Chen Hui, Chen Yu, Zheng Huizhen, Xiang Xingwei, Xu Lu
College of Food Science and Technology, Zhejiang University of Technology, Hangzhou, China.
Key Laboratory of Marine Fishery Resources Exploitment and Utilization of Zhejiang Province, Hangzhou, China.
Front Nutr. 2022 Aug 23;9:981163. doi: 10.3389/fnut.2022.981163. eCollection 2022.
In this study, a novel peptide, AEYLCEAC with high angiotensin-I-converting enzyme inhibitory (ACEI) activity was screened from oyster (Crassostrea gigas) hydrolysates, which was obtained from simulated gastro-intestinal digestion. Candidate peptides were confirmed to have a higher binding to angiotensin-I-converting enzyme (ACE) than the positive drug phosphoinic tripeptide calculated by Discovery Studio, and AEYLCEAC showed the highest ACE inhibition rate with a of 4.287 mM. Lineweaver-Burk plots confirmed that the peptidic inhibitory type of ACE is competitive. The molecular docking showed that ACEI activity of the AEYLCEAC was mainly due to the hydrogen bonding interactions with the active pockets (S1 and S2) of ACE. , AEYLCEAC effectively reduced diastolic blood pressure (DBP) and Systolic blood pressure (SBP) in hypertensive rats. These results indicate that AEYLCEAC might act as a helpful ingredient in functional foods or pharmaceuticals for the prevention and treatment of hypertension.
在本研究中，从经模拟胃肠消化获得的牡蛎（太平洋牡蛎）水解物中筛选出一种具有高血管紧张素转换酶抑制（ACEI）活性的新型肽AEYLCEAC。通过Discovery Studio计算得出，候选肽与血管紧张素转换酶（ACE）的结合力高于阳性药物膦酰三肽，且AEYLCEAC在4.287 mM时显示出最高的ACE抑制率。Lineweaver-Burk图证实该肽对ACE的抑制类型为竞争性。分子对接表明，AEYLCEAC的ACEI活性主要归因于与ACE活性口袋（S1和S2）的氢键相互作用。此外，AEYLCEAC有效降低了高血压大鼠的舒张压（DBP）和收缩压（SBP）。这些结果表明，AEYLCEAC可能作为功能性食品或药物中的有益成分用于预防和治疗高血压。
