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Anticancer Effect and Structure-Activity Analysis of Marine Products Isolated from Metabolites of Mangrove Fungi in the South China Sea

机译:南海红树林真菌代谢产物海产品的抗癌作用及结构活性分析

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摘要

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.
机译:海洋来源的真菌提供了大量结构独特且具有生物活性的次生代谢产物。我们通过MTT分析筛选了南海红树林真菌的87种海产品的抗癌活性。 14%的化合物(11/86)在体外具有有效的抗癌活性。重要的是,某些化合物(例如化合物78和81)似乎有望用于治疗具有多药耐药性的癌症患者,这应鼓励人们做出更多努力,以分离有希望的候选物作为临床有用的化学治疗药物进行进一步开发。此外,如通过DNA结合测定所确定的,DNA插入不参与其抗癌活性。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,而庞大的官能团(例如苯环)可能会导致生物活性的丧失,这将指导基于海洋产品的进一步发展。衍生品。

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