Pharmacokinetics and metabolism of oleocanthal, a natural anti-inflammatory agent of olive oil

Oleocanthal (Oleo) is a secoiridoid exclusively found in olive oil, which lately gained great scientific interest due to its strong anti-inflammatory activity [1]. Several biological properties have been ascribed to Oleo and its administration has been associated with the reduce of inflammation markers and the prevention of various human pathologies [2]. However, limited data exist for Oleo metabolic fate in in vivo systems, which could evidence the mechanisms behind its biological activities. Furthermore, its pharmacokinetic properties (PK) have never been described so far. Interestingly, Oleo has never been detected in biological fluids, possibly due to its sensitive and labile chemical structure consisted of two highly reactive aldehydes and an easily hydrolyzed ester bond. In the current study, a suitable mice model based protocol was set in a standard Oleo dose of 5 mg/Kg and plasma samples were collected in five different time points. For this purpose, an optimized extraction protocol was developed for the recovery of Oleo from mice plasma and a special UPLC-Orbitrap-MS methodology was developed and applied for the detection of Oleo and its metabolic derivatives in mice plasma. The PK characteristics (Tmax and/or Cmax) of Oleo were studied and its metabolic derivatives were identified and determined in time along with their relative content. Biomarkers were proposed and associated for the first time with Oleo supplementation in vivo.

The authors declare no conflict of interest

The authors would like to thank DDIOL project (project code: 5 070 020).

Publikationsverlauf

Artikel online veröffentlicht:
12. Dezember 2022

• References

• 1 Beauchamp GK. et al. . Nature 2005; 437(7055): 45-46
• 2 Francisco VJ. et al. . Agric Food Chem 2019; 67: 3845-3853