Abstract
Oleocanthal (OLC), a phenolic compound of extra virgin olive oil (EVOO), has emerged as a potential therapeutic agent against a variety of diseases due to its anti-inflammatory activity. The aim of the present study is to explore its in vivo intestinal absorption and metabolism. An in situ perfusion technique in rats was used, involving simultaneous sampling from the luminal perfusate and mesenteric blood. Samples were analysed by UHPLC–MS–MS for the presence of oleocanthal (OLC) and its metabolites. OLC was mostly metabolized by phase I metabolism, undergoing hydration, hydrogenation and hydroxylation. Phase II reactions (glucuronidation of hydrogenated OLC and hydrated metabolites) were observed in plasma samples. OLC was poorly absorbed in the intestine, as indicated by the low effective permeability coefficient (2.23 ± 3.16 × 10−5 cm/s) and apparent permeability coefficient (4.12 ± 2.33 × 10−6 cm/s) obtained relative to the values of the highly permeable reference compound levofloxacin (LEV). The extent of OLC absorption reflected by the area under the mesenteric blood-time curve normalized by the inlet concentration (AUC) was also lower than that of LEV (0.25 ± 0.04 vs. 0.64 ± 0.03, respectively). These results, together with the observed intestinal metabolism, suggest that OLC has a moderate-to-low oral absorption; but higher levels of OLC are expected to reach human plasma vs. rat plasma.
Highlights
The secoiridoids are the most abundant and complex family of phenolic compounds in extra virgin olive oil (EVOO)
The main secoiridoids compounds identified in EVOO are the monoaldehydic forms of oleuropein (3,4-DHPEA-EA) and ligstroside aglycones (p-HPEA-EA) and the dialdehydic forms of their decarboxymethylated derivatives, oleacein (3,4-DHPEA-EDA) and oleocanthal (p-HPEA-EDA) [1]
The difference in LEV values can be attributed to P-glycoprotein (P-gp) binding [42,43] and in the case of OLC, to microbiota and gut wall metabolism, according to the results reported in the previous section (Section 3.1)
Summary
The secoiridoids are the most abundant and complex family of phenolic compounds in extra virgin olive oil (EVOO). Since its identification in 1993 [2], oleocanthal (OLC) has been targeted by numerous in vitro and in vivo studies aiming to understand the health effects of EVOO consumption [3]. OLC exerts a neuroprotective effect in conditions such as Alzheimer’s disease [6,7] and has shown promising chemotherapeutic properties, reducing cell proliferation and promoting cell death through different mechanisms of action [8]. Antirheumatic activity has been demonstrated in in vitro studies, in which OLC ameliorated osteoarthritis and rheumatoid arthritis [3]. OLC has been shown to be beneficial for cardiovascular health, improving endothelial function in patients with early atherosclerosis and reducing platelets in healthy men [3]
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