Antiparasitic activity of piplartine (piperlongumine) in a mouse model of schistosomiasis

Autor(es):Mostrar menos -

Mengarda, Ana C. ^[1] ; Mendonca, Poliana S. ^[2] ; Morais, Cristiane S. ^[1] ; Cogo, Ramon M. ^[1] ; Mazloum, Susana F. ^[1] ; Salvadori, Maria C. ^[3] ; Teixeira, Fernanda S. ^[3] ; Morais, Thiago R. ^[1] ; Antar, Guilherme M. ^[4] ; Lago, Joao Henrique G. ^[2] ; Moraes, Josue ^[1]

Afiliação do(s) autor(es)

^[1] Univ Guarulhos, Nucleo Pesquisa Doencas Negligenciadas, Praca Tereza Cristina 229, BR-07023070 Guarulhos, SP - Brazil

^[2] Univ Fed ABC, Ctr Ciencias Nat & Humanas, BR-09210180 Santo Andre, SP - Brazil

^[3] Univ Sao Paulo, Inst Fis, Sao Paulo, SP - Brazil

^[4] Univ Sao Paulo, Inst Biociencias, Dept Bot, BR-05508090 Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Acta Tropica; v. 205, MAY 2020.
• Citações Web of Science: 0

Resumo

Schistosomiasis is one of the most important parasitic infections in terms of its negative effects on public health and economics. Since praziquantel is currently the only drug available to treat schistosomiasis, there is an urgent need to identify new anthelmintic agents. Piplartine, also known as piperlongumine, is a biologically active alkaloid/amide from peppers that can be detected in high amounts in the roots of Piper tuberculatum. Previously, it has been shown to have in vitro schistosomicidal effects. However, its anthelmintic activity in an animal host has not been reported. In the present work, in vivo antischistosomal properties of isolated piplartine were evaluated in a mouse model of schistosomiasis infected with either adult (patent infection) or juvenile (pre-patent infection) stages of Schistosoma mansoni. A single dose of piplartine (100, 200 or 400 mg/kg) or daily doses for five consecutive days (100 mg/kg/day) administered orally to mice infected with schistosomes resulted in a reduction in worm burden and egg production. Treatment with the highest piplartine dose (400 mg/kg) caused a significant reduction in a total worm burden of 60.4% (P < 0.001) in mice harbouring adult parasites. S. mansoni egg production, a process responsible for pathology in schistosomiasis, was also significantly inhibited by piplartine. Studies using scanning electron microscopy revealed substantial tegumental alterations in parasites recovered from mice. Since piplartine has well-characterized mechanisms of toxicity, is easily available, and is cost-effective, our results indicate that this bioactive molecule derived from medicinal plants could be a potential lead compound for novel antischistosomal agents. (AU)

• Processo FAPESP: 18/07885-1 - Biomoléculas oriundas de espécies vegetais de áreas remanescentes da Mata Atlântica e do Cerrado para tratamento de doenças tropicais negligenciadas - aspectos químicos e farmacológicos
• Beneficiário: João Henrique Ghilardi Lago
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Regular
• 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