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...

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Veröffentlicht in:Pharmacology, biochemistry and behavior biochemistry and behavior, 2003-06, Vol.75 (3), p.537-545
Hauptverfasser: Marder, Mariel, Viola, Haydeé, Wasowski, Cristina, Fernández, Sebastián, Medina, Jorge H, Paladini, Alejandro C
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container_issue 3
container_start_page 537
container_title Pharmacology, biochemistry and behavior
container_volume 75
creator Marder, Mariel
Viola, Haydeé
Wasowski, Cristina
Fernández, Sebastián
Medina, Jorge H
Paladini, Alejandro C
description 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 2 S(−)-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.
doi_str_mv 10.1016/S0091-3057(03)00121-7
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subjects 6-Methylapigenin
Animals
Anxiolysis
Benzodiazepine binding site
Central Nervous System Agents - chemistry
Central Nervous System Agents - pharmacology
Central Nervous System Agents - therapeutic use
CNS
Dose-Response Relationship, Drug
Drug Synergism
Flavonoids
Flavonoids - chemistry
Flavonoids - pharmacology
Flavonoids - therapeutic use
GABA A receptor
Hesperidin
Hesperidin - chemistry
Hesperidin - pharmacology
Hesperidin - therapeutic use
Hypnosis
Male
Mice
Motor Activity - drug effects
Motor Activity - physiology
Phytotherapy - methods
Plant Extracts - chemistry
Plant Extracts - pharmacology
Plant Extracts - therapeutic use
Plant Roots
Rats
Rats, Wistar
Rhizome
Sedation
Sleep - drug effects
Sleep - physiology
Valerian
Valeriana
title 6-Methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS
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