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Sesquiterpene lactone compound, preparation method and application thereof

A technology of ester compounds and sesquiterpene is applied in the field of preparation of novel sesquiterpene lactones to achieve the effects of low production cost, good application prospects and novel structure

Active Publication Date: 2016-02-03
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In terms of the application of Chinese patent medicine preparations such as Yemazhui syrup, these preparations are mostly used for the treatment of respiratory diseases such as phlegm, cough, and asthma. The index components or active ingredients detected are mainly flavonoids and alkaloids. Yemazhui and its preparations Applications in cancer therapy are rarely reported

Method used

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  • Sesquiterpene lactone compound, preparation method and application thereof
  • Sesquiterpene lactone compound, preparation method and application thereof
  • Sesquiterpene lactone compound, preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation method of the novel sesquiterpene lactone in the plant of the genus Benzei comprises the following steps:

[0049] A. Extraction: Yema chasing medicinal materials are powdered and passed through a 40-mesh sieve for use. Take 2 kg of wild horse chasing medicinal material coarse powder, add an appropriate amount of 95% ethanol to wet it, and then pack it into a column. The total solvent volume for extraction was equivalent to 18 times the amount of the drug substance (a total of 36 L of 95% ethanol was used).

[0050] B, extraction: the leaching solution obtained in step A is concentrated to near dryness under reduced pressure, to obtain 84.3g of thick extract, add water and suspend to 1L, respectively use 1L of petroleum ether, 1L of ethyl acetate, and each extraction solvent is extracted three times , Merge the extracts of each time to obtain Yema chasing petroleum ether extract and ethyl acetate extract respectively. Through TLC detection, Yema chasing...

Embodiment 2

[0054] A. Extraction: Take 2kg of Yemachai medicinal material, add 8 times the amount of 95% ethanol, reflux at 85°C for extraction, each extraction time is 2h, and extract 3 times in total, and combine the 3 extracts. A total of 48 L of 95% ethanol was used.

[0055] B, extraction: the extract obtained in step A is concentrated to near dryness under reduced pressure to obtain 92.7g of thick extract, add water and suspend to 1L, extract with 1L of petroleum ether and 1L of ethyl acetate respectively, and each extraction solvent is extracted three times , Merge the extracts of each time to obtain Yema chasing petroleum ether extract and ethyl acetate extract respectively. Through TLC detection, Yema chasing sesquiterpene lactones are mainly concentrated in the ethyl acetate extract, and ethyl acetate The solvent of the extract was recovered under reduced pressure to obtain 60.3 g of the ethyl acetate extract of Yema Chai.

[0056] C, column chromatography: get the above-mentio...

Embodiment 3

[0059] A. Extraction: Yema chasing medicinal materials are powdered and passed through a 40-mesh sieve for use. Take 2 kg of wild horse chasing medicinal material coarse powder, add an appropriate amount of 95% ethanol to wet it, and then pack it into a column. The total solvent volume for extraction was equivalent to 18 times the amount of the drug substance (a total of 36 L of 95% ethanol was used).

[0060] B, extraction: the leaching solution obtained in step A is concentrated to near dryness under reduced pressure to obtain 82.4g of thick extract, add water and suspend to 1L, extract with 1L of petroleum ether and 1L of ethyl acetate respectively, and each extraction solvent is extracted Three times, the extracts of each time were combined to obtain Yema chasing petroleum ether extract and ethyl acetate extract respectively. Through TLC detection, Yema chasing sesquiterpene lactone was mainly concentrated in the ethyl acetate extract, and ethyl acetate extraction The sol...

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Abstract

The invention discloses a sesquiterpene lactone compound, a preparation method thereof and an application of the sesquiterpene lactone compound in cancer treatment, and a structure of the sesquiterpene lactone compound is shown as a formula (I). The preparation method of the sesquiterpene lactone compound comprises the following steps: A) using an extraction solvent for extracting medicinal materials; B) concentrating an extract, adding water for suspending the extract, respectively using organic solvents having polarity from low to high for extracting a mixture to obtain an extract liquor, concentrating the extract liquor to obtain a crude extract; C) passing the crude extract through a normal-phase column, and eluting the crude extract with an eluting agent; collecting an eluent, and drying the eluent to obtain an extract product which is enriched with the novel sesquiterpene lactone compound; and D) performing reverse-phase medium-pressure column chromatography on the extract product and performing preparative high-efficiency liquid-phase column chromatography on a crude product to obtain the novel sesquiterpene lactone compound. The preparation method has the advantage of simple operation and low production cost; and the obtained product can be used for preparing cancer therapeutic drugs, and has favorable development prospects.

Description

technical field [0001] The invention belongs to the technical field of active ingredients of natural medicines, relates to the field of extraction, preparation and application of active ingredients from traditional Chinese medicines, and in particular relates to a preparation method of a novel sesquiterpene lactone from plants of the genus Asteraceae and its cancer treatment application. Background technique [0002] There are more than 600 species of plants in the genus Eupatorium L. of the Compositae family, mainly distributed in the temperate and tropical regions of Central and South America. There are 14 species and several varieties in China, all of which are produced in the whole country except Xinjiang and Tibet. As a medicinal plant, the genus Zelan is currently used more than eight species such as Lin Zelan. This genus has a long history of medicinal use. [0003] Yemazui is the dry aerial part of the genus Eupatorium lindleyanum DC. It is widely distributed in m...

Claims

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Application Information

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IPC IPC(8): C07D307/93A61K31/365A61P35/00
CPCC07D307/93
Inventor 杨波赵华军周东恒赵亚萍
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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