KR101167510B1 - Composition for preventing hair loss or promoting hair growth comprising an saponin biotransformant of Ginseng - Google Patents

Abstract

The present invention comprises one of ginseng saponin metabolites, compound K (20-0-β-D-glucopyranosyl-20 (S) -protopanaxadiol) as an active ingredient, hair loss prevention or hair growth promoting composition To provide. The compound K may promote hair growth and healthy scalp growth by having an activity of promoting growth of human dermal papilla cells and human keratinocytes. Therefore, the compound K can be usefully used in the composition to alleviate the progression of hair loss, promote hair growth, hair growth, hair growth, that is, a pharmaceutical composition or a functional cosmetic composition for preventing hair loss or promoting hair growth.

Description

Composition for preventing hair loss or promoting hair growth comprising an saponin metabolite ginseng biotransformant of Ginseng

The present invention comprises compound K (20-O- (beta-D-glucopyranosyl) -20 (S) -protopanaxadiol), one of ginseng saponin metabolites, as an active ingredient, preventing hair loss or promoting hair growth. It relates to a composition for.

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) may include 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, an agent based on US subsidiary minoxidil, Crinos, Co. trichosaccharide, etc. has been used. 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, Compound K, one of ginseng saponin metabolites, 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 to mitigate the progression of hair loss and to have hair / hair growth and growth promoting activity.

Therefore, an object of the present invention is to provide a composition for preventing hair loss or promoting hair growth, comprising compound K as an active ingredient.

According to one aspect of the present invention, a composition for preventing hair loss or promoting hair growth is provided, comprising the compound of formula 1 as an active ingredient.

According to the present invention, compound K, one of ginseng saponin metabolites, has the activity of promoting the growth of human dermal papilla cells and human keratinocytes, thereby growing hair and growing healthy scalp. It has been found that it can promote. Therefore, the compound K can be usefully used in the composition to alleviate the progression of hair loss, promote hair growth, hair growth, hair growth, that is, a pharmaceutical composition or a functional cosmetic composition for preventing hair loss or promoting hair growth.

1 shows the results of measuring cell growth promoting effects when Compound K was treated to human dermal papilla cells (HHDPC).
Figure 2 shows the results of measuring the effect of promoting the growth of cells when Compound K was treated to human keratinocytes (HaCaT cells).
3 shows the results of measuring hair growth promoting effects when Compound K was treated to C57BL / 6 mice.
4 shows the results of observing histological changes when Compound K was treated in C57BL / 6 mice.

The present invention provides a composition for preventing hair loss or promoting hair growth, comprising the compound of formula 1 as an active ingredient.

≪ Formula 1 >

The compound of Formula 1 is a compound known as compound K, and the chemical name is 20-0-β-D-glucopyranosyl-20 (S) -protopanaxadiol. Compound K exhibits potent tumor angiogenesis and cancer cell metastasis suppression activity, type IV collagenase secretion, anti-angiogenesis activity, platelet aggregation inhibitory activity, antiallergic activity, immunopotentiation activity, cancer cell infiltration inhibitory activity, etc. It is known to have. Compound K is one of the metabolites of ginseng, the saponin metabolite of ginseng. Recently, ginseng or ginseng extract is fermented with lactic acid bacteria or intestinal bacteria to disclose a ginseng extract having a high content of compound K and a method of preparing the same (for example, Korean Patent Publication No. 1997-061909).

Compound K may be prepared by Yang et al. (J. Ginseng Res. Vol. 32, No. 3, 226-231, 2008), or by Jo et al. (J. Ginseng Res. Vol. 31, No. 4, 181-. 190, 2007). In addition, compound K can be obtained by a biological conversion method using ginseng saponin microorganisms, enzymes (Le-Qin Cheng et al., Biotechnol Lett (2006) 28: 1121-1127).

According to the present invention, the compound of formula 1, that is, compound K, promotes hair growth and healthy scalp growth by having an activity of promoting growth of human dermal papilla cells and human keratinocytes. It turns out that you can. Therefore, the compound K can be usefully used in the composition to alleviate the progression of hair loss, promote hair growth, hair growth, hair growth, that is, a pharmaceutical composition or a functional cosmetic composition for preventing hair loss or promoting hair growth. The alopecia (or alopecia disease) is alopecia areata (Alopecia Areata), hereditary androgen alopecia (Androgenetic Alopecia), resting alopecia (Telogen Effluvium), traumatic, triticoti lomania, pressurization (Pressure Alopecia), alopecia, Nasal stiffness, Alopecia syphlltiac, Alopecia seborrhecia, symptomatic, scarring, congenital alopecia and the like.

The composition of the present invention may be in the form of a pharmaceutical composition comprising the compound of formula 1 described above 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,

Such solid preparations may include at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin, and the like, and lubricants such as magnesium stearate, talc, and the like. can do. 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 compound of Formula 1 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, but may be appropriately selected in some cases. For example, the compound of Formula 1 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 include the compound of Formula 1 in an amount of 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 compound of Formula 1 as an active ingredient. The cosmetic composition may be prepared in various forms according to a conventional cosmetic preparation method using the compound of Formula 1. For example, the cosmetic composition may be prepared in the form of a cosmetic product containing a compound of Formula 1, shampoo, hair lotion, hair cream, hair gel, etc., which is diluted with a conventional cleansing liquid, astringent liquid and moisturizing liquid Can be used. 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 through test examples. However, these test examples are for illustrating the present invention, and the scope of the present invention is not limited thereto.

Test Example 1 Evaluation of the Effect of Compound K on the Growth of Human Hair Dermal Papilla Cells

The effect of compound K on the cell growth effect of human dermal papilla cells was evaluated using human hair dermal papilla cells (HHDPC) (Sciencell, Cat. No. 2400).

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. Compound K was incubated in the culture solution at a concentration of 0.01, 0.1, 1 ug / ml for 72 hours, and then 5 mg / ml of MTT (3- (4,5-dimethylthiazol-2-yl) -2,5 20 µl of -diphenyl tetrazolium bromide) reagent was added to the culture and incubated at 37 ° C. under 5% CO ₂ wet conditions for 4 hours. As a positive control was treated with finasteride 200 nM and cultured in the same manner as above. 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 test was repeated three times, and the results obtained are shown in FIG. 1. From the results in FIG. 1, it can be seen that Compound K has very high hair papilla cell growth promoting activity.

Test Example 2 Evaluation of the Effect of Compound K on the Growth of Human HaCaT Cells

The effect of compound K on the cell growth effect of keratinocytes was evaluated in the same manner as in Test Example 1 using HaCaT cells (Dr. NE Fuseing, 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 shown in FIG. 2. From the results of FIG. 2, it can be seen that Compound K has very high keratinocyte growth promoting activity.

Test Example 3 Evaluation of Hair Growth Effect in Compound C57BL / 6 Mice

The back hairs of the 7-week-old C57BL / 6 mice were removed, and 4-5 mice with clean back skin were divided into 4 groups. Group A was orally administered saline (saline) once a day, 200 μl for 18 days as a control group. Groups B to D used the Wax-Rosin mixture to destroy the hair follicles, Group B was orally administered with saline for 18 days, and Group C received finasteride at a dose of 0.5 mg / kg. 18 days orally, Group D was dissolved in saline compound K was administered orally for 18 days at a dose of 5mg / kg. The results of measuring the degree of hair distribution on the 8th, 12th and 14th days are shown in FIG. 3.

In addition, in order to observe changes in hair follicle, skin thickness, and tissue in the skin, mice of each group were killed on the 8th day, and tissues of the hair growth site 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 Compound K was blackened in a short time and the hair grew quickly in comparison with the control group, and the number of hair follicles was significantly increased even in actual skin tissue and the normal hair morphology was maintained, thereby providing excellent Compound K. It can be seen that it has a hair growth effect. In addition, it was confirmed that Compound K is a safe substance without skin irritation.

Claims (2)

To include a compound of formula 1 as an active ingredient, hair loss prevention or hair growth promoting pharmaceutical composition.
≪ Formula 1 >

To include a compound of formula 1 as an active ingredient, hair loss prevention or hair growth cosmetic composition.
≪ Formula 1 >

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