EGFR, and VEGFR inhibitory activities of the crude extract from marine algae Dictyopteris acrostichoides supported by in silico analysis and metabolic profiling

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Abstract Ethanol extracts of Caulerpa racemosa, Dictyopteris acrostichoides, Halimeda opuntia and Polycladia myrica, were tested for their cytotoxicity against HepG2 (human hepatoma), MCF-7 (human breast adenocarcinoma), and Caco-2 (human colon adenocarcinoma) cells. Dictyopteris acrostichoides displayed cytotoxicity against HepG2, MCF-7 and Caco-2 with IC50 values of 11.65, 9.28 and 16.86 µg/mL, respectively in comparison to doxorubicin as a positive control, (IC50 = 5.72, 5.17 and 5.81 µg/mL, respectively). LC-HR-ESI-MS metabolic profiling of the D. acrostichoides extract characterized seventeen metabolites (1–17). In silico analysis indicated 1-(3-oxo-undecyldisulfanyl)-undecan-3-one (16) was the most active EGFR inhibitor, while 1-(3-Oxo-undecyldisulfanyl)-undecan-3-one (16) and di(3-acetoxy-5-undecenyl) disulfide (17) were the most active VEGFR inhibitors. Furthermore, the ethanol extract of D. acrostichoides was tested against epidermal growth factor receptor (EGFR) kinase (IC50 = 0.11 µg/mL) compared to lapatinib as a positive control, (IC50 = 0.03µg/mL) and against vascular endothelial growth factor (VEGF) (IC50 = 0.276 µg/mL) compared to sorafenib as a positive control, (IC50 = 0.049 µg/mL).

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