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The Effect of Phenolic Compounds in Human Diseases
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The Effect of Phenolic Compounds in Human Diseases

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: 20 April 2025 | Viewed by 15420

Special Issue Editor

Prof. Dr. Gian Carlo Tenore

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Guest Editor
Department of Pharmacy, University of Naples “Federico II”, Via Domenico Montesano, 49, 80131 Napoli, Italy
Interests: formulation of innovative nutraceutical products and their validation of pre-clinical and clinical efficacy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polyphenols are a class of natural compounds extensively occurring in the vegetable kingdom and generally consumed in high quantities by human individuals through diet. Epidemiological evidence indicates that a high dietary intake of polyphenols is correlated with a decreased risk of several types of pathologies including cardiovascular disease (CVD), certain tumoral forms, and neurodegeneration. Although the interaction between polyphenols and cells has recently been better elucidated, there is still much work to do before the specific cellular targets and mechanisms of action can be ascertained. Along with this, a deeper understanding of the bioaccessibility and bioavailability of polyphenols in vitro and in vivo have to be determined. While various lines of evidence via biomarker assessments and the use of pharmacological tools in vivo (i.e., specific enzyme inhibitors, receptor agonists or antagonists) have indicated several potential mechanisms of action, a comprehensive proof and conclusive understanding has yet to be established.

Prof. Dr. Gian Carlo Tenore
Guest Editor

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Keywords

  • nutraceuticals
  • antioxidant
  • antinflammatory
  • polyphenols
  • human dieseases

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Published Papers (4 papers)

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Research

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22 pages, 2111 KiB  
Article
Antioxidant and Antibacterial Properties of a Functional Sports Beverage Formulation
by Alexandros Kolonas, Patroklos Vareltzis, Smaro Kiroglou, Nikolaos Goutzourelas, Dimitrios Stagos, Varvara Trachana, Christina Tsadila, Dimitris Mossialos, Stamatis Mourtakos and Olga Gortzi
Int. J. Mol. Sci. 2023, 24(4), 3558; https://doi.org/10.3390/ijms24043558 - 10 Feb 2023
Cited by 4 | Viewed by 3250
Abstract
Athletes often consume functional beverages in order to improve performance and reduce oxidative stress caused by high-intensity exercise. The present study aimed to evaluate the antioxidant and antibacterial properties of a functional sports beverage formulation. The beverage’s antioxidant effects were assessed on human [...] Read more.
Athletes often consume functional beverages in order to improve performance and reduce oxidative stress caused by high-intensity exercise. The present study aimed to evaluate the antioxidant and antibacterial properties of a functional sports beverage formulation. The beverage’s antioxidant effects were assessed on human mesenchymal stem cells (MSCs) by determining thiobarbituric acid reactive substances (TBARS; TBARS levels decreased significantly by 52.67% at 2.0 mg/mL), total antioxidant capacity (TAC; TAC levels increased significantly by 80.82% at 2.0 mg/mL) and reduced glutathione (GSH; GSH levels increased significantly by 24.13% at 2.0 mg/mL) levels. Furthermore, the beverage underwent simulated digestion following the INFOGEST protocol to assess its oxidative stability. The analysis of the total phenolic content (TPC) using the Folin–Ciocalteu assay revealed that the beverage contained a TPC of 7.58 ± 0.066 mg GAE/mL, while the phenolics identified by HPLC were catechin (2.149 mg/mL), epicatechin (0.024 mg/mL), protocatechuic acid (0.012 mg/mL), luteolin 7-glucoside (0.001 mg/mL), and kaempferol-3-O-β-rutinoside (0.001 mg/mL). The beverage’s TPC was strongly correlated with TAC (R2 = 896). Moreover, the beverage showcased inhibitory and bacteriostatic effects against Staphylococcus aureus and Pseudomonas aeruginosa. Lastly, the sensory acceptance test demonstrated that the functional sports beverage was well accepted by the assessors. Full article
(This article belongs to the Special Issue The Effect of Phenolic Compounds in Human Diseases)
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13 pages, 1422 KiB  
Article
A Food-Grade Method for Enhancing the Levels of Low Molecular Weight Proanthocyanidins with Potentially High Intestinal Bioavailability
by Fortuna Iannuzzo, Vincenzo Piccolo, Ettore Novellino, Elisabetta Schiano, Emanuela Salviati, Vincenzo Summa, Pietro Campiglia, Gian Carlo Tenore and Maria Maisto
Int. J. Mol. Sci. 2022, 23(21), 13557; https://doi.org/10.3390/ijms232113557 - 4 Nov 2022
Cited by 15 | Viewed by 2291
Abstract
Proanthocyanidins (PACs) are a group of bioactive molecules found in a variety of plants and foods. Their bioavailability depends on their molecular size, with monomers and dimers being more bioavailable than those that have a higher polymerization degree. This study aimed to develop [...] Read more.
Proanthocyanidins (PACs) are a group of bioactive molecules found in a variety of plants and foods. Their bioavailability depends on their molecular size, with monomers and dimers being more bioavailable than those that have a higher polymerization degree. This study aimed to develop a method to convert high-molecular-weight PACs to low-molecular-weight ones in a grape seed extract (GSE) from Vitis vinifera L. Therefore, GSE was subjected to alkaline treatment (ATGSE), and its difference in chemical composition, compared to GSE, was evaluated using a molecular networking (MN) approach based on results obtained from HPLC-ESI HRMS/MS characterization analysis. The network analysis mainly noted the PAC cluster with about 142 PAC compounds identified. In particular, the obtained results showed a higher content of monomeric and dimeric PACs in ATGSE compared to GSE, with 58% and 49% monomers and 31% and 24% dimers, respectively. Conversely, trimeric (9%), polymeric (4%), and galloylated PACs (14%) were more abundant in GSE than in ATGSE (6%, 1%, and 4%, respectively). Moreover, in vitro antioxidant and anti-inflammatory activities were investigated, showing the high beneficial potential of both extracts. In conclusion, ATGSE could represent an innovative natural matrix rich in bioavailable and bioaccessible PACs for nutraceutical applications with potential beneficial properties. Full article
(This article belongs to the Special Issue The Effect of Phenolic Compounds in Human Diseases)
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Review

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17 pages, 2121 KiB  
Review
Phenolic Compounds of Rhodiola rosea L. as the Potential Alternative Therapy in the Treatment of Chronic Diseases
by Jurga Bernatoniene, Valdas Jakstas and Dalia M. Kopustinskiene
Int. J. Mol. Sci. 2023, 24(15), 12293; https://doi.org/10.3390/ijms241512293 - 31 Jul 2023
Cited by 19 | Viewed by 5559
Abstract
The roots and rhizomes of Rhodiola rosea L. (Crassulaceae), which is widely growing in Northern Europe, North America, and Siberia, have been used since ancient times to alleviate stress, fatigue, and mental and physical disorders. Phenolic compounds: phenylpropanoids rosavin, rosarin, and rosin, tyrosol [...] Read more.
The roots and rhizomes of Rhodiola rosea L. (Crassulaceae), which is widely growing in Northern Europe, North America, and Siberia, have been used since ancient times to alleviate stress, fatigue, and mental and physical disorders. Phenolic compounds: phenylpropanoids rosavin, rosarin, and rosin, tyrosol glucoside salidroside, and tyrosol, are responsible for the biological action of R. rosea, exerting antioxidant, immunomodulatory, anti-aging, anti-fatigue activities. R. rosea extract formulations are used as alternative remedies to enhance mental and cognitive functions and protect the central nervous system and heart during stress. Recent studies indicate that R. rosea may be used to treat diabetes, cancer, and a variety of cardiovascular and neurological disorders such as Alzheimer’s and Parkinson’s diseases. This paper reviews the beneficial effects of the extract of R. rosea, its key active components, and their possible use in the treatment of chronic diseases. R. rosea represents an excellent natural remedy to address situations involving decreased performance, such as fatigue and a sense of weakness, particularly in the context of chronic diseases. Given the significance of mitochondria in cellular energy metabolism and their vulnerability to reactive oxygen species, future research should prioritize investigating the potential effects of R. rosea main bioactive phenolic compounds on mitochondria, thus targeting cellular energy supply and countering oxidative stress-related effects. Full article
(This article belongs to the Special Issue The Effect of Phenolic Compounds in Human Diseases)
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24 pages, 867 KiB  
Review
Influence of Polyphenols on Adipose Tissue: Sirtuins as Pivotal Players in the Browning Process
by Lorenzo Flori, Eugenia Piragine, Jacopo Spezzini, Valentina Citi, Vincenzo Calderone and Alma Martelli
Int. J. Mol. Sci. 2023, 24(11), 9276; https://doi.org/10.3390/ijms24119276 - 25 May 2023
Cited by 5 | Viewed by 3277
Abstract
Adipose tissue (AT) can be classified into two different types: (i) white adipose tissue (WAT), which represents the largest amount of total AT, and has the main function of storing fatty acids for energy needs and (ii) brown adipose tissue (BAT), rich in [...] Read more.
Adipose tissue (AT) can be classified into two different types: (i) white adipose tissue (WAT), which represents the largest amount of total AT, and has the main function of storing fatty acids for energy needs and (ii) brown adipose tissue (BAT), rich in mitochondria and specialized in thermogenesis. Many exogenous stimuli, e.g., cold, exercise or pharmacological/nutraceutical tools, promote the phenotypic change of WAT to a beige phenotype (BeAT), with intermediate characteristics between BAT and WAT; this process is called “browning”. The modulation of AT differentiation towards WAT or BAT, and the phenotypic switch to BeAT, seem to be crucial steps to limit weight gain. Polyphenols are emerging as compounds able to induce browning and thermogenesis processes, potentially via activation of sirtuins. SIRT1 (the most investigated sirtuin) activates a factor involved in mitochondrial biogenesis, peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α), which, through peroxisome proliferator-activated receptor γ (PPAR-γ) modulation, induces typical genes of BAT and inhibits genes of WAT during the transdifferentiation process in white adipocytes. This review article aims to summarize the current evidence, from pre-clinical studies to clinical trials, on the ability of polyphenols to promote the browning process, with a specific focus on the potential role of sirtuins in the pharmacological/nutraceutical effects of natural compounds. Full article
(This article belongs to the Special Issue The Effect of Phenolic Compounds in Human Diseases)
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