【作者】 王冠；

【导师】 李药兰；

【作者基本信息】 暨南大学 ， 分析化学， 2006， 硕士

【摘要】 本课题对瑶族植物药白马骨（Serissa serissoides）的化学成分和抗病毒、抗肿瘤等生物活性进行了研究。 采用硅胶柱层析、Sephadex LH-20凝胶柱层析、高速逆流色谱（HSCCC）等分离手段结合传统的萃取、重结晶等方法从白马骨的乙醇提取物中分离得到10个单体化合物和1个甾醇混合物。运用波谱手段及化学反应方法鉴定单体化合物分别为：棕榈酸（1）、科罗索酸（2）、胡萝卜甙（3）、乌索烷-12-烯-28-醇（4）、齐墩果酸（6）、β-谷甾醇（7）、乌索酸（8）、对羟基间甲氧基苯甲酸（9）、2，6-二甲氧基-对苯醌（10）和一个长链烷烃（5）。甾醇混合物通过气—质联用（GC-MS）技术分析鉴定为菜油甾醇、4，4-二甲基-胆甾-22，24-二烯-5β-醇和β-谷甾醇的混合物。其中4，4-二甲基-胆甾-22，24-二烯-5β-醇和β-谷甾醇的含量较多，分别占37.8496和45.17％。除了齐墩果酸、乌索酸、和β-谷甾醇外，其余化合物均为首次从该属植物中分离得到。 采用四甲基偶氮唑盐（MTT）比色法及细胞病变（CPE）抑制法，测定了白马骨乙醇提取物不同极性溶剂萃取部位和部分单体化合物的体外抗柯萨奇B3病毒（Cox B3）及抗单纯疱疹病毒1型（HSV-1）的活性。实验结果表明，白马骨大部分供试样品在无毒浓度范围内没有明显的抗Cox B3及HSV-1病毒活性。 采用细胞病变（CPE）抑制法测定了自马骨乙醇提取物不同极性溶剂萃取部位和部分单体化合物的体外抗喉癌细胞株（Hep-2）、人肺癌细胞株（H460）、人肺腺癌细胞（A549）、肝癌细胞株（BEL-7402）、人大肠癌细胞株（Lovo）等肿瘤细胞的活性。实验结果表明，白马骨乙醇提取物的乙酸乙酯萃取部位对Lovo和H460细胞具有较强的抑制作用，CC₅₀值分别为15.6μg/mL和31.25μg/mL，而从乙酸乙酯萃取部位分离得到的单体化合物齐墩果酸对BEL-7402、Hep-2和Lovo细胞也具有一定的抑制作用，CC₅₀均为31.25μg/mL。更多还原

【Abstract】 In this project, the chemical constituents of Serissa serissoides and some biological activities, such as the antiviral activities and anti-cancer activities, were studied.Ten compounds and one sterol mixture were isolated from Serissa serissoides by various chromatographic methods such as silicon gel column chromatography, Sephadex LH-20, high speed countercurrent chromatography (HSCCC), assistant with traditional methods like extraction and recrystalization. The structures of the nine compounds had been identified on the basis of spectral and chemical evidence. They are palmitic acid (1), corosolic acid (2), daucosterol (3), urs-12-en-28-ol (4), oleanolic acid (6), 8-sitosterol (7), uroslic acid (8), 4-hydroxy-3- methoxy- benzoic acid (9), 2,6-dimethoxy-p-benzoquinone (10), and an aliphatic hydrocarbon (5). Based on GC-MS analysis, the sterol mixture had been identified as campesterol, 4, 4-dimethyl-cholesta-22, 24-dien -5-ol and β-sitosterol, among which 4,4-dimethyl-cholesta -22,24 -dien-5-ol and B-sitosterol were the major components, and their contents in the mixture were 37.84% and 45.17%, respectively. The compounds were first isolated from the Serissa Comm expect daucosterol, uroslic acid and oleanolic acid.The inhibitory activities of the ethanol extract, fractions and some isolated compounds against Cox B3 and HSV-1 in vitro were studied by cell culture methods. The cell toxicities of the samples were tested by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphe-nyltetrazolium bromide (MTT) assaying. The inhibitory effects were evaluated by cytopathic effect (CPE) reduction assaying. The results indicated that all the samples did not show any obvious antiviral effects in the range of the experimental concentrations.The inhibitory activities against tumor cells (Hep-2, H460, A549, BEL-7402, Lovo) in vitro were also studied by cell culture methods. The cell toxicities of the更多还原