrance suitable amount Deionized water residual

[0059] [Example 7] Essence       Ingredient amount (% by weight) Glycerin 5.0 Dipropylene glycol 10.0 Ethanol 10.0 Carboxy vinyl polymer 0.2 Sodium hyaluronate 0.5 Potassium hydroxide 0.1 Polyoxyethylene (20 mol) Solvanane monooleate 0.5 Polyoxyethylene (20 mol) Octyl Tedecanol 1.0 Olive oil 0.15 Placenta extract 0.1 Vitamin E acetate 0.1 Chemical 3 3.0 Sodium bisulfite suitable amount Preservative Suitable amount EDTA / 3Na suitable amount Fragrance suitable amount Purified water residue

[0060] [Example 8] Pack       Ingredient amount (% by weight) Polyvinyl acetate emulsion 15.0 Polyvinyl alcohol 10.0 Dipropylene glycol 5.0 Sorbitol 5.0 Tocopherol acetate 0.2 Olive oil 1.0 Squalane 3.0 Polyoxyethylene (20 mol) Solventane monooleate 1.5 Titanium oxide 5.0 Talc 10.0 Ethanol 7.0 Chemical 3 3.0 Preservative Suitable amount Fragrance suitable amount Purified water residue

[0061] [Example 9] Lotion       Ingredient amount (% by weight) 1,3-butylene glycol 6.0 Glycerin 5.0 Sodium hyaluronate 0.3 Polyoxyethylene (20 mol) Solventane monostearate 1.5 polyoxyethylene (20 mol) Octyl edecanol 0.5 Ethanol 15.0 Chemical 3 4.0 Preservative Suitable amount Fragrance suitable amount Purified water residue

[0062] [Example 10] Ointment       Ingredients Amount (wt%) Polyoxyethylene (30 mol) hydrogenated castor oil 2.0 Glyceryl monostearate 10.0 Squalane 10.0 Vaseline 40.0 Cetanol 6.0 Chemical 3 5.0 1,3-butylene glycol 10.0 Deionized water residual Preservative Suitable amount Fragrance suitable amount

[0063] [Example 11] Foundation       Ingredient amount (% by weight) Talc 3.0 Titanium oxide 5.0 Bengal 0.5 Iron oxide yellow 1.5 Iron oxide black 0.1 Bentonite 0.5 Polyoxyethylene (20 mol) Solventane monostearate 1.0 Triethanolamine 1.0 Glycerin 5.0 Propylene glycol 5.0 Stearic acid 2.0 Glycerin monostearate 10.0 Liquid paraffin 10.0 Dimethyl polysiloxane 5.0 Polyoxyalkylene-modified polysiloxane 3.0 Chemical 3 3.0 Purified water Remaining amount Preservative Suitable amount Fragrance suitable amount

[0064] [Example 12] Healthy drink       Ingredient amount (in 30 mL) Chemical 3 0.085 mg Carrot extract 50mg Cordyceps extract 100 mg Ginger extract 300 mg Honey 150mg Cyclic oligosaccharide 300mg Suitable amount of sweetener Acidulant Suitable amount Preservative amount Fragrance suitable amount Water level

[0065] [Example 13] Healthy drink       Ingredient amount (in 30 mL) Chemical 3 0.5 mg Carrot extract 50mg Cordyceps extract 100 mg Ginger extract 300 mg Honey 150mg Cyclic oligosaccharide 300mg Suitable amount of sweetener Acidulant Suitable amount Preservative amount Fragrance suitable amount Water level

[0066] [Example 14] Health food tablet       Ingredient amount (in 300mg) Chemical 3 0.025mg Reduced maltose 87.8mg Trehalose 41.2mg Lactose 16.5mg Sucrose fatty acid ester 6.2 mg Dextrin 148.275 mg

[0067] [Example 15] Health food tablet       Ingredient amount (in 300mg) Chemical 3 0.5 mg Reduced maltose 87.8mg Trehalose 41.2mg Lactose 16.5mg Sucrose fatty acid ester 6.2 mg Dextrin 147.8mg

[0068]

As described above in detail, according to the present invention,
A novel melanin production inhibitor, a whitening agent, and a composition having a melanin production inhibitory action and a whitening action are obtained. Furthermore, it has a melanin production inhibitory action and a whitening action, whitening of sunburn skin after UV irradiation, and stains due to sunburn etc.,
It is possible to obtain cosmetics, medicines, external preparations for skin, and foods that have excellent effects in preventing, improving and treating skin pigmentation such as freckles and chloasma.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ identification code FI theme code (reference) A61K 7/00 A61K 7/00 RU 7/02 7/02 Z 7/48 7/48 A61P 17/00 A61P 17/00 43/00 111 43/00 111 C07J 71/00 C07J 71/00 (72) Inventor Kenji Sakamoto 25, Takawazawa, Yonegi, Yonemachi, Kawabe-gun, Akita Prefecture (72) Inventor Keiji Hatake 3-1-45 Yashihashihonmachi, Akita City, Akita Prefecture Goyodai Condominium No. 203 F term (reference) 4B018 LB08 LE01 LE05 MD07 MD84 ME14 MF01 4C083 AA072 AA122 AB032 AB232 AB242 AB282 AB352 AB432 AB442 AC012 AC022 AC072 AC102 AC122 AC132 AC132 AC242 AC352 AC392 AC422 AC432 AC442 AC532 AC542 AC552 AC792 AD042 AD092 AD112 AD152 AD162 AD332 AD491 AD492 AD512 AD642 AD662 CC02 CC04 CC05 CC07 CC12 DD22 DD31 DD41 EE13 EE16 4C086 AA01 AA02 DA11 MA01 MA04 NA14 ZA89 ZC02 4C091 AA02 BB08 CC01 DD01 EE04 FF03 FF14 GG03 GG13 HH01 JJ03 KK01 LL01 MM03 NN01 PB05 QQ07

Claims (17)

[Claims] 1. The following formula (1): A melanin production inhibitor comprising an ergosterol derivative represented by: 2. A whitening agent comprising an ergosterol derivative represented by Chemical formula 1. 3. A melanin production inhibitor containing the ergosterol derivative represented by Chemical formula 1. 4. A whitening agent containing the ergosterol derivative represented by Chemical formula 1. 5. A composition for suppressing melanin production, which comprises the ergosterol derivative represented by Chemical formula 1. 6. A whitening composition containing the ergosterol derivative represented by Chemical formula 1. 7. A cosmetic containing the ergosterol derivative represented by Chemical formula 1. 8. The cosmetic according to claim 7, which is for suppressing melanin production. 9. The cosmetic according to claim 7, which is for whitening. 10. A medicine containing the ergosterol derivative represented by Chemical formula 1. 11. The method according to claim 1, which is for suppressing melanin production.
The medicine according to 0. 12. The medicine according to claim 10, which is for whitening. 13. A skin external preparation containing the ergosterol derivative represented by Chemical formula 1. 14. The method according to claim 1, which is for suppressing melanin production.
The external preparation for skin according to 3. 15. The external preparation for skin according to claim 13, which is for whitening. 16. A food for suppressing melanin production, which comprises the ergosterol derivative represented by Chemical formula 1. 17. A whitening food containing the ergosterol derivative represented by Chemical formula 1.