Depsidones, Aromatase Inhibitors and Radical Scavenging Agents from the Marine-Derived Fungus Aspergillus unguis CRI282-03

Abstract

Three new depsidones (1, 3, and 4), a new diaryl ether (5), and a new natural pyrone (9) (synthetically known), together with three known depsidones, nidulin (6), nornidulin (7), and 2-chlorounguinol (8), were isolated from the marine-derived fungus Aspergillus unguis CRI282-03. Aspergillusidone C (4) showed the most potent aromatase inhibitory activity with the IC₅₀ value of 0.74 µM, while depsidones 1, 3, 6–8 inhibited aromatase with IC₅₀ values of 1.2–11.2 µM. It was found that the structural feature of depsidones, not their corresponding diaryl ether derivatives (e.g. 5), was important for aromatase inhibitory activity. Aspergillusidones A (1) and B (3) showed radical scavenging activity in the XXO assay with IC₅₀ values of 16.0 and < 15.6 µM, respectively. Compounds 1 and 3–7 were mostly inactive or showed only weak cytotoxic activity against HuCCA-1, HepG2, A549, and MOLT-3 cancer cell lines.

Key words

Aspergillus unguis - Trichocomaceae - depsidones - aromatase inhibitor - radical scavenging activity - marine-derived fungi

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