The rapidly developing resistance of fungi to antifungal drugs is a serious health problem. Today's drugs mainly target cell membrane composition and synthesis. Moreover, some of them have serious side effects. New antifungal drugs targeting different molecular pathways are necessary. Amiodarone, an FDA approved antiarrhythmic drug displays antifungal activity. It targets calcium and pH homeostasis. In concentrations above 25 μM, it inhibits the growth of the filamentous fungi Aspergillus niger. It triggers a biphasic calcium response accompanied by a high [Ca(2+)](c) resting level and an intracellular acidification from 7.5 to 6.0, both of which are concentration dependent. Both extracellular calcium and calcium from intracellular organelles are sources of the transient second cytosolic calcium peak, whose amplitude is 0.12 μM for cells treated with 0.1mM amiodarone. In P-type ATPase deficient A. niger strains pmrAΔ and pmcAΔ, the [Ca(2+)](c) resting level after amiodarone treatment is at least twice as high as that of the wild type, which correlates with fungal viability and hypersensitivity to amiodarone. A combination of amiodarone and amphotericin B is additive in terms of cell viability and cytosolic calcium influx. In contrast, a combination of azole drugs and amiodarone has a synergistic effect on the viability of fungi.

译文

真菌对抗真菌药物的耐药性迅速发展,是一个严重的健康问题。当今的药物主要是靶向细胞膜的组成和合成。此外,其中一些有严重的副作用。针对不同分子途径的新型抗真菌药物是必要的。胺碘酮是FDA批准的抗心律失常药物,具有抗真菌活性。它的目标是钙和pH稳态。在25μm以上的浓度下,它会抑制丝状真菌黑曲霉的生长。它触发双相钙反应,伴随着高 [Ca(2)](c) 静息水平和从7.5到6.0的细胞内酸化,两者均取决于浓度。细胞外钙和来自细胞内细胞器的钙都是瞬时第二个胞质钙峰的来源,对于用0.1毫米胺碘酮处理的细胞,其振幅为0.12 μ m。在P型atp酶缺陷型黑曲霉菌株pmrAΔ 和pmca Δ 中,胺碘酮处理后的 [Ca(2)](c) 静息水平至少是野生型的两倍,这与真菌活力和对胺碘酮的超敏反应有关。胺碘酮和两性霉素b的组合在细胞活力和胞质钙内流方面是累加的。相反,唑类药物和胺碘酮的组合对真菌的生存能力具有协同作用。

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