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Application of hederagenin derivative in preparation of medicine for resisting myocardial hypoxia-reoxygenation injury

A technology of hederagenin and myocardial hypoxia, which is applied in the directions of drug combination, steroids, cardiovascular system diseases, etc. Effects of survival rate, improved solubility, decreased MDA content

Active Publication Date: 2020-06-26
JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Before the completion of the present invention, there were no reports in the literature that the derivatives of helexin of the present invention had anti-myocardial ischemia, nor did they find that the derivatives of helexin of the present invention were used in the preparation of drugs for myocardial ischemia-reperfusion injury application reports

Method used

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  • Application of hederagenin derivative in preparation of medicine for resisting myocardial hypoxia-reoxygenation injury
  • Application of hederagenin derivative in preparation of medicine for resisting myocardial hypoxia-reoxygenation injury
  • Application of hederagenin derivative in preparation of medicine for resisting myocardial hypoxia-reoxygenation injury

Examples

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example 1

[0057] The preparation of example 1 helexin

[0058] Take 1 kg of Dipsacus medicinal material, add 30 g of calcium oxide, and extract 3 times with 8 times the amount of 60% ethanol under reflux, each time for 2 hours. Combine the extracts three times, filter, and recover the ethanol from the filtrate until it has no alcohol smell, add water to 3000ml, pass through the treated macroporous resin column, and first elute with 20% ethanol containing sodium hydroxide (pH value 13) for 3 times column volume, then eluted with water to neutrality, and finally eluted with 70% ethanol for 4 times the column volume, collected the eluate, and concentrated to dryness under reduced pressure; hydrolyzed 3 times with 2N hydrochloric acid containing 40% ethanol solution Hour. Filtrate, discard the hydrolyzate, wash the filter cake with deionized water until it is neutral; then heat it to boiling with 95% ethanol, add 2% medicinal activated carbon of the volume of the liquid medicine, filter ...

example 43

[0063] Example 4 3β, 23-dihydroxyoleanane-12-ene-28 hydroxy acid-2-[4-(2-formylpyridine)-piperazinyl]-B Preparation of esters

[0064] Weigh 1.000 mmol compound 3β, 23-dihydroxyoleanane-12-ene-28 hydroxy acid-2-[4-(2-formylpyridine)-piperazinyl]-ethyl ester, dissolve with 50 mL dichloromethane , add 1.5mmol of 2-pyridinecarboxylic acid, then add 1.5mmol EDC·HCL, 1.5mmol HOBT successively, react at room temperature for 6h, after the reaction is complete, dilute the reaction solution with dichloromethane, wash the dichloromethane solution three times with water and saturated saline , 50 mL each time, dehydrated with anhydrous sodium sulfate, filtered, dried, separated on a silica gel column (chloroform:methanol=30:1), collected the same components, recovered the solvent, dried, and obtained.

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Abstract

The invention relates to the technical field of medicines, in particular to application of a hederagenin derivative in preparation of a hypoxia-reoxygenation injury medicine for myocardial ischemia and reperfusion injury prevention. The compound is stable in a solution; the compound has obvious protective activity against myocardial hypoxia-reoxygenation injury, especially the hypoxia-reoxygenation injury of myocardial ischemia and reperfusion injuries; the myocardium can be well protected from hypoxia-reoxygenation injury when the concentration is 80 micromole / L, and the derivative has stronger pharmacological activity than the parent nucleus hederagenin under the same dosage, so that a new choice is provided for protection against myocardial hypoxia-reoxygenation injury and myocardial ischemia-reperfusion injury.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to the application of a hedera saponin derivative in the preparation of anti-myocardial hypoxia-reoxygenation injury drugs. Background technique [0002] Cardiovascular disease is a family of diseases that involve the circulatory system. Coronary heart disease, heart failure, and acute myocardial infarction are common cardiovascular diseases, and their pathogenic mechanisms are all related to myocardial cell damage caused by myocardial ischemia-reperfusion. Studies have pointed out that the pathogenesis of cardiovascular diseases is complex, and the drugs that have been marketed for treating cardiovascular diseases have the disadvantages of weak activity, low selectivity, and large side effects, which make them have certain limitations and cannot fundamentally control the disease. Drugs for the treatment of myocardial ischemia-reperfusion injury are well known in existing st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61P9/10A61P9/00
CPCC07J63/008A61P9/10A61P9/00
Inventor 南敏伦杨振刘建璇赫玉芳白雪赵全成
Owner JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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