• 系統編號 RC9103-0066
• 計畫中文名稱 降血糖作用之前導化合物合成研究
• 計畫英文名稱 Synthesis of Lead Compounds for Hypoglycemics
• 主管機關 行政院國家科學委員會 • 計畫編號 NSC89-2320-B038-060
• 執行機構 台北醫學院藥學系
• 本期期間 8908 ~ 9007
• 報告頁數 9 頁 • 使用語言 中文
• 研究人員 陳繼明 Chen, Chi-Ming
• 中文關鍵字 化學合成；升麻素；葡萄糖攝取；降血糖作用
• 英文關鍵字 Chemical synthesis；Isoferulic acid；Glucose uptake；Hypoglycemic effect
• 中文摘要
Isoferulic acid 為降血糖活性成分，對第一型糖尿病較第二型糖尿病老鼠作用較為顯著；今擬以 Isoferulic acid 為目標進行構造 修飾，合成一系列 Isoferulic acid 衍生物，研討化學構造對降血糖藥效影響，23 種類似物經化學製備完成並經光譜分析確認其 化學構造。初步選擇十五種化合物進行活性試驗。測試體肌母細胞對葡萄糖吸回作用，發現化合物 6、11、16、22 及 24 的作 用較 Isoferulic acid 為佳，其中又以化合物 6 及 11 活性最為顯著。
• 英文摘要
Isoferulic acid has been identified to have in vivo antihyperglycemic activity. The lowering effect of plasma glucose by isoferulic acid in IDDM rats is more active than that in NIDDM rats. The antihyperglycemic mechanism is not only to enhance glucose utilization in peripheral tissues but also to reduce hepatic gluconeogenesis. In order to study the structure and activity relationship of isoferulic acid, 23 isoferulic acid analogues were prepared by chemical synthesis and their antidiabetic activities were evaluated. All these analogues were characterized by spectrometric analysis. Fifteen compounds were selected to evaluate the glucose uptake of soleus muscle cells from streptozotocin induced diabetic rats. It showed that 6, 11, 16, 22, and 24 were more active than that of isoferulic acid. Compound 6 and 11 have the most remarkable activities.
