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Macrocyclic diterpene compounds in fruits of Euphorbia sororia, and preparation method and use thereof

A technology for spurge leaves and compounds, applied in the field of phytochemistry, and can solve problems such as insufficient depth

Active Publication Date: 2013-05-08
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

At present, the research on the chemical constituents of Euphorbia euphorbia is not deep enough, and its active constituents need to be further excavated to clarify the relationship between its pharmacological activity and active constituents

Method used

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  • Macrocyclic diterpene compounds in fruits of Euphorbia sororia, and preparation method and use thereof
  • Macrocyclic diterpene compounds in fruits of Euphorbia sororia, and preparation method and use thereof
  • Macrocyclic diterpene compounds in fruits of Euphorbia sororia, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Take 3Kg of the fruit of Euphorbia euphorbia, crush it, extract it by percolating with 30L of acetone at room temperature, and then evaporate the solvent to dryness in vacuo to obtain the crude extract of Euphorbia ipsifolia;

[0052] Disperse the crude extract with cyclohexane, extract with acetonitrile, and evaporate the acetonitrile to dryness in vacuo to obtain the extract of acetonitrile extract;

[0053] The extract was separated by silica gel column chromatography (chromatographic separation I), and petroleum ether-acetone

[0054] Gradient elution at 100:0-0:100, collected in fractions, detected and analyzed by silica gel thin layer, combined the same fractions, and recovered the solvent to obtain the target crude product A, which was separated by Sephadex LH-20 chromatographic column (chromatographic separation II), Use volume ratio dichloromethane: the mixed solvent of methanol=1:1 is eluent, elution obtains target crude product B, gets target crude product B,...

Embodiment 2

[0056] Take 3Kg of the fruit of Euphorbia euphorbia, after pulverization, use 30L concentration of 80% acetone aqueous solution to extract by percolation at room temperature, then vacuum evaporate the solvent to dryness, and obtain the crude extract of Euphorbia ipsifolia;

[0057] Disperse the crude extract with cyclohexane, extract with acetonitrile, and evaporate the acetonitrile to dryness in vacuo to obtain the extract of acetonitrile extract;

[0058] The extract was separated by silica gel column chromatography (chromatographic separation I), and petroleum ether-acetone

[0059] Gradient elution at 100:0-0:100, collected in fractions, detected and analyzed by silica gel thin layer, combined the same fractions, and recovered the solvent to obtain the target crude product A, which was separated by Sephadex LH-20 chromatographic column (chromatographic separation II), Use volume ratio dichloromethane: the mixed solvent of methanol=1:1 is that eluent elution obtains target ...

Embodiment 3

[0061] Take 3Kg of the fruit of Euphorbia euphorbia, crush it, extract it by percolation with 30L of methanol at room temperature, and then evaporate the solvent to dryness in vacuum to obtain the crude extract of Euphorbia ipsifolia;

[0062] Disperse the crude extract with a 50% methanol aqueous solution, extract with chloroform to obtain a chloroform extract, and evaporate the solvent to dryness in vacuo to obtain a chloroform extract;

[0063] The extract was separated by polyamide column chromatography (chromatographic separation Ⅰ), and methanol-water

[0064] Gradient elution at 0:100-100:0, collected in fractions, detected and analyzed by silica gel thin layer, combined the same fractions, and recovered the solvent to obtain the target crude product A, which was separated by Sephadex LH-20 chromatographic column (chromatographic separation II), Use volume ratio trichloromethane: the mixed solvent of methanol=1:1 is that eluent elution obtains target crude product B, ge...

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Abstract

The invention relates to macrocyclic diterpene compounds in fruits of Euphorbia sororia, and a preparation method and a use thereof. The preparation method comprises the following steps: extracting a raw material which is the fruits of Euphorbia sororia with a solvent at room temperature; and recovering the solvent, separating through a solvent extraction method, a silica gel column chromatography, a reversed phase column chromatography or a Sephadex LH-20 column chromatography, carrying out detecting analysis through adopting a thin-layer chromatography, mixing the obtained eluates, and drying the obtained eluate mixture to obtain six new macrocyclic diterpene compounds. The invention also relates to the use of the six new macrocyclic diterpene compounds in the preparation of drugs for reversing the multi-drug resistance activities.

Description

technical field [0001] The invention belongs to the field of phytochemistry, specifically to the field of extraction, separation and preparation of active ingredients of traditional Chinese medicines, and in particular to the extraction and separation of six new macrocyclic diterpenoids with pharmacological activity from the fruit of Euphorbia opposite leaves. Background technique [0002] Euphorbia (Etphorbiasororria) is a plant of the genus Euphorbiaceae. Euphorbia is a commonly used medicinal material in Uighur medicine in my country. It has the functions of dispelling cold, unblocking stagnation, drying dampness and appetizing, strengthening the brain and improving intelligence. Clinically, it has been used for a long time to treat abdominal distension, weak stomach, lack of food and forgetfulness, poor speech, limb paralysis, skin diseases and other diseases. There are more than a dozen mature Uyghur medicines such as Suzi Afu Tablets, Compound Suzi Afu Honey Ointment,...

Claims

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Application Information

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IPC IPC(8): C07C69/013C07C67/48A61K31/22A61P43/00
Inventor 阿吉艾克拜尔·艾萨陆东礼
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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