中國醫藥大學機構典藏 China Medical University Repository, Taiwan:Item 310903500/969
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    題名: 番瀉葉多酚之代謝動力學及其離體抗自由基活性評估;Pharmacokinetics and Ex-vivo Free Radical Scavenging Effect of Polyphenols in Folium Sennae
    作者: 陳旻玉;Min-Yu Chen
    貢獻者: 中國醫藥大學：藥學系碩士班
    關鍵詞: 番瀉葉;多酚;動力學;自由基;Folium Sennae;polyphenols;pharmacokinetics;free radical
    日期: 2009-06-24
    上傳時間: 2009-08-13 10:54:02 (UTC+8)
    摘要: 番瀉葉之基原為豆科 (Leguminosae) 植物 Cassia angustifolia VAHL 及 Cassia acutifolia DELILE 的小葉，是全球性的常用瀉藥，富含蒽醌多酚，文獻中報導蒽醌多酚具許多優越的體外活性，如抗氧化及抗癌等，但有關其代謝動力學的資訊卻相當有限。
    本研究以大白鼠口服 10 g/kg單劑量及多劑量番瀉葉水煎劑後，於特定時間點採集血清檢體，將血清分別以葡萄糖醛酸酶 (β-glucuronidase) 與硫酸酶 (sulfatase) 水解，並於水解前、後，利用高效液相層析定量。其中蒽醌多酚與其代謝物定量結果顯示，番瀉葉中的 rhein、aloe-emodin 主要以結合態代謝物形式出現於血循環，其中葡萄糖醛酸結合態代謝物居多。Rhein 自由態之血藥面積顯著低於其結合態代謝物，而 aloe-emodin 之自由態僅微量存在。比較單劑量與多劑量給藥之動力學參數，顯示無統計上之顯著差異。
    此外，由於文獻中有關番瀉葉活性之報告，多為體外試驗的結果，對真實存在於體內分子活性的討論相當有限，因此本研究延伸代謝動力學結果，利用大鼠製備番瀉葉之血清代謝物，評估其對 2,2-azobis (2-amidinopropane) hydrochloride (AAPH) 所誘導溶血之作用，結果顯示番瀉葉血清代謝物於藥理濃度下未能抑制 AAPH 誘導之溶血，因此番瀉葉雖含蒽醌多酚，但口服後於體循環系統中並未具抗自由基活性之潛力。

    The leaves of Cassia angustifolia VAHL and Cassia acutifolia DELILE (Leguminosae), used as a potent laxative worldwide, contain several anthraquinone polyphenols. Anthraquinones have been reported to possess various beneficial bioactivities, however, they were mainly based on in vitro evidences. The information concerning the metabolic pharmacokinetics of anthraquinones in Folium Sennae decoction remained limited.
    In order to understand the absorption and disposition of Folium Sennae decoction, the metabolic pharmacokinetic studies were conducted in rats. Rats were administered orally with 10 g/kg single dose and multiple dose of Folium Sennae. The serum concentration of serum samples was assayed by HPLC before and after hydrolysis with sulfatase and β-glucuronidase, respectively. The results showed that the conjugated metabolites were predominantly present in the circulation, mainly glucuronides. The free form of rhein was present but at lower concentration than the conjugation metabolites. Only trace of aloe-emodin free form was detected in serum. Comparison of pharmacokinetic parameters following single-dose and multiple-dose administrations indicated that there were no significant differences between two treatments.
    In addition, to extend the result of metabolic pharmacokinetics, we investigated the effect of the serum metabolites of Folium Sennae decoction at pharmacological concentration on AAPH-induced hemolysis. The result indicated that oral administration of Folium Sennae could not exert promising free radical scavenging effect in vascular system.
    顯示於類別:[藥學系暨碩博士班] 博碩士論文

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