目的 研究香兰素、乙基香兰素对大鼠肝脏中多药耐药基因Mdr1、多药耐药相关蛋白Mrp2、阴离子转运蛋白Oatp1A1和阳离子转运蛋白Oct1 mRNA表达水平的影响。方法 大鼠ig香兰素或乙基香兰素3、15、75 mg/(kg?d)，连续给药7 d，提取肝脏总RNA，逆转录后荧光定量PCR检测细胞膜Mdr1、Mrp2、Oatp1A1和Oct1 mRNA的表达。结果 香兰素、乙基香兰素均能显著上调Mdr1 mRNA的表达，下调Oatp1A1、Oct1 mRNA的表达，对Mrp2 mRNA的表达无显著影响。结论 香兰素、乙基香兰素给药后能提高肝细胞Mdr1对药物的外排作用，减弱Oatp1A1、Oct1对药物的摄取能力，当香兰素和乙基香兰素与上述转运体底物药物共用时，可能会发生药物相互作用。

Objective To study the effects of vanillin and ethyl vanillin on the mRNA expression levels of multidrug resistance gene Mdr1, multidrug resistance-associated protein Mrp2, organic anion transporter Oatp1A1, and organic cation transporter Oct1 in liver of rats. Methods Wistar rats were ig administered with vanillin or ethyl vanillin at three dosage levels [3, 15, and 75 mg/(kg?d)] for consecutive 7 d, then the mRNA expression levels of Mdr1, Mrp2, Oatp1A1, and Oct1 in liver tissue of rats were detected by reverse-transcriptase fluorescence quantitative PCR. Results Both vanillin and ethyl vanillin had no significant effect on the mRNA expressions of Mrp2, but up-regulated mRNA expression of Mdr1 and down-regulated those of Oatp1A1 and Oct1 markedly. Conclusion Vanillin and ethyl vanillin could increase the drug excretion by Mdr1 in hepatocyte, and attenuate the drug intake capacity by Oatp1A1 and Oct1. The drug interaction is possible when vanillin and ethyl vanillin are used combined with the above transporter substrates.

湖北省自然科学基金资助项目（20107DB07301）