KR20100007003A - Composition for preventing hair loss or promoting hair growth comprising an extract of crataegis fructus - Google Patents

Abstract

PURPOSE: A composition containing Crataegis fructus extract for preventing hair loss or promoting hair growth is provided to promote growth of human keratinocytes and dermal papilla cells. CONSTITUTION: A composition for preventing hair loss or promoting hair growth contains Crataegis fructus extract as an active ingredient. The Crataegis fructus extract is isolated using water, alcohol of C1-C4, n-hexane, ethyl acetate, or their mixture. The extraction solvent is water, 70-95 weight% of ethanol solution, or methanol. The hair loss is Alopecia Areata, Androgenetic Alopecia, Alopecia syphlltiac, Alopecia seborrhecia, and Telogen Effluvium. The composition is formulated in powder, granule, tablet, capsule, suspension, emulsion, syrup, oral aerosol, external formulation or sterilization injection solution.

Description

Composition for preventing hair loss or promoting hair growth comprising an extract of the hawthorn extract {Crataegis fructus}

The present invention is a mountain lion ( Crataegis fructus ) relates to a composition for preventing hair loss or promoting hair growth comprising the extract as an active ingredient.

The causes of hair loss have been discussed in the role of male hormones in organs such as hair roots and sebaceous glands, lowering blood flow of hair follicles, scalp abnormalities caused by bacterial reproduction or excessive sebum secretion, genetic factors, and aging. However, no clear cause for hair loss has yet been identified, and in recent years, more and more people are suffering from alopecia and their age is decreasing.

There is still no clear effect on the treatment of alopecia, and there are some prescriptions related to hair loss, such as new quantitative diagnosis, and massage of horsetail oil (sesame) on the bald area, or prescription of herbal medicine ( There is a method of applying alcohol and a method of stimulating a specific blood level, but there are many individual differences in the effects, and generally applicable drug substance has not been reported yet.

There are more than 1.3 million hairs and 100,000 hairs in the human body. These hairs go through three stages of growth, anagen, catagen, and telogen. Hair loss refers to a condition in which hair or hair is less or less than normal due to some cause, and is classified into general hair loss phenomenon (telogen effluvium) in which hair falls out of a resting state and anagen effluvium, which is abnormal hair loss. The latter is commonly referred to as hair loss. Alopecia (or alopecia disorders) is characterized by alopecia areata, hereditary androgen alopecia, Telogen Effluvium, traumatic, tritoti lomania, and pressure, depending on the form, symptoms, or causes. Alopecia is classified as growing alopecia, nasal stiffness, alopecia syphlltiac, seborrheic alopecia (Alopecia seborrhecia), symptomatic, scarring, congenital alopecia.

Conventional methods for treating alopecia include formulations based on female hormones in relation to hormonal theory, but there are reports of not only effects but also skin inflammation and side effects caused by hormone administration. As a hair regrowth agent, a formulation consisting mainly of minoxidil, trichosaccharide (Crinos, Co., Italy), etc., of U.S., has been used, but there are no obvious effects and side effects. Finasteride, developed by Merck, is known to inhibit the activity of 5-α-reductase, an enzyme that acts on male hormone testosterone metabolism in hair follicles, but it can cause depression. This also has the problem that long-term treatment is required. In addition to these, there are Cressina and Rogaine, but they are only used if the hair roots are alive in normal scalp, before hair loss disease is fully developed. As mentioned above, various types of conventional hair regrowth have been attempted to help hair growth for the purpose of promoting blood circulation of the scalp and nourishing hair roots. However, the present invention is also toxic and side effects are severe and the effect is insufficient. .

The present inventors conducted various studies to develop extracts having hair loss prevention and hair growth promoting functions for natural products, which are safer than synthetic chemicals. As a result, the fruit of the hawthorn, that is, the extract obtained from the hawthorn, has the activity of promoting the growth of human dermal papilla cells and human keratinocytes, thereby promoting hair growth and healthy scalp growth. It has been found that by promoting the progression of hair loss, it has the activity of promoting hair / hair growth and growth of hair.

Accordingly, an object of the present invention is to provide a composition for preventing hair loss or promoting hair growth, which comprises an extract of an hawthorn as an active ingredient.

According to one aspect of the invention, mountain lion ( Crataegis fructus ) comprising an extract as an active ingredient, a composition for preventing hair loss or promoting hair growth is provided.

The hawthorn extract may be obtained by performing an extraction process comprising extracting hawthorn with an extraction solvent selected from the group consisting of water, C ₁ -C ₄ alcohols, n-hexane, ethyl acetate, and mixed solvents thereof. have. The extraction solvent may be preferably selected from the group consisting of water, methanol, ethanol, butanol, and mixed solvents thereof, more preferably water, 70 to 95% by weight of an ethanol aqueous solution, or methanol. .

According to the present invention, it has been found that the hawthorn extract can promote hair growth and healthy scalp growth by having the activity of promoting the growth of human dermal papilla cells and human keratinocytes. lost. Therefore, the hawthorn extract may be useful for alleviating the progression of hair loss, hair / hair growth of hair, growth promoting composition, that is, hair loss prevention or hair growth pharmaceutical composition or functional cosmetic composition.

The present invention is a mountain lion ( Crataegis fructus ) provides an extract for preventing hair loss or promoting hair growth comprising the extract as an active ingredient.

The hawthorn ( Crataegis fructus ) refers to the fruit of the hawthorn ( Crataegus pinnatifida ). The hawthorn blossoms in white in May and hangs on the inflorescence. Fruits are fruit (이 果) round and have white spots. Sansa's main components are essential oils, flavin, tannins, etc., and are known to have an effect on improving blood circulation, blood pressure control, and stabilizing effects. In Europe, the fruit of the European hawthorn is also called Crataegus and is also used as a cardiac medicine.

According to the present invention, it has been found that the hawthorn extract can promote hair growth and healthy scalp growth by having the activity of promoting the growth of human dermal papilla cells and human keratinocytes. lost. Therefore, the hawthorn extract may be useful for alleviating the progression of hair loss, hair / hair growth of hair, growth promoting composition, that is, hair loss prevention or hair growth pharmaceutical composition or functional cosmetic composition. The alopecia (or alopecia disease) is alopecia areata (Alopecia Areata), hereditary androgen alopecia (Androgenetic Alopecia), resting alopecia (Telogen Effluvium), traumatic, tritoti lomania, Pressure Alopecia, etc. Nasal stiffness, Alopecia syphlltiac, Alopecia seborrhecia, symptomatic, scarring, congenital alopecia and the like.

In the composition according to the present invention, the hawthorn extract comprises extracting the hawthorn extract with a solvent selected from the group consisting of water, C ₁ -C ₄ alcohol, n-hexane, ethyl acetate, and a mixed solvent thereof It can be obtained by performing the extraction process. Preferably, the extraction solvent may be selected from the group consisting of water, methanol, ethanol, butanol, and mixed solvents thereof, more preferably water, 70 to 95% by weight of an ethanol aqueous solution, or methanol.

When water is used as the extraction solvent, the extraction may be carried out at room temperature (ie, chilled) or the extraction may be performed at a temperature of about 100 ° C (ie, warmed). Extraction by hot needle using hot water can be preferably used since it can shorten the extraction time. As the extraction solvent when using the alcohol, or aqueous alcohol solution of a C ₁ ~C ₄ of the C ₁ ~C ₄ (e.g., methanol, ethanol, aqueous methanol, or aqueous ethanol), the extraction process is to 5 days at room temperature for 10 Days, preferably for about 7 days. The extraction may be carried out under shading and / or warming (eg warming) conditions as needed. In addition, the extraction process may be performed once or plural times, preferably about three times. The obtained extract can be concentrated in a reduced pressure or dried under a conventional method, for example, at 20 to 40 ° C., if necessary, to obtain a hawthorn extract in liquid or powder form.

The hawthorn extract can be obtained by performing an additional extraction process to increase the content of the active ingredient. That is, by extracting the extract obtained using water, alcohol, or an aqueous alcohol solution as described above with an organic solvent such as n-hexane, ethyl acetate, butanol (and chromatographic fractionation step) to a high content of the active ingredient Mountain lion extract can be obtained.

The composition of the present invention may be in the form of a pharmaceutical composition comprising the above-mentioned hawthorn extract and a pharmaceutically acceptable carrier. The pharmaceutical compositions may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral formulations, external preparations, and sterile injectable solutions according to conventional methods. The pharmaceutically acceptable carrier is lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline Cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil and the like. Also included are diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, surfactants, and the like. Oral solid preparations include tablets, pills, powders, granules, capsules and the like, and such solid preparations include at least one excipient such as starch, calcium carbonate, sucrose or lactose ( lactose), gelatin, and the like, and may include lubricants such as magnesium stearate, talc, and the like. Oral liquid preparations include suspensions, solvents, emulsions, syrups, and the like, and may include water, diluents such as liquid paraffin, wetting agents, sweeteners, fragrances, preservatives, and the like. Parenteral preparations include sterile aqueous solutions, non-aqueous solvents, suspending agents, emulsions, and lyophilized preparations. Non-aqueous solvents and suspending agents include propylene glycol, polyethylene glycol, and vegetable oils such as olive oil and ethyl oleate. Injectable esters such as the like and the like.

The dosage of the hawthorn extract contained in the pharmaceutical composition depends on the condition and weight of the patient, the extent of the disease, the form of the drug, the route of administration, and the duration, and may be appropriately selected in some cases. For example, the hawthorn extract may be administered at a dose of 0.0001 to 100 mg / kg, preferably 0.01 to 100 mg / kg, and the administration may be administered once or several times a day. In addition, the pharmaceutical composition may comprise the hawthorn extract 0.001 to 50% by weight relative to the total weight of the composition. The pharmaceutical compositions can be administered to mammals, such as humans, by various routes, for example by oral, intravenous, intramuscular, or subcutaneous injection.

The composition of the present invention may be in the form of a functional cosmetic composition comprising the above-mentioned mountain lion extract as an active ingredient. The cosmetic composition may be prepared in various forms according to a conventional cosmetic preparation method using the hawthorn extract. For example, the cosmetic composition may be prepared in the form of a cosmetic product containing the hawthorn extract, shampoo, hair lotion, hair cream, hair gel and the like, which is used by diluting with a conventional cleansing liquid, astringent liquid and a moisturizing liquid. Can be. In addition, the cosmetic composition may include conventional adjuvants such as stabilizers, solubilizers, vitamins, pigments, and flavorings commonly used in the field of cosmetic compositions.

Hereinafter, the present invention will be described in more detail with reference to Examples, Test Examples and Preparation Examples. However, these Examples, Test Examples and Preparation Examples are for illustrating the present invention, and the scope of the present invention is not limited thereto.

Example  1. Preparation of Hawthorn Extract (70% Ethanol Extract)

The fruit of the hawthorn was washed with running water to remove impurities and pulverized to obtain a powder. 1 L of a 70% ethanol aqueous solution was added to 100 g of the obtained powder, and extracted with stirring at room temperature for 7 days. The process was repeated three times, and the extracts were combined and concentrated under reduced pressure at 40 ° C. or lower to obtain 14.9 g (yield 14.9%) of the semi-solid extract.

Example  2. Preparation of Hawthorn Extract (95% Ethanol Extract)

The extraction was carried out in the same manner as in Example 1, except that 1 L of a 95% ethanol aqueous solution was used instead of a 70% ethanol aqueous solution to obtain an extract 10.6 g (yield 10.6%).

Example  3. Preparation of Hawthorn Extract (Methanol Extract)

Extraction was carried out in the same manner as in Example 1, except that 1 L of methanol was used instead of an aqueous 70% ethanol solution to obtain an extract of 40.18 g (a yield of 40.18%).

Example  4. Preparation of Hawthorn Extract ( Hydrothermal  extraction)

Extraction was carried out in the same manner as in Example 1, except that 1 L of water was used instead of a 70% aqueous ethanol solution, and extracted at about 100 ° C. for 4 hours to obtain an extract 56.11 g (yield 56.11%).

Test Example  1. Sansa extract extracts human dermal papilla cells ( human hair dermal papilla  cell) Assessment of impact on growth

The effect of the hawthorn extracts obtained in Examples 1 to 4 on the cell growth effect of human hair papilla cells was evaluated using human hair dermal papilla cells (HHDPC) (Sciencell, Cat. No. 2400). It was.

HHDPC in 0.25 x 10 ⁴ cells / ml in MSC (Mesenchymal Stem Cell) medium containing 10% FBS (fetal bovine serum, Cambrex ) inoculated in 96-well plate for 24 hours, 37 ℃, 5 Cultured under% CO ₂ wet conditions. After treatment with the hawthorn extract obtained in Examples 1 to 4 in a concentration of 0.1, 0.5, 1, 5, 10 ug / ml in the culture solution for 24 hours, 5 mg / ㎖ MTT (3- (4,5 20 [mu] l of -dimethylthiazol-2-yl) -2,5-diphenyl tetrazolium bromide) reagent was added to the culture solution and incubated for 4 hours under 37 ° C and 5% CO ₂ wet conditions. In culture, purple crystals form on living cells. After incubation for 4 hours, the medium was removed, 100 μl of DMSO was added, the crystals were dissolved in a shaking incubator for 10 minutes, and the absorbance at 540 nm was measured to measure the extent of cell growth. The obtained result is shown in FIG. From the results of Figure 1, it can be seen that the hawthorn extract has very high hair papilla cell growth promoting activity.

Test Example  2. Sansa extract is a human keratinocyte ( HaCaT cell ) Assessment of impact on growth

The effect of the hawthorn extracts obtained in Examples 1 and 2 on the cell growth effect of keratinocytes was determined in the same manner as in Test Example 1 using HaCaT cells (Dr. NE Fusenig (Heidelberg, Germany)). As a medium, RPMI medium containing 10% FBS (fetal bovine serum, Cambrex ) was used, and the results obtained from the MTT analysis are as shown in Fig. 2. From the results of Fig. 2, the hawthorn extract was very high in keratinocyte growth. It can be seen that it has promoting activity.

Test Example  3. Due to hawthorn extract C57BL Of hair growth effects in P / 6 mice

The back hairs of the 7-week-old C57BL / 6 mice were removed, and mice with clean back skin were divided into 4 groups of 4-5 mice each. Group A applied 70% ethanol daily for 9 days as a control. Groups B to D treated the trypsin daily to destroy the hair follicles, Group B applied 70% ethanol daily for 9 days, and Group C and D extracted the lioness extract obtained in Example 1 daily. Was dissolved in 70% ethanol and applied for 9 days at a dose of 100 ug / ml and 10 mg / ml each. The results of measuring the degree of hair distribution on days 0, 6 and 9 are shown in FIG. 3.

In addition, in order to observe changes in hair follicle, skin thickness, and tissue in the skin, the mice of each group were killed on the 10th day, and the tissues of the hairy areas of the dorsal skin were collected and 4% form was collected. Fixed with aldehyde solution. After fixation, washed with water and dehydrated, embedded in paraffin, 7 μm sections were prepared and subjected to Hematoxylin & Eosin (H & E) staining. The results of the histological changes are shown in FIG. 4.

3 and 4, the skin color of the mice treated with the hawthorn extract was changed to black in a short time and the hair grew quickly in comparison to the control group, and the actual skin tissue treated with the hawthorn extract after the hair follicle destruction compared to the control group that destroyed the hair follicles. In the group, the growth rate of 42.31% (11/26) at low concentration and 61.54% (16/26) at high concentration were maintained and normal hair morphology was maintained. . In addition, the hawthorn extract was found to be a safe substance without skin irritation.

Figure 1 shows the results of measuring cell growth promoting effect when treated with hawthorn extract human human papillary cells (HHDPC).

Figure 2 shows the results of measuring the cell growth promoting effect when treated with hawthorn extract to human keratinocytes (HaCaT cells).

Figure 3 shows the results of measuring the hair growth promoting effect when the hawthorn extract was treated to C57BL / 6 mice.

Figure 4 shows the results of observation of histological changes when treated with hawthorn extract C57BL / 6 mice.

Claims (4)

Mountain Lion ( Crataegis fructus ) Hair loss prevention or hair growth promoting composition comprising an extract as an active ingredient. The extracting process of claim 1, wherein the hawthorn extract comprises extracting the hawthorn with an extraction solvent selected from the group consisting of water, C ₁ -C ₄ alcohols, n-hexane, ethyl acetate, and a mixed solvent thereof. Composition obtained by performing the. The composition of claim 2, wherein the extractant is selected from the group consisting of water, methanol, ethanol, butanol, and mixed solvents thereof. The composition according to claim 2, wherein the extractant is water, 70-95 wt% aqueous ethanol solution, or methanol.

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