Pharmacokinetics and bioavailability of hydroxytyrosol are dependent on the food matrix in humans

Abstract

Purpose Several studies have demonstrated the properties of hydroxytyrosol, a phenolic compound present in olive oils and olives with a well-characterized impact on human health. Nevertheless, some knowledge gaps remain on its bioavailability and metabolism; overall concerning to the real rate per cent of absorption and biovailability of dietary hydroxytyrosol and the influence of the dietary food-containing hydroxytyrosol on it.Methods A double-blind study was performed including 20 volunteers who ingested 5 mg of hydroxytyrosol through diverse food matrices, to discover the influence on pharmacokinetics and bioavailability of HT metabolites (hydroxytyrosol acetate, 3,4dihydroxyphenylacetic acid (DOPAC), tyrosol, and homovanillic alcohol) of the distinct matrices by UHPLC-ESI-QqQ-MS/MS. ResultsThe HT pharmacokinetics after consumption of different food matrices was strongly dependent on the food matrix. In this aspect, the intake of extra virgin olive exhibited significantly higher plasma concentrations after 30 minutes of oral intake (3.79 ng/mL) relative to the control. Regarding the hydroxytyrosol bioavailability, the intake of extra virgin olive oil, as well as fortified refined olive, flax, and grapeseed oils provided significantly higher urinary contents (0.86, 0.63, 0.55, and 0.33 µg/mg creatinine, respectively) compared with basal urine, whereas hydroxytyrosol metabolites showed no significant changes. No differences were found between men and women. ConclusionsThe metabolic profile of hydroxytyrosol is influenced by the food matrix in which is incorporated, with the oily nature for the final bioavailability being relevant. Extra virgin olive oil was identified as the best matrix for this compound. The results described 3 contribute to the understanding of the relevance of the food matrices for the final absorption of hydroxytyrosol and hence, the achievement of the highest health protection potential.

Fatty Acid Hydroxytyrosyl Esters of Olive Oils Are Bioaccessible According to Simulated In Vitro Gastrointestinal Digestion: Unraveling the Role of Digestive Enzymes on Their Stability

“…However, the rate of bioaccessibility depended on both the specific FA-based esterification and the compositional features of the food matrix, as already reported for free HT pharmacokinetics and bioavailability, in vivo, after ingestion of different oily matrices. 25 These results are in good agreement with previous reports on the bioaccessibility of other esters of HT, namely, phosphatidyl-hydroxytyrosol (PHT, phospholipid derivatives of HT with phosphatidylcholine). 17 In their work, Martin et al described that the portion of HT within the BF, regarding the esterified form (PHT), was significantly higher relative to unesterified HT.…”

“…The concentrations of HT-FAs corresponding to EVOO were 3.68, 4.04, and 239.41 ng/g fw, while for the VOO samples, these were 8.22, 1.80, and 92.00 ng/g fw for HT-ALA, HT-LA, and HT-OA, respectively, evidencing that the esterified forms of HT were bioaccessible. However, the rate of bioaccessibility depended on both the specific FA-based esterification and the compositional features of the food matrix, as already reported for free HT pharmacokinetics and bioavailability, in vivo , after ingestion of different oily matrices …”

Therapeutic Properties and Use of Extra Virgin Olive Oil in Clinical Nutrition: A Narrative Review and Literature Update

“…Crude EVOO is the ideal food matrix for absorption of its hydroxytyrosol in the intestines, ensuring maximum concentrations in blood [ 89 , 90 ]. Among heat-based cooking methods, frying and steaming may preserve or enhance EVOO’s antioxidant capacity, while sautéing, pressure cooking, boiling, and microwaving may lead to significant reductions in its total phenolic content [ 91 , 92 ].…”

Availability and Metabolic Fate of Olive Phenolic Alcohols Hydroxytyrosol and Tyrosol in the Human GI Tract Simulated by the In Vitro GIDM–Colon Model

“…The interindividual variability is avoided, as well as the interference of endogenously produced metabolites, such as in the case of HTyr and Tyr, which are also produced through dopamine and tyramine pathways, respectively [ 6 , 7 , 40 ]. Furthermore, GIDM−colon model enables the investigation of the compounds of interest in pure form and not as a component of a more complex mixture, such as in the majority of the in vivo and human studies, which use olive oil or olive oil polyphenols extracts to study HTyr and Tyr metabolism [ 37 , 50 ].…”