| Literature DB >> 27491706 |
Andreísa Teixeira de Castro1, Aline Pereira Castro1, Matheus Siqueira Silva1, Isabella Maria Monteiro de Souza1, Raquel Lopes Martins-Souza1, Daniela Aparecida Chagas-Paula1, Luiz Felipe Leomil Coelho1, Vanderlan da Silva Bolzani2, Marcos Pivatto3, Claudio Viegas1, Marcos José Marques4.
Abstract
In this work, we present the in vitro schistosomicidal activity evaluation of the most active dichloromethane fraction (FDm) (ED50=83.5μg/mL) and of a mixture of the major alkaloids ((-)-cassine/(-)-spectaline, C/E) (ED50=37.4μg/mL) from the flowers of Senna spectabilis against adult worms and cercariae. We also demonstrate other toxic effects including paralysis of the adult worms, inhibition of the secretory activity, tegument lesions and cercaricidal activity. In the association test of Praziquantel (PZQ)-C/E, we observed up to 80% mortality of Schistosoma mansoni in comparison to PZQ monotherapy. Due to the diversity of the toxic effects, the schistosomicidal activity of C/E is likely a result of a multitarget mechanism involving the tegument, secretory system and neuromotor action.Entities:
Keywords: Alkaloids; Fluorescent probes; Schistosomiasis; Senna spectabilis
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Year: 2016 PMID: 27491706 DOI: 10.1016/j.bmcl.2016.07.058
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823