Marine Biological Resource Comprehensive Utilization Engineering Research Center of the State Oceanic Administration, the Third Institute of Oceanography of the State Oceanic Administration, Xiamen 361005, China.
Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, and National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Mar Drugs. 2018 Jul 4;16(7):228. doi: 10.3390/md16070228.
Hypertension can cause coronary heart disease. Synthetic angiotensin-converting enzyme (ACE) inhibitors are effective antihypertensive drugs but often cause side effects. The aim of this study was to prepare potential ACE inhibitors from scales. Gelatin was extracted from lizardfish scales. Then, scale gelatin was enzymolyzed to prepare ACE inhibitory peptides using response surface methodology. Proteolytic conditions after optimization were as follows: pH 7.0, enzyme substrate ratio 3.2%, temperature 47 °C, and proteolysis lasting 2 h and 50 min. The experimental ACE inhibitory activity under optimal conditions was 86.0 ± 0.4%. Among the 118 peptides identified from gelatin hydrolysates, 87.3% were hydrophilic and 93.22% had a molecular weight <2000 Da. Gelatin peptides had high stability upon exposure to high temperature and pH as well as gastrointestinal tract enzymes. Gelatin peptides showed an antihypertensive effect in spontaneously hypertensive rats at a dosage of 2 g/kg in the long-term experiments. A new ACE inhibitory peptide was isolated from gelatin hydrolysates, and was identified as AGPPGSDGQPGAK with an IC value of 420 ± 20 μM. In this way, ACE inhibitory peptides derived from scale gelatin have the potential to be used as healthy ACE-inhibiting drug raw materials.
高血压可引起冠心病。合成血管紧张素转换酶（ACE）抑制剂是有效的降压药物，但常引起副作用。本研究旨在从鱼鳞中制备潜在的 ACE 抑制剂。从尖吻鲈的鳞片中提取明胶。然后，采用响应面法，用明胶酶解制备 ACE 抑制肽。经优化后的酶解条件为：pH7.0、酶底物比 3.2%、温度 47°C、酶解 2h50min。最佳条件下的实验 ACE 抑制活性为 86.0±0.4%。在明胶水解物中鉴定出的 118 种肽中，87.3%为亲水性，93.22%的分子量<2000Da。明胶肽在高温和 pH 以及胃肠道酶存在的情况下具有较高的稳定性。在长期实验中，明胶肽以 2g/kg 的剂量在自发性高血压大鼠中显示出降压作用。从明胶水解物中分离出一种新的 ACE 抑制肽，其 IC 值为 420±20μM，鉴定为 AGPPGSDGQPGAK。这样，来源于鱼鳞明胶的 ACE 抑制肽有潜力作为健康的 ACE 抑制药物的原料。
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