title: An effective diaryl derivative against Leishmania amazonensis and its influence on the parasite X macrophage interaction.
abstract: The activity of several diarylheptanoid derivatives (curcuminoids) was previously evaluated against Leishmania amazonensis promastigotes and among them the most active compound was 5-hydroxy-7- (4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl)-1,4,6-heptatrien-3-one. This study was carried out to investigate the influence of this diaryl derivative on the infective promastigotes and Balb/c mice peritoneal macrophage interaction. The potential in vitro toxicity was also evaluated. Promastigotes pretreated for 24 hours with the compound had their infective capacity significantly decreased. When the infection of Balb/c macrophage by L. amazonensis promastigotes was already installed, addition of the drug resulted in a diminishing of the infection rate. It was demonstrated that the compound was not toxic to the host macrophage in a concentration equivalent to the LD50/24h from the previous in vitro experiment.
authors.affiliation: Department of Immunology, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro, Brazil.
authors.forename: Luciana V
authors.initials: LV
authors.lastname: Alves
authors.forename: Léa
authors.initials: L
authors.lastname: Cysne-Finkelstein
authors.forename: Rosane M
authors.initials: RM
authors.lastname: Temporal
authors.forename: Marcelo S
authors.initials: MS
authors.lastname: Genestra
authors.forename: Leonor L
authors.initials: LL
authors.lastname: Leon
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D036381:Diarylheptanoids / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006790:Host-Parasite Interactions / Q000187:drug effects; D007894:Leishmania mexicana / Q000187:drug effects* / Q000254:growth & development; D007896:Leishmaniasis / Q000469:parasitology; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology / Q000502:physiology*; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests
chemical_list: D000981:Antiprotozoal Agents; D036381:Diarylheptanoids