Compound separated from spina glandulifera as well as preparation method and application of compound

A compound and the technology of the thorn, which are applied to the compound isolated from the thorn in the thorn and the field of preparation thereof, can solve the problems of no compound isolated from the thorn of the thorn of the thorn, and the preparation method and application of the compound not found in the thorn of the thorn

Active Publication Date: 2021-04-13
贵州中医药大学
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no bibliographical report on the isolated compound 1-3 and its pharmacological activity in Dianchia sinensis at home and abroad, and there is no compound in the present invention. Reports on preparation methods and applications

Method used

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  • Compound separated from spina glandulifera as well as preparation method and application of compound
  • Compound separated from spina glandulifera as well as preparation method and application of compound
  • Compound separated from spina glandulifera as well as preparation method and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 2-Arylbenzo[b]furan compounds isolated from Rat pratense, the structural formula of which is:

[0041]

[0042] Preparation:

[0043] 1) Take 18Kg of dried and pulverized medicinal material powder, soak and extract with 4 times the amount of 95% ethanol at room temperature, and extract three times for 7 days each time.

[0044] 2) After the extraction, the extracts were combined and concentrated under reduced pressure (55°C; 0.08Mpa) to obtain 1.25Kg of crude extract.

[0045] 3) Disperse the total extract into 12L of water, extract with petroleum ether (4×24L), ethyl acetate (4×24L) and n-butanol (4×24L) sequentially, combine the extracts respectively, and concentrate under reduced pressure to remove the solvent 110.4 g of petroleum ether, 180.5 g of ethyl acetate and 210.6 g of n-butanol were obtained.

[0046] 4) The ethyl acetate part was taken, separated by silica gel column chromatography, and eluted with petroleum ether / ethyl acetate gradient (50:1→1:1, v / v)...

Embodiment 2

[0051] 2-Arylbenzo[b]furan compounds isolated from Rat pratense, the structural formula of which is:

[0052]

[0053] Preparation:

[0054] 1) Take 15Kg of dried and pulverized medicinal material powder, soak and extract with ethanol at room temperature, and extract twice, each time for 10 days;

[0055] 2) After the extraction is completed, the extracts are combined and concentrated under reduced pressure (55°C; 0.08Mpa) to obtain a crude extract;

[0056] 3) Disperse the total extract into 12L of water, and then extract 6 times with 18L of petroleum ether, 18L of ethyl acetate, extract 6 times and 18L of n-butanol, extract 6 times; after combining the extracts respectively, concentrate under reduced pressure to remove the solvent to obtain petroleum ether site, ethyl acetate site and n-butanol site;

[0057] 4) Take the ethyl acetate fraction, separate it by silica gel column chromatography, and elute with a gradient ratio of 50:1→1:1, v / v petroleum ether / ethyl acetate...

Embodiment 3

[0062] 2-Arylbenzo[b]furan compounds isolated from Rat pratense, the structural formula of which is:

[0063]

[0064] Preparation:

[0065] 1) Take 21Kg of dried and pulverized medicinal material powder, soak and extract with ethanol at room temperature, and extract 4 times, each time for 4 days;

[0066] 2) After the extraction is completed, the extracts are combined and concentrated under reduced pressure (55°C; 0.08Mpa) to obtain a crude extract;

[0067] 3) Disperse the total extract into 12L of water, extract 2 times with 30L of petroleum ether, 30L of ethyl acetate, extract 2 times and 30L of n-butanol, extract 2 times in turn; after combining the extracts respectively, concentrate under reduced pressure to remove the solvent to obtain petroleum ether site, ethyl acetate site and n-butanol site;

[0068] 4) Take the ethyl acetate fraction, separate it by silica gel column chromatography, and elute with a gradient ratio of 50:1→1:1, v / v petroleum ether / ethyl acetate...

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Abstract

The invention relates to the field of pharmaceutical compounds, and in particular relates to a compound separated from spina glandulifera as well as a preparation method and application of the compound. According to the method, systematic and deep chemical component research is mainly carried out on the spina glandulifera, the 2-aryl benzo [b] furan compound 1-4 is separated from the spina glandulifera, and the preparation method of the compound and the application of the compound in preparation of the medicine for treating liver cancer are clarified.

Description

technical field [0001] The present invention relates to the field of pharmaceutical compounds, in particular to a compound isolated from rat thorn and its preparation method and application. Background technique [0002] Liver cancer is one of the common malignant tumors, mainly primary liver cancer. According to reports, there were about 814,000 new cases of primary liver cancer in the world in 2018, ranking sixth among new cases of malignant tumors; 781,000 deaths from liver cancer, ranking fourth in the mortality rate of malignant tumors [1]. At present, surgery and chemotherapy are the main treatment strategies for liver cancer. Among them, surgical treatment is only suitable for a small number of patients with precancerous liver cancer, and is prone to secondary recurrence, with a five-year recurrence rate exceeding 70% [2-3]. For most liver cancer patients, once diagnosed, they are in the advanced stage, and systemic chemotherapy is the main treatment. The current t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/80A61P35/00A61P1/16
CPCC07D307/80A61P35/00A61P1/16
Inventor 罗国勇
Owner 贵州中医药大学
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