Division of Parasitology, Kimron Veterinary Institute, Bet Dagan 50250, Israel.
Vet Parasitol. 2012 Jun 8;187(1-2):99-104. doi: 10.1016/j.vetpar.2011.12.020. Epub 2011 Dec 26.
Neosporosis caused by Neospora caninum has global economic, clinical, and epidemiological impacts, mainly in the cattle industry. Currently, there is no useful drug for treatment of neosporosis. This publication is the first to describe the significant benefits that artemisone has on Neospora infections both in vitro and in vivo. Artemisone is a new semi-synthetic 10-alkylamino artemisinin that is superior to other artemisinin derivatives in terms of its significantly higher antimalarial activity, its tolerance in vivo, lack of detectable neurotoxic potential, improved in vivo pharmacokinetics and metabolic stability. Low micromolar concentrations of artemisone inhibited in vitro Neospora development. Prophylactic and post-infection treatment profoundly reduced the number of infected cells and parasites per cell. In the in vivo gerbil model, a non-toxic dose prevented typical cerebral symptoms, in most animals. There were no signs of clinical symptoms and brain PCR was negative. Most treated gerbils produced high specific antibody titer and were protected against a challenge. Overall, artemisone could be considered as a future drug for neosporosis.
刚地弓形虫引起的刚地弓形虫病具有全球性的经济、临床和流行病学影响，主要在牛业。目前，尚无治疗刚地弓形虫病的有效药物。本出版物首次描述了青蒿琥酯在体外和体内对刚地弓形虫感染的显著益处。青蒿琥酯是一种新型半合成 10-烷氨基青蒿素，在抗疟活性、体内耐受性、无明显神经毒性潜力、改善体内药代动力学和代谢稳定性方面均优于其他青蒿素衍生物。青蒿琥酯的低微摩尔浓度抑制了体外刚地弓形虫的发育。预防和感染后治疗显著减少了感染细胞和每个细胞内寄生虫的数量。在体内沙鼠模型中，无毒剂量可预防典型的脑部症状，在大多数动物中。没有临床症状的迹象，脑部 PCR 为阴性。大多数接受治疗的沙鼠产生了高特异性抗体滴度，并受到保护免受挑战。总的来说，青蒿琥酯可以被认为是一种治疗刚地弓形虫病的未来药物。
