Journal
FUTURE MEDICINAL CHEMISTRY
Volume 13, Issue 11, Pages -Publisher
Newlands Press Ltd
DOI: 10.4155/fmc-2020-0311
Keywords
antischistosomal compound; drug repositioning; Schistosoma; schistosomiasis; tamoxifen; target fishing
Categories
Funding
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2016/22488-3]
- Coordenac ao de Aperfeicoamento de Pessoal de N'ivel Superior (CAPES)
- FAPESP [2019/25905-2, 2019/25289-0]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico
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The study demonstrated the anti-parasitic effect of tamoxifen against adult and immature schistosomes, with significant reduction in worm burden and egg production in mice. Target fishing investigation identified propionyl-CoA carboxylase as a potential target for tamoxifen in Schistosoma mansoni.
Background: Praziquantel is the only drug available to treat schistosomiasis, and there is an urgent demand for new anthelmintic agents. Methodology & results: We conducted in-depth in vitro and in vivo studies and report a target fishing investigation. In vitro, tamoxifen was active against adult and immature worms at low concentrations (<5 mu M). Tamoxifen at a single dose (400 mg/kg) or once daily for five consecutive days (100 mg/kg/day) in mice harboring either adult (patent infection) or juvenile (prepatent infection) significantly reduced worm burden (30-70%) and egg production (70-90%). Target fishing studies revealed propionyl-CoA carboxylase as a potential target for tamoxifen in Schistosoma mansoni and glucose uptake by S. mansoni was also significantly reduced. Conclusion: Our results provide news evidence of antiparasitic effect of tamoxifen and reveal propionyl-CoA carboxylase as a potential target.
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