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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的抑制作用最明显,其IC50为3.4×10-5 mol.L-1,由此可见抗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。
In order to study the inhibitory effect of angiotensin converting enzyme (ACE) inhibitory peptide on ACE activity in vitro and to screen the lead compounds with antihypertensive effect, ACE inhibitory peptide was synthesized by Fmoc solid phase synthesis and identified by reversed-phase high performance liquid chromatography (RP-HPLC), identified by mass spectrometry, and the inhibitory activity of ACE inhibitory peptides on ACE in vitro was determined by RP-HPLC. After the synthesized six octapeptides were purified by RP-HPLC, the results of mass spectrometry were consistent with the theoretical values. The result of activity evaluation showed that the inhibitory effect of No.6 octapeptide (anti-SARS peptide) on ACE was most obvious with an IC50 of 3.4 × 10-5 mol·L-1. Therefore, the anti-SARS peptide (AVLQSGFR-OH) The role of pressure leader, with further research significance.