Anticancer effect and structure-activity analysis of marine products isolated from metabolites of mangrove fungi in the South China Sea.
Anticancer effect and structure-activity analysis of marine products isolated from metabolites of mangrove fungi in the South China Sea.
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DOI：
10.3390/md8041094
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发表时间：
2010-04-01
期刊：
影响因子：
5.4
通讯作者：
Fu LW
中科院分区：
文献类型：
--
作者：
Tao LY;Zhang JY;Liang YJ;Chen LM;Zhen LS;Wang F;Mi YJ;She ZG;To KK;Lin YC;Fu LW
海洋来源的真菌提供了大量具有独特结构和生物活性的次生代谢产物。采用四甲基偶氮唑盐比色法对中国南海红树林真菌中的87种海产品进行了抗癌活性筛选。14%(11/86)的化合物在体外表现出较强的抗癌活性。重要的是，一些化合物，如化合物78和81，似乎有希望用于治疗多药耐药的癌症患者，这应该会鼓励更多的努力，以分离出有希望的候选药物，作为临床上有用的化疗药物。此外，DNA结合实验表明，它们的抗癌活性与DNA插层无关。另一方面，结构-活性分析表明，羟基对其细胞毒活性具有重要作用，苯环等体积较大的官能团可能导致生物活性的丧失，这将为进一步开发基于海洋产品的衍生物提供指导。
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.
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