Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
J Ethnopharmacol. 2011 Mar 24;134(2):243-50. doi: 10.1016/j.jep.2010.12.004. Epub 2010 Dec 14.
The present study was carried out to evaluate the effect of dried mature unripe Morinda citrifolia L. (Rubiaceae) fruit, commonly known as "Noni", in an aqueous extract preparation (AFE) as used in Thai traditional medicine and its biomarker scopoletin on gastro-esophageal inflammatory models that are related to the claimed pharmacological properties of AFE and/or resembled the human esophagitis or gastric ulcer.
The powder of dried mature unripe Noni fruit was boiled in water until it became a sticky paste and was then dried into a powder by lyophilization. The pharmacological activity of AFE and pure scopoletin at the same equivalent dose present in AFE was investigated in rat on gastro-esophageal inflammatory models (acid reflux esophagitis, acute gastritis induced by ethanol and serotonin, and chronic gastric ulcer induced by acetic acid); gastric biochemical parameters and gastrointestinal motility.
AFE (0.63-2.50 g/kg) significantly prevented the formation of acid reflux esophagitis, reduced the formation of ethanol-induced acute gastric lesions, suppressed the development of gastric lesions in response to serotonin, and accelerated the healing of acetic acid-induced chronic gastric ulcer in rats with equal potency to those obtained by standard antisecretory agents (ranitidine and lansoprazole). AFE also significantly inhibited gastric acid secretion and pepsin activity in pylorus ligated rats. Additionally, AFE strongly increased the gastrointestinal transit of charcoal meal with a higher potency than cisapride. Pure scopoletin, when compared at the same equivalent dose containing in AFE, possessed similar antiulcer and antisecretory properties to that of AFE although it exerted a less prokinetic activity than AFE.
The findings indicated that AFE as well as its biomarker: scopoletin may be beneficial as a potential preventive and therapeutic agent for gastro-esophageal inflammatory diseases, mainly through its antisecretory and prokinetic activities including an inhibitory activity on serotonin, free radicals, and cytokine-mediated inflammation. Additionally, scopoletin might be one of the biomarker constituents to use for the quality assessment of Noni fruit products used for treating gastro-esophageal inflammatory diseases.
本研究旨在评估作为泰国传统药物使用的水提物（AFE）中干成熟未熟的巴戟天（茜草科）果实（俗称“诺丽”）及其生物标志物东莨菪内酯的作用，以及其在与 AFE 声称的药理学特性相关的胃食管炎症模型中的作用，或类似于人类食管炎或胃溃疡的模型。
将干成熟未熟的诺丽果粉末在水中煮沸，直至形成粘性糊状物，然后通过冷冻干燥将其干燥成粉末。在胃食管炎症模型（胃酸反流性食管炎、乙醇和 5-羟色胺诱导的急性胃炎、乙酸诱导的慢性胃溃疡）中，以相同的等效剂量研究 AFE 和纯东莨菪内酯的药理活性；胃生化参数和胃肠动力。
AFE（0.63-2.50 g/kg）可显著预防胃酸反流性食管炎的形成，减少乙醇诱导的急性胃损伤的形成，抑制 5-羟色胺诱导的胃损伤的发展，并加速乙酸诱导的慢性胃溃疡的愈合，其效力与标准抗分泌剂（雷尼替丁和兰索拉唑）相当。AFE 还显著抑制幽门结扎大鼠的胃酸分泌和胃蛋白酶活性。此外，AFE 强烈增加炭餐的胃肠转运，其效力高于 cisapride。与 AFE 相比，当比较相同等效剂量时，纯东莨菪内酯具有相似的抗溃疡和抗分泌作用，尽管其促动力作用弱于 AFE。
这些发现表明，AFE 及其生物标志物：东莨菪内酯可能作为胃食管炎症疾病的潜在预防和治疗药物有益，主要通过其抗分泌和促动力作用，包括对 5-羟色胺、自由基和细胞因子介导的炎症的抑制作用。此外，东莨菪内酯可能是用于治疗胃食管炎症疾病的诺丽果产品质量评估的生物标志物成分之一。
