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。
OBJECTIVE To study the metabolism of glaueocalyxin A in rat liver microsome and bile.METHODS The metabolic transformarion 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 HPIE method was established to analyze the parent drug and its metabolites. RESULTS The major metabolites were isolated and purified by liquid- liquid extraction, preparative HPIE, 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.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2006年第3期227-229,共3页
West China Journal of Pharmaceutical Sciences
基金
国家科技部863计划"创新药物和中药现代化"新药博士基金资助课题(2003AA2Z3518)
关键词
蓝萼甲素
肝微粒体酶
药物代谢
高效液相色谱法
Glaucocalyxin A
Liver microsome enzyme
Drug metabolism
High performance liquid chromatography
