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
Departamento de Microbiologia e Parasitologia, Instituto de Biologia, Universidade Federal de Pelotas, Brazil; Laboratório de Química Aplicada a Bioativos (LaQuiABio), Universidade Federal de Pelotas, Brazil.
Departamento de Microbiologia e Parasitologia, Instituto de Biologia, Universidade Federal de Pelotas, Brazil.
Exp Parasitol. 2018 Sep;192:60-64. doi: 10.1016/j.exppara.2018.07.012. Epub 2018 Jul 21.
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.
尽管有多种关于噻唑烷 - 4 - 酮衍生物的生物活性报告，但尚无针对吸虫，特别是肝片吸虫的杀卵活性数据。由于有关于肝片吸虫抗蠕虫药耐药性的报道，因此需要新药。因此，本研究评估了两个系列的噻唑烷 - 4 - 酮：2 - 芳基 - 3 -（2 - 吗啉代乙基）噻唑烷 - 4 - 酮（1a - h）和2 - 芳基 - 3 -（3 - 吗啉代丙基）噻唑烷 - 4 - 酮（2a - h）在不同浓度（20、2、0.2、0.02和0.002μg/ml）下对肝片吸虫卵的体外杀卵作用。采用虫卵孵化试验（EHA）评估此类化合物的杀卵活性。此外，通过测定线粒体脱氢酶活性评估了这些化合物对牛肾（MDBK）细胞代谢活性的潜在负面影响。EHA中使用的虫卵取自经卫生检查后屠宰废弃的牛肝脏中的寄生虫。EHA结果表明，化合物2a - h具有杀卵活性，特别是化合物2b在2μg/ml浓度下显示出90%的杀卵活性且MDBK细胞活力为93%；化合物2e在0.2μg/ml、0.02μg/ml和0.002μg/ml浓度下具有96 - 99%的杀卵活性。结果显示了化合物2b在继续开展具有驱虫作用的新化合物生产研究方面的潜力。
