Bioassay-Guided Isolation of Proanthocyanidins with Antiangiogenic Activities

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• 作者：Maria S. Pesca ; Fabrizio Dal Piaz ; Rokia Sanogo ; Antonio Vassallo ; Maryan Bruzual de Abreu ; Antonio Rapisarda ; Maria P. German貌 ; Giovanna Certo ; Sandro De Falco ; Nunziatina De Tommasi ; Alessandra Braca
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：January 25, 2013
• 年：2013
• 卷：76
• 期：1
• 页码：29-35
• 全文大小：335K
• 年卷期：v.76,no.1(January 25, 2013)
• ISSN：1520-6025

文摘

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鈥?5,7-trihydroxyflavan-(4尾鈫?)-afzelechin (1) and (2S)-4鈥?5,7-trihydroxyflavan-(4尾鈫?)-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鈥?b>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.