Effect of ferrocene-substituted porphyrin RL-91 on Candida albicans biofilm formation

Ferrocene-substituted porphyrin RL-91 exhibits antifungal activity against opportune human pathogen Candida albicans. RL-91 efficiently inhibits growth of both planktonic C. albicans cells and cells within biofilms without photoactivation. The minimal inhibitory concentration for plankton form (PMIC...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (15), p.3506-3511
Main Authors: Lippert, Rainer, Vojnovic, Sandra, Mitrovic, Aleksandra, Jux, Norbert, Ivanović-Burmazović, Ivana, Vasiljevic, Branka, Stankovic, Nada
Format: Article
Language:English
Subjects:
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Biofilms - drug effects
Candida albicans
Candida albicans - cytology
Candida albicans - drug effects
Candida albicans - growth & development
Dose-Response Relationship, Drug
Ferrous Compounds - chemistry
Ferrous Compounds - pharmacology
Metallocenes
Microbial Sensitivity Tests
Molecular Structure
Porphyrins - chemistry
Porphyrins - pharmacology
Structure-Activity Relationship
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Summary:Ferrocene-substituted porphyrin RL-91 exhibits antifungal activity against opportune human pathogen Candida albicans. RL-91 efficiently inhibits growth of both planktonic C. albicans cells and cells within biofilms without photoactivation. The minimal inhibitory concentration for plankton form (PMIC) was established to be 100 μg/mL and the same concentration killed 80% of sessile cells in the mature biofilm (SMIC80). Furthermore PMIC of RL-91 efficiently prevents C. albicans biofilm formation. RL-91 is cytotoxic for human fibroblasts in vitro in concentration of 10 μg/mL, however it does not cause hemolysis in concentrations of up to 50 μg/mL. These findings open possibility for application of RL-91 as an antifungal agent for external antibiofilm treatment of medical devices as well as a scaffold for further development of porphyrin based systemic antifungals.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.05.061