Composition for inhibiting white hair and use thereof

Abstract

The present invention relates to a composition for inhibiting white hair having an excellent effect of inhibiting the generation of white hair and use thereof. The composition for inhibiting white hair of the present invention has an excellent effect of inhibiting, preventing, ameliorating, alleviating, delaying or treating white hair (poliosis) by promoting the synthesis of melanin in hair through the activation of the Wnt / β-catenin signaling pathway.

Description

Technical Field

[0001] This invention relates to a composition for inhibiting gray hair with excellent effect in inhibiting the production of gray hair and its use. Background Technology

[0002] Gray hair appears as the scalp ages. Gray hair includes canities (white hair) and hair graying (hair turning white). Depending on its degree, gray hair makes a person appear older than their actual age. Changes in hair color can be considered a sign of aging, and the appearance of gray hair that is inconsistent with one's age can cause stress and negatively impact self-esteem. Therefore, various research and developments are underway to improve gray hair for cosmetic purposes.

[0003] Even if hair dyeing is used to improve gray hair, gray hair will continue to grow as the hair grows back, so the dyeing method has the disadvantage of being only temporarily effective. Therefore, the above-mentioned hair dyeing methods also have the disadvantage of needing to be dyed regularly. In addition, conventional oxidative hair dyes may damage the scalp and skin. Furthermore, extracts such as black beans or red Polygonum multiflorum are used to improve gray hair, but the disadvantage is that the effect is not noticeable.

[0004] The main cause of gray hair is the loss of melanocyte stem cells (MSCs) or a decrease in the physiological activity of melanocytes. This results in a reduction in the amount of melanin produced by melanocytes in the hair matrix (hair, eyebrows, eyelashes, etc.), leading to whitening or graying of the hair. Melanin produced by melanocytes is transferred to keratinocytes to form pigmented hair (head hair) or body hair. If melanin cannot move to keratinocytes, the hair lacks pigment, resulting in gray hair.

[0005] The amount and relative proportion of eumelanins (brown and black) and phenomelanins (yellow and red) significantly influence the color of hair and body hair. It is known that three enzymes—tyrosinase, DHICA oxidase (TRP-1), and DOPAchrome tautomerase (TRP-2)—are involved in melanin production, and the activity of these enzymes affects melanin synthesis. In this process, tyrosinase catalyzes the oxidation of tyrosine to DOPA, and DOPA is then oxidized to dopaquinone. This substance, called L-dopaquinone or o-dopaquinone, is a precursor to melanin. The aforementioned dopaquinone undergoes spontaneous cyclization in the presence of cysteine ​​to form dopachrome, which then undergoes tautomerism via dopachrome tautomerase 2 (TRP-2) to form DHICA. TRP-1 oxidizes the aforementioned DHICA to form quinone derivatives.

[0006] Of the enzymes mentioned above, tyrosinase and TRP-1 are expressed in melanocytes surrounding 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 earlier, gray hair is influenced by melanocytes and melanocyte stem cells. Furthermore, a decrease in melanocytes leads to a gradual reduction in melanin production and transmission. This reduction in melanin manifests in pigmentary disorders of the skin. A representative example of a pigmentary disorder is vitiligo, one of the causes of which is the reduction or destruction of melanocytes. Moreover, activation of the Wnt / β-catenin pathway has been extensively studied as a treatment for vitiligo (Journal of Investigative Dermatology (2015) 135, 2921-2923). Additionally, it has been reported that activation of the Wnt signaling mechanism in melanocyte stem cells increases pigment production in hair and epidermal melanocytes (Cell, Vol 145, Issue 6, 10, (2011), 941-955)(Medical Research Review (2016), Vol 37, Issue 4, 907-945). Summary of the Invention

[0008] Technical issues

[0009] The problem to be solved by the present invention is to provide a composition for inhibiting gray hair that can effectively suppress the production of gray hair.

[0010] In addition, the present invention aims to provide a use of the above-described composition for inhibiting the production of gray hair.

[0011] Technical solution

[0012] In order to discover substances that can effectively inhibit gray hair, including the aforementioned gray hair syndrome, the inventors of this invention have made unremitting research efforts. As a result, they discovered that the following substances activate the Wnt / β-catenin pathway: escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engleletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, or platycodin D2. Furthermore, it was discovered that the above-mentioned substances have the effect of increasing melanin synthesis in B-16 mouse melanoma cells. The inventors of this invention confirmed that when any one or more of the above-mentioned substances with excellent Wnt / β-catenin pathway activation effects are applied to the skin, the effect of inhibiting or improving gray hair is significantly superior, thus completing this invention.

[0013] This invention provides a composition for inhibiting gray hair, comprising one or more of the following: escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, enegeletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, and platycodin D2. The above-mentioned composition for inhibiting gray hair may contain one or more of the above-mentioned substances as active ingredients.

[0014] In this invention, "inhibition" of gray hair can mean inhibiting the amount or frequency of gray hair production, or inhibiting the process of change or aging from black hair to gray hair. In one embodiment, "inhibition" of gray hair can mean promoting melanin synthesis in hair by activating the Wnt / β-catenin pathway. In one embodiment, the gray hair inhibition composition of this invention can be used for the inhibition, prevention, improvement, relief, delay, or treatment of gray hair (leukothrix), and can also be used without limitation for any purpose, as long as it is for cosmetic purposes of improving gray hair. The aforementioned "prevention" can mean all actions that delay the production, growth, or proliferation of gray hair by applying the composition of this invention. The aforementioned "treatment" can mean all actions that improve or beneficially change gray hair or leukothrix by inhibiting the growth and proliferation of gray hair by applying the composition of this invention.

[0015] In one embodiment, the composition for inhibiting gray hair of the present invention may contain 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, relative to the total weight of the composition, one or more of the above-mentioned ingredients selected from the group consisting of escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engleletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, and platycodin D2. When the content of the above substances is less than 0.0001% by weight, the effect of inhibiting gray hair is weak; when it exceeds 50% by weight, the stability of the dosage form decreases, so it is not preferred.

[0016] In one embodiment, the gray hair suppression composition of the present invention can be used as a pharmaceutical composition, a quasi-pharmaceutical composition, or a cosmetic composition. Furthermore, the gray hair suppression composition of the present invention can generally be formulated into any form applicable to the skin. Preferably, the gray hair suppression composition of the present invention can be formulated into a topical skin agent. For example, the aforementioned topical skin agent formulation can be prepared into a formulation applicable to the skin, such as a liquid, cream, ointment, or solid. Additionally, the gray hair suppression composition of the present invention can be provided as a hair or scalp composition or product, for example, by adding conventional additives to prepare a composition for suppressing gray hair such as a shampoo, tonic, hair conditioner, hair lotion, gel, hair mask, cream, serum, powder, spray, oil, soap, liquid cleanser, liquid hair dye type, or aerosol type, but is not limited thereto. In the following preparation examples 1 or 2 of the present invention, the gray hair suppression composition is prepared into a hair tonic or hair lotion formulation.

[0017] In one embodiment, when the composition for inhibiting gray hair of the present invention is liquid, the carrier component may include a solvent, a solubilizing agent, or an emulsifying agent. The carrier component may include one or more fatty acid esters selected from, for example, water, alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylethylene glycol oil, glycerol aliphatic esters, polyethylene glycol, or sorbitol. The alcohol may be a commonly used alcohol, preferably a linear or branched C2-C4 monohydric alcohol, more preferably ethanol or isopropanol, but is not limited thereto.

[0018] In one embodiment, when the dosage form of the gray hair suppression composition of the present invention is a cream, lotion, or gel, animal oils, vegetable oils, waxes, paraffin wax, starch, astragalus gum, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc, or zinc oxide can be used as the carrier component. Additionally, alcohols can be used as the aforementioned carrier component. Isopropanol is preferred, but not limited thereto.

[0019] In one embodiment, when the dosage form of the gray hair suppression composition of the present invention is a powder or spray, the carrier component may include lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder. When the dosage form is a spray, it may further include a propellant, such as chlorofluorocarbon, propane / butane, or dimethyl ether.

[0020] In one embodiment, the gray hair inhibition composition of the present invention may contain ingredients that are typically used in topical skin preparations, and may additionally contain one or more additives selected from the group consisting of water, surfactants, moisturizers, lower alcohols, chelating agents, bactericides, antioxidants, preservatives, pigments and fragrances.

[0021] In one embodiment, the gray hair suppression composition of the present invention can be used by transdermal administration methods such as direct application or spraying onto the skin. The term "administration" above refers to the introduction of the gray hair suppression composition of the present invention into the body by any suitable method. The route of administration of the gray hair suppression composition of the present invention can be any conventional route, as long as it reaches the target tissue. Preferably, the gray hair suppression composition of the present invention can be administered transdermally, and more preferably by topical application. The number of applications of the gray hair suppression composition of the present invention can be determined according to the prescription, need, or purpose.

[0022] In one embodiment, the dosage of the gray hair suppression composition of the present invention can be appropriately adjusted according to individual differences such as age or the degree of the condition, or the dosage form. Furthermore, for the gray hair suppression composition of the present invention, it is preferable to apply an appropriate amount to the scalp once or several times a day for one week to several months. In Experimental Example 3 of the present invention, the gray hair suppression composition (hair tonic) was used seven times a week for six months. The results of Experimental Example 3 confirmed that, compared to the placebo control group of comparative examples, the hair tonic exhibited a superior effect in suppressing gray hair. Particularly in the dosage form containing ethanol, a higher effect in preventing hair loss and promoting hair growth was confirmed.

[0023] In one embodiment, the present invention provides a kit for inhibiting gray hair, comprising the aforementioned composition for inhibiting gray hair. In another aspect, the kit refers to a package containing a composition and accessories required for the prevention or treatment of gray hair. In yet another aspect, the accessories included in the kit are tools or devices commonly used in the technical field to which this invention pertains for the prevention or treatment of gray hair. In yet another aspect, the kit may further comprise a dosage instruction that discloses one or more of the following: dosage, route of administration, frequency of administration, and indication (gray hair syndrome) of the aforementioned ingredients.

[0024] In one embodiment, the present invention provides a method for inhibiting gray hair, comprising applying a gray hair inhibiting composition to a subject. In another aspect, the subject may be a human being requiring gray hair inhibition. Preferably, in the above method, the gray hair inhibiting composition may be applied to the subject in an effective amount. The term "effective amount" means an amount of an effective ingredient sufficient to inhibit, delay, improve, or alleviate gray hair, or to provide therapeutic or cosmetic benefits in the treatment or management of gray hair. The term "effective amount" also means an amount sufficient to inhibit or reduce gray hair production, whether in vitro or in vivo. The above method for inhibiting gray hair can promote melanin synthesis in hair by activating the Wnt / β-catenin signaling pathway, thereby exhibiting an effect of inhibiting or improving gray hair.

[0025] In one embodiment, the present invention provides a use for inhibiting gray hair, characterized by utilizing the aforementioned composition for inhibiting gray hair. In one embodiment, the aforementioned use may include all uses for inhibiting or improving gray hair, such as pharmaceutical uses, cosmetic uses, or beauty uses. In another aspect, the aforementioned use for inhibiting gray hair may exert an effect of inhibiting or improving gray hair by activating the Wnt / β-catenin signaling pathway to promote melanin synthesis in hair.

[0026] In one embodiment, the present invention provides a method for preparing a composition for inhibiting gray hair, the composition comprising one or more of the following groups: escin, 27-deoxyactein, lysionotin, nitidine chloride, lanosterol, engleletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, and platycodin D2. In the above preparation method, the composition for inhibiting gray hair can be prepared according to the preparation methods of commonly used cosmetics, quasi-pharmaceuticals, or pharmaceuticals.

[0027] In one embodiment, the composition for inhibiting gray hair of the present invention may comprise two or more of the following: escin, 27-deoxyactein, lysionotin, nitidinechloride, lanosterol, engleletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, and platycodin D2.

[0028] In one embodiment, in the gray hair suppression composition of the present invention, the content of all the ingredients described preferably does not exceed the maximum usage value specified in various regulations related to cosmetics / food / pharmaceuticals / quasi-pharmaceuticals.

[0029] Invention Effects

[0030] The composition for inhibiting gray hair of the present invention can effectively inhibit the production of gray hair. The composition for inhibiting gray hair of the present invention promotes the synthesis of melanin in hair by activating the Wnt / β-catenin signaling pathway, thereby exhibiting significant and excellent effects in inhibiting, preventing, improving, alleviating, delaying, or treating gray hair (white hair syndrome). Attached Figure Description

[0031] Figure 1 This is an experimental result confirming that aescin leads to increased melanin synthesis in B-16 melanoma cells.

[0032] Figure 2 It is a graph showing the increase in melanin synthesis based on aescin and its content. Detailed Implementation

[0033] Hereinafter, to facilitate understanding of the present invention, detailed descriptions will be provided with examples and other details. However, embodiments of the present invention can be modified into various other forms, and the scope of the present invention should not be construed as limited to the following embodiments. The embodiments of the present invention are provided to illustrate the present invention more completely to those skilled in the art.

[0034] Experimental Example 1: Increased Effect of Wnt / β-catenin Signaling

[0035] In this experiment, to confirm the activation of the Wnt / β-catenin pathway, a stable cell line (Wnt reporter HEK293A cells; WRHEK293A) was used (TCF / LEF Responsive Luciferase Reporter HEK293A). This stable cell line was maintained by subculture using MEM (Corning, USA) and fetal bovine serum (Gibco BRL, Gaithersburg, MD, USA). For the transcriptional activity assay, 30,000 cells were seeded per well in 96-well plates and cultured at 37°C for 24 hours. As shown in Table 1, the following saponins of the present invention were used for treatment: aescin, 27-deoxycicin, genistein, chlorhexidine chloride, lanosterol, scutellarin, privetin, imperatorin, rotungic acid, sesamoidin, polygala saponin D, kochia saponin Ic, valerin chloride, coltsfoot ketone, scutellarin, Paris saponin VII, and platycodon saponin D2. After 24 hours of incubation, report analysis 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 methods. To confirm the cytotoxicity caused by the treatments, GFP fluorescence expression was measured in parallel as an internal control. The luminescence value induced by the luciferase reaction was divided by the GFP fluorescence value, and the value of the untreated control group was set to 100%. The values ​​of the treated group were calculated and expressed as a percentage (%) (Table 1).

[0036] [Table 1]

[0037] Wnt / β-catenin signaling enhancement effect

[0038]

[0039] Experiment Example 2: Confirmation of Melanin Production Effect

[0040] In this experiment, the compound from Example 1, which showed an increased Wnt signaling effect, was added to the culture medium of mouse melanoma cells (B-16 mouse melanoma cells) to test the melanin production effect at the cellular level (Lotan R., Lotan D. Cancer Res. 40:3345-3350, 1980). Prior to the experiment, the toxicity of B-16 melanoma cells was evaluated, and a non-toxic concentration was selected for melanin production evaluation. B-16 melanoma cells were subcultured in DMEM (Gibco BRL, Gaithersburg, MD, USA) containing 10% FBS. Subsequently, they were seeded in 100 mm cell culture dishes for melanin synthesis and extraction, and then treated with the compound at a confluence of 70%. The compound was administered at a concentration of 10 μg / mL in the culture medium. Using α-melanocyte stimulating hormone (α-MSH) as a control, it was added to the culture medium to reach 10 nM and then used to treat B-16 melanoma cells, which were cultured for 48 hours. Afterwards, the cells were treated with trypsin, removed from the culture vessel, and centrifuged to extract melanin. 1 mL of sodium hydroxide solution (1N concentration) was added to the removed cells and the cells were boiled for 10 minutes to dissolve the melanin. The absorbance was measured at 400 nM using a spectrophotometer to determine the amount of melanin produced. The melanin amount was quantified in μg / mL using a standard absorbance curve based on melanin concentration. The untreated control group was calculated as 100%, and the values ​​of the treated group were calculated and expressed as a percentage (%) (Table 2).

[0041] [Table 2]

[0042] Melanin synthesis

[0043]

[0044] The results of melanin synthesis from the above compounds, including aescin, are shown in the figure. Figure 1 and Figure 2 .

[0045] Experimental Example 3: Confirmation Test on the Effect of Composition 1 (Hair Nourishing Agent) on Inhibiting the Production of Gray Hair

[0046] A gray hair inhibition composition 1 (hair tonic) comprising aescin and 27-deoxycimicifugine from the compounds of this invention was prepared. The gray hair reduction effect on human hair was tested using the above composition. Sixty healthy adults with gray hair were divided into five groups of 12 each. Comparative Example 1, Example 1, Example 1-2, Example 2, or Example 2-2 were applied to the scalp seven times a week for six months. After application, the degree of gray hair production was evaluated using a scalp analyzer phototrichogram compared to before application. For the experimental results, the pre-application level was set as 100%, and the values ​​compared to this are shown in Table 3.

[0047] [Table 3]

[0048]

[0049] Preparation Example 1: Composition 1 for inhibiting gray hair (hair tonic)

[0050] The hair tonic of the present invention is prepared by conventional methods according to the prescription shown in Table 4 below, using aescin, 27-deoxycicin, genistein, chlorhexidine chloride, lanosterol, scutellarin, privetin, angelica dahurica, rotonic acid, sesamoidin, polygala saponin D, kochia saponin Ic, valerin chloride, coltsfoot ketone, scutellarin, Paris saponin VII, or platycodon saponin D2.

[0051] [Table 4]

[0052]

[0053] Preparation Example 2: Composition 2 for inhibiting gray hair (hair lotion)

[0054] The avocado extract of the present invention is prepared using conventional methods according to the prescriptions shown in Table 5 below, comprising aescin, 27-deoxycicin, genistein, chlorhexidine chloride, lanosterol, scutellarin, privetin, angelica oleracea var. spp., rotonic acid, sesamoidin, polygala saponin D, kochia saponin Ic, valerin chloride, coltsfoot ketone, scutellarin, Paris polyphylla saponin VII, or platycodon saponin D2.

[0055] [Table 5]

[0056]

Claims

1. A composition for improving gray hair for cosmetic purposes, said composition comprising 27-deoxyactein as an active ingredient. The composition contains 0.0001 to 50% by weight of the 27-deoxycimicifuga tincture relative to the total weight of the composition.

2. The cosmetic use for improving gray hair as described in claim 1, wherein, The composition further comprises one or more of the following groups: escin, lysionotin, nitidine chloride, lanosterol, engelletin, specnuezhenide, praeruptorin B, rotunic acid, sesamoside, polygalacin D, momordin Ic, valechlorine, tussilagone, periplocin, polyphyllin VII, and platycodin D2.

3. The cosmetic use for improving gray hair as described in claim 1, wherein, The composition for improving gray hair activates the Wnt / β-catenin signaling system.

4. The cosmetic use for improving gray hair as described in claim 1, wherein, The composition for improving gray hair is a cosmetic composition.

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