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Article

Oleacein Attenuates Lipopolysaccharide-Induced Inflammation in THP-1-Derived Macrophages by the Inhibition of TLR4/MyD88/NF-κB Pathway †

1
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina, Italy
2
Department of Pharmacy-Drug Sciences, University of Bari “Aldo Moro”, 70125 Bari, Italy
3
Fondazione “Prof. Antonio Imbesi”, 98168 Messina, Italy
*
Author to whom correspondence should be addressed.
We wish to honor the memory of our beloved friend and colleague Dr. Nadia Ferlazzo dedicating this study to her.
Academic Editor: Monica Currò
Int. J. Mol. Sci. 2022, 23(3), 1206; https://doi.org/10.3390/ijms23031206
Received: 31 December 2021 / Revised: 14 January 2022 / Accepted: 20 January 2022 / Published: 21 January 2022
It is known that plant phenolic compounds exert anti-inflammatory activity through both anti-oxidant effects and modulation of pivotal pro-inflammatory factors. Recently, Olea europaea has been studied as a natural source of bioactive molecules; however, few studies have focused on the biological effect of oleacein (OLC), the most abundant secoiridoid. Therefore, the aim of this study was to investigate the potential anti-oxidant activity of OLC, as well as to study its anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated THP-1-derived macrophages. LPS brought a dramatic increase of both release and gene expression of pro-inflammatory cytokines (IL-6, IL-1β and TNF-α), as well as a decrease of anti-inflammatory ones (IL-10), the effects of which are reverted by OLC. Moreover, it reduced the levels of COX-2, NO and PGE2 elicited by LPS exposure in THP-1 macrophages. Interestingly, OLC modulated inflammatory signaling pathways through the inhibition of CD14/TLR4/CD14/MyD88 axis and the activation of NF-κB. Finally, OLC showed relevant anti-oxidant capability, assessed by abiotic assays, and reduced the intracellular amount of ROS generated by LPS exposure in THP-1 macrophages. Overall, these results suggest that the anti-oxidant activity and anti-inflammatory effect of OLC may cooperate in its protective effect against inflammatory stressors, thus being a possible alternative pharmacological strategy aimed at reducing the inflammatory process. View Full-Text
Keywords: oleacein; Olea europea; inflammation; LPS; THP-1 monocytes; CD14; TLR4; NF-κB; MyD88; ROS oleacein; Olea europea; inflammation; LPS; THP-1 monocytes; CD14; TLR4; NF-κB; MyD88; ROS
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MDPI and ACS Style

Cirmi, S.; Maugeri, A.; Russo, C.; Musumeci, L.; Navarra, M.; Lombardo, G.E. Oleacein Attenuates Lipopolysaccharide-Induced Inflammation in THP-1-Derived Macrophages by the Inhibition of TLR4/MyD88/NF-κB Pathway. Int. J. Mol. Sci. 2022, 23, 1206. https://doi.org/10.3390/ijms23031206

AMA Style

Cirmi S, Maugeri A, Russo C, Musumeci L, Navarra M, Lombardo GE. Oleacein Attenuates Lipopolysaccharide-Induced Inflammation in THP-1-Derived Macrophages by the Inhibition of TLR4/MyD88/NF-κB Pathway. International Journal of Molecular Sciences. 2022; 23(3):1206. https://doi.org/10.3390/ijms23031206

Chicago/Turabian Style

Cirmi, Santa, Alessandro Maugeri, Caterina Russo, Laura Musumeci, Michele Navarra, and Giovanni E. Lombardo. 2022. "Oleacein Attenuates Lipopolysaccharide-Induced Inflammation in THP-1-Derived Macrophages by the Inhibition of TLR4/MyD88/NF-κB Pathway" International Journal of Molecular Sciences 23, no. 3: 1206. https://doi.org/10.3390/ijms23031206

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