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

Articolo
Data di Pubblicazione:
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.
Tipologia CRIS:
01.01 Articolo in rivista
Keywords:
Carbonic anhydrase; metalloenzymes; sulphonamide inhibitors; marine diatom; membrane penetrability
Elenco autori:
Carginale, Vincenzo; Capasso, Clemente; Rogato, Alessandra; DEL PRETE, Sonia
Autori di Ateneo:
CAPASSO CLEMENTE
CARGINALE VINCENZO
DEL PRETE SONIA
ROGATO ALESSANDRA
Link alla scheda completa:
https://iris.cnr.it/handle/20.500.14243/386003
Pubblicato in:
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (PRINT)
Journal
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