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

Authors :
Rogato, Alessandra
Del Prete, Sonia
Nocentini, Alessio
Carginale, Vincenzo
Supuran, Claudiu T.
Capasso, Clemente
Source :
Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2019, Vol. 34 Issue 1, p510-518, 9p
Publication Year :
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 CO<subscript>2</subscript> 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
14756366
Volume :
34
Issue :
1
Database :
Complementary Index
Journal :
Journal of Enzyme Inhibition & Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
140468394
Full Text :
https://doi.org/10.1080/14756366.2018.1559840