Inhibition of the vascular-endothelial growth factor-induced intracellular signaling and mitogenesis of human endothelial cells by epigallocatechin-3 gallate.
Galloyl group-containing catechins, such as epigallocatechin-3 gallate, inhibit receptor tyrosine kinase activity of several growth factor receptors. This study investigated the effects of epigallocatechin-3 gallate, as compared to epicatechin, on vascular endothelial growth factor-induced intracellular signaling and mitogenesis of human umbilical endothelial cells. Epigallocatechin-3 gallate concentration-dependently inhibited vascular endothelial growth factor-induced DNA synthesis, cell proliferation, autophosphorylation of vascular endothelial growth factor receptors-1 and -2, phosphorylation of extracellular signal-regulated kinases-1 and -2, and mRNA expression of the early growth response factor-1. In contrast, epicatechin was not effective. Thus, epigallocatechin-3 gallate may be an attractive candidate drug to inhibit tumour angiogenesis.
Neuhaus
Thomas
T
Medizinische Universitäts-Poliklinik Bonn, Wilhelmstr. 35-37, D-53111, Bonn, Germany. t.neuhaus@uni-bonn.de
Pabst
Stefan
S
Stier
Sebastian
S
Weber
Artur-Aron
AA
Schrör
Karsten
K
Sachinidis
Agapios
A
Vetter
Hans
H
Ko
Yon D
YD
D002392:Catechin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects / Q000502:physiology; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects* / Q000502:physiology; D006131:Growth Inhibitors / Q000494:pharmacology; D006801:Humans; D008934:Mitogens / Q000494:pharmacology*; D015290:Second Messenger Systems / Q000187:drug effects* / Q000502:physiology; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors / Q000494:pharmacology*
D006131:Growth Inhibitors; D008934:Mitogens; C467484:VEGFA protein, human; D042461:Vascular Endothelial Growth Factor A; D002392:Catechin; C045651:epigallocatechin gallate