title: Antiangiogenic activity of Tripterygium wilfordii and its terpenoids.
abstract: 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.
authors.affiliation: Department of Biology, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, PR China.
authors.forename: Ming-Fang
authors.initials: MF
authors.lastname: He
authors.forename: Lin
authors.initials: L
authors.lastname: Liu
authors.forename: Wei
authors.initials: W
authors.lastname: Ge
authors.forename: Pang-Chui
authors.initials: PC
authors.lastname: Shaw
authors.forename: Renwang
authors.initials: R
authors.lastname: Jiang
authors.forename: Li-Wha
authors.initials: LW
authors.lastname: Wu
authors.forename: Paul Pui-Hay
authors.initials: PP
authors.lastname: But
mesh_terms: 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
chemical_list: 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