Li Hui, Zhang Caiqing, Chen Zuozhong, Shi Wenna, Sun Shujuan
School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong Province, China.
FEMS Yeast Res. 2014 Aug;14(5):808-11. doi: 10.1111/1567-1364.12163. Epub 2014 Jun 12.
Candida krusei is intrinsically resistant to fluconazole (FLC). This study aimed to investigate whether tacrolimus (FK506) could enhance the susceptibility of FLC against C. krusei. The tested strains included the following: five isolates with minimal inhibitory concentration (MIC) of 32 μg mL(-1), two with MIC of 256 μg mL(-1), and one with MIC of 512 μg mL(-1). MICs of FK506 and FLC alone and in combination were determined by checkerboard assay, with data analyzed by fractional inhibitory concentration index model. The time-kill curves were plotted to investigate the antifungal activity at 0, 6, 12, 24, and 48 h after drug exposure. The results revealed that FK506 reduced the resistance of all isolates obviously and degree of reduction in MICs varied with susceptibilities of strains. Addition of FK506 resulted in a fourfold and 16-fold downward shift in MICs of the isolates with MICs of 32 μg mL(-1) and of ≥ 256 μg mL(-1), respectively. The synergy was further confirmed by the time-kill assay. When they were in combination against CK4/CK9 with MIC of 32/256 μg mL(-1), there was a 2.25/2.03 log10 CFU mL(-1) decrease at 24 h compared with FLC alone, respectively. In conclusion, combination of FK506 and FLC may represent a promising approach of overcoming the intrinsic resistance of C. krusei to FLC.
克柔念珠菌对氟康唑(FLC)具有固有耐药性。本研究旨在探讨他克莫司(FK506)是否能增强FLC对克柔念珠菌的敏感性。测试菌株包括:五株最小抑菌浓度(MIC)为32 μg/mL的分离株、两株MIC为256 μg/mL的分离株和一株MIC为512 μg/mL的分离株。通过棋盘法测定FK506和FLC单独及联合使用时的MIC,并采用部分抑菌浓度指数模型分析数据。绘制时间-杀菌曲线以研究药物暴露后0、6、12、24和48小时的抗真菌活性。结果显示,FK506明显降低了所有分离株的耐药性,MIC的降低程度因菌株敏感性而异。添加FK506后,MIC为32 μg/mL和≥256 μg/mL的分离株的MIC分别下降了4倍和16倍。时间-杀菌试验进一步证实了协同作用。当它们联合作用于MIC为32/256 μg/mL的CK4/CK9时,与单独使用FLC相比,24小时时分别有2.25/2.03 log10 CFU/mL的下降。总之,FK506与FLC联合使用可能是克服克柔念珠菌对FLC固有耐药性的一种有前景的方法。