Antiangiogenic activity of Tripterygium wilfordii and its terpenoids.
BACKGROUND
Tripterygium wilfordii Hook. f. (Celastraceae) has been traditionally used as folk medicine for centuries in China for the treatment of immune-inflammatory diseases.


OBJECTIVE
This study aimed to assess the antiangiogenic activities which support the therapeutic use of Tripterygium wilfordii and its terpenoids for angiogenesis disease such as cancer.


METHODS
The ethanol extract of Tripterygium wilfordii and subsequent fractions were evaluated on an in vivo antiangiogenic zebrafish embryo model.


RESULTS
Three antiangiogenic terpenoids were isolated by bioassay-guided purification, namely, celastrol (4), cangoronine (5) and triptolide (7). Among them, triptolide manifested the most potent antiangiogenic activity against vessel formation by nearly 50% at 1.2 microM. Semi-quantitative RT-PCR analysis revealed that triptolide dose- and time-dependently reduced the mRNA expression of angiopoietin (angpt)2 and tie2 in zebrafish, indicating the involvement of angpt2/tie2 signaling pathway in the antiangiogenic action of triptolide.


CONCLUSIONS
The discovery of an alternative pathway further confirms the value of ethnopharmacological investigations into traditional botanicals for leads for potential drug development.
He
Ming-Fang
MF
Department of Biology, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, PR China.
Liu
Lin
L
Ge
Wei
W
Shaw
Pang-Chui
PC
Jiang
Renwang
R
Wu
Li-Wha
LW
But
Paul Pui-Hay
PP
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004195:Disease Models, Animal; D004224:Diterpenes / Q000737:chemistry / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D004625:Embryo, Nonmammalian / Q000098:blood supply; D004852:Epoxy Compounds / Q000737:chemistry / Q000494:pharmacology; D018919:Neovascularization, Physiologic / Q000187:drug effects; D053978:Pentacyclic Triterpenes; D010616:Phenanthrenes / Q000737:chemistry / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013729:Terpenes / Q000737:chemistry / Q000494:pharmacology*; D029757:Tripterygium / Q000737:chemistry*; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology; D015027:Zebrafish
D020533:Angiogenesis Inhibitors; D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D004852:Epoxy Compounds; D053978:Pentacyclic Triterpenes; D010616:Phenanthrenes; D013729:Terpenes; D014315:Triterpenes; C419238:cangoronine; C001899:triptolide; C050414:celastrol