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首页> 外文期刊>Parasitology >In vitro effects of arylimidamides against Besnoitia besnoiti infection in Vero cells.
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In vitro effects of arylimidamides against Besnoitia besnoiti infection in Vero cells.

机译:芳基酰胺对Vero细胞中贝氏疟原虫感染的体外作用。

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摘要

The in vitro effects of 4 arylimidamides (DB811, DB786, DB750 and DB766) against the proliferative tachyzoite stage of the apicomplexan parasite Besnoitia besnoiti were investigated. These four compounds had been shown earlier to exhibit in vitro activities in the nanomolar range against the related apicomplexans Neospora caninum and Toxoplasma gondii. Real-time-PCR was used to assess B. besnoiti intracellular proliferation in vitro. Preliminary assessment by light microscopy identified DB811 and DB750 as the most promising compounds, while DB786 and DB766 were much less effective. Three-day-growth assays and quantitative real-time PCR was used for IC50 determination of DB811 (0.079 muM) and DB750 (0.56 muM). Complete growth inhibition was observed at 1.6 muM for DB 811 and 1.7 muM for DB750. However, when infected cultures were treated for 14 days, proliferation of parasites occurred again in cultures treated with DB750 from day 4 onwards, while the proliferation of DB811-treated tachyzoites remained inhibited. Electron microscopy of B. besnoiti-infected fibroblast cultures fixed and processed at different time-points following the initiation of drug treatments revealed that DB811 exerted a much higher degree of ultrastructural alterations compared to DB750. These results show that arylimidamides such as DB811 could potentially become an important addition to the anti-parasitic arsenal for food animal production, especially in cattle.
机译:研究了四种芳基酰胺(DB811,DB786,DB750和DB766)对蜂复合体寄生虫Besnoitia besnoiti的速生速殖子阶段的体外作用。较早地表明这四种化合物在纳摩尔范围内对相关的apicomplexans canineum和弓形虫具有体外活性。实时荧光定量PCR用于评估体外双歧杆菌胞内增殖。通过光学显微镜的初步评估确定DB811和DB750是最有前途的化合物,而DB786和DB766的效果要差得多。三天生长测定和定量实时PCR用于DB811(0.079μM)和DB750(0.56μM)的IC50测定。对于DB 811为1.6μM,对于DB750为1.7μM,观察到完全的生长抑制。但是,将感染的培养物处理14天后,从第4天开始,用DB750处理的培养物中再次出现了寄生虫的增殖,而经DB811处理的速殖子的增殖仍然受到抑制。在药物治疗开始后,在不同时间点固定并处理的被贝氏芽孢杆菌感染的成纤维细胞培养物的电子显微镜观察显示,与DB750相比,DB811发挥了更高程度的超微结构改变。这些结果表明,诸如DB811之类的芳基酰胺可能会成为食用动物生产(特别是在牛)中抗寄生虫阿森纳的重要添加物。

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