Ebselen对扑热息痛的毒性代谢产物NAPQI的体外清除作用

Ebselen对扑热息痛的毒性代谢产物NAPQI的体外清除作用

李秋菊^*, 蕾义雄, 何建平, 王映芬

1. 北京医科大学天然药物及仿生药物国家重点实验室, 北京 100083;
2. 中国科学院感光化学研究所;
3. 北京第四制药厂

收稿日期:1995-06-05 修回日期:1995-10-18 出版日期:1996-03-15 发布日期:1996-03-15
通讯作者: 李秋菊*

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

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

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*

摘要/Abstract

摘要： Ebselen, 2-phenyl(-1,2-benzisoselenazol-3(2H)-one), 被谷胱甘肽激活后可与扑热息痛的毒性代谢产物NAPQI反应, 但不能与扑热息痛本身起反应。激活形式的ebselen与NAPQI反应的阈浓度为2.5 μmol/L, ebselen单独与NAPQI反应的阈浓度为50 μmol/L, 且激活形式的ebselen比ebselen本身与NAPQI反应更快而完全。比较20 μmol/L(ebselen与GSH) + 20 μmol/LNAPQI与20 μmol/L(ebselen与GSH) + 20 μmol/L扑热息痛的紫外光措, 提示NAPQI被ebselen还原成其母体化合物扑热息痛, 反应的速度受ebselen的浓度, NAPQI的浓度的影响, 反应的最佳pH范围是7.4至8.2。

关键词: Ebselen, 谷胱甘肽, NAPQI, 扑热息痛

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

Supporting:

李秋菊^*, 蕾义雄, 何建平, 王映芬. Ebselen对扑热息痛的毒性代谢产物NAPQI的体外清除作用[J]. .

Qiu-Ju Li^*, Yi-Xiong Lei, Jian-Ping He, Yin-Fen Wang. Elimination of NAPQI, the Toxic Metabolite of Paraceta-mol, by Ebselen[J]. .

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