The Antinociceptive and Anti-Inflammatory Activities of Petasites Formosanus Kitamura Extract

臺灣款冬之抗發炎與止痛主成分

林時宜(Shyr-Yi Lin) ； 鄧學聯(Hsueh-Lian Teng) ； 曾頌惠(Sung-Hui Tseng) ； 陳立耿(Lih-Geeng Chen) ； 王靜瓊(Ching-Chiung Wang)

《Botanical Studies》 53卷4期 (2012/10) Pp. 431-438

摘要

臺灣款冬（菊科）是一種臺灣原生種的植物，且為臺灣民間用來治療高血壓與氣喘的草藥。臺灣款冬的葉子以50%甲醇萃取（葉萃取物）顯示具有極強抑制脂多醣誘導RAW 264.7巨噬細胞引起的一氧化氮釋放作用，其50%的抑制濃度為22.85μg/mL。繼而利用體內試驗檢測其功效，結果顯示管餵老鼠200mg/kg萃取物可以有意義的降低醋酸誘導的扭體反應、熱板引起的疼痛刺激及鹿角菜膠誘導的足掌浮腫。因此利用管柱層析配合生物活性分析追蹤分離臺灣款冬葉萃取物中的抗發炎活性成分，結果得到4個化合物，分別是isopetasin、S-isopetasin、S-petasin及caffeic acid methyl ester。其中，S-isopetasin和S-petasin於抑制脂多醣誘導RAW 264.7巨噬細胞試驗中具較強的抑制一氧化氮釋放、誘導型一氧化氮合成酶及環氧化酶作用，且顯示劑量依存性，而S-isopetasin的作用又比S-petasin強。綜合而言，臺灣款冬具有抗發炎及止痛作用，其主要的活性成分為S-isopetasin，且其葉部具發展成抗發炎先驅藥之潛力。

關鍵字

臺灣款冬 ； 菊科 ； 止痛 ； 抗發炎作用

並列摘要

Petasites formosanus Kitamura (Compositae) is native to Taiwan and is used in folk medicine to treat hypertension and asthma. Aqueous methanolic (50%) extracts of leaves of P. formosanus (Leaves-MeOH extract) showed the strongest inhibitory effect against NO production by lipopolysaccharide (LPS)-induced RAW 264.7 cells with an IC50 of 22.85 μg/mL. In an in vivo assay, 200 mg/kg of the extract also significantly decreased the acetic acid-induced writhing response, increased the hot-plate latency, and significantly suppressed carrageenan-induced paw edema. The principle anti-inflammatory constituents of the leaf extract were isolated by column chromatography combined with bioassay-guided fractionation, and 4 compounds, isopetasin, S-isopetasin, S-petasin, and caffeic acid methyl ester, were obtained. S-Ispopetasin and S-petasin more significantly inhibited NO production, inducible nitric oxide synthase, and cyclooxygenase-2 expression in a dose-dependent manner in LPS-induced RAW 264.7 cells, and S-ispopetasin showed stronger potency than S-petasin. S-Isopetasin also showed stronger reductions in the acetic acid-induced writhing response and carrageenan- induced paw edema than S-petasin. Taken together, the results indicate that P. formosanus possesses both anti-inflammatory and anti-nociceptive activities, and S-isopetasin was the major constituent mediating those activities and may be used as a lead for new anti-inflammatory drug development.

並列關鍵字

Anti-inflammation ； Antinociceptive ； Compositae ； Petasites formosanus Kitamura ； S-isopetasin ； S-petasin