鸡毛滴虫候选新药的高通量筛选

Shengfan Jing , Qingxun Zhang , Yi Li , Han Chang , Chen Xiang , Shuyi Han , Guohui Yuan , Jinghui Fan , Hongxuan He
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引用次数: 1

摘要

鸡毛滴虫是一种原生动物寄生虫,是滴虫病的病原体,感染世界各地的圈养和野生鸟类。尽管甲硝唑几十年来一直是治疗滴虫病的首选药物,但大多数鸡毛滴虫菌株都产生了耐药性。因此,迫切需要具有新作用模式或靶点的药物。在此,我们报道了一种基于细胞的CCK-8方法的开发和应用,该方法用于高通量筛选和鉴定新的鸡毛滴虫抑制剂,作为开发新的滴虫病治疗方法的起点。我们对173种抗寄生虫化合物进行了高通量筛选,发现了16种对鸡毛滴虫潜在有效的化合物。通过测定中位抑制浓度(IC50)和中位细胞毒性浓度(CC50),我们确定了3种对鸡毛滴虫潜在安全有效的化合物:山莨菪碱、富马西林和MG132。总之,本研究成功地建立了一种化合物的高通量筛选方法,并鉴定出3种新的安全有效的抗鸡毛滴虫化合物,为滴虫病的治疗提供了新的方案。
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Identification of new drug candidates against Trichomonas gallinae using high-throughput screening

Trichomonas gallinae is a protozoan parasite that is the causative agent of trichomoniasis, and infects captive and wild bird species throughout the world. Although metronidazole has been the drug of choice against trichomoniasis for decades, most Trichomonas gallinae strains have developed resistance. Therefore, drugs with new modes of action or targets are urgently needed. Here, we report the development and application of a cell-based CCK-8 method for the high-throughput screening and identification of new inhibitors of Trichomonas gallinae as a beginning point for the development of new treatments for trichomoniasis. We performed the high-throughput screening of 173 anti-parasitic compounds, and found 16 compounds that were potentially effective against Trichomonas gallinae. By measuring the median inhibitory concentration (IC50) and median cytotoxic concentration (CC50), we identified 3 potentially safe and effective compounds against Trichomonas gallinae: anisomycin, fumagillin, and MG132. In conclusion, this research successfully established a high-throughput screening method for compounds and identified 3 new safe and effective compounds against Trichomonas gallinae, providing a new treatment scheme for trichomoniasis.

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来源期刊
CiteScore
7.90
自引率
7.50%
发文量
31
审稿时长
48 days
期刊介绍: The International Journal for Parasitology – Drugs and Drug Resistance is one of a series of specialist, open access journals launched by the International Journal for Parasitology. It publishes the results of original research in the area of anti-parasite drug identification, development and evaluation, and parasite drug resistance. The journal also covers research into natural products as anti-parasitic agents, and bioactive parasite products. Studies can be aimed at unicellular or multicellular parasites of human or veterinary importance.
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