In vitro cytotoxicity of melleolide antibiotics: structural and mechanistic aspects |
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Authors: | Bohnert Markus Miethbauer Sebastian Dahse Hans-Martin Ziemen Johannes Nett Markus Hoffmeister Dirk |
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Institution: | a Friedrich-Schiller-Universität Jena, Department Pharmaceutical Biology at the Hans-Knöll-Institute, Beutenbergstrasse 11a, 07745 Jena, Germany b Leibniz Institute for Natural Product Research and Infection Biology, Hans-Knöll-Institute, Beutenbergstrasse 11a, 07745 Jena, Germany |
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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 IC50 = 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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Keywords: | Armillaria Melleolide Antibiotics Natural product Cytotoxicity |
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