Composition for inhibiting hair graying, and use thereof

Abstract

To provide a composition for inhibiting hair graying capable of effectively inhibiting the occurrence of gray hair, and a use of the composition.SOLUTION: The composition for inhibiting hair graying activates the Wnt / β-catenin signaling pathway to promote melanin synthesis in hair, thereby having remarkably excellent hair graying (canities) inhibition, prevention, improvement, alleviation, delaying, or treatment effects.SELECTED DRAWING: Figure 1

Description

[Technical field]

[0001] The present invention relates to a composition for inhibiting the occurrence of gray hair, which has an excellent effect of inhibiting the occurrence of gray hair, and uses thereof. [Background technology]

[0002] Gray hair occurs due to aging of the scalp. Gray hair includes canities and hair graying. Depending on the extent of gray hair, the person with gray hair may appear older than their actual age. Changes in hair color can be recognized as a sign of aging, and the appearance of gray hair that is not appropriate for one's age can act as stress for an individual and have a negative impact on self-esteem. Therefore, various research and development efforts in cosmetics are being conducted to improve gray hair.

[0003] Although hair dyeing is a method for preventing gray hair, the effect of hair dyeing is temporary because gray hair continues to grow as hair grows. Therefore, this method has a disadvantage that hair must be dyed periodically. In addition, conventional oxidative hair dyes may damage the scalp and skin. In addition, black soybean or Houttuynia cordata extracts are used to prevent gray hair, but the effect is difficult to feel.

[0004] The main cause of gray hair is the disappearance of melanocyte stem cells (MSCs) or a decrease in the physiological activity of melanocytes. This reduces the amount of melanin produced by melanocytes in the matrix of hair, eyebrows, and eyelashes, causing the hair to turn white or gray. The melanin produced by melanocytes is transferred to keratinocytes to produce pigmented head hair or body hair. If melanin cannot move to keratinocytes, the hair will lack pigment and gray hair will occur.

[0005] The amount and relative ratio of eumelanin, which is brown and black, and pheomelanin, which is yellow and red, greatly affect the color of hair and body hair. Three enzymes, tyrosinase, DHICA oxidase (TRP-1), and DOPAchrome tautomerase (TRP-2), are involved in the production of melanin, and the activity of these enzymes is known to affect the synthesis of melanin. In this process, tyrosinase catalyzes the oxidation of tyrosine to DOPA and the oxidation of DOPA to dopaquinone. This substance, known as L-dopaquinone or o-dopaquinone, is the precursor of melanin. In the presence of cysteine, dopaquinone spontaneously cyclizes to dopachrome, which is tautomerized to DHICA by dopachrome tautomerase (TRP-2). TRP-1 oxidizes DHICA to form a quinone derivative.

[0006] Among these enzymes, tyrosinase and TRP-1 are expressed in melanocytes around the hair bulb and dermal papilla during the anagen phase of the hair follicle growth cycle, but are not expressed during the catagen and telogen phases.

[0007] As mentioned above, gray hair is affected by both melanocytes and melanocyte stem cells. Also, as melanocytes decrease, melanin production gradually decreases and melanin transmission decreases. This decrease in melanin can manifest as pigmentation disorders in the skin. A representative example of a pigmentation disorder is vitiligo, and one of the causes of vitiligo is the decrease or destruction of melanocytes. Activation of the Wnt / β-catenin pathway has been extensively studied as a method for treating vitiligo (Journal of Investigative Dermatology (2015) 135, 2921-2923). It has also been reported that activating the Wnt signaling mechanism in melanocyte stem cells increases pigment production in hair and epidermal melanocytes (Cell, Vol 145, Issue 6, 10, (2011), pp. 941-955; Medical Research Review (2016), Vol 37, issue 4, 907-945). Summary of the Invention [Problem to be solved by the invention]

[0008] An object of the present invention is to provide a composition for inhibiting gray hair that can effectively inhibit the occurrence of gray hair. Another object of the present invention is to provide a use of the composition for inhibiting the occurrence of gray hair. [Means for solving the problem]

[0009] The present inventors have conducted extensive research into substances capable of effectively inhibiting gray hair, including canities, and as a result have found that the present invention is capable of effectively inhibiting canities, including escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engeletin, specnuezhenide, praeruptorin B, rotunic acid, sesamosides, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, or platycodin D2. D2) activates the Wnt / β-catenin pathway. In addition, it was found that the above substances have the effect of increasing melanin synthesis in B-16 mouse melanoma cells. The present inventors have confirmed that when one or more of the above substances, which have excellent activation effects of the Wnt / β-catenin pathway, are applied (or coated) to the skin, the effect of inhibiting or improving gray hair is significantly excellent, and have completed the present invention.

[0010] The present invention provides a composition for inhibiting gray hair, comprising at least one selected from the group consisting of Escin, 27-Deoxyactein, Lysionotin, Nitidine chloride, Lanosterol, Engeletin, Specnuezhenide, Praeruptorin B, Rotunic acid, Sesamoside, Polygalacin D, Momordin Ic, Valechlorine, Tussilagone, Periplocin, Polyphyllin VII, and Platycodin D2. The composition for inhibiting gray hair may contain one or more of the above substances as active ingredients.

[0011] In the present invention, "suppression" of gray hair means suppressing the amount or frequency of gray hair occurrence, or suppressing the change from black hair to gray hair or the aging process. In one embodiment, "suppression" of gray hair may mean activating the Wnt / β-catenin pathway to promote melanin synthesis in hair. In one embodiment, the composition for suppressing gray hair of the present invention can be used for applications such as suppression, prevention, improvement, mitigation, delay or treatment of gray hair (canyostosis), and can be used for any application without limitation as long as it is for cosmetic purposes to improve gray hair. The "prevention" may mean any action of delaying the occurrence, growth or proliferation of gray hair by applying the composition of the present invention. The "treatment" may mean any action of improving or benefiting gray hair or canyostosis by applying the composition of the present invention to suppress the growth and proliferation of gray hair.

[0012] In one embodiment, the composition for inhibiting gray hair of the present invention includes Escin, 27-Deoxyactein, Lysionotin, Nitidine chloride, Lanosterol, Engeletin, Specnuezhenide, Praeruptorin B, Rotunic acid, Sesamoside, Polygalacin D, Momordin Ic, Valechlorine, Tussilagone, Periplocin, Polyphyllin VII, and Platycodin D2. D2) may contain at least one selected from the group consisting of 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition. If the content of the substance is less than 0.0001% by weight, the effect of inhibiting gray hair is insignificant, and if it exceeds 50% by weight, the stability of the formulation is poor, which is undesirable.

[0013] In one embodiment, the composition for inhibiting gray hair of the present invention can be used as a pharmaceutical composition, a quasi-drug composition, or a cosmetic composition. In addition, the composition for inhibiting gray hair of the present invention can be formulated into any form that is generally applicable to the skin. Preferably, the composition for inhibiting gray hair of the present invention can be formulated into a form of an external preparation for the skin. For example, the external preparation for the skin can be prepared into a form that is generally applicable to the skin, such as a liquid, cream, paste, or solid. In addition, the composition for inhibiting gray hair of the present invention can be provided as a composition or product for hair or scalp. For example, by adding a conventional additive, it can be prepared into a composition such as a shampoo, tonic, hair conditioner, hair lotion, gel, pack, cream, essence, powder, spray, oil, soap, liquid cleanser, liquid hair dye type, or aerosol type for inhibiting gray hair, but is not limited thereto. In the following Preparation Example 1 or 2 of the present invention, the composition for inhibiting gray hair was prepared into a hair tonic or hair lotion form.

[0014] In one embodiment, when the composition for inhibiting gray hair of the present invention is liquid, the carrier component may include a solvent, a solubilizer, or an emulsifier. The carrier component may include, for example, at least one selected from the group consisting of water, alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol, or fatty acid ester of sorbitan. The alcohol may be any commonly used alcohol. Preferably, linear or branched C2-C4 monoalcohols are used, and more preferably, ethanol or isopropanol is used, but is not limited thereto.

[0015] In one embodiment, when the formulation of the composition for inhibiting gray hair of the present invention is a paste, cream or gel, the carrier component may be animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicon, bentonite, silica, talc, zinc oxide, etc. Also, the carrier component may be alcohol, preferably isopropanol, but is not limited thereto.

[0016] In one embodiment, when the composition for inhibiting gray hair of the present invention is in the form of a powder or spray, the carrier component may include lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder. When the composition is in the form of a spray, the carrier component may further include a propellant such as chlorofluorohydrocarbon, propane / butane, or dimethyl ether.

[0017] In one embodiment, the composition for inhibiting gray hair of the present invention may contain ingredients that are generally usable in external skin preparations, for example, one or more additives selected from the group consisting of water, surfactants, moisturizers, lower alcohols, chelating agents, bactericides, antioxidants, preservatives, colorants, and fragrances.

[0018] In one embodiment, the composition for inhibiting gray hair of the present invention may be used in a transdermal administration method, such as directly applying or spraying on the skin. The term "administration" means that the composition for inhibiting gray hair of the present invention is introduced into the body in any suitable manner. The administration route of the composition for inhibiting gray hair of the present invention may be any common route that can reach the target tissue. Preferably, the composition for inhibiting gray hair of the present invention may be administered transdermally, and more preferably, may be applied topically. The number of applications of the composition for inhibiting gray hair of the present invention may be determined according to the prescription, need, or purpose.

[0019] In one embodiment, the amount of the composition for inhibiting gray hair of the present invention to be used can be appropriately adjusted depending on the dosage form and individual differences such as age and degree of lesion. In addition, the composition for inhibiting gray hair of the present invention is preferably used by applying an appropriate amount to the scalp once to several times a day for one week to several months. In Experimental Example 3 of the present invention, the composition for inhibiting gray hair (hair tonic) was used 7 times a week for 6 months. From the results of Experimental Example 3, it was confirmed that the use of the hair tonic had a superior effect of inhibiting gray hair compared to the placebo control group of the comparative example. In particular, a dosage form containing ethanol was confirmed to have a higher effect of preventing hair loss and promoting hair growth.

[0020] In one embodiment, a kit for inhibiting gray hair is provided, which includes the composition for inhibiting gray hair of the present invention. In yet another embodiment, the kit refers to a set including a composition and accessories necessary for preventing or treating gray hair. In yet another embodiment, the accessories included in the kit are tools or devices that are commonly used in the technical field to which the present invention belongs for preventing or treating gray hair. In yet another embodiment, the kit may further include a prescription that discloses any one or more selected from the group consisting of the dosage, administration route, administration frequency, and indication (gray hair syndrome) of the ingredients.

[0021] In one embodiment, the present invention provides a method for inhibiting gray hair, comprising applying a composition for inhibiting gray hair to a subject. In yet another embodiment, the subject may be a human in need of inhibiting gray hair. Preferably, in the method, the composition for inhibiting gray hair may be applied to the subject in an effective amount. The term "effective amount" refers to an amount of an active ingredient sufficient to inhibit, delay, improve or alleviate gray hair, or to provide a therapeutic or cosmetic benefit in the treatment or management of gray hair. The term "effective amount" also refers to an amount sufficient to inhibit or reduce the occurrence of gray hair, either in vitro or in vivo. The method for inhibiting gray hair may have an effect of inhibiting or improving gray hair by activating the Wnt / β-catenin signaling pathway to promote melanin synthesis in hair.

[0022] In one embodiment, the present invention provides a use for inhibiting gray hair, characterized by using the composition for inhibiting gray hair. In one embodiment, the use may include any use for inhibiting or improving gray hair. For example, it may include a pharmaceutical use, a cosmetic use, or a beauty use. In another aspect, the use for inhibiting gray hair may have an effect of inhibiting or improving gray hair by activating the Wnt / β-catenin signaling pathway to promote melanin synthesis in hair.

[0023] In one embodiment, the present invention provides a method for preparing a composition for inhibiting gray hair, comprising at least one selected from the group consisting of Escin, 27-Deoxyactein, Lysionotin, Nitidine chloride, Lanosterol, Engeletin, Specnuezhenide, Praeruptorin B, Rotunic acid, Sesamoside, Polygalacin D, Momordin Ic, Valechlorine, Tussilagone, Periplocin, Polyphyllin VII, and Platycodin D2. In the above-mentioned production method, the composition for inhibiting hair graying can be produced by the production method of commonly used cosmetics, quasi-drugs, or pharmaceuticals.

[0024] In one embodiment, the composition for inhibiting gray hair of the present invention may include two or more selected from the group consisting of Escin, 27-Deoxyactein, Lysionotin, Nitidine chloride, Lanosterol, Engeletin, Specnuezhenide, Praeruptorin B, Rotunic acid, Sesamoside, Polygalacin D, Momordin Ic, Valechlorine, Tussilagone, Periplocin, Polyphyllin VII, and Platycodin D2.

[0025] In one embodiment, the composition for inhibiting gray hair of the present invention does not contain any of the disclosed ingredients in excess of the maximum usage values ​​stipulated in various standards related to cosmetics, food, medicines, and quasi-drugs. Effect of the Invention

[0026] The composition for inhibiting gray hair of the present invention can effectively inhibit the occurrence of gray hair. The composition for inhibiting gray hair of the present invention activates the Wnt / β-catenin signaling pathway to promote the synthesis of melanin in hair, and is therefore remarkably effective in inhibiting, preventing, improving, alleviating, delaying or treating gray hair (canyosia). [Brief description of the drawings]

[0027] [Figure 1] These are experimental results confirming that escin increased melanin synthesis in B-16 melanoma cells. [Diagram 2] 1 is a graph showing an increase in melanin synthesis depending on escin and its content. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0028] The present invention will be described in detail below with reference to examples to aid in understanding the present invention. However, the examples according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following examples. The examples of the present invention are provided to more completely explain the present invention to those with average knowledge in the art.

[0029] Experimental Example 1: Increased effect of Wnt / β-catenin signal transduction In this experiment, TCF / LEF Responsive Luciferase Reporter HEK293A stable cell line (Wnt Reporter HEK293A cell; WRHEK293A) was used to confirm the activation of the Wnt / β-catenin pathway. The stable cell line was maintained by subculture using MEM (Corning, USA) and fetal bovine serum (Gibco BRL, Gaithersburg, MD, USA). For the transcription activation assay, 30,000 cells were seeded per well in a 96-well plate and then cultured in an incubator at 37°C for 24 hours. The cells were treated with escin, 27-deoxyactin, ricionotin, nitidine chloride, lanosterol, engeletin, specnuezenide, praeruptorin B, rotunic acid, sesamosid, polygalacin D, momordin Ic, valechlorin, tusilagon, periplosin, porphyrin VII, and platycodin D2 according to the present invention, as shown in Table 1. After culturing for 24 hours, reporter assay was performed using a Luciferase assay system (Promega). Luminescence was measured using a Victor multiwall plate reader (PerkinElmer, USA) according to the manufacturer's experimental method. To confirm the cytotoxicity caused by the substance treatment, the fluorescence expression of GFP was measured in parallel as an internal control. The luminescence value from the luciferase reaction was divided by the GFP fluorescence value, and the value of the untreated control group was set to 100%, and the corresponding values ​​of the treated groups were calculated and expressed as a percentage (%) (Table 1).

[0030] [Table 1]

[0031] Experimental example 2: Confirmation of melanin production effect In this experiment, the compound of Experimental Example 1, which shows an effect of increasing Wnt signaling, was added to the culture medium of B-16 mouse melanoma cells to examine the melanin production effect at the cellular level (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980). Before the experiment, the toxicity of B-16 melanoma cells was evaluated, and a non-toxic concentration was selected to evaluate melanin production. B-16 melanoma cells were subcultured in DMEM (Gibco BRL, Gaithersburg, MD, USA) containing 10% FBS. After that, for melanin synthesis and extraction, the cells were seeded on a 100 mm cell culture dish, and treated with the compound when the confluency was 70%. The compound was treated in the culture medium at a concentration of 10 μg / mL. Alpha-melanocyte stimulating hormone (alpha-MSH) was used as a control. It was added to the culture medium at 10 nM, and then each was treated with B-16 molanomas and cultured for 48 hours. The cells were then trypsinized to remove them from the culture vessel, and centrifuged to extract melanin. The removed cells were added with 1 mL of sodium hydroxide solution (1N concentration) and boiled for 10 minutes to dissolve the melanin. The absorbance was measured at 400 nM using a spectrophotometer to measure the amount of melanin produced. The amount of melanin was quantified in μg / mL units using a standard absorbance curve according to the concentration of melanin. The untreated control group was set as 100%, and the values ​​of the treated groups were calculated relative to this and expressed as a percentage (%) (Table 2).

[0032] [Table 2]

[0033] The melanin synthesis results of escin among the above compounds are shown in FIG. 1 and FIG.

[0034] Experimental Example 3: Test to confirm the effect of the composition 1 for inhibiting gray hair (hair tonic) in inhibiting the occurrence of gray hair A composition 1 (hair tonic) for inhibiting gray hair containing escin and 27-deoxyactein among the compounds of the present invention was prepared. The composition was used to test the effect of reducing gray hair in human hair. Sixty healthy adults with gray hair were divided into five groups of 12 people each, and Comparative Example 1, Example 1, Example 1-2, Example 2, or Example 2-2 was applied to the scalp seven times a week for six months. After use, the degree of gray hair occurrence was evaluated using a Folliscope phototrichogram in comparison with before application of the composition. The experimental results are shown in Table 3, with the values ​​before application taken as 100%.

[0035] [Table 3]

[0036] Production Example 1: Composition 1 for inhibiting gray hair (hair tonic) Hair tonics of the present invention were prepared by a conventional method using escin, 27-deoxyactein, ricyonotin, nitidine chloride, lanosterol, engeletin, specnuezenide, praeruptorin B, rotunic acid, sesamosid, polygalacin D, momordin Ic, valechlorin, tusilagon, periplosin, porphyrin VII or platycodin D2 according to the formulation shown in Table 4 below.

[0037] [Table 4]

[0038] Production Example 2: Composition 2 for inhibiting gray hair (hair lotion) Hair lotions were prepared by a conventional method using escin, 27-deoxyactein, ricyonotin, nitidine chloride, lanosterol, engeletin, specnuezenide, praeruptorin B, rotunic acid, sesamosid, polygalacin D, momordin Ic, valechlorin, tusilagon, periplosin, porphyrin VII or platycodin D2 of the present invention according to the formulation shown in Table 5 below.

[0039]

Table 5

Claims

1. Escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engeletin, specnuezhenide, praeruptorin B, rotunic acid, sesamosides, polygalacin D, momordin Ic A composition for inhibiting gray hair, comprising at least one selected from the group consisting of: Valechlorine, Tussilagon, Periplocin, Polyphyllin VII, and Platycodin D2.

2. The above-mentioned escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engeletin, specnuezhenide, praeruptorin B, rotunic acid, sesamosides, polygalacin D, momordin Ic, 13. The composition for inhibiting gray hair according to claim 1, wherein the one or more selected from the group consisting of 0.0001 to 50% by weight of the total weight of the composition is selected from the group consisting of 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,19,20,21,22,23,24,25,26,27,28,29,30,31,32,33,34,35,36,37,38,39,40,41,42,43,50,51,60,71,72,

3. The composition for inhibiting gray hair according to claim 1, which activates the Wnt / β-catenin signaling system.

4. The composition for inhibiting gray hair according to claim 1 , which is a pharmaceutical composition, a quasi-drug composition or a cosmetic composition.

5. A hair or scalp product for inhibiting gray hair, comprising the composition for inhibiting gray hair of claim 1.

6. A kit for inhibiting gray hair, comprising the composition for inhibiting gray hair according to claim 1.

7. A method for inhibiting gray hair, comprising applying the composition for inhibiting gray hair according to claim 1 to a subject.

8. Use of the composition for inhibiting gray hair according to claim 1 for inhibiting gray hair.

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