假地膽草化學成分及細胞毒殺作用之探討

假地膽草(Pseudelephantopus spicatus)屬於菊科，假地膽草屬。主要分佈於南部低海拔開闊處。假地膽草(P. spicatus)在台灣僅一屬一種，目前在台灣民間常用於治療高血糖，藥用部分：根或全草。基於對台灣產草藥所含生物活性成分之探討，我們選擇假地膽草，已其全草作為材料，探討其化學成分及其生物活性作用。由假地膽草全草分離純化得到二十八個化合物，按其骨架，分別為九個sesquiterpenoids: pseudolide A (1)、pitocarphin D (2)、 pseudolide B(3)、8α-acetoxy-10α-hydroxy-13-O-methyl hirsutinolide (4)、spicatolide A (5)、spicatolide C (6)、pseudolide C (7)、pseudolide D (8)和pseudolide E (9)，九個 benzenoids: p-hydroxybenzaldehyde (10)、vanillin (11)、methyl 4-hydroxy-benzoate (12)、 vanillic acid (13)、syringaldehyde (14)、 3,5-dimethoxy-4-hydroxypropiophenone (15)、methyl 4-hydroxy-3,5- dimethoxy-benzoate (16)、caffeic acid (17)和 methyl caffeate (18)，三個 flavonoids: luteolin (19)、tricin (20)和 (-)-epicatechin (21)，兩個 indoles: indole-3-carboxaldehyde (22)、 indole-3-carboxylic acid (23) 和五個steroids: stigamsterol (24)、 ß-stiosterol (25)、stigamsteryl-3-O-ß-D-glucoside (26)、 stiosteryl-3-O-ß-D-glucoside (27)、stigmast-5-en-3-O-ß-D-glucoside tetraacetate (28)。以上所分離的化合物，其中之1、3、6、7、8、9為新化合物，而化合物2、4、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24、26、27、28則為首次於假地膽草屬植物分離得到。而化合物1和6對於肝癌細胞(Hep3B)具有輕微的細胞毒殺作用，並針對其結果且進一步探討其SAR。

關鍵字

假地膽草

並列摘要

Pseudelephantopus spicatus (Juss.) C. F. Baker belongs to Compositae family and is indigenous to Taiwan and distributes at low elevation in open fields in the southern Taiwan. This plant is also a folk medicine for hyperglucagon. Therefore, we chose the plant as our research topic to disclose the bioactive compounds. Twenty nine compounds were isolated from the whole plant, including nine sesquiterpenoids: pseudolide A (1), pitocarphin D (2), pseudolide B(3), 8α-acetoxy-10α-hydroxy-13-O-methyl hirsutinolide (4), spicatolide A (5), spicatolide C (6), pseudolide C (7), pseudolide D (8),and pseudolide E (9), nine benzenoids: p-hydroxybenzaldehyde (10), vanillin (11), methyl 4-hydroxy-benzoate (12), vanillic acid (13), syringaldehyde (14), 3,5-dimethoxy-4-hydroxypropiophenone (15), methyl 4-hydroxy-3,5-dimethoxy-benzoate (16), caffeic acid (17),and methyl caffeate (18), three flavonoids: lutelin (19), tricin (20),and (-)-epicatechin(21), two indoles: indole-3-carboxaldehyde (22), indole-3-carboxylic acid (23),and five steroids: stigamsterol (24), ß-stiosterol (25), stigamsteryl-3-O-ß-D-glucoside (26), stiosteryl-3-O-ß-D-glucoside (27),and stigmast-5-en-3-O-ß-D-glucoside tetraacetate (28). The structures of these compounds were identify by spectral and mass data. Among them, 1, 3, 6, 7, 8, and 9 are new compounds. Compounds 2, 4, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 26, 27,and 28 were isolated from genus of Pseudoelephantopus for the first time. Compounds 1 and 6 exhibited weak cytotoxicity against hepatoma caner cell (Hep3B). The SAR was concluded on the basis of the results cytotoxicity.