seed ethanol extract and its active component kaempferol potentiate pentobarbital-induced sleeping behaviours in mice via a GABAergic mechanism.

Context: Lam. (Moringaceae) (MO) is an important food plant that has high nutritional and medical value. However, there is limited information on whether its seeds can improve sleep.

Objective: This study investigated the effects of MO seed ethanol extracts (EEMOS) on sleep activity improvement and examined the underlying mechanisms.

Materials And Methods: Male ICR mice were placed into six groups ( = 12) and treated as follows: Control (sodium carboxymethyl cellulose, 20 mL/kg), estazolam tablets (2 mg/kg), EEMOS (1, 2 g/kg) and kaempferol (1, 2 mg/kg). These samples were successively given intragastric for 14 d. Locomotor activity assay, pentobarbital-induced sleeping and pentetrazol-induced seizures tests were utilized to examine the sedative-hypnotic effects (SHE) of EEMOS.

Results: Compared with the control group, the results revealed that EEMOS (2 g/kg) and KA (2 mg/kg) possessed good SHE and could significantly elevate the levels of γ-aminobutyric acid and reduce the levels of glutamic acid in the mouse hypothalamus ( < 0.05). Moreover, SHE was blocked by picrotoxin, flumazenil and bicuculline ( < 0.05). EEMOS (2 g/kg) and KA (2 mg/kg) significantly upregulated the protein expression levels of glutamic acid decarboxylase-65 (GAD) and α-subunit of GABA receptors in the hypothalamus of mice ( < 0.05), not affecting glutamic acid decarboxylase-67 (GAD) and γ-subunit expression levels ( > 0.05). Additionally, they cause a significant increase in Cl influx in human cerebellar granule cells at a concentration of 8 µg/mL (  <  0.05).

Discussion And Conclusions: These findings demonstrated that EEMOS could improve sleep by regulating GABA-ergic systems, and encourage further clinical trials to treat insomnia.