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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：芳基酰胺酰亚胺含量对VERO细胞的影响。

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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4种芳酰亚胺（DB811、DB786、DB750和DB766）对尖复性寄生虫Besnoitia besnoiti增殖速殖子期的体外作用。这四种化合物在体外对相关的犬新孢子虫和弓形虫具有纳摩尔范围内的活性。实时荧光定量PCR检测贝氏双歧杆菌在体外的细胞内增殖情况。通过光学显微镜进行的初步评估确定DB811和DB750是最有希望的化合物，而DB786和DB766的效果要差得多。三天生长试验和定量实时PCR用于DB811（0.079 muM）和DB750（0.56 muM）的IC50测定。DB811和DB750分别在1.6mum和1.7mum时观察到完全生长抑制。然而，当感染的培养物被处理14天时，从第4天开始，用DB750处理的培养物中再次出现寄生虫的增殖，而用DB811处理的速殖子的增殖仍然受到抑制。在药物治疗开始后的不同时间点固定和处理的贝氏杆菌感染的成纤维细胞培养物的电子显微镜显示，与DB750相比，DB811产生了更高程度的超微结构改变。这些结果表明，像DB811这样的芳酰亚胺可能成为食用动物生产中抗寄生虫武器库的重要补充，尤其是在牛身上。

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