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.

While the number of publications on wine and health is steadily increasing, ranging from a molecular level to epidemiological studies, often with contradictory results, little attention has been given to a holistic approach to research, starting from the molecular level to arrive at pharmacological and medical conclusions. In this review, some unusual concepts are considered, such as the phytocomplex, the vehicle, and the Matrix effect. The concept of the phytocomplex is discussed, specifically the biological activities of Tyrosol, Hydroxytyrosol, and Resveratrol; indeed, the interactions among different molecules in herbal matrices provide a specific response. This is often markedly different from the response evoked by single constituents in the modulation of microbial populations in the gut, in intestinal stability and bioaccessibility, and, obviously, in inducing biological responses. Among the many alcoholic beverages which contain these molecules, wine has the most peculiar Matrix effect, which can heavily influence the bioavailability of the phytocomplex obtained by the fermentation processes that produce this beverage. Wine’s Matrix effect plays an instrumental role in improving the beneficial compounds’ bioavailability and/or in inhibiting alcohol metabolites’ carcinogenicity. Underestimation of the wine Matrix effect could lead to deceiving results, as in the case of dealcoholized wine or wine-compound-based nutritional supplements; alternatively, this can occur in the emphasis of a single component’s toxic activity, in this case, alcohol, ignoring the specific molecular-level protective action of other compounds (polyphenols) that are present in the same matrix. The dark side of the Matrix effect is also discussed. This review confirms the research recommendations made by the WHO Scientific Group, which suggests it is important “to investigate the possible protective effects of ingredients other than alcohol in alcoholic beverages”, considering that most recent studies seem not only relevant but also capable of directing future research towards innovative points of view that have so far been too neglected.

Knowledge of the chemical composition of propolis is crucial for understanding the characteristics of products of different origins, but also for quality control and regulatory purposes. To date, official monographs or official analyses that allow researchers to evaluate propolis in a proper way have not yet been released. This study focuses on the characterization of twenty-seven Italian propolis samples and the identification of chemical markers that define its geographical provenance. Total polyphenol (TP) and total flavonoid (TF) content, alongside the quantification of pinocembrin, chrysin, galangin, and caffeic acid phenethyl ester (CAPE), were identified as potential markers. Additionally, DPPH assays were conducted to evaluate the antiradical activity of propolis samples. Our findings demonstrated that TPs, TFs and pinocembrin differed in propolis of different origins, especially in samples from the islands. However, the quantification of the sum of chrysin and galangin and CAPE provided a clearer distinction of the geographical origin of the propolis samples. In contrast, the DPPH assay did not prove useful for this purpose, as most results were similar and, therefore, not significant. This study lays the groundwork for future research on propolis. These findings could contribute to the development of more refined methods for distinguishing propolis origins, enhancing the understanding, valuation and quality control of this natural product in various applications.

Berberine (BER) is an alkaloid found, together with other protoberberinoids (PROTBERs), in several species used in medicines and food supplements. While some herbal preparations containing BER and PROTBERs, such as Berberis aristata DC. bark extracts, have shown promising potential for human health, their safety has not been fully assessed. Recently, the EFSA issued a call for data to deepen the pharmacokinetic and pharmacodynamic understanding of products containing BER and PROTBERs and to comprehensively assess their safety, especially when used in food supplements. In this context, new data were collected in this work by assessing: (i) the phytochemical profile of 16 different commercial B. aristata dry extracts, which are among the most widely used preparations containing BER and PROTBERs in Europe; (ii) the In Vitro and In Silico investigation of the pharmacokinetic properties of BER and PROTBERs; (iii) the In Vitro cytotoxicity of selected extracts in different human cell lines, including tests on hepatic cells in the presence of CYP450 substrates; (iv) the effects of the extracts on cancer cell migration; and (v) the In Vitro molecular effects of extracts in non-cancer human cells. Results showed that commercial B. aristata extracts contain BER as the main constituent, with jatrorrhizine as main secondary PROTBER. BER and jatrorrhizine were found to have a good bioaccessibility rate, but they interact with P-gp. B. aristata extracts showed limited cytotoxicity and minimal interaction with CYP450 substrates. Furthermore, tested extracts demonstrated inhibition of cancer cell migration and were devoid of any pro-tumoral effects in normal cells. Overall, our work provides a valuable overview to better elucidate important concerns regarding botanicals containing BER and PROTBERs.

It is widely recognized that foods, biodiversity, and human health are strongly interconnected, and many efforts have been made to understand the nutraceutical value of diet. In particular, diet can affect the progression of intestinal diseases, including inflammatory bowel disease (IBD) and intestinal cancer. In this context, we studied the anti-inflammatory and antioxidant activities of extracts obtained from a local endangered variety of Phaseolus vulgaris L. (Fagiola di Venanzio, FV). Using in vitro intestinal cell models, we evaluated the activity of three different extracts: soaking water, cooking water, and the bioaccessible fraction obtained after mimicking the traditional cooking procedure and gastrointestinal digestion. We demonstrated that FV extracts reduce inflammation and oxidative stress prompted by interleukin 1β through the inhibition of cyclooxygenase 2 expression and prostaglandin E2 production and through the reduction in reactive oxygen species production and NOX1 levels. The reported data outline the importance of diet in the prevention of human inflammatory diseases. Moreover, they strongly support the necessity to safeguard local biodiversity as a source of bioactive compounds.

The knowledge in chemical composition of propolis is crucial for understanding the characteristics of products of different origin, but also for quality control and regulatory purposes. To date, offical monographs or official analyses that allow to evaluate propolis in a proper way have not yet been released. This study focuses on the characterization of twenty-seven Italian propolis and the identification of chemical markers that define its geographical provenance. Total polyphenol (TP) and total flavonoid (TF) content, alongside the quantification of pinocembrin, chrysin, galangin, and caffeic acid phenethyl ester (CAPE), were identified as as potential markers. Additionally, DPPH assays was conducted to evaluate antiradicalic activity of propolis samples. Our findings demonstrated that TP, TF and pinocembrin differed in propolis of different origin, especially in samples from the islands. However, the quantification of the sum of chrysin and galangin and CAP provided a clear distinction of the geographical origin of the propolis samples. In contrast, the DPPH assay did not prove useful for this purpose, as most results were similar and, therefore, not significant. This study lays the groundwork for future research on propolis. These findings could contribute to the development of more refined methods for distinguishing propolis origins, enhancing the understanding, valuation and quality control of this natural product in various applications.