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Mar. Drugs 2013, 11(7), 2616-2624;

Secondary Metabolites of a Mangrove Endophytic Fungus Aspergillus terreus (No. GX7-3B) from the South China Sea

School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China
College of Science, Guangdong Ocean University, Zhanjiang 524088, China
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, Guangzhou 510080, China
School of Science and Engineering, Jinan University, Guangzhou 510632, China
Authors to whom correspondence should be addressed.
Received: 8 April 2013 / Revised: 24 June 2013 / Accepted: 28 June 2013 / Published: 19 July 2013
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The mangrove endophytic fungus Aspergillus terreus (No. GX7-3B) was cultivated in potato dextrose liquid medium, and one rare thiophene compound (1), together with anhydrojavanicin (2), 8-O-methylbostrycoidin (3), 8-O-methyljavanicin (4), botryosphaerone D (5), 6-ethyl-5-hydroxy-3,7-dimethoxynaphthoquinone (6), 3β,5α-dihydroxy-(22E,24R)-ergosta-7,22-dien-6-one (7), 3β,5α,14α-trihydroxy-(22E,24R)-ergosta-7, 22-dien-6-one (8), NGA0187 (9) and beauvericin (10), were isolated. Their structures were elucidated by analysis of spectroscopic data. This is the first report of a natural origin for compound 6. Moreover, compounds 3, 4, 5, 7, 8 and 10 were obtained from marine microorganism for the first time. In the bioactive assays in vitro, compounds 2, 3, 9 and 10 displayed remarkable inhibiting actions against α-acetylcholinesterase (AChE) with IC50 values 2.01, 6.71, 1.89, and 3.09 μM, respectively. Furthermore, in the cytotoxicity assays, compounds 7 and 10 exhibited strong or moderate cytotoxic activities against MCF-7, A549, Hela and KB cell lines with IC50 values 4.98 and 2.02 (MCF-7), 1.95 and 0.82 (A549), 0.68 and 1.14 (Hela), and 1.50 and 1.10 μM (KB), respectively; compound 8 had weak inhibitory activities against these tumor cell lines; compounds 1, 2, 3, 4, 5, 6 and 9 exhibited no inhibitory activities against them. View Full-Text
Keywords: mangrove endophytic fungi; thiophene; secondary metabolites; cytotoxicity; AChE mangrove endophytic fungi; thiophene; secondary metabolites; cytotoxicity; AChE

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Deng, C.-M.; Liu, S.-X.; Huang, C.-H.; Pang, J.-Y.; Lin, Y.-C. Secondary Metabolites of a Mangrove Endophytic Fungus Aspergillus terreus (No. GX7-3B) from the South China Sea. Mar. Drugs 2013, 11, 2616-2624.

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