Macrocyclic diterpene compounds in fruit of euphorbia sororia A. schrenk as well as preparation method of macrocyclic diterpene compounds and use of macrocyclic diterpene compounds in reversion of multidrug resistance

A technique for treating spurge, compounds, applied in the field of medicine, can solve the problems of drug resistance, increased drug efflux, etc.

Active Publication Date: 2018-03-23
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 are many mechanisms for the formation of MDR, one of the most important mechanisms is the overexpression of ABC family transporters (currently the most widely and deeply studied P-glycoprotein encoded by the ABCB1 gene, P-gp), leading to drug efflux increase in drug resistance

Method used

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  • Macrocyclic diterpene compounds in fruit of euphorbia sororia A. schrenk as well as preparation method of macrocyclic diterpene compounds and use of macrocyclic diterpene compounds in reversion of multidrug resistance
  • Macrocyclic diterpene compounds in fruit of euphorbia sororia A. schrenk as well as preparation method of macrocyclic diterpene compounds and use of macrocyclic diterpene compounds in reversion of multidrug resistance
  • Macrocyclic diterpene compounds in fruit of euphorbia sororia A. schrenk as well as preparation method of macrocyclic diterpene compounds and use of macrocyclic diterpene compounds in reversion of multidrug resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] a. Take 10 kg of the fruit of Euphorbia euphorbia, crush it, and use 50 L of 50% ethanol-water solution to extract it by cold soaking at room temperature, and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia ipsifolia;

[0037] b. Disperse the crude extract obtained in step a with ethanol, add petroleum ether for extraction, combine the ethanol layers and evaporate to dryness under reduced pressure to obtain the ethanol extract extract;

[0038] c, the ethanol extract extract obtained in step b is separated with a normal phase silica gel column, and gradient elution is carried out with petroleum ether-ethyl acetate with a volume ratio of 10:1-0:1, and the fraction is subjected to silica gel thin layer chromatography ( TLC) analysis, the same fractions were combined to obtain 6 fractions (F1-F6); fraction F4 was subjected to normal-phase silica gel column separation, and gradient elution was carried out with chloroform-aceto...

Embodiment 2

[0040] a. Take 10 kg of the fruit of Euphorbia euphorbia, crush it, and use 60 L of 99% ethanol-water solution to reflux extract at a temperature of 80° C., and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia ipsifolia;

[0041] b. Disperse the crude extract obtained in step a with ethanol, add n-hexane for extraction, combine the ethanol layers and evaporate to dryness under reduced pressure to obtain the ethanol extract extract;

[0042] c, the ethanol extract extract obtained in step b is separated with a normal phase silica gel column, and gradient elution is carried out with n-hexane-ethyl acetate with a volume ratio of 10:1-0:1, and the fraction is subjected to silica gel thin layer chromatography ( TLC) analysis, the same fractions were combined to obtain 6 fractions (F1-F6); fraction F4 was subjected to normal phase silica gel column separation, and gradient elution was carried out with chloroform-methanol with a volume r...

Embodiment 3

[0044] a. Get 10kg of the fruit of Euphorbia euphorbia, crush it and extract it by cold soaking at room temperature with 70L of dehydrated ethanol, and evaporate the solvent under reduced pressure to obtain the crude extract of Euphorbia ipsifolia;

[0045] b. Disperse the crude extract obtained in step a with ethanol, add cyclohexane for extraction, combine the ethanol layers and evaporate to dryness under reduced pressure to obtain the ethanol extract extract;

[0046] c. Separate the ethanol extract extract obtained in step b with a normal-phase silica gel column, carry out gradient elution with cyclohexane-ethyl acetate with a volume ratio of 10:1-0:1, and fractionate through silica gel thin-layer chromatography (TLC) analysis, the same fractions were combined to obtain 6 components (F1-F6); the component F4 was subjected to normal phase silica gel column separation, and the volume ratio was 100:0-0:100 with dichloromethane-acetone Gradient elution to obtain components F4A...

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Abstract

The invention relates to macrocyclic diterpene compounds in fruit of euphorbia sororia A. schrenk as well as a preparation method of the macrocyclic diterpene compounds and use of the macrocyclic diterpene compounds in reversion of multidrug resistance. Three new macrocyclic diterpene compounds are separated from the fruit of the euphorbia sororia A. schrenk, and are then subjected to determination of activity of the reversion of multidrug resistance; a result proves that the macrocyclic diterpene compounds (I)-(III) have different levels of the activity of the reversion of multidrug resistance, can reverse the drug resistance of drug-resistant cells to anticancer drugs to varying degrees when being combined with the anticancer drugs for use, and can be used for preparing drugs with the reversion of multidrug resistance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to three new macrocyclic diterpenoids and their use in the preparation of multidrug resistance reversal medicines or combined medicines with antineoplastic medicines. Background technique [0002] Euphorbia sororia A.Schrenk is an annual herbaceous plant belonging to the genus Euphorbia of the Euphorbia family (Euphorbiaceae). It is native to Central Asia and is now mainly distributed in Central Asia and Hotan, Xinjiang. At present, a total of 57 compounds have been isolated from Euphorbia opposite, including flavonoids and their glycosides, sterols, coumarins, macrocyclic diterpenes, triterpenes, pyrimidines, adenosine, sphingolipids, ellagic acid, etc. At present, there are 17 macrocyclic diterpenoids isolated from Euphorbia spp., all of which are pseudolemane-type macrocyclic diterpenes, and some of them have certain anti-tumor multidrug resistance reversing activity. [0003] ...

Claims

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Application Information

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IPC IPC(8): C07C69/18C07C69/33C07C67/48C07C67/56C07C67/58A61P35/00
CPCC07C69/18C07C69/33
Inventor 阿吉艾克拜尔·艾萨胡蕊
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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