4.7 Article

Territrem and Butyrolactone Derivatives from a Marine-Derived Fungus Aspergillus Terreus

Journal

MARINE DRUGS
Volume 12, Issue 12, Pages 6113-6124

Publisher

MDPI AG
DOI: 10.3390/md12126113

Keywords

Aspergillus terreus; anti-acetylcholinesterase; anti-HSV-1; antifouling; butyrolactone derivative; territrem derivative

Funding

  1. National Marine Public Welfare Research Project of China [201305017]
  2. National Natural Science Foundation of China [41376160]
  3. Strategic Leading Special Science and Technology Program of Chinese Academy of Sciences [XDA100304002]
  4. 863 Program of China [2012AA092104]
  5. 973 Program of China [2010CB833803]
  6. Regional Innovation Demonstration Project of Guangdong Province Marine Economic Development [GD2012-D01-002, GD2012-D01-001]

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Seventeen lactones including eight territrem derivatives (1-8) and nine butyrolactone derivatives (9-17) were isolated from a marine-derived fungus Aspergillus terreus SCSGAF0162 under solid-state fermentation of rice. Compounds 1-3 and 9-10 were new, and their structures were elucidated by spectroscopic analysis. The acetylcholinesterase inhibitory activity and antiviral activity of compounds 1-17 were evaluated. Among them, compounds 1 and 2 showed strong inhibitory activity against acetylcholinesterase with IC50 values of 4.2 +/- 0.6, 4.5 +/- 0.6 nM, respectively. This is the first time it has been reported that 3, 6, 10, 12 had evident antiviral activity towards HSV-1 with IC50 values of 16.4 +/- 0.6, 6.34 +/- 0.4, 21.8 +/- 0.8 and 28.9 +/- 0.8 mu g . mL(-1), respectively. Antifouling bioassay tests showed that compounds 1, 11, 12, 15 had potent antifouling activity with EC50 values of 12.9 +/- 0.5, 22.1 +/- 0.8, 7.4 +/- 0.6, 16.1 +/- 0.6 mu g.mL(-1) toward barnacle Balanus amphitrite larvae, respectively.

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