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Application of IC-4 in antiangiogenesis

An IC-4, anti-vascular technology, applied in cardiovascular system diseases, medical preparations containing active ingredients, anti-inflammatory agents, etc. question

Inactive Publication Date: 2012-09-12
UNIVERSITY OF MACAU +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the prior art does not disclose any research data on whether carbamate compounds have anti-angiogenic effects, so it is impossible to know whether there are carbamate compounds with anti-angiogenic effects, let alone know Which specific compounds in carbamate compounds have anti-angiogenesis effect

Method used

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  • Application of IC-4 in antiangiogenesis
  • Application of IC-4 in antiangiogenesis
  • Application of IC-4 in antiangiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] IC-4 inhibits the activity and growth of endothelial cells

[0032] 1. Experimental method:

[0033] XTT method: Take 2-5 generations of human umbilical vein endothelial cells, press 1×10 4 / Well cells are seeded on 96-well plates. After culturing overnight to make the cells adhere to the wall, different concentrations of IC-4 and various growth inducers (including 10% fetal bovine serum FBS, 20ng / ml endothelial cell growth factor EVGF and 20ng / ml epidermal growth factor EGF) were given respectively, and set The 0.1% DMSO control group and the single growth inducer stimulation group have 6 parallel holes in each group. After the cells were cultured for 24h or 48h, they were co-cultured with the cells for 4h using Roche Cell Proliferation Kit II to form water-soluble formazan products. Use Perkin Elmer Multilabel Counter to detect the OD value with 490nm as the detection wavelength and 690nm as the reference wavelength. The experiment was carried out 3 times, the average v...

Embodiment 2

[0037] IC-4 inhibits endothelial cell migration test

[0038] 1. Experimental method:

[0039] Scratch test: Take 2-5 generations of human umbilical vein endothelial cells, press 2×10 5 Cells per well were seeded on a 24-well plate. After the cells were 100% fused, 500μl of normal medium was added to each well of the control group, and 500μl of medium containing different concentrations of IC-4 was added to each well of the administration group for 24h. In this experiment, IC-4 showed no cytotoxicity at the drug concentration. Use a tip with a specification of 100 μl to draw a straight line in the center of each well. After washing with PBS once, add 500μl culture medium to each well and continue culturing for 10h. Observed and photographed under a microscope at 0h, 6h and 10h after the scratch. The experiment was carried out 3 times, and 3 visual fields were randomly selected for each concentration to calculate the average value of the cell migration distance. Results The migr...

Embodiment 3

[0043] IC-4 inhibition of endothelial cell metastasis

[0044] 1. Experimental method:

[0045] Transwell cell migration experiment: In this experiment, a Corning 24-hole Transwell cell with 8μm pore size was used for the experiment. Take 2-5 generations of human umbilical vein endothelial cells, press 5×10 4 Cells per well were inoculated on the upper layer of the polycarbonate membrane of the Tranwell chamber. The upper layer of the Transwell chamber was cultured with 100 μl 0.1% DMSO serum-free medium as a control group, and the other wells were cultured with 100 μl serum-free medium containing different concentrations of drugs. The lower layer of the Transwell chamber is a medium containing 1% serum and 20ng / ml endothelial cell growth factor. After the cells migrated for 6 hours, they were washed with PBS, the upper cells were gently removed with cotton swabs, the lower cells were fixed with 1% paraformaldehyde for 15 minutes, and then stained with Hoechst 33342 dye and observ...

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Abstract

The invention discloses an application of a compound IC-4 with the structural formula represented by formula (I) or its salts in antiangiogenesis, and further discloses an application of the compound IC-4 with the structural formula represented by formula (I) or its salt in preparation of antiangiogenic agents. Researches on the application of the IC-4 or its salt in the antiangiogenesis are based on researches on growth factor induced endothelial cell growth inhibition, angiogenesis inhibition, endothelial cell migration inhibition and endothelial cell transfer inhibition of the IC-4 or its salts, and combine with a scientific and reasonable research system constructed through integral experiments of zebra fish embryo angiogenesis.

Description

Technical field [0001] The present invention relates to the use of a compound and its salt, in particular to the application of IC-4 and its salt in anti-angiogenesis. Background technique [0002] Angiogenesis refers to the process of forming functional new blood vessels based on the original capillaries and / or venules through vascular endothelial cell proliferation, migration, adhesion and vascular lumen formation; this process includes vascular endothelial cells and surrounding cells The interaction between the outer matrix is ​​mainly regulated by angiogenesis promoting factors and angiogenesis inhibitors. Studies have found that a variety of growth factors such as vascular endothelial cell growth factor, angiopoietin 2, basic fibroblast growth factor, and epidermal growth factor can all regulate angiogenesis in different ways. Under physiological conditions, angiogenesis is only opened for a short time during embryonic development, wound repair, and women's menstruation, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4406A61P19/02A61P29/00A61P9/10A61P17/06
Inventor 王一涛李润涛李颖博陈美婉葛泽梅闫旭
Owner UNIVERSITY OF MACAU
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