JP2002308790A - TESTOSTERONE 5alpha-REDUCTASE INHIBITOR, ANDROGEN RECEPTOR- BINDING INHIBITOR, ANTIANGROGENIC AGENT, AND HAIR GROWTH COSMETIC - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a new testosterone 5α-reductase inhibitor, to provide an androgen receptor-binding inhibitor, to provide an antiandrogenic agent, and to provide a hair growth cosmetic. SOLUTION: This testosterone 5α-reductase inhibitor contains an extract from branches and leaves of Ampelopsis grossendentata. The androgen receptor- binding inhibitor, the antiandrogenic agent, and the hair growth cosmetic contain the extract, respectively.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to testosterone 5
The present invention relates to an α-reductase inhibitor, an androgen receptor binding inhibitor, an antiandrogen, and a hair nourishing cosmetic. Specifically, a novel testosterone 5α-reductase inhibitor that inhibits the action of testosterone 5α-reductase, which reduces testosterone to active 5α-dihydrotestosterone (active 5α-DHT), and 5α-DHT generated from testosterone, A novel androgen receptor binding inhibitor that inhibits binding to a receptor, a novel antiandrogen comprising a plant extract having a testosterone 5α-reductase inhibitory activity and / or an androgen receptor binding inhibitory activity, and the testosterone 5α The present invention relates to a hair nourishing cosmetic using the reductase inhibitor and / or the androgen receptor binding inhibitor.

[0002]

2. Description of the Related Art Many steroid hormones bind to a receptor in the form of a molecule secreted from a producing organ to express its action, and in the case of a male hormone collectively called an androgen, for example, testosterone is intracellularly contained in a target organ. And then is reduced to 5α-dihydrotestosterone (5α-DHT) by testosterone 5α-reductase, and then binds to a receptor to exert its action as an androgen.

[0003] Androgens are important hormones,
When it acts excessively, male pattern baldness, hirsutism, seborrhea, acne, prostatic hypertrophy, prostate tumor, precocious boyhood,
Induces various undesirable symptoms. Therefore, these undesirable symptoms are induced by suppressing the action of excess androgen. Therefore, conventionally, a method of suppressing the action of excessive androgen in order to improve these various symptoms, specifically, testosterone is used in an active form.
A method for inhibiting the production of active 5α-DHT by inhibiting the action of testosterone 5α-reductase that reduces to α-DHT,
A method for inhibiting the binding of α-DHT to the receptor to prevent the expression of androgen activity was examined. As a result, the effectiveness of cyproterone acetate, oxendrone, chlormadinone acetate, and the like was confirmed.

However, since these are steroid hormone derivatives, they have a disadvantage that they have undesirable side effects such as hormone-like effects.

[0005]

An object of the present invention is to find a novel plant extract having a testosterone 5α-reductase inhibitory action and an androgen receptor binding inhibitory action, and to provide a powerful and safe antiandrogen. Another object of the present invention is to provide a novel hair-growth cosmetic for treatment and prevention suitable for the above-mentioned symptoms.

[0006]

The testosterone 5α-reductase inhibitor according to the present invention is characterized in that it comprises a wisteria tea leaf extract. In addition, the androgen receptor binding inhibitor is characterized by comprising a wisteria tea leaf extract.

[0007] The antiandrogen according to the present invention comprises:
A wisteria tea leaf extract, characterized by having a testosterone 5α-reductase inhibitory action and / or an androgen receptor binding inhibitory action.

[0008] Furthermore, the hair growth cosmetic according to the present invention is characterized by containing the testosterone 5α-reductase inhibitor and / or the androgen receptor binding inhibitor according to the present invention.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in more detail. The testosterone 5α-reductase inhibitor according to the present invention comprises a wisteria tea leaves extract, and comprises a testosterone 5α-reductase inhibitor. It is contained as an active ingredient.

[0010] The androgen receptor binding inhibitor according to the present invention comprises a wisteria tea leaves extract and contains an androgen receptor binding inhibitor as an active ingredient.

Further, the antiandrogen according to the present invention comprises a wisteria tea leaf extract and comprises testosterone 5
It has an α-reductase inhibitory action and / or an androgen receptor binding inhibitory action.

In the present invention, the wisteria tea is usually used in a dry state, and the branch is preferably used as the site of use. Wisteria tea belongs to the grape family and is a perennial plant that grows naturally in a wide area from central to southern China, and is also cultivated in Taiwan and other countries. Fujicha is the scientific name Ampelopsis grossed
entata (Hand.-Mazz.) WTWang CV, which has been used as a folk medicine for colds, sore throats, acute conjunctivitis, etc., except in China since ancient times there is a region where the foliage of this plant is used as a beverage.

The wisteria tea leaves used as an extraction raw material are suitably dried and pulverized immediately after collection. Drying may be performed in the sun or using a commonly used dryer. The wisteria tea leaves may be used as an extraction raw material after pretreatment such as defatting with a nonpolar solvent such as hexane or benzene. By performing a pretreatment such as degreasing, the extraction treatment of wisteria tea leaves with a polar solvent can be performed efficiently.

The details of the testosterone 5α-reductase inhibitor and the inhibitor of androgen receptor binding obtained from Fuji tea leaves are unknown, but the extract obtained from Fuji tea leaves using various solvents is not inhibited. Activity is observed. The extract according to the present invention is water, various aliphatic lower alcohols such as ethanol and isopropanol, 1,3-butylene glycol, ethylene glycol, glycerin,
It is obtained by using a hydrophilic organic solvent such as isopropylene glycol and various aqueous organic solvents such as a mixed solution of these various hydrophilic organic solvents, and this wisteria tea leaves extract has high testosterone 5α-reductase inhibitory activity and androgen receptor binding. Shows an inhibitory effect. Moreover, these aqueous solvents are easy to handle and the extraction operation can be performed relatively easily.

[0015] Wisteria tea leaves are generally used after each part is dried, and then cut, cut into pieces, or crushed.
At this time, the extraction method and the extraction conditions are not particularly limited, but preferably, the amount of wisteria tea leaves used in the weight ratio is 5 to 5.
It is immersed in a 15-fold amount of the above-mentioned extraction solvent, and the soluble component is eluted with moderate stirring under heating and heating at room temperature to about 90 ° C. Thereafter, the extract is filtered or centrifuged, and solid-liquid separated to obtain a target extract.

The extract thus obtained can be used as it is as a testosterone 5α-reductase inhibitor and an androgen receptor binding inhibitor or an antiandrogen according to the present invention. It is also possible to use a concentrated extract or a dry extract, for example, by further drying using a method such as spray drying. In addition, a simple purification treatment may be performed, if necessary, as long as the above activity is not inhibited. Needless to say, this extract or dried extract can be used as it is, or can be used by adding various excipients such as starch and lactose.

The testosterone 5α-reductase inhibitor according to the present invention thus obtained can be used as a testosterone 5α-reductase inhibitor for male pattern baldness, hirsutism, seborrhea, acne, benign prostatic hyperplasia, etc.
It can be used for various conditions caused by excessive activity of α-reductase and excessive secretion of testosterone. The androgen receptor binding inhibitor according to the present invention is also used for various symptoms caused by 5α-DHT binding to the androgen receptor, such as male pattern baldness, hirsutism, seborrhea, acne, and benign prostatic hypertrophy. . That is, the antiandrogens of the present invention are used in all applications meaningful for inhibiting the action of testosterone 5α-reductase and / or inhibiting the binding of 5α-DHT to the androgen receptor.

In addition, the wisteria tea leaves extract can be used alone or in a known manner by formulating a general plant extract, or by using an appropriate auxiliary, an agent for external skin, an internal liquid, an internal solid, an injection. Preparations, suppositories, etc., which can be widely used as constituents of arbitrary external preparations for skin, cosmetics, quasi-drugs, pharmaceuticals, etc., and are particularly suitable as the main ingredient of hair nourishing cosmetics. . As the hair nourishing cosmetic, any dosage form such as a hair tonic, a hair cream, a hair liquid, a hair lotion, a hair shampoo, and a hair rinse can be used.

The amount of the wisteria tea leaf extract in the preparation may be appropriately determined in consideration of the purpose of use, gender, symptoms and the like.
0% by weight. In addition, wisteria tea leaves have been used as beverages and folk medicines since ancient times, and their safety has been confirmed and can be used without side effects.

Further, the hair restoration cosmetic composition of the present invention contains various main ingredients and other ingredients usually used in the production of hair restoration cosmetics, as long as the testosterone 5α-reductase inhibitory action and the androgen receptor binding inhibitory action are not hindered. Any auxiliaries can be used.

The following can be specifically mentioned as those which can be used in combination as the main agent of these hair nourishing cosmetics.

Examples of astringents include citric acid or salts thereof, tartaric acid or salts thereof, lactic acid or salts thereof, aluminum chloride, potassium aluminum sulfate, allantochlorohydroxyaluminum, allantoindihydroxyaluminum, zinc paraphenolsulfonate, zinc sulfate,
Jiyu extract, Eijitsu extract, Hamamelis extract, Geno ginger extract, tea catechins, proanthocyanidins, gypsophila extract, Odrisou extract, Hypericum extract, Rhubarb extract, cornflower extract, horsetail extract, Kizuta extract, Cucumber extract, Maronier extract, Salvia extract, Melissa extract, Melissa extract, Tamarind husk extract and the like.

Also, as bactericidal and antibacterial agents, benzoic acid, sodium benzoate, paraoxybenzoate, distearylmethylammonium chloride, benzethonium chloride, alkyldiaminoethylglycine chloride solution, chlorhexidine hydrochloride, orthophenylphenol, photosensitizer 10
No. 1, Photosensitizer No. 201, salicylic acid, sodium salicylate, sorbic acid, halocarban, resorcinol, parachlorophenol, phenoxyethanol, bisabolol, hinokitiol, menthol, chitosan, chitosan hydrolyzate, zhuyu extract, kudin extract, emicou extract, loquat extract, awaurushi Extract, hop extract, yucca extract, aloe extract, cinnamon extract, gaju extract, oil-soluble licorice extract (licorice hydrophobic flavonoid, glabridine, glabrene, lycochalcone A) and the like.

Further, as an ultraviolet absorber, β-isopropylfuranone derivative, urocanic acid, ethyl urocanate, oxybenzone, oxybenzosulfonic acid, tetrahydroxybenzophenone, dihydroxydimethoxybenzophenone, dihydroxybenzophenone, sinoxate, methyl diisopropylcinnamate, methoxycinnamate Octyl acid, glyceryl paraaminobenzoate, amyl paradimethylaminobenzoate, octyl paradimethylbenzoate, octyl paraaminobenzoate, paraaminobenzoic acid, ethyl paraaminobenzoate, butylmethoxydibenzoylmethane, titanium oxide, β-carotene, γ- Oryzanol, rice bran extract, aloe extract, birch extract, birch extract, chamomile extract, kogomegusa extract, biloba Shiekisu, Hen'naekisu, butterfly jig Rumi extract, horse chestnut extract, ginkgo leaf extract,
Chamomile extract, oil-soluble licorice extract and the like.

Further, as humectants, serine, glycine, threonine, alanine, collagen, hydrolyzed collagen, hydronectin, fibronectin, keratin, elastin, royal jelly, chondroitin heparin,
Glycerophospholipid, sphingolipid, glycosphingolipid, linoleic acid or esters thereof, eicosapentaenoic acid or esters thereof, pectin, alge colloid, bifidobacterium fermentation product, lactic acid fermentation product, yeast extract, reishi mycelium culture Or an extract thereof, wheat germ oil, avocado oil, rice germ oil, jojoba oil, soybean phospholipid, γ-oryzanol, belowow oil extract, yoquinin extract,
Geo extract, diatom extract, diatom extract, Kidachi aloe extract, burdock extract, maroni extract, mannen wax extract, arnica extract, wheat bran, rice bran extract and the like.

As cell activators, placental extract, riboflavin or a derivative thereof, pyridoxine or a derivative thereof, nicotinic acid or a derivative thereof, pantothenic acid or a derivative thereof, α-tocopherol or a derivative thereof, arnica extract, carrot extract, and panax ginseng Extract, eleuthero extract, loofah extract (saponin), radish extract, birch extract, oak extract, buttonpix extract, peonies extract, mukuroji extract, safflower extract, ashitaba extract, loquat leaf extract, cypress extract, saxifrage extract, yellow leaf extract, salvia extract ,
Garlic extract, mannen wax extract and the like can be mentioned.

As anti-inflammatory and antiallergic agents, azulene, allantoin, aminocaproic acid, indomethacin, lysozyme chloride, epsilon aminocaproic acid, oxybenzone, glycyrrhizic acid or its derivatives, glycyrrhetinic acid or its derivatives, Photon 301 and Photon 401
No., diphenhydramine hydrochloride, tranexamic acid or a derivative thereof, adenosine phosphate, estradiol, ethrone, ethinyl estradiol, cortisone, hydrocortisone, prednisone, progesterone, corticosterone, arnica extract, intinko extract, sanshishi extract, juyaku extract, horse chestnut extract , Licorice extract, corn extract, mugwort extract, sprouts extract, gentian extract, psycho extract, senkyu extract, boufu extract, Achillea millefolium extract, spinach extract, perilla extract, maroni extract, and gongon extract.

As antioxidant and active oxygen scavengers, dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate, baicalin, baicalein, superoxide dismutase, catalase, rosemary extract, melissa extract, ougon extract, age extract, loquat leaf Extract, Hop extract, Hamamelis extract,
Peony extract, sage extract, kina extract, chamomile extract, eucalyptus extract, perilla extract, ginkgo leaf extract, thyme extract, cardamom extract, caraway extract, nutmeg extract, mace extract, laurel extract, clove extract, turmeric extract, willow extract, etc. .

The following can be used as an auxiliary agent: oils and fats such as soybean oil, linseed oil, drill oil, sesame oil, nuka oil, cottonseed oil, rapeseed oil, safflower oil, corn oil, olive oil, camellia oil Oil, almond oil, castor oil, peanut oil, cocoa oil, mokuro, palm oil, palm kernel oil, tallow, mink oil, egg yolk oil, jojoba oil, evening primrose oil,
Horse oil and the like.

As waxes, carnauba wax, candelilla wax, beeswax, salami beeswax, whale wax, Celax,
Lanolins and the like.

Examples of the hydrocarbons include liquid paraffin, petrolatum, microcrystalline wax, ceresin, squalane, and polyethylene powder.

Examples of the fatty acids include stearic acid, linoleic acid, lauric acid, myristic acid, palmitic acid, hevenic acid, lanolinic acid, oleic acid, undecylenic acid, isostearic acid and the like.

Further, as alcohols, lauryl alcohol, cetyl alcohol, stearyl alcohol, lanolin alcohol, hydrogenated lanolin alcohol, oleyl alcohol, hexadecyl alcohol, 2-octyldodecanol, glycerin, sorbitol, propylene glycol, 1,3-butylene Glycol, ethylene glycol or a polymer thereof, glucose, sucrose, cholesterol, phytosterol, cetostearyl alcohol and the like.

Esters such as decyl oleate, butyl stearate, myristyl myristate, hexyl laurate, isopropyl palmitate, isopropyl myristate, octyl dodecyl myristate,
Examples include hexyldecyl dimethyloctanoate, propylene glycol dioleate, diethyl phthalate, propylene glycol monostearate, ethylene glycol monostearate, glyceryl monostearate, glyceryl trimmyristate, lanolin acetate, cetyl lactate and the like.

Further, examples of the surfactant include an anionic surfactant, a cationic surfactant, an amphoteric surfactant, and a nonionic surfactant.

[0036] Fragrances include menthol, carvone, eugenol, anethole, peppermint oil, spearmint oil,
Examples include peppermint oil, eucalyptus oil, anise oil and other oily flavors from various animals and plants.

The testosterone 5α-reductase inhibitor, androgen receptor binding inhibitor and antiandrogen according to the present invention are added to dog foods and other foods for pets and livestock for the purpose of preventing and treating hair loss. can do.

[0038]

EXAMPLES Examples of the present invention will be described below, and the present invention will be described in more detail.

[Production Example 1] Fujicha [Scientific name: Ampelopsis gro
300 g of the ssedentata (Hand.-Mazz.) WT Wang CV] was poured into 2000 mL of an extraction solvent, and kept at 70 ° C. for 3 hours with gentle stirring. Thereafter, the mixture was filtered, the filtrate was concentrated at 40 ° C. under reduced pressure, and further dried with a reduced-pressure drier to obtain a wisteria tea leaf extract. When the above extraction treatment was performed using three kinds of extraction solvents, the yield of the extract was as shown in Table 1. If the extraction solvent is a mixture,
The mixing ratios shown below are based on weight.

<Table 1> Sample extraction Solvent extract yield (% by weight) 1 Water 22 2 Ethanol / water (1/1) 16 3 Ethanol 12

[Test Example 1] Test of testosterone 5α-reductase inhibitory action 4.2 mg of testosterone (manufactured by Tokyo Chemical Industry Co., Ltd.) was dissolved in 1 mL of propylene glycol, and 1 μL of the solution was added to 20 μL of the solution.
825 μL of 5 mmol / L Tris-HCl buffer (pH 7.2) containing mg / ml NADPH was added and mixed.

Further, 80 μL of each sample solution (solvent: water, ethanol or a mixture thereof) and 75 μL of S-9 (rat liver homogenate: manufactured by Oriental Yeast Co., Ltd.) were added, mixed, and incubated at 37 ° C. for 35 minutes. . Thereafter, 1 mL of methylene chloride was added to stop the reaction, and the mixture was vigorously shaken. Then, at 3000 rpm, 10
After centrifugation for 1 minute, the methylene chloride layer was separated, and the reaction products such as dihydroxytestosterone and androstanediol were quantified by gas chromatography. Separately, as a control, the same treatment (80 μL) was used in place of the sample solution in the same amount as the sample solvent, and the reaction product was quantified. According to the following equation, the concentration (pp
m) was calculated.

[0043]

[Formula 1] Concentration (ppm) = Peak area × Concentration at the time of preparing a calibration curve / Peak area at the time of preparing a calibration curve

Next, the conversion by testosterone-5α-reductase was determined. Testosterone (3) is a substrate for the reaction, and 5α-androstane-3α
(1), 17β-diol and Stanlone
(2) is a reaction product. By taking into account the decomposition of each compound at the time of the reaction, the reaction was converted to the sum of the amount of the product and the remaining mass of the substrate as the mass at the start of the reaction.

[0045]

[Formula 2] Conversion rate = total amount of (1) + (2) in organic layer / total amount of (1) + (2) + (3) in organic layer × 100

The inhibition rate of the enzyme reaction was calculated by the following equation.

[0047]

[Formula 3] Inhibition rate (%) = ｛1- (conversion rate at the time of sample addition) /
(Conversion rate at the time of addition of solvent)｝ × 100

The above-mentioned inhibition rate was measured by gradually decreasing the sample concentration, and the sample concentration (ppm) that inhibited the activity of testosterone 5α-reductase by 50% was determined by an interpolation method.

<Table 2> Sample extraction Solvent 50% inhibitory concentration (ppm) 1 Water 709 2 Ethanol / water (1/1) 639 3 Ethanol 754

From the results shown in Table 2, it was confirmed that the extract from Wisteria tea leaves had the effect of inhibiting testosterone 5α-reductase activity. In addition, the strength of the activity of inhibiting the testosterone 5α-reductase activity of the wisteria tea leaf extract changes depending on the concentration of the wisteria tea leaf extract, and the testosterone concentration is adjusted by adjusting the concentration of the wisteria tea leaf extract. It was confirmed that the effect of inhibiting 5α-reductase activity could be regulated.

Test Example 2 Test of Androgen Receptor Binding Inhibiting Activity The androgen receptor binding inhibitory activity of the wisteria tea leaf extract according to Example 1 was tested by the following test method.

Androgen-dependent mouse breast cancer cell SC-
3 cells were cultured in a MEM medium containing 2% FBS (hereinafter MEM-2).
1.0 × 10 ⁴ cells / well
A 96-well microplate was seeded at a cell density of / 100 μL, and cultured at 37 ° C. under 5% CO 2 -95% air. After 24 hours, samples and 10 ^-9 molar DHT
Was replaced with a 0.5% BSA-containing HamF1210 MEM medium (hereinafter abbreviated as HMB medium) and cultured for 48 hours. Then, the medium was added to ME containing 0.97 mM MTT.
The medium was replaced with M-2 medium, and after culturing for 2 hours, the medium was replaced with isopropanol to extract blue formazan formed in the cells. With respect to isopropanol containing the eluted blue formazan, the absorbance at 570 nm where the absorption maximum point of blue formazan was measured.

In order to correct the influence of the adherent cells, the absorbance at 650 nm was also measured at the same time, and the difference between the two absorbances was used as a value proportional to the amount of blue formazan produced. Corrected absorbance). In parallel with the above, in order to see the effect of the sample alone on SC-3 cells, the same culture and measurement were performed by adding only the sample without adding DHT to the HMB medium. Furthermore, as a control, when the cells were cultured in an HMB medium to which no sample and DHT were added,
The same measurement was performed when the cells were cultured in an HMB medium containing only HT.

From the measurement results, the binding inhibition rate showing an antiandrogen action was calculated by the following equation.

[0055]

Formula 4: Binding inhibition rate (%) = {1− (C−D) / (A−B)} × 100

A: Absorbance when DHT is added and no sample is added B: Absorbance when DHT is not added and no sample is added C: Absorbance when DHT is added and a sample is added D: No DHT is added and no sample is added Absorbance when

The inhibition rate was measured at a concentration of 50 ppm of the sample solution to determine the androgen binding inhibition rate (%). Table 3 shows the results.

<Table 3> Sample extraction Solvent inhibition rate (ppm) 1 Water 112 2 Ethanol / water (1/1) 62 3 Ethanol 46

From the results shown in Table 3, it was confirmed that the extract from Fuji Chaeda leaves had an androgen binding inhibitory action. In addition, the strength of the androgen binding inhibitory action of such wisteria tea leaf extract varies depending on the concentration of the wisteria tea leaf extract, and the strength of the androgen binding inhibitory action is controlled by adjusting the concentration of the wisteria tea leaf extract. It was confirmed that the length could be adjusted.

Test Example 3 Test of Hair Removal Inhibitory Effect The hair loss cosmetic effect containing the wisteria tea leaf extract obtained in Production Example 1 was tested for its hair loss inhibitory effect by the following method.

[0061] Ten men aged 28 to 52 with symptoms of male pattern baldness and seborrheic dermatitis were divided into a use group and a non-use group each of which was divided into two groups. 0.1% w / w of 50% ethanol extract of Wisteria tea leaves according to Example 1
A 50 v / v% ethanol aqueous solution containing (solid content) was used twice a day for three weeks twice a day in the morning and at night in place of the usual hair tonic. Everyone was allowed to wash their hair under the same conditions on the test start date and test end date, and the number of hair removals at that time was measured. In order to adjust the conditions, the hair was washed under the same conditions 24 hours before the hair was washed for counting the number of hair removals. Tables 4 and 5 show the test results.

<Table 4> Results of use group Subject test start date ( test ) Test end date (test) reduction rate (%) A 69 23 33.3 B 83 41 49.4 C 45 29 64.4 D 62 24 38.7 E 70 39 55.7 Average 65.8 31.2 47.4

<Table 5> Results of non-use group Subject test start date ( test ) Test end date (test) Reduction rate (%) F 66 69 104.5 G 77 76 98.7 H 51 55 107.8 I 72 81 112.5 J 58 61 105.2 Average 64.8 68.4 105.6

In the above use tests, no irritation or sensitization to the skin or scalp was observed and no side effects were observed by using a 50% ethanol aqueous solution containing the wisteria tea branch extract according to the production example of the present invention. Did not. Furthermore, as shown in Table 4, a clear decrease in the hair removal rate was observed, and it was confirmed that hair removal was successfully prevented.

[Formulation Examples] Next, the following formulation examples were produced using the wisteria tea leaf extract obtained above, and in each case, a good preparation could be obtained.

(Formulation Example 1 Hair tonic) Purified water 70.0 (parts by weight) Fujichae leaves 50% ethanol extract (Production example 1) 0.2 Pyridoxine hydrochloride 0.1 Resorcinol 0.01 D-pantothenyl alcohol 0 .1 dipotassium glycyrrhizinate 0.1 assembly extract 0.2 1-menthol 0.05 1,3-butylene glycol 4.0 carrot extract 0.5 kudin extract 0.3 chamomile extract 0.2 salicylic acid 0.2 pyrrolidone carboxylic acid Sodium acid 1.0 Ethanol 25.0 Perfume Appropriate amount

Based on the above component amounts, the composition was treated in the usual manner for the production of hair tonics to produce a hair tonic, which is the hair tonic cosmetic of the present invention.

(Formulation Example 2 Hair lotion) Fujichae leaves 50% ethanol extract (Production Example 1) 0.1 (parts by weight) 1,3-butylene glycol 6.0 ethanol 8.0 polyoxyethylene hydrogenated castor oil ( 40EO) 1.0 Polyoxysorbitan monostearate (20EO) 1.5 Stearyl glycyrrhetinate 0.2 Emmeiso extract 0.5 Oil-soluble licorice extract 0.02 Hinokitiol 0.05 Urea 3.0 Niacin 0.1 Diphenhydramine hydrochloride 0.1 Tocopherol acetate 0.05 Methyl parahydroxybenzoate 0.1 Phenoxyethanol 0.3 l-Menthol 0.2 Purified water Remaining amount 100.0

Based on the above component amounts, a treatment was carried out by a conventional method for producing a hair lotion to produce a hair lotion, which is a hair restoration cosmetic according to the present invention.

(Formulation Example 3 Hair restorer) Wisteria tea leaves 50% ethanol extract (Production Example 1) 0.5 (parts by weight) Hinokitiol 0.1 Glycyrrhetinic acid 0.1 Cepharanthin 0.02 Polyoxyethylene hydrogenated castor oil ( 20EO) 1.5 1,3-butylene glycol 3.0 Ethanol 60.0 Tocopherol acetate 0.1 Carrot extract 0.1 Pepper tincture 2.0 Garlic extract 0.5 Photosensitizer 301 0.005 Pyridoxine hydrochloride 0 .05 dl-menthol 0.3 purified water remaining amount 100.0

Based on the above component amounts, the hair was restored by a conventional method for producing a hair restorer to produce a hair restorer, which is a hair restoration cosmetic according to the present invention.

(Formulation Example 4 Shampoo) Wisteria tea leaf water extract (Production Example 1) 1.0 (parts by weight) Polyoxyethylene lauryl sulfate triethanolamine salt 14.0 Ethylene glycol distearate 2.0 Lauryl dimethylamino Betaine acetate 4.0 Lauric acid diethanolamide 5.0 Glycerin 2.0 Keratin hydrolyzate 3.0 Mukuro di extract 0.2 Kiraya extract 1.0 Yellow extract 0.5 Oubak extract 0.3 Rosemary extract 0. 5 Aloe extract 0.2 Peach leaf extract 0.3 Seaweed (brown algae) extract 0.5 Marronnier seed extract 0.3 Methyl parahydroxybenzoate 0.1 Perfume 0.05 Purified water Remaining amount 100.0

Based on the above-mentioned component amounts, the composition was treated by a conventional method of shampoo production to produce a shampoo which is a hair restoration cosmetic according to the present invention.

[0074]

According to the present invention, a novel testosterone 5α-reductase inhibitor and an androgen receptor binding inhibitor having few side effects can be provided. With these inhibitors, male and female baldness,
It can greatly contribute to improvement or prevention of various symptoms such as hirsutism, seborrhea, acne, benign prostatic hyperplasia, prostate tumor, precocious boys, etc. due to binding of excessive testosterone or 5α-DHT to the androgen receptor.

 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C083 AA111 AA112 AC022 AC102 AC122 AC432 AC442 AC472 AC482 AC552 AC612 AC642 AC682 AC712 AC852 AD442 AD532 AD552 AD632 AD662 CC33 CC38 DD27 EE22 4C088 AB56 AC05 CA05 CA06 CA08 MA63 ZA92 ZC10 ZC20

Claims (4)

[Claims] 1. A testosterone 5α-reductase inhibitor comprising a wisteria leaf extract. 2. An androgen receptor binding inhibitor comprising a wisteria tea leaf extract. 3. Testosterone 5 comprising a wisteria leaf extract
An antiandrogen having an α-reductase inhibitory action and / or an androgen receptor binding inhibitory action. 4. A hair-growing cosmetic comprising the testosterone 5α-reductase inhibitor according to claim 1 and / or the androgen receptor binding inhibitor according to claim 2.