Anti-tumor Activity and Epigenetic Impact of thePolyphenol Oleacein in Multiple Myeloma

In 2019, Juli and her partners By, investigated the anti-tumor potential of oleacein and the underlying bio-molecular sequelae using in vitro models of human multiple myeloma (MM). Within a low micromolar range, oleacein reduced the viability of MM primary samples and cell lines even in the presence of bone marrow stromal cells (BMSCs), while sparing healthy peripheral blood mononuclear cells. Oleacein also inhibited MM cell clonogenicity, prompted cell cycle blockade and triggered apoptosis. They evaluated the epigenetic impact of oleacein on MM cells, and observed dose-dependent accumulation of both acetylated histones and α-tubulin, along with down-regulation of several class I/II histone deacetylases (HDACs) both at the mRNA and protein level, providing evidence of the HDAC inhibitory activity of this compound; Of potential translational significance, oleacein synergistically enhanced the in vitro anti-MM activity of the proteasome inhibitor carfilzomib. Altogether, these results indicate that oleacein is endowed with HDAC inhibitory properties, which associate with significant anti-MM activity both as single agent or in combination with carfilzomib.


Oleacein is a component with histone inhibitory properties, which are associated with significant antitumor activity both as a single agent and in combination with carfilzomib.


Fig. Effects of oleacein on multiple myeloma (MM) cell survival.. Cell viability of MM cell lines as determined by Cell Titer Glo (CTG) assay 48 h after treatment with increasing doses of oleacein or vehicle (DMSO). CTG assay performed on peripheral blood mononuclear cells (PBMCs) from three different healthy donors treated with oleacein for 48 h


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