title: ANTHELMINTIC ACTIVITY OF LAPACHOL, β-LAPACHONE AND ITS DERIVATIVES AGAINST Toxocara canis LARVAE.
abstract: Anthelmintics used for intestinal helminthiasis treatment are generally effective; however, their effectiveness in tissue parasitosis (i.e. visceral toxocariasis) is moderate. The aim of this study was to evaluate the in vitro activity of lapachol, β-lapachone and phenazines in relation to the viability of Toxocara canis larvae. A concentration of 2 mg/mL (in duplicate) of the compounds was tested using microculture plates containing Toxocara canis larvae in an RPMI-1640 environment, incubated at 37 °C in 5% CO2 tension for 48 hours. In the 2 mg/mL concentration, four phenazines, lapachol and three of its derivatives presented a larvicide/larvistatic activity of 100%. Then, the minimum larvicide/larvistatic concentration (MLC) test was conducted. The compounds that presented the best results were nor-lapachol (MLC, 1 mg/mL), lapachol (MLC 0.5 mg/mL), β-lapachone, and β-C-allyl-lawsone (MLC, 0.25 mg/mL). The larvae exposed to the compounds, at best MLC with 100% in vitro activity larvicide, were inoculated into healthy BALB/c mice and were not capable of causing infection, confirming the larvicide potential in vitro of these compounds.
authors.affiliation: Laboratório de Parasitologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Taís
authors.initials: T
authors.lastname: Mata-Santos
authors.affiliation: Laboratório de Parasitologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Nitza França
authors.initials: NF
authors.lastname: Pinto
authors.affiliation: Departamento de Análises Clínicas e Toxicológicas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Hilton Antônio
authors.initials: HA
authors.lastname: Mata-Santos
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Kelly Gallan
authors.initials: KG
authors.lastname: De Moura
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Paula Fernandes
authors.initials: PF
authors.lastname: Carneiro
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Tatiane Dos Santos
authors.initials: Tdos S
authors.lastname: Carvalho
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Karina Pena
authors.initials: KP
authors.lastname: Del Rio
authors.affiliation: Núcleo de Pesquisa de Produtos Naturais, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Maria do Carmo Freire Ribeiro
authors.initials: Mdo C
authors.lastname: Pinto
authors.affiliation: Laboratório de Parasitologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Lourdes Rodrigues
authors.initials: LR
authors.lastname: Martins
authors.affiliation: Laboratório de Parasitologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Juliana Montelli
authors.initials: JM
authors.lastname: Fenalti
authors.affiliation: Laboratório de Micobactérias, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Pedro Eduardo Almeida
authors.initials: PE
authors.lastname: Da Silva
authors.affiliation: Laboratório de Parasitologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
authors.forename: Carlos James
authors.initials: CJ
authors.lastname: Scaini
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D005260:Female; D007814:Larva / Q000187:drug effects / Q000254:growth & development; D051379:Mice; D008807:Mice, Inbred BALB C; D009285:Naphthoquinones / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D017166:Toxocara canis / Q000187:drug effects*
chemical_list: D000871:Anthelmintics; D009285:Naphthoquinones; C014638:beta-lapachone; C008252:lapachol