Laboratory of Physiology, Department of Basic Veterinary Science, The United Graduate School of Veterinary Sciences, 1-1 Yanagido, Gifu 501-1193, Japan.
J Nat Med. 2011 Jan;65(1):89-94. doi: 10.1007/s11418-010-0463-0. Epub 2010 Aug 27.
Ginger (rhizome of Zingiber officinale Roscoe) is an herbal medicine for the treatment of gastrointestinal disorders including constipation and diarrhea. Zingerone is a likely active constituent responsible for the antidiarrheal activity of ginger. The current study was designed to characterize pharmacological actions of zingerone on colonic motility. To evaluate pharmacological effects of zingerone on colonic motility, we used isolated colonic segments from rats, in which mechanical responses were recorded in the longitudinal direction. In addition, we evaluated the effects on colonic motility in vivo by measuring intraluminal pressure changes and expelled fluid volume from the colon in anesthetized rats. Zingerone was applied to the lumen of the colon to allow the drug to access from the mucosal side. Zingerone inhibited spontaneous contractile movements in the isolated colonic segments in a dose-dependent manner. The inhibitory effects of zingerone on colonic movements were not affected by pretreatment with capsazepine, a typical antagonist of transient receptor potential vanilloid 1. In addition, tetrodotoxin, a blocker of voltage-dependent sodium channels on neurons, did not affect the suppression of colonic movements by zingerone, suggesting that zingerone acts on the smooth muscles directly. Zingerone also attenuated colonic motility in vivo without affecting blood pressure and heart rate. The effects were reversible and reproducible. Our findings suggest that zingerone can inhibit colonic motility via direct action on smooth muscles. Zingerone might exert beneficial therapeutic effects on hypermotility-induced diarrhea by abrogating excessive gastrointestinal motility.
生姜（姜科姜属植物的根茎）是一种治疗胃肠道疾病的草药，包括便秘和腹泻。姜酮是一种可能的活性成分，负责生姜的抗腹泻活性。本研究旨在表征姜酮对结肠运动的药理作用。为了评估姜酮对结肠运动的药理作用，我们使用了从大鼠分离的结肠段，其中在纵向方向上记录机械反应。此外，我们通过测量麻醉大鼠结肠腔内压力变化和从结肠排出的液体量来评估姜酮对体内结肠运动的影响。将姜酮应用于结肠腔，使药物从黏膜侧进入。姜酮以剂量依赖的方式抑制分离的结肠段中的自发性收缩运动。姜酮对结肠运动的抑制作用不受辣椒素预处理的影响，辣椒素是瞬时受体电位香草素 1 的典型拮抗剂。此外，河豚毒素，一种神经元电压依赖性钠通道的阻断剂，不影响姜酮对结肠运动的抑制作用，表明姜酮直接作用于平滑肌。姜酮还可抑制体内结肠运动而不影响血压和心率。这种作用是可逆和可重复的。我们的研究结果表明，姜酮可以通过直接作用于平滑肌来抑制结肠运动。姜酮可能通过消除过度的胃肠道运动对运动性腹泻发挥有益的治疗作用。
