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Marine Microbiome as a Source of Antimalarials
It is important to discover novel antimalarial pharmacophores because of the widespread emergence of Plasmodium falciparum isolates resistant to the available drugs. Secondary metabolites derived from microbes associated with marine invertebrates are a valuable resource for the discovery of novel dr...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6789460/ https://www.ncbi.nlm.nih.gov/pubmed/31337089 http://dx.doi.org/10.3390/tropicalmed4030103 |
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author | McCarthy, Peter J. Roberts, Bracken F. Carbonell, Abigail Roberts, Jill Wright, Amy E. Chakrabarti, Debopam |
author_facet | McCarthy, Peter J. Roberts, Bracken F. Carbonell, Abigail Roberts, Jill Wright, Amy E. Chakrabarti, Debopam |
author_sort | McCarthy, Peter J. |
collection | PubMed |
description | It is important to discover novel antimalarial pharmacophores because of the widespread emergence of Plasmodium falciparum isolates resistant to the available drugs. Secondary metabolites derived from microbes associated with marine invertebrates are a valuable resource for the discovery of novel drug leads. However, the potential of marine microbes as a source of antimalarials has not been explored. We investigated the promise of marine microorganisms for the production of antimalarial activities by testing 2365 diverse microbial extracts using phenotypic screening of a multidrug resistant chloroquine resistant P. falciparum strain. We conducted counter screening against mammalian cells for the 317 active extracts that exhibited more than 70% inhibition at 1 µg/mL. The screen identified 17 potent bioactive leads from a broad range of taxa. Our results establish that the marine microbiome is a rich source of antiplasmodial compounds that warrants in depth exploration. |
format | Online Article Text |
id | pubmed-6789460 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-67894602019-10-16 Marine Microbiome as a Source of Antimalarials McCarthy, Peter J. Roberts, Bracken F. Carbonell, Abigail Roberts, Jill Wright, Amy E. Chakrabarti, Debopam Trop Med Infect Dis Perspective It is important to discover novel antimalarial pharmacophores because of the widespread emergence of Plasmodium falciparum isolates resistant to the available drugs. Secondary metabolites derived from microbes associated with marine invertebrates are a valuable resource for the discovery of novel drug leads. However, the potential of marine microbes as a source of antimalarials has not been explored. We investigated the promise of marine microorganisms for the production of antimalarial activities by testing 2365 diverse microbial extracts using phenotypic screening of a multidrug resistant chloroquine resistant P. falciparum strain. We conducted counter screening against mammalian cells for the 317 active extracts that exhibited more than 70% inhibition at 1 µg/mL. The screen identified 17 potent bioactive leads from a broad range of taxa. Our results establish that the marine microbiome is a rich source of antiplasmodial compounds that warrants in depth exploration. MDPI 2019-07-13 /pmc/articles/PMC6789460/ /pubmed/31337089 http://dx.doi.org/10.3390/tropicalmed4030103 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Perspective McCarthy, Peter J. Roberts, Bracken F. Carbonell, Abigail Roberts, Jill Wright, Amy E. Chakrabarti, Debopam Marine Microbiome as a Source of Antimalarials |
title | Marine Microbiome as a Source of Antimalarials |
title_full | Marine Microbiome as a Source of Antimalarials |
title_fullStr | Marine Microbiome as a Source of Antimalarials |
title_full_unstemmed | Marine Microbiome as a Source of Antimalarials |
title_short | Marine Microbiome as a Source of Antimalarials |
title_sort | marine microbiome as a source of antimalarials |
topic | Perspective |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6789460/ https://www.ncbi.nlm.nih.gov/pubmed/31337089 http://dx.doi.org/10.3390/tropicalmed4030103 |
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