Journal
JOURNAL OF NATURAL PRODUCTS
Volume 71, Issue 4, Pages 689-692Publisher
AMER CHEMICAL SOC
DOI: 10.1021/np070341r
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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 1 (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-3 alpha/beta 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 1 (3). Likewise, butyrolactone I 3-sulfate (1) exhibited moderate cytotoxicity solely against HeLa cells (CC50 = 80.7 mu M).
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