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CHEMICAL DIVERSITY LIBRARIES FROM MEDICINAL PLANTS (RMI)

药用植物化学多样性库 (RMI)

基本信息

批准号：
7274185
负责人：
KUO-HSIUNG LEE
金额：
$ 39.22万
依托单位：
UNIV OF NORTH CAROLINA CHAPEL HILL
依托单位国家：
美国
项目类别：
财政年份：
2005
资助国家：
美国
起止时间：
2005-09-23 至 2009-07-31
项目状态：
已结题

项目摘要

DESCRIPTION (provided by applicant): The overall goal of this proposed study is the generation of pilot-scale chemical diversity libraries, which will be used for high-throughput screening (HTS) by the Molecular Libraries Screening Center Network (MLSCN). The compounds included in these libraries will be derived from medicinal plants - both isolated natural products and synthetic modified derivatives. Naturally occurring compounds representing unique chemical diversity classes will be isolated, purified, and characterized using modern chemical, physical, and spectral techniques, including LC-MSn technology. Compounds will be obtained from three main sources: bioactive natural products previously investigated by the PI's Natural Product Laboratory (NPL) in the past 34 years, constituents of medicinal plants commonly used in the US, and constituents of medicinal plants commonly used outside of the US, particularly in traditional Chinese medicine (TCM). In addition, rational chemical synthetic modification of water-insoluble natural products will provide new water-soluble analogs that will be more amenable to HTS. Totally, more than 1,200 compounds over three years with 400 compounds per year will be submitted to the NIH Repository for HTS. All submitted compounds will be in greater than 99% purity and, initially, in 10 mg per compound quantity. Additional quantity of compounds with promising biological activity based on the initial HTS might be furnished, upon request. An in-house database will store information (source, structure, production and characterization methods, etc.) on all compounds and will be made available as part of the resource-sharing plan. No intellectual property claims are anticipated on submitted compounds. The compounds chosen for study will have high potential for in vivo and/or in vitro biological activity based on the history of folkloric and clinical medicinal use of the source plants. In addition, the constituents of these plant species will cover a wide range of unique chemical diversity space and, accordingly, be likely to affect the functions of novel classes of biomacromolecules. The expertise and productivity of the PI's NPL will assure the successful generation of chemical diversity libraries that have excellent promise to generate new scientific knowledge with tangible benefits for public health in the areas of new drug discovery and development.

描述（由申请人提供）：本研究的总体目标是建立中试规模的化学多样性文库，这些文库将被分子文库筛选中心网络（MLSCN）用于高通量筛选（HTS）。这些文库中包含的化合物将来源于药用植物，包括分离的天然产物和合成的改性衍生物。天然存在的化合物代表独特的化学多样性类别将被分离，纯化，并使用现代化学，物理和光谱技术，包括LC-MSn技术进行表征。化合物将从三个主要来源获得：PI的天然产物实验室（NPL）在过去34年中先前研究的生物活性天然产物，美国常用的药用植物成分，以及美国以外常用的药用植物成分，特别是在中药（TCM）中。此外，对不溶于水的天然产物进行合理的化学合成改性，将提供更适合HTS的新型水溶性类似物。总共超过1200种化合物，每年400种化合物将在三年内提交给NIH知识库用于HTS。所有提交的化合物的纯度将大于99%，并且最初每个化合物量为10毫克。在初始HTS的基础上，可应要求提供额外数量的具有生物活性的化合物。内部数据库将存储所有化合物的信息（来源、结构、生产和表征方法等），并将作为资源共享计划的一部分提供。预计不会对提交的化合物提出知识产权索赔。根据来源植物的民俗和临床药用历史，所选择的化合物将具有很高的体内和/或体外生物活性潜力。此外，这些植物物种的成分将覆盖广泛的独特的化学多样性空间，从而可能影响新型生物大分子的功能。PI国家物理实验室的专业知识和生产力将确保化学多样性文库的成功生成，这些文库具有良好的前景，可以产生新的科学知识，为新药发现和开发领域的公共卫生带来切实利益。