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氧化阿朴菲生物碱衍生物与DNA的相互作用及抗肿瘤活性研究
引用本文:唐煌,魏永标,王晓冬,黄志纾,古练权. 氧化阿朴菲生物碱衍生物与DNA的相互作用及抗肿瘤活性研究[J]. 西北药学杂志, 2011, 26(6): 453-457. DOI: 10.3969/j.issn.1004-2407.2011.06.027
作者姓名:唐煌  魏永标  王晓冬  黄志纾  古练权
作者单位:1. 广西师范大学化学化工学院,药用资源化学与药物分子工程教育部重点实验室,广西,桂林,541004
2. 中山大学药学院,广东,广州,510080
基金项目:国家自然科学基金,广西自然科学基金
摘    要:目的研究氧化阿朴菲生物碱衍生物4位胺烷基甲酰胺取代的7 H-二苯并[de,g]喹啉-7-酮与小牛胸腺DNA的相互作用以及抗肿瘤活性。方法用紫外吸收光谱、荧光光谱和诱导CD光谱研究衍生物与小牛胸腺DNA的相互作用;用MTT法评价衍生物对NCI-H460,GLC-82和MCF 3种细胞株的细胞毒性。结果光谱研究结果表明,衍生物能与小牛胸腺DNA发生嵌入结合作用;细胞毒性测试表明,衍生物具有中等强度的抗肿瘤活性。结论衍生物的抗肿瘤活性很可能是因为衍生物能与DNA作用而产生的。

关 键 词:氧化阿朴菲衍生物  DNA结合  抗肿瘤

Oxoaporphine alkaloid derivatives:DNA binding affinity and cytotoxicity
TANG Huang,WEI Yongbiao,WANG Xiaodong,HUANG Zhishu,GU Lianquan. Oxoaporphine alkaloid derivatives:DNA binding affinity and cytotoxicity[J]. Northwest Pharmaceutical Journal, 2011, 26(6): 453-457. DOI: 10.3969/j.issn.1004-2407.2011.06.027
Authors:TANG Huang  WEI Yongbiao  WANG Xiaodong  HUANG Zhishu  GU Lianquan
Affiliation:TANG Huang1,WEI Yongbiao2,WANG Xiaodong2,HUANG Zhishu2,GU Lianquan2(1.Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources,Ministry of Education of China,School of Chemistry & Chemical Engineering of Guangxi Normal University,Guangxi Guilin 541004,China,2.School of Pharmaceutical Sciences,Sun Yat-sen University,Guangdong Guangzhou 510006,China)
Abstract:Objective To study the interaction of oxoaporphine derivatives(4-carboxylic amide-7-oxo-7H-dibenzo quinoline) with calf thymus DNA,and to study their antitumor activities.Methods The interaction of oxoaporphine derivatives with calf thymus DNA was performed by fluorescence,CD and UV spectra.The in vitro cytotoxicity of oxoaporphine derivatives for three cell lines(NCI-H460,GLC-82 and MCF) was evaluated using MTT method.Results The experimental results indicate that the derivatives could intercalate DNA and ...
Keywords:oxoaporphine derivatives  DNA binding  antitumor activity  
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