4.7 Article

Anthracenedione Derivatives as Anticancer Agents Isolated from Secondary Metabolites of the Mangrove Endophytic Fungi

Journal

MARINE DRUGS
Volume 8, Issue 4, Pages 1469-1481

Publisher

MDPI
DOI: 10.3390/md8041469

Keywords

mangrove endophytic fungi; anthracenedione derivatives; anticancer; apoptosis; structure-activity relationship

Funding

  1. China National Natural Sciences Foundation [30672407, 30600769]
  2. 863 Project Foundation [2006AA09Z419]
  3. State Key Laboratory of Oncology in South China

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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 mu M 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.

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