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Development of Biochemical Reagents to Study Signal Transduction from Awuatic Organisms

开发用于研究 Awuatic 生物体信号转导的生化试剂

基本信息

批准号：
11556039
负责人：
FUSETANI Nobuhiro
金额：
$ 8.06万
依托单位：
THE UNIVERSITY OF TOKYO
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B).
财政年份：
1999
资助国家：
日本
起止时间：
1999 至 2000
项目状态：
已结题

项目摘要

We have collected marine invertebrates along the coast of Japan and carried out screening for biological activities. Based on the results of the screening we have isolated and characterized the active principles and studied their modes of action, which may lead to the development of biochemical reagents.1. Isolation and structure elucidation of novel bioactive metabolitesFrom the marine sponge Theonella swinhoei collected off Hachijo-jima Island, we have isolated novel serine protease inhibitors, pseudotheonamides, which were related to the known cyclotheonamides with different modes of cyclization. From the sponge Stelletta globostellatta were isolated three novel isomalabaricane triterpenes which induce morphological changes in rat 3Y1 fibroblasts. We also examined the structure-activity relationships among these triterpenes. Seven 3-alkylpyridine alkaloid were isolated from sponges of genera Xestospongia and Amphimedon. Novel calyculin derivatives were isolated from Discodermia calyx. Chemically modified derivatives and novel natural calyculins were examined for their effects against protein phosphatases and some structure-activity relationships were established.2. Studies on the modes of action of bioactive marine natural productsBy using a sponge-derived alkaloid xestospongin C which inhibits the binding of IP3 to its receptor, the involvement of Ca ions in the contraction of guinea-pig papillary muscle.

我们收集了日本沿海的海洋无脊椎动物，并进行了生物活动筛选。在筛选结果的基础上，对其活性原理进行了分离和表征，并对其作用方式进行了研究，为生物化学试剂的开发奠定了基础。新型生物活性代谢物的分离与结构鉴定从八州岛海绵状海绵中分离到新型丝氨酸蛋白酶抑制剂假茶胺类化合物，它们与已知的环茶胺类化合物具有不同的环合模式。从海绵龙骨中分离到三种新型异alabalabicane三萜，可诱导大鼠3Y1成纤维细胞形态学改变。我们还研究了这些三萜之间的构效关系。从海绵属和圆齿海绵中分离得到7个3-烷基吡啶类生物碱。从盘皮菌花萼中分离到新的花萼素衍生物。研究了化学修饰衍生物和新型天然calyculins对蛋白磷酸酶的作用，并建立了一些构效关系。生物活性海洋天然产物作用方式的研究利用海绵体生物碱xestospongin C抑制IP3与其受体的结合，研究钙离子参与豚鼠乳头肌收缩。