6-methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS.
Valerian is an ancient tranquillizing drug obtained from the underground organs of several Valeriana species. Its active principles were assumed to be terpenoids in the form of valepotriates and/or as components of the essential oil. However, unknown active compounds were not discarded and synergic effects were suspected. We have recently isolated 6-methylapigenin (MA) from Valeriana wallichii and proved that it is a benzodiazepine binding site (BDZ-bs) ligand [Planta Med. 68 (2002) 934]. The present paper is the first report of the presence of 2S(-)-hesperidin in valeriana and describes that it has sedative and sleep-enhancing properties. MA, in turn, was found to have anxiolytic properties and was able to potentiate the sleep-enhancing properties of hesperidin (HN).MA and HN are new members of the growing family of natural flavonoids with activity on the CNS, and their properties suggest that they are promising drug leads in the field.
Marder
Mariel
M
Facultad de Farmacia y Bioquímica, Instituto de Química y Fisicoquímica Biológicas, Junín 956 (1113), Buenos Aires, Argentina.
Viola
Haydeé
H
Wasowski
Cristina
C
Fernández
Sebastián
S
Medina
Jorge H
JH
Paladini
Alejandro C
AC
D000818:Animals; D002491:Central Nervous System Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006569:Hesperidin / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects / Q000502:physiology; D008517:Phytotherapy / Q000379:methods; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D018517:Plant Roots; D051381:Rats; D017208:Rats, Wistar; D027343:Rhizome; D012890:Sleep / Q000187:drug effects / Q000502:physiology; D014632:Valerian
C469106:6-methylapigenin; D002491:Central Nervous System Agents; D005419:Flavonoids; D010936:Plant Extracts; D006569:Hesperidin