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Preparation of isopentenyl flavone and application of isopentenyl flavone as medicine for treating cervical cancer

A technology of prenyl flavone and acetone, which is applied in the field of medicine

Active Publication Date: 2021-05-28
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ficus hirta Vahl. is a plant of the genus Ficus moraceae. The research reports on the pharmacological activities of this plant mainly focus on anti-inflammation, antibacterial, anti-oxidation, anti-aging, etc., while the research on the effect of Ficus hirta Vahl on cervical cancer is almost no report

Method used

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  • Preparation of isopentenyl flavone and application of isopentenyl flavone as medicine for treating cervical cancer
  • Preparation of isopentenyl flavone and application of isopentenyl flavone as medicine for treating cervical cancer
  • Preparation of isopentenyl flavone and application of isopentenyl flavone as medicine for treating cervical cancer

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1: Preparation and structural identification of prenylflavones involved in the present invention

[0026] 1. Preparation of compound:

[0027] 1) Pulverize the rhizome of Prunus chinensis, add 8 times the amount of 10% ethanol solvent to reflux and extract for 3 times, and the extraction time is 3 hours each time, combine the extracts, filter, and concentrate under reduced pressure to obtain a concentrate.

[0028] 2) Suspend the concentrate obtained in step 1) with water, then go through macroporous adsorption resin column chromatography, and then select ethanol-water (0:100, 30:70, 40:60, 60:40, 95:5) Gradient elution was carried out, the eluate was collected, and concentrated under reduced pressure to obtain a concentrated solution containing prenyl flavone.

[0029] 3) The concentrated solution containing prenyl flavones is eluted with a mixed solvent of dichloromethane-methanol (100:0, 95:5, 9:1, 8:2, 7:3) through silica gel column chromatography , to obt...

Embodiment 2

[0034] Embodiment 2: the preparation of prenyl flavone involved in the present invention

[0035] 1) Pulverize the rhizome of Prunus chinensis, add 10 times the amount of 60% ethanol solvent to reflux and extract twice, and the extraction time is 2 hours each time, combine the extracts, filter, and concentrate under reduced pressure to obtain a concentrate.

[0036] 2) Suspend the concentrate obtained in step 1) with water, and then go through macroporous adsorption resin column chromatography, and then use ethanol-water (0:100, 30:70, 60:40, 95:5) for gradient elution , collect the eluate, concentrate under reduced pressure to obtain a concentrated solution containing prenyl flavone.

[0037] 3) Pass the concentrated solution containing prenyl flavone through silica gel column chromatography, cyclohexane-ethyl acetate (100: 0, 95: 5, 9: 1, 8: 2, 7: 3, 6: 4 ) mixed solvent for elution to obtain 8 fractions.

[0038] 4) The fourth fraction obtained in step 3) was subjected to...

Embodiment 3

[0040] Embodiment 3: the preparation of prenylflavone involved in the present invention

[0041] Compound preparation:

[0042] 1) Pulverize the rhizome of Prunus chinensis, add 15 times the amount of 95% ethanol solvent to reflux and extract twice, and the extraction time is 1 hour each time, combine the extracts, filter, and concentrate under reduced pressure to obtain a concentrate.

[0043]2) Suspend the concentrate obtained in step 1) with water, then undergo macroporous adsorption resin column chromatography, and then use ethanol-water (0:100, 60:40, 95:5) for gradient elution, and collect the eluted liquid, concentrated under reduced pressure to obtain a concentrated solution containing prenyl flavones.

[0044] 3) Pass the concentrated solution containing prenyl flavones through silica gel column chromatography, petroleum ether-ethyl acetate (100: 0, 95: 5, 9: 1, 8: 2, 7: 3, 6: 4, 1:1) and 10 fractions were obtained.

[0045] 4) The fifth fraction obtained in step 3...

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Abstract

The invention discloses preparation of isopentenyl flavone and application of isopentenyl flavone as a drug for treating cervical cancer, and relates to the technical field of drugs. The isopentenyl flavone is obtained by adopting dry rhizomes of ficus microcarpa plant radix fici simplicissimae through the steps of crushing, solvent extraction, macroporous adsorption resin column chromatography, silica gel column chromatography, ODS column chromatography, liquid phase preparation and the like. Pharmacological activity shows that the isopentenyl flavone compound can obviously inhibit proliferation of human cervical cancer cell strains, influence AKT / MAPK signal channels and promote apoptosis of cervical cancer cells, and the isopentenyl flavone compound has an anti-cervical cancer effect, can be used as a candidate drug for development of anti-cervical cancer drugs and has important significance in development of the anti-cervical cancer drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the preparation of a prenyl flavone and its application as a medicine for treating cervical cancer. Background technique [0002] The results of cancer censuses in recent years show that the incidence of cancer has shown an obvious upward trend. Among them, cervical cancer is a common malignant tumor in women, which seriously threatens the health of women all over the world. According to research statistics, among female malignant tumors, the incidence of cervical cancer is second only to breast cancer (Torre LA, Bray F, Siegel RL, et al. Global cancer statistics, 2012 [J]. CA Cancer J Clin, 2015, 65 (2):87-108.). The drugs currently used for the treatment of cervical cancer generally have drug resistance and serious side effects. [0003] Traditional Chinese medicine plays an important role in the treatment of various diseases. Due to its rich resources and various structure...

Claims

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Application Information

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IPC IPC(8): C07D311/30A61K31/352A61P35/00
CPCC07D311/30A61K31/352A61P35/00Y02A50/30
Inventor 陈海峰姚新生田文静王光辉林挺叶贤胜
Owner XIAMEN UNIV
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