Aconitum Alkaloid Songorine Exerts Potent Gamma-Aminobutyric Acid-A Receptor Agonist Action In Vivo and Effectively Decreases Anxiety without Adverse Sedative or Psychomotor Effects in the Rat

Songorine (SON) is a diterpenoid alkaloid from Aconitum plants. Preparations of Aconitum roots have been employed in traditional oriental herbal medicine, however, their mechanisms of action are still unclear. Since GABA-receptors are possible brain targets of SON, we investigated which subtypes of...

Teljes leírás

Elmentve itt :
Bibliográfiai részletek
Szerzők: Bali Zsolt Kristóf
Bruszt Nóra
Kőszegi Zsombor
Nagy Lili Veronika
Atlasz Tamás
Kovács Péter
Csupor Dezső
Csupor-Löffler Boglárka
Hernádi István
Dokumentumtípus: Cikk
Megjelent: 2022
Sorozat:PHARMACEUTICS 14 No. 10
Tárgyszavak:
doi:10.3390/pharmaceutics14102067

mtmt:33117614
Online Access:http://publicatio.bibl.u-szeged.hu/26074
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520 3 |a Songorine (SON) is a diterpenoid alkaloid from Aconitum plants. Preparations of Aconitum roots have been employed in traditional oriental herbal medicine, however, their mechanisms of action are still unclear. Since GABA-receptors are possible brain targets of SON, we investigated which subtypes of GABA-receptors contribute to the effects of SON, and how SON affects anxiety-like trait behavior and psychomotor cognitive performance of rats. First, we investigated the effects of microiontophoretically applied SON alone and combined with GABA-receptor agents picrotoxin and saclofen on neuronal firing activity in various brain areas. Next, putative anxiolytic effects of SON (1.0–3.0 mg/kg) were tested against the GABA-receptor positive allosteric modulator reference compound diazepam (1.0–5.0 mg/kg) in the elevated zero maze (EOM). Furthermore, basic cognitive effects were assessed in a rodent version of the psychomotor vigilance task (PVT). Local application of SON predominantly inhibited the firing activity of neurons. This inhibitory effect of SON was successfully blocked by GABA(A)-receptor antagonist picrotoxin but not by GABA(B)-receptor antagonist saclofen. Similar to GABA(A)-receptor positive allosteric modulator diazepam, SON increased the time spent by animals in the open quadrants of the EOM without any signs of adverse psychomotor and cognitive effects observed in the PVT. We showed that, under in vivo conditions, SON acts as a potent GABA(A)-receptor agonist and effectively decreases anxiety without observable side effects. The present findings facilitate the deeper understanding of the mechanism of action and the widespread pharmacological use of diterpene alkaloids in various CNS indications. 
650 4 |a Általános orvostudomány 
650 4 |a Farmakológia és gyógyszerészet 
700 0 1 |a Bruszt Nóra  |e aut 
700 0 1 |a Kőszegi Zsombor  |e aut 
700 0 1 |a Nagy Lili Veronika  |e aut 
700 0 1 |a Atlasz Tamás  |e aut 
700 0 1 |a Kovács Péter  |e aut 
700 0 1 |a Csupor Dezső  |e aut 
700 0 2 |a Csupor-Löffler Boglárka  |e aut 
700 0 2 |a Hernádi István  |e aut 
856 4 0 |u http://publicatio.bibl.u-szeged.hu/26074/1/pharmaceutics-14-02067-v2.pdf  |z Dokumentum-elérés