Morinaga Milk Industry Co., Ltd., Functional Food Research Department Food Science & Technology Institute, 1-83 5-Chome, Higashihara, Zama, Kanagawa 252-8583, Japan.
Food Chem. 2013 Dec 15;141(4):3781-9. doi: 10.1016/j.foodchem.2013.06.089. Epub 2013 Jun 28.
Bovine lactic casein was hydrolysed using a combination of three enzymes, namely, subtilisin, bacillolysin, and trypsin, and the resulting preparation was coined CH-3. CH-3 showed angiotensin I-converting enzyme (ACE)-inhibitory activity (IC50: 74 μg/mL). A single oral administration of CH-3 led to a transient but significant decrease in the systolic blood pressure (SBP) of spontaneously hypertensive rats (SHRs), while daily oral administration of CH-3 for 28 consecutive days led to a lower rate of SBP increase. The CH-3 preparation was then fractionated and the αS2-casein-derived tripeptide Met-Lys-Pro (or MKP) was identified as a novel peptide with strong ACE-inhibitory activity (IC50=0.12 μg/mL, 0.3 μM). The MKP peptide constituted only 0.053% of CH-3 but its activity was accounted for 33% of the total ACE-inhibitory activity of CH-3. In addition, a single oral administration of MKP also led to a transient but significant decrease in the SBP of SHRs.
牛乳酪蛋白经枯草杆菌蛋白酶、梭菌蛋白酶和胰蛋白酶联合水解，得到的产物命名为 CH-3。CH-3 具有血管紧张素转化酶（ACE）抑制活性（IC50：74μg/mL）。单次口服 CH-3 可使自发性高血压大鼠（SHR）的收缩压（SBP）短暂但显著降低，而连续 28 天每日口服 CH-3 可使 SBP 升高率降低。随后对 CH-3 进行了分级分离，鉴定出一种新型的、具有强 ACE 抑制活性的αS2-酪蛋白衍生三肽 Met-Lys-Pro（或 MKP）（IC50=0.12μg/mL，0.3μM）。MKP 肽仅占 CH-3 的 0.053%，但其活性占 CH-3 总 ACE 抑制活性的 33%。此外，单次口服 MKP 也可使 SHR 的 SBP 短暂但显著降低。
