Absorption and Intestinal Metabolic Profile of Oleocanthal in Rats

Pharmaceutics

Elvira Escribano-Ferrer¹  Raf Mols²  Patrick Augustijns²  Anna Vallverdú-Queralt³  Anallely López-Yerena³  Rosa M. Lamuela-Raventós³ 

[1] CIBER Physiopathology of Obesity and Nutrition (CIBEROBN), Institute of Health Carlos III, 28029 Madrid, Spain;Drug Delivery and Disposition, KU Leuven, 3000 Leuven, Belgium;Nutrition, Food Science and Gastronomy Department, XaRTA, Institute of Nutrition and Food Safety (INSA-UB), School of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain;

关键词: bioavailability;    metabolism;    in situ perfusion;    permeability;    extra virgin olive oil;    secoiridoids;   

DOI  :  10.3390/pharmaceutics12020134

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown