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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Online Access: | http://hdl.handle.net/11567/1078598 https://doi.org/10.3390/MD19080459 |
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ftunivgenova:oai:iris.unige.it:11567/1078598 2024-02-11T09:57:52+01:00 Bioactivity screening of antarctic sponges reveals anticancer activity and potential cell death via ferroptosis by mycalols Riccio G. Nuzzo G. Zazo G. Coppola D. Senese G. Romano L. Costantini M. Ruocco N. Bertolino M. Fontana A. Ianora A. Verde C. Giordano D. Lauritano C. Riccio, G. Nuzzo, G. Zazo, G. Coppola, D. Senese, G. Romano, L. Costantini, M. Ruocco, N. Bertolino, M. Fontana, A. Ianora, A. Verde, C. Giordano, D. Lauritano, C. 2021 STAMPA http://hdl.handle.net/11567/1078598 https://doi.org/10.3390/MD19080459 eng eng MDPI place:ST ALBAN-ANLAGE 66, CH-4052 BASEL, SWITZERLAND info:eu-repo/semantics/altIdentifier/pmid/34436298 info:eu-repo/semantics/altIdentifier/wos/WOS:000689361300001 volume:19 firstpage:459 lastpage:459 numberofpages:15 journal:MARINE DRUGS http://hdl.handle.net/11567/1078598 doi:10.3390/MD19080459 info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85114372132 Antarctica Drug discovery Marine biotechnology Mycalol Sponge Animal Antarctic Region Antineoplastic Agent Aquatic Organism Cell Line Tumor Fatty Alcohol Hep G2 Cell Human Phytotherapy Porifera info:eu-repo/semantics/article 2021 ftunivgenova https://doi.org/10.3390/MD19080459 2024-01-24T17:47:45Z 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. Article in Journal/Newspaper Antarc* Antarctic Antarctica Italian National Antarctic Research Program National Antarctic Research Program Università degli Studi di Genova: CINECA IRIS Antarctic Marine Drugs 19 8 459 |
institution |
Open Polar |
collection |
Università degli Studi di Genova: CINECA IRIS |
op_collection_id |
ftunivgenova |
language |
English |
topic |
Antarctica Drug discovery Marine biotechnology Mycalol Sponge Animal Antarctic Region Antineoplastic Agent Aquatic Organism Cell Line Tumor Fatty Alcohol Hep G2 Cell Human Phytotherapy Porifera |
spellingShingle |
Antarctica Drug discovery Marine biotechnology Mycalol Sponge Animal Antarctic Region Antineoplastic Agent Aquatic Organism Cell Line Tumor Fatty Alcohol Hep G2 Cell Human Phytotherapy Porifera Riccio G. Nuzzo G. Zazo G. Coppola D. Senese G. Romano L. Costantini M. Ruocco N. Bertolino M. Fontana A. Ianora A. Verde C. Giordano D. Lauritano C. Bioactivity screening of antarctic sponges reveals anticancer activity and potential cell death via ferroptosis by mycalols |
topic_facet |
Antarctica Drug discovery Marine biotechnology Mycalol Sponge Animal Antarctic Region Antineoplastic Agent Aquatic Organism Cell Line Tumor Fatty Alcohol Hep G2 Cell Human Phytotherapy Porifera |
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. |
author2 |
Riccio, G. Nuzzo, G. Zazo, G. Coppola, D. Senese, G. Romano, L. Costantini, M. Ruocco, N. Bertolino, M. Fontana, A. Ianora, A. Verde, C. Giordano, D. Lauritano, C. |
format |
Article in Journal/Newspaper |
author |
Riccio G. Nuzzo G. Zazo G. Coppola D. Senese G. Romano L. Costantini M. Ruocco N. Bertolino M. Fontana A. Ianora A. Verde C. Giordano D. Lauritano C. |
author_facet |
Riccio G. Nuzzo G. Zazo G. Coppola D. Senese G. Romano L. Costantini M. Ruocco N. Bertolino M. Fontana A. Ianora A. Verde C. Giordano D. Lauritano C. |
author_sort |
Riccio G. |
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://hdl.handle.net/11567/1078598 https://doi.org/10.3390/MD19080459 |
geographic |
Antarctic |
geographic_facet |
Antarctic |
genre |
Antarc* Antarctic Antarctica Italian National Antarctic Research Program National Antarctic Research Program |
genre_facet |
Antarc* Antarctic Antarctica Italian National Antarctic Research Program National Antarctic Research Program |
op_relation |
info:eu-repo/semantics/altIdentifier/pmid/34436298 info:eu-repo/semantics/altIdentifier/wos/WOS:000689361300001 volume:19 firstpage:459 lastpage:459 numberofpages:15 journal:MARINE DRUGS http://hdl.handle.net/11567/1078598 doi:10.3390/MD19080459 info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85114372132 |
op_doi |
https://doi.org/10.3390/MD19080459 |
container_title |
Marine Drugs |
container_volume |
19 |
container_issue |
8 |
container_start_page |
459 |
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1790593403567734784 |