Ovicidal in vitro activity of 2-aryl-3-(2-morpholinoethyl)thiazolidin-4-ones and 2-aryl-3-(3-morpholinopropyl)thiazolidin-4-ones against Fasciola hepatica (Linnaeus, 1758)
Autor: | Fabiane Knepper Zehetmeyr, Maria Antonieta Machado Pereira da Silva, Wilson Cunico, Silvia de Oliveira Hübner, José Coan Campos Júnior, Daniela P. Gouvêa, Maria Elisabeth Aires Berne, Geonir M. Siqueira, Patrícia da Silva Nascente, Karine Massia Pereira |
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Rok vydání: | 2018 |
Předmět: |
0301 basic medicine
040301 veterinary sciences Immunology Tetrazolium Salts Dehydrogenase Kidney Egg hatch assay Cell Line 0403 veterinary science 03 medical and health sciences chemistry.chemical_compound Inhibitory Concentration 50 Hepatica medicine Fasciola hepatica Animals Anthelmintic Parasite Egg Count Ovum Anthelmintics biology Traditional medicine Aryl Biological activity 04 agricultural and veterinary sciences General Medicine 030108 mycology & parasitology biology.organism_classification In vitro Thiazoles Infectious Diseases chemistry Liver Thiazolidines Parasitology Cattle Brazil medicine.drug |
Zdroj: | Experimental parasitology. 192 |
ISSN: | 1090-2449 |
Popis: | Although there is a variety of biological activity reports regarding compounds derived from thiazolidin-4-ones, no data related to ovicidal activity against trematodes, particularly Fasciola hepatica are available. Since there are reports about anthelmintic resistance in F. hepatica, new drugs are required. Thus, this study evaluated ovicidal action in vitro against F. hepatica eggs in two systematic series of thiazolidin-4-ones: 2-aryl-3-(2-morpholinoethyl)thiazolidin-4-ones (1a-h) and 2-aryl-3-(3-morpholinopropyl)thiazolidin-4-ones (2a-h) at different concentrations (20, 2, 0.2, 0.02 and 0.002 μg/ml). The egg hatch assay (EHA) was used to evaluate the ovicidal action property of such compounds. In addition, potential negative effects of the compounds on metabolic activity of bovine kidney (MDBK) cells were evaluated by determining mitochondrial dehydrogenase activity. The eggs used in the EHA were obtained from parasites removed from the liver of cattle, which were discarded by slaugh after sanitary inspection. The results of EHA showed that compounds 2a-h exhibited ovicidal activity, especially compounds 2b which showed 90% ovicidal activity and viability of 93% MDBK cells at the concentration of 2 μg/ml; and 2e with 96–99% ovicidal activity at 0.2 μg/ml, 0.02 μg/ml and 0.002 μg/ml. The results show the potential of compound 2b to continue the studies in the production of new compounds with anthelmintic action. |
Databáze: | OpenAIRE |
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