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Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to...
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Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to Clinical Translation

A special issue of Nutrients (ISSN 2072-6643). This special issue belongs to the section "Phytochemicals and Human Health".

Deadline for manuscript submissions: closed (20 January 2024) | Viewed by 4844

Special Issue Editors

Dr. Antonella Di Sotto

E-Mail Website
Guest Editor
Department of Physiology and Pharmacology “V. Erspamer”, Sapienza University of Rome, Rome, Italy
Interests: natural substances; herbal extracts; waste; plant phytocomplexes; polyphenols; terpenoids; cancer chemoprevention; chemoresistance; STAT3; Pgp; Nrf2; DNA-damage; metabolic reprogramming; autophagy; genoprotection; hypoglycemic activity; antiglycative properties; antioxidant defenses; antiviral herbal extracts; inflammation; immunomodulation
Special Issues, Collections and Topics in MDPI journals
Dr. Silvia Di Giacomo

E-Mail Website
Guest Editor
Department of Physiology and Pharmacology “V. Erspamer”, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy
Interests: terpenoids; polyphenols; chemoprevention; hepatocellular carcinoma; multidrug resistance; ABC-transporters; Nrf2; epithelial–mesenchymal transition (EMT)
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to this Special Issue entitled “Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to Clinical Translation”. 

Plant polyphenols are a large class of diverse secondary metabolites, ranging from simple phenolic acids to more complex molecules, including stilbenes, flavonoids, and tannins, all sharing the presence of multiple phenol units in their structure.

They are widely distributed in different plant species, where they perform several structural, metabolic, and defense functions and mediate biotic and abiotic interactions.

A plethora of beneficial properties, including antioxidant, anti-inflammatory, antimicrobial, and antiproliferative, have been associated with polyphenol-enriched food and plant byproducts, thus suggesting a possible role for these compounds in the prevention or treatment of several pathologies, such as neurodegenerative diseases, metabolic syndrome, diabetes, and cancer. Recent evidence has also highlighted the ability of some phenolics to boost antioxidant endogenous defenses, thus favoring health maintenance and infectious resilience.

Consequently, polyphenols appear to be interesting candidates for both pharmaceutical and nutraceutical applications. However, some pharmacokinetic issues, including reduced intestinal absorption and bioavailability, and rapid metabolic modifications, should be assessed to fully exploit their remarkable properties.

This Special Issue aims at collecting original articles and review papers evaluating the biological activities of plant polyphenols and phenolic-based plant extracts, the mechanisms involved, and their clinical relevance. Moreover, papers addressing innovative pharmaceutical formulations to improve the bioavailability of these compounds are welcome.

Dr. Antonella Di Sotto
Dr. Silvia Di Giacomo
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Nutrients is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • polyphenols
  • phenolic-based plant extracts
  • metabolic syndrome
  • diabetes
  • viral infections
  • liver
  • neuroprotection
  • synergistic effects
  • phenolic acids
  • tannins
  • gut microbiome

Published Papers (3 papers)

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Research

29 pages, 6560 KiB  
Article
ECHOPvir: A Mixture of Echinacea and Hop Extracts Endowed with Cytoprotective, Immunomodulatory and Antiviral Properties
by Ester Percaccio, Marta De Angelis, Alessandra Acquaviva, Giovanna Nicotra, Claudio Ferrante, Gabriela Mazzanti, Silvia Di Giacomo, Lucia Nencioni and Antonella Di Sotto
Nutrients 2023, 15(20), 4380; https://doi.org/10.3390/nu15204380 - 16 Oct 2023
Cited by 1 | Viewed by 1159
Abstract
Respiratory viral infections continue to pose significant challenges, particularly for more susceptible and immunocompromised individuals. Nutraceutical strategies have been proposed as promising strategies to mitigate their impact and improve public health. In the present study, we developed a mixture of two hydroalcoholic extracts [...] Read more.
Respiratory viral infections continue to pose significant challenges, particularly for more susceptible and immunocompromised individuals. Nutraceutical strategies have been proposed as promising strategies to mitigate their impact and improve public health. In the present study, we developed a mixture of two hydroalcoholic extracts from the aerial parts of Echinacea purpurea (L.) Moench (ECP) and the cones of Humulus lupulus L. (HOP) that can be harnessed in the prevention and treatment of viral respiratory diseases. The ECP/HOP mixture (named ECHOPvir) was characterized for the antioxidant and cytoprotective properties in airway cells. Moreover, the immunomodulating properties of the mixture in murine macrophages against antioxidant and inflammatory stimuli and its antiviral efficacy against the PR8/H1N1 influenza virus were assayed. The modulation of the Nrf2 was also investigated as a mechanistic hypothesis. The ECP/HOP mixture showed a promising multitarget bioactivity profile, with combined cytoprotective, antioxidant, immunomodulating and antiviral activities, likely due to the peculiar phytocomplexes of both ECP and HOP, and often potentiated the effect of the single extracts. The Nrf2 activation seemed to trigger these cytoprotective properties and suggest a possible usefulness in counteracting the damage caused by different stressors, including viral infection. Further studies may strengthen the interest in this product and underpin its future nutraceutical applications. Full article
(This article belongs to the Special Issue Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to Clinical Translation)
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14 pages, 2291 KiB  
Article
Gallation and B-Ring Dihydroxylation Increase Green Tea Catechin Residence Time in Plasma by Differentially Affecting Tissue-Specific Trafficking: Compartmental Model of Catechin Kinetics in Healthy Adults
by Joanna K. Hodges, Geoffrey Y. Sasaki, Yael Vodovotz and Richard S. Bruno
Nutrients 2023, 15(18), 4021; https://doi.org/10.3390/nu15184021 - 17 Sep 2023
Cited by 1 | Viewed by 1061
Abstract
Catechins in green tea extract (GTE) (epigallocatechin gallate (EGCG), epigallocatechin (EGC), epicatechin (EC), epicatechin gallate (ECG)) vary in bioactivity. We developed a physiologically relevant mathematical model of catechin metabolism to test the hypothesis that fractional catabolic rates of catechins would be differentially affected [...] Read more.
Catechins in green tea extract (GTE) (epigallocatechin gallate (EGCG), epigallocatechin (EGC), epicatechin (EC), epicatechin gallate (ECG)) vary in bioactivity. We developed a physiologically relevant mathematical model of catechin metabolism to test the hypothesis that fractional catabolic rates of catechins would be differentially affected by their structural attributes. Pharmacokinetic data of plasma and urine catechin concentrations were used from healthy adults (n = 19) who ingested confections containing 0.5 g GTE (290 mg EGCG, 87 mg EGC, 39 mg EC, 28 mg ECG). A 7-compartmental model of catechin metabolism comprised of the gastrointestinal tract (stomach, small and large intestine), liver, plasma, extravascular tissues, and kidneys was developed using a mean fraction dose of EGCG, ECG, EGC, and EC. Fitting was by iterative least squares regression analysis, and goodness of fit was ascertained by the estimated variability of parameters (FSD < 0.5). The interaction of gallation and B-ring dihydroxylation most greatly extended plasma residence time such that EGC > EC = EGCG > EGC. The interaction between gallation and B-ring dihydroxylation accelerated the transfer from the upper gastrointestinal tract to the small intestine but delayed subsequent transfers from the small intestine through the liver to plasma and from kidneys to urine. Gallation and B-ring dihydroxylation independently delayed the transfer from plasma to extravascular tissues, except the uptake to kidneys, which was slowed by gallation only. This multi-compartment model, to be validated in a future study, suggests that gallation and B-ring dihydroxylation affect catechin catabolism in a tissue-specific manner and thus their potential bioactivity. Full article
(This article belongs to the Special Issue Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to Clinical Translation)
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14 pages, 3768 KiB  
Article
Resveratrol Butyrate Ester Supplementation Blunts the Development of Offspring Hypertension in a Maternal Di-2-ethylhexyl Phthalate Exposure Rat Model
by You-Lin Tain, Chih-Yao Hou, Guo-Ping Chang-Chien, Sufan Lin and Chien-Ning Hsu
Nutrients 2023, 15(3), 697; https://doi.org/10.3390/nu15030697 - 30 Jan 2023
Cited by 5 | Viewed by 2010
Abstract
Resveratrol (REV) is a plant polyphenol with a plethora of beneficial properties. We previously enhanced the efficacy of REV via esterification of REV with butyrate to form resveratrol butyrate ester (RBE). Compared with REV, RBE exhibits higher bioavailability and better antioxidant effects. Hypertension [...] Read more.
Resveratrol (REV) is a plant polyphenol with a plethora of beneficial properties. We previously enhanced the efficacy of REV via esterification of REV with butyrate to form resveratrol butyrate ester (RBE). Compared with REV, RBE exhibits higher bioavailability and better antioxidant effects. Hypertension can originate in early life because of maternal toxic chemical exposure. This study aims to examine the effectiveness of RBE in the protection of offspring hypertension induced by maternal di-2-ethylhexylphthalate (DEHP) exposure and to explore the underlying mechanisms. DEHP (10 mg/kg/day) was used as oral gavage to pregnant rats during gestation and lactation. The control group received the vehicle. Three groups of DEHP-exposed dams received REV (6.67 mg/kg/day), or low-dose (3.33 mg/kg/day) or high-dose (6.67 mg/kg/day) RBE in drinking water during gestation and lactation. Perinatal DEHP exposure resulted in hypertension and bodyweight gain in adult male offspring, which was prevented by high-dose RBE. REV supplementation attenuated DEHP exposure-induced increases in blood pressure but not bodyweight. High-dose RBE decreased renal oxidative damage, increased plasma butyrate concentrations, and altered short chain fatty acid receptor (SCFA) expression. Low-dose RBE treatment reduced downstream mediators of the acryl hydrocarbon receptor (AHR) signaling pathway. Moreover, DEHP exposure, REV and RBE treatment differentially shaped the offspring’s gut microbiota. In particular, high-dose RBE increased the abundance of the genus Duncaniella. The beneficial effects of RBE treatment were related to reducing oxidative damage, increasing plasma butyrate concentrations, downregulating SCFA receptor expression, antagonizing AHR signaling, and altering the gut microbiota. This study provides the first evidence of RBE as a novel plant polyphenol bioproduct targeting the oxidative stress and gut microbiota to protect against maternal DEHP exposure-primed offspring hypertension. Full article
(This article belongs to the Special Issue Pharmacological Basis of Plant Polyphenol Bioactivities: From Preclinical Evidence to Clinical Translation)
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