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Compound, preparation method therefor and use of compound

A technology of compounds and anticancer drugs, applied in the field of compounds and their preparation, to achieve the effect of inhibiting cancer cells, inhibiting non-small cell lung cancer, and reducing the content of impurities

Inactive Publication Date: 2017-07-14
XIYUAN HOSPITAL OF CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] (3β,22α,25R)-Spironalkalk-5-enyl-3-O-β-D-glucopyranosyl-(1→2)-O-[β-D-xylopyranosyl- (1→3)]-O-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside has not been disclosed, and there is no reference to the above compounds in the prior art The report on the application in the field of treating cancer diseases has not yet been developed and applied to the clinical treatment of cancer, especially in the treatment of lung cancer. However, the applicant of the present application discovered the above-mentioned compounds during the extraction process of Baiying medicinal materials, and found that they are in The effect is remarkable in the treatment of cancer, especially lung cancer. For this reason, the present invention proposes a compound and its preparation method and its new application in the preparation of anticancer drugs

Method used

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  • Compound, preparation method therefor and use of compound
  • Compound, preparation method therefor and use of compound
  • Compound, preparation method therefor and use of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The preparation method of the compound shown in formula (I) described in the present embodiment, comprises the steps:

[0047]

[0048] (1) Get 10kg of dried whole herb of Baiying, put it in a reflux bottle, add 80L of ethanol aqueous solution with a volume concentration of 70%, and reflux extraction at 100°C for 3 times, each extraction for 2 hours, and carry out the ethanol extract obtained Filter, combine the obtained filtrates and concentrate under reduced pressure to an extract with a relative density of 1.05 (measured at 50°C), add distilled water with 10 times the mass of the extract to the extract for dispersion, filter, and add the obtained filtrate to D151 Ion-exchange macroporous adsorption resin column, then eluted with 3 times column volume of distilled water, 3 times column volume with 95% ethanol aqueous solution, discarded eluent, and then 4 times column volume containing volume The volume concentration of hydrochloric acid with a concentration of 6‰ ...

Embodiment 2

[0061] The preparation method of the compound shown in formula (I) described in the present embodiment, comprises the steps:

[0062](1) Get 10kg of dried whole herb of Baiying, put it in a reflux bottle, add 60L of ethanol aqueous solution with a volume concentration of 65%, and reflux extraction at 90°C for 2 times, each extraction for 4 hours, and the obtained alcohol extract Filter, combine the obtained filtrate and concentrate under reduced pressure to a relative density of 1.05 (50 ° C) extract, add 8 times the extract quality distilled water in the extract to disperse, filter, and add the gained filtrate to D151 ion-exchange macroporous adsorption resin column, followed by 2 times of column volume of distilled water, 4 times of column volume of ethanol solution with a volume concentration of 93%, discarding the eluate flowing out, and then passing through 3 times of column volume containing 93% ethanol solution The volume concentration of hydrochloric acid is 7‰, the vo...

Embodiment 3

[0068] The preparation method of the compound shown in formula (I) described in the present embodiment, comprises the steps:

[0069] (1) Get 10kg of dried whole herb of Baiying, put it in a reflux bottle, add 100L of ethanol solution with a volume concentration of 75%, and reflux extraction at 110°C for 3 times, each extraction for 2 hours, and the obtained alcohol extract Filter, combine the obtained filtrate and concentrate under reduced pressure to a relative density of 1.05 (50 ° C) extract, add 12 times the extract quality distilled water in the extract to disperse, filter, and add the gained filtrate to D151 ion-exchange macroporous adsorption resin column, then through 4 times of column volume distilled water, 2 times of column volume volume concentration is the ethanol solution elution of 97% successively, abandon the eluate flowing out, then pass through 5 times of column volume containing The volume concentration of hydrochloric acid is 5‰, the volume concentration ...

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Abstract

The invention belongs to the field of pharmacochemistry and particularly relates to a compound, a preparation method therefor and use of the compound, i.e., new use and preparation method of (3beta,22alpha,25R)-spirosolan-5-alkenyl-3-O-beta-D-glucopyranosyl-(1 to 2)-O-[beta-D-xylopyranosyl-(1 to 3)]-O-beta-D-glucopyranosyl-(1 to 4)-beta-D-galactopyranoside. The compound can be used for inhibiting lung cancer cells, stagnating a growth cycle of the lung cancer cells at an earlier stage and prompting the apoptosis of the lung cancer cells, so that the compound can be used for preparing anti-cancer drugs, particularly drugs for resisting lung cancers.

Description

technical field [0001] The present invention belongs to the field of medicinal chemistry, and specifically relates to a compound and its preparation method and use, namely (3β,22α,25R)-spirosteralkane-5-enyl-3-O-β-D-glucopyranosyl -(1→2)-O-[β-D-xylopyranosyl-(1→3)]-O-β-D-glucopyranosyl-(1→4)-β-D-pyranosyl Galactoside and its preparation method and use. Background technique [0002] (3β,22α,25R)-Spironalkalk-5-enyl-3-O-β-D-glucopyranosyl-(1→2)-O-[β-D-xylopyranosyl- (1→3)]-O-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside, white powder, insoluble in ethanol and water, the structural formula is as follows: [0003] [0004] (3β,22α,25R)-Spironalkalk-5-enyl-3-O-β-D-glucopyranosyl-(1→2)-O-[β-D-xylopyranosyl- (1→3)]-O-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside has not been disclosed, and there is no reference to the above compounds in the prior art The report on the application in the field of treating cancer diseases has not yet been developed and applied to the clinica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P35/00
CPCC07J71/0005
Inventor 王建农韩林
Owner XIYUAN HOSPITAL OF CHINA ACAD OF CHINESE MEDICAL SCI