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Practical High-Throughput Method to Screen Compounds for Anthelmintic Activity against Caenorhabditis elegans .
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2021 Jul 08; Vol. 26 (14). Date of Electronic Publication: 2021 Jul 08. - Publication Year :
- 2021
-
Abstract
- In the present study, we established a practical and cost-effective high throughput screening assay, which relies on the measurement of the motility of Caenorhabditis elegans by infrared light-interference. Using this assay, we screened 14,400 small molecules from the "HitFinder" library (Maybridge), achieving a hit rate of 0.3%. We identified small molecules that reproducibly inhibited the motility of C. elegans (young adults) and assessed dose relationships for a subset of compounds. Future work will critically evaluate the potential of some of these hits as candidates for subsequent optimisation or repurposing as nematocides or nematostats. This high throughput screening assay has the advantage over many previous assays in that it is cost- and time-effective to carry out and achieves a markedly higher throughput (~10,000 compounds per week); therefore, it is suited to the screening of libraries of tens to hundreds of thousands of compounds for subsequent evaluation and development. The present phenotypic whole-worm assay should be readily adaptable to a range of socioeconomically important parasitic nematodes of humans and animals, depending on their dimensions and motility characteristics in vitro, for the discovery of new anthelmintic candidates. This focus is particularly important, given the widespread problems associated with drug resistance in many parasitic worms of livestock animals globally.
- Subjects :
- Animals
Anthelmintics isolation & purification
Anthelmintics pharmacology
Anti-Infective Agents pharmacology
Antinematodal Agents analysis
Antinematodal Agents pharmacology
Caenorhabditis elegans drug effects
Drug Resistance drug effects
Larva drug effects
Small Molecule Libraries pharmacology
Anthelmintics analysis
Drug Evaluation, Preclinical methods
High-Throughput Screening Assays methods
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 26
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 34299431
- Full Text :
- https://doi.org/10.3390/molecules26144156