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Pharmaceutical composition for restraining activity of aromatizing enzyme and application thereof

A technology of aromatase activity and compound, which is applied in the direction of drug combination, organic active ingredient, anhydride/acid/halide active ingredient, etc., can solve the problem of low drug efficacy and achieve the effect of efficiently inhibiting aromatase activity

Active Publication Date: 2012-01-11
JIANGSU KANION PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported in the literature that flavonoids, fatty acid compounds, coumarin compounds and terpenoids all have aromatase inhibitory activity, and are used as active ingredients in pharmaceutical compositions for inhibiting aromatase activity separately, However, the efficacy of these pharmaceutical compositions is low

Method used

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  • Pharmaceutical composition for restraining activity of aromatizing enzyme and application thereof
  • Pharmaceutical composition for restraining activity of aromatizing enzyme and application thereof
  • Pharmaceutical composition for restraining activity of aromatizing enzyme and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Commercially available rapeseed broken wall pollen (produced by Baikang Bee Industry in Xuancheng City, Anhui Province) was dried under reduced pressure at 60°C for 24 hours, then the dried broken wall pollen was dried at 40°C, the pressure of the extraction kettle was 40MPa, and the temperature of the separation kettle 1 was 35°C. , pressure 12MPa, separation kettle II temperature 25 ℃, pressure 5MPa, with pollen weight 8% heavy concentration being 95v / v% ethanol as entrainer to carry out supercritical carbon dioxide (45L / hour circulation consumption) extraction 2.0 hours, obtain supercritical Extract the fraction and collect the supercritical extract.

[0025] Steam the obtained supercritical extract until it has no alcohol smell, take a macroporous resin with a packing volume of 20-60% (v / v) and stir it evenly with the extract to make it fully adsorbed, and mix the macroporous resin Load the top of the macroporous resin column, wherein the macroporous resin is selec...

Embodiment 2

[0031] Kaempferol, quercetin, isorhamnetin, apigenin, caprylic acid, palmitic acid, dihydroxylinoleic acid, cis-15-tetracosenoic acid, linolenic acid amide ester, Glyceryl linolenate and sterol linolenate were mixed according to the components and contents described in Table 1 to obtain pharmaceutical compositions F, G, H and I of the present invention.

[0032] Table 1. Components of pharmaceutical compositions F, G and H of the present invention

[0033]

[0034] The beneficial effects of the present invention will be further illustrated below through effect examples.

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PUM

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Abstract

The invention discloses a pharmaceutical composition for restraining the activity of aromatizing enzyme, containing a flavone compound and a fatty acid compound. The flavone compound refers to a compound of formula I, wherein a substituent R1 is selected from H or OH, and a substituent R2 is selected from H, OH or OCH3; the fatty acid compound refers to a compound with a molecular formula of CH3-CnHm-COB, wherein n is greater than 8 and less than 24, m is greater than or equal to 2n-8 and less than or equal to 2n, and B is a hydroxyl, an N-hydroxyethyl, a fructosyl or a glyceryl. The pharmaceutical composition can effectively restrain the activity of the aromatizing enzyme and can be used for preparing medicaments for treating or preventing estrogen dependent diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical compositions, in particular to a pharmaceutical composition for inhibiting the activity of aromatase and its application. Background technique [0002] Estrogen is an important class of sex hormones, which are closely related to many physiological and pathological processes in the body. The estrogen in postmenopausal women and men is mainly transformed from androgen precursors secreted by the adrenal glands, and the transformation sites occur in adipose tissue, liver, kidney, etc., through paracrine and / or autocrine methods, mainly in Work locally. Aromatase P450 is the key enzyme and rate-limiting enzyme in this conversion process, and plays an important role in various physiological and pathological processes, thus becoming an important target for the prevention and treatment of estrogen-dependent diseases. [0003] Flavonoids and fatty acid compounds widely exist in nature and have various physi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/19A61K31/20A61P35/00A61P5/30
Inventor 杨义芳李永辉李坤杨念云
Owner JIANGSU KANION PHARMA CO LTD