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Extraction and separation method of macrocyclic diterpenoid components in Euphorbia sororia A.Schrenk fruits and application thereof

A technology for spurge leaf and compounds, applied in the field of medicine, can solve the problems of weak reversal activity and high toxicity

Active Publication Date: 2021-06-01
XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There have been three generations of multidrug resistance reversal drugs, but weak reversal activity and high toxicity are the reasons why they have not been widely used

Method used

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  • Extraction and separation method of macrocyclic diterpenoid components in Euphorbia sororia A.Schrenk fruits and application thereof
  • Extraction and separation method of macrocyclic diterpenoid components in Euphorbia sororia A.Schrenk fruits and application thereof
  • Extraction and separation method of macrocyclic diterpenoid components in Euphorbia sororia A.Schrenk fruits and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021]a. Take 10kg of Euphorbia euphorbiae fruit that is naturally dried, crush it, and use 45L of 90% ethanol-water solution to extract it by percolation at room temperature, evaporate the solvent under reduced pressure, and obtain the fruit extract of Euphorbia euphorbia ipsifolia;

[0022] b. Disperse the extract obtained in step a with 6 times the volume of water, add 5 times the volume of ethyl acetate to extract 5 times, stir with a paddle stirrer for 5 minutes each time, let stand for 15 minutes to separate layers, and combine ethyl acetate layer, and concentrated under reduced pressure to obtain ethyl acetate extract extract;

[0023] c. disperse the ethyl acetate extract obtained in step b with 50% methanol at a concentration of 5 times the volume, add 5 times the volume of petroleum ether to extract 5 times, stir with a paddle stirrer for 5 minutes each time, and stand for 20 minutes Layer, combined 50% methanol layer, and concentrated under reduced pressure to obtai...

Embodiment 2

[0026] a. Take 10kg of Euphorbia euphorbia fruit that is naturally dried, crush it, and use 40L of absolute ethanol solution to extract it by cold soaking at room temperature for 4 times, combine the extracts, evaporate the solvent under reduced pressure, and obtain the fruit extraction of Euphorbia euphorbia thing;

[0027] b. disperse the extract obtained in step a with 5 times the volume of water, add 5 times the volume of n-hexane and ethyl acetate mixed solvent to extract 5 times, stir with a paddle stirrer for 5 minutes each time, and let stand for 10 minutes layer, combined n-hexane and ethyl acetate mixed solvent layer, and concentrated under reduced pressure to obtain n-hexane and ethyl acetate mixed solvent extract extract;

[0028] c. Disperse the mixed solvent extract of n-hexane and ethyl acetate obtained in step b with 5 times the volume of acetonitrile, add 5 times the volume of cyclohexane to extract 8 times, stir with a paddle stirrer for 5 minutes each time, ...

Embodiment 3

[0031] a. Take 10kg of Euphorbia euphorbia fruit that is naturally dried, heat and extract it with 70L of acetone for 12h after crushing, combine the extracts, concentrate the solvent under reduced pressure, and obtain the fruit extract of Euphorbia ipsifolia;

[0032] b. disperse the extract obtained in step a with 10 times the volume of water, add 5 times the volume of n-hexane to extract 10 times, stir with a paddle stirrer for 10 minutes each time, leave to stand for 30 minutes to separate layers, and combine the n-hexane layers, And concentrated under reduced pressure to obtain n-hexane extract extract;

[0033] c. Disperse the n-hexane extract extract obtained in step b with 10 times the volume of acetonitrile, add 5 times the volume of petroleum ether to extract 10 times, stir with a paddle stirrer for 5 minutes each time, let stand for 20 minutes to separate layers, and combine The acetonitrile layer was concentrated under reduced pressure to obtain the acetonitrile ex...

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Abstract

The invention relates to an extraction and separation method of macrocyclic diterpenoid components in Euphorbia sororia A.Schrenk fruits and an application thereof, ripe fruits of Euphorbia sororia A.Schrenk are used as raw materials, solvent extraction, solvent extraction and silica gel column chromatography are adopted for separation to obtain macrocyclic diterpenoid components 1-8, and through high performance liquid chromatography, the content of the macrocyclic diterpenoid compound in the component is more than 60%. The activity tests on the components 1-8 show strong multidrug resistance reversal activity, can reverse drug resistance of drug-resistant cells to antitumor drugs to a certain extent when being combined with the antitumor drugs, and can be used as multidrug resistance reversal drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for extracting and separating components of macrocyclic diterpenoids and its use in the preparation of multidrug resistance reversal drugs or in combination with antitumor drugs. Background technique [0002] Euphorbia sororia A.Schrenk (Euphorbia sororia A.Schrenk) is an annual herb of the genus Euphorbia (Euphorbiaceae) in the family Euphorbiaceae. Commonly used medicinal materials in Uyghur ethnic medicine. The plant is matured in more than a dozen kinds of Suzi Afu Tablets, Compound Suzi Afu Honey Ointment, Gavari Xikumeni, Yili Titi Honey Ointment, Suzi Afu Ointment, Suzafu Powder, Sairanisan, etc. It is used as the main ingredient in the national medicine compound medicine for clinical application. At present, the types of compounds isolated and identified from this plant mainly include sesquiterpenes, diterpenes, triterpenes, sterols, fatty acids, flavonoids, p...

Claims

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Application Information

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IPC IPC(8): C07C69/21C07C69/78C07C67/48C07D213/80C07D213/803C07D333/38C07D307/68C07C303/44C07C309/30A61P35/00
CPCC07C67/48C07D213/80C07D213/803C07D333/38C07D307/68C07C303/44A61P35/00C07C69/21C07C69/78C07C309/30
Inventor 阿吉艾克拜尔·艾萨杨贺群阿依提拉·麦麦提江汤丹茹仙古丽·肉孜买买提
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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