CN101961329A - Application of Silibinin in preparing anti-male hormone medicaments - Google Patents
Application of Silibinin in preparing anti-male hormone medicaments Download PDFInfo
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- CN101961329A CN101961329A CN 201010504678 CN201010504678A CN101961329A CN 101961329 A CN101961329 A CN 101961329A CN 201010504678 CN201010504678 CN 201010504678 CN 201010504678 A CN201010504678 A CN 201010504678A CN 101961329 A CN101961329 A CN 101961329A
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- male hormone
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Abstract
The invention discloses application of Silibinin in preparing anti-male hormone medicaments. Experiments show that the Silibinin extracted from seeds of a feverfew purple flower Herba Silybi has the pharmacological effect of reducing male hormone, has the advantages of safe clinical application and small side effect, and can be clinically used as an anti-male hormone medicament.
Description
Technical field
The present invention relates to a kind of new medical usage of silibinin, relate in particular to the purposes of silibinin in preparation antiandrogen medicine, belong to the medical usage field of silibinin.
Background technology
Androgen is a kind of very important hormone in the female reproduction physiological process, is the ovary especially precursor of follicle synthetic estrogen.The androgen level is too high in women's blood, and increased activity claims the excessive androgen mass formed by blood stasis, is common gynecological's endocrine regulation disease.The medicine that is used for the treatment of the excessive androgen mass formed by blood stasis clinically mainly contains several big kinds of oral contraceptive, progestogens, gonadotropin releasing hormone, glucocorticoid, spironolactone and euglycemic agent, and side effect is all bigger, is unfavorable for taking for a long time.
Silibinin is a kind of flavone compound that extracts from the seed of the pale reddish brown Herba Silybi mariani of feverfew (Herba Silybi), significant protection is arranged and stablize hepatocellular effect.Up to now, there is not silibinin to have the report that reduces androgenic pharmacological effect as yet.
Summary of the invention
The inventor is through a large amount of experimental studies have found that, silibinin has the pharmacological effect that reduces androgen, can be used as the androgen antagonist medicine and is used for clinical.In addition, silibinin is a Chinese medicine extract, and clinical practice safety is less to the side effect of human body.
The present invention as the in vitro study object, utilizes dexamethasone artificial induction granular cell with the pig ovary granular cell, finds that the ability of its secretion testosterone strengthens.After adopting the Chinese medicine monomer silibinin to intervene, find that testosterone levels obviously descends in the serum.
When the silibinin extract is added the preparation different dosage form behind the required various adjuvants and pharmaceutically acceptable excipient or carrier, method of Chinese medicinal with routine is prepared into any suitable clinical preparation, for example can be injection (powder pin, freeze-dried powder, liquid drugs injection, transfusion etc.), tablet, oral liquid, granule, capsule, soft capsule or drop pill etc.; Wherein, described adjuvant can be antioxygen chelating agent, filler, framework material etc.; Described pharmaceutically acceptable carrier is one or more in xylitol, mannitol, lactose, fructose, glucosan, glucose, polyvinylpyrrolidone, low molecular dextran, sodium chloride, calcium gluconate or the calcium phosphate.
Description of drawings
The CYP17 mRNA of Fig. 1 RT-PCR reaction detection cultured cell transcribes variation; C is the blank group, and M is the cell model group, and S is the silibinin drug group; β-actin is confidential reference items.
The specific embodiment
Further describe the present invention below in conjunction with specific embodiment, advantage of the present invention and characteristics will be more clear along with description.But these embodiment only are exemplary, scope of the present invention are not constituted any restriction.It will be understood by those skilled in the art that and down can make amendment or replace without departing from the spirit and scope of the present invention, but these modifications and replacing all fall within the scope of protection of the present invention the details of technical solution of the present invention and form.
Test the pharmacodynamics test of routine silibinin antiandrogen
Get pig ovary from slaughterhouse, road junction, Harbin City, Heilongjiang Province city and put into and be added with two anti-normal saline, in 4h, take back laboratory with thermos flask.Enter between dissection with having added two anti-normal saline flushing ovaries 4 times, enter between cell culture after peeling off fatty tissue.With containing two anti-normal saline flushing follicles 3 times, put into the culture dish that contains a small amount of culture medium, puncture follicle sucking-off follicular fluid and separate with the 1mL syringe and cut theca folliculi open and go out granular cell, the follicular fluid that will contain granular cell put into contain normal saline the 50mL centrifuge tube with 1500r/min speed, centrifugal 10min sops up supernatant after centrifugal, granular cell is suspended in contains culture medium (DMEM-F12, hyclone 10%) in the culture bottle, piping and druming repeatedly makes it to disperse.The survival rate of counting cells is with 1 * 10
6The cell concentration of/L inserts in the culture bottle, 5%CO
2, 37 ℃ of incubators of 95% air, saturated humidity cultivate 72h, observe and find inoculation back 24h cell attachment.Cell inoculation on culture plate, is divided into 1,2,3 groups, is respectively group of solvents, model group, silibinin group.Respectively the above cell of respectively organizing is handled the 1st group of normal culture medium that adds the inferior maple of dimethyl (DMSO) that contains respective concentration; 2nd, 3 groups of culture medium that add with same concentrations DMSO dissolving dexamethasone, concentration is 300nmol/L, effect 48h.Behind the 48h, the 2nd group continue to add dexamethasone 300nmol/L, and the 3rd group adds silibinin (available from last Hiroad standing grain medical sci-tech Development Co., Ltd), concentration 20 μ mol/L, continuation effect 48h when adding dexamethasone.The collecting cell supernatant is with the content of chemoluminescence method survey steroid hormone testosterone.That measures the results are shown in Table 1.
Table 1
Result of the test shows: compare with group of solvents, model group cell testosterone levels obviously raises (P＜0.05), and after adding the intervention of medicine silibinin, testosterone levels obviously reduces (P＜0.05).The result of the test explanation, silibinin can reduce the intravital content of animal androgen, can be prepared into the androgen antagonist medicine.
17 α hydroxylases (CYP17) are the key enzymes in the androgen building-up process.Utilize polymerase chain reaction (RT-PCR) detect cultured cell CYP17 mRNA transcribe variation.The result shows: the expression of comparing CYP17mRNA in model group and the group of solvents increases to some extent, and the expression of CYP17mRNA descends after the intervention of Chinese medicine silibinin, has confirmed that further silibinin reduces androgenic effect.
Claims (3)
1. the purposes of silibinin in preparation antiandrogen medicine.
2. according to the described purposes of claim 1, it is characterized in that: described silibinin extracts from the seed of the pale reddish brown Herba Silybi mariani of feverfew (Herba Silybi) and obtains.
3. according to the described purposes of claim 1, it is characterized in that: described androgen is a testosterone.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010504678 CN101961329A (en) | 2010-10-08 | 2010-10-08 | Application of Silibinin in preparing anti-male hormone medicaments |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010504678 CN101961329A (en) | 2010-10-08 | 2010-10-08 | Application of Silibinin in preparing anti-male hormone medicaments |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101961329A true CN101961329A (en) | 2011-02-02 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201010504678 Pending CN101961329A (en) | 2010-10-08 | 2010-10-08 | Application of Silibinin in preparing anti-male hormone medicaments |
Country Status (1)
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| CN (1) | CN101961329A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1980668A (en) * | 2004-01-28 | 2007-06-13 | 安德鲁科技有限公司 | Enhancement of anti-androgenic activity by a combination of inhibitors targeting different steps of a steroid-dependent gene activation pathway and uses thereof |
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2010
- 2010-10-08 CN CN 201010504678 patent/CN101961329A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1980668A (en) * | 2004-01-28 | 2007-06-13 | 安德鲁科技有限公司 | Enhancement of anti-androgenic activity by a combination of inhibitors targeting different steps of a steroid-dependent gene activation pathway and uses thereof |
Non-Patent Citations (1)
| Title |
|---|
| 《国外医药·植物药分册》 20051231 张永忠 《水飞蓟宾可减量调节前列腺癌细胞LNCaP中Ets转录因子的表达》 127-128 1-3 第20卷, 第3期 2 * |
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Application publication date: 20110202 |