Here, we report a toxicity study, conducted on zebrafish larvae, of a series of coumarin and sulfamide compounds that were previously reported as inhibitors of human (h) metalloenzymes, carbonic anhydrases (CAs, EC 4.2.1.1). Due to the high relevance of hCA inhibitors as theragnostic agents, it is of pivotal importance to address safety issues that may arise from the initial in vivo toxicological assessment using zebrafish, a relevant model for biomedical research. None of the reported compounds showed adverse phenotypic effects or tissue damage on developing zebrafish larvae after 5 days of exposure. Our study suggests that the coumarin and sulfamide derivatives considered here are safe and suitable for further development and testing.

Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases / Aspatwar, A.; Berrino, E.; Bua, S.; Carta, F.; Capasso, C.; Parkkila, S.; Supuran, C. T.. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - 35:(2020), pp. 1765-1772. [10.1080/14756366.2020.1822829]

Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases

Berrino E.;Supuran C. T.
2020

Abstract

Here, we report a toxicity study, conducted on zebrafish larvae, of a series of coumarin and sulfamide compounds that were previously reported as inhibitors of human (h) metalloenzymes, carbonic anhydrases (CAs, EC 4.2.1.1). Due to the high relevance of hCA inhibitors as theragnostic agents, it is of pivotal importance to address safety issues that may arise from the initial in vivo toxicological assessment using zebrafish, a relevant model for biomedical research. None of the reported compounds showed adverse phenotypic effects or tissue damage on developing zebrafish larvae after 5 days of exposure. Our study suggests that the coumarin and sulfamide derivatives considered here are safe and suitable for further development and testing.
2020
Carbonic anhydrases; inhibitors; toxicity screening; zebrafish
01 Pubblicazione su rivista::01a Articolo in rivista
Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases / Aspatwar, A.; Berrino, E.; Bua, S.; Carta, F.; Capasso, C.; Parkkila, S.; Supuran, C. T.. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - 35:(2020), pp. 1765-1772. [10.1080/14756366.2020.1822829]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1555660
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