Anti-tuberculosis Agents from Gorgonian Octocorals

柳珊瑚八珊瑚的抗结核剂

• 批准号: 6766444
• 负责人: ABIMAEL D RODRIGUEZ
• 金额: $ 10.82万
• 依托单位: UNIVERSITY OF PUERTO RICO RIO PIEDRAS
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-07-01 至 2005-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6766444
• 关键词: Caribbean; Puerto Rico; X ray crystallography; animal extract; antibacterial agents; bioassay; biotechnology; biotherapeutic agent; cell growth regulation; chemical structure function; communicable disease control; coral; cytotoxicity; diterpenes; drug discovery /isolation; drug screening /evaluation; emerging infectious disease; inhibitor /antagonist; mass spectrometry; metabolism; nuclear magnetic resonance spectroscopy; pharmacology; solvent extraction; systematic biology; tuberculosis

Marine invertebrates have been identified for a long time by chemists as likely sources of new biomedicinal substances. Pharmacologists, physiologists and biochemists have demonstrated that many of these novel marine products modify fundamental life processes in ways suggesting biomedical applications. These molecules can serve as leads to guide the pharmaceutical and chemical industries in developing new products. This research aims specifically at Caribbean gorgonian octocorals as a likely resource for novel anti-tuberculosis natural products. Since less than 20% of the species of gorgonian octocorals known to exist in the Caribbean region have been assessed chemically for their secondary metabolite composition, and many of these have been shown to produce metabolites possessing potent chemotherapeutic properties, gorgonians from this region have the potential to contain a wealth of novel drugs. Specifically, during the four years of this research we plan to carefully scrutinize the pharmacology and chemistry of 75 representative species belonging to all the major Caribbean gorgonian genera. Initial extraction with solvents of different polarities (e.g., hexane, methylene chloride, and methanol) will be monitored using anti-tuberculosis activity assays. Only gorgonian extract residues possessing strong anti-tuberculosis properties will be screened further for chemical structural features by 1H- and 13C-NMR spectroscopy. Further purification by chromatography (column, GC, LC) and determination of molecular structure will proceed if warranted by the screening results. Structure elucidation will rely heavily on spectral methods (e.g., 1H and 13C NMR, MS, IR, UV) and X-ray diffraction techniques.

化学家已经确定了长期以来的海洋无脊椎动物，这是新的生物医学物质的可能来源。药理学家，生理学家和生物化学家已经证明，其中许多新型海洋产品以暗示生物医学应用的方式修改了基本生命过程。这些分子可以用作指导开发新产品的药物和化学工业的铅。这项研究专门针对加勒比海八角孢子，是新型抗结核天然产物的可能资源。由于已知在加勒比地区已知存在的Gorgonian八生中只有不到20％的物种对其次级代谢产物组成进行了化学评估，因此许多这些物种已被证明产生具有有效的化学治疗特性的代谢产物，因此该地区的Gorgonians具有有效的化学治疗特性，该地区的Gorgonians具有潜在的新型药物。具体而言，在这项研究的四年中，我们计划仔细仔细检查属于所有主要加勒比海戈尔贡属的75种代表性物种的药理学和化学。将使用抗结核活性测定法监测使用不同极性（例如己烷，甲基氯化物和甲醇）的溶剂的初始提取。只有1H和13C-NMR光谱法进一步筛选具有强抗结核特性的Gorgonian提取物残基才能进一步筛选化学结构特征。如果通过筛选结果保证，将通过色谱法（列，GC，LC）进行进一步纯化，并确定分子结构。结构阐明将在很大程度上依赖于光谱方法（例如1H和13C NMR，MS，IR，UV）和X射线衍射技术。