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Sugar apple lactone high-efficiency position medicine-Ainuoning, preparation method and application thereof

A technology of annona lactone and effective parts, which is applied in the field of high-efficiency parts of annona lactone, can solve problems such as difficult large-scale production, waste, and damage to human health, and achieves simple and easy-to-implement preparation methods, human health and safety, and The effect of little environmental pollution

Inactive Publication Date: 2008-12-10
杨芃 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In China, it has been proposed to prepare antineoplastic, antineoplastic and antineoplastic drugs with total lactones (CN1224016A), part drugs (CN1370530), cinnamon (i.e. skemosin, CN1544423), bratasine (CN1460473) and extracts (CN1739586). Pesticides and anti-HIV infection / AIDS drugs, but they all exist or the ingredients are too complex, contain a large number of low-active ingredients, it is difficult to control the quality and efficacy of the drugs; Another component with high content and high biological activity is wasted; or the separation method is complicated and cumbersome; or the use of chloroform, dichloromethane, ethyl acetate, n-hexane, etc. is harmful to human health, pollutes the environment, damages the ozone layer, and the high price leads to cost Significantly increased organic solvents; or using a large proportion of silica gel as a carrier, the cycle of chromatographic separation is longer, and it is difficult to achieve large-scale production.
In addition, due to the extremely strong biological activity, problems such as drug preparation and drug safety are currently research difficulties at home and abroad.

Method used

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  • Sugar apple lactone high-efficiency position medicine-Ainuoning, preparation method and application thereof
  • Sugar apple lactone high-efficiency position medicine-Ainuoning, preparation method and application thereof
  • Sugar apple lactone high-efficiency position medicine-Ainuoning, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]Preparation of total lactones of custard apple seeds: take 4 kg of custard apple seeds washed and dried in advance, crush them into coarse powder, place them in a percolator with 6000 ml of 95%-98% alcohol added in advance, soak, and the time can be determined according to the outside temperature Change adjustment. Usually after 48 hours, leachate starts to be released, and about 12000ml of leachate is collected and combined. Recover the solvent under reduced pressure until there is no alcohol in the residue, cool slightly, add 1000ml of petroleum ether to dissolve and place it, and remove the precipitated brown-black massive precipitate; add 500ml of water to remove a small amount of saponin. The petroleum ether layer is concentrated and recovered to obtain the crude lactone of the custard apple seed. The crude lactone contains a large number of biogenic precursor compounds of the annona lactone without a lactone ring and a tetrahydrofuran ring structure and with very l...

Embodiment 2

[0026] The preparation of the total lactones of custard apple seeds: 4 kg of custard apple seeds washed and dried are ground into phase powder, placed in a percolator with 6000 ml of acetone-water (V / V, 90: 10) mixed solution added in advance, soaked , the time can be adjusted according to temperature changes. Usually after 48 hours, the leachate starts to be released, collect and combine about 12000ml of the leachate, recover the solvent under reduced pressure until there is no acetone, place it, remove the precipitated black lumps, add 1000ml of petroleum ether, remove the water layer, and recover under reduced pressure until there is no acetone. Petroleum ether is distilled off to obtain the crude lactone of custard apple seeds. The crude lactones were dissolved and extracted three times with 1000ml of 85% alcohol, and the alcohol layers were combined, recovered until there was no alcohol, placed and dried to obtain 148g of total lactones of the custard apple seeds.

Embodiment 3

[0028] Preparation of the effective part of anemone lactone: the total lactones of the anemone apple seed still contain a large amount of low-activity monotetrahydrofuran type anemone lactone and the secondary degradation products of anemone lactone in the plant, which must be removed. 150 g of total lactones obtained from 4 kg of raw materials in Example 1 were fully mixed with 225 g of 200-300 mesh silica gel and dried in the air; another 375 g of 200-300 mesh silica gel was dry-packed into a column, and the mixed sample silica gel was placed on the top of the column. Sequentially use the mixed solution of acetone-petroleum ether V / V (ml number): 5:95 (5000ml), 7:93 (10000ml), 10:90 (10000ml), 12:88 (10000ml), 15:85 ( 10000ml), 20:80 (5000ml), 30:70 (5000ml) elution, each receiving 1000ml. Combine the fractions (20-37) containing blatacin and scromosin under the guidance of TCL to obtain 40.5 g of the effective fraction of anemone lactone.

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Abstract

The present invention discloses a highly effective annonaceous acetogenins part medicine-idarubicin hydrochloride for injection, the preparation method and application thereof. The principal ingredient comprises alpha, beta-unsaturation gamma-double tetrahydrofuran loop type annonaceous acetogenins compound with lactone structure -bullatacin and shikemoxin. The ingredients of the type account for 90 percent or above of the total mass number. The preparation method of the present invention causes little environmental pollution, is simple and can be easily implemented. Large scale production can be realized. The highly effective annonaceous acetogenins part medicine-idarubicin hydrochloride for injection presented by the invention can be used for preparing medicines for curing malignant tumor, HIV infect / AIDS, resembling rheumatism, psoriasis and lupus erythematosus autoimmune disease. In the preliminary clinical test of treating malignancy, and HIV infect / AIDS, the idarubicin hydrochloride for injection shows the predominance beyond compare of the Chinese and Western medicine medication.

Description

technical field [0001] The present invention relates to a high-efficiency part medicine of Annona squamosa L., an annonaceous acetogenins (Annonins), which is prepared from the seeds of the tropical plant Annona squamosa L. Medicine-the preparation method of Ainuoning and its medicinal use. Background technique [0002] Annonaceous acetogenins (Annonaceous acetogenins) are a class of natural compounds similar to long-chain fatty acids with α, β-unsaturated γ-lactone rings and 1-3 tetrahydrofuran ring structures. found in plants. Since the mid-1980s, about 400 such compounds have been discovered, and they have attracted increasing attention due to their strong biological activities such as anti-tumor, insecticide, and inhibition of HIV and SIV. Due to the similar structure and properties, and a large number of anemone lactone compounds often coexist in a plant, their biological activity, content in plants, and difficulty of separation and purification are very different, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K36/185A61P35/00A61P31/18A61P29/00A61P17/06A61P37/02A61K131/00
Inventor 杨仁洲李远桂
Owner 杨芃
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