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

• Main Authors: Li-yang Tao, Jian-ye Zhang, Yong-ju Liang, Li-ming Chen, Li-sheng Zheng, Fang Wang, Yan-jun Mi, Zhi-gang She, Kenneth Kin Wah To, Yong-cheng Lin, Li-wu Fu
• Format: Article
• Language: English
• Published: MDPI AG 2010-04-01
• Series: Marine Drugs
• Subjects: mangrove fungi; multidrug resistance (MDR); quinones; xyloketal; isoflavone; prostaglandins
• Online Access: http://www.mdpi.com/1660-3397/8/4/1094/

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.