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Exp Parasitol ; 100(3): 155-60, 2002 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-12173400

RESUMEN

A rodent model of malaria, Plasmodium berghei was used to assess the antimalarial potential of dinitroaniline herbicides. Trifluralin, pendimethalin, oryzalin, and benfluralin were all active against P. berghei in vitro at, or close to, submicromolar concentrations, with a rank order of potency similar to that against other protozoa. The dinitroanilines did not elicit a cytotoxic effect against a mammalian cell line at concentrations 100-fold higher than those for activity against P. berghei. Neither trifluralin nor oryzalin exhibited any antimalarial activity in vivo after oral administration at the maximum dose tolerated by the host. In a pharmacokinetic study, it was found that the lack of in vivo antimalarial activity was due to poor absorption. Other DNs which have better absorption characteristics than either trifluralin or oryzalin may offer more scope for antimalarial activity in vivo.


Asunto(s)
Malaria/tratamiento farmacológico , Plasmodium berghei/efectos de los fármacos , Sulfanilamidas , Trifluralina/farmacología , Trifluralina/uso terapéutico , Animales , Antimaláricos/farmacología , Antimaláricos/uso terapéutico , Células Cultivadas , Cloroquina/farmacología , Cloroquina/uso terapéutico , Dinitrobencenos/farmacología , Dinitrobencenos/uso terapéutico , Modelos Animales de Enfermedad , Eritrocitos/parasitología , Malaria/parasitología , Pruebas de Sensibilidad Parasitaria/métodos , Plasmodium berghei/crecimiento & desarrollo , Ratas , Ratas Endogámicas Lew
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