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GABAA Receptor-Mediated Sleep-Promoting Effect of Saaz–Saphir Hops Mixture Containing Xanthohumol and Humulone
Authors:Byungjick Min  Yejin Ahn  Hyeok-Jun Cho  Woong-Kwon Kwak  Hyung Joo Suh  Kyungae Jo
Affiliation:1.Department of Integrated Biomedical and Life Science, Graduate School, Korea University, Seoul 02841, Korea; (B.M.); (Y.A.); (H.J.S.);2.Lotte R&D Center, Seoul 07594, Korea; (H.-J.C.); (W.-K.K.);3.Transdisciplinary Major in Learning Health Systems, Graduate School, Korea University, Seoul 02841, Korea
Abstract: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 GABAA receptor. As the GABA antagonists picrotoxin and bicuculline showed a decrease in sleep activity, it was confirmed that the GABAA receptor was involved in the Saaz–Saphir mixture activity. In addition, the GABAA 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 GABAA receptors. The mixture of the Saaz and Saphir hop varieties may thus help mitigate sleep disturbances compared to other hop varieties.
Keywords:hop   Saaz   Sapir   xanthohumol   humulone   GABAA receptor
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