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棘白菌素类 - 结构、作用机制及在抗真菌治疗中的应用。

Echinocandins - structure, mechanism of action and use in antifungal therapy.

机构信息

Department of Microbiology and Biotechnology, Laboratory of Cytobiochemistry, University of Bialystok, Bialystok, Poland.

Doctoral School of Exact and Natural Sciences, University of Bialystok, Bialystok, Poland.

出版信息

J Enzyme Inhib Med Chem. 2022 Dec;37(1):876-894. doi: 10.1080/14756366.2022.2050224.

DOI:10.1080/14756366.2022.2050224
PMID:35296203
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8933026/
Abstract

With increasing number of immunocompromised patients as well as drug resistance in fungi, the risk of fatal fungal infections in humans increases as well. The action of echinocandins is based on the inhibition of β-(1,3)-d-glucan synthesis that builds the fungal cell wall. Caspofungin, micafungin, anidulafungin and rezafungin are semi-synthetic cyclic lipopeptides. Their specific chemical structure possess a potential to obtain novel derivatives with better pharmacological properties resulting in more effective treatment, especially in infections caused by and species. In this review we summarise information about echinocandins with closer look on their chemical structure, mechanism of action, drug resistance and usage in clinical practice. We also introduce actual trends in modification of this antifungals as well as new methods of their administration, and additional use in viral and bacterial infections.

摘要

随着免疫功能低下患者数量的增加以及真菌的耐药性不断增强,人类致命真菌感染的风险也随之增加。棘白菌素类药物的作用机制是基于抑制真菌细胞壁组成成分β-(1,3)-d-葡聚糖的合成。卡泊芬净、米卡芬净、阿尼芬净和瑞他康唑均为半合成环状脂肽。其特定的化学结构具有获得具有更好药理特性的新型衍生物的潜力,从而使治疗更有效,尤其是在由 和 物种引起的感染中。在这篇综述中,我们总结了棘白菌素类药物的相关信息,重点关注它们的化学结构、作用机制、耐药性以及在临床实践中的应用。我们还介绍了该类抗真菌药物的最新修饰趋势,以及其新的给药方法,以及在病毒和细菌感染中的额外应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7acd/8933026/cf20cbe81dce/IENZ_A_2050224_F0014_C.jpg
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