Cheiradone: a vascular endothelial cell growth factor receptor antagonistReport as inadecuate




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BMC Cell Biology

, 9:7

First Online: 29 January 2008Received: 17 October 2007Accepted: 29 January 2008

Abstract

BackgroundAngiogenesis, the growth of new blood vessels from the pre-existing vasculature is associated with physiological for example wound healing and pathological conditions tumour development. Vascular endothelial growth factor VEGF, fibroblast growth factor-2 FGF-2 and epidermal growth factor EGF are the major angiogenic regulators. We have identified a natural product cheiradone isolated from a Euphorbia species which inhibited in vivo and in vitro VEGF- stimulated angiogenesis but had no effect on FGF-2 or EGF activity. Two primary cultures, bovine aortic and human dermal endothelial cells were used in in vitro proliferation, wound healing, invasion in Matrigel and tube formation and in vivo the chick chorioallantoic membrane models of angiogenesis in the presence of growth factors and cheiradone. In all cases, the concentration of cheiradone which caused 50% inhibition IC50 was determined. The effect of cheiradone on the binding of growth factors to their receptors was also investigated.

ResultsCheiradone inhibited all stages of VEGF-induced angiogenesis with IC50 values in the range 5.20–7.50 μM but did not inhibit FGF-2 or EGF-induced angiogenesis. It also inhibited VEGF binding to VEGF receptor-1 and 2 with IC50 values of 2.9 and 0.61 μM respectively.

ConclusionCheiradone inhibited VEGF-induced angiogenesis by binding to VEGF receptors -1 and -2 and may be a useful investigative tool to study the specific contribution of VEGF to angiogenesis and may have therapeutic potential.

Electronic supplementary materialThe online version of this article doi:10.1186-1471-2121-9-7 contains supplementary material, which is available to authorized users.

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Author: Sajjad Hussain - Mark Slevin - Mohammad A Mesaik - Mohammad I Choudhary - Abdul H Elosta - Sabine Matou - Nessar Ahmed -

Source: https://link.springer.com/article/10.1186/1471-2121-9-7







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