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Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites
The protozoan parasite Tritrichomonas foetus causes early embryonic death in cattle which results in severe economic loss. In the United States, there are no drugs are approved for treatment of this pathogen. In this study, we evaluated in vitro anti-protozoal effects of compounds from an open acces...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7326994/ https://www.ncbi.nlm.nih.gov/pubmed/32734889 http://dx.doi.org/10.1016/j.ijpddr.2020.06.003 |
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author | Martin, Katy A. Jesudoss Chelladurai, Jeba R.J. Bader, Christopher Carreiro, Elizabeth Long, Katelyn Thompson, Kylie Brewer, Matthew T. |
author_facet | Martin, Katy A. Jesudoss Chelladurai, Jeba R.J. Bader, Christopher Carreiro, Elizabeth Long, Katelyn Thompson, Kylie Brewer, Matthew T. |
author_sort | Martin, Katy A. |
collection | PubMed |
description | The protozoan parasite Tritrichomonas foetus causes early embryonic death in cattle which results in severe economic loss. In the United States, there are no drugs are approved for treatment of this pathogen. In this study, we evaluated in vitro anti-protozoal effects of compounds from an open access chemical library against T. foetus trophozoites. An initial high-throughput screen identified 16 compounds of interest. Further investigation revealed 12 compounds that inhibited parasite growth and 4 compounds with lethal effects. For lethal compounds, dose-response curves were constructed and the LD(50) was calculated for laboratory and field strains of T. foetus. Our experiments revealed chemical scaffolds that were parasiticidal in the micromolar range, and these scaffolds provide a starting point for drug discovery efforts. Further investigation is still needed to investigate suitability of these scaffolds and related compounds in food animals. Importantly, open access chemical libraries can be useful for identifying compounds with activity against protozoan pathogens of veterinary importance. |
format | Online Article Text |
id | pubmed-7326994 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-73269942020-07-06 Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites Martin, Katy A. Jesudoss Chelladurai, Jeba R.J. Bader, Christopher Carreiro, Elizabeth Long, Katelyn Thompson, Kylie Brewer, Matthew T. Int J Parasitol Drugs Drug Resist Article The protozoan parasite Tritrichomonas foetus causes early embryonic death in cattle which results in severe economic loss. In the United States, there are no drugs are approved for treatment of this pathogen. In this study, we evaluated in vitro anti-protozoal effects of compounds from an open access chemical library against T. foetus trophozoites. An initial high-throughput screen identified 16 compounds of interest. Further investigation revealed 12 compounds that inhibited parasite growth and 4 compounds with lethal effects. For lethal compounds, dose-response curves were constructed and the LD(50) was calculated for laboratory and field strains of T. foetus. Our experiments revealed chemical scaffolds that were parasiticidal in the micromolar range, and these scaffolds provide a starting point for drug discovery efforts. Further investigation is still needed to investigate suitability of these scaffolds and related compounds in food animals. Importantly, open access chemical libraries can be useful for identifying compounds with activity against protozoan pathogens of veterinary importance. Elsevier 2020-06-17 /pmc/articles/PMC7326994/ /pubmed/32734889 http://dx.doi.org/10.1016/j.ijpddr.2020.06.003 Text en © 2020 Published by Elsevier Ltd on behalf of Australian Society for Parasitology. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Article Martin, Katy A. Jesudoss Chelladurai, Jeba R.J. Bader, Christopher Carreiro, Elizabeth Long, Katelyn Thompson, Kylie Brewer, Matthew T. Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title | Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title_full | Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title_fullStr | Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title_full_unstemmed | Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title_short | Repurposing the open access malaria box reveals compounds with activity against Tritrichomonas foetus trophozoites |
title_sort | repurposing the open access malaria box reveals compounds with activity against tritrichomonas foetus trophozoites |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7326994/ https://www.ncbi.nlm.nih.gov/pubmed/32734889 http://dx.doi.org/10.1016/j.ijpddr.2020.06.003 |
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