Department of Dermatology, Peking University First Hospital, Research Center for Medical Mycology, Peking University, Beijing, People's Republic of China.
Mycopathologia. 2013 Apr;175(3-4):273-9. doi: 10.1007/s11046-012-9612-1. Epub 2013 Jan 23.
A standardized broth microdilution method was used to test the antifungal activity of geldanamycin (GA), an inhibitor of heat shock protein 90 (Hsp90), alone or in combination with the antifungal agent fluconazole (FLC) against 32 clinical isolates of Candida spp. In addition, a disk diffusion test was also used to evaluate the antifungal effect of these two drugs against Candida spp. by measuring the inhibition zone diameters. We found that the range of minimal inhibitory concentrations (MICs) for GA alone against Candida spp. was 3.2-12.8 mg/L and the geometric mean of MICs was 6.54 mg/L. In addition, the combination of GA with FLC showed synergistic effects in vitro against 2 FLC-susceptible and 6 FLC-resistant isolates of C. albicans. As for the other isolates, indifference but no antagonism was observed. In the disk diffusion assay, the diameter of inhibition zones for FLC combined with GA against FLC-resistant C. albicans isolates was 30 mm, while no inhibition was observed with FLC alone. These results demonstrate that GA possesses antifungal activity against Candida spp., and the combination of GA with FLC shows in vitro synergistic activity against some C. albicans isolates, especially those resistant to FLC.
采用标准化肉汤微量稀释法检测了格尔德霉素(GA)(一种热休克蛋白 90(Hsp90)抑制剂)单独或与抗真菌药物氟康唑(FLC)联合对 32 株临床分离的念珠菌属真菌的抗真菌活性。此外,还通过测量抑菌圈直径,采用纸片扩散法评估了这两种药物对念珠菌属真菌的抗真菌作用。结果发现,GA 单独作用于念珠菌属真菌的最小抑菌浓度(MIC)范围为 3.2-12.8 mg/L,MIC 的几何平均值为 6.54 mg/L。此外,GA 与 FLC 联合对 2 株 FLC 敏感和 6 株 FLC 耐药的白念珠菌分离株显示体外协同作用。对于其他分离株,则观察到无拮抗作用的无关现象。在纸片扩散试验中,GA 与 FLC 联合作用对白念珠菌耐药分离株的抑菌圈直径为 30 mm,而单独使用 FLC 则无抑制作用。这些结果表明,GA 对念珠菌属真菌具有抗真菌活性,GA 与 FLC 联合对某些白念珠菌分离株具有体外协同作用,尤其是对 FLC 耐药的分离株。