Isolicoflavonol-containing antitumor drug and application thereof

A technology of isoflavonol and antitumor drug, applied in the preparation of antitumor drugs, the field of preparation of active component isoflavonol, can solve the problem of not finding active components, affecting the industrialization development of antitumor drugs and the Application effect and other issues, to achieve the effect of improving bioavailability, low cost, and increasing drug absorption

Active Publication Date: 2015-04-22
BIOLOGY INST OF SHANDONG ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current natural source of active ingredient extracts with anti-cancer function is still in the stage of experimental exploration, and the public reports are limited to the separation and testing of ingredients in the laboratory, and no information about the natural source of active ingredients that can be produced on a large scale to report
It has affected the industrial development and application effect of antineoplastic drugs containing active ingredients from natural sources

Method used

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  • Isolicoflavonol-containing antitumor drug and application thereof
  • Isolicoflavonol-containing antitumor drug and application thereof
  • Isolicoflavonol-containing antitumor drug and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] 5kg of licorice sample was crushed and extracted with 10 times the amount of 95% ethanol at 50°C for 3 times, each time for 4 hours. The extract was filtered, concentrated under reduced pressure to reclaim the solvent, diluted with 15 times the amount of 20% ethanol in an appropriate amount, and after degreasing with petroleum ether, put it on a polyamide column for separation. % methanol was eluted until the effluent was colorless, and then 40% methanol was used for elution, and the eluate from 3 to 6 column volumes was collected, concentrated to remove the solvent, and subjected to silica gel column chromatography, chloroform-methanol (3 :1, v / v) for elution, the eluate is then separated by Sephadex L H-20 gel chromatographic column, eluted with methanol, the first color band is collected, the eluate is collected, concentrated, crystallized, micronized Chemical treatment to obtain isolicorice flavonol with a median particle size of ≤100 μm; the purity was 98.0%, and t...

Embodiment 2

[0056] 8 kg of licorice samples were crushed, and 5 times the amount of 75% ethanol was extracted at 80°C for 3 times, each time for 2 h. The extract was filtered, concentrated under reduced pressure to recover the solvent, diluted with 5 times the amount of 10% ethanol in an appropriate amount, degreased with petroleum ether, and separated on a polyamide column. The sample volume was 4BV, and the sample flow rate was 4BV / h. % Methanol was eluted until the effluent was colorless, then eluted with 50% Methanol, and the eluate from 3 to 6 column volumes was collected, concentrated to remove the solvent, and subjected to silica gel column chromatography, dichloromethane-ethanol (4:1, v / v) for elution, the eluate is then separated by Sephadex L H-20 gel chromatography column, eluted with methanol, the first color band is collected, the eluate is collected, concentrated, and crystallized , Micronized treatment, to obtain isoliquiritic flavonol with a median particle size of ≤100 μm...

Embodiment 3

[0058] 10kg of licorice sample was crushed and extracted 3 times with 8 times the amount of 60% ethanol at 70°C for 2 hours each time. The extract was filtered, concentrated under reduced pressure to recover the solvent, diluted with 10 times the amount of 5% ethanol in an appropriate amount, degreased with petroleum ether, and separated on a polyamide column. The sample volume was 2BV, and the sample flow rate was 5BV / h. % Methanol was eluted until the effluent was colorless, and then eluted with 60% methanol, and the eluate from 3 to 6 column volumes was collected, concentrated to remove the solvent, and subjected to silica gel column chromatography, dichloromethane-methanol (5:1, v / v) for elution, the eluate is then separated by Sephadex L H-20 gel chromatography column, eluted with ethanol, the first color band is collected, the eluate is collected, concentrated, and crystallized After micronization treatment, Islicorice flavonol with a median particle size of ≤100 μm was ...

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Abstract

The invention develops new application of isolicoflavonol. The inventor carries out a large amount of component sieving, pharmacological experiments and antitumor effect comparison to finally confirm that the isolicoflavonol derived from liquorice as a traditional Chinese medicinal herb has the function of inhibiting the generation of new vessels and the obvious function of inhibiting the generation of endothelial growth factors of tumor vessels, can achieve the purpose of resisting tumors by inhibiting the generation of new tumor vessels, and is a natural-source active component compound with development values for an antitumor medicament. The antitumor medicament provided in the invention is processed and prepared into the mixed-suspension type injection, the tablet and the microcapsule by combining the isolicoflavonol as a chemical component with pharmaceutically acceptable auxiliary materials and carriers. The antitumor medicament can be used for preventing and curing breast cancers, ovarian cancers, cervical cancers, colorectal cancers as well as common gastrointestinal tract cancers, lung cancers, kidney cancers, bladder cancers, prostate cancers, skin cancers, head and neck cancers, brain cancers or leukemia.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to an antineoplastic drug containing isolicorice flavonol and its application, and relates to a preparation method of an active component isolicorice flavonol and its application in the preparation of an antineoplastic drug. Background technique [0002] Angiogenesis is considered an absolute requirement for the growth of tumors larger than 1-2mm. In tumors smaller than this limit, oxygen and nutrients can be delivered to the cells by diffusion. However, when a certain size is reached, each tumor is dependent on angiogenesis in order to continue growing. Tumor-initiating cells in hypoxic areas respond by stimulating vascular endothelial growth factor (VEGF) production, which causes activation of quiescent endothelial cells to stimulate new blood vessel formation. Furthermore, VEGF in tumor areas without any angiogenesis can proceed through the ras signaling pathway. In situ hybridization ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00A61P35/04A61P35/02C07D311/30C07D311/40
Inventor 刘可春韩利文袁延强何秋霞王思峰陈锡强王雪楚杰侯海荣王希敏彭维兵
Owner BIOLOGY INST OF SHANDONG ACAD OF SCI
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