Department of Marine Life Sciences, Marine Science Institute, Jeju National University, Jeju, Korea.
Jeju International Marine Science Center for Research and Education, Korea Institute of Ocean Science and Technology, Jeju, Korea.
J Med Food. 2020 Feb;23(2):132-138. doi: 10.1089/jmf.2019.4415.
This study investigated the antihypertensive effects of an antioxidant peptide, Leu-Trp-His-Thr-His (LWHTH), purified from peptic hydrolysate, to assess the bioactivity of the peptide and verify the value of as a health-promoting food. Also, the study presented structural evidence for the effects of LWHTH. The inhibitory effect of LWHTH on angiotensin I-converting enzyme (ACE) was assessed using enzyme reaction methods and the simulation methods in computational space. LWHTH inhibited ACE with an IC value of 16.42 ± 0.45 M. The LWHTH structure was stable, and its ACE inhibitory effect was retained under simulated gastrointestinal conditions. simulations revealed that LWHTH binds the active site of ACE, with residues LW making the ACE-LWHTH complex stable and residues HTH making the complex strong. Furthermore, LWHTH significantly reduced blood pressure in spontaneously hypertensive rats. These results demonstrate that LWHTH has the potential to be a healthy functional food with antihypertensive effects. Therefore, consumption may be beneficial for human health.
本研究旨在探讨一种从胃蛋白酶水解物中纯化得到的抗氧化肽 Leu-Trp-His-Thr-His(LWHTH)的降压作用,以评估该肽的生物活性,并验证其作为促进健康食品的价值。此外,本研究还提供了 LWHTH 作用机制的结构证据。采用酶反应法和计算空间模拟法评估了 LWHTH 对血管紧张素转化酶(ACE)的抑制作用。LWHTH 对 ACE 的抑制作用的 IC 值为 16.42±0.45μM。LWHTH 结构稳定,在模拟胃肠道条件下仍能保持 ACE 抑制活性。分子对接模拟表明,LWHTH 与 ACE 的活性部位结合,残基 LW 使 ACE-LWHTH 复合物稳定,残基 HTH 使复合物具有较强的结合能力。此外,LWHTH 可显著降低自发性高血压大鼠的血压。这些结果表明,LWHTH 具有成为具有降压作用的健康功能性食品的潜力。因此,摄入 LWHTH 可能对人体健康有益。