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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...

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Autores principales: McCarthy, Peter J., Roberts, Bracken F., Carbonell, Abigail, Roberts, Jill, Wright, Amy E., Chakrabarti, Debopam
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
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.
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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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