臺灣款冬之抗發炎活性研究

臺灣款冬之抗發炎活性研究

 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 i NOS 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 I C50 分別為 72.09 、 41.08 、 29.57 μg/ml 。其中又以臺灣款冬葉萃取物對 iNO S 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 caf feic 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 C OX-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。

The Anti-inflammation principle constituents of Petasites formosanus Kitam.

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In Taiwan, several species of Compositae plants are used as Chinese herbs. In this study, 30 ki nds of Composite family plants were extracted by 50% MeOH, the anti-inflammatory and anal gesic 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 quantitativel y deteproduction by Griss reaction. Results showed that Bidens pilosa L. var. radiata Sch., Pet asites formosanus Kitam., Wedelia trilobata (L.) Hitchc. suppressed NO production from lipop olysaccharide （ 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 e

xhibited analgesic effects after treatment with 100mg/kg. Continuously, the anti-inflammation

principle constituents of PF were isolated by column chromatography combined bioassay-guid

ed fractionation. Four kinds of natural products, isopetasin, S-isopetasin, s-petasin, caffeic aci

d methyl ester were obtained and S-isopetasin and S-petasin more significant inhibited NO pro

duction 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 exhibit

ed 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.