Baicalein and baicalin are potent inhibitors of angiogenesis: Inhibition of endothelial cell proliferation, migration and differentiation
Journal
International Journal of Cancer
Journal Volume
106
Journal Issue
4
Pages
559-565
Date Issued
2003
Author(s)
Abstract
In recent studies, we have shown that baicalein and baicalin, 2 major flavonoids of Scutellaria baicatensis Georgi, exhibit anticancer activity against several cancers in vitro. In our present study, we assessed their potential as anti-angiogenic agents in vivo employing chicken chorioallantoic membrane (CAM) assay and in vitro human umbilical vein endothelial cells (HUVECs) culture. When CAMs were treated with either baicalein or baicalin for 48 hr, the angiogenic response induced by basic fibroblast growth factor (bFGF) was markedly reduced in a dose-dependent manner. Further characterization showed that both flavonoids exhibited dual antiproliferative (at low dose) and apoptogenic (at high dose) effects on HUVECs. In biochemical analysis, treatment of HUVECs with baicalein and baicalin for 24 hr resulted in a dose-dependent decrease in the matrix metalloproteinase (MMP)-2 activity. Moreover, the migration of endothelial cells and the differentiation of endothelial cells into branching networks of tubular structures in vitro were also inhibited by these 2 flavonoids in a dose-dependent manner. Baicalein is more potent than baicalin in anti-angiogenesis in vivo as well as in vitro. Taken together, the results of our study provide evidence that baicalein and baicalin possess an antiangiogenesis potential that is a previously unrecognized biologic activity. ? 2003 Wiley-Liss, Inc.
SDGs
Other Subjects
angiogenesis inhibitor; baicalein; baicalin; basic fibroblast growth factor; flavonoid; gelatinase A; angiogenesis; apoptosis; article; cell differentiation; cell migration; cell proliferation; chorioallantois; dose response; drug potency; endothelium cell; enzyme activity; human; human cell; in vitro study; in vivo study; nonhuman; plant; priority journal; scutellaria baicalensis; Angiogenesis Inhibitors; Animals; Cell Differentiation; Cell Division; Cell Movement; Cells, Cultured; Chick Embryo; Chorion; Collagen; DNA Topoisomerases, Type II; Drug Combinations; Endothelium, Vascular; Enzyme Inhibitors; Fibroblast Growth Factor 2; Flavanones; Flavonoids; Glucuronidase; Humans; Laminin; Matrix Metalloproteinase 2; Neovascularization, Physiologic; Proteoglycans; Umbilical Veins
Type
journal article