ETHNOPHARMACOLOGICAL RELEVANCE: Tripterygium wilfordii Hook. f. (Celastraceae) has been traditionally used as folk medicine for centuries in China for the treatment of immune-inflammatory diseases. AIM OF THE STUDY: 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. MATERIALS AND 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.
ETHNOPHARMACOLOGICAL RELEVANCE: Tripterygium wilfordii Hook. f. (Celastraceae) has been traditionally used as folk medicine for centuries in China for the treatment of immune-inflammatory diseases. AIM OF THE STUDY: 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. MATERIALS AND 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: Xiaomei Wei; Tim S Bugni; Mary Kay Harper; Imelda T Sandoval; Elizabeth J Manos; Jennifer Swift; Ryan M Van Wagoner; David A Jones; Chris M Ireland Journal: Mar Drugs Date: 2010-06-02 Impact factor: 5.118
Authors: Alexander D Crawford; Sandra Liekens; Appolinary R Kamuhabwa; Jan Maes; Sebastian Munck; Roger Busson; Jef Rozenski; Camila V Esguerra; Peter A M de Witte Journal: PLoS One Date: 2011-02-17 Impact factor: 3.240