| Texto completo | |
| Autor(es): |
Castro, Thalitta
;
Teixeira, Thaina R.
;
Siegl, Mariana
;
Lopes, Flavia B.
;
Espirito-Santo, Maria Cristina C.
;
Fernandes, Joo Paulo S.
;
de Moraes, Josue
Número total de Autores: 7
|
| Tipo de documento: | Artigo Científico |
| Fonte: | SCIENTIFIC REPORTS; v. 15, n. 1, p. 8-pg., 2025-08-01. |
| Resumo | |
Schistosomiasis, a disease caused by parasitic worms, imposes a significant global health burden, affecting over 240 million people, particularly in low-income regions. To meet the Sustainable Development Goals (SDG), the World Health Organization (WHO) emphasize the need for novel antischistosomal agents. In previous work we identified that cinnarizine, a first-generation antihistamine, has promising antischistosomal activity. This study investigates the therapeutic potential of clocinizine, a chlorinated analogue of cinnarizine, against Schistosoma mansoni. Both in vitro and in vivo studies were conducted to assess its efficacy and compare it to the standard-of-care drug, praziquantel. Clocinizine exhibited potent in vitro antiparasitic activity, with an EC50 of 4.6 mu M against adult worms. In a murine model of schistosomiasis, a single oral dose of 400 mg/kg clocinizine salt significantly reduced both worm burden and egg production by 86% and 89%, respectively. These results were comparable to the efficacy of praziquantel at 400 mg/kg, which achieved a 90% reduction in worm burden and an 84% reduction in egg counts. These findings underscore the potential of clocinizine as a promising antischistosomal agent and offer valuable insights for the development of novel cinnarizine-derived compounds with improved selectivity and efficacy. (AU) | |
| Processo FAPESP: | 19/24028-8 - Aril-alquilamido-piperazinas substituídas como ligantes multialvo: síntese e avaliação da atividade em alvos relevantes para o tratamento de desordens do SNC |
| Beneficiário: | João Paulo dos Santos Fernandes |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 23/17755-6 - Síntese e avaliação de novos derivados 1,4-diaril-piperazínicos como inibidores da tirosinase |
| Beneficiário: | Mariana Aparecida Siegl Breno |
| Modalidade de apoio: | Bolsas no Brasil - Iniciação Científica |
| Processo FAPESP: | 23/08418-6 - Busca de metabólitos bioativos oriundos da biodiversidade brasileira como candidatos a fármacos para doenças causadas por helmintos |
| Beneficiário: | Josué de Moraes |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 23/03485-7 - Inibidores duais H3R/QC como alternativas para o tratamento de doenças neurodegenerativas |
| Beneficiário: | Flávia Barrio Lopes |
| Modalidade de apoio: | Bolsas no Brasil - Doutorado |