Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2017 Apr 29;22(5):705.
doi: 10.3390/molecules22050705.

Oleuropein and Cancer Chemoprevention: The Link is Hot

Ammad Ahmad Farooqi  1 , Sundas Fayyaz  2 , Ana Sanches Silva  3   4 , Antoni Sureda  5 , Seyed Fazel Nabavi  6 , Andrei Mocan  7   8 , Seyed Mohammad Nabavi  9 , Anupam Bishayee  10
Affiliations
Review

Oleuropein and Cancer Chemoprevention: The Link is Hot

Ammad Ahmad Farooqi et al. Molecules. .

Abstract

Cancer comprises a collection of related diseases characterized by the existence of altered cellular pathways resulting in an abnormal tendency for uncontrolled growth. A broad spectrum, coordinated, and personalized approach focused on targeting diverse oncogenic pathways with low toxicity and economic natural compounds can provide a real benefit as a chemopreventive and/or treatment of this complex disease. Oleuropein, a bioactive phenolic compound mainly present in olive oil and other natural sources, has been reported to modulate several oncogenic signalling pathways. This review presents and critically discusses the available literature about the anticancer and onco-suppressive activity of oleuropein and the underlying molecular mechanisms implicated in the anticarcinogenic and therapeutic effects. The existence of limitations and the promising perspectives of research on this phenolic compound are also critically analyzed and discussed.

Keywords: cancer; chemopreventive effect; oleuropein; olive oil.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of oleuropein [19].
Figure 2
Figure 2
Various anticancer molecular mechanisms of oleuropein. (A) HER2 is proteolytically processed that is inhibited by oleuropein. Deacetoxyoleuropein aglycone inhibits activation of HER2. Malonyl-coenzyme A (CoA) plays a role in transcriptional repression of ERBB2 by facilitating entry of PEA3 in the nucleus. PEA3 binding sites are present within the promoter region of ERBB2. ERBB2 overexpressing breast cancer cells had lower levels of PEA3. As a result of oleuropein aglycone and oleuropein glycoside-mediated inhibition of FASN, higher levels of malonyl–CoA continue to be generated. Cytosolic accumulation of higher levels of malonyl-CoA triggered an increase and entry of PEA3 in the nucleus, where it occupied the PEA3 binding site and transcriptionally repressed ERBB2; (B) Hypoxia-inducible factor (HIFα) enters into the nucleus and transcriptionally represses miR-519d. miR-519d is involved in negative regulation of PDRG1 in cancer cells. However, treatment of cancer cells with oleuropein inhibits HIFα-mediated transcriptional repression of miR-519d and consequently miR-519d quantitatively inhibits PDRG1.
Figure 3
Figure 3
Pro-apoptotic molecular mechanisms of oleuropein in cancer cells. (a) Oleuropein mediated reduction of p-AKT levels. (b) Oleuropein enhanced p-JNK levels and reduced ERK1/2.
See this image and copyright information in PMC

References

    1. Aanasov A.G., Waltenberger B., Pferschy-Wenzig E.M., Linder T., Wawrosch C., Uhrin P., Temml V., Wang L., Schwaiger S., Heiss E.H. Discovery and resupply of pharmacologically active plant-derived natural products: A review. Biotechnol. Adv. 2015;33:1582–1614. doi: 10.1016/j.biotechadv.2015.08.001. - DOI - PMC - PubMed
    1. Marchese A., Orhan I.E., Daglia M., Barbieri R., Di Lorenzo A., Nabavi S.F., Gortzi O., Izadi M., Nabavi S.M. Antibacterial and antifungal activities of thymol: A brief review of the literature. Food Chem. 2016;210:402–414. doi: 10.1016/j.foodchem.2016.04.111. - DOI - PubMed
    1. Russo M., Russo G.L., Daglia M., Kasi P.D., Ravi S., Nabavi S.F., Nabavi S.M. Understanding genistein in cancer: The “good” and the “bad” effects: A review. Food Chem. 2016;196:589–600. doi: 10.1016/j.foodchem.2015.09.085. - DOI - PubMed
    1. Wolfender J.L., Eugster P.J., Bohni N., Cuendet M. Advanced methods for natural product drug discovery in the field of nutraceuticals. CHIMIA Int. J. Chem. 2011;65:400–406. doi: 10.2533/chimia.2011.400. - DOI - PubMed
    1. Nabavi S.M., Marchese A., Izadi M., Curti V., Daglia M., Nabavi S.F. Plants belonging to the genus Thymus as antibacterial agents: From farm to pharmacy. Food Chem. 2015;173:339–347. doi: 10.1016/j.foodchem.2014.10.042. - DOI - PubMed

LinkOut - more resources