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蓝萼甲素在大鼠体内外的代谢转化
引用本文:曹露晔,李云森,陈子君,李仪奎.蓝萼甲素在大鼠体内外的代谢转化[J].华西药学杂志,2006,21(3):227-229.
作者姓名:曹露晔  李云森  陈子君  李仪奎
作者单位:1. 广东化工与制药职业技术学院,广东,广州,510520
2. 中科院上海药物研究所,上海,201203
3. 上海中医药大学中药学院,上海,201203
基金项目:国家高技术研究发展计划(863计划)
摘    要:目的研究蓝萼甲素在大鼠体内外的代谢转化。方法采用大鼠肝微粒体体外温孵法,研究对蓝萼甲素的代谢转化。采用RP-HPLC法同时分离检测蓝萼甲素及其体外代谢产物。结果用液-液萃取、制备HPLC法,从大鼠胆汁中分离了一个代谢产物,经质谱分析推测结构为羟基化蓝萼甲素,并采用HPLC-MS连用,分析了肝微粒体体外温孵样品中的代谢产物,推测了蓝萼甲素的可能代谢转化途径。结论蓝萼甲素在大鼠肝微粒体和胆汁中可被代谢转化,主要代谢产物为羟基化蓝萼甲素。

关 键 词:蓝萼甲素  肝微粒体酶  药物代谢  高效液相色谱法
文章编号:1006-0103(2006)03-0227-03
收稿时间:2005-12

The metabolic study of glaucocalyxin A in rat in vivo and in vitro
CAO Lu-ye,LI Yun-sen,CHEN Zi-jun,LI Yi-kui.The metabolic study of glaucocalyxin A in rat in vivo and in vitro[J].West China Journal of Pharmaceutical Sciences,2006,21(3):227-229.
Authors:CAO Lu-ye  LI Yun-sen  CHEN Zi-jun  LI Yi-kui
Institution:1. Chemical Engineering and Pharmaeeutics College of Guangdong, Guangzhou 510520, China; 2. Shanghai Institute of Materia Medica, Shanghai 201203, China ;3. Institute of Traditional Herb, Shanghai University of Chinese Traditional Medicine, Shanghai 201203, China
Abstract:OBJECTIVE To study the metabolism of glaucocalyxin A in rat liver microsome and bile.METHODS The metabolic transformation of glaucocalyxin A was studied by using rat liver microsomal incubation containing the NADPH-generating system in vitro and in rat bile.A reversed phase HPLC method was established to analyze the parent drug and its metabolites.RESULTS The major metabolites were isolated and purified by liquid-liquid extraction,preparative HPLC,and its structure was elucidated as hydroxyl glaucocalyxin A,which supposed the metabolism pathway of glaucocalyxin A in rat liver microsome.CONCLUSION The glaucocalyxin A can be metabolite in rat liver and its main metabolism is hydroxyl glaucocalyxin A.
Keywords:Glaucocalyxin A  Liver microsome enzyme  Drug metabolism  High performance liquid chromatography
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