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<p>Abstract</p> <p>Background</p> <p>Angiogenesis, the growth of new blood vessels from the pre-existing vasculature is associated with pathological processes, in particular tumour development, and is a target for the development of new therapies. We have investigated the anti-angiogenic potential of two naturally occurring stilbene glycosides (compounds <b>1 </b>and <b>2</b>) isolated from the medicinal plant <it>Boswellia papyriferai </it>using large and smallvessel-derived endothelial cells. Compound <b>1 </b>(trans-4',5'-dihydroxy-3-methoxystilbene-5-O-{α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)}-β-D-glucopyranoside was the more hydrophilic and inhibited FGF-2-induced proliferation, wound healing, invasion in Matrigel, tube formation and angiogenesis in large and small vessel-derived endothelial cells and also in the chick chorioallantoic membrane assay. Using a binding assay we were able to show compound <b>1 </b>reduced binding of FGF-2 to fibroblast growth factor receptors-1 and -2. In all cases the concentration of compound <b>1 </b>which caused 50% inhibition (IC₅₀) was determined. The effect of compound <b>1 </b>on EGF and VEGF-induced proliferation was also investigated.</p> <p>Results</p> <p>Compound <b>1 </b>inhibited all stages of FGF-2 induced angiogenesis with IC₅₀values in the range 5.8 ± 0.18 – 48.90 ± 0.40 μM but did not inhibit EGF or VEGF-induced angiogenesis. It also inhibited FGF-2 binding to FGF receptor-1 and -2 with IC₅₀values of 5.37 ± 1.04 and 9.32 ± 0.082 μM respectively and with concommotant down-regulation of phosphorylated-ERK-1/-2 expression. Compound <b>2 </b>was an ineffective inhibitor of angiogenesis despite its structural homology to compound <b>1</b>.</p> <p>Conclusion</p> <p>Compound <b>1 </b>inhibited FGF-2 induced angiogenesis by binding to its cognate receptors and is an addition to the small number of natural product inhibitors of angiogenesis</p>