丹参酮ⅡA在大鼠肺脏和肝脏细胞器的分布  

Subcellular Distribution of Tanshinone IIA in Rat Lung and Liver

作　　者：王颖[1] 吴昭怡[1] 覃小玲[1] 陈孝[1] 

机构地区：[1]中山大学附属第一医院药学部,广东广州510080

出　　处：《今日药学》2011年第11期664-667,共4页Pharmacy Today

基　　金：广东省自然科学基金(编号:8151008901000167);广东省中医药局建设中医药强省科研课题重点项目(编号:2009159);广东省医院药学研究基金(编号:2011A25)

摘　　要：目的考察丹参酮ⅡA在大鼠肺脏、肝脏细胞器的分布,以探讨丹参酮ⅡA在大鼠肺脏高浓度储留的机制。方法雄性SD大鼠经颈静脉给予6 mg/kg丹参酮ⅡA,给药后分批处死,取其肝、肺组织,差速离心法分离细胞器,高效液相色谱-串联质谱(LC-MS/MS)法测定丹参酮ⅡA的浓度。结果给药后,丹参酮ⅡA在肺脏的浓度远高于在肝脏的浓度。丹参酮ⅡA在肝脏细胞器中主要以结合型的形式存在,在肺脏中则是原型稍多。丹参酮ⅡA在大鼠肝脏的微粒体和溶酶体部分分布较多,但是无明显的蓄积部位;而在肺脏丹参酮ⅡA主要分布于细胞器的轻线粒体部分。结论丹参酮ⅡA主要蓄积于肺脏细胞器的轻线粒体部分,而在肝脏细胞器无明显蓄积部位。这是TSⅡA在大鼠肺脏细胞器蓄积的可能机制。Objective To study the subcellular distribution of tanshinone IIA in rat lung and liver.Methods After intravenous administration of 6 mg/kg tanshinone IIA,the rats were sacrificed after dosing.Cell fractions of the lung and liver tissue were produced by differential centrifugation.Tanshinone IIA concentrations were determined using the validated LC-MS/MS method.Results Tanshinone IIA concentrations in lung and its organelles were much higher than that in liver and its organelles after administration.Tanshinone IIA in liver and its organelles was predominantly presented as glucuronidated metabolites,while the concentrations of unchanged tanshinone IIA were slightly higher than that of glucuronided form in lung and its organelles.There was no selective drug accumulation in liver organelles.Additionally,tanshinone IIA accumulated in light mitochondria in lung organelles.Conclusion The light mitochondria is the major accumulation site for tanshinone IIA in rat lung organelles,which is the possible mechanism of high concentration accumulation of tanshinone IIA in rat lung.

关 键 词：丹参酮ⅡA 药代动力学 细胞器分布 

分 类 号：R285[医药卫生—中药学]