Literature DB >> 34358112

Antiparasitic Properties of Cardiovascular Agents against Human Intravascular Parasite Schistosoma mansoni.

Raquel Porto1, Ana C Mengarda1, Rayssa A Cajas1, Maria C Salvadori2, Fernanda S Teixeira2, Daniel D R Arcanjo3, Abolghasem Siyadatpanah4, Maria de Lourdes Pereira5, Polrat Wilairatana6, Josué de Moraes1.   

Abstract

The intravascular parasitic worm Schistosoma mansoni is a causative agent of schistosomiasis, a disease of great global public health significance. Praziquantel is the only drug available to treat schistosomiasis and there is an urgent demand for new anthelmintic agents. Adopting a phenotypic drug screening strategy, here, we evaluated the antiparasitic properties of 46 commercially available cardiovascular drugs against S. mansoni. From these screenings, we found that amiodarone, telmisartan, propafenone, methyldopa, and doxazosin affected the viability of schistosomes in vitro, with effective concentrations of 50% (EC50) and 90% (EC90) values ranging from 8 to 50 µM. These results were further supported by scanning electron microscopy analysis. Subsequently, the most effective drug (amiodarone) was further tested in a murine model of schistosomiasis for both early and chronic S. mansoni infections using a single oral dose of 400 mg/kg or 100 mg/kg daily for five consecutive days. Amiodarone had a low efficacy in chronic infection, with the worm and egg burden reduction ranging from 10 to 30%. In contrast, amiodarone caused a significant reduction in worm and egg burden in early infection (>50%). Comparatively, treatment with amiodarone is more effective in early infection than praziquantel, demonstrating the potential role of this cardiovascular drug as an antischistosomal agent.

Entities:  

Keywords:  amiodarone; anthelmintic; antiarrhythmic; antiparasitic; antischistosomal; cardiovascular agents; drug repurposing; schistosomiasis

Year:  2021        PMID: 34358112     DOI: 10.3390/ph14070686

Source DB:  PubMed          Journal:  Pharmaceuticals (Basel)        ISSN: 1424-8247


  5 in total

1.  Therapeutic Efficacy of Carvacrol-Loaded Nanoemulsion in a Mouse Model of Schistosomiasis.

Authors:  Edilaine S Xavier; Rafael L de Souza; Vinícius C Rodrigues; Camila O Melo; Daniel B Roquini; Bruna L Lemes; Polrat Wilairatana; Elquio E Oliveira; Josué de Moraes
Journal:  Front Pharmacol       Date:  2022-06-17       Impact factor: 5.988

2.  Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs.

Authors:  Daniel B Roquini; Gabriel L Silva; Leonardo L G Ferreira; Adriano D Andricopulo; Polrat Wilairatana; Josué De Moraes
Journal:  Front Pharmacol       Date:  2022-06-21       Impact factor: 5.988

3.  Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity.

Authors:  Lara Soares Aleixo de Carvalho; Vinícius Carius de Souza; Vinícius C Rodrigues; Aline Correa Ribeiro; Jorge Willian Leandro Nascimento; Priscila V S Z Capriles; Priscila de F Pinto; Josué de Moraes; Ademar Alves da Silva Filho
Journal:  Pharmaceutics       Date:  2022-05-17       Impact factor: 6.525

Review 4.  Repurposing drugs to treat cardiovascular disease in the era of precision medicine.

Authors:  Mena Abdelsayed; Eric J Kort; Stefan Jovinge; Mark Mercola
Journal:  Nat Rev Cardiol       Date:  2022-05-23       Impact factor: 49.421

5.  Pyrazoline derivatives as promising novel antischistosomal agents.

Authors:  Cristiane S Morais; Ana C Mengarda; Fábio B Miguel; Karine B Enes; Vinícius C Rodrigues; Maria Cristina C Espírito-Santo; Abolghasem Siyadatpanah; Polrat Wilairatana; Mara R C Couri; Josué de Moraes
Journal:  Sci Rep       Date:  2021-12-06       Impact factor: 4.379

  5 in total

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