Li Yongchang, Rizk Mohamed Abdo, Galon Eloiza May, Liu Mingming, Li Jixu, Ringo Aaron Edmond, Ji Shengwei, Zafar Iqra, Tumwebaze Maria Agnes, Benedicto Byamukama, Yokoyama Naoaki, Igarashi Ikuo, Chahan Bayin, Xuan Xuenan
National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Obihiro, Japan.
Parasitology Laboratory, Veterinary College, Xinjiang Agricultural University, Ürümqi, China.
Front Vet Sci. 2021 Nov 29;8:762107. doi: 10.3389/fvets.2021.762107. eCollection 2021.
In the present study, we screened 502 natural product compounds against the growth of (.) . Then, the novel and potent identified compounds were further evaluated for their efficacies using viability and cytotoxicity assays. The inhibitory effects of the selected compounds were evaluated using "rodent strain" in mice model. Three potent compounds, namely, Rottlerin (RL), Narasin (NR), Lasalocid acid (LA), exhibited the lowest IC (half-maximal inhibitory concentration) as follows: 5.45 ± 1.20 μM for RL, 1.86 ± 0.66 μM for NR, and 3.56 ± 1.41 μM for LA. The viability result revealed the ability of RL and LA to prevent the regrowth of treated parasite at 4 × IC and 2 × IC, respectively, while 4 × IC of NR was sufficient to stop the regrowth of parasite. The hematology parameters of were different in the NR-treated groups as compared to the infected/untreated group. Interestingly, intraperitoneal administration of NR exhibiting inhibition in the growth of in mice was similar to that observed after administration of the commonly used antibabesial drug, diminazene aceturate (DA) (76.57% for DA, 74.73% for NR). Our findings indicate the richness of natural product compounds by novel potent antibabesial candidates, and the identified potent compounds, especially NR, might be used for the treatment of animal babesiosis.
在本研究中,我们针对(.)的生长筛选了502种天然产物化合物。然后,使用活力和细胞毒性测定法对新发现的有效化合物的功效进行了进一步评估。使用小鼠模型中的“啮齿动物品系”评估了所选化合物的抑制作用。三种有效化合物,即rottlerin(RL)、那拉菌素(NR)、拉沙洛西酸(LA),表现出如下最低半数抑制浓度(IC):RL为5.45±1.20μM,NR为1.86±0.66μM,LA为3.56±1.41μM。活力结果显示,RL和LA分别能够在4倍IC和2倍IC时阻止经处理寄生虫的再生长,而4倍IC的NR足以阻止寄生虫的再生长。与感染/未处理组相比,NR处理组的(此处原文缺失相关血液学参数所对应的主体)血液学参数有所不同。有趣的是,腹腔注射NR对小鼠体内(此处原文缺失相关寄生虫名称)生长的抑制作用与常用抗巴贝斯虫药物乙酰马嗪(DA)给药后观察到的抑制作用相似(DA为76.57%,NR为74.73%)。我们的研究结果表明天然产物化合物中有丰富的新型有效抗巴贝斯虫候选物,并且所鉴定的有效化合物,尤其是NR,可能用于治疗动物巴贝斯虫病。