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三裂蟛蜞菊Sphagneticola trilobata(L.)Pruski(又名Wedelia trilobata)为菊科(Compositae)蟛蜞菊属(Sphagneticola)植物,原产于南美洲,现已广泛分布于广东、福建、海南、香港、台湾等沿海地区。三裂蟛蜞菊对其它植物有强烈的化感作用,被列为“世界上最有害的100种外来入侵物种”之一。现代药理研究表明,三裂蟛蜞菊提取物具有抗氧化、抗肿瘤、抗炎、抗菌、保肝等作用。民间主要用其来治疗蛇伤、鱼伤、腹泻、肾结石、感冒等疾病。本论文综合运用硅胶柱色谱、ODS中低压反相柱色谱、凝胶柱色谱以及制备高效液相色谱等分离纯化手段及各种波谱学鉴定技术,从三裂蟛蜞菊花的80%乙醇提取物的氯仿萃取层中分离并鉴定68个化合物,它们化学结构分别被鉴定为:(1)倍半萜类:1α-Acetoxy-4α-hydroxy-6α-isobutyryloxy-9β-15α-methylisovaleryloxyprostatolide(1*),1β-Acetoxyl-4a-hydroxy-6β-isobutyryloxy-9a-angelinoyloxyprostatolide(2*),1β-Acetoxy-4α-hydroxy-6β-isobutyryloxy-9β-15α-methylangelinoyloxyprostatolide(3*),1a,9β-Diacetoxyl-4β-hydroxy-6amethacryloxy-11β-methylprostatolide(4*),1a,9β,4a-Trihydroxy-6β-isobutyryloxyprostatolide(5*),1a,6a,9β-Trihydroxy-4,10a-dimethyl-5a,7a,8a-endesm-3-en-8,12-olide(6*),1α,4β,8β-Trihydroxy-6α-isobutyryloxyeudesman-9,12-olide(7*),1α,9β-Dihydroxy-4β-hydroxymethyl-6β-methacryloxy-13β-methyleudesmanolide(8*),1α,4β,6α-Trihydroxy-8β-angeloyloxyprostatolide(9*),1β-Acetoxy-4α,9α-dihydroxy-6β-acetoxyprostatolide(10*),1a,9β-Dihydroxy-6aisobutyroxy-4,10β-dimethyl-5a,7β,8β-endesm-3-en-8,12-olide(11*),1β,9α-Diacetoxy-4α-hydroxy-6β-isobutyroxyprostatolide(12),1β-Acetoxy-4α,9α-dihydroxy-6β-isobutyroxyprostatolide(13),1β-Acetoxy-4α-hydroxy-6β-isobutyryloxy-9α-isovaleryloxyprostatolide(14),1β-Acetoxy-4α,9α-dihydroxy-6β-methacryloxyprostatolide(15),1β,9α-Diacetoxy-4α-hydroxy-6β-methacryloxyprostatolide(16),Trilobolide-6-O-isobutyrate(17),1β,9α-Diacetoxy-4α-hydroxy-6β-methacryloxyprostatolide(18),Oxidoisotrilobolide-6-O-methacrylate(19),Oxidoisotrilobolide-6-O-isobutyrate(20),Oxidoisotrilobolide-6-Oisobutyrate(21),1α,4β-Dihydroxy-6α-isobutyryloxy-8β-angeloyloxyprostatolide(22)。(2)二萜类:Kauradien-9(11),16-oic acid(23),Kaur-16-en-19-oic acid(24),3α-Angeloyloxy-ent-kaur-16-en-19-oic acid(25),3α-Tiglinoyloxy-ent-kaur-16-en-19-oic acid(26),3α-Cimnamoyloxy-ent-kaur-16-en-19-oic acid(27),ent-9α-Hydroxy-16-kauren-19-oic acid(28),3α-Angeloyloxy-9β-hydroxyent-kaura-16-en-19-oic acid(29),3α-Tiglinoyloxy-9β-hydroxyent-kaura-16-en-19-oic acid(30),Tetrachyrin(31)。(3)三萜类:3β-O-palmitoyl-1β-amyrin(32),3,4-seco-19(10→9)abeo-8α,9β,10α-eupha-4,24-dien-3-ol(33),Glut-5-en-3β-ol(34),3α-Acetoxy-27-hydroxylup-20(29)-en-28-oic acid methylester(35)。(4)黄酮类:4¢,6,7,8-Tetramethoxyfavones(36),3¢,8-Dimethoxyl-3,4¢,6-trihydroxyquercetin(37),3¢,8-Dimethoxy-4¢,6-dihydroxyflavone(38),(2R)-5¢,8-Dihydroxy-3¢-methoxyflavanone(39),Liquiritigenin(40),2,4,4¢-Trihydroxychalcone(41)。(5)其它类:1-[(2R,5R)-5-((E)-5-Hydroxy-3-(hydroxymethyl)pent-3-en-1-yl)-4-methylenetetrahydrofuran-2-yl]propan-2-one(42*),[(9R,3E,6Z)-8-Methyl-8-((E)-4-oxopent-2-en-1-yl)-5,8-dihydro-2H-oxocin-3-yl]methyl acetate(43*),[9R,3E,6Z)-3-(hydroxymethyl)-8-methyl-5,8-dihydro-2H-oxocin-3-yl]pent-3-en-2-one(44*)(2R)-1-(4-(Hydroxymethyl)-3,6-dihydro-2H-pyran-2-yl)propan-2-one(45*),4-((5R)-5-(Hydroxymethyl)-2,5-dihydrofuran-3-yl)butan-2-ol(46*),3-Indole formaldehyde(47),8-Hydroxy-3-methoxy-5H-pyrido[2,1-c]pyrazin-5-one(48),Methyl-(7S)-hydroxyhexadeca-8E,10Z,13Ztrienoate(49),Stigmasterol(50),Ergosta-7,24(24¢)-dien-3β-ol(51)。Syringaresinol(52),Mediolipin(53),2,6,2¢,6¢-Tetramethoxy-4,4¢-bis(2,3-epoxy-1-hydroxypropyl)biphenyl(54),Syringaresinol-O-β-Dglucopyroside(55),7-Methoxy-8-hydroxycoumarin(56),Bis(2-ethylhexyl)phthalate(57),Vanillin(58),p-Hydroxyacetophenone(59),7-Hydroxychromogen(60),Amyl benzoate(61),4-Allyl-2,6-dimethoxyphenol-β-D-glucopyranoside(62),Ethyl linoleate(63),Methyl heptadecanoate(64),6,9-Heptadecadiene(65),Linolenic acid(66),Methyl linoleate(67),Trilinolein(68)。在分离得到的68个化合物,萜类35个,包括倍半萜22个(1-22)、二萜9个(23-31)、三萜4个(32-35),黄酮6个(36-41),其他类27个(42-68)。其中化合物1-11、42-46为16个新化合物。我们对化合物1-8、12-31进行了体外抗炎和抗肿瘤活性的测试,并对化合物1-3进行克隆形成存活和细胞形态测定。结果显示,化合物2(IC50 13.85±1.63μmol/L)、16(IC50 7.06±1.39μmol/L)、19(IC5011.69±0.20μmol/L)、20(IC50 9.67±0.31μmol/L)和21(IC50 16.53±0.61μmol/L)对Hep G2肿瘤细胞的增殖显示了较强的抑制活性,化合物1-3对Hep G2细胞的群落数呈剂量依赖性降低,诱导细胞产生凋亡。化合物6(IC50 11.77±0.83μmol/L)和25(IC50 24.03±1.46μmol/L)对LPS诱导的BV-2细胞的NO产生显示较强的抑制活性。