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

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).