多烯糖甙 phialotides A 至 H，由 Pseudophialophora sp. BF-0158 产生的两性霉素 B 活性增效剂。
Polyketide glycosides phialotides A to H, new potentiators of amphotericin B activity, produced by Pseudophialophora sp. BF-0158.
机构信息
Department of Natural Product Chemistry, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University. 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi, 981-8558, Japan.
Microbial Chemistry and Medicinal Research Laboratories, Graduate School of Pharmaceutical Sciences, Kitasato University. 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
出版信息
J Antibiot (Tokyo). 2020 Apr;73(4):211-223. doi: 10.1038/s41429-019-0276-7. Epub 2020 Jan 23.
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 (C-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 being observed in combination with phialotide F at 1.0 µg ml.
从稀有真菌拟青霉 BF-0158 的发酵液中分离到了 8 种新的抗真菌两性霉素 B（AmB）活性增效剂 phialotides A 到 H。通过包括 NMR 和 MS 在内的光谱分析以及降解研究阐明了 phialotides 的结构。phialotides 是由 1,3-二甲基丁-1-烯（C 单元）重复亚结构和一个到三个己吡喃糖组成的新型聚酮糖甙。没有一种 phialotides 表现出抗真菌活性，而所有的 phialotides 都增强了 AmB 对几种真菌的活性。Phialotide F 是对白色念珠菌最有效的 AmB 活性增效剂，与 phialotide F 联合使用时，在 1.0 µg/ml 时，MIC 从 0.50 降至 0.016 µg/ml。
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