Core--Plant Natural Products

核心--植物天然产品

• 批准号: 6938240
• 负责人: CHING-JER CHANG
• 金额: $ 15.1万
• 依托单位: PURDUE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-04-01 至 2010-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6938240
• 关键词: X ray crystallography; biomedical facility; biotechnology; cancer prevention; carcinogenesis inhibitor; chemoprevention; drug discovery /isolation; liquid chromatography mass spectrometry; medicinal plants; plant extracts

The objectives of this core project are (1) the selection and procurement of plant materials having potential carcinogenesis inhibitory activity and (2) the discovery of novel natural products inhibitors of chemical carcinogenesis. Selection of plant materials for study will be focused on three major groups: (a) edible plants, primarily non-USA; (b) medicinal plants used in traditional systems of medicine such as Traditional Chinese Medicine, particularly those employed in cancer related therapies; and (c) endemic plants reported to have activity in an assay pertinent to cancer chemoprevention, but which have not been investigated chemically, especially those with no history of toxicity, and having potentials to yield novel chemical compounds. Primary emphasis will be placed on group (a) and (b) plants. These candidate plants will be identified with help from our collaborators. Most promising plant species will be selected for acquisition based on analysis of the literature. The non-toxic plant materials will be given a higher priority for collection. The candidate plant materials will be field collected, cultivated and/or commercially purchased. All plant materials will be identified and authenticated. They will be dried, milled, and extracted for bioassay. These materials (1-10 kg lots) will be extracted and subjected to bioassay-directed isolation of the active principles. The initial bioassay-directed isolation will focus on the non-polar extracts. The active extracts will be separated and purified by the most appropriate chromatographic methods. Physical and chemical methods, including LC/MS/MS (Project 4) and X-ray crystallographic methods will be used to determine the structures of the active constituents, which will serve as new lead compounds for subsequent synthetic studies, and be subjected to further in vivo inhibitory efficacy of chemical carcinogenesis, mechanistic and preclinical evaluations.

该核心项目的目标是（1）选择和采购植物材料 具有潜在的癌变抑制活性，（2）发现新型天然产物 化学癌变的抑制剂。选择用于研究的植物材料将集中在三个主要群体上：（a）可食用的植物，主要​​是非美国； （b）传统医学系统中使用的药用植物，例如中医，尤其是与癌症相关疗法的药物； （c）据报道，特有植物具有与癌症化学预防有关的测定的活性，但尚未进行化学研究，尤其是那些没有毒性史的人，并且具有产生新型化合物的潜力。 主要重点将放在植物组（a）和（b）植物上。这些候选植物将是 在我们的合作者的帮助下确定。将选择最有前途的植物物种 基于文献分析的获取。无毒的植物材料将获得更高的收集优先级。候选植物材料将被现场收集，耕种和/或商业购买。所有植物材料将被识别和认证。它们将被干燥，铣削和提取以进行生物测定。这些材料（1-10公斤批次）将被提取，并且 进行活性原理的生物测定指导隔离。初始生物测定导向的隔离将集中在非极性提取物上。活性提取物将通过最合适的色谱方法分离和纯化。物理和化学方法，包括LC/MS/MS（项目4）和X射线晶体学方法将用于确定活性成分的结构，该结构将用作随后的合成研究的新铅化合物，并将进一步进行化学癌变，机械和临床前评估的体内抑制功效。