SEPARATIONS/STRUCTURE/BIOAVAILABILITY/KRAUS, GEORGE

分离/结构/生物利用度/KRAUS, GEORGE

• 批准号: 7293906
• 负责人: DIANE F BIRTH
• 金额: $ 16.26万
• 依托单位: IOWA STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2007
• 资助国家: 美国
• 起止时间: 2007-04-01 至 2010-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7293906
• 关键词: Analytical Chemistry; Biological Availability; Biological Factors; Caco-2 Cells; Cell model; Chemicals; Collection; Complex Mixtures; Echinacea (Asteraceae); Echinacea Preparation; Educational process of instructing; Food; Fractionation; Glucuronides; Herb; High Pressure Liquid Chromatography; Human; Hypericum; Individual; Intestines; Ketones; Laboratories; Legal patent; Link; Mass Spectrum Analysis; Medicinal Plants; Metabolic Biotransformation; Metabolism; Methods; Modeling; Personal Satisfaction; Phytochemical; Plant Preparations; Plants; Prunella vulgaris; Publishing; Research; Research Personnel; Resources; Sampling; Spectrum Analysis; Standard Preparations; Standards of Weights and Measures; Structure; Techniques; Testing; Work; base; cellular targeting; chemical fingerprinting; experience; glucuronide; interest; novel; two-dimensional; uptake

The Separations/Structure/Bioavailability core will provide a resource for the extraction, fractionation and structural determination of phytochemicals. The core will build upon the experience gained by the Kraus group in the preparation of standards and structural identification of phytochemicals plus the experience gained by the Murphy group in the extraction and fractionation of Echinacea and Hypericum samples. Extraction, fractionation and structural determination/standard preparation will be conducted in close partnership with individual projects within the Center. Bioavailability studies will be conducted on bioactive compounds to determine if these chemicals are absorbed and reach relevant cellular targets. Our objectives are to: 1. Provide project researchers with extracts of medicinal plants including Hypericum, Echinacea and Prunella vulgaris. Ultrasonication and Soxhlet extraction methods will be compared to determine which method provides the most useful extracts. 2. Fractionate bioactive extracts to determine if activities separate into specific or multiple fractions. Collection of compounds of interest across gradients on HPLC will be a primary fractionation strategy. 3. Determine the structures of individual components of medicinal plants. A combination of spectroscopic methods (IR, NMR, mass spectroscopy) 4. Provide standards for chemical fingerprinting and testing. The preparation of herbal compound standards that are not commercially available will be based upon novel methods for synthesizing Echinacea alkamide- related ketones and a patented method for procyanidin synthesis developed by the Kraus laboratory. Other synthetic approaches will be developed as needed for compounds of important bioactivity. 5. Determine the bioavailability of extracts, fractions and components. CaCo-2 cells will be used as a model for human intestinal uptake and metabolism of herbal compounds of interest, as well as interactions between fractions that may alter compound uptake. Glucuronide conjugates are expected to be major and less bioactive metabolites from herbal phenolics; the inducibility of glucuronide metabolism by herbal components will also be studied.

分离/结构/生物利用度核心将为提取、分馏和 植物化学物质的结构测定。核心将建立在克劳斯获得的经验基础上 植物化学物质标准和结构鉴定编制小组 Murphy小组在紫锥菊和金丝桃属样品的提取和分级中获得的。 提取、分馏和结构测定/标准品制备将在 与中心内的个别项目建立伙伴关系。生物利用度研究将在生物活性 化合物，以确定这些化学物质是否被吸收并达到相关的细胞目标。 我们的目标是： 1.为项目研究人员提供药用植物提取物，包括金丝桃属、紫锥菊属和 夏枯草将比较超声和索氏提取方法，以确定 方法提供了最有用的提取物。 2.对生物活性提取物进行分级，以确定活性是否分离成特定或多个级分。 在HPLC上跨梯度收集感兴趣的化合物将是主要的分馏策略。 3.确定药用植物的单个成分的结构。结合光谱学 方法（IR，NMR，质谱） 4.提供化学指纹和测试标准。中药复方标准品的制备 将基于用于合成紫锥菊烷酰胺的新方法， 相关的酮和专利方法的原花青素合成开发的克劳斯实验室。其他 将根据需要开发具有重要生物活性的化合物的合成方法。 5.测定提取物、馏分和组分的生物利用度。CaCo-2细胞将被用作模型 对于感兴趣的草药化合物的人体肠道摄取和代谢，以及 可以改变化合物摄取的组分。预计葡糖苷酸结合物主要且较少 草药酚类物质的生物活性代谢物;草药成分对葡萄糖醛酸代谢的诱导作用 也将被研究。