Authors:
Nikolaos V. Angelis, Efthymios Paronis, Georgia Sarikaki, Antonios Kyriakopoulos, Anna Agapaki, Pigi-Maria Niotopoulou, Christina C. Knai, Pavlos Alexakos, Odyssefs Liagkas, Konstantinos F. Mavreas, Constantin N. Baxevanis, Alexios-Leandros Skaltsounis, Ourania E. Tsitsilonis*,†, Ioannis K. Kostakis
Inflammation is a key process in the pathophysiology of many diseases, with macrophages playing a central role in its initiation and progression. This study examines the anti-inflammatory activity of a new semisynthetic derivative of oleuropein (OP), the main metabolite of the olive tree (Olea europaea).
This derivative, named Ole-Oxy, was designed by introducing an oxygen atom between the aromatic ring and the aliphatic chain of oleuropein, with the aim of enhancing its interaction with proteins and improving its bioactivity.
Key findings:
- In vitro: Ole-Oxy showed strong anti-inflammatory activity in THP-1 macrophages differentiated with phorbol 12-myristate 13-acetate (PMA), where it:
- Significantly reduced levels of interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), and reactive oxygen species (ROS)
- Its activity surpassed that of unmodified oleuropein
- In vivo: In experimental models of acute inflammation in the skin and colon of C57BL/6J mice, Ole-Oxy demonstrated significant efficacy, probably due to their Th1-oriented immune response.
Conclusions:
The findings suggest that Ole-Oxy acts against inflammation through:
- Scavenging of ROS (antioxidant activity)
- Modulation of macrophage activation
These results highlight the need for further studies to clarify the full mechanism of action of the molecule and to optimize its pharmacokinetic properties, with the ultimate goal of its future use in therapeutic applications.
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