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Structural and Biogenic Analysis of Bioactive Marine Natural Products

生物活性海洋天然产物的结构和生物来源分析

基本信息

批准号：
12640527
负责人：
KIMURA Junji
金额：
$ 2.11万
依托单位：
AOYAMA GAKUIN UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2000
资助国家：
日本
起止时间：
2000 至 2002
项目状态：
已结题

项目摘要

I divided the theme into five next items and studied it.1. From the red alga genus Laurencia nidifica, two new halogenated sesqiterpenes, chamigrane derivatives were obtained together with ten known compounds and two artifacts. Also, three halogenated monoterpenes, octodene derivatives were isolated from the red alga, Scinecia okamurae. The structures of these compounds were elucidated by NMR and mass spectroscopy, and plausible reaction pathways were proposed.2. Nine novel oxylipin metabolites together with several known ones were isolated from the brown alga, Eisenia bicyclis. Though bioactive investigation against B. subtilis and S. aureus, was done, unfortunately these compounds have poorer inhibition against their bacteria than a standard sample of vancomycin.3. Two new cyclic depsipeptides (kulokekahilide-1, -2) which showed cytotoxity against P388 murine lymphocytic leukemia cells with IC_<50> values of 2.1 μg/mL and 3.5 ng/mL were isolated from a marine mollusk Pilinopsis speciosa in Hawaii. The absolute stereochemistry of amino acids and hydroxy acids composed with depsipeptides were determined by Marfey analysis and chiral HPLC analysis. In order to examine the relationship between activity and structure, the total synthesis of kulokekahilide-2 was attempted.4. The analysis of components contained in deep-sea organisms, Calytogena soyoae, Ifremeria nautilei, and Rimicaris kairei was studied. No novel compounds were obtained but many known compounds were isolated from their materials. It was clear that fatty acids composition in deep-sea organisms was different from that in shallow-sea organisms.5. Data-mining method applied for the active compounds against E.coli, B.subtilis, and S.aureus. Thus, it was found that the classification rules of the activity were extracted from flavonoid and terpene derivatives

我把这个主题分成五个项目来研究。从红顶凹另外，从红蜘蛛中分离出三种卤代单萜类化合物，即异双烯衍生物。通过核磁共振谱和质谱确证了化合物的结构，并提出了可能的反应途径.从棕色双环草中分离到9个新的氧脂素代谢产物和几个已知的代谢产物。通过对B. subtilis和S.金黄色葡萄球菌，但不幸的是，这些化合物对它们的细菌的抑制作用比万古霉素的标准样品差。从夏威夷的海洋软体动物美丽毛藻（Pilinopsisspeciosa）中分离得到两个新的环缩酚酸肽（kulokekahilide-1，-2），它们对小鼠淋巴细胞白血病细胞P388具有细胞毒性，IC<50>值分别为2.1 μg/mL和3.5 ng/mL。通过马氏链分析和手性HPLC分析确定了与缩肽组成的氨基酸和羟基酸的绝对立体化学。为了考察活性与结构的关系，对kulokekahilide-2进行了全合成.对深海生物Calytogena soyoae、Ifremeria nautilei和Rimicaris karei的化学成分进行了分析。没有得到新的化合物，但许多已知的化合物从他们的材料分离。深海生物的脂肪酸组成明显不同于浅海生物。数据挖掘方法应用于抗大肠杆菌、枯草杆菌B.subtilis和金黄色葡萄球菌的活性化合物。由此发现，从黄酮类和萜类衍生物中提取了活性的分类规则