Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System
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Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China
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Ministry of Education & National Engineering Laboratory for Breeding of Endangered Medicinal Materials, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China
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Hainan Provincial Key Laboratory of Resources Conservation and Development of Southern Medicine, Hainan Branch of the Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Haikou 570311, China
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Key Laboratory of State Administration of Traditional Chinese Medicine for Agarwood Sustainable Utilization, Hainan Branch of the Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Haikou 570311, China
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School of Pharmacy, Hainan Medical College, Haikou 571199, China
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Pharmacology and toxicology center, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China
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Authors to whom correspondence should be addressed.
Molecules 2017, 22(12), 2190; https://doi.org/10.3390/molecules22122190
Received: 8 November 2017
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Revised: 29 November 2017
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Accepted: 4 December 2017
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Published: 9 December 2017
(This article belongs to the Special Issue Biological Activity of Secondary Metabolites)
Although agarwood has been used as a tranquilizer in Asian countries for hundreds of years, the underlying pharmacological basis is still unclear. This study investigated the sedative-hypnotic effect of agarwood essential oil (AEO) using locomotor activity and pentobarbital-induced sleeping assays in mice. Single (1-day) and multiple (7- and 14-days) administrations of 60 mg/kg AEO generated significant sedative effect on inhibiting locomotor activity and hypnotic effect on pentobarbital-induced sleeping in mice. Interestingly, prolonged AEO treatment did not result in obvious desensitization. Concoitant measurement of the levels of brain neurotransmitters using ultrafast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) indicated that AEO had no significant effect on the levels of glutamic acid (Glu) and γ-aminobutyric acid (GABA) in the brain. However, the sedative-hypnotic effects were blocked by the type A GABA (GABAA) receptor antagonists bicuculline and flumazenil. In addition, AEO significantly elevated the expression of GABAA receptor subunits and subtypes in the cerebral cortex. Furthermore, AEO increased chlorine ion (Cl−) influx through GABAA receptors in human neuroblastoma cells. These results together demonstrate that AEO exerts its sedative-hypnotic effects through regulating gene expression of GABAA receptors and potentiating GABAA receptor function.
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MDPI and ACS Style
Wang, S.; Wang, C.; Peng, D.; Liu, X.; Wu, C.; Guo, P.; Wei, J. Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System. Molecules 2017, 22, 2190. https://doi.org/10.3390/molecules22122190
AMA Style
Wang S, Wang C, Peng D, Liu X, Wu C, Guo P, Wei J. Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System. Molecules. 2017; 22(12):2190. https://doi.org/10.3390/molecules22122190
Chicago/Turabian StyleWang, Shuai, Canhong Wang, Deqian Peng, Xinmin Liu, Chongming Wu, Peng Guo, and Jianhe Wei. 2017. "Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System" Molecules 22, no. 12: 2190. https://doi.org/10.3390/molecules22122190
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