从红树内生真菌次级代谢产物中分离得到的蒽醌二酮衍生物作为抗癌剂。

State Key Laboratory for Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, 510060, China.

Mar Drugs. 2010 Apr 23;8(4):1469-81. doi: 10.3390/md8041469.

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 IC(50) values of 3.17 and 3.21 microM 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.

在这篇文章中，我们报告了从红树林内生真菌 Halorosellinia sp.（1403 号）和 Guignardia sp.（4382 号）的次级代谢产物中分离得到的 14 个蒽二酮衍生物的抗癌活性。其中一些化合物强烈抑制 KB 和 KBv200 细胞的生长，其中化合物 6 对 KB 和 KBv200 细胞的细胞毒性分别为 3.17 和 3.21 μM。此外，我们证明了化合物 6 诱导细胞凋亡的机制可能与线粒体功能障碍有关。此外，还讨论了这些化合物的构效关系。