Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China.
School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550004, China.
Molecules. 2017 Oct 10;22(10):1686. doi: 10.3390/molecules22101686.
Dehydrocorydaline (DHC), a quaternary alkaloid from , has been demonstrated to be the active constituent in the treatment of coronary heart disease. In this study, a high-performance liquid chromatography-electrospray ionization-triple quadrupole linear ion trap mass spectrometry (HPLC-ESI-QTRAP MS) technique was used to identify DHC metabolites in plasma and bile after oral administration of DHC to rats. A total of 18 metabolites (M1 to M18) were identified and characterized by LC-MS/MS in the positive ion mode. These 18 metabolites were all present in rat bile, while only 9 were detected in plasma. -demethylation, hydroxylation, di-hydroxylation, glucuronidation of -demethyl DHC, sulfation of -demethyl DHC and di-hydroxylation of dehydro-DHC were the major metabolic pathways of DHC. This is the first time that these metabolites of DHC have been identified in rat plasma and bile, which provides useful information for further analysis of the biotransformation of DHC and other quaternary protoberberine-type alkaloids.
去氢紫堇碱（DHC）是罂粟科紫堇属植物中的一种季铵型生物碱，具有显著的抗心肌缺血作用。本研究采用高效液相色谱-电喷雾串联三重四极杆线性离子阱质谱（HPLC-ESI-QTRAP MS）技术，研究了去氢紫堇碱在大鼠体内的代谢产物。大鼠灌胃给予去氢紫堇碱后，在血浆和胆汁中共鉴定出 18 种代谢产物（M1-M18），通过 LC-MS/MS 在正离子模式下进行了结构鉴定。这些代谢产物均存在于大鼠胆汁中，而仅 9 种在血浆中被检测到。去氢紫堇碱的代谢途径主要为脱甲基化、羟化、二羟化、脱甲基去氢紫堇碱的葡萄糖醛酸化、脱甲基去氢紫堇碱的硫酸化和去氢-DHC 的二羟化。这是首次在大鼠血浆和胆汁中鉴定出这些去氢紫堇碱的代谢产物，为进一步分析去氢紫堇碱和其他季铵型原小檗碱型生物碱的生物转化提供了有用信息。
