Institute of Biophysics, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia.
Institute of Biophysics, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia.
Biochim Biophys Acta Biomembr. 2019 Feb 1;1861(2):418-430. doi: 10.1016/j.bbamem.2018.11.006. Epub 2018 Nov 17.
The incidence of resistant fungal pathogens has been increasing, especially in immuno-compromised people. As such, considerable research has been focused on discovering anti-fungal agents with new mechanisms of action and on optimizing the use of existing agents. In this context, interest in the polyene group of anti-fungals has recently been renewed, since they are known to be effective against a broad spectrum of fungal pathogens that only rarely develop a resistance to them. In the past 10 years considerable efforts have been made to improve their efficacy and, simultaneously, to reduce their toxicity. Knowledge about the basic mechanisms of their action will be of crucial importance to further optimizing their use. The mechanisms of polyene action at the membrane level are reviewed here, focusing primarily on their pore-forming activity and on the resulting osmotic responses of artificial lipid vesicles and different eukaryotic cells.
抗真菌病原体的发病率一直在增加,尤其是在免疫功能低下的人群中。因此,人们已经投入了大量的研究来寻找具有新作用机制的抗真菌药物,并优化现有药物的使用。在这种情况下,人们最近对多烯类抗真菌药物重新产生了兴趣,因为它们已知对广泛的真菌病原体有效,而这些病原体很少对它们产生耐药性。在过去的 10 年中,人们已经做出了巨大的努力来提高它们的疗效,同时降低它们的毒性。对抗真菌药物作用的基本机制的了解对于进一步优化它们的使用至关重要。本文主要关注其形成孔的活性以及由此导致的人工脂质体和不同真核细胞的渗透性反应,综述了多烯类药物在膜水平上的作用机制。