Qu Zhuo, Zhang Jingze, Gao Wenyuan, Guo Huimin, Liu Changxiao
School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
Department of Pharmacy, Logistics College of Chinese People's Armed Police Forces, Tianjin Key Laboratory of Cardiovascular Remodeling and Target Organ Injury, Tianjin 300162, China.
J Ethnopharmacol. 2014 Aug 8;155(1):203-12. doi: 10.1016/j.jep.2014.05.017. Epub 2014 Jun 11.
Wei-Chang-An pill (WCA pill), a traditional Chinese medicine, has been used for treating various gastrointestinal diseases for several decades. Despite the popular medicinal use of WCA pill, less data was available to its activity and mechanism in gastrointestinal disorders. To examine the effects of the methanol extract of WCA pill (ME) on gastrointestinal tract so as to assess some of the possible mechanisms involved in the clinical treatment.
ME was studied on gastrointestinal transit in vivo including gastric emptying and small intestinal motility in normal and neostigmine-induced mice, as well as on the isolated tissue preparations of rat jejunum in vitro.
In vivo, the gastric emptying decreased and intestinal transit increased after administration of ME in normal mice. However, administration of ME accelerated the intestinal transit ranging from 0.01 to 0.8 mg/mL and reduced it at the concentration of 1.6 and 3.2 mg/mL, while the gastric emptying was inhibited throughout the concentrations in neostigmine-induced mice. in vitro, ME caused inhibitory effect on the spontaneous contraction of rat-isolated jejunum in dose-dependent manner ranging from 0.01 to 6 mg/mL and also relaxed the acetylcholine chloride (Ach, 10(-6) M)-induced and K+ (60 mM)-induced contractions. ME shifted the Ca2+ concentration-response curves to right, similar to that caused by verapamil (0.025 mM).
These results indicated that ME might play a bidirectional role in gastrointestinal transit modulation and the effects on isolated tissue are probably mediated through calcium influx and muscarinic receptors, which provides pharmacological basis for the clinical use of WCA pill in gastrointestinal tract disorders.
胃肠安丸(WCA丸)是一种传统中药,已用于治疗各种胃肠道疾病数十年。尽管WCA丸在医学上广泛应用,但其在胃肠道疾病中的活性和作用机制的数据较少。为了研究胃肠安丸甲醇提取物(ME)对胃肠道的影响,以评估其临床治疗中可能涉及的一些机制。
研究ME对正常小鼠和新斯的明诱导小鼠的体内胃肠转运,包括胃排空和小肠运动,以及对大鼠空肠离体组织标本的体外作用。
在体内,正常小鼠给予ME后胃排空减少,肠转运增加。然而,给予ME在0.01至0.8mg/mL范围内加速肠转运,在1.6和3.2mg/mL浓度时减少肠转运,而在新斯的明诱导的小鼠中,在所有浓度下胃排空均受到抑制。在体外,ME在0.01至6mg/mL范围内对大鼠离体空肠的自发收缩产生剂量依赖性抑制作用,并且还松弛了氯化乙酰胆碱(Ach,10(-6)M)诱导的和K+(60mM)诱导的收缩。ME将Ca2+浓度-反应曲线向右移动,类似于维拉帕米(0.025mM)引起的移动。
这些结果表明,ME可能在胃肠转运调节中起双向作用,对离体组织的作用可能通过钙内流和毒蕈碱受体介导,这为胃肠安丸在胃肠道疾病中的临床应用提供了药理学依据。