title: Activity of epiisopiloturine against Schistosoma mansoni.
abstract: Schistosomiasis, caused by blood flukes of the genus Schistosoma, still imposes a considerable public health burden on large parts of the world. The control of this disease depends almost exclusively on the drug praziquantel, and there are no alternative drugs in sight. Natural compounds have recently attracted significant attention due to their relevance to parasitic infection and potential development into new therapeutic agents. Epiisopiloturine is an imidazole alkaloid isolated from the leaves of Pilocarpus microphyllus (Rutaceae), a native plant from Brazil. Here, we report the in vitro effect of this drug on the survival time of Schistosoma mansoni of different ages, such as 3 h old and 1, 3, 5, and 7 days old schistosomula, 49-day-old adults, and on egg output by adult worms. Epiisopiloturine at a concentration of 300 μg/mL caused the death of all schistosomula within 120 h. Extensive tegumental alterations and death were observed when adult schistosomes had been exposed to 150 μg/mL of the epiisopiloturine. At the highest sub-lethal dose of alkaloid (100 μg/mL), a 100% reduction in egg laying of paired adult worms was observed. Additionally, epiisopiloturine showed selective antischistosomal activity and exhibited no cytotoxicity to mammalian cells. This report provides the first evidence that epiisopiloturine is able to kill S. mansoni of different ages and inhibit worm egg laying.
authors.affiliation: Núcleo de Pesquisa em Biodiversidade e Biotecnologia, BIOTEC, Campus de Parnaíba, Universidade Federal do Piauí, Brazil.
authors.forename: L M
authors.initials: LM
authors.lastname: Veras
authors.forename: M A
authors.initials: MA
authors.lastname: Guimaraes
authors.forename: Y D
authors.initials: YD
authors.lastname: Campelo
authors.forename: M M
authors.initials: MM
authors.lastname: Vieira
authors.forename: C
authors.initials: C
authors.lastname: Nascimento
authors.forename: D F
authors.initials: DF
authors.lastname: Lima
authors.forename: L
authors.initials: L
authors.lastname: Vasconcelos
authors.forename: E
authors.initials: E
authors.lastname: Nakano
authors.forename: S S
authors.initials: SS
authors.lastname: Kuckelhaus
authors.forename: M C
authors.initials: MC
authors.lastname: Batista
authors.forename: J R
authors.initials: JR
authors.lastname: Leite
authors.forename: J
authors.initials: J
authors.lastname: Moraes
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D002522:Chlorocebus aethiops; D007093:Imidazoles / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D032103:Pilocarpus / Q000737:chemistry; D012098:Reproduction / Q000187:drug effects; D012550:Schistosoma mansoni / Q000187:drug effects* / Q000502:physiology; D014709:Vero Cells
chemical_list: D007093:Imidazoles; C575691:epiisopiloturine; C029899:imidazole; D015107:4-Butyrolactone