Abstract
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.
Highlights
The majority of species are found in the oceans, which constitute 70% of the world’s surface.Marine organisms are a rich source of chemical products [1,2]
Compounds 78 and 81 exhibited similar IC50 values in both ABCB1/P-glycoprotein (P-gp) overexpressing MDR cells such as KBv200, MCF-7/adr and their parental sensitive cells such as KB, MCF-7 (Table 1). These results suggest that we found some lead compounds from marine production and some are promising to treat MDR cancer patients
The analysis of structure-activity will direct the further development of marine product-based derivatives
Summary
The majority of species are found in the oceans, which constitute 70% of the world’s surface. Marine organisms are a rich source of chemical products [1,2]. Emerging evidence suggests that marine natural products, especially the secondary metabolites from marine organisms, are far more likely to yield anticancer drugs than terrestrial sources [1,5]. Marine-derived fungi have proven to be a rich source of structurally unique and biologically active secondary metabolites [7]. The development of multidrug resistance (MDR) to chemotherapeutic drugs is a main obstacle for the successful treatment of malignant tumors. It is believed that a rich source of anticancer drug candidates could be obtained from marine organisms or their metabolites. We describe qualitative structure-activity relations for a number of mangrove-derived secondary metabolites. Some further compounds have not been obtained from nature and will be described in detail later elsewhere
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