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Flazinamide, a novel beta-carboline compound with anti-HIV actions

文献类型：期刊论文

作者Wang, Yun-Hua; Tang, Jian-Guo; Wang, Rui-Rui; Yang, Liu-Meng; Dong, Ze-Jun; Du, Li; Shen, Xu; Liu, Ji-Kai; Zheng, Yong-Tang
刊名BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
出版日期2007-04-20
卷号355期号:4页码:1091-1095
ISSN号0006-291X
关键词Beta-carboline Flazinamide Synthesis Anti-hiv Agents Hiv-1 Hiv-2
DOI10.1016/j.bbrc.2007.02.081
文献子类Article
英文摘要A beta-carboline compound, flazin isolated from Suillus granulatus has been shown weak anti-HIV-1 activity. Based on the structure of flazin, flazinamide [1-(5'-hydromethyl-2'-furyl)-beta-carboline-3-carboxamide] was synthesized and its anti-HIV activities were evaluated in the present study. The cytotoxicity of flazinamide was about 4.1-fold lower than that of flazin. Flazinamide potently reduced syncytium formation induced by HIV-1IIIB with EC50 value of 0.38 mu M, the EC50 of flazinamide was about 6.2-fold lower than that of flazin. Flazinamide also inhibited HIV-2ROD and HIV-2CBL-20 infection with EC50 values of 0.57 and 0.89 mu M, respectively. Flazinamide reduced p24 antigen expression in HIV-1IIIB acute infected C8166 and in clinical isolated strain HIV-1KM018 infected PBMC, with EC50 values of 1.45 and 0.77 mu M, respectively. Flazinamide did not suppress HIV-1 replication in chronically infected H9 cells. Flazinamide blocked the fusion between normal cells and HIV-1 or HIV-2 chronically infected cells. It weakly inhibited activities of recombinant HIV-1 reverse transcriptase, protease or integrase at higher concentrations. In conclusion, the conversion of the carboxyl group in 3 position of flazin markedly enhanced the anti-viral activity (TI value increased from 12.1 to 312.2) and flazinamide might interfere in the early stage of HIV life cycle. (c) 2007 Elsevier Inc. All rights reserved.
学科主题Biochemistry & Molecular Biology ; Biophysics
WOS关键词TAT-TAR INTERACTION ; IN-VITRO ; DERIVATIVES ; DESIGN ; DNA ; INHIBITORS ; AGENTS
WOS研究方向Biochemistry & Molecular Biology ; Biophysics
语种英语
WOS记录号WOS:000245115000040
公开日期2011-11-24
源URL[http://ir.kib.ac.cn:8080/handle/151853/2099]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Yun-Hua,Tang, Jian-Guo,Wang, Rui-Rui,et al. Flazinamide, a novel beta-carboline compound with anti-HIV actions[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2007,355(4):1091-1095.
APA Wang, Yun-Hua.,Tang, Jian-Guo.,Wang, Rui-Rui.,Yang, Liu-Meng.,Dong, Ze-Jun.,...&Zheng, Yong-Tang.(2007).Flazinamide, a novel beta-carboline compound with anti-HIV actions.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,355(4),1091-1095.
MLA Wang, Yun-Hua,et al."Flazinamide, a novel beta-carboline compound with anti-HIV actions".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 355.4(2007):1091-1095.

入库方式： OAI收割

来源：昆明植物研究所

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