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Two sterol derivatives, separation and extraction method thereof and application thereof in preventing and treating prostatoplasia diseases

An extraction method, a technology of methylene cholesterol, applied in two kinds of sterol derivatives and their separation and extraction, and the application field in the prevention and treatment of benign prostatic hyperplasia

Active Publication Date: 2009-11-04
JIANGSU KANION PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are not many clinical reports on the treatment of BPH with aromatase, and its efficacy needs further verification

Method used

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  • Two sterol derivatives, separation and extraction method thereof and application thereof in preventing and treating prostatoplasia diseases
  • Two sterol derivatives, separation and extraction method thereof and application thereof in preventing and treating prostatoplasia diseases

Examples

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Embodiment 1

[0033] 1) Supercritical extraction: take the broken corn pollen, extract it with supercritical carbon dioxide, and collect the supercritical extracted part. According to the present invention, the temperature of the supercritical carbon dioxide extraction is preferably at 50°C, the pressure is 40MP, and the extraction is performed twice, each time for 30min, CO 2 The flow rate is 30L / min. The entraining agent is ethanol, and its dosage is 8% of the weight of the broken pollen;

[0034] 2) Column chromatography: The above extract is subjected to silica gel column chromatography, the silica gel is 100 mesh, the dosage is 20 times the mass of the crude product, and the specification is 100mm×1000mm; gradient elution is carried out with the eluent, the eluent Petroleum ether-ethyl acetate, the amount of each gradient eluent is 5 times the column volume, the eluent volume ratio is: 100:0, 100:1, 100:5, 100:20; Chromatographic detection, when the developer is petroleum ether-chloro...

Embodiment 2

[0037] 1) Extraction: take corn pollen after breaking the wall, pulverize it, use 95% (volume percentage) ethanol to reflux or cold soak and percolate 3 times with the ratio of 10ml / g corn pollen, filter, combine the filtrates, and recover the solvent under reduced pressure. Obtain liquid extract; Suspend in water, the consumption of water is 5ml / g liquid extract; Use sherwood oil, chloroform and ethyl acetate extraction respectively, every kind of solvent extracts 3 times, and each extraction solvent consumption is the equal volume of aqueous solution, Take the ethyl acetate extraction part, recover the solvent under reduced pressure, and obtain the effective part;

[0038] 2) Column chromatography: perform silica gel column chromatography on the above-mentioned effective parts, the silica gel is 200 mesh, the dosage is 5 times the mass of the crude product, and the specification is 100mm×1000mm; gradient elution is carried out with the eluent, and the eluent Petroleum ether-...

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Abstract

The invention discloses two sterol derivatives, a separation and extraction method thereof and an application thereof in preventing and treating prostatoplasia diseases. The two sterol derivatives are compounds 24-methylene cholesterol linoleate and cycloeucalenol linoleate shown as formula 1 and formula 2. The compounds which are not reported have the function of inhibiting the activity of aromatizing enzyme. The invention also discloses an application of the two sterol derivatives in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent or treat prostatoplasia diseases.

Description

technical field [0001] The present invention relates to two new compounds, their preparation method and application, and the pharmaceutical composition containing them, in particular to two sterol derivatives, their preparation methods and applications, and their pharmaceutical compositions containing them. Background technique [0002] Benign prostatic hyperplasia (BPH) is a common physiological lesion in elderly men. When the lesion causes a series of symptoms such as urinary obstruction, it is called benign prostatic hyperplasia. Autopsy reports of 1075 cases abroad showed that: at the age of 25 to 30, 10% of men could see early benign prostatic hyperplasia lesions under the microscope; as the age increases, the incidence of benign prostatic hyperplasia diagnosed by histology also increases accordingly; By the age of 51 to 60, the incidence rate increases to 75%; by the age of 85, about 90% of men have histological BPH. It can be seen from the above that with the acceler...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00C07J53/00A61K31/575A61K36/899A61P13/08
Inventor 杨义芳李永辉李坤杨念云
Owner JIANGSU KANION PHARMA CO LTD
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