Mroczyńska Martyna, Brillowska-Dąbrowska Anna
Department of Molecular Biotechnology and Microbiology, Gdańsk University of Technology, Narutowicza 11/12, 80-233 Gdańsk, Poland.
Antibiotics (Basel). 2020 May 2;9(5):227. doi: 10.3390/antibiotics9050227.
Fungal infections are rising all over the world every year. There are only five medical compound classes for treatment: triazoles, echinocandins, polyenes, flucytosine and allylamine. Currently, echinocandins are the most important compounds, because of their wide activity spectrum and much lower sides effects that may occur during therapy with other drugs. Echinocandins are secondary metabolites of fungi, which can inhibit the biosynthesis of β-(1,3)-D-glucan. These compounds have fungicidal and fungistatic activity depending on different genera of fungi, against which they are used. Echinocandin resistance is rare-the major cause of resistance is mutations in the gene encoding the β-(1,3)-D-glucan synthase enzyme. In this review of the literature we have summarized the characteristics of echinocandins, the mechanism of their antifungal activity with pharmacokinetics and pharmacodynamics, and the resistance issue.
真菌感染在全球范围内逐年增加。目前仅有五类医学化合物用于治疗:三唑类、棘白菌素类、多烯类、氟胞嘧啶和烯丙胺类。当前,棘白菌素类是最重要的化合物,因为它们具有广泛的活性谱,且在与其他药物治疗期间可能出现的副作用要低得多。棘白菌素类是真菌的次级代谢产物,可抑制β-(1,3)-D-葡聚糖的生物合成。这些化合物根据所使用的不同真菌属具有杀菌和抑菌活性。棘白菌素耐药性罕见——耐药的主要原因是编码β-(1,3)-D-葡聚糖合酶的基因突变。在本次文献综述中,我们总结了棘白菌素类的特性、其抗真菌活性机制以及药代动力学和药效学,还有耐药性问题。