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).