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Refined cherimoya total inner ester with anti-tumor activity and preparation method thereof

A technology of custard apple lactone and total lactone, which is applied in the directions of antitumor drugs, organic active ingredients, pharmaceutical formulations, etc., can solve problems such as difficulty in controlling the quality and efficacy of drugs, high content of low active ingredients, and unclear composition of ingredients. , to achieve the effect of safe and controllable quality, less active ingredients and clear ingredients

Inactive Publication Date: 2009-07-22
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The prior art Chinese invention patent (CN1739586A) discloses the crude extract of custard apple, and the Chinese invention patent (CN1224016A) discloses the total lactones of custard apple, but in the prior art, there are complex components, unclear component composition, low active ingredient content and high content , it is difficult to control the quality and efficacy of drugs

Method used

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  • Refined cherimoya total inner ester with anti-tumor activity and preparation method thereof
  • Refined cherimoya total inner ester with anti-tumor activity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The extraction of the total lactones of cherimoya, get 2 kilograms of dry seeds of cherimoya, pulverize, and percolate twice with chloroform of 10 times the amount of seed meal, detect with silica gel thin-layer chromatography, the nearly percolation extraction of cinnamon lactones is complete, in Recover under reduced pressure below 60°C to obtain the concentrate, let it stand for 24 hours, centrifuge at 3000 rpm, and then take the centrifuged upper layer concentrate (88.7g) to obtain the crude extract of total lactones of custard apple.

[0040] Take 80g of the crude extract of total lactones of custard apple, add 1 times the amount of petroleum ether, heat and dissolve in a water bath at 60°C, mix well, and after standing for layers, absorb the upper layer of petroleum ether, concentrate, dry, and repeat the above operation for 3 times, to obtain the total lactones of custard apple 46g.

[0041] Take 46g of the above-mentioned total lactones of custard apple, mix it wi...

Embodiment 2

[0043] Extract the crude extract of total lactones of cherimoya according to the method of Example 1, extract 86.6g of total lactones from 2 kilograms of dry seeds of custard apple, get the crude extract of total lactones of custard apple 82g, add 10 times the amount Petroleum ether-water (5:1), heat and dissolve in a water bath at 80°C, mix evenly, and after standing to separate layers, absorb the upper layer of petroleum ether, concentrate, dry, repeat the above operation 3 times, and obtain the total lactones of custard apple 47g.

[0044] Take 47g of the above-mentioned total lactones of custard apple, mix with the same amount of silica gel, grind it evenly, apply silica gel (400g, 200 to 300 mesh, Qingdao Ocean Chemical Factory) column chromatography, and use petroleum ether-ethyl acetate gradient elution, petroleum ether Ether - ethyl acetate (50:1) 1 to 21 fractions, petroleum ether - ethyl acetate (20:1) 22 to 55 fractions, petroleum ether - ethyl acetate (10:1) 56 to ...

Embodiment 3

[0046] The extraction of the total lactones of cherimoya, take 2 kilograms of dry seeds of cherimoya, pulverize, percolate twice with ethyl acetate of 10 times the amount of seed powder, detect with silica gel thin-layer chromatography, the cherimolides are nearly extracted completely, in The concentrate was recovered under reduced pressure below 60°C, left to stand for 24 hours, centrifuged at 3000 revolutions per minute, and then the supernatant concentrate (76.8g) obtained by centrifugation was taken, that is, the crude extract of total lactones of cherimoya.

[0047] Take 75g of the crude extract of total lactones of custard apple, add 5 times the amount of petroleum ether-water (1:1), heat and dissolve in a water bath at 50°C, mix well, and after standing for layers, absorb the upper petroleum ether layer and concentrate , dried, and the above operation was repeated once to obtain 41 g of total lactones of custard apple.

[0048] Get 40g of the above-mentioned total lacto...

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Abstract

The invention relates to a refined sweetsop total lactone for anticancer and a method for preparing the same. The method comprises that: Root, leaf and bark or seed of sweetsop are used as raw materials, are percolated and extracted by petroleum ether, chloroform, and acetic ether, or a mixed solution of the petroleum ether, the chloroform and acetic ether, or the raw materials are extracted by supercritical carbon dioxide; the raw materials adopts solvent method, namely the raw materials are heated and dissolved by the petroleum ether and are subjected to impurity removal to obtain sweetsop total lactone; and the sweetsop total lactone is subjected to silica gel column chromatography, is subjected to gradient elution by the petroleum ether-the acetic ether or the chloroform-methanol, and is separated and is refined to obtain the sweetsop total lactone taking Shikemoxin and valeric sweetsop as main compositions. The raw materials have rich sources, low price and availability; the obtained refined sweetsop total lactone has high content, clear compositions and controllable quality; and the preparation method has a simple process, low consumption and high yield, and can realize large industrialized production.

Description

technical field [0001] The invention relates to a plant extract, in particular to a refined total lactone of anemone apple, its preparation method and its application in the preparation of antitumor drugs. Background technique [0002] Annonaceae lactones are a class of natural compounds extracted and isolated from Annonaceae plants. Annonaceae lactones have a wide range of biological activities, the most typical ones are insecticidal and anti-tumor cell activities. Studies have shown that annonaceae lactones It has strong tumor cytotoxicity in vivo and in vitro, and shows good biological activity against a variety of tumor cells. Studies have shown that the mechanism of anti-tumor activity of anemone lactone is by blocking the three-dimensional NADH oxidoreductase, thereby preventing respiration The transfer of chain electrons inhibits the generation of ATP in tumor cells and causes tumor cells to die due to starvation. Its mechanism of action is unique and different from t...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61P35/00A61K31/365A61K125/00A61K127/00A61K129/00A61K131/00
Inventor 李祥杨海军陈建伟
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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