中国药理学通报2017，Vol.33Issue(8)：1114-1119,6.DOI:10.3969/j.issn.1001-1978.2017.08.015
丹参素冰片酯影响大鼠脑组织P-糖蛋白表达研究
Effect of Danshensu borneol esteron P-glycoprotein expression level in rat brain
摘要
Abstract
Aim To investigate the relationship between the brain targeting effect and P-glycoprotein(P-gp)expression level of Danshensu borneol ester(DBE)and the combination use of sodium Danshensu and borneol(SDSS-B).Methods The liquid chromatography mass spectrometry(LC-MS)method was applied to investigate the accumulation of Danshensu(DSS)in rat brain tissues after intravenous injection of DBE,SDSS-B and SDSS.Also their effect on regulating the expression level of P-gp in rat hippocampus was investigated using Western blot.Results The brain targeting effect of DBE,SDSS-B was qualitatively analyzed through the brain distribution of DSS,and the result was DBE(SDSS-B)>SDSS(P<0.01).Meanwhile,the brain distribution of DBE group was slightly lower than SDSS-B group at 15 min,while at 30 min DBE was higher than that of SDSS-B.DBE demonstrated a better slow release property compared to SDSS-B.Western blot analysis indicated that DBE,SDSS-B were more effective in inhibiting the expression of P-gp than SDSS in rat hippocampus(P<0.01 vs control or SDSS group),and the lowest P-gp expression was obtained with(47.58±2.28)％and(46.54±1.41)％at 45 min after administration of DBE or SDSS-B.Once the administration time was extended to 60 min,the inhibitory effect on P-gp expression of DBE was stronger than SDSS-B[(85.04±1.42)％vs(95.29±0.98)％].However,no significant inhibition of P-gp expression in rat hippocampus was found throughout the treatment of SDSS(P>0.05 at 5,15,45,60 min,vs control group).Conclusion An attenuated expression level of P-gp can be realized by DBE and SDSS-B,which is advantageous to their brain targeting.关键词
丹参素/冰片/丹参素冰片酯/联合用药/脑靶向/P-糖蛋白/蛋白免疫印迹法Key words
Danshensu/borneol/Danshensu borneol ester/drug combination/brain targeting/P-glycoprotein/Western blot分类
医药卫生引用本文复制引用
张郑,杨黎,朱凯莉,周安,惠爱玲,张文成,吴泽宇..丹参素冰片酯影响大鼠脑组织P-糖蛋白表达研究[J].中国药理学通报,2017,33(8):1114-1119,6.基金项目
国家自然科学基金资助项目(No 21302037) （No 21302037）
安徽省科技重大专项项目(No 16030701072) （No 16030701072）
