Drug repositioning: antiprotozoal activity of terfenadine against Entamoeba histolytica trophozoites

Itzia Azucena Rangel-Castañeda, Araceli Castillo-Romero, Gloria León-Ávila, Martin Zermeño-Ruiz, José Manuel Hernández-Hernández

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

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.

Original languageEnglish
Pages (from-to)303-309
Number of pages7
JournalParasitology Research
Volume121
Issue number1
DOIs
StatePublished - Jan 2022
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2021, The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.

Keywords

  • Amoebicidal activity
  • Entamoeba histolytica
  • Terfenadine
  • Virulence

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