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Internal ester monomer compound and its application in preparing anti cancer medicine

A compound and technology for the treatment of liver cancer, applied in the fields of drug combination, anti-tumor drugs, organic chemistry, etc., can solve the problems of unsatisfactory curative effect, low cancer curative effect, large toxic and side effects, etc., and achieve the effect of improving the clinical curative effect of anti-cancer

Inactive Publication Date: 2009-08-19
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although chemotherapeutic drugs have a certain effect on cancer, they have large toxic and side effects. The curative effect of Chinese patent medicines on cancer is generally low. For example, the remission rate of ginseng and lotus jelly on lung and gastric cancer is only 3.5%, and the curative effect is not ideal.

Method used

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  • Internal ester monomer compound and its application in preparing anti cancer medicine
  • Internal ester monomer compound and its application in preparing anti cancer medicine
  • Internal ester monomer compound and its application in preparing anti cancer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1: A kind of anticancer drug anemone lactone monomer compound (expoxyrolin B) extraction method

[0013] An anticancer drug annonaceous lactone monomer compound, which is an anticancer monomer compound extracted from cherimoya seeds. Its preparation method is that after the custard apple seeds are air-dried, they are crushed into coarse powder, and first cold-extracted with 10 times the amount of petroleum ether (at room temperature) for 3 times (at room temperature), each time for 2 days; the petroleum ether is recovered to obtain a red oily liquid, which is placed at room temperature, and there is a large amount of The white precipitate is separated out, and the white precipitate is filtered out, and the white precipitate is subjected to repeated silica gel column chromatography; with sherwood oil, sherwood oil-ethyl acetate, ethyl acetate-methanol gradient elution, a kind of annonaceous lactone monomer compound ( expoxyrolin B).

Embodiment 2

[0014] Embodiment 2: a kind of anticancer medicine annona lactone monomer compound, it is characterized in that white powdery material, easily soluble in organic solvents such as ethyl acetate, methyl alcohol, chloroform. It is identified as expoxyrolin B with molecular formula C 36 h 66 o 3 , the chemical structural formula is as follows:

[0015]

Embodiment 3

[0016] Embodiment 3: the inhibitory action of a kind of anemone lactone monomer compound (expoxyrolin B) to human liver cancer cell

[0017] 1. Cell culture:

[0018] SMMC-7721 or HepG2 cell lines were inoculated in culture flasks, and RPMI-1640 culture solution (containing 10% calf serum, penicillin 100u / ml, streptomycin 100ug / ml) was added, and the cells were incubated at 37°C and 5% CO 2 Cultured in an incubator, the cells grow in a single layer adherent to the wall, passaged every 3 to 5 days, digested with 0.25% trypsin for 3 minutes, blown with the culture medium to make a cell suspension, and then inoculated.

[0019] 2. Drug treatment

[0020] Cells in the logarithmic growth phase were divided into 2×10 5 / ml inoculated in a cell culture flask, and after the cells were completely adhered to the wall (about 4 hours), the culture medium containing the drug was added and cultured for a predetermined time. The experimental drug is an anemone lactone monomer compound (ex...

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Abstract

An anticancer drug anemone lactone monomer compound, which is the anticancer lactone monomer compound expoxyrolin B extracted from the seeds of anemone apple. Its preparation method is that after the custard apple seeds are air-dried, they are crushed into coarse powder, and firstly extracted with petroleum ether cold immersion; the petroleum ether is recovered to obtain a red oily liquid, which is placed at room temperature, and a large amount of white precipitate is precipitated at the bottom, and the white precipitate is filtered out. Silica gel column chromatography; using petroleum ether, petroleum ether-ethyl acetate, ethyl acetate-methanol gradient elution, to obtain a kind of anemone lactone monomer compound. According to in vivo and in vitro anticancer pharmacological experiments, it has obvious inhibitory effect on the growth of human liver cancer cells and transplanted liver cancer in mice, and its anticancer activity is several times higher than that of chemotherapeutic drug 5-fluorouracil.

Description

1. Technical field [0001] The invention relates to an anticancer drug, in particular to an anemone lactone monomer compound extracted from cherimoya seeds as a raw material and its application in the preparation of an anticancer drug. 2. Background technology [0002] Cancer is a formidable enemy that endangers human health. There are about 1.6 million new cases of cancer in my country every year, and about 1.3 million people die of cancer every year. The number of deaths due to cancer in the country is increasing year by year. my country has a high incidence of liver cancer, gastric cancer, esophageal cancer, breast cancer, and lung cancer. The region has a high cancer mortality rate. [0003] There are currently no effective drugs that cure most cancer patients. Although chemotherapeutic drugs have a certain effect on cancer, they have large toxic and side effects. The curative effect of Chinese patent medicines on cancer is generally low. For example, the remission rate ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D407/06A61K31/365A61P35/00
Inventor 章永红李祥
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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