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Benzoquinone compound and use thereof for preparing anti-tumour drug

A technology of anti-tumor drugs and compounds, applied in anti-tumor drugs, drug combinations, organic chemistry, etc., can solve the problem of affecting tumor cell metabolism, proliferation and differentiation, no anti-tumor effect of benzoquinone compounds, anti-tumor drugs, hindering tumor cells. cell growth and other issues

Inactive Publication Date: 2013-05-22
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is also reported that natural shikonin compounds and their derivatives have cytotoxicity and anti-tumor activity mainly because shikonin can induce tumor cell apoptosis by activating caspase protease, activate mitogen-activated protein kinase ( mitogen-activated protein kinase), inhibit the activity of protein tyrosine kinase and DNA topoisomerase I, thereby affecting the metabolism, proliferation, differentiation, signal transmission, gene expression and other processes of tumor cells, thereby hindering the growth of tumor cells
[0004] It has been reported that the benzoquinone phenolic compounds in Zicao have the effect of inhibiting the biosynthesis of prostaglandins in vitro; taking a comprehensive look at the reports at home and abroad, there is no antitumor drug effect of benzoquinone compounds in Zicao and the antitumor drugs prepared by it. drug

Method used

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  • Benzoquinone compound and use thereof for preparing anti-tumour drug
  • Benzoquinone compound and use thereof for preparing anti-tumour drug

Examples

Experimental program
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Effect test

Embodiment 1

[0015] Embodiment 1 prepares shikonin

[0016] Comfrey root coarse powder 20kg, at room temperature with 95% ethanol after repeated cold soaking, percolation and extraction for several times, the solvent was recovered under reduced pressure to obtain 820g of extractum, which was suspended in distilled water and mixed with petroleum ether, ethyl acetate and n-butanol Extraction to obtain 220g of petroleum ether extract, 420g of ethyl acetate extract and 180g of n-butanol extract; 200g of ethyl acetate extract was mixed with silica gel and dried, followed by silica gel column chromatography, followed by petroleum ether, petroleum ether- Acetone and acetone were used for gradient elution to obtain 9 fractions Fr.1-Fr.9; the resulting fraction Fr.6 was subjected to petroleum ether-acetone (8:1, 5:1, 5:2, 2:1) silica gel Column chromatography obtained 4 eluted fractions of Fr.6A~Fr.6D, among which Fr.6C was recrystallized from petroleum ether-acetone to obtain the compound shikonon...

Embodiment 2

[0017] Example 2 In vitro cytotoxicity test

[0018] Four tumor cell lines A549, DU145, KB and its drug-resistant strain (KB-VIN) were cultured in 10% calf serum RPMI1640 containing 25mM HEPES, 0.2% (w / v) sodium bicarbonate and 100μg / ml kanamycin Liquid 4ml in a 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 test compound samples 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 562nm. ED 50 The drug concentration at the time of half cell growth inhibition was converted according to the dose-effect data. Each experiment was repeated three times with less than 5% difference in absorbance values, ED 50 The difference is less than 30%. to ED 50 ≤20μg / ml is the effective standard....

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Abstract

The invention belongs to the field of pharmacy and relates to a benzoquinone compound and use thereof for preparing an anti-tumour drug, in particular to preparation of Arnebinone B and use thereof for resisting lung cancer, prostatic cancer and nasopharynx cancer. The benzoquinone compound provided by the invention is Arnebinone B, which is separated from arnebiae. In-vitro anti-tumour activity experimental results show that the median inhibitory concentration of Arnebinone B on lung carcinoma cell A549 is 4.86 mu g / ml, the median inhibitory concentration of Arnebinone B on prostate cancer cell DU145 is 5.16 mu g / ml, the median inhibitory concentration of Arnebinone B on nasopharyngeal carcinoma cell KB is 5.2 mu g / ml, and the median inhibitory concentration of Arnebinone B on KB drug-resistant strain KB-VIN is 4.98 mu g / ml. The result shows that Arnebinone B can be used for preparing the anti-tumour drug, in particular drugs for treating lung cancer, prostatic cancer and nasopharynx cancer.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to benzoquinone compounds and their application in the preparation of antitumor drugs, in particular to the preparation of shikonin B in benzoquinone compounds and its anti-lung cancer, prostate cancer and nasopharyngeal cancer. the use of. Background technique [0002] According to the statistics of the World Health Organization (WH0), there are about 10 million cancer cases worldwide and about 7 million deaths every year. It has become the second killer of human beings after cardiovascular diseases. Finding effective anticancer drugs has become a It is imperative. At present, in the research of anticancer drugs, the research and clinical application of chemotherapy drugs have made great progress; among them, chemically synthesized anticancer drugs such as metal complex platinum complexes, gallium salts, organic germanium compounds, tin complexes, etc. It has the characteristics of strong a...

Claims

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Application Information

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IPC IPC(8): C07D307/77A61K31/343A61P35/00
Inventor 陈道峰朱红薇李国雄
Owner FUDAN UNIV
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