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

• Dieckol isolated from edible brown algae, Ecklonia cava.
• Dieckol as potent anti-proliferative and anti-angiogenic agent.
• Dieckol exerts an anti-angiogenic activity most probably via MAPK signaling pathway.
• Structure–activity relationship analysis of dieckol.
• Dieckol docking calculations were carried out on proteins model.

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.