臺灣款冬之抗發炎活性研究

The Anti-inflammation principle constituents of Petasites formosanus Kitam.

鄧學聯(Hsueh-Lian Teng)

指導教授 ： 王靜瓊

臺北醫學大學/藥學院/生藥學研究所/碩士(2008年)

摘要

菊科植物被報導指出具有諸多生理活性，如抗腫瘤、抗菌、抗虐以及抗發炎等…，且台灣菊科植物種類繁多，因此本研究將選用30種菊科植物，將其利用50%甲醇迴流萃取，並利用酯多糖來誘導老鼠RAW 264.7巨噬細胞表現iNOS及釋放一氧化氮，並以Griess reaction 分析方法來測NO含量變化。結果顯示：大花咸豐草、南美蟛蜞菊、台灣款冬具有明顯的抑制NO產生，其IC50分別為72.09、41.08、29.57 μg/ml。其中又以臺灣款冬葉萃取物對iNOS的表現具有顯著抑制作用，且於Carrageenan誘導小鼠足掌發炎、醋酸扭體和輻射熱源法等動物實驗中，結果顯示：餵服400 mg/kg之實驗組，在誘導後的 4、5、6小時皆具有意義的抑制足腫反應；而餵服100 mg/kg即有意義的抑制疼痛。進而利用NO抑制活性追縱方式，分離臺灣款冬葉之消炎和止痛活性成份。分離純化結果得到isopetasin、S-isopetasin、S-petasin和caffeic acid methyl ester等活性成份。再以體內、體外試驗評估天然物消炎、止痛作用，結果顯示：S-isopetasin和S-petasin皆會抑制NO的產生，其IC50分別為4.67 μM、4.45 μM，且S-isopetasin和S-petasin具有抑制iNOS及COX-2的表現；於體內實驗中，餵服5mg/kg即具有很明顯的消炎、止痛作用，其中以S-isopetasin作用較為明顯，所以S-isopetasin是一個具有開發為消炎止痛潛力的天然物，而臺灣款冬是經濟價值高的藥用植物。

關鍵字

臺灣款冬 ； 菊科 ； 抗發炎 ； 止痛 ； S-isopetasin ； S-petasin

並列摘要

In Taiwan, several species of Compositae plants are used as Chinese herbs. In this study, 30 kinds of Composite family plants were extracted by 50% MeOH, the anti-inflammatory and analgesic effects of these extracts were measured by in vitro and in vivo models. The nitric oxide (NO) production which induced by LPS-stimulated RAW 264.7 macrophage and quantitatively deteproduction by Griss reaction. Results showed that Bidens pilosa L. var. radiata Sch., Petasites formosanus Kitam., Wedelia trilobata (L.) Hitchc. suppressed NO production from lipopolysaccharide（LPS）induced RAW 264.7 cells and the IC50 values were 72.09, 29.57, 41.08 μg/ml, respectively. P. formosanus (PF) inhibited inducible nitric oxide synthase (iNOS) a expression on LPS induced RAW 264.7 cells but COX-2 not. Therefore, the anti-inflammation effects of PF were evaluated by carrageenan-induced paw edema in mice. PF also significantly inhibited the paw edema after treatment with 400 mg/kg. The analgesic activity evaluated by Acetic acid-induce writhing response in mice and Radiant heat method. PF also significantly exhibited analgesic effects after treatment with 100mg/kg. Continuously, the anti-inflammation principle constituents of PF were isolated by column chromatography combined bioassay-guided fractionation. Four kinds of natural products, isopetasin, S-isopetasin, s-petasin, caffeic acid methyl ester were obtained and S-isopetasin and S-petasin more significant inhibited NO production than the others and IC50 values were 4.67 μM and 4.45 ?nμM and inhibited iNOS and COX-2 expression in LPS induced-RAW 264.7 cells. In vivo studies, S-isopetasin also exhibited anti-inflammatory and analgesic effects and more than effects than S-petasin. Therefore, we suggested S-isopetasin was major anti-inflammatory and analgesic components in PF and was a good lead compound.

並列關鍵字

Petasites formosanus Kitam ； RAW 264.7 ； iNOS ； Carrageenan ； Acetic acid-induce writhing response

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