Environmental Toxicology and Pharmacology 2015-01-01

Dieckol as a novel anti-proliferative and anti-angiogenic agent and computational anti-angiogenic activity evaluation.

Yong-Xin Li, Yong Li, Jae-Young Je, Se-Kwon Kim

Index: Environ. Toxicol. Pharmacol. 39(1) , 259-70, (2015)

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Abstract

In the current study it was found that dieckol isolated from edible brown algae, Ecklonia cava (EC), as potent anti-proliferative and anti-angiogenic agent. Vascular endothelial growth factor (VEGF) induced EA.hy926 cell proliferation was suppressed by dieckol treatment. Further, it showed a significant inhibition of cell migration via inhibiting the protein and gene expression levels of matrix metalloproteinases, MMP-2 and -9. The signaling cascade underlying these responses was found as the dieckol induced inhibition of mitogen-activated protein kinase (MAPK) signaling pathway molecules, ERK and p38. Docking calculations were carried out on AP-N, VEGFR-1, MMP-2, MMP-9, Akt and Erk2 proteins model. Collectively, these results demonstrate the effective anti-proliferative and anti-migratory activity of dieckol on VEGF induced EA.hy926 through MAPK molecular signaling pathways which could be effectively correlated to its potential as an anti-angiogenic candidate. Therefore, this study reveals the potential of dieckol to be used in the design of anti-angiogenic agents. Copyright © 2014 Elsevier B.V. All rights reserved.