【作者】 于泉林；

【导师】 高文远； 段宏泉；

【作者基本信息】 天津大学 ， 应用化学， 2005， 博士

【摘要】 积雪草(Centella asiatica (L.)Urban) ,为伞形科积雪草属植物积雪草的干燥全草,为《中国药典》收载的常用中药。积雪草具有清热利湿、解毒消肿的功效,临床上多用于治疗跌打损伤、皮肤病等。积雪草主要化学成分为三萜及其苷类化合物。为寻找具有活性的化学单体,本文对积雪草地上部位的乙醇提取物进行化学成分研究。采用多种现代分离技术(快速层析法,凝胶色谱法和制备HPLC等)对积雪草乙酸乙酯和正丁醇提取部位进行分离,从积雪草中分离得到28个化学单体,通过1H-NMR,13C-NMR,2D-NMR,高分辨质谱等波谱解析方法鉴定了其中的22个化合物的结构,其中2个为新的化合物,5个化合物为首次从该植物分离得到。狗筋蔓(Cucubalus baccifer L.),为石竹科狗筋蔓属植物,该植物全株入药,民间用于治疗风湿性关节炎、骨折、跌打损伤、肾炎水肿、小儿疳积、泌尿系统感染及肺结核,外敷治疗疮痒疖肿及淋巴节结核。其化学成分主要为降倍半萜、甾酮、黄酮类。为寻找具有活性的化学单体,本文对狗筋蔓全草的石油醚、乙酸乙酯和正丁醇提取部位进行化学成分研究,从狗筋蔓中分离得到46个化学单体,通过1H-NMR,13C-NMR,2D-NMR,高分辨质谱等波谱解析方法鉴定了其中15个化合物的结构。这些化合物均为从狗筋蔓中首次分离得到。本文对积雪草乙酸乙酯、正丁醇提取物及部分单体进行了抗肿瘤活性筛选,结果表明积雪草乙酸乙酯提取物有一定的抗肿瘤活性。从积雪草和狗筋蔓中分到的化合物6、7、9、10、13、14、17、18、21和33对Hela细胞表现出一定的抑制作用,化合物7、9、11、14、17、33对A549细胞有一定的细胞毒作用。本文还进行了淋巴细胞转换实验,结果表明单体化合物1、2、13和30具有较好的免疫抑制作用。本文对积雪草和狗筋蔓中分离所得到的及其相关的黄酮分子进行了抗组胺的分子对接计算,利用打分函数筛选出苜蓿素、槲皮素、山奈酚等5个黄酮分子抗组胺活性较好,但结果有待于药理试验的进一步验证,为它们在抗组胺的应用提供理论基础。更多还原

【Abstract】 Centella asiatica has been used for treatment of skin diseases, diarrhea, eye diseases, inflammation and leprosy in China, India, Sri Lanka, Africa and oceanic countries. Many constituents has been reported, such as triterpenoid saponins, polyacetylenes, flavone, sterols and lipids. In order to search the active compounds, we began to study on the chemical constituents from C. asiatica. By column chromatography, including Silica gel, Sephadex LH-20, Toyopearl HW-40 and preparative HPLC, 28 compounds were isolated from the EtOH extract of C. asiatica, among them, two new (isoasiatic acid 1, isoasiaticoside 2) and 22 known compounds (3-22) were identified by 1H-NMR,13C-NMR and 2D-NMR spectra.Cucubalus baccifer L. is a Chinese folk herb used for treatment of nephritis, hydropsy, bone-fractures, arthritis, pulmonary tuberculosis and scrofula. Oligosaccharides, tocopherol, phytoecdysterones, norsesquiterpenoid have been reported from C. baccifer. By column chromatography, including Silica gel, Toyopearl HW-40 and preparative HPLC, 46 compounds were isolated from the EtOH extract of C. baccifer and 15 known compounds were elucidated by 1H-NMR,13C-NMR and 2D-NMR spectra. In addition, the identified 15 compounds were first isolated from this genus .The EtOAc, BuOH extracts of C. asiatica, and PE, EtOAc, BuOH extracts of C. baccifer as well as isolated compounds, were screened by antitumor experiments. The EtOAc extracts of C. asiatica showed some antitumor activity. Compounds 6, 7, 9, 10, 13, 14, 17, 18, 21 and 33 have some activity to inhibit Hela cell. Compounds 7, 9, 11, 14, 17and 33 have some activity to inhibit A549 cell.In the lymphocyte transformation experimation, compounds 1, 2, 13 and 30 showed a significant distinction to the concanavalin (Con A) control group (p<0.01, n = 6) and positively showed immunosuppressive activity.In this paper, 15 flavone molecular for antihistamine were selected to dock into carbonic anhydrase by using the Dock program. The results showed that tricin, quercetin and kaemferol were better than other compounds for antihistamine.更多还原