| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1147 | |
| Phytochemical name or plant extracts | Oleuropein | |
| PMID | 33297339 | |
| Literature evidence | This compound has been shown to have potent properties in various types of cancers, including breast cancer. | |
| IUPAC name | methyl (4S,5E,6S)-4-[2-[2-(3,4-dihydroxyphenyl)ethoxy]-2-oxoethyl]-5-ethylidene-6-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4H-pyran-3-carboxylate | |
| Phytochemicals’ class or type of plant extracts | Polyphenol | |
| Source of phytochemicals or plant Extracts | Olea europaea | |
| Geographical availability | Afghanistan, Albania, Algeria, Angola, Baleares, Botswana, Burundi, Canary Is., Cape Provinces, China South-Central, Cyprus, Djibouti, East Aegean Is., Eritrea, Ethiopia, Free State, Greece, Iran, Italy, Kenya, Kriti, KwaZulu-Natal, Lesotho, Libya, Madeira, Malawi, Mauritius, Morocco, Mozambique, Namibia, Nepal, Niger, Northern Provinces, Oman, Pakistan, Palestine, Portugal, Rwanda, Réunion, Sardegna, Saudi Arabia, Sicilia, Somalia, Spain, Sudan, Swaziland, Tanzania, Tunisia, Turkey, Turkey-in-Europe, Uganda, West Himalaya, Yemen, Yugoslavia, Zambia, Zaïre, Zimbabwe | |
| Plant parts | Fruits and Leaves | |
| Other cancers | Breast cancer | |
| Target gene or protein | CASP1, CASP14, FADD, TNFRSF21, GADD45A, CYCS, BNIP2, BNIP3, BID, BCL10, CFLAR, BFAR, BRAF, IAP, BIRC3, RIPK2, TNFRSF10A, CASP4, CASP6, PYD, PAYCARD, BIRC5, TNFRSF11B, HDAC2, HDAC3 | |
| Gene or Protein evidence | In MDA-MB-468 cells, OL induced a noticeable transcription activation in fourteen genes, including two members of the caspase family: caspase 1 (CASP1) and caspase 14 (CASP14), two members of the TNF receptor superfamily: Fas-associated via death domain (FADD) and TNF receptor superfamily 21 (TNFRSF21), six other proapoptotic genes: growth arrest and DNA damage-inducible 45 alpha (GADD45A), cytochrome c somatic (CYCS), BCL-2 interacting protein 2 (BNIP2), BCL-2 interacting protein 3 (BNIP3), BH3 interacting domain death agonist (BID), and B-cell lymphoma/leukemia 10 (BCL10), and the CASP8 and FADD-like apoptosis regulator (CFLAR) gene. Moreover, in MDA-MB-468 cells, OL induced a significant upregulation in two antiapoptotic genes: bifunctional apoptosis regulator (BFAR) and B-Raf proto-oncogene (BRAF) and a baculoviral inhibitor of apoptosis (IAP) repeat-containing 3 (BIRC3). On the contrary, in MDA-MB-231 cells, OL showed mixed impacts on gene expression. OL significantly upregulated the mRNA expression of four genes: BIRC3, receptor-interacting serine/threonine kinase 2 (RIPK2), TNF receptor superfamily 10A (TNFRSF10A), and caspase 4 (CASP4). Additionally, another four genes were repressed, including caspase 6 (CASP6), pyrin domain (PYD), and caspase recruitment domain (CARD)-containing (PAYCARD), baculoviral IAP repeat-containing 5 (BIRC5), and the most downregulated TNF receptor superfamily member 11B (TNFRSF11B, 16.34-fold). Downregulation of HDAC2 and HDAC3 via oleuropein as a potent prevention and therapeutic agent in MCF-7 breast cancer cells. | |
| Target pathways | OL modulates the inflammatory pathway and inhibits the Toll-like receptor (TLR) signaling by downregulating NOS, COX2, ERK1/2, JNK, and nuclear factor of kappa light polypeptide gene, as well as the pro-inflammatory cytokine interleukin 6 (IL-6), interleukin 1β (IL-1β), and the gene AP-1. In MDA-MB-468 cells, the significantly upregulated FADD receptor may be involved in the extrinsic and TRAIL-induced apoptotic pathway through caspase activation | |
| IC50 | 492.45 ± 3.28 µM against MDA-MB-231 266.5 ± 5.24 µM against MDA-MB-468 | |
| Potency | We confirmed that OLE, containing a quantity of oleuropein of 87 % of the total extract, shows anti-proliferative and pro-apoptotic activity on MDA-MB-231 cells. The results obtained from this study should also guide the potential utilization of oleuropein as an adjunct therapy for TNBC to increase chemotherapy effectiveness and prevent cancer progression. | |
| Cell line/ mice model | MDA-MB-468, MDA-MB-231, SKBR-3 | |
| Additional information | OL was found to reduce inflammatory angiogenesis by suppressing different MMPs family members’ expression and the vascular endothelial growth factor (VEGF) by reducing the pro-inflammatory enzyme COX2. Moreover, OL modulates the inflammatory pathway and inhibits the Toll-like receptor (TLR) signaling by downregulating NOS, COX2, ERK1/2, JNK, and nuclear factor of kappa light polypeptide gene, as well as the pro-inflammatory cytokine interleukin 6 (IL-6), interleukin 1β (IL-1β), and the gene AP-1. | |
| PubChem ID | 5281544 | |
| Additional PMIDs | 33117773 26873189 32013090 31038081 33297339 30618185 23201137 18069902 18813848 19094209 23146235 29753866 33360155 18208790 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:610675-1 | |
| Safety | NA |