Application of long-chain fatty acid derivative or plant extracts containing same in inhibiting the activity of aromatizing enzyme

A technology for aromatase activity and long-chain fatty acids, which is applied in the application field of a class of long-chain fatty acid derivatives or plant extracts containing them in inhibiting aromatase activity, so as to inhibit aromatase activity and prevent and treat benign prostatic hyperplasia effect of disease

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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  • Application of long-chain fatty acid derivative or plant extracts containing same in inhibiting the activity of aromatizing enzyme
  • Application of long-chain fatty acid derivative or plant extracts containing same in inhibiting the activity of aromatizing enzyme
  • Application of long-chain fatty acid derivative or plant extracts containing same in inhibiting the activity of aromatizing enzyme

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The preparation of embodiment 1N-(2-hydroxyethyl) linolenamide, dihydroxy octadecadienoic acid, linolenic acid fructoside and palmitic acid sorbitol ester

[0032] 1) Supercritical extraction: commercially available rape pollen (produced by Baikang Bee Industry, Xuancheng City, Anhui Province) was dried under reduced pressure at 60°C for 24 hours, and then the dried pollen was dried at 40°C and the pressure of the extraction kettle was 40MPa. Separation kettle I temperature 35 ℃, pressure 12MPa, separation kettle II temperature 25 ℃, pressure 5MPa, the weight concentration of pollen weight 8% is 95v / v% ethanol as entrainer to carry out supercritical carbon dioxide (45L / hour circulation consumption) extraction After 2.0 hours, the supercritical extraction fraction was obtained, and the supercritical extract was collected.

[0033] 2) Macroporous resin enrichment: use macroporous resin column chromatography (DA201 resin with 10 times the sample mass, Tianjin Huida Chemic...

Embodiment 2

[0037] The preparation of embodiment 2N-(2-hydroxyethyl) linolenamide, 1-linolenic acid glyceride, dihydroxy octadecadienoic acid, linolenic acid fructoside and palmitic acid sorbitol ester

[0038] 1) Extraction: take rapeseed pollen after breaking the wall, pulverize, heat and reflux 3 times with 95% ethanol aqueous solution with a volume concentration of 10ml / g rapeseed pollen, filter, combine the filtrates, and recover the solvent under reduced pressure to obtain a relative density of 1.28 The liquid extract is dissolved in water at the ratio of 2ml water / g liquid extract, and is extracted successively with sherwood oil, chloroform and ethyl acetate. colorless. Take the ethyl acetate extraction part, recover the solvent under reduced pressure, and evaporate to dryness to obtain the effective part.

[0039] 2) Column chromatography: Mix the above-mentioned effective parts with silica gel on the column, perform silica gel (300-400 mesh) column chromatography (silica gel 10 ...

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Abstract

The invention discloses an application of a long-chain fatty acid derivative shown as formula 5 or plant extracts containing the same in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent or treat prostatoplasia diseases. The application opens up a new application field for the compound and also provides a new way for preventing and treating the diseases in the field.

Description

technical field [0001] The invention relates to a new application of a class of long-chain fatty acid derivatives or plant extracts thereof. 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 acceleration of population aging in my country, the incidence of benign prostatic hyperplasia caused by old age continues to rise, and benign prostatic hyperplasia has become ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/164A61K31/232A61K31/7028A61K36/31A61P13/08
Inventor 杨义芳李坤李永辉杨念云
Owner JIANGSU KANION PHARMA CO LTD
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