College of Food Science and Engineering, Nanjing University of Finance and Economics , Nanjing, Jiangsu, People's Republic of China 210003.
J Agric Food Chem. 2013 Sep 4;61(35):8396-402. doi: 10.1021/jf400865m. Epub 2013 Aug 21.
A novel antihypertensive peptide (Gly-His-Ser or GHS) with dual inhibition of angiotensin I-converting enzyme (ACE) and renin activities was isolated from the 3 kDa membrane ultrafiltration permeate of a pepsin+pancreatin rapeseed protein digest. The IC50 values of GHS were 0.52 ± 0.01 mg/mL and 0.32 ± 0.01 mg/mL for ACE and renin inhibitions, respectively, which are 1.5 times the ACE inhibition and 3.5 times the renin inhibition of the 3 kDa permeate. Oral administration (30 mg/kg body weight) to spontaneously hypertensive rats showed GHS to be an effective hypotensive agent with maximum blood pressure reduction of -17.29 ± 2.47 mmHg after 6 h. In contrast, the 3 kDa permeate exhibited a maximum of -21.29 ± 9.29 mmHg after 4 h, although at a relatively higher dose of 100 mg/kg body weight). GHS inhibited ACE and renin activities noncompetitively, but the renin inhibition became uncompetitive at a higher peptide concentration.
一种新型的抗高血压肽（Gly-His-Ser 或 GHS），具有双重抑制血管紧张素 I 转换酶（ACE）和肾素活性的作用，从胃蛋白酶+胰蛋白酶油菜蛋白消化物的 3 kDa 膜超滤渗透物中分离得到。GHS 的 IC50 值分别为 0.52±0.01mg/mL 和 0.32±0.01mg/mL，对 ACE 和肾素的抑制作用分别是 3 kDa 渗透物的 ACE 抑制作用的 1.5 倍和肾素抑制作用的 3.5 倍。口服（30mg/kg 体重）给自发性高血压大鼠，GHS 是一种有效的降压剂，6 小时后最大血压降低-17.29±2.47mmHg。相比之下，3 kDa 渗透物在 4 小时后表现出最大的-21.29±9.29mmHg，尽管在相对较高的剂量 100mg/kg 体重时）。GHS 非竞争性抑制 ACE 和肾素活性，但在较高肽浓度下肾素抑制变为竞争性抑制。
