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

doi:10.1016/j.bbrc.2007.02.081

	Flazinamide, a novel beta-carboline compound with anti-HIV actions
	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
	2007-04-20
卷号	355 期号:4 页码:1091-1095
关键词	beta-carboline flazinamide synthesis anti-HIV agents HIV-1 HIV-2
ISSN号	0006-291X
DOI	10.1016/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.
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
出版者	ACADEMIC PRESS INC ELSEVIER SCIENCE
WOS记录号	WOS:000245115000040
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/273283]
专题	中国科学院上海药物研究所
通讯作者	Zheng, Yong-Tang
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.