Leishmanicidal activity of two canthin-6-one alkaloids, two major constituents of Zanthoxylum chiloperone var. angustifolium.
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.
Ferreira
M E
ME
Department of Tropical Medicine, Institute de Investigaciones en Ciencias de la Salud, Casilla de Correo 2511, Asunción, Paraguay.
Rojas de Arias
A
A
Torres de Ortiz
S
S
Inchausti
A
A
Nakayama
H
H
Thouvenel
C
C
Hocquemiller
R
R
Fournet
A
A
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
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