Effect of Danshensu borneol esteron P-glycoprotein expression level in rat brain
10.3969/j.issn.1001-1978.2017.08.015
- VernacularTitle:丹参素冰片酯影响大鼠脑组织P-糖蛋白表达研究
- Author:
Zheng ZHANG
;
Li YANG
;
Kaili ZHU
;
An ZHOU
;
Ailing HUI
;
Wencheng ZHANG
;
Zeyu WU
- Keywords:
Danshensu;
borneol;
Danshensu borneol ester;
drug combination;
brain targeting;
P-glycoprotein;
Western blot
- From:
Chinese Pharmacological Bulletin
2017;33(8):1114-1119
- CountryChina
- Language:Chinese
-
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.
