淫羊藿苷在大鼠体内的代谢

METABOLISM OF ORALLY ADMINISTERED ICARIIN IN RATS

摘要: 目的：为阐明淫羊藿苷在体内的作用形式，对淫羊藿苷的代谢产物及活性进行研究。方法：将淫羊藿苷给大鼠ig后，分析、分离并鉴定了其在小肠、尿、胆汁中的主要代谢产物。结果：在小肠及尿中鉴定有淫羊藿次苷II(icariside II)及淫羊藿素(icaritin)，胆汁中有淫羊藿素3-O-α-L-鼠李吡喃糖基-7-O-β-D-葡萄吡喃糖醛酸苷(icaritin 3-O-α-L-rhamnopyranosyl-7-O-β-D-glucopyranuronoside)和淫羊藿次苷II，并对淫羊藿苷在大鼠体内主要代谢途径进行了探讨。结论：淫羊藿苷在吸收之前已发生代谢，在体内主要是以其代谢产物的形式存在。

Abstract: AIM: To evaluate the pharmacological action of icariin in traditional Chinese medicines. METHODS: Icariin was given orally to rats, the major metabolites of icariin in gastric, small intestinal, urine and bile samples were determined and isolated by HPLC and identified by chemical and spectroscopic evidences. RESULTS: Two metabolites, icariside II and icaritin in both small intestine and urine, and two metabolites, icaritin-3-O-α-L-rhamnopyranosyl-7-O-β-D-glucopyranuronoside and icariside II in bile were identified. The major metabolic route of orally administered icariin in rats was also proposed. CONCLUSION: Icariin is metabolized prior to absorption and exists mainly as its metabolites in vivo.