De Cremer Kaat, Lanckacker Ellen, Cools Tanne L, Bax Marijke, De Brucker Katrijn, Cos Paul, Cammue Bruno P A, Thevissen Karin
Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Leuven, Belgium Department of Plant Systems Biology, VIB, Ghent, Belgium.
Laboratory of Microbiology, Parasitology and Hygiene, University of Antwerp, Antwerp, Belgium.
Antimicrob Agents Chemother. 2015 Jan;59(1):421-6. doi: 10.1128/AAC.04229-14. Epub 2014 Nov 3.
Mucosal biofilm-related fungal infections are very common, and the incidence of recurrent oral and vulvovaginal candidiasis is significant. As resistance to azoles (the preferred treatment) is occurring, we aimed at identifying compounds that increase the activity of miconazole against Candida albicans biofilms. We screened 1,600 compounds of a drug-repositioning library in combination with a subinhibitory concentration of miconazole. Synergy between the best identified potentiators and miconazole was characterized by checkerboard analyses and fractional inhibitory concentration indices. Hexachlorophene, pyrvinium pamoate, and artesunate act synergistically with miconazole in affecting C. albicans biofilms. Synergy was most pronounced for artesunate and structural homologues thereof. No synergistic effect could be observed between artesunate and fluconazole, caspofungin, or amphotericin B. Our data reveal enhancement of the antibiofilm activity of miconazole by artesunate, pointing to potential combination therapy consisting of miconazole and artesunate to treat C. albicans biofilm-related infections.
黏膜生物膜相关的真菌感染非常常见,复发性口腔和外阴阴道念珠菌病的发病率很高。由于对唑类药物(首选治疗药物)的耐药性正在出现,我们旨在鉴定能增强咪康唑对白色念珠菌生物膜活性的化合物。我们将一个药物重新定位文库中的1600种化合物与亚抑菌浓度的咪康唑联合进行筛选。通过棋盘分析和部分抑菌浓度指数来表征最佳鉴定的增效剂与咪康唑之间的协同作用。六氯酚、双萘羟酸噻嘧啶和青蒿琥酯与咪康唑协同作用,影响白色念珠菌生物膜。青蒿琥酯及其结构类似物的协同作用最为明显。在青蒿琥酯与氟康唑、卡泊芬净或两性霉素B之间未观察到协同作用。我们的数据揭示了青蒿琥酯增强了咪康唑的抗生物膜活性,表明由咪康唑和青蒿琥酯组成的潜在联合疗法可用于治疗白色念珠菌生物膜相关感染。