Use of composition containing 24-epicastasterone and 24-iso-epicastasterone as androgen acceptor modulator

A technology of epibrassinolide and androgen receptor, which is applied in the field of medicine, can solve the problems of application limitations, low brassinolide content, difficulty in large-scale synthesis, etc., and achieve the effect of reducing the weight of the prostate gland and improving sexual function

Inactive Publication Date: 2014-05-07
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the extremely low content of brassinolide in natural plants and the difficulty of large-scale synthesis, its application is greatly limited

Method used

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  • Use of composition containing 24-epicastasterone and 24-iso-epicastasterone as androgen acceptor modulator
  • Use of composition containing 24-epicastasterone and 24-iso-epicastasterone as androgen acceptor modulator
  • Use of composition containing 24-epicastasterone and 24-iso-epicastasterone as androgen acceptor modulator

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: 24-mixed epibraschiolide (BR-3) has an androgen receptor regulating effect on young male rats

[0032] 1.1. Test drugs

[0033] 24-Epibrassinolide (BR-3), off-white crystalline powder, purchased from Shanghai Weidi Biochemical (Nanchang) Co., Ltd. Finasteride, white or off-white crystalline powder, was purchased from Zhejiang Xianju Pharmaceutical Co., Ltd. Testosterone propionate injection (TP) was purchased from Shanghai Ninth Pharmaceutical Factory. Both BR-3 and finasteride were prepared with distilled water containing 1% PEG400.

[0034] 1.2. Experimental animals

[0035] 4-week-old male SD rats were purchased from Shanghai Slack Experimental Animal Co., Ltd. Certificate number: SCXK (Shanghai) 2003-0003. Breeding environment: normal grade.

[0036] 1.3. Experimental steps

[0037]After the rats were anesthetized, the bilateral testes were removed under aseptic conditions, and the skin was sutured. On the 2nd day after orchiectomy, the patients w...

Embodiment 2

[0042] Example 2: 24-mixed epibraschiolide (BR-3) has an androgen receptor regulating effect on aged male rats

[0043] 2.1 Test drugs

[0044] BR-3, off-white crystalline powder. Finasteride, white or off-white crystalline powder.

[0045] 2.2 Experimental animals

[0046] 10-week-old male SD rats were purchased from Shanghai Slack Experimental Animal Co., Ltd. Certificate number: SCXK (Shanghai) 2007-0005. Breeding environment: normal grade.

[0047] 2.3 Experimental steps

[0048] 40 male SD rats were randomly divided into groups, 8 rats in each group; continuous intragastric administration for 21 days, during which the body weight was weighed; 24 hours after the last administration, the rats were killed by neck breaking, and the ventral prostate and seminal vesicles were taken. Gland, bilateral adrenal glands, weighed, according to the weight of each organ. The changes of the body weight, seminal vesicles, prostate and adrenal glands of rats in 5 groups were tested....

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Abstract

The invention relates to a use of a composition containing 24-epicastasterone and 24-iso-epicastasterone as an androgen acceptor modulator. The composition containing 24-epicastasterone and 24-iso-epicastasterone can substantially improve the weights of accessory sex organs comprising the prostate and the seminal vesicle of a castrated young male rat, has an androgen effect, can be used for adjusting the sub-healthy state of human bodies, and can be especially used for improving the sexual function and the like; and the composition can obviously mitigate the weight of the prostate of an old male rat, basically has no influences on the weight of the seminal vesicle, has an antagonistic effect on the androgen acceptor, and can be used for specifically inhibiting the hyperplasia and the like of the prostate.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to the use of a composition containing 24-epibrassinolide and 24-isoepbrassinolide as an androgen receptor modulator. Background technique [0002] Brassinosteroids are a class of phytosterols with a unique structure, which widely exist in many animals and plants. Its representative compound, brassinolide, is a kind of plant sterol isolated and identified from rape pollen by American agricultural scientists Grove. Plant growth hormone with high growth and physiological activity. Brassinolide exhibits extremely strong physiological activity at a very low concentration (10ng / plant), and has the advantages of high efficiency, broad spectrum, strong stress resistance, low toxicity, and safety. It is known as the sixth generation plant growth hormone. Because the content of brassinolide in natural plants is extremely low, and it is difficult to synthesize in large quantities, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61P5/26A61P15/00A61P13/08
Inventor 楼丽广李援朝姜标陈红莉施晶晶杜娟娟
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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