KR101541470B1 - Composition for preventing hair loss or promoting hair growth comprising Ginsenoside F2 - Google Patents

Abstract

The present invention provides a hair loss preventing or hair growth promoting composition comprising ginsenoside F2 as an active ingredient. The composition of the present invention can alleviate the progress of hair loss, promote wool / hair growth and growth of hair, and is effective in preventing hair loss or promoting hair growth.

Description

[0001] The present invention relates to a composition for preventing hair loss or promoting hair growth comprising ginsenoside F2,

The present invention relates to a composition for preventing hair loss or promoting hair growth.

The causes of hair loss have been discussed in male or female organs such as hair follicles, hair follicle blood flow, bacterial growth or scalp irregularity due to excessive sebum secretion, genetic factors, and aging Korean Patent Application No. 10-2006-0067229, 2006.07.19, page 2, [0002] paragraph). However, the definite cause of hair loss has not yet been clarified. Recently, people who are suffering from alopecia are increasing and the age group is lowering.

There are no clear effects on the treatment of alopecia, and there are some prescriptions for taking hair loss, such as diagnosis of neonatal volume in Donguibogam, massage of sesame seeds on hair loss site, And the method of stimulating specific blood circulation. However, it is known that there are many individual differences in the effect, and there is not yet reported a new drug substance which can be generally applied.

The human body has more than 1.3 million hairs and more than 100,000 hairs. These hairs go through three cycles of anagen, catagen, and telogen, and each hair is run in an independent cycle. Hair loss refers to a state in which hair or hair is less or no more than normal due to any cause (Korean Patent Application No. 10-2005-0015941, Feb. 25, 2005, paragraph [0002]), The distinction between hair loss (telogen effluvium) and abnormal hair loss phenomenon (anagen effluvium) is distinguished, the latter is generally referred to as hair loss. Alopecia Areata, Androgenetic Alopecia, Telogen Effluvium, Traumatic, Trichotillomania, Pressure, and Alopecia are the most common forms of hair loss (or hair loss disease) (Alopecia syphiltiac), Alopecia seborrhecia, symptomatic, scarring, congenital alopecia, and the like.

As a conventional method for treating alopecia, there is a preparation based on female hormone in relation to hormonal theory, but its use has been discontinued due to reports of skin inflammation and adverse effects caused by administration of hormone. Minoxidil of the US-based company and trichosaccharide of Crinos Co. are used as hair growth promoters, but there is a problem of lack of clear effects and side effects (Korean Patent Application 10-2008-0086248, September 2, 2008, page 2, [0005] paragraph). In addition, finasteride, developed by Merck, is known to inhibit the activity of 5-α-reductase, an enzyme that acts on the male hormone testosterone metabolism in hair follicles, but can cause depression This also has the problem that long-term treatment is necessary.

In addition, there are Crescina and Rogaine, but only when the hair follicle is alive on the normal scalp before the hair loss disease is fully progressed. Thus, various conventional hair growth promoting methods have generally been attempted to promote hair growth with the aim of promoting blood circulation and nourishment of hair follicles, but the toxicity and side effects are also severe and the effect thereof is insufficient at present (Korean Patent Application No. 10-2006-0021965, March 2003, pp. 4-5, [0015] to [0016] paragraph).

Ginseng (Panax ginseng CA Meyer: Ginseng radix) is known as one of the most important medicines used mainly in Chinese medicine, and it is listed in many Chinese books including China. It is used for restoring fatigue, (Korean Ginseng) (1996), which has been used as a sole or prescription constituent herbal medicine for the control of functions of the ginseng, The effects of ginseng on saponin have been studied and the pharmacological effects of central nervous system, various stress, antidiabetic and cardiovascular disorders have been clarified (Benishin CG et al., Effects of Ginsenoside Rb1 on Central Cholinergic (1991), Kang SY et al., Dietary ginsenosides improve endotheliumdependent relaxation in the thoracic aorta of hypercholesterolemic rabbit (1995), Elma ZT et al., Effect of ginsenoside Rg 1 on insulin- ).

Ginsenosides, known as the active ingredients of ginseng, are a major index component of ginseng and about 30 ginsenosides are known in addition to major ginsenosides such as Rb1, Rb2, Rb3, Rc, Rd, Re, Rf, Rg1, Rg2, Rg3 and Rh.

A problem to be solved by the present invention is to provide a composition effective in preventing hair loss or promoting hair growth.

In order to achieve the above object, the inventors of the present invention have searched a variety of active substances that can prevent hair loss or promote hair growth in natural products having excellent safety, and found that ginsenoside F2 is superior to hair papilla cells, Forming cells, and the hair growth promoting effect. The present invention has been completed based on these findings.

Accordingly, the present invention provides a hair loss preventing or hair growth promoting composition comprising ginsenoside F2 as an active ingredient.

The ginseng (Panax ginseng CA Meyer. Ginseng radix) is a perennial herbaceous plant belonging to Panax ginseng (Araliaceae). It has been used for a long time as a medicinal herb and has been used for various pharmacological treatments Has been regarded as the best health food in the world. The chemical composition of ginseng consists of saponin, essential oil, polyacetylene, phenol, alkaloid, polysaccharide, amino acid, organic acid, free sugar, vitamins and inorganic components. Ginseng saponins are classified as protopanaxadiol (PPD), protopanaxatriol (PPT) and oleanane saponins, depending on the structure of the non-sugar moiety. Among them PPD and PPT are ginseng It is known that Ginseng is a unique saponin and has strong potency such as enhanced immunity and anticancer effect. In the present invention, ginseng can be ginseng which is commonly available in the art, and commercially available ginseng can be used.

In the composition of the present invention, the ginsenoside F2 is characterized by being a conversion from ginsenoside Rb1, Rb2, Rc or Rd, which is a ginseng saponin.

The ginsenoside F2 of the present invention is a substance not found in ginseng, which is a saponin-converted product in which ginseng saponin is converted by intestinal bacteria and produced in small quantities. In the examples of the present invention, ginsenoside F2 was obtained by incubating protopanaxadiol-type saponins (ginsenosides Rb1, Rb2, Rc and Rd) and Aspergillus niger-derived cellulase.

The composition of the present invention may contain 0.001 to 99% by weight of ginsenoside F2 relative to the total weight of the composition.

The composition of the present invention may be a pharmaceutical composition, a food composition or a cosmetic composition.

The composition of the present invention can be used for the prevention, treatment or improvement of alopecia. Alopecia Areata, Androgenetic Alopecia, Telogen Effluvium, Traumatic alopecia, Trichotillomania ), Pressure alopecia, alopecia alopecia, alopecia alopecia, Alopecia syphlltiac, Alopecia seborrhecia, symptomatic alopecia, cicatric alopecia, or congenital alopecia.

In addition, the present invention provides the use of the active ingredient contained in the composition of the present invention for preventing hair loss or promoting hair growth.

The present invention also provides a method for preventing hair loss or promoting hair growth comprising the step of administering the active ingredient contained in the composition of the present invention to a mammal, including a human, in need thereof.

Unless otherwise indicated, the description of compositions, uses, and methods of the present invention are equally applicable, unless they are mutually contradictory.

INDUSTRIAL APPLICABILITY As described above, the present invention provides a pharmaceutical composition for preventing hair loss or promoting hair growth, which comprises ginsenoside F2 as an active ingredient, for the prevention or treatment of alopecia.

The pharmaceutical composition may further comprise a pharmaceutically acceptable carrier in addition to the active ingredient. The pharmaceutical composition may be formulated in the form of powders, granules, tablets, capsules, oral preparations such as suspensions, emulsions, syrups and aerosols, external preparations and sterilized injection solutions according to a conventional method. The pharmaceutically acceptable carrier may be selected from the group consisting of lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, Cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, and the like. It also includes diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, surfactants, and the like. Solid form preparations for oral use include tablets, pills, powders, granules, capsules and the like, which may contain at least one excipient such as starch, calcium carbonate, sucrose or lactose ), Gelatin and the like, and may include a lubricant such as magnesium stearate, talc, and the like. Oral liquid preparations include suspensions, solutions, emulsions, syrups, and the like, and may contain diluents such as water and liquid paraffin, wetting agents, sweetening agents, fragrances, preservatives and the like. Examples of the non-aqueous solution include sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions and freeze-dried preparations, and non-aqueous solvents and suspensions include vegetable oils such as propylene glycol, polyethylene glycol and olive oil, And the like.

In the composition, use and method of the present invention, the dosage of the active ingredient varies depending on the condition and body weight of the patient, the degree of disease, the drug form, the administration route and the period, but may be appropriately selected depending on the case. For example, it may be administered in a dose of 0.0001 to 100 mg / kg, preferably 0.01 to 100 mg / kg per day on the basis of the ginsenoside F2, and the administration may be administered once a day or divided into several times have.

Also, the composition may contain 0.001 to 50% by weight of ginsenoside F2 relative to the total weight of the composition. The pharmaceutical compositions may be administered to mammals, such as humans, by a variety of routes, for example, by oral, intravenous, intramuscular, or subcutaneous injection.

The composition of the present invention may be administered or applied locally. Topical application or topical application means direct application of the active ingredient (and composition) to the skin and / or hair. The topical compositions of the present invention may be in the form of solutions, lozenges, pads, creams, ointments, liposomes, sprays, gels, foams, roller sticks, or any other formulations routinely used in dermatology have.

As described above, the present invention provides a food composition for preventing hair loss or promoting hair growth comprising ginsenoside F2 as an active ingredient.

The formulation of the food composition of the present invention may be prepared by a conventional method and may be formulated in the form of capsules or other tablets, granules, powders, beverages, porridge, etc. after drying together with the carrier. .

The food composition of the present invention can be used as a health functional food. "Health functional food" refers to foods prepared and processed using raw materials or ingredients having useful functions in the human body pursuant to Law No. 6727 on Health Functional Foods, and the term "functional" It is intended to take nutrients for the purpose of controlling nutrients and obtaining effects that are useful for health use such as physiological action.

The food composition of the present invention may contain conventional food additives and, unless otherwise specified, the suitability of the food additives as "food additives" is to be determined by the Food and Drug Administration in accordance with General Regulations and General Test Methods approved by the Food and Drug Administration. Shall be determined according to the relevant standards and standards.

Examples of the substances described in the above-mentioned "Food Additive Code" include natural compounds such as ketones, chemical compounds such as glycine, potassium citrate, nicotinic acid and cinnamic acid, persimmon extracts, licorice extract, crystalline cellulose, high- - Mixed preparations such as a sodium glutamate preparation, a noodle-added alkaline agent, a preservative preparation, a tar coloring agent and the like.

The health functional food composition of the present invention can be used in various foods and beverages for prevention of hair loss or promoting hair growth and can be used for various foods, beverages, gums, tea, vitamin complex, health functional auxiliary food, And may be in the form of powders, granules, tablets, capsules, rings or beverages. May be in any food form other than those described above.

As described above, the present invention provides a cosmetic composition for preventing hair loss or promoting hair growth comprising ginsenoside F2 as an active ingredient.

The cosmetic composition may be prepared in various forms according to a conventional cosmetic preparation method using the ginsenoside F2. For example, the cosmetic composition may be manufactured in the form of a perfume product containing ginsenoside F2, shampoo, hair lotion, hair cream, hair gel, hair tonic, shampoo, rinse, soap, lotion, essence, It can be diluted with a normal cleansing liquid, a converging liquid, and a moisturizing liquid. In addition, the cosmetic composition may contain conventional auxiliaries or cosmetically acceptable carriers such as stabilizers, solubilizers, vitamins, pigments, and perfumes which are commonly used in the field of cosmetic compositions.

The carrier for cosmetics includes, but is not limited to, purified water, oils, waxes, fatty acids, fatty acid alcohols, fatty acid esters, surfactants, moisture absorbers, thickeners, viscosity stabilizers, chelating agents, buffers, preservatives, It is not. If necessary, moisturizing agents, anti-inflammatory agents, antibacterial agents, antifungal agents, vitamins, sunscreen agents, antibiotics, perfumes, and dyes may be included.

The active ingredient contained in the composition of the present invention can be formulated by adding a pharmaceutically or pharmacologically acceptable carrier, excipient or diluent. For formulation, Remington's Pharmaceutical Science (recent edition), Mack Publishing Company, Easton PA et al.

The active ingredient of the composition of the present invention, ginsenoside F2, has activities such as promoting the growth of human dermal papilla cells and human keratinocytes. As a result, hair growth and healthy scalp growth can be promoted. Therefore, the composition of the present invention is useful as a pharmaceutical composition, a food composition, or a cosmetic composition for alopecia suppressing or promoting growth of wool / hair growth and hair of hair, and for preventing hair loss or promoting hair growth.

Figure 1 shows the chemical structure of ginsenoside F2.
FIG. 2 shows the results of measuring the effect of ginsenoside F2 on human dermal papilla cells (HHDPC) at different concentrations ((-): negative control, MXD: positive control, F2: ginsenoside F2 ).
Figure 3 shows the effect of ginsenoside F2 and other saponins (ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Re, Rg1, Rg2 and Rg3) on human dermal papilla cells (HHDPC) ((-): negative control, MXD: positive control, F2: ginsenoside F2).
FIG. 4 shows the results of measuring the cell growth promoting effect when ginsenoside F2 was treated with human keratinocyte (HaCaT cell) at different concentrations ((-): negative control, MXD: positive control, F2: Side F2).
FIG. 5 is a graph showing the effect of ginsenoside F2 and other saponins (ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Re, Rg1, Rg2 and Rg3) on human keratinocytes (HaCaT cells) ((-): negative control, MXD: positive control, F2: ginsenoside F2).
FIG. 6 shows the results of measuring the hair growth promoting effect when treating ginsenoside F2 with C57BL / 6 mice.
FIG. 7 shows the results of observing histological changes when treating ginsenoside F2 with C57BL / 6 mice.

Hereinafter, the present invention will be described in more detail through 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 ]

< Example  1> Gin Senocide  Preparation and separation of F2

The ginsenoside F2 according to the present invention can be obtained by the method described in Yang (J. Ginseng Res. Vol. 32, No. 3, 226-231, 2008), Jo (J. Ginseng Res. Vol.31, No. 4, 2007), and the like. According to such an enzymatic method, conventionally, a high-purity ginsenoside standard product was prepared by reacting with enzymes Hesperidinase, Naringinase, pectinase, or by separating from the intestinal metabolites of saponin. However, The reaction of the saponin mixture with the beta-galactosidase enzyme, which is an enzyme isolated from aspergillus without the difficult process of separating the ginsenoside Rb1, Rb2, Rc, Rd, etc., as a substrate of high purity, There is an advantage that it is easy to separate because only the synocide F2 is generated. The structure of the separated ginsenoside F2 is shown in Fig.

[ Test Example ]

< Test Example  1> Gin Senocide  F2 to prevent hair loss or to promote hair growth promoting effect - Human papillary cells ( human hair dermal papilla cell ) Evaluation of growth impact

The effect of ginsenoside F2 on cell growth of human papillary cells was assessed using human hair dermal papilla cells (HHDPC) (Sciencell, cat. No. 2400).

The cells were inoculated to a 96-well plate in a medium of MSC (Mesenchymal Stem Cell) containing 10% FBS (fetal bovine serum, Cambrex) such that HHDPC was 0.25 × 10 ⁴ cells / % CO ₂ and incubated under humid conditions. The cultures were treated with ginsenoside F2 at concentrations of 0.01, 0.1 and 1 ug / ml, respectively, and cultured for 24, 48, and 72 hours. Then, 5 mg / ml of MTT (3- (4,5-dimethylthiazole 2-yl) -2,5-diphenyltetrazolinium bromide) reagent was added to the culture solution and cultured at 37 ° C under 5% CO ₂ wet condition for 4 hours. As a negative control, the culture medium treated with 10 μM of minoxidil (Hyundai Pharm) was used as a positive control in the same condition as above, but in the culture medium in which 200 μl of the solvent was treated instead of ginsenoside F2. In culture, purple crystals form in living cells. After 4 hours of incubation, the medium was removed, and 100 μl of DMSO was added. The crystal was dissolved in a shaking incubator for 10 minutes, and the absorbance was measured at 540 nm to measure the degree of cell growth. The above test was repeated three times, and the obtained results were as shown in Fig.

As shown in FIG. 2, ginsenoside F2 improved mature papillary cell growth by about 2.8-40.4% and showed better activity of promoting growth of papillary cells than minoxidil treated group, which is a positive control group. From the above results, it can be seen that the active ingredient ginsenoside F2 contained in the composition of the present invention has an effect of preventing hair loss or promoting hair growth.

< Test Example  2> Gin Senocide  F2 and other Ginenoside  Comparison of Hair Loss Prevention or Hair Growth Promotion Effect

The effect of ginsenoside F2 on the cell growth of the papillary cells was compared with the other nine saponins (ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Re, Rg1, Rg2 and Rg3). And evaluated in the same manner as in Test Example 1.

As shown in Fig. 3, ginsenoside F2 improved mature papillary cell growth by about 43.7% and the other saponin ginsenosides Rb1 (20.4%), Rb2 (14.9%), Rb3 (14.9% (15.4%), Rd (15.6%), Re (17.5%), Rg1 (19.9%), Rg2 (21.3%) and Rg3 (26.2% , And it was confirmed that it exhibited an activity of promoting the growth of the papillary cell superior to that of the positive control group, minoxidil treatment group.

< Test Example  3> Gin Senocide  F2 to prevent hair loss or promoting hair growth - Human keratinocyte ( HaCaT cell ) Evaluation of growth impact

The effect of ginsenoside F2 on the cell growth effect of keratinocytes was examined in the same manner as in Test Example 1 except that keratinocyte (HaCaT cell) (Dr. NE Fuseing, Heidelberg, Germany) Respectively.

The medium was RPMI medium containing 10% FBS (fetal bovine serum, Cambrex), and the results obtained from the MTT analysis were as shown in FIG.

As shown in FIG. 4, ginsenoside F2 improved keratinocyte cell growth by about 8.3 to 30.8% and exhibited keratinocyte growth promoting activity superior to that of the positive control group, minoxidil. From the above results, it can be seen that the active ingredient ginsenoside F2 contained in the composition of the present invention has an effect of preventing hair loss or promoting hair growth.

< Test Example  4> Gin Senocide  F2 and other Ginenoside  Comparison of Hair Loss Prevention or Hair Growth Promotion Effect

The effect of ginsenoside F2 on the cell growth of keratinocytes was compared with the other nine saponins (ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Re, Rg1, Rg2 and Rg3). And evaluated in the same manner as in Test Example 3.

As shown in FIG. 5, ginsenoside F2 improved keratinocyte cell growth by about 36.9% and other saponin ginsenoside Rb1 (16.7%), Rb2 (14.5%), Rb3 (14.4% (20%), Rd (12.8%), Re (17.5%), Rg1 (19.9%), Rg2 (21.8%) and Rg3 It was confirmed that it exhibited keratinocyte growth promoting activity superior to that of the positive control group, minoxidil-treated group.

< Test Example  5> Gin Senocide  F2 to prevent hair loss or promote hair growth - C57BL / 6 Evaluation of hair growth effect in mouse

Seven-week-old C57BL / 6 mice were divided into three groups (group A-C), from which their backs were removed, Groups A to C were treated with a Wax-Rosin mixture to disrupt the hair follicles, followed by application of saline solution for 18 days (negative control group), and group B received 5 mg / kg For 18 days (positive control group), and group C dissolve ginsenoside F2 in saline and applied for 18 days at a dose of 5 mg / kg. The results of measuring the distribution of hair on days 8 and 12 were as shown in FIG.

In order to observe changes in hair follicles, skin thickness, and texture of the skin, mice of each group were sacrificed on days 4, 8, and 12, and tissues of the hairy areas of the dorsal skin were collected And fixed with 4% formaldehyde solution. After fixing, washing with water, dehydration, embedding with paraffin, and cutting of 7 μm, hematoxylin and eosin (H & E) staining were performed, and histological changes were observed as shown in FIG.

As can be seen in Figs. 6 and 7, in the mice treated with ginsenoside F2, the skin color changed to black in a short time and the hair rapidly grows, and the number of hair follicles was significantly increased in actual skin tissue and the shape of normal hair was maintained . As a result, it was confirmed that ginsenoside F2 exhibited excellent hair growth and was a safe substance without skin irritation.

[ Formulation example ]

< Formulation example  1> Preparation of pharmaceutical composition

100 mg of ginsenoside F2, 100 mg of corn starch, 100 mg of lactose and 2 mg of magnesium stearate prepared in the same manner as in Example 1 were filled in gelatin capsules to prepare capsules.

< Formulation example  2> Preparation of food composition

(4 wt.%), Liquid fructose (0.5 wt.%), Oligosaccharide (2 wt.%), Sugar (2 wt.%) And salt (0.5 wt.%) Prepared in the same manner as in Example 1 Were added, and the remaining amount was adjusted, and homogeneously blended and instant sterilized to prepare a health drink.

< Formulation example  3> Cosmetics  Composition manufacturing

1. Manufacture of nutrition lotion

The nutritional lotion containing ginsenoside F2 prepared in the same manner as in Example 1 was prepared by the following method with the contents in the following table.

[Table 1]

The raw materials 10, 11, 13, and 15 in the above table were heated to 80 to 85 degrees Celsius while being mixed and stirred, and charged into an emulsifier. The raw materials 2, 3, 4, 5, 6, 7, 8, And the mixture was emulsified by charging it into an emulsifier by heating the emulsion. After the emulsification is completed, the raw material 12 is cooled to 50 ° C with stirring using a stirrer, and then the raw material 14 is added thereto, cooled to 35 ° C and then cooled to 25 ° C. .

2. Manufacture of nutritional cream

The composition for the preparation of the nutritional cream containing ginsenoside F2 is shown in Table 2 below.

[Table 2]

Water, purified water, triethanolamine and glycol (1,3-Propanediol) are heated and dissolved at 70 DEG C, and a fatty acid, an oily component, an emulsifier and an antioxidant are heated to 70 DEG C to dissolve. After the emulsification is complete, the solution is cooled to 45 DEG C and the ginsenoside F2 and flavor are added and dispersed and then cooled to 30 &lt; 0 &gt; C.

Claims (9)

A composition comprising 0.1 to 5 wt% of ginsenoside F2, 0.1 to 5 wt% of liquid fructose, 0.1 to 5 wt% of oligosaccharide, 0.1 to 5 wt% of sugar, 0.1 to 5 wt% of salt, Functional foods. The health functional food according to claim 1, wherein the health functional food is a beverage formulation. The health functional food according to claim 1, wherein the health functional food is for preventing or improving alopecia. 4. The method of claim 3, wherein the alopecia are selected from the group consisting of alopecia areata, hereditary alopecia, alopecia areata, traumatic alopecia, hairy wall, compression alopecia, alopecia alopecia, non-rigic alopecia, alopecia alopecia, , Or congenital alopecia.





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