Danshensu (3-(3, 4-dihydroxyphenyl)
lactic acid), a water-soluble active component isolated from the root of Salvia miltiorrhiza Bunge, is widely used for the treatment of
cerebrovascular diseases. The present study aims to investigate the role of
P-glycoprotein in transport of
Danshensu across the blood-brain barrier. Sprague-Dawley rats were pretreated with
verapamil at a dose of 20 mg kg(-1) (
verapamil group) or the same volume of
normal saline (control group). Ninety minutes later, the animals were administrated with
Danshensu (15 mg kg(-1)) by
intravenous injection. At 15 min, 30 min, and 60 min after
Danshensu administration, the levels of
Danshensu in the blood and brain were detected by high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). The results showed that
Danshensu concentrations in the brain of the rats pretreated with
verapamil were significantly increased. In addition, the brain-plasma ratios of the group pretreated with
verapamil were much higher than that of the control group. There was no difference in
Danshensu level in plasma between the
verapamil group and control group. The findings indicated that
Danshensu can pass the blood-brain barrier, and
P-glycoprotein plays an important role in
Danshensu transportation in brain.