Abstract

The Mediterranean diet (MD) is a combination of foods mainly rich in antioxidants and anti-inflammatory nutrients that have been shown to have many health-enhancing effects. Extra-virgin olive oil (EVOO) is an important component of the MD. The importance of EVOO can be attributed to phenolic compounds, represented by phenolic alcohols, hydroxytyrosol, and tyrosol, and to secoiridoids, which include oleocanthal, oleacein, oleuropein, and ligstroside (along with the aglycone and glycosidic derivatives of the latter two). Each secoiridoid has been studied and characterized, and their effects on human health have been documented by several studies. Secoiridoids have antioxidant, anti-inflammatory, and anti-proliferative properties and, therefore, exhibit anti-cancer activity. This review summarizes the most recent findings regarding the pharmacological properties, molecular targets, and action mechanisms of secoiridoids, focusing attention on their preventive and anti-cancer activities. It provides a critical analysis of preclinical, in vitro and in vivo, studies of these natural bioactive compounds used as agents against various human cancers. The prospects for their possible use in human cancer prevention and treatment is also discussed.

Highlights

  • Cancer incidence and mortality are rapidly growing worldwide, cancer’s prominence as a cause of premature death is related to national levels of social and economic development

  • The Mediterranean diet (MD) is considered one of the healthiest worldwide dietary patterns due to a combination of foods rich in antioxidants and anti-inflammatory nutrients, such as fresh fruits and vegetables, and extra-virgin olive oil (EVOO), which play a protective role in cancer onset and which may remarkably reduce the risk of cancer [3,4,5]

  • More recently, De Stefanis et al have shown that exposure of hepatocellular carcinoma (HCC) cells to a phenolic extract, essentially composed of a mixture of OC and ligstroside aglycone, induced cell death and autophagy and these antitumor effects could be enhanced by the addition of TNF-α [83] (Table 3)

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Summary

Introduction

Cancer incidence and mortality are rapidly growing worldwide, cancer’s prominence as a cause of premature death is related to national levels of social and economic development. The Mediterranean diet (MD) is considered one of the healthiest worldwide dietary patterns due to a combination of foods rich in antioxidants and anti-inflammatory nutrients, such as fresh fruits and vegetables, and extra-virgin olive oil (EVOO), which play a protective role in cancer onset and which may remarkably reduce the risk of cancer [3,4,5]. The beneficial effects of EVOO have been attributed to phenolic compounds, such as phenolic alcohols, hydroxytyrosol (3,4-dihydroxyphenylethanol; 3,4-DHPEA), and tyrosol (p-hydroxyphenylethanol; p-HPEA), along with their secoiridoid derivatives 3,4-DHPEA-EA (oleuropein aglycone), p-HPEA-EA (ligstroside aglycone), 3,4DHPEA-EDA (oleacein, OA), p-HPEA-EDA (oleocanthal, OC), and oleuropein [10] All these components have been isolated, and their biological activities investigated, addressing the definition of pharmacological properties, molecular targets, and action mechanisms. This review aims to summarize the most recent findings regarding the preventive and anti-cancer activity of secoiridoids, providing a critical analysis of preclinical, in vitro and in vivo, studies in which these natural bioactive compounds are used as agents against various human cancers

Chemistry of Secoiridoids
Oleocanthal
Oleacein
Tyrosol and Hydroxytyrosol
Oleuropein
Ligstroside Aglycone
Findings
Conclusions
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