RESUMO
Perkinsus protozoan parasites have been associated with high mortality of bivalves worldwide, including Brazil. The use of antiproliferative drugs to treat the Perkinsosis is an unusual prophylactic strategy. However, because of their environment impact it could be used to control parasite proliferation in closed system, such as hatchery. This study evaluated the anti-Perkinsus activity potential of synthesized and commercial compounds. Viability of hypnospores of Perkinsus spp. was assessed in vitro. Cells were incubated with three 2-amino-thiophene (6AMD, 6CN, 5CN) and one acylhydrazone derivatives (AMZ-DCL), at the concentrations of 31.25; 62.5; 125; 250 and 500⯵M and one commercial chlorinated phenoxy phenol derivative, triclosan (2, 5, 10 and 20⯵M), for 24-48â¯h. Two synthetic molecules (6CN and AMZ-DCL) caused a significant decline (38 and 39%, respectively) in hypnospores viability, at the highest concentration (500⯵M), after 48â¯h. Triclosan was the most cytotoxic compound, causing 100% of mortality at 20⯵M after 24â¯h and at 10⯵M after 48â¯h. Cytotoxic effects of the compounds 6CN, AMZ-DCL, and triclosan were investigated by measuring parasite's zoosporulation, morphological changes and metabolic activities (esterase activity, production of reactive oxygen species and lipid content). Results showed that zoosporulation occurred in few cell. Triclosan caused changes in the morphology of hypnospores. The 6CN and AMZ-DCL did not alter the metabolic activities studied whilst Triclosan significantly increased the production of reactive oxygen species and changed the amount and distribution of lipids in the hypnospores. These results suggest that three compounds had potential to be used as antiprotozoal drugs, although further investigation of their mechanism of action must be enlightened.
Assuntos
Alveolados/efeitos dos fármacos , Antiprotozoários/farmacologia , Ostreidae/parasitologia , Alveolados/patogenicidade , Alveolados/fisiologia , Análise de Variância , Animais , Antiprotozoários/uso terapêutico , Aquicultura , Bivalves/parasitologia , Brasil , Carboxilesterase/efeitos dos fármacos , Carboxilesterase/metabolismo , Estuários , Proteínas de Fluorescência Verde , Hidrazonas/química , Hidrazonas/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Substâncias Luminescentes , Espécies Reativas de Oxigênio/metabolismo , Água do Mar , Esporos de Protozoários/efeitos dos fármacos , Tiofenos/química , Tiofenos/farmacologia , Triclosan/farmacologiaRESUMO
In the present work, we evaluate in vivo the activity of carboxylesterase of Fasciola hepatica exposed to triclabendazole. We observed a statistically significant increase in enzyme activity at 24 and 48 h post treatment (P<0.01 and P<0.001, respectively). The zymogram of cytosolic fractions identified a protein of 170 kDa containing the carboxylesterase activity. The densitograms of the zymograms confirmed the phenomenon of enzyme induction under the experimental conditions of the assay. These results provide not only the understanding of the importance of this metabolic pathway in flukes but carboxylesterase would also be an enzyme that could participate more actively in the development of anthelmintic resistance at TCBZ.