Titre du document / Document title

Kavalactones and dihydrokavain modulate GABAergic activity in a rat gastric-brainstem preparation

Auteur(s) / Author(s)

YUAN Chun-Su ^{(1 2 3)} ; DEY Lucy ^{(1 3)} ; ANBAO WANG ^{(1 3)} ; MEHENDALE Sangeeta ^{(1 3)} ; XIE Jing-Tian ^{(1 3)} ; AUNG Han H. ^{(1 3)} ; ANG-LEE Michael K. ⁽³⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Tang Center for Herbal Medicine Research, The Pritzker School of Medicine, University of Chicago, Chicago, ETATS-UNIS
⁽²⁾ Committee on Clinical Pharmacology, The Pritzker School of Medicine, University of Chicago, Chicago, ETATS-UNIS
⁽³⁾ Department of Anesthesia & Critical Care, The Pritzker School of Medicine, University of Chicago, Chicago, ETATS-UNIS

Résumé / Abstract

Using an in vitro neonatal rat gastric-brainstem preparation, the activity of majority neurons recorded in the nucleus tractus solitarius (NTS) of the brainstem were significantly inhibited by GABAA receptor agonist, muscimol (30 pM), and this inhibition was reversed by selective GABA_A receptor antagonist, bicuculline (10 μM). Application of kavalactones (300 μg/ml) and dihydrokavain (300 μM) into the brainstem compartment of the preparation also significantly reduced the discharge rate of these NTS neurons (39% and 32%, respectively, compared to the control level), and this reduction was partially reversed by bicuculline (10 μM). Kavalactones or dihydrokavain induced inhibitory effects were not reduced after co-application of saclofen (10 μM; a selective GABA_B receptor antagonist) or naloxone (100 nM; an opioid receptor antagonist). Pretreatment with kavalactones (300 μg/ml) or dihydrokavain (300 μM) significantly decreased the NTS inhibitory effects induced by muscimol (30 μM), approximately from 51 % to 36%. Our results demonstrated modulation of brainstem GABAergic mechanism by kavalactones and dihydrokavain, and suggested that these compounds may play an important role in regulation of GABAergic neurotransmission.

Revue / Journal Title

Planta medica   ISSN 0032-0943   CODEN PLMEAA 

Source / Source

2002, vol. 68, n^o12, pp. 1092-1096 [5 page(s) (article)] (20 ref.)

Langue / Language

Anglais

Editeur / Publisher

Thieme, Stuttgart, ALLEMAGNE  (1953) (Revue)

Mots-clés anglais / English Keywords

Spermatophyta ; Angiospermae ; Dicotyledones ; Piperaceae ; Vertebrata ; Mammalia ; Rodentia ; Acids ; Biological fixation ; Biological activity ; In vitro ; Central nervous system ; Brain (vertebrata) ; Solitary nucleus ; Neuron ; Piper ; Gabaergic transmission ; Gabaergic receptor A ; Rat ; Animal ; Pharmacognosy ; Medicinal plant ; Plant origin ;

Mots-clés français / French Keywords

Spermatophyta ; Angiospermae ; Dicotyledones ; Piperaceae ; Vertebrata ; Mammalia ; Rodentia ; Piper methysticum ; Acide ; Fixation biologique ; Activité biologique ; In vitro ; Système nerveux central ; Encéphale ; Noyau faisceau solitaire ; Neurone ; Piper ; Transmission gabaergique ; Récepteur gabaergique A ; Rat ; Animal ; Pharmacognosie ; Plante médicinale ; Origine végétale ;

Mots-clés espagnols / Spanish Keywords

Spermatophyta ; Angiospermae ; Dicotyledones ; Piperaceae ; Vertebrata ; Mammalia ; Rodentia ; Acido ; Fijación biológica ; Actividad biológica ; In vitro ; Sistema nervioso central ; Encéfalo ; Núcleo fascículo solitario ; Neurona ; Piper ; Transmisión gabaérgica ; Receptor gabaminérgico A ; Rata ; Animal ; Farmacognosia ; Planta medicinal ; Origen vegetal ;

Mots-clés d'auteur / Author Keywords

Kava ; Piper methysticum ; Piperaceae ; kavalactones ; dihydrokavain brainstem ; nucleus tractus solitarius ; gastric vagal input ; gamma-aminobutyric acid (GABA) ;

Localisation / Location

INIST-CNRS, Cote INIST : 9624, 35400010722354.0090