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A polyhydroxy long-chain fatty acid, its separation and extraction method and its application in inhibiting aromatase activity

A long-chain fatty acid and polyhydroxyl technology, which is applied in the separation/purification of carboxylic acid compounds, organic active ingredients, medical preparations containing active ingredients, etc., to achieve strong aromatase inhibitory activity

Active Publication Date: 2012-02-01
SHANGHAI INST OF PHARMA IND 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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  • A polyhydroxy long-chain fatty acid, its separation and extraction method and its application in inhibiting aromatase activity
  • A polyhydroxy long-chain fatty acid, its separation and extraction method and its application in inhibiting aromatase activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 The preparation of 10,11,12-trihydroxyheptadecadienoic acid

[0040] 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.

[0041] 2) Macroporous resin enrichment: steam the extract obtained in step 1 until it has no alcohol smell, and mix the sample in a way similar to the traditional silica gel column dry method, that is, take 20-60% of the column volum...

Embodiment 2

[0044] Example 2 Preparation of 10,11,12-trihydroxyheptadecadienoic acid

[0045] 1) Extraction: take rapeseed pollen after breaking the wall, pulverize, add 10ml / g rapeseed pollen, heat reflux or cold soak and percolate 3 times with 95% ethanol by volume, filter, combine filtrates, recover solvent under reduced pressure, and obtain relative Fluid extract with a density of 1.28. Distributed in water, extracted successively with petroleum ether, chloroform and ethyl acetate, the amount of each extraction solvent is equal to the volume of aqueous solution, and each solvent is extracted several times until it is almost colorless. The ethyl acetate extraction part was taken, the solvent was recovered under reduced pressure, and the effective part was obtained by evaporating to dryness.

[0046] 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 with ten times the samp...

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Abstract

The invention discloses a polyhydroxy long-chain fatty acid, namely the compound 10,11,12-trihydroxy heptadecadienoic acid shown in formula 1, and its separation and extraction method. The compound of the present invention has not been reported, and it has strong aromatase inhibitory activity. The invention also discloses the application of the polyhydroxy long-chain fatty acid or the plant extract containing it in the preparation of preparations for inhibiting aromatase activity and in the preparation of pharmaceutical compositions for preventing and treating prostatic hyperplasia. Formula 1

Description

technical field [0001] The present invention relates to a new compound and its separation and extraction method and application, in particular to a new polyhydroxy long-chain fatty acid and its separation and extraction method and application. 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C51/42C07C59/42A61K31/202A61P13/08A61K36/31
Inventor 杨义芳李永辉李坤杨念云
Owner SHANGHAI INST OF PHARMA IND CO LTD
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