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Exp Parasitol ; 127(4): 762-7, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21241694

RESUMO

Sulphobromophthalein (SBP) inhibits isolated glutathione S-transferase of the porcine nodule worm Oesophagostomum dentatum (Od-GST) and reduces larval development in vitro. In this study possible inhibitory effects of various inhibitors were evaluated in an enzymatic (CDNB) assay with isolated Od-GST and in a larval development assay (LDA). Reversibility was tested in the LDA by removing the inhibitor from culture halfway through the cultivation period. SBP, indomethacin and ethacrynic acid inhibited both enzyme activity and larval development in a dose-dependent and reversible manner. HQL-79 also reduced larval development but had only a minor effect on the isolated enzyme. The phospholipase A(2) inhibitors dexamethasone and hydrocortisone had no major effect. High thermal stability of Od-GST was demonstrated with increasing activity between 4 and 50°C. Differences between Od-GST and GST of other organisms indicate structural and possibly functional peculiarities and highlight the potential of such enzymes as targets of intervention.


Assuntos
Inibidores Enzimáticos/farmacologia , Glutationa Transferase/antagonistas & inibidores , Oesophagostomum/efeitos dos fármacos , Animais , Bioensaio , Dexametasona/farmacologia , Relação Dose-Resposta a Droga , Ácido Etacrínico/farmacologia , Feminino , Hidrocortisona/farmacologia , Indometacina/farmacologia , Concentração Inibidora 50 , Intestino Grosso/parasitologia , Oxirredutases Intramoleculares/antagonistas & inibidores , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Lipocalinas/antagonistas & inibidores , Masculino , Oesophagostomum/enzimologia , Oesophagostomum/crescimento & desenvolvimento , Piperidinas/farmacologia , Sulfobromoftaleína/farmacologia , Suínos , Temperatura
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