miRNA Modulation and Antitumor Activity by the Extra-Virgin Olive Oil Polyphenol Oleacein in Human Melanoma Cells50

In this study, Carpi et al aimed at determining in vitro the antimelanoma activity of oleacein and the relative mechanism of action. Oleacein induced cell growth inhibition in 501Mel melanoma cells with an IC50 in the low micromolar range of concentrations. Moreover, an oleacein concentration approximating the IC50 induced G1/S phase arrest, DNA fragmentation, and downregulation of genes encoding antiapoptotic (BCL2 and MCL1) and proproliferative (c-KIT, K-RAS, PIK3R3, mTOR) proteins, while increased transcription levels of the proapoptotic protein BAX. Concordantly, oleacein increased the levels of miR-193a-3p, miR-34a-5p and miR-16-5p, while decreased miR-214-3p (targeting BAX). These modulatory effects might contribute to the inhibition of 501Mel melanoma cell growth observed after treatment with an olive leaves-derived formulation rich in oleacein, with potential application against in situ cutaneous melanoma.


Altogether, these results demonstrate the ability of OA to contrast the proliferation of cutaneous melanoma cells through the transcriptional modulation of relevant genes and microRNAs,confirming the anticancer potential of EVOO and suggesting OA as a chemopreventive agent for cancer disease therapy.



Fig| Oleacin® and Imiquimod decrease 501Mel cell viability, 501Mel cells were treated with 1, 50, and 100 µg/ml of
either Oleacin® or Imiquimod. Growth inhibition was measured at 72 h


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