title: Schistosoma mansoni: In vitro schistosomicidal activity of piplartine.
abstract: Schistosomiasis is one of the world's greatly neglected tropical diseases, and its control is largely dependent on a single drug, praziquantel. Here, we report the in vitro effect of piplartine, an amide isolated from Piper tuberculatum (Piperaceae), on Schistosoma mansoni adult worms. A piplartine concentration of 15.8 μM reduced the motor activity of worms and caused their death within 24h in a RPMI 1640 medium. Similarly, the highest sub-lethal concentration of piplartine (6.3 μM) caused a 75% reduction in egg production in spite of coupling. Additionally, piplartine induced morphological changes on the tegument, and a quantitative analysis carried out by confocal microscopy revealed an extensive tegumental destruction and damage in the tubercles. This damage was dose-dependent in the range of 15.8-630.2 μM. At doses higher than 157.6 μM, piplartine induced morphological changes in the oral and ventral sucker regions of the worms. It is the first time that the schistosomicidal activity has been reported for piplartine.
authors.affiliation: Laboratório de Parasitologia, Instituto Butantan, São Paulo, Brazil. josuem@usp.br
authors.forename: Josué de
authors.initials: Jd
authors.lastname: Moraes
authors.forename: Carlos
authors.initials: C
authors.lastname: Nascimento
authors.forename: Priscilla O M V
authors.initials: PO
authors.lastname: Lopes
authors.forename: Eliana
authors.initials: E
authors.lastname: Nakano
authors.forename: Lydia F
authors.initials: LF
authors.lastname: Yamaguchi
authors.forename: Massuo J
authors.initials: MJ
authors.lastname: Kato
authors.forename: Toshie
authors.initials: T
authors.lastname: Kawano
mesh_terms: D000818:Animals; D001700:Biomphalaria; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D006224:Cricetinae; D005260:Female; D008297:Male; D008647:Mesocricetus; D018613:Microscopy, Confocal; D031701:Piper / Q000737:chemistry; D010881:Piperidones / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D012550:Schistosoma mansoni / Q000187:drug effects*; D014709:Vero Cells
chemical_list: D010881:Piperidones; D010936:Plant Extracts; C498077:piperlongumine