KR20230094216A - Composition for preventing hair loss and promoting hair growth comprising Genkwanin - Google Patents

Abstract

The present invention relates to a composition for preventing hair loss and promoting hair growth containing genkwanin, and more particularly, to a composition for preventing hair loss and promoting hair growth containing genkwanin; And it relates to a pharmaceutical composition for preventing and treating hair loss.

Description

Composition for preventing hair loss and promoting hair growth comprising Genkwanin

The present invention relates to a composition for preventing hair loss and promoting hair growth containing genkwanin, and more particularly, to a composition that can be safely used without side effects on the skin and has an excellent effect of preventing hair loss and promoting hair growth by increasing the expression of hair growth-related genes. it's about

In general, the cycle of hair consists of an anagen phase, a catagen phase, and a telogen phase, and hair loss and hair growth continue while repeating the cycle. In the case of men, the growth period of hair is 3 to 5 years, and in the case of women, it is a little longer 4 to 6 years, the hair degeneration period is 30 to 45 days, and the resting period is about 3 to 4 months. When the telogen phase is reached, the anagen phase in which new hair is produced begins. Hair loss in this process is a natural phenomenon, but when a relatively long resting period lasts for a long time and the amount of hair decreases, it becomes a hair loss disease.

Until now, the exact cause of hair loss has not been identified, but hair loss due to inhibition of proliferation or functional decline of dermal papilla cells related to hair cycle control, abnormality of hair cycle by the action of male hormones, and reduced blood flow to the scalp Abnormal changes in cycles, drugs such as anticancer drugs, mental stress, physical stimulation, and environmental pollution are considered to be factors. On the other hand, dermal papilla cells are hair growth core cells located at the bottom of the hair root and determine the number and thickness of hair. Recently, studies on many regulators involved in hair growth and hair loss have been actively conducted. Proteins that affect hair growth include EGF, VEGF, and IGF, which affect the hair cycle by regulating the activity of dermal papilla cells. known to affect In addition, studies on substances that inhibit 5-α reductase and hair loss induction gene DKK, which are related to hair loss, are also being conducted.

One example of hair loss treatment for improving such scalp diseases or hair loss is a method of transplanting a plug of skin with hair from a scalp region where hair grows to a hair loss region by means of a hair transplantation method. This method is time consuming, relatively painless, and expensive. Other treatments include drug therapy, such as minoxidil applied to the scalp to prevent hair loss through capillary dilation, or finasteride, the male hormone that causes hair loss, DHT (5- It is possible to prevent hair loss by inhibiting the production of a dihydrotestosterone. However, although the drug as described above has an effect of improving hair loss prevention, there is a problem of causing side effects accordingly.

For the above reasons, research on hair loss prevention, hair growth, and hair growth promoting compositions using natural extracts has been conducted, and for example, as a patent application related thereto, hair loss including Jeonyeop Yinyanggwak, Skytari, Kangjinhyang, Snake Radish, and Jogu, etc. A number of patent applications exist in relation to technologies such as a composition for preventing and promoting hair growth (Korean Patent Publication No. 10-2009-0076671).

However, it is expected to be widely applied in the related field if a composition containing a single component of a natural component having excellent hair loss prevention and hair growth promoting effects in addition to such an extract is provided.

Accordingly, according to one aspect of the present invention, a composition for preventing hair loss and promoting hair growth containing natural ingredients without side effects is provided.

Accordingly, according to another aspect of the present invention, a pharmaceutical composition for preventing hair loss and promoting hair growth containing natural ingredients without side effects is provided.

According to one aspect of the present invention, there is provided a composition for preventing hair loss and promoting hair growth, including genkwanin (Genkwanin).

According to another aspect of the present invention, there is provided a pharmaceutical composition for preventing and treating hair loss, including Genkwanin.

Since the composition of the present invention promotes the proliferation of all hair cells and has an excellent expression effect of genes that promote hair growth, the composition of the present invention is for treating hair loss having excellent hair loss prevention and hair growth promoting effects without side effects on the human body. It can be usefully used as a pharmaceutical composition, a cosmetic composition for preventing hair loss and promoting hair growth, and the like.

Figure 1 shows the results of dermal papilla cell growth and proliferation according to the concentration of genkwanin treatment.
Figure 2 shows the result of confirming the mRNA expression level of hair growth-related genes (a) FGF7 and (b) VEGF genes by Genkwanin.
Figure 3 shows the result of confirming the mRNA expression level of hair loss-related genes (a) 5α-reductase and (b) DKK gene by Genkwanin.

Hereinafter, preferred embodiments of the present invention will be described with reference to the accompanying drawings. However, the embodiments of the present invention may be modified in various forms, and the scope of the present invention is not limited to the embodiments described below.

According to the present invention, there is provided a composition containing a naturally-derived component that promotes the proliferation of human-derived dermal papilla cells and activates the expression of genes associated with hair growth or the inhibition of expression of genes associated with hair loss.

In more detail, the composition of the present invention may be a composition for preventing hair loss and promoting hair growth, including Genkwanin of the following formula (I):

[화학식 1]

[Formula 1]

In this case, the active ingredient Genkwanin may be included in the composition at a concentration of 0.1 to 50 ppm, for example, 0.2 to 20 ppm, or 0.2 to 10 ppm. When genkwanin is included in the composition in an amount of less than 0.1 ppm, a sufficient hair growth promoting effect cannot be obtained, and when it exceeds 50 ppm, formulation stability may be lowered.

The composition of the present invention activates the proliferation of dermal papilla cells by genkwanin, an active ingredient, thereby promoting hair growth and preventing hair loss, as well as controlling the hair follicle cycle to prevent or delay hair follicle cells from going to the catagen phase By making it stay in the growth phase for a long time, it can provide an effect of promoting hair growth.

The composition according to the present invention may be, for example, a cosmetic composition, a pharmaceutical composition, or a health food composition, and may be formulated as a composition for external application to the skin or a composition for oral use.

In the case of the oral composition, dosage forms include, for example, tablets, pills, hard and soft capsules, solutions, suspensions, emulsifiers, syrups, powders, powders, granules, granules, pellets, etc., and these dosage forms are active ingredients In addition, it may contain surfactants, diluents (eg lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine), glidants (eg silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycol). there is. Tablets may also contain binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, optionally starch, agar, alginic acid or its sodium salt. and pharmaceutical additives such as disintegrants, absorbents, colorants, flavoring agents, and sweeteners. The tablets may be prepared by conventional mixing, granulating or coating methods. In addition, the parenteral administration form may be a transdermal dosage form, for example, a formulation such as injection, drop, ointment, lotion, gel, cream, spray, suspension, emulsion, suppository, patch, etc. It can, but is not limited thereto.

For example, the composition may be a cosmetic composition including genkwanin and the rest of the cosmetic base, and may include any other ingredients that can be conventionally formulated in cosmetic compositions together with genkwanin as an active ingredient.

Components that can be added to the cosmetic composition of the present invention include, for example, fats and oils, humectants, emollients, surfactants, organic and inorganic pigments, preservatives, bactericides, antioxidants, pH adjusters, alcohols, pigments, fragrances, blood circulation An accelerator, a cooling agent, etc. are mentioned.

Examples of the oil and fat component include ester-based oils and fats, hydrocarbon-based oils and fats, silicone-based oils and fats, fluorine-based oils, animal fats and vegetable oils, and the like.

On the other hand, examples of the emollient agent include long-chain acyl glutamic acid cholesteryl ester, hydroxystearate cholesteryl, 12-hydroxystearic acid, stearic acid, rosin acid, lanolin fatty acid cholesteryl ester, etc., and surfactants Examples of the surfactant include nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants.

As organic and inorganic pigments, silicic acid, silicic anhydride, magnesium silicate, talc, sericite, mica, kaolin, bengala, clay, bentonite, titanium-coated mica, bismuth oxychloride, zirconium oxide, magnesium oxide, zinc oxide, titanium oxide, aluminum oxide inorganic pigments such as calcium sulfate, barium sulfate, magnesium sulfate, calcium carbonate, magnesium carbonate, iron oxide, ultramarine blue, chromium oxide, chromium hydroxide, calamine and complexes thereof; Polyamide, polyester, polypropylene, polystyrene, polyurethane, vinyl resin, urea resin, phenolic resin, fluororesin, silicon resin, acrylic resin, melamine resin, epoxy resin, polycarbonate resin, divinylbenzene/styrene copolymer, organic pigments such as silk powder, cellulose, CI pigment yellow and CI pigment orange, and composite pigments of these inorganic pigments and organic pigments.

Bactericides include hinokitiol, triclosan, trichlorohydroxydiphenyl ether, chlorhexidine gluconate, phenoxyethanol, resorcin, isopropylmethylphenol, azulene, salicylic acid, zincophylthione, benzalkonium chloride, photosensitizer So No. 301, mononitroguacol sodium, undecyrenic acid, etc. are mentioned. As antioxidants, butylhydroxyanisole, propyl gallic acid, elisorbic acid, etc. are mentioned. As pH adjusters, citric acid, sodium citrate, malic acid, Sodium malate, fumaric acid, sodium fumarate, succinic acid, sodium succinate, sodium hydroxide, sodium monohydrogenphosphate, etc. are mentioned. Examples of alcohol include higher alcohols such as cetyl alcohol.

The preservative may be benzoic acid, paraoxybenzoic acid ester, a mixture of methylchloroisothiazolinone, phenoxyethanol, DMDMhydantoin, and the like. As for the fragrance, ingredients generally used in cosmetic compositions for scalp and hair may be used.

In addition, the blending components that may be added are not limited thereto, and any of the above components can be blended within a range not impairing the objects and effects of the present invention, but preferably 1 to 20% by weight based on the total weight of the composition, More preferably, it is blended at 5 to 10% by weight.

The cosmetic composition of the present invention can be prepared in any formulation commonly prepared in the art, and examples thereof include solutions, emulsions, suspensions, pastes, creams, gels, powders, sprays, and the like.

Ingredients included in the cosmetic composition of the present invention to be formed into such a formulation may include auxiliary agents and carrier components commonly used in cosmetic compositions in addition to the water bongseon extract as an active ingredient.

When the formulation of the present invention is a paste, cream or gel, animal fiber, vegetable fiber, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as a carrier component. can

When the formulation of the present invention is a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluorohydrocarbon, propane / May contain a propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solvating agent or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 ,3-butyl glycol oil, fatty acid esters of glycerol, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, an ethoxylated isostearyl alcohol, a suspending agent such as polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline Cellulose, aluminum metahydroxide, bentonite, agar or tracanth and the like may be used.

In the cosmetic composition of the present invention, if necessary, any components included in general cosmetic compositions may be blended. Examples of other components included include oil and fat components, humectants, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, bactericides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, Spices, blood circulation accelerators, cooling agents, antiperspirants, purified water and the like can be mentioned.

The hair loss prevention and hair growth promoting composition of the present invention may be, for example, any one of the above shampoos, rinses, treatments, essences, tonics, creams, packs and lotions, but is not limited thereto.

More specifically, hair tonic, hair conditioner, hair essence, hair lotion, hair shampoo, hair conditioner, hair treatment, hair cream, hair wax, hair pack, hair soap, hair cleansing foam, hair oil, hair dryer, hair preservation Treatment agents, hair dyes, hair waving agents, hair bleaching agents, hair gels, hair moisturizers, hair mousse, eyebrow nutrients, eyelash nutrients, and hair spray formulations, but are not limited thereto.

On the other hand, in another aspect of the present invention, there is provided a pharmaceutical composition for preventing and treating hair loss, including Genkwanin.

In this case, the active ingredient Genkwanin may be included in the composition at a concentration of 0.1 to 50 ppm, for example, 0.2 to 20 ppm, or 0.2 to 100 ppm. When genkwanin is included in the composition in an amount of less than 0.1 ppm, a sufficient hair growth promoting effect cannot be obtained, and when it exceeds 50 ppm, formulation stability may be lowered.

On the other hand, the pharmaceutical composition for preventing and treating hair loss of the present invention may be a pharmaceutical composition for preventing and treating hair loss comprising Genkwanin and a pharmaceutically acceptable carrier. The pharmaceutical composition according to the present invention may be administered parenterally, rectally, topically, transdermally, subcutaneously, etc., for example, topically applied to the scalp.

Furthermore, the pharmaceutical composition of the present invention can be used in the form of oral formulations such as powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, sterile injection solutions, parenteral formulations, etc. according to conventional methods according to the purpose of use. It can be formulated and used in various forms.

Examples of suitable carriers, excipients and diluents that may be included in such pharmaceutical compositions are lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginates, gelatin, calcium phosphate, calcium silicate, cellulose. , methyl cellulose, amorphous cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil.

In addition, the pharmaceutical composition of the present invention may further include fillers, anti-coagulants, lubricants, wetting agents, flavoring agents, emulsifiers, preservatives, and the like.

Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations contain at least one excipient, for example, starch, calcium carbonate, sucrose, in the pharmaceutical composition for preventing and treating hair loss. , lactose, gelatin, etc. may be mixed and formulated. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Oral liquid formulations include suspensions, solutions for internal use, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, aromatics, and preservatives may be included.

Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried formulations, and suppositories. Propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate may be used as non-aqueous solvents and suspending agents. The base of the injection may include conventional additives such as solubilizers, tonicity agents, suspending agents, emulsifiers, stabilizers and preservatives.

Preferably, the pharmaceutical composition is a formulation for external application, and the pharmaceutical composition for external application on the skin is an external application for the skin having an effect of preventing hair loss and promoting hair growth, such as creams, gels, patches, sprays, ointments, warning agents, lotions, liniments, Pasta or cataplasma may be prepared and used as a pharmaceutical composition in the form of an external skin preparation, but is not limited thereto.

The preferred dosage of the present invention varies depending on the condition and body weight of the patient, the severity of the disease, the type of drug, the route and duration of administration, and can be appropriately selected by those skilled in the art. Administration may be administered once a day, or may be administered in several divided doses.

In particular, the pharmaceutical composition of the present invention may be a pharmaceutical composition for the treatment of androgenetic alopecia, the prevention and treatment of hair loss.

In addition, the composition of the present invention may be in the form of a health food composition for preventing, improving, alleviating hair loss and promoting hair growth. In the health food composition of the present invention, the composition may be a liquid or solid formulation, and may be a tablet, capsule, soft capsule, pill, granule, beverage (drink), diet bar, chocolate, caramel formulation or confectionery formulation It may be, and the formulation is not particularly limited.

The health food composition of the present invention may contain excipients, sugars, flavorings, pigments, fats and oils, proteins, etc. as needed in addition to the above active ingredients. In addition, the composition of the present invention may contain a substance that promotes skin absorption in order to increase hair growth and hair growth promoting effects.

Hereinafter, the present invention will be described in more detail through specific examples. The following examples are merely examples to aid understanding of the present invention, and the scope of the present invention is not limited thereto.

Example

1. Dermal papilla cell culture and proliferation test

CCK-8 (Cell counting kit-8) is a water-soluble tetrazolium salt reagent called WST-8, which forms orange-colored water-soluble Formazan by dehydrogenase in the mitochondria of living cells. will do The absorbance at an orange wavelength of 450 nm exhibited by CCK-8 reflects the number of cells, so it was used to measure cell growth and proliferation. Through the CCK-8 assay, the growth promoting efficacy of human dermal papilla cells was measured using Genkwanin at concentrations of 0.2 ppm, 1 ppm, and 5 ppm, respectively. Specifically, after culturing 3x10 ³ dermal papilla cells in a 96-well plate for 24 hours, the culture medium was changed to a serum-free medium, growth factors contained in the medium were removed, and genkwanin was treated. As a negative control group, the same amount of DMSO as a solvent was used, and as a positive control group, minoxidil at a concentration of 1 ppm was used. After culturing for 24 hours, CCK8 was treated and cell growth was analyzed by measuring absorbance at 450 nm.

As a result, as shown in FIG. 1, it was confirmed that cell growth and proliferation significantly increased when genkwanin was treated at concentrations of 0.2 ppm, 1 ppm, and 5 ppm compared to the negative control group (T-test, *p <0.05) .

2. Expression of hair growth related genes

(1) Verification of mRNA expression of genes related to hair growth

Hair growth is promoted by growth factors such as fibroblast growth factor 7 (hereinafter referred to as 'FGF7)' and VEGF (Vascular endothelial growth factor).

FGF7 is one of several types of FGFs, and is known to be highly expressed in the growth phase of hair. Therefore, it can be said that high expression of FGF7 has a close relationship with hair growth. In addition, it has been reported that minoxidil, one of the representative hair loss treatments, induces hair growth and highly expresses VEGF. Therefore, the hair growth effect can be confirmed by checking the FGF7 and VEGF gene expression levels by Genkwanin.

Genkwanin at 1 ppm, which sufficiently induced dermal papilla cell proliferation in 1. above, was treated with dermal papilla cells cultured in a serum-free medium, and each gene expression change was analyzed 24 hours later. Specifically, mRNA extraction is performed using ReliaPrep?? RNA Miniprep Systems (Promega) was used, and cDNA was created by reverse transcription polymerase chain reaction (RT-PCR) using poly-A primers and reverse transcriptase, and real-time polymerase chain reaction ( Real-time quantitative PCR) was used to measure the amount of each mRNA. The amount of each mRNA was corrected with the amount of Gapdh, an endogenous gene.

As a result, as shown in FIG. 2, FGF7 and VEGF mRNAs were increased by gankwanin.

(2) Verification of hair loss-related gene mRNA expression

A representative gene associated with male pattern baldness is 5α-reductase. It has been reported that testosterone, a male hormone, is converted into DHT by 5α-reductase, and hair thinning and hair loss are promoted by DHT. In addition, it has been reported that DHT inhibits hair growth by promoting the expression of related genes such as DKK. Propexia (substance name Finasteride) is known to slow down the progress of male pattern baldness by inhibiting 5α-reductase. Therefore, the hair loss inducing effect of genkwanin can be confirmed through the expression of 5α-reductase and DKK genes. Specific mRNA extraction and gene analysis were performed in the same way as described in 2.

As a result, as shown in FIG. 3, 5α-reductase and DKK mRNA were decreased by genkwanin.

Although the embodiments of the present invention have been described in detail above, the scope of the present invention is not limited thereto, and various modifications and variations are possible without departing from the technical spirit of the present invention described in the claims. It will be obvious to those skilled in the art.

Claims (9)

A composition for preventing hair loss and promoting hair growth, comprising Genkwanin.
According to claim 1, wherein the genkwanin (Genkwanin) is contained in a concentration of 0.1 to 50 ppm in the composition, hair loss prevention and hair growth promoting composition.
According to claim 1, wherein the composition is a health food composition or a cosmetic composition, hair loss prevention and hair growth promoting composition.
According to claim 3, wherein the cosmetic composition is shampoo, rinse, treatment, essence, tonic, cream, pack and lotion of any one formulation, hair loss prevention and hair growth promoting composition.
Genkwanin containing (Genkwanin), a pharmaceutical composition for preventing and treating hair loss.
According to claim 5, wherein the genkwanin (Genkwanin) is contained in the composition at a concentration of 0.1 to 50 ppm, hair loss prevention and treatment pharmaceutical composition.
[Claim 6] The pharmaceutical composition for preventing and treating hair loss according to claim 5, wherein the composition comprises Genkwanin and a pharmaceutically acceptable carrier.
According to claim 5, wherein the pharmaceutical composition is a formulation for external use, a pharmaceutical composition for preventing and treating hair loss.
The pharmaceutical composition for preventing and treating hair loss according to claim 5, wherein the pharmaceutical composition is for the treatment of male pattern baldness.

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