Effect of α-asarone on the Function and Expression of P-glycoprotein in Rat Brain Microvascular Endothelial Cells

Zhongguo yi xue ke xue yuan xue bao. Acta Academiae Medicinae Sinicae
Si Yuan YuanJin Min Liu

Abstract

Objective To investigate the effect of α-asarone on the function and expression of P-glycoprotein(P-gp)in rat brain microvascular endothelial cells(rBMECs). Methods rBMECs were exposed to L-glutamate(100 μmol/L) for 30 mins to induce the overexpression of P-gp/multidrug resistance gene 1a(Mdr1a)on the cell membranes,which mimicked the overexpression of P-gp/Mdr1a in blood brain barrier(BBB) when drug-resistant epilepsy attacked.MTT assay was used to detect the safe range of α-asarone concentration.The model cells were intervened with different concentrations of α-asarone at 12.5,25.0,and 50.0 μg/μl for 24 hours.After the treatment of α-asarone,the expression and the function of P-gp/Mdr1 were measured by Western blotting,real-time PCR,and intracellular rhodamine 123 accumulation assays. Results The rBMECs,stimulated by glutamine,showed a high expression of P-gp(F=1.924,P=0.020)/Mdr1a(F=1.788,P=0.019) compared to the normal rBMECs.The treatment with 25.0(F=1.924,P=0.025;F=1.788,P=0.017) and 50.0 μg/μl(F=1.924,P=0.035;F=1.788,P=0.026) α-asarone significantly depressed the expression of P-gp/Mdr1a.The treatment with 25.0 and 50.0 μg/μl α-asarone significantly increased intracellular accumulation of Rhodamine 123 by 40% and 60% res...Continue Reading

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