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Elimination of NAPQI, the Toxic Metabolite of Paraceta-mol, by Ebselen

Qiu-Ju Li*, Yi-Xiong Lei, Jian-Ping He, Yin-Fen Wang   

  1. 1. National Research Lab of Natural and Biomimetic Drugs. Beijing 100083 Medical Universily Beijing 100083
    2. Institute of photographic Chemislry Chinese Academy. of Sciences
    3. The Fourth Beijing Pharmaceutical Coinpany
  • Received:1995-06-05 Revised:1995-10-18 Online:1996-03-15 Published:1996-03-15
  • Contact: Qiu-Ju Li*

Abstract: Ebselen. 2-phenyl-1,2-benzisoselenazol-3 (2H)-one, activated by. glutathione(GSH) was shown to react with N-acetyl-p-benzoquinone imine (NAPQI). the toxic rnetabolite ofparacetamol, but not to react with paracetamol. The GSH-activaled ebselen reacts uith NAPQI fasterand more complete than with ebselen alone. Compared xvith the UV-spectra of the solution containing20 μmol/L ebselen tactivated by 20 μmol/L GSH) and 20 μmol/L NAPQI with the solution contain-ing 20 μmol/L ebselen tactivated by 20 μmol/LGSH) and 20 μmol/L paracetamol, NAPQI was foundto be reduced to paracetamol by activated ebselen. The optimal PH range for this reaction was foundto be 7.4 to 8.2.

Key words: Ebselen: Glutathione, NAPQI, paracetamol

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