JP2781594B2 - 5α-reductase activity inhibitor - Google Patents

Description

The present invention relates to a 5α-reductase activity inhibitor comprising a spruce extract.

[Problems to be solved by conventional technology and invention]

In recent years, the involvement of hormones in hair growth and the like has been suggested. That is, in the hair follicle including the hair papilla cells, the male hormone (testosterone) is replaced by 5α-reductase (Δ
4-3-Ketosteroid-5α-oxide reductase) activates the active androgen (dihydrotestosterone), binds to a receptor, is taken up into the nucleus, and transmits information at the DNA level. The transmitted information regulates oxygen synthesis related to keratin synthesis,
Suppresses keratin synthesis in hair and eventually promotes hair loss. Therefore, in the development of a hair restorer, attention has been paid to studies on inhibitors of the activity of 5α-reductase, which is an androgen activating enzyme. In addition, 5α-reductase activity inhibitors have received attention as preventive and therapeutic agents for benign prostatic hyperplasia.

Conventionally, scalp blood circulation promoting substances such as pepper tincture, assembly extract, Korean ginseng extract, nicotinic acid, methyl nicotinate, etc., which are blended in hair nourishing cosmetics and the like, are 5α.
-Has little ability to inhibit reductase activity, and has no effect as a 5α-reductase activity inhibitor.

The present invention relates to a 5α compound that can be added to a hair restoration cosmetic or the like to improve various effects such as hair growth, hair loss prevention and dandruff prevention.
-To provide a reductase activity inhibitor.

[Means for solving the problem]

The present invention is a 5α-reductase activity inhibitor comprising a spruce extract.

The spruce used in the present invention is a die-dai (Citrus auranti).
um Linn.subsp.amara Engler) is a dried fruit peel.

The spruce extract used in the present invention is obtained by the following method.

The spruce fruit ratio is preferably obtained by drying and pulverizing, followed by immersion extraction in a solvent or extraction using an extractor such as a Soxhlet extractor. In addition, as the extraction solvent, an organic solvent such as methanol and ethanol and water can be mentioned, and among them, a hydroalcohol is preferable.

The spruce extract of the present invention has an appropriate transdermal absorption property, so that the effective concentration of the drug in the scalp is maintained, the skin irritation is low, and the activity of inhibiting 5α-reductase activity is low. is there. For example, the ability to inhibit 5α-reductase activity suppresses the production of active androgen (dihydrotestosterone) in hair papilla cells, thereby exhibiting hair growth and hair loss prevention effects, and further normalizes the scalp metabolic function. It can be applied to hair-growing cosmetics and the like that enhance the effect of preventing dandruff.

The amount of the 5α-reductase activity inhibitor consisting of a spruce extract is, for example, in the case of a hair nourishing cosmetic, 0.004 to 0.4% by weight as a dry matter based on the total weight of the composition.
(Hereinafter abbreviated as wt%), and is preferably 0.
004 to 3.2 wt%. If the amount is less than 0.004% by weight, the desired effect of the present invention is not sufficient. If the amount exceeds 0.4% by weight, the effect corresponding to the increase cannot be expected.

〔Example〕

Hereinafter, the present invention will be described in detail based on Examples and Comparative Examples.

The 5α-reductase activity inhibition test method, mouse hair growth promotion effect test method, human hair growth promotion effect test method and practical test methods described in the Examples are shown below.

(1) 5α-Reductase activity inhibition test method Prostate (wet weight, about 4 g) isolated from a male rat weighing 350 to 400 g contains 3 times the amount of 0.15 M sucrose containing 0.15 M sucrose.
M HEPES (pH 7.4) was added, and homogenized using a Teflon potter homogenizer. Then 3,000rpm
Centrifuge for 10 minutes, suspend the precipitate in 10 ml of the above buffer solution,
Centrifugation was again performed at 3,000 rpm for 10 minutes. The precipitate was resuspended by adding 3 ml of the above buffer solution, and used as an enzyme solution.

Enzyme activity, ^[4-14 C] - testosterone (1.5Nmo
l, 1.5 × 10 ⁵ cpm), NADPH (0.5 μmol), the above enzyme solution (0.03 ml) and a reaction solution having a total volume of 0.1 ml containing each sample.
C. for 60 minutes (enzyme reaction was [4
- ¹⁴ C] - it was initiated by the addition of testosterone). The enzymatic reaction was stopped by mixing 0.4 ml of a mixed solvent of chloroform / methanol (1: 2), and then stopped at 3,000 rpm for 10 minutes.
Centrifuged for minutes. 0.05 ml of the supernatant was adsorbed on a silica gel glass plate, and developed using chloroform / methanol / acetic acid (99.2 / 0.6 / 0.2) as a developing solvent for 15 cm at room temperature. Testosterone and dihydrotestosterone (DHT) were simultaneously developed as reference materials. After the development was completed, the thin plate was scanned using a chromatoscanner, the amount of dihydrotestosterone (DHT) produced by the enzyme reaction was measured, and the 5α-reductase activity inhibition rate (%) was calculated.

Inhibition rate (%) = [1- (A / B)] × 100 A: Amount of DHT produced when each sample was added B: Amount of DHT produced without addition (2) Mouse hair growth promoting effect test Method The skin of the back of the tail of a ddY strain white mouse (male, 6 weeks old, average weight 35 g) was cut with an electric hair clipper, and then completely depilated with a depilatory cream. From the next day, each sample of Examples and Comparative Examples was tested. 0.2 ml per animal was applied to the skin once a day. A group of 10 animals was used for one sample.

The hair growth effect was determined by comparing the evaluation points of the visual evaluation according to the criteria shown in the table below, and the hair length and hair weight with the control group.

On the 14th day after the start of the experiment, the animals were sacrificed, visually evaluated according to criteria, and their evaluation points were totaled to obtain an average evaluation per animal. Furthermore, after removing the skin of the test part, punching out a certain area of skin with a punch having a diameter of 12 mm and drying, the weight of the hair was measured, and the length of the 20 hairs in the hair was also measured. Values were calculated.

(3) Human hair growth promotion effect test method On the ears of the heads of 10 test subjects who are male pattern baldness patients
A sample of the example or the comparative example was applied to the test site where the hair at a position of 5 cm was shaved in a circular shape having a diameter of 1 cm at two places on the left and right at the left and right sides of the hair at a position of 5 cm. And compared to the untreated right side. The results were measured on the 28th day after the start of the test by shaving 20 hairs on each of the left and right test sites, and averaging the length of the 20 hairs on the left side (to which the example or the comparative example was applied) (B ) Was divided by the average value (A) of the lengths of the 20 right hairs (untreated) to evaluate.

The judgment results were shown as the average of (B) / (A) of 10 test subjects.

(4) Practical test method The effect of application to the heads of 20 test subjects who are male pattern baldness patients twice daily in the morning and evening for 6 consecutive months was evaluated. The test results show that the hair growth effect, the hair loss prevention effect, and the dandruff prevention effect are “hair is bristle or hair is increased”, “hair loss is reduced”, and “hair loss is reduced”. The number of respondents. "

In addition, the spruce extract extracted in the Example used what was obtained by the following method.

The spruce fruit peel was dried and pulverized, and 30.0 g of the spruce extract was subjected to reflux extraction using 200 ml of aqueous ethanol (90.0 wt% of ethanol).
got l. 4wt% of dry spruce extract extract
Met.

Examples 1-4, Comparative Examples 1-4 Oily hair tonics In the following raw material composition, as shown in Table 1, various components (5α-reductase activity inhibitor) were blended to prepare respective hair tonics. Then, the various tests described above were performed.

(1) Composition (2) Preparation method In the component (B), nicotinic acid and methyl nicotinate are dissolved in the component (A), and pepper extract and spruce extract are dissolved in the component (C). , And the components (A) and (B) are mixed, stirred and dispersed, and then charged into a container. When used, the contents are shaken and dispersed uniformly.

(3) Characteristics Table 1 shows the results of various tests performed on each oily hair tonic.

As shown in Table 1, Comparative Examples 1 to 4 hardly had the ability to inhibit 5α-reductase activity. In addition, Comparative Examples 2, 3,
4 had skin irritation, and testing on human skin was not possible.

5 consisting of the spruce extract of the present invention of Examples 1-4
The α-reductase activity inhibitor has an excellent ability to inhibit 5α-reductase activity, and showed clearly good results in all tests.

In Examples 1-4, no skin irritation occurred in various tests on human skin.

Examples 5 to 8 and Comparative Examples 5 to 8 Hair Creams Each hair cream was prepared and tested in the same manner as in Example 1, and the results are shown in Table 1.

(1) Composition (2) Preparation method In the component (B), nicotinic acid and methyl nicotinate are dissolved in the component (A), and the pepper tincture and spruce extract are dissolved in the component (C), and each of the components (A) and (C) has a temperature. 80
What was heated and melted at ° C was mixed. Then, while stirring and cooling to a temperature of 50 ° C., add the component (D) and continue stirring to a temperature of 30 ° C. A cream was prepared.

(3) Properties As shown in Table 1, Examples 5 to 5 containing a spruce extract which is a 5α-reductase activity inhibitor of the present invention were blended.
The hair growth cosmetic composition No. 8 has a higher 5α- in comparison with Comparative Examples 5 to 8.
In addition to showing the reductase activity inhibition rate, it showed an excellent effect in various tests.

〔The invention's effect〕

As described above, the 5α-reductase activity inhibitor of the present invention comprising a spruce extract has an excellent ability to inhibit 5α-reductase activity, and can be applied to hair growth cosmetics and the like.

Claims (1)

(57) [Claims] (1) Spruce (Citrus aurantium Linn.subsp.am)
5α-reductase activity inhibitor comprising an extract of ara Engler).