Leporizines A鈥揅: Epithiodiketopiperazines Isolated from an Aspergillus Species

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• 作者：Ricardo Reategui ; Joshua Rhea ; Janet Adolphson ; Kathryn Waikins ; Ryan Newell ; John Rabenstein ; Ulla Mocek ; Michele Luche ; Grant Carr
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：September 27, 2013
• 年：2013
• 卷：76
• 期：9
• 页码：1523-1527
• 全文大小：282K
• 年卷期：v.76,no.9(September 27, 2013)
• ISSN：1520-6025

文摘

Three new compounds named leporizines A鈥揅 (1鈥?b>3) have been isolated from an Aspergillus sp. strain. Their structures were elucidated by analysis of 1D and 2D NMR spectra. Leporizines A and B were isolated during dereplication of hits from a high-throughput screening campaign for correctors of the cystic fibrosis transmembrane conductance regulator (CFTR), and leporizine C was isolated while preparing additional material for characterization of leporizines A and B. CFTR activity observed for leporizines A and B was highly correlated with cell toxicity and was determined to be a nonspecific effect. Leporizine C was not cytotoxic to cells and did not elicit a response in the CFTR assays. To the best of our knowledge, leporizines A鈥揅 represent the first examples of this unusual epithiodiketopiperazine skeleton.