Down-regulation of P-glycoprotein expression contributes to an increase in Danshensu accumulation in the cerebral ischemia/reperfusion brain.

P-glycoprotein (P-gp) plays a key role in the distribution and elimination of many clinically important therapeutic substances. P-gp inhibition is capable of increasing the concentration of various drugs in the brain. Danshensu is a main hydrophilic constituent of Salvia miltiorrhiza Bunge which is used traditionally to treat cerebrovascular diseases. In the present study, the effects of cerebral ischemia/reperfusion on the transport of Danshensu in the brain were observed by assaying the concentration at 15, 30 and 60 min after cerebral ischemia/reperfusion in the brain of rats. Furthermore, the expression of P-gp in the brain was also measured. Results showed that Danshensu concentrations in the ischemic hemisphere significantly increased compared to those in the non-ischemic hemisphere and the brain of the sham group. P-gp expression was inhibited by cerebral ischemia/reperfusion to some extent, and down-regulated much more by Danshensu treatment. The findings indicate that the down-regulation of P-gp expression induced by both cerebral ischemia/reperfusion and Danshensu treatment contributes to the increase of Danshensu accumulation in the brain.

Citation

Yating Chong, Tian Wang, Wenyan Wang, Leiming Zhang, Chong Li, Pengfei Yu, Hongsheng Wang, Fenghua Fu. Down-regulation of P-glycoprotein expression contributes to an increase in Danshensu accumulation in the cerebral ischemia/reperfusion brain. Molecular medicine reports. 2012 Mar;5(3):812-6

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PMID: 22134431

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