Institute of Parasitology, Vetsuisse Faculty, University of Berne, Berne, Switzerland.
Antimicrob Agents Chemother. 2013 Nov;57(11):5747-54. doi: 10.1128/AAC.02446-12. Epub 2013 Aug 26.
Upon the screening of 16 antiproliferative compounds against Toxoplasma gondii and Neospora caninum, two hydrolytically stable ruthenium complexes (compounds 16 and 18) exhibited 50% inhibitory concentrations of 18.7 and 41.1 nM (T. gondii) and 6.7 and 11.3 nM (N. caninum). To achieve parasiticidal activity with compound 16, long-term treatment (22 to 27 days at 80 to 160 nM) was required. Transmission electron microscopy demonstrated the rapid impact on and ultrastructural alterations in both parasites. These preliminary findings suggest that the potential of ruthenium-based compounds should thus be further exploited.
在对 16 种抗增殖化合物进行弓形体和新生隐球菌的筛选后，两种水解稳定的钌配合物（化合物 16 和 18）对弓形体和新生隐球菌的 50%抑制浓度分别为 18.7 和 41.1 nM（T. gondii）和 6.7 和 11.3 nM（N. caninum）。为了使化合物 16 具有杀寄生虫活性，需要进行长期治疗（在 80 至 160 nM 下治疗 22 至 27 天）。透射电子显微镜显示，这两种寄生虫均受到快速影响并发生超微结构改变。这些初步研究结果表明，基于钌的化合物具有进一步开发的潜力。
