山梗菜脂溶性化学成分的研究

【作者】 辛国；

【导师】 张辉；

【作者基本信息】 长春中医药大学 ， 中药学， 2008， 硕士

【摘要】 山梗菜是桔梗科（Campanulacea）半边莲属（Lobelia L.）植物山梗菜Lobeliasessilifolia Lamb.的根及或带根全草。产于我国云南西北部、广西北部、浙江、台湾、山东、河北、辽宁、吉林和黑龙江。目前对山梗菜有效成分的研究并不全面,药理学的研究也刚刚起步。为更加深入研究其化学成分,并为阐明其药效提供化学依据,有必要对其进行系统分离研究。作者通过硅胶柱层析,凝胶柱层析等分离手段从山梗菜中分离出5个单体化合物,通过ESI-MS、¹HNMR、¹³CNMR、HMBC、HMQC、DEPT、H¹-H¹COSY等光谱分析,确定它们的结构分别β-香树脂醇3-0-β-棕榈酸酯、马尼拉二醇3-0-β-棕榈酸酯、齐墩果酸、熊果酸、豆甾醇。其中豆甾醇在该属植物中首次发现。五环三萜类化合物熊果酸和齐墩果酸有抗人肺癌细胞增殖、侵袭和诱导细胞凋亡的作用,并探讨其抗侵袭作用的机理。方法是药物处理后通过重建基底膜侵袭试验、对层粘连蛋白的粘附试验、趋化运动试验以及组织蛋白酶B活性测定观察细胞侵袭能力的变化。结果是熊果酸和齐墩果酸均可降低PGCL3细胞增殖能力（P＜0.001）,ICm分别为44.73μmol/L和40.71μmol/L。30和40μmol/L熊果酸、和35和45μmol/L齐墩果酸均能抑制PGCl3细胞的侵袭能力（P＜0.001）且有剂量依赖性。抗侵袭作用机理的分析结果显示上述浓度的两种药物对细胞的运动、粘附能力及组织蛋白酶B分泌均有明显的抑制作用。更多还原

【Abstract】 Lobelia sessilifolia Lamb is the root or the whole grass with root of Campanulacea.the study on active principles in the Lobelia sessilifolia Lamb aren’t comprehensive and the study on pharmacology is just on the first step.Base of the previous research,I have got five compounds from Lobelia sessilifolia Lamb by using silica gel column chromatography, preparative thin-layer chromatography,reversed phase column chromatography,preparative HPLC.They are identified by EI-MS、¹HNMR、¹³CNMR.The two compounds were determined asβ-amyrin 3-O-β-palmitate、maniladiol 3-O-β-palmitate、Oleanolic acid、ursolic acid、stigmasterol.One of them was isolated from the genus Lobelia L.for the first time.To study the anti—invasive effects and its mechanisim and apoptosis induction of pentacyclic triterpenoid including ursolic acid and oleanolic acid in highly potentially metastatic lung cancer cell line.The Methods are invasive a—bilit Y,the adhesive ability, the migration ability and the activity of cathepsin B（CB）of PGCI 3 cells treated with the two drugs were determined by the invasion test or reconstituted basement membranc,the laminin adhesion test,the chemotactic migration test and the enzymologicaI method of CB.The apoptosis of the cells was detected with acridine orange ethidium bromide fluorescent s.tain（A（）/EB）and TU-NEL.The result is All of the two drugs can inhibit the proliferative and invasive ability,and induce apoptosis of the PGCL3 human lung cancer cell.The mechanism of anti-invasion may be to inhibit the adhesion,migration,and the CB secreation of the cell.更多还原