新药用资源菠萝叶对小鼠相关药物代谢酶的诱导作用  

CYPs Induction of Polyphenol Extract from New Medicinal Resource Ananas Comosus Leaf on Mice

作　　者：姜敬非[1] 王玉刚[1] 胡珺[1] 冯天师[1] 卢希[1] 袁梽漪[1] 詹宏磊[1] 李慧玉[1] 雷帆[1] 邢东明[1] 杜力军[1] 

机构地区：[1]清华大学蛋白质科学教育部重点实验室/生命科学学院医学院药物药理研究室,北京100084

出　　处：《世界科学技术-中医药现代化》2012年第6期2149-2153,共5页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：科学技术部国家"十二五"计划"重大新药创制"科技重大专项(2012ZX09103-201-041):糖脂代谢新药BLP的研究;负责人:邢东明;清华大学SRT项目(121T0450):新药用资源菠萝叶对小鼠药物代谢酶表达的影响;负责人:杜力军

摘　　要：目的:观察菠萝叶对小鼠肝脏药物代谢酶CYP1A2、2E1和3A11的诱导表达及其活性作用,为药物相互作用提供实验依据。方法:采用整体动物实验方法,灌胃给予不同剂量的菠萝叶酚,取肝脏做mRNA和蛋白的表达。同时制备粗酶液,以相应的特异性底物探针观察相关酶活的影响。结果:小鼠连续灌胃给药3天,对CYP 2E1的mRNA表达有一定的诱导作用,但对蛋白表达及其活性没有明显影响;对CYP 1A2活性有一定的诱导作用,但对mRNA及蛋白无明显影响;对CYP 3A11的诱导作用不明显。结论:菠萝叶酚对CYP 1A2和2E1部分指标有一定的影响,表明其作用具有一定的复杂性,尚需进一步深入研究。This study was aimed to determine the induction of polyphenol extract from Ananas comosus leaf, which is a new medicinal resource, on CYP1A2, 2E1 and 3A11 in order to present data for possible interaction between Ananas cornosus leaf and other drugs. After oral administration of the extract for 3 days, the liver was removed for the detection of CYP1A2, 2El and 3A11. Expressions of mRNA （qPCR assay） and protein （Western blot assay） were carried out. Phenacetin （CYP 1A2）, chlorzoxazone （CYP 2El） and erythromycin （CYP 3A11） were employed for the enzyme activity of CYP 1A2, CYP 2E1 and CYP 3A11, respectively. It was shown that the extract promoted the mRNA expression of CYP 2E1, enhanced the activity of CYP 1A2. These complex effects need to be studied further.

关 键 词：菠萝叶 肝药酶 小鼠 诱导作用 

分 类 号：R285.5[医药卫生—中药学]