Abstract
The aim of this study was to investigate novel chalcones with potent angiogenic activities in vivo. Chalcone-based derivatives were evaluated using a transgenic zebrafish line with fluorescent vessels to real-time monitor the effect on angiogenesis. Results showed that the chalcone analogues did not possess anti-angiogenic effect on zebrafish vasculatures; instead, some of them displayed potent pro-angiogenic effects on the formation of the sub-intestinal vein. Similar pro-angiogenic effects can also be seen on wild type zebrafish embryos. Moreover, the expression of vegfa, the major regulator for angiogenesis, was also upregulated in their treatment. Taken together, we have synthesized and identified a series of novel chalcone-based derivatives as potent in vivo pro-angiogenic compounds. These novel compounds hold potential for therapeutic angiogenesis.
Keywords:
angiogenesis; chalcones; in vivo; zebrafish embryos.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiogenesis Inducing Agents / chemical synthesis
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Angiogenesis Inducing Agents / pharmacology*
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Animals
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Animals, Genetically Modified
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Chalcones / chemical synthesis
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Chalcones / pharmacology*
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Embryo, Nonmammalian
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Gene Expression Regulation, Developmental*
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Genes, Reporter
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Green Fluorescent Proteins / genetics
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Green Fluorescent Proteins / metabolism
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Molecular Structure
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Morphogenesis / drug effects
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Neovascularization, Physiologic / drug effects*
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Structure-Activity Relationship
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Vascular Endothelial Growth Factor A / agonists*
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Vascular Endothelial Growth Factor A / genetics
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Vascular Endothelial Growth Factor A / metabolism
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Zebrafish
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Zebrafish Proteins / agonists*
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Zebrafish Proteins / genetics
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Zebrafish Proteins / metabolism
Substances
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Angiogenesis Inducing Agents
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Chalcones
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Vascular Endothelial Growth Factor A
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Zebrafish Proteins
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enhanced green fluorescent protein
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Green Fluorescent Proteins