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Discovery and Characterization of a Peptoid with Antifungal Activity against Cryptococcus neoformans
Ashley E Corson1, Scott A Armstrong1, Matthew E Wright1
1Department of Chemistry and Department of Biology, Middle Tennessee State University , 1301 East Main Street, Murfreesboro, Tennessee 37132, United States.
Abstract:
Studies show there is an increasing rate of fungal infections, especially in immunocompromised patients and treatments for fungal genera, such as Aspergillus, Candida, and Cryptococcus, carry significant cytotoxicity with an increasing prevalence of antifungal resistance. We have previously reported a high-throughput assay for identifying peptoids with antimicrobial properties from combinatorial libraries. Here we report the application of this assay in identifying a peptoid with antifungal properties against Cryptococcus neoformans. Termed AEC5, this peptoid has comparable potency to existing clinical antifungal agents, excellent stability, and minimal cytotoxicity in mammalian cells.
Insights
Researchers identified a new peptoid, AEC5, effective against Cryptococcus neoformans fungal infections. This compound shows potent antifungal activity with low toxicity, offering a promising alternative to current treatments.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Mycology
Background:
- Increasing incidence of fungal infections, particularly in immunocompromised individuals.
- Existing antifungal treatments for genera like Aspergillus, Candida, and Cryptococcus exhibit significant cytotoxicity and rising antifungal resistance.
Purpose of the Study:
- To apply a previously developed high-throughput assay for identifying novel antimicrobial peptoids.
- To identify a peptoid with potent antifungal properties against Cryptococcus neoformans.
Main Methods:
- Utilized a high-throughput screening assay to evaluate peptoids from combinatorial libraries.
- Tested the identified peptoid for antifungal activity against Cryptococcus neoformans.
- Assessed the peptoid's potency, stability, and cytotoxicity in mammalian cells.
Main Results:
- Successfully identified a peptoid, designated AEC5, with significant antifungal properties.
- AEC5 demonstrated comparable potency to existing clinical antifungal agents.
- The peptoid exhibited excellent stability and minimal cytotoxicity in mammalian cell assays.
Conclusions:
- AEC5 is a promising novel antifungal agent effective against Cryptococcus neoformans.
- The identified peptoid offers a potentially safer and effective alternative to current antifungal therapies.
- The high-throughput assay is a valuable tool for discovering new antimicrobial agents.
