Schmeda-Hirschmann Guillermo, Yesilada Erdem
Instituto de Química de Recursos Naturales, Universidad de Talca, Casilla 747, Talca, Chile.
J Ethnopharmacol. 2005 Aug 22;100(1-2):61-6. doi: 10.1016/j.jep.2005.06.002.
A frequent question when dealing with the search for gastroprotective compounds from natural sources is how far or close are both the plant preparations and extract amounts from the doses recommended in traditional medicine and what should be considered realistic levels for experimental studies. The administration way is oral and therefore extracts and products should be administered by gavage when looking for validation of ethnopharmacological uses. Suggestions of doses for both crude extracts and pure compounds are presented and discussed. For plant extracts prepared from single herbs and herbal mixtures, dose-response studies in the range between 100 and 300 mg/kg are suggested, with more than a single gastric ulcer model either in rats or mice. A suitable reference compound should be used according to the ulcer model and in doses resembling those used for human patients. For pure compounds and structure-activity studies or trends, dose-response results should be provided for at least a parent compound in order to select a reasonable dose for comparison purposes. We suggest an evaluation of the activity of the parent compound in the 50-300 mg/kg range and to look for structural modification leading to derivatives with similar or higher gastroprotective effects than the reference antiulcer compounds.
在从天然来源寻找胃保护化合物时,一个常见的问题是,植物制剂和提取物的用量与传统医学推荐剂量相差多远或接近程度如何,以及在实验研究中应将哪些水平视为现实可行的水平。给药方式为口服,因此在寻求民族药理学用途验证时,提取物和产品应通过灌胃给药。本文提出并讨论了粗提取物和纯化合物的剂量建议。对于由单一草药和草药混合物制备的植物提取物,建议在100至300mg/kg范围内进行剂量反应研究,使用大鼠或小鼠中的多种胃溃疡模型。应根据溃疡模型并以类似于人类患者使用的剂量使用合适的参考化合物。对于纯化合物以及结构活性研究或趋势,应至少为一种母体化合物提供剂量反应结果,以便为比较目的选择合理的剂量。我们建议评估母体化合物在50至300mg/kg范围内的活性,并寻找结构修饰以产生具有比参考抗溃疡化合物相似或更高胃保护作用的衍生物。