Inhibition of Trypanosoma cruzi growth in vitro by Solanum alkaloids: a comparison with ketoconazole.
The glycoalkaloids alpha-chaconine, alpha-solamargine, alpha-solanine, solasonine, sycophantine, and tomatine, as well as the aglycones demissidine, solanidine, solanocapsine, solasodine, tomatidine, and veratrine were tested as growth inhibitors of Trypanosoma cruzi, strain EP, in LIT medium. Their activity was compared with the antifungal ketoconazole. Glycoalkaloids containing alpha-chacotriose showed trypanolytic activity against the epimastigote form and trypanocidal activity against the bloodstream and metacyclic trypomastigote form of Trypanosoma cruzi in culture medium in micromolar concentrations. Ketoconazole showed a lower activity, at the same concentrations of alpha-chaconine and alpha-solamargine. The observations indicate that the initial target of the compound is at the membrane level with a concomitant change in the parasite morphology. Moreover, internal compartments of the parasites were observed to be affected by the drugs, revealing the dissolution of some organelles as mitocondrias and glycosomes.
Chataing
B
B
Departamento de Biologia, Universidad de Los Andes, Mérida, Venezuela. chataing@ciens.ula.ve
Concepción
J L
JL
Lobatón
R
R
Usubillaga
A
A
D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002240:Carbohydrate Sequence; D007654:Ketoconazole / Q000494:pharmacology*; D051379:Mice; D008969:Molecular Sequence Data; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development
D000470:Alkaloids; D007654:Ketoconazole