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Preparation method for extracting anticancer valid-position medicine SHIKEMOXIN from sweetsop

A technology of effective parts and lychees, which is applied in the field of extraction of active ingredients of the plant Annuus apple, can solve problems such as difficult large-scale production, endangering human health, and toxic damage to the body, and achieves low environmental pollution, improved extraction rate, and high safety Effect

Inactive Publication Date: 2011-05-25
贵州正鑫实业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are many domestic research reports on the preparation method of custard apple lactones and most of them have applied for patents, such as CN1224016A, CN1370530A, CN1228334C. In these published patents, a large amount of toxic organic solvents are first used to extract the total content of cinnamon apples. Ester liquid, and then use the separation method of silica gel column chromatography to separate the effective part drug Shicomoxin. The eluent and extractant used are mostly petroleum ether, ethyl acetate, acetone, chloroform, n-hexane, methanol , acetonitrile and other organic solvents. Most of the above substances have different degrees of toxicity. If they are used in large quantities in production, they will cause physical toxicity to the personnel engaged in production operations and seriously endanger human health. Moreover, the entire preparation method is only suitable for small-scale laboratories. production, it is difficult to achieve industrial scale production

Method used

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  • Preparation method for extracting anticancer valid-position medicine SHIKEMOXIN from sweetsop

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation of custard apple total lactone medicinal liquid: take 2 kg of custard apple seeds washed and dried (moisture must not exceed 9%) and pulverize into coarse powder, put in a three-necked flask, add 6000 ml of 90% alcohol, place in an electric heating mantle, and heat The temperature of the jacket was adjusted to 60°C, and the speed of the agitator was adjusted to a suitable value. After boiling, the temperature was adjusted to 50°C, and the extraction was slightly boiled for 1 hour. Once, add 4000ml of 90% alcohol each time, combine the three extracts and filter to obtain 10000ml of extract, then concentrate under reduced pressure (vacuum degree is controlled at 0.60Mpa) and reclaim the solvent until the concentrated solution specific gravity is 0.92, obtaining 1.3 times the seed weight About 2800ml of the concentrated solution is added to purified water for water precipitation, and the weight is added to 5 times the weight of the original medicinal materia...

Embodiment 2

[0025] The preparation of the total lactones of custard apple liquid: take 2 kg of cinnamon apple seeds washed and dried (moisture must not exceed 9%) and pulverize into coarse powder, put in a three-necked flask, add 7000 ml of 95% alcohol, place in an electric heating mantle, and heat The temperature of the jacket was adjusted to 60°C, and the speed of the agitator was adjusted to a suitable value. After boiling, the temperature was adjusted to 50°C, and the extraction was slightly boiled for 1 hour. Once, add 95% alcohol 6000ml at every turn, combine three extracts and filter to obtain extract 14000ml, then concentrate under reduced pressure (vacuum degree is controlled at 0.80Mpa) and reclaim the solvent until the concentrated solution specific gravity is 0.97, obtaining 1.3 times the seed weight About 2700ml of the concentrated solution is added to purified water for water precipitation, and the weight is added to 5 times the weight of the original medicinal material, and ...

Embodiment 3

[0028] The preparation of custard apple total lactone medicinal liquid: take 2 kg of custard apple seeds washed and dried (moisture must not exceed 9%) and pulverize into coarse powder, put in a three-necked flask, add 8000 ml of 93% alcohol, place in an electric heating mantle, and heat The temperature of the jacket was adjusted to 60°C, and the speed of the agitator was adjusted to a suitable value. After boiling, the temperature was adjusted to 50°C, and the extraction was slightly boiled for 1 hour. Once, add 93% alcohol 5000ml at every turn, combine three extracts and filter to obtain extract 13500ml, then concentrate under reduced pressure (vacuum degree is controlled at 0.70Mpa) and reclaim the solvent until the concentrated solution specific gravity is 0.95, obtaining 1.4 times the seed weight About 2900ml of the concentrated solution is added to purified water for water precipitation, and the weight is added to 5 times the weight of the original medicinal material, and...

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Abstract

The invention discloses a preparation method for extracting anticancer valid-position medicine SHIKEMOXIN from sweetsop, comprising the steps of crushing sweetsop seeds, putting the crushed sweetsop seeds in an ethanol solution with the volume that is 3-5 times of that of the sweetsop seeds, leaching for 1 hour in a slight boiling manner in the ethanol solution, carrying out reduced pressure distillation for leaching liquor to recycle ethanol; extracting the medicine dreg for two times by the same method, merging and separating sweetsop total lactones liquid medicine, separating and eluting the sweetsop total lactones liquid medicine by a macroporous resin column, guiding and merging the desired fraction by thin layer chromatography or high efficiency liquid chromatography, recycling solvents, and drying under reduced pressure to obtain the sweetsop lactones anti-cancer valid-position medicine, namely SHIKEMOXIN. The method not only solves the problem that the toxic organic solvent used in the production harms health of operators, but also the production technology is more suitable for industrial production on a large scale, and the method has strong practicality and promotional value.

Description

technical field [0001] The invention relates to a preparation method for extracting squamocin, an anti-cancer effective fraction drug, from custard apples, and belongs to the field of extracting effective components of plant custard apples (Annona squamosa L.). Background technique [0002] Annonasquamosa L. is native to tropical America and is now cultivated in tropical regions all over the world. In my country, it is mainly cultivated in Hainan, Guangdong, Taiwan, Fujian, Guangxi, Yunnan and other places. In 1982, it was first discovered that annonaceae extracts from Annonaceae plants (Annonaceae) have typical anticancer activity, and more than 350 kinds of annonaceae compounds have been discovered so far. Most of these natural anemone lactones have different degrees of anticancer activity, among which squamocin and bullatacin have the strongest activity, and the two account for 70% or more of the total mass fraction of anemone lactones. Annonaceous lactones are a class o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/58B01D15/08
Inventor 杨正强脱冰林袁胜伟
Owner 贵州正鑫实业有限公司
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