KR100444102B1 - Cosmetic composition for trichogenousness containing Thujae semen extract - Google Patents

Abstract

The present invention relates to a hair growth promoting cosmetic composition containing white porcelain extract. More specifically, the present invention reveals that the organic solvent extract of white porcelain known to have a hair growth effect has an effect of inhibiting 5 alpha-reductase which promotes the production of dihydrotestosterone, an active male hormone causing hair loss, The present invention relates to a cosmetic composition having the effect of preventing hair loss and promoting hair growth by containing such white porcelain extract as an active ingredient.

Description

Cosmetic composition for promoting hair growth containing white porcelain extract {Cosmetic composition for trichogenousness containing Thujae semen extract}

The present invention relates to a hair growth promoting cosmetic composition containing white porcelain extract. More specifically, the present invention reveals that the organic solvent extract of white porcelain known to have a hair growth effect has an effect of inhibiting 5 alpha-reductase which promotes the production of dihydrotestosterone, an active male hormone which causes hair loss, The present invention relates to a cosmetic composition having the effect of preventing hair loss and promoting hair growth by containing such white porcelain extract as an active ingredient.

In male expression, testosterone is involved in male impulse, skeletal muscle increase, male external genital development, scrotum growth, and spermatogenesis, and dehydrotestosterone is involved in acne, sebum increase, hair loss and prostatic hyperplasia. Known ( J. Invest. Dermatol . 1995; 105 (2): 209-14). Since male-type hair loss among male hormone-dependent diseases causes serious mental pain for men in the modern society, which emphasizes beauty, researches are being actively conducted to clarify and improve the mechanism of hair loss.

5alpha-reductase is present in male hormone-reactive tissues such as sebaceous glands, hair follicles, prostate or epididymis, and is a testosterone, a male hormone that is biosynthesized in the testes. It is known to be a reductase involved in the conversion of NADPH as a coenzyme. Excessive secretion of dihydrotestosterone after puberty acts as a major causative agent in the production of sebum in sebocytes, causing acne and male hair loss. In particular, many hair follicle cells provide a cause for hair loss because dihydrotestosterone binds to hormone receptors better than testosterone. Accordingly, studies are being actively conducted to develop a substance that inhibits the activity and production of 5-alpha-reductase, which promotes the production of dihydrotestosterone, and to use it as a hair regrowth or hair loss prevention agent.

Conventionally, female hormones such as estrogen have been used for the treatment of androgenetic alopecia, but female hormones have been reported to cause skin inflammation and side effects due to hormone administration. I'm using it. Recently, Merck in the United States has synthesized finasteride (finasteride, proscar), a drug that inhibits the action of 5 alpha-reductase and inhibits the production of dihydrotestosterone, and is commercially available as an oral administration hair regrowth, but is expensive and applied to the scalp If manufactured for direct application and the effect is ineffective and other side effects of oral administration occurs, there is a limit to use.

Accordingly, the present inventors have extracted white porcelain, known to have hair loss prevention and hair growth promoting effects, using organic solvents, and have studied the physiological mechanism of white porcelain. As a result, the white porcelain extract of the present invention converts testosterone to dihydrotestosterone. The present invention was completed by finding a hair growth promoting cosmetic composition containing such white porcelain extract because it contains a large amount of an effective substance that effectively inhibits 5 alpha-reductase which causes hair loss.

Therefore, an object of the present invention is to extract the active ingredient white porcelain using an organic solvent. In addition, the active ingredient of the white porcelain extract has been found to have a 5 alpha-reductase inhibitory effect, by containing it as an active ingredient to provide a cosmetic composition for promoting hair growth to prevent hair loss and promote hair growth or hair growth.

Figure 1 shows the effect and delivery process of the male hormone in the hair cells.

Figure 2 shows the process of separating the white porcelain extract of the present invention containing the hair growth promoting active ingredient.

Figure 3 shows the effect of inhibiting 5 alpha-reductase for each solvent extract of the white porcelain extract preparation of the present invention containing the hair growth promoting active ingredient.

Figure 4 shows the effect of inhibiting 5 alpha-reductase by concentration of the white porcelain extract of the present invention containing the hair growth promoting active ingredient.

5 is a test result of 5 alpha-reductase inhibitory effect using the fuzzy rat of the white porcelain extract of the present invention containing the hair growth promoting active ingredient.

In order to achieve the above object, the present invention is to extract the white porcelain extract having the effect of inhibiting the 5 alpha-reductase by heating and extracting the natural solvent and the organic solvent mixed with the organic solvent and heat-extracted, and the white porcelain extract is effective It is characterized by producing a cosmetic composition for promoting hair growth that is effective in preventing hair loss and promoting hair growth by containing it as a component.

The white porcelain extract-containing hair growth promoting cosmetic composition of the present invention has an excellent effect of inhibiting the action of 5-alpha-reductase, which promotes the production and activity of dihydrotestosterone that induces hair loss.

That is, the white porcelain extract of the present invention exhibits a specific effect on 5-alpha-reductase, which is advantageous for selective prescription for therapeutic or cosmetic purposes. Therefore, the present invention is to prepare a white porcelain extract having a 5 alpha-reductase inhibitory effect and to prepare a cosmetic composition for promoting hair growth using the same to prevent hair loss and promote hair growth, but acne due to excessive sebum secretion It can also be manufactured and used as a therapeutic agent or cosmetic composition, such as seborrheic dermatitis or dandruff. In addition, the white porcelain extract of the present invention, which has been found to have an effect of inhibiting 5 alpha-reductase, may be used in addition to male alopecia in preparations for the treatment and prevention of various diseases involving 5 alpha-reductase, such as prostate cancer and prostatic hyperplasia. .

Hereinafter, the configuration of the present invention will be described in detail.

The present invention white phosphorus extract has a 5 alpha-reductase inhibitory effect to prevent hair loss and promote hair growth;

(1) preparing a white porcelain extract by adding and mixing an organic solvent with white porcelain in a dose of 2 to 5 times alone with respect to dry weight of the crude white porcelain;

`(2) preparing a white porcelain extract by heating the white porcelain-organic solvent mixture in an extractor equipped with a cooling capacitor;

(3) concentrating the white porcelain extract under reduced pressure in a reduced pressure evaporator equipped with a cooling capacitor and completely drying it;

It is characterized by being manufactured by a method comprising a.

The white porcelain can be used that is sold as a herbal medicine.

As the organic solvent, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, hexane, hexane, ethyl ether or ethylacetate may be used. At this time, it can be simply extracted using only one solvent of the organic solvent, it may be fractionally extracted using the organic solvent and water.

In the heating of (2), it is preferable to heat at 50 to 100 ° C. for 1 to 10 hours, but is not limited thereto. In addition to the heat extraction method described above, an active ingredient of white porcelain may be extracted by depositing white porcelain in the organic solvent at 0 to 40 ° C. for 1 to 30 days.

White porcelain (柏子仁, Thujae semen Linne) used in the present invention is 3 to 5 mm in length, 2 to 3 mm in diameter, the shape is a seed of the Thuja orientalis oval-long oval or long columnar. The outer surface is light yellowish white or light yellowish brown, and when it is old, it gradually changes to yellowish brown color, and oil leaks out. The outer surface of the seed is often enclosed by a thin membranous inner epithelium, the tip is usually pointed, and the round triad has dark brown spots. The lower part is a dull round and light in color. When viewed under a microscope, it is white or yellowish white, rich in endosperm, and rich in fat. It is sweet, flat, nontoxic and fragrant, and works on the heart to replenish blood and to stabilize the mind to stop sweating. It is known to soothe the liver and kidneys, to treat heavy and painful symptoms of the lower back or bone, and to have the effect of conscience and deity (, 心 安神), Yunjangtongpyeon (개 通便). .

White porcelain extract with hair growth promoting effect prepared by the above method was tested using 5-alpha-reductase extracted from the prostate gland of the mouse and the test using fuzzy red which caused excessive sebum due to the action of dihydrotestosterone and yellowed skin color. It was shown to have an excellent 5-alpha-reductase inhibitory effect. In addition, the hair growth effect test using a mouse showed a significant hair growth promoting effect.

At this time, the amount of white porcelain extract to be added may be blended in an amount of 0.0001 to 5% by weight (w / w), preferably 0.001 to 1% by weight (w / w) based on the dry weight of the cosmetic composition. The cosmetic composition for promoting hair growth of the present invention can be prepared and used in formulations such as flexible cosmetics, nourishing cosmetics, nourishing cream, massage cream, essence, pack, hair tonic, hair lotion, shampoo and tonic that can be applied to hair or skin. have.

Hereinafter, the configuration of the present invention will be described in detail by the production examples and test examples, but the scope of the present invention is not limited thereto.

Preparation Example 1 Preparation of White Porcelain Extract I

250 g of 70% ethanol (ethanol) was added to 100 g of white porcelain, boiled for about 2 hours in an extractor equipped with a cooling capacitor, extracted, filtered to remove the residue, and white porcelain extract was prepared. The white porcelain extract obtained above was concentrated under reduced pressure at 60 ^° C. using a distillation apparatus equipped with a cooling capacitor to obtain 8 g of dried white porcelain extract I.

Preparation Example 2 Preparation of White Porcelain Extract II

250 mL of hexane (hexane) was added to 100 g of white porcelain, boiled and extracted for about 2 hours in an extractor equipped with a cooling capacitor, filtered to remove residue, and white porcelain extract was prepared. The white porcelain extract obtained above was concentrated under reduced pressure at 60 ^° C. using a distillation apparatus equipped with a cooling capacitor to obtain 6 g of dried porcelain extract II.

Preparation Example 3 Preparation of White Porcelain Extract III

200 ml of ethyl acetate (ethylacetate) was added to 100 g of white porcelain, boiled and extracted for about 2 hours in an extractor with cooling condensate, filtered to remove residue, and white porcelain extract was prepared. The white porcelain extract obtained above was concentrated under reduced pressure at 50 ^° C. using a distillation apparatus equipped with a cooling capacitor to obtain 4 g of dried white porcelain extract III.

Preparation Example 4 Preparation of Porcelain Extract IV

To 100 g of white porcelain, 200 ml of hydrated or anhydrous ethanol (ethylacohol) was added, boiled and extracted for about 2 hours in an extractor equipped with a cooling capacitor, followed by adding 200 ml of hexane and water each to separate the hexane layer, Repeat the process. After eluting with ethyl ether again, ethylacetate and water were added 200ml, respectively, to separate the ethylacetate layer and reduced pressure at 50 ^o C using a distillation apparatus equipped with a cooling capacitor. Concentrated 5g of dried white porcelain extract IV was obtained.

Formulation Example 1 Formulation Example of Anti-Hair Loss Nourishing Lotion Containing White Porcine

ingredient Weight ratio (%) White porcelain extract 0.5 Beeswax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.7 Liquid paraffin 5.0 Squalane 5.0 Caprylic / Capric Triglycerides 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxy Vinyl Polymer 0.1 Triethanolamine 0.2 antiseptic Quantity Pigment Quantity Spices Quantity Purified water balance system 100.0

Formulation Example 2 Formulation Example of Hair Loss Prevention Hair Tonic Containing White Porcelain Extract

ingredient Weight ratio (%) ethanol 55.0 Castor Oil 5.0 glycerin 3.0 Pyrotonamine 0.1 White porcelain extract 1.0 Spices Quantity Purified water balance system 100.0

Formulation Example 3 Formulation Example of Hair Loss Prevention Hair Lotion Containing White Porcelain Extract

ingredient Weight ratio (%) Cetostearyl alcohol 2.0 Stearyl Triethyl Ammonium Chloride 2.0 Hydroxyethyl cellulose 0.5 Pyrotonolamine 0.1 White porcelain extract 1.0 Spices 0.5 Purified water balance system 100.0

Formulation Example 4 Formulation Example of Hair Loss Prevention Hair Soap Containing White Porcelain Extract

ingredient Weight ratio (%) White porcelain extract 0.1 Titanium dioxide 0.2 Polyethylene glycol 0.8 glycerin 0.5 Ethylenediaminetetraacetic Acid 0.05 salt 1.0 Pigment Quantity Soap Quantity Toilet soap base (13% moisture, parts by weight) to 100 system 100.0

In order to determine the 5 alpha-reductase inhibitory effect of the extracts I to IV of the present invention white porcelain prepared in Preparation Examples 1 to 4 was carried out according to the test method according to the following method.

Experimental Example 1 Test of 5-alpha-Reductase Inhibitory Effect Using Sprague Dawley Prostate

7-8 weeks old male Sprague-Dawley was killed with diethylether and the abdominal prostate was removed to remove connective tissue. Buffer (0.32M sucrose, 0.1 mM dithiothreitol, 20 mM sodium acetate) was added thereto, chopped finely by a grinder and suspended. The suspension was filtered with gauze, and the filtrate was centrifuged at 1500 x g, and then pellets were taken and the buffer was mixed and suspended at a concentration of 20-30 mg / ml.

After taking a portion of the suspension was placed in a 0.02M phosphate buffer, it is reacted with a substrate which is a testosterone isotopes ³ H attached to measure the amount of dihydrotestosterone product. At this time, the reaction solution is dithiothreitol, 20mM of phosphate buffer (pH 6.5) in 1mM, of 50μM NADPH, [1,2,6,7- ³ H] testosterone 0.1μCi / testosterone (1 × 10 ^-7 M ) And 36 μg enzyme suspension were added to prepare a total reaction solution of 565 μl.

The amount of the white porcelain extract I of the present invention prepared above was dissolved in 10% dimethyl sulfoxide (DMSO) and added to 10 μl per reaction. The same volume of solvent was used as a control and linolenic acid was used as a positive control.

In addition, the reaction was carried out for 30 minutes at 37 ℃ to add the enzyme suspension prepared above, the reaction was stopped by addition of 600 μl of ethyl acetate and the product was dried through nitrogen gas. This is a drip on the total amount of ethyl acetate to the silica plastic sheet kayijel gel 60 F was dissolved in ₂₅₄ of 50㎕ (Silica plastic sheet kieselgel 60 F ₂₅₄₎ and then a developing solvent ethyl acetate: (1: 1) cyclohexane (cyclohexane) Developed using.

After drying the silica plastic sheet in the natural state, a bath (Bas, FUJIFILM, Japan) system was used to measure the amount of isotopes, and the dried plastic sheet and the exposed film were put together in a bath cassette and stored for one week. The isotope amounts of testosterone and resulting dihydrotestosterone exposed to the film were then quantified using the exposed intensity.

The experiment was used repeatedly for two times, and based on the measurement result, each of 5 alpha-reductase inhibition rates was calculated by the following calculation method. Table 5 shows the results of the 5 alpha-reductase inhibition of the white porcelain extract of the present invention.

Item density Hormone density % Conversion Average conversion rate % Inhibition One Control group 1 - Testosterone 1.9 26.36 25.27 0.00 DHT 0.68 2 Control 2 - Testosterone 1.96 28.73 - - DHT 0.79 3 Positive control (linolenic acid) 10 ppm Testosterone 1.61 12.97 - 48.67 DHT 0.24 4 Preparation Example 1 10 ppm Testosterone 1.66 9.28 - 63.27 DHT 0.17 5 Preparation Example 2 10 ppm Testosterone 2.67 2.20 - 91.29 DHT 0.06 6 Preparation Example 3 10 ppm Testosterone 2.58 1.90 - 92.48 DHT 0.25 7 Preparation Example 4 10 ppm Testosterone 2.67 7.93 - 68.61 DHT 0.25 [Note] * Density: ³ H radioactivity in the testosterone and dihydrotestosterone domains * Conversion rate: Radioactivity amount in the DHT area / total radiation dose * Inhibition rate: 100 × (control conversion rate-sample conversion rate) / control conversion rate

As described in the above results, it can be seen that the extract containing the white porcelain of the present invention has a 5 alpha-reductase inhibitory effect.

Experimental Example 2 5-alpha-reductase inhibitory effect test using fuzzy rat

Fuzzy rat males sold by Charles & River Lab, USA, are naturally controlled by male hormones and are sebum as testosterone is converted to dehydrotestosterone as described above. ) And yellowing of the surface due to overproduction ( Skin Pharmacol . 1997; 10 (5-6): 288-297). This purgelet was used to confirm the 5 alpha-reductase inhibitory effect of the white porcelain extract containing the present invention.

When Finasteride (Merck, USA), a drug known to have an activity that inhibits 5 alpha-reductase, is involved in testosterone metabolism, it was confirmed that the surface of rats did not turn yellow. The white porcelain extract III of the present invention extracted with acetate was diluted to a concentration of 1.0% in a propylene glycol: anhydrous ethanol (7: 3) solution and applied twice a day for 6 weeks to observe that the surface color of the fuzzy rat did not change. It could be confirmed (Figure 5). Therefore, it can be seen that the white porcelain extract of the present invention has an alpha-reductase inhibitory effect.

Test Example 3 Hair Growth Effect Test of White Porcelain Extract through Mouse

30% hydrous ethanol solution containing 2% of the dried extract of the present invention white porcelain extract was prepared to test the hair growth effect of the white porcelain extract of the present invention.

The hair of the back of 47-53 days old (C57BL / 6) was removed, and the back skin was selected to be clean, and 10 rats were selected for each substance group, and 100 μl of the white porcelain extract test substance was applied daily. .

The length of hair and the extent of hair growth over time were compared by adding scores from 0 to 3 according to the degree of restoration after hair removal. In order to compare the degree of hair growth, the control group was applied with 30% alcohol solution to each individual to observe the hair growth state. The results are shown in Table 6.

Test substance Elapsed days 7 days 10 days 15th 20 days Production Examples I to IV 0.42 ± 0.2 1.25 ± 0.31 2.64 ± 0.65 2.95 ± 0.52 Control 0.10 ± 0.1 0.41 ± 0.15 1.53 ± 0.45 1.95 ± 0.40 [Note] Score range: 0-3 points

In the above results, it was confirmed that the extract containing agent of the present invention white porcelain according to the preparation example has a significant hair growth promoting effect.

As described through the preparation and test examples, the white porcelain extract of the present invention, heated and fractionated with natural white porcelain as an organic solvent and concentrated under reduced pressure, has an excellent 5 alpha-reductase inhibitory effect and does not affect the safety of the product. Since there is an excellent effect of promoting hair growth at a concentration, when added to produce a cosmetic, it can be usefully used as a cosmetic for promoting hair growth and hair loss treatment.

Claims (8)

delete delete delete delete delete delete delete 5 alpha-reductase inhibitor composition containing white porcelain extract as an active ingredient.