Antiproliferative Activity of Olive Oil Phenolics against Human Melan oma Cells

Title:Antiproliferative Activity of Olive Oil Phenolics against Human Melan oma Cells

Volume: 14 Issue: 9

Author(s): A. L.M. Batista de Carvalho, F. Caselli, V. Rodrigues, F. Paiva-Martins and M.P. M. Marques*

Affiliation:

• Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia,Universidade de Coimbra, Calçada Martim de Freitas, 3000-456 Coimbra,Portugal

Keywords: Virgin olive oil, hydroxytyrosol, secoiridoid polyphenols, anticancer, melanoma, fibroblasts.

Abstract: Background: Virgin olive oil, the main source of lipids in a mediterranean diet, is broadly recognised to possess health-beneficial features, namely a protective role against cancer. It comprises several phenolic compounds, the major ones being tyrosol (p-hydroxyphenylethanol), hydroxytyrosol (3,4-dihydroxyphenylethanol), lignans and secoiridoids, namely oleuropein (OP) and the oleuropein aglycones 3,4-(dihydroxyphenyl) ethanol elenolic acid ester and 3,4-(dihydroxyphenyl)ethanol elenolic acid di-aldehyde.

Objective: The goal of this work is the in vitro evaluation of the anti-proliferative activity against human amelanotic melanoma (C32 cell line) for hydroxytyrosol and the most important secoiridoids of olive oil. The effect of hydroxytyrosol on non-neoplastic cells (BJ fibroblass) was also investigated.

Methods: Inhibition of cell proliferation was assessed by the Sulforhodamine colorimetric method, in both neoplastic and non-tumorigenic cells.

Results: 3,4-(Dihydroxyphenyl)ethanol elenolic acid di-aldehyde and 3,4-(dihydroxyphenyl)ethanol elenolic acid ester secoiridoid aglycones were found to display growth-inhibiting activity (at ca. 100 µM), as opposed to oleuropein that elicited a strong protective effect at all concentrations (100 to 1000 μM). 3,4-Dihydroxyphenylethanol evidenced a dual effect (strongly dose-dependent) - cytoprotective for lower dosages and cytotoxic at high concentrations.

Conclusion: Attending to the recognised structural dependence of the biological activity of phenolic derivatives, the previously gathered conformational data on the olive oil constituents presently investigated assisted the interpretation of their biological properties. This type of studies, coupling structural characterisation to biological assessment, allows the establishment of reliable structure activity relationships for polyphenolic compounds, ruling their cytoprotective vs cytotoxic activity and therefore their potential use as natural-based pharmacological agents.

Cite this article as:

de Carvalho Batista A. L.M., Caselli F., Rodrigues V., Paiva-Martins F. and Marques M. M.P.*, Antiproliferative Activity of Olive Oil Phenolics against Human Melan oma Cells, Letters in Drug Design & Discovery 2017; 14 (9) . https://dx.doi.org/10.2174/1570180814666170110145658

DOI https://dx.doi.org/10.2174/1570180814666170110145658	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X