BIOACTIVE CONSTITUENTS OF MARINE ORGANISM

海洋生物的生物活性成分

• 批准号: 3734334
• 负责人: PAUL J SCHEUER
• 金额: --
• 依托单位: UNIVERSITY OF HAWAII AT MANOA
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3734334
• 关键词: Mollusca; Porifera; Tunicata; alternatives to animals in research; animal extract; aquatic organism; chemical structure function; chromatography; cytotoxicity; drug design /synthesis /production; high performance liquid chromatography; nuclear magnetic resonance spectroscopy; physical separation; solvent extraction

The objective of this research is the isolation and molecular structure determination of bioactive constituents of marine organisms, particularly sponges, mollusks and tunicates. Freeze-dried organisms are extracted with water and with an organic solvent. Both extracts are assayed for cytotoxicity (KB cell line) and structural features (1H NMR). Those samples which show promising activity (MIC < 1 mug/mL) are purified by solvent partition and chromatography. The KB assay is used to guide the fractionation. Pure samples, as judged by HPLC, are subjected to spectral analysis (1H and 13C NMR, MS, UV, IR) in order to determine the molecular structure. MARINELIT and CAS ONLINE are used to determine whether the compound is new. All compounds, new and those described previously, are submitted to the National Cooperative Natural Products Drug Discovery Program for assay against solid tumors; to NCI for broad anti-tumor and anti-AIDS assays; and to Pharma Mar, S.A. for antiviral, antimicrobial, and immunomodulatory activities. For active samples which are slated for in vivo assay re-isolation and/or recollection may be necessary.

本研究的目的是分离和分子结构 海洋生物的生物活性成分的测定，特别是 海绵、软体动物和被囊动物。 提取冻干生物体 与水和与有机溶剂。 两种提取物均经过检测 细胞毒性（KB 细胞系）和结构特征（1H NMR）。 那些 显示出有希望的活性（MIC < 1 mug/mL）的样品通过以下方法纯化 溶剂分配和色谱法。 KB 测定用于指导 分馏。 纯样品，通过 HPLC 判断，进行 光谱分析（1H 和 13C NMR、MS、UV、IR）以确定 分子结构。 MARINELIT 和 CAS ONLINE 用于确定 该化合物是否是新的。 所有新化合物和描述过的化合物 此前，已提交至国家天然产物合作社 用于针对实体瘤进行检测的药物发现计划； NCI 广泛 抗肿瘤和抗艾滋病检测；以及 Pharma Mar, S.A. 的抗病毒药物， 抗菌和免疫调节活性。 对于活性样品 预计用于体内测定重新分离和/或重新收集可能是 必要的。