【作者】 王世盛；

【导师】 韩秀文； 梁鑫淼；

【作者基本信息】 中国科学院研究生院（大连化学物理研究所） ， 有机化学， 2004， 博士

【摘要】 藏茵陈是传统高寒藏药，在治疗肝胆疾病方面具有独特疗效。龙胆科植物抱茎獐牙菜是我国青藏高原特有植物，常作为藏茵陈的主要原料入药，临床治疗急慢性肝炎疗效显著。为充分阐释藏茵陈的化学物质基础，本论文对抱茎獐牙菜的活性组分进行了系统的制备分离和化学表征，主要工作如下： 首先建立了药材甲醇粗提物的HPLC-UV-MS联用分析方法，获得了粗提物中各种成分的结构信息，为确定分离制备的目标和策略提供了依据。利用各种硅胶层析方法从药材脂溶性部位中分离制备了14个单体，包括11个（口山）酮甙元，其中7个为首次从抱茎獐牙菜中分离得到。从药材正丁醇萃取部位中分离表征了24个化合物，其中包括2个新（口山）酮甙和2个新环烯醚萜甙，有4个环烯醚萜甙、7个（口山）酮甙、1个黄酮甙及赤矢车菊素为首次从抱茎獐牙菜中分离到。用HPLC-UV-MS技术对分离到的一个环烯醚萜组分进行了在线分析表征，推测了其中两个微量新环烯醚萜甙的结构。 用单扫描示波极谱法和荧光分光光度法测定了Bellidifolin等5种（口山）酮甙元的抗自由基作用，结果均表现出较强的抑制超氧阴离子自由基和羟基自由基作用。通过缺血性脑损伤动物模型的药理研究，首次发现Bellidifolin具有较强的脑保护作用，显示了良好的应用前景。论文还归纳总结了天然氧代（口山）酮及其甙类化合物的¹H和¹³C核磁共振谱学规律，为（口山）酮类化合物的核磁共振表征提供了理论依据。更多还原

【Abstract】 ’Zang-Yin-Chen’ ( ZYC) is a traditional Tibetan medicine for the treatment of hepatitis and cholecystitis. The plant Swertia franchetiana Smith (family Gentianaceae) is distributed in Qinghai-Tibet Plateau and used as plant materials of ZYC. In order to clarify the chemical foundation of this herb, the dissertation describes the preparation, isolation and characterization of bioactive principles from S. franchetiana. The main research results are as follows:The methanol crude extract of ZYC was screened by means of combined HPLC-UV-MS technique. The structural information was obtained from on-line UV and MS spectra at the early stage of preparative isolation. Phytochemical investigation of liposoluble fractions of the methanol extracts led to the isolation of fourteen pure compounds including eleven xanthone aglycones, of which seven compounds were isolated from this plant for the first time. Additional twenty-four compounds were isolated and characterized from n-BuOH fractions of methanol extracts from ZYC. Among them, two new iridoid glycosides and two new xanthone glycosides were obtained by means of preparative HPLC. The other 4 iridoid glycosides and 7 xanthone glycosides, together with isovitexin and erythrocentaurin, were all firstly found from this plant. Besides, two minor compounds from an aqueous fraction were tentatively identified as two new iridoid glycosides by means of HPLC-UV-MS analysis.Five xanthones from this plant were tested for the properties of radical scavenging by means of oscillopolarography and fluorescent spectrophotometry, and showedcapacity to scavenge both superoxide anion radical and hydroxyl radical. Bellidifolin was further tested for the protective activity on cerebral-ischemia animals in vivo. The results revealed that Bellidifolin possessed potent brain-protective activity and showed prospects of pharmaceutical application.The 1H and 13C NMR data of natural xanthones from ZYC and literatures were analyzed and summarized. Some rules of 1H and 13C chemical shifts were deduced in order to supply a theoretic reference for the NMR characterization of natural xanthone compounds.更多还原