【作者】 刘抗伦；

【导师】 胡英杰；

【作者基本信息】 广州中医药大学 ， 中药学， 2008， 硕士

【摘要】 牛蒡子（Fructus arctii）为菊科（Compositae）牛蒡属植物牛蒡的干燥成熟果实,属辛凉解表药,具疏散风热、宣肺透疹、消肿解毒之功效;用于治疗风热感冒、咳嗽痰多、咽喉肿痛、斑疹不透、风疹作痒、痈肿疮毒等症。自1929年日本人田川越等从牛蒡子中获得牛蒡苷以来,关于牛蒡化学成分的研究取得了重要进展,前人对化学成分及其抗肿瘤、抗病毒作用进行过研究,从牛蒡种子,茎叶和根中获得了多种化合物,主要有木脂素,脂肪油及有机酸类化合物,硫炔类,挥发油类,倍半萜,三萜,糖,蛋白质等,其中牛蒡子苷和牛蒡子苷元具有多种生物活性。但对其他化学成分的药理报道还不多。为了进一步寻找该植物的有效成分,本项研究对其化学成分进行了分离、鉴定和体外抗肿瘤作用研究,以期有新的发现,为牛蒡子的深入研究和开发应用奠定基础。牛蒡子乙醇提取物的氯仿萃取部分经过硅胶柱层析、反相硅胶柱层析、SephadexLH-20凝胶柱层析、半制备高效液相色谱分离,得到13个化合物。运用光谱分析（UV、MS、ESIMS、1D-NMR,2D-NMR）鉴定了13个化合物的结构,这些化合物分别是:异牛蒡酚C（isolappaol C）（1）、牛蒡酚C（lappaol C）（2）、牛蒡酚H（lappaol H）（3）、油酸（oleie acid）（4）、牛蒡酚F（lappaol F）（5）、牛蒡子苷元（arctigenin）（6）、罗汉松脂素（matairesinol）（7）、牛蒡酚B（lappaol B）（8）、7,8-双脱氢牛蒡苷元[（+）-7,8-didehydroarctigenin]（9）、牛蒡子苷（arctiin）（10）、牛蒡酚E（lappaol E）（11）、异牛蒡酚A（isolappaol A）（12）、牛蒡酚A（lappaol A）（13）。本研究以人慢性髓原白血病细胞K562为靶标,初步测试了从牛蒡子分得的木脂素类化合物对白血病细胞株K562的影响。实验结果显示,lappaol B,isolappaol A,lappaolA对K562细胞的IC₅₀分别为38.5μg/ml,53.5μg/ml,51.1μg/ml。更多还原

【Abstract】 Fructus arctii is the dried seeds of Arctium lappa L. （Compositae）. In theory of traditional Chinese medicine, this medicine can disperse wind-heat from the superficies, smooth the throat and disperse the mass due to retention of evils. Ventilating the lung and facilitating eruption, and remove toxic materials and relieve pyogenic infection of the skin. Many chemical and pharmacologic studies on Fructus arctii have been reported. The chemical constituents of it are lignans, essential oil, fatty acid, sesquiterpene, triterpene, and so on. It was reported that arctigenin and arctiin could be used for anti-virus and anti-tumor . whereas the pharmacological reports of other chemical constituents were insufficient. In this paper, isolation, purification, structural elucidation, in vitro activities of the lignan isolates against tumor cells were investigated.Thirteen compounds were isolated from the ethanol extract of Fructus arctii through repeated silica gel, ODS and Sephadex LH-20 and/or separated by preparative HPLC column chromatographies.From the physico-chemical data, including NMR, MS, UV and IR, the chemical structures of the compounds were determined, as isolappaol C （1）, lappaol C （2）, lappaol H （3）, oleic acid （4）, lappaol F （5）, arctigenin （6）, matairesinol （7）, lappaol B （8）, （+）-7,8-didehydroarctigenin （9）, arctiin.（10） , lappaol E（11）, isolappaol A（12）, and lappaol A（13）.In this study anti-tumor effect was evaluated for the lignans isolated from the seeds of Arctium lappa L. and the cytotoxicity of lappaol B, lappaol A, and isolappaol A to K562 cells was reported for the first time. The results showed that IC₅₀ values of lappaol B, lappaol A, and isolappaol A to K 562 cells were 38.5μg/ml, 53.5μg/ml, 51.1μg/ml, respectively.更多还原