Oleacein Intestinal Permeation and Metabolism in Rats Using an In Situ Perfusion Technique
| Autor: | Maria Pérez, Anna Vallverdú-Queralt, Anallely López-Yerena, Elvira Escribano-Ferrer, Eleftherios Miliarakis, Rosa M. Lamuela-Raventós |
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| Rok vydání: | 2021 |
| Předmět: |
Naproxen
secoiridoids Metabolite Pharmaceutical Science Ileum phenolic compounds Absorption (skin) 030226 pharmacology & pharmacy Article extra virgin olive oil Permeability 03 medical and health sciences chemistry.chemical_compound Pharmacy and materia medica 0302 clinical medicine medicine 030304 developmental biology 0303 health sciences Intestins Intestinal permeability Chromatography biology intestinal permeability Permeabilitat medicine.disease biology.organism_classification Metabolisme Bioavailability RS1-441 Oli d'oliva Intestines medicine.anatomical_structure Metabolism chemistry Olea bioavailability metabolism Olive oil Blood sampling medicine.drug |
| Zdroj: | Dipòsit Digital de la UB Universidad de Barcelona Pharmaceutics, Vol 13, Iss 719, p 719 (2021) Pharmaceutics Volume 13 Issue 5 |
| Popis: | Oleacein (OLEA) is one of the most important phenolic compounds in extra virgin olive oil in terms of concentration and health-promoting properties, yet there are insufficient data on its absorption and metabolism. Several non-human models have been developed to assess the intestinal permeability of drugs, among them, single-pass intestinal perfusion (SPIP), which is commonly used to investigate the trans-membrane transport of drugs in situ. In this study, the SPIP model and simultaneous luminal blood sampling were used to study the absorption and metabolism of OLEA in rats. Samples of intestinal fluid and mesenteric blood were taken at different times and the ileum segment was excised at the end of the experiment for analysis by LC–ESI–LTQ–Orbitrap–MS. OLEA was mostly metabolized by phase I reactions, undergoing hydrolysis and oxidation, and metabolite levels were much higher in the plasma than in the lumen. The large number of metabolites identified and their relatively high abundance indicates an important intestinal first-pass effect during absorption. According to the results, OLEA is well absorbed in the intestine, with an intestinal permeability similar to that of the highly permeable model compound naproxen. No significant differences were found in the percentage of absorbed OLEA and naproxen (48.98 ± 12.27% and 43.96 ± 7.58%, respectively). |
| Databáze: | OpenAIRE |
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