DRUG DISCOVERY FROM PLANTS OF VIETNAM AND LAOS FOR AIDS AND MALARIA THERAPIES

协理项目-3（AP-3）的主要目标是分离和 鉴定HIV复制特异性抑制剂和活性剂 抗氯喹的恶性疟原虫它将提供生物测定 支持发现有效防治疟疾的天然产品 通过筛选约500种植物提取物， 每年进行一次生物活性分级分离程序。源 将根据老挝和老挝文挑选和收集评价材料。 人民民主共和国。一个主要基于生物多样性的选择 方法将被采用，虽然民族植物学调查可能被采用 在有限的范围内。该项目还将进行初步提取 植物材料和确认的活性植物化学物质的放大分离。 光谱和化学方法将用于确定 纯生物活性化合物的结构。将努力尽量减少 已知抗HIV或抗疟疾化合物的再分离 通过文献（NAPRALERT）和LC/MS/MS去复制获得的特性 技术.此外，几种HIV-1抑制剂可以逆转 转录酶（RT）和许多有前途的抗疟疾化合物， 提取物已经通过正在进行的合作药物发现被鉴定 与越南的研究人员合作。这些生物活性的天然 产品将被重新分离，并在更复杂的生理条件下进行评估。 生物测定系统和相关的机械测定，以便优先考虑 用于更先进的体内研究。与葛兰素威康合作， 活性化合物将作为药物开发的候选物进行评价。 或者，新的分离株可被视为新的线索， 开发选择性抑制剂。

The major objective of Associate Project-3 (AP-3) is to isolate and identify specific inhibitors of HIV replication and agents active against chloroquine-resistant Plasmodium falciparum. It will provide bioassay support for the discovery of natural products effective against malaria and AIDS through the screening of approximately 500 plant extracts annually followed by bioactivity fractionation procedures. Source materials for evaluation will be selected and collected under and Lao People's Democratic Republic. A primarily biodiversity-based selection approach will be adopted, although ethnobotanical inquiry may be employed to a limited extent. This project will also perform initial extraction of plant materials and scale-up isolation of confirmed active phytochemicals. Spectroscopic and chemical methods will be used to determine the structures of pure bioactive compounds. Efforts will be made to minimize the re-isolation of compounds with known anti-HIV or anti-malarial properties through literature (NAPRALERT) and LC/MS/MS dereplication techniques. Additionally, several inhibitors of HIV-1 reverse transcriptase (RT) and numerous promising anti-malarial compounds and extracts have been identified through ongoing collaborative drug discovery efforts with researchers in Vietnam. These biologically active natural products will be re-isolated and evaluated in more physiologically complex bioassay systems and relevant mechanistic assays in order to prioritize them for more advanced in vivo studies. In concert with Glaxo Wellcome, active compounds will be evaluated as candidates for development as drugs. Alternatively, novel isolates may be considered as new leads for the development of selective inhibitors.