Antiangiogenic activity of xanthomicrol and calycopterin, two polymethoxylated hydroxyflavones in both in vitro and ex vivo models

Abbaszadeh, H. and Ebrahimi, S.A. and Akhavan, M.M. (2014) Antiangiogenic activity of xanthomicrol and calycopterin, two polymethoxylated hydroxyflavones in both in vitro and ex vivo models. Phytotherapy Research, 28 (11). pp. 1661-1670.

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Our previous studies had shown xanthomicrol and calycopterin, two plant-derived flavonoids, to have selective antiproliferative activity against some malignant cell lines. The present study is focused on the investigation of antiangiogenic potential of these two flavonoids, using in vitro and ex vivo models. Xanthomicrol and calycopterin were found to have potent inhibitory effects on microvessel outgrowth in the rat aortic ring assay. Xanthomicrol was able to completely block microvessel sprouting at 10 μg/mL, and calycopterin suppressed microvessel outgrowth by 89 at 5 μg/mL. Suramin and thalidomide, used at 20 μg/mL as positive controls, inhibited microvessel formation by 23 and 64, respectively. The flavones also inhibited endothelial cell tube formation and human umbilical vein endothelial cell proliferation at 0.5, 5, and 10 μg/mL. In order to delineate the underlying mechanisms of antiangiogenic activity of these flavones, we investigated the influences of xanthomicrol and calycopterin on expression of vascular endothelial growth factor (VEGF) and basic-fibroblast growth factor (b-FGF) in endothelial cells. These flavones were able to inhibit VEGF expression at 0.5, 5, and 10 μg/mL, but they had little or no effect on b-FGF expression. These findings suggest that xanthomicrol and calycopterin possess potent antiangiogenic activities, which may be due to their inhibitory influences on VEGF expression. Copyright © 2014 John Wiley & Sons, Ltd.

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Uncontrolled Keywords: calycopterin; fibroblast growth factor 2; flavonoid; suramin; thalidomide; unclassified drug; vasculotropin; vasculotropin receptor; xanthomicrol; angiogenesis inhibitor; calycopterin; fibroblast growth factor 2; flavone derivative; vasculotropin A; VEGFA protein, human; xanthomicrol, animal cell; animal experiment; animal model; animal tissue; antiangiogenic activity; Article; cell proliferation; concentration response; controlled study; drug determination; drug potency; drug purification; drug structure; endothelium cell; ex vivo study; growth inhibition; human; human cell; in vitro study; microvasculature; microvessel outgrowth; nonhuman; protein expression; solvent extraction; sprouting; umbilical vein endothelial cell; vascular ring; animal; aorta; chemistry; drug effects; Lamiaceae; male; metabolism; rat; Wistar rat, Rattus, Angiogenesis Inhibitors; Animals; Aorta; Cell Proliferation; Fibroblast Growth Factor 2; Flavones; Human Umbilical Vein Endothelial Cells; Humans; In Vitro Techniques; Lamiaceae; Male; Rats; Rats, Wistar; Vascular Endothelial Growth Factor A
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Date Deposited: 19 Jul 2017 10:13
Last Modified: 19 Jul 2017 10:13

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