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Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors

Carbonic anhydrases (CAs) are ubiquitous metalloenzymes, which started to be investigated in detail in pathogenic, as well as non-pathogenic species since their pivotal role is to accelerate the physiological CO(2) hydration/dehydration reaction significantly. Here, we propose the marine unicellular...

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Autores principales: Rogato, Alessandra, Del Prete, Sonia, Nocentini, Alessio, Carginale, Vincenzo, Supuran, Claudiu T., Capasso, Clemente
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352938/
https://www.ncbi.nlm.nih.gov/pubmed/30688123
http://dx.doi.org/10.1080/14756366.2018.1559840
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author Rogato, Alessandra
Del Prete, Sonia
Nocentini, Alessio
Carginale, Vincenzo
Supuran, Claudiu T.
Capasso, Clemente
author_facet Rogato, Alessandra
Del Prete, Sonia
Nocentini, Alessio
Carginale, Vincenzo
Supuran, Claudiu T.
Capasso, Clemente
author_sort Rogato, Alessandra
collection PubMed
description Carbonic anhydrases (CAs) are ubiquitous metalloenzymes, which started to be investigated in detail in pathogenic, as well as non-pathogenic species since their pivotal role is to accelerate the physiological CO(2) hydration/dehydration reaction significantly. Here, we propose the marine unicellular diatom Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of CA inhibitors (CAIs). Seven inhibitors belonging to the sulphonamide type and possessing a diverse scaffold have been explored for their in vitro inhibition of the whole diatom CAs and the in vivo inhibitory effect on the growth of P. tricornutum. Interesting, inhibition of growth was observed, in vivo, demonstrating that this diatom is a good model for testing the cell wall penetrability of this class of pharmacological agents. Considering that many pathogens are difficult and dangerous to grow in the laboratory, the growth inhibition of P. tricornutum with different such CAIs may be subsequently used to design inhibition studies of CAs from pathogenic organisms.
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spelling pubmed-63529382019-02-06 Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors Rogato, Alessandra Del Prete, Sonia Nocentini, Alessio Carginale, Vincenzo Supuran, Claudiu T. Capasso, Clemente J Enzyme Inhib Med Chem Research Paper Carbonic anhydrases (CAs) are ubiquitous metalloenzymes, which started to be investigated in detail in pathogenic, as well as non-pathogenic species since their pivotal role is to accelerate the physiological CO(2) hydration/dehydration reaction significantly. Here, we propose the marine unicellular diatom Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of CA inhibitors (CAIs). Seven inhibitors belonging to the sulphonamide type and possessing a diverse scaffold have been explored for their in vitro inhibition of the whole diatom CAs and the in vivo inhibitory effect on the growth of P. tricornutum. Interesting, inhibition of growth was observed, in vivo, demonstrating that this diatom is a good model for testing the cell wall penetrability of this class of pharmacological agents. Considering that many pathogens are difficult and dangerous to grow in the laboratory, the growth inhibition of P. tricornutum with different such CAIs may be subsequently used to design inhibition studies of CAs from pathogenic organisms. Taylor & Francis 2019-01-27 /pmc/articles/PMC6352938/ /pubmed/30688123 http://dx.doi.org/10.1080/14756366.2018.1559840 Text en © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Rogato, Alessandra
Del Prete, Sonia
Nocentini, Alessio
Carginale, Vincenzo
Supuran, Claudiu T.
Capasso, Clemente
Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title_full Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title_fullStr Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title_full_unstemmed Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title_short Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
title_sort phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352938/
https://www.ncbi.nlm.nih.gov/pubmed/30688123
http://dx.doi.org/10.1080/14756366.2018.1559840
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