Probing the Therapeutic Potential of Marine Phyla by SPE Extraction

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...

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Autores principales:	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, Angelo Fontana
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	marine natural products small molecules drug discovery platform pre-fractionation method active metabolites cytotoxic Biology (General) QH301-705.5
Acceso en línea:	https://doaj.org/article/f6f7bd68349546a7b50cb53e71f6c882
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spelling	oai:doaj.org-article:f6f7bd68349546a7b50cb53e71f6c8822021-11-25T18:13:00ZProbing the Therapeutic Potential of Marine Phyla by SPE Extraction10.3390/md191106401660-3397https://doaj.org/article/f6f7bd68349546a7b50cb53e71f6c8822021-11-01T00:00:00Zhttps://www.mdpi.com/1660-3397/19/11/640https://doaj.org/toc/1660-3397The 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.Alejandro Moreiras-FiguerueloGenoveffa NuzzoChristian GalassoClementina SansoneFabio CrocettaValerio MazzellaCarmela GalloGiusi BarraAngela SardoAntonella IulianoEmiliano ManzoGiuliana d’IppolitoMarte AlbrigtsenJeanette H. AndersenAdrianna IanoraAngelo FontanaMDPI AGarticlemarine natural productssmall moleculesdrug discovery platformpre-fractionation methodactive metabolitescytotoxicBiology (General)QH301-705.5ENMarine Drugs, Vol 19, Iss 640, p 640 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	marine natural products small molecules drug discovery platform pre-fractionation method active metabolites cytotoxic Biology (General) QH301-705.5
spellingShingle	marine natural products small molecules drug discovery platform pre-fractionation method active metabolites cytotoxic Biology (General) QH301-705.5 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 Angelo Fontana Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
description	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.
format	article
author	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 Angelo Fontana
author_facet	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 Angelo Fontana
author_sort	Alejandro Moreiras-Figueruelo
title	Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
title_short	Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
title_full	Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
title_fullStr	Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
title_full_unstemmed	Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
title_sort	probing the therapeutic potential of marine phyla by spe extraction
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f6f7bd68349546a7b50cb53e71f6c882
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Probing the Therapeutic Potential of Marine Phyla by SPE Extraction

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