Ren Jin, Cao Gang, Zhang Rui-Jie, Li Da-Wei, Wei Ting-Ting, Qin Chuan-Guang
Faculty of Life Science, Northwestern Polytechnical University, Xi'an 710072, China.
Yao Xue Xue Bao. 2011 Jan;46(1):58-63.
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 x 10(-5) mol x 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.
为寻找抗高血压先导药物,合成了血管紧张素转换酶(ACE)抑制肽,并研究了它们对ACE活性的抑制作用。通过Fmoc固相合成法合成ACE抑制肽,采用反相高效液相色谱(RP-HPLC)进行分离纯化,并通过质谱进行鉴定。运用RP-HPLC分析方法检测这些ACE抑制肽的体外ACE抑制活性。成功合成了六种八肽,质谱分析结果与理论计算数据一致。在这些合成的八肽中,抗SARS(严重急性呼吸综合征)八肽具有最明显的ACE抑制活性,IC50值为3.4×10(-5)mol×L(-1)。因此,八肽AVLQSGFR-OH(抗SARS肽)被发现是作为抗高血压药物潜在开发的最强候选物,具有进一步研究的意义。