Citrinin Hydrate Inhibit Serotonin N-Acetyltransferase Catalyzing the Conversion of Serotonin to N-Acetylserotonin

  • Lee, In-Kyoung (The korean Research Institute of Bioscience and Biotechnology) ;
  • Yun, Bong-Sik (The korean Research Institute of Bioscience and Biotechnology) ;
  • Kim, Kyong-Tai (Department of Life Science, Pohang University of Technology) ;
  • Choi, Bo-Hwa (Department of Life Science, Pohang University of TechnologyDepartment of Life Science, Pohang University of Technology) ;
  • Park, Tae-Ju (Department of Life Science, Pohang University of Technology) ;
  • Kim, Young-Ho (College of Pharmacy, Chungnam National University) ;
  • Yoo, Ick-Dong (The korean Research Institute of Bioscience and Biotechnology)
  • Published : 2001.12.01

Abstract

In an attempt to search for serotonin N-acetyltransferase (arylalkylamine N-acetyltransferasem, AA-NAT) inhibitors from microbial metabolites, we fecund the culture broth of Penicillium sp. 80722 which showed a strong inhibitory activity against AA-NNT. The active principle has been identified as citrinin hydrate through bioassay-guided fractionation of cultural broth, and structure elucidation derived by spectroscopic analyses. Citrinin hydrate inhibits AA-NAT with an $IC_50$ value of $173{\mu}M$ in a dose-dependent manner. Although citrinin hydrate was previously isolated as human rhinovirus 3C-protease inhibitor, this was recognized as the first AA-NAT inhibitor isolated from natural sources.

Keywords

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