LAUSR

BACKGROUND Sargassum is a marine organism, it tends to increase its population drastically damaging the environment and risking other organisms, however sargassum could represent a source of bioactive compounds to treat different diseases such as cancer. Thus, aqueous, ethanolic, and ethyl acetate extracts of sargassum from Playa del Carmen Mexico were obtained to be subjected to metabolomic and antiproliferative assays in breast cancer cells. OBJECTIVE To evaluate the effect of aqueous, ethanolic, and ethyl acetate extracts from Mexican sargassum in Artemia salina bioassays and its antiproliferative effects in MCF-7, MDA-MB-231 and NIH3T3 cell lines, finally by UHPLC-MS/MS to identify the metabolites in each extract and relate them with its antiproliferative effect. METHODS The sargassum sample collection was carried out in September, in 3 different points of Playa del Carmen, Quintana Roo, Mexico. The aqueous, ethanolic and ethyl acetate extracts of Mexican sargassum were obtained by evaporation of solvent and lyophilization. Then, these extracts were evaluated in the cytotoxicity bioassay in Artemia salina, next its antiproliferative effect was assessed in MCF-7, MDA-MB-231, NIH3T3 cell lines. By means of UHPLC-MS/MS the metabolites present in each extract were identified. Finally, docking studies on sphingosine kinase 1 (PDB ID: 3VZB) of sphingosine were carried out. RESULTS The extracts obtained from sargassum showed a greater effect in the antiproliferative assays in cells than in cytotoxic assays in artemia salina. The ethanolic extract obtained from Sargassum showed the best antiproliferative activity in MCF7 and MDA-MB-231 cells and despite its antiproliferative effect on NIH3T3 cells more amount of extract is required indicating this results that this extract has compounds that could have better effect on cancer cells that in fibroblast (NIH3T3). The UHPLC-MS/MS of ethanolic and the ethyl acetate extract showed that this extract has compound such as sphinganine C16, N,N-Dimethylphingosine compound, then could be possible that the effect observed be due to their metabolites which could be ligands for the sphingosine kinase 1 as was demonstrated by docking studies. CONCLUSION The ethanolic extract obtained from sargassum has better antiproliferative activity, despite not having cytotoxic effect in Artemia salina. The antiproliferative effect could be related with the sphinganine C16, N,N-Dimethylphingosine identified with more abundance by UHPLC-MS/MS. In addition, these metabolites could be target of sphingosine kinase 1.