KR102249431B1 - Composition for treating alopecia comprising Cocos nucifera extract - Google Patents

Abstract

Skin whitening containing coconut extract, anti-wrinkle, moisturizing, or as for the composition of the coconut house thorium (Coconut haustorium) Extract before germination or coconut (Cocos nucifera) germ extract is re-5α- reductase inhibition activity of the kinase in accordance with an aspect In addition to showing, there is an effect that can be usefully used in a composition for preventing, improving, or treating hair loss, or promoting hair growth since it can generate new hair.

Description

Composition for improving hair loss containing coconut extract {Composition for treating alopecia comprising Cocos nucifera extract}

It relates to a composition for improving hair loss or promoting hair growth, containing coconut extract.

The skin barrier is composed of dead keratinocytes and intercellular lipids, and plays a key function in skin health as a skin protective film that protects the skin from external stimuli and prevents moisture from evaporating from the skin. In other words, it prevents the release of excess moisture from the body and prevents harmful substances such as chemicals and microorganisms from entering our body. The keratinocyte envelope, which forms the surface of dead keratinocytes, plays an important role in the stability of intercellular lipids. Keratinocytes form the skin barrier through the process of keratinization through differentiation. The skin barrier function can be destroyed by aging or external factors, and damage to the skin barrier can lead to reduced skin moisture content and wrinkles.

Hair loss refers to a phenomenon in which capillaries in the scalp are contracted due to various factors such as genetic, environmental, and mental factors, resulting in itching and hair removal from the scalp tissue, which is one of the concerns of modern people. The causes of such hair loss are due to excessive mental stress, brain labor, and instant diet, which leads to poor blood circulation in the scalp, malnutrition of the hair follicle cells, and deterioration of the endocrine circulatory system. The number of hair follicle cells significantly decreases, leading to early hair loss even during the growth phase.

Therefore, in recent years, research for the development of materials using natural products is actively being conducted, and there is an increasing demand for the development of materials that are safe for the human body and have an activity for improving hair loss.

One aspect is to provide a cosmetic composition for preventing, improving, or treating hair loss, or promoting hair growth, containing a coconut haustorium extract or a pre-germination coconut ( Cocos nucifera) embryo extract.

Another aspect is to provide a skin external preparation for preventing, improving, or treating hair loss, or promoting hair growth, containing a coconut haustorium extract or a pre-emergence coconut ( Cocos nucifera) embryo extract.

Another aspect is to provide a pharmaceutical composition for preventing, improving, or treating hair loss, or promoting hair growth, containing a coconut haustorium extract or a pre-emergence coconut ( Cocos nucifera) embryo extract.

Another aspect is to provide a health functional food composition for preventing, improving, or treating hair loss, or promoting hair growth, containing a coconut haustorium extract or a pre-germination coconut ( Cocos nucifera) embryo extract.

One aspect is to provide a composition for preventing, improving, or treating hair loss, or promoting hair growth, containing a coconut haustorium extract or a pre-emergence coconut ( Cocos nucifera) embryo extract.

As used herein, "Coconut haustorium" is used interchangeably with "an embryo of a coconut or a portion thereof after germination", and refers to a sponge absorbent tissue formed from the distal end of the embryo during the germination of the coconut. It can mean.

As used herein, the term "active ingredient" or "effective amount" refers to any amount of a composition used in the practice of the invention provided herein sufficient to alleviate, inhibit or prevent progression of a disease, disorder or condition, or one or more symptoms thereof. Can mean

As used herein, the terms "administering," "applying", and "introducing" are used interchangeably and into a subject by a method or route that results in at least partial localization of a composition according to one embodiment to a desired site. It may mean the arrangement of the composition according to one embodiment of.

As used herein, the term "alopecia" refers to a phenomenon in which hair is removed from the scalp or a condition in which the hair is thin or thin, and "preventing or improving hair loss" means preventing and suppressing hair loss as described above. It means, and "promoting hair growth or promoting hair growth" means not only promoting the generation of new hair, but also allowing existing hair to grow healthy. The hair loss is alopecia areata, hereditary androgenetic alopecia, telogen effluvium, traumatic alopecia, tricotillomania, pressure alopecia, growth stage alopecia, non-rigid alopecia, falconia. It may be one or more selected from toxic alopecia (Alopecia syphlltiac), seborrheic alopecia (Alopecia seborrhecia), symptomatic alopecia, scarring alopecia, and congenital alopecia.

The extract may be extracted using water, alcohol, for example, C1-C6 alcohol, for example, C1-C4 alcohol, or a mixture thereof as a solvent. The C1-C6 alcohol may be methanol, ethanol, propanol, isopropanol, 1,3-propanediol, butanol, pentanol, hexanol, and the like. The solvent may be, for example, a mixture of water and alcohol, that is, an aqueous alcohol solution. The alcohol concentration of the aqueous alcohol solution is 1 to 99.5 (v/v)%, for example, 10 to 99.5 (v/v)%, 1 to 70 (v/v)%, 1 to 40 (v/v)%, 5 to 25 (v/v)%, 7 to 20 (v/v)%, 5 to 25 (v/v)%, or 10 to 20 (v/v)%. The aqueous alcohol solution may be an aqueous ethanol solution.

The extraction is performed by 3 to 10 (vol/w) times, for example, 3 to 7 (vol/w), of the extraction solvent with respect to the whole, a part of the coconut, or a material derived therefrom, or a coconut embryo before germination. It may include adding weight) times, 3 to 5 (volume/weight) times, 5 to 10 (volume/weight) times, or 4 to 10 times. For example, it may include adding 3 to 10 L of the extraction solvent to 1 kg of the outpost of the phosphorus or rhubarb, a portion thereof, or a material derived therefrom.

The extraction is performed by warmed liquid extraction, pressurized liquid extraction (PLE), microwave assisted extraction (MAE), subcritical extraction (SE), or a combination thereof. Can be. The subcritical extraction may be subcritical water extraction (SWE). Subcritical water extraction is also referred to as superheated water extraction or pressurized hot water extraction (PHWE). The heated liquid extraction may be reflux extraction.

The extraction is 4 to 70, for example, 4 to 50, 4 to 40, 4 to 30, 10 to 70, 15 to 70, 20 to 70, 4 to 50, 10 to 50, It may be performed at 4°C to 40, 4°C to 30, 10°C to 40, 10°C to 35, or 10 to 30. The extraction time may vary depending on the selected temperature, for example, 1 hour to 2 months, for example, 1 hour to 1 month, 1 hour to 15 days, 1 hour to 10 days, 1 hour to 5 days, 1 hour to 3 days. , 1 hour to 2 days, 1 hour to 1 day, 5 hours to 1 month, 5 hours to 15 days, 5 hours to 10 days, 5 hours to 5 days, 5 hours to 3 days, 5 hours to 2 days, 5 It may be time to 1 day, 10 hours to 1 month, 10 hours to 15 days, 10 hours to 10 days, 10 hours to 5 days, 10 hours to 3 days, or 10 hours to 2 days. The extraction may include mixing the whole of the coconut Huis Thorium, a portion thereof, or a material derived therefrom, or a coconut embryo before germination in the solvent, and leaving it for a predetermined time. The standing may include suitable agitation. The extraction may be repeated one or more times, for example, 1 to 5 times.

The extraction may be performed by separating plant residues and extracts by known methods such as filtration. The extraction may also include removing the solvent from the obtained extract by known methods such as concentration under reduced pressure. The extraction may also include preparing a dried extract by drying the obtained extract, such as lyophilization.

The composition is from 0.001% to 80% by weight based on the total weight of the composition, for example, from 0.01% to 60% by weight, from 0.01% to 40% by weight, from 0.01% to 30% by weight, from 0.01% to 20% by weight %, 0.01% to 10%, 0.01% to 5%, 0.05% to 60%, 0.05% to 40%, 0.05% to 30%, 0.05% to 20%, 0.05% to 10% by weight, 0.05% to 5% by weight, 0.1% to 60% by weight, 0.1% to 40% by weight, 0.1% to 30% by weight, 0.1% to 20% by weight, 0.1% by weight % To 10% by weight, or 0.1% to 5% by weight of the extract may be contained.

In another embodiment, the extract may be a fermented extract.

In one embodiment, the fermentation may be performed for 1 to 7 days at pH 6 to 7 at 30 to 60° C. in a medium containing a carbon source. In one embodiment, the fermentation is Bacillus genus, Streptococcus genus, Lactococcus genus, Enterococcus genus, Lactobacillus genus, Pediococcus genus , Leukonostoc (Leuconostoc), Weissella (Weissella), Bifidobacterium (Bifidobacterium), Saccharomyces (Saccharomyce) and Galactomyces (Galactomyces) genus selected from the group consisting of one or more strains selected from the group consisting of It may be fermented. More specifically, the strain is Lactobacillus plantarum , Lactobacillus casei , Lactobacillus acidophilus , Lactobacillus fermentum , Lactobacillus fermentum Bacillus curvatus , Lactobacillus confusus , Lactobacillus gasseri , Bifidobacterium breve , Bifidobacterium breve, Bifidobacterium thermophilum (Bifidobacterium thermophilum) Streptococcus thermophilus , Leuconostoc mesenteroides , S. cerevisiae , S. bayanus , Saccharomyces para. reading can be one's (S. paradoxus), Saccharomyces access to US Mai category (S. mikatae), access to Sakae-ku My'll Havre lots (S. kudriavzevii), or galactose Mai Seth Kandy Doom (Galactomyces candidum).

Without being limited by a particular theory, the coconut haus thorium, or an extract (or fermented extract) of a coconut embryo before germination may be one that inhibits the activity of 5α-reductase. Accordingly, the composition has an effect that can be usefully used for preventing, improving, or treating hair loss, or promoting hair growth.

In one embodiment, the composition may be a cosmetic composition. The cosmetic composition may be, for example, a softening lotion, a nutritional lotion, a massage cream, a nutritional cream, an essence, a pack, a gel, an ampoule, or a cosmetic formulation of a skin adhesion type. Ingredients included in the cosmetic composition may include ingredients commonly used in cosmetic compositions in addition to the composition as an active ingredient. For example, conventional adjuvants and carriers such as stabilizers, solubilizers, vitamins, pigments and fragrances It may include.

In another embodiment, the composition may be a composition for external application for skin.

The external preparation for skin may be a cream, a gel, an ointment, a skin emulsifier, a skin suspension, a transdermal delivery patch, a drug-containing bandage, a lotion, or a combination thereof. The above skin external preparations are ingredients commonly used in external preparations for skin such as cosmetics and pharmaceuticals, such as aqueous ingredients, oily ingredients, powder ingredients, alcohols, moisturizers, thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants, surfactants, fragrances. , Colorants, various skin nutrients, or a combination thereof and may be appropriately formulated according to need. The external preparations for the skin include metal sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, and gluconic acid, caffeine, tannin, bellapamil, licorice extract, glavidine, and caline. Hot-water extract of fruit, various herbal medicines, drugs such as tocopherol acetate, glytilithic acid, tranexamic acid and derivatives or salts thereof, vitamin C, ascorbic acid magnesium phosphate, ascorbic acid glucoside, arbutin, kojic acid, glucose, fructose, Sugars such as trehalose can also be appropriately blended.

In another embodiment, the composition may be a pharmaceutical composition.

The pharmaceutical composition may additionally include a pharmaceutically acceptable diluent or carrier. The diluent may be lactose, corn starch, soybean oil, microcrystalline cellulose, or mannitol, and as a lubricant, magnesium stearate, talc, or a combination thereof. The carrier may be an excipient, a disintegrant, a binder, a lubricant, or a combination thereof. The excipient may be microcrystalline cellulose, lactose, low-substituted hydroxycellulose, or a combination thereof. The disintegrant may be calcium carboxymethylcellulose, sodium starch glycolate, anhydrous calcium monohydrogen phosphate, or a combination thereof. The binder may be polyvinylpyrrolidone, low-substituted hydroxypropylcellulose, hydroxypropylcellulose, or a combination thereof. The lubricant may be magnesium stearate, silicon dioxide, talc, or a combination thereof.

The pharmaceutical composition may be formulated as an oral or parenteral dosage form. The oral dosage form may be a granule, a powder, a liquid, a tablet, a capsule, a dry syrup, or a combination thereof. The parenteral dosage form may be an injection.

In another embodiment, the composition may be a health functional food. The health functional food composition may be used alone or with other foods or food ingredients, or may be appropriately used according to a conventional method, such as a coconut haus thorium extract or a coconut germ extract before germination according to an embodiment. The mixing amount of the active ingredient may be appropriately determined according to the purpose of use (prevention, health or therapeutic treatment). In general, when preparing food or beverage, the composition of the present specification may be added in an amount of 15 parts by weight or less based on the raw material. There is no particular limitation on the kind of the health functional food. Among the types of health functional foods, the beverage composition may contain various flavoring agents or natural carbohydrates as an additional component, like ordinary beverages. The natural carbohydrates are monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, and polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As the sweetener, natural sweeteners such as taumatin and stevia extract, and synthetic sweeteners such as saccharin and aspartame can be used. The health food composition may also be used in nutrients, vitamins, electrolytes, flavoring agents, coloring agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonated beverages. It may contain a carbonation agent to be used, or a combination thereof. The health functional food composition may also contain natural fruit juice, fruit juice beverage, pulp for the production of vegetable beverages, or a combination thereof.

Coconut Haustorium (Coconut haustorium) extract according to one aspect or the Cocos nucifera embryo extract before germination shows the inhibitory activity of 5α-reductase, as well as the generation of new hair, preventing, improving, or treating hair loss. , Or there is an effect that can be usefully used in a composition for promoting hair growth.

Hereinafter, the present invention will be described in more detail through examples. However, these examples are for illustrative purposes only, and the scope of the present invention is not limited to these examples.

Example 1. Preparation of Coconut Germ (Coconut Haus Thorium) Extract after Germination

After germination, a coconut germ (coconut haus thorium) extract was prepared as follows.

First, embryos (Coconut House Thorium) were isolated from germinated coconuts (directly imported from Vanuat). After separating about 100 g of coconut haus thorium, they were pulverized, 200 ml of water was added, and the mixture was stirred at room temperature for 48 hours, followed by extraction. After extraction, it was filtered with filter paper (Whatman NO. 2, Maidstone, UK), concentrated with a reduced pressure reflux cooling device (N-1110S, EYELA, Tokyo, Japan) in a water bath of 40° C. or lower, and then freeze-dried. All samples were stored frozen at 80 °C until the experiment, dissolved in dimethyl sulfoxide (DMSO) and used in the experiment. The recovery rate was 17.89%.

Example 2. Preparation of coconut germ extract before germination

First, embryos were isolated from coconuts (directly imported from Vanuat) before germination. After separating about 100 g of coconut embryos, they were pulverized, and then 200 ml of water were each added, stirred at room temperature for 48 hours, and then extracted. After extraction, it was filtered with filter paper (Whatman NO. 2, Maidstone, UK), concentrated with a reduced pressure reflux cooling device (N-1110S, EYELA, Tokyo, Japan) in a water bath of 40° C. or lower, and then freeze-dried. All samples were stored frozen at 80 °C until the experiment, dissolved in dimethyl sulfoxide (DMSO) and used in the experiment. The recovery rate was 19.21%.

Example 3. Preparation of fermented extract of coconut germ (coconut hausthorium) after germination

First, embryos (Coconut House Thorium) were isolated from germinated coconuts (directly imported from Vanuat). After activating Saccharomyces cerevisiae in YM solid medium at 37°C for 24 hours, the formed colonies were inoculated in sterilized YM liquid medium and then cultured with shaking in a temperature incubator at 25°C to 50°C for 24 hours. Thereafter, the crushed coconut Haus Thorium was added to the strain culture solution to a concentration of 10 g/L, and then cultured at 37° C. for 1 to 3 days. Thereafter, in order to terminate the fermentation, heat was applied at 100° C. for 40 minutes to induce a loss of function of the bacteria. The precipitate was removed using a centrifuge and the supernatant was collected, or the filtered supernatant was used. The prepared fermentation broth was mixed in the same amount with MEM, an animal cell culture medium, and then filtered through a 0.22 μm filter to remove bacteria.

Experimental Example 1. Analysis of 5α-reductase activity inhibitory ability of coconut germ extract

In order to analyze the hair loss improvement activity of the coconut haus thorium extract prepared in Examples 1 and 2 and the coconut germ extract before germination, the inhibitory effect of 5α-reductase activity was measured.

Specifically, 1.0 ml of Tris-HCL buffer (pH 7.2), 0.3 ml of testosterone (500 ug/ml), and 1.0 ml of enzyme solution were mixed, and the extracts prepared in Examples 1 to 3 were respectively 50, 100, and 200 ug/ It was added to a concentration of ml. Thereafter, 0.5ml of NADPH (0.77mg/ml) was added to initiate the reaction, followed by incubation at 37°C for 30 minutes. The reaction was stopped by adding 5 ml of dichloromethane. Next, 0.5ml of an internal standard (p-hydroxybenzoicacid n-hexyl ester, 0.1mg/ml) was added, shaken for 10 minutes, and centrifuged at 3000rpm for 10 minutes. Next, the upper layer was removed, and 5 ml of methanol was added to the remaining dichloromethane layer, which was used as a sample for high-speed liquid chromatography (HPLC). As a control group, dichloromethane was added before adding NADPH to prevent a reaction, and as a control group, the same amount of coconut oil and coconut fruit extract were used. Coconut fruit extract was prepared in the same manner as in Example 1 after separating the kernel portion of the coconut. The enzyme inhibitory activity compared to the control is shown in Table 1 below.

sample 5α-reductase inhibitory activity (%) 50 ug/ml 100 ug/ml 200 ug/ml CH extract 18.74 30.45 70.58 CB extract 10.84 25.26 48.19 CH fermented extract 17.25 35.81 68.77 CO 4.59 7.14 11.59 CN extract 5.78 8.58 15.54

CH extract: Coconut Huisthorium extract; CB extract: pre-emergence coconut germ extract; CO: coconut oil; CN Extract: Coconut Fruit Extract

As shown in Table 1, it was found that the coconut haus thorium extract or the coconut germ extract before germination according to one embodiment inhibited the activity of 5α-reductase in a concentration-dependent manner. On the other hand, it was found that coconut oil, which is a comparative group, has little effect of inhibiting the activity of 5α-reductase, and the coconut Huis Thorium extract has an effect of about 5 to 6 times more than that of coconut oil. These results show that the coconut haus thorium extract or the coconut embryo extract before germination according to an embodiment inhibits 5α-reductase, which promotes the production of dihydrotestosterone, a male hormone that causes hair loss, to prevent or improve hair loss. It means that it can be used usefully.

Experimental Example 2. Vivo, which is the hair growth effect of coconut germ extract ( in vivo ) analysis

A mouse model was used to analyze whether the coconut humus thorium extract prepared in Examples 1 and 2 and the coconut germ extract before germination exhibited activity in vivo.

Specifically, a total of 6 mice (C57BL/6, OrientBio) of about 5-6 weeks old were used to remove the hair on the back, and each of the prepared coconut Huis Thorium extract and the coconut germ extract 200 ug/ml before germination were added to each of 3 mice. It was applied once a day for 4 weeks. The ratio of the area grown by the new hair to the area from which the hair was removed was photographed with a digital camera (Japan, olympia) and compared using an image analyzer (Image analyzer/Image-Pro Plus, USA), and the results are shown in Table 2 below. I got it.

sample Hair-regrown area/shaved area
Area ratio (%) CH extract 70.33±3.45 CB extract 50.16±4.22

CH extract: Coconut Huisthorium extract; CB extract: Coconut germ extract before germination

As shown in Table 2, the coconut huis thorium extract or the coconut germ extract before germination according to one embodiment has a remarkable hair growth effect, and in particular, the coconut huis thorium extract is about 1.5 times as much as the coconut germ extract before germination. It was found that there was a remarkable effect.

Claims (10)

A cosmetic composition for improving hair loss or promoting hair growth, containing coconut haustorium extract. The cosmetic composition of claim 1, wherein the extract is extracted using water, C1-C4 alcohol, or a combination thereof as a solvent. The cosmetic composition of claim 1, wherein the composition inhibits the activity of 5α-reductase. The method according to claim 1, wherein the hair loss is alopecia areata, hereditary androgenetic alopecia, telogen effluvium, traumatic 　 alopecia, tricotillomania, pressure 　 alopecia, pressure 　 alopecia, pressure alopecia Non-rigid 　 alopecia, syphilis 　 alopecia (Alopecia syphlltiac), seborrheic 　 alopecia (Alopecia seborrhecia), symptomatic 　 alopecia, scarring 　 alopecia, congenital 　 a cosmetic composition for hair loss improvement or hair growth promotion. The cosmetic composition of claim 1, wherein the extract is a fermented extract. delete delete delete A composition for external application for skin for improving hair loss or promoting hair growth, containing coconut haustorium extract as an active ingredient. A health functional food for improving hair loss or promoting hair growth that contains coconut haustorium extract as an active ingredient.