Effect of antimycotic agents on the activity of aspartyl proteinases secreted by Candida albicans.
The inhibitory effect of human immunodeficiency virus (HIV) proteinase inhibitors amprenavir and saquinavir and antifungal agents terbinafine, ketoconazole, amphotericin B and ciclopiroxolamine on aspartyl proteinases (Saps) secreted by Candida albicans was tested in an in vitro spectophotometric assay. As expected, both HIV proteinase inhibitors showed a significant inhibitory effect on Sap activity, which was comparable to that of the classical aspartyl proteinase inhibitor pepstatin A (P < 0.001). Antifungal drugs such as ketoconazole, terbinafine and amphotericin B had no, or only minor, inhibitory effects on proteolytic activity. In contrast, a significant reduction in Sap activity could be demonstrated during treatment with the antifungal agent ciclopiroxolamine (P < 0.001). These results point to a multiple effect of this antimycotic agent and might explain the reduced adherence of C. albicans to human epithelial cells at subinhibitory doses.
Schaller
Martin
M
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
Krnjaic
Nikola
N
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
Niewerth
Markus
M
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
Hamm
Gerald
G
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
Hube
Bernhard
B
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
Korting
Hans C
HC
Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
D000935:Antifungal Agents / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D002176:Candida albicans / Q000187:drug effects* / Q000201:enzymology* / Q000378:metabolism; D002219:Carbamates; D002448:Cell Adhesion; D004305:Dose-Response Relationship, Drug; D005663:Furans; D017320:HIV Protease Inhibitors / Q000494:pharmacology; D019258:Saquinavir / Q000494:pharmacology; D013449:Sulfonamides / Q000494:pharmacology
D000935:Antifungal Agents; D002219:Carbamates; D005663:Furans; D017320:HIV Protease Inhibitors; D013449:Sulfonamides; C095108:amprenavir; D016282:Aspartic Acid Endopeptidases; D019258:Saquinavir