| 虎杖抗H1N1流感病毒神经氨酸酶活性成分研究 |
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| 引用本文： | 陈考坛,周伟玲,刘嘉炜,祖勉,何紫凝,杜冠华,陈蔚文,刘艾林. 虎杖抗H1N1流感病毒神经氨酸酶活性成分研究[J]. 中国中药杂志, 2012, 37(20): 3068-3073 |
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| 作者姓名： | 陈考坛 周伟玲 刘嘉炜 祖勉 何紫凝 杜冠华 陈蔚文 刘艾林 |
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| 作者单位： | 1. 广州中医药大学中药资源科学与工程研究中心,岭南中药资源教育部重点实验室,广东广州510006
2. 中国医学科学院北京协和医学院药物研究所,北京,100050 |
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| 基金项目： | 国家"重大新药创制"科技重大专项(2008ZX09401-004,2009ZX09302-00);北京市自然基金项目(7103172);广州中医药大学《南药的现代研究与综合开发利用》 "211工程"重点学科建设项目 |
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| 摘 要： | 目的:分离和鉴定虎杖乙酸乙酯提取物中能显著抑制H1N1流感病毒神经氨酸酶(neuraminidase,NA)的活性成分。方法:基于药理活性导向法,综合利用硅胶,葡聚糖凝胶和制备液相等色谱分离虎杖提取物活性成分,采用MS和NMR等波谱数据及其理化性质鉴定分子结构。结果:从虎杖乙酸乙酯活性部位分离出7个化合物,分别鉴定为:2-methoxystypandrone(1),大黄素(2),白藜芦醇(3),虎杖苷(4),大黄素-8-O-β-D-吡喃葡萄糖苷(5),(E)-3,5,12-trihydroxystilbene-3-O-β-D-glucopy-ranoside-2’-(3″,4″,5″-trihydroxybenzoate)(6)和儿茶素-3-O-没食子酸酯(7);NA测试表明化合物3,6和7显著抑制NA活性,IC50分别为129.8,44.8,21.3μmol·L-1,进一步CPE测试表明化合物6和7具有显著抗H1N1流感病毒效果(EC50分别为5.9,0.9μmol·L-1),对宿主MDCK细胞表现出非常低的细胞毒性,选择性指数分别为56和269。结论:基于药理活性导向从虎杖提取物中分离鉴定出能显著抗H1N1流感病毒的神经氨酸酶抑制剂,对阐明其药效物质基础和抗流感药物研发具有指导意义。
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| 关 键 词： | 虎杖 甲型H1N1流感 神经氨酸酶 抑制剂 |
| 收稿时间： | 2012-03-16 |
Active neuraminidase constituents of Polygonum cuspidatum against influenza A(H1N1) influenza virus |
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| CHEN Kao-tan,ZHOU Wei-ling,LIU Jia-wei,ZU Mian,HE Zi-ning,DU Guan-hu,CHEN Wei-wen and LIU Ai-lin. Active neuraminidase constituents of Polygonum cuspidatum against influenza A(H1N1) influenza virus[J]. China Journal of Chinese Materia Medica, 2012, 37(20): 3068-3073 |
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| Authors: | CHEN Kao-tan ZHOU Wei-ling LIU Jia-wei ZU Mian HE Zi-ning DU Guan-hu CHEN Wei-wen LIU Ai-lin |
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| Affiliation: | Key Laboratory of Chinese Medicinal Resource from Lingnan, Ministry of Education, Research Center of Medicinal Plant Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;Beijing Key Laboratory of Drug Target Research and Drug Screening, Institiute of Matetia Medica, Chinese Academy Science and Peking Union Medical College, Beijing 100050, China;Key Laboratory of Chinese Medicinal Resource from Lingnan, Ministry of Education, Research Center of Medicinal Plant Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;Beijing Key Laboratory of Drug Target Research and Drug Screening, Institiute of Matetia Medica, Chinese Academy Science and Peking Union Medical College, Beijing 100050, China;Key Laboratory of Chinese Medicinal Resource from Lingnan, Ministry of Education, Research Center of Medicinal Plant Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;Beijing Key Laboratory of Drug Target Research and Drug Screening, Institiute of Matetia Medica, Chinese Academy Science and Peking Union Medical College, Beijing 100050, China;Key Laboratory of Chinese Medicinal Resource from Lingnan, Ministry of Education, Research Center of Medicinal Plant Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;Beijing Key Laboratory of Drug Target Research and Drug Screening, Institiute of Matetia Medica, Chinese Academy Science and Peking Union Medical College, Beijing 100050, China |
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| Abstract: | |
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| Keywords: | Polygonum cuspidatum H1N1 influenza A neuraminidase inhibitor |
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