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Potent anti-angiogenicactivity of B19-a mono-carbonyl analogue of curcumin

Potent anti-angiogenicactivity of B19-a mono-carbonyl analogue of curcumin

  • 摘要: AIM:The compound B19(C21H22O5) is a newly synthesized,mono-carbonyl analog of curcumin that has exhibited potentialantitumor effects.This present study was performed to identify the anti-angiogenic activity of this compound.METHODS AND RESULTS:B19 inhibited migration and tube formation of human umbilical vein endothelial cells,and arrested microvessel outgrowth from rat aortic rings.In addition,B19 suppressed the neovascularization of chicken chorioallantoic membrane.Mechanistic studies revealed that B19 suppressed the downstream protein kinase activation of vascular endothelial growth factor(VEGF) by decreasing phosphorylated forms of serine/threonine kinase Akt,extracellular signal-regulated kinase,and p38 mitogen-activated protein kinase,with or without stimulating vascular endothelial growth factor(VEGF).CONCLUSIONS:B19 exerted anti-angiogenic activity in vitro and ex vivo,which suggests that it merits further investigation as a promising anticancer angiogenesis compound.

     

    Abstract: AIM:The compound B19(C21H22O5) is a newly synthesized,mono-carbonyl analog of curcumin that has exhibited potentialantitumor effects.This present study was performed to identify the anti-angiogenic activity of this compound.METHODS AND RESULTS:B19 inhibited migration and tube formation of human umbilical vein endothelial cells,and arrested microvessel outgrowth from rat aortic rings.In addition,B19 suppressed the neovascularization of chicken chorioallantoic membrane.Mechanistic studies revealed that B19 suppressed the downstream protein kinase activation of vascular endothelial growth factor(VEGF) by decreasing phosphorylated forms of serine/threonine kinase Akt,extracellular signal-regulated kinase,and p38 mitogen-activated protein kinase,with or without stimulating vascular endothelial growth factor(VEGF).CONCLUSIONS:B19 exerted anti-angiogenic activity in vitro and ex vivo,which suggests that it merits further investigation as a promising anticancer angiogenesis compound.

     

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