Abstract
In the present study, we screened 502 natural product compounds against the in vitro growth of Babesia (B.) bovis. Then, the novel and potent identified compounds were further evaluated for their in vitro efficacies using viability and cytotoxicity assays. The in vivo inhibitory effects of the selected compounds were evaluated using B. microti “rodent strain” in mice model. Three potent compounds, namely, Rottlerin (RL), Narasin (NR), Lasalocid acid (LA), exhibited the lowest IC50 (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 × IC50 and 2 × IC50, respectively, while 4 × IC50 of NR was sufficient to stop the regrowth of parasite. The hematology parameters of B. microti in vivo 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 B. microti 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.
Highlights
Babesiosis is an important tick-borne disease (TBD) caused by the protozoa Babesia (B.) that infects domestic and wild animals, sometimes humans [1]
In vitro screening of 502 natural product compounds (NPCs) against the growth of B. bovis at 2.5 μg/ml concentration revealed that 14 compounds including RL, Berberine·HCl, Cepharanthine, Chartreusin, Citreoviridin, Daunorubicin, Ellagic acid, Ellipticine, Harringtonine, Lasalocid Acid (LA), Mitomycin C, Monensin, NR, and Streptonigrin exhibited over 60% inhibitory effects (Figure 1)
The results showed that RL, NR, and LA-treated B. bovis lack the ability to regrow at 1×, 2×, and 4× the IC50 values
Summary
Babesiosis is an important tick-borne disease (TBD) caused by the protozoa Babesia (B.) that infects domestic and wild animals, sometimes humans [1]. The commonly used antibabesial drugs, diminazene aceturate (DA) and imidocarb dipropionate (ID), exhibited resistance either from the treated parasites or toxic effect to the host [7,8,9], subsequently leading to discovery of safer and effective novel antibabesial compounds and becoming an urgent demand. In this regard, a non-biased screening of large libraries of compounds was recently developed to identify novel inhibitors for babesiosis [9,10,11,12]. The antiparasitic efficacy of RL, NR, and LA has been reported against the growth of Plasmodium spp., Eimeria spp., Toxoplasma gondii, and Trypanosoma spp. [16,17,18,19]
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