title: 4-Phenylcoumarins as HIV transcription inhibitors.
abstract: 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-kappaB inhibition. Two coumarins 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-kappaB and Tat, and suggest that these types of compounds can be useful in the treatment of HIV infection as viral transcription inhibitors.
authors.affiliation: Unidad de Inmunopatalogía, Centro Nacional de Microbiología, Instituto de Salud Carlos III, 28220-Majadahonda, Madrid, Spain.
authors.forename: Luis M
authors.initials: LM
authors.lastname: Bedoya
authors.forename: Manuela
authors.initials: M
authors.lastname: Beltrán
authors.forename: Rocío
authors.initials: R
authors.lastname: Sancho
authors.forename: Dionisio A
authors.initials: DA
authors.lastname: Olmedo
authors.forename: Sonsoles
authors.initials: S
authors.lastname: Sánchez-Palomino
authors.forename: Esther
authors.initials: E
authors.lastname: del Olmo
authors.forename: José L
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Eduardo
authors.initials: E
authors.lastname: Muñoz
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
authors.forename: José
authors.initials: J
authors.lastname: Alcamí
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology*; D015696:Gene Products, tat / Q000037:antagonists & inhibitors; D006678:HIV / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D006367:HeLa Cells; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors; D014158:Transcription, Genetic / Q000187:drug effects*; D014779:Virus Replication; D054322:tat Gene Products, Human Immunodeficiency Virus
chemical_list: D019380:Anti-HIV Agents; D003374:Coumarins; D015696:Gene Products, tat; D016328:NF-kappa B; D054322:tat Gene Products, Human Immunodeficiency Virus; C094411:4-phenylcoumarin