Oleocanthal: New data on its effect on human health

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In January 2021, a new study was published titled «Spontaneous In Vitro and In Vivo Interaction of Oleocanthal with Glycine in Biological Fluids: Novel Pharmacokinetic Markers».

This particular publication was made by the following scientists: Lucy I. Darakjian, Aimilia Rigakou, Andrew Brannen, Mohammed H. Qusa, Niki Tasiakou, Panagiotis Diamantakos, Miranda N. Reed, Peter Panizzi, Melissa D. Boersma, Eleni Melliou, Khalid A. El Sayed, Prokopios Magiatis, and Amal Kaddoumi. It was published in ACS Pharmacology & Translational Science on January 5, 2021 (ACS Pharmacol. Transl. Sci. 2021, 4, 1, 179–192).

This publication is about the discovery of the way in which oleocanthal, when entering our body, is transformed into an active form through a specific mechanism, which can quickly reach even the brain.

Since the first discovery of its ibuprofen-like anti-inflammatory activity in 2005, the olive phenolic oleocanthal gained great scientific interest and popularity due to its reported health benefits.

Oleocanthal is a monophenolic secoiridoid exclusively occurring in extra-virgin olive oil (EVOO). While several groups have investigated oleocanthal pharmacokinetics and disposition, none was able to detect oleocanthal in biological fluids or identify its pharmacokinetic profile that is essential for translational research studies. Besides, oleocanthal could not be detected following its addition to any fluid containing amino acids or proteins such as plasma or culture media, which could be attributed to its unique structure with two highly reactive aldehyde groups.

Here, the scientists demonstrated that oleocanthal spontaneously reacts with amino acids, with high preferential reactivity to glycine compared to other amino acids or proteins, affording two products: an unusual glycine derivative with a tetrahydropyridinium skeleton that is named oleoglycine, and according to their collective data, the plausible formation of tyrosol acetate as the second product.

They performed extensive studies to validate and confirm oleocanthal reactivity, which were followed by pharmacokinetic disposition studies in mice, as well as cell culture transport studies to determine the ability of the formed derivatives to cross physiological barriers such as the blood-brain barrier.

Thus, they showed for the first time that oleocanthal is biochemically transformed to novel products in amino acids/glycine-containing fluids, which were successfully monitored in vitro and in vivo, creating a completely new perspective to understand the well-documented bioactivities of oleocanthal in humans.

Nick Sakellaropoulos
Chemical Engineer M.Sc.
Production Manager
Sakellaropoulos Organic Farms

SourceSpontaneous In Vitro and In Vivo Interaction of (−)-Oleocanthal with Glycine in Biological Fluids: Novel Pharmacokinetic Markers , ACS Pharmacol. Transl. Sci. 2021, 4, 1, 179–192