Abstract
In this article, we report anticancer activity of 14 anthracenedione derivatives separated from the secondary metabolites of the mangrove endophytic fungi Halorosellinia sp. (No. 1403) and Guignardia sp. (No. 4382). Some of them inhibited potently the growth of KB and KBv200 cells, among which compound 6 displayed strong cytotoxicity with IC50 values of 3.17 and 3.21 μM to KB and KBv200 cells, respectively. Furthermore, we demonstrate that the mechanism involved in the apoptosis induced by compound 6 is probably related to mitochondrial dysfunction. Additionally, the structure-activity relationships of these compounds are discussed.
Highlights
Cancer has become an increasing public health problem due to its high rates of morbidity and mortality
We investigated the anticancer activity of several anthracenedione derivatives, which was separated from the secondary metabolites of the mangrove endophytic fungus Halorosellinia sp
The results showed that apoptosis rates of drug-treated cells were 25.3 ± 3.5% and 26.4 ± 2.4% for KB and KBv200 cells, respectively
Summary
Cancer has become an increasing public health problem due to its high rates of morbidity and mortality. The natural environment is still the most important supply of novel drugs despite development of combinatorial chemistry, which can quickly generate thousands of new chemicals. Many promising compounds of new and complicated structure types have been isolated from the oceans and some have been identified as leading preclinical anticancer compounds. Marine-derived fungi have been rich sources of structurally novel and biologically active secondary metabolites, which have become attractive as important resources for new chemicals in drug discovery [12,13]. As part of our ongoing investigations directed toward the discovery of structurally new and biologically active natural products from marine endophytic fungi, we studied the anthracenedione derivatives acting as the potent anticancer agents screened from the mangrove endophytic fungus Halorosellinia sp. We analyze the structureactivity relationships (SAR) of these compounds
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