Cancer is a multifaceted and genomically complex disease. Rapidly accumulating preclinical
and clinical studies are emphasizing on wide ranging molecular mechanisms that underpin
cancer development, progression and metastasis. Intratumor heterogeneity, loss of apoptosis, rapidly
developing resistance against molecular therapeutics and off-target effects are some of the deeply
studied resistance mechanisms. Data obtained through high-throughput technologies has considerably enhanced our understanding
of the intracellular signaling cascades frequently dysregulated spatio-temporally. There is an ever-expanding
list of synthetic and natural agents reported to activate tumor suppressor genes and inhibit oncogenes in cancer cells.
Markedly reduced tumor growth has also been documented in xenografted mice administered with phytochemicals. Oleuropein
is a bioactive ingredient isolated from various sources and there is evidence of complete regression of tumors in 9-
12 days in mice orally administered with Oleuropein. In this review we summarize recent developments in use of Oleuropein
as an anticancer agent. Extraction and isolation of Oleuropein and how it modulates intracellular signaling network
to induce apoptosis in cancer cells. Human epidermal growth factor receptor 2 (HER2) frequently overexpressed in breast
cancer cells is inhibited by Oleuropein. Interestingly, trastuzumab efficacy was notably enhanced in Oleuropein treated
breast cancer cells. There is still insufficient information related to Oleuropein mediated microRNA regulation in cancer
cells. We still do not have information about regulation of different signaling cascades by Oleuropein which are deregulated
in cancer. Future studies must converge on a deeper analysis of target molecular network of Oleuropein and its efficacy
as a tumor growth inhibitor in xenografted mice.
Keywords: Oleuropein, HER2, Cancer cell apoptosis, MAPK pathway, PI3K/AKT.
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