PHYTOCHEMISTRY AND AFRICAN BASED BIOASSAYS AND PHYTOMEDICINE DEVELOPMENT

植物化学和非洲生物测定以及植物药物开发

• 批准号: 6359023
• 负责人: JOHNSON FOYERE AYAFOR
• 金额: $ 7.8万
• 依托单位: WALTER REED ARMY INSTITUTE OF RESEARCH
• 依托单位国家: 美国
• 财政年份: 2000
• 资助国家: 美国
• 起止时间: 2000-09-30 至 2001-09-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6359023
• 关键词: Africa; Leishmania; Plasmodium falciparum; agriculture; antifungal agents; antimalarial agents; bioassay; chemical information system; chemical registry /resource; chemical structure function; chromatography; cooperative study; drug screening /evaluation; ethnic group; insect control; international cooperation; medicinal plants; plant ecology; plant extracts; plant growth regulators; training

The goals of this AP are 1) to identify and characterize the biologically active constituents of plants used as remedies in African ethnomedicine; 2) to carry out the optimization of selected lead compounds with potential for human health in Africa; and 3) to train a cadre of young African scientists in natural products chemistry and synthetic medicinal chemistry. We will conduct the extraction of selected medicinal plants, perform initial bioassay screens of extracts and conduct bulk extraction of plant material for drug development. An inventory of the extracts, their distribution and their status in the test systems will be maintained. Sufficiently active extracts will undergo bioassay-guided fractionation. We will use three bioassays: the brine shrimp lethality bioassay, a rapid, low-cost test for biologically active compounds, a potato disc assay for antiviral and cytotoxic properties, and an antimicrobial test using a panel of fungi as well as gram-positive and gram-negative bacteria. In addition, we will test extracts for potential agricultural protection properties. The active compounds will be isolated by a combination of chromatographic techniques. The structure of isolated compounds will be determined by a combination of spectra studies and chemical analyses, and the structure-activity relationship will be determined for the isolated chemical class. A lead optimization program based on isolated compounds from selected plants will be undertaken to increase their therapeutic potential as antimalarials and antileishmanials. Some extracts will be developed as phytomedicines for domestic marketing, while others will be sent to the appropriate individuals and institutions within this ICBG for further development as pharmaceuticals. We will maintain a database of phytomedical information which will be linked with the databases of ecology and ethnobotany developed by the other APs.

该 AP 的目标是 1）从生物学角度识别和表征 非洲民族医学中用作药物的植物的活性成分； 2）对选定的具有潜力的先导化合物进行优化 为了非洲的人类健康； 3）培养非洲青年干部 天然产物化学和合成药物科学家 化学。我们将进行精选药用植物的提取， 对提取物进行初步生物测定筛选并进行批量提取 用于药物开发的植物材料。提取物清单， 它们的分布及其在测试系统中的状态将是 维持。足够活性的提取物将进行生物测定指导 分馏。我们将使用三种生物测定： 丰年虾致死率 生物测定，一种快速、低成本的生物活性化合物测试， 马铃薯盘测定抗病毒和细胞毒性特性，以及 使用一组真菌以及革兰氏阳性和 革兰氏阴性细菌。此外，我们还将测试提取物的潜力 农业保护特性。活性化合物将被分离 通过色谱技术的组合。隔离结构 化合物将通过光谱研究和 化学分析，构效关系为 确定为孤立的化学类别。先导化合物优化计划 基于从选定植物中分离出的化合物，将进行 增加其作为抗疟药的治疗潜力 反莱什曼尼亚人。一些提取物将被开发为植物药 国内营销，其他的会发往相应的 该 ICBG 内的个人和机构进一步发展 药品。我们将维护植物医学信息数据库 将与生态学和民族植物学数据库链接 由其他 AP 开发。