TY - JOUR
T1 - Evaluation of three novel azasterols against Toxoplasma gondii
AU - Martins-Duarte, Érica S.
AU - Lemgruber, L.
AU - de Souza, W.
AU - Vommaro, R.C.
AU - Lorente, S.O.
AU - Gros, L.
AU - Magaraci, F.
AU - Gilbert, I.H.
N1 - MEDLINE® is the source for the MeSH terms of this document.
PY - 2011/4/19
Y1 - 2011/4/19
N2 - Previous studies from our group have demonstrated the high susceptibility of Toxoplasma gondii tachyzoites to the sterol analogues 22,26-azasterol and 24,25-(R,S)-epiminolanosterol. In this work we present data on testing in vitro three novel azasterols as potential agents for the treatment of toxoplasmosis. The three compounds inhibited parasite growth at micromolar concentrations, in a dose-dependent manner. Electron microscopy analysis of intracellular tachyzoites after treatment with the most effective compound showed drastic mitochondrion swelling associated with the appearance of an electron-lucent matrix and disrupted cristae. Parasite lysis also took place. The appearance of electron dense cytoplasmic structures similar to amylopectin granules distributed throughout the parasite suggests that azasterols might be inducing differentiation of those tachyzoites which were not lysed to the bradyzoite stage.
AB - Previous studies from our group have demonstrated the high susceptibility of Toxoplasma gondii tachyzoites to the sterol analogues 22,26-azasterol and 24,25-(R,S)-epiminolanosterol. In this work we present data on testing in vitro three novel azasterols as potential agents for the treatment of toxoplasmosis. The three compounds inhibited parasite growth at micromolar concentrations, in a dose-dependent manner. Electron microscopy analysis of intracellular tachyzoites after treatment with the most effective compound showed drastic mitochondrion swelling associated with the appearance of an electron-lucent matrix and disrupted cristae. Parasite lysis also took place. The appearance of electron dense cytoplasmic structures similar to amylopectin granules distributed throughout the parasite suggests that azasterols might be inducing differentiation of those tachyzoites which were not lysed to the bradyzoite stage.
UR - http://www.scopus.com/inward/record.url?scp=79953163874&partnerID=8YFLogxK
U2 - 10.1016/j.vetpar.2010.11.034
DO - 10.1016/j.vetpar.2010.11.034
M3 - Article
AN - SCOPUS:79953163874
SN - 0304-4017
VL - 177
SP - 157
EP - 161
JO - Veterinary Parasitology
JF - Veterinary Parasitology
IS - 1-2
ER -