Efficacy of carvacryl acetate in vitro and following oral administration to mice harboring either prepatent or patent Schistosoma mansoni infections

Autor(es)

Silva, Bianca C. ^[1] ; Mengarda, Ana C. ^[1] ; Rodrigues, Vinicius C. ^[1] ; Cajas, Rayssa A. ^[1] ; Carnauba, Paulo U. ^[1] ; Espirito-Santo, Maria Cristina C. ^{[2, 3]} ; Bezerra-Filho, Carlos S. M. ^[4] ; de Sousa, Damiao P. ^[4] ; de Moraes, Josue ^[1]

Afiliação do(s) autor(es)

^[1] Univ Guarulhos, Nucleo Pesquisa Doencas Negligenciadas, R Eng Prestes Maia 88, BR-07023070 Guarulhos, SP - Brazil

^[2] Univ Sao Paulo, Fac Med, Dept Molestias Infecciosas & Parasitarias, Lab Imunopatol Esquistossomose LIM06, Sao Paulo, SP - Brazil

^[3] Univ Sao Paulo, Inst Med Trop Sao Paulo, Lab Helmintol, Sao Paulo, SP - Brazil

^[4] Univ Fed Paraiba, Dept Ciencias Farmaceut, Joao Pessoa, PB - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Parasitology Research; v. 120, n. 11 OCT 2021.
• Citações Web of Science: 0

Resumo

Schistosomiasis is a major public health problem that afflicts more than 240 million individuals globally, particularly in poor communities. Treatment of schistosomiasis relies heavily on a single oral drug, praziquantel, and there is interest in the search for new antischistosomal drugs. This study reports the anthelmintic evaluation of carvacryl acetate, a derivative of the terpene carvacrol, against Schistosoma mansoni ex vivo and in a schistosomiasis animal model harboring either adult (patent infection) or juvenile (prepatent infection) parasites. For comparison, data obtained with gold standard antischistosomal drug praziquantel are also presented. Initially in vitro effective concentrations of 50% (EC50) and 90% (EC90) were determined against larval and adult stages of S. mansoni. In an animal with patent infection, a single oral dose of carvacryl acetate (100, 200, or 400 mg/kg) caused a significant reduction in worm burden (30-40%). S. mansoni egg production, a process responsible for both life cycle and pathogenesis, was also markedly reduced (70-80%). Similar to praziquantel, carvacryl acetate 400 mg/kg had low efficacy in pre-patent infection. In tandem, although carvacryl acetate had interesting in vitro schistosomicidal activity, the compound exhibited low efficacy in terms of reduction of worm load in S. mansoni-infected mice. (AU)

• Processo FAPESP: 19/25905-2 - Avaliação pré-clínica para administração oral de formulações nanoestruturadas contendo fármacos com atividade anti-helmíntica
• Beneficiário: Ana Carolina Araujo Mengarda
• Modalidade de apoio: Bolsas no Brasil - Doutorado
• Processo FAPESP: 16/22488-3 - Reposicionamento de fármacos para doenças negligenciadas: identificação de novos agentes anti-helmínticos
• Beneficiário: Josué de Moraes
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 19/25289-0 - Atividade anti-helmíntica in vitro do praziquantel e ácido mefenâmico nanocarreados
• Beneficiário: Vinícius de Castro Rodrigues
• Modalidade de apoio: Bolsas no Brasil - Iniciação Científica