中 文 摘 要 芸香?為一具多種生物活性的黃酮類配醣體，槐花中有豐富的含量。本研究以大白鼠口服芸香?、槐花水煎劑及槐花濃縮散劑，比較其動力學之差異。結果顯示，槐花水煎劑及濃縮散劑之吸收均優於芸香?，而濃縮散劑之吸收又比水煎劑為佳。 環孢靈為治療指數狹窄的免疫抑制劑，其代謝及吸收與CYP3A及P-glycoprotein有關。因許多研究顯示槲皮素會影響CYP3A及P-glycoprotein之活性，本研究以大白鼠單服環孢靈及分別併服槲皮素、槐花水煎劑，探討其對環孢靈動力學之影響，環孢靈血中濃度以螢光偏極免疫法定量。結果顯示併服槲皮素時，平均血藥面積降低43.3 %，而併服槐花水煎劑則降低63.6 %。 吞噬細胞分泌的NO、TNF-α及IL-12是發炎反應中重要的訊息傳遞者。本研究以兔體製備芸香?之主要代謝物quercetin glucuronides/sulfates進行體外實驗，探討其對活化的巨噬細胞產生NO、TNF-α及IL-12之能力的影響。結果顯示，槲皮素結合態代謝物會抑制NO、TNF-α及IL-12的生成。另外以小白鼠長期給予槐花水煎劑後，測定血液中巨噬細胞之活性。結果顯示，給予槐花水煎劑後，血中巨噬細胞的吞噬活性會降低。由體外及體內的實驗結果顯示，槐花具有調節吞噬細胞功能之作用，進而影響免疫反應之進行。; Rutin is a flavonoid glycoside with many biological activities and is abundant in Huaimi (Sophora japonica L). The oral pharmacokinetics of rutin, Huaimi decoction and commercial extract were studied and compared in rats. The result showed that the absorption of Huaimi decoction or commercial extract was better than that of rutin, and the absorption of commercial extract was superior to decoction. Cyclosporine is a commonly used immunosuppressive agent with narrow therapeutic range. Its metabolism and absorption is related to CYP3A and P-glycoprotein. It was reported that quercetin affected the activity of CYP3A and P-glycoprotein. In this study, the rats were given cyclosporine alone and coadministration with quercetin, Huaimi decoction, respectively. The blood cyclosporine concentration was determined by fluorescence polarization immunoassay. The result showed that the mean area under blood concentration-time curve of cyclosporine was decreased by 43.3 % after coadministration of quercetin, and by 63.3 % after coadministration with Huaimi decoction. NO, TNF-α and IL-12 secreted by phagocytes are important cytokine signals in inflammation. The effect of quercetin conjugates on the production of NO, TNF-α and IL-12 by activated macrophages was investigated in vitro. Quercetin glucuronides/sulfates was prepared by using rabbit. The results indicated that quercetin conjugates inhibit the production of NO, TNF-α and IL-12. Moreover, the effect of Huaimi decoctionon on the phagocytic activity of macrophage in the blood was studied by its daily administration to mice for up to 3 months. The result showed that the phagocytic activity was decreased. Both in vivo and in vitro studies implied that Huaimi might affect the immune response through regulating the function of phagocytes.
