Repurposing Terfenadine as a Novel Antigiardial Compound

Giardia lamblia is a highly infectious protozoan that causes giardiasis, a gastrointestinal disease with short-term and long-lasting symptoms. The currently available drugs for giardiasis treatment have limitations such as side effects and drug resistance, requiring the search for new antigiardial c...

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Published inPharmaceuticals (Basel, Switzerland) Vol. 16; no. 9; p. 1332
Main Authors Suárez-Rico, Daniel Osmar, Munguía-Huizar, Francisco Javier, Cortés-Zárate, Rafael, Hernández-Hernández, José Manuel, González-Pozos, Sirenia, Perez-Rangel, Armando, Castillo-Romero, Araceli
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 01.09.2023
MDPI
Subjects
Arthritis
Aspirin
Auranofin
autophagy
Cytotoxicity
Diagnosis
Dosage and administration
drug repurposing
Drug resistance
Drug therapy
Ethylenediaminetetraacetic acid
Gastrointestinal diseases
Giardia lamblia
Giardiasis
ion channels
Localization
Metronidazole
Microscopy
Morphology
Parasites
Protozoa
Scientific equipment and supplies industry
Terfenadine
Testing
Tropical diseases
tubulin
Tubulins
Mexico
United States
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Summary:Giardia lamblia is a highly infectious protozoan that causes giardiasis, a gastrointestinal disease with short-term and long-lasting symptoms. The currently available drugs for giardiasis treatment have limitations such as side effects and drug resistance, requiring the search for new antigiardial compounds. Drug repurposing has emerged as a promising strategy to expedite the drug development process. In this study, we evaluated the cytotoxic effect of terfenadine on Giardia lamblia trophozoites. Our results showed that terfenadine inhibited the growth and cell viability of Giardia trophozoites in a time–dose-dependent manner. In addition, using scanning electron microscopy, we identified morphological damage; interestingly, an increased number of protrusions on membranes and tubulin dysregulation with concomitant dysregulation of Giardia GiK were observed. Importantly, terfenadine showed low toxicity for Caco-2 cells, a human intestinal cell line. These findings highlight the potential of terfenadine as a repurposed drug for the treatment of giardiasis and warrant further investigation to elucidate its precise mechanism of action and evaluate its efficacy in future research.
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ISSN:1424-8247
1424-8247
DOI:10.3390/ph16091332