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Novel skeleton meroterpenoid compound and its preparation method, pharmaceutical composition and application in anticancer medicines

A technology of compounds and compositions, applied in the field of medicine

Active Publication Date: 2018-02-09
CHINA JAPAN FRIENDSHIP HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous studies have reported that phloroglucinol is mostly conjugated with monoterpenes or sesquiterpenes, but few conjugates of phloroglucinol and diterpenes

Method used

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  • Novel skeleton meroterpenoid compound and its preparation method, pharmaceutical composition and application in anticancer medicines
  • Novel skeleton meroterpenoid compound and its preparation method, pharmaceutical composition and application in anticancer medicines
  • Novel skeleton meroterpenoid compound and its preparation method, pharmaceutical composition and application in anticancer medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (1) Get 10 kg of dried Euphorbia chamaejascens root, pulverize, add 10 times the amount of 95% ethanol to reflux and extract 3 times, the extraction temperature is preferably 75 ° C, extract for 2 hours each time, combine the extracts, filter, concentrate under reduced pressure, to obtain a concentrate;

[0043] (2) The concentrated solution obtained in (1) was extracted 3 times with ethyl acetate, combined, and the organic solvent was recovered to obtain extract I;

[0044] (3) The extract I was subjected to silica gel column chromatography, and gradient elution was carried out by using an organic reagent, using petroleum ether-ethyl acetate gradient elution (0:1-1:0), and using a silica gel thin-layer plate for detection, Combined into 7 (A-G) fractions; then select E to carry out reversed-phase silica gel column chromatography, methanol-water gradient elution (20:80-100:0), and a total of 5 fractions ( E1-E5) fractions; select EE5 to carry out column chromatography ...

Embodiment 2

[0047] (1) Take 20kg of dry Euphorbia chamaejasmeum roots, crush them, add 10 times the amount of 80% ethanol to reflux and extract for 3 times, the extraction temperature is preferably 70°C, extract for 2.5 hours each time, combine the extracts, filter, concentrate under reduced pressure, to obtain a concentrate;

[0048] (2) The concentrated solution obtained in (1) was extracted 3 times with ethyl acetate, combined, and the organic solvent was recovered to obtain extract I;

[0049] (3) Extract I was subjected to silica gel column chromatography, gradient elution was carried out using organic reagents, petroleum ether-acetone gradient elution (0: 1-1: 0), and detection by silica gel thin-layer plate was combined into 8 (A-H) fractions; then choose F to carry out reverse-phase silica gel column chromatography, methanol-water gradient elution (30:70-100:0), and obtain 7 (F1- F7) Fractions; select F5 to carry out column chromatography through Sephadex LH-20 dextran gel, chlor...

Embodiment 3

[0052] (1) Take 5 kg of dry Euphorbia chamaejasba root, pulverize it, add 12 times the amount of 85% ethanol to reflux and extract 4 times, the extraction temperature is preferably 80 ° C, extract for 2 hours each time, combine the extracts, filter, and concentrate under reduced pressure to obtain Concentrate;

[0053] (2) The concentrated solution obtained in (1) was extracted 3 times with ethyl acetate, combined, and the organic solvent was recovered to obtain extract I;

[0054] (3) Extract I was subjected to silica gel column chromatography, gradient elution was carried out with organic reagents, gradient elution with chloroform-methanol (0: 100-1: 0), and detection by silica gel thin-layer plate was combined into 6 (A-F) fractions; then choose D to carry out reverse-phase silica gel column chromatography, methanol-water gradient elution (10:90-100:0), and obtain 8 (D1-D8) in total by silica gel thin-layer plate detection ) fractions; select D4 to carry out column chromat...

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Abstract

The invention discloses a novel skeleton meroterpenoid compound and its preparation method, pharmaceutical composition and application in anticancer medicines. Abietane-type diterpene and phloroglucinol are connected through an alpha-pyrone unit so that the compound is formed. A pharmacological experiment shows that the compound has significant anti-tumor activity to pancreatic cancer, colon cancer, liver cancer, lung cancer, breast cancer, gastric cancer and esophageal cancer and can be used as an anti-tumor drug in clinical application.

Description

technical field [0001] The invention relates to the technical field of medicine, a class of heteroterpene compounds with a new skeleton, its preparation method, pharmaceutical composition and its clinical antitumor application. Background technique [0002] In recent years, with the deteriorating living environment, aging population and unhealthy lifestyle and other factors, the incidence and mortality of cancer in my country have continued to increase. Cancer has become the "killer" with the highest fatality rate in our country, seriously affecting the health of the people. China's population accounts for about 19.3% of the global population, and the incidence of cancer accounts for 21.8% of the global cancer incidence, which is equal to the average incidence of cancer in the world. Cancer deaths in China account for about 26.9% of global cancer deaths, and the mortality rate is relatively high (CA Cancer J Clin, 2016, 66: 115-132). In my country, the most common cancers ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/16A61K31/37A61K31/675A61K31/454A61K31/475A61P35/00
CPCA61K31/37A61K31/454A61K31/475A61K31/675A61K36/47C07D311/16A61K2300/00
Inventor 张维库续洁琨赫军张佳
Owner CHINA JAPAN FRIENDSHIP HOSPITAL
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