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Marine Drugs
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Bioassay Platforms for the Disclosure of the Pharmaceutical Potential of...
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Bioassay Platforms for the Disclosure of the Pharmaceutical Potential of Marine Natural Products

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (31 August 2021) | Viewed by 7150

Special Issue Editors

Dr. Nuzzo Genoveffa

E-Mail Website
Guest Editor
Bio-Organic Chemistry Research Group, Consiglio Nazionale delle Ricerche - Istituto di Chimica Biomolecolare, Via Campi Flegrei 34, 80078 Pozzuoli, Napoli, Italy
Interests: development and application of a novel spe-method for bioassay-guided fractionation of marine extracts
Special Issues, Collections and Topics in MDPI journals
Dr. Carmela Gallo

E-Mail Website
Guest Editor
Institute of Biomolecular Chemistry, Cnr Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Italy
Interests: immunology; natural product drug discovery; cell biology; inflammation; microalgae
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Marine organisms have proven to be a rich source of diverse natural products with distinctive antibacterial, antifungal, antiviral, antiparasitic, antitumor, antiinflammatory, antioxidant, and immunomodulatory activities. Various marine metabolites have shown drug-like physicochemical properties through specific mechanisms of action. A bioassay-guided fractionation is usually conducted for the identified of the pharmaceutical potential of marine natural products, but other strategies can be applied. To purify novel secondary metabolites, it is crucial to develop efficient screening platforms to recognize the samples with the most promise early in the workflow so that resources can be efficiently and cost-effectively used. To avoid the isolation of known molecules, dereplication analysis can now be used to identify candidate bioactive molecules early in the purification step to rationalize the isolation scheme.

A screening platform of bioactive compounds may involve a huge number of analysis assays for assessing the potential of biological extracts or molecules from marine organisms. The assays can be performed at the whole animal, cell, or molecular levels by two different complementary approaches: classical pharmacology, also known as phenotypic drug discovery, which is the historical basis of drug discovery, and reverse pharmacology or target-based drug discovery. The improvement of the whole procedure needs innovative assay platforms that can be used to help to automate testing processes with greater throughput, speed, reliability, and reproducibility.

Dr. Nuzzo Genoveffa
Dr. Carmela Gallo
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. Marine Drugs is an international peer-reviewed open access monthly 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

  • marine natural products
  • lead compound
  • drug discovery platform
  • bioassay guided fractionation
  • bioactive marine metabolite
  • bioassay screening platform

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Published Papers (2 papers)

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16 pages, 3022 KiB  
Article
Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
by Alejandro Moreiras-Figueruelo, Genoveffa Nuzzo, Christian Galasso, Clementina Sansone, Fabio Crocetta, Valerio Mazzella, Carmela Gallo, Giusi Barra, Angela Sardo, Antonella Iuliano, Emiliano Manzo, Giuliana d’Ippolito, Marte Albrigtsen, Jeanette H. Andersen, Adrianna Ianora and Angelo Fontana
Mar. Drugs 2021, 19(11), 640; https://doi.org/10.3390/md19110640 - 16 Nov 2021
Cited by 3 | Viewed by 2926
Abstract
The marine environment is potentially a prolific source of small molecules with significant biological activities. In recent years, the development of new chromatographic phases and the progress in cell and molecular techniques have facilitated the search for marine natural products (MNPs) as novel [...] Read more.
The marine environment is potentially a prolific source of small molecules with significant biological activities. In recent years, the development of new chromatographic phases and the progress in cell and molecular techniques have facilitated the search for marine natural products (MNPs) as novel pharmacophores and enhanced the success rate in the selection of new potential drug candidates. However, most of this exploration has so far been driven by anticancer research and has been limited to a reduced number of taxonomic groups. In this article, we report a test study on the screening potential of an in-house library of natural small molecules composed of 285 samples derived from 57 marine organisms that were chosen from among the major eukaryotic phyla so far represented in studies on bioactive MNPs. Both the extracts and SPE fractions of these organisms were simultaneously submitted to three different bioassays—two phenotypic and one enzymatic—for cytotoxic, antidiabetic, and antibacterial activity. On the whole, the screening of the MNP library selected 11 potential hits, but the distribution of the biological results showed that SPE fractionation increased the positive score regardless of the taxonomic group. In many cases, activity could be detected only in the enriched fractions after the elimination of the bulky effect due to salts. On a statistical basis, sponges and molluscs were confirmed to be the most significant source of cytotoxic and antimicrobial products, but other phyla were found to be effective with the other therapeutic targets. Full article
(This article belongs to the Special Issue Bioassay Platforms for the Disclosure of the Pharmaceutical Potential of Marine Natural Products)
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14 pages, 1889 KiB  
Article
A New Bioassay Platform Design for the Discovery of Small Molecules with Anticancer Immunotherapeutic Activity
by Carmela Gallo, Giusi Barra, Marisa Saponaro, Emiliano Manzo, Laura Fioretto, Marcello Ziaco, Genoveffa Nuzzo, Giuliana d’Ippolito, Raffaele De Palma and Angelo Fontana
Mar. Drugs 2020, 18(12), 604; https://doi.org/10.3390/md18120604 - 29 Nov 2020
Cited by 10 | Viewed by 3260
Abstract
Immunotherapy takes advantage of the immune system to prevent, control, and eliminate neoplastic cells. The research in the field has already led to major breakthroughs to treat cancer. In this work, we describe a platform that integrates in vitro bioassays to test the [...] Read more.
Immunotherapy takes advantage of the immune system to prevent, control, and eliminate neoplastic cells. The research in the field has already led to major breakthroughs to treat cancer. In this work, we describe a platform that integrates in vitro bioassays to test the immune response and direct antitumor effects for the preclinical discovery of anticancer candidates. The platform relies on the use of dendritic cells that are professional antigen-presenting cells (APC) able to activate T cells and trigger a primary adaptive immune response. The experimental procedure is based on two phenotypic assays for the selection of chemical leads by both a panel of nine tumor cell lines and growth factor-dependent immature mouse dendritic cells (D1). The positive hits are then validated by a secondary test on human monocyte-derived dendritic cells (MoDCs). The aim of this approach is the selection of potential immunotherapeutic small molecules from natural extracts or chemical libraries. Full article
(This article belongs to the Special Issue Bioassay Platforms for the Disclosure of the Pharmaceutical Potential of Marine Natural Products)
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