,Effect of baicalin and berberine on transport of nimodipine on primary-cultured, rat brain microvas

• 作 者: Dong-mei ZHANG Hai-yan LIU Lin XIE Xiao-dong LIU
• 机 构: Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Chi
• 出 处: 中国药理学报（英文版）
• 发表日期: 2007年4期
• 关键词: nimodipine baicalin berberine P-glycoprotein

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 ef-fects of baicalin and berberine on the efflux of NMD from rBMEC were also studied.Results: Baicalin (2-5 μg/mL) increased the uptake of NMD, and baicalin (10-20 μg/mL) decreased the uptake. The steady-state uptake of NMD was higher than that of control group in the presence of 0.01-1 μg/mL berberine, but was lower in the presence of 2-10 μg/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.