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Abies holophylla triterpenoid compound, extraction separation thereof and application thereof

A technology of compounds and triterpenoids, applied in the field of medicinal chemistry, can solve problems such as obvious side effects, and achieve the effects of small toxic effects, large practical application value, and good curative effect

Inactive Publication Date: 2011-04-27
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the research and development of tumor drugs still face great challenges. For example, most anti-tumor drugs are cytotoxic drugs, and their side effects are obvious, which limits the efficacy of these drugs.

Method used

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  • Abies holophylla triterpenoid compound, extraction separation thereof and application thereof
  • Abies holophylla triterpenoid compound, extraction separation thereof and application thereof
  • Abies holophylla triterpenoid compound, extraction separation thereof and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The raw material of the following examples is fir pine collected from the Changbai Mountains in Northeast China, and its dried branches and leaves are taken.

[0045] (1) Extraction: Grind 10Kg of dried branches and leaves of fir pine, extract once with 80L of 75% ethanol under reflux, each time for 2 hours, combine the extracts, concentrate the extracts under reduced pressure to form a fluid extract, the fluid extract is equivalent to 1ml containing fir Pine 0.9g, the liquid extract was diluted with 12L of water, extracted 3 times with 6L of chloroform to obtain the chloroform extraction fraction;

[0046] (2) Separation: The above-mentioned chloroform extraction part is subjected to silica gel column chromatography, and the petroleum ether / ethyl acetate system gradient elution with a volume ratio of 100:0-1:1 is used for thin-layer chromatography detection. The fractions of compounds, the elution order is compound 2, 1, 3, 5, 4. The five compounds were chromatographed...

Embodiment 2

[0058] (1) Extraction: crush 5Kg of dried branches and leaves of fir pine, extract 3 times with 100L of 80% ethanol under reflux, each time for 3 hours, combine the extracts, and concentrate the extracts under reduced pressure to form a liquid extract, which is equivalent to 1ml containing Chinese fir Pine 1.0g, the liquid extract was diluted with 10L of water, extracted 4 times with 20L of chloroform to obtain the chloroform extraction fraction;

[0059] (3) Separation: apply silica gel column chromatography to the above-mentioned chloroform extraction part, and use the petroleum ether / ethyl acetate system gradient elution with a volume ratio of 100:0-1:1, and detect by thin-layer chromatography. Compound fractions, the elution order is compound 2, 1, 3, 5, 4, 5 compounds respectively? Sephadex chromatography, eluted with chloroform / methanol with a volume ratio of 1:1, and then C18 reverse-phase column chromatography, eluted with methanol / water with a volume ratio of 6:4-10:0...

Embodiment 3

[0061] (1) Extraction: Grind 20Kg of dried branches and leaves of fir pine, reflux extraction with 95% ethanol 200L for 3 times, each time for 3 hours, combine the extracts, and concentrate the extracts under reduced pressure to form a liquid extract, which is equivalent to 1ml containing Chinese fir Pine 1.1g, the liquid extract was diluted with 54L of water, extracted 5 times with 54L of chloroform to obtain the chloroform extraction fraction;

[0062] (4) Separation: The above-mentioned chloroform extraction part is subjected to silica gel column chromatography, and the petroleum ether / ethyl acetate system gradient elution with a volume ratio of 100:0-1:1 is used for thin-layer chromatography detection. The fractions of compounds, the elution order is compound 2, 1, 3, 5, 4. The five compounds were chromatographed on Sephadex gel, eluted with chloroform / methanol with a volume ratio of 1:1, and finally reacted with C18 Phase column chromatography, eluting with methanol / water...

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Abstract

The invention provides an abies holophylla triterpenoid compound, which comprises the following compounds 1, 2, 3, 4 and 5. The compounds are subjected to an experiment of cytotoxic activity, and a result shows that the five compounds have good inhibitory activity and excellent anti-tumor effect on human lung cancer cells, human intestinal cancer cells, human small cell lung cancer cells and human breast cancer cells. The five compounds are proved by a curative effect experiment on sarcoma (entities) of mice S180 to have the obvious tumor-inhibitory effect. The abies holophylla triterpenoid compound can be used for preparing anti-cancer medicaments. The medicaments of the invention consist of the abies holophylla triterpenoid compound serving as active ingredients and a conventional medicinal carrier, and can be prepared into preparations according to the conventional method. The medicaments of the invention are Chinese medicinal preparations, have small toxic and side effect and highcurative effect, provide new anti-cancer medicaments clinically, have large practical application value and can create good social benefit.

Description

technical field [0001] The invention relates to medicinal chemistry, in particular to fir-pine triterpenoids and their extraction, separation and application. In particular, it relates to the application of fir pine triterpenoids in the preparation of anticancer drugs. Background technique [0002] Tumor is one of the main causes of human death. The Ministry of Health of China announced the main causes of death of urban and rural residents in 2006. Statistics show that malignant tumors have become the leading cause of death. It can be seen that the prevention and treatment of tumors is very urgent. Drug therapy is one of the main treatments for tumors. At present, although dozens of anti-tumor drugs have been developed, they can effectively prolong the life of patients or improve the quality of life of patients. However, the research and development of tumor drugs is still facing great challenges. For example, most anti-tumor drugs are cytotoxic drugs, and their side ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00C07J7/00C07D307/58C07J17/00A61K31/575A61K31/573A61K31/365A61K31/585A61P35/00
Inventor 张卫东杨献文苏娟沈云亨单磊李慧梁柳润辉徐希科李永利
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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