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Multilateral Studies on Biologically Active Natural Substances

生物活性天然物质的多边研究

基本信息

批准号：
01303003
负责人：
UDA Hisashi
金额：
$ 1.22万
依托单位：
Tohoku University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Co-operative Research (A)
财政年份：
1989
资助国家：
日本
起止时间：
1989 至 1990
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-01303003/
关键词：
Biologically active substance Structural determination Total synthesis Terpenoid Alkaloid Iridoid Secosteroid Peptide

项目摘要

The studies have been carried out by dividing two research groups.1. Isolations, structures, and biobeneses of biologically active natural substances : Several terpenoids, secosteroids, and alkaloids, possessing cytotoxic, antibacterial, or antiflammatory activities, have been isolated from the marine molluscs, such as soft corals and sponges, and determined their chemical structures. A neurotoxic peptide from the venom of Cyphononyx dorsalis, The neuroexcitatory amino acids and the antitumor lanostanoids from two Kinds of mushrooms, the antibactrial macrolides from Streptomyces strain, and a growth regulatory substance from rice husk have been also isolated and the structures have been elucidated. Furthermore, the enzymatic cyclization process of laurendiol to the ether-containing derivatives and the coordination of geranyl diphosphate with magnesium ion and the stereoselective elimination of a hydrogen from geranyl diphosphate have been clarified.2. Synthetic reactions, syntheses, and action mechanisms of biologically active natural substances : For the synthesis of terpenoids and iridolids, possessing biologically active properties, such as antitumor, antibacterial etc, new synthetic reactions and synthetically useful blocks have been developed, and the total synthesis of about ten terpenoids and about six iridoiss have been accomplished. And also, lampteroflavin, a mushroom light emitter, the peptides as the plausible active center of vancomycin, an antibiotic, the lipopolysaccharide parts in the constituents of grampositive bacteria, and the key intermediate for the synthesis of tetrodotoxin have been synthesized. Furthermore, the characteristic of the alkylation of nucleosides by dehydromonocrotaline and the mode of aromatization of an enyne-3-cumulene derivative as a model of neocarzinostatin chromophore have been clarified.

本研究分为两个研究小组进行。天然生物活性物质的分离、结构和生物基础：从海洋软体动物如软珊瑚和海绵中分离出几种具有细胞毒性、抗菌或抗炎活性的萜类、开环甾类和生物碱，并测定了它们的化学结构。本文还分离得到了一种来自于树蛙毒液的神经毒肽，两种蘑菇中的神经兴奋性氨基酸和抗肿瘤的羊毛甾烷类化合物，链霉菌中的抗菌大环内酯类化合物，以及一种来自于稻壳的生长调节物质，并鉴定了它们的结构。进一步阐明了月桂二醇的酶促环化反应生成含醚衍生物的过程，香叶基二磷酸与镁离子的配位反应以及香叶基二磷酸中氢的立体选择性消除反应.天然生物活性物质的合成反应、合成及作用机理：在具有抗肿瘤、抗菌等生物活性的萜类化合物和环烯醚萜类化合物的合成方面，开发了新的合成反应和合成有用的嵌段，完成了约10个萜类化合物和约6个环烯醚萜类化合物的全合成。此外，还合成了蘑菇发光体灯黄素、抗生素万古霉素可能的活性中心肽、革兰氏阳性菌组分中的脂多糖部分以及合成河豚毒素的关键中间体。进一步阐明了脱氢野百合碱对核苷的烷基化反应的特征和一种烯炔-3-枯烯衍生物作为新制癌素发色团模型的芳构化反应模式。