New Immuno-Active Compound for Optimizing Echinacea

描述(申请人提供)：紫锥菊是美国草药市场上使用最广泛的免疫刺激植物之一。这些产品在使用的品种、植物部分和配方方面有很大的不同。由于这些不同的产品都有明显不同的化学成分，因此它们表现出不同的药理作用也就不足为奇了。配方的可变性，因此化学可变性造成了解释迄今为止在这些不同制剂上进行的临床试验的问题。它还强调了确定不同制剂中与临床相关的化合物的重要性，以便为消费者市场生产标准化的一致产品，并用于临床试验。 根据我们由NCAAM资助的R21提案，我们的工作发现了一种以前未被认识的有效的单核细胞激活化合物，它存在于高浓度(植物干重的5%)中。一种可重复性的提取方法显示，其活性在商业上相关的紫锥菊物种的不同植物部分之间可以差异高达1000倍。这种强大的免疫刺激成分未能被检测到的主要原因是它在天然产品化学实验室中通常使用的溶剂中的溶解度有限。我们的长期工作假设是，这种化合物是这种草药增强免疫性能的主要贡献者，与其他成分贡献的活性一起产生紫锥菊的整体治疗效果。该项目的目标是提供使用这种有效的免疫刺激化合物来更准确地标准化紫锥菊材料的手段，以便更多明确的产品可以用于动物研究和临床试验。它可以更直接地影响人类健康，因为它提供了关于含有大量这种化合物的紫锥菊产品类型的信息(即药酒、压榨果汁、植物部分或物种)。目标是： 1.确定这种对活性重要的新化合物的结构特征，并制定标准化程序 2.评价市售紫锥菊植物原料和制剂中该活性的变异性。 3.调查可能影响该化合物水平和活性的农艺措施。

DESCRIPTION (provided by applicant): Echinacea species represent one of the most widely used immunostimulatory botanicals in the United States herbal market. These products vary considerably with respect to the species used, the plant part, and the formulation. Since these different products all have distinctly different chemistries, it should not be surprising that they would exhibit different pharmacological effects. Formulation variability and therefore chemical variability contributes to the problem in interpreting clinical trials performed to date on these different preparations. It also underscores the importance of identifying the clinically relevant compounds within the different preparations so that standardized consistent products could be produced for the consumer market and for use in clinical trials. Work under our NCAAM funded R21 proposal uncovered a previously unrecognized and potent, monocyte-activating compound, that is present in high concentrations (5% of dry plant weight). A reproducible method for its extraction revealed that its activity can vary as much as 1,000 times among different plant parts of the commercially relevant Echinacea species. The main reason this potent immunostimulatory component has eluded detection is its limited solubility in solvents normally used in natural product chemistry laboratories. Our long-term working hypothesis is that this compound is a major contributor to the immune enhancing properties of this herb and together with the activities contributed by other components produce the overall therapeutic effectiveness of Echinacea. The goal of this project is to provide the means to more accurately standardize Echinacea material using this potent immunostimulatory compound so that more defined products can be used for animal research and clinical trials. It could more directly influence human health by providing information on the types of Echinacea products that contain substantial amounts of this compound (i.e. tinctures, pressed juice, plant part or species). The objectives are: 1. Determine the structural characteristics of this new compound important for activity and develop a standardization procedure 2. Evaluate the variability of this activity in commercial Echinacea plant material and preparations. 3. Investigate agronomic practices that might influence the levels and activity of this compound.