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

Abstract
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.
AuthorsYun-Hua Wang, Jian-Guo Tang, Rui-Rui Wang, Liu-Meng Yang, Ze-Jun Dong, Li Du, Xu Shen, Ji-Kai Liu, Yong-Tang Zheng
JournalBiochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 355 Issue 4 Pg. 1091-5 (Apr 20 2007) ISSN: 0006-291X [Print] United States
PMID17336271 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-HIV Agents
  • Carbolines
  • Furans
  • flazinamide
  • HIV Integrase
Topics
  • Anti-HIV Agents (chemistry, pharmacology, toxicity)
  • Carbolines (chemistry, pharmacology, toxicity)
  • Cell Line
  • Cell Survival (drug effects)
  • Furans (chemistry, pharmacology, toxicity)
  • HIV Integrase (metabolism)
  • HIV-1 (drug effects, physiology)
  • Molecular Structure
  • Protein Binding
  • Virus Replication (drug effects)

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