Effect of baicalin and berberine on transport of nimodipine on primary-cultured, rat brain microvascular endothelial cells.
OBJECTIVE
To investigate whether baicalin and berberine affects the transport of nimodipine (NMD) across the blood-brain barrier (BBB).


METHODS
Primary-cultured, rat brain microvascular endothelial cells (rBMEC) were used as an in vitro model of the BBB. When cells became confluent, the steady-state uptake of NMD by rBMEC with or without baicalin and berberine was measured. The effects of baicalin and berberine on the efflux of NMD from rBMEC were also studied.


RESULTS
Baicalin (2-5 microg/mL) increased the uptake of NMD, and baicalin (10-20 microg/mL) decreased the uptake. The steady-state uptake of NMD was higher than that of control group in the presence of 0.01-1 microg/mL berberine, but was lower in the presence of 2-10 microg/mL berberine.


CONCLUSIONS
The bidirectional effect of baicalin and berberine on the uptake of NMD by rBMEC was found. Higher concentration showed an inhibitory effect, and lower concentration demonstrated an increasing effect.
Zhang
Dong-mei
DM
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
Liu
Hai-yan
HY
Xie
Lin
L
Liu
Xiao-dong
XD
D000818:Animals; D001599:Berberine / Q000494:pharmacology*; D001812:Blood-Brain Barrier / Q000187:drug effects; D001921:Brain / Q000166:cytology / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000378:metabolism*; D002196:Capillaries / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D002478:Cells, Cultured; D002560:Cerebrovascular Circulation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism*; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D005419:Flavonoids / Q000494:pharmacology*; D009553:Nimodipine / Q000378:metabolism*; D020011:Protective Agents / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D002121:Calcium Channel Blockers; D005419:Flavonoids; D020011:Protective Agents; D001599:Berberine; C038044:baicalin; D009553:Nimodipine