JPH1017456A - Cell-activating agent, cosmetic and hair-growing agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a cell-activating agent containing the extract of a plant belonging to the genus Boehmeria and having a testosterone-5α-reductase (referred to as TSR)-inhibiting activity, an epidermal moisture-retaining activity, a cell-proliferating activity or their combined activities. SOLUTION: This cell-activating agent contains the solvent extract of a plant to the genus Boehmeria as an active ingredient in an amount of >=0.0001wt.%, especially 0.0001-20wt.%, converted into the solvent extract. The plant includes Boehmeria longispica Steud, Boehmeria tricuspis Makino and Boehmeria nivea Gaud, and the extraction solution is obtained by immersing the desired site of the plant in a solvent (e.g. acetone). The cell-activating agent is low toxic, exhibits a vasodilator activity, a tyrosinase-inhabiting activity, a SOD-like activity, and an antioxidizing activity in addition to the above- described activity, and can be utilized for cosmetics, especially hair-growing agents, and for various kinds of medicines and quasi drugs. The hair-growing agents safely inhibit TSR causing the falling of hair and give an excellent hair-growing effect.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a testosterone 5α-reductase inhibitory activity, vasodilatory activity, epidermal moisturizing activity, cell growth activity, tyrosinase inhibitory activity, SOD-like activity, comprising a plant-derived solvent extract as an active ingredient. A cell activator exhibiting an antioxidant action or an activity combining these,
It relates to cosmetics and hair tonics.

[0002]

2. Description of the Related Art Plants belonging to the genus Boehmeria are perennial shrubs or small trees, and are widely distributed in tropical and temperate zones around the world. It is used as a hemostatic agent, fever, etc., and young shoots are sometimes consumed. However, solvent extracts of plants of the genus Mao have not been studied hitherto. On the other hand, conventionally, solvent extracts of various plants have been studied as substances that can be used for cosmetics and the like having a cell activating action and a moisturizing action. However, the action of the solvent extract of the above-mentioned plant of the genus Mao is not known at all.

[0003] By the way, various substances that suppress androgen have been proposed for the purpose of preventing hair loss or growing hair. For example, substances having a female hormone action such as estradiol and ethinyl estradiol are also known as substances having an antiandrogen action, but have a problem in safety. On the other hand, as a result of studies on the mechanism of androgen suppression, testosterone showed that testosterone 5α-reductase (hereinafter referred to as TSR)
Is referred to as 5α-dihydrotestosterone (hereinafter abbreviated as DHT). This DHT is known to have several times to ten and several times more potent androgen action than testosterone, and this DHT binds to an intracellular receptor and acts on hair mother cells to suppress their cell division. It is believed that this hinders hair growth. Therefore, some substances related to such a mechanism of inhibiting the TSR activity have been reported, but in reality, their actions and safety are insufficient, and there are problems in terms of cost.

[0004]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide an excellent safety, TSR inhibitory activity, vasodilatory activity, epidermal moisturizing activity, cell proliferation activity, tyrosinase inhibitory activity,
An object of the present invention is to provide a cell activator and a cosmetic that are excellent in OD-like activity, antioxidant activity, or a combination thereof.
Another object of the present invention is to provide a hair nourishing material excellent in hair loss prevention and hair-growth action.

[0005]

According to the present invention, there is provided a genus Mao
(Boehmeria) A cell activator comprising a plant solvent extract as an active ingredient is provided. Further, according to the present invention, there is provided the cell activator wherein the solvent extract of the plant of the genus Mao (Boehmeria) as the active ingredient exhibits TSR inhibitory activity, epidermal moisturizing activity, cell growth activity or an activity combining these. Is done. Further, according to the present invention, there is provided a cosmetic containing the cell activator. Furthermore, according to the present invention, the TSR
A hair restoration comprising a cell activator exhibiting inhibitory activity is provided.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in more detail. The active ingredient of the cell activator of the present invention is a solvent extract of a plant of the genus Mao, which has a TSR inhibitory activity,
In addition to exhibiting cell activity such as vasodilator activity, epidermal moisturizing activity, cell proliferation activity, tyrosinase inhibitory activity, SOD-like activity, antioxidant activity, or an activity combining these, especially epidermal moisturizing activity required for cosmetics and the like It has excellent cell growth activity and the like, and further exhibits TSR inhibitory activity, and can be used as a hair restorer and the like, as well as various pharmaceuticals and quasi-drugs. The plants belonging to the genus Mao are perennial shrubs or small trees, and are widely distributed in tropical and temperate zones around the world, and their numbers are abundant. In addition, the fiber has been used for ropes, nets and the like for a long time, and is used as a hemostatic agent and fever, and the young shoots are used for edible use. Specific examples of plants belonging to the genus Mao include, for example, yabumao (Boehmeria longispica Ste
ud), Meabumao (Boehmeria platanifolia Franch. e)
t Sav.), Boehmeriaholosericea Blum
e), Nagahayabumao (Boehmeria sieboldiana Blum)
e), red scorpion (Boehmeria tricuspis Makino), coa scorpion (Boehmeria spicata Thumb.),
meria biloba Wedd.), Karamushi (Boehmeria nivea Ga)
ud.) and the like.

[0007] To prepare the active ingredient, for example, a method of immersing a desired portion of a plant of the genus Mao in a solvent to obtain an extract, and from the extract, desired cell activity, particularly TSR inhibitory activity, epidermal moisturizing activity, It can be produced by a method of further purifying a component exhibiting cell growth activity or the like, or a method of concentrating and drying the extract to obtain a solid extract. The site for solvent extraction of the plant of the genus Mao is not particularly limited, and may be any of leaves, stems, roots or a mixture thereof, or may be dried. At the time of solvent extraction, usually, a desired site of a plant of the genus Mao may be adjusted to about several mm and immersed in a solvent.

Examples of the solvent include hot water; lower alcohols such as methanol, ethanol, propanol, isopropanol and n-butanol; propylene glycol;
Glycols such as butylene glycol and polyethylene glycol; glycerins such as glycerin, diglycerin and triglycerin; ketones such as acetone and methyl ethyl ketone; various esters such as ethyl acetate and ethyl esters of fatty acids; Various polar organic solvents such as hydrogen; hydrates thereof, and mixtures thereof. These solvents can be heated or pH-adjusted as needed.

The time for immersing the plant of the genus Mao in a solvent varies depending on the type and temperature of the solvent, and is not particularly limited.
Usually, it is about 3 days or more, preferably about 7 to 15 days, particularly preferably about 8 to 10 days. The obtained extract can be used as an active ingredient as it is, or the extract is concentrated under reduced pressure to remove the solvent, and may be used as an extracted solid,
Furthermore, an extract or purified solid obtained by subjecting an extract or solid extract to a high concentration by adsorption, molecular sieving, centrifugation, ion exchange, various types of chromatography, or various purification steps in combination thereof can be used as an active ingredient.

The cell activator of the present invention may contain the extract as an active ingredient, and its content varies depending on the type of the extract, but is not less than 0.0001% by weight, preferably 0.1% by weight. What is necessary is just to contain 0001-20 weight%. If the amount is less than 0.0001% by weight, a desired cell activity may not be obtained, which is not preferable.

The cosmetic of the present invention contains the above-mentioned cell activator, and preferably exhibits at least one or more of TSR inhibitory activity, epidermal moisturizing activity, cell proliferation activity, and the like,
The dosage form is not particularly limited as long as it can be applied to the outer skin such as a liquid, emulsion, cream, gel, aerosol, and powder. As a kind of cosmetics,
Packing agents, haptics, plasters, shampoos, rinses, hair tonics, conditioners, scalp treatments, hair tonics, foundations, lotions, emulsions, bath agents, body cleansers, lotions, facial cleansers,
Toothpaste, mouth freshener, anti-inflammatory, soap, nutrition cream,
Examples include axillary odor inhibitor, deodorant agent, anti-bad breath agent, sensation agent, skin oil, antiseptic solution, ultraviolet ray inhibitor, powdery flour, etc. The desired effect is exhibited by blending a cell activator with these various cosmetics Can be done. The mixing ratio and form of the cell activator in the cosmetic can be appropriately selected according to the type of the above-mentioned cosmetics and the like, but the mixing ratio is usually the plant of the genus Mao which is the active ingredient in the cell activator. 0.0001% by weight or more, particularly preferably 0.0001 to 20% by weight in terms of solvent extract. If the amount is less than 0.0001% by weight, a desired cell activity may not be obtained, which is not preferable.

The cosmetics of the present invention contain active ingredients, oils and fats, surfactants, alcohols, fatty acids, and the like which are usually required according to the kind of the desired cosmetics.
Preservatives, bactericides, thickeners, antioxidants, pigments, fragrances, water-soluble polymers, ultraviolet absorbers, chelating agents, pH adjusters,
Other components such as a buffer, purified water or a mixture thereof can be appropriately blended. The mixing ratio of these other components is
It can be appropriately selected according to the type of cosmetic and the desired effect.

[0013] The hair restorer of the present invention contains a cell activator containing, as an active ingredient, a solvent extract of a plant of the genus Mao showing the TSR inhibitory activity. The blending ratio of this cell activator can be appropriately selected depending on the degree of purification and form of the contained solvent extract, but is usually calculated in terms of the solvent extract of the plant of the genus Mao, which is the active ingredient in the cell activator. , 0.0001% by weight or more, particularly 0.0001 to 20% by weight. 0.0
If the amount is less than 001% by weight, a desired TSR inhibitory activity or the like may not be obtained, which is not preferable.

The hair restoration of the present invention may contain various known materials usually contained in hair restoration. For example, an appropriate amount of a hair tonic, an antibacterial agent, a cooling agent, a humectant, or a mixture thereof can be added.

Examples of the hair restorer include nicotinic acid esters such as vitamin B ₆ , vitamin E and its derivatives, glycyrrhetinic acid and its derivatives, and benzyl nicotinate.
Cyclosporins, carpronium chloride, cepharanthin, oxendrone, diazoxide, minoxidil,
Ethynyl estradiol, estradiol, animal and plant extracts containing these, and the like can be mentioned. When used, they can be used alone or as a mixture. Examples of the antibacterial agent include hinokitiol, pyroctolamine, zinc pyrothione, hexachlorophen, phenol, benzalkonium chloride, cetylpyridium chloride, undecylenic acid, trichlorocarbanilide, and mixtures thereof. As a freshener,
Menthol and the like can be mentioned. As a moisturizer,
For example, polyhydric alcohols such as glycerin, propylene glycol, 1,3-butylene glycol, sorbitol, mannitol, polyethylene glycol, dipropylene glycol; NMF components such as amine acid, sodium lactate and sodium pyrrolidone carboxylate; hyaluronic acid;
Collagen; elastin; chondroitin sulfate; fibronectin; ceramides; heparin-like substances; water-soluble high-molecular substances such as chitosan or mixtures thereof.

The form of the hair restorer according to the present invention may be a usual liquid or the like, or may be a cream. Various additives that are usually added can be added to the hair restorer. As additives, for example, fats and oils, surfactants, alcohols, fatty acids, preservatives, antioxidants, dyes, fragrances, ultraviolet absorbers, chelating agents, pH adjusters, buffers,
Purified water and the like can be mentioned, and the blending amount can be appropriately selected.

[0017]

The cell activator of the present invention comprises a solvent extract of a plant of the genus Mao, which is sometimes edible, as an active ingredient.
Low toxicity, excellent TSR inhibitory activity, vasodilator activity,
Epidermal moisturizing activity, cell growth activity, tyrosinase inhibitory activity,
It exhibits cellular activity such as SOD-like activity, antioxidant activity, or an activity combining these. In addition, the solvent extract can exhibit a particularly strong TSR activity inhibitory activity, and exhibits excellent epidermal moisturizing activity and cell growth activity. It can also be used for quasi-drugs. Since the cosmetics and hair nourishes of the present invention contain a cell activator containing the solvent extract of the plant of the genus Mao, they show excellent moisturizing properties and cell activities such as cell proliferation,
In a hair restorer, TSR that causes hair loss can be safely suppressed and inhibited, and an excellent hair-growth effect can be obtained.

[0018]

The present invention will be described in more detail with reference to the following Examples, but it should not be construed that the invention is limited thereto.

Example 1 A total of 1 kg of leaves and stems of squid was cut into small pieces of about several mm, immersed in 3 liters of 90% by volume acetone solution, allowed to stand at room temperature for 1 week, and filtered to collect the filtrate. did. The filtrate was sufficiently concentrated under reduced pressure, and 6.9 of acetone-dried dried product was obtained.
6 g were obtained. The obtained dried product was dissolved in dimethylsulfoxide (DMSO) so as to have a concentration of 20000 ppm to prepare a sample solution.

<Keratinocyte cell proliferation test> In 5 ml of a K-GM medium (manufactured by Kurabo Industries) in which 5 × 10 ⁴ / μl of keratinocyte cells were suspended, 25 μl of the sample solution was added.
Was added so that the final concentration was 100 ppm in the medium. The keratinocyte cells were then cultured at 37 ° C.
The cells were cultured in an O ₂ incubator (CO ₂ concentration: 5%) for 5 days. At this time, the medium was changed every two days. After culturing, keratinocyte cells were determined by microscopic proliferation judgment using a microscope, cells were detached from the medium with a trypsin / EDTA solution, collected by centrifugation at 3000 rpm for 5 minutes, and counted using a hemocytometer (manufactured by Kayagaki Rika Kogyo Co., Ltd.). Evaluation of proliferation was performed.
As a control, the same evaluation was performed when no sample solution was added and when only the control (DMSO) was added. The evaluation was performed according to the following criteria. Table 1 shows the results. From the results in Table 1, it was found that the sample solution exhibited an excellent cell growth effect and was effective as a cell activator. Cell proliferation evaluation criteria ++: remarkable proliferation, +: proliferation, ±: proliferation tendency is observed but small,-: no proliferation.

[0021]

[Table 1]

<TSR activity inhibition test> tris-HCl
To 1.7 ml of buffer (pH 7.8), 75 μl of testosterone solution (5.8 mg / ml), NADPH solution (5.0 mg / ml of solution B) and 0.3 ml of the prepared sample solution were mixed. Next, 0.5 ml of a TSR enzyme solution (supernatant of a rat liver homogenate solution) was added, stirred, and incubated at 37 ° C. to start a reaction.
After 30 minutes, the reaction was stopped with 1 ml of dichloromethane.
Next, extraction was performed with 30 ml of dichloromethane. The dichloromethane layer was dried over anhydrous magnesium sulfate, filtered, and the filtrate was sufficiently concentrated under reduced pressure. 3 ml of methanol was added to the obtained filtrate to prepare a sample for measurement. For the obtained measurement sample, the testosterone peak was changed to H
It was detected by PLC and the TSR inhibition rate was calculated from the decrease (HPLC conditions: detection wavelength 240 nm, acetonitrile: water = 85: 15, flow rate 0.8 ml / min). As a result, the TSR activity was reduced to 50%, indicating that the sample solution exhibited extremely excellent TSR inhibitory activity. The TSR activity was 100% in the control without mixing the sample solution. From these results, it was found that the sample solution exhibited an excellent TSR activity inhibitory effect in addition to the cell activity effect.

<Moisturizing Test> The above prepared acetone-extracted dried product was dissolved in distilled water to prepare a 0.010% by weight aqueous solution (hereinafter, referred to as "Example 1 solution"). Example 1 The moisture retention test of the solution was performed by three panels. First, the inside of the forearm flexure of three panelists was wiped with 70% ethanol,
It was left for 10 minutes in an environment of 7 to 18 ° C and a relative humidity of 70% or less. Next, four test sites having an appropriate area were set as the portions wiped with the ethanol, and one drop of distilled water was dropped on each site. After 10 seconds, the water droplets were wiped off with dry gauze. Immediately thereafter, 30 seconds, 60 seconds, and 120 seconds later, the impedance of each part was measured using a vector impedance meter (manufactured by Hewlett-Packard). Next, after 30 minutes, the solution of Example 1, a 0.010% by weight aqueous solution of hyaluronic acid and a 0.010% by weight aqueous solution of squalane, which are known to have a moisturizing action, and distilled water as a control were added to each site after 30 minutes. 10 μl was applied to each site. Immediately after the application, one drop of distilled water was dropped on each site, and after 10 seconds, the water drops were wiped off with dry gauze.
Immediately thereafter, 30 seconds, 60 seconds, and 120 seconds later, the impedance of each part was measured using a vector impedance meter (manufactured by Hewlett-Packard). Based on these measurement results, the skin conductivity and the following formula were calculated.

[0024]

(Equation 1)

W ₀ : skin impedance immediately after water load W ₃₀ : skin impedance after 30 seconds water load W ₆₀ : skin impedance after 60 seconds water load W ₉₀ : skin impedance after 90 seconds water load W ₁₂₀ : Impedance of skin after 120 seconds of water load Further, each water retention ability was calculated by the formula (water retention ability (△ Ω △ ¹ ) = skin conductivity-skin conductivity). Figure 1 shows the results
Shown in At this time, the skin conductivity is correlated with the water retention ability, and the higher the skin conductivity, the higher the moisture retention. Therefore, from the results shown in FIG. 1, it can be seen that the solution of Example 1 has excellent moisture retention at the same concentration (0.010% by weight) as compared with the aqueous solution of hyaluronic acid and squalane, which is generally said to have high moisture retention. It can be seen that it can be used especially for cosmetics.

<Test of hair growth effect> C3H mice (6 weeks old,
(Weight: 18.3 to 20.5 g) The back of 12 animals was shaved with a hair clipper, and the hair was further removed under the trade name “Eva Claim S” (manufactured by Tokyo Tanabe Seiyaku Co., Ltd.). Confirmed that there is. Four days after hair removal, a measurement site of hair removal site 1 × 2 cm was set, and a sample solution prepared with 0.1 ml of the acetone-extracted and dried product in groups of 3 animals, a commercially available hair restorer (semble extraction paste) and a control were used. D
A solution of MSO: ethanol = 1: 1 twice a day (morning,
Evening), it was applied for 28 days. On the 10th, 15th, 17th, 20th, 24th and 28th days after the start of the application, the hair growth was photographed and the hair growth area was measured. In addition, the hair growth state was similarly observed for the group without application. In the measurement of the hair growth area, the weight of a 1 × 2 cm clear sheet is defined as T (the weight of the clear sheet corresponding to the entire measurement site), the clear sheet is placed on the measurement site, and a mark is placed on the hair growth site. The clear sheet at the marked position was cut out and the weight was defined as P (the weight of the clear sheet corresponding to the hair growth site), and this weight ratio (P / T) was used as the ratio of the hair growth area. The results are shown in Table 2, and the results up to the 15th day when the area where the sample solution was applied reached 100% are shown in FIG.
Shown in

As a result, it can be seen that the sample solution in this example has a hair growth effect in a very short time as compared with a commercially available hair restorer, and 100% hair growth is reproduced. Furthermore, since the hair growth was started from the 10th day onward in the non-application group, the hair growth was in a telogen rest period until the 10th day after the start of the test, but the hair growth period was entered after the 10th day. You can see that.
From this point, it can be seen that hair growth during the telogen resting period is not recognized at all in the control or commercial hair restorer, but in the present example, the hair growth effect can be exhibited even during the telogen resting period.

[0028]

[Table 2]

Example 2 A hair tonic having the following composition was prepared. (1) 2.0% by weight of dried acetone extract of yamaumao prepared in Example 1, (2) 0.1% by weight of resorcinol, (3) 0.05% by weight of β-glycyrrhizic acid, (4) l-menthol 0.1% by weight (5) Glycerin 10.0% by weight (6) Fragrance 0.3% by weight (7) Chelating agent 0.1% by weight (8) Ethanol 60.0% by weight (9) Purified water Residue.

Example 3 A shampoo having the following composition was prepared. (1) 2.0% by weight of dried acetone extract of yamaumao prepared in Example 1, (2) 15.0% by weight of sodium polyoxyethylene lauryl ether sulfate, (3) 10.0% by weight of triethanolamine lauryl sulfate (4) Alkanolamide 5.0% by weight (5) Glycol distearate 5.0% by weight (6) Propylene glycol 3.0% by weight (7) Benzoic acid 1.0% by weight (8) Fragrance 0.2 % By weight (9) Purified water Residue.

Example 4 A rinse having the following composition was prepared. (1) 2.0% by weight of dried acetone extract of yamabuma prepared in Example 1, (2) 2.0% by weight of stearyltrimethylammonium chloride, (3) 1.0% by weight of alkyltrimethylammonium chloride, (4) Polyoxyethylene stearyl ether 1.0% by weight (5) Glycer monostearate 3.0% by weight (6) Cetanol 1.0% by weight (7) Stearyl alcohol 1.0% by weight (8) Hysolve EPH 0.1% by weight % (9) Paraoxybenzoate 0.1% by weight (10) Fragrance 0.4% by weight (11) Purified water Residue.

Example 5 A hair cream having the following composition was prepared. (1) 2.0% by weight of dried acetone extract of yamaumao prepared in Example 1, (2) 0.2% by weight of stearic acid, (3) 1.0% by weight of liquid lanolin, (4) Liquid paraffin 0% by weight (5) Polyoxyethylene stearyl ether 1.5% by weight (6) Polyoxyethylene sorbitan monostearate 3.5% by weight (7) Paraoxybenzoate 0.1% by weight (8) 2-amino- 2-methyl-1-propanediol 0.1% by weight (9) Tetrasodium edetate 0.1% by weight (10) Propylene glycol 2.0% by weight (11) Fragrance 0.3% by weight (12) Purified water residue .

Example 6 A hair restorer having the following composition was prepared. (1) 2.0% by weight of dried acetone extract of yamaumao prepared in Example 1, (2) 0.1% by weight of dl-α-tocopherol acetate, (3) 0.1% by weight of pantothenyl ethyl ether, 4) Hinokitiol 0.1% by weight (5) l-menthol 0.1% by weight (6) Fragrance 0.3% by weight (7) Glycerin 10.0% by weight (8) Ethanol 40.0% by weight (9) Glycyrrhizin Dipotassium acid 0.1% by weight (10) Polyoxyethylene nonyl phenyl ether 1.0% by weight (11) Purified water Residue.

[Brief description of the drawings]

FIG. 1 is a graph showing the results of a moisture retention test performed in Example 1.

FIG. 2 is a graph showing the results of a hair growth effect test performed in Example 1.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code Agency reference number FI Technical display location A61K 35/78 ADA A61K 35/78 ADAC

Claims (5)

[Claims] 1. A cell activator comprising a solvent extract of a Boehmeria plant as an active ingredient. 2. The cell activator according to claim 1, wherein the solvent extract of Boehmeria plant as an active ingredient has testosterone 5α-reductase inhibitory activity. 3. The cell activator according to claim 1, wherein the solvent extract of Boehmeria plant as an active ingredient has an epidermal moisturizing activity and / or a cell growth activity. 4. A cosmetic comprising the cell activator according to claim 1. 5. A hair restorer comprising the cell activator according to claim 2.