title: Leishmanicidal activity of two canthin-6-one alkaloids, two major constituents of Zanthoxylum chiloperone var. angustifolium.
abstract: The crude alkaloidal extract of Zanthoxylum chiloperone stem bark exhibited in vitro activity against various strains of Leishmania ssp. at 100 microg/ml. Two active major constituents were isolated and identified as canthin-6-one and 5-methoxycanthin-6-one. The effect of these compounds was also tested in an in vivo assay using BALB/c mice infected with Leishmania amazonensis. The mice were treated for 5 weeks postinfection with these alkaloids by oral (14 days) or intralesional route (4 days) at 10 mg/kg daily. The reference drug, N-methylglucamine antimonate was administered by subcutaneous injections at 100 mg/kg for 10 days. Intralesional administration of canthin-6-one reduced the parasite burden but not significantly when it was compared with the untreated group, while the reference drug reduced by 91% the parasite loads in the lesion.
authors: Department of Tropical Medicine, Institute de Investigaciones en Ciencias de la Salud, Casilla de Correo 2511, Asunción, Paraguay.
authors: M E
authors: ME
authors: Ferreira
authors: A
authors: A
authors: Rojas de Arias
authors: S
authors: S
authors: Torres de Ortiz
authors: A
authors: A
authors: Inchausti
authors: H
authors: H
authors: Nakayama
authors: C
authors: C
authors: Thouvenel
authors: R
authors: R
authors: Hocquemiller
authors: A
authors: A
authors: Fournet
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D002243:Carbolines; D005260:Female; D026121:Indole Alkaloids / Q000737:chemistry / Q000627:therapeutic use*; D007211:Indoles / Q000737:chemistry / Q000627:therapeutic use*; D007891:Leishmania / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009287:Naphthyridines / Q000737:chemistry / Q000627:therapeutic use*; D008517:Phytotherapy; D028321:Plant Preparations / Q000737:chemistry / Q000627:therapeutic use; D014344:Trypanocidal Agents / Q000737:chemistry / Q000627:therapeutic use*; D032106:Zanthoxylum
chemical_list: D000470:Alkaloids; D002243:Carbolines; D026121:Indole Alkaloids; D007211:Indoles; D009287:Naphthyridines; D028321:Plant Preparations; D014344:Trypanocidal Agents; C453379:canthin-6-one; C468517:5-methoxycanthin-6-one