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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
- 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.
- Subjects :
- Models, Molecular
sulphonamide inhibitors
Cell Membrane Permeability
ved/biology.organism_classification_rank.species
carbonic anhydrase
01 natural sciences
Cell wall
chemistry.chemical_compound
Structure-Activity Relationship
membrane penetrability
In vivo
Carbonic anhydrase
Drug Discovery
Phaeodactylum tricornutum
Model organism
Carbonic Anhydrase Inhibitors
Carbonic Anhydrases
Pharmacology
Diatoms
Sulfonamides
metalloenzymes
biology
Dose-Response Relationship, Drug
Molecular Structure
010405 organic chemistry
ved/biology
marine diatom
lcsh:RM1-950
General Medicine
biology.organism_classification
In vitro
0104 chemical sciences
010404 medicinal & biomolecular chemistry
Diatom
lcsh:Therapeutics. Pharmacology
Biochemistry
chemistry
biology.protein
Growth inhibition
Research Paper
Subjects
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