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Application of a class of fatty acid glycerides or plant extracts containing them in inhibiting aromatase activity

A technology of fatty acid glycerides and plant extracts, applied in the field of long-chain fatty acid glycerides or plant extracts containing them, to achieve the effect of inhibiting aromatase activity and preventing and treating benign prostatic hyperplasia

Active Publication Date: 2011-12-14
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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  • Application of a class of fatty acid glycerides or plant extracts containing them in inhibiting aromatase activity
  • Application of a class of fatty acid glycerides or plant extracts containing them in inhibiting aromatase activity
  • Application of a class of fatty acid glycerides or plant extracts containing them in inhibiting aromatase activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0027] Preparation of embodiment 11-glyceryl linolenate

[0028] 1) Supercritical extraction: 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 extracted at 40°C Still pressure 40MPa, 35 ℃ of separating kettle I temperature, 12MPa of pressure, 25 ℃ of separating kettle II temperature, 5MPa of pressure, be that 95v / v% ethanol is carried out supercritical carbon dioxide (45L / hour's) as entrainer with pollen weight 8% heavy concentration Circulation amount) was extracted for 2.0 hours to obtain a supercritical extraction part, and the supercritical extract was collected.

[0029] 2) Macroporous resin enrichment: use macroporous resin column chromatography (DA201 resin with 10 times the sample mass, Tianjin Huida Chemical Co., Ltd. or Anhui Sanxing Resin Technology Co., Ltd., 120cm*6cm column), supercritical extraction ...

Embodiment 21

[0032] Preparation of embodiment 21-glyceryl linolenate

[0033]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 corn pollen, filter, combine the filtrates, recover the solvent under reduced pressure, and 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.

[0034] 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 times the sample mass, 120cm*6cm column), use petroleum ether-ethyl acetate Carry out gradient elution, the gradient is volume ratio 10:1→8:...

Embodiment 31

[0036] Example 31, Preparation of 3-dipalmitic acid-2-linolenic acid glyceride and 1,3-dilinolenic acid-2-palmitic acid glyceride

[0037] 1) Extraction: take corn pollen after breaking the wall, pulverize it, heat and reflux three times with 95% ethanol aqueous solution with a volume ratio of 10ml / g corn pollen, filter, combine the filtrates, and recover the solvent under reduced pressure to obtain a relative density of 1.28 The liquid extract of the above-mentioned extract was distributed in water, and extracted with petroleum ether, chloroform and ethyl acetate in sequence, and the amount of each extraction solvent was equal to the volume of aqueous solution, and each solvent was extracted several times until it was almost colorless. The petroleum ether extraction part was taken, the solvent was recovered under reduced pressure, and the effective part was obtained by evaporating to dryness.

[0038] 2) Column chromatography: Mix the above-mentioned effective parts with sili...

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Abstract

The invention discloses the application of a class of fatty acid glycerides shown in formula 4 or plant extracts containing them in the preparation of preparations for inhibiting aromatase activity, and pharmaceutical compositions for preventing or treating benign prostatic hyperplasia, wherein R1, R2 and R3 is independently C16-C18 saturated or unsaturated aliphatic chain acyl or H, but not H at the same time. The application of the present invention opens up a new application field of the compound, and also provides a new approach for the prevention and treatment of diseases in the above fields. Formula 4

Description

technical field [0001] The invention relates to a new application of a class of long-chain fatty acid glycerides or plant extracts 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 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/26A61K31/232A61K36/31A61K36/899A61P13/08
Inventor 杨义芳李坤李永辉杨念云
Owner SHANGHAI INST OF PHARMA IND CO LTD
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