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

	Flazinamide, a novel beta-carboline compound with anti-HIV actions
	Wang YH 1,4; Tang JG 2,4; Wang RR 1,4; Yang LM 1; Dong ZJ 2; Du L 3,4; Shen X 3; Liu JK2; Zheng YT1; zhengyt@mail.kiz.ac.cn
	2007
发表期刊	BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
ISSN	0006-291X
卷号	355 期号:4 页码:1091-1095
合作性质	其它
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.
关键词	B-carboline Flazinamide Synthesis Anti-hiv Agents Hiv-1 Hiv-2
资助者	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. ; 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. ; 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. ; 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.
URL	查看原文
收录类别	SCI
语种	英语
资助者	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. ; 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. ; 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. ; 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.
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/4605
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者	zhengyt@mail.kiz.ac.cn
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.,...&zhengyt@mail.kiz.ac.cn.(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.

条目包含的文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
20073551091.pdf（197KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	请求全文