ArticleInternational journal for parasitology. Drugs and drug resistance2015
Buparvaquone is active against Neospora caninum in vitro and in experimentally infected mice.
Article in International journal for parasitology. Drugs and drug resistance, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 48 citations in OpenAlex.
- Article
- Molecular investigation of Neospora caninum in cattle in the Khomas region of Namibia.The Onderstepoort journal of veterinary research · 2025Article
- Article
- Enhanced Anti-Babesia Efficacy of Buparvaquone and Imidocarb When Combined with ELQ-316 In Vitro Culture ofPharmaceuticals (Basel, Switzerland) · 2025Article
- The Combination of Buparvaquone and ELQ316 Exhibit a Stronger Effect than ELQ316 and Imidocarb AgainstPharmaceutics · 2024Article
- Molecular Targets of the 5-Amido-Carboxamide Bumped Kinase Inhibitor BKI-1748 inInternational journal of molecular sciences · 2024Article
- Synthesis and Antiparasitic Activity of New Trithiolato-Bridged Dinuclear Ruthenium(II)-arene-carbohydrate Conjugates.Molecules (Basel, Switzerland) · 2023Article
- New Nucleic Base-Tethered Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Compounds: Synthesis and Antiparasitic Activity.Molecules (Basel, Switzerland) · 2022Article
- Conjugates Containing Two and Three Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Units as In Vitro Antiparasitic and Anticancer Agents.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Coumarin-Tagged Dinuclear Trithiolato-Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity.Chembiochem : a European journal of chemical biology · 2020Article
- In Vitro Activities of MMV Malaria Box Compounds against the Apicomplexan ParasiteMolecules (Basel, Switzerland) · 2020Article
- Discovery of New Inhibitors of Toxoplasma gondii via the Pathogen Box.Antimicrobial agents and chemotherapy · 2018Article
- Endochin-Like Quinolones Exhibit Promising Efficacy AgainstFrontiers in veterinary science · 2018Article
- Treatment of Toxoplasmosis and Neosporosis in Farm Ruminants: State of Knowledge and Future Trends.Current topics in medicinal chemistry · 2018Review
- Characterization of the Activities of Dinuclear Thiolato-Bridged Arene Ruthenium Complexes against Toxoplasma gondii.Antimicrobial agents and chemotherapy · 2017Article
- Development of a murine vertical transmission model for Toxoplasma gondii oocyst infection and studies on the efficacy of bumped kinase inhibitor (BKI)-1294 and the naphthoquinone buparvaquone against congenital toxoplasmosis.The Journal of antimicrobial chemotherapy · 2017Article
- Two Novel Calcium-Dependent Protein Kinase 1 Inhibitors Interfere with Vertical Transmission in Mice Infected with Neospora caninum Tachyzoites.Antimicrobial agents and chemotherapy · 2017Article
- Efficacy, safety and tolerance of imidocarb dipropionate versus atovaquone or buparvaquone plus azithromycin used to treat sick dogs naturally infected with the Babesia microti-like piroplasm.Parasites & vectors · 2017Article
- Drug target identification in protozoan parasites.Expert opinion on drug discovery · 2016Review
- In Vitro Screening of the Open-Source Medicines for Malaria Venture Malaria Box Reveals Novel Compounds with Profound Activities against Theileria annulata Schizonts.Antimicrobial agents and chemotherapy · 2016Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The naphthoquinone buparvaquone is currently the only drug used against theileriosis. Here, the effects of buparvaquone were investigated in vitro and in an experimental mouse model for Neospora caninum infection. In 4-day proliferation assays, buparvaquone efficiently inhibited N. caninum tachyzoite replication (IC50 = 4.9 nM; IC100 = 100 nM). However, in the long term tachyzoites adapted and resumed proliferation in the presence of 100 nM buparvaquone after 20 days of cultivation. Parasiticidal activity was noted after 9 days of culture in 0.5 µM or 6 days in 1 µM buparvaquone. TEM of N. caninum infected fibroblasts treated with 1 µM buparvaquone showed that the drug acted rather slowly, and ultrastructural changes were evident only after 3-5 days of treatment, including severe alterations in the parasite cytoplasm, changes in the composition of the parasitophorous vacuole matrix and a diminished integrity of the vacuole membrane. Treatment of N. caninum infected mice with buparvaquone (100 mg/kg) either by intraperitoneal injection or gavage prevented neosporosis symptoms in 4 out of 6 mice in the intraperitoneally treated group, and in 6 out of 7 mice in the group receiving oral treatment. In the corresponding controls, all 6 mice injected intraperitoneally with corn oil alone died of acute neosporosis, and 4 out of 6 mice died in the orally treated control group. Assessment of infection intensities in the treatment groups showed that, compared to the drug treated groups, the controls showed a significantly higher parasite load in the lungs while cerebral parasite load was higher in the buparvaquone-treated groups. Thus, although buparvaquone did not eliminate the parasites infecting the CNS, the drug represents an interesting lead with the potential to eliminate, or at least diminish, fetal infection during pregnancy.
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