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Sedative and hypnotic effects of icariin through the GABAergic system pathway
Wenbin Dai1, Wenwen Zhu1, Lishan Huang1
1Geriatric Department, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou, Sichuan, China.
Background:
Icariin (ICA) is a bioactive monomer derived from Epimedium. The aim of this study was to evaluate the sedative-hypnotic effect of ICA and to investigate its mechanism.
Methods:
C57BL/6J mice were injected intraperitoneally with a suspension of PCPA (300 mg/kg) for two consecutive days to establish an insomnia model. Three different doses of ICA (50, 100, and 200 mg/kg/day) were given to C57BL/6J mice for 7 days. The weight changes were measured, and open field tests and pentobarbital sodium-induced sleep tests were conducted. The levels of 5-hydroxytryptamine (5-HT) and γ-Aminobutyric acid (GABA) in the cerebral cortex, hippocampus, and hypothalamus were measured using enzyme-linked immunosorbent assay (ELISA) kits. The expression of GABAAα1 and GABAAγ2 was measured by Western blot (WB) and Real-time PCR (qPCR).
Results:
Notably, ICA increased body weight, shortened sleep latency, and prolonged sleep duration in insomniac mice. Furthermore, ICA effectively increased the contentl of GABA and 5-HT in the brain tissue of insomnia mice. Moreover, ICA significantly increased the expression of GABAAα1 and GABAAγ2 in insomnia mice.
Conclusion:
ICA showed significant sedative-hypnotic effects in insomnia mice through the GABAergic system pathway.
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