Abstract

Background: The importance of polyphenols in human health is well known; these compounds are common in foods, such as fruits, vegetables, spices, extra virgin olive oil and wine. On the other hand, the different factors that modulate the biological activity of these compounds are less well known. Conceptualization of the work: In this review we took into account about 200 relevant and recent papers on the following topics: “polyphenols bioavailability”, “polyphenols matrix effect”, “food matrix effect”, “polyphenols-cytochromes interaction”, after having reviewed and updated information on chemical classification and main biological properties of polyphenols, such as the antioxidant, anti-radical and anti-inflammatory activity, together with the tricky link between in vitro tests and clinical trials. Key findings: the issue of polyphenols bioavailability and matrix effect should be better taken into account when health claims are referred to polyphenols, thus considering the matrix effect, enzymatic interactions, reactions with other foods or genetic or gender characteristics that could interfere. We also discovered that in vitro studies often underrate the role of phytocomplexes and thus we provided practical hints to describe a clearer way to approach an investigation on polyphenols for a more resounding transfer to their use in medicine.

Highlights

  • Polyphenols are natural compounds synthesized exclusively by plants, with chemical features related to phenolic substances with reported bioactivities to modulate oxidative and inflammatory stress, to alter macronutrient digestion and to exert prebiotic-like effects on gut microbiota.Polyphenols are almost ubiquitous in plants, being generally involved in the attraction of pollinators, the execution of structural functions, the defense against ultraviolet radiation and the protection of plants against microbial invasion and herbivores [1,2,3].These compounds are common in dietary, such as fruits, vegetables, nuts, seeds, flowers and tree barks and common beverages such as wine, beer and tea and are, an integral part of the human diet

  • In this review we primarily aimed to focus some pivotal, but often underrated aspects of polyphenols related with their role in health maintenance; in detail, we called into the question bioavailability limits and metabolic interactions of this large class of secondary metabolites

  • The knowledge of the pharmacokinetic of polyphenols is fundamental to plan in vitro experiments testing plausible concentrations, and to avoid upstream methodological errors: for example, many papers have been published on several biological effects exerted by high concentrations of hyperoside and genistin in cell models, despite these two glycosylated polyphenols undergo a rapid and extensive metabolism produced by gut flora, their absorption is even lower than aglycone forms [89,90] and they are converted in quercetin and genistein that should have been tested as well

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Summary

Introduction

Polyphenols are natural compounds synthesized exclusively by plants, with chemical features related to phenolic substances with reported bioactivities to modulate oxidative and inflammatory stress, to alter macronutrient digestion and to exert prebiotic-like effects on gut microbiota. Polyphenols are almost ubiquitous in plants, being generally involved in the attraction of pollinators, the execution of structural functions, the defense against ultraviolet radiation and the protection of plants against microbial invasion and herbivores [1,2,3] These compounds are common in dietary, such as fruits, vegetables, nuts, seeds, flowers and tree barks and common beverages such as wine, beer and tea and are, an integral part of the human diet. Some can bind and precipitate macromolecules, such as dietary proteins, carbohydrates and digestive enzymes, thereby reducing food digestibility [5] These compounds attained the prominent position due to their wide distribution in plant-based foods and significant evidence of negative correlation of their consumption with cancers, diabetes and cardiovascular diseases. We took into account about 200 relevant and recent papers on specific topics such as polyphenols bioavailability, polyphenols matrix effect, food matrix effect, polyphenolscytochromes interaction, whereas the most impacting and recent literature on chemical and biological properties was comprehensively reviewed, by searching in vitro, in vivo and clinical studies

Polyphenols
The Problem of Bioavailability of Polyphenols
Bioavailability of Polyphenols
From the Bench to Pre-Clinical and Clinical Studies on Polyphenols
Single Polyphenols or Phytocomplex
Pharmacokinetic Aspects
Study of the Mechanism of Action
Findings
Conclusions
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