ANTITUMOUR AGENTS FROM MARINE MICROALGAE

提案这一部分的长期目标是发展 抗肿瘤、抗病毒、一种来源于微藻的抗微生物药物。 这项建议是基于最近发生的 甲藻和其他微藻中有希望的化合物。 预期的化合物包括聚醚、大环内酯类、其他 多氧化合物、环肽和脱脂多肽。那里 都是强烈的迹象表明，在 海洋无脊椎动物实际上是由微藻衍生而来的。这个 申请者小组在培养微藻方面有长期的经验和 研究他们的次生代谢产物，并拥有大量 收集未经检验的微藻菌株。 具体来说， L。金藻中自由生活的甲藻、硅藻、藻类和 其他来自温带和热带水域的微藻，以及一些 将被收集、培养和筛选，以供 生物活性。 2.与海洋共生或有关连的上述类别的生物 无脊椎动物和藻类将被分离、培养和筛选。 3.活性化合物将被分离出来，其结构 纯化的化合物将通过物理化学方法进行研究。 包括高场核磁共振、质谱学和X射线 结晶学。抗肿瘤和抗病毒检测以及进一步 药物的开发将由百时美施贵宝公司进行， 但有限的内部细胞毒性和抗菌测试将是 作为快速隔离指南执行。

The long-term objective of this part of the proposal is to develop antitumor, antiviral, an antimicrobial drugs from microalgal sources. The proposal is based on the recent findings of the occurrence of promising compounds in dinoflagellates and other microalgae. Anticipated compounds include polyethers, macrolides, other polyoxygenated compounds, cyclic peptides and depsipeptides. There are strong indications that many of the unique metabolites found in marine invertebrates are actually derived from microalgae. The applicant's group has lengthy experience in culturing microalgae and studying their secondary metabolites and is in possession of a vast collection of unexamined microalgal strains. Specifically, l. Free-living dinoflagellates, diatoms, algae in Chrysophyta, and other microalgae from both temperate and tropical waters, and some from freshwater, will be collected, cultured and screened for the bioactivity. 2. Organisms of the above classes symbiotic or associated with marine invertebrates and algae will be isolated, cultured and screened. 3. Active compounds will be isolated, and the structures of the purified compounds will be studied by physico-chemical methods including high field NMR, mass spectroscopy, and X-ray crystallography. Antitumor and antiviral assays and further development of drugs will be conducted by Bristol-Myers Squibb Co., but limited in-house cytotoxicity and antimicrobial tests will be performed as quick isolation guides.