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Metabolism of bicyclol in rat and human liver microsomes in vitro
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 2
- DOI:
- 10.3321/j.issn:0513-4870.2005.02.003
- Key Word:
- 双环醇;代谢产物;细胞色素P450;肝微粒体
Abstract： 目的研究参与双环醇代谢的主要药物代谢酶及代谢动力学参数,分离鉴定双环醇代谢产物.方法双环醇与大鼠和人肝微粒体进行温孵,以高效液相色谱、质谱、核磁共振技术检测并分离鉴定双环醇及其代谢产物.结果双环醇在地塞米松诱导大鼠肝微粒体中的代谢速率显著高于正常大鼠肝微粒体,酮康唑可显著抑制双环醇的代谢.双环醇主要代谢产物为:4-羟基-4′-甲氧基-6-羟甲基-6′-甲氧羰基-2,3,2′,3′-双亚甲二氧基联苯和4-甲氧基-4′-羟基-6-羟甲基-6′-甲氧羰基-2,3,2′,3′-双亚甲二氧基联苯.结论双环醇在大鼠和人肝微粒体的主要代谢产物为4-羟基-4′-甲氧基-6-羟甲基-6′-甲氧羰基-2,3,2′,3′-双亚甲二氧基联苯和4-甲氧基-4′-羟基-6-羟甲基-6′-甲氧羰基-2,3,2′,3′-双亚甲二氧基联苯,细胞色素P450 3A主要参与双环醇代谢.
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