Anticancer molecular mechanisms of oleocanthal

Abstract

Cancer is among the leading causes of mortality worldwide. Current cancer therapies are associated with serious side effects, which further damage patients' health. Therefore, the search for new anticancer agents with no toxic effects on normal and healthy cells is of great interest. Recently, we and other groups have demonstrated that oleocanthal (OLC), a phenolic compound from extra virgin olive oil, exhibits antitumor activity in various tumor models. However, the underlying mechanisms and intracellular targets of OLC remain to be completely elucidated. This review summarizes the current advancers concerning the anticancer activity of OLC, with particular emphasis on the molecular signaling pathways modulated by this compound in different tumor cell types. The major mechanisms of action of OLC include modulation of the apoptotic pathway, the HGF/c-Met pathway, and the signal transducer and activator of transcription 3 signaling pathway, among others. Furthermore, OLC has synergistic effects with anticancer drugs in vitro. Also discussed are OLC bioavailability and its concentration in olive oil. Data summarized here will represent a database for more extensive studies aimed at providing information on molecular mechanisms against cancer induced by OLC.

Dietary Oleocanthal Supplementation Prevents Inflammation and Oxidative Stress in Collagen-Induced Arthritis in Mice

“…The OLE-linked pungent sensation seems to be mediated via the activation of transient receptor potential cation channel subtype A1 (TRPA1), which is known to mediate neurogenic and chronic inflammation [ 15 ]. Nevertheless, OLE is getting more scientific attention due to its interesting biological activities, most antioxidant, anti-inflammatory, antimicrobial, anticancer and neuroprotective effects [ 13 , 16 ] , even though it makes up only 10% of the olive’s polyphenols (0.2 mg/kg up to 498 mg/kg) influenced by several different factors such as geographical location, olive fruit maturity, agricultural techniques, oil extraction and storage conditions, or even cooking procedures [ 16 ]. It is noteworthy that diet consumption of 25–50 mL EVOO provides around 10 mg of OLE daily, corresponding to near 10% of ordinary ibuprofen dose [ 15 , 16 ].…”

Therapeutic Properties and Use of Extra Virgin Olive Oil in Clinical Nutrition: A Narrative Review and Literature Update

“… Control of cell proliferation. Phenolic compounds, such as oleocanthal, are able to act on the expression of genes that control the proliferation, apoptosis, and differentiation of cancer cells [ 13 , 33 , 34 , 133 ]. There is in vitro evidence showing that polyphenols in EVOO alter microRNAs in cancer cells, while hydroxytyrosol appears to exert strong antiproliferative effects in human colon adenocarcinoma cells [ 14 ].…”

“…Of particular interest in this clinical population are the possible effects of oleic acid on satiety and oral tolerance to oleic acid-based formulas. In clinical trials with healthy volunteers, oleic acid ingestion was shown to induce greater postprandial satiety [ 132 ] by increasing levels of the endocannabinoid oleylethanolamide, which was associated with a reduced caloric intake at the next meal [ 133 ]. However, this satiating capacity may be lost in overweight or obese individuals, due to a reduced hormonal and motor response to oleic acid intake because of their higher BMI and habitual dietary fat intake [ 134 ].…”

An Oleocanthal-Enriched EVO Oil Extract Induces the ROS Production in Gastric Cancer Cells and Potentiates the Effect of Chemotherapy

“…In this study, we used an OC enriched EVO oil extract (OCF), in which the OC represents 55.1% of the total content. The OC concentration in the EVO oils is variable, ranging from 0.2 mg/kg to 498 mg/kg [ 41 ], depending on several factors, such as the cultivar and the production techniques [ 42 ], and it represents about 10% of the total phenolic compounds in the EVO oil [ 43 , 44 ]. The data regarding the OC bioavailability are very few, even if the OC metabolites have been found in human urine [ 45 , 46 ].…”