In vitro cytotoxicity of melleolide antibiotics: structural and mechanistic aspects.

Bohnert M, Miethbauer S, Dahse HM, Ziemen J, Nett M, Hoffmeister D (2011) In vitro cytotoxicity of melleolide antibiotics: structural and mechanistic aspects. Bioorg Med Chem Lett 21, 2003-2006.

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.

Leibniz-HKI-Autor*innen

Markus Bohnert
Dirk Hoffmeister
Markus Nett

Identifier

doi: 10.1016/j.bmcl.2011.02.026

PMID: 21376582