Asunto(s)
Colinesterasas/metabolismo , Hicantona/farmacología , Niridazol/farmacología , Esquistosomiasis/enzimología , Tioxantenos/farmacología , Animales , Proteínas Sanguíneas/metabolismo , Colinesterasas/sangre , Femenino , Hicantona/efectos adversos , Masculino , Ratones , Niridazol/efectos adversosRESUMEN
AMMI MAJUS L., a plant belonging to the family Umbellifereae was found to possess a certain antischistosomal effect in mice infected with S. mansoni. This was proved by applying two techniques, the worm burden and the Oogram change. Bergapten, a pure furocoumarin naturally present in Ammi majus was found to have certain schistosomicidal effect.
Asunto(s)
Extractos Vegetales/uso terapéutico , Plantas Medicinales , Esquistosomicidas , Animales , Ratones , Schistosoma mansoniRESUMEN
BILHARCID inhibited malate and pyruvate oxidation. The degree of inhibition reached 50% when the concentration of Bilharcid was 10(-3) M. The mechanisms of the inhibitory action of the drug are discussed with reference to the effects of both adenine and pyridine nucleotides on the activity of the oxidoreductase enzymes.
Asunto(s)
Antimonio/metabolismo , Hígado/metabolismo , Consumo de Oxígeno , Esquistosomicidas/metabolismo , Animales , Citratos/metabolismo , Malatos/metabolismo , NAD/metabolismo , Oxidorreductasas/metabolismo , Piruvatos/metabolismo , Ratas , Especificidad por SustratoRESUMEN
IN THIS INVESTIGATION, the effects of the examined antibilharzial agents are as follows: Bilharcid and tartar-emetic similarly affected succinate oxidation. 50% inhibition could be obtained at a concentration of 10(-3) of both drugs. Malate oxidation was differently affected by the drugs. Bilharcid and tartar-emetic at a concentration of 10(-3) M induced 50% and 70% inhibition respectively, while tartar-emetic stimulated malate oxidation if added in a concentration of 10(-5) M. Pyruvate oxidation was affected in the same manner and to the same extent as malate oxidation. Citrate oxidation was slightly inhibited by Bilharcid and tartar-emetic. 10% and 30% inhibition could be obtained if the concentration was 10(-3) M of both drugs respectively. Bilharcid had a biphasic effect on citrate oxidation. Stimulation could be observed at low concentrations (up to 10(-8) M and inhibition at higher ones (up to 10(-3) M. Piperazine hexahydrate was nearly without effect on the rate of oxidation of the four mentioned substrates.
Asunto(s)
Tartrato de Antimonio y Potasio/farmacología , Antimonio/farmacología , Hígado/efectos de los fármacos , Oxidorreductasas/metabolismo , Piperazinas/farmacología , Esquistosomicidas/farmacología , Animales , Tartrato de Antimonio y Potasio/metabolismo , Ensayos Clínicos como Asunto , Hígado/enzimología , Piperazinas/metabolismo , Ratas , Esquistosomicidas/metabolismoRESUMEN
THE INHIBITION of succinate oxidation by Piperazine diantimonyl tartarate (Bilharcid) could be in part attributed to accumulation of oxaloacetate. This is discussed with reference to the effect of ATP, glutamate and cysteine on the reversal of the inhibitory action, of the drug on succinate oxidation.
Asunto(s)
Antimonio/farmacología , Hígado/metabolismo , Esquistosomicidas/farmacología , Succinato Deshidrogenasa/metabolismo , Adenosina Trifosfato/farmacología , Animales , Antimonio/metabolismo , Cisteína/farmacología , Glutamatos/farmacología , Hígado/efectos de los fármacos , Hígado/enzimología , Oxaloacetatos/metabolismo , Ratas , Esquistosomicidas/metabolismoRESUMEN
The effect of Piperazine diantimonyl tartrate (Bilharcid) as compared with that of tartar emetic on Schistosoma mansoni has been studied. In vitro experiments on living worms in tyrode/serum cultures have proved that Bilharcid 5-10 gamma/ml has the same antibilharzial activity as tartar emetic in 5-10 gamma/ml. In vivo experiments on Schistosoma mansoni infected mice have proved also that Bilharcid has more or less the same effect as that of tartar emetic. In this study, the worm burden load and the oogram techniques were used as the criteria for antibilharzial assessment.
Asunto(s)
Antimonio/farmacología , Schistosoma mansoni/efectos de los fármacos , Esquistosomiasis/tratamiento farmacológico , Animales , Antimonio/uso terapéutico , Femenino , Masculino , Ratones , Esquistosomiasis/parasitologíaRESUMEN
Bilharcid inhibited citrate oxidation and the inhibition was decreased by time. The inhibition is not restored or reduced by increasing citrate concentration. NAD stimulated citrate oxidation in the presence of Bilharcid. Cysteine slightly stimulated citrate oxidation, while ATP had no effect. Addition of citrate before Bilharcid protected the enzyme against the inhibitory action of the drug.