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考察全粉及提取物对正常和特异质(LPS)大鼠胆红素相关转运体Oatp1a1,Oatp1b2和MRP2活性及mRNA表达的影响,探讨首乌藤致肝损伤的可能机制。正常及LPS大鼠分别连续灌胃首乌藤全粉及提取物7 d后,静脉注射转运体底物磺溴酞钠(BSP),测定其药动学参数,考察各转运体的活性,同时取肝组织检测转运体mRNA的表达。结果首乌藤全粉及提取物可使BSP的t_(1/2)和AUC显著升高,CL显著降低;AST和ALT显著性降低;Oatp1a1,Oatp1b2及MRP2的mRNA表达水平明显下降(P<0.05),但未见二者与LPS的协同作用。综上首乌藤及其提取物对胆红素相关转运体功能的抑制作用,可能是其是否造成肝损伤的原因之一。
To investigate the effects of whole meal and extract on the activity of Oatp1a1, Oatp1b2 and MRP2 and the mRNA expression of bilirubin-related transporters in normal and atypical (LPS) rats, and to explore the possible mechanism of liver injury induced by Radix et Rhodioma. Normal and LPS rats were fed gavage and extract for 7 d respectively, and then intravenously injected sulfosalicylate sodium (BSP), which was the transporter substrate. The pharmacokinetic parameters were determined and the activity of each transporter was examined. Meanwhile, Liver tissue was taken to detect the expression of transporter mRNA. Results The total and extract of Amomum villosum could significantly increase t 1/2 and AUC of BSP, CL significantly decreased, AST and ALT decreased significantly, mRNA expression of Oatp1a1, Oatp1b2 and MRP2 decreased significantly (P < 0.05), but no synergies between the two and LPS. In summary, the inhibitory effect of Polygonum vinculifera and its extracts on bilirubin-related transporter function may be one of the reasons for its liver damage.