State Key Laboratory for Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, 510060, China.
Mar Drugs. 2010 Apr 1;8(4):1094-105. doi: 10.3390/md8041094.
Marine-derived fungi provide plenty of structurally unique and biologically active secondary metabolites. We screened 87 marine products from mangrove fungi in the South China Sea for anticancer activity by MTT assay. 14% of the compounds (11/86) exhibited a potent activity against cancer in vitro. Importantly, some compounds such as compounds 78 and 81 appeared to be promising for treating cancer patients with multidrug resistance, which should encourage more efforts to isolate promising candidates for further development as clinically useful chemotherapeutic drugs. Furthermore, DNA intercalation was not involved in their anticancer activities, as determined by DNA binding assay. On the other hand, the structure-activity analysis indicated that the hydroxyl group was important for their cytotoxic activity and that bulky functional groups such as phenyl rings could result in a loss of biological activity, which will direct the further development of marine product-based derivatives.
海洋来源的真菌提供了大量结构独特和具有生物活性的次级代谢产物。我们通过 MTT assay 筛选了南海红树林真菌中的 87 种海洋产物,以寻找抗癌活性。14%的化合物(11/86)在体外对癌症具有很强的活性。重要的是,一些化合物,如化合物 78 和 81,似乎对治疗多药耐药的癌症患者有很大的希望,这应该鼓励更多的努力来分离有前途的候选物,进一步开发为临床有用的化疗药物。此外,通过 DNA 结合实验确定,化合物的抗癌活性与 DNA 嵌入无关。另一方面,结构活性分析表明,羟基对于它们的细胞毒性活性很重要,而苯环等大体积的官能团可能导致生物活性丧失,这将指导基于海洋产物的衍生物的进一步开发。