JP2001288098A - Melanogenesis promoter and gray hair ameliorant - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain both a melanogenesis promoter excellent in safety and productivity and having an excellent melanogenic activity and a gray hair ameliorant comprising the melanogenesis promoter and extremely effective in preventing the gray hair and ameliorating the gray hair. SOLUTION: This melanogenesis promoter is characterized as consisting essentially of one or more plant extracts selected from Panax ginseng C.A. Meyer, Panax notoginseng, Salvia miltiorrhiza Bunge, Yucca sidigera or Yucca recurvifolia Salisb, Eriobotrya japonica Lindley, Lonicera japonica Thunberg and Salsaparrilha falsa. The gray hair ameliorant comprises the melanogenesis promoter.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a melanin production promoter capable of exerting an excellent melanin production promotion effect by acting on melanocytes (pigment-forming cells) present near hair matrix cells of hair roots, and a melanin production promoter therefor. And a gray hair improving agent effective for preventing and preventing gray hair.

[0002]

2. Description of the Related Art It has been found that the mechanism of white hair development is caused by the melanin pigment granules not being transferred to keratinocytes (hair). Although there is a theory that the number of melanocytes (pigment-forming cells) decreases, a theory that melanin-forming enzymes decrease, and a theory that impaired melanocyte pigment granule migration from melanocytes to keratinocytes, there is still a fundamental cause Has not yet been elucidated.

[0003] Therefore, in order to achieve the purpose of preventing and improving gray hair, components effective for the mechanism of gray hair development or melanin pigment formation (eg, tyrosinase activity promoting component, melanin production promoting component, etc.) are studied. Also, many proposals have been made to use various substances and compounds obtained as an active ingredient, which are obtained by examining the anti-grey action of various substances at random.

[0004] For example, ω-
It has been proposed that alkoxycarbonylalkylammonium and / or a salt thereof, and ω-alkoxycarbonylalkyltrialkylammonium and / or a salt thereof are effective (JP-A-7-316048 and JP-A-7-316048). . However, these are synthetic chemicals and there are concerns about safety.

[0005] Moreover, melanocyte cyclic AMP
A blackening agent for preventing white hair by improving the productivity has been proposed (JP-A-4-124122). An anti-whitening agent comprising water or ethanol extract of spinach as an active ingredient has been proposed (JP-A-5-78222). It has been proposed that a pressed product and / or an extract of a plant belonging to the genus Tangerine exhibits both a hair-growth effect and a gray-hair preventing effect (Japanese Patent Application Laid-Open No. 7-126129). A melanin production promoter comprising the essence of shellfish such as cockle, green mussel and oyster has been proposed (JP-A-7-28).
No. 5874). One type of melanin production-enhancing component of a basidiomycete culture or fungal extract group selected from the group consisting of Shimejiaceae, Agaricaceae, Sarnoshikomie, Licorice, Asteraceae, Novoliaceae, Moegitatake and Agaricaceae Alternatively, a hair material containing two or more types has been proposed (Japanese Patent Application Laid-Open No. 7-316026).

[0006] In addition, horsetail, honeysuckle, hikikoshi,
There has been proposed a gray hair inhibitor containing one or more selected from grape, loofah, elderberry, butcher bloom and syrup, or an extract thereof as an active ingredient (Japanese Patent Application Laid-Open No. 11-124318).

[0007] However, there is an extremely high demand for preventing the generation of gray hair and improving the generated gray hair as much as possible, regardless of age and gender, and it has a more effective, safe, mass-producible, and inexpensive melanin production promoting effect. The emergence of ingredients is eagerly awaited.

The present invention has been made in view of the above circumstances, and provides a safe and inexpensive melanocyte (pigment forming cell) present in the vicinity of a hair matrix of a hair root, which can exert an excellent melanin production promoting effect. Melanin production promoter,
It is another object of the present invention to provide a gray hair improving agent comprising the melanin production promoter, which has a remarkable effect on improving and preventing gray hair.

[0009]

Means for Solving the Problems and Embodiments of the Invention In order to achieve the above object, the present inventors have conducted intensive studies to find a component having a melanin production promoting action.
Panax ginseng, rice ginseng, tanjin, yucca, loquat,
One or more plant extracts selected from Kingkinka and salsa have an excellent melanin production promoting effect, these are plant extracts that have been popular since ancient times, and have high safety, Moreover, since it is present in a large amount in the natural world, it can be supplied stably and inexpensively, and a white hair improving agent consisting of a melanin production promoter containing these extracts as an active ingredient can prevent the generation of white hair and slightly reduce the generated white hair. However, they have found that they can sufficiently respond to the strong demands of consumers for improvement and can effectively solve the conventional problems, and have accomplished the present invention.

[0010] Therefore, the present invention is characterized by firstly comprising, as a main component, one or more plant extracts selected from Panax ginseng, Panax ginseng, Tanjin, Yucca, Loquat, Kingkinka and Salsa. A melanin production promoter. Secondly, the present invention provides a gray hair improving agent comprising the above melanin production promoter.

Hereinafter, the present invention will be described in more detail. The melanin production promoter of the present invention, Panax ginseng,
One or more plant extracts selected from rice ginseng, tanjin, yucca, loquat, goldfish, and salsa are the main components.

Here, the melanin production promoter of the present invention comprises:
The following plants are used as extraction raw materials.

[0013] The Panax ginseng is a Panax ginseng C.
A. (Meyer) root or the like is used as a raw material. The above-mentioned rice ginseng is Panax ginseng (Panax
Notoginseng root is used as a raw material. The tanzine is a tanzine (Sal) belonging to the Labiatae family.
Via Miltiorrhiza Bunge) is used as a raw material. The Yucca is a Yucca sigger belonging to the Agave family.
a and Yucca recurvifolia Sal
isb) Leaves and rhizomes are used as raw materials. The loquat is a loquat belonging to the family Rosaceae (Eriobotrya ja).
ponica Lindley) leaves and branches are used as raw materials. The goldfish is a honeysuckle (Lonicera japonica Thu) belonging to the honeysuckle family.
nberg) buds, flowers, leaves and stems (goldfish) are used as raw materials. As the salsa, salsa (Salsaparrilha falsa) bark and rhizome belonging to the lily family are used as raw materials.

All the extracts extracted using the above-mentioned raw materials have a high melanin production promoting effect. Among them, Panax ginseng and Yucca have an extremely high melanin production promoting effect. In addition, loquat, yucca, goldfish, and salsa are preferable in that the extract yield (solid content) is high. Further, loquat has a high tyrosinase activity promoting effect together with an excellent melanin production promoting effect.

The melanin production promoter of the present invention can be obtained from the above-mentioned plant-derived raw material by an extraction method generally used for extracting plants.

For example, it can be obtained by raw or dried plant raw material, or by pulverizing it as it is or using a crusher and subjecting it to solvent extraction. As a solvent used for extraction, a common solvent used for extracting an active ingredient from a plant can be used at a temperature from room temperature to the boiling point of the solvent or lower. For example, water, lower alcohols such as methanol, water-ethanol and ethanol or hydrated lower alcohols, acetone, 1,3-butylene glycol or an aqueous solution thereof, polar solvents such as propylene glycol, chloroform, ethyl acetate, ethyl ether, etc. Polar solvents and the like can be mentioned. When a mixed solvent of water and lower alcohols is used, it is usually preferable that the weight ratio of water to lower alcohols is 5:95 to 70:30. When a mixed solvent of water and 1,3-butylene glycol is used, the weight ratio of water: 1,3-butylene glycol is usually 5: 95-7.
It is preferably 0:30.

In this case, the extraction conditions vary depending on the raw materials to be extracted, the degree of crushing of the raw materials, the extraction solvent, and the like, and cannot be specified unconditionally. However, when water, ethanol-water, or ethanol is used as the extraction solvent, the extraction conditions are usually It is about 2 to 8 hours at 50 to 80 ° C. When 1,3-butylene glycol or an aqueous solution thereof or propylene glycol is used as the extraction solvent, it is usually at 50 to 90 ° C. for about 2 to 5 hours.

The extract obtained by extraction with these solvents can be used as an active ingredient of the melanin production promoter of the present invention by blending it as it is if the extraction solvent has high safety. An extract obtained by distilling the extraction solvent from the liquid, or an extract dried after drying as required, can also be blended.

The melanin production promoter of the present invention is absorbed percutaneously to reach the hair root site and acts on melanocytes (pigment forming cells) to exhibit an excellent melanin production promoting action. The easiest and most effective way to use this effect is
A white hair improving agent comprising a melanin production promoter is used by blending it into a hair material or any other external preparation for skin.

In this case, the hair and skin external preparations to be compounded are not particularly limited, but include, for example, hair tonic, hair liquid, hair gel, hair cream, scalp treatment, hair spray, emulsion, lotion, emollient lotion, Aerosol mousse, shampoo,
It can take the form of a rinse or the like. In addition, an optional auxiliary effective for enhancing the efficacy of the melanin production promoter can be appropriately blended into the hair preparation and the external preparation for skin.

The amount of the melanin production promoter of the present invention is
It is appropriately adjusted according to the use mode of the melanin production promoter.
It is preferable to mix in the range of 1 to 10% by weight.

The melanin production promoter of the present invention can be suitably used as an anti-vitilation therapeutic agent for skin, a skin cosmetic for blackening skin, etc., in addition to a white hair improving agent.

[0023]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to Production Examples, Examples and Comparative Examples, but the present invention is not limited to the following Examples.

Production Example 1 Panax ginseng root, rice ginseng root, tanjin whole plant, yucca leaf, loquat leaf, goldfish, and bark of salsa were each crushed using a crusher into 100 g of each crushed material. , Water as an extraction solvent, 50% by weight
Add 2000 mL of ethanol or ethanol and add 70 mL
After gently stirring for 3 hours while keeping the temperature at ° C., each extract was obtained by filtration with filter paper. After these extracts were concentrated under reduced pressure at 40 ° C., each extract was dried in a vacuum drier to obtain each dried extract. Table 1 shows the yields of the obtained dried extracts.

[0025]

[Table 1]

Production Example 2 Panax ginseng root, ginseng root, tanjin whole plant, yucca leaf, loquat leaf, goldfish and salsa bark were each crushed using a crusher into 100 g of each crushed material. 50% by weight of 1,
3-butylene glycol or propylene glycol in 1
After gently stirring for 3 hours while adding 000 mL and keeping the temperature at 50 ° C., each extract was obtained by filtration with filter paper. Table 2 shows the solid content concentration of each of the obtained extracts.

[0027]

[Table 2]

Example 1 Melanin Production Enhancing Effect 1 × 10 ⁶ B-16 melanoma cells were precultured in a 25 cm ² flask in a 10% FBS-Dulbecco minimal medium, 5% carbon dioxide, 95% air, and trypsinized. The cells were processed and collected. The collected 4.0 × 10 ⁵ cells were subjected to 10% FB
S-Dulbecco's minimum medium was inoculated into a φ60 mm Petri dish containing 5 mL, and cultured for 24 hours. Thereafter, each of the 50% by weight ethanol extracts (melanin production promoter) obtained in Production Example 1 shown in Table 1 was added to 100 μg / mL, 200 μL.
The culture was performed for 3 days after adding g / mL. After completion of the culture, cells were collected by trypsin treatment, and the total number of cells was calculated. Next, 5.0 × 10 ⁶ cells were collected and 10% DMSO-
3 mL of a 1N sodium hydroxide solution was added, and homogenized with an ultrasonic crusher to destroy cells. This is 3
The supernatant was centrifuged at 500 rpm, and the absorbance at 470 nm of the supernatant was measured using a spectrophotometer.

As a control, the absorbance at 470 nm was measured in the same manner as above except that each extract (melanin production promoter) of 50% by weight obtained in Production Example 1 shown in Table 1 was not added. Using the obtained absorbance, the melanin production enhancement rate was determined from the following formula. Table 3 shows the results.

(Equation 1) A: Absorbance at 470 nm without melanin production promoter (control) B: Absorbance at 470 nm with melanin production promoter

[0030]

[Table 3] From the results shown in Table 3, it is confirmed that Panax ginseng, Panax ginseng, Tanjin, Yucca, Loquat, Kingkinka and Salsa have a melanin production enhancing effect. In particular, Panax ginseng, Yucca, loquat and salsa have a high melanin production-enhancing effect.

Example 2 A test tube containing 1 ml of McClubine buffer (pH 6.8) was placed in a test tube for enhancing tyrosinase activity.
L, tyrosinase solution (50,000 uni, manufactured by Sigma)
t Mushroom-derived 4.5 mg / 15 mL)
3 mL of 5 mg of the loquat extract of 50% by weight ethanol obtained in Production Example 1 was dissolved in 5 ml of a 50% DMSO solution, and pre-incubated at 37 ° C. for 10 minutes (2
00 μg / mL sample solution). In a test tube, 1 mL of McClubine buffer (pH 6.8), 0.3 mL of tyrosinase solution (50,000 units from Sigma, 4.5 mg / 15 mL from mushroom), and 50% by weight of ethanol obtained in Production Example 1 5 mg of extract 10 mg
It was dissolved in 5 ml of a 0% DMSO solution and preincubated at 37 ° C. for 10 minutes (400 μg / mL sample solution).

The obtained 200 μg / mL and 400 μg
To each sample solution (0.9 mL / mL), 0.1 mL of a tyrosinase solution (50,000 units from Sigma, 2 mg / 2 mL from mushrooms) was added, and the mixture was added at 37 ° C. for 1 hour.
Incubated for 5 minutes. After the reaction was completed, the absorbance at 475 nm was measured with a spectrophotometer. As a blank, Macclebine buffer (pH 6.8) was used instead of the tyrosinase solution. As a control, 50% DMS was used instead of a 50% DMSO solution of loquat extract.
An O solution was used. The enhancement rate of tyrosinase activity was calculated from the obtained absorbance according to the following equation. Table 4 shows the results.

(Equation 2) St: Absorbance of test sample (with tyrosinase) Sb: Absorbance of blank sample (without tyrosinase) Ct: Test of control (50% instead of sample)
% DMSO solution) Absorbance Cb: Control blank (no tyrosinase added)
Absorbance

[0033]

[Table 4] From the results shown in Tables 3 and 4, it is recognized that loquat has both an excellent melanin production promoting effect and a high tyrosinase activity promoting effect.

[0034] Example 3, Comparative Example 1 modified for gray hair
8 male subjects, 32 male subjects, each with good effect gray hair
50% by weight of Production Example 1 shown in Table 1 after washing
A hair tonic having the composition shown in Table 5 in which the ethanol extract was dissolved was applied for 3 months, and the effect on improving white hair was evaluated according to the following criteria. Table 5 shows the results. In addition, the same evaluation was performed about the comparative product of the composition of Table 5. Evaluation Criteria A: 75% or more of the subjects showed "significant effect", "effective" and "moderately effective" B: 50% of the subjects showed "significant effect", "effective" and "moderately effective" % To less than 75% C: 25% to less than 50% of the subjects showed "excellent", "effective" and "moderately effective" D: Subject was "excellent", "effective" and "moderately effective" In this case, "effective" means that the gray hair has disappeared, and "effective"
Means that the gray hair is clearly reduced,
"Slightly effective" means that the gray hair is felt to be reduced, and "ineffective" means that no change is found in the gray hair.

[0035]

[Table 5] From the results in Table 5, it can be seen that all of the products of the present invention have a higher white hair improving effect than the comparative products. In particular, panax ginseng, radish ginseng, loquat, and yucca are recognized to have excellent white hair improving effects.

The formulation examples containing the extracts (melanin production promoters) obtained in Production Examples 1 and 2 are shown below.

Example 4 Hair tonic Panax ginseng 50% by weight ethanol extract 1.0% by weight hydrogenated castor oil EO (40) 2.0% by weight 95% ethanol 70.0% by weight Perfume Appropriate amount of purified water 100. 0% by weight (Production method) 50% by weight of ginseng in 95% ethanol
After adding ethanol extract, hydrogenated castor oil EO (40) and flavor, stirring and dissolving, purified water was added to obtain a hair tonic.

Example 5 Hair Tonic 50% by weight of Tanzan Carrots Ethanol Extract 1.0% by Weight Hardened Castor Oil EO (40) 2.0% by Weight 95% Ethanol 70.0% by Weight Perfume Appropriate amount of purified water 100.0% by weight (Preparation method) A 50% by weight ethanol extract of ginseng, a hydrogenated castor oil EO (40) and a fragrance were added to 95% ethanol and stirred to dissolve, and purified water was added to obtain a hair tonic.

Example 6 Hair tonic Polyethylene glycol 2000 2.0% by weight L-menthol 0.2% by weight Tanzine 50% by weight 1,3-butylene glycol extract 2.0% by weight 95% ethanol 50.0% by weight % Perfume Appropriate amount of purified water Residual total 100.0% by weight (Preparation method) Polyethylene glycol 2000, L-menthol, 95% ethanol and perfume are added to a 1,3-butylene glycol extract of 50% by weight, and the mixture is stirred and dissolved. Water was added to obtain the hair tonic.

Example 7 Hair Liquid Polyoxypropyl butyl ether (40PO) 15.0% by weight Polyoxypropyl butyl ether phosphoric acid (40PO) 15.0% by weight Yucca 50% by weight 1,3-butylene glycol extract 0% by weight 95% ethanol 50.0% by weight Perfume Appropriate amount of purified water Residual 100.0% by weight (Production method) 95% ethanol in Yucca 50% by weight 1,3-
A butylene glycol extract, polyoxypropyl butyl ether (40PO), polyoxypropyl butyl ether phosphoric acid (40PO) and a fragrance were added and dissolved by stirring, and purified water was added to obtain a hair liquid.

Example 8 Hair gel Carboxyvinyl polymer 0.5% by weight Polyvinylpyrrolidone 2.0% by weight Glycerin 4.0% by weight Loquat ethanol extract 3.0% by weight Polyoxyethylene octyl dodecyl ether Suitable amount Sodium hydroxide 0 .15 wt% ethyl alcohol 20.0 wt% Perfume Appropriate amount of purified water Residual 100.0 wt% (Preparation method) The carboxyvinyl polymer and glycerin were uniformly dispersed in a part of purified water. Next, the other components were dissolved in the remaining purified water, and this was added to the above-mentioned dispersion with stirring to obtain a hair gel.

Example 9 Hair gel Carboxyvinyl polymer 0.5% by weight Polyvinylpyrrolidone 2.0% by weight Glycerin 4.0% by weight Kingfisher ethanol extract 3.0% by weight Polyoxyethylene octyl dodecyl ether Suitable amount sodium hydroxide 0.15% by weight Ethyl alcohol 20.0% by weight Perfume Appropriate amount Purified water Residue 100.0% by weight (Preparation method) In the same manner as in Example 8, a hair gel was obtained.

Example 10 Hair gel Carboxyvinyl polymer 0.5% by weight Glycerin 50.0% by weight Salsa ethanol extract 2.0% by weight Polyoxyethylene octyl dodecyl ether proper amount Sodium hydroxide proper amount Ethyl alcohol 10.0% by weight Perfume Appropriate amount Edetic acid Appropriate amount Purified water Residue 100.0% by weight (Preparation method) In the same manner as in Example 8, a hair gel was obtained.

Example 11 Scalp treatment 1,3-propylene glycol 0.5% by weight Pentaerythritol tetra-2-ethylhexanate 1.2% by weight 95% ethanol 60.0% by weight Loquat 50% by weight ethanol extract 2.0% by weight Fragrance Appropriate amount DME / LPG (95/5) Appropriate amount 100.0% by weight (Preparation method) 50% ethanol extract of loquat in 95% ethanol, 1,3-propylene glycol, pentaerythritol tetra-2- Ethyl hexanate, fragrance and D
ME / LPG (95/5) was added and dissolved by stirring to obtain a scalp treatment.

Example 12 Scalp treatment 1,3-propylene glycol 0.5% by weight Pentaerythritol tetra-2-ethylhexanate 1.2% by weight 95% ethanol 60.0% by weight Panax ginseng 50% by weight ethanol extract 1.0% by weight Perfume Appropriate amount DME / LPG (95/5) Appropriate amount 100.0% by weight (Production method) Scalp treatment was obtained in the same manner as in Example 11.

Example 13 Hair Cream (Oil Phase) Liquid Paraffin 5.0% by weight Cetostearyl alcohol 5.0% by weight Vaseline 6.0% by weight Glycerin monostearate 3.0% by weight 2-octyldodecyl ether 3 6.% by weight butyl paraben 0.2% by weight Perfume Appropriate amount (aqueous phase) Dipropylene glycol 20.0% by weight Polyethylene glycol 4000 5.0% by weight Rice field ginseng 50% by weight Ethanol extract 2.0% by weight Glycerin 7. 0% by weight Sodium hexametaphosphate 0.005% by weight Purified water Residual total 100.0% by weight (Preparation method) After heating and dissolving the oil phase and mixing it, the heat-dissolved mixture of the aqueous phase was added thereto and emulsified with a homogenizer. Then, a hair cream was obtained.

Example 14 Hair Cream (Oil Phase) Liquid Paraffin 5.0% by weight Cetostearyl alcohol 5.0% by weight Vaseline 6.0% by weight Glycerin monostearate 3.0% by weight 2-octyldodecyl ether 3 0.0% by weight Butyl paraben 0.2% by weight Perfume Appropriate amount (aqueous phase) Dipropylene glycol 20.0% by weight Polyethylene glycol 4000 5.0% by weight Tanzine aqueous extract 3.0% by weight Glycerin 7.0% by weight Hexamethalic acid Soda 0.005% by weight purified water Residual total 100.0% by weight (Production method) In the same manner as in Example 13, a hair cream was obtained.

[Example 15] Hair spray (stock solution) Acrylic resin alkanolamine salt (50%) 7.0% by weight Cetyl alcohol 0.1% by weight Silicone oil 0.3% by weight Ethyl alcohol 92.4% by weight Yucca 50 0.2% by weight ethanol extract 0.2% by weight Perfume Appropriate amount (filling) Stock solution 50.0% by weight Dimethyl ether 45.0% by weight LPG 5.0% by weight Total 100.0% by weight (Production method) Acrylic resin alkanolamine salt (50
%), Cetyl alcohol and silicone oil were emulsified with a homogenizer, and this was added to other components to prepare a stock solution. For filling, a can was filled with the stock solution, and after attaching a valve, dimethyl ether and LPG gas were filled to obtain a hair spray. Example 16 Hair spray (stock solution) Acrylic resin alkanolamine salt (50%) 7.0% by weight Cetyl alcohol 0.1% by weight Silicone oil 0.3% by weight Ethyl alcohol 92.4% by weight Kingkinka 50% by weight ethanol Extract 0.3% by weight Appropriate amount of perfume (filling) Undiluted solution 50.0% by weight Dimethyl ether 45.0% by weight LPG 5.0% by weight Total 100.0% by weight (Preparation method) Obtained.

[0049]

Industrial Applicability According to the present invention, a melanin production promoter having excellent safety and productivity and having excellent melanin production ability, and a melanin production promoter comprising this melanin production promoter, which is very effective for preventing and improving gray hair Agent is obtained.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (reference) A61P 17/00 A61P 17/00 F term (reference) 4C083 AA111 AA112 AB032 AC012 AC022 AC072 AC102 AC122 AC172 AC182 AC422 AC432 AC442 AC482 AC612 AC902 AD042 AD072 AD092 AD112 AD152 AD532 CC32 CC33 CC37 EE24 4C088 AB12 AB16 AB38 AB51 AB85 AC05 AC11 BA08 MA17 MA28 MA63 ZA92 ZC02

Claims (2)

[Claims] 1. Panax ginseng, rice ginseng, tanjin,
A melanin production promoter comprising one or more plant extracts selected from yucca, loquat, goldfish and salsa as a main component. 2. A white hair improving agent comprising the melanin production promoter according to claim 1.