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。
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 calculated data.Among these synthetic octapeptides,the anti-SARS(severe acute respiratory syndromes) octapeptide had the most obvious ACE inhibitory activity with an IC50 value of 3.4×10·5 mol·L-1.So octapeptide AVLQSGFR-OH(anti-SARS peptide) was found to be the strongest candidate for potential development as an anti-hypertensive drug and had the implication of further study.