Beggs W H
Antimicrob Agents Chemother. 1984 Mar;25(3):316-8. doi: 10.1128/AAC.25.3.316.
The antifungal imidazoles miconazole and ketoconazole inhibit synthesis of essential cell membrane components. Furthermore, miconazole can exert direct physicochemical cell membrane damage at relatively high levels, but ketoconazole cannot. Experiments were designed to explain our previous observation that concentrations of miconazole capable of causing direct membrane damage were no more active against Candida albicans than equimolar levels of ketoconazole. When stationary-phase cells were inoculated into medium containing either drug at 3.8 X 10(-5) M, fungistatic effects were indistinguishable. If, however, such cultures were incubated 3 h before drug addition, differences were remarkable. After 3 h, miconazole caused a 99% reduction in CFU per milliliter within 20 min, but ketoconazole again was only fungistatic. The immediate onset, rapidity, and magnitude of the miconazole effect were indicative of direct lethal cell damage. Miconazole concentrations as low as 1.0 X 10(-5) M were similarly active. It was concluded that C. albicans undergoes phenotypic changes during the growth cycle that coincidentally confer susceptibility or resistance to the lethal direct membrane damage effect of miconazole. The fungistatic or metabolic effects of ketoconazole or low-level miconazole appeared to be independent of growth phase.
抗真菌咪唑类药物咪康唑和酮康唑可抑制细胞必需膜成分的合成。此外,咪康唑在相对高浓度时可造成直接的物理化学性细胞膜损伤,而酮康唑则不能。开展实验旨在解释我们之前的观察结果:能够造成直接膜损伤的咪康唑浓度,其抗白色念珠菌的活性并不高于等摩尔浓度的酮康唑。将稳定期细胞接种于含有3.8×10⁻⁵ M任一药物的培养基中时,抑菌效果并无差异。然而,如果在添加药物前将此类培养物孵育3小时,差异就会很显著。3小时后,咪康唑在20分钟内使每毫升菌落形成单位减少99%,但酮康唑再次仅表现出抑菌作用。咪康唑作用的迅速起效、速度和程度表明其对细胞有直接致死性损伤。低至1.0×10⁻⁵ M的咪康唑浓度也有类似活性。得出的结论是,白色念珠菌在生长周期中会发生表型变化,这恰好使其对咪康唑的致死性直接膜损伤效应产生易感性或抗性。酮康唑或低浓度咪康唑的抑菌或代谢作用似乎与生长阶段无关。