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)

• Published in: Experimental parasitology 2018-09, Vol.192, p.60-64
• Main Authors: Zehetmeyr, Fabiane Knepper, da Silva, Maria Antonieta Machado Pereira, Pereira, Karine Massia, Berne, Maria Elisabeth Aires, Cunico, Wilson, Campos, José Coan, Gouvea, Daniela Pires, da Silva Nascente, Patrícia, de Oliveira Hübner, Silvia, Siqueira, Geonir Machado
• Format: Article
• Language: English
• Subjects: Egg hatch assay; Fasciola hepatica; Fasciolicide; Thiazolidinones
• ISSN: 0014-4894; 1090-2449
• DOI: 10.1016/j.exppara.2018.07.012

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. [Display omitted] •Egg hatch assay is used to measure the F. hepatica ovicidal activity.•The thiazolidin-4-one 2b showed the best EC50 0.01631 μg/mL.•The thiazolidin-4-one 2b shows cell viability at MDB Kidney-cells since 2 μg/ml.