Baicalein and baicalin are potent inhibitors of angiogenesis

Inhibition of endothelial cell proliferation, migration and differentiation

Jun Jen Liu, Tien Shang Huang, Wen Fang Cheng, Fung Jou Lu

Research output: Contribution to journalArticle

99 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)559-565
Number of pages7
JournalInternational Journal of Cancer
Volume106
Issue number4
DOIs
Publication statusPublished - Sep 10 2003
Externally publishedYes

Fingerprint

Angiogenesis Inhibitors
Cell Movement
Cell Differentiation
Endothelial Cells
Cell Proliferation
Human Umbilical Vein Endothelial Cells
Flavonoids
Scutellaria
Chorioallantoic Membrane
Matrix Metalloproteinase 2
Fibroblast Growth Factor 2
Chickens
Cell Culture Techniques
baicalin
baicalein
In Vitro Techniques
Neoplasms

Keywords

  • Angiogenesis
  • Anti-angiogenic agent
  • Baicalein
  • Baicalin
  • CAM

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Baicalein and baicalin are potent inhibitors of angiogenesis : Inhibition of endothelial cell proliferation, migration and differentiation. / Liu, Jun Jen; Huang, Tien Shang; Cheng, Wen Fang; Lu, Fung Jou.

In: International Journal of Cancer, Vol. 106, No. 4, 10.09.2003, p. 559-565.

Research output: Contribution to journalArticle

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