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Drug for treating cardiovascular and cerebrovascular diseases, preparation method and application of drug

A technology for cardiovascular and cerebrovascular diseases and drugs, applied in cardiovascular system diseases, drug combinations, pharmaceutical formulations, etc., can solve the problem of no other activity or efficacy, and achieve the effect of enhancing hypoxia tolerance

Active Publication Date: 2017-12-08
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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  • Drug for treating cardiovascular and cerebrovascular diseases, preparation method and application of drug
  • Drug for treating cardiovascular and cerebrovascular diseases, preparation method and application of drug
  • Drug for treating cardiovascular and cerebrovascular diseases, preparation method and application of drug

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 drug for treating cardiovascular and cerebrovascular diseases, a preparation method and application of the drug, belonging to the field of medicinal chemistry. The drug is prepared by taking 6-hydroxy genistein as an active ingredient, and adding pharmaceutically acceptable auxiliary materials or auxiliary ingredients. The invention also discloses a preparation method and application of 6-hydroxy genistein. The 6-hydroxy genistein is prepared by utilizing tectoridin genin, tectoridin, kakkalide genin and kakkalide, has pharmacological activity, namely has the effects of obvious anoxia resistance and inhibition of tumor cell proliferation, can be used for reinforcing the anti-anoxia capability of a body and meanwhile has obvious inhibition effect on tumor cells proliferation, so that the 6-hydroxy genistein can be used for preparing drugs for treating cardiovascular and cerebrovascular diseases, vascular dementia and some tumors, and especially can be prepared into injection, tablets, capsules, drop pills or oral solution and other preparations, thus having wide application range.

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 Applications(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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