New Immuno-Active Compound for Optimizing Echinacea

描述（由申请方提供）：紫锥菊属是美国草药市场上使用最广泛的免疫刺激植物药之一。这些产品在使用的物种、植物部分和配方方面差异很大。由于这些不同的产品都具有明显不同的化学性质，因此它们表现出不同的药理作用也就不足为奇了。处方变异性和化学变异性导致了迄今为止对这些不同制剂进行的临床试验的解释问题。它还强调了在不同制剂中识别临床相关化合物的重要性，以便可以为消费者市场和临床试验生产标准化的一致产品。 在我们的NCAAM资助的R21提案下开展的工作发现了一种以前未被识别的强效单核细胞活化化合物，其浓度很高（占植物干重的5%）。一种可重复的提取方法表明，其活性在商业相关的紫锥菊属物种的不同植物部分之间可以变化多达1,000倍。这种有效的免疫刺激成分未被检测到的主要原因是其在天然产物化学实验室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的免疫增强特性的主要贡献者，并且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更准确地标准化紫锥菊材料的方法，以便更明确的产品可用于动物研究和临床试验。它可以通过提供关于含有大量这种化合物的紫锥菊产品类型的信息（即酊剂，压榨果汁，植物部分或物种）更直接地影响人类健康。目标是： 1.确定这种新化合物对活性重要的结构特征，并制定标准化程序 2.评价这种活性在商业紫锥菊属植物材料和制剂中的变异性。 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.