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Assessment of the DPP-IV inhibitory activity of a novel octapeptide derived from rapeseed using Caco-2 cell monolayers and molecular docking analysis.
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2020-07-30 , DOI: 10.1111/jfbc.13406 Feiran Xu 1, 2 , Elvira Gonzalez de Mejia 2 , Hong Chen 2 , Kowalski Rebecca 2 , Mengmeng Pan 3 , Rong He 3 , Yijun Yao 1, 3 , Lifeng Wang 3 , Xingrong Ju 1, 3
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2020-07-30 , DOI: 10.1111/jfbc.13406 Feiran Xu 1, 2 , Elvira Gonzalez de Mejia 2 , Hong Chen 2 , Kowalski Rebecca 2 , Mengmeng Pan 3 , Rong He 3 , Yijun Yao 1, 3 , Lifeng Wang 3 , Xingrong Ju 1, 3
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The Octapeptide ELHQEEPL, which was identified from the rapeseed protein napin showed prominent Dipeptidyl peptidase‐IV (DPP‐IV) inhibitory activity. The objective of this study was to investigate the DPP‐IV inhibitory activity and transepithelial transport of ELHQEEPL in an approaching intestinal condition using Caco‐2 cell monolayers. ELHQEEPL and its degraded fragments EL, HQEEP, and methylated ELHQEEPL were transported across Caco‐2 cell monolayers through different pathways. Compared with the nonbiological enzyme inhibition test, the in vitro experiment on Caco‐2 cell monolayers showed that the IC50 value of DPP‐IV inhibition increased by 43.11% for ELHQEEPL. There was no significant change in DPP‐IV gene expression in the Caco‐2 cell monolayers upon treatment with ELHQEEPL. Furthermore, molecular docking predicted that the weaker binding between inhibitory peptide and enzyme for the degradation products from ELHQEEPL during transepithelial transport greatly limited its role in inhibiting DPP‐IV.
中文翻译：
使用 Caco-2 细胞单层和分子对接分析评估源自油菜籽的新型八肽的 DPP-IV 抑制活性。
从油菜籽蛋白 napin 中鉴定出的八肽 ELHQEEPL 显示出显着的二肽基肽酶 IV (DPP-IV) 抑制活性。本研究的目的是使用 Caco-2 单层细胞研究 ELHQEEPL 在接近肠道条件下的 DPP-IV 抑制活性和跨上皮转运。 ELHQEEPL 及其降解片段 EL、HQEEP 和甲基化 ELHQEEPL 通过不同途径跨 Caco-2 细胞单层转运。与非生物酶抑制试验相比，Caco-2单层细胞体外实验表明，ELHQEEPL抑制DPP-IV的IC 50值增加了43.11%。 ELHQEEPL 处理后，Caco-2 细胞单层中 DPP-IV 基因表达没有显着变化。此外，分子对接预测，跨上皮转运过程中 ELHQEEPL 降解产物的抑制肽与酶之间的结合较弱，极大限制了其抑制 DPP-IV 的作用。
更新日期：2020-07-30
中文翻译：
使用 Caco-2 细胞单层和分子对接分析评估源自油菜籽的新型八肽的 DPP-IV 抑制活性。
从油菜籽蛋白 napin 中鉴定出的八肽 ELHQEEPL 显示出显着的二肽基肽酶 IV (DPP-IV) 抑制活性。本研究的目的是使用 Caco-2 单层细胞研究 ELHQEEPL 在接近肠道条件下的 DPP-IV 抑制活性和跨上皮转运。 ELHQEEPL 及其降解片段 EL、HQEEP 和甲基化 ELHQEEPL 通过不同途径跨 Caco-2 细胞单层转运。与非生物酶抑制试验相比，Caco-2单层细胞体外实验表明，ELHQEEPL抑制DPP-IV的IC 50值增加了43.11%。 ELHQEEPL 处理后，Caco-2 细胞单层中 DPP-IV 基因表达没有显着变化。此外，分子对接预测，跨上皮转运过程中 ELHQEEPL 降解产物的抑制肽与酶之间的结合较弱，极大限制了其抑制 DPP-IV 的作用。
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