Antiparasitic Properties of Cardiovascular Agents against Human Intravascular Parasite Schistosoma mansoni
authors Porto, R; Mengarda, AC; Cajas, RA; Salvadori, MC; Teixeira, FS; Arcanjo, DDR; Siyadatpanah, A; Pereira, MD; Wilairatana, P; de Moraes, J
nationality International
journal PHARMACEUTICALS
author keywords antiparasitic; anthelmintic; antischistosomal; drug repurposing; amiodarone; cardiovascular agents; antiarrhythmic; schistosomiasis
keywords ANTISCHISTOSOMAL AGENTS; DRUGS; AMIODARONE; CHANNELS; RECEPTOR
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 mu M. 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.
publisher MDPI
isbn 1424-8247
year published 2021
volume 14
issue 7
digital object identifier (doi) 10.3390/ph14070686
web of science category 15
subject category Chemistry, Medicinal; Pharmacology & Pharmacy
unique article identifier WOS:000677186800001
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journal analysis (jcr 2019):
journal impact factor 4.286
5 year journal impact factor Not Available
category normalized journal impact factor percentile 82.037
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