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  5. 分子免疫药理学
Flazinamide, a novel beta-carboline compound with anti-HIV actions

文献类型：期刊论文

作者Wang YH1,4; Tang JG2,4; Wang RR1,4; Yang LM1; Dong ZJ2; Du L3,4; Shen X3; Liu JK[*]2; Zheng YT[*]1
刊名BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
出版日期2007
卷号355期号:4页码:1091-1095
关键词b-Carboline Flazinamide Synthesis Anti-HIV agents HIV-1 HIV-2
ISSN号0006-291X
通讯作者zhengyt@mail.kiz.ac.cn
合作状况其它
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 0.38muM, 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 0.89microM, 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 0.77microM, 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.
收录类别SCI
资助信息The work was supported by grants from the Chinese Academy of Sciences (KSCX1-YW-R-15 and KSCX1- YW-R-24), National 973 project of China (2006CB504200 and 2006CB504300), Key Scientific and Technological projects of China (2004BA719A14), and Yunnan province (2004NG12), the Natural Science Foun- dation of China (30471605) to Dr. Y.-T. Zheng. We acknowledge MRC AIDS Research Project (UK) and NIH AIDS Research and Reference Reagent Program (USA) for providing cell lines and virus.
原文出处20073551091.pdf
语种英语
公开日期2010-08-24
源URL[http://159.226.149.42:8088/handle/152453/4605]  
专题昆明动物研究所_分子免疫药理学
昆明动物研究所_动物模型与人类重大疾病机理重点实验室
作者单位1.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China
2.State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, Yunnan 650204, China
3.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
4.Graduate School of the Chinese Academy of Sciences, Beijing 100039, China
推荐引用方式
GB/T 7714		 Wang YH,Tang JG,Wang RR,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 YH.,Tang JG.,Wang RR.,Yang LM.,Dong ZJ.,...&Zheng YT[*].(2007).Flazinamide, a novel beta-carboline compound with anti-HIV actions.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,355(4),1091-1095.
MLA Wang YH,et al."Flazinamide, a novel beta-carboline compound with anti-HIV actions".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 355.4(2007):1091-1095.

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来源：昆明动物研究所

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