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- Title
Souroubea sympetala (Marcgraviaceae): a medicinal plant that exerts anxiolysis through interaction with the GABA<sub>A</sub> benzodiazepine receptor.
- Authors
Mullally, Martha; Cayer, Christian; Kramp, Kari; Otárola Rojas, Marco; Sanchez Vindas, Pablo; Garcia, Mario; Poveda Alvarez, Luis; Durst, Tony; Merali, Zul; Trudeau, Vance L.; Arnason, John T.
- Abstract
The mode of action of the anxiolytic medicinal plant Souroubea sympetala was investigated to test the hypothesis that extracts and the active principle act at the pharmacologically important GABAA-benzodiazepine (GABAA-BZD) receptor. Leaf extracts prepared by ethyl acetate extraction or supercritical extraction, previously determined to have 5.54 mg/g and 6.78 mg/g of the active principle, betulinic acid, respectively, reduced behavioural parameters associated with anxiety in a rat model. When animals were pretreated with the GABAA-BZD receptor antagonist flumazenil, followed by the plant extracts, or a more soluble derivative of the active principle, the methyl ester of betulinic acid (MeBA), flumazenil eliminated the anxiety-reducing effect of plant extracts and MeBA, demonstrating that S. sympetala acts via an agonist action on the GABAA-BZD receptor. An in vitro GABAA-BZD competitive receptor binding assay also demonstrated that S. sympetala extracts have an affinity for the GABAA-BZD receptor, with an EC50 value of 123 μg/mL (EtOAc leaf extract) and 154 μg/mL (supercritical CO2 extract). These experiments indicate that S. sympetala acts at the GABAA-BZD receptor to elicit anxiolysis.
- Subjects
MEDICINAL plants; PLANT extracts; ANGIOSPERMS; ETHYL acetate; BENZODIAZEPINE receptors; TRANQUILIZING drugs; ANXIETY
- Publication
Canadian Journal of Physiology & Pharmacology, 2014, Vol 92, Issue 9, p758
- ISSN
0008-4212
- Publication type
Article
- DOI
10.1139/cjpp-2014-0213