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Drug repositioning: antiprotozoal activity of terfenadine against Entamoeba histolytica trophozoites

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Abstract

The infection caused by Entamoeba histolytica is still a serious public health problem, especially in developing countries. The goal of this study was to evaluate the effect of terfenadine against Entamoeba histolytica. The trophozoites were exposed to 1, 2, 3, and 4 μM of terfenadine, for 24 and 48 h. Consequently, the viability of cells was determined by trypan blue exclusion test. The effect of terfenadine on adhesion of Entamoeba histolytica was evaluated in Caco-2 cells. In addition, the effect of terfenadine on the erythrophagocytic capacity of the parasite was investigated. The results show that terfenadine affects the growth and cell viability in a time- and dose-dependent manner. The higher inhibitory effects were observed with 4 µM at 48 h; 91.6% of growth inhibition and only 22.5% of trophozoites were viable. Additionally, we demonstrate that terfenadine is highly selective for the parasite and has low toxicity on Caco-2 cells. Furthermore, adhesion to Caco-2 cells and erythrophagocytic capacity were significantly inhibited. These findings demonstrate that terfenadine exerts significant effects on the virulence of Entamoeba histolytica. This is the first study demonstrating the amoebicidal activity of terfenadine and the results suggest it may be effective in the treatment of amoebiasis.

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Data availability

The datasets generated and/or analyzed during the current study are available from the corresponding author on reasonable request.

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Acknowledgements

Itzia Azucena Rangel-Castañeda wants to thank CONACYT for the Postdoctoral Fellowship (741102).

Funding

This research was partially supported by Consejo Estatal de Ciencia y Tecnología de Jalisco (COECYTJAL) (FODECIJAL 8129–2019).

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Contributions

All authors contributed to the study conception and design. Material preparation and the experiments were performed by IARC and MZR. IARC, ACR, and GLA performed the data analysis and interpretation. The manuscript was written by IARC, JMHH, and ACR. All authors reviewed the manuscript and Enago made the proofreading.

Corresponding author

Correspondence to José Manuel Hernández-Hernández.

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The authors declare no competing interests.

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Section Editor: Philippe Grellier

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Rangel-Castañeda, I.A., Castillo-Romero, A., León-Ávila, G. et al. Drug repositioning: antiprotozoal activity of terfenadine against Entamoeba histolytica trophozoites. Parasitol Res 121, 303–309 (2022). https://doi.org/10.1007/s00436-021-07354-x

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  • DOI: https://doi.org/10.1007/s00436-021-07354-x

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