Polyketide glycosides phialotides A to H, new potentiators of amphotericin B activity, produced by Pseudophialophora sp. BF-0158.,The Journal of Antibiotics

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Polyketide glycosides phialotides A to H, new potentiators of amphotericin B activity, produced by Pseudophialophora sp. BF-0158.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2020-01-23 , DOI: 10.1038/s41429-019-0276-7
Akiho Yagi ₁ , Ryuji Uchida ₁ , Keisuke Kobayashi ₂ , Hiroshi Tomoda ₂

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Eight new potentiators of antifungal amphotericin B (AmB) activity, phialotides A to H, were isolated from the fermentation broths of the rare fungus Pseudophialophora sp. BF-0158. The structures of phialotides were elucidated by spectroscopic analyses, including NMR and MS, and degradation studies. Phialotides were novel polyketide glycosides consisting of a 1,3-dimethylbut-1-ene (C6-unit) repeating substructure and one to three hexopyranoses. None of the phialotides exhibited antifungal activity, whereas all potentiated AmB activity against several fungi. Phialotide F was the most effective potentiator of AmB activity against Candida albicans, with a decrease in the MIC from 0.50 to 0.016 µg ml-1 being observed in combination with phialotide F at 1.0 µg ml-1.

中文翻译：

Pseudophialophora sp。生产的两性霉素B活性新增效剂聚酮苷糖脂A至H。BF-0158。

从稀有真菌假单胞菌属菌种的发酵液中分离出八个抗真菌两性霉素B（AmB）活性增效剂，即拟肽A至H。BF-0158。通过光谱分析，包括NMR和MS，以及降解研究，阐明了脂环肽的结构。磷脂是由1，3-二甲基丁-1-烯（C6-单元）重复亚结构和1-3个六吡喃糖组成的新型聚酮糖苷。phialotides均未显示出抗真菌活性，而所有增强的AmB活性均针对几种真菌。Phialotide F是最有效的AmB对抗白色念珠菌的增强剂，与1.0μgml-1的phialotide F组合使用时，MIC从0.50降至0.016μgml-1。

更新日期：2020-01-23

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