title: NF-kappaB modulators from Valeriana officinalis.
abstract: Valeriana officinalis (Valerianaceae) has been of great interest for its therapeutic uses for treating mild nervous tension and temporary sleeping problems. In traditional European medicine it has been also reported as an antiinflammatory remedy. This study reports that the EtOAc extract of the underground parts of V. officinalis showed inhibitory activity against NF-kappaB at 100 microg/mL in the IL-6/Luc assay on HeLa cells and provided protection against excitotoxicity in primary brain cell cultures at micromolar concentrations. Bioassay-guided fractionation of the EtOAc extract led to the isolation of three known sesquiterpenes: acetylvalerenolic acid (1), valerenal (2) and valerenic acid (3), 1 and 3 were active as inhibitors of NF-kappaB at a concentration of 100 microg/mL. Acetylvalerenolic acid (1) reduced NF-kappaB activity to 4%, whereas valerenic acid (3) reduced NF-kappaB activity to 25%.
authors.affiliation: Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, UK.
authors.forename: Nadia J
authors.initials: NJ
authors.lastname: Jacobo-Herrera
authors.forename: Nina
authors.initials: N
authors.lastname: Vartiainen
authors.forename: Paul
authors.initials: P
authors.lastname: Bremner
authors.forename: Simon
authors.initials: S
authors.lastname: Gibbons
authors.forename: Jari
authors.initials: J
authors.lastname: Koistinaho
authors.forename: Michael
authors.initials: M
authors.lastname: Heinrich
mesh_terms: D001253:Astrocytes / Q000166:cytology / Q000187:drug effects; D018920:Coculture Techniques; D006367:HeLa Cells; D006801:Humans; D007608:Kainic Acid / Q000037:antagonists & inhibitors; D016202:N-Methylaspartate / Q000037:antagonists & inhibitors; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D009474:Neurons / Q000166:cytology / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014632:Valerian / Q000737:chemistry*
chemical_list: D016328:NF-kappa B; D010936:Plant Extracts; D016202:N-Methylaspartate; D007608:Kainic Acid