【作者】 陈定奔；

【导师】 义祥辉； 陈全斌；

【作者基本信息】 广西师范大学 ， 有机化学， 2004， 硕士

【摘要】 目前全国患乙肝与乙肝病毒携带者人数有2亿人多，且患者常导致肝硬化和肝癌。而目前临床上又缺乏真正的制剂，故有必要寻找新药。荔枝核(Semen Litchi)是一种中药，为无患子科植物荔枝的干燥成熟种子，性温、味甘、微苦、归肝、肾经，功效行气散节、祛寒止痛。药理研究表明，荔枝核水提取物是一种能使HBsAg转阴且仅次于夏枯草的高效抑制HBsAg的药物[24-25]。目前，国内外对荔枝核水溶性化学成分研究较少，并且未见有抗乙肝病毒确切有效成分的报道。因此本课题的研究旨在从荔枝核中分出抗乙肝病毒有效部位甚至有效成分。本课题的研究内容如下：1. 从荔枝核50%乙醇总提取物B的水溶部分出发，经D-101型大孔吸附树脂吸附、洗脱等分离手段，最终得C、D、E、F部位。应用HepG2.2.15细胞系检测这几个部位对HBsAg和HBeAg的抑制作用。结果表明E的抑制作用非常显著，在不影响细胞正常生长的药物浓度200μg·mL-1下,于实验第九天对HBsAg和HBeAg的抑制率分别为90.9%和84.3%。2. 从从抗乙肝病毒有效部位E 出发，经聚酰胺柱层析分离得四个部位H、I、J、K，应用HepG2.2.15细胞系检测出I和J的抑制HBV作用非常显著。在不影响细胞正常生长的药物浓度800μg·mL-1下,于实验第六天对HBsAg和HBeAg的抑制率：I为90.1%和83.4%，J为86.8%和81.8%。3. 进一步从I 和J 部位出发，利用硅胶柱层析、薄层制备、高压液相色谱制备分离得4个单体，测试了其中3个。根据其IR、FAB-MS、1HNMR、13CNMR数值，鉴定了其中2个化合物，分别为原花色素-A1和原花色素-A2。这两个化合物均从荔枝核中首次分离得到，其中原花色素-A1是从该属植物中首次得到。更多还原

【Abstract】 There are more than two billion people sufferred from hepatitis B and carried hepatitis B virus at present, the patients often lead to cirrhosis and liver cancer. Because of lack of true clinical pharmaceutical preparation , so it is necessary to find new drug to treat hepatitis B . Semen Litchi is a kind of traditional chinese medicine, it is the dry and mature seed of the Sapindaceae plant- Litchi Chinensis Sonn. Its quality is mild, flavour is sweetish and tiny bitter. It can protect the liver and kidney from disease. It has the effects of scattering the nodes through line spirit and relieving pian. The pharmacological study shows the water extraction of Semen Litchi is a high efficient anti-HBsAg drug, whose inhibiting rate is only less than Prunella vulgaris [24-25]. At present, there is little report about water-solubility compositions and no report about anti-HBV pharmaceutical compositions in Semen Litchi. Therefore, the aim of our study is extracting anti-HBV pharmaceutical parts or compositions from Semen Litchi. The contents of this article are as follows:1. The total extraction B was extracted from Semen Litchi with 50% ethanol. Then the water-soluble part of B was passed through D-101 macroporous resin and eluted by water and, 80% ethanol. The 80% ethanol part was extracted with anhydrous ethanol . So we gained five part(B, C, D, E, F) at last. Their inhibition on HBsAg and HBeAg were surveyed with HePG2.2.15 cells system. The results showed that E had obvious inhibition on HBsAg and HBeAg on the sixth experimental day , whose inhibiting rate on HBsAg and HBeAg are 90.9% and 84.3%(consistency:200μg/ml).2. The anti-HBV effective part E was passed through the poliamide resin and gradually desorbed by 30% ethanol, 50% ethanol, 70% ethanol and 95% ethanol. Then we got four part: H, I, J, K. Their inhibition on HBsAg and HBeAg were surveyed with HePG2.2.15 cells system. The results showed that I and J had obvious <WP=4>inhibition on HBsAg and HBeAg on the thirdth and sixth experiment day. The inhibiting rates of I on HBsAg and HBeAg are 90.1% and 83.4% on the sixth experiment day . The inhibiting rates of J are86.8%and 81.8%(consistency:800μg/ml).3. Four compounds were separated from I and J parts through silica gel chromatography, TLC preparation and HPLC preparation. Three compounds were tested by sepectroscopic means. On the basis of 1HNMR, 13CNMR, IR, FAB-MS data, we had identificated chemical structures of two compounds: Proanthocyanidin-A1, Proanthocyanidin-A2 which are firstly separated from Semen Litchi. Proanthocyanidin-A1 is the first compound separated from species of Litchi。更多还原