ArticleParasites & vectors2022
Sensitivity of Haemonchus contortus to anthelmintics using different in vitro screening assays: a comparative study.
Article in Parasites & vectors, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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9 citing papers in PubMed, 26 citations in OpenAlex.
- Synthesis and Antiparasitic Activities of New Organometallic Derivatives of the Benzimidazole Anthelmintic Drugs.Chembiochem : a European journal of chemical biology · 2026Article
- Metabolomic and proteomic differences in susceptible and benzimidazole-resistant adult females and males of Haemonchus contortus.Veterinary research · 2025Article
- Automated larval motility assays reveal links between eprinomectin treatment failure and drug resistance in Haemonchus contortus.Veterinary research · 2025Article
- Article
- Evaluation of nematode susceptibility and resistance to anthelmintic drugs with a WMicrotracker motility assay.Scientific reports · 2025Article
- In vitro analysis of the activities of commercial anthelmintics in the presence of inhibitors of xenobiotic detoxification pathways in Haemonchus contortus exsheathed L3 stage.Parasitology research · 2025Article
- High-Throughput Screening of Five Compound Libraries for Anthelmintic Activity and Toxicity Leads to the Discovery of Two Flavonoid Compounds.International journal of molecular sciences · 2025Article
- A proteasomal β5 subunit of Haemonchus contortus with a role in the growth, development and life span.Parasites & vectors · 2023Article
- Current Landscape of Methods to Evaluate Antimicrobial Activity of Natural Extracts.Molecules (Basel, Switzerland) · 2023Review
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9 authors at 1 institution in 1 country.
Funding
Abstract
backgroundHelminthiasis and resistance to commercial anthelmintic compounds are major causes of economic losses for livestock producers, resulting in an urgent need for new drugs and reliable in vitro screening tests capable of detecting potentially active products. Considering this, a series of novel benzimidazole derivatives (5-methylbenzimidazole 1,2-disubstituted, 5-carboxybenzimidazole, 5-methylbenzimidazole 2-one) was screened on exsheathed L3 (xL3) and on the adult stage of Haemonchus contortus (Kirby anthelmintic-susceptible McMaster isolate).
methodsThis work presents the set-up of an automated motility assay on the xL3 stage of H. contortus using an infrared tracking device (WMicrotracker One) together with a larval development test (xL3 to L4) and a motility assay on the adult stage of H. contortus. A comparative study of the sensitivity of these in vitro assays using commercial anthelmintics with different mechanisms of action was carried out, also evaluating anthelmintic activity of a series of novel benzimidazole derivatives.
resultsThe automated xL3 assay had the great advantage of being able to analyze many compounds simultaneously, but it showed the limitation of having lower sensitivity, requiring higher concentrations of the commercial anthelmintics tested compared to those needed for the adult motility or development assays. Although none of the novel 1,2,5-tri-substituted benzimidazole derivatives could significantly decrease the motility of xL3s, one of them (1e) significantly affected the development of xL3s to L4, and five new compounds (1b, 1d, 1e, 2a and 2c) reduced the motility of H. contortus adult stage.
conclusionsThe analysis of the results strongly suggests that the in vitro xL3 to L4 development test, particularly for the L4 stage, could be closer to the pharmacological sensitivity of the adult stage of H. contortus (target of interest) for commercial anthelmintic selected, with different mechanisms of action, and for the series of benzimidazole derivatives assayed. Therefore, an automated motility assay on L4 using the infrared tracking device is being set up. Further studies will be conducted to evaluate the in vivo anthelmintic activity of the most active novel benzimidazole derivatives.
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