4-phenylcoumarins as HIV transcription inhibitors

We have evaluated the anti-HIV activity of eleven natural 4-phenylcoumarins isolated from Marila pluricostata and three of their derivatives. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase gene as reporter. Inhibitions of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Most of the coumarins tested displayed NF-kappa B inhibition. Two cournarins were also Tat antagonists and the presence of both activities correlated with a stronger inhibition of HIV replication. Our results show that antiviral effect of 4-phenylcoumarins can be related to the inhibition of NF-kappa B and Tat, and suggest that these types of compounds can be useful in the treatment of HIV infection as viral transcription inhibitors. (c) 2005 Elsevier Ltd. All rights reserved.