Qiao Haoyi, Ye Xiansheng, Bai Xiaoyu, He Jun, Li Tingli, Zhang Jia, Zhang Weiku, Xu Jiekun
School of Life Sciences, Beijing University of Chinese Medicine, Beijing 100029, China; Institute of Clinical Medical Sciences, China-Japan Friendship Hospital, Beijing 100029, China.
School of Chinese Medicine Sciences, Beijing University of Chinese Medicine, Beijing 100029, China.
Neurosci Lett. 2017 Oct 17;659:48-53. doi: 10.1016/j.neulet.2017.08.063. Epub 2017 Aug 31.
Theacrine (l,3,7,9-tetramethyluric acid), a purine alkaloid from Camellia assamica var. kucha, has diverse pharmacological properties, including sedative and hypnotic activities, anti-inflammatory and analgesic activities, antidepressant effects, and a protective effect against stress-provoked liver damage. The present study aims to investigate the possible mechanism of the hypnotic activity of theacrine. The results revealed that theacrine significantly enhanced pentobarbital-induced sleep at a dose of 3.0mg/kg (i.g.) in mice. Sleep parameter analysis by EEG and EMG showed that theacrine obviously shortened wake time and increased NREM sleep time and that theacrine almost had no effect on REM sleep. Meanwhile, theacrine markedly attenuated caffeine (a nonselective antagonist of adenosine receptor)-induced insomnia. In pretreatment with the adenosine A receptor antagonist DPCPX and the A receptor antagonist SCH 58261, theacrine significantly reversed the decrease in sleeping time in pentobarbital-treated mice. In addition, theacrine also markedly increased the adenosine content in the hippocampus of rats. These results suggested that theacrine might mediate the adenosine system to augment pentobarbital-induced sleep.
茶氨酸（1,3,7,9 - 四甲基尿酸）是一种从普洱茶变种库车茶中提取的嘌呤生物碱，具有多种药理特性，包括镇静催眠活性、抗炎和镇痛活性、抗抑郁作用以及对应激引起的肝损伤的保护作用。本研究旨在探讨茶氨酸催眠活性的可能机制。结果显示，茶氨酸以3.0mg/kg（灌胃）的剂量显著增强了小鼠戊巴比妥诱导的睡眠。通过脑电图和肌电图进行的睡眠参数分析表明，茶氨酸明显缩短了清醒时间，增加了非快速眼动睡眠（NREM）时间，并且茶氨酸对快速眼动睡眠（REM）几乎没有影响。同时，茶氨酸显著减轻了咖啡因（一种腺苷受体非选择性拮抗剂）诱导的失眠。在用腺苷A受体拮抗剂DPCPX和A受体拮抗剂SCH 58261预处理后，茶氨酸显著逆转了戊巴比妥处理小鼠睡眠时间的减少。此外，茶氨酸还显著增加了大鼠海马体中的腺苷含量。这些结果表明，茶氨酸可能通过介导腺苷系统来增强戊巴比妥诱导的睡眠。
