Terpenoid in euphorbia soongarica as well as preparation method and application of terpenoid

A technology of Junggar euphorbia and terpenoids, which is applied in the field of terpenoids and their preparation, and can solve problems such as the formation of drug resistance and increased drug efflux

Active Publication Date: 2017-05-31
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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  • Terpenoid in euphorbia soongarica as well as preparation method and application of terpenoid
  • Terpenoid in euphorbia soongarica as well as preparation method and application of terpenoid
  • Terpenoid in euphorbia soongarica as well as preparation method and application of terpenoid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] a. Take 10 kg of the whole herb of Euphorbia Junggar, pulverize it and extract it by percolation at room temperature with 50 L of acetone, and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia Junggar;

[0069] b. Disperse the crude extract obtained in step a with acetonitrile, add cyclohexane to extract, combine the acetonitrile layers and evaporate to dryness under reduced pressure to obtain the acetonitrile extract extract;

[0070] c, the acetonitrile 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 100:1-0:1, and the fraction is subjected to silica gel thin layer chromatography ( TLC) analysis, combined the same fractions to obtain 12 components (F1-F12); Component F6 was subjected to normal phase silica gel column separation, carried out with n-hexane-ethyl acetate with a volume ratio of 40:1-0:1...

Embodiment 2

[0072] a. Take 10 kg of Euphorbia euphorbia whole herb, crush it, and use 60 L of acetone-water solution with a concentration of 80% to extract by cold soaking at room temperature, and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia euphorbia;

[0073] b. Disperse the crude extract obtained in step a with acetonitrile, add n-hexane to extract, combine the acetonitrile layers and evaporate to dryness under reduced pressure to obtain the acetonitrile extract extract;

[0074] c. Separate the acetonitrile extract extract obtained in step b with a normal-phase silica gel column, and carry out gradient elution with petroleum ether-ethyl acetate with a volume ratio of 100:1-0:1. The fractions are analyzed by TLC and merged with the same Fraction, obtain 12 components (F1-F12); Component F6 is subjected to normal phase silica gel column separation, is 40:1-0:1 cyclohexane-ethyl acetate gradient elution with the volume ratio, obtains gro...

Embodiment 3

[0076]a. Take 10 kg of the whole herb of Euphorbia Junggar, pulverize it and extract it by percolation at room temperature with 70 L of ethanol, and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia Junggar;

[0077] b. Disperse the crude extract obtained in step a with acetonitrile, add petroleum ether for extraction, combine the acetonitrile layers and evaporate to dryness under reduced pressure to obtain the acetonitrile extract extract;

[0078] c. Separate the acetonitrile extract extract obtained in step b with a normal phase silica gel column, and carry out gradient elution with cyclohexane-ethyl acetate with a volume ratio of 100:1-0:1, and the fractions are analyzed by TLC and merged into the same Fractions were obtained to obtain 12 components (F1-F12); the component F6 was subjected to normal phase silica gel column separation, and the petroleum ether-ethyl acetate gradient elution with a volume ratio of 40:1-0:1 was use...

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Abstract

The invention relates to a terpenoid in euphorbia soongarica as well as a preparation method and application of the terpenoid. The method takes herb of euphorbia soongarica (E.soongarica) as a raw material, and comprises the following steps: extracting with an organic solvent, separating by utilizing three to four methods in a solvent extraction method, a normal phase silica gel column chromatography, a reverse phase silica gel column chromatography and a Sephadex LH-20 gel column chromatography, so as to obtain 10 new terpenoids (comprising 5 diterpenes, 3 nortriterpenoid and 2 triterpenoid compounds). The obtained 10 new terpenoids are subjected to multi-drug drug resistance reversal activity determination and a result shows that the new terpenoid has different extents of multi-drug drug resistance reversal activity and can be used for preparing a multi-drug drug resistance reversal medicine or can be combined with an anti-tumor medicine to prepare an anti-tumor combined medicine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to terpenoids in Euphorbia Junggar and its preparation method and application. Background technique [0002] Euphorbia is a large genus in Euphorbiaceae (Euphorbiaceae). There are more than 2000 species of plants in the world, which are widely distributed in tropical and temperate regions. Euphorbia plants have important medicinal value, and are mostly used for laxative, diuretic, and treatment of tuberculosis, edema, psoriasis, and scabies. Junggar Euphorbia (Euphorbia soongarica Boiss.) is a perennial herb of the genus Euphorbia, produced in northern Xinjiang and western Gansu, and distributed in China, West Siberia to Central Asia and Mongolia. Its root is used as medicine, which has the effects of dispelling water, reducing swelling, and dispelling blood stasis. It is also used as a substitute for Euphorbia in Xinjiang. More than 50 compounds have been reported from Euphorbia...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D301/32C07D303/48C07C67/48C07C67/56C07C69/78C07C67/58C07C45/78C07C45/79C07C45/80C07C49/743C07C231/24C07C233/32C07J1/00C07J63/00A61K31/336A61K31/122A61K31/24A61K31/235A61K31/569A61K31/56A61P35/00
CPCC07C45/78C07C45/79C07C45/80C07C67/48C07C67/56C07C67/58C07C231/24C07D301/32C07D303/48C07J1/00C07J63/008C07C69/78C07C49/743C07C233/32
Inventor 阿吉艾克拜尔·艾萨高洁
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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