Pachymic Acid Enhances Pentobarbital-Induced Sleeping Behaviors via GABAA-ergic Systems in Mice
| Autor: | Jin Tae Hong, Vikash Kumar Shah, Mi Kyeong Lee, Jin-Yi Han, Ki-Wan Oh, Jae Joon Choi |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Pachymic acid (PA)
Pentobarbital Insomnia medicine.drug_class Pharmacology Biochemistry Hypnotic chemistry.chemical_compound Oral administration Drug Discovery medicine Receptor Glutamic acid decarboxylase (GAD) business.industry GABAA receptor GABAA receptors Poria cocos (Hoelen) Muscimol chemistry Pentobarbital (PENT) Molecular Medicine Original Article medicine.symptom Sleep onset business medicine.drug |
| Zdroj: | Biomolecules & Therapeutics |
| ISSN: | 2005-4483 1976-9148 |
| Popis: | This study was investigated to know whether pachymic acid (PA), one of the predominant triterpenoids in Poria cocos (Hoelen) has the sedative-hypnotic effects, and underlying mechanisms are mediated via γ-aminobutyric acid (GABA)-ergic systems. Oral administration of PA markedly suppressed locomotion activity in mice. This compound also prolonged sleeping time, and reduced sleep latency showing synergic effects with muscimol (0.2 mg/kg) in shortening sleep onset and enhancing sleep time induced by pentobarbital, both at the hypnotic (40 mg/kg) and sub-hypnotic (28 mg/kg) doses. Additionally, PA elevated intracellular chloride levels in hypothalamic primary cultured neuronal cells of rats. Moreover, Western blotting quantitative results showed that PA increased the amount of protein level expression of GAD65/67 over a broader range of doses. PA increased α- and β-subunits protein levels, but decreased γ-subunit protein levels in GABAA receptors. The present experiment provides evidence for the hypnotic effects as PA enhanced pentobarbital-induced sleeping behaviors via GABAA-ergic mechanisms in rodents. Taken together, it is proposed that PA may be useful for the treatment of sleep disturbed subjects with insomnia. |
| Databáze: | OpenAIRE |
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