Institute of Parasitology, Department of Pathobiology, University of Veterinary Medicine, Veterinärplatz 1, A-1210, Vienna, Austria.
Institute of Parasitology, Department of Pathobiology, University of Veterinary Medicine, Veterinärplatz 1, A-1210, Vienna, Austria.
Int J Parasitol Drugs Drug Resist. 2020 Dec;14:37-45. doi: 10.1016/j.ijpddr.2020.08.005. Epub 2020 Aug 21.
Bumped kinase inhibitors (BKIs) are a new class of antiprotozoal drugs that target calcium-dependent protein kinase 1 (CDPK1) in various apicomplexan parasites. A multiple dose regimen of BKI 1369 has been shown to be highly effective against Cystoisospora suis (syn. Isospora suis), the causative agent of neonatal porcine coccidiosis. However, multiple dosing may not be widely applicable in the field. The present study aimed to determine the efficacy of reduced treatment frequencies with BKI 1369 against porcine cystoisosporosis in vitro and in vivo. Pre-incubation of sporozoites with BKI 1369 completely failed to inhibit the infection in vitro unless treatment was prolonged post-infection. Notably, a single treatment of infected cell cultures 2 days post-infection (dpi) resulted in a significant reduction of merozoite replication. In an experimental infection model, treatment of suckling piglets experimentally infected with C. suis 2 and 4 dpi with 20 mg BKI 1369/kg body weight completely suppressed oocyst excretion. A single treatment on the day of infection or 2 dpi suppressed oocyst excretion in 50% and 82% of the piglets and reduced the quantitative excretion in those that shed oocysts by 95.2% and 98.4%, respectively. Moreover, a significant increase in body weight gain and reduced number of diarrhea days were observed in BKI 1369 treated piglets compared to the control piglets, irrespective of time points and frequencies of treatment. Given that reduced treatment frequencies with BKI 1369 are comparable in efficacy to repeated applications without any adverse effects, this could be considered as a practical therapeutic alternative against porcine cystoisosporosis.
bumped 激酶抑制剂 (BKIs) 是一类新型的抗寄生虫药物,靶向各种顶复门寄生虫中的钙依赖性蛋白激酶 1 (CDPK1)。BKI 1369 的多剂量方案已被证明对仔猪球虫病的病原体猪等孢球虫(原名猪等孢球虫)高度有效。然而,多次给药在野外可能并不广泛适用。本研究旨在确定 BKI 1369 减少治疗频率对体外和体内猪等孢球虫病的疗效。在体外,只有延长感染后处理,才能完全阻止孢子虫与 BKI 1369 预孵育从而抑制感染。值得注意的是,在感染后 2 天(dpi)对受感染的细胞培养物进行单次治疗可显著减少裂殖体的复制。在实验感染模型中,对 2 和 4 dpi 感染猪等孢球虫的仔猪用 20mg/kg 体重的 BKI 1369 治疗可完全抑制卵囊排泄。在感染当天或 2 dpi 进行单次治疗可使 50%和 82%的仔猪不再排出卵囊,并分别使排出卵囊的仔猪的定量排泄减少 95.2%和 98.4%。此外,与对照组仔猪相比,用 BKI 1369 治疗的仔猪体重增加显著,腹泻天数减少,无论治疗时间点和频率如何。鉴于 BKI 1369 减少治疗频率的疗效与重复应用相当,且没有任何不良反应,因此可考虑将其作为一种针对猪等孢球虫病的实用治疗替代方案。