College of Medical Technology and Engineering, Henan University of Science and Technology, Luoyang, 471023, China.
College of Medical Technology and Engineering, Henan University of Science and Technology, Luoyang, 471023, China.
Peptides. 2019 Mar;113:52-65. doi: 10.1016/j.peptides.2019.02.002. Epub 2019 Feb 7.
Lipopeptide antibiotics have linear or cyclic structures with one or more hydrocarbon tails linked to the N-terminus of a short oligopeptide that may be chemically modified and/or contain unusual amino acid residues in their structures. They possess huge potential as pharmaceutical drugs and biocontrol agents, and ˜30 representative genera of fungi are known to produce them. Some chemically synthesised derivatives have already been developed into commercial products or subjected to clinical trials, including cilofungin, caspofungin, micafungin, anidulafungin, rezafungin, emodepside, fusafungine and destruxins. This review summarizes 200 fungi-derived compounds reported since 2000, including 95 cyclic depsipeptides, 67 peptaibiotics (including 35 peptaibols, eight lipoaminopeptides, and five lipopeptaibols), and 38 non-depsipeptide and non-peptaibiotic lipopeptides. Their sources, structural sequences, antibiotic activities (e.g. antibacterial, antifungal, antiviral, antimycobacterial, antimycoplasmal, antimalarial, antileishmanial, insecticidal, antitrypanosomal and nematicidal), structure-activity relationships, mechanisms of action, and specific relevance are discussed. These compounds have attracted considerable interest within the pharmaceutical and agrochemical industries.
脂肽类抗生素具有线性或环状结构，其 N 端连接一个或多个碳氢链，而碳氢链连接一个短的寡肽，该寡肽可能经过化学修饰，并且在其结构中含有不常见的氨基酸残基。它们具有巨大的药用和生物防治潜力，已知约 30 个真菌属能够产生脂肽类抗生素。一些化学合成的衍生物已经开发成商业产品或进行临床试验，包括棘白菌素、卡泊芬净、米卡芬净、阿尼芬净、瑞他康唑、埃博霉素、 Fusafungine 和几丁质酶抑制剂。本文综述了 2000 年以来报道的 200 种真菌来源的化合物，包括 95 种环状 depsipeptides、67 种肽抗生素（包括 35 种肽类、8 种脂酰氨基肽、5 种脂肽类）和 38 种非 depsipeptide 和非肽类脂肽类。讨论了它们的来源、结构序列、抗生素活性（如抗细菌、抗真菌、抗病毒、抗结核分枝杆菌、抗支原体、抗疟原虫、抗利什曼原虫、杀虫、抗锥虫和杀线虫活性）、构效关系、作用机制和特定相关性。这些化合物在制药和农用化学品行业引起了相当大的兴趣。
