Abstract
In our continuing search for novel antiangiogenic agents, a new lignan glycoside, (7R,8R)-1-(4-O-β-d-glucopyranosyl-3-methoxyphenyl)-2-{2-methoxy-4-[1-(E)-propene-3-ol]-phenoxyl}-propane-1,3-diol (1), along with three known lignans (2-4), were isolated from the 80% EtOH extract of Brandisia hancei stems and leaves. These isolates (1-4) were subjected to an in vitro bioassay to evaluate their effects on vascular endothelial growth factor (VEGF)-induced vascular permeability and migration of human retinal endothelial cells (HRECs). Of the compounds tested, compound 1 resulted in the greatest reduction in VEGF-induced vascular permeability by about 31.5% at 10 μM compared to the VEGF-treated control. In the migration assay, compounds 1 and 2 significantly decreased VEGF-induced HREC migration. Furthermore, zebrafish embryos treated with compounds 1 and 2 showed mild reductions of dorsal longitudinal anastomotic vessel (DLAV) formation.
Keywords:
Brandisia hancei; Scrophulariaceae; lignans; vascular endothelial growth factor; zebrafish.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Angiogenesis Inhibitors / chemistry
-
Angiogenesis Inhibitors / isolation & purification
-
Angiogenesis Inhibitors / pharmacology*
-
Animals
-
Biological Assay
-
Blood Vessels / drug effects*
-
Blood Vessels / embryology
-
Capillary Permeability / drug effects*
-
Cell Movement / drug effects*
-
Embryo, Nonmammalian / blood supply
-
Embryo, Nonmammalian / drug effects
-
Endothelial Cells / cytology
-
Endothelial Cells / drug effects
-
Endothelial Cells / metabolism
-
Gene Expression
-
Glycosides / chemistry
-
Glycosides / isolation & purification
-
Glycosides / pharmacology*
-
Humans
-
Lamiales / chemistry
-
Lignans / chemistry
-
Lignans / isolation & purification
-
Lignans / pharmacology*
-
Molecular Structure
-
Morphogenesis / drug effects
-
Morphogenesis / genetics
-
Plant Extracts / chemistry
-
Plant Leaves / chemistry
-
Plant Stems / chemistry
-
Retina / cytology
-
Retina / drug effects
-
Retina / metabolism
-
Vascular Endothelial Growth Factor A / genetics
-
Vascular Endothelial Growth Factor A / metabolism
-
Vascular Endothelial Growth Factor A / pharmacology
-
Zebrafish
Substances
-
Angiogenesis Inhibitors
-
Glycosides
-
Lignans
-
Plant Extracts
-
VEGFA protein, human
-
Vascular Endothelial Growth Factor A