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题名: Flazinamide, a novel beta-carboline compound with anti-HIV actions
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
关键词: beta-carboline ; flazinamide ; synthesis ; anti-HIV agents ; HIV-1 ; HIV-2
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.
出版日期: 2007-04-20
卷号: 355, 期号:4, 页码:1091-1095
语种: 英语
收录类别: SCI
学科分类: Biochemistry & Molecular Biology; Biophysics
ISSN号: 0006-291X
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/2099
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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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

Recommended Citation:
Wang, YH; Tang, JG; Wang, RR; Yang, LM; Dong, ZJ; Du, L; Shen, X; Liu, JK; Zheng, YT.Flazinamide, a novel beta-carboline compound with anti-HIV actions,BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2007,355(4):1091-1095
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