ORGANIC CHEMISTRY OF THE BIOSYSTEM CONTROL SUBSTANCES

生物系统控制物质的有机化学

• 批准号: 03303003
• 负责人: SHIRAHAMA Haruhisa
• 金额: $ 11.65万
• 依托单位: HOKKAIDO UNIVERSITY,(FACULTY OF SCIENCE)
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Co-operative Research (A)
• 财政年份: 1991
• 资助国家: 日本
• 起止时间: 1991 至 1992
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-03303003/
• 关键词: Neurotoxins; Isolation of neurotoxins; Neurotrophic compounds; Cell grouth control factors; Carcinogenic promotors; Cell decision inhibitors; Antifeedant; Allelopasic substances; 神経毒の合成; 発癌プロモ-タ-; 発癌性物質

1.Structural determination,synthesis and transmission mechanism of neurotoxin: Spatial arrangement of action points in glutamate receptor was studied using various substrates(Shirahama). Absolute configuration of cigatoxin was studied using synthesized models(Hirama). Structures of two neurotoxins isolated from wasps were deduced(Okumura). Mechanism of poisoning for palytoxin and okadaic acid was studied(Uemua). An important intermediate for synthesis of tetrodotoxin was synthesized via new method (Isobe). The structures of neurotrophic compounds isolated from plants were determined(Kodama).2. Control factor for cell growth: (+)-Laurencin and (-)-dactylyne were totally synthesized by newly developed method(Murai). Antiinfection activity of plants is found to be closely related with allylperoxidation of unsaturated fatty acids existing in the cells(T.Kato). The active part of vancomycin was synthesized and the structures of products from hybrid strains were determined(Yamamura). Analogs … More of bracken carcinogen,whose DNA cleaving activities were equivalents to ptaxiloside were synthesized and antitumoric compound was isolated from ptaxiloside, were synthesized and antitumoric compounds was isolated from marine animals (Yamada). Eight antitumoric activity promotors were isolated from Polypolaceae and their structures were determined(Hayashi). The determination of absolute configuration and configurational analysis were performed about various marine bioactive compounds(Kusumi). Cytotoxic ent-udoteatrial diacetate was synthesized (Isoe). Cytotoxic cumarines were isolated from Toddalis species(Mori).3. Antifeadant,allelopasy and immnoadjuvant activities: The structures of defensive peptides of flatfishes were determined(Tachibana). Immnoadjuvant lipoteichoic acid from gram-negative bacteria was synthesized (Kusumoto). Synthetic studies on clerodane diterpenoids were performed(Tokoroyama). Synthetic studies on jubavion and secopseudopeterocin A were carried out employing nopinone as a starting material(M,Kato). Total synthesis and absolute configuration of dysideapalaunic acid,antienzymatic agent, were achieved(Uda). The compounds showing allelopasy and promotors of iontransport were isolated from ferns(Suga). Antienzymatics were isolated from leaves of perilla(Nakayama). Five diterpenes, which show inhibitory activity on the cell devisoin of fertilized ascidian eggs, were isolated from marine plants and their structures were determined(Ochi). Less

1.神经毒素的结构确定、合成和传递机制：使用各种底物（Shirahama）研究谷氨酸受体中作用点的空间排列。使用合成模型（Hirama）研究了烟曲霉毒素的绝对构型。从黄蜂中分离的两种神经毒素的结构被推断出来（Okumura）。研究了海葵毒素和软冈藻酸的中毒机理。采用新方法合成了河豚毒素的重要中间体Isobe。确定了从植物中分离的神经营养化合物的结构（Kodama）.细胞生长的控制因子：（+）-Laurencin和（-）-dactylyne完全通过新开发的方法（Murai）合成。植物的抗感染活性被发现与细胞中存在的不饱和脂肪酸的烯丙基过氧化密切相关（T.Kato）。合成了万古霉素的活性部分，并确定了杂交菌株产物的结构（Yamamura）。类似物 ...更多信息 合成了具有与紫杉醇苷相当的DNA切割活性的蕨菜致癌物的三个新化合物，并从紫杉醇苷中分离出抗肿瘤化合物，从海洋动物（Yamada）中分离出抗肿瘤化合物。从Polypolaceae中分离出八种抗肿瘤活性启动子，并确定了它们的结构（Hayashi）。对多种海洋生物活性化合物（Kusumi）进行了绝对构型测定和构型分析。合成了具有细胞毒性的内分泌腺二乙酸酯（Isoe）。从Toddalis物种（Mori）中分离出具有细胞毒性的香豆素.拒食、化感作用和免疫佐剂活性：测定了比目鱼防御肽的结构（立花）。合成了来自革兰氏阴性菌的免疫佐剂脂磷壁酸（Kusumoto）。进行了氯罗烷二萜类化合物的合成研究（Tokoroyama）。使用诺匹酮作为起始原料（M，Kato）进行了jubavion和secoptera dopeterocin A的合成研究。实现了抗酶剂dysideapalaunic acid的全合成和绝对构型。从蕨类植物中分离出具有化感作用和离子转运促进作用的化合物。从紫苏叶中分离得到抗酶活性物质。从海洋植物中分离出对受精海鞘卵的细胞发育具有抑制活性的五种二萜，并确定了它们的结构（Ochi）。少

项目成果

C.S.M.Chairul: "Applanoxidic Acids E,F.G and H,Biologically Active Lanostanoid Triterpenes from Ganoderma applanatum as an Inhibitor against Tumro Promoter" Phytochemistry. (1993)

C.S.M.Chairul：“Applanacids E、F.G 和 H，来自灵芝的生物活性羊毛甾烷三萜作为 Tumro 启动子的抑制剂”植物化学。

Y.Naya: "Marine Biotechnology,Vol.1:Pharmaceutical and Bioactive Natural Products" Plenum, (1993)

Y.Naya：“海洋生物技术，第 1 卷：药物和生物活性天然产品”全会，（1993 年）

C. T. Barrow: "Structure and Activity Studies of Pardaxin and Analogues Using Model Membranes of Phosphatidyl Choline" Biochem. Biophys. Acta. 112. 285-240 (1992)

C. T. Barrow：“使用磷脂酰胆碱模型膜对 Pardaxin 及其类似物进行结构和活性研究”Biochem。

H. Shirahama: "Poisonous Substrances from Fungi" Seibutsudoku no Sekai. 93-116 (1992)

H. Shirahama：“真菌中的有毒物质”《Seibutsudoku no Sekai》。

H. Shirahama: "Principle of a Poisonous Mushroom Working as Neurotransmitters. A Dynamic Aspect of Natural Product-Chemistry" Organic Synthesis in Japan. 373-384 (1992)

H. Shirahama：“毒蘑菇作为神经递质的原理。天然产物化学的动态方面”日本有机合成。