Liu Feifan, Liu Mingzhen, Zhang Tao, Zhao Xuan, Wang Xiaozhi, Kong Weimei, Cui Li, Luo Haibo, Guo Lili, Guo Yuxing
Department of Food Science and Technology, School of Food Science and Pharmaceutical Engineering, Nanjing Normal University, Nanjing, Jiangsu, PR China.
Institute of Agro-Product Processing, Jiangsu Academy of Agricultural Sciences, Nanjing, PR China.
Food Nutr Res. 2023 May 25;67. doi: 10.29219/fnr.v67.9079. eCollection 2023.
The increasing morbidity and mortality of cardiovascular disease have become a major factor in human death. Serum cholesterol is considered to be an important risk factor for inducing coronary heart disease, atherosclerosis and other cardiovascular diseases. To screen intestinal absorbable functional small peptides with cholesterol-lowering activity by enzymatic hydrolysis of whey protein and develop cholesterol-based functional food that may become a substitute for chemically synthesized drugs, providing new ideas for diseases caused by high cholesterol.
This study aimed to evaluate the cholesterol-lowering activity of intestinal absorbable whey protein-derived peptides hydrolyzed by alkaline protease, trypsin and chymotrypsin, respectively.
The whey protein hydrolysates acquired by enzymatic hydrolysis under optimal conditions were purified by a hollow fiber ultrafiltration membrane with a molecular weight cutoff of 10 kDa. The fractions obtained by Sephadex G-10 gel filtration chromatography were transported through a Caco-2 cell monolayer. The transported peptides were detected in the basolateral aspect of Caco-2 cell monolayers using ultra- performance liquid chromatography-tandem mass spectrometry (UPLC-MS).
His-Thr-Ser-Gly-Tyr (HTSGY), Ala-Val-Phe-Lys (AVFK) and Ala-Leu-Pro-Met (ALPM) were unreported peptides with cholesterol-lowering activity. The cholesterol-lowering activities of the three peptides did not change significantly during simulated gastrointestinal digestion.
This study not only provides theoretical support for the development of bioactive peptides that can be directly absorbed by the human body, but also provides new treatment ideas for hypercholesterolemia.
心血管疾病发病率和死亡率的不断上升已成为人类死亡的主要因素。血清胆固醇被认为是诱发冠心病、动脉粥样硬化等心血管疾病的重要危险因素。通过酶解乳清蛋白筛选具有降胆固醇活性的肠道可吸收功能性小肽，并开发基于胆固醇的功能性食品，有望成为化学合成药物的替代品，为高胆固醇引起的疾病提供新思路。
本研究旨在分别评估碱性蛋白酶、胰蛋白酶和糜蛋白酶水解得到的肠道可吸收乳清蛋白衍生肽的降胆固醇活性。
在最佳条件下通过酶解获得的乳清蛋白水解物，用截留分子量为10 kDa的中空纤维超滤膜进行纯化。通过Sephadex G-10凝胶过滤色谱得到的组分通过Caco-2细胞单层进行转运。使用超高效液相色谱-串联质谱（UPLC-MS）在Caco-2细胞单层的基底外侧检测转运的肽。
His-Thr-Ser-Gly-Tyr（HTSGY）、Ala-Val-Phe-Lys（AVFK）和Ala-Leu-Pro-Met（ALPM）是未报道过的具有降胆固醇活性的肽。这三种肽在模拟胃肠消化过程中降胆固醇活性没有显著变化。
本研究不仅为开发可被人体直接吸收的生物活性肽提供了理论支持，也为高胆固醇血症提供了新的治疗思路。
