【作者】 杨国勋；

【导师】 胡昌奇；

【作者基本信息】 复旦大学 ， 药物化学， 2004， 博士

【摘要】 红花锦鸡儿(Caragana rosea Turcz.)是豆科锦鸡儿属的一种矮小灌木,在我国东北、华北及华东地区都有分布。据《中药大辞典》记载,其有健脾强胃、活血催乳、利尿通经的功效,可以治疗虚损劳热、阴虚喘咳,淋浊白带等症。为了开发祖国传统药学资源,我们在锦鸡儿(C. sinica)化学成分和生物活性研究的基础上,对红花锦鸡儿地上部分的乙醇提取物进行了抗艾滋病病毒(HIV)筛选,发现其乙酸乙酯部位显示一定的生物活性。本研究的目的是寻找并确定红花锦鸡儿中抗病毒活性成分:即在抗HIV生物活性测试指导下,对红花锦鸡儿乙酸乙酯部位中的化学成分进行分离和结构鉴定。本论文涉及16个化学成分,包括1个茋木脂体:cararosin A (4);11个茋类:piceatannol (5), (+) α-viniferin (6), kobophenol A (7), cis-scirpusin A (8) , scirpusin A (9), scirpusin B (10), maackin(12)和cararosinols A (13)、B (14)、C (15)、D (16);2个黄酮:myricetin (1)和mearnsetin (2);1个苯丙酸:对羟基桂皮酸(3);以及1个邻苯二甲酸酯:邻苯二甲酸二 (2-乙基-己醇) 酯(11)。其中化合物cararosinols A、B、C、D和cararosin A为新化合物,cis-scirpusin A是第一次分到的天然产物。体外生物活性测试显示,scirpusin A和scirpusin B具有明显的抑制HIV-1IIIB作用(IC50分别为10ug/ml和7ug/ml)。更多还原

【Abstract】 Caragana rosea Turcz. is a small shrub of genus Caragana Fabra., Leguminosae. The plant is widely distributed in northeast、north and east China. The root of C. rosea has been used as a folk medicine to treat fever, asthma, cough and some kinds of women diseases. To harness Traditional Chinese Medicine, we tested the ethanol extract of C. rosea against HIV-1IIIB and found the EtOAc soluble fraction of the crude extract showed moderate activity. The research is to find out anti-HIV constituents of C. rosea. Thus, chromatographic separation of EtOAc soluble fraction of C. rosea is carried out under the guide of anti-HIV bioassay in vitro. To date, 16 pure compounds were obtained, their structures were established mainly on the basis of spectroscopic data: including 1 stilbenolignan: cararosin A (4); 11 stilbenoids: piceatannol (5), (+) α-viniferin (6), kobophenol A (7), cis-scirpusin A (8) , scirpusin A (9), scirpusin B (10), maackin(12), cararosinols A (13)、B (14)、C (15)、D (16); 2 flavonoids: myricetin (1) and mearnsetin (2);1 phenylpropanoid: p-hydroxycinnamic acid (3) and 1 phthalic ester:bis(2-ethylhexyl) phthalate (11). Of the 16 compounds, cararosinols A (13)、B (14)、C (15)、D (16) and cararosin A (4) bear new structures; cis-scirpusin A (8) is the first time to be isolated as natural compound. Scirpusins A and B are identified as potent active constituents against HIV-1IIIB with IC50 values 10ug/ml and 7ug/ml respectively.更多还原