Abstract
The opportunistic fungal pathogen, Candida albicans, causes a range of diseases in susceptible individuals. The adverse sideeffects of many of the current anti-fungal prescription drugs and the emergence of C. albicans isolates and other Candida species which are resistant to these compounds have accelerated the search for new drug candidates which have different modes of action. A family of metal chelators, which are based on the 1,10-phenanthroline core, exhibit excellent growth inhibitory effects in vitro against a number of Candida species, including clinical isolates. The compounds sequester transition metal ions, damage mitochondrial function and uncouple cell respiration. Additionally, fungal cell morphology undergoes dramatic changes and there is evidence of apoptotic cell death. Importantly, in vivo studies have confirmed that the compounds have an acceptably low toxicity profile.
Keywords: Antimicrobial, bacterial, fungal, chelate, phenanthroline
Current Medicinal Chemistry
Title:Deciphering the Antimicrobial Activity of Phenanthroline Chelators
Volume: 19 Issue: 17
Author(s): M. McCann, A. Kellett, K. Kavanagh, M. Devereux and A. L.S. Santos
Affiliation:
Keywords: Antimicrobial, bacterial, fungal, chelate, phenanthroline
Abstract: The opportunistic fungal pathogen, Candida albicans, causes a range of diseases in susceptible individuals. The adverse sideeffects of many of the current anti-fungal prescription drugs and the emergence of C. albicans isolates and other Candida species which are resistant to these compounds have accelerated the search for new drug candidates which have different modes of action. A family of metal chelators, which are based on the 1,10-phenanthroline core, exhibit excellent growth inhibitory effects in vitro against a number of Candida species, including clinical isolates. The compounds sequester transition metal ions, damage mitochondrial function and uncouple cell respiration. Additionally, fungal cell morphology undergoes dramatic changes and there is evidence of apoptotic cell death. Importantly, in vivo studies have confirmed that the compounds have an acceptably low toxicity profile.
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Cite this article as:
McCann M., Kellett A., Kavanagh K., Devereux M. and L.S. Santos A., Deciphering the Antimicrobial Activity of Phenanthroline Chelators, Current Medicinal Chemistry 2012; 19 (17) . https://dx.doi.org/10.2174/092986712800609733
DOI https://dx.doi.org/10.2174/092986712800609733 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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