KR100832404B1 - Extract of Cuscutae Semen for preventing production of hair loss causative agent and its composition - Google Patents

Abstract

The present invention relates to an active extract for inhibiting testosterone 5 alpha-reductase obtained from a medicinal plant, and more particularly, tosa, pulmonosa, and lump of medicinal plants traditionally used in the Orient. An active extract capable of inhibiting the action of testosterone 5 alpha-reductase from saturation and inhibiting the production of dihydrotestosterone, which causes hair loss, a method of extracting it efficiently, and containing the extract as an active ingredient It relates to raw materials, health foods, cosmetics and herbal medicines for the prevention and treatment of hair loss.

Earth and sand, Macmundong, lump flower, Testosterone 5 alpha-reductase, Dihydrotestosterone, Prostatic hypertrophy, Acne, Hair loss prevention and treatment

Description

Extract of Cuscutae Semen for preventing production of hair loss causative agent and its composition

1 is a thin layer chromatography image of radiolabeled testosterone and DHT.

2 is the earth and sand (兎絲子, Cuscutae) Semen ) is a graph showing the testosterone 5 alpha-reductase inhibition level by the concentration of the extract.

3 is a graph showing the degree of inhibition of testosterone 5 alpha-reductase by concentrations of Sophorae Flos extract.

Figure 4 is a graph showing the testosterone 5 alpha-reductase inhibition degree by concentration of Ligongdong ( 麥 門冬 , Liriopis Tuber ) extract.

FIG. 5 is an image showing the growth of hair by transdermal coating of Tosa, Macmun-dong, and lump flower for 20 days on the hair removal site of C57BL / 6 mice. FIG.

FIG. 6 is a graph showing the area in which hairs were grown by transdermal coating of earth and sand, macmundong, and lump flower extracts on the hair removal site of C57BL / 6 mice for 20 days.

FIG. 7 is a graph showing the weight of hair grown by transdermal coating of earth and sand, macmundong, and lump flower extracts on the hair removal site of C57BL / 6 mice for 20 days.

The present invention relates to a novel 5-alpha-reductase inhibitor which can be used for the treatment of enlarged prostate, acne and androgenetic alopecia, and more particularly, 5-alpha-reductase containing extracts of lumps, tosa and pulmonary dong as active ingredients. It relates to an inhibitor.

5-alpha-reductase is an enzyme found in the prostate, the dermis, sebaceous glands, and hair follicles, and converts testosterone, a male hormone, to dihydrotestosterone (DHT). DHT binds to androgen receptors, enters the nucleus and acts as a transcription factor, which plays a larger role than testosterone in promoting growth and differentiation of the prostate and maintaining homeostasis and function. As we age, male hormone testosterone increases to 5-HT reductase to DHT, which promotes the growth and differentiation of prostate gland, resulting in prostate cancer, prostatic hypertrophy, difficulty urinating, weakness, frequent urination, and nocturia. This can cause a variety of symptoms. In the scalp, as the hair follicles in the forehead and the crown gradually decrease as the DHT increases, the hairs produced from these cells become shorter, thinner and lighter than normal. In these cells, the anagen phase is shorter than before or delayed entry into the anagen phase, resulting in a decrease in the anagen / telogen ratio or the release of telogen hair before new anagen hair is produced. Finasteride (MSD ltd.), A representative 5-alpha-reductase inhibitor, is a 4-azasteroid synthetic derivative that has been approved by the US FDA and is actually used as a treatment for prostatic hyperplasia and male hair loss.

However, Finasteride is limited in terms of its use and usage, such as side effects such as decreased libido and erectile dysfunction, and thus requires little attention and practicality.

In the present invention, the results of intensive search on thousands of extracts of native plants, including all medicinal plants that have been used in herbal medicine to effectively inhibit 5 alpha-reductase and minimize side effects such as Finasteride It was confirmed that the extracts of the earth and sand, lumps, and pulses each inhibit 5 alpha-reductase activity and completed the present invention.

The present invention is characterized in that the testosterone 5 alpha-reductase inhibitory activity of the extract isolated from the earth and sand, lumps, Macmundong.

In the present invention to prepare an extract of earth and sand, lumps, pulses,

(1) drying and pulverizing the earth and sand, lump, pulmonary dong;

(2) extracting hot water by adding 5-10 times the amount of purified water to the herbal medicine content;

(3) Another method is to separate the extract having testosterone 5 alpha-reductase inhibitory activity from the earth and sand, lump, and pulmonary dong, which comprises the step of filtering the purified water extract using a filter paper and then lyophilizing.

The present invention has an excellent effect of inhibiting the activity of testosterone 5 alpha-reductase using the extracts of earth and sand, pulmonary dong, lumped extract isolated according to the extraction method as raw materials for the prevention and treatment of enlarged prostate, acne, hair loss, It may be used as a health food, cosmetics, herbal medicines and the like.

As described above in more detail the present invention.
The present invention is a method for measuring the inhibitory effect of the 5 alpha-reductase activity, the earth and sand, which shows the effect of inhibiting the enzyme activity by treating medicinal plant extracts with testosterone which is the substrate of this enzyme in LNCaP cell line, DU-145 cell line, It relates to the pulsed dong, lump extract.

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In other words, the extract obtained from earth and sand, Macmun-dong, and lump flower had the effect of inhibiting the activity of 5-alpha-reductase for the first time. An active composition with 5 alpha-reductase inhibitory effect was developed.

In addition to the active compositions according to the invention, pharmaceutically acceptable carriers or excipients may be used in the form of unit or multiple dosage forms for tablets, powders, granules, capsules, ointments, suspensions, emulsions or parenteral administration. Can be.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to Examples.

Example  1: earthenware ( 兎 絲 子 ), Macmundong ( 麥 門冬 ), Lump of flowers  Extract separation

The dried earthenware, pulmundong, and lumps were pulverized, and 5-10 times the amount of purified water was added to the sample to extract the hot water at 70 degrees or more for 2 hours to elute the active substance. Thereafter, the purified water extract solution was filtered using a filter paper and then used by lyophilization.

Example  2: testosterone 5 alpha - Reductase  Quantitative Measurement of Activity

5-alpha-reductase serves to convert testosterone to dihydrotestosterone. Therefore, after enzymatic reaction using testosterone labeled with radioisotopes as a substrate, the activity of 5 alpha-reductase was calculated by measuring the amount of dihydrotestosterone converted from testosterone using thin-film chromatography and image analyzer. It was.

As shown in FIG. 1, testosterone and dihydrotestosterone were separated using thin film chromatography and an image analyzer, and it was confirmed that they were quantitatively measured.

Example  3: testosterone 5 alpha - Reductase  Activity inhibition

To investigate the activity-inhibitory activity of 5-alpha-reductase enzyme, LNCaP or DU145 (American Type Culture Collection, CRL-1740, HTB-81), which expresses 5-alpha reductase enzyme, was incubated for 48 hours and then the substrate [ ³ H] Testosterone and Tosa extract, lumped extract, and Macmundong extract were treated and incubated for another 12 hours. After the reaction, the culture solution was extracted twice with ethyl acetate, separated by thin layer chromatography, transferred to an image plate, and radioactivity was analyzed using an image analyzer (Fuji, BAS-1000). The amount of DHT produced was measured. The rate at which testosterone is converted to DHT was compared by calculating the relative value for the amount of DHT produced in the control treated with 0.5% DMSO.

The IC50 value, which is an indicator of the efficacy of the enzyme inhibitor, was calculated by applying the following formula to the measured DHT production rate after treatment with different extract concentrations.

Inhibitory Effect of Each Extract on 5-alpha-reductase

Raw material name IC50 (ug / ml) Tosa Extract 1.1 Lump extract 3.6 Macmundong Extract 10.7
Example 4 Evaluation of the Effect on Hair Growth of C57BL / 6 Mice

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To evaluate the effect of transdermal application of extracts from Tosa, Macmun-dong, and lump flower on hair growth in animals, C57BL / 6 mice (Source: KOATEC Co., Ltd.) ) And the next day only skin-red (pause) animals were used in the experiment. Transdermal application of the extract was performed once daily, at which time it was applied by rubbing 10 times on the same site. The effect on the hair growth was measured by measuring the area of hair growth (%) relative to the application area during the test period, and was evaluated by comparing the weight of the hair grown within the area of the application area 2 × 2.5 cm at the end of the test period.

As described above, the extracts of earth and sand, lumps, ganmundong according to the present invention has excellent testosterone 5 alpha-reductase inhibitory effect, so as an active ingredient, prostate hyperplasia, acne, hair loss prevention and treatment raw materials, health foods, Can be used as a cosmetic or herbal medicine.

Claims (11)

delete delete delete A cosmetic composition for preventing hair loss and promoting hair growth containing the water-soluble extract of Tosa as an active ingredient. delete A health functional food for preventing hair loss and promoting hair growth containing the water-soluble extract of earth and sand as an active ingredient. A health functional food for preventing prostate cancer, which contains a water-soluble extract of earth and sand as an active ingredient. delete Hair loss prevention and hair growth promoting pharmaceutical composition containing a water-soluble extract of earth and sand as an active ingredient. A pharmaceutical composition for preventing and treating prostate cancer, comprising a water-soluble extract of earth and sand extract as an active ingredient. delete

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