Prenylflavanone compound and use thereof in preparation of anti-tumor medicaments

A technology of isopentenyl dihydroflavonoids and antitumor drugs, applied in the field of traditional Chinese medicine pharmacy, can solve the problems of high cost, large toxic and side effects, poor water solubility and the like

Inactive Publication Date: 2011-06-22
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemically synthesized anticancer drugs, such as metal complex platinum complexes, gallium salts, organic germanium compounds, tin complexes, etc., have the characteristics of strong anticancer properties and broad antitumor spectrum, but they also have large toxic and side effects and high cost , Poor water solubility and other defects

Method used

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  • Prenylflavanone compound and use thereof in preparation of anti-tumor medicaments
  • Prenylflavanone compound and use thereof in preparation of anti-tumor medicaments
  • Prenylflavanone compound and use thereof in preparation of anti-tumor medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 prepares bean root flavonoids composition

[0023]Get the mountain bean root medical material (25kg) and extract by percolation with 95% ethanol, and the extract is concentrated under reduced pressure to obtain 4.8kg of extract. Take 1.0kg of extract, suspend in water, extract with petroleum ether, ethyl acetate and n-butanol successively, and concentrate to dryness respectively. Take 200g of the extract from the ethyl acetate part, perform silica gel column chromatography (column specification: 11x85cm, silica gel: 200-300 mesh, 2.0kg), and use petroleum ether-acetone gradient elution, and the obtained fractions are subjected to silica gel column chromatography with different eluents. Column chromatography, the specific steps are as follows:

[0024] 1. The fractions eluted with petroleum ether-acetone (10:1) were chromatographed on a silica gel column with petroleum ether-ethyl acetate (5:1, 2:1) to obtain 4 fractions 1A-1D. Fraction 1A was subjected to...

Embodiment 2

[0026] Example 2 In vitro cytotoxicity test

[0027] Four kinds of tumor cell lines A549, DU145, KB and HCT-8 were prepared in 4 mL T- 25 flask, 37°C, 5% CO 2 cultivated under conditions. The cell suspension digested by trypsin was added to a 96-well plate, and the cell concentration was 0.25-1×10 4 / hole. Tumor cells were added different concentrations of components to be tested and cultured at 37°C for 72 hours, fixed with ice-cold 50% trichloroacetic acid and stained with 0.4% (SRB). After the dye was dissolved, the absorbance was measured at 562 nm. The drug concentration at which half of the cell growth was inhibited (GI 50 ) is converted according to the dose-effect data. Each experiment was repeated three times, and the difference in absorbance value was less than 5%, GI 50 The difference is less than 30%.

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Abstract

The invention belongs to the pharmaceutical field of traditional Chinese medicines and relates to a prenylflavanone compound shown formula 1 and a new use thereof in preparation of anti-tumor medicaments. The flavonoid compound is extracted from a Sophora tonkinensis ethyl acetate part and proved to have stronger inhibition effect for tumor cell lines of lung cancer, prostatic cancer, nasopharyngeal cancer or colorectal cancer through an in vitro cytotoxicity screening test, wherein the compound comprises 5.41-7.19 mu g / mL of GI50 which has the inhibition effect on the cells of the nasopharyngeal cancer, 6.48-7.21 mu g / mL of the GI50 which has the inhibition effect on the cells of the lung cancer, 5.10-5.15 mu g / mL of the GI50 which has the inhibition effect on the cells of the prostatic cancer and 7.52-14.81 mu g / mL of the GI50 which has the inhibition effect on the cells of the colorectal cancer. The compound can be further used for preparing the anti-tumor medicaments for clinical treatment of the lung cancer, the prostatic cancer, the nasopharyngeal cancer or the colorectal cancer.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to new uses of medicines, in particular to a new use of prenyl dihydroflavonoids in the traditional Chinese medicine Bean root in the preparation of antitumor drugs. Background technique [0002] Clinical practice shows that among various diseases, cancer has always been one of the most dreadful diseases threatening human life. According to the data released by the World Health Organization (WHO), in 2005 alone, 7.6 million people died of cancer worldwide. Relevant experts predict that by 2020, the annual number of cancer deaths worldwide will double, and about 84 million people will die of cancer in the next 10 years. Therefore, finding effective anticancer drugs has become a top priority. In the research of anticancer drugs, the research and clinical application of chemotherapy drugs have made great progress. Chemically synthesized anticancer drugs, such as me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P35/00
Inventor 陈道峰何常明李国雄
Owner FUDAN UNIV
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