The Biological Activities of Oleocanthal from a Molecular Perspective

Kok-Lun Pang, Kok-Yong Chin, Kok-Lun Pang, Kok-Yong Chin

Abstract

Oleocanthal is a minor constituent of olive oil with strong anti-inflammatory activities. Since the pathogenesis of many chronic diseases involves inflammatory and oxidative components, oleocanthal is a promising agent to prevent these conditions. This review aimed to summarise the current beneficial health effects of oleocanthal and the molecular basis of its biological actions. The anti-inflammatory, antioxidative, antimicrobial, anticancer and neuroprotective activities of oleocanthal have been examined by previous studies. Of these, studies on the anticancer effects have been the most extensive. Oleocanthal was reported to suppress melanoma, breast, liver, and colon cancer cells. Neurological studies focused on the effects of oleocanthal against Alzheimer’s disease. Oleocanthal improved clearance of the amyloid beta protein from neurons and reduced the inflammation of astrocytes. Despite the positive results, validation of the biological effects of oleocanthal in animal disease models is limited and should be emphasized in the future. As a conclusion, oleocanthal may act together with other bioactive compounds in olive oil to achieve its therapeutic potential. The use of oleocanthal alone as a single therapeutic measure awaits validation from future studies.

Keywords: Alzheimer’s disease; antioxidant; cancer; inflammation; neuroprotection; oleocanthal; olive.

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of natural oleocanthal (OC).
Figure 2
Figure 2
Anti-inflammatory, antioxidant and antimicrobial activities of OC. Abbreviation: ↓ stands for downregulation; NOX = nicotinamide adenine dinucleotide phosphate oxidase; ROS = reactive oxygen species; COX 1/2 = cyclooxygenase 1/2; 5-LOX = 5-lipoxygenase; iNOS = inducible nitric oxide synthase; eNOS = endothelial nitric oxide synthase; NO = nitric oxide; GFAP = glial fibrillary acidic protein; IL-1β = interleukin-1β; IL-6 = interleukin-6; GM-CSF = granulocyte-macrophage colony-stimulating factor; MIP-1α = macrophage inflammatory protein-1α; TBI = traumatic brain injury; LPS = lipopolysaccharide;TNF-α = tumour necrosis factor-α
Figure 3
Figure 3
Anticancer properties of OC and the molecular mechanisms of action. Abbreviation: ↓ stands for downregulation; ↑ stands for upregulation; AMPK = adenosine monophosphate-activated protein kinase; ROS = reactive oxygen species; MIP-1α = macrophage inflammatory protein-1α; RANKL = receptor activator of nuclear factor κB ligand; ERK 1/2 = extracellular signal-regulated kinase 1/2; mTOR = mammalian targets of rapamycin; Bcl-2 = B cell lymphoma-2; Bcl-XL = B cell lymphoma-XL; Mcl-1 = myeloid cell leukemia-1; gp80 = interleukin-6 receptor; gp130 = interleukin-6 receptor’s signal-transducing subunit; SHP-1 = Src homology 2 domain tyrosine phosphatase-1; JAK 1/2 = Janus kinase 1/2; STAT3 = signal transducer and activator of transcription 3; VEGF = vascular endothelial growth factor; Hsp90 = heat shock protein 90; Cdk4 = cyclin-dependent kinase 4; Cdk6 = cyclin-dependent kinase 6; MMP 2/9 = matrix metalloproteinase 2/9; EMT = epithelial-to-mesenchymal transition; C8 = caspase-8; ERα/β = oestrogen receptor α and β isoform; LMP = lysosomal membrane permeabilization.
Figure 4
Figure 4
Neuroprotective effects of OC and the molecular mechanisms of action. Abbreviation: ↓ stands for downregulation; ↑ stands for upregulation; Aβ = amyloid β; P-gp = P-glycoprotein; LRP1 = low-density lipoprotein receptor-related protein 1; ABCA1 = ATP-binding cassette transporter-A1; ApoE = apolipoprotein E; IDE = insulin-degrading enzyme; NEP = neprilysin; PPARγ = peroxisome proliferator-activated receptor γ; GFAP = glial fibrillary acidic protein; IL-1β = interleukin-1β; IL-6 = interleukin-6; GLT1 = glutamate transporter-1; GLUT1 = glucose transporter-1; PSD-95 = postsynaptic marker postsynaptic density protein 95; SNAP-25 = synaptosomal-associated protein 25.

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