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Polyphenols and Their Impact on Human Health

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (20 April 2023) | Viewed by 20420

Special Issue Editor


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Guest Editor
Department of Chemical Sciences, University of Naples “Federico II”, Via Cintia 4, I-80126 Naples, Italy
Interests: structural characterization, extraction, and evaluation/modulation of the antioxidant properties of natural phenolic compounds; exploitation of phenolic compounds, especially from agri-food by-products for the development of functional materials to be used in cosmetics, food packaging, and biomedicine; reactivity of natural phenolic compounds with reactive oxygen and nitrogen species and their manipulation/derivatization to improve their functional properties; evaluation of the antioxidant properties of phenolic compounds and of complex extracts/matrices using validated chemical assays; chemistry of melanin pigments
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Special Issue Information

Dear Colleagues,

Polyphenols are widely present not only in foods but also in easily accessible sources such as waste materials from agri-food industries. Based on their potent antioxidant and biological properties, the possible exploitation of these compounds as food supplements as well as functional ingredients for biomedical and cosmetic applications has gained more and more attention. This Special Issue welcomes original research articles relating to innovative applications of natural polyphenols from edible or non-edible natural sources in the field of nutrition and biomedicine, e.g., in food supplements or functional foods for the prevention of oxidative-stress-related diseases, as well as additives in biomedical devices, skincare formulations and cosmetic products. The identification of the main phenolic components and the characterization of the antioxidant and other relevant specific properties for their exploitation as functional ingredients in the health, food and/or cosmetic sectors are required. Review articles describing the current state of the art are also welcome.

Prof. Dr. Lucia Panzella
Guest Editor

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Keywords

  • polyphenols
  • antioxidants
  • food supplements
  • biomedical devices
  • skincare
  • agri-food by-products
  • sustainability

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Published Papers (9 papers)

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Editorial

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3 pages, 192 KiB  
Editorial
Polyphenols and Their Impact on Human Health
by Lucia Panzella
Int. J. Mol. Sci. 2023, 24(23), 16683; https://doi.org/10.3390/ijms242316683 - 24 Nov 2023
Viewed by 670
Abstract
Given their potent antioxidant and biological properties [...] Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)

Research

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23 pages, 3063 KiB  
Article
Lavandula austroapennina (Lamiaceae): Getting Insights into Bioactive Polyphenols of a Rare Italian Endemic Vascular Plant
by Claudia Gravina, Marialuisa Formato, Simona Piccolella, Marika Fiorentino, Adriano Stinca, Severina Pacifico and Assunta Esposito
Int. J. Mol. Sci. 2023, 24(9), 8038; https://doi.org/10.3390/ijms24098038 - 28 Apr 2023
Cited by 3 | Viewed by 1191
Abstract
Lavandula austroapennina N.G. Passal., Tundis and Upon has recently been described as a new species endemic to the southern Apennines (Italy). Locally, this species has a long ethnobotanical tradition of use for curative and decoration purposes and has been the protagonist of a [...] Read more.
Lavandula austroapennina N.G. Passal., Tundis and Upon has recently been described as a new species endemic to the southern Apennines (Italy). Locally, this species has a long ethnobotanical tradition of use for curative and decoration purposes and has been the protagonist of a flourishing essential oil production chain. Currently, while this tradition has long since ended, attention to the species is necessary, with a view to enhancing marginal and rural areas, as a recovery of a precious resource to (i) get insights into its (poly)phenolic fraction and (ii) address new and innovative uses of all its organs in various application fields (e.g., cosmeceutical sector). Therefore, after field sampling and dissection of its organs (i.e., corolla, calyx, leaf, stem and root), the latter, previously deterpenated and defatted, were subjected to accelerated ultrasound extraction and the related alcoholic extracts were obtained. Chemical composition, explored by UHPLC-QqTOF-MS/MS, and the following multivariate data analysis showed that the hydroxycinnamoyl derivatives are abundant in the leaf, stem and root, while flavonoids are more present in corolla and calyx. In particular, coumaroyl flavonoids with glyconic portion containing also hexuronyl moieties differentiated corolla organ, while yunnaneic acid D isomers and esculin distinguished root. When antiradical and reducing properties were evaluated (by means of ABTS, DPPH and PFRAP tests), a similar clustering of organs was achieved and the marked antioxidant efficacy of leaf, stem and root extracts was found. Thus, following cytotoxicity screening by MTT test on HaCaT keratinocytes, the protective effects of the organ extracts were assessed by wound closure observed after the scratch test. In addition, the extracts from corolla, leaf and stem were particularly active at low doses inducing rapid wound closure on HaCaT cells at a concentration of 1 μg/mL. The diversity in (poly)phenols of each organ and the promising bioactivity preliminarily assessed suggest further investigation to be carried out to fully recover and valorize this precious endemic vascular plant. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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14 pages, 3079 KiB  
Article
In Vitro Anti-Inflammatory and Antioxidant Activities of pH-Responsive Resveratrol-Urocanic Acid Nano-Assemblies
by Heegyeong Song, Seok Kang, Ying Yu, Sung Yun Jung, Kyeongsoon Park, Sang-Min Kim, HaK-Jun Kim, Jae Gyoon Kim and Sung Eun Kim
Int. J. Mol. Sci. 2023, 24(4), 3843; https://doi.org/10.3390/ijms24043843 - 14 Feb 2023
Cited by 3 | Viewed by 1993
Abstract
Inflammatory environments provide vital biochemical stimuli (i.e., oxidative stress, pH, and enzymes) for triggered drug delivery in a controlled manner. Inflammation alters the local pH within the affected tissues. As a result, pH-sensitive nanomaterials can be used to effectively target drugs to the [...] Read more.
Inflammatory environments provide vital biochemical stimuli (i.e., oxidative stress, pH, and enzymes) for triggered drug delivery in a controlled manner. Inflammation alters the local pH within the affected tissues. As a result, pH-sensitive nanomaterials can be used to effectively target drugs to the site of inflammation. Herein, we designed pH-sensitive nanoparticles in which resveratrol (an anti-inflammatory and antioxidant compound (RES)) and urocanic acid (UA) were complexed with a pH-sensitive moiety using an emulsion method. These RES-UA NPs were characterized by transmission electron microscopy, dynamic light scattering, zeta potential, and FT-IR spectroscopy. The anti-inflammatory and antioxidant activities of the RES-UA NPs were assessed in RAW 264.7 macrophages. The NPs were circular in shape and ranged in size from 106 to 180 nm. The RES-UA NPs suppressed the mRNA expression of the pro-inflammatory molecules inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages in a concentration-dependent manner. Incubation of LPS-stimulated macrophages with RES-UA NPs reduced the generation of reactive oxygen species (ROS) in a concentration-dependent manner. These results suggest that pH-responsive RES-UA NPs can be used to decrease ROS generation and inflammation. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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17 pages, 2044 KiB  
Article
Colonic Coffee Phenols Metabolites, Dihydrocaffeic, Dihydroferulic, and Hydroxyhippuric Acids Protect Hepatic Cells from TNF-α-Induced Inflammation and Oxidative Stress
by Andrea Sánchez-Medina, Mónica Redondo-Puente, Rudolf Dupak, Laura Bravo-Clemente, Luis Goya and Beatriz Sarriá
Int. J. Mol. Sci. 2023, 24(2), 1440; https://doi.org/10.3390/ijms24021440 - 11 Jan 2023
Cited by 7 | Viewed by 1830
Abstract
Coffee presents beneficial health properties, including antiobesity effects. However, its effects on inflammation are controversial. Hydroxycinnamic acids are the main coffee phenolic bioactive compounds. In human bioavailability studies carried out with coffee, among the most abundant compounds found in urine and plasma were [...] Read more.
Coffee presents beneficial health properties, including antiobesity effects. However, its effects on inflammation are controversial. Hydroxycinnamic acids are the main coffee phenolic bioactive compounds. In human bioavailability studies carried out with coffee, among the most abundant compounds found in urine and plasma were the colonic metabolites, dihydrocaffeic (DHCA), dihydroferulic (DHFA), and hydroxyhippuric (HHA) acids. To understand the hepato-protective potential of these three compounds, we tested whether treatment with realistic concentrations (0.5–10 µM) were effective to counteract inflammatory process and oxidative status induced by tumor necrosis factor α (TNF-α). First, we established a novel model of inflammation/oxidation using TNF-α and HepG2 cells. Afterwards, we evaluated the activity of DHCA, DHFA, and HHA against the inflammatory/oxidative challenge through the determination of the inflammatory mediators, interleukins (IL)-6, and IL-8 and chemokines, monocyte chemoattractant protein-1, and macrophage inflammatory protein-1, as well as the levels of biomarkers of oxidative stress, such as reactive oxygen species, reduced glutathione, and the antioxidant enzymes glutathione peroxidase and reductase. Results showed that all three compounds have a potential hepato-protective effect against the induced inflammatory/oxidative insult. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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23 pages, 2551 KiB  
Article
Polyphenol-Rich Beverage Consumption Affecting Parameters of the Lipid Metabolism in Healthy Subjects
by Celina Rahn, Tamara Bakuradze, Simone Stegmüller, Jens Galan, Sonja Niesen, Peter Winterhalter and Elke Richling
Int. J. Mol. Sci. 2023, 24(1), 841; https://doi.org/10.3390/ijms24010841 - 3 Jan 2023
Cited by 2 | Viewed by 2062
Abstract
Polyphenols are a diverse and widely distributed class of secondary metabolites, which possess numerous beneficial properties including a modulation of glucose and lipid metabolism. This placebo-controlled human intervention study was performed to explore effects of polyphenol-rich beverage (PRB) uptake on lipid metabolism, as [...] Read more.
Polyphenols are a diverse and widely distributed class of secondary metabolites, which possess numerous beneficial properties including a modulation of glucose and lipid metabolism. This placebo-controlled human intervention study was performed to explore effects of polyphenol-rich beverage (PRB) uptake on lipid metabolism, as well as DNA integrity. In this case, 36 healthy men were randomly divided to consume either 750 mL of a PRB (containing 51% chokeberry, cranberry, and pomegranate) or a placebo drink daily for eight weeks. Only PRB consumption was found to decrease fat and protein intakes significantly compared to the preceding one-week washout period. During the intervention with PRB an increased fat-free mass was shown after four weeks, whereas a significant elevation in body weight and leptin was observed in placebo group. Blood lipids were not significantly altered after PRB consumption, while triglyceride levels increased after placebo drink intake. In platelets, a significant inhibition of phosphodiesterase (PDE) activity was observed, more pronounced in test group. Consuming the PRB decreased total DNA strand breaks in whole blood as well as H2O2-induced breaks in isolated lymphocytes. Overall, our study suggested beneficial effects on lipid metabolism by reduced energy intake, modulation of biomarkers such as PDE activity and improved DNA integrity associated with PRB consumption. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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20 pages, 4400 KiB  
Article
In Vitro Anti-Proliferative and Apoptotic Effects of Hydroxytyrosyl Oleate on SH-SY5Y Human Neuroblastoma Cells
by Valentina Laghezza Masci, Roberta Bernini, Noemi Villanova, Mariangela Clemente, Vittoria Cicaloni, Laura Tinti, Laura Salvini, Anna Rita Taddei, Antonio Tiezzi and Elisa Ovidi
Int. J. Mol. Sci. 2022, 23(20), 12348; https://doi.org/10.3390/ijms232012348 - 15 Oct 2022
Cited by 14 | Viewed by 1752
Abstract
The antitumor activity of polyphenols derived from extra virgin olive oil and, in particular the biological activity of HTyr, has been studied extensively. However, the use of HTyr as a therapeutic agent for clinical applications is limited by its low bioavailability and rapid [...] Read more.
The antitumor activity of polyphenols derived from extra virgin olive oil and, in particular the biological activity of HTyr, has been studied extensively. However, the use of HTyr as a therapeutic agent for clinical applications is limited by its low bioavailability and rapid excretion in humans. To overcome these limitations, several synthetic strategies have been optimized to prepare lipophenols and new compounds derived from HTyr to increase lipophilicity and bioavailability. One very promising ester is hydroxytyrosyl oleate (HTyr-OL) because the chemical structure of HTyr, which is responsible for several biological activities, is linked to the monounsaturated chain of oleic acid (OA), giving the compound high lipophilicity and thus bioavailability in the cellular environment. In this study, the in vitro cytotoxic, anti-proliferative, and apoptotic induction activities of HTyr-OL were evaluated against SH-SY5Y human neuroblastoma cells, and the effects were compared with those of HTyr and OA. The results showed that the biological activity of HTyr was maintained in HTyr-OL treatments at lower dosages. In addition, the shotgun proteomic approach was used to study HTyr-OL-treated and untreated neuroblastoma cells, revealing that the antioxidant, anti-proliferative and anti-inflammatory activities of HTyr-OL were observed in the unique proteins of the two groups of samples. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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Review

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17 pages, 1469 KiB  
Review
Bioaccessibility and Bioavailability of Diet Polyphenols and Their Modulation of Gut Microbiota
by Tamara Lippolis, Miriam Cofano, Giusy Rita Caponio, Valentina De Nunzio and Maria Notarnicola
Int. J. Mol. Sci. 2023, 24(4), 3813; https://doi.org/10.3390/ijms24043813 - 14 Feb 2023
Cited by 30 | Viewed by 3345
Abstract
It is generally accepted that diet-derived polyphenols are bioactive compounds with several potentially beneficial effects on human health. In general, polyphenols have several chemical structures, and the most representative are flavonoids, phenolic acids, and stilbenes. It should be noted that the beneficial effects [...] Read more.
It is generally accepted that diet-derived polyphenols are bioactive compounds with several potentially beneficial effects on human health. In general, polyphenols have several chemical structures, and the most representative are flavonoids, phenolic acids, and stilbenes. It should be noted that the beneficial effects of polyphenols are closely related to their bioavailability and bioaccessibility, as many of them are rapidly metabolized after administration. Polyphenols—with a protective effect on the gastrointestinal tract—promote the maintenance of the eubiosis of the intestinal microbiota with protective effects against gastric and colon cancers. Thus, the benefits obtained from dietary supplementation of polyphenols would seem to be mediated by the gut microbiota. Taken at certain concentrations, polyphenols have been shown to positively modulate the bacterial component, increasing Lactiplantibacillus spp. and Bifidobacterium spp. involved in the protection of the intestinal barrier and decreasing Clostridium and Fusobacterium, which are negatively associated with human well-being. Based on the diet–microbiota–health axis, this review aims to describe the latest knowledge on the action of dietary polyphenols on human health through the activity of the gut microbiota and discusses micro-encapsulation of polyphenols as a strategy to improve the microbiota. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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22 pages, 739 KiB  
Review
Natural Polyphenols for Prevention and Treatment of Urinary Tract Infections
by Maria Maisto, Fortuna Iannuzzo, Ettore Novellino, Elisabetta Schiano, Vincenzo Piccolo and Gian Carlo Tenore
Int. J. Mol. Sci. 2023, 24(4), 3277; https://doi.org/10.3390/ijms24043277 - 7 Feb 2023
Cited by 3 | Viewed by 4286
Abstract
Urinary tract infections (UTIs) are the second most common type of bacterial infection worldwide. UTIs are gender-specific diseases, with a higher incidence in women. This type of infection could occur in the upper part of the urogenital tract, leading to pyelonephritis and kidney [...] Read more.
Urinary tract infections (UTIs) are the second most common type of bacterial infection worldwide. UTIs are gender-specific diseases, with a higher incidence in women. This type of infection could occur in the upper part of the urogenital tract, leading to pyelonephritis and kidney infections, or in the lower part of the urinary tract, leading to less serious pathologies, mainly cystitis and urethritis. The most common etiological agent is uropathogenic E. coli (UPEC), followed by Pseudomonas aeruginosa and Proteus mirabilis. Conventional therapeutic treatment involves the use of antimicrobial agents, but due to the dramatic increase in antimicrobial resistance (AMR), this strategy has partially lost its therapeutic efficacy. For this reason, the search for natural alternatives for UTI treatment represents a current research topic. Therefore, this review summarized the results of in vitro and animal- or human-based in vivo studies aimed to assess the potential therapeutic anti-UTI effects of natural polyphenol-based nutraceuticals and foods. In particular, the main in vitro studies were reported, describing the principal molecular therapeutic targets and the mechanism of action of the different polyphenols studied. Furthermore, the results of the most relevant clinical trials for the treatment of urinary tract health were described. Future research is needed to confirm and validate the potential of polyphenols in the clinical prophylaxis of UTIs. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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21 pages, 750 KiB  
Review
Preventive and Therapeutic Effects of Punica granatum L. Polyphenols in Neurological Conditions
by Simona Aleksandrova, Ralitza Alexova, Stela Dragomanova, Reni Kalfin, Ferdinando Nicoletti, Paolo Fagone, Maria Cristina Petralia, Katia Mangano and Lyubka Tancheva
Int. J. Mol. Sci. 2023, 24(3), 1856; https://doi.org/10.3390/ijms24031856 - 17 Jan 2023
Cited by 4 | Viewed by 2138
Abstract
Pomegranate (Punica granatum L.) is a polyphenol-rich food and medicinal plant containing flavonols, anthocyanins, and tannins. Ellagitannins (ETs) are the most abundant polyphenols in pomegranate. A growing body of research shows that polyphenol-rich pomegranate extracts and their metabolites target multiple types of [...] Read more.
Pomegranate (Punica granatum L.) is a polyphenol-rich food and medicinal plant containing flavonols, anthocyanins, and tannins. Ellagitannins (ETs) are the most abundant polyphenols in pomegranate. A growing body of research shows that polyphenol-rich pomegranate extracts and their metabolites target multiple types of brain cell and support their redox balance, proliferation and survival, as well as cell signaling. Independent studies have demonstrated that the significant neuroprotective effects of ETs are mediated by their antioxidant and anti-inflammatory effects, their chelating properties, by their ability to activate various signaling pathways, as well as the ability to influence mitochondrial damage, thus regulating autophagy, apoptosis and neurotransmitter signaling. The multitude of in vitro and in vivo studies summarized in the present review suggest that pomegranate polyphenols act on both neuronal and glial cells directly, and also affect blood–brain barrier function, restoring redox balance in the blood and brain and increasing blood flow to the brain. Full article
(This article belongs to the Special Issue Polyphenols and Their Impact on Human Health)
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