title: Evidences for leishmanicidal activity of the naphthoquinone derivative epoxy-α-lapachone.
abstract: In this work, we analyze the leishmanicidal effects of epoxy-α-lapachone on Leishmania (Viannia) braziliensis and Leishmania (Leishmania) amazonensis. Promasigotes and amastigotes (inhabiting human macrophages) from both species were assayed to verify the compound's activity over the distinct morphological stages. The incubation with epoxy-α-lapachone led to a significant decrease in the numbers of promastigotes from both species in the cultures, in a dose-and time-dependent fashion. The survival of amastigotes inhabiting human macrophages was also drastically affected by the compound, as shown by the variations in the endocytic index. Our results indicate that the epoxy-α-lapachone has an antiparasitic effect over Leishmania in both morphological stages and may potentially affect a range of species in two distinct subgenera of this parasite.
authors.affiliation: Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Av. Brasil, 4365, Maguinhos, CEP 21040-360, Rio de Janeiro, Brazil. Electronic address: fsilva@ioc.fiocruz.br.
authors.forename: Franklin
authors.initials: F
authors.lastname: Souza-Silva
authors.affiliation: Instituto de Biologia, Pós-Graduação em Ciências e Biotecnologia, Universidade Federal Fluminense, Outeiro de São João Baptista s/n - Centro, Niterói, CEP 24020-150 Rio de Janeiro, Brazil.
authors.forename: Samara Braga
authors.initials: SB
authors.lastname: do Nascimento
authors.affiliation: Instituto de Biologia, Pós-Graduação em Ciências e Biotecnologia, Universidade Federal Fluminense, Outeiro de São João Baptista s/n - Centro, Niterói, CEP 24020-150 Rio de Janeiro, Brazil.
authors.forename: Saulo Cabral
authors.initials: SC
authors.lastname: Bourguignon
authors.affiliation: Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Av. Brasil, 4365, Maguinhos, CEP 21040-360, Rio de Janeiro, Brazil.
authors.forename: Bernardo Acácio Santini
authors.initials: BA
authors.lastname: Pereira
authors.affiliation: Núcleo de Pesquisas de Produtos Naturais, Universidade Federal do Rio de Janeiro, Cidade Universitária CEP 21944-970, Rio de Janeiro, Brazil.
authors.forename: Paula Fernandes
authors.initials: PF
authors.lastname: Carneiro
authors.affiliation: Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Imunologia Clínica, Av. Brasil, 4365, Maguinhos, CEP 21040-360 Rio de Janeiro, Brazil.
authors.forename: Wellington Seguis
authors.initials: WS
authors.lastname: da Silva
authors.affiliation: Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Av. Brasil, 4365, Maguinhos, CEP 21040-360, Rio de Janeiro, Brazil.
authors.forename: Carlos Roberto
authors.initials: CR
authors.lastname: Alves
authors.affiliation: Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Imunologia Clínica, Av. Brasil, 4365, Maguinhos, CEP 21040-360 Rio de Janeiro, Brazil.
authors.forename: Rosa Teixeira
authors.initials: RT
authors.lastname: de Pinho
mesh_terms: D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007892:Leishmania braziliensis / Q000187:drug effects*; D007894:Leishmania mexicana / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D009285:Naphthoquinones / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors
chemical_list: C540757:2,2-dimethyl-3,4-dihydrospiro(benzo(g)chromene-10,2'-oxiran)-5(2H)-one; D000981:Antiprotozoal Agents; D009285:Naphthoquinones
keywords: Epoxy-α-lapachone; Leishmania (Leishmania) amazonensis; Leishmania (Viannia) braziliensis; Naphthoquinones