抗真菌剂对白色念珠菌分泌的天冬氨酸蛋白酶活性的影响。

Effect of antimycotic agents on the activity of aspartyl proteinases secreted by Candida albicans.

作者信息

Schaller Martin, Krnjaic Nikola, Niewerth Markus, Hamm Gerald, Hube Bernhard, Korting Hans C

机构信息

Department of Dermatology and Allergology1 and Department of Periodontology2, University of Munich, Frauenlobstr. 9-11, D-80337 München, Germany 3Robert Koch-Institut, Berlin, Germany.

出版信息

J Med Microbiol. 2003 Mar;52(Pt 3):247-249. doi: 10.1099/jmm.0.05048-0.

DOI:10.1099/jmm.0.05048-0

PMID:12621090

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.

摘要

在体外分光光度测定法中，测试了人类免疫缺陷病毒（HIV）蛋白酶抑制剂安普那韦和沙奎那韦以及抗真菌剂特比萘芬、酮康唑、两性霉素B和环吡酮胺对白色念珠菌分泌的天冬氨酸蛋白酶（Saps）的抑制作用。正如预期的那样，两种HIV蛋白酶抑制剂均对Sap活性表现出显著抑制作用，这与经典天冬氨酸蛋白酶抑制剂胃蛋白酶抑制剂A相当（P < 0.001）。酮康唑、特比萘芬和两性霉素B等抗真菌药物对蛋白水解活性没有或只有轻微抑制作用。相比之下，在用抗真菌剂环吡酮胺治疗期间，可证明Sap活性显著降低（P < 0.001）。这些结果表明这种抗真菌剂具有多种作用，并且可能解释了在亚抑制剂量下白色念珠菌对人上皮细胞的黏附减少。