title: Toxocara canis: anthelmintic activity of quinone derivatives in murine toxocarosis.
abstract: Human toxocarosis is a chronic tissue parasitosis most often caused by Toxocara canis. The seroprevalence can reach up to 50%, especially among children and adolescents. The anthelmintics used in the treatment have moderate efficacy. The aim of this study was to evaluate the in vitro and in vivo anthelmintic activity of quinones and their derivatives against T. canis larvae and the cytotoxicity of the larvicidal compounds. The compounds were evaluated at 1 mg mL(-1) concentration in microculture plates containing third stage larvae in an Roswell Park Memorial Institute (RPMI) 1640 environment, incubated at 37 °C in 5% CO2 tension for 48 h. Five naphthoxiranes were selected for the cytotoxicity analysis. The cell viability evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and lactate dehydrogenase assays using murine peritoneal macrophages isolated from C57BL/6 mice revealed that the naphthoxiranes (1 and 3) were less cytotoxic at a concentration of 0.05 mg mL(-1). The efficacy of naphthoxiranes (1 and 3) was examined in murine toxocarosis also. The anthelmintic activity was examined by evaluating the number of larvae in the brain, carcass, liver, lungs, heart, kidneys and eyes. Compound (3) demonstrated anthelmintic activity similar to that of albendazole by decreasing the number of larvae in the organs of mice and thus could form the basis of the development of a new anthelmintic drug.
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: T
authors.initials: T
authors.lastname: Mata-Santos
authors.affiliation: Universidade Federal do Rio de Janeiro - Faculdade de Farmácia - Departamento de Análises Clínicas e Toxicológicas,Rio de Janeiro,Brazil.
authors.forename: H A
authors.initials: HA
authors.lastname: Mata-Santos
authors.affiliation: Universidade Federal do Rio de Janeiro - Faculdade de Farmácia - Instituto de Pesquisa de Produtos Naturais,Rio de Janeiro,Brazil.
authors.forename: P F
authors.initials: PF
authors.lastname: Carneiro
authors.affiliation: Universidade Federal do Rio de Janeiro - Faculdade de Farmácia - Instituto de Pesquisa de Produtos Naturais,Rio de Janeiro,Brazil.
authors.forename: K C G
authors.initials: KC
authors.lastname: De Moura
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: J M
authors.initials: JM
authors.lastname: Fenalti
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: G B
authors.initials: GB
authors.lastname: Klafke
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: L A X
authors.initials: LA
authors.lastname: Cruz
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: L H R
authors.initials: LH
authors.lastname: Martins
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: N F
authors.initials: NF
authors.lastname: Pinto
authors.affiliation: Universidade Federal do Rio de Janeiro - Faculdade de Farmácia - Instituto de Pesquisa de Produtos Naturais,Rio de Janeiro,Brazil.
authors.forename: M C F R
authors.initials: MC
authors.lastname: Pinto
authors.affiliation: Departamento de Microbiologia e Parasitologia,Universidade Federal de Pelotas - Instituto de Biologia,Pelotas,Brazil.
authors.forename: M E A
authors.initials: ME
authors.lastname: Berne
authors.affiliation: Universidade Federal do Rio Grande -Núcleo de Pesquisa e Microbiologia Médica - Faculdade de Medicina,Rio Grande,Brazil.
authors.forename: P E A
authors.initials: PE
authors.lastname: Da Silva
authors.affiliation: Universidade Federal do Rio Grande - Faculdade de Medicina - Área Interdisciplinar em Ciências Biomédicas - Laboratório de Parasitologia,Rio Grande,Brazil.
authors.forename: C J
authors.initials: CJ
authors.lastname: Scaini
mesh_terms: D015766:Albendazole / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000871:Anthelmintics / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D007814:Larva / Q000187:drug effects; D017737:Macrophages, Peritoneal / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D011809:Quinones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D017166:Toxocara canis / Q000187:drug effects*; D014120:Toxocariasis / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D000871:Anthelmintics; D011809:Quinones; D015766:Albendazole
keywords: Toxocariasis; chemotherapy; larvicidal; naphthoxiranes