Effect of baicalin and berberine on transport of nimodipine on primary-cultured, rat brain microvascular endothelial cells

Dong-mei Zhang, Hai-yan Liu, Lin Xie, Xiao-dong Liu
Acta Pharmacologica Sinica 2007, 28 (4): 573-8

AIM: 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.

CONCLUSION: 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.

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