ace 抑制肽的合成及其活性研究synthesis and activity of - 药学学报.pdfVIP

58 药学学报 Acta Pharmaceutica Sinica 20 11, 46 ( 1) : 5863 ACE 抑制肽的合成及其活性研究 锦, 曹 刚, 张瑞洁, 李大为, 魏婷婷, 钦传光* (西北工业大学生命学院, 陕西 西安 710072) 摘要: 为研究血管紧张素转换酶 (angiotensin converting enzyme, ACE) 抑制肽体外抑制ACE 活性以期筛选 出有降压作用的先导物, 采用Fmoc 固相合成法合成ACE 抑制肽, 经反相高效液相色谱法 (RP-HPLC) 分离纯化, 采用质谱对其进行鉴定, 并使用RP-HPLC 法直接测定ACE 抑制肽对ACE 的体外抑制活性。合成的6 个八肽经 RP-HPLC 纯化后, 质谱分析结果与理论值一致。活性评价结果表明6 号八肽 (抗SARS 肽) 对ACE 的抑制作用 −5 −1 最明显, 其IC50 为3.4 10 mol·L , 此可见抗SARS 肽 (AVLQSGFR-OH) 是一个具有降压作用的先导物, 具 有进一步研究的意义。 关键词: ACE 抑制肽; 固相合成; 降压药物 中图分类号: R916 文献标识码:A 文章编号: 05 13-4870 (20 11) 01-0058-06 Synthesis and activity of ACE inhibitory peptides * REN Jin, CAO Gang, ZHANG Rui-ji e, LI Da-wei, WEI Ting-ting, QIN Chuan-guang (Faculty of Life Science, Northwestern Poly technical University, Xi an 710072, China) Abstract: To find anti-hypertensive lead drug, angiotensin converting enzyme (ACE) inhibitory peptides were synthesized and their effects on inhibiting ACE activity were investigated. ACE inhibitory peptides were synthesized via Fmoc solid-phase synthesis, isolated and purified through reversed phase high-performance liquid chromatography (RP-HPLC), and identified by mass spectrometry. A RP-HPLC analysis method was used to test ACE inhibitory activity in vitro of these ACE inhibitory peptides. Six octapeptides were successfully synthesized, and the analytical results of mass spectrum were consistent with their theoretically