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Mar. Drugs 2013, 11(7), 2616-2624; doi:10.3390/md11072616

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

1,3,*  and 1,3,*
1 School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China 2 College of Science, Guangdong Ocean University, Zhanjiang 524088, China 3 Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, Guangzhou 510080, China 4 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.
Keywords: mangrove endophytic fungi; thiophene; secondary metabolites; cytotoxicity; AChE mangrove endophytic fungi; thiophene; secondary metabolites; cytotoxicity; AChE
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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