Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols
Sponges are known to produce a series of compounds with bioactivities useful for human health. This study was conducted on four sponges collected in the framework of the XXXIV Italian National Antarctic Research Program (PNRA) in November-December 2018, i.e., Mycale (Oxymycale) acerata, Haliclona (R...
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ftpubmed:oai:pubmedcentral.nih.gov:8400861 2023-05-15T13:57:19+02:00 Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols Riccio, Gennaro Nuzzo, Genoveffa Zazo, Gianluca Coppola, Daniela Senese, Giuseppina Romano, Lucia Costantini, Maria Ruocco, Nadia Bertolino, Marco Fontana, Angelo Ianora, Adrianna Verde, Cinzia Giordano, Daniela Lauritano, Chiara 2021-08-14 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8400861/ http://www.ncbi.nlm.nih.gov/pubmed/34436298 https://doi.org/10.3390/md19080459 en eng MDPI http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8400861/ http://www.ncbi.nlm.nih.gov/pubmed/34436298 http://dx.doi.org/10.3390/md19080459 © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). CC-BY Mar Drugs Article Text 2021 ftpubmed https://doi.org/10.3390/md19080459 2021-09-05T00:59:07Z Sponges are known to produce a series of compounds with bioactivities useful for human health. This study was conducted on four sponges collected in the framework of the XXXIV Italian National Antarctic Research Program (PNRA) in November-December 2018, i.e., Mycale (Oxymycale) acerata, Haliclona (Rhizoniera) dancoi, Hemimycale topsenti, and Hemigellius pilosus. Sponge extracts were fractioned and tested against hepatocellular carcinoma (HepG2), lung carcinoma (A549), and melanoma cells (A2058), in order to screen for antiproliferative or cytotoxic activity. Two different chemical classes of compounds, belonging to mycalols and suberitenones, were identified in the active fractions. Mycalols were the most active compounds, and their mechanism of action was also investigated at the gene and protein levels in HepG2 cells. Of the differentially expressed genes, ULK1 and GALNT5 were the most down-regulated genes, while MAPK8 was one of the most up-regulated genes. These genes were previously associated with ferroptosis, a programmed cell death triggered by iron-dependent lipid peroxidation, confirmed at the protein level by the down-regulation of GPX4, a key regulator of ferroptosis, and the up-regulation of NCOA4, involved in iron homeostasis. These data suggest, for the first time, that mycalols act by triggering ferroptosis in HepG2 cells. Text Antarc* Antarctic Italian National Antarctic Research Program National Antarctic Research Program PubMed Central (PMC) Antarctic Marine Drugs 19 8 459 |
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Article Riccio, Gennaro Nuzzo, Genoveffa Zazo, Gianluca Coppola, Daniela Senese, Giuseppina Romano, Lucia Costantini, Maria Ruocco, Nadia Bertolino, Marco Fontana, Angelo Ianora, Adrianna Verde, Cinzia Giordano, Daniela Lauritano, Chiara Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
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description |
Sponges are known to produce a series of compounds with bioactivities useful for human health. This study was conducted on four sponges collected in the framework of the XXXIV Italian National Antarctic Research Program (PNRA) in November-December 2018, i.e., Mycale (Oxymycale) acerata, Haliclona (Rhizoniera) dancoi, Hemimycale topsenti, and Hemigellius pilosus. Sponge extracts were fractioned and tested against hepatocellular carcinoma (HepG2), lung carcinoma (A549), and melanoma cells (A2058), in order to screen for antiproliferative or cytotoxic activity. Two different chemical classes of compounds, belonging to mycalols and suberitenones, were identified in the active fractions. Mycalols were the most active compounds, and their mechanism of action was also investigated at the gene and protein levels in HepG2 cells. Of the differentially expressed genes, ULK1 and GALNT5 were the most down-regulated genes, while MAPK8 was one of the most up-regulated genes. These genes were previously associated with ferroptosis, a programmed cell death triggered by iron-dependent lipid peroxidation, confirmed at the protein level by the down-regulation of GPX4, a key regulator of ferroptosis, and the up-regulation of NCOA4, involved in iron homeostasis. These data suggest, for the first time, that mycalols act by triggering ferroptosis in HepG2 cells. |
format |
Text |
author |
Riccio, Gennaro Nuzzo, Genoveffa Zazo, Gianluca Coppola, Daniela Senese, Giuseppina Romano, Lucia Costantini, Maria Ruocco, Nadia Bertolino, Marco Fontana, Angelo Ianora, Adrianna Verde, Cinzia Giordano, Daniela Lauritano, Chiara |
author_facet |
Riccio, Gennaro Nuzzo, Genoveffa Zazo, Gianluca Coppola, Daniela Senese, Giuseppina Romano, Lucia Costantini, Maria Ruocco, Nadia Bertolino, Marco Fontana, Angelo Ianora, Adrianna Verde, Cinzia Giordano, Daniela Lauritano, Chiara |
author_sort |
Riccio, Gennaro |
title |
Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
title_short |
Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
title_full |
Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
title_fullStr |
Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
title_full_unstemmed |
Bioactivity Screening of Antarctic Sponges Reveals Anticancer Activity and Potential Cell Death via Ferroptosis by Mycalols |
title_sort |
bioactivity screening of antarctic sponges reveals anticancer activity and potential cell death via ferroptosis by mycalols |
publisher |
MDPI |
publishDate |
2021 |
url |
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8400861/ http://www.ncbi.nlm.nih.gov/pubmed/34436298 https://doi.org/10.3390/md19080459 |
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Antarctic |
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Antarctic |
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Antarc* Antarctic Italian National Antarctic Research Program National Antarctic Research Program |
genre_facet |
Antarc* Antarctic Italian National Antarctic Research Program National Antarctic Research Program |
op_source |
Mar Drugs |
op_relation |
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8400861/ http://www.ncbi.nlm.nih.gov/pubmed/34436298 http://dx.doi.org/10.3390/md19080459 |
op_rights |
© 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
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CC-BY |
op_doi |
https://doi.org/10.3390/md19080459 |
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Marine Drugs |
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19 |
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8 |
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459 |
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1766264928556023808 |