title: Effect of antimycotic agents on the activity of aspartyl proteinases secreted by Candida albicans.
abstract: 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.
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Martin
authors.initials: M
authors.lastname: Schaller
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Nikola
authors.initials: N
authors.lastname: Krnjaic
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Niewerth
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Gerald
authors.initials: G
authors.lastname: Hamm
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Bernhard
authors.initials: B
authors.lastname: Hube
authors.affiliation: Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.
authors.forename: Hans C
authors.initials: HC
authors.lastname: Korting
mesh_terms: 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
chemical_list: D000935:Antifungal Agents; D002219:Carbamates; D005663:Furans; D017320:HIV Protease Inhibitors; D013449:Sulfonamides; C095108:amprenavir; D016282:Aspartic Acid Endopeptidases; D019258:Saquinavir