Spiroindolone that inhibits PfATPase4 is a potent, cidal inhibitor of Toxoplasma gondii tachyzoites in vitro and in vivo.
Antimicrob Agents Chemother
; 58(3): 1789-92, 2014.
Article
em En
| MEDLINE
| ID: mdl-24366743
ABSTRACT
Here, we show that spiroindolone, an effective treatment for plasmodia, is also active against Toxoplasma gondii tachyzoites. In vitro, spiroindolone NITD609 is cidal for tachyzoites (50% inhibitory concentration [IC50], 1µM) and not toxic to human cells at ≥10µM. Two daily oral doses of 100 mg/kg of body weight reduced the parasite burden in mice by 90% (P=0.002), measured 3 days after the last dose. This inhibition of T. gondii tachyzoites in vitro and in vivo indicates that spiroindolone is a promising lead candidate for further medicine development.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Compostos de Espiro
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Toxoplasma
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Toxoplasmose
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Coccidiostáticos
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Indóis
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article