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Lactone monomer compound and its application in preparing anticancer medicine

A technology of anti-cancer drugs and compounds, applied in anti-tumor drugs, drug combinations, digestive system and other directions, 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: 2006-11-29
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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  • Lactone monomer compound and its application in preparing anticancer medicine
  • Lactone monomer compound and its application in preparing anticancer medicine
  • Lactone monomer compound and its application in preparing anticancer medicine

Examples

Experimental program
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Effect test

Embodiment 1

[0013] Example 1: An extraction method of an anticancer drug desacetyluvaricin monomer compound (desacetyluvaricin) is an anticancer drug desacetyluvaricin 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, refluxed and extracted with 10 times the amount of 95% ethanol for 3 times, each time for 2 hours, concentrated at normal pressure, the extract is suspended in an appropriate amount of water, and sequentially washed with petroleum ether (60~ 90 ℃), water-saturated n-butanol extraction, through repeated silica gel column chromatography, gel column chromatography, high-efficiency preparative liquid chromatography and recrystallization, etc., a kind of anemone lactone monomer compound ( desacetylluvaricin).

Embodiment 2

[0014] Example 2: Annona lactone monomer compound is a white waxy solid, easily soluble in organic solvents such as chloroform and ethyl acetate. It is identified as desacetylluvaricin with the molecular formula C 37 h 66 o 6 , the chemical structure is as follows (R 1 , R 2 , R 3 Both are H, THF-THF rel configuration is threo / trans / threo / trans / erythro):

[0015]

Embodiment 3

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

[0017] 1. Cell culture:

[0018] The HepG2 cell line was inoculated in a culture flask, added RPMI-1640 culture medium (containing 10% calf serum, penicillin 100u / ml, streptomycin 100ug / ml), and incubated at 37°C, 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 (desaeetyluvaricin) identified by che...

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Abstract

A lactone monomer compound used for preparing the medicines to prevent and treat cancer, especially the liver cancer is prepared from soursop seeds through drying, breaking, reflux extracting in alcohol, concentrating, suspending the extract in water, extracting sequentially by petroether, water saturated ethyl acetate and water saturated n-butanol, purifying, and recrystallizing.

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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IPC IPC(8): C07D307/58A61K31/365A61P1/16A61P35/00
Inventor 章永红
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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