分析淫羊藿苷在大鼠体内的胆汁排泄情况。

Analysis of biliary excretion of icariin in rats.

机构信息

Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan.

出版信息

J Agric Food Chem. 2010 Sep 22;58(18):9905-11. doi: 10.1021/jf101987j.

DOI:10.1021/jf101987j

PMID:20735037

Abstract

Icariin is a bioactive herbal ingredient isolated from Epimedii Herba. This study evaluates the distribution of icariin in rats by microdialysis sampling and high-performance liquid chromatography with ultraviolet detection (HPLC-UV). Microdialysis probes were simultaneously placed in the jugular vein, brain striatum, and bile duct of each anesthetized rat for sampling after the administration of icariin (dose=10 or 20 mg/kg) via the femoral vein. The role of P-glycoprotein (P-gp) on icariin distribution was assessed by pretreatment with cyclosporine (CsA, dose=20 mg/kg). This study is the first report of the biliary excretion of icarin in rats, defined as the blood-to-bile distribution (k value), calculated by dividing the area under the concentration-time curve (AUC) of icariin in bile by that in blood (k=AUCbile/AUCblood). The k values were 19.0±5.9 and 18.8±3.8 at the doses of 10 and 20 mg/kg, respectively. The decreased biliary excretion of icariin due to pretreatment with CsA was evidenced by the reduced k values (18.8±3.8 vs 9.9±1.9, p=0.005). This work demonstrates that biliary excretion is the major elimination pathway for icariin disposition and that transporters, such as P-gp, might be related to icariin's biliary excretion.

摘要

朝藿定 C 是从淫羊藿中提取的一种生物活性草药成分。本研究通过微透析采样和高效液相色谱-紫外检测（HPLC-UV）评估了朝藿定 C 在大鼠体内的分布。在麻醉大鼠的颈静脉、纹状体和胆管中同时放置微透析探针，在通过股静脉给予朝藿定 C（剂量=10 或 20mg/kg）后进行采样。通过预先给予环孢菌素（CsA，剂量=20mg/kg）评估 P 糖蛋白（P-gp）对朝藿定 C 分布的作用。这是首次报道大鼠胆汁中朝藿定 C 的排泄，定义为胆汁与血液的分布（k 值），通过将朝藿定 C 在胆汁中的浓度-时间曲线下面积（AUC）除以血液中的 AUC（k=AUCbile/AUCblood）来计算。在 10 和 20mg/kg 的剂量下，k 值分别为 19.0±5.9 和 18.8±3.8。CsA 预处理导致朝藿定 C 的胆汁排泄减少，表现为 k 值降低（18.8±3.8 比 9.9±1.9，p=0.005）。这项工作表明胆汁排泄是朝藿定 C 处置的主要消除途径，转运体（如 P-gp）可能与朝藿定 C 的胆汁排泄有关。