Fluorescence method for determining the mechanism and speed of action of surface-active drugs on yeast cells
Language English Country England, Great Britain Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
21231924
DOI
10.2144/000113568
PII: 000113568
Knihovny.cz E-resources
- MeSH
- Amphotericin B chemistry pharmacology MeSH
- Antifungal Agents chemistry pharmacology MeSH
- Benzalkonium Compounds chemistry pharmacology MeSH
- Sodium Dodecyl Sulfate chemistry pharmacology MeSH
- Spectrometry, Fluorescence MeSH
- Imines MeSH
- Kinetics MeSH
- Microbial Sensitivity Tests methods MeSH
- Nystatin chemistry pharmacology MeSH
- Cell Membrane Permeability drug effects MeSH
- Surface-Active Agents chemistry pharmacology MeSH
- Pyridines chemistry pharmacology MeSH
- Saccharomyces cerevisiae cytology drug effects genetics MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Amphotericin B MeSH
- Antifungal Agents MeSH
- Benzalkonium Compounds MeSH
- Sodium Dodecyl Sulfate MeSH
- Imines MeSH
- Nystatin MeSH
- octenidine MeSH Browser
- Surface-Active Agents MeSH
- Pyridines MeSH
New antifungal agents are needed to treat life-threatening fungal infections, particularly with the development of resistance. Surface-active antifungals have the advantages of minimizing host toxicity and the emergence of drug resistance. We have developed a time-dependent drug exposure assay that allows us to rapidly investigate the mechanism of surface-active antifungal drug action. The assay uses a multidrug pump-deficient strain of Saccharomyces cerevisiae and the potentiometric dye 3,3'-dipropylthiacarbocyanine iodide [diS-C₃(3)] and can assess whether cells are depolarized, hyperpolarized, or permeabilized by drug exposure. In this work, we investigated the mechanisms of action of five surface-active compounds: SDS, nystatin, amphotericin B, octenidine dihydrochloride, and benzalkonium chloride. The diS-C₃(3) time-dependent drug exposure assay can be used to identify the mechanisms of action of a wide range of drugs. It is a fast and cost-effective method for screening drugs to determine their lowest effective concentrations.
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