Search for the inhibitors of the glycosidases from marine invertebrates

寻找海洋无脊椎动物糖苷酶抑制剂

• 批准号: 08458172
• 负责人: MATSUNAGA Shigeki
• 金额: $ 4.74万
• 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: 1996
• 资助国家: 日本
• 起止时间: 1996 至 1997
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-08458172/
• 关键词: sponge; coelenterate; glycosidase; galactosidase; juhibitor; 海綿動物; ガウクトシダーゼ; 阻害剤; グルコシダーゼ

Screening of the extracts of marine invertebrates (88 sponges, 11 coelenterates, and 5 tunicates) against alpha-glucosidase, beta-glucosidase, and beta-galactosidase was carried out. Activity was found approximately 10% of sponges, but none of coelenterates or tunicates exhibited activity.The extract of an unidentified sponge collected at Hachijo Island was fractionated directed by alpha-glucosidase-inhibitory activity. From a lipophilic fraction a branched C15 carboxylic acid was obtained, however, the active material in the aqueous fraction was not purified.The sponge Penares sp. collected at Hachijo Island was also active against a-glucosidase. From the CH2Cl2 fraction, 4mg of a compound named S6215-A was obtained. Its molecular formula was shown to be C36H69NO11S2 on the basis of high resolution FAB mass spectrometry. The 1HNMR spectrum exhibited two methyls, huge methylene envelop, a methylene adjacent to a carbonyl, and five protons on hetero-atom-substituted carbons. The 13 NMR spectrum revealed two amide or ester carbons, two oxygenated mathine, one each of nitrogenous methine and methylene, and O-methyl groups. Two-dimensional NMR spectra revealed the gross feature of the active compound. The structure of another active compound was similarly analyzed.

对海洋无脊椎动物（88种海绵、11种腔肠动物和5种被囊动物）的提取物进行了抗α-葡萄糖苷酶、β-葡萄糖苷酶和β-半乳糖苷酶的筛选。活性被发现约10%的海绵，但没有腔肠动物或被囊动物表现出activity.The提取物的身份不明的海绵收集在八丈岛分馏α-葡萄糖苷酶抑制活性的指导。从亲脂性部分得到支链C15羧酸，然而，水相部分中的活性物质没有纯化。从CH 2Cl 2馏分中，获得4 mg命名为S6215-A的化合物。经高分辨FAB质谱分析，其分子式为C36 H69 NO11 S2。1HNMR谱显示出两个甲基，巨大的亚甲基包络，一个亚甲基与一个羰基相邻，杂原子取代的碳上有五个质子。13 NMR光谱揭示了两个酰胺或酯碳，两个氧化的甲基，含氮次甲基和亚甲基各一个，以及O-甲基。二维核磁共振谱显示了活性化合物的总体特征。类似地分析了另一种活性化合物的结构。