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Research on antitumor mechanism of Combretastatin A-4 derivative

A technology of combretastatin and derivatives, applied in the field of analysis of tumor vascular endothelial cell migration mechanism

Inactive Publication Date: 2017-05-31
CHINA PHARM UNIV
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

For most tumors, due to their uncontrolled proliferation, the existing vascular system is difficult to meet the normal supply of nutrients and oxygen, and the metabolites continue to accumulate. Therefore, tumor cells can up-regulate some factors that promote the migration of vascular endothelial cells: vascular endothelial growth factor (VEGF ), Src kinase, focal adhesion kinase (FAK), and paxillin are activated to promote the migration of endothelial cells into tumor tissue to form blood vessels
However, there is no report on the migration mechanism of CPU-TX-008 on human umbilical vein endothelial cells

Method used

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  • Research on antitumor mechanism of Combretastatin A-4 derivative
  • Research on antitumor mechanism of Combretastatin A-4 derivative
  • Research on antitumor mechanism of Combretastatin A-4 derivative

Examples

Experimental program
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Effect test

Embodiment

[0014] The drug CPU-XT-008 was administered to human umbilical vein endothelial cells (HUVECs), and its anti-HUVECs proliferation activity was detected by MTT method, and the optimal concentration was obtained:

[0015] HUVECs were inoculated in 96-well culture plates, and after synchronization, the cells were divided into a blank group (DMEM medium without serum), a model group (DMEM medium with 10% neonatal bovine serum), a positive control group, and an administration group. The positive control group was 10 μmol / L CA-4, the administration group was 0.01, 0.1, 1, 10 μmol / L CPU-XT-008 respectively, the positive control group and the administration group both used 10% newborn calf serum DMEM medium, continued Cultivate for 24h. Add 20 μL of 5 mg / mL MTT solution to each well, and incubate at 37° C. for 4 h. After the culture solution was aspirated, 150 μL of DMSO was added to each well to dissolve the crystals, and the absorbance of each well was measured at 562 nm after shak...

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Abstract

The invention discloses and relates to the field of biomedicine, in particular to inhibition of Src-FAK (Src focal adhesion kinase) signal pathways by Combretastatin A-4 derivative CPU-TX-008 to inhibit VEGF-induced (vascular endothelial growth factor induced) migration of vascular endothelial cells. As a CA-4 (Combretastatin A-4) derivative, CPU-TX-008 is acquired by replacing hydroxy of CA-4 structure with more water-soluble glucosamine groups. In-vitro cell experiments show that the derivative plays a role in inhibiting the migration of HUVECs (human umbilical vein endothelial cells); it is discovered through the research on the influence of related migrated proteins Src and FAK that CPU-TX-008 inhibits cell migration by inhibiting the phosphorylation of Src and FAK proteins in HUVECs, finally inhibiting the growth of tumor vessels; by adding chemical groups to CA-4 to prepare tumor vessel inhibitory drugs, new clinical antitumor paths are provided.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the analysis of the migration mechanism of tumor vascular endothelial cells induced by VEGF by combretastatin A-4 derivative CPU-TX-008. [0002] The invention relates to the field of biomedicine, in particular to the analysis of the migration mechanism of tumor vascular endothelial cells induced by VEGF by combretastatin A-4 derivative CPU-TX-008. Background technique [0003] Angiogenesis is a highly regulated process, and in mature mammalian organisms, physiological angiogenesis occurs only in the ovary, uterus and placenta, and in other tissues the turnover rate of vascular endothelial cells is quite low. For most tumors, due to their uncontrolled proliferation, the existing vascular system is difficult to meet the normal supply of nutrients and oxygen, and the metabolites continue to accumulate. Therefore, tumor cells can up-regulate some factors that promote the migration of vasc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P35/00
CPCA61K31/7034
Inventor 何书英黄青林吴纲
Owner CHINA PHARM UNIV
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