AI Article Synopsis
- Comparative studies were conducted on the effectiveness and toxicity of amphotericin B (AmB) and its derivatives against the standard yeast Saccharomyces cerevisiae and its genetically modified versions that have multidrug resistance (MDR) pumps from Candida albicans.
- The AmB derivatives were found to be both fungistatic and fungicidal, using a mechanism that disrupts the fungal cell membrane.
- The research suggests that AmB and its derivatives are able to bypass fungal MDR because their large molecular sizes do not make them targets for the multidrug export pumps.
Article Abstract
Comparative studies were performed to determine the activity and cytotoxicity of amphotericin B (AmB) and its derivatives on standard strain of Saccharomyces cerevisiae and its transformants with cloned genes from Candida albicans encoding multidrug resistance (MDR) pumps of ATP-binding cassette and major facilitator superfamilies. The AmB derivatives: amphotericin B 3-dimethylaminopropyl amide and N-methyl-N-D-fructopyranosylamphotericin B methyl ester were shown to be fungistatic and fungicidal towards MDR strains, by membrane permeabilization mechanism. Antibiotic-cell interaction monitored by energy transfer method indicates similar membrane affinity in parent strain and its MDR transformants. Experiments with fungal cells loaded with rhodamine 6G point to lack of competition between this dye and AmB and its derivatives for efflux driven by CDR2p. It can be thus assumed that AmB and its derivatives overcome fungal MDR by not being substrates of the multidrug exporting pumps, presumably due to their large molecular volumes.
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| http://dx.doi.org/10.1038/ja.2007.56 | DOI Listing |
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