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种新的 海洋环境中的生物。生物测定指导这些 分离通常基于抗微生物，抗肿瘤， 抗病毒或抗病毒活性。 几乎没有采取什么措施来 探索海洋，寻找具有抗HIV和AIDS活性的化合物。 另外，由于与常规的制造方法相关联的限制， 自给式水下呼吸器（SCUBA），大多数 海洋环境中的特征化合物是 浅水收集（-30米）。大规模筛查的价值 天然产品的复杂提取物，再加上生物活性指导， 分馏和化合物鉴定，以发现新的 天然产物化学型是众所周知的。一进程的主要重点 应用于新化学型的分离和表征 对于潜在的治疗艾滋病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 相关生物测定中的样品。 将从以下深度采集样本： 0至-800米，其中使用的收集方法将是CCUBA （闭路水下呼吸器），这将允许 更长的时间和更深的潜水比可能的水肺，并将允许 申请人从事以前未勘探的海洋底栖物种的工作。 生物体的活性提取物将使用各种 色谱技术（包括HPLC）和化学结构 生物活性次级代谢产物将通过以下方法测定： 光谱和化学方法，特别强调两个- 三维NMR技术。特别是额外数量的 体内试验所需的有前途的化合物将是 通过合成、半合成或重复分离获得。

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.