KR19990055304A - 5α-reductase activity inhibiting composition containing cloves - Google Patents

Abstract

The present invention relates to a 5α-reductase activity inhibiting composition containing a clove extract, wherein the 5α-reductase activity inhibiting composition according to the present invention comprises 0.001 to 10% by weight of a clove extract based on the total weight of the composition. In addition, it provides a 5α-reductase composition having not only the effect of preventing hair and hair loss on alopecia, but also has an antibacterial action against the main causes of dandruff and acne and shows excellent effect on human stability.

Description

Compositions having inhibitory activity of 5α-reductase based on Eugenia Caryophyllata

The present invention relates to a composition for inhibiting 5α-reductase activity containing clove, and more particularly, to inhibit the activity of 5α-reductase and to be an anti-dandruff phytilosporum obale and propionibacterium acne. A hair growth promoting composition and a composition for skin containing a clove extract having an antimicrobial action against ness.

In general, the causes of hair loss have been discussed, such as excessive testosterone action, excess sebum secretion, poor blood circulation, the deterioration of scalp function caused by bacteria, flexible factors, aging, stress, and the like. However, to date, no clear cause of hair loss is known, and in recent years, a growing number of people are suffering from hair loss due to changes in diet and stress caused by social conditions. The hair loss population is also on the rise.

Among them, androgenetic alopecia is directly dependent on testosterone because it is dependent on testosterone, and in addition to alopecia, acne and seborrheic dermatitis are also testosterone-dependent chronic skin diseases (Van Luu-The et al. Expression, and Mission No histochemical localization of 5α-reductase in Human Skin, J. Invest.Dermatol , 102, 221-226, 1994).

Referring to the action of the testosterone in relation to the mechanism of hair loss and sebum production is as follows. Testosterone, one of the male hormones, is converted to the active male hormone Dihydrotestosterone by an enzyme called 5α-reductase, which then binds to certain receptors to induce proteins that cause hair loss. Hair loss will proceed. On the other hand, dehydrotestosterone also acts as a major source of overproduction of sebum in sebocytes. The excessive production and secretion of sebum will cause sebum-related diseases such as acne and seborrheic dermatitis. As a result, masculine alopecia, acne and seborrheic dermatitis are due to the excessive production of dihydrotestosterone by the action of 5α-reductase, and if the activity of 5α-reductase is inhibited, these diseases can be fundamentally and effectively prevented and treated.

In order to prevent or treat male hormone-related diseases such as androgenetic alopecia, acne and seborrheic dermatitis, many studies have been conducted to suppress the activity of 5α-reductase, and some substances have been reported, but the effects and practicality are low. Great care was needed for its use.

Accordingly, the present invention provides a composition for inhibiting the activity of 5α-reductase having excellent antimicrobial activity against the main causes of dandruff and acne as well as hair and hair loss prevention against hair loss. It is done.

5α-reductase activity inhibitory composition according to the present invention for achieving the above object is characterized in that it comprises a clove extract.

Hereinafter, the present invention will be described in detail.

The 5α-reductase activity inhibitory composition according to the present invention comprises a clove extract. In the present invention, the clove is the scientific name Eugene caryophyllata (Eugenia caryophyllata), the herbal name is Caryophlii Flos (Cryptium Flos), yet the bud of the clove tree. The clove has a dark brown or dark red color with 10 to 18 mm long hilly burns and four thick calyx and four membranous stools above, with a characteristic scent and a strong taste and later numbing the tongue. . The main active ingredient of this clove is eugenol (70-85%) and contains acetoeugenol, galactic acid, β-carophyllene, 2-hydroxy 4,6-dimethoxy 5-methylacetophenone, etc. do. The eugenol is a colorless or sulfuric clear oil with a specific gravity of 1.035 to 1.1055, which is different from that of other essential oils. In addition, the use of the clove is a dry stomach, it is used for indigestion, acute gastroenteritis, vomiting, hari (Han Dae Seok et al., Herbal medicine, Dongmyeongsa, 265-267, 1994).

The 5α-reductase activity inhibiting composition according to the present invention is preferably composed of 0.001 to 10% by weight of the clove extract based on the total weight of the composition. If the amount of clove extract is less than 0.001% by weight, the effect was not sufficiently exhibited. If it is more than 10% by weight, the stability of the formulation is not good and does not show a dose-proportional effect.

In addition, the 5α-reductase activity inhibiting composition according to the present invention includes a hair growth promoting composition, an antibacterial hair composition, and a skin composition. The hair growth promoting composition includes hinokithiol, pepper tink, tocopherol acetate, nicotinamide benzine, pyrotonolamine, salicylic acid, L-menthol, and the like, which are conventional compounding ingredients, and include shampoo, hair conditioner, hair lotion, and liquid. All formulations that can be applied to the scalp, such as wool type, are possible. The skin composition includes alpha hydroxy acid (α-Hydroxy acid), beta hydroxy acid (β-Hydroxy acid), fragrances, pigments, fungicides, antioxidants, preservatives, moisturizers, etc. Formulations such as creams are possible.

In order to obtain the clove extract, first, the buds of the clove tree are washed and powdered and cooled for 5 days in an extract solvent of about 10 times to obtain a clove extract stock solution, which is then used as a test extract. The extraction solvent used at this time is one or two or more of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, hexane, diethyl ether, dichloromethane It is preferable to mix a solvent.

Hereinafter, the present invention will be described in detail by Examples and Experimental Examples. However, the present invention is not limited to the following examples and experimental examples. Unless otherwise stated in the table below, the unit is% by weight.

Experimental Example 1 Test of Inhibitory Activity of 5α-Reductase Activity of Clove Extract

Inhibition of 5α-reductase activity of the clove extract was tested in the following manner.

First, 5α-reductase was obtained in the liver of 8-10 week old rats (adult, Sprague-Dawley, male rat). Then, a predetermined amount of protein suspension was prepared by protein quantification, and an enzyme reaction solution was prepared by a general method. As a reactor of 5α-reductase, using a radiolabeled testosterone ( ³ H testosterone), the reaction solvent was reacted in an incubator for 2 minutes at a ratio of enzyme reaction solution: protein suspension: clove extract = 70: 20: 10. The remaining material was blown out and dissolved in a developing solvent, which was then developed on a thin layer chromatography (TLC), and the amount of testosterone and the amount of dehydrotestosterone developed were quantitatively analyzed using a densitometer. This measured the conversion rate of testosterone to dihydrotestosterone by 5α-reductase and compared the results with the control (conversion rate without the addition of the clove extract) to determine the inhibition rate of 5α-reductase. Evaluated. Inhibition rate evaluation method is as follows.

Inhibition Rate (%) = [(A-B) / A] * 100

In Equation 1, A is the conversion rate of testosterone to dihydrotestosterone when no extract is added, and B is the conversion rate of testosterone to dihydrotestosterone when the extract is added.

The result of said inhibition rate evaluation is as follows.

Concentration of Clove Extract (%) 0.1 0.01 0.001 0.0001 Inhibition Rate (%) 100.0 100.0 78.2 42.3%

As can be seen from the results of Table 1, the inhibition of 5α-reductase activity of the clove extract is clear.

Experimental Example 2 Antibacterial Activity Test of Dandelion Clove Extract against Dandruff

In order to evaluate the antimicrobial activity of Pyrosporm ovale, a dandruff bacterium of clove extract, was tested by the following method.

After extracting a clove extract of a certain concentration into the phytirosporum obale cultured in a liquid medium and incubating in an anaerobic culture tank to obtain a minimum inhibitory concentration (MIC) inhibiting the development of the phytirosporum obale. The minimum inhibitory concentration range for the phytilosporum obale of the clove extract by solvent was 10 to 100 ppm.

Experimental Example 3: Blood of Clove Extract. Antibacterial test for acnes

Blood of clove extract. In order to evaluate the antimicrobial activity against Acnes was tested by the following method. Blood cultured in liquid medium. Clove extract of a certain concentration was added to Aknes and incubated in an anaerobic culture tank. The minimum inhibitory concentration that inhibits the growth of Acnes was determined. The minimum inhibitory concentration range for Acnes ranged from 10 to 100 ppm.

Experimental Example 4 Isolation and Identification of Active Ingredients

To isolate and identify the active ingredient that strongly inhibits 5α-reductase from the clove extract, transfer the clove extract to a nonpolar solvent and perform column chromatography, thin layer chromatography, and high performance liquid chromatography (HPLC). As a result of the identification of the water-active component of 5α-reductase inhibition and antimicrobial experiments, it was identified as eugenol and the content of eugenol in the extract was 0.01-80. It is in the weight% range.

Examples 1-5 and Comparative Examples 1,2

According to a conventional liquid wool preparation method, a liquid wool preparation containing a clove extract having the components and ratios shown in Table 2 below was prepared.

ingredient Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 ethanol 40.0 40.0 40.0 40.0 40.0 40.0 40.0 Clove Extract 0.1 0.001 0.01 0.1 1.0 Hinokitinol 0.02 0.02 0.02 Pepper Tink 0.3 0.3 0.3 Benzyl nicotinate 0.01 0.01 0.01 Tocopherol Acetate 0.1 Nicotinic acid amide 0.1 0.1 Pyrotonolamine 0.1 0.1 0.1 Salicylic acid 0.3 0.3 0.3 0.3 L-menthol 0.2 0.2 0.2 0.2 0.2 0.2 0.2 Twin 20 0.4 0.4 0.4 0.4 0.4 0.4 0.4 Spices Quantity Quantity Quantity Quantity Quantity Quantity Quantity Purified water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount

Experimental Example 5

In order to determine the inhibitory activity against 5α-reductase of the wool composition prepared according to Examples and Comparative Examples, the inhibitory activity of 5α-reductase activity was evaluated according to the method of Experimental Example 1.

Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 Inhibition rate (%) 100.0 80.2 100.0 100.0 100.0 32.4 24.6

As can be seen from the results of Table 3, the compositions of Examples 1 to 5 containing the clove extract according to the present invention showed a significantly higher inhibitory activity of 5α-reductase activity than the comparative example.

Experimental Example 6

In order to determine the bactericidal power of the dandruff bacteria of the wool composition prepared according to the Examples and Comparative Examples, the wool agent obtained in Examples and Comparative Examples was added to the liquid medium at 5.0%, 1.0%, 0.1%, and 0.01%, respectively. Ptyrosporum obale was inoculated and incubated for 3 to 4 days and the minimum microbial inhibition concentration (MIC) was measured. The results are shown in Table 4.

Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 MIC (%) 0.01 or less 0.01-0.1 0.01-0.1 0.01 or less 0.01 or less 0.1-1.0 1.0-5.0

As can be seen from the results of Table 4, the composition of Examples 1 to 5 containing the extract of the clove according to the present invention exhibits 10 times or more bactericidal power against dandruff than the comparative example containing other fungicides such as pyrotonolamine or salicylic acid. It was.

Experimental Example 7

In order to determine the hair growth promoting effect of the wool composition prepared according to the Examples and Comparative Examples was tested as follows.

Hair on the back of 42-56 days old mice (C57BL / 6, male) was removed. Then, 100 μl of the compositions of Examples and Comparative Examples were applied to the back of 10 mice each day. After that, the ratio of the area where the fresh radish was grown to the area from which hair was removed was determined using an image analyzer. The results are shown in Table 5.

Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 Area ratio (%) 76.8 72.4 81.0 85.6 89.2 38.2 34.2

As can be seen from the results of Table 5, the compositions of Examples 1 to 5 containing the clove extract according to the present invention showed a hair growth promoting effect two or more times higher than the comparative example.

Experimental Example 8

In order to confirm the effect of inhibiting the activity of the excellent 5α-reductase of the composition containing the clove confirmed in the above experimental example and the hair growth promoting effect shown in animal experiments, volunteers with alopecia were selected and tested as follows.

The hair growth promoting effect of the composition according to Example 4 containing the clove extract and Comparative Example 2 containing the same, 5 people each of those with alopecia of adult male alopecia of 30 to 50 years old or a person with an average number of hair loss of 100 or more per day It was measured as a subject.

That is, water drops (approximately 2 ml) were applied to the hair loss site at least 1 month to 3 months, and further use was not effective.

As a result, the hair loss at the time of hair removal, the subject's self-sympathy symptoms, visual evaluation, etc. were evaluated as a result of the composition according to Example 4 containing the clove extract was found to have an improvement effect of 4 out of 5 people, Comparative Example 2 One composition was found to be effective. In addition, no side effects were found in the subject's message during the use period, and thus it was confirmed that the composition is stable to the human body.

Examples 6 to 10 and Comparative Examples 3 and 4

Soap composition in the form of a solid soap containing the clove extract of the ingredients and ratios as shown in Table 6 after mixing the soap base and the clove extract well in a mixer, followed by extrusion, cutting and shaping in a soap manufacturing machine. Was prepared. Also for comparison a soap composition containing no clove extract was prepared.

ingredient Example 6 Example 7 Example 8 Example 9 Example 10 Comparative Example 3 Comparative Example 4 Soap Base (13% of moisture) Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Clove Extract 0.1 0.001 0.01 0.1 1.0 Lactic acid (α-Hydroxyacid) 0.5 0.5 0.5 Spices Quantity Quantity Quantity Quantity Quantity Quantity Quantity Color Quantity Quantity Quantity Quantity Quantity Quantity Quantity Antioxidant Quantity Quantity Quantity Quantity Quantity Quantity Quantity

Experimental Example 9

In order to determine the inhibitory power of 5α-reductase activity of the soap composition prepared according to Examples 6 to 10 and Comparative Examples 3 and 4, the test was performed in the same manner as in Experimental Example 1.

Example 6 Example 7 Example 8 Example 9 Example 10 Comparative Example 3 Comparative Example 4 Inhibition rate (%) 100.0 76.8 100.0 100.0 100.0 24.1 42.5

As can be seen from the results of Table 7, the compositions of Examples 6 to 10 containing the clove extract according to the present invention showed a significantly higher inhibitory activity of 5α-reductase activity than the comparative example.

Experimental Example 10

Blood of the soap composition prepared according to Examples 6 to 10 and Comparative Examples 3,4. In order to determine the bactericidal activity against Acnes, the soap compositions obtained in Examples and Comparative Examples were dissolved in water at 10% by weight and added to the liquid medium at 50.0%, 10.0%, 1.0%, and 0.1%, respectively. Inoculated with Acnes and incubated for 3 to 4 days and measured the minimum microbial inhibitory concentration (MIC). The results are shown in Table 8.

Example 6 Example 7 Example 8 Example 9 Example 10 Comparative Example 3 Comparative Example 4 MIC (%) 0.01 or less 0.01-0.1 0.01-0.1 0.01 or less 0.01 or less 1.0-5.0 0.1-1.0

As can be seen from the results of Table 8, the soaps of Examples 6 to 10 containing the clove extract according to the present invention exhibited an excellent sterilizing power of 10 times or more compared to soaps not containing the same.

Experimental Example 11

The effect of inhibiting the activity of the superior 5α-reductase of the composition containing the clove identified in the above experimental example and blood. In order to confirm the strong bactericidal action against Acnes, the effects on acne, a representative disease caused by their complex action, were tested as follows.

In order to examine the effect of preventing and treating acne for soap according to Example 6 containing the extract of Clove and Comparative Example 3 not containing the same, five men in their late teens to late twenties were selected as test subjects. It was used three times a month.

The results were evaluated by visual observation of the reduction of cotton cloth, the progress of inflammation, and the like. According to Comparative Example 3, three out of five people were found to have an improvement effect. No one showed any improvement on soap.

As described above, the 5α-reductase activity inhibiting composition according to the present invention comprises a clove extract as a component thereof, which not only has the effect of preventing hair and hair loss against alopecia, but also has an antibacterial effect against the main causes of acne. It has an excellent effect on human stability.

Claims (5)

5α-reductase activity inhibiting composition comprising clove extract in an amount of 0.001 to 10% by weight based on the total weight of the composition. The 5α-reductase activity inhibiting composition according to claim 1, wherein the clove extract is eugenol. A method of using the 5α-reductase activity inhibitory composition according to claim 1 as a hair growth promoting composition, having an anti-hair loss action. A method of using the 5α-reductase activity inhibiting composition according to claim 1 as an anti-dandruff and anti-itching hair composition, which has an antibacterial action against phytirosporum obale. A method of using the 5α-reductase activity inhibitory composition according to claim 1 as an anti-acne treatment and prevention skin composition, which has an antibacterial action against propionibactium acnes.