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(+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro

Potent drugs are desperately needed to counteract bacterial biofilm infections, especially those caused by gram-positive organisms, such as Staphylococcus aureus. Moreover, anti-biofilm compounds/agents that can be used as chemical tools are also needed for basic in vitro or in vivo studies aimed at...

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Autores principales: Fallarero, Adyary, Skogman, Malena, Kujala, Janni, Rajaratnam, Mohanathas, Moreira, Vânia M., Yli-Kauhaluoma, Jari, Vuorela, Pia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3709773/
https://www.ncbi.nlm.nih.gov/pubmed/23739682
http://dx.doi.org/10.3390/ijms140612054
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author Fallarero, Adyary
Skogman, Malena
Kujala, Janni
Rajaratnam, Mohanathas
Moreira, Vânia M.
Yli-Kauhaluoma, Jari
Vuorela, Pia
author_facet Fallarero, Adyary
Skogman, Malena
Kujala, Janni
Rajaratnam, Mohanathas
Moreira, Vânia M.
Yli-Kauhaluoma, Jari
Vuorela, Pia
author_sort Fallarero, Adyary
collection PubMed
description Potent drugs are desperately needed to counteract bacterial biofilm infections, especially those caused by gram-positive organisms, such as Staphylococcus aureus. Moreover, anti-biofilm compounds/agents that can be used as chemical tools are also needed for basic in vitro or in vivo studies aimed at exploring biofilms behavior and functionability. In this contribution, a collection of naturally-occurring abietane-type diterpenes and their derivatives was tested against S. aureus biofilms using a platform consisting of two phenotypic assays that have been previously published by our group. Three active compounds were identified: nordehydroabietylamine (1), (+)-dehydroabietic acid (2) and (+)-dehydroabietylamine (3) that prevented biofilm formation in the low micromolar range, and unlike typical antibiotics, only 2 to 4-fold higher concentrations were needed to significantly reduce viability and biomass of existing biofilms. Compound 2, (+)-dehydroabietic acid, was the most selective towards biofilm bacteria, achieving high killing efficacy (based on log Reduction values) and it was best tolerated by three different mammalian cell lines. Since (+)-dehydroabietic acid is an easily available compound, it holds great potential to be used as a molecular probe in biofilms-related studies as well as to serve as inspirational chemical model for the development of potent drug candidates.
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spelling pubmed-37097732013-07-12 (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro Fallarero, Adyary Skogman, Malena Kujala, Janni Rajaratnam, Mohanathas Moreira, Vânia M. Yli-Kauhaluoma, Jari Vuorela, Pia Int J Mol Sci Article Potent drugs are desperately needed to counteract bacterial biofilm infections, especially those caused by gram-positive organisms, such as Staphylococcus aureus. Moreover, anti-biofilm compounds/agents that can be used as chemical tools are also needed for basic in vitro or in vivo studies aimed at exploring biofilms behavior and functionability. In this contribution, a collection of naturally-occurring abietane-type diterpenes and their derivatives was tested against S. aureus biofilms using a platform consisting of two phenotypic assays that have been previously published by our group. Three active compounds were identified: nordehydroabietylamine (1), (+)-dehydroabietic acid (2) and (+)-dehydroabietylamine (3) that prevented biofilm formation in the low micromolar range, and unlike typical antibiotics, only 2 to 4-fold higher concentrations were needed to significantly reduce viability and biomass of existing biofilms. Compound 2, (+)-dehydroabietic acid, was the most selective towards biofilm bacteria, achieving high killing efficacy (based on log Reduction values) and it was best tolerated by three different mammalian cell lines. Since (+)-dehydroabietic acid is an easily available compound, it holds great potential to be used as a molecular probe in biofilms-related studies as well as to serve as inspirational chemical model for the development of potent drug candidates. Molecular Diversity Preservation International (MDPI) 2013-06-05 /pmc/articles/PMC3709773/ /pubmed/23739682 http://dx.doi.org/10.3390/ijms140612054 Text en © 2013 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 license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Fallarero, Adyary
Skogman, Malena
Kujala, Janni
Rajaratnam, Mohanathas
Moreira, Vânia M.
Yli-Kauhaluoma, Jari
Vuorela, Pia
(+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title_full (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title_fullStr (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title_full_unstemmed (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title_short (+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro
title_sort (+)-dehydroabietic acid, an abietane-type diterpene, inhibits staphylococcus aureus biofilms in vitro
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3709773/
https://www.ncbi.nlm.nih.gov/pubmed/23739682
http://dx.doi.org/10.3390/ijms140612054
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