JP5085018B2 - Hair restorer - Google Patents

Description

  The present invention relates to a novel testosterone-5α-reductase (hereinafter, abbreviated as 5α-reductase) inhibitor, an outer hair root cell growth promoter and a hair restorer.

  Conventionally, the cause of male pattern alopecia has been proposed as (1) hormone imbalance theory, (2) genetic theory, (3) blood circulation failure theory, (4) nutrition theory, etc. It has long been suggested that the male hormone testosterone plays an important role in the outbreak. That is, testosterone biosynthesized by testicles is converted to dihydrotestosterone by 5α-reductase present in hair follicles, sebaceous glands and the like in the head. This dihydrotestosterone can significantly reduce the activity of adenyl cyclase resulting in a decrease in intracellular cyclic AMP levels, resulting in a decrease in hair and surrounding energy production and suppression of protein synthesis It is thought that androgenetic alopecia progresses.

Dihydrotestosterone is also considered to be involved in acne generation and exacerbation and prostate enlargement (Non-patent Document 1). On the other hand, a decrease in the proliferative power of outer root sheath cells is considered to be one cause of male pattern baldness.
5α-reductase inhibitors have been reported in assembly, hermanus, etc., but are not known in Tochu, Mozuika, Ganoderma spores and black yeast (Patent Documents 1 and 2). No growth promoter for outer root sheath cells has been reported for Tochu, Mozuika, Ganoderma spore and black yeast.
J. et al. Steroid Biochemistry, 11, 609 (1979) JP 62-116520 A JP-A-5-17365

  However, an effective drug for these diseases, in particular, a sufficiently effective drug based on suppression of dihydrotestosterone production or promotion of proliferation of outer root sheath cells has not been found, and development thereof has been desired.

  In view of the above circumstances, the present inventors have promoted the growth of 5α-reductase inhibitors and outer hair root sheath cells that suppress excessive production of dihydrotestosterone that causes androgenetic alopecia, acne development and exacerbation, and prostatic hypertrophy. As a result of conducting sincere research to find the agent, it was found that extracts of Tochu, Mozuika, Ganoderma spore and black yeast met the purpose, and the present invention was completed.

  That is, the present invention relates to a 5α-reductase inhibitor, an outer hair root sheath cell growth promoter, and a hair-growth agent comprising one or more extracts selected from Tochu, musk squid, reishi spore and black yeast as active ingredients. Is.

  Tochu used in the present invention is a deciduous tree of the genus Eucommia and has a scientific name of Eucommia ulmoides OLIV. It is. Since the bark, leaves, etc. are in circulation, those commercial products can be used. Mud squid is a plant included in the genus Mudskipper, velvet mud squid, Verbascum thapsus L. You can use flowers distributed as herbs and aboveground parts. Ganoderma spores are mushroom spores belonging to the genus Amanentake genus, and can use spores such as red ganoderma and black ganoderma. Black yeast has the scientific name Aureobasidium pullulans and is different from the yeast Saccharomyces cerevisiae. Bacterial cells proliferated by ordinary culture can be obtained by obtaining strains distributed for a fee, and their culture solutions.

  With the extract used by this invention, the dried product of the plant marketed can be shredded and extracted, for example. The preparation method is not particularly limited, and for example, it may be extracted by heating or extracted at room temperature. The cells of black yeast can be extracted by, for example, a conventional method after autolysis.

  Examples of the solvent to be extracted include water, lower monohydric alcohols (methanol, ethanol, 1-propanol, 1-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohols (1,3-butylene glycol, Propylene glycol, glycerin, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, liquid paraffin, etc.), ethers (ethyl ether, propyl ether) Etc.). Preferred are water, lower monohydric alcohol and liquid polyhydric alcohol, and particularly preferred are water, ethanol, 1,3-butylene glycol and propylene glycol. Supercritical extraction using carbon dioxide or the like can also be used. These solvents may be used alone or in combination of two or more.

  These extracts may be used as they are in the extracted solvent, or may be used after processing such as concentration, dilution, and filtration, if necessary. Furthermore, the extracted solution may be subjected to a treatment such as concentration to dryness, spray drying, or freeze drying, and used as a dried product.

  Since the extract of the present invention has a 5α-reductase inhibitory action and an outer hair root sheath cell growth promoting action, it results from excessive production of dihydrotestosterone by 5α-reductase in mammals, particularly humans, or a decrease in the function of outer hair root sheath cells. It is useful for the treatment and prevention of diseases caused by Examples of such diseases include alopecia including male pattern alopecia, acne and benign prostatic hyperplasia.

  In order to use the extract according to the present invention for the above purpose, it is usually administered systemically or locally, orally or transdermally. The dose varies depending on age, body weight, symptoms, therapeutic effect, administration method, treatment time, etc., but in the case of treatment or prevention of benign prostatic hyperplasia, it is usually 1 mg to 1 g per adult, preferably 20 mg to 200 mg. In the range of once to several times a day. In the treatment and prevention of alopecia and acne, it is usually administered transdermally once to several times a day within the range of 10 μg to 50 mg, preferably 100 μg to 5 mg per adult. Of course, as described above, since the dosage varies depending on various conditions, an amount smaller than the above-mentioned administration range may be sufficient, or it may be necessary to administer beyond the range.

  Examples of the solid preparation for oral administration according to the present invention include tablets, pills, powders, granules, capsules and the like. For such solid preparations, in addition to the extract as the active ingredient, for example, lactose, mannitol, glucose, hydroxypropylcellulose, microcrystalline cellulose, starch, polyvinylpyrrolidone, magnesium aluminate metasilicate and other inert dilutions Agents, lubricants such as magnesium stearate, and disintegrants such as fibrin calcium gluconate. If necessary, tablets or pills may be coated with a gastric solvent such as sucrose, gelatin, hydroxypropylcellulose, hydroxypropylmethylcellulose, phthalate, or a film of an enteric substance.

  Examples of liquid preparations for oral administration include emulsions, solutions, suspensions, syrups, and elixirs. Such liquid preparations may contain, in addition to the active ingredient and inert diluent, adjuvants such as wetting agents and suspending agents, sweeteners, flavors, fragrances, preservatives and the like. Examples of other preparations for oral administration include sprays.

  Typical preparations for transdermal administration in the present invention include creams, emulsions, lotions, hair tonics, sprays, packs, solutions such as ointments, emulsions, suspensions, for rectal administration. Suppositories and pessaries for intravaginal administration. In particular, lotions, hair tonics, sprays, and solutions are preferred as preparations for the treatment and prevention of alopecia. In addition to active ingredients, these preparations include water, lower alcohols such as ethanol, higher alcohols such as cetanol, polyhydric alcohols such as polyethylene glycol and propylene glycol, celluloses such as hydroxypropylcellulose, animal Also, vegetable oils and fats, waxes, hydrocarbons such as petrolatum, silicon, surfactants, zinc oxide and the like can be blended.

  One or two or more extracts selected from Tochu, musk squid, reishi spore, and black yeast of the present invention showed excellent 5α-reductase inhibitory action, growth promotion action and hair growth action of outer root sheath cells.

  Next, in order to describe the present invention in detail, examples of production of the extract used in the present invention, formulation examples of the present invention, and experimental examples are given as examples, but the present invention is not limited thereto. In the examples, the part of the amount is part by weight, and% is% by weight.

Production Example-1
1 kg of purified water was added to 100 g of shredded product of Tochu leaf and extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure and freeze-dried to obtain 10 g of hot water extract of Tochu.

Production Example-2
Purified water (500 g) and 1,3-butylene glycol (500 g) were added to 100 g of shrunken leaf shredded product and extracted at room temperature for 2 weeks. After extraction, it was filtered to obtain 950 g of Tochuchu 1,3-butylene glycol extract.

Production Example-3
1 kg of ethanol was added to 100 g of shredded products of Tochu leaf and extracted at room temperature for 2 weeks. The obtained extract was concentrated under reduced pressure to obtain 5 g of a paste-like extract.

Production Example-4
1 kg of purified water was added to 100 g of the above-ground shredded product of velvet musk squid and extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure, and lyophilized to obtain 11 g of a hot water extract of the musk squid above ground.

Production Example-5
Purified water (500 g) and 1,3-butylene glycol (500 g) were added to 100 g of the above-ground shredded product of velvet musk squid and extracted at room temperature for 2 weeks. After the extraction, the mixture was filtered to obtain 950 g of 1,3-butylene glycol extract of the musk squid above-ground part.

Production Example-6
1 kg of ethanol was added to 100 g of the above-ground shredded product of velvet squid, and extracted at room temperature for 2 weeks. The obtained extract was concentrated under reduced pressure to obtain 2 g of a paste-like extract.

Production Example-7
1 kg of purified water was added to 100 g of shredded velvet squid flowers and extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure and freeze-dried to obtain 9 g of musk squid flower hot water extract.

Production Example-8
1 kg of purified water was added to 100 g of red ganoderma spores and extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure and freeze-dried to obtain 11 g of hot water extract of red ganoderma spore.

Production Example-9
To 100 g of red ganoderma spores, 500 g of purified water and 500 g of 1,3-butylene glycol were added and extracted at room temperature for 2 weeks. After extraction, it was filtered to obtain 950 g of 1,3-butylene glycol extract of red ganoderma spore.

Production Example-10
1 kg of ethanol was added to 100 g of red ganoderma spores and extracted at room temperature for 2 weeks. The obtained extract was concentrated under reduced pressure to obtain 2 g of a paste-like extract.

Production Example-11
1 kg of purified water was added to 100 g of black reishi spore and extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure and lyophilized to obtain 11 g of a hot water extract of black reishi spore.

Production Example-12
Black yeast was inoculated into potato dextrose medium and cultured at 30 ° C. for 3 days. 100 g of purified water was added to 10 g of cells obtained by centrifugation at 10,000 rpm, and the mixture was extracted at 95-100 ° C. for 2 hours. The obtained extract was concentrated under reduced pressure and freeze-dried to obtain 0.5 g of a black yeast hot water extract. Moreover, the centrifugal supernatant was used as a culture solution.

Production Example-13
Black yeast was inoculated into potato dextrose medium and cultured at 25 ° C. for 5 days. 10 g of cells obtained by centrifugation at 10000 rpm were self-melted (50 ° C., 3 hours), and the obtained self-melt was freeze-dried to obtain 0.4 g of black yeast self-melt.

Formulation Example-1 Lotion Formulation Formulation 1. Tochu hot water extract (Production Example 1) 0.1 part 2.1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume proper amount11. [Manufacturing method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved in purified water, and both are mixed and filtered to obtain a product.

Comparative Example-1 A conventional lotion was obtained by replacing the hot water extract of Tochu in the conventional lotion formulation example-1 with purified water.

Formulation Example-2 Cream Formulation Formulation 1. Tochu hot water extract (Production Example 1) 0.05 part2. Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11.1,3-butylene glycol 8.5
12 Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14 [Manufacturing method] Components 2 to 9 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-3 Emulsion Formulation Formulation 1. Tochu's ethanol extract (Production Example 3) 0.5 part2. Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total volume 100 with purified water
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example 4 Hair Tonic Formulation Ethanol 60.0 parts2. Tochu's 1,3-butylene glycol extract (Production Example-2) 2.0
3. Glycerin 2.0
4). [Manufacturing method] Tosaka's 1,3-butylene glycol extract is dissolved in ethanol, and glycerin and purified water are added thereto, followed by thorough stirring and mixing to obtain a product.

Formulation Example-5 Pack
Formulation Formulation 1. Tochu hot water extract (Production Example-1) 0.1 part2. Polyvinyl alcohol 12.0
3. Ethanol 5.0
4.1,3-Butylene glycol 8.0
5. Methyl paraoxybenzoate 0.2
6). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
7). Citric acid 0.1
8). Sodium citrate 0.3
9. Perfume
10. [Production method] Components 1 to 10 are uniformly dissolved in purified water to give a product of 100.

Formulation Example-6 Lotion Formulation Formulation 1. Mud Squid Hot Water Extract (Production Example 4) 0.1 part 2.1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume proper amount11. [Manufacturing method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved in purified water, and both are mixed and filtered to obtain a product.

Formulation Example-7 Cream Formulation Formulation 1. Mud Squid Hot Water Extract (Production Example-7) 0.05 part2. Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11.1,3-butylene glycol 8.5
12 Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14 [Manufacturing method] Components 2 to 9 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-8 Emulsion Formulation Formulation 1. Mud Squid Ethanol Extract (Production Example-6) 0.5 part Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total volume 100 with purified water
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-9 Hair Tonic Formulation Ethanol 60.0 parts2. Mud squid 1,3-butylene glycol extract (Production Example-5) 2.0
3. Glycerin 2.0
4). [Manufacturing method] A 1,3-butylene glycol extract of musk squid is dissolved in ethanol, glycerin and purified water are added, and the mixture is sufficiently stirred and mixed to obtain a product.

Formulation example-10 packs
Formulation Formulation 1. Mud Squid Hot Water Extract (Production Example 4) 0.1 part2. Polyvinyl alcohol 12.0
3. Ethanol 5.0
4.1,3-Butylene glycol 8.0
5. Methyl paraoxybenzoate 0.2
6). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
7). Citric acid 0.1
8). Sodium citrate 0.3
9. Perfume
10. [Production method] Components 1 to 10 are uniformly dissolved in purified water to give a product of 100.

Formulation Example-11 Lotion Formulation Formulation 1. Black Reishi Spore Hot Water Extract (Production Example 11) 0.1 part 2.1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume proper amount11. [Manufacturing method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved in purified water, and both are mixed and filtered to obtain a product.

Formulation Example-12 Cream Formulation Formulation 1. Hot water extract of red ganoderma spore (Production Example-8) 0.05 part2. Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11.1,3-butylene glycol 8.5
12 Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14 [Manufacturing method] Components 2 to 9 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-13 Emulsion Formulation Formulation 1. Ethanol extract of red ganoderma spore (Production Example-10) 0.5 part2. Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total volume 100 with purified water
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-14 Hair Tonic Formulation Ethanol 60.0 parts2. 1,3-Butylene glycol extract of red ganoderma spore (Production Example-9) 2.0
3. Glycerin 2.0
4). [Manufacturing method] A 1,3-butylene glycol extract of red ganoderma spore is dissolved in ethanol, glycerin and purified water are added, and the mixture is sufficiently stirred and mixed to obtain a product.

Formulation example-15 packs
Formulation Formulation 1. Red hot turf spore hot water extract (Production Example-8) 0.1 part2. Polyvinyl alcohol 12.0
3. Ethanol 5.0
4.1,3-Butylene glycol 8.0
5. Methyl paraoxybenzoate 0.2
6). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
7). Citric acid 0.1
8). Sodium citrate 0.3
9. Perfume
10. [Production method] Components 1 to 10 are uniformly dissolved in purified water to give a product of 100.

Formulation Example-16 Lotion Formulation Formulation 1. Black yeast hot water extract (Production Example-12) 0.1 part 2.1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume proper amount11. [Manufacturing method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved in purified water, and both are mixed and filtered to obtain a product.

Formulation Example-17 Cream Formulation Formulation 1. 1. Black yeast culture solution (Production Example-12) 0.05 part Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11.1,3-butylene glycol 8.5
12 Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14 [Manufacturing method] Components 2 to 9 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-18 Emulsion Formulation Formulation 1. 1. Self-melted black yeast (Production Example-13) 0.5 part Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total volume 100 with purified water
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example-19 Hair Tonic Formulation Ethanol 60.0 parts2. Black yeast culture solution (Production Example-12) 2.0
3. Glycerin 2.0
4). [Manufacturing method] A black yeast culture solution is dissolved in purified water, and ethanol and glycerin are added, and the mixture is sufficiently stirred and mixed to obtain a product.

Formulation example-20 packs
Formulation Formulation 1. 1. Hot water extract of black yeast (Production Example-12) 0.1 part Polyvinyl alcohol 12.0
3. Ethanol 5.0
4.1,3-Butylene glycol 8.0
5. Methyl paraoxybenzoate 0.2
6). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
7). Citric acid 0.1
8). Sodium citrate 0.3
9. Perfume
10. [Production method] Components 1 to 10 are uniformly dissolved in purified water to give a product of 100.

Experimental Example-1 Inhibitory Effect on 5α-Reductase Using 5α-reductase extracted from the liver of an SD male rat (7 weeks old), the measurement was performed under the conditions in the following reaction system.

(Reaction conditions) After dissolving testosterone (0.6 μM) with 10 drops of propylene glycol, 5 mL of Tris-HCl buffer (pH 7.2) was added, and then 5 mg of NADPH and 2 mL of 5α-reductase solution were sequentially added. React at 30 ° C. for 30 minutes. After the reaction, methylene chloride is added to stop the reaction, and the whole is extracted with 50 mL of methylene chloride. Next, the methylene chloride layer is distilled off under reduced pressure, and the reaction amount is measured by gas chromatography. (Conditions for gas chromatography: column OV-17 (3 mmφ, 2 m); column temperature 250 ° C .; detector; FID)
The extract according to the present invention is added to the reaction system after the testosterone is dropped. As comparative examples, a hot water extract of Ganoderma fruit bodies prepared in the same manner as in Production Example-8 and a hot water extract of yeast prepared in the same manner as in Production Example-12 were used.

Inhibition rate: The reaction rate when the extract is not added (control) is regarded as 100% (inhibition rate 0%), and the decrease in the reaction rate when the extract is added is calculated to obtain the inhibition rate. The formula is as follows. Since dihydrotestosterone was further metabolized to produce androstanediol, the peak area (amount) of the 5α-reductase metabolite was calculated including androstanediol.

Inhibition rate (%) = (b / a−b ′ / a ′) / (b / a) × 100

a: Control (peak area of testosterone)
b: Control (peak area of dihydrotestosterone and androstanediol)
a ′: peak area of testosterone (addition of extract)
b ′: peak area of dihydrotestosterone and androstanediol
(Extract addition)

  These results are summarized in Table 1. As a result, excellent inhibitory action against 5α-reductase was observed in Tochu, Mozu squid, Reishi spore and black yeast.

Experimental example-2
Cell growth promotion test of outer hair sheath cells The cell growth promotion effect of outer hair sheath cells was measured under the following conditions.

The outer hair root sheath cells were seeded in a 96-well culture dish at 3,000 cells / hole, and the sample was added with a Humedia-KG2 medium containing no bovine pituitary extract to a final concentration of 1 to 20 μg / ml. ° C., 5% CO ₂ conditions, were cultured for 5 days. Thereafter, the medium containing the sample was removed, and an MTT solution adjusted to 0.5 mg / mL with a Humeria-KG2 medium was added, followed by culturing at 37 ° C. under 5% CO ₂ for 2 hours. After removing the MTT solution, DMSO was added to lyse the cells, and the amount of MTT incorporated was measured by absorbance at 590 nm. The cell growth promotion rate of the outer root sheath cells was determined from the ratio of the absorbance at the time of sample addition to the absorbance of the control. As comparative examples, a hot water extract of Ganoderma fruit bodies prepared in the same manner as in Production Example-8 and a hot water extract of yeast prepared in the same manner as in Production Example-12 were used.

  The test results are shown in Table 2. As a result, an excellent growth promoting effect of outer root sheath cells was observed in Tochu, Mozu squid, Ganoderma spore and black yeast.

Experimental Example-3 Hair growth effect Hattori et al. [J. Dermatology, 10, 45-54 (1983)], the 45-day-old C3H mouse dorsal hair was shaved with a clipper, and this part was divided into two parts. On the other hand, 1 mL of a conventional lotion (Comparative Example-1) containing no extract related to the present invention was applied once a day. The comparison was made based on the number of days required for hair growth to be recognized throughout each site. As a result, the period of the lotions of Examples-1, 6, 11 and 16 was shortened compared to the period until the hair growth of the lotion preparation containing no extract according to the present invention was observed (Table 3). ). Moreover, the same effect was recognized also in the other Example.

The 5α-reductase inhibitor and the outer hair root sheath cell growth promoter containing one or more extracts selected from Tochu, musk squid, ganoderma spore and black yeast of the present invention can be used as hair restorers.

Claims (3)

A testosterone-5α-reductase inhibitor characterized by containing one or more extracts selected from mud squid, reishi spore (excluding spores contained in the ganoderma fruit body) and black yeast. An outer hair root sheath cell growth promoter characterized by containing one or more extracts selected from musk squid, reishi spore (excluding spores contained in the ganoderma fruit body) and black yeast . A hair restorer comprising an extract of musk squid and / or black yeast, wherein the blending concentration of the extract of musk squid is 0.0001 to 0.0005% by weight as a solid content .