Hydroxytyrosol and Potential Uses in Cardiovascular Diseases, Cancer, and AIDS

Abstract

Hydroxytyrosol is one of the main phenolic components of olive oil. It is present in the fruit and leaf of the olive (Olea europaea L.). During the past decades, it has been well documented that this phenolic compound has health benefits and a protective action has been found in preclinical studies against several diseases. Here, we review its bioavailability in human beings and several assays showing significant results related with cardiovascular diseases, cancer, and acquired immunodeficiency syndrome (AIDS). Mechanisms of action include potent anti-oxidant and anti-inflammatory effects, among others. The importance of hydroxytyrosol in protection of low-density lipoproteins and consequently its implication in the reduction of cardiovascular disease risk has been highlighted by the European Food Safety Authority, concluding that 5 mg of hydroxytyrosol and its derivatives should be consumed daily to reach this effect at physiological level. We discuss the potential uses of this compound in supplements, nutraceutic foods, or topical formulations in the disease risk reduction. Finally, we conclude that more studies are needed to sustain or reject many other health claims not yet fully documented and to validate these newly available hydroxytyrosol-based products, because it seems to be a good candidate to reduce the risk of diseases mentioned.

Nutrigenomics of extra‐virgin olive oil: A review

“…If the biological activity of HT or other biophenols could be attributed to endogenous metabolites is still matter of investigation and preliminary data on antioxidant properties of HT have provided conflicting results (reviewed in ). The role of cellular esterase enzymes in the local metabolism and bioactivation of derivatized forms is poorly understood, but of sure interest to explain effects on the pathophysiology of GI tract, mainly in gut and hepatic tissue.…”

Hydroxytyrosol

“…5-Hydroxytyrosol is a natural compound with antioxidant [21], anti-inflammatory [22,23] and antiviral properties [8–10]. We show here that 5-hydroxytyrosol inhibits HIV-1 replication with inhibitory concentrations 50% in the micromolar range.…”

“…Although 5-hydroxytyrosol inhibitory concentrations 50% values could be considered ‘high’ for a drug candidate, as a low oral bioavailability could hamper its antiviral effect, previous reports show that 5-hydroxytyrosol oral bioavailability is close to 99% when isotopic labelled 5-hydroxytyrosol was used [21]. In addition, microbicides are used topically, applied directly in vaginal mucosae, which would bypass any problem derived from first pass effect and will yield higher concentrations in the site of action.…”

Dietary Strategies Implicated in the Prevention and Treatment of Metabolic Syndrome

“…It acts as a powerful scavenger of free radicals, as a radical chain breaker and as metal chelator [134]. It has the ability of inhibiting LDL-c oxidation by macrophages [132]. In this sense, it is the only phenol recognized by the European Food Safety Authority (EFSA) as a protector of blood lipids from oxidative damage [135].…”

“…It presents anti-atherogenic properties by decreasing the expression of vascular cell adhesion protein 1 (VCAM-1) and intercellular adhesion molecule 1 (ICAM-1) [132,137], which are probably the result of an inactivation of the nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB), activator protein 1 (AP-1), GATA transcription factor and nicotinamide adenine dinucleotide phosphate (NAD(P)H) oxidase [138,139]. Hydroxytyrosol also provides antidyslipidemic effects by lowering plasma levels of LDL-c, total cholesterol and TG, and by rising HDL-c [138].…”