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Updated: Jun 3, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
In vitro cytotoxicity of melleolide antibiotics: structural and mechanistic aspects
Markus Bohnert1, Sebastian Miethbauer, Hans-Martin Dahse
1Department Pharmaceutical Biology, Friedrich-Schiller-Universität Jena, Hans-Knöll-Institute, Beutenbergstrasse 11a, 07745 Jena, Germany.
Abstract:
Melleolide sesquiterpene aryl esters are secondary products of the mushroom genus Armillaria. We compared the cytotoxicity of eleven melleolides--five thereof are new natural products--against four human cancer cell lines. Armillaridin, 4-O-methylarmillaridin, and dehydroarmillylorsellinate were most active, at IC(50) = 3.0, 4.1 and 5.0 μM, respectively, against Jurkat T cells for the former two compounds, and K-562 cells for the latter. Dehydroarmillylorsellinate did not inhibit respiration and RNA-synthesis of K-562 cells at 5 μM. However, replication of DNA dropped to 35% after 120 min at this concentration, and translational activity also decreased.
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