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

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

Authors :
Claudiu T. Supuran
Sonia Del Prete
Clemente Capasso
Vincenzo Carginale
Alessio Nocentini
Alessandra Rogato
Source :
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 510-518 (2019), Journal of Enzyme Inhibition and Medicinal Chemistry
Publication Year :
2019
Publisher :
Taylor & Francis Group, 2019.

Abstract

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 CO2 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.

Details

Language :
English
ISSN :
14756374 and 14756366
Volume :
34
Issue :
1
Database :
OpenAIRE
Journal :
Journal of Enzyme Inhibition and Medicinal Chemistry
Accession number :
edsair.doi.dedup.....18ce8a35d01b1c68ee6bf5646510fcf6