ZFIN ID: ZDB-PUB-151009-3
Kaempferol Identified by Zebrafish Assay and Fine Fractionations Strategy from Dysosma versipellis Inhibits Angiogenesis through VEGF and FGF Pathways
Liang, F., Han, Y., Gao, H., Xin, S., Chen, S., Wang, N., Qin, W., Zhong, H., Lin, S., Yao, X., Li, S.
Date: 2015
Source: Scientific Reports   5: 14468 (Journal)
Registered Authors: Lin, Shuo, Zhong, Hanbing
Keywords: none
MeSH Terms:
  • Angiogenesis Inhibitors/isolation & purification
  • Angiogenesis Inhibitors/pharmacology*
  • Animals
  • Animals, Genetically Modified
  • Berberidaceae/chemistry*
  • Biological Assay
  • Cell Movement/drug effects
  • Cell Proliferation/drug effects
  • Chemical Fractionation/methods
  • Embryo, Nonmammalian
  • Fibroblast Growth Factors/antagonists & inhibitors
  • Fibroblast Growth Factors/genetics
  • Fibroblast Growth Factors/metabolism
  • Gene Expression Regulation
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Kaempferols/isolation & purification
  • Kaempferols/pharmacology*
  • Medicine, Chinese Traditional
  • Neovascularization, Physiologic/drug effects*
  • Plant Extracts/chemistry
  • Plants, Medicinal
  • Small Molecule Libraries/isolation & purification
  • Small Molecule Libraries/pharmacology*
  • Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors
  • Vascular Endothelial Growth Factor Receptor-2/genetics
  • Vascular Endothelial Growth Factor Receptor-2/metabolism
  • Zebrafish
  • Zebrafish Proteins/antagonists & inhibitors
  • Zebrafish Proteins/genetics
  • Zebrafish Proteins/metabolism
PubMed: 26446489 Full text @ Sci. Rep.
Natural products are a rich resource for the discovery of therapeutic substances. By directly using 504 fine fractions from isolated traditional Chinese medicine plants, we performed a transgenic zebrafish based screen for anti-angiogenesis substances. One fraction, DYVE-D3, was found to inhibit the growth of intersegmental vessels in the zebrafish vasculature. Bioassay-guided isolation of DYVE-D3 indicates that the flavonoid kaempferol was the active substance. Kaempferol also inhibited the proliferation and migration of HUVECs in vitro. Furthermore, we found that kaempferol suppressed angiogenesis through inhibiting VEGFR2 expression, which can be enhanced by FGF inhibition. In summary, this study shows that the construction of fine fraction libraries allows efficient identification of active substances from natural products.