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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: 30 August 2024 | Viewed by 4642

Special Issue Editor


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Guest Editor
Department of Medicine and Biological Sciences, Universitatea Stefan cel Mare din Suceava, 720229 Suceava, Romania
Interests: metabolic pathways; antimicrobial; phenolics; photosystems

Special Issue Information

Dear Colleagues,

Healthcare systems worldwide are facing burdens associated with non-optimal lifestyle, pollution, microbial antibiotic resistance, etc. Since many diseases are, in essence, alterations of normal metabolic pathways or gene expression processes, a multitude of challenges, but also opportunities arise for diagnosing, preventing, and treating such diseases. Phenolic compounds, with their broad chemical diversity, represent a significant pool of bioactive molecules, interacting with numerous human but also with pathogen druggable targets. The aim of this Special Issue is to update current knowledge on phenolic compounds relevance for human diseases, and original research and review papers are welcome in the fields of:

  • Novel compounds identification, synthesis and/or functionalisation;
  • Purification and structural characterisation, coupled with qualitative or quantitative biological activity assessment;
  • Phenolic compounds—microbiota interactions;
  • Dietary intake or supplementation in relation to health or specific diseases;
  • Elucidation of interactions with molecular targets relevant for human health;
  • Pharmacodynamics and pharmacokinetics of phenolic compounds, including statistical models;
  • Development or improvement of assays or protocols related to biological activities of compounds;
  • Summarization of knowledge on specific topics pertaining to phenolic compounds.

Dr. Andrei Lobiuc
Guest Editor

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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • novel sources
  • synthesis
  • biological activity
  • molecular interactions
  • pharmacodynamics
  • pharmacokinetics
  • assay development
  • microbiota
  • sources and intake

Published Papers (4 papers)

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Research

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18 pages, 3219 KiB  
Article
Integrated Membrane Process in Organic Media: Combining Organic Solvent Ultrafiltration, Nanofiltration, and Reverse Osmosis to Purify and Concentrate the Phenolic Compounds from Wet Olive Pomace
by Carmen M. Sánchez-Arévalo, Fausto Aldegheri, M. Cinta Vincent-Vela and Silvia Álvarez-Blanco
Int. J. Mol. Sci. 2024, 25(10), 5233; https://doi.org/10.3390/ijms25105233 - 11 May 2024
Viewed by 497
Abstract
Phenolic compounds from a hydroalcoholic extract of wet olive pomace were purified and concentrated by an integrated membrane process in organic media. First, UF010104 (Solsep BV) and UP005 (Microdyn Nadir) membranes were tested to be implemented in the ultrafiltration stage, with the aim [...] Read more.
Phenolic compounds from a hydroalcoholic extract of wet olive pomace were purified and concentrated by an integrated membrane process in organic media. First, UF010104 (Solsep BV) and UP005 (Microdyn Nadir) membranes were tested to be implemented in the ultrafiltration stage, with the aim of purifying the extract and obtaining a permeate enriched in phenolic compounds. Despite the high flux observed with the UF010104 membrane (20.4 ± 0.7 L·h−1·m−2, at 2 bar), the UP005 membrane was selected because of a more suitable selectivity. Even though some secoiridoids were rejected, the permeate stream obtained with this membrane contained high concentrations of valuable simple phenols and phenolic acids, whereas sugars and macromolecules were retained. Then, the ultrafiltration permeate was subjected to a nanofiltration step employing an NF270 membrane (DuPont) for a further purification and fractionation of the phenolic compounds. The permeate flux was 50.2 ± 0.2 L·h−1·m−2, working at 15 bar. Hydroxytyrosol and some phenolic acids (such as vanillic acid, caffeic acid, and ferulic acid) were recovered in the permeate, which was later concentrated by reverse osmosis employing an NF90 membrane. The permeate flux obtained with this membrane was 15.3 ± 0.3 L·h−1·m−2. The concentrated phenolic mixture that was obtained may have important applications as a powerful antioxidant and for the prevention of diabetes and neurodegenerative diseases. Full article
(This article belongs to the Special Issue Phenolic Compounds in Human Diseases)
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24 pages, 8872 KiB  
Article
Anti-Proliferative Potential of Cynaroside and Orientin—In Silico (DYRK2) and In Vitro (U87 and Caco-2) Studies
by Lucia Camelia Pirvu, Lucia Pintilie, Adrian Albulescu, Amalia Stefaniu and Georgeta Neagu
Int. J. Mol. Sci. 2023, 24(23), 16555; https://doi.org/10.3390/ijms242316555 - 21 Nov 2023
Cited by 2 | Viewed by 1438
Abstract
Luteolin derivates are plant compounds with multiple benefits for human health. Stability to heat and acid hydrolysis and high resistance to (auto)oxidation are other arguments for the laden interest in luteolin derivates today. The present study was designed to compare the in silico [...] Read more.
Luteolin derivates are plant compounds with multiple benefits for human health. Stability to heat and acid hydrolysis and high resistance to (auto)oxidation are other arguments for the laden interest in luteolin derivates today. The present study was designed to compare the in silico and in vitro anti-proliferative potential of two luteolin derivates, luteolin-7-O-glucoside/cynaroside (7-Lut) and luteolin-8-C-glucoside/orientin (8-Lut). In silico investigations were carried out on the molecular target, namely, the human dual specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) in association with its natural ligand, curcumin (PDB ID: 5ZTN), by CLC Drug Discovery Workbench v. 1.5.1. software and Molegro Virtual Docker (MVD) v. MVD 2019.7.0. software. In vitro studies were performed on two human tumor cell lines, glioblastoma (U87) and colon carcinoma (Caco-2), respectively. Altogether, docking studies have revealed 7-Lut and 8-Lut as effective inhibitors of DYRK2, even stronger than the native ligand curcumin; in vitro studies indicated the ability of both luteolin glucosides to inhibit the viability of both human tumor cell lines, up to 85% at 50 and 100 µg/mL, respectively; the most augmented cytotoxic and anti-proliferative effects were obtained for U87 exposed to 7-Lut (IC50 = 26.34 µg/mL). The results support further studies on cynaroside and orientin to create drug formulas targeting glioblastoma and colon carcinoma in humans. Full article
(This article belongs to the Special Issue Phenolic Compounds in Human Diseases)
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32 pages, 10205 KiB  
Article
Discovery of New Hydrazone-Thiazole Polyphenolic Antioxidants through Computer-Aided Design and In Vitro Experimental Validation
by Gabriel Marc, Anca Stana, Mihaela Tertiş, Cecilia Cristea, Alexandra Ciorîţă, Ștefan-Mihai Drăgan, Vlad-Alexandru Toma, Raluca Borlan, Monica Focșan, Adrian Pîrnău, Laurian Vlase, Smaranda Oniga and Ovidiu Oniga
Int. J. Mol. Sci. 2023, 24(17), 13277; https://doi.org/10.3390/ijms241713277 - 26 Aug 2023
Cited by 2 | Viewed by 1206
Abstract
Oxidative stress is linked to a series of diseases; therefore, the development of efficient antioxidants might be beneficial in preventing or ameliorating these conditions. Based on the structure of a previously reported compound with good antioxidant properties and on computational studies, we designed [...] Read more.
Oxidative stress is linked to a series of diseases; therefore, the development of efficient antioxidants might be beneficial in preventing or ameliorating these conditions. Based on the structure of a previously reported compound with good antioxidant properties and on computational studies, we designed several catechol derivatives with enhanced antioxidant potential. The compounds were synthesized and physicochemically characterized, and their antioxidant activity was assessed through different antiradical, electron transfer and metal ions chelation assays, their electrochemical behavior and cytotoxicity were studied. The results obtained in the in vitro experiments correlated very well with the in silico studies; all final compounds presented very good antioxidant properties, generally superior to those of the reference compounds used. Similarly, the results obtained from studying the compounds’ electrochemical behavior were in good agreement with the results of the antioxidant activity evaluation assays. Regarding the compounds’ cytotoxicity, compound 7b had a dose-dependent inhibitory effect against all cell lines. In conclusion, through computer-aided design, we developed several catechol thiazolyl-hydrazones with excellent antioxidant properties, of which compound 7b, with two catechol moieties in its structure, exhibited the best antioxidant activity. Full article
(This article belongs to the Special Issue Phenolic Compounds in Human Diseases)
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Review

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22 pages, 2276 KiB  
Review
Molecular Pathways of Genistein Activity in Breast Cancer Cells
by Evangelia K. Konstantinou, Aristea Gioxari, Maria Dimitriou, George I. Panoutsopoulos and Athanasios A. Panagiotopoulos
Int. J. Mol. Sci. 2024, 25(10), 5556; https://doi.org/10.3390/ijms25105556 - 20 May 2024
Viewed by 695
Abstract
The most common malignancy in women is breast cancer. During the development of cancer, oncogenic transcription factors facilitate the overproduction of inflammatory cytokines and cell adhesion molecules. Antiapoptotic proteins are markedly upregulated in cancer cells, which promotes tumor development, metastasis, and cell survival. [...] Read more.
The most common malignancy in women is breast cancer. During the development of cancer, oncogenic transcription factors facilitate the overproduction of inflammatory cytokines and cell adhesion molecules. Antiapoptotic proteins are markedly upregulated in cancer cells, which promotes tumor development, metastasis, and cell survival. Promising findings have been found in studies on the cell cycle-mediated apoptosis pathway for medication development and treatment. Dietary phytoconstituents have been studied in great detail for their potential to prevent cancer by triggering the body’s defense mechanisms. The underlying mechanisms of action may be clarified by considering the role of polyphenols in important cancer signaling pathways. Phenolic acids, flavonoids, tannins, coumarins, lignans, lignins, naphthoquinones, anthraquinones, xanthones, and stilbenes are examples of natural chemicals that are being studied for potential anticancer drugs. These substances are also vital for signaling pathways. This review focuses on innovations in the study of polyphenol genistein’s effects on breast cancer cells and presents integrated chemical biology methods to harness mechanisms of action for important therapeutic advances. Full article
(This article belongs to the Special Issue Phenolic Compounds in Human Diseases)
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