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Special Issue "From Natural Polyphenols to Synthetic Bioactive Analogues"

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: 30 September 2019

Special Issue Editor

Guest Editor
Prof. Dr. Corrado Tringali

Dipartimento di Scienze Chimiche, Università di Catania, Viale A. Doria 6, I-95125 Catania, Italy
Website 1 | Website 2 | E-Mail
Phone: +39 0957385025
Interests: synthesis of natural-derived polyphenols; low environmental impact reagents and enzymes; isolation and identification of bioactive compounds; extraction and fractionation of biological material from natural sources

Special Issue Information

Dear Colleagues,

In recent years, phenolic compounds from plant sources, commonly referred to as ‘plant polyphenols’, have been the subject of an impressive number of research studies, to a large extent focused on the healthy properties attributed to diet polyphenols, including antioxidant, anti-inflammatory, antineoplastic, antidiabetic, neuroprotective, and other biological activities. Additionally, phenolic compounds isolated from toxic plants and showing cytotoxic or antiproliferative activity have been intensively investigated in view of a possible exploitation of their anticancer properties. In parallel, many research groups have focused their work on obtaining synthetic or semisynthetic analogues of these molecules, with the aim of enhancing their biological activity and possibly improving their metabolic stability and bioavailability, as a first step towards the discovery of new chemotherapeutics agents. The preparation of libraries of analogues derived from natural polyphenols may also contribute to a better understanding of the molecular mechanisms of action of the most promising compounds through structure-activity relationship (SAR) studies. Finally, synthetic compounds inspired to a natural scaffold may also show new and unexpected biological properties. Thus, this Special Issue aims to highlight the most recent results in the field of synthetic bioactive analogues of natural polyphenols. Original articles, as well as reviews, regarding studies on analogues of flavonoids, stilbenoids, curcuminoids, lignans, neolignans and other polyphenol-derived compounds are welcome.

Prof. Dr. Corrado Tringali
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 papers will be 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. Molecules is an international peer-reviewed open access bimonthly 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 1800 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.


  • Polyphenols
  • Organic synthesis
  • Medicinal chemistry
  • Molecular modeling
  • Structure–activity relationship (SAR)
  • Biological activity
  • Bioinspired compounds
  • Antiproliferative
  • Anti-inflammatory
  • Neuroprotective

Published Papers (1 paper)

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Open AccessArticle Melaleuca styphelioides Sm. Polyphenols Modulate Interferon Gamma/Histamine-Induced Inflammation in Human NCTC 2544 Keratinocytes
Molecules 2018, 23(10), 2526; https://doi.org/10.3390/molecules23102526
Received: 10 September 2018 / Revised: 28 September 2018 / Accepted: 29 September 2018 / Published: 2 October 2018
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Melaleuca styphelioides, known as the prickly-leaf tea tree, contains a variety of bioactive compounds. The purposes of this study were to characterize the polyphenols extracted from Melaleuca styphelioides leaves and assess their potential antioxidant and anti-inflammatory effects. The polyphenol extracts were prepared
[...] Read more.
Melaleuca styphelioides, known as the prickly-leaf tea tree, contains a variety of bioactive compounds. The purposes of this study were to characterize the polyphenols extracted from Melaleuca styphelioides leaves and assess their potential antioxidant and anti-inflammatory effects. The polyphenol extracts were prepared by maceration with solvents of increasing polarity. The LC/MS-MS technique was used to identify and quantify the phenolic compounds. An assessment of the radical scavenging activity of all extracts was performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) (ABTS+), and ferric reducing antioxidant power (FRAP) assays. The anti-inflammatory activity was determined on interferon gamma (IFN-γ)/histamine (H)-stimulated human NCTC 2544 keratinocytes by Western blot and RT-PCR. Compared to other solvents, methanolic extract presented the highest level of phenolic contents. The most frequent phenolic compounds were quercetin, followed by gallic acid and ellagic acid. DPPH, ABTS+, and FRAP assays showed that methanolic extract exhibits strong concentration-dependent antioxidant activity. IFN-γ/H treatment of human NCTC 2544 keratinocytes induced the secretion of high levels of the pro-inflammatory mediator inter-cellular adhesion molecule-1 (ICAM-1), nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and nuclear factor kappa B (NF-κB), which were inhibited by extract. In conclusion, the extract of Melaleuca styphelioides leaves is rich in flavonoids, and presents antioxidant and anti-inflammatory proprieties. It can be proposed as a useful compound to treat inflammatory skin diseases. Full article
(This article belongs to the Special Issue From Natural Polyphenols to Synthetic Bioactive Analogues)

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