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A kind of medicine for treating cardiovascular and cerebrovascular diseases and its preparation method and application

A compound, genistein technology, applied in the field of medicinal chemistry, can solve the problem of no other activity or efficacy, and achieve the effect of enhancing hypoxia resistance

Active Publication Date: 2021-03-26
SICHUAN ACAD OF CHINESE MEDICINE SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, only 6-hydroxygenistein has hepatoprotective activity in the reports of its pharmacological activity, and there are no reports of other activities or efficacy

Method used

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  • A kind of medicine for treating cardiovascular and cerebrovascular diseases and its preparation method and application
  • A kind of medicine for treating cardiovascular and cerebrovascular diseases and its preparation method and application
  • A kind of medicine for treating cardiovascular and cerebrovascular diseases and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Preparation of 6-hydroxygenistein by Shegan aglycon

[0026] Add Shegan aglycon into the reaction kettle, then add 5 times the amount (ml / g) of 95% ethanol (V / W), stir with a mixer and heat to reflux, and then add 3 times the amount (ml / g) after the Shegan aglycon is completely dissolved. g) Hydroiodic acid (content ≥ 45% V / W), stirred, heated to reflux for 5 to 24 hours, using silica gel GF 254 TLC inspection to determine the end point of the reaction (developing solvent is chloroform: methanol: formic acid 10:1:0.1). Release the reaction solution, leave it at room temperature overnight, and precipitate pale yellow needle-like crystals, filter and wash with water until neutral to obtain crude 6-hydroxygenistein; use recrystallization to obtain refined 6-hydroxygenistein with a yield of 85%.

[0027] The product obtained in this embodiment is pale yellow needle crystal; odorless and tasteless. Soluble in methanol, ethanol, almost insoluble in water. Melting...

Embodiment 2

[0030] Example 2 Preparation of 6-hydroxygenistein by Sheganoside

[0031] Put Shegan glycosides into the reaction kettle, add 5 times the amount (ml / g) of 95% ethanol (V / W), stir with a mixer and heat to reflux, and then add 3 times the amount (ml / g) when it becomes a uniform paste Hydroiodic acid (content ≥ 45%) (V / W), stirred, heated to reflux for 5 to 24 hours, using silica gel GF 254 Thin-layer chromatography inspection to determine the reaction end point (developing solvent is chloroform: methanol: formic acid 10:1:0.1), release the reaction solution, leave it at room temperature overnight, precipitate off-white precipitate, filter, wash with water until neutral, and obtain 6-hydroxy dye Crude lignin; 6-hydroxygenistein was obtained by recrystallization method, with a yield of 70%.

[0032] The chemical reaction equation is as follows:

[0033]

Embodiment 3

[0034] Example 3 Preparation of 6-hydroxygenistein from puereticin

[0035] Put puerarin into the reaction kettle, then add 5 times the amount (ml / g) of 95% ethanol (V / W), stir with a mixer and heat to reflux, and then add 3 times the amount ( ml / g) of hydroiodic acid (content ≥ 45%) (V / W), stir, heat and reflux for 5 to 24 hours, use silica gel GF 254 Thin-layer chromatography was used to determine the end point of the reaction (the developer was chloroform:methanol:formic acid 10:1:0.1), the reaction liquid was released, and left overnight at room temperature, and light yellow needle-like crystals were precipitated, filtered, washed with water until neutral, and 6 -Crude hydroxygenistein; 6-hydroxygenistein was obtained by recrystallization method, with a yield of 80%.

[0036] The chemical reaction equation is as follows:

[0037]

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Abstract

The invention discloses a medicine for treating cardiovascular and cerebrovascular diseases, a preparation method and application thereof, and belongs to the field of medicinal chemistry. The medicine of the present invention is a preparation prepared by taking 6-hydroxygenistein as an active ingredient and adding pharmaceutically acceptable auxiliary materials or auxiliary ingredients. The present invention also discloses a preparation method and application of 6-hydroxygenistein. The 6-hydroxygenistein prepared by using shegan aglycon, sheganin, puereticin and pueretin has pharmacological activity, that is, it has The obvious effect of anti-hypoxia and inhibition of tumor cell proliferation can significantly enhance the body's ability to withstand hypoxia, and at the same time have a significant inhibitory effect on cancer cell proliferation, so 6-hydroxygenistein can be used to prepare and treat cardiovascular and cerebrovascular diseases , vascular dementia, certain tumor drugs, especially can be prepared into preparations such as injections, tablets, capsules, dropping pills or oral solutions to make it more widely used.

Description

technical field [0001] The invention relates to a medicine for treating cardiovascular and cerebrovascular diseases, a preparation method and an application thereof, and belongs to the field of medicinal chemistry. Background technique [0002] 6-Hydroxygenistein, molecular formula C 15 h 10 o 6 , the chemical name is 5,6,7,4'-tetrahydroxyisoflavone or 5,6,7-trihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one, Its structural formula is [0003] [0004] There are few studies on 6-hydroxygenistein. At present, it is mainly considered to be a bacterial metabolite, which is mainly obtained by isolating from bacterial metabolites. Currently, only 6-hydroxygenistein has hepatoprotective activity, and no other activity or efficacy has been reported on its pharmacological activity. Contents of the invention [0005] In order to solve the above problems, the present invention provides a preparation method and application of 6-hydroxygenistein. [0006] The invention disc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352C07D311/36A61P25/28A61P35/00A61P9/00
CPCA61K31/352C07D311/36
Inventor 袁崇均谭正怀陈帅罗霞罗森余梦瑶王笳陈雏熊静悦
Owner SICHUAN ACAD OF CHINESE MEDICINE SCI
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