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Application of two bi-sesquiterpenes compound for preparing antineoplastic and antiinflammatory medicine

A technology of terpenoids and anti-inflammatory drugs is applied in the application field of preparing anti-tumor and anti-inflammatory drugs, and can solve problems such as obvious side effects and the like

Inactive Publication Date: 2008-10-15
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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  • Application of two bi-sesquiterpenes compound for preparing antineoplastic and antiinflammatory medicine
  • Application of two bi-sesquiterpenes compound for preparing antineoplastic and antiinflammatory medicine
  • Application of two bi-sesquiterpenes compound for preparing antineoplastic and antiinflammatory medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Zhongdian Rabbit Ear Wind (Ainsliaea fulvioides) whole plant 50kg, reflux extraction with 80% ethanol 3 times, 1.5 hours each time, combine three extracts and concentrate under reduced pressure to an extract with no alcohol smell. The extract was diluted with an appropriate amount of water to a volume of about 50L, and extracted successively with petroleum ether (50L×3), chloroform (50L×3), ethyl acetate (50L×3), and n-butanol (50L×3), respectively, to obtain Chloroform site extract is about 485g. The chloroform part is put on a silica gel column, and the dichloromethane: methanol gradient elution with a volume ratio of 100:1 to 10:1 is detected by thin layer chromatography. The 20:1 polar part of dichloromethane: methanol contains Zhongdian rabbit Auripterpene A and Zhongdian Rabbit Auriperne B. Concentrate the part to dryness and continue to put it on the silica gel column, and use the petroleum ether: ethyl acetate gradient elution with a volume ratio of 10:1 to 0:1...

Embodiment 2

[0023] 20kg of whole herb of Ainsliaea macrocephala was refluxed with 95% ethanol for 3 times, each time for 2 hours, and the extracts were combined and concentrated under reduced pressure until an alcohol-free extract. The extract was diluted with an appropriate amount of water to a volume of about 20L, and extracted successively with petroleum ether (20L×3), chloroform (20L×3), ethyl acetate (20L×3), and n-butanol (20L×3), respectively, to obtain Chloroform site extract is about 195g. The chloroform part is put on a silica gel column, and the chloroform: methanol gradient elution with a volume ratio of 100:1 to 10:1 is detected by thin-layer chromatography. The 15:1 polar part of dichloromethane: methanol contains Zhongdian rabbit Auripterpene A and Zhongdian Rabbit Auriperne B. After the part is concentrated to dryness, it is continued to be applied to a silica gel column, and is eluted with a gradient of petroleum ether: ethyl acetate with a volume ratio of 10:1 to 1:1. I...

Embodiment 3

[0025] Active ingredient (one or both of the above two compounds) 8g

[0026] Microcrystalline Cellulose 80g

[0027] Cornstarch 12g

[0028] Talc powder 5g

[0029] Made into 1000 pieces

[0030]Preparation method: mix active ingredients, microcrystalline cellulose and cornstarch, uniformly moisten with water to make a soft material, granulate the wetted mixture, pass through a 20-mesh sieve, dry at 80°C, add magnesium stearate, and Sieve, and then compress the mixture into tablets, each tablet weighs 105 mg, and the active ingredient content is 8 mg. Oral administration of this product can be used to treat tumors.

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Abstract

The invention relates to an application of two sesquiterpenoids in preparing antitumor and anti-inflammatory medicines. The sesquiterpenoids are gochnatiolide A and gochnatiolide B, which can be extracted and separated from Ainsliaea fulvioides or other plants, or obtained by chemical synthesis. The experimental results show that the two sesquiterpenoids have good inhibitory effect on human tumor cells and have distinct inhibitory effect on inflammations. Therefore, the two sesquiterpenoids can be used for preparing antitumor and anti-inflammatory medicines.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of two bisesquiterpene compounds, Zhongdian terpene A and Zhongdian terpene B, in the preparation of antitumor and anti-inflammatory 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. Some of these anti-tumor drug treatments have very significant curative effects, such as drug treatment of acute leukemia in children. However, the research and deve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P35/00A61P29/00
Inventor 张卫东金慧子单磊苏娟柳润辉李慧梁王燕
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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