Department of Chemistry and Biochemistry, University of North Carolina at Greensboro, Greensboro, NC 27402, USA.
J Antibiot (Tokyo). 2012 Nov;65(11):541-9. doi: 10.1038/ja.2012.71. Epub 2012 Sep 19.
Enniatins are cyclohexadepsipeptides isolated largely from Fusarium species of fungi, although they have been isolated from other genera, such as Verticillium and Halosarpheia. They were first described over 60 years ago, and their range of biological activities, including antiinsectan, antifungal, antibiotic and cytotoxic, drives contemporary interest. To date, 29 enniatins have been isolated and characterized, either as a single compound or mixtures of inseparable homologs. Structurally, these depsipeptides are biosynthesized by a multifunctional enzyme, termed enniatin synthetase, and are composed of six residues that alternate between N-methyl amino acids and hydroxy acids. Their structure elucidation can be challenging, particularly for enniatins isolated as inseparable homologs; however, several strategies and tools have been utilized to solve these problems. Currently, there is one drug that has been developed from a mixture of enniatins, fusafungine, which is used as a topical treatment of upper respiratory tract infections by oral and/or nasal inhalation. Given the range of biological activities observed for this class of compounds, research on enniatins will likely continue. This review strives to digest the past studies, as well as, describe tools and techniques that can be utilized to overcome the challenges associated with the structure elucidation of mixtures of enniatin homologs.
恩镰菌素是从真菌镰刀菌属中分离出来的环己二肽，尽管它们也从其他属如轮枝孢属和海鞘属中分离出来。它们在 60 多年前首次被描述，其广泛的生物活性，包括抗昆虫、抗真菌、抗生素和细胞毒性，激发了当代的兴趣。迄今为止，已经分离和鉴定了 29 种恩镰菌素，要么是单一化合物，要么是不可分离的同系物混合物。这些环二肽是由一种多功能酶，称为恩镰菌素合酶，生物合成的，由六个交替的 N-甲基氨基酸和羟基酸残基组成。它们的结构解析可能具有挑战性，特别是对于作为不可分离的同系物分离的恩镰菌素；然而，已经利用了几种策略和工具来解决这些问题。目前，已经开发了一种从恩镰菌素混合物中提取的药物，fusafungine，它被用作上呼吸道感染的局部治疗，通过口服和/或鼻腔吸入。鉴于这类化合物观察到的广泛的生物活性，对恩镰菌素的研究可能会继续。这篇综述旨在总结过去的研究，并描述可以用来克服解析恩镰菌素同系物混合物结构所面临的挑战的工具和技术。
