KR20030083159A - Composition for preventing and treating of androgen-dependent disorders comprising curcuma longa extract - Google Patents

Abstract

PURPOSE: Provided is a composition for prevention and treatment of androgen-dependent disorders comprising a Curcuma longa extract that inhibits 5-alpha-reductase activity. CONSTITUTION: A composition for prevention and treatment of androgen-dependent disorders is characterized by containing 0.01-99 wt.5 of a Curcuma longa extract, wherein the Curcuma longa extract is prepared by using a solvent selected from the group consisting of purified water, methanol, ethanol, propanol, butanol, glycerol, propyleneglycol, 1,3-butyleneglycol, ethylacetate, benzene, hexane, diethylether and dichloromethane.

Description

COMPOSITION FOR PREVENTING AND TREATING OF ANDROGEN-DEPENDENT DISORDERS COMPRISING CURCUMA LONGA EXTRACT}

The present invention relates to a composition comprising an extract of Curcuma longa having an activity of inhibiting the activity of 5α-reductase, and more particularly, inhibits overproduction of dihydrotestosterone by 5α-reductase. It relates to a composition comprising turmeric extract effective to prevent and treat male hormone-dependent skin diseases.

Acne, androgenetic alopecia, seborrheic dermatitis, etc. are chronic skin diseases with androgen-dependent disorders (Van Luu-The et al. 5; Characterization, Expression, and Immunohistochemical Localization of 5α-Reductase in Human Skin, J. Invest. Dermatol , 102, 221-226, 1994). Among them, androgenetic alopecia is directly related to the amount of androgen hormones, and thus, many studies have been conducted to prevent and treat hair loss by inhibiting androgen activity.

In addition, acne and seborrheic dermatitis in chronic skin diseases are sebum-related disorders caused by excess sebum produced by male hormones. For fundamental treatment, sebum overproduction is suppressed through inhibition of male hormone activity. It must be restrained.

Briefly explaining the action of male hormones in connection with the sebum production mechanism is as follows. Testosterone, one of the male hormones, is converted to dihydrotestosterone, an active male hormone, by 5α-reductase. The abnormal hyperactivity of this hormone acts as a substance that causes male hair loss and at the same time sebum It acts as a major source of overproduction of sebum in sebocytes. If the sebum is abnormally overproduced or secreted by the above mechanism, sebum-related diseases (acne, hair loss, seborrheic dermatitis) are caused. As a result, male hormone-dependent diseases such as male hair loss, acne, and seborrheic dermatitis are due to the overproduction of dehydrotestosterone by the action of 5α-reductase. Could be.

In order to prevent and treat male hormone-dependent diseases such as acne, androgenetic alopecia and seborrheic dermatitis, many studies have been reported to inhibit the activity of 5α-reductase (Yasuro Sugimoto et al. 3; Cations Inhibit Specific Type I 5α). -Reductase Found in Human Skin, J. Invest.Dermatol, 104, 775-778, 1995), but some substances have been discovered, but the effects are insignificant and the practicality is insufficient due to lack of safety on the skin. .

On the other hand, the Republic of Korea Application No. 1999-034697 discloses a cosmetic composition containing turmeric extract, which contains an extract extracted from the tuber of turmeric, only for the anti-aging cosmetic composition having a free radical scavenging effect It is starting.

Therefore, it is necessary to develop a composition that is excellent in the prevention and treatment of male hormone-dependent diseases such as acne, male hair loss, seborrheic dermatitis, and can be safely and easily applied to the skin.

In order to solve the problems of the prior art, the present invention can effectively inhibit the production of dihydrotestosterone as a potent inhibitory effect on 5α-reductase, and also prevents male hormone-dependent skin diseases including turmeric extract which is safe for skin. And it aims to provide a composition for treatment.

In order to achieve the above object, the present invention provides a composition for the prevention and treatment of male hormone-dependent skin disease comprising turmeric extract.

Hereinafter, the present invention will be described in detail.

The present inventors strongly inhibit the activity of 5α-reductase, which is directly involved in the production of a method for inhibiting the production of active male hormone (dihydrotestosterone), which is a fundamental cause of male hormone-dependent skin diseases, and is safe for long-term use. As a result of pursuing systematic research on various natural products to develop high materials, it was confirmed that turmeric extract strongly inhibits the activity of 5α-reductase at a low concentration, and completed the present invention based on this.

Curcumal longa of the present invention is a perennial herb belonging to the family of Ginger (Zingiberaceae), and in Korea, Eum gold, Gumgeum, jade gold, Wanggeum, and turmeric Also called (深 黃), it is cultivated in all parts of the country except the northern mountainous region. The main ingredient is about 15% curcuminoids, of which curcumin (diferuloylmethane) is the most abundant, and there are also decaffeoylmethane and caffeoylferuloylmethane. . The essential oil is about 15% sesquiterpene and sesquiterpene alcohol. Curcumin in turmeric has antimicrobial activity against Staphylococcus, and para-tolylmethyl carbinol (PTMC) has been reported to be effective for hepatic diseases as well as promoting bile secretion. Fat-soluble components include campesterol, stigmasterol, β-sitosterol, cholesterol, and the like. The pharmacological effects of turmeric reported to date include bile secretion promotion, hepatic disease, bile disease, and it is known that it has an effect of stimulating the detoxification function of the odorant, catarrhal cholelithiasis, diuretic, dipharyngeal effect. In addition, the root stem is called turmeric, tuber root is turmeric, and turmeric has been used as a placebo and pain medication, and it is used for nosebleeds, pisces, and blood.

The turmeric extract is first purified and powdered turmeric root and cooled in about 10 times the amount of the extraction solvent for 5 days, and then the extract can be separated by the usual method of filtration, concentration, and lyophilization. Extraction solvents that may be used include purified water, methanol, ethanol, propanol, butanol, gglycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, nucleic acid, diethyl ether, and dichloromethane. One or more solvents selected from the group consisting of two or more solvents may be mixed and extracted, or one or two solvents may be used for extraction, followed by solvent fractionation using one or two or more solvents.

Turmeric extract of the present invention extracted as described above comprises 0.01 to 99% by weight of curcuminoids depending on the extraction solvent. In addition, the turmeric extract inhibits the activity of 5α-reductase, which causes abnormal hyperactivity of dihydrotestosterone, and is very effective in preventing and treating male hormone-dependent skin diseases such as acne, male hair loss and seborrheic dermatitis. to be.

The turmeric extract prepared as described above may be prepared by adding a conventional additive to a composition such as cosmetics, face wash, and skin ointment.

Turmeric extract of the present invention is preferably contained in an amount of 0.01 to 10% by weight based on the entire composition, such as cosmetics, face wash, skin external ointment. When the content of the turmeric extract is less than 0.01% by weight, the prevention and treatment effect of male hormone-dependent skin disease is insignificant, and when the content of the turmeric extract exceeds 10% by weight, the workability during manufacturing is low, and there is difficulty in stabilization even after the preparation, There is a problem that is not appropriate to use economically because the increase of the effect of the increase of the small.

The cosmetic composition, which is used on the skin, may be prepared in the form of a basic cosmetic, a color cosmetic, or a cosmetic for hair, and may include various conventional carriers and additives suitable for each of these formulations and well known in the art. Can be.

In addition, the face wash composition may be prepared by a common method of mixing turmeric extract with a perfume on a general face wash base, can be added a pigment, fungicide, anti-inflammatory, antioxidant, preservatives, etc., if necessary, to improve the physical properties Inorganic salts and synthetic polymer materials may also be used. In addition, the face wash prepared as described above may be prepared in any formulation such as solid, liquid, cream, paste, pad.

In addition, the skin external ointment composition can be prepared by a conventional method.

The composition for the prevention and treatment of male hormone-dependent skin diseases comprising turmeric extract of the present invention has excellent effects and safety on male hair loss, acne, seborrheic dermatitis, especially when used on acne-prone skin Do.

Hereinafter, preferred examples are provided to aid in understanding the present invention. However, the following examples are provided only to more easily understand the present invention, and the present invention is not limited to the following examples.

EXAMPLE

Example 1. Evaluation of 5α-Reductase Inhibition Rate

In order to measure the inhibition rate of 5α-reductase activity of turmeric extract, 5α-reductase was obtained from livers of 8 to 10 weeks old Sprague-Dawley rats, and a certain amount of protein suspension was prepared by protein quantification. In addition, an enzyme reaction solution was prepared by a general method, and radiolabeled testosterone (3Htestosterone) was used as a reaction substrate of 5α-reductase.

In addition, the turmeric root was purified and powdered and placed in 10 times the amount of purified water and extracted by cooling for 5 days at about 20 ℃, which was filtered with a 300 mesh (filter) filter cloth. The mixture was left at 10 ° C. for 10 days, aged at low temperature, filtered, concentrated under reduced pressure at 60 ° C., and dried.

After the concentration of the turmeric extract is 0.1%, 0.01%, 0.001%, 0.0001%, the enzyme reaction solution: protein suspension: turmeric extract = 70: 20: 20, reacted in an incubator for 2 minutes, the reaction solvent Was blown and the remaining material was dissolved in a developing solvent and developed on a thin layer chromatography (TLC). The amount of testosterone developed and the amount of dihydrotestosterone were quantitatively analyzed using a densitometer. Conversion rate when no turmeric extract is added) is shown in Table 1 below. Inhibition rate was calculated according to the following formula.

[formula]

A: Conversion rate of testosterone to dihydrotestosterone when no extract is added

B: Conversion rate of testosterone to dihydrotestosterone upon addition of extract

Concentration of turmeric extract 0.1% 0.01% 0.001% 0.0001% 5α-reductase activity inhibition rate (%) 100.0 100.0 90.1 46.9

Through Table 1, it was found that turmeric extract strongly inhibits the activity of 5α-reductase.

Examples 2 to 5 and Comparative Example 1. Preparation of face wash

After the cleanser base (containing water) and 0.1% turmeric extract isolated in Example 1 was added to a homomixer with a composition as shown in Table 2 below, the mixture was stirred and heated, and then degassed and cooled to obtain a composition material. This was mixed uniformly to prepare a face wash containing turmeric extract.

division Example 2 Example 3 Example 4 Example 5 Comparative Example 1 glycerin 5.0 wt% 5.0 wt% 5.0 wt% 5.0 wt% 5.0 wt% Monoalkyl phosphates 40.0 wt% 40.0 wt% 40.0 wt% 40.0 wt% 40.0 wt% 50% sodium hydroxide 15.0 wt% 15.0 wt% 15.0 wt% 15.0 wt% 15.0 wt% Myristic acid 5.0 wt% 5.0 wt% 5.0 wt% 5.0 wt% 5.0 wt% Turmeric extract 0.01 wt% 0.1 wt% 1.0 wt% 10.0 wt% - Spices Quantity Quantity Quantity Quantity Quantity Pigment Quantity Quantity Quantity Quantity Quantity Purified water to 100 to 100 to 100 to 100 to 100

Example 6 Acne Prevention and Treatment Effect

In order to measure the clinical effect of the acne prevention and treatment of the facial cleanser prepared in Examples 2 to 5, and Comparative Example 1, after dividing the number of volunteers in the late teens to late 20s to 20 people in each group, 1 It was used three times a day for one month.

As for the determination method, the condition of acne was graded before and after the start of the clinical trial, respectively, and the extent of the difference was determined based on the criteria of Table 3 below.

In addition, if the grade of acne of the clinical trial subjects shows a reduction of 3 or more levels before the test, the effect is excellent; if the decrease is 1 to 2 grades, the effect is moderate; if the decrease does not appear, the effect is not higher. It was determined that the result, and the results are shown in Table 4.

Rating condition 0 Normal condition One Very small number or size of cotton cloth or no inflammation 2 Inflammation does not progress moderately in number or size of cotton cloth 3 Scrub with a small number of inflammatory papules 4 Small and widespread nodules and inflammatory scalp 5 Small number, sized papular nodules 6 Moderate inflammatory nodules 7 A large number of inflammatory nodules are present 8 Severe nodular sclera 9 Severe cystic and inflammatory nodules are present

division Example 2 Example 3 Example 4 Example 5 Comparative Example 1 effect Great 5 people (25%) 8 people (40%) 9 people (45%) 11 people (55%) - middle 10 people (50%) 11 people (55%) 9 people (45%) 8 people (40%) 2 people (10%) none 5 people (25%) 1 person (5%) 2 people (10%) 1 person (5%) 18 people (90%) worse - - - - - Side effects (skin outbreaks, etc.) - - - - - Sum 20 people (100%) 20 people (100%) 20 people (100%) 20 people (100%) 20 people (100%)

Through Table 4, the facial cleansing agent containing the turmeric extracts of Examples 2 to 5 is not only excellent in the acne treatment effect compared to that containing no turmeric extract of Comparative Example 1, and also does not show side effects such as skin redness. I could confirm it.

According to the present invention, the composition containing turmeric extract has an excellent effect on the prevention and treatment of male hormone-dependent skin diseases such as acne, male hair loss, seborrheic dermatitis by inhibiting the excessive production of dihydrotestosterone by 5α-reductase.

Claims (7)

Composition for the prevention and treatment of male hormone-dependent skin disease comprising turmeric extract. The method of claim 1, The male hormone-dependent skin disease is acne, male hair loss, or seborrheic dermatitis composition for the prevention and treatment of male hormone-dependent skin diseases. The method of claim 1, The turmeric extract is a group consisting of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, nucleic acid, diethyl ether, and dichloromethane. A composition for the prevention and treatment of male hormone-dependent skin diseases that is extracted by mixing one or two or more solvents selected from. The method of claim 1, The turmeric extract is selected from the group consisting of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, nucleic acid, diethyl ether, and dichloromethane. After extraction with a solvent that is, and then one or two or more kinds of solvents fractionated by solvent fraction for the prevention and treatment of male hormone-dependent skin diseases. The method of claim 1, The turmeric extract is curcuminoids (curcuminoids) containing 0.01 to 99% by weight of the composition for the prevention and treatment of male hormone-dependent skin diseases. The method of claim 1, The composition for the prevention and treatment of male hormone-dependent skin diseases, the composition for the prevention and treatment of male hormone-dependent skin diseases of the cosmetics, face wash, or skin ointment. The method of claim 1, The turmeric extract is a composition for the prevention and treatment of male hormone-dependent skin diseases comprising 0.01 to 10% by weight of the total composition.