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Echinocystic acid derivative and application thereof in preparation of anti-tumor medicine

A kind of derivative, the technology of echinocystic acid, which is applied in the field of medicine, can solve the problems of no literature report on the growth of echinocystic acid tumor cells, no report on the application of echinocystic acid derivative antitumor drugs, etc.

Active Publication Date: 2016-06-22
JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Before the completion of the present invention, there was no literature report that the derivatives of echinocysic acid had the effect of inhibiting the growth of tumor cells, and there was no report on the application of echinocysic acid derivatives in the preparation of antitumor drugs.

Method used

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  • Echinocystic acid derivative and application thereof in preparation of anti-tumor medicine
  • Echinocystic acid derivative and application thereof in preparation of anti-tumor medicine
  • Echinocystic acid derivative and application thereof in preparation of anti-tumor medicine

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0026] The preparation of example 1 echinocystic acid

[0027] Take 1 kg of saponin root medicinal material, add 30 g of calcium oxide by weight of the medicinal material, and reflux extract with 8 times the amount of 50% ethanol for 3 times, each time for 2 hours. Combine the extracts three times, filter, and recover the ethanol from the filtrate until it has no alcohol smell, add water to the weight of the medicinal material to 3000ml, pass through the treated macroporous resin column, and first elute with 20% ethanol containing sodium hydroxide (pH value is 13) 3 times the column volume, then eluted with water until neutral, and finally eluted with 70% ethanol for 4 times the column volume, collected the eluate, and concentrated to dryness under reduced pressure; Hydrolyzed for 3 hours. Filtrate, discard the hydrolyzate, wash the filter cake with deionized water until it is neutral; then heat it to boiling with 95% ethanol, add 2% medicinal activated carbon of the volume ...

example 2

[0028] The preparation of example 2 (3,16-dibenzoyl) echinocytic acid (compound 1)

[0029] Echinocysic acid 0.47g, dissolved in 25ml CH 2 Cl 2 2ml of benzoyl chloride was slowly added dropwise in an ice bath, then 2ml of triethylamine was added, and the reaction was stirred at room temperature for 24 hours. After the reaction was complete, the solvent was recovered under reduced pressure and dried to obtain a crude product. The crude product was first recrystallized from dichloromethane-petroleum ether, and then separated and purified by silica gel column (petroleum ether: ethyl acetate = 5:1) to obtain 0.35 g of white powdery crystals.

example 3

[0030] The preparation of example 3 (3,16-two o-methylbenzoyl) echinocytic acid (compound 2)

[0031] Echinocysic acid 0.47g, dissolved in 25ml CH 2 Cl 2 2 ml of o-toluyl chloride was slowly added dropwise in an ice bath, then 2 ml of triethylamine was added, and the reaction was stirred at room temperature for 24 hours. After the reaction was complete, the solvent was recovered under reduced pressure and dried to obtain a crude product. The crude product was first recrystallized from dichloromethane-petroleum ether, and then separated and purified by silica gel column (petroleum ether: ethyl acetate = 5:1) to obtain 0.38 g of white powdery crystals.

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PUM

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Abstract

The invention discloses a series of derivatives which are prepared through corresponding chemical reactions by taking echinocystic acid obtained through extracting, separating and purifying dry mature fruits of gleditsia sinensis lam. as a lead compound. A pharmacological experiment proves that an echinocystic acid derivative has anti-tumor activity and has an inhibiting effect on prostate cancer cells, lung cancer cells, liver cancer cells, cervical cancer cells, gastric cancer cells and breast cancer cells, and the inhibiting effect of the echinocystic acid derivative on tumor cells is better than that of a mother nucleus compound-the echinocystic acid on the tumor cells.

Description

technical field [0001] The present invention relates to a preparation method of echinocysic acid derivatives obtained from natural Chinese medicines. To be exact, a series of derivatives are prepared with the chemical components extracted from Chinese medicines as the lead compound, and the structure is modified with the anti-tumor activity as the index. , belonging to the field of medicine. Background technique [0002] Echinocysic acid is a kind of pentacyclic triterpenoids obtained from the dry mature fruit of legume plant Gleditsia Sinensis Lam. through extraction, purification, separation, and acid degradation (Zhao Quancheng, Nan Minlun, etc., echinocytic acid Preparation methods, pharmaceutical preparations and new uses of medicine, ZL03100676.0), this patent describes the preparation method of echinocystic acid, and has the pharmacological effect of dilating coronary arteries, and can be used to prevent and treat coronary heart disease, angina pectoris, myocardial is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61P35/00
CPCC07J63/008
Inventor 南敏伦赵昱玮赫玉芳吕娜何忠梅赵全成
Owner JILIN ACAD OF TRADITIONAL CHINESE MEDICINE