Oleacein

Oleacein is a secoiridoid polyphenol that has been found in O. europea and has diverse biological activities.^1,2,3,4 It inhibits 5-lipoxygenase (5-LO; IC₅₀ = 2 µM for the human enzyme).¹ Oleacein (20 and 50 µM) reduces lipid accumulation and inhibits the transition into foam cells in human monocyte-derived macrophages.² It decreases lipid accumulation and levels of peroxisome proliferator-activated receptor γ (PPARγ) and fatty acid synthase (FASN), as well as increases adiponectin levels, in 3T3-L1 adipocytes.³ In vivo, oleacein (20 mg/kg) reduces macrophage and lymphocyte infiltration in abdominal fat tissue and adipocyte size in a mouse model of high-fat diet-induced obesity. Oleacein also delays disease onset and progression in a mouse model of experimental autoimmune encephalomyelitis (EAE).⁴

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1. Vougogiannopoulou, K., Lemus, C., Halabalaki, M., et al. One-step semisynthesis of oleacein and the determination as a 5-lipoxygenase inhibitor. J. Nat. Prod. 77(3), 441-445 (2014).

2. Filipek, A., Mikołajczyk, T.P., Guzik, T.J., et al. Oleacein and foam cell formation in human monocyte-derived macrophages: A potential strategy against early and advanced atherosclerotic lesions. Pharmaceuticals (Basel) 13(4), 64 (2020).

3. Lepore, S.M., Maggisano, V., Bulotta, S., et al. Oleacein prevents high fat diet-induced adiposity and ameliorates some biochemical parameters of insulin sensitivity in mice. Nutrients 11(8), 1829 (2019).

4. Gutiérrez-Miranda, B., Gallardo, I., Melliou, E., et al. Oleacein attenuates the pathogenesis of experimental autoimmune encephalomyelitis through both antioxidant and anti-inflammatory effects. Antioxidants (Basel) 9(11), 1161 (2020).