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New bioactive compounds from aquatic endophyte Chaetomium globosum.

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Two new compounds from Chinese yam fermentation, 10,11-dihydroxyl-aureonitol and yamchaetoglobosin A, show potential. Yamchaetoglobosin A exhibits significant anti-acetylcholinesterase activity and cytotoxicity against cancer cells.

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Area of Science:

  • Natural Product Chemistry
  • Pharmacology
  • Microbiology

Background:

  • Chaetomium globosum is a fungus known to produce bioactive metabolites.
  • Chinese yam (Dioscorea opposita) is a traditional medicinal plant.
  • Aureonitol and cytochalasan derivatives have limited reported bioactivities.

Purpose of the Study:

  • To isolate and characterize new compounds from Chaetomium globosum fermented with Chinese yam.
  • To evaluate the pharmacological activities of the isolated compounds, including anti-inflammatory, anti-acetylcholinesterase, cytotoxic, and anticoagulant effects.
  • To explore the preliminary structure-activity relationships of these novel compounds.

Main Methods:

  • Fermentation of Chaetomium globosum in Chinese yam medium.
  • Isolation and structure elucidation of compounds using spectroscopic methods (NMR, MS).
  • In vitro assays for nitric oxide inhibition, anti-acetylcholinesterase activity, cytotoxicity against various cancer cell lines, and anticoagulant activity.

Main Results:

  • Two new compounds, 10,11-dihydroxyl-aureonitol (1) and yamchaetoglobosin A (2), were isolated.
  • Yamchaetoglobosin A (2) demonstrated significant inhibition of nitric oxide production in LPS-activated macrophages.
  • Compound 2 exhibited potent anti-acetylcholinesterase activity (92.5% inhibition at 50 μM) and broad-spectrum cytotoxicity against HL-60, A-549, SMMC-7721, MCF-7, and SW480 cancer cell lines (51-96% inhibition at 40 μM).
  • Both compounds showed weak anticoagulant activity.
  • Preliminary structure-activity relationship analysis suggested that oxidation and ring-opening in yamchaetoglobosin A preserve inhibitory effects against nitric oxide production and tumor cells.

Conclusions:

  • Novel aureonitol and cytochalasan derivatives were identified from a fungal-plant fermentation system.
  • Yamchaetoglobosin A possesses significant anti-acetylcholinesterase and anticancer properties, warranting further investigation.
  • The study highlights the potential of microbial fermentation of traditional medicinal plants for discovering new bioactive compounds.