College of Pharmacy, Hubei University of Chinese Medicine, Wuhan 430065, China.
Hubei Provincial Chinese Medicine-Derived Health Food Engineering Research Center, Wuhan 430065, China.
Molecules. 2022 Aug 24;27(17):5421. doi: 10.3390/molecules27175421.
The renin-angiotensin system (RAS) is the primary pathway for regulating blood pressure in the body, and angiotensin-converting enzymes (ACEs) play a crucial role in it. is an invertebrate that contains a variety of active peptides; however, there are no studies on the ACE inhibitory activity of hirudo. In the present study, our aim was to identify the active peptides in hirudo based on active peptide database analysis, unexpectedly filling the gap in hirudo ACE inhibitory activity research. Prep-HPLC was used to separate the part below 3 kD from hirudo. The peptide composition of the isolates was obtained based on Orbitrap LC-MS. The activity of each group of peptides was predicted by the database and the activity was determined by bioassay. Peptides with validation activity were screened through the database. In total, 337 peptides and 18 peptides matching the NCBI leech protein database were identified. All four fractions showed ACE inhibitory activity, and the IC50 was 0.8266, 0.2708, 0.4432, and 0.1764 mg/mL, respectively. Six screened peptides showed good affinity for ACE. This work reveals for the first time that low-molecular-weight peptides from have ACE inhibitory activity, which can provide a new explanation for leech treatment of hypertension.
肾素-血管紧张素系统（RAS）是调节体内血压的主要途径，血管紧张素转换酶（ACE）在其中起着至关重要的作用。水蛭是一种无脊椎动物，含有多种活性肽；然而，目前还没有关于水蛭 ACE 抑制活性的研究。在本研究中，我们的目的是根据活性肽数据库分析鉴定水蛭中的活性肽，意外填补了水蛭 ACE 抑制活性研究的空白。采用 Prep-HPLC 从水蛭中分离出 3 kD 以下的部分。根据 Orbitrap LC-MS 获得分离物的肽组成。通过数据库预测各肽组的活性，并通过生物测定确定活性。通过数据库筛选具有验证活性的肽。共鉴定出 337 条肽和 18 条与 NCBI 水蛭蛋白数据库匹配的肽。所有四个馏分均显示出 ACE 抑制活性，IC50 分别为 0.8266、0.2708、0.4432 和 0.1764 mg/mL。六种筛选出的肽与 ACE 具有良好的亲和力。这项工作首次揭示了来自的低分子量肽具有 ACE 抑制活性，这可为水蛭治疗高血压提供新的解释。
