陵水暗罗枝、叶中的巯基吡啶类化合物及其细胞毒活性研究
投稿时间:2009-08-21    责任编辑:  点此下载全文
引用本文:吕子明,戴胜军,陈若芸,于德泉.陵水暗罗枝、叶中的巯基吡啶类化合物及其细胞毒活性研究[J].中国中药杂志,2010,35(1):53.
DOI:10.4268/cjcmm20100111
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作者中文名作者英文名单位中文名单位英文名E-Mail
吕子明 LU Ziming 中国医学科学院 北京协和医学院 药物研究所 中草药物质基础与资源利用教育部重点实验室, 北京 100050 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine ,Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China  
戴胜军 DAI Shengjun 烟台大学 药学院, 山东 烟台 264005 School of Pharmaceutical Science, Yantai University, Yantai 264005, China  
陈若芸 CHEN Ruoyun 中国医学科学院 北京协和医学院 药物研究所 中草药物质基础与资源利用教育部重点实验室, 北京 100050 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine ,Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China  
于德泉 YU Dequan 中国医学科学院 北京协和医学院 药物研究所 中草药物质基础与资源利用教育部重点实验室, 北京 100050 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine ,Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China dqyu@imm.ac.cn 
中文摘要:目的: 对陵水暗罗Polyalthia nemoralis 枝、叶中的巯基吡啶类化合物进行分离、鉴定,并进行体外细胞毒活性筛选。 方法 :以硅胶、大孔吸附树脂和Sephadex LH-20色谱柱进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构。采用MTT法对所得到的化合物进行5种人肿瘤细胞系的生物活性检测。 结果 :分离鉴定了8个化合物,分别为:暗罗素( 1 ),2-巯基-N-氧化吡啶镍盐( 2 ),2-巯基-N-氧化吡啶铜盐( 3 ),2-甲磺酰基吡啶( 4 ),2,2'-二吡啶基二硫醚( 5 ),2-吡啶基硫醇-N-氧化物( 6 ),2-巯基吡啶-N-氧化物-2-β-D-吡喃葡萄糖苷( 7 ),以及吡啶-N-氧化物( 8 )。 结论 : 化合物 2, 4~6, 8 是新天然产物。体外活性筛选结果表明化合物 1~3,6 具有较强的细胞毒活性,化合物 5 具有较弱的细胞毒活性。
中文关键词:陵水暗罗  化学成分  巯基吡啶类化合物  细胞毒活性
 
2-Pyridinethiolate derivatives from branches and leaves of Polyalthianemoralis and their cytotoxic activities
Abstract:Objective : To investigate the active constituents of the branches and leaves of Polyalthia nemoralis. Method : The compounds were isolated and purified by silica gel, macroporous adsorption resin and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data. Result : Eight compounds were isolated and identified as: zincpolyanemin( 1 ), nickel bis-(pyridine-N-oxide-2-thiolate)( 2 ), cupric bis(pyridine-N-oxide-2-thiolate( 3 ), 2-methanesulfonyl-pyridine( 4 ), 2-pyridinethiolate N-oxide( 5 ), 2,2'-dithiodipyridine( 6 ), 2-thiohydroxypyridin-N-oxide-2-S-β-D-gluco pyranoside ( 7 ) and pyridine-N-oxide(8), respectively. Conclusion : Compounds 2, 4-6, 8 were new natural products. The bioassays in vitro against five human tumor cell lines with MTT method showed stronger cytotoxic activities(IC50 0.05-0.09 mg·L-1) for compounds 1-3 and 6 , and weaker cytotoxic activities(IC50 5.49-7.71 mg·L-1) for compound 5 .
keywords:Polyalthia nemoralis  chemical constituents  2-pyridinethiolate derivatives  cytotoxic activities
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