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A composition for inhibiting 5α-reductase activity and its application

A composition and reductase technology, applied in the field of medicine, can solve the problems of high cost, large side effects of drugs, long cycle, etc., and achieve the effects of inhibiting 5α-reductase activity, reducing DHT content, and preventing and treating synergistic effects.

Active Publication Date: 2021-03-12
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these treatment methods have a long cycle, large dosage, high cost, and the drugs have relatively large side effects, including that various physiological functions of the prostate will be hindered

Method used

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  • A composition for inhibiting 5α-reductase activity and its application
  • A composition for inhibiting 5α-reductase activity and its application
  • A composition for inhibiting 5α-reductase activity and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The in vitro study of the antiproliferative activity of embodiment 1 pharmaceutical composition

[0042] 1. Purpose of the experiment

[0043] In this experiment, the MTT method was used to measure the inhibitory effect of the drug on the abnormal proliferation of prostate epithelial and stromal cells, and the anti-proliferation activity of the drug on the prostate hyperplasia cells was preliminarily verified by in vitro experiments.

[0044] 2. Experimental materials and methods

[0045] (1) Experimental materials

[0046] Proliferating human prostate stromal cells (WPMY-1) and proliferating human prostate epithelial cells (BPH-1) were used as experimental cells.

[0047] (2) Experimental grouping

[0048] The cell experiment is divided into a blank control group and a drug group, wherein the drug group includes a lycopene group (L), a curcumin group (C), an aromatic curcumone group (O), and a composition group (L / C / O), The dose concentrations used in each group we...

Embodiment 2

[0062] Example 2 Study on the proliferative activity of the pharmaceutical composition on papillary dermal cells

[0063] 1. Purpose of the experiment

[0064] Papillary dermal cells are specially differentiated mesenchymal cells that play a role in traditional Chinese medicine in the hair growth cycle. Stimulation and proliferation of these cells promote hair growth in the anagen phase, and such cells can be used as model cells for evaluating hair growth promoting agents.

[0065] 2. Materials and methods

[0066] Papillary dermal cells (DP cells) from human hair follicles were cultured in DMEM supplemented with 10% fetal bovine serum and 10 μl / ml streptomycin / penicillin; the culture was maintained at 37°C in an incubator with 5% CO2 In 2-3 days, the medium was changed; then the DP cells were inoculated on a 96-well plate, and after culturing for 24 hours, according to the drug concentrations of different groups (drug concentrations were the same as in Example 1), the drugs...

Embodiment 3

[0069] Example 3 Study on the Proliferation Inhibitory Activity of Pharmaceutical Compositions on Human Sebocytes

[0070] 1. Purpose of the experiment

[0071] The pilosebaceous unit constitutes a skin structure that is more sensitive to the action of androgens. In particular, sebocytes have significant 5α-reductase activity, so this cell is used as a target cell and model for androgen-dependent skin diseases such as acne.

[0072] 2. Materials and methods

[0073] Human immortalized sebocytes (SZ95 sebocyte line) were cultivated in DMEM medium supplemented with 10% fetal bovine serum, streptomycin / penicillin of 10 μl / ml and recombinant human epidermal growth factor of 5 μg / mL; the culture was maintained at 37 Under ℃, 5% CO In the incubator, change culture medium every 2-3 days; Then SZ95 sebocytes are inoculated on 96 well plate, after cultivating 24h, according to the drug concentration of different groups (drug concentration is the same as embodiment 1) , drugs were ad...

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Abstract

The invention discloses a composition for inhibiting the activity of 5 alpha-reductase. The composition comprises lycopene, curcumin and aromatic turmerone. Researches find that compared with a singleplant extract and a model control group, the composition disclosed by the invention can obviously inhibit the activity of the 5alpha-reductase, reduces the dihydrotestosterone content in animal tissues and serum, obviously induces the activity reduction of benign prostatic hyperplasia cells and human prostatic hyperplasia epithelial cells, obviously induces the proliferation of human sebaceous gland cells, obviously promotes the proliferation of human papilla dermal cells, and has an obvious synergistic interaction effect on the prevention and treatment of prostate diseases, androgenic alopecia or acne and other androgenic diseases. The plant extract composition provided by the invention is efficient and free of toxic and side effects, and has important application value in prevention andtreatment of androgen diseases..

Description

technical field [0001] The invention belongs to the technical field of medicine. More specifically, it relates to a composition for inhibiting the activity of 5α-reductase and its application. Background technique [0002] Testosterone is an androgen synthesized by Leydig cells under the control of hypothalamus and anterior pituitary gland. 5α-reductase is a membrane protease dependent on reduced coenzyme II (NADPH). It is known that human 5α-reductase has two isozymes, type I and type II, and its function is to catalyze the conversion of testosterone (T) into dihydrotestosterone (DHT), the resulting DHT can bind to the androgen receptor and act on the transcription and expression of specific nuclear genes. DHT acts on the differentiation and growth of prostate tissue, the growth of male genitalia, the growth of facial and body hair, and is involved in several diseases such as benign prostatic hyperplasia, prostate cancer, androgenetic alopecia, and androgenic disorders su...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/12A61K31/01A61P35/00A61P13/08A61P5/28A61P17/10A61P17/14
CPCA61K31/01A61K31/12A61P5/28A61P13/08A61P17/10A61P17/14A61P35/00A61K2300/00
Inventor 杜志云王珊珊胡锦荣蔡伊娜许坤城胡蒙蒙潘春杏张泽钧唐丹丹周渭张焜
Owner GUANGDONG UNIV OF TECH
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