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3-phenylcoumarin robustic acid as well as extraction method and application thereof

An extraction method, the technology of soil licorice, applied in the field of medicinal chemistry, can solve the problems of low plant content and application limitations, and achieve the effect of high extraction rate and simple and easy extraction method

Active Publication Date: 2015-02-11
北京华诺信得科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound was originally derived from licorice Derris eriocarpa How, but the content in this plant is low, which limits its application

Method used

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  • 3-phenylcoumarin robustic acid as well as extraction method and application thereof
  • 3-phenylcoumarin robustic acid as well as extraction method and application thereof
  • 3-phenylcoumarin robustic acid as well as extraction method and application thereof

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Experimental program
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Embodiment 1

[0020] The extraction method of soil licorice A of the present invention comprises following specific steps:

[0021] 1) Take 10.0kg of the coarse powder of Dalbergia japonica, extract by percolation with 10 times the amount of 80% ethanol, combine the extracts, and evaporate the solvent to obtain the extract extract;

[0022] 2) add water to suspend the extract extract, then add petroleum ether to the suspension to extract and separate the extract from petroleum ether, then add ethyl acetate to the suspension to extract to obtain the extract from ethyl acetate;

[0023] 3) Take 30 g of the extract from the part of ethyl acetate, and repeatedly separate it by silica gel column chromatography to obtain a colorless and transparent granular crystalline compound, which is the target product Glycyrrhizae A. The way of this silica gel column chromatographic separation can be according to following operation: first with chloroform-acetone gradient elution (chloroform → 80: 1 → 50: 1 ...

Embodiment 2

[0028] The soil licorice A that is extracted from the above-mentioned embodiment 1 is carried out in vitro anti-tumor activity experiment:

[0029] MTT method is widely used in the activity detection of some biologically active factors, large-scale antitumor drug screening, cytotoxicity test and tumor radiosensitivity determination, etc. It has the characteristics of high sensitivity and economy. Exogenous MTT can be reduced to water-insoluble blue-purple crystalline formazan (Formazan) by succinate dehydrogenase in the mitochondria of living cells and deposited in the cells, and its light absorption value is measured at a wavelength of 490nm by an enzyme-linked immunosorbent assay , which can indirectly reflect the number of living cells. Within a certain cell number range, the amount of MTT crystal formation is proportional to the cell number. By calculating the concentration of the corresponding drug when the inhibitory rate of the compound on tumor cells is 50%, it is cal...

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Abstract

The invention discloses 3-phenylcoumarin robustic acid as well as an extraction method and application thereof. 3-phenylcoumarin robustic acid has a structural formula as shown in the specification as well as a chemical name of 3-(p-methoxyphenyl)-4-hydroxy-5-methoxy-2', 2'-dimethyl-6,7-dihydropyrancoumarin, a molecular formula of C22H20O6, and relative molecular weight of 380. 3-phenylcoumarin robustic acid disclosed by the invention has anti-tumor and other biological activities, can be effectively applied in preparation of anti-tumor drugs and has very strong inhibition effect on human gastric cancer cells, liver cancer cell lines, human lung cancer cells, cervical cancer cells, ovarian cancer cells and the like, the extraction method is simple and feasible and the extraction efficiency is relatively high.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a soil licorice A and an extraction method thereof, and the use of soil licorice A to prepare antitumor drugs. Background technique [0002] Cancer has risen to become the second largest "killer" disease of human beings after cardiovascular disease. Cancer and cardiovascular disease have become the leading causes of death. The prospect of finding and developing effective new anti-tumor drugs from plants is broad. At present, many natural active products with different structures and mechanisms of action have become a hot spot in the research of new anti-tumor drugs at home and abroad. Among the two batches of major new drug development projects launched continuously in my country, the research and development of plant-derived drugs, especially natural drugs using plant resources in my country, has been listed as key support objects. Due to the unique mechanism of act...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/37A61P35/00
CPCA61K31/37C07D493/04
Inventor 韦建华霍丽妮黄茂春陈睿冯旭
Owner 北京华诺信得科技有限公司
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