The proangiogenic members of the vascular endothelial growth factor (VEGF) family and related receptors play a central role in the modulation of pathological angiogenesis. In order to identify plant compounds able to interfere in the VEGFs/VEGFR-1 (Flt-1) recognition by VEGF family members, the extracts of the aerial parts of Campsiandra guayanensis and Feretia apodanthera were screened by a competitive ELISA-based assay. By using this bioassay-oriented approach five proanthocyanindins, including the new natural compounds (2S)-4′,5,7-trihydroxyflavan-(4β→8)-afzelechin (1) and (2S)-4′,5,7-trihydroxyflavan-(4β→8)-epiafzelechin (2) and the known geranin B (3), proanthocyanidin A2 (4), and proanthocyanidin A1 (5), were isolated. The study of the antiangiogenic activities of compounds 1-5 using ELISA and SPR assays showed compound 1 as being the most active. The antiangiogenic activity of 1 was also confirmed in vivo by the chicken chorioallantoic membrane assay. Our results indicated 1 as a new antiangiogenic compound inhibiting the interaction between VEGF-A or PlGF and their receptor VEGRF-1.
|Autori:||M. S. Pesca; F. Dal Piaz; R. Sanogo; A. Vassallo; M. Bruzual de Abreu; A. Rapisarda; M. P. Germanò; G. Certo; S. De Falco; N. De Tommasi; A. Braca|
|Titolo:||Bioassay-guided isolation of proanthocyanidins with antiangiogenic activities|
|Anno del prodotto:||2013|
|Digital Object Identifier (DOI):||10.1021/np300614u|
|Appare nelle tipologie:||1.1 Articolo in rivista|