Department of Biological Sciences, University of Limerick, Limerick, Ireland.
School of Biomedical Sciences, Ulster University, Coleraine, Co. Derry, Northern Ireland, United Kingdom.
Food Res Int. 2020 May;131:108989. doi: 10.1016/j.foodres.2020.108989. Epub 2020 Jan 21.
Twenty-two novel dipeptidyl peptidase-IV (DPP-IV) inhibitory peptides (with IC values <200 µM) and fifteen novel insulinotropic peptides were identified in a boarfish protein hydrolysate generated at semi-pilot scale using Alcalase 2.4L and Flavourzyme 500L. This was achieved by bioassay-driven semi-preparative reverse phase-high performance liquid chromatography fractionation, liquid chromatography-mass spectrometry and confirmatory studies with synthetic peptides. The most potent DPP-IV inhibitory peptide (IPVDM) had a DPP-IV half maximal inhibitory concentration (IC) value of 21.72 ± 1.08 µM in a conventional in vitro and 44.26 ± 0.65 µM in an in situ cell-based (Caco-2) DPP-IV inhibition assay. Furthermore, this peptide stimulated potent insulin secretory activity (1.6-fold increase compared to control) from pancreatic BRIN-BD11 cells grown in culture. The tripeptide IPV exhibited potent DPP-IV inhibitory activity (IC: 5.61 ± 0.20 µM) comparable to that reported for the known DPP-IV inhibitor IPI (IC: 3.20 µM). Boarfish proteins contain peptide sequences with potential to play a role in glycaemic management in vivo.
二十二种新型二肽基肽酶-IV（DPP-IV）抑制肽（IC 值<200µM）和十五种新型胰岛素促分泌肽在使用 Alcalase 2.4L 和 Flavourzyme 500L 进行半工业规模的猪鱼蛋白水解物中被鉴定出来。这是通过基于生物测定的半制备反相高效液相色谱分级、液相色谱-质谱和用合成肽进行的确认研究来实现的。最有效的 DPP-IV 抑制肽（IPVDM）在常规体外试验中具有 21.72±1.08µM 的 DPP-IV 半最大抑制浓度（IC）值，在原位基于细胞（Caco-2）的 DPP-IV 抑制试验中具有 44.26±0.65µM 的 IC 值。此外，这种肽从培养的胰腺 BRIN-BD11 细胞中刺激了强烈的胰岛素分泌活性（与对照相比增加了 1.6 倍）。三肽 IPV 表现出强烈的 DPP-IV 抑制活性（IC：5.61±0.20µM），与已知的 DPP-IV 抑制剂 IPI（IC：3.20µM）相当。猪鱼蛋白含有潜在的肽序列，可在体内发挥血糖管理作用。
