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草珊瑚,紫荆和小叶石楠的化学成分及生物活性研究

Studies on the Chemical Constituents and Bioactivities of Sarcandra Glabra, Cercis Chinensis and Photinia Parvifolia

【作者】 李媛

【导师】 庾石山; 张东明;

【作者基本信息】 中国协和医科大学 , 药物化学, 2006, 博士

【摘要】 草珊瑚Sarcandra glabra(Thunb.)Nakai[曾用名Chloranthus glabra(Thunb.)Makino],又名接骨金粟兰(通称),肿节风、九节风(江西),九节茶(浙江)等,属于金粟兰科(Chloranthaceae)草珊瑚属(Sarcandra Gardn.)植物,产于安徽、浙江、江西、福建、台湾、广东、广西、湖南、四川、贵州和云南。全株供药用,有良好的生物学活性,如抗肿瘤,抗炎,抗病毒,提高机体免疫力等。本所药理室筛选表明:草珊瑚70%乙醇提取物过大孔树脂70%乙醇洗脱部分有良好的肝保护和抗炎活性。 紫荆Cercis chinensis Bunge,又名满条红,为豆科(Leguminosae)紫荆属(Cercis)植物,产于我国东南部大部分省区。紫荆属植物化学成分以黄酮类成分为主,生物活性集中在抗炎、抗氧化。日本大正制药公司对紫荆根95%乙醇提取物进行筛选后,发现具有良好的抗肿瘤活性。 小叶石楠Photinia parvifolia(Pritz.)Schneid.,别名牛李子(湖南)、山红子(贵州)、牛筋木(四川)。为蔷薇科(Rosaceae)石楠属(Photinia Lindl.)植物。分布于河南、江苏、安徽、浙江、江西、四川、贵州、台湾、广东和广西。该属植物全世界约60余种,仅5种进行过化学成分研究。药理筛选发现小叶石楠茎的95%乙醇提取物粗分后的乙酸乙酯部分有抗肿瘤活性。 为从天然产物中寻找活性成分,本论文运用多种色谱方法和波谱技术,对上述3种植物进行了系统的化学成分研究,并对其进行了粗提物及单体成分的药理活性筛选。共从3种植物中分离得到80个化合物,确定了72个化合物的结构,其中包括12个新化合物,具有保肝、抗炎、抗癌等活性的化合物28个,并对草珊瑚中新化合物8和9及其苷元进行了合成。 从草珊瑚70%乙醇提取物通过大孔树脂柱粗分后的30%,70%乙醇洗脱部分分离得到45个化合物,确定了其中的41个化合物的结构(包括11个新化合物),分别为:10个倍半萜(苷)类化合物(1-6,12-15),15个黄酮类化合物(7-11,16-25),7个酚酸类化合物(26-32),2个香豆素类化合物(33-34),3个木脂素苷类化合物(35-37),1个三萜类化合物(38),3个甾体化合物(39-41)。经理化及波谱数据分析测定为:sarcaglaboside A(1),sarcaglaboside B (2),

【Abstract】 Sarcandra glabra (Thunb.) Nakai [syn. Chloranthus glabra (Thunb.) Makino] belongs to the genus Sarcandra of Chloranthaceae, which is distributed in Anhui, Zhejiang, Jiangxi. Fujian, Taiwan, Guangdong, Guangxi, Hunan, Sichuan, Guizhou and Yunnan Provinces. The whole plant was used as a drug for anticancer, antibacterial, antivirus and increasing the level of immunity. The result of bioassay displayed that the 70 % alcohol extract of Sarcandra glabra showed anti-inflammation and potent hepatoprotective activities.Cercis chinensis Bunge belongs to the genus Cercis of Leguminosae, which grows widely in southeast of China. The main components of the genus Cercis are flavornoids and aromatic compounds with antibacterial and anti-oxidation activities. In addition, the 95 % alcohol extract showed potent cyto-toxicities having been tested by Taisho Pharmacentical CO. LTD Japan..Photinia parvifolia (Pritz.) Schneid. belongs to the genus Photinia of Rosaceae, which is distributed in Henan, Jiangsu, Anhui, Zhejiang, Jiangxi, Taiwan, Sichuan, Guizhou, Guangdong and Guangxi Provinces. Although the genus comprises 60 species, among which only five plants were studied on their chemical constituents. The pharmacological screens in vitro disclosed that the EtOAc part of the 95% alcohol extract of Photinia parvifolia showed significant anticancer activity.By means of chromatography methods and spectral technologies, the three plants mentioned above were studied systemically in chemistry and related bioassays. Eighty compounds were obtained, in which 12 are new and 28 have remarkable hepato-protective, anticancer and anti-inflammation activities. We also synthesized new compounds 8. 9 and their aglycones.Forty five compounds were obtained from the 70% alcohol extract (30%, 70% alcohol elution fractions) from the whole plant of Sarcandra glabra, in which the structures of forty one were determined by spectroscopic analysis and chemical methods. As a result, there are 10 sesquiterpenoids (1-6, 12-15), 15 flavonoids (7-11,

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