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Article

Sulfonamide Inhibition Studies of a New β-Carbonic Anhydrase from the Pathogenic Protozoan Entamoeba histolytica

1
Sezione di Scienze Farmaceutiche e Nutraceutiche, Neurofarba Dept., Università degli Studi di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy
2
Faculty of Medicine and Health Technology, Tampere University, 33100 Tampere, Finland
3
Fimlab Ltd., Tampere University Hospital, 33100 Tampere, Finland
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2018, 19(12), 3946; https://doi.org/10.3390/ijms19123946
Received: 9 November 2018 / Revised: 27 November 2018 / Accepted: 6 December 2018 / Published: 8 December 2018
A newly described β-carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic protozoan Entamoeba histolytica, EhiCA, was recently shown to possess a significant catalytic activity for the physiologic CO2 hydration reaction (kcat of 6.7 × 105 s−1 and a kcat/Km of 8.9 × 107 M−1 s−1). A panel of sulfonamides and one sulfamate, some of which are clinically used drugs, were investigated for their inhibitory properties against EhiCA. The best inhibitors detected in the study were 4-hydroxymethyl/ethyl-benzenesulfonamide (KIs of 36–89 nM), whereas some sulfanilyl-sulfonamides showed activities in the range of 285–331 nM. Acetazolamide, methazolamide, ethoxzolamide, and dichlorophenamide were less effective inhibitors (KIs of 509–845 nM) compared to other sulfonamides investigated here. As β-CAs are not present in vertebrates, the present study may be useful for detecting lead compounds for the design of more effective inhibitors with potential to develop anti-infectives with alternative mechanisms of action. View Full-Text
Keywords: carbonic anhydrase; metalloenzymes; protozoan; Entamoeba histolytica; sulfonamides; sulfamates; inhibitor carbonic anhydrase; metalloenzymes; protozoan; Entamoeba histolytica; sulfonamides; sulfamates; inhibitor
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MDPI and ACS Style

Bua, S.; Haapanen, S.; Kuuslahti, M.; Parkkila, S.; Supuran, C.T. Sulfonamide Inhibition Studies of a New β-Carbonic Anhydrase from the Pathogenic Protozoan Entamoeba histolytica. Int. J. Mol. Sci. 2018, 19, 3946. https://doi.org/10.3390/ijms19123946

AMA Style

Bua S, Haapanen S, Kuuslahti M, Parkkila S, Supuran CT. Sulfonamide Inhibition Studies of a New β-Carbonic Anhydrase from the Pathogenic Protozoan Entamoeba histolytica. International Journal of Molecular Sciences. 2018; 19(12):3946. https://doi.org/10.3390/ijms19123946

Chicago/Turabian Style

Bua, Silvia, Susanna Haapanen, Marianne Kuuslahti, Seppo Parkkila, and Claudiu T. Supuran 2018. "Sulfonamide Inhibition Studies of a New β-Carbonic Anhydrase from the Pathogenic Protozoan Entamoeba histolytica" International Journal of Molecular Sciences 19, no. 12: 3946. https://doi.org/10.3390/ijms19123946

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