Butyrolactone I Derivatives from Aspergillus terreus Carrying an Unusual Sulfate Moiety

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• 作者：Xuemei Niu ; Hans-Martin Dahse ; Klaus-Dieter Menzel ; Olivier Lozach ; Grit Walther ; Laurent Meijer ; Susanne Grabley ; Isabel Sattler
• 刊名：Journal of Natural Products
• 出版年：2008
• 出版时间：April 2008
• 年：2008
• 卷：71
• 期：4
• 页码：689 - 692
• 全文大小：84K
• 年卷期：v.71,no.4(April 2008)
• ISSN：1520-6025

文摘

In our ongoing search for new bioactive metabolites from microbial resources, Aspergillus terreus (HKI0499) was examined by chemical metabolite profiling. Together with the known butyrolactone I (3), the unusual sulfate derivatives butyrolactone I 3-sulfate (1) and butyrolactone I 4′′-sulfate (2) were discovered. The chemical structures were determined by NMR and MS data analyses. All compounds were tested on CDK1/cyclin B, CDK5/p25, DYRK1A, CK1, and GSK-3α/β kinases; compounds 2 and 3 were also evaluated for their cytotoxic and antiproliferative activities. Butyrolactone I 3-sulfate (1) exhibited specific inhibitory activity against CDK1/cyclin B and CDK5/p25, yet 15–30-fold less than butyrolactone I (3). Likewise, butyrolactone I 3-sulfate (1) exhibited moderate cytotoxicity solely against HeLa cells (CC₅₀ = 80.7 µM).