ArticleParasites & vectors2020
H1-antihistamines as antischistosomal drugs: in vitro and in vivo studies.
Article in Parasites & vectors, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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27 citing papers in PubMed, 46 citations in OpenAlex.
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- Anthelmintic efficacy ofJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2024Article
- The 3D pharmacophore modeling to explore new antischistosomal agents among US FDA approved drugs.Future medicinal chemistry · 2024Article
- Targeting the Schistosoma mansoni nutritional mechanisms to design new antischistosomal compounds.Scientific reports · 2023Article
- Molluscicidal activity of sodium hypochlorite againstParasite epidemiology and control · 2023Article
- Evaluating the Antischistosomal Activity of Dehydrodieugenol B and Its Methyl Ether Isolated fromACS omega · 2023Article
- The Existing Drug Nifuroxazide as an Antischistosomal Agent:Microbiology spectrum · 2023Article
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
backgroundSchistosomiasis is a socioeconomically devastating parasitic infection afflicting hundreds of millions of people and animals worldwide. It is the most important helminth infection, and its treatment relies solely on the drug praziquantel. Oral H1-antihistamines are available worldwide, and these agents are among the most widely used of all medications in children and adults. Given the importance of the drug repositioning strategy, we evaluated the antischistosomal properties of the H1-antihistamine drugs commonly used in clinical practices.
methodsTwenty-one antihistamine drugs were initially screened against adult schistosomes ex vivo. Subsequently, we investigated the anthelmintic properties of these antihistamines in a murine model of schistosomiasis for both early and chronic S. mansoni infections at oral dosages of 400 mg/kg single dose or 100 mg/kg daily for five consecutive days. We also demonstrated and described the ability of three antihistamines to induce tegumental damage in schistosomes through the use of scanning electron microscopy.
resultsFrom phenotypic screening, we found that desloratadine, rupatadine, promethazine, and cinnarizine kill adult S. mansoni in vitro at low concentrations (5-15 µM). These results were further supported by scanning electron microscopy analysis. In an animal model, rupatadine and cinnarizine revealed moderate worm burden reductions in mice harboring either early or chronic S. mansoni infection. Egg production, a key mechanism for both transmission and pathogenesis, was also markedly inhibited by rupatadine and cinnarizine, and a significant reduction in hepatomegaly and splenomegaly was recorded. Although less effective, desloratadine also revealed significant activity against the adult and juvenile parasites.
conclusionsAlthough the worm burden reductions achieved are all only moderate, comparatively, treatment with any of the three antihistamines is more effective in early infection than praziquantel. On the other hand, the clinical use of H1-antihistamines for the treatment of schistosomiasis is highly unlikely.
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