Academic Journal
Unpacking amphotericin B toxicity: a critical review of amphotericin B aggregation and its link to toxicity and antifungal activity.
| Τίτλος: | Unpacking amphotericin B toxicity: a critical review of amphotericin B aggregation and its link to toxicity and antifungal activity. |
|---|---|
| Συγγραφείς: | Chavali CH; School of Chemistry and Molecular Biosciences, University of Queensland, St Lucia, QLD, 4072, Australia., Deplazes E; School of Chemistry and Molecular Biosciences, University of Queensland, St Lucia, QLD, 4072, Australia. e.deplazes@uq.edu.au. |
| Πηγή: | Archives of toxicology [Arch Toxicol] 2026 Sep; Vol. 100 (9), pp. 3803-3817. Date of Electronic Publication: 2026 May 20. |
| Τύπος έκδοσης: | Journal Article; Review |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Springer-Verlag Country of Publication: Germany NLM ID: 0417615 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1432-0738 (Electronic) Linking ISSN: 03405761 NLM ISO Abbreviation: Arch Toxicol Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Berlin, New York, Springer-Verlag. |
| Ιατρικοί όροι (MeSH): | Amphotericin B*/chemistry , Amphotericin B*/toxicity , Antifungal Agents*/chemistry , Antifungal Agents*/toxicity , Antifungal Agents*/pharmacology, Hemolysis/drug effects ; Animals ; Humans |
| Περίληψη: | Amphotericin B (AmB) is a polyene antifungal that, despite its severe dose-limiting toxicity, is the most effective drug to treating invasive fungal infections. The drug's toxicity arises from its poor selectivity for ergosterol over cholesterol and its tendency to aggregate. Understanding the relationship between toxicity and aggregation is challenging due to the drug's complex mechanism of action, yet imperative to improve the safety profiles of existing and new polyene-based antifungal drugs. In this review, we critically examine and summarise studies that investigate the aggregation of AmB and its relationship to toxicity. As the aggregation behaviour of AmB is highly sensitive to environmental conditions, we provide an in-depth analysis of sample preparation, characterisation of aggregates and control experiments. While data from haemolysis, animal, and cell-based studies consistently show that oligomeric AmB is more toxic than larger aggregates, findings on the toxicity of monomeric AmB inconsistent. Our collated data underscores the need for careful consideration of sample preparation and proper use of vehicle controls when studying the complex relationship between the supramolecular organisation of AmB and its biological effects. (© 2026. The Author(s).) |
| Competing Interests: | Declarations. Conflict of interest: The authors declare that they have no conflict of interest. |
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| Contributed Indexing: | Keywords: Aggregation; Amphotericin B; Antifungal drugs; Drug formulation; Haemolysis; Polyene drugs; Toxicity |
| Substance Nomenclature: | 7XU7A7DROE (Amphotericin B) 0 (Antifungal Agents) |
| Entry Date(s): | Date Created: 20260520 Date Completed: 20260809 Latest Revision: 20260922 |
| Update Code: | 20260922 |
| PubMed Central ID: | PMC13454006 |
| DOI: | 10.1007/s00204-026-04420-0 |
| PMID: | 42159739 |
| Βάση Δεδομένων: | MEDLINE |
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