Guo Huimin, Zhang Jingze, Gao Wenyuan, Qu Zhuo, Liu Changxiao
Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
Department of Pharmacy, Logistics College of Chinese People's Armed Police Forces, Tianjin 300162, China.
J Ethnopharmacol. 2014 Jul 3;154(3):704-10. doi: 10.1016/j.jep.2014.04.043. Epub 2014 May 6.
ETHNOPHARMACOLOGICAL RELEVANCE: Santalum album L., namely Sandalwood, honored as "Green Gold", is a traditional Chinese herb which has the effects of anti-diarrhoeal and antibacterial activity. But there is limit scientific study on its activity and mechanism in gastrointestinal disorders. MATERIALS AND METHODS: in vivo, after intragastric administration, the methanol extract of Sandalwood (SE) (200, 400 and 800 mg/kg) were studied in castor oil-induced diarrhoea mice. By the test of small intestinal hyperfunction induced by neostigmine, SE was studied on gastrointestinal transit including gastric emptying and small intestinal motility. Meanwhile, in vitro, the effects of SE (0.02, 0.05, 0.1, 0.2, 0.3, 0.4 mg/mL) on the isolated tissue preparations of rat jejunum were also investigated. The rat jejunum strips were pre-contracted with acetylcholine (Ach; 10(-6)M), 5-hydroxytryptamine (5-HT, 200 μM) or potassium chloride (KCl; 60 mM) and tested in the presence of SE. In addition, the possible myogenic effect was analyzed in the pretreatment of the jejunum preparations with SE or verapamil in Ca(2+)-free high-K(+) (60 mM) solution containing EDTA. RESULTS: At doses of 200, 400 and 800 mg/kg, SE showed significant anti-diarrhoeal activity against castor oil-induced diarrhoea as compared with the control. At the same doses, it also inhibited the gastric emptying and small intestinal motility in the mice of which small intestinal hyperfunction induced by neostigmine. It caused inhibitory effects on the spontaneous contraction of rat-isolated jejunum in dose-dependent manner ranging from 0.02 to 0.4 mg/mL, and it also relaxed the Ach-induced, 5-HT-induced and K(+)-induced contractions. SE shifted the Ca(2+) concentration-response curves to right, similar to that caused by verapamil (0.025 mM). CONCLUSIONS: These findings indicated that SE played a spasmolytic role in gastrointestinal motility which was probably mediated through inhibition of muscarinic receptors, 5-HT receptors and calcium influx. All these results provide pharmacological basis for its clinical use in gastrointestinal tract.
民族药理学相关性：檀香，即白檀，被誉为“绿色黄金”，是一种具有止泻和抗菌活性的传统中草药。但目前对其在胃肠道疾病中的活性和作用机制的科学研究有限。 材料与方法：在体内，灌胃给药后，研究檀香甲醇提取物（SE）（200、400和800mg/kg）对蓖麻油诱导腹泻小鼠的影响。通过新斯的明诱导的小肠功能亢进试验，研究SE对包括胃排空和小肠运动在内的胃肠转运的影响。同时，在体外，还研究了SE（0.02、0.05、0.1、0.2、0.3、0.4mg/mL）对大鼠空肠离体组织标本的作用。大鼠空肠条先用乙酰胆碱（Ach；10(-6)M）、5-羟色胺（5-HT，200μM）或氯化钾（KCl；60mM）预收缩，然后在SE存在下进行测试。此外，在不含钙的高钾（60mM）溶液中，用SE或维拉帕米预处理空肠标本，分析其可能的肌源性作用。 结果：与对照组相比，200、400和800mg/kg剂量的SE对蓖麻油诱导的腹泻具有显著的止泻活性。在相同剂量下，它还抑制了新斯的明诱导的小肠功能亢进小鼠的胃排空和小肠运动。它对大鼠离体空肠的自发收缩有剂量依赖性的抑制作用，范围为0.02至0.4mg/mL，并且还能松弛Ach诱导、5-HT诱导和K(+)诱导的收缩。SE使Ca(2+)浓度-反应曲线右移，类似于维拉帕米（0.025mM）引起的右移。 结论：这些发现表明，SE在胃肠运动中起解痉作用，可能是通过抑制毒蕈碱受体、5-HT受体和钙内流介导的。所有这些结果为其在胃肠道疾病中的临床应用提供了药理学依据。
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