Macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey and application

A compound and diterpenoid technology, applied in the field of preparing anti-tumor drugs, can solve the problems of unknown chemical composition of Euphorbia vulgaris

Active Publication Date: 2015-03-04
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

However, the chemical composition of Euphorbia grandis is still unknown

Method used

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  • Macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey and application
  • Macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey and application
  • Macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey and application

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Preparation of new macrocyclic diterpenoids

[0047] Take 2.4kg of the whole plant of Euphorbia euphorbia, crush it, extract it with 25L acetone percolation method at room temperature, and evaporate the solvent to dryness under reduced pressure to obtain the crude extract of Euphorbia euphorbia; the crude extract is dispersed with cyclohexane, added Acetonitrile is extracted, and the acetonitrile layer is combined, and the acetonitrile is evaporated to dryness under reduced pressure to obtain the acetonitrile extract extract;

[0048] The obtained acetonitrile extract extract was separated by normal phase silica gel column, and gradient elution was carried out with petroleum ether-ethyl acetate=100:1-0:1 as the solvent system, and the fraction was analyzed by silica gel thin layer chromatography (TLC) , combined the same fractions to obtain 11 sections of components (F1-F11), wherein the section F5 components were then separated by a normal phase silica gel column, usin...

Embodiment 2

[0079] The application of the macrocyclic diterpenoids isolated from Euphorbia rhizome in the present invention in the preparation of antitumor drugs is exemplified by human oral epidermoid cancer cell lines and drug-resistant strains.

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Abstract

The invention relates to macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey and application. The macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey respectively belong to five different diterpenoid scaffold types. The macrocyclic diterpenoid compounds are subjected to in-vitro cytotoxic activity determination and anti-drug-resistance activity determination. Experiment results show that the macrocyclic diterpenoid compounds separated from euphorbia macrorrhiza C.A.Mey have cytotoxic activity on human oral-cavity epidermoid carcinoma KB cell and human oral-cavity epidermoid carcinoma drug-resistant strain KBv200 to different degrees, have certain anti-drug-resistance activity, and is applicable to antitumor medicines.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new macrocyclic diterpenoid compound and its application in the preparation of antitumor drugs. Background technique [0002] Euphorbia L. is the largest genus in the Euphorbia family. There are more than 2,000 species of plants distributed all over the world, including 80 species in my country, mostly distributed in the Hengduan Mountains in the southwest and the arid regions in the Northwest. Euphorbia plants have important medicinal value, and are mostly used for laxative, diuretic, and treatment of tuberculosis, edema, psoriasis, and scabies. Studies have shown that most of the plants in this genus have anti-tumor, anti-leukemia and other activities, and also have skin-irritating, inflammatory and carcinogenic effects, and these activities are closely related to the diterpenes contained in them. [0003] Euphorbia macrorrhiza C.A. Mey is a perennial herb of the Euphorbia ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D303/32C07D301/32C07C49/737C07C49/743C07C49/753C07C45/79A61K31/336A61K31/122A61P35/00
CPCC07C49/727C07C49/733C07C49/743C07C49/753C07C2602/32C07C2603/38C07C2603/40C07D303/32
Inventor 阿吉艾克拜尔·艾萨
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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