ANTI AIDS AGENTS FROM MARINE ORGANISMS

描述：(改编自申请人摘要)。天然产物 在过去的几十年里，研究已经产生了数千部小说 来自海洋环境的生物。指导这些的生物化验 分离通常是基于抗微生物，抗肿瘤， 抗病毒或抗炎活性。几乎没有采取什么措施来 探索海洋，寻找具有抗艾滋病毒和艾滋病活性的化合物。 此外，由于与常规技术相关的限制 自给式水下呼吸器(Scuba)，大部分 从海洋环境中提取的化合物就是结果 浅水区(-30米)。大规模筛查的价值 天然产物的复杂萃取物与生物活性导向相结合 分离和化合物鉴定在新发现中的应用 天然产物的化学类型是众所周知的。这件事的主要焦点是 应用于新化学类型的分离和鉴定 对于艾滋病的潜在治疗和艾滋病相关的机会主义 感染(OI)，申请人将收集和筛选海洋 相关生物检测中的样品。样本将从海洋深处采集 0到-800米，使用的采集方法之一是CCUBA (闭路式水下呼吸器)，这将允许 比水肺潜水更长更深的潜水，将允许 申请从事以前未被探索的海洋底栖动物物种的工作。 生物体的活性提取物将使用各种不同的方法进行分离 包括高效液相色谱在内的色谱技术，以及化学结构 具有生物活性的次生代谢物将通过 光谱和化学方法，特别强调两种- 三维核磁共振技术。特别是额外的数量 体内测试所需的有希望的化合物将是 通过合成、半合成或重复分离获得的。

DESCRIPTION: (Adapted from Applicant's Abstract). Natural products research during the last few decades has yielded thousands of novel organisms from the marine environment. The bioassays guiding these isolations typically have been based on antimicrobial, antitumor, antiviral, or antiinflammatory actvities. Little has been done to explore the oceans for compounds with activity against HIV and AIDS OI. Additionally, because of the limits associated with the conventional Self-Contained Underwater Breathing Apparatus (SCUBA), the majority of the compounds characterized from the marine environment are the results of shallow-water collections (-30 meters). The value of mass screening of complex extracts of natural products coupled with bioactivity-guided fractionation and compound identification for the discovery of new natural product chemotypes is well known. The primary focus of this application is on the isolation and characterization of new chemotypes for the potential treatment of AIDS and AIDS-related opportunistic infections (OI), and the applicant will collect and screen marine samples in relevant bioassays. Samples will be obtained from depths of 0 to -800 meters, and among the collection methods used will be CCUBA (Closed Circuit Underwater Breathing Apparatus), which will permit longer and deeper dives than possible by SCUBA, and will allow the applicant to work on previously unexplored marine benthic species. Active extracts of organisms will be isolated using various chromatographic techniques inclusive of HPLC, and chemical structures of biologically active secondary metabolites will be determined through spectroscopic and chemical methods, with special emphasis on two- dimensional NMR techniques. Additional quantities of particularly promising compounds that are required for in vivo testing will be obtained via synthesis, semi-synthesis, or repeated isolation.