REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, R. Jorge Viterbo Ferreira, nº 228, 4050-313 Porto, Portugal.
REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, R. Jorge Viterbo Ferreira, nº 228, 4050-313 Porto, Portugal; IINFACTS-Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, University Institute of Health Sciences (IUCS), CESPU, CRL, Gandra, Portugal.
Biomed Pharmacother. 2021 Aug;140:111756. doi: 10.1016/j.biopha.2021.111756. Epub 2021 May 26.
Despite the increasing number of novel marine natural products being reported from fungi in the last three decades, to date only the broad-spectrum cephalosporin C can be tracked back as marine fungal-derived drug. Cephalosporins were isolated in the early 1940s from a strain of Acremonium chrysogenum obtained in a sample collected in sewage water in the Sardinian coast, preliminary findings allowing the discovery of cephalosporin C. Since then, bioprospection of marine fungi has been enabling the identification of several metabolites with antibacterial effects, many of which proving to be active against multi-drug resistant strains, available data suggesting also that some might fuel the pharmaceutical firepower towards some of the bacterial pathogens classified as a priority by the World Health Organization. Considering the success of their terrestrial counterparts on the discovery and development of several antibiotics that are nowadays used in the clinical setting, marine fungi obviously come into mind as producers of new prototypes to counteract antibiotic-resistant bacteria that are no longer responding to available treatments. We mainly aim to provide a snapshot on those metabolites that are likely to proceed to advanced preclinical development, not only based on their antibacterial potency, but also considering their targets and modes of action, and activity against priority pathogens.
尽管在过去三十年中，从真菌中报道的新型海洋天然产物的数量不断增加，但迄今为止，只有广谱头孢菌素 C 可以追溯到海洋真菌来源的药物。头孢菌素于 20 世纪 40 年代初从在撒丁岛海岸污水中采集的样本中获得的一株顶头孢霉属（Acremonium chrysogenum）菌株中分离出来，初步发现允许发现头孢菌素 C。从那时起，海洋真菌的生物勘探已经能够识别出几种具有抗菌作用的代谢物，其中许多对多药耐药菌株有效，现有数据还表明，一些代谢物可能为一些被世界卫生组织列为优先的细菌病原体提供药物火力。考虑到它们的陆地对应物在发现和开发几种抗生素方面的成功，这些抗生素如今在临床环境中使用，海洋真菌显然成为对抗生素耐药细菌的新型原型的生产者，这些细菌对现有治疗方法不再有反应。我们的主要目的是提供那些可能进入高级临床前开发的代谢物的快照，不仅基于它们的抗菌效力，还考虑它们的靶点和作用模式，以及针对优先病原体的活性。
