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  • Screening of a small, well-curated natural product-based library identifies two rotenoids with potent nematocidal activity against Haemonchus contortus

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    Dilrukshi HerathPUB4159.pdf (152.9Kb)
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    Author(s)
    Herath, HMP Dilrukshi
    Preston, Sarah
    Hofmann, Andreas
    Davis, Rohan A
    Koehler, Anson V
    Chang, Bill CH
    Jabbar, Abdul
    Gasser, Robin B
    Griffith University Author(s)
    Davis, Rohan A.
    Year published
    2017
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    Abstract
    The control of parasitic roundworms (nematodes) is heavily reliant on the use of a limited number of anthelmintic drugs. However, drug resistance is now very widespread and no vaccines are available, such that the discovery of new chemical entities is crucial. Within this context, we screened a library of pure natural products (n = 400) against exsheathed third-stage (xL3) larvae of the parasitic nematode Haemonchus contortus using a whole-organism screening method. We identified two plant-derived rotenoids, deguelin and rotenone, with inhibitory activity on xL3 motility. Rotenone was not investigated further, because of its ...
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    The control of parasitic roundworms (nematodes) is heavily reliant on the use of a limited number of anthelmintic drugs. However, drug resistance is now very widespread and no vaccines are available, such that the discovery of new chemical entities is crucial. Within this context, we screened a library of pure natural products (n = 400) against exsheathed third-stage (xL3) larvae of the parasitic nematode Haemonchus contortus using a whole-organism screening method. We identified two plant-derived rotenoids, deguelin and rotenone, with inhibitory activity on xL3 motility. Rotenone was not investigated further, because of its toxicity to some vertebrates. The dose response and cytotoxicity studies showed potent and selective inhibitory activity of deguelin on motility of xL3 larvae of H. contortus. Detailed future work needs to be conducted to explore the mode of action of this compound on H. contortus and related nematodes, and to assess its potential as an anthelmintic candidate.
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    Journal Title
    Veterinary Parasitology
    Volume
    244
    DOI
    https://doi.org/10.1016/j.vetpar.2017.07.005
    Copyright Statement
    © 2017 Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International Licence (http://creativecommons.org/licenses/by-nc-nd/4.0/) which permits unrestricted, non-commercial use, distribution and reproduction in any medium, providing that the work is properly cited.
    Subject
    Fisheries sciences
    Microbiology
    Veterinary parasitology
    Veterinary sciences
    Publication URI
    http://hdl.handle.net/10072/353298
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    • Journal articles

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