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Alkaloid with anticancer activity and preparation method and application thereof

A technology of anti-cancer activity and alkaloids, applied in the field of alkaloids, can solve the problems of unsatisfactory tumor chemotherapy and toxic and side effects, and achieve good windproof and sand-fixing effects

Inactive Publication Date: 2011-02-02
BEIFANG UNIV OF NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, traditional antitumor drugs lack selectivity to cancer cells and normal cells, thus producing many serious toxic and side effects, so tumor chemotherapy is far from ideal

Method used

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  • Alkaloid with anticancer activity and preparation method and application thereof
  • Alkaloid with anticancer activity and preparation method and application thereof
  • Alkaloid with anticancer activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A method for preparing an alkaloid active site with anticancer activity, comprising the steps of:

[0027] a. Take the aboveground part of the old melon head plant and cut it into sections with a width of 0.5 cm, soak it with methanol, the soaking temperature is 20 ° C, and the soaking time is 240 hours, and the extract is ready for use;

[0028] b. Concentrate the extract under reduced pressure at 20°C to a density of 1.2g / mL, wash with hydrochloric acid with a concentration of 1.5% by volume, extract the wash with ethyl acetate until there is no alkaloid positive reaction, and store the extract at 20°C Concentrate under reduced pressure to a density of 1.20 g / mL, and the concentrated solution is precipitated for 72 hours, and the precipitated part is the alkaloid active site.

[0029] It has been proved by experiments that chlorinated alkanes or toluene can be used instead of ethyl acetate for extraction.

Embodiment 2

[0031] A method for preparing an alkaloid active site with anticancer activity, comprising the steps of:

[0032] a. Take the aboveground part of the old melon head plant and cut it into sections with a width of 0.8 cm, soak it with ethanol, the soaking temperature is 60 ° C, and the soaking time is 96 hours, and the extract is ready for use;

[0033] c. Concentrate the extract under reduced pressure at 50°C to a density of 1.25g / mL, then separate it by silica gel column chromatography, chloroform-methanol 10:0 to 5:5, combined chloroform-methanol 9:1 to 6:4 The part is the alkaloid active site.

Embodiment 3

[0035] A method for preparing an alkaloid active site with anticancer activity, comprising the steps of:

[0036] a, take the section of the aboveground part of the old melon head plant, the width is 1 cm, soak with ethanol and acetone with a volume ratio of 1:1, the soaking temperature is 100 ° C, the soaking time is 12 hours, and the extract is ready for use;

[0037] c. Separation and purification with weakly polar macroporous adsorption resin, specifically using any one of the GDX series, pass the concentrated solution through weakly polar macroporous adsorption resin, elute with distilled water of 5 times the column volume, and then use the volume percentage concentration It is eluted with 95% ethanol, and the eluted part is the active part of the alkaloid;

[0038] It has been proved by experiments that any one of the models in XAD series, Diaion series, HPD series, D series, or AB series can be used instead.

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Abstract

The invention relates to an alkaloid with anticancer activity, which is separated from Asclepiadaceae Cynanchum per nnial herb Cynanchum Komarrovii, in particular to the alkaloid with anticancer activity and a preparation method and application thereof. The alkaloid is mainly 3 compounds: Antofine, 14-hydroxyantofine, delta 11,12-antofine, the proportion of the three alkaloids in active sites of alkaloid is 65-80%, and the proportion among the three alkaloids is 35-45%:35-45%:10-25%. The invention provides the phenanthroindolizidine alkaloids with the anticancer activity, and the evaluation of activity by an in vitro antineoplastic activity screening system discovers that the phenanthroindolizidine alkaloids provided by the invention can effectively inhibit the growth of BEL-7402 human hepatoma cells, A549 human lung carcinoma cells and MOLT-4 human leukemia cells. As a wild plant resource, the effects of windbreak and sand fixation of the Cynanchum Komarrovii can be unaffected when in use.

Description

technical field [0001] The invention relates to an alkaloid with anticancer activity isolated from the perennial herb Cynanchum komarrovii of Asclepiadaceae (Asclepiadaceae), especially an alkaloid with anticancer activity and its preparation method and application . Background technique [0002] Tumor is a kind of disease characterized by cell division, cell death, and cell-cell and cell-mechanism interaction serious disorder, which seriously threatens human health and life. The death caused by malignant tumor is second only to cardiovascular and cerebrovascular diseases. Disease is the second leading cause of death in humans. [0003] Tumor treatment methods include surgical treatment, radiotherapy and drug treatment (commonly known as chemotherapy or chemotherapy), etc., but chemotherapy is still the main method to a large extent. Chemotherapy can cure part of the tumor or prolong the patient's life, so anti-tumor drugs play an increasingly important role in the treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/02A61P35/00A61K31/4745C07D471/04A61K36/27
Inventor 杨晋祁利民
Owner BEIFANG UNIV OF NATITIES
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