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Use of brusatol in preparation of drugs for resisting tumor angiogenesis

A brucea brucea bitter alcohol and anti-tumor technology, which is applied in the field of natural compounds, can solve problems affecting the formation of tumor neovascularization, achieve the effect of controlling the formation of tumor blood vessels, and have a good application prospect

Inactive Publication Date: 2017-04-05
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no literature report on the effect of Brucea brucea on tumor neovascularization by inhibiting the HIF-1 pathway

Method used

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  • Use of brusatol in preparation of drugs for resisting tumor angiogenesis
  • Use of brusatol in preparation of drugs for resisting tumor angiogenesis
  • Use of brusatol in preparation of drugs for resisting tumor angiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Brucea Brucea inhibits HIF-1α protein expression in colon cancer cells

[0026] Human colorectal cancer HCT-116 cells were cultured in DMEM medium containing 10% inactivated fetal bovine serum (Sijiqing), 100 U / mL penicillin and 100 μg / mL streptomycin at 37°C, 5% CO 2 cultivated under conditions. Drug treatment: Brucea brucea was dissolved in DMSO to 15nM, 30nM, 60nM and other 200× different concentrations of the mother solution, and the HCT116 cells were treated after being diluted 200 times with the culture medium according to the final concentration required by the experiment.

[0027] Chemical hypoxia: CoCl 2 Dissolve in triple-distilled water to prepare a 200 μM × 200 mother solution, store in the dark at 4°C, and filter and sterilize with a sterile filter before using the cells.

[0028] Hypoxia (1%O 2 ) treatment: the cells grow to 80% for hypoxic treatment, and the culture condition of the hypoxic workstation is set to be 37°C, 1% O 2 , 5% CO 2 , ...

Embodiment 2

[0031] Example 2 Effect of Brucea Brucea on the Transcriptional Activity of Downstream Target Genes Promoted by HIF-1

[0032] Human lung adenocarcinoma cell A549, breast cancer cell MCF-7, liver cancer HepG2 and cervical cancer Hela cells were cultured in DMEM containing 10% inactivated fetal bovine serum (Sijiqing), 100 U / mL penicillin and 100 μg / mL streptomycin Medium, 37°C, 5% CO 2 cultivated under conditions.

[0033] Drug treatment: Brucea brucea was dissolved in DMSO to 15nM, 30nM, 60nM and other 200× different concentrations of the mother solution. According to the final concentration required by the experiment, it was diluted 200 times with the culture medium to treat A549 and MCF-7 cells.

[0034] Hypoxia (1%O 2 ) treatment: the cells grow to 80% for hypoxic treatment, and the culture condition of the hypoxic workstation is set to be 37°C, 1% O 2 , 5% CO 2, after the hypoxic condition stabilized, the cells were divided into normoxic control group and hypoxic grou...

Embodiment 3

[0037] Example 3 Effect of Brucea Brucea on Inhibiting Colon Cancer Cell HCT116 Vascular Growth Factor (VEGF) and Erythropoietin (EPO) mRNA Expression

[0038] Human colon cancer HCT-116 cells were cultured in 1640 medium containing 10% inactivated fetal bovine serum (Sijiqing), 100 U / mL penicillin and 100 μg / mL streptomycin at 37°C, 5% CO 2 cultivated under conditions.

[0039] Drug treatment: Brucea brucea was dissolved in DMSO to 15nM, 30nM, 60nM and other 200× different concentrations of the mother solution, and the final concentration required by the experiment was diluted 200 times with the culture solution before treatment

[0040] Chemical hypoxia: CoCl 2 Dissolve in triple-distilled water to prepare a 200 μM × 200 mother solution, store in the dark at 4°C, and filter and sterilize with a sterile filter before using the cells.

[0041] Hypoxia (1%O 2 ) treatment: the cells grow to 80% for hypoxic treatment, and the culture condition of the hypoxic workstation is set...

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Abstract

The invention provides a use of brusatol in preparation of drugs for resisting tumor angiogenesis. Brusatol is known as brusatol, CAS No. 14907-98-3 and has a molecular formula of C26H32O11 and molecular weight of 520.54. The brusatol drug can promote degradation of a hypoxia-inducible factor-1 alpha (HIF-1 alpha), inhibit activation of HIF-1 signaling pathway and expression of a vascular endothelial growth factor (VEGF) and effectively inhibit the angiogenesis of tumors, has low toxicity and has a very good clinical application prospect. The brusatol drug comprises a pharmaceutically acceptable drug excipient or carrier. The dosage forms of the brusatol drug mainly comprise enteric or parenteral combined drug dosage forms. The brusatol drug can be processed to form a liquid preparation, granules, tablets, electuary, gelatin pills, capsules, dripping pills or an injection.

Description

[0001] Technical field: [0002] The invention belongs to the use of natural compounds, and relates to the new use of brucea brucea picrol extracted from the traditional Chinese medicine Brucea javanica, in particular to the use of brucea brucea picryl in the preparation of anti-tumor angiogenesis drugs. [0003] Background technique: [0004] During the development of tumors, especially solid tumors, the problem of neovascularization has received great attention. Current studies have confirmed that there is a clear correlation between tumor proliferation and angiogenesis, and it is one of the important targets in tumor therapy. Angiogenesis in tumor tissue is closely related to the activation of HIF-1 pathway. HIF-1 is a member of the bHLH-PAS family of transcription factors, a heterodimer composed of two subunits, oxygen-labile α and stable β. HIF-1 is the most important transcription factor found so far to regulate the expression of multiple genes under hypoxia, and it is ...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P35/00
Inventor 朱俐陆亚鹏王丹赵育王雪婷
Owner NANTONG UNIVERSITY
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