GABA A Receptor-Mediated Sleep-Promoting Effect of Saaz-Saphir Hops Mixture Containing Xanthohumol and Humulone

• Published in: Molecules (Basel, Switzerland) Switzerland), 2021-12, Vol.26 (23)
• Main Authors: Min, Byungjick, Ahn, Yejin, Cho, Hyeok-Jun, Kwak, Woong-Kwon, Suh, Hyung Joo, Jo, Kyungae
• Format: Article
• Language: English
• Subjects: Acids - chemistry; Animals; Bicuculline - pharmacology; Caffeine - adverse effects; Cyclohexenes - chemistry; Cyclohexenes - pharmacology; Disease Models, Animal; Electroencephalography; Flavonoids - chemistry; Flavonoids - pharmacology; GABA-A Receptor Agonists - chemistry; GABA-A Receptor Agonists - pharmacology; gamma-Aminobutyric Acid - genetics; Humans; Humulus - chemistry; Hypnotics and Sedatives - chemistry; Hypnotics and Sedatives - pharmacology; Mice; Picrotoxin - pharmacology; Propiophenones - chemistry; Propiophenones - pharmacology; Receptors, GABA-A - genetics; Sleep - drug effects; Sleep - physiology; Sleep Initiation and Maintenance Disorders - chemically induced; Sleep Initiation and Maintenance Disorders - drug therapy; Sleep Initiation and Maintenance Disorders - pathology; Terpenes - chemistry; Terpenes - pharmacology
• ISSN: 1420-3049
• DOI: 10.3390/molecules26237108

Hops contain flavonoids that have sedative and sleep-promoting activities such as α-acid, β-acid, and xanthohumol. In this study, the sleep-enhancing activity of a Saaz-Saphir hops mixture was measured. In the caffeine-induced insomnia model, the administration of a Saaz-Saphir mixture increased the sleep time compared to Saaz or Saphir administration alone, which was attributed to the increase in NREM sleep time by the δ-wave increase. Oral administration of the Saaz-Saphir mixture for 3 weeks increased the γ-amino butyric acid (GABA) content in the brain and increased the expression of the GABA receptor. As the GABA antagonists picrotoxin and bicuculline showed a decrease in sleep activity, it was confirmed that the GABA receptor was involved in the Saaz-Saphir mixture activity. In addition, the GABA receptor antagonist also reduced the sleep activity induced by xanthohumol and humulone contained in the Saaz-Saphir mixture. Therefore, xanthohumol and humulone contained in the Saaz-Saphir mixture showed sleep-promoting activity mediated by the GABA receptors. The mixture of the Saaz and Saphir hop varieties may thus help mitigate sleep disturbances compared to other hop varieties.