Nong Nhung Thi Phuong, Chen Yu-Kuo, Shih Wen-Ling, Hsu Jue-Liang
Department of Tropical Agriculture and International Cooperation, National Pingtung University of Science and Technology, Pingtung 91201, Taiwan.
Department of Basic Science, Thainguyen University of Agriculture and Forestry, Quyetthang Ward, Thai Nguyen 250000, Vietnam.
Pharmaceuticals (Basel). 2020 Oct 14;13(10):308. doi: 10.3390/ph13100308.
Five novel peptides (LPLF, WLQL, LPSW, VPGLAL, and LVGLPL) bearing dipeptidyl peptidase IV (DPP-IV) inhibitory activities were identified from the gastrointestinal enzymatic hydrolysate of soft-shelled turtle yolk (SSTY) proteins. Peptides were isolated separately using reversed-phase (RP) chromatography in parallel with off-line strong cation exchange (SCX) chromatography followed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis to determine sequences. Among these peptides, LPSW showed the highest DPP-IV inhibitory activity with an IC value of 269.7 ± 15.91 µM. The results of the pre-incubation experiment and the kinetic study of these peptides indicated that WLQL is a true inhibitor and its inhibition toward DPP-IV is of an uncompetitive model, while LPLF, LPSW, and VPGLAL are real-substrates and competitive inhibitors against DPP-IV. The DPP-IV inhibitory peptides derived from SSTY hydrolysate in study are promising in the management of hyperglycemia in Type 2 diabetes.
从中华鳖蛋黄（SSTY）蛋白的胃肠道酶解产物中鉴定出五种具有二肽基肽酶IV（DPP-IV）抑制活性的新型肽（LPLF、WLQL、LPSW、VPGLAL和LVGLPL）。使用反相（RP）色谱与离线强阳离子交换（SCX）色谱并行分离肽，随后进行液相色谱-串联质谱（LC-MS/MS）分析以确定序列。在这些肽中，LPSW表现出最高的DPP-IV抑制活性，IC值为269.7±15.91μM。这些肽的预孵育实验和动力学研究结果表明，WLQL是一种真正的抑制剂，其对DPP-IV的抑制作用为非竞争性模型，而LPLF、LPSW和VPGLAL是真正的底物和DPP-IV的竞争性抑制剂。本研究中源自SSTY水解产物的DPP-IV抑制肽在2型糖尿病高血糖管理方面具有前景。
