Abstract
One new meroterpenoid, named 2-hydroacetoxydehydroaustin (1), together with nine known meroterpenoids, 11-acetoxyisoaustinone (2), isoaustinol (3), austin (4), austinol (5), acetoxydehydroaustin (6), dehydroaustin (7), dehydroaustinol (8), preaustinoid A2 (9), and 1,2-dihydro-acetoxydehydroaustin B (10), were isolated from the mangrove endophytic fungus, Aspergillus sp. 16-5c. These structures were characterized by spectroscopic analysis, further the absolute configurations of stereogenic carbons for Compounds 1, 3, 4, 6, 7, 8, 9, and 10 were determined by single crystal X-ray diffraction analysis using Cu Kα radiation. Moreover, the absolute configurations of stereogenic carbons for Known Compounds 3, 7, 8, and 9 are identified here for the first time. Compounds 3, 7, and 8 showed acetylcholinesterase (AchE) inhibitory activity with IC50 values of 2.50, 0.40, and 3.00 μM, respectively.
Highlights
Meroterpenoids are natural products derived from terpenoids mixed biosynthetic origin [1].Meroterpenoids display structural diversity with widespread biological activities including antimicrobial, antiviral, and antitumoral activities and enzyme inhibition
Austin was first isolated as a novel polyisoprenoid mycotoxin from Aspergillus ustus in 1976 [3]
The results showed Compounds 3, 7, and 8 were potential AChE inhibitors with IC50 values of 2.50, 0.40, and 3.00 μM, respectively
Summary
Meroterpenoids are natural products derived from terpenoids mixed biosynthetic origin [1]. Meroterpenoids display structural diversity with widespread biological activities including antimicrobial, antiviral, and antitumoral activities and enzyme inhibition. Austin and austin analogues are mixed polyketide–terpenoid meroterpenoids derived from. Austin was first isolated as a novel polyisoprenoid mycotoxin from Aspergillus ustus in 1976 [3]. As part of our ongoing investigations on novel bioactive compounds from mangrove endophytic-derived fungi [17,18,19,20], ten meroterpenoids, including one new meroterpenoids named 2-hydro-acetoxydehydroaustin (1), together with nine known meroterpenoids, 11-acetoxyisoaustinone (2), isoaustinol (3), austin (4), austinol (5), acetoxydehydroaustin (6), dehydroaustin (7), dehydroaustinol (8), preaustinoid A2 (9), and. We report the isolation, structural elucidation, acetylcholinesterase (AChE) inhibitory activity, and cytotoxicity of these meroterpenoids.
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