Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective

Oleacein (Olea) and Oleocanthal (Oleo) are two phenolic compounds found in olive oil. Cell and animal studies have shown these two compounds can modulate inflammation, cancer, and neurodegenerative diseases. Unfortunately, the study of the pharmacokinetics of these two compounds appears difficult du...

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Main Authors: Daniel Di Risola, Davide Laurenti, Francesca Ferraro, Alessia Ciogli, Simone Manetto, Yuri Gazzilli, Rodolfo Federico, Antonio Francioso, Luciana Mosca, Roberto Mattioli
Format: Article
Language:English
Published: MDPI AG 2025-04-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/7/1645
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author Daniel Di Risola
Davide Laurenti
Francesca Ferraro
Alessia Ciogli
Simone Manetto
Yuri Gazzilli
Rodolfo Federico
Antonio Francioso
Luciana Mosca
Roberto Mattioli
author_facet Daniel Di Risola
Davide Laurenti
Francesca Ferraro
Alessia Ciogli
Simone Manetto
Yuri Gazzilli
Rodolfo Federico
Antonio Francioso
Luciana Mosca
Roberto Mattioli
author_sort Daniel Di Risola
collection DOAJ
description Oleacein (Olea) and Oleocanthal (Oleo) are two phenolic compounds found in olive oil. Cell and animal studies have shown these two compounds can modulate inflammation, cancer, and neurodegenerative diseases. Unfortunately, the study of the pharmacokinetics of these two compounds appears difficult due to their high reactivity with primary amines. Indeed, the presence of primary amines in culture media and biological fluids raises the question as to whether the observed biological effects are attributable to the parent compounds or to their amine derivatives. In the present work, we investigated the adduct formation between Olea or Oleo and tris(hydroxymethyl)aminomethane (Tris), a well-known primary amine used primarily as a buffer system, showing that the reaction kinetics were extremely rapid. In addition, we assessed whether the newly formed Tris adducts, i.e., Olea-Tris and Oleo-Tris, retained their antioxidant capacity by means of the ABTS and DPPH radical scavenging assays, showing that their activity was partially maintained. Finally, we evaluated the anti-inflammatory activity of these adducts on murine BV-2 microglial cells stimulated with lipopolysaccharide (LPS) and kept in an amine-free culture medium, showing how the biological response varied as the compound was degraded. Taken together, these data demonstrate that the biological effects reported in the literature are mainly due to the amino-derivatives of Olea and Oleo rather than the polyphenols derived from their breakdown (tyrosol and hydroxytyrosol).
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spelling doaj-art-9dddcfc8eaf14726857ba3e821faf1982025-08-20T02:17:01ZengMDPI AGMolecules1420-30492025-04-01307164510.3390/molecules30071645Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical PerspectiveDaniel Di Risola0Davide Laurenti1Francesca Ferraro2Alessia Ciogli3Simone Manetto4Yuri Gazzilli5Rodolfo Federico6Antonio Francioso7Luciana Mosca8Roberto Mattioli9Department of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Chemistry and Technology of Drugs, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Chemistry and Technology of Drugs, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Chemistry and Technology of Drugs, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyActive-Italia S.r.l., Via delle Terme Deciane 10, 00153 Rome, ItalyDepartment of Bioscience and Technology for Food Agriculture and Environment, University of Teramo, 64100 Teramo, ItalyDepartment of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyDepartment of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, pl.e Aldo Moro 5, 00185 Rome, ItalyOleacein (Olea) and Oleocanthal (Oleo) are two phenolic compounds found in olive oil. Cell and animal studies have shown these two compounds can modulate inflammation, cancer, and neurodegenerative diseases. Unfortunately, the study of the pharmacokinetics of these two compounds appears difficult due to their high reactivity with primary amines. Indeed, the presence of primary amines in culture media and biological fluids raises the question as to whether the observed biological effects are attributable to the parent compounds or to their amine derivatives. In the present work, we investigated the adduct formation between Olea or Oleo and tris(hydroxymethyl)aminomethane (Tris), a well-known primary amine used primarily as a buffer system, showing that the reaction kinetics were extremely rapid. In addition, we assessed whether the newly formed Tris adducts, i.e., Olea-Tris and Oleo-Tris, retained their antioxidant capacity by means of the ABTS and DPPH radical scavenging assays, showing that their activity was partially maintained. Finally, we evaluated the anti-inflammatory activity of these adducts on murine BV-2 microglial cells stimulated with lipopolysaccharide (LPS) and kept in an amine-free culture medium, showing how the biological response varied as the compound was degraded. Taken together, these data demonstrate that the biological effects reported in the literature are mainly due to the amino-derivatives of Olea and Oleo rather than the polyphenols derived from their breakdown (tyrosol and hydroxytyrosol).https://www.mdpi.com/1420-3049/30/7/1645oleaceinoleocanthaloleo-trisolea-trisadduct stability
spellingShingle Daniel Di Risola
Davide Laurenti
Francesca Ferraro
Alessia Ciogli
Simone Manetto
Yuri Gazzilli
Rodolfo Federico
Antonio Francioso
Luciana Mosca
Roberto Mattioli
Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
Molecules
oleacein
oleocanthal
oleo-tris
olea-tris
adduct stability
title Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
title_full Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
title_fullStr Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
title_full_unstemmed Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
title_short Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
title_sort spontaneous reaction of oleacein and oleocanthal with primary amines a biochemical perspective
topic oleacein
oleocanthal
oleo-tris
olea-tris
adduct stability
url https://www.mdpi.com/1420-3049/30/7/1645
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