Schisantherin A Exerts Sedative and Hypnotic Effects Through Regulating GABA and its Receptor in Mice and Rats

Abstract

Schisandra has been used to treat insomnia for hundreds of years in China. This study was aimed at proving the contribution of Schisantherin A (STA), the most abundant component in Schisandra, on sleeping, and uncover its mechanisms. Mouse autonomic activity and sleep tests were conducted for the behavioral examinations. The γ-aminobutyric acid (GABA), glutamic acid (Glu), and glutamic acid decarboxylase (GAD) in the blood and/or brain tissues of mice and rats were measured by enzyme-linked immunosorbent assay kits, and GABA A Rα1 and GABA A Rγ2 expressions in the brain tissues of rats were detected by reverse transcriptase polymerase chain reaction (RT-PCR) and Western blot. STA decreased the autonomic activities and sleep latency, increased the number of sleeping periods, sleep time, and duration in mice, showing a sedative and hypnotic effect. STA significantly elevated GABA, reduced Glu in the blood and brain, and increased GAD in the brain. STA upregulated the expressions of GABA A Rα1 and GABA A Rγ2 mRNA in the brain of rats. Thus, STA is an active component for sedative and hypnotic effects in Schisandra and these effects may be through its regulation of the GABA/Glu ratio, GAD, and GABA A expression in mice and rats.

Aralia continentalis Root Enhances Non-Rapid Eye Movement Sleep by Activating GABAA Receptors

“…Saponins from Ziziphus jujube seeds exert hypnotic effects on pentobarbital-induced sleep in mice models [8]. Schisantherin A from Schisandra chinensis increases the number of sleeping periods and sleep time in mice by Nutrients 2023, 15, 5020 2 of 12 regulating GABA A expression in mice and rats [9]. Marine polyphenol phlorotannins derived from Ecklonia cava demonstrate sedative-hypnotic effects in mice by acting through the GABA A -BDZ receptor [10,11].…”