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Asperfuran, a novel antifungal metabolite from Aspergillus oryzae

W Pfefferle1, H Anke, M Bross

  • 1Department of Biotechnology, University of Kaiserslautern, FRG.

The Journal of Antibiotics
|June 1, 1990
PubMed

Insights

Asperfuran, a novel antifungal compound from Aspergillus oryzae, shows weak inhibition of chitin synthase and induces morphological changes in fungi. Its cytotoxicity in mammalian cells is also minimal.

Area of Science:

  • Mycology
  • Biochemistry
  • Pharmacology

Background:

  • Aspergillus oryzae produces novel secondary metabolites.
  • Dihydrobenzofuran derivatives are explored for biological activities.

Purpose of the Study:

  • To characterize the antifungal properties of asperfuran.
  • To investigate the mechanism of action of asperfuran on chitin synthase.
  • To evaluate the cytotoxicity of asperfuran in mammalian cell lines.

Main Methods:

  • Enzyme inhibition assays using chitin synthase from Coprinus cinereus.
  • Agar diffusion assays with Mucor miehei.
  • Cytotoxicity assays with HeLa S3 and L1210 cells.

Main Results:

  • Asperfuran weakly inhibited fungal chitin synthase.
  • Egg lecithin abolished the inhibitory effect on chitin synthase.
  • Low concentrations of asperfuran induced morphological changes in Mucor miehei.
  • Asperfuran exhibited weak cytotoxicity against HeLa S3 and L1210 cells (IC50 = 25 µg/mL).

Conclusions:

  • Asperfuran is a novel antifungal dihydrobenzofuran derivative.
  • The antifungal activity of asperfuran may involve chitin synthase, but this is modulated by lipids.
  • Asperfuran demonstrates potential as a minimally cytotoxic antifungal agent.

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