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Paper | Special issue | Vol 79, No. 1, 2009, pp.909-916
Published online, 5th December, 2008
DOI: 10.3987/COM-08-S(D)63
Antineoplastic Agents. 575. The Fungus Aspergillus phoenicis

George R. Pettit,* Jiang Du, Robin K. Pettit, John C. Knight, and Dennis L. Doubek

*Department Chemistry and Biochemistry, Arizona State University, Physical Sciences bldg. PSD118 1711 S. Rural Rd., Tempe, Arizona 85287, U.S.A.


Cancer cell line bioassay-guided separation of an extract from the fungus Aspergillus phoenicis collected in Saskatchewan, Canada, resulted in the isolation of three new constituents designated asperlactone (1), aspergillol A (2), and aspergillol B (3), accompanied by four previously known constituents: asperic acid (4), hexylitaconic acid (5), methyl 2-hydroxyphenylacetate (6), and methyl 4-hydroxyphenylacetate (7). The structure of each was determined by analyses of high-resolution mass spectra and high-field NMR data. Asperic acid (4) was found to inhibit growth of the murine lymphocytic leukemia P388 (ED50 0.18 μg/mL) and a panel of human cancer cell lines (GI50 1.7–2.0 μg/mL; pancreas, breast, CNS, lung, colon, and prostate), while aspergillol A (2) showed moderate inhibition against the breast adenocarcinoma MCF-7 (GI50 7.2 μg/mL).