【作者】 陈海永；

【导师】 赵昱； 周长新；

【作者基本信息】 浙江大学 ， 药物化学， 2005， 硕士

【摘要】 本论文由两部分组成,第一部分介绍了自1907年以来香薷属植物的研究进展及作者对香薷属植物中的四方蒿进行的化学成分研究,共从该植物中分离得到了24个化合物,鉴定了其中18个。第二部分介绍了黄酮类化合物的药理活性研究概况,并对四方蒿中总黄酮提取工艺进行了研究和优化,以适应工业化大生产的需求。 第一部分 四方蒿化学成分的研究 四方蒿(Elsholtzia blanda),又名四棱蒿、滇香薷、白香薷、鸡肝散等,全株有香气,茎四棱形,为唇形科香薷属多年生草本植物。广泛分布于云南、广西西部及贵州东南部。尤以云南的西双版纳等地分布较广,为当地拉祜族常用药。资源十分丰富,其叶、花或全草均可入药,性味苦、辛、凉。有清热消炎、明目、利尿作用。主治夜盲症、痢疾、感冒、咽喉炎、扁桃腺炎、急性胃肠炎、急性肾盂肾炎、肝炎、老花眼等症。为进一步阐明四方蒿的药效物质基础,给在更深层次上开发、利用四方蒿丰富的植物资源奠定良好的基础,我们对采自云南耿马地区的四方蒿的50%乙醇提取物中共分离得到24个单体化合物。运用ESI-MS、1D NMR及2D NMR等现代波谱技术鉴定了其中的18个,它们分别为:芹菜素-6,8-二-β-D-吡喃葡萄糖碳苷(apigenin-6,8-di-C-β-D-glucopyranoside)(1),木犀草素-7-O-β-D-葡萄糖苷(luteolin-7-O-β-D-glucopyranoside)(2),木犀草素-5-O-β-D-葡萄糖苷(luteolin-5-D-β-D-glucopyranoside)(3),木犀草素(luteolin)(4),5-羟基-7,8-二甲氧基黄酮(5-hydroxy-7,8-dimethoxyflavone)(5),5-羟基-6,7-二甲氧基黄酮(5-hydroxy-6,7-dimethoxyflavone)(6),5-羟基-7-甲氧基黄酮(5-hydroxy-7-methoxyflavone)(7),5,7-二羟基-6,8-二甲氧基黄酮(5,7-dihydroxy-6,8-dimethoxyflavone)(8),5,8-二羟基-7-甲氧基黄酮(5,8-dihydroxy-7-methoxyflavone)(9),4,4′-亚甲基双苯乙醇(4,4’-methylenebis[phenethylalcohol])(10),β-谷甾醇(β-sitosterol)(11),豆甾醇(stigmasterol)(12),β-胡罗卜苷(β-sistosterol-3-D-β-D-glucopyranoside)(13),熊果酸(ursolic acid)(14),齐墩果酸(oleanolic acid)(15),2β,3β,23-三羟基齐墩果烷-30-甲氧基羰基-11,13(18)-二烯-28-更多还原

【Abstract】 This thesis is composed of two parts. Part Ⅰ includes a research review of Elsholtzia plant, and studies on the chemical constituents of Elsholtzia blanda. In this part, 24 chemical compounds were isolated from E. blanda, among which 18 chemical compounds had been identified by multi-spectral techniques (1D and 2D NMR, ESI-MS). Part Ⅱ mainly introduces activities of flavonoids and a research about total flavones separation and purification of E. blanda.Part Ⅰ The Chemical Constituents of Elsholtzia blandaElsholtzia blanda named Silenghao, Dixiangru, Jigansan and so on, is a Chinese medicinal plant, which is distributed in Yunnan, Guizhou and Guangxi Province of China. It is a daily medicine of local Lahu in Xishuangbanna of Yunnan province. E. blanda, belonging to Elsholtzia genus of Labiatae, is the perennial herb with fragrance, whose leaves, flowers or whole grass are used as medicine. Its character is bitter, peppery, cool and having the effect on reducing fever, anti-inflammation, improving eyesight, diuresis. E. blanda cures mainly nyctalopia, dysentery, cold, angina, tonsillitis, acute gastroenteritis, acute pyelonephritis, hepatitis, presbyopia, etc. In order to utilize the abundant plant resource of E. blanda and find out the active constituents of E. blanda, 50% ethanol extracts of E. blanda was isolated and 24 compounds were obtained, among which 18 chemical compounds were characteristed by ESI-MS, 1D NMR, 2D NMR as apigenin-6,8-di-C-β-D-glucopyranoside(1), luteolin-7-O-β-D-glucopyranoside(2),luteolin-5-O-β-D-glucopyranoside(3),luteolin(4), 5-hydroxy-7,8-dimethoxyflavone(5), 5-hydroxy-6,7-dimethoxyflavone(6), 5-hydroxy-7-methoxyflavone(7),5,7-dihydroxy-6,8-dimethoxyflavone(8),5,8-dihydroxy-7-methoxyflavone(9), 4,4’-methylenebis[phenethyl alcohol](10), β-sitosterol(11), stigmasterol(12), β-sistosterol-3-O-β-D-glucopyranoside(13), ursolic acid(14), oleanolic acid(15), 2β,3β,23-trihydroxyolean-30-methoxycarbonyl-11,13(18) -diene-28-oic acid(16), 2β,3β,23-trihydroxyolean-30-methoxycarbonyl-12-ene-28-oic acid(17), 2β,3β,23-trihydroxyolean-12-ene-28,30-dioic acid(18). Among themcompound 16 was a new chemical compound, compound 1, 7, 8, 9, 10, 11, 17 and 18were isolated from Elsholtzia plant for the first time.Part II Studies on separation and purification of the total flavoncs fromElsholtzia blandaFlavonoids, including the basic structure of C6-C3-C6, are the plant secondary metabolites, and exist in the natural plant in the form of dissociate or glucoside. Not only are flavonoids quantity and sort various, but also their structure type are complicated. These characteristics determaine the activities of flavonoids on respiratory system disease, heart and brain blood-vascular disease, such as anti-inflammation, restraining fungus, anti-oxidant, anti-radiation, anti-tumor and strengthening immune ability, etc. In order to explore the abundant resources of E. blanda and look for the effective chemical component on cardiovascular disease, a research on the total flavones separation and purification of E. blanda had been carried through. Finally, a simple and feasible method was found and used for industrialized production.更多还原