Analysis of Biliary Excretion of Icariin in Rats

作者：Wu Yu Tse; Lin Chia Wen; Lin Lie Chwen; Chiu Allen W; Chen Kuang Kuo; Tsai Tung Hu^*

来源：Journal of Agricultural and Food Chemistry, 2010, 58(18): 9905-9911.

DOI：10.1021/jf101987j

• Icariin
• biliary excretion
• P-glycoprotein
• microdialysis

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 = AUC(bilo)/AUC(blood)). 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.

• 出版日期2010-9-22