a Department of Pharmacy , Special Drugs R&D Center of People's Armed Police Forces , Logistics University of Chinese People's Armed Police Forces , Tianjin , China.
b School of Pharmaceutical Science and Technology , Tianjin University , Tianjin , China.
Pharm Biol. 2018 Dec;56(1):559-566. doi: 10.1080/13880209.2018.1492000.
Aquilariae Lignum Resinatum (ALR), the dry rhizome of Aquilaria agallocha R. (Thymelaeaeeae), has been widely used to treat emesis, stomachache and gastrointestinal dysfunction.
This study evaluates the effects of ALR methanol extract on gastrointestinal motility (GIM) and possible mechanisms of the action involved.
In vivo, the study evaluated the effects of ALR (200-800 mg/kg) on gastric emptying and small intestinal motility in normal and neostigmine-induced adult KM mice. The in vitro effects of ALR (0.2-1.6 mg/mL) on GIM were performed on isolated jejunum of Wistar rats, pretreated with acetylcholine (ACh), KCl, CaCl, and pre-incubation with l-NAME (a selective inhibitor of the nitric oxide synthase).
In vivo, ALR (800 mg/kg) decreased gastric emptying (70.82 ± 9.81%, p < 0.01, compared with neostigmine group 91.40 ± 7.81%), small intestinal transit (42.82 ± 3.82%, p < 0.01, compared with neostigmine group 85.53 ± 5.57%). In vitro, ALR concentration dependently decreased the contractions induced by ACh (10 M) and KCl (60 mM) with respective EC values of 0.35 and 0.32 mg/mL. The Ca concentration-response curves were shifted by ALR to the right, similar to that caused by verapamil (the positive). The spasmolytic activity of ALR was inhibited by pre-incubation with l-NAME.
ALR played a spasmolytic role in GIM, which is probably mediated through inhibition of muscarinic receptors, blockade of Ca influx and NO release. This is the first study presenting a comprehensive description of the effects of ALR on GIM.
沉香（Aquilariae Lignum Resinatum，ALR）是瑞香科沉香属白木香Aquilaria agallocha R.（Thymelaeaeeae）的干燥根茎，被广泛用于治疗呕吐、胃痛和胃肠功能障碍。
本研究评估沉香甲醇提取物对胃肠动力（GIM）的影响及其可能的作用机制。
体内实验中，评估了沉香（200-800mg/kg）对正常和新斯的明诱导的成年 KM 小鼠胃排空和小肠运动的影响。体外实验中，采用乙酰胆碱（ACh）、KCl、CaCl 预处理的 Wistar 大鼠离体空肠，评估了沉香（0.2-1.6mg/mL）对 GIM 的作用，并用 l-NAME（一种选择性一氧化氮合酶抑制剂）进行预孵育。
体内，沉香（800mg/kg）降低胃排空率（70.82±9.81%，p<0.01，与新斯的明组 91.40±7.81%相比）和小肠传输率（42.82±3.82%，p<0.01，与新斯的明组 85.53±5.57%相比）。体外，沉香浓度依赖性地降低 ACh（10μM）和 KCl（60mM）诱导的收缩，EC 值分别为 0.35 和 0.32mg/mL。ALR 使 Ca 浓度-反应曲线向右移位，类似于维拉帕米（阳性对照）的作用。ALR 的解痉活性被 l-NAME 预孵育抑制。
ALR 在 GIM 中发挥了抗痉挛作用，这可能是通过抑制毒蕈碱受体、阻断 Ca 内流和 NO 释放来介导的。这是首次全面描述 ALR 对 GIM 影响的研究。
