COMPOSITION FOR PREVENTING HAIR LOSS AND PROMOTING HAIR REGROWTH
20230023847 · 2023-01-26
Assignee
Inventors
Cpc classification
A61K31/7048
HUMAN NECESSITIES
International classification
Abstract
Provided is a method of alleviating or treating hair loss, or promoting hair growth by administering to a subject in need thereof composition comprising an active ingredient for preventing hair loss and inducing new hair growth or hair regrowth promotion by reducing the transition period from a telogen stage to an anagen stage in the hair growth cycle, and thereby exhibiting excellent effects of preventing hair loss and promoting hair regrowth by delaying conversion to a catagen stage.
Claims
1-9. (canceled)
10. A method of alleviating or treating hair loss, or promoting hair growth, comprising administering to a subject in need thereof, a composition comprising one or more active ingredient selected from the group consisting of gypsogenin 3-O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X, and chikusetsusaponin Iva, and thereby alleviating or treating hair loss, or promoting hair growth in the subject.
11. The method of claim 10, wherein the active ingredient is in an amount of 0.0001-50 wt % based on the total weight of the composition.
12. The method of claim 10, wherein the composition inhibits the action of male hormones.
13. The method of claim 10, wherein the composition inhibits the expression of hair follicle catagen factor Dkk-1.
Description
DESCRIPTION OF DRAWINGS
[0037]
[0038]
[0039]
[0040]
BEST MODE
[0041] Hereinafter, the present disclosure is described in more detail through examples, etc. However, the examples of the present disclosure may be changed into various forms and it should not be construed that the scope of the present disclosure is not limited by the following examples. The examples of the present disclosure are provided so that the present disclosure is more completely understood by those having ordinary knowledge in the art.
Test Example 1: Androgenic Activity
[0042] A stable cell line constructed by permanently transfecting androgen receptor-positive 22Rv1 human prostate cancer cells with the pGL4.36-MMTV-Luc vector, which possesses two androgen-responsive elements and a firefly luciferase reporter gene, was used for this experiment. The stable cell line was maintained by subculturing using RPMI1640 and 10% fetal bovine serum (GIBCO BRL, Gaithersburg, Md., USA). For transcriptional activation assay, the cells were seeded in a 96-well plate, with 25,000 cells per well, while replacing the medium with phenol red-free RPMI1640 containing 5% charcoal-stripped fetal bovine serum. After culturing in an incubator at 37° C. for 48 hours and then treating with gypsogenin 3O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X or chikusetsusaponin IVa together with 1 nM DHT, the cells were cultured for 24 hours and the inhibition of luciferase activity increased by DHT was measured using a luciferase assay system (Promega). The result was expressed as the inhibition of the luciferase activity by gypsogenin 3O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X or chikusetsusaponin IVa with respect to the luciferase activity increased by treatment with 1 M DHT as 100%. Bicalutamide (Casodex) was used as a positive control group and CCK-8 assay was conducted in parallel to investigate cytotoxicity. The cell culture was treated and incubated with CCK-8 at 1:10 for 2 hours. 2 hour later, the absorbance of each well was measured at 450 nm. All the experiments were 3 times and the absorbance was averaged. The result was expressed as percentage of the group treated with 1 nM DHT as 100%. The experimental result is shown in Table 1, Table 2 and
TABLE-US-00001 TABLE 1 Androgenic activity Androgenic activity (% Groups Concentration of 1 nM DHT) Untreated group — 0 DHT 1 nM 100.0 1 nM DHT Bicalutamide 20 μM 29.8 Gypsogenin 3-O-β-D- 0.2 ppm 98.1 glucuronopyranoside 2 ppm 79.1 20 ppm −9.8 Deapioplatycodin D 0.2 ppm 89.1 2 ppm 72.2 20 ppm 34.9 Congmunoside X 2 ppm 104.4 20 ppm 85.9 200 ppm 14.9 Chikusetsusaponin IVa 0.2 ppm 84.7 2 ppm 79 20 ppm 77.5
TABLE-US-00002 TABLE 2 Cell viability Cell viability Groups Concentration (% of 1 nM DHT) Untreated group — 96.2 DHT 1 nM 100.0 1 nM DHT Bicalutamide 20 μM 101.6 Gypsogenin 3-O-β-D- 0.2 ppm 109.4 glucuronopyranoside 2 ppm 107.6 20 ppm 104.8 Deapioplatycodin D 0.2 ppm 102.2 2 ppm 99.4 20 ppm 81.6 Congmunoside X 2 ppm 97.1 20 ppm 95.9 200 ppm 89.9 Chikusetsusaponin IVa 0.2 ppm 102.0 2 ppm 105.2 20 ppm 99.4
Test Example 2: Inhibition of Expression of Hair Follicle Catagen Factor
[0043] The inhibition of the expression of the hair follicle catagen marker Dkk-1 was investigated using human dermal papilla cells (hDPCs). The human dermal papilla cells were purchased from PromoCell. The hDPCs were subcultured in an hDPC culture medium (follicle dermal papilla cell growth medium; PromoCell, Heidelberg, Germany) containing a medium additive (Supplement Mix; PromoCell, Heidelberg, Germany), 100 units/mL penicillin and 100 ng/mL streptomycin under the condition of 37° C. and 5% CO.sub.2. One million subcultured hDPCs were seeded onto a 100-mm cell culture dish and then cultured in an incubator at 37° C. 48 hours later, after treating with each of gypsogenin 3-O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X and chikusetsusaponin IVa at 2 ppm or 20 ppm for 24 hours, the cell culture was subjected to Dkk-1 ELISA assay (R&D Systems, USA). The protein amount of each test group was identified by BCA assay and corrected with the result of Dkk-1 ELISA. The result is shown in Table 3.
TABLE-US-00003 TABLE 3 Expression of Dkk-1 Concentration Relative expression level of Groups (ppm) Dkk-1 (% of untreated group) Untreated — 100.0 Gypsogenin 3-O-β-D- 2 96.5 glucuronopyranoside 20 77.5 Deapioplatycodin D 2 86.4 20 76.7 Congmunoside X 2 90.8 20 81.2 Chikusetsusaponin IVa 2 85.2 20 70.9
Test Example 3: Hair-Growing Effect of Composition for Treating Hair Loss 1
(Hair Tonic)
[0044] Preparation of Composition for Treating Hair Loss 1 (Hair Tonic) Hair tonic compositions of Examples 1 to 4-2, which contain gypsogenin 3-O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X or chikusetsusaponin Iva as an active ingredient, were prepared as described in Table 4.
TABLE-US-00004 TABLE 4 Flavorant Castor and Purified Ingredients Ethanol oil Glycerin Active ingredient colorant water Weight Comp. 55 5 3 — Adequate Balance ratio (%) Ex. 1 (100 in Comp. 55 5 3 Minoxidil 1 Adequate total) Ex. 2 Ex. 1 55 5 3 Gypsogenin 3-O-β-D- 0.5 Adequate glucuronopyranoside Ex. 1-2 0 5 3 Gypsogenin 3-O-β-D- 0.5 Adequate glucuronopyranoside Ex. 2 55 5 3 Deapioplatycodin D 0.5 Adequate Ex. 2-2 0 5 3 Deapioplatycodin D 0.5 Adequate Ex. 3 55 5 3 Congmunoside X 0.5 Adequate Ex. 3-2 0 5 3 Congmunoside X 0.5 Adequate Ex. 4 55 5 3 Chikusetsusaponin IVa 0.5 Adequate Ex. 4-2 0 5 3 Chikusetsusaponin IVa 0.5 Adequate
[0045] Preparation of Composition for Treating Hair Loss 2 (Hair Lotion)
[0046] Hair lotion compositions, which contain gypsogenin 3-O-β-D-glucuronopyranoside, deapioplatycodin D, congmunoside X or chikusetsusaponin IVa as an active ingredient, were prepared as described in Table 5.
TABLE-US-00005 TABLE 5 Ingredients Weight ratio (%) Cetostearyl alcohol 2 Stearyl triethyl ammonium chloride 2 Hydroxyethyl cellulose 0.5 One or more of gypsogenin 3-O-β-D- 0.01 glucuronopyranoside, deapioplatycodin D, congmunoside X and chikusetsusaponin IVa Flavorant and colorant Adequate Purified water Balance (100 in total)
[0047] The compositions for treating hair loss 1 (hair tonic) of Comparative Examples 1 and 2 and Examples 1 to 4-2 were applied to the hair and scalp of a total of 110 males and females who have significantly fewer hairs than normal people or show the symptoms of alopecia and have weak hairs (10 groups with 11 people in each group) for 6 months, 7 times a week. Then, the improvement of hair thickness, hair density, hair elasticity and overall assessment (very good; +3, good; +2, slightly good; +1, no change; 0, slightly poor; −1, poor; −2, very poor; −3) was evaluated by the users 6 months later. The result is shown in Table 6.
TABLE-US-00006 TABLE 6 Hair Hair Hair Overall thickness density elasticity assessment Comparative 0.2 ± 0.3 0.1 ± 0.2 0.3 ± 0.4 0.2 ± 0.3 Example 1 Comparative 2.2 ± 0.2 2.3 ± 0.4 2.1 ± 0.2 2.2 ± 0.3 Example 2 Example 1 3.6 ± 0.2 3.0 ± 0.2 3.3 ± 0.2 3.3 ± 0.2 Example 1-2 2.6 ± 0.1 2.5 ± 0.3 3.0 ± 0.2 2.7 ± 0.2 Example 2 3.1 ± 0.3 3.4 ± 0.1 3.1 ± 0.2 3.2 ± 0.1 Example 2-2 2.8 ± 0.3 2.8 ± 0.2 2.5 ± 0.4 2.7 ± 0.3 Example 3 2.9 ± 0.1 3.0 ± 0.2 2.7 ± 0.4 2.9 ± 0.2 Example 3-2 2.5 ± 0.4 2.8 ± 0.3 2.5 ± 0.2 2.6 ± 0.3 Example 4 2.9 ± 0.1 2.7 ± 0.3 2.8 ± 0.2 2.8 ± 0.2 Example 4-2 2.2 ± 0.4 2.3 ± 0.3 2.4 ± 0.2 2.3 ± 0.3