Gabaa receptor-mediated sleep-promoting effect of saaz–saphir hops mixture containing xanthohumol and humulone

Byungjick Min, Yejin Ahn, Hyeok Jun Cho, Woong Kwon Kwak, Hyung Joo Suh, Kyungae Jo

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


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, xantho-humol 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.

Original languageEnglish
Article number7108
Issue number23
Publication statusPublished - 2021 Dec 1

Bibliographical note

Funding Information:
Funding: This research was supported by Lotte Chilsung Beverage Co., Ltd. (Q2018291).

Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.


  • GABAA receptor
  • Hop
  • Humulone
  • Saaz
  • Sapir
  • Xanthohumol

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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