WO2020101414A1 - Composition for promoting skin regeneration and hair growth, containing apigenin - Google Patents

Abstract

The present invention relates to a composition for promoting skin regeneration and hair growth, containing apigenin. More specifically, the composition for promoting skin regeneration and hair growth promotes cell differentiation through Wnt/beta-catenin signaling, thereby exhibiting effects of promoting skin regeneration and hair growth.

Description

Composition for skin regeneration and hair growth promotion containing apigenin

This application claims the benefit of priority based on Korean Patent Application No. 10-2018-0140423 dated November 15, 2018, and all contents disclosed in the literature of the Korean patent application are included as part of this specification.

The present invention relates to a composition for promoting skin regeneration and hair growth comprising apigenin.

Since the skin exists at the outermost part of the human body and is directly in contact with the external environment, it protects the human body from external damage and prevents excessive evaporation of moisture and heat in the body. The skin is composed of three layers of epidermis, dermis, and subcutaneous tissue. Most of the outermost epidermis is composed of keratinocytes. Keratinocytes in the epidermis protect the skin by forming keratin through the proliferation, migration and differentiation process from the base layer, and produce various cytokines to participate in inflammatory and immune responses. In addition, proliferation and migration of keratinocytes not only provides wound healing and skin regeneration, but also induces collagen synthesis to improve skin elasticity and basement membrane formation, thereby controlling adhesion and proliferation of skin cells and harmful. It provides an improvement in barrier function that selectively penetrates substances and interaction between the epidermis and the dermis. Due to this, the movement and proliferation of skin epidermal keratinocytes not only improves skin regeneration and wound healing, but also promotes skin elasticity and helps maintain healthy skin.

As the interest in skin beauty has increased, in order to maintain a healthier and more beautiful skin, the unique function of the skin is maintained by using physiologically active substances derived from various natural substances with high safety obtained from various animals, plants, and microorganisms. And various attempts to effectively suppress or alleviate skin aging by enhancing and activating skin cells have been extensively performed.

Apigenin (apigenin) is a nutritional component well known as an antioxidant contained in vegetables, and is used as a component for skin whitening, skin regeneration, and hair growth promotion.

Korean Patent Publication No. 2017-0119757 discloses that a cosmetic composition using apigenin, germanium, and amino acids, can exhibit skin regeneration and stabilizing effects by synergistically expressing the effects of each component.

Chinese Registered Patent No. 106880693 discloses a composition comprising apigenin and ginseng extract, which has the effect of preventing hair loss.

As such, technological development has been steadily developed for products related to skin regeneration or hair loss using apigenin, but consumers' satisfaction with the efficacy is still low.

Accordingly, apigenin, which is effective in promoting skin regeneration and hair growth, is used, but research and development of a product capable of maximizing the efficacy by using apigenin and synergistic ingredients are continuously required.

[Advanced technical literature]

[Patent Document]

China registered patent No. 106880693

In order to solve the above problems, the present inventors prepared a composition containing at least one of caffeine, ginseng extract, and green tea extract and apigenin at the same time, and confirmed that the composition was excellent in promoting skin regeneration and hair growth.

Accordingly, an object of the present invention is to provide a composition for promoting skin regeneration and hair growth comprising apigenin.

In order to achieve the above object, the present invention apigenin (apigenin); And caffeine, ginseng extract and one or more selected from the group consisting of green tea extract; provides a composition for promoting skin regeneration and hair growth comprising a.

The apigenin may be contained in 40 to 60% by weight based on the total weight of the composition.

The caffeine, ginseng extract and one or more selected from the group consisting of green tea extract may be included in 40 to 60% by weight based on the total weight of the composition.

The composition may be to activate the Wnt / beta-catenin signal.

The concentration of the composition may be 10 to 40 ppm based on the solid content concentration.

The composition may include apigenin and caffeine.

The composition may include apigenin and ginseng extract.

The composition may include apigenin and green tea extract.

The composition may be one or more selected from the group consisting of cosmetic compositions, food compositions and pharmaceutical compositions.

The composition for promoting skin regeneration and growth of hair growth of the present invention includes apigenin, at least one of caffeine, ginseng extract, and green tea extract, resulting in synergistic effect of the efficacy of each component, specifically excellent skin It can exhibit wound healing and scar reduction effects.

In addition, the composition for promoting skin regeneration and hair growth has an effect of preventing or improving hair loss by promoting hair growth.

In addition, the composition for promoting skin regeneration and hair growth promotes cell differentiation through signaling of Wnt / beta-catenin, thereby further improving skin regeneration and hair growth growth promoting effects.

In addition, the composition for promoting skin regeneration and hair growth can be widely applied to cosmetic compositions, food compositions, and pharmaceutical compositions having skin regeneration and hair growth promoting effects.

1 is a graph showing Wnt signal transduction activity of compositions prepared in Examples and Comparative Examples, respectively.

Hereinafter, it will be described in detail so that those skilled in the art to which the present invention pertains can easily practice. However, the present invention may be implemented in various different forms, and is not limited to the embodiments described herein.

Composition for skin regeneration and hair growth promotion

The present invention relates to a composition for promoting skin regeneration and hair growth, wherein the composition for promoting skin regeneration and hair growth comprises apigenin; And one or more selected from the group consisting of caffeine, ginseng extract, and green tea extract.

The apigenin; And one or more selected from the group consisting of caffeine, ginseng extract, and green tea extract; each has a skin regeneration or hair growth growth promoting effect, but when combined, the skin regeneration or hair growth growth promoting effect by synergistic action of these ingredients It can be significantly improved.

Preferably, the composition for promoting skin regeneration and hair growth may include apigenin and caffeine, or apigenin and ginseng extract, or a combination of apigenin and green tea extract. When the composition for promoting skin regeneration and hair growth includes components of such a combination, synergy for promoting skin regeneration and hair growth may be the best.

In the present invention, the apigenin is a kind of flavonoid component contained in a fruit, vegetable or herb, and may be extracted from these fruits, vegetables or herbs.

The apigenin may be included in an amount of 40 to 60% by weight, preferably 42 to 58% by weight, and more preferably 45 to 55% by weight based on the total weight of the composition for promoting skin regeneration or hair growth. If it is less than or equal to the above range, the synergistic effect with one or more selected from the group consisting of the caffeine, ginseng extract and green tea extract may be lowered.

In the present invention, at least one selected from the group consisting of the caffeine, ginseng extract and green tea extract may exhibit a synergistic effect for promoting skin regeneration and hair growth by combining with the apigenone.

One or more selected from the group consisting of the caffeine, ginseng extract and green tea extract is 40 to 60% by weight, preferably 42 to 58% by weight, more preferably based on the total weight of the composition for promoting skin regeneration or hair growth 45 to 55% by weight. If it is less than or equal to the above range, the synergistic effect with the apigenone may be reduced.

The caffeine is not particularly limited, synthetic caffeine; Alternatively, a form of at least one natural caffeine extract selected from the group consisting of guarana extract, coffee extract and tea extract may be used.

The caffeine may have a concentration of 5 to 20 ppm, preferably 5 to 15 ppm, and preferably 7 to 12 ppm, based on the solid content concentration. If it is less than the above range, the effect of promoting skin regeneration and hair growth may be negligible, and if it is more than the above range, the optimum concentration for synergistic action with apigenone may be exceeded, and thus the effect of promoting skin regeneration and hair growth may be reduced. At this time, the concentration of caffeine means the concentration of an aqueous solution of caffeine in the case of synthetic caffeine, and the concentration of solid content in the form of a natural caffeine extract.

The ginseng extract may be one or more selected from the group consisting of ginseng root extract, ginseng leaf extract, ginseng fruit extract, and ginseng seed extract, preferably ginseng root extract.

The ginseng extract may have a concentration of 5 to 20 ppm, preferably 5 to 15 ppm, and preferably 7 to 12 ppm based on the solid content concentration. If it is less than the above range, the effect of promoting skin regeneration and hair growth may be negligible, and if it is more than the above range, the optimum concentration for synergistic action with apigenone may be exceeded, and thus the effect of promoting skin regeneration and hair growth may be reduced.

In addition, the ginseng extract may be extracted using an extraction solvent selected from the group consisting of water, an organic solvent and a mixed solvent of water and an organic solvent. The organic solvent may be one or more selected from the group consisting of ethanol, methanol, butanol, ether, ethyl acetate and chloroform. Preferably, the extraction solvent may be ethanol.

In addition, the method for preparing the ginseng extract is not particularly limited as long as it is a common extraction method used in the art, for example, it can be prepared by extracting for 3 to 24 hours at 10 to 80 ° C using the extraction solvent. have.

The green tea extract may be at least one selected from the group consisting of green tea leaf extract, green tea flower extract and green tea stem extract, preferably green tea leaf extract.

The green tea extract may have a concentration of 5 to 20 ppm, preferably 5 to 15 ppm, and preferably 7 to 12 ppm, based on the solid content concentration. If it is less than the above range, the effect of promoting skin regeneration and hair growth may be negligible, and if it is more than the above range, the optimum concentration for synergistic action with apigenone may be exceeded, and thus the effect of promoting skin regeneration and hair growth may be reduced.

In addition, the green tea extract may be a hot water extract or a lower alcohol extract of C ₁ to C ₅ . Preferably, the green tea extract may be an ethanol extract.

In addition, the method for preparing the green tea extract is not particularly limited as long as it is a conventional extraction method used in the art. For example, when the green tea extract is a hot water extract, it may be obtained through the processes of green tea input, hot water extraction, filtration, concentration under reduced pressure, and spray drying. Alternatively, if the green tea extract is an ethanol extract, it may be prepared by extracting for 3 to 24 hours at 10 to 80 ° C using ethanol.

In the present invention, the concentration of the composition for promoting skin regeneration and hair growth may be 10 to 40 ppm, preferably 10 to 30 ppm, more preferably 15 to 25 ppm, based on the solid content concentration. If it is less than or equal to the above range, the effect of promoting skin regeneration and hair growth may be reduced. In addition, when the composition is in the concentration range, it is possible to enable the win / beta-catenin signal activation as described below.

In addition, the composition for promoting skin regeneration and hair growth can promote skin regeneration and hair growth by activating the Wnt / beta-catenin signal.

Wnt / beta-catenin signaling is a signaling system related to the development of living organisms and is known to act on skin formation and hair follicle development. Furthermore, when a wound is formed on the skin, it is known that wind signal transmission is essentially expressed in the process of skin tissue recovery to promote differentiation of epithelial cells (Fathke et al ., "Wnt signaling induces epithelial differentiation during cutaneous wound healing", BMC Cell Biology 2006, 7: 4). Therefore, when the wind signal transmission is promoted, differentiation of epithelial cells is promoted, skin regeneration can be promoted, and further, healing of skin wounds can be promoted. Gardenia extract promotes stem cell wint / beta-catenin signaling. Therefore, formulations containing the same can promote skin regeneration and specifically promote healing of skin wounds (Kateri A. Moore et al ., "Stem Cells and Their Niches", Science, VOL 311, p1880-1885 ).

In the present invention, the composition for promoting skin regeneration and hair growth may be at least one selected from the group consisting of cosmetic compositions, food compositions and pharmaceutical compositions.

When the composition for promoting skin regeneration and hair growth is a cosmetic composition, it may be formulated by containing a cosmetic or dermatologically acceptable medium or base. In addition, the cosmetic composition for promoting skin regeneration and hair growth may be provided in any formulation suitable for topical application, for example, a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an oil phase in an oil phase, a suspension, It can be provided in the form of a solid, gel, powder, paste, foam or aerosol composition. Compositions of these formulations can be prepared according to conventional methods in the art.

In addition, the cosmetic composition for promoting skin regeneration and growth of hair growth may include other ingredients that can give a synergistic effect to the main effect, within a range that does not impair the main effect other than the above-mentioned substances. In addition, the cosmetic composition for promoting skin regeneration and hair growth may further include a moisturizing agent, an emollient, an ultraviolet absorbent, a preservative, a disinfecting agent, an antioxidant, a pH adjusting agent, organic and inorganic pigments, flavoring agents, cooling agents, or limiting agents. The compounding amount of the components can be easily selected by those skilled in the art within a range that does not impair the objects and effects of the present invention, and the blending amount may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, based on the total weight of the composition. .

When the composition for promoting skin regeneration and hair growth is a food composition, it may be applied to various types of food additives or functional foods. It can be processed into fermented milk, cheese, yogurt, juice, probiotic and health supplements including the food composition for promoting skin regeneration and hair growth, and can be used in the form of various other food additives.

In addition, the food composition for promoting skin regeneration and hair growth may contain other ingredients and the like that can give a synergistic effect to the main effect within a range that does not impair the main effect targeted by the present invention. For example, in order to improve physical properties, additives such as fragrances, pigments, disinfectants, antioxidants, preservatives, moisturizers, thickeners, inorganic salts, emulsifiers, and synthetic polymer materials may be further included. In addition, auxiliary components such as water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, and seaweed extract may be further included. The ingredients may be appropriately selected and blended without difficulty by a person skilled in the art depending on the formulation or the purpose of use, and the amount added may be selected within a range not impairing the objects and effects of the present invention. For example, the added amount of the components may be in the range of 0.01 to 5% by weight, more specifically 0.01 to 3% by weight, based on the total weight of the composition.

The food composition for promoting skin regeneration and hair growth according to the present invention may be formulated in various forms such as solutions, emulsions, viscous mixtures, tablets, powders, etc., such as simple drinking, injection, spray, or squeeze methods. It can be administered in a variety of ways.

When the composition for promoting skin regeneration and growth of hair growth is a pharmaceutical composition, it can be applied to pharmaceuticals, orally or in a solid, semi-solid or liquid form by adding an inorganic or organic carrier compatible with the active ingredient used in the present invention, or It can be formulated as a parenteral administration agent, and the pharmaceutical composition according to the present invention can be administered orally, parenterally, rectal, topical, transdermal, intravenous, intramuscular, intraperitoneal, subcutaneous, and the like.

Examples of the dosage form for oral administration include tablets, pills, granules, capsules, powders, granules, powders, emulsions, syrups, pellets, and the like. In addition, formulations for parenteral administration include injections, drops, ointments, lotions, sprays, suspensions, emulsions, suppositories, and the like. The composition according to the present invention can be easily formulated into an active ingredient by carrying out according to the commercial method, in which case surfactants, excipients, colorants, spices, preservatives, stabilizers, buffers, suspending agents, and other commonly used adjuvants can be suitably used. have.

In addition, the dosage of the active ingredient of the pharmaceutical composition of the present invention will vary depending on the age, gender, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Determination of a suitable dose based on these factors is within the level of those skilled in the art, and the daily dose administered is, for example, 0.1 mg / kg / day to 100 mg / kg / day, more specifically 5 mg / kg / day to 50 mg / kg. / Can be a day, but is not limited to this.

The composition for promoting skin regeneration and hair growth as described above includes apigenin, and at least one of caffeine, ginseng extract, and green tea extract, resulting in a skin regeneration effect due to synergistic effect of the efficacy of each component, specifically excellent It has the effect of healing skin wounds and reducing scars, and has the effect of promoting hair growth, and thus can be widely applied to the fields of cosmetics, food, and pharmaceuticals having such effects.

How to promote skin regeneration and hair growth

The present invention also relates to a method for promoting skin regeneration and hair growth using the composition for promoting skin regeneration and hair growth.

The composition may be applied to the skin, including the scalp, to regenerate the skin or promote hair growth.

Alternatively, it may be administered orally depending on the formulation of the composition.

Hereinafter, preferred examples are provided to help understanding of the present invention, but the following examples are merely illustrative of the present invention, and it is apparent to those skilled in the art that various changes and modifications are possible within the scope and technical thought scope of the present invention. It is natural that such changes and modifications fall within the scope of the appended claims.

Preparation Example 1: Preparation of apigenin

Thistle (circium japonicum) was collected and used in mountainous areas of Chungbuk Province. What was purchased from Gyeongdong Market (Seoul, Korea) was dried and used. The dried thistle (circium japonicum) was extracted by adding 95% alcohol, and concentrated using a vacuum concentrator to prepare a spirit crude extract.

The crude crude extract was dissolved in distilled water and ethyl acetate, mixed at a ratio of 1: 1 (v / v), and the distribution between the abnormalities was repeated three times, and the ethyl acetate extract was reduced, concentrated, and dried.

The dried product was subjected to silica gel flash chromatography (solvent system: chloroform / ethyl acetate = 2: 1) to reduce the active fraction again under reduced pressure, dry, and then dissolve in a small amount of methanol saturated with millipore (0.45 nm). Filtration was performed to collect apigenin as an active material with a high-performance analyzer (HPLC, column: ODS 20 × 250 nm; 80% methanol).

Preparation Example 2: Caffeine production

Caffeine was purchased from Sigma Chemical Corporation (St. Louis, MO, USA).

Preparation Example 3: Preparation of ginseng extract

After crushing 1 kg of dried white ginseng with a blender, 5 liters of purified water was added thereto, and stirred and extracted with hot water at 38 to 42 ° C. for 24 hours, and then deposited at 15 ° C. for 1 day. Thereafter, the residue and the filtrate were separated through filtration and filtration and centrifugation, and the separated filtrate was concentrated under reduced pressure to obtain 270 g of the extract.

Preparation Example 4: Preparation of green tea extract

After crushing 1 kg of green tea leaves that were primarily processed (steaming process) with a blender, 5 l of purified water was added thereto, and the mixture was stirred for 24 hours with hot water at 38 to 42 ° C., and then deposited at 15 ° C. for 1 day. Thereafter, the residue and the filtrate were separated through filtration and filtration and centrifugation, and the separated filtrate was concentrated under reduced pressure to obtain 290 g of the extract.

Example 1

Apigenin 50% by weight and caffeine 50% by weight, respectively prepared in Preparation Example 1 and Preparation Example 2, were mixed to prepare a 20 ppm composition.

Example 2

Apigenin 50 wt% and ginseng extract 50 wt% prepared in Preparation Example 1 and Preparation Example 3, respectively, were mixed to prepare a 20 ppm composition.

Example 3

Apigenin 50 wt% and green tea extract 50 wt%, respectively prepared in Preparation Example 1 and Preparation Example 3, were mixed to prepare a 20 ppm composition.

Comparative Examples 1 to 8

For Comparative Examples 1 to 8, compositions as described in Table 1 below were prepared at 20 ppm each.

	Composition
Example 1	Apigenin + Caffeine
Example 2	Apigenin + Ginseng Extract
Example 3	Apigenin + Green Tea Extract
Comparative Example 1	Control
Comparative Example 2	LiCl
Comparative Example 3	Apigenin
Comparative Example 4	Caffeine
Comparative Example 5	Ginseng extract
Comparative Example 6	Green tea extract
Comparative Example 7	Madecassoside
Comparative Example 8	Apigenin + Madecassoside

Experimental Example 1

When Wnt signal is given to epidermal stem cells, the protein complex (GSK3, APC, Axin) that inhibits intracellular beta-catenin is inhibited, and beta-catenin moves into the cell nucleus and is involved in development and hair growth Using the principle in which various genes are expressed, experiments were performed on the degree of Wnt signal transmission by the compositions of Examples and Comparative Examples. The specific experimental method is as follows.

[Wnt signal transmission experiment]

(1) Cell culture

After purchasing the Wnt reporter cell line (# ENZ-61002-0001), the Wnt reporter cell line was seeded at 1x10 ⁴ cells / well in a 96well plate on a white / clear flat bottom coated with Collagen type I.

(2) Material treatment

Using the serum free medium (Serum free medium) for 24 hours, the compositions of Examples and Comparative Examples were treated at 100 μl for each concentration.

As a positive control (Positive control), 10 mM of LiCl was used (depending on the cell state, 10 mM shows 150-300% of control compared to control, and 50mM shows 1000-4000% of activity compared to control).

(3) Luciferase activity measurement

For each well, 100 µL of ONE-Glo ™ Luciferase Assay reagent was added and the light was blocked and reacted for 3 minutes at room temperature.

Activity was measured using a Wallac Victor2 multilabel counter.

(4) Data processing method

Based on the absorbance of the control group without material treatment, the value obtained by converting the luminescence intensity of the material treatment group to the control group as a percentage value was taken as a response ratio (%). The larger the response ratio, the better the Wnt signal transduction activity.

1 is a graph showing Wnt signal transduction activity of compositions prepared in Examples and Comparative Examples, respectively.

Referring to FIG. 1, a composition comprising a combination of apigenin and caffeine in Example 1, a combination of apigenin and ginseng extract in Example 2, and a combination of apigenin and green tea extract in Example 3 has Wnt signal transduction activity. You can see that it is excellent.

On the other hand, as in Comparative Examples 3 to 7, the composition comprising apigenin, caffeine, ginseng extract, green tea extract, and madecassoside alone, and a combination of apigenin and madecassoside as in Comparative Example 8 The composition to be found that Wnt signal transduction activity is significantly reduced compared to Examples 1,2,3.

From this, the composition comprising a combination of apigenin and caffeine in Example 1, a combination of apigenin and ginseng extract in Example 2, and a combination of apigenin and green tea extract in Example 3, synergistic action by combination of each component As a result, it was confirmed that the efficiency of Wnt signaling was greatly improved.

Although the present invention has been described above by way of limited embodiments and drawings, the present invention is not limited by this, and is described below by the person skilled in the art to which the present invention pertains, and the technical idea of the present invention. Of course, various modifications and variations are possible within the scope of the equivalent claims.

Claims (10)

1. Apigenin; And Caffeine, ginseng extract and one or more selected from the group consisting of green tea extract; Skin regeneration and hair growth promoting composition comprising a.
2. According to claim 1,

   The apigenin is contained in 40 to 60% by weight based on the total weight of the composition, the composition for promoting skin regeneration and hair growth.
3. According to claim 1,

   At least one selected from the group consisting of the caffeine, ginseng extract and green tea extract is contained in 40 to 60% by weight based on the total weight of the composition, the composition for promoting skin regeneration and hair growth.
4. According to claim 1,

   The composition is to activate a win / beta-catenin signal, a composition for promoting skin regeneration and hair growth.
5. According to claim 1,

   The concentration of the composition is 10 to 40 ppm based on the solid content concentration, the composition for promoting skin regeneration and hair growth.
6. According to claim 1,

   The composition will include apigenin and caffeine, skin regeneration and hair growth promoting composition.
7. According to claim 1,

   The composition comprises apigenin and ginseng extract, a composition for promoting skin regeneration and hair growth.
8. According to claim 1,

   The composition will contain apigenin and green tea extract, a composition for promoting skin regeneration and hair growth.
9. According to claim 1,

   The composition is at least one selected from the group consisting of cosmetic composition, food composition and pharmaceutical composition, a composition for promoting skin regeneration and hair growth.
10. A method for promoting skin regeneration and hair growth using the composition according to any one of claims 1 to 9.

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