【作者】 于治成；

【导师】 沈志滨；

【作者基本信息】 广东药学院 ， 中药学， 2011， 硕士

【摘要】 狗肝菜为爵床科植物狗肝菜Dicliptera chinensis（L.）Nees.的全草,分布于广西、广东、福建、安徽等地,为我国南方常见草药之一。狗肝菜具有清热解毒、凉血、生津、利尿等功效,用于治疗肺热咳嗽、咳血、急性肝炎等症。该植物民间应用广泛,疗效确切,但国内外对其化学成分及药理作用的研究报道很少。为了进一步明确狗肝菜的化学成分,我们对狗肝菜的化学成分进行了研究。通过硅胶、凝胶柱色谱反复柱层析,从狗肝菜的75%乙醇提取物中共分离得到17个化合物,并通过理化常数测定、波谱数据分析等手段(包括IR,UV,TLC,TOF-MS, ¹H-NMR, ¹³C-NMR),鉴定出14个化合物,其中黄酮类2个,分别为表儿茶素（epicatechin,2）、山奈苷（Kaempferitrin, 16）。萜类、甾体及甾体皂苷4个,分别为薯蓣皂苷元（Diosgenin,4）,β-谷甾醇（β-Stitosterol,15）,齐墩果酸（Oleanic acid,11）,胡萝卜苷（Daucosterol ,14）。苯丙素类5个,分别为绿原酸（Chlorogenic acid,5）,阿魏酸（Ferulic acid,6）,6-羟基香豆素（6-hydroxycoumarin,9）,异土木香内酯（Isoalantolactone,10）,滨篙内酯（Scoparone,13）及其它3个化合物分别为正十八烷醇（1-octadecanol, 1）,栀子苷（Gardenoside,7）,乌苏酸（Ursolic acid,8）,其中10个化合物2,4,5,6,7,8,9,10, 13, 16为首次从该属植物中分离得到。本文亦比较了狗肝菜不同分子量多糖对CCl₄致大鼠急性肝损伤的保肝降酶作用。采用CCl₄致大鼠急性肝损伤模型,观察狗肝菜不同分子量多糖组对血清谷丙转氨酶（ALT）活力、谷草转氨酶（AST）活力、总蛋白（TP）含量;对肝组织中过氧化物歧化酶（SOD）活性、谷胱甘肽过氧化物酶（GSH-Px）活性、丙二醛（MDA）含量及肝组织形态学的变化以及对脏器指数影响。实验结果表明:（1）狗肝菜各多糖给药组中,大鼠血清ALT、AST活性与模型组比较有显著降低,其中分子量<6000多糖组效果最为显著（P<0.01）,其效果与阳性药物联苯双酯滴丸相当。（2）分子量<6000多糖组与总多糖组可显著降低血清中TP含量（P<0.05）,且分子量<6000多糖组效果优于总多糖组（P<0.05）及阳性药物组（P<0.05）。（3）总多糖组可显著增强SOD酶活性,效果优于阳性药联苯双酯滴丸组;分子量<6000多糖组也可显著增强SOD酶活性（P<0.01）。（4）总多糖组与分子量6000-10000多糖组显著增强GSH-Px酶活性（P<0.01）,效果接近阳性药联苯双酯滴丸组。（5）各多糖给药组中,大鼠肝组织MDA含量与模型组比较显著降低（P<0.01）,其中总多糖组、分子量<6000多糖组与分子量>10000多糖组效果优于阳性药联苯双酯滴丸组,且总多糖组效果最优（P<0.01）。（6）肝组织病理切片检查显示,狗肝菜总多糖及3段分子量多糖均对CCl4致大鼠急性肝损伤有良好的保护作用。（7）综合分析分子量<6000多糖组保肝效果与阳性药联苯双酯滴丸组相当。本文通过对狗肝菜化学成分及其多糖保肝活性的研究,为狗肝菜进一步开发研究奠定了坚实的理论基础。更多还原

【Abstract】 The Dicliptera chinensis （L.） Nees（ Acanthaceae ） regionally distributes in Guangxi, Guangdong, Fujian, Anhui as one of the common wild herbs in South China. The dicliptera chinensis can clear heat and detoxicate, cool the blood, promote saliva or body fluids, improve the diuresis function, used in the fever macula, acute hepatitis, having blood in stool, drowning the blood, the difficult urination, swelling and furunculosis and so on.. Up to now, there was little report about the chemical constituents and bioactivities of Dicliptera chinensis （L.） Nees.In order to elucidate the constituents of this plant, fourteen compounds were isolated from the 75% EtOH extract of Dicliptera chinensis by means of the repeated column chromatography on silica gel, recrystallizing. Their chemical structures were elucidated on the basis of physico-chemical properties and spectroscopic analysis, including IR,UV,TLC,TOF-MS, 1H-NMR, 13C-NMR etc. These compounds were（1）1-octadecanol, （2 ）Epicatechin（,4）Diosgenin, （5）Chlorogenic acid, （6）Ferulic acid, （7 ）Gardenoside , （8）Ursolic acid, （9）6-hydroxycoumarin, （10）Isoalantolactone, （11）Oleanic acid, （12）Daphnoretin, （13）Scoparone, （14）Daucosterol, （15）β-Stitosterol, （16）Kaempferitrin。Among them, compound 2,4,5,6,7,8,9,10,13,16 were isolated from this genus for the first time.We also Compared the function of different molecular weight polysaccharide of Dicliptera chinensis to decrease the enzyme action. Uses the carbon-tetrachloride （CCl₄）- induced rats acute liver damage model, observe the content of dicliptera chinensis different molecular weight polysaccharide to the Alanine aminotransferase （ALT） activity, aspartate aminotransferase （AST） activity, the total protein （TP） content in blood serum; change in liver superoxide dismutase （SOD）, glutathione peroxidase （GSH-Px） activeness, malondialdehyde （MDA） content and liver morphological changes; effect on organindexThe results shows:（1）Various polysaccharides-treated group with CCl₄-treated group and find significant difference in rats’s serum AST and ALT activities and group with the molecular weight <6000 has the most remarkable effect （P<0.01）which was comparable to that of the reference drug, bifendate.（2）The group with molecular weight <6000 polysaccharide and the total polysaccharide group may obviously reduce the rise of TP（P<0.05）, and the group with molecular weight <6000 has superior effect compared with the total polysaccharide group（P<0.05） and the positive medicine group（P<0.05）.（3）The group with molecular weight <6000 can enhance the decreased activity of SOD in liver（P<0.01）.（4）Total polysaccharide group and group with molecular weight between 6000 and 10000 polysaccharide can remarkably enhance the decreased activity of GSH-Px in liver（P<0.01）, and the effect was comparable to that of the reference drug, bifendate.（5）The MDA content in rats liver in various polysaccharides group remarkably decreases compared with that of the model control group（P<0.01）, among which the total polysaccharide group, the molecular weight <6000 group and the molecular weight >10000 group have superior effect to that of bifendate group, and the effect of the total polysaccharide group is most superior（P<0.01）.（6）According to the microscopy, the dicliptera chinensis polysaccharide may reduce CCl₄-induced acute liver damage. The dicliptera chinensis total polysaccharide and 3-section molecular weight polysaccharides have remarkable effect on rats acuite liver injury caused by the carbon tetrachloride.（7）In all, The group with the molecular weight <6000 has the most remarkable effect which was comparable to that of the reference drug.In conclusion, this paper provided valuable experimental data for further development of Dicliptera chinensis.更多还原