Department of Physiology, Graduate School of Medical Science, Kanazawa University, Kanazawa, Japan.
Department of Environmental Physiology, School of Medicine, Shimane University, Izumo, Japan.
Basic Clin Pharmacol Toxicol. 2019 May;124(5):575-581. doi: 10.1111/bcpt.13175. Epub 2018 Dec 12.
Theobromine is a caffeine derivative and the primary methylxanthine in Theobroma cacao. We have shown previously that theobromine inhibits the Akt-mammalian target of rapamycin (mTOR) signal in vitro. In this study, we investigated whether orally administered theobromine could inhibit mTOR activity in rats. mTOR is phosphorylated by Akt. Thus, the level of phosphorylated mTOR was used as an index of mTOR activity. Male Wistar rats were divided into two groups. The control group (CN) was fed a normal diet, while the theobromine group (TB) was fed a diet supplemented with 0.05% theobromine for 40 days. We measured body-weights and tissue weights, food and water intake, blood count, concentrations of theobromine in the plasma, liver and brain, and the levels of phosphorylated mTOR in the liver and brain. Orally administered theobromine did not affect the body-weights and tissue weights, food and water intake, and blood count as determined by comparison with levels in rats that were fed standard chow. Theobromine was detected in the plasma, liver and brain obtained from TB rats, but was not detected in tissues obtained from CN rats. The phosphorylated mTOR levels in the liver and brain were significantly lower in TB rats than in CN rats. The results suggest that oral theobromine inhibits mTOR signalling in vivo.
可可碱是一种咖啡因衍生物,也是可可豆中主要的甲基黄嘌呤。我们之前已经表明,可可碱可以在体外抑制 Akt-雷帕霉素靶蛋白(mTOR)信号。在这项研究中,我们研究了口服可可碱是否可以抑制大鼠的 mTOR 活性。mTOR 被 Akt 磷酸化。因此,磷酸化 mTOR 的水平被用作 mTOR 活性的指标。雄性 Wistar 大鼠分为两组。对照组(CN)喂食正常饮食,而可可碱组(TB)喂食添加 0.05%可可碱的饮食 40 天。我们测量了体重和组织重量、食物和水的摄入量、血液计数、血浆、肝脏和大脑中可可碱的浓度,以及肝脏和大脑中磷酸化 mTOR 的水平。与喂食标准饲料的大鼠相比,口服可可碱对体重和组织重量、食物和水的摄入量以及血液计数没有影响。TB 大鼠的血浆、肝脏和大脑中检测到可可碱,但 CN 大鼠的组织中未检测到可可碱。TB 大鼠的肝脏和大脑中的磷酸化 mTOR 水平明显低于 CN 大鼠。结果表明,口服可可碱可抑制体内 mTOR 信号。