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. 2020 Feb 5;12(2):134.
doi: 10.3390/pharmaceutics12020134.

Absorption and Intestinal Metabolic Profile of Oleocanthal in Rats

Anallely López-Yerena  1 , Anna Vallverdú-Queralt  1   2 , Raf Mols  3 , Patrick Augustijns  3 , Rosa M Lamuela-Raventós  1   2 , Elvira Escribano-Ferrer  2   4
Affiliations

Absorption and Intestinal Metabolic Profile of Oleocanthal in Rats

Anallely López-Yerena et al. Pharmaceutics. .

Erratum in

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.

Keywords: bioavailability; extra virgin olive oil; in situ perfusion; metabolism; permeability; secoiridoids.

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Conflict of interest statement

R.M.L.-R. reports receiving lecture fees from Cerveceros de España and receiving lecture fees and travel support from Adventia. The other authors declare no conflict of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, or in the decision to publish the results.

Figures

Figure 1
Figure 1
Chemical structure of oleocanthal and metabolites (A) = hydroxylated OLC; (B) = hydrated OLC; (C) = hydrogenated glucuronide; (D) = hydrated glucuronide).
Figure 2
Figure 2
Peak area ratio metabolite/oleocanthal (OLC) as a function of time in lumen. Results are expressed as the mean ± standard deviation.
Figure 3
Figure 3
Peak area ratio metabolite/OLC as a function of time in plasma. Results are expressed as the mean ± standard deviation.
Figure 4
Figure 4
Tentative interactions of oleocanthal (OLC) with metabolic enzymes and transporters.
Figure 5
Figure 5
Transport of oleocanthal (OLC) (right Y-axis scale) and levofloxacin (left Y-axis scale) from the intestinal lumen to the mesenteric blood. Cumulative amount values are normalised to a 10-cm intestinal segment. Results are expressed as the mean ± standard deviation.
See this image and copyright information in PMC

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