Phenotypic screening of nonsteroidal anti-inflammatory drugs identified mefenamic acid as a drug for the treatment of schistosomiasis

非甾体抗炎药表型筛选确定甲芬那酸为治疗血吸虫病的药物

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作者:Eloi M Lago, Marcos P Silva, Talita G Queiroz, Susana F Mazloum, Vinícius C Rodrigues, Paulo U Carnaúba, Pedro L Pinto, Jefferson A Rocha, Leonardo L G Ferreira, Adriano D Andricopulo, Josué de Moraes

Background

Treatment and control of schistosomiasis, one of the most insidious and serious parasitic diseases, depend almost entirely on a single drug, praziquantel. Since the funding for drug development for poverty-associated diseases is very limited, drug repurposing is a promising strategy. In this study, 73 nonsteroidal anti-inflammatory drugs (NSAIDs) commonly used in medical and veterinary fields were evaluated for their anti-schistosomal properties.

Methods

The efficacy of NSAIDs was first tested against adult Schistosoma mansoni ex vivo using phenotypic screening strategy, effective drugs were further tested in a murine model of schistosomiasis. The disease parameters measured were worm and egg burden, hepato- and splenomegaly. Findings: From 73 NSAIDs, five (mefenamic acid, tolfenamic acid, meclofenamic acid, celecoxib, and diclofenac) were identified to effectively kill schistosomes. These

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