In vitro evaluation of the schistosomicidal effect of the extracts, fractions and major 3-hydroxy-2, 6-dialkyl-substituted piperidine alkaloids from the flowers of Senna spectabilis (Fabaceae). Issue 17 (1st September 2016)

• Record Type: Journal Article
• Authors: de Castro, Andreísa Teixeira; Castro, Aline Pereira; Silva, Matheus Siqueira; de Souza, Isabella Maria Monteiro; Martins-Souza, Raquel Lopes; Chagas-Paula, Daniela Aparecida; Coelho, Luiz Felipe Leomil; da Silva Bolzani, Vanderlan; Pivatto, Marcos; Viegas, Claudio; Marques, Marcos José
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 17(2016)
• Page Start: 4197
• Page End: 4204
• Publication Date: 2016-09-01
• Subjects: Schistosomiasis -- Senna spectabilis -- Alkaloids -- Fluorescent probes; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.07.058
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: In this work, we present the in vitro schistosomicidal activity evaluation of the most active dichloromethane fraction (FDm) (ED50 = 83.5 μg/mL) and of a mixture of the major alkaloids ((−)-cassine/(−)-spectaline, C/E) (ED50 = 37.4 μg/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.