PLANT ANTIHIV AGENTS

作为我们目前抗HIV新单宁及其化合物研究的延伸 类似物以及其他相关的天然产品，长期 这项研究的目的是发现新的有用的抗HIV化合物 来自植物来源的天然产品及其类似物。具体来说，我们 不断提出分离和鉴定有效的抗HIV病毒 33种从未见过的植物提取物中的化学成分 先前对其抗艾滋病毒成分进行了调查。这些提取物 已经显示出对艾滋病毒复制的有效抑制作用 H9淋巴细胞和HIV逆转录酶。提取， 对有效原则的分离和分离将在 H9淋巴细胞P24抗原捕获试验的体外检测 细胞。在上述生物测定指导的活性物质的分离之后 原则，其结构的确定将由 现代物理方法，包括光谱分析和X射线分析。 将在细胞培养基础上进行作用机制研究 化验。部分新化合物的结构修饰和类似物的合成 活性先导化合物以阐明其构效关系 关系，以及改善它们的药理学特征将 也是启动的。

As an extension to our current studies on new anti-HIV tannins and their analogs as well as other related natural products, the long-term objective of this research is to discover novel useful anti-HIV compounds from plant-derived natural products and their analogs. Specifically, we propose continuously to isolate and characterize the potent anti-HIV principles from extracts of 33 plant species which have never been investigated previously for their anti-HIV constituents. These extracts have already demonstrated potent inhibitory effects on HIV replication in H9 lymphocyte cells and HIV reverse transcriptase. Extraction, fractionation, and isolation of the active principles will be guided at every stage by an in vitro P24 antigen capture assay in H9 lymphocyte cells. Following the above bioassay-directed isolation of the active principles, the determination of their structures will be carried out by modern physical methods, including spectral and X-ray analyses. Mechanism of action studies will be conducted in cell culture-based assays. Structural modification and synthesis of analogs of selected new active leads in order to elucidate their structure-activity relationships, as well as to improve their pharmacological profiles will also be initiated.